RESUMO
Four undescribed amide alkaloids hongkongensines A-C and 1-(1-oxo-6-hydroxy-2E,4E-dodecadienyl)-piperidine, five known amide alkaloids, and three known neolignans were isolated from the aerial part of Piper hongkongense. The planar structures of these compounds were determined by detailed analyses of HR-ESI-MS and NMR data. The absolute configurations of hongkongensines A-C were elucidated by single-crystal X-ray diffraction analysis and ECD calculations. Moreover, the inhibitory activities of PCSK9 expression in vitro for all compounds were assessed by PCSK9 AlphaLISA screening. Kadsurenone (10) displayed a significant inhibitory activity at 5 µM with an inhibition rate of 51.98%, compared with 55.55% of berberine (BBR 5 µM).
Assuntos
Alcaloides , Lignanas , Inibidores de PCSK9 , Compostos Fitoquímicos , Piper , Componentes Aéreos da Planta , Piper/química , Estrutura Molecular , Alcaloides/farmacologia , Alcaloides/isolamento & purificação , Alcaloides/química , Lignanas/farmacologia , Lignanas/isolamento & purificação , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Componentes Aéreos da Planta/química , Amidas/farmacologia , Amidas/isolamento & purificação , Amidas/química , Pró-Proteína Convertase 9/metabolismo , ChinaRESUMO
Thirteen previously undescribed iridoids (1-13), together with five known iridoids (14-18) were isolated from the roots and rhizomes of Valeriana jatamansi Jones. Their structures with absolute configurations were elucidated by analysis of MS, NMR, optical rotation and their experimental and calculated electronic circular dichroism spectra. All of the isolated compounds were tested for their protective effects against α-hemolysin-induced cell death in A549 cells. Compounds 14, 16 and 17 showed moderate protective effects, and compounds 15 and 18 showed weak protective effects.
Assuntos
Nardostachys , Valeriana , Rizoma , Valeriana/química , Proteínas Hemolisinas/análise , Estrutura Molecular , Iridoides/farmacologia , Iridoides/química , Raízes de Plantas/químicaRESUMO
Five undescribed guanidine alkaloids, plumbagines HK (1-4) and plumbagoside E (5), as well as five known analogues (6-10) were isolated from the roots of Plumbago zeylanica. Their structures were established by extensive spectroscopic analyses and chemical methods. In addition, 1-10 were accessed their anti-inflammatory activities by measuring nitric oxide (NO) concentrations in LPS-induced RAW 264.7 cells. However, all compounds especially 1 and 3-5 could not inhibit the secretion of NO but significant increase the secretion of NO. The result reminded us that 1-10 may become potential novel immune potentiators.