- 1. The genus Rhododendron: An ethnopharmacological and toxicological review.
ETHNOPHARMACOLOGICAL RELEVANCE:
The vast genus Rhododendron includes species that have been used in traditional medicine for the treatment of inflammatory conditions, pain, gastro-intestinal disorders, common cold, asthma, skin disease, etc. Rhododendrons are also well known for their toxicity and some species have been traditionally used as poison.
AIM OF THE REVIEW:
The work reviews and analyses the traditional use, biological activities with the corresponding chemical constituents, and toxicological data on Rhododendron species. The review aims at characterizing the ethnopharmacology of the genus in relation to its toxicity in order to identify the therapeutic potential of Rhododendron species and future directions for research.
METHODS:
Data regarding Rhododendron spp. was collected using electronic databases (SciFinder, PubMed, Google Scholar) and library search for selected peer-reviewed articles. Plant taxonomy was validated by the databases The Plant List, Tropicos, eFloras, Flora Iberica and Flora Europaea (RBGE). Additional information on traditional use and botany was obtained from published books. The review encompasses literature, mainly regarding biological activity and toxicological data, from 1898 to the end of December 2012.
RESULTS:
Rhododendrons have been used in Asian, North American and European traditional medicine mainly against inflammation, pain, skin ailments, common cold and gastro-intestinal disorders. In vivo and in vitro testing of plant extracts and isolated compounds determined diverse biological activities including anti-inflammatory, analgesic, anti-microbial, anti-diabetic, insecticidal and cytotoxic activity. Rhododendron spp. can cause intoxications in humans following intake of rhododendron honey or medicinal preparations. The toxicity is due to grayanotoxins, diterpenes which activate voltage-gated sodium channels and lead to gastro-intestinal, cardiac and central nervous system symptoms.
CONCLUSION:
Rhododendron species are useful traditional remedies for the treatment of inflammation, pain, skin ailments, common cold and gastro-intestinal disorders. Pharmacological data has validated most indications of rhododendrons in ethnomedicine and toxicology studies have confirmed the toxicity observed by traditional use. Ethnopharmacological data point to the therapeutic potential of the genus Rhododendron for the treatment of inflammatory conditions and pain and, thus, research should focus on identification of active compounds and related mechanistic studies. Prolonged and high dose intake of traditional formulations containing rhododendrons should be avoided until more in depth toxicity studies become available.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Popescu R, et al. J Ethnopharmacol 2013 May 2;147(1):42-62.
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- 2. Pharmacological evaluation of hyperin for antihyperglycemic activity and effect on lipid profile in diabetic rats.
Antihyperglycemic potential of hyperin at 25 and 50 mg/kg doses for 30 days to streptozotocin induced diabetic rats has been reported. In oral glucose tolerance test, hyperin treated rats showed a significant reduction in blood glucose level after 120 min. It was found that hyperin exhibited dose dependent and significant antihyperglycemic activity in streptozotocin induced diabetic rats which were nearly similar with standard drug glybenclamide. Activities of glucose-6-phosphatase, fructose-1,6-bisphosphatase, glycogen phosphorylase, glycosylated haemoglobin and level of serum urea and creatinine were significantly decreased in hyperin supplemented diabetic rats, dose dependently. Activities of hexokinase and glycogen synthase were increased with augmentation in liver glycogen, insulin and haemoglobin content in hyperin treated diabetic rats. General hematological parameters did not show any significant change in hyperin treated diabetic rats hence it is safe at these doses. Histopathological studies showed significant morphological changes in pancreatic beta-cells of streptozotocin induced diabetic rats. A decreased number of secretory granules of beta-cells were observed in diabetic rats and these pathological abnormalities were normalized after treatment with hyperin and standard drug glybenclamide. Further, hyperin decreases significant in serum total cholesterol, triglyceride, low density lipoprotein, very low density lipoprotein levels coupled with elevation of high density lipoprotein in diabetic rats. These results suggest that hyperin has a pivotal role in blood glucose level in streptozotocin induced hyperglycemia by improving the function of pancreatic islets and increasing glycolysis and decreasing gluconeogenesis....(more)
Verma N, et al. Indian J Exp Biol 2013 Jan;51(1):65-72.
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- 3. How endangered is sexual reproduction of high-mountain plants by summer frosts? Frost resistance, frequency of frost events and risk assessment.
In temperate-zone mountains, summer frosts usually occur during unpredictable cold spells with snow-falls. Earlier studies have shown that vegetative aboveground organs of most high-mountain plants tolerate extracellular ice in the active state. However, little is known about the impact of frost on reproductive development and reproductive success. In common plant species from the European Alps (Cerastium uniflorum, Loiseleuria procumbens, Ranunculus glacialis, Rhododendron ferrugineum, Saxifraga bryoides, S. moschata, S. caesia), differing in growth form, altitudinal distribution and phenology, frost resistance of reproductive and vegetative shoots was assessed in different reproductive stages. Intact plants were exposed to simulated night frosts between -2 and -14 °C in temperature-controlled freezers. Nucleation temperatures, freezing damage and subsequent reproductive success (fruit and seed set, seed germination) were determined. During all reproductive stages, reproductive shoots were significantly less frost resistant than vegetative shoots (mean difference for LT50 -4.2 ± 2.7 K). In most species, reproductive shoots were ice tolerant before bolting and during fruiting (mean LT50 -7 and -5.7 °C), but were ice sensitive during bolting and anthesis (mean LT50 around -4 °C). Only R. glacialis remained ice tolerant during all reproductive stages. Frost injury in reproductive shoots usually led to full fruit loss. Reproductive success of frost-treated but undamaged shoots did not differ significantly from control values. Assessing the frost damage risk on the basis of summer frost frequency and frost resistance shows that, in the alpine zone, low-statured species are rarely endangered as long as they are protected by snow. The situation is different in the subnival and nival zone, where frost-sensitive reproductive shoots may become frost damaged even when covered by snow. Unprotected individuals are at high risk of suffering from frost damage, particularly at higher elevations. It appears that ice tolerance in reproductive structures is an advantage but not an absolute precondition for colonizing high altitudes with frequent frost events....(more)
Ladinig U, et al. Oecologia 2013 Mar;171(3):743-60.
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- 4. Rhododendron tomentosum (Ledum palustre). A review of traditional use based on current research.
Rhododendron tomentosum Harmaja (previously: Ledum palustre) is a fragrant evergreen shrub found in peaty soils in northern Europe, Asia and North America, commonly referred to as wild rosemary, marsh tea, marsh rosemary or northern Labrador tea. At least since the eighteenth century it has been used in ethnomedicine for the treatment of various ailments, such as rheumatism, cough, cold and insect bites, as well as a repellent. The essential oil of wild rosemary with the rich polyphenolic fraction possesses analgesic, anti-inflammatory, antimicrobial, antiviral, antifungal and insecticidal potential, demonstrated by in vivo and in vitro studies. In addition, recent scientific research reported the promising antidiabetic, antioxidant and anticancer properties. This review summarizes the information concerning taxonomy, botany, ecology, chemical composition, biological activities, toxicology and traditional and contemporary application of Rhododendron tomentosum plants.
Copyright © 2013 Elsevier B.V. All rights reserved....(more)
Dampc A, et al. Fitoterapia 2013 Mar;85:130-43.
