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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Monoamine oxidase inhibitory activities of indolylalkaloid toxins from the venom of the colonial spider Parawixia bistriata: Functional characterization of PwTX-I

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Saidemberg, Daniel M. [1] ; Ferreira, Marco A. B. [2] ; Takahashi, Tatiane N. [1] ; Gomes, Paulo C. [1, 3] ; Cesar-Tognoli, Lilian M. M. [1] ; da Silva-Filho, Luiz C. [4] ; Tormena, Claudio F. [5] ; da Silva, Gil V. J. [2] ; Palma, Mario S. [1]
Total Authors: 9
[1] Sao Paulo State Univ, UNESP, Inst Biosci, Dept Biol, CEIS, Lab Struct Biol & Zoochem, BR-13506900 Rio Claro, SP - Brazil
[2] Univ Sao Paulo, FFCLRP, Dept Chem, BR-14040901 Ribeirao Preto, SP - Brazil
[3] Ezequiel Dias Fdn FUNED, Directory Res & Dev, BR-30510010 Belo Horizonte, MG - Brazil
[4] Sao Paulo State Univ, UNESP, Fac Sci, Dept Chem, BR-17033360 Sao Paulo - Brazil
[5] Univ Estadual Campinas, Inst Chem, BR-13084971 Campinas, SP - Brazil
Total Affiliations: 5
Document type: Journal article
Source: Toxicon; v. 54, n. 6, p. 717-724, NOV 2009.
Web of Science Citations: 15

Colonial spiders evolved a differential prey-capture behaviour in concert with their venom chemistry, which may be a source of novel drugs. Some highly active tetrahydro-beta-carboline (TH beta C) toxins were recently isolated from the venom of the colonial spider Parawixia bistriata; the spiders use these toxins as part of their chemical arsenal to kill and/or paralyze preys. The major TH beta C compound isolated from this venom was identified as 6-hydroxytrypargine, also known as PwTX-I. Most natural compounds of animal origin occur in low abundance, and the natural abundance of PwTX-I is insufficient for complete functional characterization. Thus, PwTx-I was synthesized using a Pictet-Spengler condensation strategy, and the stereoisomers of the synthetic toxin were separated by chiral chromatography. The fraction of venom containing a mixture of three natural TH beta C toxins and enantiomers of PwTx-I were analyzed for inhibition of monoamine oxidase (MAO)-A and -B and for toxicity to insects. We reveal that the mixture of the natural TH beta C toxins, as well as the enantiomers of PwTx-I, were non-competitive inhibitors of MAO-A and MAO-B and caused potent paralysis of honeybees. The (-)-PwTX-I enantiomer is 2-fold more potent than the (+)-PwTX-I enantiomer in the assays performed. (C) 2009 Elsevier Ltd. All rights reserved. (AU)

FAPESP's process: 06/57122-7 - Searching for lead compounds for rational development of new drugs and pesticides through bioprospecting in Brazilian arthropods
Grantee:Mario Sergio Palma
Support type: BIOTA-FAPESP Program - Thematic Grants
FAPESP's process: 04/07942-2 - Bioprospetion of the Brazilian arthropods fauna searching for leader drugs for rational development of novel pharmaceuticals and pesticides
Grantee:Mario Sergio Palma
Support type: BIOTA-FAPESP Program - Regular Research Grants