827320-51-4Relevant academic research and scientific papers
Potent inhibition of human phosphodiesterase-5 by icariin derivatives
Dell'Agli, Mario,Galli, Germana V.,Dal Cero, Esther,Belluti, Federica,Matera, Riccardo,Zironi, Elisa,Pagliuca, Giampiero,Bosisio, Enrica
, p. 1513 - 1517 (2008)
Plant extracts traditionally used for male impotence (Tribulus terrestris, Ferula hermonis, Epimedium brevicornum, Cinnamomum cassia), and the individual compounds cinnamaldehyde, ferutinin, and icariin, were screened against phosphodiesterase-5A1 (PDE5A1) activity. Human recombinant PDE5A1 was used as the enzyme source. Only E. brevicornum extract (80% inhibition at 50 μg/mL) and its active principle icariin (1) (IC50 5.9 μM) were active. To improve its inhibitory activity, 1 was subjected to various structural modifications. Thus, 3,7-bis(2-hydroxyethyl)icaritin (5), where both sugars in 1 were replaced with hydroxyethyl residues, potently inhibited PDE5A1 with an IC50 very close to that of sildenafil (IC50 75 vs 74 nM). Thus, 5 was 80 times more potent than 1, and its selectivity versus phosphodiesterase-6 (PDE6) and cyclic adenosine monophosphate-phosphodiesterase (cAMP-PDE) was much higher in comparison with sildenafil. The improved pharmacodynamic profile and lack of cytotoxicity on human fibroblasts make compound 5 a promising candidate for further development.
Herba Epimedii glycoside compound and use thereof
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Paragraph 0136; 0137; 0138, (2017/08/14)
The invention relates to a kind of icariin compounds shown in a formula (I) or stereoisomers, geometrical isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs of the compounds shown in the formula (I). The invention also discloses a drug composition containing the compounds, a preparation method of the compounds or the drug composition and an application of the compounds or the drug composition to inhibiting the activity of phosphoesterase, promoting development of gonads and preventing and treating sexual dysfunction.
