Use of chemodiversity of plant species in remaining areas of Atlantic Forest from São Paulo State in the selection of biologically active prototypes

• Grant number: 15/11936-2
• Support Opportunities: Regular Research Grants
• Start date: November 01, 2015
• End date: October 31, 2017
• 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 ; Diogo de Oliveira Silva ; Luiz Felipe Domingues Passero ; Marcelo Afonso Vallim ; Patricia Sartorelli ; Rafael Carlos Guadagnin ; Renata Castiglioni Pascon

Abstract

In this project will be continued aiming the selection of plant species that occur in the remaining areas of the Atlantic Forest of São Paulo State, with the main purpose of conducting pharmacological studies, isolation and structural determination of active compounds, in addition to establishing relations structure/biologic activities obtained with compounds of vegetable matrices. This study began in 2008 with the project entitled " Selection of Potential Molecules in Plant Species of São Paulo Altitude Regions - Chemical Structure, Structure Relations/Biological Activity Associated with Ecophysiological Considerations " - FAPESP 2006/51626-6 (2008 - 2011) followed by the project "Sustainable Use of Biodiversity from Remaining Areas of Atlantic Forest of São Paulo State - Evaluation, Isolation and Molecular Characterization of Bioactive Secondary Metabolites in Plant Species" - FAPESP 2011/51739-0 (2012 - 2014). In this proposal, we intend to continue their studies with bioactive extracts, especially those with antimicrobial (antibacterial and antifungal), antitumor/cytotoxic and antiprotozoal (anti-Leishmania and trypanocidal). To carry out the work, the extracts that show promising will be submitted to molecular identification analysis (HPLC/MS and NMR) being the active metabolites subjected to purification and characterization by chromatographic and spectroscopic/spectrometric techniques. After isolation of the active substances, essentially those which present new or rare structures, they might be subject to SAR tests through different molecular changes aimed determination of pharmacophore groups. In addition, it is intended, in this proposal, conduct specific tests to action mode setting of substances with proven antiprotozoal and/or cytotoxic/antitumor activities. Additionally, in the final stage of the project, the compounds that present high potential and reduced toxicity in vitro will be subjected to evaluation studies of activity in vivo (preclinical studies). Thus, this project aims to add new compounds and/or extracts with pharmacological activity to the restricted herbal therapeutic arsenal by providing tools for sustainable development of endangered areas. (AU)

Scientific publications

(22)

(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)

GRECCO, SIMONE S.; COSTA-SILVA, THAIS A.; JERZ, GEROLD; DE SOUSA, FERNANDA S.; LONDERO, VINICIUS S.; GALUPPO, MARIANA K.; LIMA, MARTA L.; NEVES, BRUNO J.; ANDRADE, CAROLINA H.; TEMPONE, ANDRE G.; et al. Neolignans from leaves of Nectandra leucantha (Lauraceae) display in vitro antitrypanosomal activity via plasma membrane and mitochondrial damages. Chemico-Biological Interactions, v. 277, p. 55-61, NOV 1 2017. (15/50075-2, 15/11936-2, 13/50228-8)

DE SOUSA, CAROLINA BRUNO; GANGADHAR, KATKAM N.; MORAIS, THIAGO R.; CONSERVA, GEANNE A. A.; VIZETTO-DUARTE, CATARINA; PEREIRA, HUGO; LAURENTI, MARCIA D.; CAMPINO, LENEA; LEVY, DEBORA; UEMI, MIRIAM; et al. Antileishmanial activity of meroditerpenoids from the macroalgae Cystoseira baccata. Experimental Parasitology, v. 174, p. 1-9, MAR 2017. (13/16297-2, 15/11936-2)

PONCI, VITOR; FIGUEIREDO, CARLOS R.; MASSAOKA, MARIANA H.; DE FARIAS, CAMYLA F.; MATSUO, ALISSON L.; SARTORELLI, PATRICIA; LAGO, JOAO HENRIQUE G.. Neolignans from Nectandra megapotamica (Lauraceae) Display in vitro Cytotoxic Activity and Induce Apoptosis in Leukemia Cells. Molecules, v. 20, n. 7, p. 12757-12768, JUL 2015. (15/11936-2)

