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HIV‐1 protease and HIV‐1 integrase inhibitory substances from Eclipta prostrata
Author(s) -
Tewtrakul Supinya,
Subhadhirasakul Sanan,
Cheenpracha Sarot,
Karalai Chatchanok
Publication year - 2007
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.2252
Subject(s) - integrase , ic50 , hiv 1 protease , stereochemistry , chemistry , hydroxymethyl , pharmacognosy , coumarin , traditional medicine , protease , biological activity , enzyme , biochemistry , in vitro , medicine , organic chemistry , dna
The bioassay‐guided fractionation for anti‐HIV‐1 integrase activity led to the isolation of six compounds from the whole plant extract of Eclipta prostrata extract. They were identified as 5‐hydroxymethyl‐(2,2′:5′,2″)‐terthienyl tiglate (1), 5‐hydroxymethyl‐(2,2′:5′,2″)‐terthienyl agelate (2), 5‐hydroxymethyl‐(2,2′:5′,2″)‐terthienyl acetate (3), ecliptal (4), orobol (5) and wedelolactone (6). Of these, compound 6 showed the highest activity against HIV‐1 integrase (IN) with an IC 50 value of 4.0 ± 0.2 µ m , followed by compound 5 (IC 50 = 8.1 ± 0.5 µ m ), whereas the four terthiophene compounds (1–4) were inactive (IC 50 > 100 µ m ). Regarding HIV‐1 protease (PR) inhibitory activity, compound 1 exhibited appreciable activity against HIV‐1 PR with an IC 50 of 58.3 ± 0.8 µ m , followed by compound 4 (IC 50 = 83.3 ± 1.6 µ m ) and compound 3 (IC 50 = 93.7 ± 0.8 µ m ), while compounds 2, 5 and 6 were inactive against HIV‐1 PR (IC 50 > 100 µ m ). This is the first report of anti‐HIV‐1 IN activities for wedelolactone (6), a coumarin derivative, and orobol (5), an isoflavone derivative. This study supports the use of E. prostrata in AIDS patients, which is in accord with its traditional use by Thai traditional doctors for curing blood related diseases. Copyright © 2007 John Wiley & Sons, Ltd.