TY - JOUR
T1 - Constituents of Croton megalocarpus with Potential Anti-HIV Activity
AU - Terefe, Ermias Mergia
AU - Okalebo, Faith A
AU - Derese, Solomon
AU - Muriuki, Joseph
AU - Rotich, Winnie
AU - Mas-Claret, Eduard
AU - Sadgrove, Nicholas
AU - Padilla-González, Guillermo F
AU - Prescott, Thomas A K
AU - Siddique, Holly
AU - Langat, Moses K
PY - 2022/6/16
Y1 - 2022/6/16
N2 - 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.
AB - 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.
KW - Croton
KW - Diterpenes
KW - HIV-1
KW - Kenya
U2 - 10.1021/acs.jnatprod.1c01013
DO - 10.1021/acs.jnatprod.1c01013
M3 - Article
C2 - 35709365
SN - 0163-3864
VL - 85
SP - 1861
EP - 1866
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 7
ER -