- 1. Gastrodin attenuation of the inflammatory response in H9c2 cardiomyocytes involves inhibition of NF-κB and MAPKs activation via the phosphatidylinositol 3-kinase signaling.
The phenolic glucoside gastrodin, a main constituent of a Chinese traditional herbal medicine, has been known to display several biological and pharmacological properties. However, the role and precise molecular mechanisms explaining how gastrodin suppresses the inflammatory response in septic cardiac dysfunction are unknown. To study this, rat H9c2 cardiomyocytes were treated with gastrodin and/or lipopolysaccharide (LPS). Our results showed that gastrodin treatment strongly suppressed nuclear factor-κB (NF-κB) and mitogen-activated protein kinases (MAPKs) family activation and upregulation of the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6) in LPS-stimulated H9c2 cardiomyocytes. Simultaneously, gastrodin obviously upregulated the phosphatidylinositol 3-kinase (PI3-K)/Akt signaling in a dose-dependent manner. However, wortmannin, a specific PI3-K inhibitor, blocked the inhibitory effects of gastrodin on LPS-stimulated H9c2 cardiomyocytes. Furthermore, PI3-K/Akt inhibition partially abolished the inhibitory effects of gastrodin on the phosphorylation of inhibitor κB-α (IκB-α), extracellular signal-regulated kinase 1/2 (ERK1/2), c-Jun N-terminal protein kinase (JNK), and p38 mitogen-activated protein kinase (p38 MAPK), and activity of NF-κB. Here we report activation of the PI3-K/Akt signaling by gastrodin and that inhibition of this pathway reverses the inhibitory effects of gastrodin on NF-κB and MAPKs activation in H9c2 cardiomyocytes....(more)
Yang P, et al. Biochem Pharmacol 2013 Apr 15;85(8):1124-33.
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- 2. Experimental analysis on the main contents of Rhizoma gastrodiae extract and inter-transformation throughout the fermentation process of Grifola frondosa.
Gastrodin (GA), p-hydroxylbenzaldehyde (HBA), p-hydroxybenzyl alcohol (gastrodigenin, HA) and parishin not only are the major active ingredients of Rhizoma gastrodiae, but exist transformed relations from each other throughout the fermentation process of Grifola frondosa in this work. We had found that parishin (non-free gastrodin) almost could completely transformed into gastrodin (GA, free gastrodin) after R. gastrodiae alcohol extract was sterilized by moist heat (121 °C, 30 min), but before was added into submerged cultivation of G. frondosa. However, interestingly and importantly, gastrodin re-synthesized of parishin after R. gastrodiae alcohol extract's addition into submerged cultivation of G. frondosa. In addition, the reduction of p-hydroxylbenzaldehyde and p-hydroxybenzyl alcohol in G. frondosa fermentation process reconfirmed that the G. frondosa strain 51616 really could synthesize gastrodin into parishin by submerged fermentation. This paper firstly also reported G. frondosa's effects on R. gastrodiae....(more)
Wang N, et al. Arch Pharm Res 2013 Mar;36(3):314-21.
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- 3. Role of glucose transporters in the intestinal absorption of gastrodin, a highly water-soluble drug with good oral bioavailability.
Abstract Gastrodin, a sedative drug, is a highly water-soluble phenolic glucoside with poor liposolubility but exhibits good oral bioavailability. The current study aims to investigate whether glucose transporters (GLTs) are involved in the intestinal absorption of gastrodin. The intestinal absorption kinetics of gastrodin was determined using the rat everted gut sac model, the Caco-2 cell culture model and the perfused rat intestinal model. In vivo pharmacokinetic studies using diabetic rats with high GLT expression were performed. Saturable intestinal absorption of gastrodin was observed in rat everted gut sacs. The apparent permeability (Papp) of gastrodin from the apical (A) to basolateral (B) side in Caco-2 cells was two-fold higher than that from B to A. Glucose or phlorizin, a sodium-dependent GLT (SGLT) inhibitor, reduced the absorption rates of gastrodin from perfused rat intestines. In vivo pharmacokinetic studies showed that the time of maximum plasma gastrodin concentration (Tmax) was prolonged from 28 to 72 min when orally co-administered with four times higher dose of glucose. However, the Tmax of gastrodin in diabetic rats was significantly lowered to 20 min because of the high intestinal SGLT1 level. In conclusion, our findings indicate that SGLT1 can facilitate the intestinal absorption of gastrodin....(more)
Cai Z, et al. J Drug Target 2013 Mar 12.
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- 4. Gastrodin Production from p-2-Hydroxybenzyl Alcohol Through Biotransformation by Cultured Cells of Aspergillus foetidus and Penicillium cyclopium.
The objective of this work was to take advantage of the resting cells of suitable fungus as an in vitro model to prepare gastrodin from p-2-hydroxybenzyl alcohol (HBA), which mainly exists in the metabolites of the plant Gastrodia elata Blume. The one-step biotransformation of HBA into gastrodin was examined with the filamentous fungi cells of Aspergillus foetidus and Penicillium cyclopium AS 3.4513 in this study. The fundamental conditions of biotransformation were screened and compared for both fungi. P. cyclopium AS 3.4513 had better gastrodin-producing capability than A. foetidus through one-step bioconversion. The highest yield of gastrodin was 36 mg/L for A. foetidus ZU-G1 and 65 mg/L for P. cyclopium AS 3.4513 under the respective development condition during 6 days of biotransformation. The comparative results show that P. cyclopium AS 3.4513 reveals great potential to form gastrodin using HBA as the precursor. The products catalyzed by the resting cells of P. cyclopium AS 3.4513 were identified through NMR and ESI-MS. Current results can be applied not only to the chemical synthesis processes that may involve the hydroxylation reaction but also to the industrial production. The selected fungus is the potential biocatalyst for HBA glucosylation....(more)
Fan L, et al. Appl Biochem Biotechnol 2013 May;170(1):138-48.
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- 5. Synthesis and anti-influenza virus activities of a novel class of gastrodin derivatives.
A series of substituted aryl glycoside analogues of gastrodin have been identified as potential anti-influenza agents. The most potent inhibitor 1a exhibited moderate inhibitory activity against the A/Hanfang/359/95(H3N2) and A/FM/1/47(H1N1) strains of the influenza A virus (IC(50) values of 44.40 and 34.45 μM, respectively) and the oseltamivir-null B/Jifang/13/97 strain of influenza B (IC(50) value of 33.01 μM). In this article, multiple doses of compound 1a (80 mg/kg/day, oral administration) were used for the treatment of mice infected with influenza A/FM/1/47-MA (H1N1), and surprisingly we found that compound 1a significantly increased the number of survivors and prolonged the mean survival time. The preliminary studies on the mechanism of antiviral activity showed no interaction between compound 1a and the neuraminidase or the M2 protein. The novel target to overcome drug resistance combined with its good in vivo profile support compound 1a to be a new lead for further development of antiviral agents....(more)
Xue ST, et al. Molecules 2013 Mar 26;18(4):3789-805.