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- 5. Population versus hospital controls in the assessment of dietary intake of isoflavone for case-control studies on cancers in China.
To assess dietary isoflavone intake between population and hospital outpatient controls and examine if cancer risks estimated for isoflavone using hospital outpatient controls would be different from those using population controls. Three parallel case-control studies on leukemia, breast, and colorectal cancers in China in 2009-2010 were conducted, using population and hospital outpatient controls to separately match 560 incident cases at a 1:1 ratio. A validated food frequency questionnaire was administered by face-to-face interview. Conditional logistic regression analysis was used to estimate odds ratios (ORs) and 95% confidence intervals (CIs). The 2 control groups had closely similar distributions of dietary isoflavone intake. Risk estimates for breast cancers were adjusted ORs (95% CI) of 0.39 (0.23-0.66) and 0.31 (0.18-0.55) for daidzein, 0.35 (0.20-0.61) and 0.28 (0.16-0.52) for genistein, 0.66 (0.41-1.08) and 0.53 (0.32-0.88) for glycitein, and 0.53 (0.33-0.85) and 0.43 (0.26-0.71) for total isoflavone using hospital outpatient and population controls respectively. The study found that hospital outpatient controls were comparable to population controls in measured dietary intake of isoflavone in the Chinese hospital setting....(more)
Li L, et al. Nutr Cancer 2013;65(3):390-7.
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- 6. Influence of isoflavone intake and equol-producing intestinal flora on prostate cancer risk.
BACKGROUND:
The age-adjusted incidence rate of prostate cancer (PCa) has been reported to be lower among Asians than Western populations. A traditional Japanese meal, high in soybean products or isoflavones, may be associated with a decreased risk of PCa. Equol, which is converted from daidzein by human intestinal flora, is biologically more active than any other isoflavone aglycone.
MATERIALS AND METHODS:
We reviewed not only recent epidemiological studies on association of isoflavones with PCa risk, but also recent research on human intestinal bacteria responsible for converting daidzein into equol. Studies were systematically searched from the database published within the last 5 years of from 2008-2012.
RESULTS:
Five out of 6 articles showed significant association of isoflavones with a decreased risk of PCa, and two of them consistently showed that equol-producers carry a significantly reduced risk of PCa. Furthermore, 5 human intestinal bacteria that can convert daidzein into equol were identified in the last 5 years.
CONCLUSIONS:
If equol can reduce risk of PCa, a possible strategy for reducing the risk of PCa may be to increase the proportion of equol-producers by changing the intestinal flora to carrying an equol-producing bacterium with dietary alteration or probiotic technology....(more)
Sugiyama Y, et al. Asian Pac J Cancer Prev 2013;14(1):1-4.
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- 7. Identification and Expression of Genes Involved in the Conversion of Daidzein and Genistein by the Equol-Forming Bacterium Slackia isoflavoniconvertens.
Gut bacteria play a key role in the metabolism of dietary isoflavones, thereby influencing the availability and bioactivation of these polyphenols in the intestine. The human intestinal bacterium Slackia isoflavoniconvertens converts the main soybean isoflavones daidzein and genistein to equol and 5-hydroxy-equol, respectively. Cell extracts of S. isoflavoniconvertens catalyzed the conversion of daidzein via dihydrodaidzein to equol and that of genistein to dihydrogenistein. Growth of S. isoflavoniconvertens in the presence of daidzein led to the induction of several proteins as observed by two-dimensional difference gel electrophoresis. Based on determined peptide sequences, we identified a cluster of eight genes encoding the daidzein-induced proteins. Heterologous expression of three of these genes in Escherichia coli and enzyme activity tests with the resulting cell extracts identified the corresponding gene products as a daidzein reductase (DZNR), a dihydrodaidzein reductase (DHDR), and a tetrahydrodaidzein reductase (THDR). The recombinant DZNR also converted genistein to dihydrogenistein at higher rates than were observed for the conversion of daidzein to dihydrodaidzein. Higher rates were also observed with cell extracts of S. isoflavoniconvertens. The recombinant DHDR and THDR catalyzed the reduction of dihydrodaidzein to equol, while the corresponding conversion of dihydrogenistein to 5-hydroxy-equol was not observed. The DZNR, DHDR, and THDR were expressed as Strep-tag fusion proteins and subsequently purified by affinity chromatography. The purified enzymes were further characterized with regard to their activity, stereochemistry, quaternary structure, and content of flavin cofactors....(more)
Schröder C, et al. Appl Environ Microbiol 2013 Jun;79(11):3494-502.
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- 8. TPGS Emulsified Zein Nanoparticles Enhanced Oral Bioavailability of Daidzin: In Vitro Characteristics and In Vivo Performance.
A novel drug delivery system, TPGS 1000 (TPGS) emulsified zein nanoparticles (TZN), were designed with an objective to improve the oral bioavailability of daidzin, an isoflavone glycoside with estrogenic activities. Zein nanoparticles (ZN) and TZN were fabricated using an antisolvent method. They were found to be spherical in shape with a mean size around 200 nm and a low polydispersity. Their zeta potentials were about +25 mV at pH 5.5 and -23 mV at pH 7.4. Adding TPGS as an emulsifier increased the encapsulation efficiency of daidzin in ZN from 53% to 63%. Daidzin loaded TZN had a slower daidzin release compared with daidzin loaded ZN in both simulated digestive fluids and a pH 7.4 buffer. Confocal laser scanning microscopy suggested that the cellular uptake of coumarin-6 labeled TZN in human intestinal epithelial Caco-2 cells were significantly higher than fluorescent ZN. Cellular uptake and transport studies revealed that daidzin in TZN were taken up more efficiently into Caco-2 cells and transported more quickly through Caco-2 monolayer than daidzin solution. A pharmacokinetic study demonstrated that the Cmax of daidzein in mice after oral administration of daidzin loaded TZN was 5.66 ± 0.16 μM, which was improved by 2.64-fold compared with that of daidzin solution (2.14 ± 0.04 μM). Moreover, the areas under the curve (AUC0-12 h) for daidzin loaded in TZN were enhanced by 2.4-fold compared with that of daidzin solution. These results suggested that TZN could be an effective strategy to improve the oral bioavailability of isoflavone glycosides like daidzin....(more)
Zou T, et al. Mol Pharm 2013 May 6;10(5):2062-70.
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- 9. Associations between urinary soy isoflavonoids and two inflammatory markers in adults in the United States in 2005-2008.
PURPOSE:
The aim of this study was to determine the association between urinary isoflavonoid (genistein, daidzein, and the daidzein metabolites O-desmethylangolensin (O-DMA) and equol) excretion and markers of inflammation in adults in the United States in National Health and Nutrition Examination Survey (NHANES) 2005-2008.
METHODS:
The NHANES is a cross-sectional study conducted by the National Center for Health Statistics to study the health and nutritional status of people living in the United States. The analysis included 1,683 participants from study years 2005-2008 for whom urinary isoflavonoids were measured and who met inclusion criteria. Urinary isoflavonoids were measured by HPLC-APPI-MS/MS. Serum C-reactive protein (CRP) was measured by latex-based nephelometry. White blood cell (WBC) count was measured by Coulter counting. Multivariable linear regression was used to calculate the geometric mean values of the markers, and multivariable logistic regression was used to estimate the odds of high CRP (≥3 mg/L) and of high WBC count (≥7,900/μL) by quartile of urinary isoflavonoid (nmol/mg creatinine).
