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Inhibitors of HIV-1 integrase from Dioscorea bulbifera |
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| รหัสดีโอไอ | |
| Creator | 1. Prapaporn Chaniad 2. Chatchai Wattanapiromsakul 3. Somsak Pianwanit 4. Supinya Tewtrakul |
| Title | Inhibitors of HIV-1 integrase from Dioscorea bulbifera |
| Publisher | Research and Development Office, Prince of Songkla University |
| Publication Year | 2559 |
| Journal Title | Songklanakarin Journal of Science and Technology (SJST) |
| Journal Vol. | 38 |
| Journal No. | 3 |
| Page no. | 229-236 |
| Keyword | anti-HIV-1 integrase activity,Dioscorea bulbifera L.,molecular docking,diosbulbin E acetate,clerodane diterpenoid |
| ISSN | 0125-3395 |
| Abstract | A search for HIV-1 integrase (IN) inhibitors from natural sources has led to the isolation of compounds from Dioscoreabulbifera bulbils. From the bioassay-guided isolation, the chloroform fraction was then fractionated to obtain one newclerodane diterpenoid (diosbulbin E acetate, 4), two known clerodane diterpenoids (1-2), four flavonoids (5-8) and one sterolglucoside (3). Quercetin (7) exhibited the strongest anti-HIV-1 IN activity with an IC50 value of 16.28 ?M, followed bykaempferol (8, IC50 = 37.71 ?M), whereas (+)-catechin (6) possessed moderate activity (IC50 = 62.36 ?M). Moreover, theclerodane-type diterpenoids (1 and 4) also exhibited moderate inhibitory effects with IC50 values of 70.39 and 73.49 ?M,respectively. The flavonoid compounds (5-8) were also investigated for their interactions with the IN active sites usinga molecular docking method. They interacted with Thr66, His67, Gln148, Glu152 and Lys159, which are important aminoacid residues for inhibition of HIV-1 IN activity. |
