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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Antimalarial activity of piperidine alkaloids from Senna spectabilis and semisynthetic derivatives

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Author(s):
Pivatto, Marcos [1] ; Baccini, Luciene R. [2] ; Sharma, Abhinay [3] ; Nakabashi, Myna [3] ; Danuello, Amanda [4] ; Viegas Junior, Claudio [2] ; Garcia, Celia R. S. [3] ; Bolzani, Vanderlan S. [2]
Total Authors: 8
Affiliation:
[1] Univ Fed Uberlandia, Inst Quim, BR-38400902 Uberlandia, MG - Brazil
[2] Univ Estadual Paulista, Inst Quim, Dept Quim Organ, Nucl Bioensaios Biossintese & Ecofisiol Prod Nat, BR-14801970 Araraquara, SP - Brazil
[3] Univ Sao Paulo, Inst Biociencias, Dept Fisiol, BR-05508900 Sao Paulo - Brazil
[4] Univ Fed Triangulo Mineiro, Inst Ciencias Exatas Nat & Educ, Dept Quim, BR-38064200 Uberlandia, MG - Brazil
Total Affiliations: 4
Document type: Journal article
Source: Journal of the Brazilian Chemical Society; v. 25, n. 10, p. 1900+, OCT 2014.
Web of Science Citations: 7
Abstract

In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids ( - )-cassine and ( - )-spectaline were isolated from the flowers of Senna spectabilis (syn. Cassia spectabilis). Their structures were elucidated using a combination of spectroscopic and spectrometric data analysis. Further, these compounds were acetylated yielding the derivatives ( - )-3-O-acetylcassine and ( - )-3-O-acetylspectaline. All compounds were screened against P. falciparum-infected red blood cells (RBC) in culture, aiming to identify antimalarial prototypes. Among all compounds screened, the first two alkaloids (IC50 1.82 µM and IC50 2.76 µM) were more effective than the derivatives (IC50 24.47 µM and IC50 25.14 µM) in comparison to the standard compound chloroquine (IC50 0.30 µM). These data show that piperidine alkaloids constitute a class of natural products that feature a broad spectrum of biological activities, and are, therefore, important templates for drug design, including antimalarial. (AU)

FAPESP's process: 03/02176-7 - Conservation and sustainable use of the diversity from Cerrado and Atlantic Forest: chemical diversity and prospecting for potential drugs - phase II
Grantee:Vanderlan da Silva Bolzani
Support Opportunities: BIOTA-FAPESP Program - Thematic Grants
FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC