Icarisid II, a PDE5 inhibitor from Epimedium wanshanense, increases cellular cGMP by enhancing NOS in diabetic ED rats corpus cavernosum tissue
- 6 July 2011
- journal article
- research article
- Published by Hindawi Limited in Andrologia
- Vol. 44, 87-93
- https://doi.org/10.1111/j.1439-0272.2010.01144.x
Abstract
The aim of this study was to explore the effects and mechanisms of Icarisid II (ICA-II) on enhancing the cellular cGMP in rat corpus cavernosum tissue (RCCT). Diabetes mellitus Wistar rats were induced by streptozotocin, and diabetic ED rats were selected for the RCCT culture by apomorphine. ICA-II was extracted and purified from Icariin (ICA) by enzymatic method. The RCCT was treated with ICA-II, ICA and Sildenafil at different concentrations. cGMP and nitric oxide synthase (NOS) activities were checked respectively by enzyme immunoassay. Meanwhile, nNOS, iNOS and eNOS in RCCT were checked by western blot. ICA-II evaluated the intracellular cGMP to 8.01 ± 1.02 pmol mg−1 min−1, which is much weaker than that from Sildenafil (12.4 ± 1.16 pmol mg−1 min−1) (P < 0.05). There is no significant difference between ICA-II and ICA. With the treatment of 10 μm ICA-II for 24 and 48 h, nNOS expression was significantly increased in RCCT (P < 0.05), while the eNOS expression level was very low without any change. Notably, ICA-II increased the intracellular NOS activity significantly in vitro in RCCT. Except the PDE5 inhibitory effect, ICA-II increases the intracellular cGMP through the enhancement of nNOS expression and NOS activity in RCCT in vitro. ICA-II implies a potential compound for neurogenic erectile dysfunction by NO–cGMP pathway.Keywords
This publication has 22 references indexed in Scilit:
- Erectogenic and Neurotrophic Effects of Icariin, a Purified Extract of Horny Goat Weed (Epimediumspp.) In Vitro and In VivoThe Journal of Sexual Medicine, 2010
- Icariin inhibits neurotoxicity of β-amyloid by upregulating cocaine-regulated and amphetamine-regulated transcriptsNeuroReport, 2009
- Pharmacokinetics of prenylflavonoids and correlations with the dynamics of estrogen action in sera following ingestion of a standardized Epimedium extractJournal of Pharmaceutical and Biomedical Analysis, 2009
- Icariin stimulates angiogenesis by activating the MEK/ERK- and PI3K/Akt/eNOS-dependent signal pathways in human endothelial cellsBiochemical and Biophysical Research Communications, 2008
- Icaritin and its glycosides enhance osteoblastic, but suppress osteoclastic, differentiation and activity in vitroLife Sciences, 2007
- Novel phosphodiesterase-5 inhibitors: Current indications and future directionsIndian Journal of Medical Sciences, 2007
- Protective effects of icariin on human umbilical vein endothelial cell injury induced by H2O2 in vitroPharmacological Research, 2005
- Determination of icariin and metabolites in rat serum by capillary zone electrophoresis: rat pharmacokinetic studies after administration of icariinJournal of Pharmaceutical and Biomedical Analysis, 2004
- Flavonoids from Epimedium wanshanensePhytochemistry, 1996
- Antihepatotoxic Activity of Icariin, a Major Constituent ofEpimedium koreanumPlanta Medica, 1995