Abstract
Context: Pimenta dioica (L.) Merr. (Myrtaceae) is used in Costa Rican traditional medicine for women’s health. Our previous work showed that P. dioica extracts were oestrogenic.Objectives: This work identifies phytochemicals from P. dioica that are responsible for the plant’s oestrogen-like activities.Materials and methods: P. dioica leaves were collected in Costa Rica in 2005. Fractions resulting from chromatographic separation of a methanol extract were tested at 50 μg/mL in a competitive oestrogen receptor-binding assay. Active compounds were isolated by HPLC and identified by NMR and MS. Pure compounds were tested at 1 μM in the oestrogen-responsive SEAP reporter gene assay. The effects on cell viability, cytotoxicity and apoptosis were investigated in breast cancer (MCF-7 and SK-BR3) and gastric cancer (AGS and NCI-N87) cell lines using the ApoTox-Glo and Caspase-Glo assays and qPCR.Results: Quercitrin and three new chromones, including a 2-phenoxychromone, 6,8-di-C-methylcapillarisin (1) were isolated and identified. Compound 1 caused a 6.2-fold increase in SEAP expression at 1 μM (p < 0.05). This activity was blocked by the ER antagonist ICI 182,780. Compound 2 caused a 6.0-fold increase in SEAP, inhibited the growth of MCF-7, AGS and NCI-N87 cells (IC50 54.27, 38.13 and 51.22 μg/mL, respectively), and induced apoptosis via caspase 8 and increased the Bax/Bcl-2 mRNA ratio in MCF-7 cells. Compound 3 was anti-oestrogenic in MCF-7 cells.Discussion and conclusions: Compounds from P. dioica have oestrogenic, anti-oestrogenic and cytotoxic effects that may explain the ethnomedical use of this plant.
Highlights
Menopause is defined as the termination of menstruation due to a reduction in the number and function of ovarian follicles, resulting in a decline in estradiol and progesterone production (Gold 2011)
Hormone therapy is the gold standard for the management of menopausal symptoms, Latin American women use more natural therapies to manage their menopausal symptoms, including a wide range of herbal medicines to improve the quality of life in the peri- and postmenopausal periods (Michel et al 2006; Locklear et al 2007, 2017; Doyle et al 2009)
This work was performed as a collaborative project between the University of Illinois at Chicago (UIC) and the University of Costa Rica (UCR) based on a Memorandum of Agreement signed by authorities from UIC and UCR
Summary
Menopause is defined as the termination of menstruation due to a reduction in the number and function of ovarian follicles, resulting in a decline in estradiol and progesterone production (Gold 2011). Hormone therapy is the gold standard for the management of menopausal symptoms, Latin American women use more natural therapies to manage their menopausal symptoms, including a wide range of herbal medicines to improve the quality of life in the peri- and postmenopausal periods (Michel et al 2006; Locklear et al 2007, 2017; Doyle et al 2009). Pimenta dioica is sold in Costa Rica as an herbal therapy for menopausal symptoms and is usually prepared as a decoction, infusion or as a tincture, alone or in combination with other herbs (Doyle et al 2009). Preparations of P. dioica are further used in Costa Rica for the treatment of dysmenorrhea and dyspepsia, and extracts have been shown to have antitumor effects (Zhang and Lockeschwar 2012). Cha et al (2006) showed that extracts of allspice inhibit the growth of Helicobacter pylori, the bacteria responsible for dyspepsia and gastric cancer
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