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Gossypol has been known to exert a potential for anti-cancer, anti-inflammatory and other important therapeutic activities, gossypol binds and antagonizes anti-apoptotic effect of Bcl-2 family proteins. IC50 value: Target: Bcl-2; anticancer agent The substance, a yellow pigment similar to flavonoids, is present in cottonseed oil. In the plant, it acts as a natural defensive agent against predators, provoking infertility in insects. In most animals, gossypol provokes infertility, and in man it causes spermatogenesis arrest at relatively low doses. in vitro: The natural product and putative BH3 mimetic gossypol enhanced the cytotoxicity of BRD4770 in a synergistic manner in p53-mutant PANC-1 cells but not in immortalized non-tumorigenic pancreatic cells. The combination of gossypol and BRD4770 increased LC3-II levels and the autophagosome number in PANC-1 cells, and the compound combination appears to act in a BNIP3 (B-cell lymphoma 2 19-kDa interacting protein)-dependent manner. Gossypol treatment resulted in cell death through oxidative stress. Metabolite analysis showed that gossypol induces a decrease of the cellular levels of GSH, aspartic acid, and FAD in ovarian cancer cell line, SKOV3. gossypol blocked the phosphorylation of IκBα protein, p65, p38, c-Junterminal kinase (JNK) and extracellular signal-regulated kinase (ERK) in LPS stimulated RAW 264.7 cells. gossypol could down-regulate activation of ConA-induced NF-κB, NFAT and AP-1 signal transduction pathways in mouse T lymphocyte [4]. in vivo: gossypol significantly inhibited the production of LPS-induced TNF-α, IL-6 and IL-1β both in vitro and vivo.gossypol attenuated lung histopathologic changes in mouse models. Preliminary studies in vivo showed that 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.
Patent. CN118453551A 2024 Aug 09.
Patent. CN118453551A
Gossypol purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | bovine granulosa cells |
| Preparation method | In bovine granulosa cells, treatment with gossypol dose-dependently decreased hCG-induced cAMP formation. |
| Concentrations | 12.5 μg/ml |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c mice |
| Formulation | |
| Dosages | 25 mg/kg |
| Administration | i.p. |
| Molecular Weight | 518.55 |
| Formula | C30H30O8 |
| CAS Number | 303-45-7 |
| Solubility (25°C) | 25 mM in DMSO |
| Storage | 2-8°C, protect from light |
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| AT-101
AT-101 (R-(-)-gossypol acetic acid) is a pan small molecule inhibitor of Bcl-2, Bcl-xL, and Mcl-1. |
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