Anti-Estrogenic Activity of Guajadial Fraction, from Guava Leaves (Psidium guajava L.)

Autor(es)

Bazioli, Jaqueline Moraes ^{[1, 2]} ; Costa, Jonas Henrique ^[2] ; Shiozawa, Larissa ^{[1, 3]} ; Gois Ruiz, Ana Lucia Tasca ^[1] ; Foglio, Mary Ann ^[1] ; de Carvalho, Joao Ernesto ^[1]

Afiliação do(s) autor(es)

^[1] Univ Estadual Campinas, Fac Pharmaceut Sci, Campinas 13083859, SP - Brazil

^[2] Univ Estadual Campinas, Inst Chem, POB 6154, Campinas 13083970, SP - Brazil

^[3] Univ Estadual Campinas, Piracicaba Dent Sch, Postgrad Program Dent, Piracicaba 13414903, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Molecules; v. 25, n. 7 APR 2020.
• Citações Web of Science: 0

Resumo

The research of natural products has allowed for the discovery of biologically relevant compounds inspired by plant secondary metabolites, which contributes to the development of many chemotherapeutic drugs used in cancer treatment. Psidium guajava leaves present a diverse phytochemical composition including flavonoids, phenolics, meroterpenoids, and triterpenes as the major bioactive constituents. Guajadial, a caryophyllene-based meroterpenoid, has been studied for potential anticancer effects tested in tumor cells and animal experimental models. Moreover, guajadial has been reported to have a mechanism of action similar to tamoxifen, suggesting this compound as a promisor phytoestrogen-based therapeutic agent. Herein, the anti-estrogenic action and anti-proliferative activity of guajadial is reported. The enriched guajadial fraction was obtained by sequential chromatographic techniques from the crude P. guajava dichloromethane extract showing promising anti-proliferative activity in vitro with selectivity for human breast cancer cell lines MCF-7 and MCF-7 BUS (Total Growth Inhibition = 5.59 and 2.27 mu gmL(-1), respectively). Furthermore, evaluation of anti-estrogenic activity in vivo was performed demonstrating that guajadial enriched fraction inhibited the proliferative effect of estradiol on the uterus of pre-pubescent rats. These results suggest a relationship between anti-proliferative and anti-estrogenic activity of guajadial, which possibly acts in tumor inhibition through estrogen receptors due to the compounds structural similarity to tamoxifen. (AU)

• Processo FAPESP: 19/11563-2 - Prospecção de metabólitos secundários com atividade anticâncer produzidos por fungos fitopatogênicos
• Beneficiário: Jaqueline Moraes Bazioli
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto
• Processo FAPESP: 14/01283-9 - Mecanismo de ação anticâncer e sua relação com a atividade hormonal de extratos e frações obtidos das folhas da Psidium guajava L.
• Beneficiário: Larissa Shiozawa
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto