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Search for bioactive metabolites with antiparasitic action in plant species from Atlantic Forest and Cerrado regions - a chemical, phenotypical, and metabolomic approach

Grant number: 21/02789-7
Support Opportunities:BIOTA-FAPESP Program - Regular Research Grants
Start date: August 01, 2021
End date: July 31, 2023
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:João Henrique Ghilardi Lago
Grantee:João Henrique Ghilardi Lago
Host Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Ministério da Educação (Brasil). Santo André , SP, Brazil
Associated researchers:André Gustavo Tempone Cardoso ; Célio Fernando Figueiredo Angolini ; Josué de Moraes ; Luiz Felipe Domingues Passero ; Patricia Sartorelli

Abstract

In the present project, the prospective studies of bioactive molecules will be continued, especially with antiparasitic action (antileishmanial, antitrypanosomal and/or anthelmintic), originating from plant species belonging mainly to Annonaceae, Asteraceae, Lauraceae and Piperaceae occurring in Atlantic Forest and "Cerrado" areas of the State of São Paulo. Initially, selected species will be collected, and their extracts prepared, and those with proven antiparasitic action will be subjected to molecular dereplication processes through analysis via HPLC/MS assisted by the open platform Global Natural Products Social Molecular Networking (GNPS). Once new bioactive chemical entities are recognized, they will be isolated by chromatographic fractionation and structurally characterized by spectroscopic/spectrometric techniques (UV, IR, NMR, MS, DC, VCD). After identification of the active substances, they may be subjected to molecular changes guided by analysis of ADME/Tox properties in silico in order to optimize biological activities and/or reduce toxicity. Additionally, it is intended, in this proposal, to carry out specific tests to define the phenotypic mode of action of substances with proven activity in relation to the parasite, especially the evaluation in the membrane pore and ultrastructural studies as well as using metabolomic tools (HPLC/MS and GC/MS in conjunction with chemometric analyzes) to study the effect on the production of metabolites in the parasite, after treatment with the tested substances, in order to corroborate the phenotypic information. Finally, selected compounds (natural or semi-synthetic) that have high in vitro potential, reduced toxicity and that meet the criteria recommended by the analyzes via ADME/Tox in silico, will be subjected to pre-clinical studies. In this way, the present project intends to add new compounds with proven pharmacological activity to the restricted therapeutic arsenal of these neglected diseases, providing tools for the development of new drugs of plant origin. (AU)

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Scientific publications (37)
(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)
MATHEUS L. SILVA; LEILA GIMENES; PAULETE ROMOFF; MARISI G. SOARES; FERNANDA F. CAMILO; ERICA VALADARES DE C. LEVATTI; ANDRE G. TEMPONE; JOÃO HENRIQUE G. LAGO. FENILPROPANOIDES COM AÇÃO ANTI-Trypanosoma cruzi ISOLADOS DE Baccharis ligustrina C. DC. (ASTERACEAE). Química Nova, v. 46, n. 1, p. 39-42, . (21/02789-7)
