Abstract
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 µg·mL−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.
Highlights
Cancer is one of the leading causes of death worldwide [1], with an estimation of 27 million new individual diagnoses by 2050 [2]
Ehrlich’s solid tumoranti-estrogenic model besidesactivity anti-estrogenic activity by inhibition in Ehrlich’s solid model besides evidenced by theevidenced uterotrophic the uterotrophic modelwere where animals were treated through the intraperitoneal route. These results model where animals treated through the intraperitoneal route. These results suggested a suggestedtamoxifen-like a possible tamoxifen-like of action for the meroterpens identified in P. guajava possible mechanismmechanism of action for the meroterpens identified in P. guajava leaves leaves extract
Chromatographic analysis of FFINAL showed the presence of three major compounds (retention time (RT): 28, 45 and 46 min) (Figure S4A)
Summary
Cancer is one of the leading causes of death worldwide [1], with an estimation of 27 million new individual diagnoses by 2050 [2]. There is a constant demand for new approaches for cancer therapy to be used instead of the conventional treatments that can cause side effects [1,2]. Natural products have demonstrated a powerful alternative in cancer chemotherapy, providing many structures or inspiring the construction of novel anticancer molecules. Many compounds from plants or microorganisms are reported as anti-cancer agents [3,4]. One of the most known examples are vinblastine and vincristine; compounds obtained from Catharanthus roseus (Vinca rosea) demonstrating to have potent cytotoxic effects [3]. Psidium guajava L. (Myrtaceae), a native species from tropical areas, has been reported as a good source of secondary metabolites with pharmacological activity, such as flavonoids, terpenoids, Molecules 2020, 25, 1525; doi:10.3390/molecules25071525 www.mdpi.com/journal/molecules
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