Anti-HIV‐1 Diterpenoids from Leaves and Twigs of Polyalthia sclerophylla

Abstract

Bioassay-guided fractionation and purification of the anti-HIV-1-active MeOH extract from the leaves and twigs of Polyalthia sclerophylla led to the isolation of two new compounds, ent-kaur-sclerodimer (1) and cyclotucanol 3-palmitate (2), along with the known ent-kaur-16-en-19-oic acid (3), 15β-hydroxy-ent-kaur-16-en-19-oic acid (4), 15β-acetoxy-ent-kaur-16-en-19-oic acid (5), 15-oxo-ent-kaur-16-en-19-oic acid (6), 16α,17-dihydroxy-ent-kauran-19-oic acid (7), 16α-hydroxy-ent-kauran-19-oic acid (xylopic acid) (8), a pseudodimer (15α-hydroxy-ent-kaur-16-en-19-oic acid/17-hydroxy-ent-kaur-15-en-19-oic acid) (9), ermanin, nicotiflorin, and allantoin. Among these isolates, compound 3 was the most active in both anti-syncytium (EC₅₀ 13.7 µg/mL and selectivity index 3.1) and HIV-1 reverse transcriptase (IC₅₀ 34.1 µg/mL) assays.

Key words

Polyalthia sclerophylla - Annonaceae - ent‐kuarane diterpenoids - anti‐HIV‐1 activity

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