RESUMEN
An investigation of the potential neuroprotective natural product constituents of the rhizomes of Typhonium giganteum led to the isolation of two new cerebrosides, typhonosides E (1) and F (2), along with 11 known analogues (3-13). The structures of compounds 1 and 2 were elucidated by spectroscopic data interpretation. The activity of these compounds against glutamate-induced cell apoptosis was investigated in PC12 cells. All compounds exhibited such activity, which was related to the length of the fatty acyl chain. Among them, longan cerebroside II (11), with the longest fatty acyl chain, showed the most potent protective effect in PC12 cells from glutamate injury, with an EC50 value of 2.5 µM. Moreover, at the molecular level, longan cerebroside II (11) downregulated the expression of caspase-9, caspase-3, and Bax, upregulated the expression of Bcl-2, and decreased the level of cytosolic cytochrome c in a concentration-dependent manner.
Asunto(s)
Cerebrósidos/aislamiento & purificación , Cerebrósidos/farmacología , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/farmacología , Animales , Apoptosis/efectos de los fármacos , Caspasa 3/metabolismo , Caspasa 9/metabolismo , Cerebrósidos/química , Citocromos c/metabolismo , Ácido Glutámico/farmacología , Estructura Molecular , Fármacos Neuroprotectores/química , Células PC12 , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Ratas , Rizoma/química , Sapindaceae , Transducción de Señal/efectos de los fármacosRESUMEN
OBJECTIVE: To study optimal water extraction condition of LiYan granule. METHODS: HPLC methods were developed for the determination of irisfloremin in LiYan granule. The contents of irisfloremin and extraction rate were selected as assessment indices. Three factors were studied by Doehlert design, including water-adding amount, decoction time and times of decoction. RESULTS: The optimal extracting condition was water consumed as 8 times of curd herb, and 3 times for 2 hours each time. CONCLUSION: The water extraction process is feasible, and the experiment result can provide basic and instruction data for the ascertainment of water extraction process of LiYan granule.
Asunto(s)
Algoritmos , Medicamentos Herbarios Chinos/aislamiento & purificación , Plantas Medicinales/química , Tecnología Farmacéutica/métodos , Cromatografía Líquida de Alta Presión , Combinación de Medicamentos , Medicamentos Herbarios Chinos/química , Proyectos de Investigación , Solventes , Factores de Tiempo , AguaRESUMEN
AIM: To investigate the water-soluble steroidal saponins in total saponin from Dioscorea nipponica Makino and look for new active compounds. METHODS: The compounds were isolated with silica gel, PTLC and HPLC, and their structures were elucidated by acid hydrolysis, physical and chemical data and spectral analysis (IR, NMR, MS, HMQC, HMBC) as well as chemical correlations. RESULTS: The two steroidal saponins (water-insoluble saponin and water-soluble saponin) were isolated from the total saponin of Dioscorea nipponica Makino. The structures were elucidated as diosgenin 3-O-[alpha-L-rhamnopy ranosyl (1-->2)-[beta-D-glucopyranosyl(1-->3)]]-beta-D-glucopyranoside (I), diosgenin 3-O-[alpha-L-rhamnopyranosyl (1-->3)-alpha-L-rhamnopyranosyl (1-->4)-alpha-L-rhamnopyranosyl (1-->4)]-beta-D-glucopyranoside (II). CONCLUSION: Compound II is a new steroidal saponin and firstly isolated from Dioscorea nipponica Makino. It was named as dioscin Dc.
