Constituents of Croton megalocarpus with Potential Anti-HIV Activity

被引:12
作者
Terefe, Ermias Mergia [1 ,2 ]
Okalebo, Faith A. [2 ]
Derese, Solomon [3 ]
Muriuki, Joseph [4 ]
Rotich, Winnie [5 ]
Mas-Claret, Eduard [6 ]
Sadgrove, Nicholas [6 ]
Padilla-Gonzalez, Guillermo F. [6 ]
Prescott, Thomas A. K. [6 ]
Siddique, Holly [6 ]
Langat, Moses K. [6 ]
机构
[1] US Int Univ Africa, Sch Pharm & Hlth Sci, Dept Pharmacol & Pharmacognosy, Nairobi 1463400800, Kenya
[2] Univ Nairobi, Dept Pharmacol & Pharmacognosy, Coll Hlth Sci, Nairobi 1463400800, Kenya
[3] Univ Nairobi, Dept Chem, Nairobi 3019700100, Kenya
[4] Kenya Govt Med Res Ctr, Ctr Virus Res, Nairobi 5462800200, Kenya
[5] Sigowet Soin Sub Cty Hosp, Kericho 11220200, Kenya
[6] Royal Bot Gardens, Kew, Richmond TW9 3AE, Surrey, England
来源
JOURNAL OF NATURAL PRODUCTS | 2022年
关键词
CROTOFOLANE-TYPE DITERPENOIDS; REVERSE-TRANSCRIPTASE; NATURAL-PRODUCTS; LEAVES; ROOTS; ASSAY; AIDS;
D O I
10.1021/acs.jnatprod.1c01013
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Reported herein is an anti-HIV monochlorinated compound, 1 beta-acetoxy-3 beta-chloro-5 alpha,6 alpha-dihydroxycrotocascarin L (1), of the rare crotofolane diterpenoid class. Compound 1, a suspected artifact of extraction, along with the previously undescribed 11 beta-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 mu M. Compounds 1 and 3 were both found to inhibit HIV-1 protease.
引用
收藏
页码:1861 / 1866
页数:6
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