RESUMEN
Various separation methods in combination with spectral data analysis, X-ray single crystal diffraction analysis, and litera-ture data comparison were employed to clarify the chemical constituents of Itea yunnanensis. Seven compounds were obtained from I. yunnanensis, which were identified as(S)-3-[1-(4-hydroxyphenyl)propane-2-yl]-4-methoxybenzoate methyl ester(1), iteafuranal B(2), syringaresinol(3), dihydrokaempferol(4), trimethoxybenzene(5), eicosane(6), and nonacosane(7), respectively. Among them, compound 1 was a new nor-neolignan compound named iteanorneoligan A, and the rest of the compounds were identified from I. yunnanensis for the first time. The anti-hepatocellular carcinoma effect of the compound was evaluated based on Sk-hep-1 cells model via MTT assay, and compound 2 showed a significant inhibitory effect on the proliferation of Sk-hep-1 cells with an IC_(50) of 9.4 µmol·L~(-1). The antioxidant capacity was determined via DPPH, ABTS~(·+), and Oâ radical scavenging ability, and compound 1 exhibited a significant ABTS~(·+) radical scavenging effect with an IC_(50) of 0.178 mg·mL~(-1).
Asunto(s)
Lignanos , Estructura Molecular , Benzotiazoles , Ácidos Sulfónicos , Antioxidantes/farmacología , Antioxidantes/químicaRESUMEN
Five 3-formyl-2-arylbenzofuran derivatives, including three new compounds (1-3) and two known analogues (4-5), were identified from the 95% EtOH extract of Itea yunnanensis. Extensive spectroscopic analyses were performed for the structure elucidation of all new benzofurans, and single-crystal X-ray diffraction analyses were further employed for the structure verification of iteafuranals C (1) and D (2). In MTT assay, iteafuranal E (3) and iteafuranal A (4) displayed significant growth inhibition effect on SK-Hep-1 cells with IC50 values of 5.365 µM and 6.013 µM, respectively. The colony formation assay of 3 and 4 further confirmed their remarkable inhibitory effect on cell growth. Preliminary mechanism study demonstrated that 3 remarkably down-regulated the phosphorylation level of ERK, which suggested 3 could inhibit cell growth and induce apoptosis of SK-Hep-1 cells by blocking RAS/RAF/MEK/ERK signaling pathway. This study highlighted the potential of 3-fomyl-2-benzofuran derivatives as novel lead compounds to treat Hepatocellular carcinoma.[Formula: see text].
Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Apoptosis , Carcinoma Hepatocelular/patología , Línea Celular Tumoral , Proliferación Celular , Humanos , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/patología , Sistema de Señalización de MAP Quinasas , Transducción de SeñalRESUMEN
Three compounds with diuretic potential were identified from the 95% ethanol extract of Pyrrosia petiolosa (Christ) Ching. Among them, one was a new benzanilide named petiolide A (1), and the other two were phenolic derivatives barbatic acid (2) and kaempferol (3). Their structures were elucidated based on extensive spectral analyses and comparison with the literature data. The docking experiments of all compounds into the active site of the With-No-Lysine kinase 1 (WNK1) domain demonstrated that kaempferol (3) was the most effective component with diuretic potential for its comparative diuretic effect to that of an orally bioavailable WNK inhibitor WNK463 (docking score -10.99 vs -11.09).[Formula: see text].