Dehydroandrographolide succinic acid monoester as an inhibitor against the human immunodeficiency virus.
Dehydroandrographolide succinic acid monoester (DASM) is the dehydroandrographolyl ester of succinic acid; and andrographolide, from which DASM is made, is the major diterpenoid lactone found in the Chinese medicinal herb, Andrographis paniculata. DASM has been found to be an inhibitor against the human immunodeficiency virus (HIV) in vitro. It was nontoxic to the H9 cell at the concentrations of 50-200 (average, 108) micrograms/ml and was inhibitory to the HIV-1 (IIIB) at the minimal concentration of 1.6-3.1 (average 2.0) micrograms/ml. It was also inhibitory to two other strains of HIV-1 and a strain of HIV-2. This inhibitory effect could also be demonstrated in cultures of activated human blood mononuclear cells; the 50% toxic dose and the 50% HIV inhibitory dose were about 200-greater than or equal to 400 and 0.8-2 micrograms/ml, respectively. At the subtoxic concentration, DASM partially interfered with HIV-induced cell fusion and with the binding of HIV to the H9 cell. Presumably, it also interfered with HIV replication at another unidentified step(s).
Chang
R S
RS
Department of Medical Microbiology, University of California, Davis 95616.
Ding
L
L
Chen
G Q
GQ
Pan
Q C
QC
Zhao
Z L
ZL
Smith
K M
KM
D000998:Antiviral Agents / Q000494:pharmacology*; D002459:Cell Fusion / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002681:China; D004261:DNA Replication / Q000187:drug effects; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D015498:HIV-2 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007372:Interferons / Q000096:biosynthesis; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D008517:Phytotherapy; D010946:Plants, Medicinal; D011070:Poly I-C / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors; D013386:Succinates / Q000302:isolation & purification / Q000494:pharmacology*; D014721:Vesicular stomatitis Indiana virus / Q000187:drug effects / Q000502:physiology; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D004224:Diterpenes; D018894:Reverse Transcriptase Inhibitors; D013386:Succinates; C068599:dehydroandrographolide 6-succinic acid monoester; C068600:dehydroandrographolide 5-succinic acid monoester; D007372:Interferons; D011070:Poly I-C