- 1. Naringin improves diet-induced cardiovascular dysfunction and obesity in high carbohydrate, high fat diet-fed rats.
Obesity, insulin resistance, hypertension and fatty liver, together termed metabolic syndrome, are key risk factors for cardiovascular disease. Chronic feeding of a diet high in saturated fats and simple sugars, such as fructose and glucose, induces these changes in rats. Naturally occurring compounds could be a cost-effective intervention to reverse these changes. Flavonoids are ubiquitous secondary plant metabolites; naringin gives the bitter taste to grapefruit. This study has evaluated the effect of naringin on diet-induced obesity and cardiovascular dysfunction in high carbohydrate, high fat-fed rats. These rats developed increased body weight, glucose intolerance, increased plasma lipid concentrations, hypertension, left ventricular hypertrophy and fibrosis, liver inflammation and steatosis with compromised mitochondrial respiratory chain activity. Dietary supplementation with naringin (approximately 100 mg/kg/day) improved glucose intolerance and liver mitochondrial dysfunction, lowered plasma lipid concentrations and improved the structure and function of the heart and liver without decreasing total body weight. Naringin normalised systolic blood pressure and improved vascular dysfunction and ventricular diastolic dysfunction in high carbohydrate, high fat-fed rats. These beneficial effects of naringin may be mediated by reduced inflammatory cell infiltration, reduced oxidative stress, lowered plasma lipid concentrations and improved liver mitochondrial function in rats....(more)
Alam MA, et al. Nutrients 2013 Feb 27;5(3):637-50.
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- 2. Functions of monocyte chemotactic protein-3 in transgenic mice fed a high-fat, high-cholesterol diet.
Monocyte chemotactic protein-3 (MCP-3), a chemokine that is in a superfamily of structurally related small chemotactic cytokines involved in leukocyte trafficking, is regarded as a key factor in atherogenesis. In this study, we examined the changes in atherogenic parameters including hepatic lipid accumulation and oxidative balance in MCP- 3-overexpressing transgenic mice (MCP-3 mice) under atherogenic conditions. To induce an extreme atherogenic condition, mice were fed a high-fat, high-cholesterol (HFHC) diet for 12 weeks. The body weight and food intake were not changed by MCP-3 overexpression in the aorta. On a HFHC diet, the MCP-3 mice had higher plasma levels of total cholesterol and a higher atherogenic index compared with wild-type mice, although there were no differences in the plasma HDL-cholesterol and triglyceride levels. Furthermore, an increase in lipid accumulation was observed in the aortas as well as the livers of the HFHC diet-fed MCP-3 mice compared with wild-type mice. The activities of antioxidant enzymes increased in the livers of the HFHC diet-fed MCP-3 mice, whereas supplementation with antioxidants, naringin and hesperidin, reversed the activities of the hepatic antioxidant enzymes in HFHC diet-fed MCP-3 mice, indicating that there might be more oxidative damage to the tissues in the HFHC diet-fed MCP-3 mice leading to progression towards atherosclerosis and hepatic steatosis. Microarray analyses of the aorta revealed atherosclerosis-, PPARs-, lipoprotein receptor, and apolipoprotein-related genes that were affected by the HFHC diet in MCP-3 mice. These findings suggest that aortic MCP-3 overexpression may contribute to the development of atherosclerosis and hepatic steatosis under atherogenic conditions....(more)
An SJ, et al. J Microbiol Biotechnol 2013 Mar;23(3):405-13.
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- 3. Naringin Enhances CaMKII Activity and Improves Long-Term Memory in a Mouse Model of Alzheimer's Disease.
The Amyloid-β (Aβ)-induced impairment of hippocampal synaptic plasticity is an underlying mechanism of memory loss in the early stages of Alzheimer's disease (AD) in human and mouse models. The inhibition of the calcium/calmodulin-dependent protein kinase II (CaMKII) autophosphorylation plays an important role in long-term memory. In this study, we isolated naringin from Pomelo peel (a Citrus species) and studied its effect on long-term memory in the APPswe/PS1dE9 transgenic mouse model of AD. Three-month-old APPswe/PS1dE9 transgenic mice were randomly assigned to a vehicle group, two naringin (either 50 or 100 mg/kg body weight/day) groups, or an Aricept (2 mg/kg body weight/day) group. After 16 weeks of treatment, we observed that treatment with naringin (100 mg/kg body weight/day) enhanced the autophosphorylation of CaMKII, increased the phosphorylation of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic (AMPA) receptor at a CaMKII-dependent site and improved long-term learning and memory ability. These findings suggest that the increase in CaMKII activity may be one of the mechanisms by which naringin improves long-term cognitive function in the APPswe/PS1dE9 transgenic mouse model of AD....(more)
Wang DM, et al. Int J Mol Sci 2013 Mar 11;14(3):5576-86.
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- 4. Naringin protects memory impairment and mitochondrial oxidative damage against aluminum-induced neurotoxicity in rats.
Aluminum has been indicated in neurodegenerative disorders and naringin, a bioflavonoid has been used to reduce neurotoxic effects of aluminum against aluminum chloride-induced rats. Therefore, present study has been designed to explore the possible role of naringin against aluminum-induced cognitive dysfunction and oxidative damage in rats. Aluminum (100 mg/kg) and naringin (40 and 80 mg/kg) drug treatment were administered orally for six weeks to male wistar rats. Various behavioral performance tasks, biochemical, mitochondrial oxidative parameters, and aluminum concentration in the brain were assessed. Aluminum chloride treatment significantly caused cognitive dysfunction and mitochondria oxidative damage as compared to vehicle treated control group. Besides, aluminum chloride treatment significantly increased acetyl cholinesterase activity and aluminum concentration in the brain as compared to sham. Chronic administration of naringin significantly improved cognitive performance and attenuated mitochondria oxidative damage, acetyl cholinesterase activity, and aluminum concentration in aluminum-treated rats as compared to control rats. Results of the study demonstrate neuroprotective potential of naringin against aluminum chloride-induced cognitive dysfunction and mitochondrial oxidative damage....(more)
Prakash A, et al. Int J Neurosci 2013 Apr 26.
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- 5. 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.
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- 6. Investigation of the interaction of naringin palmitate with bovine serum albumin: spectroscopic analysis and molecular docking.
BACKGROUND:
Bovine serum albumin (BSA) contains high affinity binding sites for several endogenous and exogenous compounds and has been used to replace human serum albumin (HSA), as these two compounds share a similar structure. Naringin palmitate is a modified product of naringin that is produced by an acylation reaction with palmitic acid, which is considered to be an effective substance for enhancing naringin lipophilicity. In this study, the interaction of naringin palmitate with BSA was characterised by spectroscopic and molecular docking techniques.
