- 1. Potential nephrotoxic effects produced by steroidal saponins from hydro alcoholic extract of Tribulus terrestris in STZ induced diabetic rats.
Abstract Chronic hyperglycemia leads to the development of microvascular complications like diabetic nephropathy. The present study investigated the potential effects of the hydroalcoholic extract of Tribulus terrestris, a plant of Zygophyllaceae family, on the renal complications in STZ induced diabetic rats. Diabetes was induced by administering streptozotocin (90mg/kg) to the 2 days old neonates. After 6 weeks of induction, diabetic rats were treated with 50mg/kg hydroalcoholic extract of T. terrestris for 8 weeks. The anti-hyperglycaemic nature was confirmed by reduction in blood glucose and improvement in insulin levels. Diabetic renal injury associated with decrease in total proteins and albumin levels was observed to be improved by T.terrestris extract. Glomerular filtration rate along with inflammatory and growth factors, adiponectin and erythropoietin were also improved by the treatment, though the findings were not significant. However, the beneficial antidiabetic effects of T.terrestris extract in plasma were not observed in kidney histopathology. This was confirmed by the quantitative estimation of unhydrolysed fraction of saponins (major component: protodioscin) in plasma and kidney samples of normal and diabetic rats. Hence, it can be concluded that 8 weeks treatment with T.terrestris extract produces potential toxic effects in kidney, which are independent of its antidiabetic action....(more)
Gandhi S, et al. Toxicol Mech Methods 2013 Apr 18.
Related Products: Protodioscin
- 2. Solanum incanum and S. heteracanthum as sources of biologically active steroid glycosides: confirmation of their synonymy.
A new spirostanol saponin (1), along with four known saponins, dioscin (2), protodioscin (3), methyl-protodioscin (4), and indioside D (5), and one known steroid glycoalkaloid solamargine (6) were isolated from the two synonymous species, Solanum incanum and S. heteracanthum. The structure of the new saponin was established as (23S,25R)-spirost-5-en-3β,23-diol 3-O-{β-D-xylopyranosyl-(1→2)-O-α-L-rhamnopyranosyl-(1→4)-[O-α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside}, by using a combination of 1D and 2D NMR techniques including (1)H, (13)C, COSY, TOCSY, NOESY, HSQC and HMBC experiments and by mass spectrometry. The compounds 1, 3, 4 and 5 were evaluated for cytotoxicity against five cancer cell lines and for antioxidant and cytoprotective activity....(more)
Manase MJ, et al. Fitoterapia 2012 Sep;83(6):1115-9.
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- 3. Fenugreek with reduced bitterness prevents diet-induced metabolic disorders in rats.
BACKGROUND:
Various therapeutic effects of fenugreek (Trigonella foenum-graecum L.) on metabolic disorders have been reported. However, the bitterness of fenugreek makes it hard for humans to eat sufficient doses of it for achieving therapeutic effects. Fenugreek contains bitter saponins such as protodioscin. Fenugreek with reduced bitterness (FRB) is prepared by treating fenugreek with beta-glucosidase. This study has been undertaken to evaluate the effects of FRB on metabolic disorders in rats.
METHODS:
Forty Sprague-Dawley rats were fed with high-fat high-sucrose (HFS) diet for 12 week to induce mild glucose and lipid disorders. Afterwards, the rats were divided into 5 groups. In the experiment 1, each group (n = 8) was fed with HFS, or HFS containing 2.4% fenugreek, or HFS containing 1.2%, 2.4% and 4.8% FRB, respectively, for 12 week. In the experiment 2, we examined the effects of lower doses of FRB (0.12%, 0.24% and 1.2%) under the same protocol (n = 7 in each groups).
RESULTS:
In the experiment 1, FRB dose-dependently reduced food intake, body weight gain, epididymal white adipose tissue (EWAT) and soleus muscle weight. FRB also lowered plasma and hepatic lipid levels and increased fecal lipid levels, both dose-dependently. The Plasma total cholesterol levels (mmol/L) in the three FRB and Ctrl groups were 1.58 ± 0.09, 1.45 ± 0.05*, 1.29 ± 0.07* and 2.00 ± 0.18, respectively (*; P < 0.05 vs. Ctrl). The Hepatic total cholesterol levels (mmol/g liver) were 0.116 ± 0.011, 0.112 ± 0.006, 0.099 ± 0.007* and 0.144 ± 0.012, respectively (*; P < 0.05 vs. Ctrl). The calculated homeostasis model assessment as an index of insulin resistance (HOMA-IR) indicated 0.52 ± 0.04*, 0.47 ± 0.06*, 0.45 ± 0.05* and 1.10 ± 0.16, respectively (*; P < 0.05 vs. Ctrl). None of the FRB groups showed any adverse effect on the liver, kidney or hematological functions. In the experiment 2, no significant difference of food intake was observed, while the 1.2% FRB group alone showed nearly the same effects on glucose and lipid metabolism as in the experiment 1.
CONCLUSIONS:
Thus we have demonstrated that FRB (1.2 ~ 4.8%) prevents diet-induced metabolic disorders such as insulin resistance, dyslipidemia and fatty liver....(more)
Muraki E, et al. Lipids Health Dis 2012 May 29;11:58.
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- 4. Effects of various asparagus production methods on rutin and protodioscin contents in spears and cladophylls.
The purpose of this study was to clarify the relationship between various cultivation conditions and the amounts of the rutin (RT) and protodioscin (PD) in asparagus spears. Green and white spears were grown in open culture and under two different blanching conditions. Although RT was detected only in the green spears, PD was detected mainly in white spears produced by covering with soil. The RT and PD contents of cladophylls grown in an open field and in a closed cultivation system were also investigated, and the closed system resulted in cladophylls with low RT and high PD, unlike the open field....(more)
Motoki S, et al. Biosci Biotechnol Biochem 2012;76(5):1047-50.
Related Products: Protodioscin
- 5. The effect of fenugreek on the gene expression of arachidonic acid metabolizing enzymes.
