12-O-acetylphorbol-13-decanoate potently inhibits cytopathic effects of human immunodeficiency virus type 1 (HIV-1), without activation of protein kinase C.
Through bioactivity-guided fractionation, eight phorbol diesters, including five new ones (1-5), were isolated from the seeds of Croton tiglium collected in Egypt. 12-O-Acetylphorbol-13-decanoate (6) and 12-O-decanoylphorbol-13-(2-methylbutyrate) (4) potently inhibited the HIV-1-induced cytopathic effect on MT-4 cells (IC100 values of 7.6 ng/ml and 7.81 micrograms/ml, and CC0 values of 62.5 micrograms/ml and 31.3 micrograms/ml, respectively) without activating protein kinase C.
el-Mekkawy
S
S
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Japan.
Meselhy
M R
MR
Nakamura
N
N
Hattori
M
M
Kawahata
T
T
Otake
T
T
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D003651:Decanoates / Q000138:chemical synthesis* / Q000494:pharmacology; D004534:Egypt; D004789:Enzyme Activation / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D010704:Phorbols / Q000138:chemical synthesis* / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry; D011493:Protein Kinase C / Q000378:metabolism*; D012639:Seeds / Q000737:chemistry
D019380:Anti-HIV Agents; D003651:Decanoates; D010704:Phorbols; C401232:12-O-acetylphorbol-13-decanoate; D011493:Protein Kinase C