| Catalogue number |
C100831 |
| Chemical name | Crebanine |
| CAS Number | 25127-29-1 |
| Synonyms | 9,10-dimethoxy-7-methyl-6,7,7a,8-tetrahydro-5H-[1,3]benzodioxolo[6,5,4-de]benzo[g]quinoline |
| Molecular Weight | C20H21NO4 |
| Formula | 339.4 |
| Purity | 98% |
| Physical Description | Cryst. |
| Solvent | Chloroform, Dichloromethane,DMSO |
| Storage | Stored at 2-8°C, Protected from air and light, refrigerate or freeze |
| Applications | Crebanine (Cre) iv 5mg/kg could eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and could significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. The drug could also decrease the incidence of VF and CA by CaCl_2 in rats and by chloroform in mice, but had no proteetive effects on ouahain-indueed arrhythmias in guinea pigs.
The observed actions of crebanine against amnesia and its effect on α7-nAChRs will be beneficial for target-based drug design; crebanine or its scaffold can be used as the starting point to develop a drug for Alzheimer's disease. The cognition-enhancing effects of crebanine and the underlying mechanism based on α7-nAChRs are consistent with its traditional use. These findings demonstrate the potential utility of crebanine in the development of neurodegenerative therapy.
Crebanine treatment was found to significantly inhibit the proliferation of human leukemic cells (HL-60, U937 and K562), human fibrosarcoma cells (HT1080) and cervix cancer cell lines (KB-3-1 and KB-V1), of which HL-60 cells were the most sensitive to its treatment. In contrast, crebanine caused much less toxicity in human normal fibroblast cells. Our results demonstrated that crebanine mediated cell cycle arrest at G0/G1 phase and this was associated with down-regulation of cyclins A and D. In addition, crebanine induced apoptosis, which was detected by observation of the membrane phospholipid exposure in flow cytometry. Its induction of apoptosis was accompanied by an increase in cleavage of caspase-3, -8, -9 and poly(ADP-ribose) polymerase (PARP), and was attributable to the augmentation of Bax/Bcl proteins level. Crebanine also decreased mitochondrial membrane potential. Taken together, crebanine exerts anti-proliferative effects on human cancer cells through the induction of cell cycle arrest at the G1 phases and apoptosis. Our results suggest that crebanine is a promising new candidate as a chemotherapeutic agent for cancer therapy.
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| References | 1. J. Chem. Soc., 1958, 983-985.
2. Zhongguo Zhong Yao Za Zhi, 1992, 17(11), 685-687, 704.
3. Phytochemistry, 2003, 63, 711-720.
4. Life Sci., 2012, 91(3-4), 107-114.
5. Chem. Pharm. Bull., 2012, 60(10), 1283-1289.
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| Size | Price(USD) | Discount |
| 5mg | Inquiry | N/A |
| 10mg | Inquiry | N/A |
| 25mg | Inquiry | N/A |
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