RESULTS:
The highest quartile of genistein (OR = 0.62; 95 % CI 0.39-0.99) was associated with significantly decreased odds of high CRP compared with the lowest quartile. The sum of daidzein and its metabolites was significantly inversely associated with serum CRP concentration (p-trend = 0.017). Equol was inversely associated with WBC count (p-trend < 0.0001). O-DMA was the only isoflavonoid whose excretion was significantly associated with a decrease in both CRP (p-trend = 0.024) and WBC count (p-trend < 0.0001).
CONCLUSIONS:
Though no clear pattern emerged, higher excretion of certain soy isoflavonoids was associated with decreased CRP concentration and WBC counts, suggesting a possible inverse association between soy intake and inflammation....(more)
Nicastro HL, et al. Cancer Causes Control 2013 Jun;24(6):1185-96.
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- 10. Self-reported menopausal symptoms in a racially diverse population and soy food consumption.
OBJECTIVES:
Evaluate the association of self-reported vasomotor symptom (VMS) frequency with race/ethnicity among a diverse midlife US population and explore menopause symptom differences by dietary soy isoflavone (genistein+daidzein) consumption.
STUDY DESIGN:
Cross-sectional population-based study of peri- and postmenopausal women, ages 45-58.
OUTCOMES:
Recent VMS frequency, VMS ever; recent symptom bother (hot flashes, night sweats, headache and joint-ache).
RESULTS:
Of 18,500 potentially eligible women, 9325 returned questionnaires (50.4% response); 3691 were excluded (premenopausal, missing data, taking hormones). Of 5634 remaining women, 82.1% reported hot flashes ever, 73.1% reported night sweats ever; 48.8% and 38.6% reported recent hot flashes or night sweats, respectively. Compared with White women, Chinese, Japanese, Vietnamese, other Asian (each p<0.001) and Filipino (p<0.01) women less commonly reported ever having hot flashes; Asian women less commonly reported recent VMS bother (p<0.001). Black women more commonly reported hot flashes ever (p<0.05) and recent VMS bother (p<0.05). Compared with non-Hispanic White women, Hispanic women were less likely to report hot flashes (p<0.05) or night sweats (p<0.001) ever. Women were classified by isoflavone consumption: (1) none (n=1819), (2) 0.01-4.30mg/day (n=1931), (3) 4.31-24.99mg/day (n=1347) and (4) ≥25mg/day (n=537). There were no group differences in recent VMS number/day: (1) 7.0 (95% CI 6.5, 7.5); (2) 6.4 (95% CI 6.0, 7.1); (3) 7.0 (95% CI 6.3, 8.2); and (4) 6.8 (95% CI 6.1, 7.7).
CONCLUSIONS:
Menopausal symptoms, independent of isoflavone intake, varied considerably by race/ethnicity and were least common among Asian races.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Reed SD, et al. Maturitas 2013 Apr 2.
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- 11. Dietary supplements and prostate cancer: a systematic review of double-blind, placebo-controlled randomised clinical trials.
Dietary supplements are popular among patients with prostate cancer (PC). The objective of this systematic review was to critically examine double-blind, placebo-controlled randomised clinical trials (RCTs) of non-herbal dietary supplements and vitamins (NHDS) for evidence that prostate specific antigen (PSA) levels were reduced in PC patients. Five databases were searched from their inception through December 2012 to identify studies that met our inclusion criteria. Methodological quality was independently assessed by two reviewers using the Cochrane tool. Eight RCTs met the eligibility criteria and were of high methodological quality. The following supplements were tested: isoflavones (genistein, daidzein, and glycitein), minerals (Se) or vitamins (vitamin D) or a combination of antioxidants, bioflavonoids, carotenoids, lycopenes, minerals (Se, Zn, Cu, and Mg), phytoestrogens, phytosterols, vitamins (B2, B6, B9, B12, C, and E), and other substances (CoQ10 and n-acetyl-l cysteine). Five RCTs reported no significant effects compared with placebo. Two RCTs reported that a combination of antioxidants, isoflavones, lycopenes, minerals, plant oestrogens and vitamins significantly decreased PSA levels compared with placebo. One RCT did not report differences in PSA levels between the groups. In conclusion, the hypothesis that dietary supplements are effective treatments for PC patients is not supported by sound clinical evidence. There are promising data for only two specific remedies, which contained a mixture of ingredients, but even for these supplements, additional high quality evidence is necessary before firm recommendations would be justified....(more)
Posadzki P, et al. Maturitas 2013 Apr 5.
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- 12. Daidzein, R-(+)equol and S-(-)equol inhibit the invasion of MDA-MB-231 breast cancer cells potentially via the down-regulation of matrix metalloproteinase-2.
PURPOSE:
Soy isoflavones may inhibit tumor cell invasion and metastasis via their effects on matrix metalloproteinases (MMPs) and their tissue inhibitors (TIMPs). The current study investigates the effects of daidzein, R- and S-equol on the invasion of MDA-MB-231 human breast cancer cells and the effects of these compounds on MMP/TIMP expression at the mRNA level.
METHODS:
The anti-invasive effects of daidzein, R- and S-equol (0, 2.5, 10, 50 μM) on MDA-MB-231 cells were determined using the Matrigel invasion assay following 48-h exposure. Effects on MMP-2, MMP-9, TIMP-1 and TIMP-2 expression were assessed using real-time PCR. Chiral HPLC analysis was used to determine intracellular concentrations of R- and S-equol.
RESULTS:
The invasive capacity of MDA-MB-231 cells was significantly reduced (by approximately 50-60 %) following treatment with 50 μM daidzein, R- or S-equol. Anti-invasive effects were also observed with R-equol at 2.5 and 10 μM though overall equipotent effects were induced by all compounds. Inhibition of invasion induced by all three compounds at 50 μM was associated with the down-regulation of MMP-2, while none of the compounds tested significantly affected the expression levels of MMP-9, TIMP-1 or TIMP-2 at this concentration. Following exposure to media containing 50 μM R- or S-equol for 48-h intracellular concentrations of R- and S-equol were 4.38 ± 1.17 and 3.22 ± 0.47 nM, respectively.
CONCLUSION:
Daidzein, R- and S-equol inhibit the invasion of MDA-MB-231 human breast cancer cells in part via the down-regulation of MMP-2 expression, with equipotent effects observed for the parent isoflavone daidzein and the equol enantiomers....(more)
Magee PJ, et al. Eur J Nutr 2013 Apr 9.
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- 13. In vitro effects of genistein and daidzein on the activity of adrenocortical steroidogenic enzymes in mature female pigs.
