RESUMEN
AIMS: We evaluated the in vitro antioxidant and antimicrobial potential of Schimpera arabica extract and fractions (2-Hexadecen-1-ol and beta sitosterol). METHODS AND RESULTS: Free radical scavenging activity was estimated by using ABTS and DPPH methods, reducing power and iron chelation was studied to investigate antioxidant potential of the extracts. Well-diffusion method was utilized to evaluate the antimicrobial activity of the extracts. Gas chromatography-mass spectroscopy analysis of the extract revealed the presence of 27 compounds. Phenolic and flavonoid contents were found in high amount (7·6-18 mg GAE, mg g-1 ; 3·2-10·8 mg catechin, mg g-1 ) in dry plant material. CONCLUSIONS: Among all the extracts, 2-Hexadecen-1-ol and beta sitosterol were the major constituents of crude extract and exhibited significant antioxidant potential as well antimicrobial activity; however, all other fractions also exhibited fare degree of antioxidant potential. 93% DPPH was scavenged by 100 µg ml-1 of the ethyl acetate fraction; in ABTS assay chelation was 86·2 and 88% in ferric chloride reducing power assay. SIGNIFICANCE AND IMPACT OF THE STUDY: Schimpera arabica is naturally present and used in food preparation in most Arabian nations. The characterization of S. arabica would provide an insight into its medicinal use as home remedial for bacterial infection and as antioxidant. Significant and comparable antimicrobial activity was demonstrated by both 2-Hexadecen-1-ol and beta sitosterol fractions. The results suggest that S. arabica contain a good amount of natural antioxidants of medicinal importance. However, further investigations are needed to characterize the further activity of 2-Hexadecen-1-ol and beta sitosterol in vivo.
Asunto(s)
Antiinfecciosos/farmacología , Antioxidantes/farmacología , Brassicaceae/química , Alcoholes Grasos/farmacología , Sitoesteroles/farmacología , Terpenos/farmacología , Antibacterianos/análisis , Alcoholes Grasos/química , Alcoholes Grasos/aislamiento & purificación , Flavonoides/análisis , Cromatografía de Gases y Espectrometría de Masas , Fenoles/análisis , Extractos Vegetales/química , Extractos Vegetales/farmacología , Terpenos/química , Terpenos/aislamiento & purificaciónRESUMEN
A novel series of newly synthesized thiophene derivatives, ethyl-4,5-dimethyl-2-(3-(3,4,5-trimethoxyphenyl)thioureido)thiophene-3-carboxylate 3, ethyl-2-[(2-(dimethylamino)ethoxy)mercapto)methyleneamino)]-4,5-dimethyl-thiophene-3-carboxylate 9, thienopyrimidines 4, 7, 10-20, triazolothienopyrimidines 5, 6 were prepared and tested for their antiproliferative activity. The structures of the synthesized compounds were confirmed on the basis of elemental analysis, IR, (1)H-NMR, (13)C-NMR and mass spectral data. The results showed that the synthesized compounds were more active on breast cancer than on colon cancer cell lines and the most potent compounds in this study are compounds 3 and 13 which exerted remarkable activity against MDA-MB-231 (breast cancer) and HT-29 (colon cancer) cell lines with IC50 values (40.68, 49.22 µM) for compound 3 and (34.04, 45.62 µM) for compound 13. Also, compounds 4-6, 9 showed a moderate activity against breast cancer cell line, while compounds 15, 19 and 20 showed no activity.
Asunto(s)
Antineoplásicos/farmacología , Pirimidinas/farmacología , Tiofenos/farmacología , Antineoplásicos/síntesis química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Humanos , Pirimidinas/síntesis química , Relación Estructura-Actividad , Tiofenos/síntesis químicaRESUMEN
A variety of thiophene derivatives bearing diphenylsulfone 3,4, diazepines 5b, 6b, phenylamino 7, piperidine 8, benzylpiperidine 9, oxazepines 10b, 11b, acrylaldehydes 12-14 and benzeonesulfanamide 15 were synthesized. some newly synthesized compounds were evaluated for their in vitro cytotoxic activity against human tumor breast cancer cell lines. The tested compounds showed moderate to good cytotoxic activity and indeed, some of them were more potent than doxorubicin as a reference drug.