Destruxin B (Synonyms:黑僵菌素 B)
目录号 : KM20483 CAS No. : 2503-26-6

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。

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生物活性

Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.

体外研究

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.
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.
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.
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 .

Cell Proliferation Assay

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 IC50 of 4.1 μM.

Apoptosis Analysis

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

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

Cell Line: A549 cells
Concentration: 10 or 20 μM
Incubation Time: 12 and 24  hours
Result: Regulates Mcl-1 and PUMA.
体内研究

Destruxin B (DB) ( injection; 0.6-15 mg/kg/day for 6 weeks) attenuates the tumor growth in time- and dose-dependent manners.

Animal Model: Athymic female nude mice (BALB/cAnN.Cg-Foxn1nu/CrlNarl), approximately 4-5 weeks old on arrival
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.
分子式
C30H51N5O7
分子量
621.81
CAS号
2503-26-6
中文名称
黑僵菌素 B
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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The dilution calculator equation
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This equation is commonly abbreviated as: C1V1 = C2V2
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