Title:In Vitro, In Vivo and In Silico Analysis of the Anticancer and Estrogen-like Activity of Guava Leaf Extracts
VOLUME: 21 ISSUE: 20
Author(s):L.Y. Rizzo, G.B. Longato, A.LT.G. Ruiz, S.V. Tinti, A. Possenti, D.B. Vendramini-Costa, A. Sartoratto, G.M. Figueira, F.L.N. Silva, M.N. Eberlin, T.A.C.B. Souza, M.T. Murakami, E. Rizzo, M.A. Foglio, F. Kiessling, T. Lammers and J.E. Carvalho
Affiliation:Department of Experimental Molecular Imaging (ExMI), RWTH Aachen University, Pauwelsstrasse 20, 52074, Aachen, Germany.
Keywords:Active principles, cancer, P. guajava L. (guava), phytoestrogens, SERM, tamoxifen.
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.
