Shin, HJ Kim, HJ Kwak, JH Chun, HO Kim, JH Park, H Kim, DH Lee, YS 2024-01-21T10:05:50Z 2024-01-21T10:05:50Z 2021-09-01 2002-09 0960-894X https://pubs.kist.re.kr/handle/201004/139214 During the search for naturally occurring cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) inhibitors, it was found that the extracts from Sophora flavescens exhibit potent inhibitory activity against cGMP PDE5 prepared from rat diaphragm. Therefore, the inhibitory activities of five flavonoids, kushenol H (1), kushenol K (2), kurarinol (3), sophoflavescenol (4) and kuraridine (5), isolated from S. flavescens were measured against cGMP PDE5 to identify potent cGMP PDE5 inhibitory constituents. Among tested compounds, sophoflavescenol (4), a C-8 prenylated flavonol, showed the most potent inhibitory activity (IC50 = 0.013 muM) against cGMP PDE5 with 31.5- and 196.2-fold selectivity over PDE3 and PDE4, respectively. Kinetic analysis revealed that sophoflavescenol was a mixed inhibitor of PDE5 with a K-i value of 0.005 muM. (C) 2002 Elsevier Science Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD A prenylated flavonol, sophoflavescenol: A potent and selective inhibitor of cGMP phosphodiesterase 5 Article 10.1016/S0960-894X(02)00401-8 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.12, no.17, pp.2313 - 2316 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 12 17 2313 2316 N scie scopus 000177603200012 2-s2.0-1842842609 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article SILDENAFIL RELAXATION sophoflavescenol