Urinary metabolites of icariin, present in Epimedium, were investigated using rats. In the urine of rats administered icariin orally, two major metabolites were detected, which were identified as icariside II and icar...Urinary metabolites of icariin, present in Epimedium, were investigated using rats. In the urine of rats administered icariin orally, two major metabolites were detected, which were identified as icariside II and icaritin by means of spectral data.展开更多
Erectile dysfunction (ED) is a major complication of diabetes mellitus. Icariin has been shown to enhance erectile function through its bioactive form, icarisid Ih This study investigates the effects of icarisid Ⅱ ...Erectile dysfunction (ED) is a major complication of diabetes mellitus. Icariin has been shown to enhance erectile function through its bioactive form, icarisid Ih This study investigates the effects of icarisid Ⅱ on diabetic rats with ED and its potential mechanism viathe assessment of advanced glycosylation end products (AGEs), autophagy, mTOR and the NO-cGMP pathway. Icarisid Ⅱ was extracted from icariin by an enzymatic method. In the control and diabetic ED groups, rats were administered normal saline; in the icarisid Ⅱ group, rats were administered icarisid Ⅱ intragastrically. Erectile function was evaluated by measuring intracavernosal pressure/mean arterial pressure (ICP/MAP). AGE concentrations, nitric oxide synthase (NOS) activity and cGMP concentration were assessed by enzyme immunoassay. Cell proliferation was analysed using methyl thiazolyl tetrazolium assay and flow cytometry. Autophagosomes were observed by transmission electron microscopy, monodansylcadaverine staining and GFP-LC3 Iocalisation. The expression of NOS isoforms and key proteins in autophagy were examined by western blot. Our results have shown that Icarisid Ⅱ increased ICP/MAP values, the smooth muscle cell (SMC) growth curve, S phase and SMC/collagen fibril (SMC/CF) proportions and decreased Beclin 1 (P〈0.05). Icarisid Ⅱ significantly increased the proliferative index and p-p70S6K(Thr389) levels and decreased the numbers of autophagosomes and the levels of LC3-11 (P〈0.01). Icarisid Ⅱ decreased AGE concentrations and increased cGMP concentration, NOS activity (P〈0.05) and cNOS levels (P〈0.01) in the diabetic ED group. Therefore, Icarisid Ⅱ constitutes a promising compound for diabetic ED and might be involved in the upregulation of SMC proliferation and the NO-cGMP pathway and the downregulation of AGEs, autophagy and the mTOR pathway.展开更多
The biliary metabolites of orally administered icariin in rats were investigated. Two metabolites B-l and B-2 were isolated and identified as icaritin 3-O-alpha-L-rhamnopyranosyl-7-O-beta-D-glucopyranuronoside and ica...The biliary metabolites of orally administered icariin in rats were investigated. Two metabolites B-l and B-2 were isolated and identified as icaritin 3-O-alpha-L-rhamnopyranosyl-7-O-beta-D-glucopyranuronoside and icariside II, respectively, on the basis of chemical and spectroscopic evidences.展开更多
文摘Urinary metabolites of icariin, present in Epimedium, were investigated using rats. In the urine of rats administered icariin orally, two major metabolites were detected, which were identified as icariside II and icaritin by means of spectral data.
文摘Erectile dysfunction (ED) is a major complication of diabetes mellitus. Icariin has been shown to enhance erectile function through its bioactive form, icarisid Ih This study investigates the effects of icarisid Ⅱ on diabetic rats with ED and its potential mechanism viathe assessment of advanced glycosylation end products (AGEs), autophagy, mTOR and the NO-cGMP pathway. Icarisid Ⅱ was extracted from icariin by an enzymatic method. In the control and diabetic ED groups, rats were administered normal saline; in the icarisid Ⅱ group, rats were administered icarisid Ⅱ intragastrically. Erectile function was evaluated by measuring intracavernosal pressure/mean arterial pressure (ICP/MAP). AGE concentrations, nitric oxide synthase (NOS) activity and cGMP concentration were assessed by enzyme immunoassay. Cell proliferation was analysed using methyl thiazolyl tetrazolium assay and flow cytometry. Autophagosomes were observed by transmission electron microscopy, monodansylcadaverine staining and GFP-LC3 Iocalisation. The expression of NOS isoforms and key proteins in autophagy were examined by western blot. Our results have shown that Icarisid Ⅱ increased ICP/MAP values, the smooth muscle cell (SMC) growth curve, S phase and SMC/collagen fibril (SMC/CF) proportions and decreased Beclin 1 (P〈0.05). Icarisid Ⅱ significantly increased the proliferative index and p-p70S6K(Thr389) levels and decreased the numbers of autophagosomes and the levels of LC3-11 (P〈0.01). Icarisid Ⅱ decreased AGE concentrations and increased cGMP concentration, NOS activity (P〈0.05) and cNOS levels (P〈0.01) in the diabetic ED group. Therefore, Icarisid Ⅱ constitutes a promising compound for diabetic ED and might be involved in the upregulation of SMC proliferation and the NO-cGMP pathway and the downregulation of AGEs, autophagy and the mTOR pathway.
文摘The biliary metabolites of orally administered icariin in rats were investigated. Two metabolites B-l and B-2 were isolated and identified as icaritin 3-O-alpha-L-rhamnopyranosyl-7-O-beta-D-glucopyranuronoside and icariside II, respectively, on the basis of chemical and spectroscopic evidences.