HIV-1 reverse transcriptase inhibitory activity of flavones and chlorogenic acid derivatives from Moquiniastrum floribundum (Asteraceae)

Abstract In the search for new bioactive natural products, plant sources represent a particularly suitable starting point in drug discovery. Among natural products, phenolic derivatives have a prominent place with several compounds exhibiting remarkable activities. This paper described the phenolic composition of Moquiniastrum floribundum (Asteraceae) and evaluated the inhibitory effect of isolated compounds on HIV-1 reverse transcriptase. From M. floribundum was isolated three flavones, genkwanin ( 1 ), hispidulin ( 2 ), and cirsimaritin ( 3 ), and eight chlorogenic acid derivatives, 4,5-di- O -caffeoylquinic acid ( 4 ), 3,5-di- O -caffeoylquinic acid ( 5 ), 3,4-di- O -caffeoylquinic acid ( 6 ), 3,5-di- O -caffeoylquinic acid methyl ester ( 7 ), 3,4,5-tri- O -caffeoylquinic acid methyl ester ( 8 ), 3- O -caffeoylquinic acid ( 9 ), 4- O -caffeoylquinic acid ( 10 ) and 5- O -caffeoylquinic acid ( 11 ). The most active compound was 4,5-di- O -caffeoylquinic acid ( 4 ), with 65.0 ± 7.9% of inhibitory activity on HIV-1 reverse transcriptase and IC 50 0.240 mmol L −1 .