J Ethnopharmacol [journal]
- Spica prunellae and its marker compound rosmarinic acid induced the expression of efflux transporters through activation of Nrf2-mediated signaling pathway in HepG2 cells. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 12.
Spica prunellae (SP) is a well-known traditional Chinese medicinal herb with properties of antihypertensive, antihyperglycemic, antiviral, anti-inflammatory, and antitumor activities. This herb is also popularly consumed as a food additive in some drinks or other food forms for treating pyreticosis. Rosmarinic acid (RA) is the marker compound from SP, which possesses anti-oxidative and anti-inflammatory functions.This study aims to investigate the regulatory effect of the water extract of SP (WESP) and RA on efflux transports (ETs), including P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (MRP2), and breast cancer resistance protein (BCRP) in HepG2 cell line. Results would provide beneficial information for the proper application of SP in clinics.HepG2 cells were treated with different doses of the tested drugs for 24 or 96h. MTT assay was used to examine cell viability. The protein and mRNA levels of the ETs were measured by using Western blot and real-time PCR, respectively. Reporter assay was used to study the antioxidant response element (ARE)-luciferin activity by using HepG2-C8 cells, which were generated by transfecting plasmid containing ARE-luciferin gene into HepG2 cells. The transport activities of ETs were tested by using substrate probes.WESP significantly (p < 0.05) increased the expression of ETs in a dose-dependent manner. The increase caused by WESP was stronger than RA alone. Both WESP and RA promoted the translocation of nuclear factor E2-related factor-2 (Nrf2) from cytoplasm to the nucleus as well as significantly (p < 0.05) enhanced the ARE-luciferin activity. WESP and RA also enhanced the efflux activity of P-gp and MRP2, accompanied by marked increase (p < 0.05) in the intracellular ATP levels.WESP could significantly induce the expression of ETs through the activation of Nrf2-mediated signaling pathway in HepG2 cells. RA could be one of the active compounds responsible for the induction. WESP and RA also enhanced the efflux activity of P-gp and MRP2, and the increased intracellular ATP levels were likely involved in this induction. Results of this study provide a better understanding of the regulation of SP on ETs and the underlying molecular mechanism. Results indicated that potential drug-drug interactions may exist when SP is co-administered with other substrate drugs that are transported via the ETs, especially P-gp and MRP2, thereby providing beneficial information for appropriate use of SP for clinical therapy.
- Echinacoside and Cistanchetubulosa (Schenk) R. Wight ameliorate bisphenol A-induced testicular and sperm damage in rats through gonad axis regulated steroidogenic enzymes. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 12.
Male infertility has been increasing over the last decades and being a pressing health problem nowadays. Cistanche tubulosa (CT) is a traditional Chinese medicine used to boost male sexual function. Echinacoside (ECH) is one of the major compounds exist in CT and might be a potential agent to protect testis and sperm injury.To investigate the mechanisms behind the possible protective effects of CT and ECH against testicular and sperm toxicity.CT was identified by 5.8s gene sequencing. The major compositions (echinacoside and acteoside) of CT were quantified by HPLC method. The adult male Sprague-Dawley rats were exposed to BPA, CT or ECH for 42 consecutive days. The sperm parameters were observed by dark-field microscope; serum hormone levels (FSH, LH and testosterone) were tested by radio immunosorbent; LDH-x activity were evaluated using commercial kits; the expressions of the key steroidogenic enzymes were evaluated by qRT-PCR, heat map, immunofluorescence and western blot.The CT and ECH treatments against BPA-induced testicular and sperm toxicity showed that CT and ECH have reversed BPA-induced abnormality in sperm characteristics, testicular structure and normalized serum testosterone. This was concomitant with the increased expression of LDH-x as well as the key steroidogenic enzymes including StAR, CYP11A1, 3β-HSD, 17β-HSD and CYP17A1, suggesting that CT and ECH enhanced testosterone biosynthesis.CT and ECH attenuated poor sperm quality and testicular toxicity in rats through up-regulation steroidogenesis enzymes and ECH is the active compound of CT as a potential natural reproductive agent.
- A quantitative ethnobotanical survey of phytocosmetics used in the tropical island of Mauritius. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 12.
