Objective-Outcomes from the Women's Health Initiative have demonstrated adverse effects associated with hormone therapy (HT), and have prioritized the need to develop new alternative treatments for the management of menopause and osteoporosis. To this end, we have been investigating natural herbal medicines used by Costa Rican women to manage menopausal symptoms.Design-Seventeen plant species were collected and extracted in Costa Rica. To establish possible mechanisms of action, and determine their potential future use for menopause or osteoporosis, the estrogenic activities of the herbal extracts were investigated in an estrogen reporter gene ERβ-CALUX® assay in U2-OS cells, and in reporter and endogenous gene assays in MCF-7 cells.Results-Six of the plant extracts bound to the estrogen receptors. Four of the six extracts stimulated reporter gene expression in the ERβ-CALUX® assay. All six extracts modulated expression of endogenous genes in MCF-7 cells, with four extracts acting as estrogen agonists and two extracts, Pimenta dioica and Smilax domingensis, acting as partial agonist/antagonists by enhancing E2-stimulated pS2 mRNA expression, but reducing E2-stimulated PR and PTGES mRNA expression. Both P. dioica and S. domingensis induced a 2ERE-luciferase reporter gene in transient transfected MCF-7 cells, which was inhibited by the ER antagonist ICI 182780.Conclusions-This work presents a plausible mechanism of action for many of the herbal medicines used by Costa Rican women to treat menopausal symptoms. However, it further suggests that studies of safety and efficacy are needed before these herbs should be used as alternative therapies to HT.
Objectives-To investigate the biological activities of Justicia pectoralis Jacq. (Acanthaceae), an herbal medicine used in Costa Rica (CR) for the management of menopausal symptoms and dysmenorrhea.Study design-The aerial parts of Justicia pectoralis were collected, dried and extracted in methanol. To establish possible mechanisms of action of JP for the treatment of menopausal symptoms, the estrogenic and progesterone agonist, and antiinflammatory activities were investigated.Main outcome measures-The methanol extract (JP-M) was tested in ER and PR binding assays, a COX-2 enzyme inhibition assay, the ERβ-CALUX assay in U2-OS cells, as well as reporter and endogenous gene assays in MCF-7 K1 cells.Results-The JP-M extract inhibited COX-2 catalytic activity (IC 50 4.8µg/ml); bound to both ERα and ERβ (IC 50 50 µg/ml and 23.1µg/ml, respectively); induced estrogen-dependent transcription in the ERβ-CALUX; and bound to the progesterone receptor (IC 50 22.8 µg/ml). The extract also modulated the expression of endogenous estrogen responsive genes pS2, PR, and PTGES in MCF-7 cells at a concentration of 20 µg/ml. Activation of a 2 ERE-construct in transiently transfected MCF-7 cells by the extract was inhibited by the estrogen receptor antagonist ICI 182,780, indicating that the effects were mediated through the estrogen receptor. Finally, the extract weakly enhanced the proliferation of MCF-7 cells, however this was not statistically significant as compared with DMSO controls.
MeOH (4:1) (BST inactive) and EtOAc (BST l3Opg/ml). Column chromatography of the EtOAc fraction over silica gel, and elution with CHC13, followed by CHC13-MeOH
A novel chromone, granulosin (1), has been isolated from the bark of Galipea granulosa. The extract of the bark, as well as granulosin (1), exhibited lethality in the brine shrimp test. The structure of granulosin (1) as 2-propyl-7,8-(methylenedioxy)chromone was established via spectroscopic analysis.
Arbutoid mycorrhizal plants are commonly found as understory vegetation in forests worldwide where ectomycorrhiza-forming trees occur. Comarostaphylis arbutoides (Ericaceae) is a tropical woody plant and common in tropical Central America. This plant forms arbutoid mycorrhiza, whereas only associations with Leccinum monticola as well as Sebacina sp. are described so far. We collected arbutoid mycorrhizas of C. arbutoides from the Cerro de la Muerte (Cordillera de Talamanca), Costa Rica, where this plant species grows together with Quercus costaricensis. We provide here the first evidence of mycorrhizal status for the Ascomycete Leotia cf. lubrica (Helotiales) that was so far under discussion as saprophyte or mycorrhizal. This fungus formed arbutoid mycorrhiza with C. arbutoides. The morphotype was described morphologically and anatomically. Leotia cf. lubrica was identified using molecular methods, such as sequencing the internal-transcribed spacer (ITS) and the large subunit (LSU) ribosomal DNA regions, as well as phylogenetic analyses. Specific plant primers were used to confirm C. arbutoides as the host plant of the leotioid mycorrhiza.
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