绿僵菌素B, 来源于绿僵菌属

中文名称:

绿僵菌素B, 来源于绿僵菌属

中文同义词:

绿僵菌素B, 来源于绿僵菌属;绿僵菌素B;黑僵菌素 B

英文名称:

destruxin B

英文同义词:

destruxin B;N-[N-[(2R)-1-Oxo-2-hydroxy-4-methylpentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone;N-[N-[(R)-2-Hydroxy-4-methyl-1-oxopentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone;Destruxin B, 97.5%, from Metarrhizium anisopliae;Destruxin B from Metarhizium anisopliae;Cyclo[N-methyl-L-alanyl-β-alanyl-(2R)-2-hydroxy-4-methylpentanoyl-L-prolyl-L-isoleucyl-N-methyl-L-valyl];Destruxin B, from Metarrhizium anisopliae

CAS号:

2503-26-6

分子式:

C30H51N5O7

分子量:

593.76

EINECS号:

相关类别:

医药原料

Mol文件:

2503-26-6.mol

熔点 

234 °C

沸点 

875.0±65.0 °C(Predicted)

密度 

1.17±0.1 g/cm3(Predicted)

酸度系数(pKa)

13.54±0.70(Predicted)

生物活性

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。

靶点

Bcl-2 Caspase-3

Bcl-2

Caspase-3

体外研究

Destruxin B (1-30 μM; 48 hours) inhibits cell proliferation of H1299 cells and A549 cells, with IC 50 s 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 IC 50 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 IC 50 s 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.

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 IC 50 of 4.1 μM.

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 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 IC 50 s at 24 h, 48 h and 72h were determined as 14.97, 2.00 and 0.67 μM, respectively.

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.

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.