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Isolation, Biochemical Characterization and Antiparasitic Activity of BmatTX-IV, A Basic Lys49-Phospholipase A2 from the Venom of Bothrops mattogrossensis from Paraguay.
- Source :
-
Current topics in medicinal chemistry [Curr Top Med Chem] 2019; Vol. 19 (22), pp. 2041-2048. - Publication Year :
- 2019
-
Abstract
- Background: Functional and structural diversity of proteins of snake venoms is coupled with a wide repertoire of pharmacological effects. Snake venoms are targets of studies linked to searching molecules with biotechnological potential.<br />Methods: A homologue phospholipase A2 (BmatTX-IV) was obtained using two chromatographic techniques. Mass spectrometry and two-dimensional gel electrophoresis were used to determine the molecular mass and isoelectric point, respectively. By means of Edman degradation chemistry, it was possible to obtain the partial sequence of amino acids that comprise the isolated toxin. Trypanocidal, leishmanicidal and cytoxic activity against Trypanosoma cruzi, Leishmania infantum and murine fibrobasts was determinated.<br />Results: Combination of both chromatographic steps used in this study demonstrated efficacy to obtain the PLA2-Lys49. BmatTX-IV showed molecular mass and isoelectric point of 13.55 kDa and 9.3, respectively. Amino acid sequence of N-terminal region (51 residues) shows the presence of Lys49 residue at position 49, a distinctive trait of enzymatically inactive PLA2. Bothrops mattogrossensis snake venom showed IC50 values of 11.9 μg/mL against Leishmania infantum promastigotes and of 13.8 μg/mL against Trypanosoma cruzi epimastigotes, respectively. On the other hand, the venom showed a high cytotoxic activity (IC50 value of 16.7 μg/mL) against murine fibroblasts, whereas the BmatTX-IV showed IC50 value of 81.2 μg/mL.<br />Conclusion: Physicochemical and biological characterization of snake venoms components is critically important, since these complex mixtures provide a source of molecules with antiparasitic potential, making further studies necessary to identify and characterize components with higher efficacy and selectivity.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
- Subjects :
- Animals
Antiparasitic Agents chemistry
Antiparasitic Agents isolation & purification
Bothrops
Dose-Response Relationship, Drug
Fibroblasts drug effects
Mice
Paraguay
Parasitic Sensitivity Tests
Phospholipases A2 chemistry
Phospholipases A2 isolation & purification
Snake Venoms chemistry
Snake Venoms isolation & purification
Structure-Activity Relationship
Antiparasitic Agents pharmacology
Leishmania infantum drug effects
Phospholipases A2 pharmacology
Snake Venoms pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1873-4294
- Volume :
- 19
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Current topics in medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31340737
- Full Text :
- https://doi.org/10.2174/1568026619666190723154756