The main bioactive compounds of Trigonella foenum graecum L. (fenugreek) seeds are protodioscin, trigoneoside, diosgenin and yamogenin, which have anticarcinogenic potency through inhibition of cell proliferation and inhibition of prostaglandin synthesis. The effect of fenugreek on ALOX and COX genes was examined in AKR/J H-2(k) mice exposed to dimethylbenz[α]anthracene (DMBA), a potent carcinogen. The expression pattern of these genes was determined by detecting the mRNA expression in various tissues (the lungs, liver, spleen and the kidneys) in four groups of mice. Two groups were fed with normal and two of them with fenugreek containing nutriment. Each group divided into DMBA treated and control groups. Mice were autopsied on day 7 after DMBA treatment for mRNA isolation. Fenugreek consumption itself did not change gene expression compared with the control group. DMBA could increase the expression of ALOX12, ALOX15, ALOX5 genes mainly in all organs. Fenugreek consumption was generally protective in each organ in a different manner. DMBA treatment increased COX2 gene expression, but fenugreek was protective in all tissues examined. In COX1 gene, the fenugreek diet could suppress the expression, except for spleen, independently from carcinogen exposure. Therefore by inhibiting the arachidonic acid metabolism fenugreek may prevent tumorigenesis....(more)
Varjas T, et al. Phytother Res 2011 Feb;25(2):221-7.
Related Products: Protodioscin
- 6. Differential activity of multiple saponins against omnivorous insects with varying feeding preferences.
A variety of glycosylated and unglycosylated saponins from seven different plant families (Aquifoliaceae, Asparagaceae, Caryophyllaceae, Dioscoreaceae, Leguminosae, Rosaceae, Sapindaceae) were tested against the corn earworm, Helicoverpa zea, and the fall armyworm, Spodoptera frugiperda. The corn earworm feeds readily on both monocots and dicots, while the fall armyworm is primarily a grass feeder. Most of the saponins were similarly effective or ineffective against both insect species, with the glycosides being the primary active form (compared to aglycones). However, one aglycone possessed antifeedant properties toward the fall armyworm. Thus, in contrast to many plant secondary metabolites effective against either of these two species where the aglycone is more effective, in the case of the saponins the opposite is generally true. This appears to be a contradictory strategy of plant defenses that requires further consideration. The activity of protodioscin against insects is reported for the first time and may be important in insect defense by the bioenergy crop switchgrass....(more)
Dowd PF, et al. J Chem Ecol 2011 May;37(5):443-9.
Related Products: Protodioscin
- 7. Relative feeding and development of armyworm on switchgrass and corn, and its potential effects on switchgrass grown for biomass.
To help assess the potential for damage by armyworms [Mythimna (Pseudaletia) unipuncta (Haworth) (Lepidoptera: Noctuidae)] to switchgrass (Panicum virgatum L.) and surrounding crops, survival and development were evaluated for larvae reared on leaves of switchgrass, corn (Zea mays L.), and miscanthus (Miscanthus x giganteus Greef and Deuter ex Hodkinson and Renvoize). Additional tests assessed the relationship between leaf position and the concentration of saponins (plant compounds which can provide protection from insect herbivores) and examined the effect of defoliation on switchgrass dry mass. Survival to adulthood was similar when larvae were reared on field-grown leaves of switchgrass and corn. However, lower larval mass (10 d) and delayed development of M. unipuncta (to pupation, adult emergence) suggest switchgrass is an inferior host relative to corn. When fed field-grown miscanthus, no larvae survived 10 d. Few differences were noted between switchgrass and corn grown under controlled (laboratory) conditions, but M. unipuncta survival seemed to decline rapidly when larvae were fed the fourth and fifth leaves of switchgrass. Switchgrass leaf samples collected from different leaf positions and stages of tiller maturity showed up to 10-fold differences in the concentration of the saponin protodioscin, with the greatest concentrations in the fourth and fifth leaves. However, other saponins showed an opposite pattern, indicating the role of protodioscin on insect development should be tested in isolation (e.g., by addition of the purified compound to an artificial diet). Defoliation trials indicated that extremely high M. unipuncta populations may be necessary to cause any significant reduction in switchgrass biomass. Collectively, results suggest M. unipuncta may not present a significant risk to biomass production in switchgrass, but that the spring emergence of switchgrass provides an alternate host for M. unipuncta before colonizing annual food and feed crops....(more)
Prasifka JR, et al. J Econ Entomol 2011 Oct;104(5):1561-7.
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- 8. The osteoprotective effect of psoralen in ovariectomy-induced osteoporotic rats via stimulating the osteoblastic differentiation from bone mesenchymal stem cells.
OBJECTIVE:
Psoralea corylifolia extract has been reported to promote bone formation in osteoporotic animals. Psoralen (PSO), a flavonoid glycoside, as the active component of P corylifolia L, is effective in increasing new bone-forming osteoblasts in parietal bone defects. However, the effect and molecular mechanisms of PSO on bone mesenchymal stem cells (bMSCs) in the osteoporotic state are widely unknown. This study was designed to evaluate the osteoprotective effect of PSO in ovariectomy (OVX)-induced rats and to seek possible molecular mechanisms of PSO in bMSCs.
METHODS:
We observed the osteogenic effect of PSO (3-month treatment) on osteoporotic rat models induced by OVX via testing bone densitometry, histomorphometries, and immunohistochemistry in vivo. Alkaline phosphatase staining and colony-forming unit-fibroblast and colony-forming unit-adipocyte assays were performed to evaluate the differentiation potential of bMSCs ex vivo. In addition, the molecular targets of PSO in bMSCs were detected by stem cell microarray analysis of 256 genes and confirmed by real-time reverse transcription-polymerase chain reaction.
RESULTS:
Micro-CT morphometry analysis showed that PSO significantly improved bone mass indicators including increased trabecular thickness and decreased trabecular space. Meanwhile, PSO elevated the well-known osteogenic marker osteocalcin level in OVX-induced osteoporotic rats. Next, in ex vivo studies, we revealed that PSO facilitated alkaline phosphatase staining and increased the colony-forming unit-fibroblasts. Based on gene expression profile analysis, we screened a set of genes dysregulated in OVX but reversed by PSO treatment. These genes were highly enriched in the Notch signaling pathway, which was documented to play a role in bMSC differentiation.
CONCLUSIONS:
Our findings show that PSO promotes bone mass in OVX-induced osteoporotic rats. This effect of PSO is highly related to the stimulation of differentiation of bMSCs to osteoblasts....(more)
Yang Z, et al. Menopause 2012 Oct;19(10):1156-64.
Related Products: Psoralea Corylifolia Extract
- 9. Psoralea corylifolia extract ameliorates experimental osteoporosis in ovariectomized rats.