SILVA, MATHEUS L.; COSTA-SILVA, THAIS A.; ANTAR, GUILHERME M.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. Chemical Constituents from Aerial Parts of Baccharis sphenophylla and Effects against Intracellular Forms of Trypanosoma cruzi. CHEMISTRY & BIODIVERSITY, v. 18, n. 10, . (21/02789-7)
CARNAUBA, PAULO U.; MENGARDA, ANA C.; RODRIGUES, VINICIUS C.; MORAIS, THIAGO R.; DE OLIVEIRA, ALBERTO; LAGO, JOAO HENRIQUE G.; DE MORAES, JOSUE. Evaluation of Gibbilimbol B, Isolated from Piper malacophyllum (Piperaceae), as an Antischistosomal Agent. CHEMISTRY & BIODIVERSITY, v. 18, n. 10, . (16/22488-3, 19/25289-0, 21/02789-7, 19/25905-2)
SILVA MAIOLINI, TATIANE CRISTINA; ROSA, WELTON; MIRANDA, DANIEL OLIVEIRA; COSTA-SILVA, THAIS A.; TEMPONE, ANDRE G.; PIRES BUENO, PAULA CAROLINA; DIAS, DANIELLE FERREIRA; CHAGAS DE PAULA, DANIELA APARECIDA; SARTORELLI, PATRICIA; LAGO, JOAO HENRIQUE G.; et al. Essential Oils from Different Myrtaceae Species from Brazilian Atlantic Forest Biome - Chemical Dereplication and Evaluation of Antitrypanosomal Activity. CHEMISTRY & BIODIVERSITY, v. 19, n. 6, p. 13-pg., . (21/02789-7, 21/04464-8)
ARAUJO, SHEILA CRUZ; DE ANGELO, RAFAELA MOLINA; BARBOSA, HENRIQUE; COSTA-SILVA, THAIS ALVES; TEMPONE, ANDRE GUSTAVO; LAGO, JOAO HENRIQUE GHILARDI; HONORIO, KATHIA MARIA. Identification of inhibitors as drug candidates against Chagas disease. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 248, p. 17-pg., . (21/02789-7, 16/24524-7)
BRITO, JULIANA R.; WILAIRATANA, POLRAT; ROQUINI, DANIEL B.; PARRA, BEATRIZ C.; GONCALVES, MARINA M.; SOUZA, DALETE CHRISTINE S.; FERREIRA, EDGARD A.; SALVADORI, MARIA C.; TEIXEIRA, FERNANDA S.; LAGO, JOAO HENRIQUE G.; et al. Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni. SCIENTIFIC REPORTS, v. 12, n. 1, p. 12-pg., . (20/01441-4, 21/02789-7)
COSTA, MAYRA F.; LUIZ, MAYARA M.; SOUZA, LEONARDO C. DE; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.; NASCIMENTO, ISABELE R.. Phenylnaphthalic anhydrides from water hyacinth (Pontederia crassipes Mart.). PHYTOCHEMISTRY LETTERS, v. 46, p. 1-5, . (21/02789-7)
LONDERO, VINICIUS S.; ROSA, MATHEUS E.; BAITELLO, JOAO B.; COSTA-SILVA, THAIS A.; CRUZ, LUCAS MONTEIRO S.; TEMPONE, ANDRE G.; CASELI, LUCIANO; LAGO, JOAO HENRIQUE G.. Barbellatanic acid, a new antitrypanosomal pseudo-disesquiterpenoid isolated from Nectandra barbellata, displayed interaction with protozoan cell membrane. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, v. 1865, n. 7, p. 9-pg., . (22/03736-7, 18/22214-6, 14/50869-6, 21/02789-7, 21/15084-1, 17/17044-1)
FERREIRA, BRUNO ANTONIO; ROSA DE MOURA, FRANCYELLE BORGES; GOMES, KAIO SOUZA; DA SILVA SOUZA, DALETE CHRISTINE; GHILARDI LAGO, JOAO HENRIQUE; ARAUJO, FERNANDA DE ASSIS. Biseugenol from Ocotea cymbarum (Lauraceae) attenuates inflammation, angiogenesis and collagen deposition of sponge-induced fibrovascular tissue in mice. INFLAMMOPHARMACOLOGY, v. 31, n. 3, p. 11-pg., . (21/02789-7)
ROSA, MATHEUS ELIAS; CONSERVA, GEANNE A. ALVES; PASSERO, LUIZ FELIPE D.; LAGO, JOAO HENRIQUE G.; CASELI, LUCIANO. Unsaturated lipids modulating the interaction of the antileishmanial isolinderanolide E with models of cellular membranes. BIOORGANIC CHEMISTRY, v. 124, p. 7-pg., . (21/02789-7, 19/04407-4, 16/20633-6, 18/22214-6, 18/24077-6, 19/03239-0)
