Flavonoids and Acid-Hydrolysis derivatives of <i>Neo</i>-Clerodane diterpenes from <i>Teucrium flavum</i> subsp. <i>glaucum</i> as inhibitors of the HIV-1 reverse transcriptase–associated RNase H function
نویسندگان
چکیده
Bioassay-guided fractionation of the ethyl acetate extract from Teucrium flavum subsp. glaucum, endowed with inhibitory activity towards HIV-1 reverse transcriptase–associated RNase H function, led to isolation salvigenin (1), cirsimaritin (2) and cirsiliol (3) along neo-clerodanes teuflavin (4) teuflavoside (5). Acid hydrolysis inactive provided three undescribed neo-clerodanes, flavuglaucins A-C (7-9) one known neo-clerodane (10). Among all flavuglaucin B showed highest function a IC50 value 9.1 ?M. Molecular modelling site-directed mutagenesis analysis suggested that binds into an allosteric pocket close catalytic site. This is first report clerodane diterpenoids anti-reverse transcriptase activity. Neo-clerodanes represent valid scaffold for development new class inhibitors.
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: ['1475-6374', '1475-6366']
DOI: https://doi.org/10.1080/14756366.2021.1887170