VARELA, MARINA T.; DIAS, ROBERTO Z.; MARTINS, LIGIA F.; FERREIRA, DAIANE D.; TEMPONE, ANDRE G.; UENO, ANDERSON K.; LAGO, JOAO HENRIQUE G.; FERNANDES, JOAO PAULO S.. Gibbilimbol analogues as antiparasitic agents-Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum. Bioorganic & Medicinal Chemistry Letters, v. 26, n. 4, p. 1180-1183, FEB 15 2016. (13/20479-9, 12/18756-1, 15/11936-2, 14/16564-3)

MORAIS, THIAGO R.; COUTINHO, ANA PAULA R.; CAMILO, FERNANDA F.; MARTINS, TEREZA S.; SARTORELLI, PATRICIA; MASSAOKA, MARIANA H.; FIGUEIREDO, CARLOS R.; LAGO, JOAO HENRIQUE G.. Application of an Ionic Liquid in the Microwave Assisted Extraction of Cytotoxic Metabolites from Fruits of Schinus terebinthifolius Raddi (Anacardiaceae). Journal of the Brazilian Chemical Society, v. 28, n. 3, SI, p. 492-497, MAR 2017. (15/11936-2)

GAMES, ELLEN; GUERREIRO, MARINA; SANTANA, FERNANDA R.; PINHEIRO, NATHALIA M.; DE OLIVEIRA, EMERSON A.; LOPES, FERNANDA D. T. Q. S.; OLIVO, CLARICE R.; TIBERIO, IOLANDA F. L. C.; MARTINS, MILTON A.; LAGO, JOAO HENRIQUE G.; et al. Structurally Related Monoterpenes p-Cymene, Carvacrol and Thymol Isolated from Essential Oil from Leaves of Lippia sidoides Cham. (Verbenaceae) Protect Mice against Elastase-Induced Emphysema. Molecules, v. 21, n. 10, OCT 2016. (15/11936-2, 14/25689-4, 11/51739-0, 13/02881-4)

DE SOUSA, FERNANDA S.; NUNES, EMILENE A.; GOMES, KAIO S.; CERCHIARO, GISELLE; LAGO, JOAO HENRIQUE G.. Genotoxic and cytotoxic effects of neolignans isolated from Nectandra leucantha (Lauraceae). TOXICOLOGY IN VITRO, v. 55, p. 116-123, MAR 2019. (15/11936-2, 14/24475-0, 15/04143-6, 18/07885-1)

MACIEL, DAYANY DA SILVA A.; FREITAS, VIVIANE P.; ALVES CONSERVA, GEANNE A.; ALEXANDRE, TATIANA R.; PURISCO, SONIA U.; TEMPONE, ANDRE G.; MELHEM, MARCIA SOUZA C.; KATO, MASSUO J.; GUIMARAES, ELSIE F.; LAGO, JOAO HENRIQUE G.. Bioactivity-guided isolation of laevicarpin, an antitrypanosomal and anticryptococcal lactam from Piper laevicarpu (Piperaceae). Fitoterapia, v. 111, p. 24-28, JUN 2016. (15/11936-2)

VARELA, MARINA T.; LIMA, MARTA L.; GALUPPO, MARIANA K.; TEMPONE, ANDRE G.; DE OLIVEIRA, ALBERTO; LAGO, JOAO HENRIQUE G.; FERNANDES, JOAO PAULO S.. New alkenyl derivative from Piper malacophyllum and analogues: Antiparasitic activity against Trypanosoma cruzi and Leishmania infantum. CHEMICAL BIOLOGY & DRUG DESIGN, v. 90, n. 5, p. 1007-1011, NOV 2017. (12/18756-1, 13/50228-8, 15/11936-2, 16/00195-4)

