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。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。
Destruxin B (9CI);.β.-Alanine, N-[N-[N-[N-[1-(D-2-hydroxy-4-methyl-1-oxopentyl)-L-prolyl]-L-isoleucyl]-N-methyl-L-valyl]-N-methyl-L-alanyl]-, .ρ.-lactone;destruxin B
Cas No.
2503-26-6
分子式
C30H51N5O7
分子量
593.76
包装储存
Powder; -20°C; 3 years; 4°C; 2 years;
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.
性状
Solid
IC50 & Target[1][2]
Bcl-2 Caspase-3
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?μMand 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 . Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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.Medlife has not independently confirmed the accuracy of these methods. They are for reference only.Animal Model:Athymic fe