METHODOLOGYPRINCIPAL FINDINGS:
The goal of this study was to investigate the interactions between naringin palmitate and BSA under physiological conditions, and differences in naringin and naringin palmitate affinities for BSA were further compared and analysed. The formation of naringin palmitate-BSA was revealed by fluorescence quenching, and the Stern-Volmer quenching constant (KSV ) was found to decrease with increasing temperature, suggesting that a static quenching mechanism was involved. The changes in enthalpy (ΔH) and entropy (ΔS) for the interaction were detected at -4.11±0.18 kJ·mol(-1) and -76.59±0.32 J·mol(-1)·K(-1), respectively, which indicated that the naringin palmitate-BSA interaction occurred mainly through van der Waals forces and hydrogen bond formation. The negative free energy change (ΔG) values of naringin palmitate at different temperatures suggested a spontaneous interaction. Circular dichroism studies revealed that the α-helical content of BSA decreased after interacting with naringin palmitate. Displacement studies suggested that naringin palmitate was partially bound to site I (subdomain IIA) of the BSA, which was also substantiated by the molecular docking studies.
CONCLUSIONSSIGNIFICANCE:
In conclusion, naringin palmitate was transported by BSA and was easily removed afterwards. As a consequence, an extension of naringin applications for use in food, cosmetic and medicinal preparations may be clinically and practically significant, especially in the design of new naringin palmitate-inspired drugs....(more)
Zhang X, et al. PLoS One 2013;8(3):e59106.
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- 7. Naringin promotes osteoblast differentiation and effectively reverses ovariectomy-associated osteoporosis.
BACKGROUND:
Osteoporosis is a common pathological condition that influences 20 % of women over 50 years of age. This condition decreases bone strength and increases the risk of bone fracture. Naringin is a major flavonoid found in grapefruit and an active compound extracted from a Chinese herbal medicine (Rhizoma Drynariae). Studies have shown that naringin possesses many pharmacological effects. The current study evaluated the influence of naringin on osteoblastic cell differentiation and proliferation, and assessed its therapeutic effects on a rat osteoporosis model.
METHOD:
The proliferation, differentiation, and function of rat bone marrow stromal cells (BMSCs) were determined following treatment with various concentrations of naringin. Ovariectomy (OVX)-induced osteoporotic rats were orally administered naringin daily at low, medium, and high dosages, while a control group received PBS for 2 months. Femoral X-ray images and microCT scans were used for bone mineral density (BMD) and BV/TV (bone volume/total volume) analyses, and histological assessments of left tibiae were employed to check for changes in trabecular thickness (Tb.Th) and trabecular space (Tb.Sp) in the groups.
RESULTS:
Naringin was effective at enhancing the proliferation and osteogenic differentiation of BMSCs, and a concentration of 10 μg/ml prompted the highest levels of osteocalcin expression among the in vitro study groups. There appeared to be a delayed response pattern of BMSCs to the naringin treatment. Naringin also effectively reversed OVX-induced bone loss via increasing BMD, bone volume, and trabecular thickness. The medium dose (300 mg/kg) appeared to be the optimal dosage for delivering satisfactory therapeutic effects.
CONCLUSION:
Naringin promotes the proliferation and differentiation of BMSCs, and increases osteocalcin expression. Naringin also effectively reverses ovariectomy-induced osteoporosis in rats. The study suggests that naringin administration may represent an effective treatment for osteoporosis....(more)
Li N, et al. J Orthop Sci 2013 Apr 4.
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- 8. Cultivar variations in antioxidant and antihyperlipidemic properties of pomelo pulp (Citrus grandis [L.] Osbeck) in Thailand.
Pomelo (Citrus grandis L. Osbeck) is a native fruit of great economic importance in Southeast Asia. To provide experimental evidence for the antioxidant and antihyperlipidemic properties of pomelo, 6 cultivars, including Kao-Yai (KY), Thong-dee (TD), Kao-Tangkwa (KT), Kao-Numpueng (KN), Ta-Koi (TK), and Tubtim Siam (TS) were evaluated. KY had the highest phenolic content, and the strongest 1,1-diphenyl-2-pireyhydrazyl radical scavenging capacity and hydroxyl radical scavenging activity. From the high-performance liquid chromatography analysis, naringin and naringenin were the major flavonoids in the KT and TK cultivars. Six pomelo cultivars had antihyperlipidemic activities including the inhibition of pancreatic lipase and cholesterol esterase, as well as cholesterol micelle formation and bile acid binding. Hierarchical clustering analysis showed that the 6 cultivars were separated into 2 classifications. In addition, the total phenolics of the pomelo cultivars were significantly correlated with ferric reducing antioxidant power and Trolox equivalent antioxidant capacity. The results suggest that pomelo provides significant health benefits and may be used for developing functional foods....(more)
Mäkynen K, et al. Food Chem 2013 Aug 15;139(1-4):735-43.
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- 9. Extraction of naringin from pomelo peels as dihydrochalcone's precursor.
A new method for the separation of naringin from pomelo peels was investigated by using ultrasonic-assisted extraction and macroporous resin purification technology. The ultrasonic extraction efficiency was dependent on agent's concentration, ratio of sample and solvent and ultrasonic time. Several parameters of macroporous resin-purified process, including resin selection, initial concentration, concentration of eluted agent and pH, were optimized. The experimental results showed that the naringin content in the mature pomelo peels was 2.20% and purification rate of naringin was 77.26% under optimum conditions of purification. The structure of synthetic naringin dihydrochalcone was determined by a series of spectroscopic methods, such as UV, NMR and MS....(more)
Tang DM, et al. J Sep Sci 2011 Jan;34(1):113-7.
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- 10. Hypouricemic action of selected flavonoids in mice: structure-activity relationships.
