An HIV-1 integrase inhibitor and free radical scavenger
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1,5-Dicaffeoylquinic acid (1,5-DCQA) has been found in A. montana and is an HIV-1 integrase inhibitor and free radical scavenger.1,2 1,5-DCQA inhibits HIV-1 integrase 3' end processing, end joining, and disintegration with IC50 values of 0.35, 0.56, and 0.84 μg/ml, respectively.2 It also inhibits HIV-1 replication in MT-2 T lymphoblastoid cells with an ED50value of 2 μg/ml. 1,5-DCQA (0.25-1 μM) reduces the level of free radicals released from human polymorphonuclear (PMN) cells stimulated by N-formyl-Met-Leu-Phe in a dose-dependent manner.1 It also dose-dependently increases cell survival and glutathione (GSH) levels and decreases reactive oxygen species (ROS) production and lactate dehydrogenase (LDH) release in an oxygen-glucose deprivation/reperfusion assay in rat cerebral astrocytes when used at concentrations ranging from 5 to 100 ?M.3
1.Heilmann, J., Merfort, I., and Weiss, M.Radical scavenger activity of different 3',4'-dihydroxyflavonols and 1,5-dicaffeoylquinic acid studied by inhibition of chemiluminescencePlanta Med.61(5)435-438(1995) 2.Robinson, W.E., Jr., Cordeiro, M., Abdel-Malek, S., et al.Dicaffeoylquinic acid inhibitors of human immunodeficiency virus integrase: Inhibition of the core catalytic domain of human immunodeficiency virus integraseMol. Pharmacol.50(4)846-855(1996) 3.Cao, X., Xiao, H., Zhang, Y., et al.1, 5-Dicaffeoylquinic acid-mediated glutathione synthesis through activation of Nrf2 protects against OGD/reperfusion-induced oxidative stress in astrocytesBrain Res.1347142-148(2010)
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