[CAS NO. 2503-26-6] Destruxin B
PRODUCTS SPECIFICATIONS [2503-26-6]
DESCRIPTION [2503-26-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 621.81 |
| Molecular Formula | C32H55N5O7 |
| SMILES | O=C(N[C@]([C@@H](C)CC)(C)C(N(C)[C@@H](C(C)C)C(N(C)[C@@H](C)C(NCC1)=O)=O)=O)[C@@](CCC2)(C)N2C([C@@H](CC(C)C)OC1=O)=O |
Summary
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 [1] . Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis , not only in vitro but also in vivo [2] .
IC50 & Target
|
Bcl-2 |
Caspase-3 |
In Vitro
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
[1]
.
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
[1]
.
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
[2]
.
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| 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 [1]
| 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 [2]
| 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 [1]
| Cell Line: | A549 cells |
| Concentration: | 10 or 20 μM |
| Incubation Time: | 12 and 24 hours |
| Result: | Regulates Mcl-1 and PUMA. |
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Athymic female nude mice (BALB/cAnN.Cg-Foxn1nu/CrlNarl), approximately 4-5 weeks old on arrival [2] |
| 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. |
Appearance
Solid
Source
Metarhizium anisopliae
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
References
- [1] Wu CC, et al. Destruxin B Isolated from Entomopathogenic Fungus Induces Apoptosis via a Bcl-2 Family-Dependent Mitochondrial Pathway in Human NonsmallCell Lung Cancer Cells. Evid Based Complement Alternat Med. 2013;2013:548929.
- [2] Lee YP, et al. In vitro and in vivo anticancer effects of destruxin B on human colorectal cancer. Anticancer Res. 2012 Jul;32(7):2735-45.