With a net turnover worth of £181 billion, the cosmetic industry is a leading worldwide business with a very lucrative future. Nonetheless, due to recent concerns regarding toxicity of synthetic cosmetics, herbal products have come into the limelight of cosmetology. The tropical island of Mauritius has a well-anchored diversity of indigenous plant species which are exploited for various purposes but no study has been designed to (i) quantitatively document, (ii) assess the effectiveness, and (iii) study the incidence of adverse effects and perception associated with the use of herbal products for cosmetic applications.Data was collected from herbal users via face-to-face interviews using semi-structured questionnaire from key informants. Quantitative ethnobotanical indices (fidelity level (FL), variety of use (VU) and relative frequency of citation (RFC)) were calculated.Twenty five herbs belonging to 21 families were recorded in use for 29 different cosmetics applications. Many of the documented species represented well-known plants, although we also recorded a few plants being exploited for new cosmetic applications. Plants with the highest RFC were Curcuma longa L. (0.45), Lawsonia inermis L. (0.42) and Aloe vera (L.) Burm.f. (0.42). A total of 8 plants were reported to score 100% with respect to the FL. Interestingly, Lawsonia inermis L. being the highly cited plant species showed a clear dominance as a popular phytocosmetic and which has also been extensively documented for its pharmacological properties. Moreover, it was found that 25% of the respondents experienced adverse effects; with pruritus (11%) being the most reported condition. It was also observed that participants perceived herbs/herbal products to be free from adverse effects.Most of the plants reported have been described in previous studies for their bioactive components which tend to justify their use as phytocosmetics. Further research should be geared to explore the potential of these plant products for the cosmetic industry.
- Comparative proteomic and metabolomic analysis reveal the antiosteoporotic molecular mechanism of icariin from Epimedium brevicornu Maxim. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 12.
Icariin, a principal flavonoid glycoside of Epimedium brevicornu Maxim, has been widely proved to possess antiosteoporotic activity with promoting bone frormation and decreasing bone resorption. However, the involving mechanisms remain unclear.To clear a global insight of signal pathways involved in anti-osteoporotic mechanism of icariin at proteins and metabolites level by integrating the proteomics and NMR metabonomics, in a systems biology approach.Mice were divided into sham, OVX model and icariin-treated OVX group, after 90 days treatment, difference gel electrophoresis combined with MALDI-TOF/TOF proteomics analysis on bone femur and serum metabolomics were carried out for monitor intracellular processes and elucidate anti-osteoporotic mechanism of icariin. Osteoblast and osteoclast were applied to evaluate the potential signal pathways.23 proteins in bone femur, and 8 metabolites in serum, were significantly altered and identified, involving in bone remodeling, energy metabolism, cytoskeleton, lipid metabolism, MAPK signaling, Ca(2+) signaling et, al. Furthermore, animal experiment show icariin could enhance the BMD and BMC, decrease CTX-I level in ovariectomized mice. The mitochondrial membrane potential and the intracellular ATP levels were increased significantly, and the cytoskeleton were improved in icariin-treatment osteoblast and osteoclast. Icariin also increased mRNA expression of Runx2 and osterix of OB, decreased CTR and CAII mRNA expression and protein expression of P38 and JNK. However, icariin did not reveal any inhibition of the collagenolytic activity of cathepsin K, mRNA expression of MMP-9 and protein expression of ERK in osteoclast.we consider icariin as multi-targeting compounds for treating with osteoporosis, involve intiating osteoblastogenesis, inhibiting adipogenesis, and preventing osteoclast differentiation.
- Intestinal anti-inflammatory effect of the rhizome extracts of Menispermum dauricum DC. on trinitrobenzene sulfonic acid induced ulcerative colitis in mice. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 16.
Menispermum dauricum DC., commonly known as "Bei Dou Gen" (BDG) in China, has been used extensively in folk medicine to treat inflammatory diseases, especially intestinal inflammations such as enteritis and dysentery, and in pharyngitis, tonsillitis, rheumatism and bronchitis. Although previous studies showed that BDG has anti-inflammatory activities, its effects on ulcerative colitis (UC) have not yet been explored.To investigate the intestinal anti-inflammatory effect of the rhizome extracts of Menispermum dauricum DC. on UC model induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS) in mice.UC in mice was induced by colonic administration with TNBS. BDG (100, 200 and 400mg/kg/day) and sulfasalazine (500mg/kg/day) were administered orally for 7 consecutive days. The inflammatory degree was assessed by gross appearance, macroscopic and histological analysis, and accumulation of myeloperoxidase (MPO) activity. Pro-inflammatory mediators, including tumor necrosis factor (TNF)-α, interleukin (IL)-1β and IL-6, were determined by enzyme-linked immunoassay. The expression of cyclooxygenase (COX)-2 was assessed by immunohistochemical analysis.Treatment with different doses of BDG significantly ameliorated macroscopic damage and histological changes, reduced the accumulation of MPO activity, depressed serum and colonic tissue levels of TNF-α, IL-1β and IL-6 in a dose-dependent manner. In addition, administration of BDG effectively reduced COX-2 overexpression in colon.We demonstrated for the first time that BDG possessed marked intestinal anti-inflammatory effect in TNBS induced colitis in mice, which might be related to the reduction of up-regulated productions and expressions of pro-inflammatory mediators, suggesting that it may have beneficial use for the treatment of inflammatory bowel disease.