We evaluated the protective effect of Psoralea corylifolia L. (PCL) extract on the ovariectomized (OVX) rat model. The biochemical markers of bone turnover, calcium metabolism, and calcium balance were examined. PCL extract (25 mg or 50 mg/kg body weight/day) was orally administrated to OVX rats for 3 months. PCL extract did not alter weight gain or uterus weight in OVX rats. PCL extract significantly increased serum Ca (calcium) levels (p < 0.05, vs. OVX group) as well as decreased urinary Ca excretion (p < 0.05 vs. OVX group) in OVX rats. The upregulation of serum osteocalcin level by ovariectomy was suppressed by treatment with PCL extract in rats (p < 0.05, vs. OVX group). PCL extract increased bone mineral density at 50 mg/kg body weight/day in OVX rats (p < 0.05, vs. OVX group). Our results indicate that orally administrated PCL extract can decrease urinary calcium excretion and decrease serum osteocalcin in OVX rats, resulting in positive effects on bone mineral density as well as bone formation. In conclusion, our studies showed that PCL might be a potential candidate for treatment of postmenopausal osteoporosis....(more)
Tsai MH, et al. Am J Chin Med 2007;35(4):669-80.
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- 10. The inhibitory effect of pterostilbene on inflammatory responses during the interaction of 3T3-L1 adipocytes and RAW 264.7 macrophages.
Chronic inflammation is characterized by the upregulation of proinflammatory cytokines in obese adipose tissue. Accumulations of adipose tissue macrophages enhance a chronic inflammatory state in adipose tissues. Many studies have indicated that the adipocyte-related inflammatory response in obesity is characterized by an enhanced infiltration of macrophages. The aim of this work was to study the inhibitory effects of garcinol and pterostilbene on the change in inflammatory response due to the interaction between 3T3-L1 adipocytes and RAW 264.7 macrophages. In the TNF-α-induced 3T3-L1 adipocyte model, garcinol and pterostilbene significantly decreased the mRNA expression of COX-2, iNOS, IL-6, and IL-1β and IL-6 secretion by suppressing phosphorylation of p-IκBα and p-p65. In a coculture model of 3T3-L1 adipocytes and RAW 264.7 macrophages, pterostilbene suppressed IL-6 and TNF-α secretion and proinflammatory mRNA expression and also reduced the migration of macrophages toward adipocytes. In the RAW 264.7 macrophage-derived conditioned medium (RAW-CM)-induced 3T3-L1 adipocyte and 3T3-CM-induced RAW 264.7 macrophage models, pterostilbene significantly decreased IL-6 and TNF-α secretion and proinflammatory mRNA expression (COX-2, iNOS, IL-6, TNF-α, PAI-1, CRP, MCP-1, resistin, and leptin). Our findings suggest that garcinol and pterostilbene may provide novel and useful applications to reduce the chronic inflammatory properties of adipocytes. We also found that pterostilbene inhibits proinflammatory responses during the interaction between 3T3-L1 adipocytes and RAW 264.7 macrophages....(more)
Hsu CL, et al. J Agric Food Chem 2013 Jan 23;61(3):602-10.
Related Products: Pterostilbene
- 11. Pterostilbene exerts antitumor activity against human osteosarcoma cells by inhibiting the JAK2/STAT3 signaling pathway.
Osteosarcoma is a high-grade malignant bone tumor. Pterostilbene (PTE) is a natural, dimethylated analog of resveratrol with higher bioavailability. While PTE has been shown to have potent antitumor activity against various types of cancer, the molecular mechanisms underlying the effects of PTE remain largely unknown. The Janus kinase 2/Signal Transducer and Activator of Transcription 3 (JAK2/STAT3) signaling pathway plays a crucial role in tumorigenesis and immune development. In this study, we assessed the antitumor activity of PTE against human osteosarcoma cells and explored the role of JAK2/STAT3 and apoptosis-related signaling pathways on the activity of PTE. PTE treatment resulted in a dose- and time-dependent inhibition of osteosarcoma cell viability. Additionally, PTE exhibited strong antitumor activity, as evidenced not only by reductions in tumor cell adhesion, migration and mitochondrial membrane potential (MMP) but also by increases in the apoptotic index, reactive oxygen species (ROS) and several biochemical parameters. Furthermore, PTE treatment directly inhibited the phosphorylation of JAK2 at Tyr 1007 and the downstream activation of STAT3. PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27. PTE, used in combination with a known JAK2/STAT3 inhibitor, AG490, further decreased the viability of osteosarcoma cells. Taken together, PTE is a potent inhibitor of osteosarcoma cell growth that targets the JAK2/STAT3 signaling pathway. These data suggest that inhibition of JAK2/STAT3 signaling is a novel mechanism of action for PTE during therapeutic intervention in osteosarcoma cancers....(more)
Liu Y, et al. Toxicology 2013 Feb 8;304:120-31.
Related Products: Pterostilbene
- 12. Growth inhibitory effect of grape phenolics against wine spoilage yeasts and acetic acid bacteria.
This paper investigates the in vitro antimicrobial potential of 15 grape phenolic compounds of various chemical classes (phenolic acids, stilbenes and flavonoids) using the broth microdilution method against yeasts and acetic acid bacteria frequently occurring in deteriorated wine. Pterostilbene (MICs=32-128 μg/mL), resveratrol (MICs=256-512 μg/mL) and luteolin (MICs=256-512 μg/mL) are among six active compounds that possessed the strongest inhibitory effects against all microorganisms tested. In the case of phenolic acids, myricetin, p-coumaric and ferulic acids exhibited selective antimicrobial activity (MICs=256-512 μg/mL), depending upon yeasts and bacteria tested. In comparison with potassium metabisulphite, all microorganisms tested were more susceptible to the phenolics. The results revealed the antibacterial and antiyeast effects against wine spoilage microorganisms of several highly potent phenolics naturally occurring in grapes. These findings also provide arguments for further investigation of stilbenes as prospective compounds reducing the need for the use of sulphites in winemaking....(more)
Pastorkova E, et al. Int J Food Microbiol 2013 Feb 15;161(3):209-13.
Related Products: Pterostilbene
- 13. Pterostilbene inhibits dimethylnitrosamine-induced liver fibrosis in rats.
