RESUMEN
Four undescribed neolignans and three undescribed amide alkaloids, along with twelve known compounds, were isolated from the stems of Piper kadsura (Choisy) Ohwi. The structures of the new compounds were determined by spectroscopic analysis, quantum-chemical calculations, and Mo2(OAc)4-induced ECD analysis. The neuroprotective effects of these compounds against Aß25-35-induced cell damage in PC12 cells were investigated, and eight compounds exhibited significant neuroprotective effects against Aß25-35-induced PC12 cell damage, with the EC50 values of 3.06-29.3 µM. Three of these compounds were selected for further experiments, and they appear to reduce apoptosis and enhance autophagy against Aß25-35-induced PC12 cell damage.
Asunto(s)
Alcaloides , Kadsura , Lignanos , Fármacos Neuroprotectores , Piper , Alcaloides/química , Alcaloides/farmacología , Amidas/química , Amidas/farmacología , Animales , Lignanos/química , Lignanos/farmacología , Estructura Molecular , Fármacos Neuroprotectores/farmacología , Piper/química , Tallos de la Planta , RatasRESUMEN
Highly enantioselective arylation of aryl aldehydes catalyzed by (S)-H8 -BINOL-Ti(Oi-Pr)2 complex in the presence of N-methylmorpholine (NMM) as an effective and inexpensive additive is described for the first time. We found high enantioselectivity and yield but successfully reduced the equivalents of nucleophiles triarylaluminums by 50% compared with our previous report. The practicability of the process was thereby greatly increased.
RESUMEN
OBJECTIVE: To explore the function of Caspase-3 and p38 MAPK in MMT-induced apoptosis in PC-3M cells. METHODS: After incubation of PC-3M cells with 1 mmol/L MMT, the activity of Caspase-3 was examined. The influence on cells viability of Z-DEVD-FMK, a Caspase-3-specific peptide inhibitor, was also examined. Western blot was used to examine the change of p38 MAPK. The effect on cells viability and Caspase-3 activity of SB203580, a specific inhibitor of p38 MAPK, were also examined. RESULTS: The activity of Caspase-3 increased significantly in MMT-induced apoptosis in PC-3M cells /9P < 0.01), and Z-DEVD-FMK could protect cells from apoptosis (P < 0.01). In this course, the phosphorylation of p38 MAPK could be observed. SB203580 inhibited Caspase-3 activity (P < 0.05) and prevented PC-3M cells from MMT-induced apoptosis (P < 0.05). CONCLUSION: Caspase-3 and p38 MAPK are involved in MMT-induced PC-3M cells apoptosis.