Hyperuricemia and gout appear to be rapidly increasing worldwide and frequently cause symptoms of metabolic syndrome. Dietary flavonoids have their potential beneficial effects on human health. In the present study, 15 flavonoids (quercetin, morin, myricetin, kaempferol, icariin, apigenin, luteolin, baicalin, silibinin, naringenin, formonoetin, genistein, puerarin, daidzin and naringin dihydrochalcone) were selected to investigate for their hypouricemic action in mice. Oral administration of quercetin, morin, myricetin, kaempferol, apigenin and puerarin at 50 and 100 mg/kg for 3 d was able to elicit hypouricemic actions in hyperuricemic mice induced by potassium oxonate. Luteolin, formonoetin and naringenin showed the significant effects only at 100 mg/kg. Quercetin, puerarin, myricetin, morin and kaempferol significantly reduced liver uric acid level in hyperuricemic animals. In addition, quercetin, morin, myricetin, kaempferol and puerarin exhibited significant inhibition on the liver xanthine oxidase (XOD) activities. It seems to be likely that these flavonoids reduce serum urate levels by mainly inhibiting XOD activity. However, the hypouricemic effect of apigenin observed seemed not to parallel with the changes in liver uric acid level and liver XOD activity, implying that apigenin might act via other mechanisms apart from inhibiting enzyme activity simply. Analysis of the chemical structure showed that a planar structure with the hydroxyl groups played a crucial role in hypouricemic activity of flavonoids. The exact mechanism of the hypouricemic action of flavonoids in vivo should be investigated in the future....(more)
Mo SF, et al. Biol Pharm Bull 2007 Aug;30(8):1551-6.
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- 11. HPLC-PDA-MS and NMR characterization of a hydroalcoholic extract of Citrus aurantium L. var. amara peel with antiedematogenic activity.
The phytochemical profile of a hydroalcoholic extract of Citrus aurantium var. amara L. peel, used as herbal medicine, was characterized by HPLC-PDA-MS. Two di-C-glycosyl flavones (vincenin II and diosmetin 6,8-di-C-glucoside), a series of flavones (luteolin 7-O-neohesperidoside, rhoifolin, and neodiosmin), and flavanone (neoeriocitrin, naringin, and neohesperidin) 7-O-neohesperidosides and two methoxyflavones (nobiletin and tangeretin), commonly present in Citrus, were identified. Furthermore, brutieridin and melitidin, two 3-hydroxy-3-methylglutaryl flavanone glycosides, were also characterized along with rhoifolin 4'-glucoside and three coumarins (8,3'-β-D-glucopyranosyloxy-2'-hydroxy-3'-methylbutyl-7-methoxycoumarin, merazin hydrate, and isomerazin). A preparative isolation procedure followed by NMR spectroscopy confirmed the proposed structures of the major flavonoids and identified the coumarins. The phenolic content was found to be 14.8 mg mL(-1), and naringin and neohesperidin were the compounds present in the highest concentration (3.6 and 2.6 mg mL(-1)). The extract of C. aurantium peel inhibited significantly (p < 0.05) both histamine- and dextran-induced edema in rats in a concentration-dependent manner (IC(50) = 119.6 and 118.3 mg kg(-1), respectively), providing evidence for the therapeutic use of C. aurantium var. amara peel....(more)
Mencherini T, et al. J Agric Food Chem 2013 Feb 27;61(8):1686-93.
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- 12. Phytochemical profile and antioxidant activity of physiological drop of citrus fruits.
The phytochemical content and the antioxidant activity (AA) of physiological drop of the main citrus species grown in China were investigated. Among the flavonoids, hesperidin was found mostly in mandarin and sweet orange, naringin was found mostly in sour orange, pummelo, grapefruit and a hybrid (Gaocheng), narirutin was found in most varieties, neohesperidin was found in Gaocheng and Huyou, and nobiletin and tangeretin were found in most varieties. Hydroxycinnamic acids were the main phenolic acids present, ferulic acid and caffeic acid were the dominant in most cases. There was a greater amount of free (extractable) than bound (insoluble) phenolic acids. Levels of limonoids were higher in Foyou, Eureka lemon, and Gaocheng than those in the other cultivars. The highest level of synephrine was found in Ponkan and Weizhang Satsuma. AA was highest in Ponkan and Weizhang Satsuma and lowest in Huyou, pummel, and lemon. These results suggest that physiological drop of citrus fruits have good potential as sources of different bioactive compounds and antioxidants. PRACTICAL APPLICATION: Physiological drop of citrus fruits may be a good resource of bioactive compounds including flavonoids, phenolic acids, limonoids, synephrine, and a good material of nutraceuticals....(more)
Sun Y, et al. J Food Sci 2013 Jan;78(1):C37-42.
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- 13. Neohesperidin dihydrochalcone: presentation of a small molecule activator of mammalian alpha-amylase as an allosteric effector.
Flavonoids and their precursor trans-chalcone have been reported as inhibitors of mammalian alpha-amylase. With regard to this background, neohesperidin dihydrochalcone (NHDC) effect was investigated toward porcine pancreatic alpha-amylase (PPA), and found to be an activator of the enzyme. The maximal activation (up to threefold) was found to occur at 4.8mM of NHDC, which could be considered to have a high activation profile, with regard to the alpha and beta parameters (alpha<1<beta). NHDC is a non-essential activator of the enzyme and based on the results obtained from modeling tools, it is suggested to interact with PPA at a hydrophilic site located at the N-terminal, far from the active site of the enzyme....(more)
Kashani-Amin E, et al. FEBS Lett 2013 Mar 18;587(6):652-8.
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- 14. 2-Hydroxychalcone and xanthohumol inhibit invasion of triple negative breast cancer cells.
Breast cancer is estimated as one of the most common causes of cancer death among women. In particular, triple negative breast cancers (TNBCs), which do not express the genes for estrogen/progesterone receptors (ER/PR) and human epidermal growth factor receptor 2 (HER2), have been associated with poor prognosis and metastasis. Chalcones, the biosynthetic precursors of flavonoids present in edible plants, exert cytotoxic and chemopreventive activities. Although mounting evidence suggests the anticancer properties of chalcones, limited information is available regarding the inhibitory effects of chalcones on the aggressiveness of breast cancer cells. The present study aimed to investigate the effects of chalcone and its derivatives on the growth and the invasiveness of TNBC cells. Here, we showed that treatment with chalcone, 2-hydroxychalcone, and xanthohumol for 24h inhibited the growth of MDA-MB-231cells with IC50 values of 18.1, 4.6, and 6.7μM, respectively. Similarly, Chalcone, 2-hydroxychalcone, and xanthohumol also exerted cytotoxicity in another TNBC cell line, Hs578T. Neohesperidin dihydrochalcone, 4-methoxychalcone, and hesperidin methylchalcone did not show the cytotoxicity on the MDA-MB-231cells. Xanthohumol and 2-hydroxychalcone induced apoptosis by Bcl-2 downregulation. Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone. These results suggest a potential application of these chalcones as anticancer agents that can alleviate malignant progression of TNBC....(more)
Kim SY, et al. Chem Biol Interact 2013 Apr 3;203(3):565-572.