Pterostilbene, found in grapes and berries, exhibits pleiotropic effects, including anti-inflammatory, antioxidant, and anti-proliferative activities. This study was conducted to investigate the effect of pterostilbene on liver fibrosis and the potential underlying mechanism for such effect. Sprague-Dawley rats were intraperitoneally given dimethyl n-nitrosamine (DMN) (10mg/kg) 3 days per week for 4 weeks. Pterostilbene (10 or 20mg/kg) was administered by oral gavage daily. Liver function, morphology, histochemistry, and fibrotic parameters were examined. Pterostilbene supplementation alleviated the DMN-induced changes in the serum levels of alanine transaminase and aspartate transaminase (p<0.05). Fibrotic status and the activation of hepatic stellate cells were improved upon pterostilbene supplementation as evidenced by histopathological examination as well as the expression of α-smooth muscle actin (α-SMA), transforming growth factor-β1 (TGF-β1), and matrix metalloproteinase 2 (MMP2). These data demonstrated that pterostilbene exhibited hepatoprotective effects on experimental fibrosis, potentially by inhibiting the TGF-β1/Smad signaling....(more)
Lee MF, et al. Food Chem 2013 Jun 1;138(2-3):802-7.
Related Products: Pterostilbene
- 14. Pterostilbene and its emerging antineoplastic effects: a prospective treatment option for systemic malignancies.
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- 15. Invadopodia-associated proteins blockade as a novel mechanism for 6-shogaol and pterostilbene to reduce breast cancer cell motility and invasion.
SCOPE:
Invadopodia are actin-rich membrane protrusions of tumor cells that are thought to initiate the local migration and invasion during cancer metastasis. The blockade of invadopodia-associated proteins has been reported as a promising approach for prevention of tumor metastasis. The aim of this study was to investigate the modulatory effects of 6-shogaol and pterostilbene on invadopodia in aggressive breast cancer cells.
METHODS AND RESULTS:
By wound-healing, transwell, and gelatin zymography assays, we found that 6-shogaol and pterostilbene effectively attenuated the motility and invasion of MDA-MB-231 cells, and suppressed the activities of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9). Further investigation into the underlying molecular mechanisms revealed that the levels of key modulators of invadopodium maturation, including c-Src kinase, cortactin, and membrane type 1-matrix metalloproteinase (MT1-MMP) decreased when cells were treated with 6-shogaol or pterostilbene.
CONCLUSION:
These data suggest that the repression of these factors might affect the maturation of invadopodia, inhibiting the metastasis of MDA-MB-231 cells. In conclusion, the present study demonstrates for the first time that 6-shogaol and pterostilbene can inhibit invadopodium formation and MMP activity in highly invasive breast cancer cells. We suggest that these compounds may be clinically useful in chemopreventive treatments for metastatic breast cancer.
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Hong BH, et al. Mol Nutr Food Res 2013 May;57(5):886-95.
Related Products: Pterostilbene
- 16. Pharmacokinetics of pterostilbene in Sprague-Dawley rats: The impacts of aqueous solubility, fasting, dose escalation, and dosing route on bioavailability.
SCOPE:
Pterostilbene (trans-3,5-dimethoxy-4'-hydroxystilbene, PTS) possesses various health-promoting effects. This study aimed to investigate the impacts of aqueous solubility, fasting, dose escalation, and dosing route on its bioavailability in Sprague-Dawley rats.
METHODS AND RESULTS:
Upon intravenous administration (2.5 mg/kg), PTS had rapid clearance (Cl = 68.2 ± 9.8 mL/min/kg) and moderate terminal elimination half-life (t(1/2λz) = 93.9 ± 22.3 min). Dose-escalation led to about twofold decline in clearance at the dose of 25 mg/kg (Cl = 36.4±7.8 mL/min/kg). When given in oral suspension (15 mg/kg), PTS had relatively low bioavailability (F = 15.9 ± 7.8%) while fasting substantially attenuated its bioavailability (F< 5.5 %). However, when dosed in a solution formulated with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) (15 mg/kg), PTS possessed good bioavailability (F = 59.2 ± 19.6%). Dose escalation resulted in about twofold increase in bioavailability at the dose of 60 mg/kg. Sublingual delivery (2.5 mg/kg) led to rapid absorption and moderate bioavailability (F = 25.8 ± 13.1%). Statistical comparison clearly indicated that the pharmacokinetics of PTS was more favorable than resveratrol.
CONCLUSION:
Aqueous solubility was identified as a barrier to its oral bioavailability while solubilizing PTS with HP-β-CD substantially increased its bioavailability; dose manipulation was a practical strategy to enhance its bioavailability and systemic exposure; and its delivery through oral mucosa was feasible. As PTS possessed superior pharmacokinetics, it is a favorable candidate for further development.
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Yeo SC, et al. Mol Nutr Food Res 2013 Feb 18.
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- 17. Analysis of safety from a human clinical trial with pterostilbene.
Objectives. The purpose of this trial was to evaluate the safety of long-term pterostilbene administration in humans. Methodology. The trial was a prospective, randomized, double-blind placebo-controlled intervention trial enrolling patients with hypercholesterolemia (defined as a baseline total cholesterol ≥200 mg/dL and/or baseline low-density lipoprotein cholesterol ≥100 mg/dL). Eighty subjects were divided equally into one of four groups: (1) pterostilbene 125 mg twice daily, (2) pterostilbene 50 mg twice daily, (3) pterostilbene 50 mg + grape extract (GE) 100 mg twice daily, and (4) matching placebo twice daily for 6-8 weeks. Safety markers included biochemical and subjective measures. Linear mixed models were used to estimate primary safety measure treatment effects. Results. The majority of patients completed the trial (91.3%). The average age was 54 years. The majority of patients were females (71%) and Caucasians (70%). There were no adverse drug reactions (ADRs) on hepatic, renal, or glucose markers based on biochemical analysis. There were no statistically significant self-reported or major ADRs. Conclusion. Pterostilbene is generally safe for use in humans up to 250 mg/day....(more)
Riche DM, et al. J Toxicol 2013;2013:463595.
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- 18. Pterostilbene acts through metastasis-associated protein 1 to inhibit tumor growth, progression and metastasis in prostate cancer.
