We aimed to develop a standardized methodology to determine the metabolic profile of organic extracts from Malvaviscus arboreus Cav. (Malvaceae), a Mexican plant used in traditional medicine for the treatment of hypertension and other illnesses. Also, we determined the vasorelaxant activity of these extracts by ex vivo rat thoracic aorta assay. Organic extracts of stems and leaves were prepared by a comprehensive maceration process. The vasorelaxant activity was determined by measuring the relaxant capability of the extract to decrease a contraction induced by noradrenaline (0.1 μM). The hexane extract induced a significant vasorelaxant effect in a concentration‐ and endothelium‐dependent manner. Secondary metabolites, such as polyunsaturated fatty acids, terpenes and one flavonoid, were annotated by liquid chromatography/quadrupole time‐of‐flight mass spectrometry (LC/QTOF‐MS) in positive ion mode. This exploratory study allowed us to identify bioactive secondary metabolites from Malvaviscus arboreus, as well as identify potentially‐new vasorelaxant molecules and scaffolds for drug discovery.
La escuaramida y sus derivados representan un importante grupo de sustancias que actualmente se están aplicando exitosamente en estrategias de organocatálisis asimétrica. En esta contribución se presenta un resumen del estado del arte relativo a la síntesis de los derivados de escuaramida y su papel como inductores de quiralidad en secuencias sintéticas relevantes. Por ello, se establece un proceso de búsqueda sistemática y selección de reportes publicados en revistas especializadas del área, con la finalidad de presentar los aspectos más notables de síntesis y la aplicación de los derivados de escuaramida en esta sustancial área de la química orgánica.
Herein we report an exploratory study based on the cytotoxicity and antiproliferative activity of four previously synthesized coumarins derivatives (compounds 1a-d). The cytotoxic effect of the compounds was assessed on mononuclear cells, which were obtained from blood samples of healthy donors and measured by XTT method. The antiproliferative activity experiments were developed using HeLa, CaSKi and SiHa cervical cancer cell lines, and was evaluated by the MTT assay. In every single experiment, Cisplatin as internal control was employed. The cytotoxic assessment revealed that the four compounds did not significantly affect the viability on normal cells, whereas the antiproliferative activity on cancer cells was variable, according to the substituent located at position 3 of the coumarin core. It is worth mentioning that compound 1c, compared with the other products, presented a remarkable effect against CaSKi cell line, likewise 1d but in HeLa cells. These findings suggest that there is a relationship between biological activity and the alkoxycarbonyl chain since this is the only structural difference among the four tested compounds. The results lead to conclude that butyl group which is the substituent in compound 1d, was the key element in the antiproliferative effect presented by the molecule against SiHa, CaSKi and HeLa cell lines.
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