Bioprospetion of the Brazilian arthropods fauna searching for leader drugs for rational development of novel pharmaceuticals and pesticides

• Grant number: 04/07942-2
• Support Opportunities: BIOTA-FAPESP Program - Regular Research Grants
• Start date: February 01, 2005
• End date: January 31, 2007
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Mario Sergio Palma
• Grantee: Mario Sergio Palma
• Host Institution: Instituto de Biociências (IB). Universidade Estadual Paulista (UNESP). Campus de Rio Claro. Rio Claro , SP, Brazil

Abstract

Many of the medicines prescribed today were initially discovered in nature. Despite the advances in chemistry and the sophisticated instruments used for the combinatorial synthesis of new drugs, scientists still have recourse to nature as a source of inspiration for the development of new compounds. A substantial fraction of the medicines in use today was directly or indirectly derived from bioactive compounds produced by plants and/or microorganisms. Recently, compounds of low molecular weight of animal origin have also been the object of interest of agrochemical and/or pharmaceutical industries. Arthropods are considered a potentially very important source of new molecules which offer notable properties such as: high efficiency, low probability of microbial resistance, limited toxicity and low immunogenicity for humans. Spiders and wasps constitute a large group of arthropods present in the majority of terrestrial ecosystems. The toxic secretions of spiders and wasps are used to paralyze the insect-prey through the paralysis of the synaptic transmission of the neuromuscular junctions of those insects (Palma et al., 1997). Considerable efforts have been made to isolate and identify neuroactive compounds in the secretions of spiders and wasps, resulting in the discovery of many molecules which block the receptors of glutamate and/or calcium channels. Thus, many of these compounds have become structural models for the rational development of neuroprotective drugs for different neurological disorders. The small organic molecules existing in many of the toxic secretions of spiders and wasps are natural candidates for bioprospection for leader-compounds for the development of drugs for neurotherapeutic use and/or as selective bioinsecticides. The principal proposal of this project is the systematic investigation from the point of view of chemical characterization and of biological trials, of the natural products present in the exocrine secretions of a toxic nature, principally in venoms of Arthropods of the Brazilian fauna, such as spiders and wasps. (AU)

Scientific publications

(18)

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

CESAR-TOGNOLI, LILIAN M. M.; SALAMONI, SIMONE D.; TAVARES, ANDREA A.; ELIAS, CAROL F.; DA COSTA, JADERSON C.; BITTENCOURT, JACKSON C.; PALMA, MARIO S.. Effects of Spider Venom Toxin PWTX-I (6-Hydroxytrypargine) on the Central Nervous System of Rats. TOXINS, v. 3, n. 2, p. 142-162, FEB 2011. (06/57122-7, 04/07942-2)

SAIDEMBERG, DANIEL M.; BAPTISTA-SAIDEMBERG, NICOLI B.; PALMA, MARIO S.. Chemometric analysis of Hymenoptera toxins and defensins: A model for predicting the biological activity of novel peptides from venoms and hemolymph. Peptides, v. 32, n. 9, p. 1924-1933, SEP 2011. (04/07942-2)

GOMES, PAULO C.; DE SOUZA, BIBIANA M.; DIAS, NATHALIA B.; CESAR-TOGNOLI, LILIAN M. M.; SILVA-FILHO, LUIZ C.; TORMENA, CLAUDIO F.; RITTNER, ROBERTO; RICHARDSON, MICHAEL; CORDEIRO, MARTA N.; PALMA, MARIO S.. Nigriventrine: A low molecular mass neuroactive compound from the venom of the spider Phoneutria nigriventer. Toxicon, v. 57, n. 2, p. 266-274, FEB 2011. (04/07942-2)

BRIGATTE, P.; CURY, Y.; DE SOUZA, B. M.; BAPTISTA-SAIDEMBERG, N. B.; SAIDEMBERG, D. M.; GUTIERREZ, V. P.; PALMA, MARIO SERGIO. Hyperalgesic and edematogenic effects of peptides isolated from the venoms of honeybee (Apis mellifera) and neotropical social wasps (Polybia paulista and Protonectarina sylveirae). Amino Acids, v. 40, n. 1, p. 101-111, JAN 2011. (04/07942-2)

DE SOUZA, BIBIANA MONSON; DOS SANTOS CABRERA, MARCIA PEREZ; RUGGIERO NETO, JOAO; PALMA, MARIO SERGIO. Investigating the effect of different positioning of lysine residues along the peptide chain of mastoparans for their secondary structures and biological activities. Amino Acids, v. 40, n. 1, p. 77-90, JAN 2011. (04/07942-2)

BAPTISTA-SAIDEMBERG, NICOLI B.; SAIDEMBERG, DANIEL M.; DE SOUZA, BIBIANA M.; CESAR-TOGNOLI, LILIAN M. M.; FERREIRA, VIRGINIA M. R.; MENDES, MARIA ANITA; DOS SANTOS CABRERA, MARCIA P.; RUGGIERO NETO, JOAO; PALMA, MARIO S.. Protonectin (1-6): A novel chemotactic peptide from the venom of the social wasp Agelaia pallipes pallipes. Toxicon, v. 56, n. 6, p. 880-889, NOV 2010. (04/07942-2)

DA SILVA, ALESSANDRA. V. R.; DE SOUZA, BIBIANA M.; DOS SANTOS CABRERA, MARCIA P.; DIAS, NATHALIA B.; GOMES, PAULO C.; RUGGIERO NETO, JOAO; STABELI, RODRIGO G.; PALMA, MARIO S.. The effects of the C-terminal amidation of mastoparans on their biological actions and interactions with membrane-mimetic systems. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, v. 1838, n. 10, p. 2357-2368, OCT 2014. (04/07942-2, 11/51684-1)

