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.
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Bcl-2 Products |
|---|
| BAD (103-127) (human)
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. |
| Bim BH3, Peptide IV
Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins. |
| Bax inhibitor peptide, negative control
Bax inhibitor peptide, negative control is a inhibitor of Bax. |
| Bad BH3 (mouse)
Bad BH3 (mouse) is a biological active peptide. |
| Bid BH3 (80-99)
Bid BH3 (80-99) is a biological active peptide. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