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- 6. Gastrodin protects apoptotic dopaminergic neurons in a toxin-induced Parkinson's disease model.
Gastrodia elata (GE) Blume is one of the most important traditional plants in Oriental countries and has been used for centuries to improve various conditions. The phenolic glucoside gastrodin is an active constituent of GE. The aim of this study was to investigate the neuroprotective role of gastrodin in 1-methyl-4-phenylpyridinium (MPP(+))/1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine- (MPTP) induced human dopaminergic SH-SY5Y cells and mouse model of Parkinson's disease (PD), respectively. Gastrodin significantly and dose dependently protected dopaminergic neurons against neurotoxicity through regulating free radicals, Bax/Bcl-2 mRNA, caspase-3, and cleaved poly(ADP-ribose) polymerase (PARP) in SH-SY5Y cells stressed with MPP(+). Gastrodin also showed neuroprotective effects in the subchronic MPTP mouse PD model by ameliorating bradykinesia and motor impairment in the pole and rotarod tests, respectively. Consistent with this finding, gastrodin prevented dopamine depletion and reduced reactive astrogliosis caused by MPTP as assessed by immunohistochemistry and immunoblotting in the substantiae nigrae and striatata of mice. Moreover, gastrodin was also effective in preventing neuronal apoptosis by attenuating antioxidant and antiapoptotic activities in these brain areas. These results strongly suggest that gastrodin has protective effects in experimental PD models and that it may be developed as a clinical candidate to ameliorate PD symptoms....(more)
Kumar H, et al. Evid Based Complement Alternat Med 2013;2013:514095.
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- 7. Gastrodin stimulates anticancer immune response and represses transplanted H22 hepatic ascitic tumor cell growth: Involvement of NF-κB signaling activation in CD4+ T cells.
Gastrodia elata Blume (G. elata) is a famous restorative food in East Asia. It can be used as an auxiliary reagent in hepatocellular carcinoma (HCC) treatment. Previous studies unveiled that G. elata exhibited immunomodulatory activities. To explore the active ingredients contributing to its immunomodulatory activities, gastrodin, vanillin, and parishin B were purified from G. elata and their anti-HCC effects were assessed in vivo. Among these compounds, only gastrodin was capable of repressing transplanted H22 ascitic hepatic tumor cell growth in vivo with low toxicity. Further investigations were designed to explore the effects of gastrodin on the immune system of tumor-bearing mice and potential molecular mechanisms underlying these effects. Our data showed that gastrodin ameliorated tumor cell transplantation-induced activation of endogenous pro-apoptotic pathway in CD4+ T cells and abnormalities in serum cytokine profiles in host animals. These events enhanced cytotoxic activities of natural killer and CD8+ T cells against H22 hepatic cancer cells. Gastrodin administration specifically upregulated mRNA levels of several nuclear factor κB (NF-κB) responsive genes in CD4+ T cells but not in CD8+ T cells. Chromatin immunoprecipitation assay showed that gastrodin increased the association of NF-κB p65 subunit to the promoter regions of IL-2 and Bcl-2 encoding genes in CD4+ T cells. Our investigations demonstrated that gastrodin is the main active ingredient contributing to the anticancer immunomodulatory properties of G. elata. Promoting NF-κB-mediated gene transcription in CD4+ T cells is implicated in its immunomodulatory activity....(more)
Shu G, et al. Toxicol Appl Pharmacol 2013 Apr 9;269(3):270-279.
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- 8. Identification of three novel polyphenolic compounds, origanine A-C, with unique skeleton from Origanum vulgare L. using the hyphenated LC-DAD-SPE-NMR/MS methods.
Identification of new compounds especially those with new skeletons from plant kingdom has long been a vital aspect for understanding phytochemistry, plant metabolisms and discovering new bioactive compounds. In this study, we identified and isolated three novel polyphenolic compounds, origanine A-C, from a well-researched plant Origanum vulgare L. using the hyphenated LC-DAD-SPE-NMR/MS methods. Based on the combined information from UV-visible, accurate mass and 2D NMR spectra together with computational calculations, we found that these compounds all had a novel skeleton of cyclohexenetetracarboxylic acids attached with some well-known bioactive moieties including 3,4-dihydroxyphenyl, 4-(β-d-glucopyranosyloxy)benzyl alcohol (gastrodin), and 3-(3,4-dihydroxyphenyl)lactic acid (danshensu) residues. These findings provided crucial information to fill the gaps in our knowledge in terms of the plant secondary metabolism. This study also indicated the necessity for further research in plant secondary metabolism for even well-studied plants and demonstrated the powerfulness of the hyphenated LC-DAD-SPE-NMR/MS methods for comprehensive analysis of plant metabolites in particular for discovering new natural compounds....(more)
Liu H, et al. J Agric Food Chem 2012 Jan 11;60(1):129-35.
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- 9. Gastrodin inhibits allodynia and hyperalgesia in painful diabetic neuropathy rats by decreasing excitability of nociceptive primary sensory neurons.
Painful diabetic neuropathy (PDN) is a common complication of diabetes mellitus and adversely affects the patients' quality of life. Evidence has accumulated that PDN is associated with hyperexcitability of peripheral nociceptive primary sensory neurons. However, the precise cellular mechanism underlying PDN remains elusive. This may result in the lacking of effective therapies for the treatment of PDN. The phenolic glucoside, gastrodin, which is a main constituent of the Chinese herbal medicine Gastrodia elata Blume, has been widely used as an anticonvulsant, sedative, and analgesic since ancient times. However, the cellular mechanisms underlying its analgesic actions are not well understood. By utilizing a combination of behavioral surveys and electrophysiological recordings, the present study investigated the role of gastrodin in an experimental rat model of STZ-induced PDN and to further explore the underlying cellular mechanisms. Intraperitoneal administration of gastrodin effectively attenuated both the mechanical allodynia and thermal hyperalgesia induced by STZ injection. Whole-cell patch clamp recordings were obtained from nociceptive, capsaicin-sensitive small diameter neurons of the intact dorsal root ganglion (DRG). Recordings from diabetic rats revealed that the abnormal hyperexcitability of neurons was greatly abolished by application of GAS. To determine which currents were involved in the antinociceptive action of gastrodin, we examined the effects of gastrodin on transient sodium currents (I(NaT)) and potassium currents in diabetic small DRG neurons. Diabetes caused a prominent enhancement of I(NaT) and a decrease of potassium currents, especially slowly inactivating potassium currents (I(AS)); these effects were completely reversed by GAS in a dose-dependent manner. Furthermore, changes in activation and inactivation kinetics of I(NaT) and total potassium current as well as I(AS) currents induced by STZ were normalized by GAS. This study provides a clear cellular basis for the peripheral analgesic action of gastrodin for the treatment of chronic pain, including PDN....(more)
Sun W, et al. PLoS One 2012;7(6):e39647.
