Abstract
AIM: To investigate the effect of melittin (Mel) of Na+, K+-ATPase activity and it's kinetic mode of action on guinea pig myocardial mitochondria. METHODS: Effect of Mel on heart mitochondrial Na+, K+-ATPase activity was determined with colorimetry method. RESULTS: Mel inhibited Na+, K+-ATPase in a concentration and time dependent manner, IC50 was 2.60 μmol/L. Kinetic studies of interaction between Mel and K+, Na+, ATP revealed that inhibitory effect of Mel was competitive with K+, but not with Na+ and ATP. CONCLUSION: Mel polypeptide potently inhibits Na+, K+-ATPase, possibly by binding to the K+ site.
| Original language | English |
|---|---|
| Pages (from-to) | 279-282 |
| Number of pages | 4 |
| Journal | Acta Pharmacologica Sinica |
| Volume | 22 |
| Issue number | 3 |
| State | Published - 2001 |
| Externally published | Yes |
Keywords
- Bee venoms
- Melittin
- Mitochondria
- Myocardium
- Na, K-exchanging ATPase