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Inhibitors of HIV-1 integrase from Dioscorea bulbifera

By Prapaporn Chaniad, Chatchai Wattanapiromsakul, Somsak Pianwanit and Supinya Tewtrakul


A search for HIV-1 integrase (IN) inhibitors from natural sources has led to the isolation of compounds from Dioscorea\ud bulbifera bulbils. From the bioassay-guided isolation, the chloroform fraction was then fractionated to obtain one new\ud clerodane diterpenoid (diosbulbin E acetate, 4), two known clerodane diterpenoids (1-2), four flavonoids (5-8) and one sterol\ud glucoside (3). Quercetin (7) exhibited the strongest anti-HIV-1 IN activity with an IC50 value of 16.28 µM, followed by\ud kaempferol (8, IC50 = 37.71 µM), whereas (+)-catechin (6) possessed moderate activity (IC50 = 62.36 µM). Moreover, the\ud clerodane-type diterpenoids (1 and 4) also exhibited moderate inhibitory effects with IC50 values of 70.39 and 73.49 µM,\ud respectively. The flavonoid compounds (5-8) were also investigated for their interactions with the IN active sites using\ud a molecular docking method. They interacted with Thr66, His67, Gln148, Glu152 and Lys159, which are important amino\ud acid residues for inhibition of HIV-1 IN activity

Topics: anti-HIV-1 integrase activity, Dioscorea bulbifera L., molecular docking, diosbulbin E acetate, clerodane diterpenoid, Technology, T, Technology (General), T1-995, Science, Q, Science (General), Q1-390
Publisher: Prince of Songkla University
Year: 2016
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