BUANA C. DE ALMEIDA; BRUNO Q. ARAÚJO; ELCIO D. S. BARROS; SÂMYA D. L. FREITAS; DAYANY S. A. MACIEL; ARI J. S. FERREIRA; RAFAEL C. GUADAGNIN; GERARDO M. VIEIRA JÚNIOR; JOÃO H. G. LAGO; MARIANA H. CHAVES. Dammarane Triterpenoids from Carnauba, Copernicia prunifera (Miller) H. E. Moore (Arecaceae), Wax. Journal of the Brazilian Chemical Society, v. 28, n. 8, p. 1371-1376, 2017-08-00. (15/11936-2)

BRITO, JULIANA R.; CAMILO, FERNANDA F.; FIGUEIREDO, CARLOS R.; AZEVEDO, RICARDO A.; ROMOFF, PAULETE; BUTURI, FATIMA O. S.; FAVERO, ORIANA A.; LAGO, JOAO HENRIQUE G.; FERREIRA, EDGARD A.. ISOLATION OF CYTOTOXIC NEOLIGNANS FROM Saururus cernuus L. (SAURURACEAE) USING IONIC LIQUID IN THE MICROWAVE ASSISTED EXTRACTION (MAE). Química Nova, v. 41, n. 7, p. 4-pg., 2018-07-01. (15/11936-2)

DE ALMEIDA, BUANA C.; ARAUJO, BRUNO Q.; CARVALHO, ADONIAS A.; FREITAS, SAMYA DANIELLE L.; ALVES MACIEL, DAYANY DA S.; FERREIRA, ARI JOSE S.; TEMPONE, ANDRE G.; MARTINS, LIGIA F.; ALEXANDRE, TATIANA R.; CHAVES, MARIANA H.; et al. Antiprotozoal activity of extracts and isolated triterpenoids of 'carnauba' (Copernicia prunifera) wax from Brazil. Pharmaceutical Biology, v. 54, n. 12, p. 5-pg., 2016-12-01. (15/11936-2)

BRITO, JULIANA R.; CAMILO, FERNANDA F.; FIGUEIREDO, CARLOS R.; AZEVEDO, RICARDO A.; ROMOFF, PAULETE; BUTURI, FATIMA O. S.; FAVERO, ORIANA A.; LAGO, JOAO HENRIQUE G.; FERREIRA, EDGARD A.. ISOLATION OF CYTOTOXIC NEOLIGNANS FROM Saururus cernuus L. (SAURURACEAE) USING IONIC LIQUID IN THE MICROWAVE ASSISTED EXTRACTION (MAE). Química Nova, v. 41, n. 7, p. 778-781, JUL 2018. (15/11936-2)

DE ALMEIDA, BUANA C.; ARAUJO, BRUNO Q.; CARVALHO, ADONIAS A.; FREITAS, SAMYA DANIELLE L.; ALVES MACIEL, DAYANY DA S.; FERREIRA, ARI JOSE S.; TEMPONE, ANDRE G.; MARTINS, LIGIA F.; ALEXANDRE, TATIANA R.; CHAVES, MARIANA H.; et al. Antiprotozoal activity of extracts and isolated triterpenoids of `carnauba' (Copernicia prunifera) wax from Brazil. Pharmaceutical Biology, v. 54, n. 12, p. 3280-3284, DEC 2016. (15/11936-2)

GRECCO, SIMONE S.; COSTA-SILVA, THAIS A.; JERZ, GEROLD; DE SOUSA, FERNANDA S.; ALVES CONSERVA, GEANNE A.; MESQUITA, JULIANA T.; GALUPPO, MARIANA K.; TEMPONE, ANDRE G.; NEVES, BRUNO J.; ANDRADE, CAROLINA H.; et al. Antitrypanosomal activity and evaluation of the mechanism of action of dehydrodieugenol isolated from Nectandra leucantha (Lauraceae) and its methylated derivative against Trypanosoma cruzi. Phytomedicine, v. 24, p. 62-67, JAN 15 2017. (15/11936-2, 13/07275-5)