- Genotoxic, mutagenic and antigenotoxic effects of Cecropia pachystachya Trécul aqueous extract using in vivo and in vitro assays. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 16.
Cecropia pachystachya is a medicinal plant native to South and Central Americas used to treat asthma and diabetes.In this study, we evaluated the genotoxic, mutagenic and antigenotoxic effects of crude aqueous extract of C. pachystachya (CAE-Cp) leaves.CAE-Cp was analyzed by the Folin-Ciocalteu method to determine total phenolic and tannin contents. High performance liquid chromatography (HPLC) was used to identify major compounds. Distinct tissues from female and male adult mice were treated with 500-2000mg/kg of CAE-Cp by gavage for the comet assay and micronucleus test analyses. In addition, peripheral blood slides of the group treated with 2000mg/kg CAE-Cp were analyzed 3, 6, and 24h after treatment and were exposed to hydrogen peroxide (ex vivo) to evaluate the genotoxic effect using the comet assay. The Salmonella/microsome assay was carried out against to TA100, TA98, TA97a, TA102, and TA1535 strains in presence and absence of the S9 mix.HPLC showed the presence of chlorogenic acid, isoorientin, orientin, and isovitexin as major compounds. Total phenolic and tannin contents were, respectively, 305.6±0.80 and 144.6±19.04mg of gallic acid equivalent/g of extract. Brain DNA damage was observed in all groups treated with CAE-Cp. The H2O2 challenge indicated genotoxic effect only 6h after the administration of the extract. No increase was detected in micronucleus frequency for any group treated with the extract. Mutagenic effects were detected by Salmonella/microsome assay only in TA102 strain without S9 mix at higher doses.The results obtained indicate that CAE-Cp was genotoxic to brain tissue. This result is supported by other papers, showing that compounds present in this extract can cross the blood-brain barrier and act on central nervous system.
- Antinociceptive and antidepressant-like effects of the crude extract of Vitex megapotamica in rats. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 16.
Vitex megapotamica (Spreng) Moldenke has been used in South American folk medicine to treat inflammatory diseases. However, the effects of V. megapotamica on animal models of nociception and depression have not been evaluated.This study investigated whether the crude leaf extract of V. megapotamica exhibits antinociceptive and antidepressant-like effects in a Freund's adjuvant-induced chronic inflammation and depression model.Chronic inflammation was induced in rats by the intraplantar administration of complete Freund's adjuvant (CFA; 100 ul). The effect of oral crude extract of V. megapotamica (VmE; 3-30mg/kg, p.o.) on nociception (thermal hyperalgesia, mechanical allodynia and arthritis score), inflammation (edema, myeloperoxidase activity), immobility (forced swimming test), locomotor activity (open field), gastrointestinal transit, hyperalgesia and naloxone-precipitated morphine withdrawal syndrome was evaluated. Naloxone (0.4mg/kg, i.p.) was used to investigate the involvement of opioid system in the currently described effects of VmE.Crude extract caused antinociceptive/antidepressant-like effects in the CFA-induced chronic inflammation model, which was prevented by naloxone. The VmE extract (10mg/kg, p.o.) did not alter the locomotor activity, gastrointestinal function and inflammatory parameters and did not cause hyperalgesia.V. megapotamica induces opioid-dependent antinociception and antidepressant-like effect, without anti-inflammatory activity. The results support the use of VmE as analgesic and antidepressant.
- Stachytarpheta cayennensis extract inhibits promastigote and amastigote growth in Leishmania amazonensis via parasite arginase inhibition. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 15.
Stachytarpheta cayennensis is a plant that is traditionally used to treat tegumentary leishmaniasis and as an anti-inflammatory agent.This study aimed to evaluate the action of S. cayennensis extracts on the Leishmania (Leishmania) amazonensis arginase enzyme.S. cayennensis was collected from the Brazilian Amazon region. Aqueous extracts were fractionated with n-butanol. The leishmanicidal effects of the n-butanolic fraction (BUF) were evaluated in L. (L.) amazonensis promastigotes and amastigotes. BUF was tested against recombinant arginase from both L. (L.) amazonensis and macrophage arginase. Promastigote cultures and infected macrophage cultures were supplemented with l-ornithine to verify arginase inhibition. NMR analysis was used to identify the major components of BUF.BUF showed an EC50 of 51 and 32µg/mL against promastigotes and amastigotes of L. (L.) amazonensis, respectively. BUF contains a mixture of verbascoside and isoverbascoside (7:3 ratio) and is a potent L. (L.) amazonensis arginase inhibitor (IC50 = 1.2µg/mL), while macrophage arginase was weakly inhibited (IC50 > 1000µg/mL). The inhibition of arginase by BUF in promastigotes and amastigotes could be demonstrated by culture media supplementation with l-ornithine, a product of the hydrolysis of l-arginine by arginase.Leishmanicidal effects of the S. cayennensis BUF fraction on L. (L.) amazonensis are associated with selective parasite arginase inhibition.
