| Autor: |
Terefe EM; Department of Pharmacology and Pharmacognosy, School of Pharmacy and Health Sciences, United States International University-Africa, 14634-00800, Nairobi, Kenya.; Department of Pharmacology and Pharmacognosy, College of Health Sciences, University of Nairobi, 14634-00800, Nairobi, Kenya., Okalebo FA; Department of Pharmacology and Pharmacognosy, College of Health Sciences, University of Nairobi, 14634-00800, Nairobi, Kenya., Derese S; Department of Chemistry, University of Nairobi, 30197-00100, Nairobi, Kenya., Muriuki J; Centre for Virus Research, Kenya Medical Research Institute, 54628-00200, Nairobi, Kenya., Rotich W; Sigowet-Soin Sub-County Hospital, Sondu-Kapsoit Road, Sigowet, Kericho County, 112-20200, Kericho, Kenya., Mas-Claret E; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K., Sadgrove N; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K., Padilla-González GF; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K., Prescott TAK; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K., Siddique H; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K., Langat MK; Royal Botanic Gardens, Kew, Kew Green, Richmond, Surrey, TW9 3AE, U.K. |
| Abstrakt: |
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 IC 50 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. |