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- 10. Genetic And Epigenetic Studies For Determining Molecular Targets Of Natural Product Anticancer Agents.
Cancer is a disease caused by a series of genetic and epigenetic alterations. Therefore, agents targeting the genetic and/or epigenetic machinery offer potential for the development of anticancer drugs. Accumulating evidence has demonstrated that some common natural products (such as epigallocatechin-3-gallate (EGCG), curcumin, genistein, sulforaphane (SFN) and resveratrol) have anticancer properties through the mechanisms of altering epigenetic processes [including DNA methylation, histone modification, chromatin remodeling, microRNA (miRNA) regulation] and targeting cancer stem cells (CSCs). These bioactive compounds are able to revert epigenetic alterations in a variety of cancers in vitro and in vivo. They exert the anticancer effects by targeting various signaling pathways related to the initiation, progression and metastasis of cancer. It appears that natural products hold great promise for cancer prevention and treatment by altering various epigenetic modifications. This review aims to discuss our current understanding of genetic and epigenetic targets of natural products and the effects of some common natural products on cancer chemoprevention and treatment....(more)
Wang Y, et al. Curr Cancer Drug Targets 2013 Apr 17.
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- 11. DNA Methylation and Histone Modifications of Wnt Genes by Genistein During Colon Cancer Development.
The current study aims to elucidate the epigenetic mechanisms by which genistein maintains a normal level of WNT genes during colon cancer development. We have reported that soy protein isolate (SPI) and genistein (GEN) repressed WNT signaling, correlating with the reduction of preneoplastic lesions in rat colon. We hypothesized that SPI and GEN induced epigenetic modifications on Sfrp2, Sfrp5, and Wnt5a genes, suppressing their gene expression induced by azoxymethane (AOM), a chemical carcinogen, to the similar level as that of pre-AOM period. We identified that in the post-AOM period the acetylation of histone H3 (H3Ac) was downregulated by SPI and GEN at the promoter region of Sfrp2, Sfrp5, and Wnt5a, which was in parallel with the reduced binding of RNA Polymerase II. Nuclear level of histone deacetylase 3 (HDAC3) was enhanced by SPI and GEN. The diets suppressed the trimethylation of histone H3 Lysine 9 (H3K9Me3) and the phosphorylation of histone H3 Serine 10 (H3S10P). Methylation of the specific region of Sfrp2, Sfrp5, and Wnt5a genes was increased by SPI and GEN, which was inversely correlated with the reduction of gene expression. Bisulfite sequencing further confirmed that dietary genistein induced DNA methylation at CpG island of the promoter region of Sfrp5. Importantly, this region includes a fragment that had decreased acetylation of histone H3. Here we present a potential epigenetic mechanism by which dietary genistein controls the responses of WNT genes during carcinogen induction, which involves DNA methylation, histone modifications, and their interactions at the regulatory region of gene....(more)
Zhang Y, et al. Carcinogenesis 2013 Apr 18.
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- 12. Biotransformation and recovery of the isoflavones genistein and daidzein from industrial antibiotic fermentations.
The objective of this study was to follow the metabolic fate of isoflavone glucosides from the soybean meal in a model industrial fermentation to determine if commercially useful isoflavones could be harvested as coproducts from the spent broth at the end of the fermentation. The isoflavone aglycones, genistein, and daidzein together make up 0.1-0.2 % of the soybean meal by weight but serve no known function in the manufacturing process. After feeding genistein to washed cells of the erythromycin-producing organism, Saccharopolyspora erythraea, the first biotransformation product (Gbp1) was determined by X-ray crystallography to be genistein-7-O-α-rhamnoside (rhamnosylgenistein). Subsequent feeding of rhamnosylgenistein to growing cells of Saccharopolyspora erythraea led to the production of a second biotransformation product, Gbp2. Chromatographic evidence suggested that Gbp2 accumulated in the spent broth of the erythromycin fermentation. When the spent broth was hydrolyzed with acid or industrial enzyme preparations, the isoflavone biotransformation products were returned back to their parental forms, genistein and daidzein, which were then recovered as coproducts. Desirable features of this method are that it does not require modification of the erythromycin manufacturing process or genetic engineering of the producing organism to be put into practice. A preliminary investigation of five additional antibiotic fermentations of industrial importance also found isoflavone coproduct potential....(more)
Weber JM, et al. Appl Microbiol Biotechnol 2013 Apr 19.
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- 13. Individual And Combined Effects Of Genistein And Hesperidin Supplementation On Meat Quality In Meat-Type Broiler Chickens.
BACKGROUND:
There is a growing interest to improve production and meat quality of farm animals through supplementation of phytochemical (e.g., flavonoids) rich plants and/or their extracts. This study was conducted to analyze the supplemental effects of two purified flavonoids (genistein and hesperidin) individually and in combination on oxidative status, sensory score and quality of breast meat in meat-type broiler chickens.
RESULTS:
A significant raise (P < 0.05) was observed for meat color (L<sup>*</sup> score) and pH in 20 mg kg<sup>-1</sup> genistein and hesperidin (GH20) supplemented group. Water holding capacity (WHC) was also improved significantly (P < 0.01) for all genistein and hesperidin treated groups, while sensorial quality of breast meat remained unaffected. Lipid oxidation of breast meat was dropped significantly (P < 0.01) at 0 and 15 d of refrigeration in a dose-dependent manner for all supplemented groups. While, few treated groups showed improved (P < 0.05) body weight, feed: gain and hot carcass weight.
CONCLUSION:
Genistein and hesperidin supplementation to broilers improved the meat quality in a dose-dependent fashion with pronounced effects of combinatorial treatment. The results indicated that purified flavonoids (genistein and hesperidin) could potentially use as feed additive in broiler production to promote quality of meat.
This article is protected by copyright. All rights reserved....(more)
Kamboh AA, et al. J Sci Food Agric 2013 Apr 19.
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- 14. Functional Characterization of a Flavonoid Glycosyltransferase Gene from Withania somnifera (Ashwagandha).
