Colletofragarone A2 可从真菌Colletotrichum sp. (13S020) 中分离获得。Colletofragarone A2 抑制p53突变蛋白和HSP90，具有抗癌活性。Colletofragarone A2 能够促进p53突变蛋白降解和聚合，并抑制体内肿瘤生长。
| 生物活性 | Colletofragarone A2 can be be isolated from the fungusColletotrichum sp. (13S020). Colletofragarone A2 inhibits mutantp53andHSP90with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutantp53and suppressing tumor growth in vivo[1]. |
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体外研究
(In Vitro) | Mutant p53 loses original tumor suppressor function but acquires new abilities regarding oncogenic progression[1].
Colletofragarone A2 (0.05-5 μM; 72 h) shows high selectivity and more cytotoxic activity on cells with p53R175H structural mutants than with other p53 statuses such as a DNA-contact mutant, wild-type, and null cells[1].
Colletofragarone A2 (2 μM; 8 h) decreases mutant p53 levels in SK-BR-3 (p53R175H) cells by promoting p53 degradation[1].
Colletofragarone A2, combinded with 10 μMMG-132(HY-13259), (2 or 4 μM; 4 h) induces the accumulation of the aggregated mutant p53[1].
Western Blot Analysis[1] | Cell Line: | SK-BR-3 (p53R175H), HuCCT1 (p53R175H), Saos-2 (p53R175H), OVCAR-3 (p53R248Q), and A549 (wild-type p53) | | Concentration: | 0, 0.5, 1, 2, 4 μM | | Incubation Time: | 4 hours | | Result: | Decreased the mutant p53R175Hlevels in SK-BR-3 and HuCCT1 cells in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | SK-BR-3 (p53R175H) cells | | Concentration: | 2 μM, 4 μM (with 10 μMMG-132(HY-13259), respectively) | | Incubation Time: | 4 hours | | Result: | Promoted the proteasome-mediated degradation of mutant p53 and the accumulation of precipitated mutant p53. |
Cell Viability Assay[1] | Cell Line: | SK-BR-3 (p53R175H), HuCCT1 (p53R175H), OVCAR-3 (p53R248Q), and A549 (wild-type p53) cells | | Concentration: | 0.05-5 μM | | Incubation Time: | 72 hours | | Result: | Decreased the level of p53 and showed high selectivity and more cytotoxic activity on cells with p53R175H structural mutants, IC50s of 0.18 μM (SK-BR-3), 0.35 μM (HuCCT1), respectively. |
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体内研究
(In Vivo) | Colletofragarone A2 (0.35 mM, 100 μL; injected intratumorally and daily; 13 d) markedly decreases tumor cell growth in mouse infected with HuCCT1 (p53R175H) cells[1].
| Animal Model: | Xenograft model with HuCCT1 (p53R175H) cells in mouse[1] | | Dosage: | 0.35 mM with 100 μL (DMSO solution) | | Administration: | Injected intratumorally; daily; 13 days; tested tumor growth at 1, 3, 5, 7, 9, 13 days | | Result: | Inhibited tumor growth without lowing body weight of mouse. |
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| 结构分类 | - Terpenoids
- Other Terpenoids
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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