In vitro anti-Trypanosoma cruzi evaluation of sesquiterpenes from the branches of Oxandra sessiliflora

Author(s)

Silva, Armenio A. de Carvalho A. da ^{[1, 2]} ; Sousa, Elcilene A. de ^[1] ; Veras, Marcia D. Alves ^[1] ; Araujo, Bruno Q. ^[1] ; Thevenard, Fernanda ^[3] ; Lago, Joao Henrique G. ^[3] ; Costa-Silva, Thais A. ^[3] ; Tempone, Andre G. ^[4] ; Chaves, Mariana H. ^[1]

Affiliation

^[1] Univ Fed Piaui, Dept Quim, BR-64049550 Teresina, PI - Brazil

^[2] Inst Fed Educ Ciencia & Tecnol Piaui, BR-64770000 Seo Raimundo Nonato, PI - Brazil

^[3] Univ Fed ABC, Ctr Ciencias Nat & Humanas, BR-09210580 Santo Andre, SP - Brazil

^[4] Adolfo Lutz Inst, Ctr Parasitol & Micol, BR-01246902 Sao Paulo, SP - Brazil

• Document type: Journal article
• Source: PHYTOCHEMISTRY LETTERS; v. 37, p. 59-62, JUN 2020.
• Web of Science Citations: 1

Abstract

In this work, the CH2Cl2 phase from the EtOH extract of Oxandra sessiliflora (Annonaceae) branches was subjected to chromatographic fractionation to afford six sesquiterpenoids: 4 alpha,10 beta-aromadendranediol (1), 4 beta,10 alpha-aromadendranediol (2), 4 alpha,10 alpha-aromadendranediol (3), 1 beta,6 alpha-dihydroxy-4(15)-eudesmene (4), 4 beta,10 alpha-dihydroxy-guai-6-ene (5), and 4 beta,6 beta,7 beta,10 alpha-tetrahydroxy-guaiane (6), the last one identified as a new natural product. The structures of isolated compounds were identified by analysis of NMR and HRESIMS spectral data. Compounds 1-6 exhibited activity against T. cruzi with EC50 values ranging from 16.3-47.5 mu M. Additionally, no cytotoxicity to mammalian cells (NCTC- L929 clone) was observed for tested compounds at the highest concentration (200 mu M). Sesquiterpenes 5 and 6 exhibited higher selectivity index (SI) with values higher than 12.3 and 11.4, respectively. This data suggests that guaiane sesquiterpenes 5 and 6, isolated from O. sessiliflora, may contribute as scaffolds for the design of novel and selective drug candidates for treatment of neglected diseases, mainly for Chagas disease. (AU)

• FAPESP's process: 18/10279-6 - Selection and Optimization of New Drug Candidates for Leishmaniasis and Chagas Disease
• Grantee: André Gustavo Tempone Cardoso
• Support Opportunities: Regular Research Grants
• FAPESP's process: 18/07885-1 - Biomolecules from plant species of remnant areas of the Atlantic Forest and Cerrado to treat neglected tropical diseases - chemical and pharmacological aspects
• Grantee: João Henrique Ghilardi Lago
• Support Opportunities: BIOTA-FAPESP Program - Regular Research Grants