Glycosylation of flavonoids is mediated by family 1 uridine diphosphate (UDP)-dependent glycosyltransferases (UGTs). Until date, there are few reports on functionally characterized flavonoid glycosyltransferases from Withania somnifera. In this study, we cloned the glycosyltransferase gene from W. somnifera (UGT73A16) showing 85-92 % homology with UGTs from other plants. UGT73A16 was expressed as a His6-tagged fusion protein in Escherichia coli. Several compounds, including flavonoids, were screened as potential substrates for UGT73A16. HPLC analysis and hypsochromic shift indicated that UGT73A16 transfers a glucose molecule to several different flavonoids. Based on kinetic parameters, UGT73A16 shows more catalytic efficiency towards naringenin. Here, we explored UGT73A16 of W. somnifera as whole cell catalyst in E. coli. We used flavonoids (genistein, apigenin, kaempferol, naringenin, biochanin A, and daidzein) as substrates for this study. More than 95 % of the glucoside products were released into the medium, facilitating their isolation. Glycosylation of substrates occurred on the 7- and 3-hydroxyl group of the aglycone. UGT73A16 also displayed regiospecific glucosyl transfer activity towards 3-hydroxy flavone compound, which is the backbone of all flavonols and also for a chemically synthesized compound, not found naturally. The present study generates essential knowledge and molecular as well as biochemical tools that allow the verification of UGT73A16 in glycosylation....(more)
Singh S, et al. Appl Biochem Biotechnol 2013 Apr 23.
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- 15. Role of protein tyrosine kinase in the effect of IP6 on IL-8 secretion in intestinal epithelial cells.
Phytic acid (IP6) is a major fiber-associated component of a diet physiologically present in human intestines. Studies showed that this phytochemical can modulate immune functions of intestinal epithelium through regulation of proinflammatory cytokines secretion but mechanisms underlying these cellular response to IP6 have weakly been examined, as yet. The aim of this study was to determine the role of protein tyrosine kinase (PTK) in secretion of IL-8, a central proinflammatory cytokine, by unstimulated and IL-1beta-stimulated intestinal epithelial cells Caco-2 treated with IP6 (1 and 2.5 mM). To study the involvement of PTK signal pathway in IL-8 secretion, inhibitors of phosphotyrosine phosphatase (sodium orthovanadate, OV) and tyrosine kinase (genistein, GEN) were incubated with Caco-2 cells prior to IP6 treatment. IP6 had suppressive effect on basal and IL-1beta-stimulated IL-8 secretion by cells. The effect of OV on IL-8 release by cells treated with IP6 was different under constitutive and stimulated conditions. Secretion of IL-8 was significantly down-regulated in cells with GEN and GEN plus IP6 treatment. In addition, total PTK activity in both unstimulated and IL-1beta stimulated cells was determined in the presence of IP6. The results suggest that physiological intestinal concentrations of IP6 may have an inhibitory effect on IL-8 secretion by Caco-2 cells and one of the mechanisms of its action is the inhibition of PTK signaling cascade. The study revealed for the first time that PTKs could be one of the molecular targets for IP6 effects in the intestinal epithelial cells....(more)
Wawszczyk J, et al. Acta Pol Pharm 2013 Jan-Feb;70(1):79-86.
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- 16. Influence of genistein on c-Jun, c-Fos and Fos-B of AP-1 subunits expression in skin keratinocytes, fibroblasts and keloid fibroblasts cultured in vitro.
Genistein is a well known flavonoid that exhibits antioxidant, antiproliferative, proapoptotic, antiangiogenic, as well as estrogenic and anti-estrogenic activity. Extensive studies in the field of dermatology and cosmetology in recent years revealed that genistein is a promising anti-aging, anti-photoaging and anti-carcinogenic agent for skin care. Essential role in skin prematuring aging and carcinogenesis play AP-1 transcription factors that are activated, among others, by environmental factors: ultraviolet light and free radicals. Genistein is a potent antioxidant and inhibitor of AP-1 activity. The aim of the study was to investigate genistein as a potential regulator of C-JUN, C-FOS and FOS-B of AP-1 subunits expression in skin keratinocytes, fibroblasts and keloid fibroblasts cultured in vitro. In presented study, genistein modulated C-JUN expression in epidermal keratinocytes and dermal fibroblasts cultured in vitro. The expression of C-JUN was higher in keratinocytes treated with 37 and 370 microM genistein. In dermal fibroblasts genistein regulated C-JUN expression in dose-dependent manner. The expression of C-JUN was lower in fibroblasts treated with 370 microM genistein and higher in fibroblasts treated with 37 microM genistein. Genistein in 370 microM concentration inhibited C-FOS expression in fibroblasts, whereas in 370 and 37 microM concentration genistein inhibited FOS-B expression in keratinocytes. Furthermore, genistein was able to modulate C-JUN and C-FOS genes expression in keloid fibroblasts cultured in vitro. In these cells, transcriptional activity of C-JUN and C-FOS expression depended on employed concentration of genistein. The expression of C-JUN and C-FOS was higher in keloid fibroblasts treated with 370 microM genistein and lower in keloid fibroblasts treated with 37 microM genistein....(more)
Jurzak M, et al. Acta Pol Pharm 2013 Mar-Apr;70(2):205-13.
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- 17. RESOLUTION OF THE DIRECT INTERACTION AND INHIBITION OF THE HUMAN GLUT1 HEXOSE TRANSPORTER BY RESVERATROL FROM ITS EFFECT ON GLUCOSE ACCUMULATION.
Resveratrol acts as a chemopreventive agent for cancer and as a potential anti-obesity and anti-diabetic compound, by leading to reduced body fat and improved glucose homeostasis. The exact mechanisms involved in improving hyperglycemic state are not known, but most of glucose uptake into mammalian cells is facilitated by the GLUT hexose transporters. Resveratrol is structurally similar to isoflavones such as genistein, which inhibit the glucose uptake facilitated by the GLUT1 hexose transporter. Here we examined the direct effects of resveratrol on glucose uptake and accumulation in HL-60 and U937 leukemic cell lines, which express mainly GLUT1, under conditions that discriminate transport from the intracellular substrate phosphorylation/ accumulation. Resveratrol blocks GLUT1-mediated hexose uptake and thereby affects substrate accumulation on these cells. Consequently, we characterized the mechanism involved in inhibition of glucose uptake in human red cells. Resveratrol inhibits glucose exit in human red cells, and the displacement of previously bound cytochalasin B revealed the direct interaction of resveratrol with GLUT1. Resveratrol behaves as a competitive blocker of glucose uptake under zero-trans exit and exchange kinetic assays, but it becomes a mixed noncompetitive blocker when zero-trans entry transport was assayed, suggesting that the binding site for resveratrol lies on the endofacial face of the transporter. We propose that resveratrol interacts directly with the human GLUT1 hexose transporter by binding to an endofacial site and that this interaction inhibits the transport of hexoses across the plasma membrane. This inhibition is distinct from the effect of resveratrol on the intracellular phosphorylation/ accumulation of glucose....(more)
Salas M, et al. Am J Physiol Cell Physiol 2013 Apr 24.
