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HIV‐1 integrase inhibitory substances from Coleus parvifolius
Author(s) -
Tewtrakul Supinya,
Miyashiro Hirotsugu,
Nakamura Norio,
Hattori Masao,
Kawahata Takuya,
Otake Toru,
Yoshinaga Tomokazu,
Fujiwara Tamio,
Supavita Tanomjit,
Yuenyongsawad Supreeya,
Rattanasuwon Pranee,
DejAdisai Sukanya
Publication year - 2003
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.1111
Subject(s) - rosmarinic acid , luteolin , coleus , daucosterol , chemistry , stereochemistry , ic50 , ether , biochemistry , biology , flavonoid , organic chemistry , in vitro , botany , silica gel , antioxidant
Abstract For the purpose of discovering anti‐HIV‐1 agents from natural sources, water and EtOH extracts of 50 Thai plants were screened for their inhibitory activity against HIV‐1 integrase (IN), an enzyme essential for viral replication. Of these plants, an EtOH extract of Coleus parvifolius Benth. (aerial parts) showed potent activity against HIV‐1 IN with an IC 50 value of 9.2 µg/mL. From this extract, 11 compounds were isolated and identied as luteolin 5‐ O ‐ β ‐d‐glucopyranoside ( 1 ), luteolin ( 2 ), luteolin 7‐methyl ether ( 3 ), luteolin 5‐ O ‐ β ‐d‐glucuronide ( 4 ), 5‐ O‐ β ‐d‐glucopyranosyl‐luteolin 7‐methyl ether ( 5 ), rosmarinic acid ( 6 ), rosmarinic acid methyl ester ( 7 ), daucosterol ( 8 ), a mixture of α ‐ and β ‐amyrin ( 9 , 10 ) and phytol ( 11 ). Of these compounds, rosmarinic acid methyl ester ( 7 ), rosmarinic acid ( 6 ), luteolin ( 2 ) and luteolin 7‐methyl ether ( 3 ) exhibited inhibitory activities against HIV‐1 IN with IC 50 values of 3.1, 5.0, 11.0 and 11.0 µM, respectively. Among rosmarinic acid derivatives, the HIV‐1 IN inhibitory activity increased in turn for a dimer (IC 50 = 5.0 µM), a trimer (IC 50 = 1.4 µM), and a tetramer (IC 50 = 1.0 µM). Copyright © 2003 John Wiley & Sons, Ltd.