Soy products, commonly used as a protein source in farm animals' diets, contain considerable quantities of non-nutrient constituents such as phytoestrogens. Genistein and daidzein are known to affect the reproductive processes in humans and animals. However, reports concerning phytoestrogens and porcine adrenal steroidogenesis are scarce, and the adrenal mechanism of phytoestrogen action in species other than humans and rodents is poorly recognized. The goal of the present paper was to examine the in vitro effects of genistein and daidzein on the activity of key enzymes for cortisol and corticosterone synthesis in porcine adrenocortical cells harvested during the luteal or follicular phase of the porcine estrous cycle. The cells were treated with genistein or daidzein (10 μM), with or without ACTH (5 nM), in the presence or absence of precursors (1 μM) of cortisol (pregnenolone, P5; progesterone, P4; 17-hydroxyprogesterone, 17OH-P4; or 11-deoxycortisol, 11d-cortisol) or corticosterone: (P5 or P4) synthesis. The supplementation of a medium with P5, P4, 17OH-P4 or 11d-cortisol enabled us to measure the activity of cholesterol side-chain cleavage enzyme (P450scc), 3β-hydroxysteroid dehydrogenase (3β-HSD), 17α-hydroxylase/C17-20 lyase (P450c17) or 21-hydroxylase (P450c21) and 11β-hydroxylase (P45011β), respectively. We demonstrated that in sexually mature, cyclic pigs, regardless of the phase of the estrous cycle, phytoestrogens genistein and daidzein suppressed basal and ACTH-stimulated in vitro secretion of cortisol and corticosterone via progesterone synthesis inhibition. This indicates that phytoestrogens specifically inhibit the 3β-HSD activity in porcine adrenocortical cells. We suggest that genistein and daidzein present in soy products may negatively affect glucocorticoid synthesis of mature gilts by disrupting adrenal steroidogenesis at the 3β-HSD level....(more)
Kaminska B, et al. J Physiol Pharmacol 2013 Feb;64(1):103-8.
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- 14. Production of a Novel O-Methyl-Isoflavone by Regioselective Sequential Hydroxylation and O-Methylation Reactions in Streptomyces avermitilis Host System.
Distinct isoflavone O-methyltransferases (IOMTs) from Streptomyces species were isolated and expressed using S. avermitilis host system. Previously reported isoflavone 7-O-methyltransferases (I7OMTs, E.C. 2.1.1.150) and two putative O-methyltransferases (OMTs) from Saccharopolyspora erythraea were selected by comparative sequence grouping and expressed in S. avermitilisΔSaOMT2 under the control of constitutive ermE promoter. During whole-cell biotransformation of 4',7-dihydroxyisoflavone (daidzein) by constructed recombinant strains, production of O-methylated daidzein was investigated. S. avermitilisΔSaOMT2::SeOMT3 (SeOMT3) produced 7-methoxy-4'-hydroxyisoflavone (7-OMD) with 4.5% of low conversion yield due to competitive oxidation reactions. However, SeOMT3 could produce a novel 4',7-dihydroxy-3'-methoxyisoflavone (3'-OMD) (<1%) resulted from subsequent 3'-O-methylation of 3',4',7-trihydroxyisoflavone (3'-OHD) which was a hydroxylated product catalyzed by oxygenases. Although external addition of SAM did not change the conversion yield of O-methylation reaction, co-expression of SAM synthetase gene (metK) with SeOMT3 greatly induced the regiospecific O-methylation reaction at 3'-hydroxyl group with final conversion of 12.1% using 0.1 mM of daidzein. Biotechnol. Bioeng. 2013;9999: XX-XX. © 2013 Wiley Periodicals, Inc....(more)
Choi KY, et al. Biotechnol Bioeng 2013 Apr 16.
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- 15. Sensitization patterns in Compositae-allergic patients with current or past atopic dermatitis.
Background. An association between Compositae sensitization and atopic dermatitis has been suggested on the basis of case reports and clinical studies. Objectives. To describe the characteristics of sensitization in Compositae-allergic patients with current and/or past atopic dermatitis. Patients/materials/methods. Consecutive Compositae-sensitive patients were selected for analysis if they had a history of (i) present and/or past atopic dermatitis or (ii) childhood flexural eczema or (iii) childhood eczema of any kind and a positive prick test result. Results. Fifty-one persons (35 females and 16 males) were included. The mean age was lower and the percentage of males was slightly higher than in non-atopics. Testing with sesquiterpene lactone mix, parthenolide and Compositae mix 6% or 5% detected 96% of the patients. Occupational sensitization occurred in 22%. The sensitizing pattern did not differ much from that of non-atopics, except that dandelion was an important allergen in children. Cobalt allergy was the most frequent other contact allergy, occurring in 37%. Conclusions. Persons with current or past atopic dermatitis may become sensitized to Compositae at any age, both occupationally and non-occupationally. They should be screened for Compositae allergy on equal terms with non-atopics, except that dandelion extract should always be tested in children. Co-sensitization to cobalt was frequent, but probably not related to the plant allergy....(more)
Paulsen E, et al. Contact Dermatitis 2013 May;68(5):277-85.
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- 16. The Effect of Taraxacum officinale Hydroalcoholic Extract on Blood Cells in Mice.
Objectives. Dandelion (Taraxacum officinale) is a herbaceous perennial plant of the family Asteraceae and has medicinal and culinary uses. Dandelion has been used as a remedy for anemia, purifing the blood, and providing immune modulation. Therefore, the aim of this study was to investigate the effect of hydro alcoholic extract on blood cells in mice. Methods. Five groups each including ten adult female (Balb/C) mice weighing 30 ± 5 g were chosen. Normal saline was administered as placebo for group, and dandelion hydro alcoholic extract in doses of 50,100, and 200 mg/kg was injected intraperitoneally for 20 days to test groups and the last group was control group.WBC, RBC, HB, HCT, platelet, and other cells were measured with automated cell counter. Main Results. The number of RBC and the rate of HB in three doses of 100 and 200 mg/kg significantly increased (P < 0.05). As compared with control group, the number of WBC in three doses of 50, 100, and 200 mg/kg increased, but it was significantly in 200 mg/kg dandelion treated group as compared with control group(P < 0.05). The rate of platelet in three doses of 50, 100 and 200 mg/kg significantly decreased as compared with control group (P < 0.01). 3 doses of dandelion increased lymphocyte numbers significantly compared with controls. Conclusion. The study indicates efficacy of dandelion extract on RBC and HB in doses of 50, 100, and 200 mg/kg and in 200 mg/kg on WBC to achieve normal body balance....(more)
Modaresi M, et al. Adv Hematol 2012;2012:653412.
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- 17. Inhibitory effect of aqueous Dandelion extract on HIV-1 replication and reverse transcriptase activity.
BACKGROUND:
Acquired immunodeficiency syndrome (AIDS), which is caused by the human immunodeficiency virus (HIV), is an immunosuppressive disease that results in life-threatening opportunistic infections. The general problems in current therapy include the constant emergence of drug-resistant HIV strains, adverse side effects and the unavailability of treatments in developing countries. Natural products from herbs with the abilities to inhibit HIV-1 life cycle at different stages, have served as excellent sources of new anti-HIV-1 drugs. In this study, we aimed to investigate the anti-HIV-1 activity of aqueous dandelion extract.
METHODS:
The pseudotyped HIV-1 virus has been utilized to explore the anti-HIV-1 activity of dandelion, the level of HIV-1 replication was assessed by the percentage of GFP-positive cells. The inhibitory effect of the dandelion extract on reverse transcriptase activity was assessed by the reverse transcriptase assay kit.