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- 18. Estrogen Receptor-Mediated Effects of Isoflavone Supplementation Were Not Observed in Whole-Genome Gene Expression Profiles of Peripheral Blood Mononuclear Cells in Postmenopausal, Equol-Producing Women.
Isoflavones (genistein, daidzein, and glycitein) are suggested to have benefits as well as risks for human health. Approximately one-third of the Western population is able to metabolize daidzein into the more potent metabolite equol. Having little endogenous estradiol, equol-producing postmenopausal women who use isoflavone supplements to relieve their menopausal symptoms could potentially be at high risk of adverse effects of isoflavone supplementation. The current trial aimed to study the effects of intake of an isoflavone supplement rich in daidzein compared with placebo on whole-genome gene expression profiles of peripheral blood mononuclear cells (PBMCs) in equol-producing, postmenopausal women. Thirty participants received an isoflavone supplement or a placebo for 8 wk each in a double-blind, randomized cross-over design. The isoflavone supplement was rich in daidzein (60%) and provided 94 mg isoflavones (aglycone equivalents) daily. Gene expression in PBMCs was significantly changed (P < 0.05) in 357 genes after the isoflavone intervention compared with placebo. Gene set enrichment analysis revealed downregulated clusters of gene sets involved in inflammation, oxidative phosphorylation, and cell cycle. The expression of estrogen receptor (ER) target genes and gene sets related to ER signaling were not significantly altered, which may be explained by the low ERα and ERβ expression in PBMCs. The observed downregulated gene sets point toward potential beneficial effects of isoflavone supplementation with respect to prevention of cancer and cardiovascular disease. However, whether ER-related effects of isoflavones are beneficial or harmful should be studied in tissues that express ERs....(more)
van der Velpen V, et al. J Nutr 2013 Apr 24.
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- 19. Bioavailability enhancers of herbal origin: An overview.
Recently, the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines. However, many herbal drugs and herbal extracts despite of their impressive <i>in-vitro</i> findings demonstrates less or negligible <i>in-vivo</i> activity due to their poor lipid solubility or improper molecular size, resulting in poor absorption and hence poor bioavailability. Nowadays with the advancement in the technology, novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems. For last one decade many novel carriers such as liposomes, microspheres, nanoparticles, transferosomes, ethosomes, lipid based systems <i>etc.</i> have been reported for successful modified delivery of various herbal drugs. Many herbal compounds including quercetin, genistein, naringin, sinomenine, piperine, glycyrrhizin and nitrile glycoside have demonstrated capability to enhance the bioavailability. The objective of this review is to summarize various available novel drug delivery technologies which have been developed for delivery of drugs (herbal), and to achieve better therapeutic response. An attempt has also been made to compile a profile on bioavailability enhancers of herbal origin with the mechanism of action (wherever reported) and studies on improvement in drug bioavailability, exhibited particularly by natural compounds....(more)
Kesarwani K, et al. Asian Pac J Trop Biomed 2013 Apr;3(4):253-266.
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- 20. Distribution of isoflavones and coumestrol in neglected tropical and subtropical legumes.
BACKGROUND:
Isoflavones and coumestrol from dietary legumes are plant constituents showing multiple beneficial effects on humans. Owing to their ability to bind with mammalian estrogenic receptors and thereby intervention in several kinds of hormone-related cancers, they have received much attention. Soybean (Glycine max) is currently the major source of isoflavonoids in human diet. However, dozens of tropical and subtropical leguminous species remain unexplored for their isoflavonoids content.
RESULTS:
We have analyzed 55 extracts from 41 tropical and subtropical legume species used either in human or animal diet by high-performance liquid chromatography for the content of soy isoflavones, biochanin A, daidzein, daidzin, formononetin, genistein, genistin, sissotrin, ononin and the coumestan coumestrol. Genistein and biochanin A were the most abundant compounds. The highest content of genistein was found in aerial parts of Andira macrothyrsa, seeds of Pachyrhizus tuberosus and aerial parts of Calopogonium mucunoides (598, 250 and 184 µg g(-1), respectively) and biochanin A in aerial parts of Cratylia argentea, C. mucunoides and flowers of A. macrothyrsa (76, 53 and 40 µg g(-1), respectively).
CONCLUSION:
None of the samples tested was richer overall source of soy isoflavones and coumestrol than soybean; nevertheless several species (C. mucunoides or A. macrothyrsa) may serve as a promising source of individual compounds.
Copyright © 2012 Society of Chemical Industry....(more)
Leuner O, et al. J Sci Food Agric 2013 Feb;93(3):575-9.
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- 21. Genistein and dicarboximide fungicides in infant formulae from the EU market.
A method based on ultrasonic extraction and purification by solid phase extraction followed by LC-MS/MS and GC-MS analysis was developed for the determination of genistein, genistin, iprodione, vinclozolin and procymidone in infant powdered formulas. The method was tested for different formulations: milk, soy and hypoallergenic, and was applied to European pooled samples. Spike recoveries ranged from 53.1% to 91.5% and the relative standard deviation values for repeatability ranged from 9.6% to 17.7%, except for iprodione in milk formula (22.3%). None of the fungicides were found in the European pooled formulae, while genistein was found at 9.7μg/g in soy formula and the concentration of genistin, its β-glycosylated form, was respectively 31.4ng/g and 476ng/g in milk and soy formula....(more)
Maggioni S, et al. Food Chem 2013 Jan 1;136(1):116-9.
Related Products: Genistin
- 22. Characterization and application of an acidophilic and thermostable β-glucosidase from Thermofilum pendens.
The gene encoding a β-glucosidase from the archaeon Thermofilum pendens (Tpbgl) was cloned and expressed in Escherichia coli. The purified recombinant enzyme had a molecular mass of 77.8 kDa and released glucose or mannose from p-nitrophenyl-β-d-glucopyranoside (pNPG), cellobiose, mannobiose, and genistin. Peak Tpbgl activity was detected at 90°C, and 50% activity remained after incubation for 60 min at 95°C. The optimal pH for pNPG hydrolysis was 3.5. When the enzyme was incubated with pNPG in the presence of ethanol and propanol, the glucose moiety was transferred to acceptor alcohols. Tpbgl is the archaeal β-glucosidase from glucoside hydrolase family 3 and found to be most heat stable under extremely acidic conditions (pH 3.5). The kinetic parameters revealed that Tpbgl had the highest catalytic efficiency toward pNPG (kcat/Km = 3.05) with strong substrate affinity for such natural substrates as cellobiose (Km = 0.149) and mannobiose (Km = 0.147). Genistin solubilized in 10-40% DMSO was hydrolyzed to genistein with nearly 99% conversion, indicating that high concentrations of the water-insoluble isoflavone glycoside can be treated by the enzyme. Our results indicate that Tpbgl has great potential in cellulose saccharification and the glucoside hydrolysis of natural compounds....(more)
Li D, et al. J Biosci Bioeng 2013 May;115(5):490-6.
