The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside...The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration(MIC). Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.展开更多
We evaluated the effect of isoquercetin(quercetin-O-3-glucoside-quercetin,IQ)as a functional component of Abeliophyllum disistichum Nakai ethanol extract(ADLE)on prostate cell proliferation and apoptosis and its effec...We evaluated the effect of isoquercetin(quercetin-O-3-glucoside-quercetin,IQ)as a functional component of Abeliophyllum disistichum Nakai ethanol extract(ADLE)on prostate cell proliferation and apoptosis and its effects on the IGF-1/PI3K/Akt/mTOR pathway in benign prostatic hyperplasia(BPH).Metabolites in ADLE were analyzed using UHPLC-qTOF-MS and HPLC.IQ was orally administered(1 or 10 mg/kg)to a testosterone propionate-induced BPH rat model,and its effects on the prostate weight were evaluated.The effect of IQ on androgen receptor(AR)signaling was analyzed in LNCaP cells.Whether IGF-1 and IQ affect the IGF-1/PI3K/Akt/mTOR pathway in BPH-1 cells was also examined.The metabolites in ADLE were identified and quantified,which confirmed that ADLE contained abundant IQ(20.88 mg/g).IQ significantly reduced the prostate size in a concentration-dependent manner in a BPH rat model,and significantly decreased the expression of AR signaling factors in the rat prostate tissue and LNCaP cells in a concentration-dependent manner.IQ also inhibited the PI3K/AKT/mTOR pathway activated by IGF-1 treatment in BPH-1 cells.In BPH-1 cells,IQ led to G0/G1 arrest and suppressed the expression of proliferation factors while inducing apoptosis.Thus,IQ shows potential for use as a pharmaceutical and nutraceutical for BPH.展开更多
Bone marrow mesenchymal stem cells(BMSCs)are non-hematopoietic multipotent stem cells capable of differentiating into mature cells.Isoquercetin,an extract from natural sources,has shown promise as a potential treatmen...Bone marrow mesenchymal stem cells(BMSCs)are non-hematopoietic multipotent stem cells capable of differentiating into mature cells.Isoquercetin,an extract from natural sources,has shown promise as a potential treatment for osteoporosis.To investigate the therapeutic effects of isoquercetin on osteoporosis,bone marrow mesenchymal stem cells(BMSCs)were cultured in vitro,and osteogenesis or adipogenesis was induced in the presence of isoquercetin for 14 days.We evaluated cell viability,osteogenic and adipogenic differentiation,as well as mRNA expression levels of Runx2,Alpl,and OCN in osteoblasts,and mRNA expression levels of Pparγ,Fabp4,and Cebpαin adipocytes.The results showed that isoquercetin dose-dependently increased cell viability and promoted osteogenic differentiation,as evidenced by Alizarin Red and alkaline phosphatase staining and mRNA expression levels of Runx2,Alpl,and OCN in osteoblasts(P<0.05).In contrast,isoquercetin inhibited adipogenic differentiation and decreased the mRNA expres-sion levels of Pparγ,Fabp4,and Cebpαin adipocytes(P<0.05).In vivo,isoquercetin treatment increased bone quan-tity and density in an osteoporosis model mice group,as determined byμCT scanning and immunohistochemistry(P<0.05).These findings suggest that isoquercetin may have therapeutic potential for osteoporosis by promoting the proliferation and differentiation of BMSCs towards osteoblasts while inhibiting adipogenic differentiation.展开更多
Background:The present study was designed to evaluate the potential of isoquercetin-based cream formulation on scald burn wound injury in rats.Methods:Four isoquercetin-based cream formulations viz.0.01,0.02,0.04,and ...Background:The present study was designed to evaluate the potential of isoquercetin-based cream formulation on scald burn wound injury in rats.Methods:Four isoquercetin-based cream formulations viz.0.01,0.02,0.04,and 0.06%w/w were prepared.Cream base and standard anti-burn cream containing silver sulfadiazine were also used for comparison.Scald burn was given to rats by pouring water at 90℃on a shaved dorsal area of 20 mm2.Deep second-degree burn injury was produced which was evaluated for the next 21 days for the percentage of wound contraction and period of epithelialization.On day 21,the rats were sacrificed and histopathological slides were prepared using hematoxylin-eosin staining.Burned tissue was also screened for levels of oxidative stress using thiobarbituric acid reactive species(TBARS)and reduced glutathione(GSH)estimation.Results:There was a significant increase in the percentage of wound contraction and a significant decrease in the period of epithelialization in isoquercetin-based cream-treated groups as compared with the control group.However,most significant results were obtained with isoquercetin 0.06%w/w cream.Histological y,isoquercetin 0.06%w/w cream treatment resulted in almost complete re-epithelialization and re-structuring of the wound tissue.There was a significant rise in TBARS and a decrease in GSH levels in the burn injury group which was reversed to a major extent by the application of isoquercetin-based cream.Conclusions:The results indicate the wound healing potential of isoquercetin-based cream.Tissue biochemical studies indicate towards a possible role of free radical scavenging in the observed effects of isoquercetin in wound healing.展开更多
基金supported by National Natural Science Foundation of China(NSFC,No.81274044)
文摘The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration(MIC). Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.
