绿僵菌素B, 来源于绿僵菌属

生物活性靶点体外研究体内研究绿僵菌素B, 来源于绿僵菌属试剂级价格

绿僵菌素B, 来源于绿僵菌属

CAS号:2503-26-6
英文名:destruxin B
中文名:绿僵菌素B, 来源于绿僵菌属
CBNumber:CB81304031
分子式:C30H51N5O7
分子量:593.761
MOL File:2503-26-6.mol

绿僵菌素B, 来源于绿僵菌属化学性质

熔点 :234 °C
沸点 :875.0±65.0 °C(Predicted)
密度 :1.17±0.1 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :Soluble in DMSO (up to 10 mg/ml)
形态 :solid
酸度系数(pKa) :13.54±0.70(Predicted)
颜色 :White
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

安全信息

海关编码 :2933790090

绿僵菌素B, 来源于绿僵菌属性质、用途与生产工艺

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

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.

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.