The development of natural product agents with targeted strategies holds promise for enhanced anticancer therapy with reduced drug-associated side effects. Resveratrol found in red wine, has anticancer activity in various tumor types. We reported earlier on a new molecular target of resveratrol, the metastasis-associated protein 1 (MTA1), which is a part of nucleosome remodeling and deacetylation (NuRD) co-repressor complex that mediates gene silencing. We identified resveratrol as a regulator of MTA1/NuRD complex and re-activator of p53 acetylation in prostate cancer (PCa). In the current study, we addressed whether resveratrol analogues also possess the ability to inhibit MTA1 and to reverse p53 deacetylation. We demonstrated that pterostilbene (PTER), found in blueberries, had greater increase in MTA1-mediated p53 acetylation, confirming superior potency over resveratrol as dietary epigenetic agent. In orthotopic PCa xenografts, resveratrol and PTER significantly inhibited tumor growth, progression, local invasion and spontaneous metastasis. Furthermore, MTA1-knockdown sensitized cells to these agents resulting in additional reduction of tumor progression and metastasis. The reduction was dependent on MTA1 signaling showing increased p53 acetylation, higher apoptotic index and less angiogenesis in vivo in all xenografts treated with the compounds, and particularly with PTER. Altogether, our results indicate MTA1 as a major contributor in prostate tumor malignant progression, and support the use of strategies targeting MTA1. Our strong pre-clinical data indicate PTER as a potent, selective and pharmacologically safe natural product that may be tested in advanced PCa....(more)
Li K, et al. PLoS One 2013;8(3):e57542.
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- 19. Pterostilbene, a bioactive component of blueberries, suppresses the generation of breast cancer stem cells within tumor microenvironment and metastasis via modulating NF-κB/microRNA 448 circuit.
SCOPE:
Tumor-associated macrophages (TAMs) have been shown to promote metastasis and malignancy. Pterostilbene, a natural stilbene isolated from blueberries, has been suggested for anti-cancer effects. Here, we explored the potential cancer stem cells (CSCs)/TAM modulating effects of pterostilbene in breast cancer.
METHODS AND RESULTS:
Using flowcytometric and Boyden chamber assay, we showed MCF7 and MDA-MB-231 cells cocultured with M2 TAMs exhibited increased percentage of CD44<sup>+</sup> /CD24<sup>-</sup> CSC population and migratory/invasive abilities. RT-PCR results showed that CD44<sup>+</sup> /CD24<sup>-</sup> cells expressed an increased level of HIF-1α, β-catenin, Twist1, and NF-κB and enhanced tumor sphere forming ability. Additionally, pterostilbene treatment dose dependently overcame M2 TAM-induced enrichment of CSCs and metastatic potential of breast cancer cells. Mechanistically, pterostilbene suppressed NFκB, Twist1, vimentin, and increased E-cadherin expression. Using siRNA technique, we demonstrated that pterostilbene-mediated NFκB downregulation was correlated to an increased amount of microRNA 448. Finally, pterostilbene-mediated suppression in tumorigenesis and metastasis was validated by noninvasive bioluminescence in mice bearing M2 TAM cocultured MDA-MB-231 tumor.
CONCLUSION:
Pterostilbene effectively suppresses the generation of CSCs and metastatic potential under the influence of M2 TAMs via modulating EMT associated signaling pathways, specifically NF-κB/miR488 circuit. Thus, pterostilbene could be an ideal anti-CSC agent in clinical settings.
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Mak KK, et al. Mol Nutr Food Res 2013 Mar 15.
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- 20. Antiobesity effects of Chinese black tea (Pu-erh tea) extract and gallic acid.
The antiobesity effects of Chinese black tea (Pu-erh tea) and of gallic acid (GA) were investigated using in vitro and in vivo assays. Chinese black tea extract (BTE) and GA inhibited pancreatic lipase activity in a dose-dependent manner in vitro; the IC(inhibitory concentration)(50) values were 101.6 and 9.2 µg/mL, respectively. Black tea extract (50, 100 mg/kg body weight (b.w.)) and GA (15, 45 mg/kg b.w.) significantly suppressed the elevation of blood triglyceride after oral administration of a corn oil emulsion (8 mL oil/kg b.w.) to male ddY mice. Moreover, the antiobesity effects of BTE and GA were also evaluated in a mouse model of diet-induced obesity. Female ddY mice were divided into seven groups; normal diet (ND) group, high fat diet (HFD) group, BTE (0.2% and 0.6% of diets) groups, and GA (0.007%, 0.02% and 0.1% of diets) groups; the experimental groups were fed the test diets for 12 weeks. The BTE 0.6% and GA 0.1% groups showed significant suppression of weight gain. The weight of parametrial adipose tissue was strongly correlated with the body weight. These results suggest that GA contributes to the antiobesity effect of BTE as an active constituent by inhibiting pancreatic lipase activity....(more)
Oi Y, et al. Phytother Res 2012 Apr;26(4):475-81.
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- 21. Effect of pu-erh tea on body fat and lipid profiles in rats with diet-induced obesity.
The antiobesity and antihyperlipidaemic effects of pu-erh tea in rats with high fat diet (HFD)-induced obesity were investigated. Male Sprague-Dawley rats were randomly divided into five groups and fed varying diets for an 8-week period: control diet, HFD, and HFD supplemented with low, moderate or high doses of pu-erh tea extract (0.5 g, 2 g and 4 g/kg BW/day, respectively). Pu-erh tea significantly reduced the total body weight and the weight of various adipose pads. Pu-erh tea administration also significantly lowered plasma total cholesterol, triglyceride concentrations and low-density lipoprotein-cholesterol levels in rats with HFD-induced obesity, but did not affect high-density lipoprotein-cholesterol levels. Moreover, pu-erh tea significantly increased lipoprotein lipase, hepatic lipase and hormone-sensitive lipase activities in epididymal fat tissue in rats with HFD-induced obesity. Analysis of real-time reverse transcription-polymerase chain reaction results indicated that pu-erh tea significantly enhanced mRNA levels of hormone-sensitive lipase in rats with HFD-induced obesity. These results suggest that pu-erh tea attenuated visceral fat accumulation and improved hyperlipidemia in a rat model of HFD-induced obesity....(more)
Cao ZH, et al. Phytother Res 2011 Feb;25(2):234-8.
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- 22. Improvements of mean body mass index and body weight in preobese and overweight Japanese adults with black Chinese tea (Pu-Erh) water extract.
