Destruxin B 是从昆虫病原真菌中分离的绿僵菌 (Metarhizium anisopliae)，是一种具有杀虫和抗癌活性的环肽。 Destruxin B 通过Bcl-2 家族依赖的线粒体途径在人类非小细胞肺癌细胞中诱导细胞凋亡。Destruxin B 显著激活caspase-3，并在体外和体内通过 caspase 介导的细胞凋亡减少肿瘤细胞增殖。
| 生物活性 | Destruxin B, isolated from entomopathogenic fungusMetarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B inducesapoptosisvia aBcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lungcancercells[1]. Destruxin B significantly activatescaspase-3and reduces tumor cell proliferation through caspase-mediatedapoptosis, not only in vitro but also in vivo[2]. |
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体外研究
(In Vitro) | Destruxin B (1-30 μM; 48 hours) inhibits cell proliferation of H1299 cells and A549 cells, with IC50s of 4.1 μM and 4.9 μM, respectively[1].
Activation of mitochondria-dependent caspase cascade plays an important role in Destruxin B (1-30 μM; 48 hours) induced apoptotic cell death in A549 cells[1].
Destruxin B (1.25-20.00 μM; 72 hours) treatment significantly inhibits HT-29 human colorectal cancer cells viability in time- and dose-dependent manners[2].
Destruxin B (10 or 20 μM; 12 and 24 hours) treatment markedly increases levels of the proapoptotic protein PUMA and reduces levels of antiapoptotic proteins Mcl-1 of A549 cells in a concentration- and time-dependent manner[1].
Cell Proliferation Assay[1] | Cell Line: | H1299 cells | | Concentration: | 1, 5, 10, 20, 30 μM | | Incubation Time: | 48 hours | | Result: | Inhibited H1299 cells proliferation of H1299 cells with an IC50of 4.1 μM. |
Apoptosis Analysis[1] | Cell Line: | Lung adenocarcinoma A549 cells | | Concentration: | 1, 5, 10, 20, 30 μM | | Incubation Time: | 48 hours | | Result: | Induces caspase-dependent Lung adenocarcinoma A549 cells death. |
Cell Viability Assay[2] | Cell Line: | HT-29 human colorectal cancer cells | | Concentration: | 1.25, 2.50, 5.00, 10.00 and 20.00 μM | | Incubation Time: | 72 hours | | Result: | The IC50s at 24 h, 48 h and 72h were determined as 14.97, 2.00 and 0.67 μM, respectively. |
Western Blot Analysis[1] | Cell Line: | A549 cells | | Concentration: | 10 or 20 μM | | Incubation Time: | 12 and 24 hours | | Result: | Regulates Mcl-1 and PUMA. |
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体内研究
(In Vivo) | Destruxin B (DB) ( injection; 0.6-15 mg/kg/day for 6 weeks) attenuates the tumor growth in time- and dose-dependent manners[2].
| Animal Model: | Athymic female nude mice (BALB/cAnN.Cg-Foxn1nu/CrlNarl), approximately 4-5 weeks old on arrival[2] | | Dosage: | Low dose (0.6 mg/kg), medium dose (3 mg/kg), high dose (15 mg/kg) | | Administration: | Injection; daily; for 6 weeks | | Result: | Low dose, medium dose and high dose indicated a reduction of 23.9%, 33.4% and 55.8% in mean tumor size, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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