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Psidium guajava L. (popular name guava) in vitro and in vivo anticancer activity

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Author(s):
Larissa Yokota Rizzo
Total Authors: 1
Document type: Master's Dissertation
Press: Campinas, SP.
Institution: Universidade Estadual de Campinas (UNICAMP). Instituto de Biologia
Defense date:
Examining board members:
João Ernesto de Carvalho; Carmen Silvia Passos Lima; Cristina Pontes Vicente
Advisor: Mary Ann Foglio; João Ernesto de Carvalho
Abstract

Anticancer drug research based on screening of natural sources enabled the discovery of several drugs that are used in cancer treatment. This project aimed to evaluate the in vitro and in vivo anticancer activity of Psidium guajava L. (popular name: guava), elected for its ethnopharmacological use for antiparasitic activity. After harvesting, the vegetal material was extracted in Soxhlet with dicloromethane and then ethanol 95%, leading to the dicloromethane crude extract (DCE) and the ethanolic crude extract (ECE), respectively.The active extract, DCE, was submitted to several biomonitored fractionating processes and an active mixture of meroterpenes identified guajadial, psidial A and its isomers as active principles. All samples (crude extract and enriched fractions) were evaluated in vitro for cytotoxic activity against ten human cancer lines (donated by National Cancer Institute, USA): K562 (leukemia), MCF-7 (breast), NCI/ADR-RES (resistant ovarian cancer), NCI-H460 (lung), UACC62 (melanoma), PC-3 (prostate), HT-29 (colon), OVCAR-03 (ovary), U251 (glioma) and 786-0 (kidney). Meroterpenes enriched fraction was evaluated in vivo in the Solid Ehrlich Tumor, in Balb/C mice, and significantly reduced tumor growth. Besides antitumoral activity, macroscopic analysis of uterus showed increased size and weight in comparison to both negative (vehicle) and positive (doxorubicin) control groups. The molecules of guajadial and psidial A display similar physicochemical properties to estradiol and tamoxifen and in silico molecular docking studies suggest that both molecules bind to the estrogen-binding site of ERs analogously to tamoxifen. The ability to reduce breast cancer tumor growth and stimulate the uterus suggests that guajadial and psidial A may act as phytoestrogens, giving insights for a mechanism of action similar to tamoxifen, acting as SERMs (Selective Estrogen Receptor Modulators), having both agonist and antagonist tissue-specific activities (AU)

FAPESP's process: 09/06573-7 - Anticancer activity in vitro and in vivo of Psidium guajava L. (Myrtaceae)
Grantee:Larissa Yokota Rizzo
Support type: Scholarships in Brazil - Master