RESULTS:
Compared to control values obtained from cells infected without treatment, the level of HIV-1 replication and reverse transcriptase activity were decreased in a dose-dependent manner. The data suggest that dandelion extract has a potent inhibitory activity against HIV-1 replication and reverse transcriptase activity. The identification of HIV-1 antiviral compounds from Taraxacum officinale should be pursued.
CONCLUSIONS:
The dandelion extract showed strong activity against HIV-1 RT and inhibited both the HIV-1 vector and the hybrid-MoMuLV/MoMuSV retrovirus replication. These findings provide additional support for the potential therapeutic efficacy of Taraxacum officinale. Extracts from this plant may be regarded as another starting point for the development of an antiretroviral therapy with fewer side effects....(more)
Han H, et al. BMC Complement Altern Med 2011 Nov 14;11:112.
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- 18. Amelioration of oxidative stress by dandelion extract through CYP2E1 suppression against acute liver injury induced by carbon tetrachloride in Sprague-Dawley rats.
The protective effects of common dandelion leaf water extract (DLWE) were investigated by carbon tetrachloride (CCl4) induced hepatitis in Sprague-Dawley rats. The animals were divided into five groups: normal control, DLWE control, CCl4 control, and two DLWE groups (0.5 and 2 g/kg bw). After 1 week of administering corresponding vehicle or DLWE, a single dose of CCl4 (50% CCl4/olive oil; 0.5 mL/kg bw) was administered 24 h before killing in order to produce acute liver injury. The DLWE treatment significantly decreased CCl4-induced hepatic enzyme activities (AST, ALT and LDH) in a dose dependent manner. Also, the obstructed release of TG and cholesterol into the serum was repaired by DLWE administration. Hepatic lipid peroxidation was elevated while the GSH content and antioxidative enzyme activities were reduced in the liver as a result of CCl4 administration, which were counteracted by DLWE administration. Furthermore, the hepatocytotoxic effects of CCl4 were confirmed by significantly elevated Fas and TNF-α mRNA expression levels, but DLWE down-regulated these expressions to the levels of the normal control. Highly up-regulated cytochrome P450 2E1 was also lowered significantly in the DLWE groups. These results indicate that DLWE has a protective effect against CCl4-induced hepatic damage with at least part of its effect being attributable to the attenuation of oxidative stress and inflammatory processes resulting from cytochrome P450 activation by CCl4....(more)
Park CM, et al. Phytother Res 2010 Sep;24(9):1347-53.
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- 19. DeoxyArbutin and its derivatives inhibit tyrosinase activity and melanin synthesis without inducing reactive oxygen species or apoptosis.
Safety is a major concern in developing commercial skin-lightening agents. Here, we report the modulating effects of deoxyArbutin (dA) and its second-generation derivatives - deoxyFuran (dF), 2-fluorodeoxyArbutin (fdA), and thiodeoxyArbutin (tdA) - on tyrosinase, and consequently, on melanization. Results demonstrate that dA and its derivatives inhibit tyrosine hydroxylase and dopa oxidase activity of tyrosinase. The inhibition is dose-dependent, thereby inhibiting melanin synthesis in intact melanocytes, when used at concentrations that retain 95% viability of the treated cells in culture. Herein we demonstrate that dA, and its second-generation derivatives dF, fdA, and tdA, exhibit dose-dependent reductions in melanocyte cell number, primarily due to inhibition of proliferation rather than initiation of apoptosis as exemplified by hydroquinone (HQ), ie, cytostatic as opposed to cytotoxic. Human and murine melanocytes with functional mutations in either tyrosinase or tyrosinase-related protein 1 (Tyrp1) are less sensitive to the cytostatic effects of dA and its derivatives. Minimal amounts of reactive oxygen species (ROS) were generated upon treatment with dA and its derivatives, in contrast to a dramatic amount of ROS induced by HQ. This increase in ROS subsequently induced the expression of the endogenous antioxidant catalase in treated melanocytes. Treatment with exogenous antioxidants provided protection for melanocytes treated with HQ, but not dA and its derivatives, suggesting that HQ exerts more oxidative stress. These studies demonstrate that dA and its derivatives are relatively safe tyrosinase inhibitors for skin lightening or for ameliorating hyperpigmented lesions....(more)
Chawla S, et al. J Drugs Dermatol 2012 Oct;11(10):e28-34.
Related Products: Deoxyarbutin
- 20. Study on the Stability of DeoxyArbutin in an Anhydrous Emulsion System.
The skin-whitening agent, deoxyArbutin, is a potent tyrosinase inhibitor that is safer than hydroquinone and arbutin. However, it is thermolabile in aqueous solutions, where it decomposes to hydroquinone. Pharmaceutical and cosmetic emulsions are normally oil-in-water (o/w) or water-in-oil (w/o) systems; however, emulsions can be formulated with no aqueous phase to produce an anhydrous emulsion system. An anhydrous emulsion system could offer a stable vehicle for compounds that are sensitive to hydrolysis or oxidation. Therefore, to enhance the stability of deoxyArbutin in formulations, we chose the polyol-in-silicone, anhydrous emulsion system as the basic formulation for investigation. The quantity of deoxyArbutin and the accumulation of hydroquinone in both hydrous and anhydrous emulsions at various temperatures were analyzed through an established high performance liquid chromatographic (HPLC) method. The results indicated that water increased the decomposition of deoxyArbutin in the formulations and that the polyol-in-silicone, oil-based, anhydrous emulsion system provided a relatively stable surrounding for the deoxyArbutin that delayed its degradation at 25 °C and 45 °C. Moreover, the composition of the inner hydrophilic phase, containing different amounts of glycerin and propylene glycol, affected the stability of deoxyArbutin. Thus, these results will be beneficial when using deoxyArbutin in cosmetics and medicines in the future....(more)
Lin CC, et al. Int J Mol Sci 2011;12(9):5946-54.
Related Products: Deoxyarbutin
- 21. Determination of the Thermodegradation of deoxyArbutin in Aqueous Solution by High Performance Liquid Chromatography.
Tyrosinase is the key and rate-limiting enzyme responsible for the conversion of tyrosine into melanin. Competitive inhibition of tyrosinase enzymatic activity results in decreased or absent melanin synthesis by melanocytes in human skin. DeoxyArbutin (4-[(tetrahydro-2H-pyran-2-yl)oxy]phenol), a novel skin whitening agent, was synthesized through the removal of hydroxyl groups from the glucose side-chain of arbutin. DeoxyArbutin not only shows greater inhibition of tyrosinase activity but is also safer than hydroquinone and arbutin. Hence, deoxyArbutin is a potential skin whitening agent for cosmetics and depigmenting drugs; however, stability of this compound under some conditions remains a problem. The lack of stability poses developmental and practical difficulties for the use of deoxyArbutin in cosmetics and medicines. Improving the thermostability of deoxyArbutin is an important issue for its development. In this research, we established an analytical procedure to verify the amount of deoxyArbutin in solutions using a high performance liquid chromatographic (HPLC) method. The results indicate that this novel skin whitening agent is a thermolabile compound in aqueous solutions. Additionally, the rate constant for thermodegradation (k) and the half-life (t(1/2)) of deoxyArbutin were determined and can be used to understand the thermodegradation kinetics of deoxyArbutin. This information can aid in the application of deoxyArbutin for many future uses....(more)
Yang CH, et al. Int J Mol Sci 2010 Oct 15;11(10):3977-87.