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- 15. Separation and purification of neohesperidin from the albedo of Citrus reticulata cv. Suavissima by combination of macroporous resin and high-speed counter-current chromatography.
In this article, a simple and efficient protocol for rapid preparation and separation of neohesperidin from the albedo of Citrus reticulata cv. Suavissima was established by the combination of macroporous resin column chromatography and high-speed counter-current chromatography (HSCCC). Six types of resin were investigated by adsorption and desorption tests, and D101 macroporous resin was selected for the first cleaning-up procedure, in which 55% aqueous ethanol was used to elute neohesperidin. After treatment with D101 resin, the neohesperidin purity increased 11.83-fold from 4.92% in the crude extract to 58.22% in the resin-refined sample, with a recovery of 68.97%. The resin-refined sample was directly subjected to HSCCC purification with a two-phase solvent system composed of ethyl acetate-n-butanol-water (4:1:5, v/v), and 23.6 mg neohesperidin with 97.47% purity was obtained from 60 mg sample in only one run. The recovery of neohesperidin in HSCCC separation procedure was 65.85%. The chemical structure of the purified neohesperidin was identified by both HPLC and LC-MS. The established purification process will be helpful for further characterization and utilization of Citrus neohesperidin....(more)
Zhang J, et al. J Sep Sci 2012 Jan;35(1):128-36.
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- 16. Phenolic composition and antioxidant effect of aqueous extract of Arisaema cum Bile, the Oriental Herb Medicine, in human fibroblast cells.
Phenolic composition and antioxidant activities of the aqueous extract of Arisaema cum Bile, which is widely used as a folk medicine in Korea, were determined. Phenolic composition profile revealed that the aqueous extract is rich in sinapic acid (13.14 mg/100 g extract), catechin (9.88 mg/100 g extract), neohesperidin (7.38 mg/100 g extract), and chlorogenic acid (3.64 mg/100 g extract). The aqueous extract effectively scavenged toward 2,2-diphenyl-1-picrylhydrazyl (90.63%), hydrogen peroxide (98.13%), and hydroxyl radical (59.62%) at 2.0 mg/mL, and also showed high reducing power. In cytotoxic evaluation, the aqueous extract exhibited no significant cytotoxicity in human fibroblast, and it also exhibited appreciable suppression of intracellular reactive oxygen species and inhibition of lipid peroxidation. In addition, the aqueous extract upregulated the level of glutathione in a dose-dependent manner. Taken together, the aqueous extract of Arisaema cum Bile could be considered as a potential natural source that may be useful for curing diseases arising from oxidative deterioration....(more)
Ahn CB, et al. Immunopharmacol Immunotoxicol 2012 Aug;34(4):661-6.
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- 17. Characterization and quantification of major constituents of Xue Fu Zhu Yu by UPLC-DAD-MS/MS.
Xue Fu Zhu Yu (XFZY), a classic recipe in traditional Chinese medicine (TCM), has been demonstrated to show protective effects on cardiovascular system. For quality control of XFZY products, qualitative analysis using ultra high performance liquid chromatography with diode-array detector-tandem mass spectrometry (UPLC-DAD-MS) was undertaken. Twenty-eight compounds from XFZY were simultaneously detected; among them, seventeen compounds were unequivocally identified, and another eight compounds were tentatively characterized. According to qualitative results, a new method for quantitative analysis of XFZY has been established by ultra high performance liquid chromatography coupled with diode array detector (UPLC-DAD). Twelve representative compounds unequivocally identified were used as chemical markers in quantitative analysis, including 5-hydroxymethyl-2-furaldehyde (5-HMF), hydroxysafflor yellow A (HSYA), amygdalin, albiflorin, paeoniflorin, liquiritin, ferulic acid (FA), naringin, hesperidin, neohesperidin (NH), isoliquiritigenin (IL) and glycyrrhizic acid (GA), which were derived from nine of eleven herbs of XFZY except Platycodon grandiflorum (Jacq.) A. DC. (Jiegeng) and Bupleurum chinense DC. (Chaihu). This UPLC method was validated in terms of linearity, LOD and LOQ, precision, repeatability, stability, and recovery tests. Quality control of XFZY products in total fourteen samples by four dosage forms was examined by this method, and results confirmed its feasibility and reliability in practice....(more)
Zhang L, et al. J Pharm Biomed Anal 2012 Mar 25;62:203-9.
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- 18. Inhibition of quorum sensing (QS) in Yersinia enterocolitica by an orange extract rich in glycosylated flavanones.
Flavanones, flavonoids abundant in Citrus , have been shown to interfere with quorum sensing (QS) and affect related physiological processes. We have investigated the QS-inhibitory effects of an orange extract enriched in O-glycosylated flavanones (mainly naringin, neohesperidin, and hesperidin). The QS-inhibitory capacity of this extract and its main flavanone components was first screened using the bacteriological monitoring system Chromobacterium violaceum . We next examined the ability of the orange extract and of some of the flavanones to (i) reduce the levels of the QS mediators produced by Y. enterocolitica using HPLC-MS/MS, (ii) inhibit biofilm formation, and (iii) inhibit swimming and swarming motility. Additionally, we evaluated changes in the expression of specific genes involved in the synthesis of the lactones (yenI, yenR) and in the flagellar regulon (flhDC, fleB, fliA) by RT-PCR. The results showed that the orange extract and its main flavanone components inhibited QS in C. violaceum, diminished the levels of lactones secreted by Y. enterocolitica to the media, and decreased QS-associated biofilm maturation without affecting bacterial growth. Among the tested compounds, naringin was found to inhibit swimming motility. Exposure to the orange extract and (or) to naringin was also found to be associated with induction of the transcription levels of yenR, flhDC, and fliA. This work shows the in vitro QS-inhibitory effects of an orange extract enriched in flavanones against a human enteropathogen at doses that can be achieved through the diet and suggests that consumption of these natural extracts may have a beneficial antipathogenic effect....(more)
Truchado P, et al. J Agric Food Chem 2012 Sep 12;60(36):8885-94.
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- 19. Protective effects of an extract from Citrus bergamia against inflammatory injury in interferon-γ and histamine exposed human keratinocytes.
AIMS:
The present work evaluated the anti-inflammatory/antioxidant activity of a well characterized extract from Citrus bergamia Risso and Poiteau (CBE), containing neoeriocitrin, naringin, neohesperidin and other flavonoids, on human NCTC 2544 keratinocytes treated with interferon-gamma (IFN-γ) and histamine (H).