Related Products: Genistin
- 23. The characteristics of genistin-induced inhibitory effects on intestinal motility.
Genistin belongs to isoflavones. Based on the facts that genistin exerts inhibitory effects on the contractility of vascular smooth muscle,the present study was designed to characterize the effects of genistin on intestinal contractility and evaluate its potential clinical implication. Ex vivo [isolated jejunal segment (IJS) of rat], in vitro, and in vivo assays were used in the study. The results indicated that genistin (5-80 μmol/L) inhibited the contraction of IJS in a dose-dependent manner and inhibited the increased-contractility of IJS induced by acetylcholine (ACh), histamine, high Ca(2+), and erythromycin, respectively. The inhibitory effects of genistin were correlated with the stimulation of alpha adrenergic and beta adrenergic receptors since these inhibitory effects were significantly blocked in the presence of phentolamine and propranolol respectively. No further inhibitory effects of genistin were observed in the presence of verapamil or in Ca(2+)-free condition, indicating genistin-induced inhibitory effects are Ca(2+)-dependent. Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects. The study suggests the potential clinical implications of genistin in relieving intestinal hypercontractility....(more)
Xiong YJ, et al. Arch Pharm Res 2013 Mar;36(3):345-52.
Related Products: Genistin
- 24. Genista sessilifolia DC. extracts induce apoptosis across a range of cancer cell lines.
OBJECTIVES:
Restorative properties of medicinal plants such as Genista sessilifolia DC. have often been suggested to occur, in epidemiological studies. However, full characterization of effective principles responsible for this action has never previously been performed. Here, we have characterized G. sessilifolia's anti-cancer effects and identified the chemical components involved in this anti-tumour action.
MATERIALS AND METHODS:
Cell cycle, apoptosis, necrosis, differentiation analyses, high-performance liquid chromatography, western blotting, RNA extraction, real-time PCR and primers have all been observed/used in the study.
RESULTS:
We report that G. sessilifolia methanol extract has anti-cancer activity on solid and haematological cancer cells. G. sessilifolia extract's anti-proliferative action is closely bound to induction of apoptosis, whereas differentiation is only weakly modulated. Analysis of G. sessilifolia extract, by high-performance liquid chromatography, identifies fraction 18-22 as the pertinent component for induction of apoptosis, whereas fractions 11-13 and 27-30 both seem to contribute to differentiation. G. sessilifolia extract induces apoptosis mediated by caspase activation and p21, Rb, p53, Bcl2-associated agonist of cell death (BAD), tumour necrosis factor receptor super-family, member 10 (TRAIL) overexpression and death receptor 5 (DR5). Accordingly, fraction 18-22 inducing apoptosis was able to induce TRAIL.
CONCLUSIONS:
Our results indicate that G. sessilifolia extract and its fraction 18-22 containing genistin and isoprunetin, were able to induce anti-cancer effects supporting the hypothesis of a pro-apoptotic intrinsic content of this natural medicinal plant.
© 2013 Blackwell Publishing Ltd....(more)
Bontempo P, et al. Cell Prolif 2013 Apr;46(2):183-92.
Related Products: Genistin
- 25. Evaluation of the mutagenicity and antimutagenicity of soy phytoestrogens using micronucleus and comet assays of the peripheral blood of mice.
Studies show that soy imparts many favorable properties in the human body, including the prevention of chronic diseases such as osteoporosis, heart disease, cancer, and diabetes. Soy is rich in isoflavones, and it is a candidate for the chemoprevention of diseases owing to its low toxicity. In this study, a soy phytoestrogen (with high levels of the isoflavones genistin and daidzein) was tested in mice to investigate its mutagenicity and genotoxicity using micronucleus and comet assays of mouse peripheral blood. Phytoestrogen (0.083, 0.83 and 8.3 mg/kg body weight) was evaluated with and without the chemotherapeutic agent cyclophosphamide. For the micronucleus assay, blood was collected before treatment and after 24 and 48 h. For the comet assay, blood was collected only after 24 h. Phytoestrogen was not mutagenic and reduced cyclophosphamide-induced DNA damage. The results from the comet assay revealed a reduction of DNA damage; however, phytoestrogen did induce genotoxic damage during the 24-h treatment. This genotoxic damage could have been repaired and was therefore not identified in the micronucleus assay, which detects mutations. The results suggested that the reduction of DNA damage observed in associated treatments could also reduce the side effects of chemotherapy. Moreover, they suggested that phytoestrogen might be a candidate of interest for the chemoprevention of cancer because it protects against DNA damage....(more)
Niwa AM, et al. Genet Mol Res 2013 Feb 27;12(1):519-27.
Related Products: Genistin
- 26. Qualitative and quantitative analysis of the major constituents in Chinese medicinal preparation Dan-Lou tablet by ultra high performance liquid chromatography/diode-array detector/quadrupole time-of-flight tandem mass spectrometry.
A rapid ultra high performance liquid chromatography/diode-array detector/quadrupole time-of-flight tandem mass spectrometry (UPLC-DAD-QTOF) method and a ultra high performance liquid chromatography coupled with diode-array detector (UPLC-DAD) method were developed for qualitative and quantitative analyses of the major chemical constituents in Dan-Lou tablet. Sixty-eight compounds including flavonoids, phenolic acids, tanshinones, protostane triterpenoids, lactones, and paeoniflorins were unambiguously or tentatively identified by comparing their retention times and accurate mass measurement in 40min with references or literature data. Among them, 19 compounds: gallic acid, danshensu, 5-hydroxymethyl-2-furaldehyde, 3'-hydroxy puerarin, puerarin, 3'-methoxy puerarin, mirificin, daidzin, paeoniflorin, calycosin-7-O-β-D-glucoside, naringin, genistin, rosmarinic acid, salvianolic acid B, salvianolic acid A, formononetin, calycosin, cryptotanshinone and tanshinone IIA were further quantified in 30min as marker substances. It was found that the calibration curves for all analytes showed good linearity (R(2)>0.9997) within the test ranges. The overall limits of detection (LODs) and limits of quantification (LOQs) were 0.0073-0.34μg/mL and 0.022-1.04μg/mL, respectively. The relative standard deviations (RSDs) for intra- and inter-day precisions were below 1.90% and 2.85%, respectively. The results of repeatability were less than 2.74%. The sample was stable for at least 48h. The mean recovery rates ranged from 95.5% to 105% with the relative standard deviations (RSDs) less than 2.96%. The results showed that the developed quantitative method was linear, sensitive, and precise for quality control of Dan-Lou tablet....(more)
Dong J, et al. J Pharm Biomed Anal 2013 Jun;80:50-62.
