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Two-step inactivation of bee venom phospholipase A2 by scalaradial
Two-step inactivation of bee venom phospholipase A2 by scalaradial
- Source :
- Biochemical Pharmacology. 42:1621-1626
- Publication Year :
- 1991
- Publisher :
- Elsevier BV, 1991.
-
Abstract
- Scalaradial (SLD), a marine natural product isolated from the sponge (Cacospongia sp., possesses anti-inflammatory properties in vivo and in vitro (Pharmacologist 32: 168, 1990). In this study we characterize its effects against bee venom phospholipase A2 (PLA2; EC 3.1.1.4). SLD is a potent inactivator of bee venom PLA2 with an IC50 value of 0.07 microM. Inactivation of bee venom PLA2 occurred in a time-dependent, irreversible manner. The rate of inactivation followed first-order reaction kinetics and was dependent on the concentration of SLD. Kinetic analysis suggested a two-step mechanism of inactivation: an initial apparent noncovalent binding (Ki = 4.5 x 10(-5) M) followed by covalent modification. The rate of inactivation was reduced markedly in the presence of excess phosphatidylcholine, suggesting that modification of the enzyme occurs at or near the substrate binding site.
- Subjects :
- Sesterterpenes
Anti-Inflammatory Agents
Venom
complex mixtures
Biochemistry
Phospholipases A
chemistry.chemical_compound
Phospholipase A2
Phosphatidylcholine
Botany
medicine
Binding site
Pharmacology
chemistry.chemical_classification
HEPES
biology
Terpenes
Hydrogen-Ion Concentration
Bee Venoms
Kinetics
Phospholipases A2
Enzyme
Mechanism of action
chemistry
Enzyme inhibitor
biology.protein
Homosteroids
Steroids
medicine.symptom
Mathematics
Subjects
Details
- ISSN :
- 00062952
- Volume :
- 42
- Database :
- OpenAIRE
- Journal :
- Biochemical Pharmacology
- Accession number :
- edsair.doi.dedup.....cc2d366181be66081a9db3da4752b79c
- Full Text :
- https://doi.org/10.1016/0006-2952(91)90432-5