Related Products: Deoxyarbutin
- 22. Effects of hydroquinone and its glucoside derivatives on melanogenesis and antioxidation: Biosafety as skin whitening agents.
BACKGROUND AND OBJECTIVE:
The biosafety of hydroquinone and its derivatives as skin whitening agent remains controversial. Here, we investigated the effects of hydroquinone, arbutin, and deoxyarbutin (d-arb) on melanogenesis and antioxidation using cultured melan-a melanocytes in the presence or absence of ultraviolet A (UVA)-induced oxidative stress and determined whether d-arb enables to be an alterative to hydroquinone and arbutin for skin whitening use.
METHODS:
d-arb was synthesized in this study by removing all hydroxyl groups from the glucose side-chain of arbutin. Tyrosinase activity was measured by (14)C-tyrosine incorporation, the intracellular reactive oxygen species (ROS) level was monitored by H(2)DCFDA fluorescence labeling, and the cell viability was determined by MTT assay in murine melan-a melanocytes treated with hydroquinone, arbutin and deoxyarbutin in the presence or absence of UVA-induced oxidative stress.
RESULTS:
The cytotoxicity of hydroquinone and arbutin except for d-arb was increased while the cells exposed to a nontoxic dose (3J/cm(2)) of UVA irradiation. Suppressed ROS generation was noted by the treatment of d-arb to compare with arbutin and hydroquinone. All three compounds had a similar inhibition on tyrosinase activity in dose-dependent manners with two- to three-fold decreases over the untreated control. There was no change in expression of tyrosinase protein in cells treated with arbutin or hydroquinone, but a decreased protein expression of tyrosinase was seen in deoxyarbutin-treated cells.
CONCLUSIONS:
Deoxyarbutin exerts potent tyrosinase inhibition, lessened cytotoxicity, and certain antioxidation potential, may serve as an effective and safe alternative to hydroquinone for use in skin whitening....(more)
Hu ZM, et al. J Dermatol Sci 2009 Sep;55(3):179-84.
Related Products: Deoxyarbutin
- 23. Mechanism of tyrosinase inhibition by deoxyArbutin and its second-generation derivatives.
BACKGROUND:
Disorders, such as age spots, melasma and hyperpigmentation at sites of actinic damage, emanate from the augmentation of an increased amount of epidermal melanin.<br/>OBJECTIVES:
The ineptness of current therapies in treating these conditions, as well as high cytotoxicity, mutagenicity, poor skin penetration and low stability of skin-depigmenting formulations led us to investigate new compounds that meet the medical requirements for depigmentation agents. We have shown previously that the tyrosinase inhibitor deoxyArbutin (dA) is a more effective and less toxic skin lightener than hydroquinone (HQ).
METHODS:
The efficacy and reversibility of dA and its derivatives on inhibiting tyrosine hydroxylase and DOPAoxidase was assessed using standard assays.
RESULTS:
dA and its second-generation derivatives inhibit tyrosine hydroxylase and DOPAoxidase activities of tyrosinase dose dependently thereby inhibiting melanin synthesis in intact melanocytes, when used at concentrations that retain 95% cell viability in culture. This depigmenting effect was completely reversible when the compounds were removed. Tyrosinase inhibition was also observed in vitro when tested using human and purified mushroom tyrosinase, establishing that they are direct enzyme inhibitors. Lineweaver-Burk reciprocal plot analysis using mushroom tyrosinase illustrated that dA and its derivatives are more robust competitive inhibitors than HQ, when tyrosine is used as substrate.
CONCLUSIONS:
Thus, dA and its second-generation derivatives, which inhibit melanogenesis at safe concentrations by specifically acting on the tyrosinase enzyme at a post-translational level, are promising agents to ameliorate hyperpigmented lesions or lighten skin....(more)
Chawla S, et al. Br J Dermatol 2008 Dec;159(6):1267-74.
Related Products: Deoxyarbutin
- 24. Retrospective evaluation of biopsychosocial determinants and treatment response in patients receiving devil's claw extract (doloteffin).
In a retrospective evaluation of patients taking part for 2 months in a postmarketing surveillance study on the effectiveness and safety of Harpagophytum procumbens, associations were found to known explanators of pain, disability and depression. Therefore, treatment non-responders might best be referred to a multimodal pain relief program that deals with fear avoidance beliefs, enhances experiences that decrease perceptions linking disability and pain and forces the patients to rethink the way they deal with the problem. However, during treatment with the aqueous Harpagophytum extract, this decision might reasonably be postponed to the end of month 4, since it has been shown that the maximum pain relief occurs after 3-4 months....(more)
Thanner J, et al. Phytother Res 2009 May;23(5):742-4.
Related Products: Devil's Claw Extract
- 25. Studies on synthesis, stability, release and pharmacodynamic profile of a novel diacerein-thymol prodrug.
Involvement of oxidative stress, leading to chondrocyte senescence and cartilage ageing has been implicated in the pathogenesis of osteoarthritis (OA). New efforts to prevent the development and progression of OA include strategies and interventions aimed at reducing oxidative damage in articular cartilage using antioxidants as adjuncts to conservative therapy. Diacerein is an anthraquinone derivative with a marked disease modifying effect on OA owing to IL-1 β inhibition. In the present work an attempt was made at design and development of a co-drug of diacerein with antioxidant thymol. Structural elucidation was carried out by spectral analysis. When release kinetics of prodrug was studied in phosphate buffer (pH 7.4) and small intestinal homogenates of rats, 91% and 94% diacerein was available respectively at the end of 4.5 h. Chemical linkage of thymol with diacerein improved its lipophilicity and hence bioavailability. Screening of prodrug in Freud's adjuvant-induced arthritis and ulcerogenic potential by Rainsford's cold stress model exhibited significant reduction in paw volume, joint diameter and ulcer index with superior anti-inflammatory/anti-arthritic activities than the standards. Results of histopathology of tibio-tarsal joint indicated that animals treated with diacerein exhibited moderate synovitis while thymol and physical mixture-treated animals showed mild synovitis. Interestingly in prodrug-treated animals synovitis was not observed. The results of this study underline the promising potential of co-drug of diacerein and thymol in the management of OA....(more)
Dhaneshwar S, et al. Bioorg Med Chem Lett 2013 Jan 1;23(1):55-61.
Related Products: Diacerein
- 26. Disease-modifying osteoarthritis drugs: in vitro and in vivo data on the development of DMOADs under investigation.
INTRODUCTION:
Osteoarthritis is a disabling affliction, and disease-modifying osteoarthritis drugs (DMOADs) would be highly desirable adjuncts to symptomatic relief as they may delay the disease process.
AREAS COVERED:
This study is a comprehensive review of the recent literature on the efficacy of DMOADs in the treatment of OA. In vitro and in vivo evidence was collected using MEDLINE® (1950 to November 2012) and EMBASE (1980 to November 2012) databases. Several drugs have demonstrated DMOAD effects in OA. They can be divided into three groups based on their predominant mode of action: those targeting cartilage, inflammatory pathways and subchondral bone. OARSI guidelines recommend glucosamine and chondroitin sulphates and diacerein as DMOADS, and NICE will recommend glucosamine sulphate in the next update of guidelines. Exploration of improved outcome measures and identification of subgroups of patients most likely to benefit from different DMOADs are likely to be the most important areas of development over the coming years.