基金supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF)funded by the Ministry of Education,Science and Technology (NRF2020R1A2C1014798 to E-K Kim)。
文摘We evaluated the effect of isoquercetin(quercetin-O-3-glucoside-quercetin,IQ)as a functional component of Abeliophyllum disistichum Nakai ethanol extract(ADLE)on prostate cell proliferation and apoptosis and its effects on the IGF-1/PI3K/Akt/mTOR pathway in benign prostatic hyperplasia(BPH).Metabolites in ADLE were analyzed using UHPLC-qTOF-MS and HPLC.IQ was orally administered(1 or 10 mg/kg)to a testosterone propionate-induced BPH rat model,and its effects on the prostate weight were evaluated.The effect of IQ on androgen receptor(AR)signaling was analyzed in LNCaP cells.Whether IGF-1 and IQ affect the IGF-1/PI3K/Akt/mTOR pathway in BPH-1 cells was also examined.The metabolites in ADLE were identified and quantified,which confirmed that ADLE contained abundant IQ(20.88 mg/g).IQ significantly reduced the prostate size in a concentration-dependent manner in a BPH rat model,and significantly decreased the expression of AR signaling factors in the rat prostate tissue and LNCaP cells in a concentration-dependent manner.IQ also inhibited the PI3K/AKT/mTOR pathway activated by IGF-1 treatment in BPH-1 cells.In BPH-1 cells,IQ led to G0/G1 arrest and suppressed the expression of proliferation factors while inducing apoptosis.Thus,IQ shows potential for use as a pharmaceutical and nutraceutical for BPH.
基金the National Natural Science Foundation of China(Grant Nos.22276221,21675176)the Fundamental Research Funds for the Central Universities,and South-Central Minzu University(Grant No.CZP21002)for financial support.
文摘Bone marrow mesenchymal stem cells(BMSCs)are non-hematopoietic multipotent stem cells capable of differentiating into mature cells.Isoquercetin,an extract from natural sources,has shown promise as a potential treatment for osteoporosis.To investigate the therapeutic effects of isoquercetin on osteoporosis,bone marrow mesenchymal stem cells(BMSCs)were cultured in vitro,and osteogenesis or adipogenesis was induced in the presence of isoquercetin for 14 days.We evaluated cell viability,osteogenic and adipogenic differentiation,as well as mRNA expression levels of Runx2,Alpl,and OCN in osteoblasts,and mRNA expression levels of Pparγ,Fabp4,and Cebpαin adipocytes.The results showed that isoquercetin dose-dependently increased cell viability and promoted osteogenic differentiation,as evidenced by Alizarin Red and alkaline phosphatase staining and mRNA expression levels of Runx2,Alpl,and OCN in osteoblasts(P<0.05).In contrast,isoquercetin inhibited adipogenic differentiation and decreased the mRNA expres-sion levels of Pparγ,Fabp4,and Cebpαin adipocytes(P<0.05).In vivo,isoquercetin treatment increased bone quan-tity and density in an osteoporosis model mice group,as determined byμCT scanning and immunohistochemistry(P<0.05).These findings suggest that isoquercetin may have therapeutic potential for osteoporosis by promoting the proliferation and differentiation of BMSCs towards osteoblasts while inhibiting adipogenic differentiation.
文摘Background:The present study was designed to evaluate the potential of isoquercetin-based cream formulation on scald burn wound injury in rats.Methods:Four isoquercetin-based cream formulations viz.0.01,0.02,0.04,and 0.06%w/w were prepared.Cream base and standard anti-burn cream containing silver sulfadiazine were also used for comparison.Scald burn was given to rats by pouring water at 90℃on a shaved dorsal area of 20 mm2.Deep second-degree burn injury was produced which was evaluated for the next 21 days for the percentage of wound contraction and period of epithelialization.On day 21,the rats were sacrificed and histopathological slides were prepared using hematoxylin-eosin staining.Burned tissue was also screened for levels of oxidative stress using thiobarbituric acid reactive species(TBARS)and reduced glutathione(GSH)estimation.Results:There was a significant increase in the percentage of wound contraction and a significant decrease in the period of epithelialization in isoquercetin-based cream-treated groups as compared with the control group.However,most significant results were obtained with isoquercetin 0.06%w/w cream.Histological y,isoquercetin 0.06%w/w cream treatment resulted in almost complete re-epithelialization and re-structuring of the wound tissue.There was a significant rise in TBARS and a decrease in GSH levels in the burn injury group which was reversed to a major extent by the application of isoquercetin-based cream.Conclusions:The results indicate the wound healing potential of isoquercetin-based cream.Tissue biochemical studies indicate towards a possible role of free radical scavenging in the observed effects of isoquercetin in wound healing.