Water-soluble black Chinese (Pu-Erh) tea extract (BTE), which contains high gallic acid content, has been demonstrated to elicit antiobese effects in animals. Because gallic acid is related with the reduction of visceral fat and cholesterol contents and improvement of obesity in animals, we investigated the effects of BTE intake on 36 preobese Japanese adults (body mass index [BMI], >25- <30 kg/m(2)) in a 12-week double-blind, randomized, placebo-controlled group comparison study using powdered barley tea with or without (placebo) BTE. A follow-up 4-week period after BTE intake termination was monitored to observe the withdrawal effect. All subjects ingested barley tea with or without BTE (333 mg) before each of the 3 daily meals. In the BTE-treated group, the mean pretreament values of body weight and BMI significantly decreased after intake and after BTE withdrawal. However, the corresponding values scored significant differences only from 8 weeks after intake (vs the placebo-treated group). The mean values of the waist circumference indicated a similar tendency. Furthermore, coronal navel section (same anatomical position) images of computed tomography of all BTE- and non-BTE-treated subjects revealed that the visceral fat areas (cm(2)) were significantly (P < .05) less in the former 12 weeks after BTE ingestion. Measured biochemical parameters did not indicate significant differences, and BTE-treated subjects did not complain of any adverse effects (abdominal distension, etc). Ingestion of BTE exhibited significant effects in reducing the mean waist circumference, BMI, and visceral fat values and might be useful for weight control and prevention of obesity development (or metabolic syndrome) in humans....(more)
Kubota K, et al. Nutr Res 2011 Jun;31(6):421-8.
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- 23. Pu-erh tea aqueous extracts lower atherosclerotic risk factors in a rat hyperlipidemia model.
Pu-erh tea is believed to possess many beneficial health effects since it is a natural source of cardioprotective lipid lowering and antioxidant compounds, although, the major constituents putatively responsible for these beneficial effects remain unknown. In this study, we examined the effects of two commonly consumed forms of Pu-erh tea, fermented and unfermented, on weight gain, serum levels of lipids and lipoprotein, lipid oxidation, and blood antioxidant enzymes in a rat hyperlipidemia model. Hyperlipidemic rats were treated with water extracts of either 0.5, 1.5 or 3.0 mg/kg fermented or unfermented Pu-erh tea. Serum low density lipoprotein-cholesterol (LDL-C) and triglyceride levels were significantly lowered by tea extract compared to the control group. (p < 0.05) and in most cases were indistinguishable from rats fed normal chow, basal diet. Conversely, levels of high density lipoprotein-cholesterol (HDL-C) were elevated in the groups given daily doses of tea extract (p < 0.05). Compared to the hyperlipidemic control group, activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in serum were significantly elevated in Pu-erh tea-treated groups while levels of malondiadehyde (a byproduct of lipid peroxidation) decreased in the same groups. These effects were most pronounced in the groups treated with the highest dose of fermented Pu-erh tea extract. Our results suggest that Pu-erh tea exerts strong antioxidative and lipid-lowering effects and therefore can be used to reduce the risk of cardiovascular disorders....(more)
Hou Y, et al. Exp Gerontol 2009 Jun-Jul;44(6-7):434-9.
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- 24. Effect of microbial fermentation on content of statin, GABA, and polyphenols in Pu-Erh tea.
Besides cancer prevention, the hypolipidemic effects of tea have been well studied in animals and humans. Recently, statin has been identified in Pu-erh tea extract. Clinical trials have confirmed that statin decreases the incidence of major coronary and cerebrovascular events and this may be due to its hypolipidemic and antiinflammatory effects. Since a good Pu-erh tea needs longer storage (10 years or more) of fermentation to enhance the flavor and fragrance, we screened microorganisms from two Pu-erh teas, 20 and 25 years old. Species of fungi and bacteria strains that contributed to a good taste of Pu-erh tea were isolated. The effect of fermentation was investigated by inoculating fresh tea leaves with individual strains of isolated microorganisms. Results showed that statin, total polyphenol content, and the scavenging activities of alpha,alpha-diphenyl-beta-picrylhydrazyl (DPPH) radicals increased during fermentation. Tea leaves inoculated with Streptomyces bacillaris strain R9 had the highest polyphenol content (3.3 mg/100 g) and scavenging ability to DPPH radicals (92%). Streptomyces cinereus strain Y11 was equally good for polyphenol content but yielded the highest amount of statin (1012 ng/g) after 42 days of fermentation. Interestingly, the statin content of fresh tea leaves fermented with strain R9 or Y11 after 180 days was much higher (4- and 8-fold, respectively) than that of the 25-year-old Pu-erh tea (513 ng/g) as measured by the HPLC method. Similarly, these two strains also increased the content of gamma-aminobutyric acid (GABA) 5.7- and 4.7-fold in tea fermented for 180 days as compared with the fresh leaves (1270 microg/g) and that were higher than that of the Pu-erh tea (4900 microg/g). Taken together, the present results indicate that tea short-term fermented with S. bacillaris or S. cinereus enhances the color and content of statin, GABA, and polyphenols....(more)
Jeng KC, et al. J Agric Food Chem 2007 Oct 17;55(21):8787-92.
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- 25. Simultaneous determination of gastrodin and puerarin in rat plasma by HPLC and the application to their interaction on pharmacokinetics.
Gastrodin (Gas) and puerarin (Pur) are bioactive substances derived from traditional Chinese medicine Gastrodia elata and Radix Puerariae, respectively, which were often used together in Chinese clinical prescriptions. Their injections were used in combined way for treatment of some cardiocerebrovascular diseases in clinic, especially for vertigo due to vertebrobasilar ischemia. In this paper, interaction of gastrodin and puerarin in rat plasma pharmacokinetics via intragastic (i.g.)/intravenous (i.v.) administration was investigated. A reliable HPLC method was developed for simultaneous determination of Gas and Pur in rat plasma with a linear range of 0.101-101 μg/mL for Gas and 0.0500-5.98 μg/mL for Pur (r(2)>0.993). The LLOQ, LOD of Gas and Pur were determined to be 0.101, 0.0486 μg/mL, and 0.05, 0.0245 μg/mL, respectively. The intra-day and inter-day precision were all less than 12.0%, whilst the accuracy were all within 96.4±6.00%. The proposed method has been successfully applied to the pharmacokinetic study of the analytes in rats after i.g./i.v. administration of Gas and Pur alone or combined with each other (i.g.: 40 mg/kg Gas, 400 mg/kg Pur; i.v.: 20 mg/kg Gas, 20 mg/kg Pur). Blood samples were collected from retinal vein plexus of rats at predetermined time points and plasma containing the internal standard tyrosol (IS) were precipitated by methanol and chromatography was carried out on a C(18) column with a gradient mobile phase of ACN-H(2)O with 0.05% phosphoric acid as a modifier. The pharmacokinetic profiles of combined administration were found to be distinct from those of given alone. The C(max), T(max), T(1/2), MRT of Gas administrated alone or combined with Pur via i.g. were 21.7 μg/mL, 0.250 h, 2.81 h, 0.830 h and 18.4 μg/mL, 0.550 h, 0.970 h, 1.37 h, respectively, of Pur administrated alone or combined with Gas via i.g. were 0.490 μg/mL, 1.95 h, 1.33 h, 2.10 h and 2.01 μg/mL, 0.570 h, 4.00 h, 5.10 h, respectively. The relative oral bioavailability of Pur in combined administration was 10.7 times as much as that of single administration, whilst 1.52 folds in Gas. These results indicate that co-administration of Gas and Pur is a promising combination to gain higher bioavailability and it is suggested that doctors pay more attention to the dosages of the two when simultaneously using both of them....(more)
Jiang L, et al. J Chromatogr B Analyt Technol Biomed Life Sci 2013 Feb 1;915-916:8-12.
