RESUMO
Two new compounds, 19-hydroxy-melodinine K (1) and melodiside (2), and 25 known compounds were isolated from leaves and twigs of Melodinus suaveolens. Their structures were elucidated based on 1- and 2-D NMR, FTIR, UV and MS spectroscopic data. 19-hydroxy-melodinine K showed cytotoxic activity against MDA-MB-231 breast, BCG-823 gastric, SW480 colon and Hela cancer cells.
Assuntos
Apocynaceae/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Folhas de Planta/químicaRESUMO
Continued interest in cytotoxic alkaloids resulted in the isolation of 37 alkaloids including 29 known monoterpenoid indole alkaloids from the aerial parts of Tabernaemontana officinalis. Of the remaining 8 alkaloids, six were bisindole alkaloids named taberdivarines A-F (1-6) and the two were monomers named taberdivarines G and H (7-8). Alkaloids 1 and 2 are voaphylline-vobasinyl type bisindole alkaloids, a structural type previously unknown, while 3-6 exhibited cytotoxicity against three human cancer cell lines HeLa, MCF-7, and SW480 with IC50 values ranging from 1.42 to 11.35 µM.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Alcaloides de Triptamina e Secologanina/isolamento & purificação , Alcaloides de Triptamina e Secologanina/farmacologia , Tabernaemontana/química , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Alcaloides de Triptamina e Secologanina/químicaRESUMO
OBJECTIVE: To prepare positive-ionized liposome gel containing paeonol and study its stability and cutaneous permeation kinetics in vitro. METHODS: Prepared the liposome gel by dispersion-ultrasonic and gridding method, and studied the stability with the impact factor experiments. Compared the permeation rate of liposome gel with conventional gel in vitro using the Franz-diffusion cell. RESULTS: Mean diameter of the liposome was (132.7 +/- 14.1) nm with Zeta potential of (+33.54 +/- 1.95) mV and mean entrapment efficiency of (73.04 +/- 1.24)% (n=3), and the content of paeonol was (3.17 +/- 0.13) mg/g (n=3). The liposome gel had a promising appearance. It was stable at the humidity and the room temperature while was sensitive at the light and the temperature from 40 degrees C to 60 degrees C. The cumulative penetration amounts of the liposome gel was higher than that of the conventional gel (P < 0.05). Its cutaneous penetration rate and cumulative amounts in skin were higher than those of the conventional gel (P < 0.05). CONCLUSION: The positive-ionized liposome gel containing paeonol is stable and feasibly prepared. It can enhance the cutaneous permeation efficiency and guarantee the persistent release rate.