Related Products: Genistin
- 27. Determination of phenolic compounds level variations in soybean (Glycine max Merr.) sprouts infected by anthracnose (Colletotrichum gloeosporioides).
BACKGROUND:
Soybean sprouts (Kongnamool) are one of the most popular and nutritive traditional vegetables in East Asia. Anthracnose caused by Colletotrichum gloeosporioides is one of the most serious diseases of soybean sprouts. In order to obtain basic information for breeding and/or selecting soybean genotypes with increased natural defense against anthracnose, phenolic compounds were profiled for healthy and infected soybean (Glycine max Merr.) sprouts via high performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS).
RESULTS:
Tryptophan and eight phenolic compounds (daidzin, genistin, malonyldaidzin, malonylgenistin, daidzein, glycitein, genistein, and coumestrol) were determined from the healthy and inoculated sprouts. Total identified phenolic content was 40.02 ± 0.03 mg kg<sup>-1</sup> , 99.4% of which was isoflavones.
CONCLUSION:
The monitoring suggested that de novo induced glycitein appeared to act as a phytoalexin in the defense mechanism of the soybean sprouts against C. gloeosporioides, and constitutively formed seven phenolic components functioned as phytoanticipins in the diseased soybean sprouts.
Copyright © 2013 Society of Chemical Industry....(more)
Lee JH, et al. J Sci Food Agric 2013 Mar 22.
Related Products: Genistin
- 28. Enrichment of two isoflavone aglycones in black soymilk by using spent coffee grounds as an immobiliser for β-glucosidase.
Spent coffee grounds, discarded as environmental pollutants, were adopted as enzyme immobilisation solid carriers instead of commercialised solid supports to establish an economical catalytic system. β-Glucosidase was covalently immobilised onto spent coffee grounds for the conversion of isoflavone glycosides into their aglycones in black soymilk. Optimum conditions were determined to be 40°C and pH 6 using 4-nitrophenyl β-d-glucuronide as an indicator. Operational reusability was confirmed for more than 30 batch reactions and the storage stability was capable of sustaining its highest catalytic activity for 20days. The kinetic parameters including rate constant (K), time (τ50) in which 50% of isoflavone deglycosylation was reached, and time (τcomplete) required to achieve complete isoflavone deglycosylation, were0.16±0.02min(-1), 4.54±0.32min, 60min for daidzin and 0.16±0.02min(-1), 2.28±0.11min, 60min for genistin, respectively. The total aglycone content in black soymilk was enriched by 67.14±0.60% in the enzymatic treatment of 60min duration....(more)
Chen KI, et al. Food Chem 2013 Aug 15;139(1-4):79-85.
Related Products: Genistin
- 29. Anti-inflammatory and antioxidant activities of constituents isolated from Pueraria lobata roots.
In order to evaluate the anti-inflammatory and antioxidant activities of Pueraria lobata roots and its active components, in vitro inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) protein expression, and tert-butylhydroperoxide (t-BHP)-induced reactive oxygen species (ROS) generation in RAW 264.7 cells, as well as in vitro scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH), peroxynitrite (ONOO(-)), nitric oxide (NO·), superoxide anion (·O(2)(-)) and total ROS, and inhibitory activities against ONOO(-)-mediated tyrosine nitration, were determined. Repeated column chromatography was performed to isolate four known compounds from the anti-inflammatory and antioxidant EtOAc fraction: daidzein; genistein; puerarin; (+)-puerarol B-2-O-glucopyranoside; four known compounds from the anti-inflammatory n-hexane fraction: lupenone; lupeol; puerarol; coumestrol; seven known compounds from the antioxidant n-BuOH fraction: allantoin; 3'-hydroxypuerarin; daidzein 8-C-apiosyl-(1→6)-glucoside; puerarin; genistin; 3'-methoxypuerarin; daidzin. Among these compounds, lupenone and lupeol reduced NO production, as well as iNOS and COX-2 protein levels in LPS-stimulated RAW 264.7 cells. Furthermore, lupeol showed significant inhibitory activity against intracellular ROS generation by t-BHP. Meanwhile, 3'-hydroxypuerarin showed marked ONOO(-), NO·, total ROS scavenging activities, and weak ·O(2)(-) scavenging activity, while 3'-methoxypuerarin showed ONOO(-) scavenging activity and weak NO· and O(2)(-) scavenging activities, suggesting that existence of the 3'-hydroxyl group in puerarin plays an important role in the scavenging of ONOO(-), NO·, and total ROS, as well as inhibiting the ONOO(-)-mediated tyrosine nitration mechanism. These results indicate that P. lobata roots and its constituents may be a useful therapeutic and preventive approach to various inflammatory diseases and oxidative stress-related disease....(more)
Jin SE, et al. Arch Pharm Res 2012 May;35(5):823-37.
Related Products: Genistin
- 30. Bone Marrow Tinctures for Cardiovascular Disease: Lost in Translation.
Warburg's Tincture was a blockbuster anti-fever remedy in the 19th century. It was invented by Dr. Carl Warburg to treat a broad range of fevers, achieving widespread usage in the British Empire, the Austrian Empire and also in the United States. Many renowned physicians prescribed it, but others were envious of Warburg's success and not too happy about the fact that he kept its formulation secret. In 1870, Warburg finally revealed the secret ingredients and gave permission to Professor W. C. Maclean, one of the most ardent supporters of the remedy, to publish them in the Lancet<sup>1</sup>: The elusive tincture contained many components, such as Rhubarb root, Angelica seeds, gentian root, Saffron, Fennel seeds, Myrrh, Camphor among others and, unsurprisingly, quinine. In his letter to the Lancet, Maclean effusively praises the tincture, but he also emphasizes that its healing power was not just due to the known antipyretic quinine, but that it was the unique composition of various extracts that was responsible for its efficacy. In the 21st century, few physicians would prescribe such tinctures, which are plant or animal extracts. The idea of using such extracts which contain a large array of substances, some active and some inactive, goes against the tenets of modern medical practice, in which we strive to define and titrate every single therapeutic agent to optimize efficacy. There is, however, one notable exception to this practice in an emerging area of cardiovascular medicine: the use of bone marrow mononuclear cells....(more)
Rehman J. Circulation 2013 Apr 17.
Related Products: Gentian Root Extract
- 31. Antiviral activity in vitro of two preparations of the herbal medicinal product Sinupret® against viruses causing respiratory infections.