CONSERVA, GEANNE A.; COSTA-SILVA, THAIS A.; QUIROS-GUERRERO, LUIS M.; MARCOURT, LAURENCE; WOLFENDER, JEAN-LUC; QUEIROZ, EMERSON F.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. Kaempferol-3-O-alpha-(3,4-di-E-p-coumaroyl)-rhamnopyranoside from Nectandra oppositifolia releases Ca2+from intracellular pools of Trypanosoma cruzi affecting the bioenergetics system. Chemico-Biological Interactions, v. 349, . (16/20633-6, 21/04464-8, 21/02789-7, 18/18975-1)
DA COSTA-SILVA, THAIS A.; SILVA, MATHEUS L.; ANTAR, GUILHERME M.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. Ent-kaurane diterpenes isolated from n-hexane extract of Baccharis sphenophylla by bioactivity-guided fractionation target the acidocalcisomes in Trypanosoma cruzi. Phytomedicine, v. 93, . (21/04464-8, 21/02789-7)
GONCALVES, GIULIA ELISA G.; UMEHARA, ERIC; LAGO, JOAO HENRIQUE G.; CASELI, LUCIANO. Incorporation of dehydrodieugenol, a neolignan isolated from Nectandra leucantha (Lauraceae), in lipid Langmuir monolayers as biomembrane models. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, v. 1864, n. 11, p. 10-pg., . (19/03239-0, 21/02391-3, 21/02789-7)
ROMANELLI, MAIARA M.; AMARAL, MAIARA; THEVENARD, FERNANDA; CRUZ, LUCAS M. SANTA; REGASINI, LUIS O.; MIGOTTO, ALVARO E.; LAGO, JOAO HENRIQUE G.; TEMPONE, ANDRE G.. Mitochondrial Imbalance of Trypanosoma cruzi Induced by the Marine Alkaloid 6-Bromo-2 '-de-N-Methylaplysinopsin. ACS OMEGA, v. 7, n. 32, p. 10-pg., . (17/50333-7, 21/04464-8, 21/02789-7)
LEAO, LUIZ P. M. O.; VIEIRA, NATALIE DE B.; OLIVEIRA, PAULA P. S.; CHAGAS-PAULA, DANIELA A.; SOARES, MARISI G.; SOUZA, THIAGO B.; BALDIM, JOAO L.; COSTA -SILVA, THAIS A.; TEMPONE, ANDRE G.; DIAS, DANIELLE F.; et al. Structure-activity relationship study of antitrypanosomal analogues of gibbilimbol B using multivariate analysis and computation-aided drug design. Bioorganic & Medicinal Chemistry Letters, v. 83, p. 4-pg., . (21/02789-7)
GONCALVES, GIULIA ELISA G.; OLIVEIRA, SAMUEL; GOMES, KAIO DE SOUZA; COSTA-SILVA, THAIS ALVES; TEMPONE, ANDRE GUSTAVO; LAGO, JOAO HENRIQUE GHILARDI; CASELI, LUCIANO. Effect of partial O-methylation in dehydrodieugenol on its antitrypanosomal activity-correlation with the toxicity using cell membrane models. Biophysical Chemistry, v. 296, p. 11-pg., . (19/03239-0, 21/02789-7, 22/03736-7)
PIRES, GUILHERME HENRIQUE DA CRUZ RAMOS; BARBOSA, HENRIQUE; ALMEIDA, ROBERTO BAPTISTA PEREIRA; LAGO, JOAO HENRIQUE GHILARDI; CASELI, LUCIANO. Ethanolamine phospholipids at the air-water interface as cell membranes models of microorganisms to study the nanotoxicology of sakuranetin. Thin Solid Films, v. 770, p. 8-pg., . (19/03239-0, 19/18125-0, 18/22214-6, 21/02789-7, 22/03736-7)
ARAUJO, SHEILA C.; SOUSA, FERNANDA S.; COSTA-SILVA, THAIS A.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.; HONORIO, KATHIA M.. Discovery of New Hits as Antitrypanosomal Agents by In Silico and In Vitro Assays Using Neolignan-Inspired Natural Products from Nectandra leucantha. Molecules, v. 26, n. 14, . (18/07885-1, 21/04464-8, 16/24524-7, 21/02789-7)
REIS, ISABELLA MARY A.; UMEHARA, ERIC; CONCEICAO, RODRIGO S.; DE M. OLIVEIRA, LARISSA; DOS S. JUNIOR, MANOELITO COELHO; COSTA-SILVA, THAIS A.; AMARAL, MAIARA; TEMPONE, ANDRE G.; BRANCO, ALEXSANDRO; LAGO, JOAO HENRIQUE G.. gamma-Lactones from Persea americana and Persea fulva - in Vitro and in Silico Evaluation of Trypanosoma cruzi Activity. CHEMISTRY & BIODIVERSITY, v. 18, n. 9, . (18/07885-1, 21/02789-7)
