Abstract Title:

HIV-1 integrase inhibitory substances from Coleus parvifolius.

Abstract Source:

Phytother Res. 2003 Mar;17(3):232-9. PMID: 12672152

Abstract Author(s):

Supinya Tewtrakul, Hirotsugu Miyashiro, Norio Nakamura, Masao Hattori, Takuya Kawahata, Toru Otake, Tomokazu Yoshinaga, Tamio Fujiwara, Tanomjit Supavita, Supreeya Yuenyongsawad, Pranee Rattanasuwon, Sukanya Dej-Adisai

Article Affiliation:

Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Toyama, Japan.


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 IC50 value of 9.2 microg/mL. From this extract, 11 compounds were isolated and identified as luteolin 5-O-beta-d-glucopyranoside (1), luteolin (2), luteolin 7-methyl ether (3), luteolin 5-O-beta-d-glucuronide (4), 5-O-beta-d-glucopyranosyl-luteolin 7-methyl ether (5), rosmarinic acid (6), rosmarinic acid methyl ester (7), daucosterol (8), a mixture of alpha- and beta-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 IC50 values of 3.1, 5.0, 11.0 and 11.0 microM, respectively. Among rosmarinic acid derivatives, the HIV-1 IN inhibitory activity increased in turn for a dimer (IC50 = 5.0 microM), a trimer (IC50 = 1.4 microM), and a tetramer (IC50 = 1.0 microM).

Study Type : In Vitro Study

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