MOURELLE, D.; BRIGATTE, P.; BRINGANTI, L. D. B.; DE SOUZA, B. M.; ARCURI, H. A.; GOMES, P. C.; BAPTISTA-SAIDEMBERG, N. B.; RUGGIERO NETO, J.; PALMA, M. S.. Hyperalgesic and edematogenic effects of Secapin-2, a peptide isolated from Africanized honeybee (Apis mellifera) venom. Peptides, v. 59, p. 42-52, SEP 2014. (04/07942-2, 11/51684-1)

CESAR, LILIAN M. M.; MENDES, MARIA A.; TORMENA, CLAUDIO F.; MARQUES, MAURÍCIO R.; SOUZA, BIBIANA M. DE; SAIDEMBERG, DANIEL MENEZES; BITTENCOURT, JACKSON C.; PALMA, MÁRIO S.. Isolation and chemical characterization of PwTx-II: A novel alkaloid toxin from the venom of the spider Parawixia bistriata (Araneidae, Araneae). Toxicon, v. 46, n. 7, p. 786-796, Dec. 2005. (04/07942-2)

SALLES, HELIANA C.; VOLSI, EVELYN CRISTINA F. R.; MARQUES, MAURÍCIO R.; SOUZA, BIBIANA M.; SANTOS, LUCILENE D. DOS; TORMENA, CLÁUDIO F.; MENDES, MARIA A.; PALMA, MÁRIO S.. The venomous secrets of the web droplets from the viscid spiral of the orb-weaver spider Nephila clavipes (Araneae, Tetragnatidae). CHEMISTRY & BIODIVERSITY, v. 3, n. 7, p. 727-741, 2006. (04/07942-2)

CABRERA, MARCIA PEREZ DOS SANTOS; COSTA, SABRINA THAIS BROGGIO; SOUZA, BIBIANA MONSON DE; PALMA, MÁRIO SÉRGIO; RUGGIERO, JOSÉ ROBERTO; RUGGIERO NETO, JOÃO. Selectivity in the mechanism of action of antimicrobial mastoparan peptide Polybia-MP1. EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS, v. 37, n. 6, p. 879-891, July 2008. (04/07942-2)

SALLES‚ H.C.; VOLSI‚ E.C.F.R.; MARQUES‚ M.R.; SOUZA‚ B.M.; DOS SANTOS‚ L.D.; TORMENA‚ C.F.; MENDES‚ M.A.; PALMA‚ M.S.. The Venomous Secrets of the Web Droplets from the Viscid Spiral of the Orb-Weaver Spider Nephila clavipes (Araneae‚ Tetragnatidae). CHEMISTRY & BIODIVERSITY, v. 3, n. 7, p. 727-741, 2006. (04/07942-2)

CESAR, LILIAN MARI MARCONDES; TORMENA, CLAUDIO FRANCISCO; MARQUES, MAURICIO RIBEIRO; SILVA, GIL V. J.; MENDES, MARIA ANITA; RITTNER, ROBERTO; PALMA, MARIO SERGIO. Structure determination of hydroxytrypargine: A new tetrahydro-beta-carboline toxin from the venom of the spider Parawixia bistriata. Helvetica Chimica Acta, v. 88, n. 4, p. 796-801, Apr. 2005. (04/07942-2)

SAIDEMBERG, DANIEL M.; FERREIRA, MARCO A. B.; TAKAHASHI, TATIANE N.; GOMES, PAULO C.; CESAR-TOGNOLI, LILIAN M. M.; DA SILVA-FILHO, LUIZ C.; TORMENA, CLAUDIO F.; DA SILVA, GIL V. J.; PALMA, MARIO S.. Monoamine oxidase inhibitory activities of indolylalkaloid toxins from the venom of the colonial spider Parawixia bistriata: Functional characterization of PwTX-I. Toxicon, v. 54, n. 6, p. 717-724, NOV 2009. (06/57122-7, 04/07942-2)

SAIDEMBERG, DANIEL M.; DA SILVA-FILHO, LUIZ C.; CESAR TOGNOLI, LILIAN M. M.; TORMENA, CLAUDIO F.; PALMA, MARIO S.. Polybioside, a Neuroactive Compound from the Venom of the Social Wasp Polybia paulista. Journal of Natural Products, v. 73, n. 4, p. 527-531, APR 2010. (04/07942-2)

DE SOUZA, BIBIANA MONSON; PALMA, MARIO SERGIO. Monitoring the positioning of short polycationic peptides in model lipid bilayers by combining hydrogen/deuterium exchange and electrospray ionization mass spectrometry. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, v. 1778, n. 12, p. 2797-2805, DEC 2008. (04/07942-2)

DE SOUZA, BIBIANA MONSON; RODRIGUES DA SILVA, ALESSANDRA VASO; FERREIRA RESENDE, VIRGINIA MARIA; ARCURI, HELEN ANDRADE; DOS SANTOS CABRERA, MARCIA PEREZ; RUGGIERO NETO, JOAO; PALMA, MARIO SERGIO. Characterization of two novel polyfunctional mastoparan peptides from the venom of the social wasp Polybia paulista. Peptides, v. 30, n. 8, p. 1387-1395, AUG 2009. (04/07942-2)

MENDES‚ M.A.; PALMA‚ M.S.. Two new bradykinin-related peptides from the venom of the social wasp Protopolybia exigua( Saussure). Peptides, v. 27, n. 11, p. 2632-2639, 2006. (04/07942-2)