RESUMEN
Two new compounds (1 and 2), belonging to C-20 oxygenated ent-kauranes-type diterpenoids, were identified from the aerial parts of Isodon serra. Their structures were elucidated by extensive analysis of HRESI-MS and NMR spectroscopic data. Both these two compounds possess a common 7,20-epoxy-ent-kauranes skeleton with a hydroxyl group rarely occurring at C-13. Compounds 1 and 2 were evaluated for their cytotoxic activity against Hela-60 and HepG2 as well as the antibacterial activity against Staphylococcus aureus, Bacillus cereus and Escherichia coli.
Asunto(s)
Antineoplásicos Fitogénicos , Diterpenos de Tipo Kaurano , Diterpenos , Isodon , Antineoplásicos Fitogénicos/química , Diterpenos/análisis , Diterpenos/farmacología , Diterpenos de Tipo Kaurano/química , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Isodon/química , Estructura Molecular , Componentes Aéreos de las Plantas/químicaRESUMEN
One new oleanane-type nortriterpene, rosanortriterpene A (1), and one new ursane-type nortriterpene, rosanortriterpene B (2), were isolated from the fruits of Rosa laevigata var. leiocapus. The structures of 1-2 were fully characterised on the basis of extensive spectroscopic analysis, including IR, HRESIMS, as well as 1D and 2D NMR spectral data (HSQC, 1H-1H COSY, and HMBC). To the best of our knowledge, this represents the first study on the chemical constituents of R. laevigata var. leiocapus. Compounds 1-2 exhibited moderate inhibitory effects on NO production in LPS stimulated RAW264.7 cells with IC50 values of 29.29 ± 3.64 and 14.28 ± 1.20 µM, respectively.
Asunto(s)
Frutas/química , Rosa/química , Triterpenos/aislamiento & purificación , Animales , Antibacterianos/farmacología , Antiinflamatorios/farmacología , Bacterias/efectos de los fármacos , Espectroscopía de Resonancia Magnética con Carbono-13 , Concentración 50 Inhibidora , Ratones , Pruebas de Sensibilidad Microbiana , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Ácido Oleanólico/farmacología , Espectroscopía de Protones por Resonancia Magnética , Células RAW 264.7 , Triterpenos/química , Triterpenos/farmacologíaRESUMEN
Rosanortriterpenes A-B (RTA and RTB), two nortriterpenoids, are characteristic constituents in the fruits of Rosa laevigata var. leiocapus. However, pharmacological studies on these compounds are still scarce. In the present study, we aim to investigate the anti-inflammatory mechanisms associated with the effects of RTA-B in RAW264.7 macrophages and LO2 cells by detecting cell viabilities, nitric oxide (NO) production, tumour necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) production. Simultaneously, the anti-inflammatory action mechanisms of these two compounds were illustrated through western blot assay. Besides, the antihepatic fibrosis activities of these compounds have also been explored. The results demonstrated that RTA and RTB inhibited the production of NO, TNF-α, and IL-6 and suppressed liver fibrosis. RTA and RTB treatment also greatly inhibited the activation of NF-kappaB (NF-κB) pathway. Our study confirmed the promising anti-inflammatory and anti-liver fibrosis actions of RTA-B, suggesting that they might be developed as alternative and promising drugs for the treatment of hepatic inflammatory and fibrotic diseases.