Phosphodiesterase 5 Inhibitors

Publication Title: 
The Journal of Sexual Medicine

INTRODUCTION: Herbs have been used as an aphrodisiac since ages. Cinnamomum cassia is an important ingredient of many Ayurvedic formulations to treat male sexual disorder including erectile dysfunction (ED). AIM: The objective of the present study was to evaluate erectogenic and aphrodisiac activity of methanol extract of C. cassia bark in young male rats. METHODS: Methanol extract of C. cassia was screened in vitro for arginase inhibition potential and IC50 was determined.

Goswami, Sumanta K.
Inamdar, Mohammed N.
Jamwal, Rohitash
Dethe, Shekhar
Publication Title: 
Chemical & Pharmaceutical Bulletin

We isolated a new illegal sildenafil analogue named mutaprodenafil from a dietary supplement for erectile dysfunction (ED) and proposed that it is an aildenafil derivative containing an imidazole moiety. We subsequently synthesized mutaprodenafil from a thioaildenafil and authenticated its structure.

Demizu, Yosuke
Wakana, Daigo
Kamakura, Hiroyuki
Kurihara, Masaaki
Okuda, Haruhiro
Goda, Yukihiro
Publication Title: 
Acta Pharmacologica Sinica

AIM: To explore the potent inhibitor from one of the Traditional Chinese medicine (TCM), Epimedium sagittatum. METHODS: We predicted the potent compound, ES03b, de novo evolution from the four Epimedium sagittatum components were verified by molecular docking, pharmacophore analysis, and analysis of quantitative structure-activity relationship (QSAR) model, which was constructed by multiple linear regression. RESULTS: ES03b was chosen to undergo drug modification via de novo evolution.

Chen, Chien-yu
Chang, Yea-huey
Bau, Da-tian
Huang, Hung-Jin
Tsai, Fuu-Jen
Tsai, Chang-Hai
Chen, Calvin Yu-Chian
Publication Title: 
The Journal of Sexual Medicine

INTRODUCTION: Epimedium species (aka horny goat weed) have been utilized for the treatment of erectile dysfunction in Traditional Chinese Medicine for many years. Icariin (ICA) is the active moiety of Epimedium species. AIM: To evaluate the penile hemodynamic and tissue effects of ICA in cavernous nerve injured rats. We also studied the in vitro effects of ICA on cultured pelvic ganglia. METHODS: Rats were subjected to cavernous nerve injury and subsequently treated for 4 weeks with daily gavage feedings of a placebo solution of normal saline and Dimethyl sulfoxide (DMSO) vs.

Shindel, Alan W.
Xin, Zhong-Chen
Lin, Guiting
Fandel, Thomas M.
Huang, Yun-Ching
Banie, Lia
Breyer, Benjamin N.
Garcia, Maurice M.
Lin, Ching-Shwun
Lue, Tom F.
Publication Title: 
Molecules (Basel, Switzerland)

Epimedium sagittatum (Sieb. et Zucc.) Maxim is one of the herbs used to treat erectile dysfunction in Traditional Chinese Medicine. Sildenafil is a phosphodiesterase 5 inhibitor used to treat erectile dysfunction in Western Medicine. This study evaluates the herbal-drug interaction of Epimedium sagittatum extract on the pharmacokinetics of sildenafil in rats by ultra-performance liquid chromatography. The rat plasma was sampled from each anesthetized rat after pretreatment with 3-days Epimedium sagittatum extract (1/2 g/kg/day) and intravenous injection with sildenafil (10/30 mg/kg).

Hsueh, Thomas Y.
Wu, Yu-Tse
Lin, Lie-Chwen
Chiu, Allen W.
Lin, Chi-Hung
Tsai, Tung-Hu
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