Cas No.: | 1189561-66-7 |
Synonyms: | (S)-(+)-Gossypol acetic acid |
SMILES: | OC1=C2C(C=O)=C(O)C(O)=C(C(C)C)C2=CC(C)=[C@@]1[C@@]3=C(C)C=C4C(C(C)C)=C(O)C(O)=C(C=O)C4=C3O.CC(O)=O |
Formula: | C32H34O10 |
M.Wt: | 578.6064 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | (S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM). in vitro: Gossypol-acetic acid significantly inhibited the proliferation of RAW264.7 cells in a dose-dependent manner, and caused obvious cell apoptosis and a loss of ΔΨm in RAW264.7 cells. Gossypol-acetic acid-induced cell apoptosis was markedly inhibited by caspase inhibitors. gossypol acetate resulted in a dose- and time-dependent inhibition of multiple myeloma cell proliferation, with an IC50 value to both U266 and Wus1 cells at 2.4, 2.2 μM at 48 h after treatment. Gossypol acetate effectively induced the apoptosis of multiple myeloma cells. Colorimetric assays showed activation of both caspase-3 and caspase-9. Bcl-2 and Bcl-xl expression was decreased by 86.5% and 35.9%, respectively, after treatment with gossypol acetate at 25 μM for 24 h . Gossypol-acetic acid (5-40 μM) inhibited the growth of MEC-1 cells in a dose- and time-dependent manner. Gossypol-acetic acid inhibits the proliferation of MEC-1, and DSB maybe one of the mechanisms of inhibitory effect of Gossypol-acetic acid on the growth of tumor cells. in vivo: A growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. In addition, there was no body weight loss for the treated group in comparison with the vehicle mice. Male rats were treated with gossypol acetic acid, GSH-Px specific activity increased in gossypol acetic acid group. gossypol acetic acid induce significant increases in the hepatic NEFA with remarkable decrease in the total saturated fatty acids with a significant increase of PUFA. Gossypol-acetic acid has selective action on the sperm membrane of the rats, it inhibited sperm Ca2+ influx in a dose-dependent manner, and exerts no effect on the high K+ induced contraction of smooth muscle of isolated rat. |