MAIN METHODS:
High performance liquid chromatography (HPLC) coupled with diode array detectors was used to characterize and quantify phenolic compounds in CBE. Anti-inflammatory/antioxidant ability on keratinocytes was determined through evaluation of inter-cellular adhesion molecule-1 (ICAM-1) and inducible nitric oxide synthase (iNOS) expression by Western blot, production of nitric oxide (NO) with Griess reagent and concentration of reactive oxygen species (ROS) by fluorescent quantitative analysis with 2',7'-dichlorfluorescein-diacetate (DCFH-DA). Cell viability was assessed using 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Antioxidant activity was also measured by oxygen radical absorbance capacity (ORAC) assay. Glycosaminoglycans (GAGs) were quantified using 1.9-dimethyl methylene blue (DMB).
KEY FINDINGS:
CBE exhibited high antioxidant activity confirmed by elevated ORAC values related to high capacity in oxygen radical scavenging. The assays on keratinocytes demonstrated that CBE does not inhibit cell proliferation and is shown to significantly reduce dose-dependently ICAM-1, iNOS, NO, ROS and GAG production in cells exposed to IFN-γ and H.
SIGNIFICANCE:
Our study demonstrates that the pools of compounds of an extract from C. bergamia efficiently block the proinflammatory actions induced by IFN-γ and H on human keratinocytes. CBE may be used for topic employment in some inflammatory diseases of the skin and to represent an important opportunity for the essential oil processing industries.
Copyright © 2012 Elsevier Inc. All rights reserved....(more)
Graziano AC, et al. Life Sci 2012 Jun 27;90(25-26):968-74.
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- 20. In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: identifying sinensetin as a novel antiangiogenesis agent.
SCOPE:
Polymethoxylated flavonoids are present in citrus fruit in a range of chemical structures and abundance. These compounds have potential for anticarcinogenesis, antitumor, and cardiovascular protective activity, but the effect on angiogenesis has not been well studied.
METHODS AND RESULTS:
Human umbilical vein endothelial cells (HUVECs) in vitro and zebrafish (Danio rerio) in vivo models were used to screen and identify the antiangiogenesis activity of seven polymethoxylated flavonoids; namely, hesperetin, naringin, neohesperidin, nobiletin, scutellarein, scutellarein tetramethylether, and sinensetin. Five, excluding naringin and neohesperidin, showed different degrees of potency of antiangiogenesis activity. Sinensetin, which had the most potent antiangiogenesis activity and the lowest toxicity, inhibited angiogenesis by inducing cell cycle arrest in the G0/G1 phase in HUVEC culture and downregulating the mRNA expressions of angiogenesis genes flt1, kdrl, and hras in zebrafish.
CONCLUSION:
The in vivo structure-activity relationship (SAR) analysis indicated that a flavonoid with a methoxylated group at the C3' position offers a stronger antiangiogenesis activity, whereas the absence of a methoxylated group at the C8 position offers lower lethal toxicity in addition to enhancing the antiangiogenesis activity. This study provides new insight into how modification of the chemical structure of polymethoxylated flavonoids affects this newly identified antiangiogenesis activity.
© 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Lam IK, et al. Mol Nutr Food Res 2012 Jun;56(6):945-56.
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- 21. Neohesperidin dihydrochalcone: presentation of a small molecule activator of mammalian alpha-amylase as an allosteric effector.
Flavonoids and their precursor trans-chalcone have been reported as inhibitors of mammalian alpha-amylase. With regard to this background, neohesperidin dihydrochalcone (NHDC) effect was investigated toward porcine pancreatic alpha-amylase (PPA), and found to be an activator of the enzyme. The maximal activation (up to threefold) was found to occur at 4.8mM of NHDC, which could be considered to have a high activation profile, with regard to the alpha and beta parameters (alpha<1<beta). NHDC is a non-essential activator of the enzyme and based on the results obtained from modeling tools, it is suggested to interact with PPA at a hydrophilic site located at the N-terminal, far from the active site of the enzyme....(more)
Kashani-Amin E, et al. FEBS Lett 2013 Mar 18;587(6):652-8.
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- 22. 2-Hydroxychalcone and xanthohumol inhibit invasion of triple negative breast cancer cells.
Breast cancer is estimated as one of the most common causes of cancer death among women. In particular, triple negative breast cancers (TNBCs), which do not express the genes for estrogen/progesterone receptors (ER/PR) and human epidermal growth factor receptor 2 (HER2), have been associated with poor prognosis and metastasis. Chalcones, the biosynthetic precursors of flavonoids present in edible plants, exert cytotoxic and chemopreventive activities. Although mounting evidence suggests the anticancer properties of chalcones, limited information is available regarding the inhibitory effects of chalcones on the aggressiveness of breast cancer cells. The present study aimed to investigate the effects of chalcone and its derivatives on the growth and the invasiveness of TNBC cells. Here, we showed that treatment with chalcone, 2-hydroxychalcone, and xanthohumol for 24h inhibited the growth of MDA-MB-231cells with IC50 values of 18.1, 4.6, and 6.7μM, respectively. Similarly, Chalcone, 2-hydroxychalcone, and xanthohumol also exerted cytotoxicity in another TNBC cell line, Hs578T. Neohesperidin dihydrochalcone, 4-methoxychalcone, and hesperidin methylchalcone did not show the cytotoxicity on the MDA-MB-231cells. Xanthohumol and 2-hydroxychalcone induced apoptosis by Bcl-2 downregulation. Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone. These results suggest a potential application of these chalcones as anticancer agents that can alleviate malignant progression of TNBC....(more)
Kim SY, et al. Chem Biol Interact 2013 Apr 3;203(3):565-572.
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- 23. Determination of nine high-intensity sweeteners in various foods by high-performance liquid chromatography with mass spectrometric detection.
