TY - JOUR
T1 - Anti-HIV Ermiasolides from Croton megalocarpus
AU - Terefe, Ermias Mergia
AU - Okalebo, Faith Apolot
AU - Derese, Solomon
AU - Langat, Moses K.
AU - Mas-Claret, Eduard
AU - Qureshi, Kamal A.
AU - Jaremko, Mariusz
AU - Muriuki, Joseph
N1 - KAUST Repository Item: Exported on 2022-10-21
Acknowledgements: This research was funded by the King Abdullah University of Science and Technology, Thuwal, Jeddah, Saudi Arabia and United States International University, Nairobi, Kenya. EMT acknowledges United States International University-Africa Internal Grant No. 10-2854, and University of Nairobi, Kenya Medical Research institute, the Institute of Primate Research and King Abdullah University of Science and Technology for their support toward the successful completion of the research work.
PY - 2022/10/19
Y1 - 2022/10/19
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10754/685041
UR - https://www.mdpi.com/1420-3049/27/20/7040
U2 - 10.3390/molecules27207040
DO - 10.3390/molecules27207040
M3 - Article
C2 - 36296633
SN - 1420-3049
VL - 27
SP - 7040
JO - Molecules
JF - Molecules
IS - 20
ER -