EXPERT OPINION:
It is expected that a wider range of prospective clinical studies will be embarked upon in the coming years. Trials including MRI as well as joint space narrowing (JSN) should be designed in a systematic manner, powered with sufficient numbers to demonstrate clinical benefit at different stages of disease....(more)
Davies PS, et al. Expert Opin Investig Drugs 2013 Apr;22(4):423-41.
Related Products: Diacerein
- 27. The efficacy of diacerein in hand osteoarthritis: a double-blind, randomized, placebo-controlled study.
BACKGROUND:
Diacerein is a drug used in osteoarthritis (OA) that elicits an inhibitory effect on interleukin-1 and metalloproteases. Although diacerein has shown modest efficacy and safety in the treatment of knee and hip OA, there have been no placebo-controlled clinical trials for hand OA.
OBJECTIVE:
The aim of the current study was to investigate the efficacy and tolerability of diacerein in patients with hand OA.
METHODS:
Patients fulfilling the American College of Rheumatology criteria for hand OA participated in this randomized, double-blind, placebo-controlled study. Eligible patients were >40 years of age, had at least 1 tender joint, and had a joint pain visual analog scale of >30 mm. Patients received diacerein (50 mg) or placebo BID for 12 weeks. The primary end point was the Australian/Canadian Osteoarthritis Hand Index (AUSCAN) pain score at 4 weeks. Secondary end points were AUSCAN pain score at 12 weeks and AUSCAN physical function and stiffness score, patient and physician global assessment, functional index of hand OA scores, and multidimensional health assessment questionnaire results at 4 weeks and 12 weeks.
RESULTS:
Eighty-six Korean patients were enrolled (42 diacerein, 44 placebo). The intention-to-treat and per-protocol analyses revealed no significant differences between the 2 groups in terms of change in AUSCAN pain score at 4 weeks, except for improvement in physician global assessment at 4 weeks (per-protocol analysis, P = 0.004). The safety profile of diacerein was comparable to placebo, except for frequent discoloration of the urine (88% vs 20%).
CONCLUSION:
These results suggest that diacerein 50 mg BID may be ineffective in controlling the symptoms of hand OA. ClinicalTrials.gov identifier: NCT00685542.
Copyright © 2013 Elsevier HS Journals, Inc. All rights reserved....(more)
Shin K, et al. Clin Ther 2013 Apr;35(4):431-9.
Related Products: Diacerein
- 28. A comparison of the therapeutic efficacy of diclofenac in osteoarthritis: a systematic review of randomised controlled trials.
OBJECTIVE:
Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) commonly prescribed for pain relief in osteoarthritis (OA). The relative efficacy of diclofenac compared to other pain relief medications used in OA (e.g., alternative NSAIDs, cyclooxygenase type 2 [COX-2] inhibitors) is uncertain. The objective of this systematic review is to compare the current evidence on efficacy of diclofenac versus other pain relief medications.
RESEARCH DESIGN AND METHODS:
A systematic literature search was carried out for randomised, well controlled clinical trials comparing the efficacy of diclofenac with other pain relief medications in OA (reviews, meta-analyses and n = 1 trials were excluded). The databases searched were EMBASE, Ovid MEDLINE, Ovid MEDLINE In-Process and Other Non-Indexed Citations, and Ovid MEDLINE Daily Update. Articles were included from 1999 onwards. Retrieved articles were discussed by comparator medication.
RESULTS:
Of the 263 articles identified in the literature search, 37 were eventually included in this review. These were comparisons with the selective COX-2 inhibitors etoricoxib, celecoxib, lumiracoxib and rofecoxib; comparisons with the NSAIDs aceclofenac, dexketoprofen, etodolac, lornoxicam, meloxicam, nabumetone and nimesulide; and comparisons to acetaminophen, tramadol, diacerein, oxaceprol, oral hydrolytic enzyme therapies, Chinese herbal remedies and castor oil supplementation. Overall, in the majority of the trials at therapeutic doses diclofenac provided similar efficacy to comparator treatments; and in general diclofenac was able to support its position as a reference medication of choice for OA trials.
CONCLUSIONS:
The efficacy of diclofenac is largely unchallenged in that it remains as effective as newer pain relief medications employed in OA. A review of the available data demonstrates that diclofenac continues to provide physicians with a benchmark pharmacological treatment for OA....(more)
Pavelka K. Curr Med Res Opin 2012 Jan;28(1):163-78.
Related Products: Diacerein
- 29. Comment on: Ramos-Zavala et al. Effect of diacerein on insulin secretion and metabolic control in drug-naïve patients with type 2 diabetes: a randomized clinical trial. Diabetes Care 2011;34:1591-1594.
Related Products: Diacerein
- 30. Diacerein as adjuvant to diclofenac sodium in osteoarthritis knee.
AIM:
To evaluate clinical effectiveness of diacerein as an adjuvant to diclofenac sodium in treatment of Indian patients with symptomatic osteoarthritis (OA) knee.
METHODS:
This is a prospective, double-blind, placebo-controlled and intention-to-treat study. An initial washout period of 1 week, was followed by 3 months treatment period during which patients were randomly divided to receive either capsule diacerein 50 mg or matched placebo once daily for the first month and twice daily for the next 2 months with diclofenac sodium 75 mg sustained release tablet once daily given to both groups. Patients were observed for one more month, using paracetamol as rescue therapy. Treatment efficacy was assessed by a visual analogue scale (VAS) and the Western Ontario and McMaster University (WOMAC) Osteoarthritis Index, patient and physician global assessment of OA, daily paracetamol intake.
RESULTS:
Of 84 patients screened, 74 patients formed the intent-to-treat population (37 patients in each group). At baseline, both groups were comparable and at the third month functional index and pain intensity were better in the diacerein group (VAS 15.33 ± 5.07; WOMAC 15.9 ± 2.40) as compared to the placebo group (VAS 22.83 ± 6.90;WOMAC 36.8 ± 2.92; P < 0.05). When analyzed at the fourth month, improvement persisted in the iacerein group (VAS 14.83 ± 5.16; WOMAC 16 ± 2.5) as compared to placebo group (VAS 33 ± 7.72; WOMAC 48.26 ± 3.5; P < 0.05), demonstrating the carry-over effect of diacerein, which was confirmed by lesser paracetamol consumption in the diacerein group (5.967 ± 0.8087) as compared to the placebo group (12.433 ± 2.128; P < 0.05).
CONCLUSION:
Use of diacerein and diclofenac sodium together decreases pain and improves joint function significantly more than diclofenac alone in OA knee.
© 2011 The Authors. International Journal of Rheumatic Diseases © 2011 Asia Pacific League of Associations for Rheumatology and Blackwell Publishing Asia Pty Ltd....(more)
Singh K, et al. Int J Rheum Dis 2012 Feb;15(1):69-77.
Related Products: Diacerein
- 31. [Clinical efficacy of bushen huoxue qubi decoction on treatment of knee-osteoarthritis and its effect on hemarheology, anti-inflammation and antioxidation].
OBJECTIVE:
To prove the clinical effect and mechanism of Bushen Huoxue Qubi Decoction on treatment of knee-osteoarthritis.
