Biomolecules from Nectandra barbellata Coe-Teixeira (Lauraceae): use of a sustainable alternative method for extraction, molecular characterization and evaluation of antiparasitic potential

• Grant number: 17/17044-1
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: February 01, 2018
• End date: January 31, 2022
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: João Henrique Ghilardi Lago
• Grantee: Vinicius Silva Londero
• Host Institution: Instituto de Ciências Ambientais, Químicas e Farmacêuticas (ICAQF). Universidade Federal de São Paulo (UNIFESP). Campus Diadema. Diadema , SP, Brazil

Abstract

Brazil has great biological diversity and can enjoy many species with unknown pharmacological properties. Phytochemical studies with different species of the genus Nectandra have shown great structural diversity of bioactive metabolites, however, there is no information in the literature related to the chemical composition and/or biological potential of the species Nectandra barbellata. Because it is a restricted species, it is necessary the chemical and biological study of N. barbellata in order to support research on the conservation and sustainable use of this species. Thus, this project has a dual purpose - to describe the chemical composition of extracts, obtained from alternative methods using ionic liquid assisted by microwave, through techniques of de-duplication (HPLC, HPLC and EMR) and to evaluate the antiparasitic potential Anti-Leishmania and anti-T. cruzi) of the extracts obtained. After these steps, the active extracts will be fractionated and the bioactive compounds isolated through biomonitoring will be characterized by spectroscopic/spectrometric techniques (NMR, ms, IR, UV, etc). In the sequence, the activity of the active metabolites will be evaluated against intracellular forms of the parasites L. infantum and T. cruzi and aspects related to the mechanisms of action of these substances will be determined. Finally, pharmacokinetic properties, especially Absorption (A), Distribution (D), Metabolism (M), Excretion (E) and Toxicity (T) - ADMET will be evaluated in silico in order to rationalize possible structural changes in active substances in order to improve the observed potential for the naturally occurring substance. Therefore, the results obtained will contribute to the number of molecular prototypes for the development of new drugs, mainly in the scope of antiparasitic activity, which can be obtained through an alternative and sustainable procedure of endemic species of the Atlantic Forest region in the State from São Paulo. (AU)

Scientific publications

(4)

(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)

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., 2023-10-01. (22/03736-7, 18/22214-6, 14/50869-6, 21/02789-7, 21/15084-1, 17/17044-1)

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., 2022-09-07. (18/01258-5, 18/10279-6, 21/02789-7, 21/04464-8, 17/17044-1, 16/05006-5, 18/07885-1)

LONDERO, VINICIUS S.; COSTA-SILVA, THAIS A.; TEMPONE, ANDRE G.; NAMIYAMA, GISLENE M.; THEVENARD, FERNANDA; ANTAR, GUILHERME M.; BAITELLO, JOAO B.; LAGO, JOAO HENRIQUE G.. Anti-Trypanosoma cruzi activity of costic acid isolated from Nectandra barbellata (Lauraceae) is associated with alterations in plasma membrane electric and mitochondrial membrane potentials. BIOORGANIC CHEMISTRY, v. 95, JAN 2020. (18/10279-6, 17/17044-1, 18/07885-1)

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, MAY 28 2021. (14/25222-9, 18/07885-1, 21/02789-7, 18/10279-6, 17/17044-1)