An analytical procedure involving solid-phase extraction (SPE) and high-performance liquid chromatography-mass spectrometry has been developed for the determination of nine high-intensity sweeteners authorised in the EU; acesulfame-K (ACS-K), aspartame (ASP), alitame (ALI), cyclamate (CYC), dulcin (DUL), neohesperidin dihydrochalcone (NHDC), neotame (NEO), saccharin (SAC) and sucralose (SCL) in a variety of food samples (i.e. beverages, dairy and fish products). After extraction with a buffer composed of formic acid and N,N-diisopropylethylamine at pH 4.5 in ultrasonic bath, extracts were cleaned up using Strata-X 33 μm Polymeric SPE column. The analytes were separated in gradient elution mode on C(18) column and detected by mass spectrometer working with an electrospray source in negative ion mode. To confirm that analytical method is suitable for its intended use, several validation parameters, such as linearity, limits of detection and quantification, trueness and repeatibilty were evaluated. Calibration curves were linear within a studied range of concentrations (r(2) ≥ 0.999) for six investigated sweeteners (CYC, ASP, ALI, DUL, NHDC, NEO). Three compounds (ACS-K, SAC, SCL) gave non-linear response in the investigated concentration range. The method detection limits (corresponding to signal-to-noise (S/N) ratio of 3) were below 0.25 μg mL(-1) (μg g(-1)), whereas the method quantitation limits (corresponding to S/N ratio of 10) were below 2.5 μg mL(-1) (μg g(-1)). The recoveries at the tested concentrations (50%, 100% and 125% of maximum usable dose) for all sweeteners were in the range of 84.2 ÷ 106.7%, with relative standard deviations <10% regardless of the type of sample matrix (i.e. beverage, yoghurt, fish product) and the spiking level. The proposed method has been successfully applied to the determination of the nine sweeteners in drinks, yoghurts and fish products. The procedure described here is simple, accurate and precise and is suitable for routine quality control analysis of foodstuffs....(more)
Zygler A, et al. Anal Bioanal Chem 2011 Jun;400(7):2159-72.
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- 24. Dihydrochalcone glycosides from Oxytropis myriophylla.
Chemical investigations of the 70% alcohol extract of Oxytropis myriophylla (Pall.) DC. (Leguminosae) have afforded the new natural product neohesperidin dihydrochalcone (1) and the known phloretin-4'-O-β-D-glucopyranoside (2), which was the first reported from the genus Oxytropis. This paper reports the isolation and full spectroscopic characterization of compounds 1 and 2 by NMR, UV, IR and MS data....(more)
She G, et al. Chem Cent J 2011 Nov 9;5:71.
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- 25. Expression of Na+/glucose co-transporter 1 (SGLT1) is enhanced by supplementation of the diet of weaning piglets with artificial sweeteners.
In an intensive livestock production, a shorter suckling period allows more piglets to be born. However, this practice leads to a number of disorders including nutrient malabsorption, resulting in diarrhoea, malnutrition and dehydration. A number of strategies have been proposed to overcome weaning problems. Artificial sweeteners, routinely included in piglets' diet, were thought to enhance feed palatability. However, it is shown in rodent models that when included in the diet, they enhance the expression of Na+/glucose co-transporter (SGLT1) and the capacity of the gut to absorb glucose. Here, we show that supplementation of piglets' feed with a combination of artificial sweeteners saccharin and neohesperidin dihydrochalcone enhances the expression of SGLT1 and intestinal glucose transport function. Artificial sweeteners are known to act on the intestinal sweet taste receptor T1R2/T1R3 and its partner G-protein, gustducin, to activate pathways leading to SGLT1 up-regulation. Here, we demonstrate that T1R2, T1R3 and gustducin are expressed together in the enteroendocrine cells of piglet intestine. Furthermore, gut hormones secreted by the endocrine cells in response to dietary carbohydrates, glucagon-like peptides (GLP)-1, GLP-2 and glucose-dependent insulinotrophic peptide (GIP), are co-expressed with type 1 G-protein-coupled receptors (T1R) and gustducin, indicating that L- and K-enteroendocrine cells express these taste elements. In a fewer endocrine cells, T1R are also co-expressed with serotonin. Lactisole, an inhibitor of human T1R3, had no inhibitory effect on sweetener-induced SGLT1 up-regulation in piglet intestine. A better understanding of the mechanism(s) involved in sweetener up-regulation of SGLT1 will allow the identification of nutritional targets with implications for the prevention of weaning-related malabsorption....(more)
Moran AW, et al. Br J Nutr 2010 Sep;104(5):637-46.
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- 26. Retention behaviour of some high-intensity sweeteners on different SPE sorbents.
The objective of this paper is to provide information about application of solid-phase extraction (SPE) for isolation of nine high-intensity sweeteners (acesulfame-K, alitame, aspartame, cyclamate, dulcin, neotame, saccharin, sucralose and neohesperidin dihydrochalcone) from aqueous solutions. The influence of several types of LC-MS compatible buffers (different pH values and compositions) on their recovery has been studied and discussed. A number of commercially available SPE cartridges, such as Chromabond C18ec, Strata-X RP, Bakerbond Octadecyl, Bakerbond SDB-1, Bakerbond SPE Phenyl, Oasis HLB, LiChrolut RP-18, Supelclean LC-18, Discovery DSC-18 and Zorbax C18 were tested in order to evaluate their applicability for the isolation of analytes. Very high recoveries (better than 92%) of all studied compounds were obtained using formic acid-N,N-diisopropylethylamine buffer adjusted to pH 4.5 and C(18)-bonded silica sorbents. Behaviour of polymeric sorbents strongly depends on their structure. Strata-X RP behaves much like a C(18)-bonded silica sorbent. Recoveries obtained using Oasis HLB were comparable with those observed for silica-based sorbents. The only compound less efficiently (83%) retained by this sorbent was cyclamate. Bakerbond SDB-1 shows unusual selectivity towards aspartame and alitame. Recoveries of these two sweeteners were very low (26 and 42%, respectively). It was also found that aspartame and alitame can be selectively separated from the mixture of sweeteners using formic acid-triethylamine buffer at pH 3.5....(more)
Zygler A, et al. Talanta 2010 Oct 15;82(5):1742-8.
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- 27. Analysis and occurrence of seven artificial sweeteners in German waste water and surface water and in soil aquifer treatment (SAT).
A method for the simultaneous determination of seven commonly used artificial sweeteners in water is presented. The analytes were extracted by solid phase extraction using Bakerbond SDB 1 cartridges at pH 3 and analyzed by liquid chromatography electrospray ionization tandem mass spectrometry in negative ionization mode. Ionization was enhanced by post-column addition of the alkaline modifier Tris(hydroxymethyl)amino methane. Except for aspartame and neohesperidin dihydrochalcone, recoveries were higher than 75% in potable water with comparable results for surface water. Matrix effects due to reduced extraction yields in undiluted waste water were negligible for aspartame and neotame but considerable for the other compounds. The widespread distribution of acesulfame, saccharin, cyclamate, and sucralose in the aquatic environment could be proven. Concentrations in two influents of German sewage treatment plants (STPs) were up to 190 microg/L for cyclamate, about 40 microg/L for acesulfame and saccharin, and less than 1 microg/L for sucralose. Removal in the STPs was limited for acesulfame and sucralose and >94% for saccharin and cyclamate. The persistence of some artificial sweeteners during soil aquifer treatment was demonstrated and confirmed their environmental relevance. The use of sucralose and acesulfame as tracers for anthropogenic contamination is conceivable. In German surface waters, acesulfame was the predominant artificial sweetener with concentrations exceeding 2 microg/L. Other sweeteners were detected up to several hundred nanograms per liter in the order saccharin approximately cyclamate > sucralose....(more)
Scheurer M, et al. Anal Bioanal Chem 2009 Jul;394(6):1585-94.