JESUS, JESSICA A.; FRAGOSO, THAIS N.; YAMAMOTO, EDUARDO S.; LAURENTI, MARCIA D.; SILVA, MARCELO S.; FERREIRA, AUREA F.; LAGO, JOAO HENRIQUE G.; GOMES, GABRIELA S.; PASSERO, LUIZ FELIPE D.. Therapeutic effect of ursolic acid in experimental visceral leishmaniasis. INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE, v. 7, n. 1, p. 1-11, APR 2017. (13/10133-8, 16/00468-0, 13/16297-2, 15/11936-2)

UENO, ANDERSON K.; BARCELLOS, ALINE F.; COSTA-SILVA, THAIS A.; MESQUITA, JULIANA T.; FERREIRA, DAIANE D.; TEMPONE, ANDRE G.; ROMOFF, PAULETE; ANTAR, GUILHERME M.; LAGO, JOAO HENRIQUE G.. Antitrypanosomal activity and evaluation of the mechanism of action of diterpenes from aerial parts of Baccharis retusa (Asteraceae). Fitoterapia, v. 125, p. 55-58, MAR 2018. (15/23403-9, 15/11936-2, 14/08961-2)

DE SOUSA, FERNANDA S.; BALDIM, JOAO L.; AZEVEDO, RICARDO A.; FIGUEIREDO, CARLOS R.; PIEPER, PAULINE; SEAR, CLAIRE E.; ANDERSON, EDWARD A.; LAGO, JOAO HENRIQUE G.. Structure-activity relationship study of cytotoxic neolignan derivatives using multivariate analysis and computation-aided drug design. Bioorganic & Medicinal Chemistry Letters, v. 30, n. 16, AUG 15 2020. (15/11936-2, 15/04143-6, 16/19269-8, 18/07885-1)

BARROSA, KAIDU H.; MECCHI, MURILO C.; RANDO, DANIELA G.; FERREIRA, ARI JOSE S.; SARTORELLI, PATRICIA; VALLE, MAIRA M. R.; BORDIN, SILVANA; CAPERUTO, LUCIANA C.; LAGO, JOAO HENRIQUE G.; LELLIS-SANTOS, CAMILO. Polygodial, a sesquiterpene isolated from Drimys brasiliensis (Winteraceae), triggers glucocorticoid-like effects on pancreatic beta-cells. Chemico-Biological Interactions, v. 258, p. 245-256, OCT 25 2016. (10/10778-0, 15/11936-2)

UENO, ANDERSON K.; BARCELLOS, ALINE F.; GRECCO, SIMONE DOS S.; SARTORELLI, PATRICIA; GUADAGNIN, RAFAEL C.; ROMOFF, PAULETE; FERREIRA, MARCELO JOSE P.; TCACENCO, CELIZE M.; LAGO, JOAO HENRIQUE G.. Sesquiterpenes, diterpenes, alkenyl p-coumarates, and flavonoid from the aerial parts of Baccharis retusa (Asteraceae). Biochemical Systematics and Ecology, v. 78, p. 39-42, JUN 2018. (15/11936-2, 14/21593-2)

GIROLA, NATALIA; FIGUEIREDO, CARLOS R.; FARIAS, CAMYLA F.; AZEVEDO, RICARDO A.; FERREIRA, ADILSON K.; TEIXEIRA, SARAH F.; CAPELLO, TABATA M.; MARTINS, EUDER G. A.; MATSUO, ALISSON L.; TRAVASSOS, LUIZ R.; et al. Camphene isolated from essential oil of Piper cernuum (Piperaceae) induces intrinsic apoptosis in melanoma cells and displays antitumor activity in vivo. Biochemical and Biophysical Research Communications, v. 467, n. 4, p. 928-934, NOV 27 2015. (11/51739-0, 15/11936-2)

DE SOUSA, FERNANDA S.; GRECCO, SIMONE S.; GIROLA, NATALIA; AZEVEDO, RICARDO A.; FIGUEIREDO, CARLOS R.; LAGO, JOAO HENRIQUE G.. Neolignans isolated from Nectandra leucantha induce apoptosis in melanoma cells by disturbance in mitochondrial integrity and redox homeostasis. Phytochemistry, v. 140, p. 108-117, AUG 2017. (15/04143-6, 15/11936-2)