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- 26. Protective effects of puerarin on experimental chronic lead nephrotoxicity in immature female rats.
Puerarin (PU), a natural flavonoid, has been reported to possess anti-oxidative and anti-inflammatory activities. In the present study, female Sprague-Dawley rats received lead (Pb) nitrate (300 mg/L, via drinking water) and/or PU (400 mg/kg/day, orally) to investigate the protective effects of PU on Pb-induced renal damage. Renal toxicity was evaluated by detecting urinary proteins excretion as well as levels of serum urea nitrogen and serum creatinine. Ultrastructural observations and real-time quantitative polymerase chain reaction analyses were performed on kidney cortex tissues to identify the mitochondrial damage and quantify gene expression levels of cytochrome oxidase submits (COX-I/II/III), respectively. Renal cell damage was assessed by light microscopic examination. Lipid peroxidation (LPO) levels and antioxidant status in kidney were also evaluated. Animals that received both Pb and PU showed a better renal function than those that received Pb alone, with minor pathological damage. Moreover, PU significantly reduced LPO and markedly restored the enzymatic and non-enzymatic antioxidants levels in kidney of Pb-treated rats, which may be related to its restoring mitochondrial function. Furthermore, PU administration significantly increased urinary Pb excretion and decreased its level in the serum and kidney. In conclusion, these results suggested that PU reduces renal damage induced by chronic Pb administration through its antioxidant properties and chelating ability....(more)
Wang L, et al. Hum Exp Toxicol 2013 Feb;32(2):172-85.
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- 27. Enzymatic cleavage of the C-glucosidic bond of puerarin by three proteins, mn2+, and oxidized form of nicotinamide adenine dinucleotide.
We previously isolated the human intestinal bacterium, strain PUE, which can cleave the C-glucosidic bond of puerarin to yield its aglycone daidzein and glucose. In this study, we partially purified puerarin C-glucosidic bond cleaving enzyme from the cell-free extract of strain PUE and demonstrated that the reaction was catalyzed by at least three proteins, Mn(2+), and oxidized form of nicotinamide adenine dinucleotide (NAD(+)). We completely purified one of the proteins, called protein C, by chromatographic separation in three steps. The molecular mass of protein C was approximately 40 kDa and the amino acid sequence of its N-terminal region shows high homology to those of two putative proteins which belong to Gfo/Idh/MocA family oxidoreductase. Protein C catalyzed hydrogen-deuterium exchange reaction of puerarin to 2″-deuterated puerarin in D2O condition, which closely resembles those of glycoside hydrolase family 4 and 109....(more)
Nakamura K, et al. Biol Pharm Bull 2013;36(4):635-40.
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- 28. Metabolic profile of puerarin in rats after intragastric administration of puerarin solid lipid nanoparticles.
Puerarin has multiple pharmacological effects and is widely prescribed for patients with cardiovascular diseases including hypertension, cerebral ischemia, myocardial ischemia, diabetes mellitus, and arteriosclerosis. We have successfully prepared puerarin-loaded solid lipid nanoparticles (Pue-SLNs) for oral administration. Pue-SLNs are prepared using monostearin, soya lecithin, and poloxamer 188. SLNs may alter the course of puerarin absorption predominantly to and through lymphatic routes and regions, presumably following a transcellular path of lipid absorption, especially by enterocytes and polar epithelial cells of the intestine. The alteration of absorption might influence the metabolic profile of puerarin when incorporated into SLNs. In the present study, we investigated the metabolic profile of puerarin in rat plasma and urine using rapid resolution liquid chromatography-tandem mass spectrometry after a single-dose intragastric administration of Pue-SLNs in comparison with puerarin suspension. Two glucuronidated metabolites of puerarin, puerarin-4'-O-glucuronide and puerarin-7-O-glucuronide, were detected in rat plasma and urine after intragastric administration of Pue-SLNs, with the latter acting as the major metabolite. Similar results were found in rat plasma and urine after intragastric administration of puerarin suspension. The results suggest that incorporation of puerarin into SLNs does not change either the position of glucuronidation or the metabolic pathway of puerarin in rats....(more)
Luo CF, et al. Int J Nanomedicine 2013;8:933-40.
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- 29. The Role of Traditional Chinese Medicines in Osteogenesis and Angiogenesis.
The article aims to review various Traditional Chinese Medicines (TCMs) with both osteogenic and angiogenic effects, alone and in combination, and to consider whether these TCMs promote osteogenesis via angiogenesis and vascular endothelial growth factor (VEGF). Each of the TCMs involving in osteogenesis was searched through PubMed and CBMdisc using its Latin name and English name, and keywords such as 'osteogenesis', 'bone', 'osteoblast', 'angiogenesis', 'VEGF' were used. A total of 241 articles were screened from PubMed and CBMdisc. The articles were only chosen if they discussed the relationship of the TCMs with bone formation and/or angiogenesis. Twenty-seven articles were chosen, of which 16 were in English and 11 were in Chinese with English abstract. As a result, the TCMs (Danshen or Salvia miltiorrhiza Bunge, Danggui or Angelica sinensis, Astragalus membranaceus Bunge or Huangqi, and Ge Gan or Puerarin radix) that have a relationship with both osteogenesis and angiogenesis were screened out. It is found that the aforementioned TCMs enhance angiogenesis and osteogenesis. They show a positive effect on bone formation, and the possible mechanisms may be related to their ability to promote angiogenesis via an effect on substances such as VEGF. Copyright © 2013 John Wiley & Sons, Ltd....(more)
Yang Y, et al. Phytother Res 2013 Mar 15.
