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Type: Artigo de periódico
Title: In Vitro, In Vivo and In Silico Analysis of the Anticancer and Estrogen-like Activity of Guava Leaf Extracts
Author: Rizzo, LY
Longato, GB
Ruiz, ALG
Tinti, SV
Possenti, A
Vendramini-Costa, DB
Sartoratto, A
Figueira, GM
Silva, FLN
Eberlin, MN
Souza, TACB
Murakami, MT
Rizzo, E
Foglio, MA
Kiessling, F
Lammers, T
Carvalho, JE
Abstract: Anticancer drug research based on natural compounds enabled the discovery of many drugs currently used in cancer therapy. Here, we report the in vitro, in vivo and in silico anticancer and estrogen-like activity of Psidium guajava L. (guava) extracts and enriched mixture containing the meroterpenes guajadial, psidial A and psiguadial A and B. All samples were evaluated in vitro for anticancer activity against nine human cancer lines: K562 (leukemia), MCF7 (breast), NCI/ADR-RES (resistant ovarian cancer), NCI-H460 (lung), UACC-62 (melanoma), PC-3 (prostate), HT-29 (colon), OVCAR-3 (ovarian) and 786-0 (kidney). Psidium guajava's active compounds displayed similar physicochemical properties to estradiol and tamoxifen, as in silico molecular docking studies demonstrated that they fit into the estrogen receptors (ERs). The meroterpene-enriched fraction was also evaluated in vivo in a Solid Ehrlich murine breast adenocarcinoma model, and showed to be highly effective in inhibiting tumor growth, also demonstrating uterus increase in comparison to negative controls. The ability of guajadial, psidial A and psiguadials A and B to reduce tumor growth and stimulate uterus proliferation, as well as their in silico docking similarity to tamoxifen, suggest that these compounds may act as Selective Estrogen Receptors Modulators (SERMs), therefore holding significant potential for anticancer therapy.
Subject: Active principles
P. guajava L. (guava)
Country: Emirados Árabes Unidos
Editor: Bentham Science Publ Ltd
Citation: Current Medicinal Chemistry. Bentham Science Publ Ltd, v. 21, n. 20, n. 2322, n. 2330, 2014.
Rights: fechado
Identifier DOI: 10.2174/0929867321666140120120031
Date Issue: 2014
Appears in Collections:Unicamp - Artigos e Outros Documentos

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