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- 28. Antioxidant properties of neohesperidin dihydrochalcone: inhibition of hypochlorous acid-induced DNA strand breakage, protein degradation, and cell death.
Neohesperidin dihydrochalcone (NHDC), a non-nutritive sweetening agent, is simply produced by hydrogenation of neohesperidin. The aim of this study is to evaluate the antioxidant and radical scavenging properties of neohesperidin dihydrochalcone and other structurally related compounds (phloridzin, neohesperidin) toward different reactive radical and oxygen species including .ABTS+, .O2-, .OH, H2O2, and HOCl in vitro. NHDC showed remarkable radical scavenging activity against stable radical and reactive oxygen species (ROS) in concentration dependent manner. Especially, NHDC was the most potent inhibitor of H2O2 and HOCl. NHDC showed HOCl scavenging activity of 93.5% and H2O2 scavenging property of 73.5% which was more than those of all the tested compounds including ascorbic acid and BHT. Moreover, NHDC could inhibit protein degradation, plasmid DNA strand cleavage and HIT-T15, HUVEC cell death from HOCl attack while mannitol, BHT, and ascorbic acid could not protect them effectively. These results suggest that NHDC is a potent antioxidant, especially it is evaluated as a novel HOCl scavenger. This study implies the possibility of therapeutic effect of NHDC on ROS-related inflammatory diseases....(more)
Choi JM, et al. Biol Pharm Bull 2007 Feb;30(2):324-30.
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- 29. The binding site for neohesperidin dihydrochalcone at the human sweet taste receptor.
BACKGROUND:
Differences in sweet taste perception among species depend on structural variations of the sweet taste receptor. The commercially used isovanillyl sweetener neohesperidin dihydrochalcone activates the human but not the rat sweet receptor TAS1R2+TAS1R3. Analysis of interspecies combinations and chimeras of rat and human TAS1R2+TAS1R3 suggested that the heptahelical domain of human TAS1R3 is crucial for the activation of the sweet receptor by neohesperidin dihydrochalcone.
RESULTS:
By mutational analysis combined with functional studies and molecular modeling we identified a set of different amino acid residues within the heptahelical domain of human TAS1R3 that forms the neohesperidin dihydrochalcone binding pocket. Sixteen amino acid residues in the transmembrane domains 2 to 7 and one in the extracellular loop 2 of hTAS1R3 influenced the receptor's response to neohesperidin dihydrochalcone. Some of these seventeen residues are also part of the binding sites for the sweetener cyclamate or the sweet taste inhibitor lactisole. In line with this observation, lactisole inhibited activation of the sweet receptor by neohesperidin dihydrochalcone and cyclamate competitively, whereas receptor activation by aspartame, a sweetener known to bind to the N-terminal domain of TAS1R2, was allosterically inhibited. Seven of the amino acid positions crucial for activation of hTAS1R2+hTAS1R3 by neohesperidin dihydrochalcone are thought to play a role in the binding of allosteric modulators of other class C GPCRs, further supporting our model of the neohesperidin dihydrochalcone pharmacophore.
CONCLUSION:
From our data we conclude that we identified the neohesperidin dihydrochalcone binding site at the human sweet taste receptor, which overlaps with those for the sweetener cyclamate and the sweet taste inhibitor lactisole. This readily delivers a molecular explanation of our finding that lactisole is a competitive inhibitor of the receptor activation by neohesperidin dihydrochalcone and cyclamate. Some of the amino acid positions crucial for activation of hTAS1R2+hTAS1R3 by neohesperidin dihydrochalcone are involved in the binding of allosteric modulators in other class C GPCRs, suggesting a general role of these amino acid positions in allosterism and pointing to a common architecture of the heptahelical domains of class C GPCRs....(more)
Winnig M, et al. BMC Struct Biol 2007 Oct 12;7:66.
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- 30. Multi-element analysis of mineral and trace elements in medicinal herbs and their infusions.
Twelve mineral and trace elements (Al, B, Ba, Fe, Zn, Mn, Mg, K, Na, P, Cu, Sr, and Ca) were determined in the herbs and their infusions consumed for medical purposes in Poland such as chamomile (Matricaria chamomilla L.), peppermint (Mentha xpiperita), melissa (Melissa officinalis), sage (Salvia officinalis), nettle (Urtica dioica), linden (Tilia vulgaris) and St. John's wort (Hypericum calycinum). Dry digestion procedure for total concentration and wet digestion procedure for infusions were applied under optimized conditions for dissolution of medicinal herbs. Element concentrations in herbs and their infusions were determined by ICP-OES. The accuracy and precision were verified against NCS DC 73349 - bush branches and leaves certified reference material. The result of total concentrations of elements in herb leaves shows that all herbs contain most of the elements, except K and P, in the μg/g range, and that elemental concentrations varied widely. Moreover, on the basis of experimental results for the extraction efficiencies, the elements in herb infusions were classified into three specific groups: highly-extractable (>55%) including K; moderately-extractable (20-55%) including Mg, Na, P, B, Zn and Cu and poorly-extractable (<20%) including Al, Fe, Mn, Ba, Ca and Sr. The results of analysis were evaluated statistically using ANOVA one-way and three-way analysis of variance, variance correlation test and Spearman's test.
Copyright © 2012 Elsevier Ltd. All rights reserved....(more)
Pytlakowska K, et al. Food Chem 2012 Nov 15;135(2):494-501.
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- 31. A review of animal and human studies for management of benign prostatic hyperplasia with natural products: perspective of new pharmacological agents.
OBJECTIVE:
In this paper, we reviewed plants being effective in treatment of BPH for the purpose of finding new sources of pharmaceutical agents.
METHODS:
All pertinent literature databases were searched. The search keywords were plant, herb, herbal therapy, phytotherapy, benign prostatic hyperplasia, BPH, and prostate. All of the human, animal and in vitro studies were evaluated.
