Abstract
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.
MeSH terms
-
Anti-HIV Agents / chemical synthesis*
-
Anti-HIV Agents / pharmacology
-
Cytopathogenic Effect, Viral / drug effects
-
Decanoates / chemical synthesis*
-
Decanoates / pharmacology
-
Egypt
-
Enzyme Activation / drug effects
-
HIV-1 / drug effects*
-
HIV-1 / enzymology
-
Humans
-
Phorbols / chemical synthesis*
-
Phorbols / pharmacology
-
Plants, Medicinal / chemistry
-
Protein Kinase C / metabolism*
-
Seeds / chemistry
Substances
-
Anti-HIV Agents
-
Decanoates
-
Phorbols
-
12-O-acetylphorbol-13-decanoate
-
Protein Kinase C