GALHARDO, THALITA S.; UENO, ANDERSON K.; COSTA-SILVA, THAIS A.; TEMPONE, ANDRE G.; CARVALHO, WAGNER A.; FISCHMEISTER, CEDRIC; BRUNEAU, CHRISTIAN; MANDELLI, DALMO; LAGO, JOAO HENRIQUE G.. New derivatives from dehydrodieugenol B and its methyl ether displayed high anti-Trypanosoma cruzi activity and cause depolarization of the plasma membrane and collapse the mitochondrial membrane potential. Chemico-Biological Interactions, v. 366, p. 6-pg., . (18/01258-5, 18/10279-6, 21/02789-7, 21/04464-8, 17/17044-1, 16/05006-5, 18/07885-1)
ADRIANA JESUS, JESSICA; LAURENTI, MARCIA DALASTRA; LOPES SILVA, MATHEUS; GHILARDI LAGO, JOAO HENRIQUE; DOMINGUES PASSERO, LUIZ FELIPE. Leishmanicidal Activity and Ultrastructural Changes of Maslinic Acid Isolated from Hyptidendron canum. Evidence-based Complementary and Alternative Medicine, v. 2021, . (16/10324-6, 16/00468-0, 21/02789-7, 18/04080-2)
SOUZA, DALETE CHRISTINE S.; COSTA-SILVA, THAIS A.; MORAIS, THIAGO R.; BRITO, JULIANA R.; FERREIRA, EDGARD A.; ANTAR, GUILHERME M.; SARTORELLI, PATRICIA; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. implified Derivatives of Dibenzylbutyrolactone Lignans from Hydrocotyle bonariensis as Antitrypanosomal Candidate. CHEMISTRY & BIODIVERSITY, v. 18, n. 10, . (19/13906-4, 21/02789-7, 21/04464-8)
SILVA, MATHEUS L.; OLIVEIRA, CYNTIA S.; DOS SANTOS, WAGNER J. O.; OLIVEIRA JUNIOR, VANI X.; ANTAR, GUILHERME M.; LAGO, JOAO H. G.; CERCHIARO, GISELLE. Selective cytotoxicity of ent-kaurene diterpenoids isolated from Baccharis lateralis and Baccharis retusa (Asteraceae). ARCHIV DER PHARMAZIE, v. N/A, p. 7-pg., . (21/02789-7, 20/14175-0)
SILVA, MATHEUS L.; GIMENES, LEILA; ROMOFF, PAULETE; SOARES, MARISI G.; CAMILO, FERNANDA F.; LEVATTI, ERICA VALADARES DE. C.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. ANTI-Trypanosoma cruzi PHENYLPROPANOIDS ISOLATED FROM Baccharis ligustrina C. DC. (ASTERACEAE). Química Nova, v. N/A, p. 4-pg., . (21/02789-7)
MONTEIRO, JACKSON; PASSERO, LUIZ FELIPE D.; JESUS, JESSICA A.; LAURENTI, MARCIA D.; LAGO, JOAO H. G.; SOARES, MARISI G.; BATISTA, ANDREA N. L.; BATISTA JR, JOAO M.; SARTORELLI, PATRICIA. Absolute Configuration and Antileishmanial Activity of (-)-Cyclocolorenone Isolated from Duguetia lanceolata (Annonaceae). CURRENT TOPICS IN MEDICINAL CHEMISTRY, v. 22, n. 19, p. 8-pg., . (18/24077-6, 21/02789-7, 19/22319-5, 16/24985-4)
BRITO, JULIANA R.; COSTA-SILVA, THAIS A.; LONDERO, VINICIUS S.; BALDIM, JOAO L.; TEMPONE, ANDRE G.; FERREIRA, EDGARD A.; LAGO, JOAO HENRIQUE G.. MOLECULAR DEREPLICATION OF VOLATILE OILS FROM Saururus cernuus L. AND EVALUATION OF ANTI-Trypanosoma cruzi ACTIVITY. Química Nova, v. 45, n. 2, p. 6-pg., . (21/02789-7, 18/10279-6)
DOS SANTOS, AUGUSTO L. L.; AMARAL, MAIARA; HASEGAWA, FLAVIA RIE; LAGO, JOAO HENRIQUE G.; TEMPONE, ANDRE G.; SARTORELLI, PATRICIA. (-)-T-Cadinol, a Sesquiterpene Isolated From Casearia sylvestris (Salicaceae)-Displayed In Vitro Activity and Causes Hyperpolarization of the Membrane Potential of Trypanosoma cruzi (vol 12, 734127, 2021). FRONTIERS IN PHARMACOLOGY, v. 13, p. 1-pg., . (16/24985-4, 18/10279-6, 21/02789-7)
LONDERO, VINICIUS S.; COSTA-SILVA, THAIS A.; ANTAR, GUILHERME M.; BAITELLO, JOAO B.; DE OLIVEIRA, LARISSA V. F.; CAMILO, FERNANDA F.; BATISTA, ANDREA N. L.; BATISTA, JR., JOAO M.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. Antitrypanosomal Lactones from Nectandra barbellata. Journal of Natural Products, v. 84, n. 5, p. 1489-1497, . (14/25222-9, 18/07885-1, 21/02789-7, 18/10279-6, 17/17044-1)