RESULTS:
According to the studies, some of the substantial effective constituents of the plants in treatment of BPH are oenothein B, icaritin, xanthohumol, diarylheptanoid, 2,6,4'-trihydroxy-4-methoxybenzophenone, emodin, fatty acids, atraric acid, n-butylbenzene-sulfonamide, curbicin, theaflavin-3,30-digallate, penta-O-galloyl-b-D-glucose, lycopene, sinalbin, β-sitosterol, secoisolariciresinol diglucoside, genistein, apigenin, baicalein, and daidzein. Besides, Serenoa repens, Pygeum africanum, Curcubita pepo, and Urtica dioica as the most prevalent plants used to treat BPH. S. repens in human studies showed equivalent effectiveness to tamsulosin and in combination to U. dioica revealed equal effects to finastride with less side effects.
CONCLUSION:
There are numerous plants that have beneficial influence on BPH although the mechanisms of action in some plants are not well understood yet. Active ingredients of some of these plants are known and can be used as lead components for development of new effective and safe drugs....(more)
Azimi H, et al. Inflamm Allergy Drug Targets 2012 Jun;11(3):207-21. Review.
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- 32. Herbal infusions as a source of calcium, magnesium, iron, zinc and copper in human nutrition.
The study material consisted of five herbs: chamomile (flowers), mint (leaves), St John's wort (flowers and leaves), sage (leaves) and nettle (leaves), sourced from three producers. The calcium, magnesium, iron, zinc and copper contents were determined for both dried herb samples and prepared infusions, and the extraction rates were calculated. Mineral components were determined using atomic absorption spectrometry. Analysis showed that the contents of individual elements in herbs and infusions depended on the type of raw material, as well as on its origin. Moreover, it was found that iron penetrated the herbal infusions to the lowest degree (4.4-12.4%), while copper did so to the highest (26.7-50.7%). It is felt that in average consumption the herbal infusions are not important as calcium, magnesium, iron, zinc and copper sources in human nutrition....(more)
Suliburska J, et al. Int J Food Sci Nutr 2012 Mar;63(2):194-8.
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- 33. Elemental and structural analysis of silicon forms in herbal drugs using silicon-29 MAS NMR and WD-XRF spectroscopic methods.
The objective of this work was to study concentration of silicon and its structural forms present in herbal drugs. Equisetum arvense and Urtica dioica L. from teapot bags, dietary supplements (tablets and capsules) containing those herbs, dry extract obtained from a teapot bag of E. arvense, and samples of the latter herb harvested in wild habitat over four months were studied using wavelength dispersive X-ray spectroscopy (WD-XRF) and high-resolution solid-state (29)Si NMR. The highest concentration of Si, ca. 27mg/g, was found in the herbal material from the teapot bags containing E. arvense. The Si content in natural E. arvense (whole plants) increased from May to August by ca. 7mg/g, reaching value 26mg/g. Three different silicon forms were detected in the studied herbal samples: Si(OSi)4 (Q(4)), Si(OH)(OSi)3 (Q(3)) and Si(OH)2(OSi)2 (Q(2)). Those sites were populated in E. arvense in the following order: Q(4)Q(3)>Q(2). A dramatic, ca. 50-fold decrease of the Si concentration during the infusion process was observed. The infusion process and the subsequent drying procedure augmented population of the Q(4) sites at the cost of the Q(2) sites. The WD-XRF and (29)Si NMR methods occurred useful and complementary in the study of herbal materials.
Copyright © 2011 Elsevier B.V. All rights reserved....(more)
Pajchel L, et al. J Pharm Biomed Anal 2011 Dec 5;56(4):846-50.
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- 34. Regulation of inflammatory gene expression in PBMCs by immunostimulatory botanicals.
Many hundreds of botanicals are used in complementary and alternative medicine for therapeutic use as antimicrobials and immune stimulators. While there exists many centuries of anecdotal evidence and few clinical studies on the activity and efficacy of these botanicals, limited scientific evidence exists on the ability of these botanicals to modulate the immune and inflammatory responses. Using botanogenomics (or herbogenomics), this study provides novel insight into inflammatory genes which are induced in peripheral blood mononuclear cells following treatment with immunomodulatory botanical extracts. These results may suggest putative genes involved in the physiological responses thought to occur following administration of these botanical extracts. Using extracts from immunostimulatory herbs (Astragalus membranaceus, Sambucus cerulea, Andrographis paniculata) and an immunosuppressive herb (Urtica dioica), the data presented supports previous cytokine studies on these herbs as well as identifying additional genes which may be involved in immune cell activation and migration and various inflammatory responses, including wound healing, angiogenesis, and blood pressure modulation. Additionally, we report the presence of lipopolysaccharide in medicinally prepared extracts of these herbs which is theorized to be a natural and active component of the immunostimulatory herbal extracts. The data presented provides a more extensive picture on how these herbs may be mediating their biological effects on the immune and inflammatory responses....(more)
Denzler KL, et al. PLoS One 2010 Sep 3;5(9):e12561.
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- 35. Herbal supplement use and blood lead levels of United States adults.
BACKGROUND:
Some herbal supplements may contain lead.
OBJECTIVE:
To examine whether use of specific herbal dietary supplements during the last 30 days is associated with blood lead levels in US men and women.
DESIGN:
Cross-sectional analysis.
STUDY POPULATION:
NHANES participants from 1999-2004, a representative sample of the civilian non-institutionalized US population.
MEASUREMENTS:
Lead was measured in blood. Associations between lead and self-reported supplement use were estimated using multivariable regression weighted to account for NHANES sampling. Herbal supplements investigated were those previously reported to contain high heavy metal content: Ayurvedic or traditional Chinese medicine herbs, echinacea, ginkgo, ginseng, St. John's wort, and "other" herbs (specifically, kava, valerian, black cohosh, bee pollen, and nettle).
MAIN RESULTS:
Among 6,712 women > or =20 years, those using herbal supplements had lead levels that were 10% higher than non-users (95% CI 3%-17%, p = 0.005). Women using Ayurvedic or traditional Chinese medicine herbs, St. John's wort, and "other" herbs had lead levels 24% (95% CI 5%-45%, p = 0.01), 23% (95% CI 4%-46%), p = 0.02), and 21% (95% CI 2%-44%, p = 0.03) higher, respectively, than non-users. No significant associations were observed between herb use and lead levels among men (n = 6,095). Among reproductive-aged women (16-45 years), herbal supplement users had lead levels 20% higher than non-users (95% CI 5%-34%, p = 0.008). In contrast, garlic and other dietary supplements were not associated with higher lead levels.
CONCLUSION:
Use of specific herbal supplements is associated with higher blood lead levels among women. Our data suggest testing guidelines for herbal supplements and regulations limiting lead in supplements are needed....(more)
Buettner C, et al. J Gen Intern Med 2009 Nov;24(11):1175-82.
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