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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.)

Cytotoxicity of Structurally Diverse Anthranoids and Correlation with Mechanism of Action and Side Effects

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Author(s):
Demarque, Daniel P. [1] ; da Silva, Rui M. P. [2] ; Santos, Leandro F. [1] ; Leopoldino, Andreia M. [1] ; Espreafico, Enilza M. [2] ; Lopes, Norberto P. [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, Dept Phys & Chem, Ribeirao Preto, SP - Brazil
[2] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Cell & Mol Biol & Pathogen Bioagents, Ribeirao Preto, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES; v. 21, p. 347-353, 2018.
Web of Science Citations: 0
Abstract

The purpose of this contribution is to evaluate the cytotoxicity and apoptosis inducing ability of structurally diverse anthraquinones to establish a relationship between structure and toxicity. Besides the wide spread use of anthraquinones in pharmacological drugs for constipation and non-prescription dietary supplements for weight loss, extracts are still commercialized as crude extracts and long-term side effects are still relevant. In this work we developed a method to quantify the cascarosides isolated from Rhamnus purshiana (Cascara Sagrada) using LC-MS/MS and evaluated the effects of this extract and isolated compounds on cellular viability using NOK-SI, HeLa, and T98G cell lineages. Apoptosis inducing ability was also analyzed via evaluating key-proteins involved in apoptosis pathways. Using cascarosides isolated from bark extracts, we found that the presence of glucose moieties in the chemical structure reduced the toxicity. This communication reviewed the mechanisms of action, toxicity of anthraquinones and correlated the toxicity with chemical structures of cascarosides. Results indicate that cascarosides-enriched cascara extract, as well as glycosylated anthraquinones, may have some beneficial effects for laxative action of herbal medicines. Considering our results, a cascarosides-enrichment in cascara extract is recommended. (AU)

FAPESP's process: 14/50265-3 - Distribution and metabolism of natural and synthetic xenobiotics: from the comprehension of reactional process to tissue imaging generation
Grantee:Norberto Peporine Lopes
Support Opportunities: BIOTA-FAPESP Program - Thematic Grants
FAPESP's process: 14/18052-0 - Tissue localization of tannins and Anthraquinones acting on gastrointestinal system
Grantee:Daniel Pecoraro Demarque
Support Opportunities: Scholarships in Brazil - Doctorate