Sinupret(®), a herbal medicinal product made from Gentian root, Primula flower, Elder flower, Sorrel herb, and Verbena herb is frequently used in the treatment of acute and chronic rhinosinusitis and respiratory viral infections such as common cold. To date little is known about its potential antiviral activity. Therefore experiments have been performed to measure the antiviral activity of Sinupret(®) oral drops (hereinafter referred to as "oral drops") and Sinupret(®) dry extract (hereinafter referred to as "dry extract"), in vitro against a broad panel of both enveloped and non-enveloped human pathogenic RNA and DNA viruses known to cause infections of the upper respiratory tract: influenza A, Chile 1/83 (H1N1) virus (FluA), Porcine Influenza A/California/07/2009 (H1N1) virus (pFluA), parainfluenza type 3 virus (Para 3), respiratory syncytial virus, strain Long (RSV), human rhinovirus B subtype 14 (HRV 14), coxsackievirus subtype A9 (CA9), and adenovirus C subtype 5 (Adeno 5). Concentration-dependent antiviral activity (EC(50) between 13.8 and 124.8 μg/ml) of Sinupret(®) was observed against RNA as well as DNA viruses independent of a viral envelope. Remarkable antiviral activity was shown against Adeno 5, HRV 14 and RSV in which dry extract was significantly superior to oral drops. This could be ascertained with different assays as plaque-reduction assays in plaque forming units (PFU), the analyses of a cytopathogenic effect (CPE) and with enzyme immunoassays (ELISA) to determine the amount of newly synthesised virus. Our results demonstrate that Sinupret(®) shows a broad spectrum of antiviral activity in vitro against viruses commonly known to cause respiratory infections.
Copyright © 2011 Elsevier GmbH. All rights reserved....(more)
Glatthaar-Saalmüller B, et al. Phytomedicine 2011 Dec 15;19(1):1-7.
Related Products: Gentian Root Extract
- 32. The effect of a herbal combination of primrose, gentian root, vervain, elder flowers, and sorrel on olfactory function in patients with a sinonasal olfactory dysfunction.
Olfactory dysfunction is a common symptom in patients with inflammation of the nasal mucosa. Among numerous drugs, so far only the use of steroids has been shown to have a positive effect on olfactory function. Therefore the aim of the present study was to investigate whether patients with sinonasal disease would benefit in terms of olfactory function from oral treatment with a herbal drug (combination of primrose, gentian root, vervain, elder flowers, and sorrel: Sinupret(r)) which is commonly used in sinusitis. Olfactory function was tested using a standardised olfactory test kit (`sniffin` sticks`). The drug was applied in a double-blind fashion: after an initial therapy of 7 days of oral prednisolone for all participants with a sinonasal olfactory disease, participants were divided into a placebo- and a verum-group; tests were performed before and after treatment over a 2 months period. Statistical analysis did not reveal any major differences in olfactory function in relation to treatment. Considering that its benefit for the inflammatory component of sinusitis has been shown, the herbal drug may exhibit positive effects on olfactory function in a different setting, e.g., when applied without preceding administration of prednisolone, or when used in patients with certain degrees of rhinosinusitis....(more)
Reden J, et al. Rhinology 2011 Aug;49(3):342-6.
Related Products: Gentian Root Extract
- 33. [Optimal technique of wine-processed gentian].
OBJECTIVE:
To optimize technique of wine-processed gentian (root of Gentiana manshurica, G. scabra, G. triflora and G. rigescens.
METHOD:
Orthogonal design L9 (3(4)) was used to select the best processing technical parameters by yields of the water extracts and amounts of gentiopicroside in the processing products.
RESULT:
The optimal procedure was suggested as follows: Gentiana Radix was cut into 5-10 millimetres' long, added one-fifth amounts of wine by gentian's weight, moistened for two hours, and then dried by slow fire.
CONCLUSION:
The amounts of gentiopicroside in wine-processed gentian were closely related to the types and amounts of wine, moistened time and dried method....(more)
Wang CJ, et al. Zhongguo Zhong Yao Za Zhi 2008 Oct;33(20):2335-8. Chinese.
Related Products: Gentian Root Extract
- 34. Phenylacetonitrile from the giant knotweed, Fallopia sachalinensis, infested by the Japanese beetle, Popillia japonica, is induced by exogenous methyl jasmonate.
Phenylacetonitrile, (E)-β-ocimene, linalool, (E)-4,8-dimethyl-1,3,7-nonatriene and (E,E)-α-farnesene were identified as Japanese beetle, Popillia japonica, feeding-induced volatiles from the leaves of the giant knotweed, Fallopia sachalinensis, but not by mechanical damage. Volatile emission was also induced by treatment with a cellular signaling molecule, methyl jasmonate. These results suggest that volatiles will be synthesized de novo by a biotic elicitor from P. japonica oral secretion....(more)
Noge K, et al. Molecules 2011 Aug 3;16(8):6481-8.
Related Products: Giant Knotweed Extract
- 35. Blockade of Her2/neu binding to Hsp90 by emodin azide methyl anthraquinone derivative induces proteasomal degradation of Her2/neu.
Overexpression of HER2/neu, a transmembrane tyrosine kinase acting as a coreceptor for other EGFR family members, is well-known to be associated with a poor prognosis in cancer. In the present study, we observed that emodin AMAD, a novel emodin azide methyl anthraquinone derivative, extracted from nature's giant knotweed rhizome of traditional Chinese herbs, potently decreased Her2/neu protein in dose- and time-dependent manners and also inhibited the downstream MAPK and PI3K-Akt signaling pathway. Intriguingly, reverse transcription-PCR and protein turnover assay revealed that the decrease of Her2/neu was independent of mRNA level but primarily owing to its protein stability. Meanwhile, proteasome inhibitor MG132 but not lysosome inhibitor chloroquine could restore Her2/neu and polyubiquitination of Her2/neu was augmented during emodin AMAD treatment. Furthermore, immunofluorescence study with anti-Her2/neu antibody showed that emodin AMAD disturbed the subcellular distribution of Her2/neu, with decreased location in the plasma membrane. Molecular docking studies predicted that AMAD can interact with the ATP-binding pocket of both Hsp90 and Her2/neu. Importantly, coimmunoprecipitation and immunofluorescence study revealed that emodin AMAD markedly impaired the binding between Hsp90 and Her2/neu and could bind to both Hsp90 and Her2/neu as reinforced by molecular modeling studies. In addition, combination of emodin AMAD treatment and siRNA against Her2 synergistically inhibited proliferation and induced apoptosis. Taken together, these data suggest that blockade of Her2/neu binding to Hsp90 and following proteasomal degradation of Her2/neu were involved in emodin AMAD-induced apoptosis in Her2/neu-overexpressing cancer cells. Our results provide suggestions that emodin AMAD could be promising as a new targeting therapeutic strategy in the treatment of Her2/neu-overexpressing cancers....(more)
Yan YY, et al. Mol Pharm 2011 Oct 3;8(5):1687-97.
Related Products: Giant Knotweed Extract