RESUMO
Eight pentacyclic triterpenoids including two new ones (1, 2) were isolated from the fruits of Xanthium strumarium. Their structures were elucidated by extensive spectroscopic analysis. All isolates were evaluated for in vitro cytotoxic activity on HepG2, A549, HCT116 and SW480 cancer cells. Among them, the new compound 2 was found to exhibit significant cytotoxic activity on A549, HCT116 and SW480 cancer cells with IC50 values of 9.68, 4.27 and 7.58 µM, respectively. Further, 2 was selected for cell cycle analysis and results revealed that 2 could cause HCT116 cell cycle arrest in G1 phase. In addition, Annexin V-FITC/PI staining assay showed that 2 could induce the death of HCT116 cells.
Assuntos
Antineoplásicos , Xanthium , Frutas , Compostos Fitoquímicos/farmacologia , Xanthium/químicaRESUMO
Two new flavonoid glycosides named 6-hydroxy-3-methoxy-apigenin 7-O-α-Ê-rhamnopyranoside (1) and 3-hydroxyl-apigenin 8-C-ß-á´ -xylopyranoside (2), along with five known compounds (3-7), were isolated from Xanthium strumarium. Their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All compounds were evaluated for in vitro inhibitory activity against PTP1B. Among them, compounds 1 and 5 showed significant inhibitory activity on PTP1B with IC50 values of 11.3 ± 1.7 and 8.9 ± 0.7 µM, respectively.
Assuntos
Flavonoides , Glicosídeos , Proteína Tirosina Fosfatase não Receptora Tipo 1 , Xanthium , Flavonoides/farmacologia , Glicosídeos/farmacologia , Estrutura Molecular , Compostos Fitoquímicos/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Xanthium/químicaRESUMO
Five new metabolites, including two monoterpene glycosides Pubescenosides L-M (1-2) and three phenolic glycosides, Pubescenosides N-P (3-5), along with nineteen known ones, including liganoids, hemiterpenoids and caffeoylquinic acid derivates, were isolated from the roots of Ilex pubescens. Their structures were elucidated from extensive spectroscopic analysis, including 1D and 2D NMR experiments. This study is the first to report monoterpene glycosides with ß-pinene aglycone in Aquifoliaceae. Nine of these compounds were evaluated in vitro for their anti-platelet aggregation activities. Among them, compounds 3 and 4 showed moderate inhibitory activities on ADP-induced blood platelet aggregation [inhibition (%): 32.3 and 33.6, respectively] as compared to aspirin.