THEVENARD, FERNANDA; BRITO, IVANILDO A.; COSTA-SILVA, THAIS A.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.. Enyne acetogenins from Porcelia macrocarpa displayed anti-Trypanosoma cruzi activity and cause a reduction in the intracellular calcium level. SCIENTIFIC REPORTS, v. 13, n. 1, p. 10-pg., . (21/02789-7, 21/04464-8, 20/01221-4)
TOTINI, CARLOS H.; UMEHARA, ERIC; REIS, ISABELLA M. A.; LAGO, JOAO HENRIQUE G.; BRANCO, ALEXSANDRO. Chemistry and Bioactivity of the Genus Persea - A Review. CHEMISTRY & BIODIVERSITY, v. N/A, p. 18-pg., . (21/02789-7, 18/07885-1)
LEVATTI, ERICA V. DE CASTRO; COSTA-SILVA, THAIS A.; MORAIS, THIAGO R.; FERNANDES, JOAO PAULO S.; LAGO, JOAO HENRIQUE G.; TEMPONE, ANDRE G.. Lethal action of Licarin A derivatives in Leishmania (L.) infantum Imbalance of calcium and bioenergetic metabolism. Biochimie, v. 208, p. 10-pg., . (21/02789-7, 21/04464-8, 17/50333-7)
SILVA, TAIS C.; MENGARDA, ANA C.; LEMES, BRUNA L.; LESCANO, SUSANA A. Z.; SOUZA, DALETE CHRISTINE S.; LAGO, JOAO HENRIQUE G.; DE MORAES, JOSUE. N-(4-Methoxyphenyl)Pentanamide, a Simplified Derivative of Albendazole, Displays Anthelmintic Properties against the Nematode Toxocara canis. MICROBIOLOGY SPECTRUM, v. N/A, p. 7-pg., . (19/25905-2, 20/01441-4, 21/02789-7)
ROSA, MATHEUS ELIAS; ALVES CONSERVA, GEANNE A.; LAGO, JOAO HENRIQUE G.; CASELI, LUCIANO. Monolayer nanoarchitectonics at the air-water interface for molecular understanding of the interaction of isolinderanolide E with cholesterol. Thin Solid Films, v. 754, p. 7-pg., . (19/03239-0, 16/20633-6, 18/22214-6, 21/02789-7, 19/04407-4)
FERREIRA, BRUNO ANTONIO; SOUZA, RAFAEL APARECIDO CARVALHO; DE MOURA, FRANCYELLE BORGES ROSA; ADRIANO, TAIS DA SILVA; FRANCA, EDUARDO DE FARIA; SILVA, TIARA DA COSTA; DE SOUSA, RAQUEL MARIA FERREIRA; ARAUJO, FERNANDA DE ASSIS; LAGO, JOAO HENRIQUE GHILARDI; DE OLIVEIRA, ALBERTO. An In Vivo Assessment of the Effect of Hexane Extract from Endlicheria paniculata Branches and Its Main Compound, Methyldehydrodieugenol B, on Murine Sponge-Induced Inflammation. Molecules, v. 28, n. 13, p. 13-pg., . (21/02789-7)
GALHARDO, THALITA S.; UENO, ANDERSON K.; CARVALHO, WAGNER A.; COSTA-SILVA, THAIS A.; GONCALVES, MARINA M.; ABIUZI, MARIANA B.; TEMPONE, ANDRE G.; LAGO, JOAO HENRIQUE G.; MANDELLI, DALMO; FISCHMEISTER, CEDRIC; et al. Synthesis of New Dehydrodieugenol Derivatives via Olefin Cross Metathesis and In Vitro Evaluation of Their Trypanocidal Activity. CATALYSTS, v. 13, n. 7, p. 13-pg., . (21/12342-0, 21/04464-8, 18/10279-6, 17/50333-7, 21/02789-7, 18/01258-5, 18/07885-1)
BARBOSA, HENRIQUE; THEVENARD, FERNANDA; REIMAO, JULIANA QUERO; TEMPONE, ANDRE GUSTAVO; HONORIO, KATHIA MARIA; LAGO, JOAO HENRIQUE GHILARDI. The Potential of Secondary Metabolites from Plants as Drugs or Leads against Trypanosoma cruzi-An Update from 2012 to 2021. CURRENT TOPICS IN MEDICINAL CHEMISTRY, v. 23, n. 3, p. 55-pg., . (21/02789-7)
CABRERA, VITORIA ISABELA MONTANHERO; SIVIDANES, GABRIELLE DO NASCIMENTO; QUINTILIANO, NATALIA FERNANDA; TOYAMA, MARCOS HIKARI; LAGO, JOAO HENRIQUE GHILARDI; DE OLIVEIRA, MARCOS ANTONIO. Exploring functional and structural features of chemically related natural prenylated hydroquinone and benzoic acid from Piper crassinervium (Piperaceae) on bacterial peroxiredoxin inhibition. PLoS One, v. 18, n. 2, p. 21-pg., . (20/02868-1, 13/07937-8, 17/19942-7, 21/02789-7, 17/20291-0)