Constituents of Croton Megalocarpus With Potential Anti-hiv Activity
Date
2022Author
Terefe, Ermias M
Okalebo, Faith A
Derese, Solomon
Muriuki, Joseph
Rotich, Winnie
Mas-Claret, Eduard
Sadgrove, Nicholas
Padilla-González, Guillermo F
Prescott, Thomas A K
Siddique, Holly
Langat, Moses K
Type
ArticleLanguage
enMetadata
Show full item recordAbstract
Reported herein is an anti-HIV monochlorinated compound, 1β-acetoxy-3β-chloro-5α,6α-dihydroxycrotocascarin L (1), of the rare crotofolane diterpenoid class. Compound 1, a suspected artifact of extraction, along with the previously undescribed 11β-acetoxycrotocascarin L (2) and a known compound, crotocascarin K (3), were isolated from the bark of Croton megalocarpus, a Kenyan oil-producing seed crop. Compounds 1 and 3 inhibited HIV-1 replication with IC50 values of 28 and 5.5 nM, respectively. Furthermore, both compounds lacked cytotoxicity toward MT-4 cells and FM-55-M1 cells at concentrations of up to 50 μM. Compounds 1 and 3 were both found to inhibit HIV-1 protease.
Citation
Terefe EM, Okalebo FA, Derese S, Muriuki J, Rotich W, Mas-Claret E, Sadgrove N, Padilla-González GF, Prescott TAK, Siddique H, Langat MK. Constituents of Croton megalocarpus with Potential Anti-HIV Activity. J Nat Prod. 2022 Jun 16. doi: 10.1021/acs.jnatprod.1c01013. Epub ahead of print. PMID: 35709365.Publisher
University of Nairobi
Rights
Attribution-NonCommercial-NoDerivs 3.0 United StatesUsage Rights
http://creativecommons.org/licenses/by-nc-nd/3.0/us/Collections
- Faculty of Health Sciences (FHS) [10378]
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