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2503-26-6

中文名称 绿僵菌素B, 来源于绿僵菌属
英文名称 destruxin B
CAS 2503-26-6
分子式 C30H51N5O7
分子量 593.76
MOL 文件 2503-26-6.mol
2503-26-6 结构式 2503-26-6 结构式

基本信息

中文别名
绿僵菌素B
黑僵菌素 B
绿僵菌素B, 来源于绿僵菌属
英文别名
destruxin B
Destruxin B from Metarhizium anisopliae
Destruxin B, from Metarrhizium anisopliae
Destruxin B, 97.5%, from Metarrhizium anisopliae
N-[N-[(R)-2-Hydroxy-4-methyl-1-oxopentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone
Cyclo[N-methyl-L-alanyl-β-alanyl-(2R)-2-hydroxy-4-methylpentanoyl-L-prolyl-L-isoleucyl-N-methyl-L-valyl]
N-[N-[(2R)-1-Oxo-2-hydroxy-4-methylpentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone

物理化学性质

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
溶解度溶于DMSO(高达10mg/ml)
酸度系数(pKa)13.54±0.70(Predicted)
形态固体
颜色白色
稳定性可在-20°C下的DMSO溶液保存长达1个月。

安全数据

海关编码2933790090
绿僵菌素B, 来源于绿僵菌属价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-N6690绿僵菌素B, 来源于绿僵菌属
Destruxin B
2503-26-61mg7800元
2023/10/26HY-N6690绿僵菌素B, 来源于绿僵菌属
Destruxin B
2503-26-65mg27500元

常见问题列表

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.
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