Niruriside, a new HIV REV/RRE binding inhibitor from Phyllanthus niruri.
During the screening of natural products for their ability to inhibit the binding of HIV-REV protein to [33P]-labeled RRE RNA, one novel compound, niruriside (1), was isolated from the MeOH extract of the dried leaf of Phyllanthus niruri L. by bioassay-guided fractionation. The structure of niruriside was determined by spectroscopic methods. Niruriside showed specific inhibitory activity against the binding of REV protein to RRE RNA with an IC50 value of 3.3 microM; however, niruriside did not protect CEM-SS cells from acute HIV infection at concentrations up to 260 microM using an XTT dye reduction assay.
Qian-Cutrone
J
J
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
Huang
S
S
Trimble
J
J
Li
H
H
Lin
P F
PF
Alam
M
M
Klohr
S E
SE
Kadow
K F
KF
D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001667:Binding, Competitive; D002934:Cinnamates / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004187:Disaccharides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D015967:Gene Expression Regulation, Viral / Q000187:drug effects*; D015694:Gene Products, rev / Q000187:drug effects* / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D007194:India; D015458:Leukemia, T-Cell; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry*; D011485:Protein Binding / Q000187:drug effects / Q000235:genetics; D012367:RNA, Viral / Q000187:drug effects; D014407:Tumor Cells, Cultured; D054321:rev Gene Products, Human Immunodeficiency Virus
D000998:Antiviral Agents; D002934:Cinnamates; D004187:Disaccharides; D015694:Gene Products, rev; D010936:Plant Extracts; D012367:RNA, Viral; C102783:niruriside; D054321:rev Gene Products, Human Immunodeficiency Virus