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- 30. Pharmacokinetics of puerarin in pregnant rats at different stages of gestation after oral administration.
This study aims to observe the effects of gestational stage on the pharmacokinetics of puerarin after oral administration in rats. The pharmacokinetics of puerarin was studied in pregnant rats using a sensitive and reproducible high-performance liquid chromatography/ultraviolet method. The concentration-time curves in both normal and pregnant rats were fit into a two-compartment model. The results indicated that gestation influences the pharmacokinetics of puerarin at different levels, especially during the early stages of pregnancy. Furthermore, puerarin penetrates the placental barrier and maintains high concentrations in fetal rat plasma. Therefore, puerarin administration should be carefully considered in pregnant women....(more)
Cao L, et al. Fitoterapia 2013 Apr;86:202-7.
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- 31. Anti-fibrotic effects of puerarin on CCl4-induced hepatic fibrosis in rats possibly through the regulation of PPAR-γ expression and inhibition of PI3K/Akt pathway.
Hepatic fibrosis (HF) is a chronic disease, which primarily leads to liver unregulated metabolism. In this study, we aimed to investigate the therapeutic effects of puerarin (PR), an active ingredient from kudzu root, on CCl4-induced HF rats. PR effectively ameliorated the liver metabolic function, resulting in reduced serum enzymatic activities of alanine aminotransferase (ALT), aspartate aminotransferase (AST), total-bilirubin (T-bilirubin), extracellular matrix (ECM) contents and increased levels of albumin, total-protein (T-protein) in HF rats. Similarly, pathological examination showed that the CCl4-lesioned liver was mitigated by PR treatments. Meanwhile, we also detected significantly reduced levels of hydroxyproline (Hyp), type III precollagen (PCIII) and collagen I (Col I) in the liver tissue of HF rats, whereas the peroxisome proliferator-activated receptor-gamma (PPAR-γ) expression was effectively increased. Moreover, the expression of tissue inhibitor of metal protease-1 (TIMP-1) was decreased, while the expression of matrix metalloproteinase-2 (MMP-2) was increased. In addition, the expression of p-PI3K and p-Akt was significantly down-regulated by PR treatments. Taken together, PR could attenuate the CCl4-induced toxicity in the hepatocytes of HF rats. It played a protective role in the liver tissue probably through regulating the PPAR-γ expression and blocking the PI3K/Akt pathway to inhibit the excessive deposition of collagen....(more)
Guo C, et al. Food Chem Toxicol 2013 Jun;56:436-42.
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- 32. Protective effect of puerarin on lead-induced mouse cognitive impairment via altering activities of acetyl cholinesterase, monoamine oxidase and nitric oxide synthase.
Puerarin (PU), a natural flavonoid, has been reported to have many benefits and medicinal properties. The present study aimed to investigate the protective effects of puerarin on neurotoxicity in mice exposed to lead. ICR mice were exposed to lead acetate in the drinking water (500ppm) with or without puerarin coadministration (100 and 200mgPU/kg intragastrically once daily) for three months. We found puerarin significantly prevented Pb-induced neurotoxicity in a dose-dependent manner, indicated by behavioral indicators. Puerarin also decreased Pb contents in blood and brain. Puerarin increased activities of acetyl cholinesterase (AChE) and monoamine oxidase (MAO) in brain of Pb-treated mice. Moreover, Pb-induced profound elevation of oxidative stress, as evidenced by increasing of lipid peroxidation level and depleting of total antioxidant capacity in brain, were suppressed by treatment with puerarin. Puerarin markedly increased NO production and PKA activity in brain of Pb-treated mice. Western blot analysis showed that puerarin dramatically increased the expression levels of nNOS, eNOS and phosphor-Akt in brains of Pb-treated mice. In conclusion, these results suggested that puerarin can inhibit Pb-induced neurotoxicity, at least in part, by suppressing oxidative stress, reversing the Pb-induced alterations in transmitters and enzymes and modulating the PKA/Akt/NOS signaling pathway....(more)
Liu CM, et al. Environ Toxicol Pharmacol 2013 May;35(3):502-10.
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- 33. Neuroprotective Effects of Puerarin on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine induced Parkinson's Disease Model in Mice.
Puerarin, an active component of Pueraria montana var. lobata (Willd.) Sanjappa & Pradeep is well-known for its anti-oxidative and neuroprotective activities. Although anti-Parkinson's disease activity of puerarin was reported in both of in vivo and in vitro model, detailed mechanisms are not clarified. In this study, we addressed that puerarin attenuated 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced behavioral deficits, dopaminergic neuronal degeneration and dopamine depletion. Puerarin administration enhanced glutathione (GSH) activity, glial cell line-derived neurotrophic factor (GDNF) expression and PI3K/Akt pathway activation, which might ameliorate MPTP injection-induced progressive elevation of reactive oxygen species (ROS) formation in mice. In addition to the effect on ROS, puerarin ameliorated MPTP-reduced lysosome-associated membrane protein type 2A (Lamp 2A) expression. Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression. Copyright © 2013 John Wiley & Sons, Ltd....(more)
Zhu G, et al. Phytother Res 2013 Mar 20.
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- 34. 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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- 35. DPPH assay of vegetable oils and model antioxidants in protic and aprotic solvents.
The rate of reaction of phenolic antioxidants with DPPH depends on solvent composition. The rate constants can differ by more than two orders of magnitude for the same phenolic compound. Reactions are faster in alcohols than in ethyl acetate that is used routinely for the analysis of antioxidant potential (AOP) of nonpolar samples such as vegetable oils. Incorporation of an acid base pair into the assay solvent buffers the system against acid impurities such as free fatty acids and CO2 from the air. This is shown to increase the rate of oxidation and number of electrons of phenolic compounds exchanged with DPPH. Typically, DPPH assays are performed for predetermined time intervals at which phenolic compounds are not fully oxidized and therefore higher reaction rates result in higher values of AOP. More than twofold AOP was obtained for oleuropein, sesamol, sinapic acid, caffeic acid and protocatechuic acid in buffered alcohols than in ethyl acetate. The AOP of sesame, pumpkin seed and extra virgin olive oil is accordingly higher when determined in buffered alcohols. DPPH assays in ethyl acetate result in underestimation of AOP of unrefined vegetable oils.
Copyright © 2013 Elsevier B.V. All rights reserved....(more)
Prevc T, et al. Talanta 2013 May 15;109:13-9.
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