- The anti-tumor effect and bioactive phytochemicals of Hedyotis diffusa willd on ovarian cancer cells. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 14.
hedyotis diffusa willd (HDW) is a widely used medicinal herb in China. It processed various medicinal properties including antioxidative, anti-inflamatory and anti-cancer effects. This study aimed to investigate the anti-tumor effects of HDW on ovarian cancer cells and the underlying mechanisms as well as identify the bioactive compounds.Effects of HDW on the viability of ovarian cancer A2780 cells were detected by MTT assay. Apoptosis was detected by cell morphologic observation through DAPI staining and flow cytometry analysis. The migration of ovarian cancer cells which exposed to HDW were detected by wound healing and transwell assays. The protein levels of caspase 3/9, Bcl-2 and MMP-2/9 in human ovarian cancer cells treated with HDW were assessed by western blotting analysis. The potential bioactive compounds were characterized by HPLC-Q-TOF-MS.HDW significantly inhibited the growth of A2780 ovarian cancer cells and induced apoptosis. The induction of apoptosis by HDW was associated with down-regulation of anti-apoptotic protein Bcl-2 and the activation of caspase 3/9. Wound healing and transwell chamber assays indicated HDW suppressed the migration of ovarian cancer cells. HDW dramatically decreased MMP-2/9 expression. A HPLC-Q-TOF-MS analysis of HDW indicated the presence of 13 flavonoids compounds and one anthraquinone compound, which may contribute to the anticancer activity of the HDW.HDW effectively restricted the growth of ovarian cancer cells and induced apoptosis through the mitochondria-associated apoptotic pathway. Furthermore, HDW suppressed the migration of ovarian cancer cells through down-regulation of MMP-2 and MMP-9 expression. These results showed that HDW hold potential therapeutic effect for ovarian cancer patients.
- Curative effect of Amorphophallus paeoniifolius tuber on experimental hemorrhoids in rats. [JOURNAL ARTICLE]
- J Ethnopharmacol 2016 Jul 14.
Amorphophallus paeoniifolius (Dennst.) Nicolson (Family- Araceae) is a crop of south East Asian origin. In India, its tuber is widely used in ethnomedicinal practices by different tribes for the treatment of piles (hemorrhoid).The present study evaluated the effect of methanolic and aqueous extract of Amorphophallus paeoniifolius tuber on croton oil induced hemorrhoids in rats.The methanolic extract was standardized with the major phenolic compound, betulinic acid, by HPLC. The hemorrhoids were induced by applying 6% croton oil preparation in the ano-rectal region. Rats were orally administered methanolic and aqueous extract at doses of 250 and 500mg/kg, each for 7 days. Pilex (200mg/kg) was used as reference anti-hemorrhoidal drug. Hemorrhoids were assessed on eighth day by measuring hemorrhoidal and biochemical parameters along with histology of ano-rectal tissue.Croton oil application caused induction of hemorrhoids as indicated by significant (p<0.001) increase in plasma exudation of Evans blue in ano-rectal tissue, macroscopic severity score and ano-rectal coefficient as compared to normal rats. It significantly (p<0.001) elevated lactate dehydrogenase and cytokines (TNF- α and IL-6) levels in serum and increased myeloperoxidase activity and lipid peroxidation in ano-rectal tissue along with marked histological damage as compared to normal rats. Treatment with tuber extracts and pilex significantly (p<0.05-0.001) ameliorated Evans blue exudation, hemorrhoidal parameters and other biochemical parameters with attenuation of tissue damage compared to hemorrhoid control rats. The results indicate that tuber extracts exhibited curative action on hemorrhoids. The aqueous extract showed more pronounced effect than methanolic extract. The effects may be attributed to anti-inflammatory and antioxidant properties.Results indicate that tuber of Amorphophallus paeoniifolius exhibited curative action on hemorrhoids through anti-inflammatory and antioxidant properties. The study validates the ethnomedicinal use of tuber in hemorrhoids and implicates its therapeutic potential as an anti-hemorrhoidal agent.