METHOD:
Ninty-six knee-osteoarthritic patients accompanied with symptoms of liver and kidney deficiency and blocked main and collateral channels were divided into two groups randomly. Patients in the treatment group (n = 48) were administrated by Bushen Huoxue Qubi Decoction one bag/day for four weeks; and those in the control group (n = 48) were given diacerein (50 mg Bid, Po) and celecoxib (0.2 Qd, Po) for four weeks. The changes of VAS score, Womac score, relative viscosity, aggregation index and IL-1beta, NO, iNOS, LPO, SOD in serum were observed. Adverse effects were determined during follow-up visit and detection for blood routine and hepatic and renal functions.
RESULT:
Its clinical control rates as per Western medicine and TCM standards for treatment of knee-osteoarthritis and effective rate were 33.3%, 37.5% and 97.9% respectively, which was remarkably higher than those in the control group (18.8%, 20.8% and 95.5%). Their difference showed statistical significance, P<0.05 or 0.01. Bushen Huoxue Qubi Decoction had an effect in obviously improving hemarheological index in 42 days and inhibiting IL-1beta, NO, iNOS and LPO better than the control group, by the contrast of 58.6% vs 47.3%, 50.1% vs 36%, 55.1% vs 41.9% and 46.7% vs 20.6% (P<0.05 or P<0.01). The treatment group also displayed a higher SOD capability the control group (2 514.71 +/- 812.65) vs (2 013.41 +/- 781.3), (P<0.01). Both groups reported no adverse effect.
CONCLUSION:
Bushen Huoxue Qubi Decoction has a better efficacy on knee-OA than traditional treatment methods (diacereinand + celecoxib) and showed no adverse effect....(more)
Gao G, et al. Zhongguo Zhong Yao Za Zhi 2012 Feb;37(3):390-6. Chinese.
Related Products: Diacerein
- 32. Diacerein: a potential therapeutic drug for periodontal disease.
Periodontal diseases are chronic inflammatory diseases characterized by the destruction of the tooth-supporting structures. They are the most prevalent form of bone pathology in humans and act as a modifying factor of the systemic health of patients. Accumulating evidence has provided insight into mechanisms of periodontal inflammation revealing that oral pathogens induce inflammatory cascades, including a variety of cytokines produced by different cell types, which promotes host-mediated tissue destruction. Cytokine networks established in diseased periodontal tissues are extremely complex, and substances regulating immuno-inflammatory reactions and signaling pathways, in addition to traditional periodontal treatment, could potentially be targeted as an approach for prevention and treatment of periodontal diseases. Diacerein, a purified anthraquinone derivative, was derived originally from plants with profound anti-inflammatory and analgesic activities. Its wide range of biological activities have been applied and discussed for several decades; however, studies of diacerein have mainly concentrated on effects on joint-derived tissues/cells, which suggest a beneficial role in osteoarthritis treatment. Diacerein reduces association of the IL-1 receptor to form heterodimer complexes, repressing IL-1 and its related downstream events and impairing active IL-1 release due to the inhibition of the IL-1-converting enzyme (ICE). To date, there are no reports describing the therapeutic effect of diacerein for treatment of periodontitis. Given the involvement of inflammation and occurrence of tissue destruction in periodontal disease, we propose that diacerein might be a promising biological drug for periodontal disease due to its therapeutic advantages. In addition, we hypothesize that the underlying mechanisms might involve the capacity of diacerein to selectively inhibit signal transduction to affect the cytokine profiles and, consequently, produce the outcome of ameliorating disease breakdown....(more)
Huang RY, et al. Med Hypotheses 2012 Aug;79(2):165-7.
Related Products: Diacerein
- 33. Fast-dissolving and high-drug-loaded, Fatty Acid-based self-emulsifying solid dispersions of diacerein.
The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions (SDs) containing polyethylene glycol 6000 (PEG 6000), surfactant, and self-emulsifying excipient with high drug content. Ternary and self-emulsifying SDs containing high drug content were prepared and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based SDs, a remarkable enhancement of the dissolution rate was observed, even in SDs with high drug content. The presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the PXRD spectra and absence of drug melting peak in DSC spectra demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix. The utilization of self-emulsifying excipient and surfactant in PEG 6000-based SDs could be a useful tool to enhance the dissolution and bioavailability of diacerein by forming solubilizing and microemulsifying systems with high drug content. LAY ABSTRACT: The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions with high drug content. These solid dispersions were prepared and characterized by powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based solid dispersions, a remarkable enhancement of the dissolution rate was observed, even in solid dispersions with high drug content. Moreover, the presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the powder X-ray diffraction spectra and absence of drug melting peak in the spectra obtained by differential scanning calorimetry demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix....(more)
Aggarwal AK, et al. PDA J Pharm Sci Technol 2012 May-Jun;66(3):201-13.
Related Products: Diacerein
- 34. Combined effect of subchondral drilling and hyaluronic acid with/without diacerein in full-thickness articular cartilage lesion in rabbits.
The osteochondral healing potential of hyaluronic acid (HA) plus diacerein was evaluated in subchondral-drilling- (SCD-) induced fibrocartilage generation in rabbits. A full-thickness chondral defect was created along the patellar groove of both knees and then SCD was subsequently performed only in the left knee. A week later, the rabbits were allocated into 3 groups to receive weekly intra-articular (IA) injection for 5 weeks with normal saline solution (NSS) (group 1) or with HA (group 2 and group 3). Starting at the first IA injection, rabbits were also gavaged daily for 9 weeks with NSS (group 1 and group 2) or with diacerein (group 3). The animals were then sacrificed for evaluation. The newly formed tissue in SCD lesions showed significantly better histological grading scale and had higher content of type II collagen in HA-treated group compared to NSS control. In addition, adding oral diacerein to HA injection enhanced healing potential of HA....(more)
Suwannaloet W, et al. ScientificWorldJournal 2012;2012:310745.
Related Products: Diacerein
- 35. Inhibitory effect of dihydroartemisinin against phorbol ester-induced cyclooxygenase-2 expression in macrophages.
Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin isolated from the traditional Chinese herb Artemisia annua L., has recently been shown to possess antitumor activity in various cancer cells. However, the effect of anti-inflammatory potentials of DHA in murine macrophage RAW 264.7 cells has not been studied. The present study investigated the effect of COX-2 and molecular mechanisms by DHA in PMA stimulated RAW 264.7 cells. DHA dose-dependently decreased PMA-induced COX-2 expression and PGE2 production, as well as COX-2 promoter-driven luciferase activity. Additionally, DHA decreased luciferase activity of COX-2 regulation-related transcription factors including NF-κB, AP-1, C/EBP and CREB. DHA also remarkably reduced PMA-induced p65, C/EBPβ, c-jun and CREB nuclear translocation. Furthermore, DHA evidently inhibited PMA-induced phosphorylation of AKT and the MAP Kinases, such as ERK, JNK and p38. Taken together, our data indicated that DHA effectively attenuates COX-2 production via down-regulation of AKT and MAPK pathway, revealing partial molecular basis for the anti-inflammatory properties of DHA....(more)
Kim HG, et al. Food Chem Toxicol 2013 Jun;56:93-9.
Related Products: Dihydroartemisinin