Anti-HIV Ermiasolides from Croton megalocarpus.

Terefe, Ermias Mergia; Okalebo, Faith Apolot; Derese, Solomon; Langat, Moses K.; Mas-Claret, Eduard; Qureshi, Kamal Ahmad; Jaremko, Mariusz; Muriuki, Joseph

Anti-HIV Ermiasolides from Croton megalocarpus.

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Journal article

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Terefe, Ermias Mergia

ORCID

Okalebo, Faith Apolot

Derese, Solomon

Langat, Moses K.

Mas-Claret, Eduard

Qureshi, Kamal Ahmad

Jaremko, Mariusz

Muriuki, Joseph

Date published

October 19, 2022

Abstract

In recent years, elucidation of novel anti-HIV bioactive compounds from natural products is gaining importance rapidly, not only from the research and publications, but also from controlled clinical studies. Here we report three new anti-HIV eudesmane-type sesquiterpenes, 5β-Hydroxy-8α-methoxy eudesm-7(11)-en-12,8-olide (1), 5β,8α-Dihydroxy eudesm-7(11)-en-12,8-olide (2) and 5β-Hydroxy-8H-β-eudesm-7(11)-en-12,8-olide (3). These are trivially named ermiasolide A-C and were isolated from the bark of Croton megalocarpus. 5β-Hydroxy-8α-methoxy eudesm-7(11)-en-12,8-olide (1), showed the highest anti-HIV activity by inhibiting 93% of the viral replication with an IC50 = 0.002 µg/mL. On the other hand, 5β-Hydroxy-8H-β-eudesm-7(11)-en-12,8-olide (3) and 5β,8α-dihydroxy eudesm-7(11)-en-12,8-olide (2), inhibited viral replication by 77.5% at IC50 = 0.04 µg/mL and 69.5% at IC50 = 0.002 µg/mL, respectively. Molecular docking studies showed that the proposed mechanism of action leading to these results is through the inhibition of HIV-protease.