RESUMEN
A series of lamiridosin A derivatives were synthesized through simple procedures. Their antitumor activities were evaluated against EC9706, MGC803, and B16 cell lines in vitro. Several compounds showed potent antitumor activity, especially compound 10, with IC50 value of 2.36 µmol/L against MGC803 cell lines, is more potent than marketed positive drug 5-fluorouridine (5-FU).
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Iridoides/síntesis química , Iridoides/farmacología , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Iridoides/química , Estructura Molecular , Estereoisomerismo , Relación Estructura-Actividad , Uridina/análogos & derivados , Uridina/farmacologíaRESUMEN
OBJECTIVE: To investigate the chemical constituents of Melissa officinalis leaves. METHODS: The chemical constituents were separated by silica gel column chromatography and their structures were determined by spectroscopic experiments. RESULTS: 13 compounds were isolated and identified as protocatechuyl aldehyde(1), serratagenic acid(2), vanillin(3), 2α,3ß-dihydroxy-urs-12-en-28-oic acid(4), ursolic acid(5), oleanolic acid(6), daucosterol(7),2α,3ß,23,29-tetrahydroxyolean-12-en-28-oic acid-29-O-ß-D-gluco- pyranoside(8), luteolin(9) rosmarinic acid(10), luteolin-7-O-ß-D-glucoside (11), ß-stitosterol(12) and palmitic acid(13). CONCLUSION: Compounds 1 ~ 8 are separated from this plant for the first time and compounds 1-4 and 8 are isolated from this genus for the first time.