Kuribayashi Y, Naritomi H, Sasaki M, Sawada T
Division of Cerebral Circulation Research, National Cardiovascular Center, Osaka, Japan.
Arzneimittelforschung. 1994 Sep;44(9):995-8.
Effect of L-ascorbic acid 2-[3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H -1- benzopyran-6yl-hydrogen phosphate] potassium salt (EPC-K1, CAS 127061-56-7), a diester of alpha-tocopherol and ascorbic acid, on transient cerebral ischemia was studied in Mongolian gerbils. Cerebral energy metabolism and intracellular pH (pHi) were estimated employing in vivo 31P nuclear magnetic resonance (NMR) spectroscopy. Intraperitoneal injection of EPC-K1 (5 or 10 mg/kg) prior to ischemia significantly ameliorated pHi reduction in a dose dependent manner during ischemia. After reperfusion, energy and pHi recoveries were significantly faster in the EPC-K1 groups than in the control group. EPC-K1 (10 mg/kg) significantly reduced the extent of cerebral edema. Moreover, administration of EPC-K1 immediately after reperfusion significantly shortened the consciousness recovery in a dose dependent manner. The results suggest that EPC-K1 may exert protective effects on ischemic brain and may have therapeutic value in ischemic stroke.
研究了α-生育酚与抗坏血酸的二酯L-抗坏血酸2-[3,4-二氢-2,5,7,8-四甲基-2-(4,8,12-三甲基十三烷基)-2H-1-苯并吡喃-6-基-氢磷酸酯]钾盐（EPC-K1，CAS 127061-56-7）对蒙古沙鼠短暂性脑缺血的影响。采用体内31P核磁共振（NMR）波谱法评估脑能量代谢和细胞内pH（pHi）。缺血前腹腔注射EPC-K1（5或10mg/kg）可在缺血期间以剂量依赖的方式显著改善pHi降低。再灌注后，EPC-K1组的能量和pHi恢复明显快于对照组。EPC-K1（10mg/kg）可显著减轻脑水肿程度。此外，再灌注后立即给予EPC-K1可显著以剂量依赖的方式缩短意识恢复时间。结果表明，EPC-K1可能对缺血性脑发挥保护作用，在缺血性卒中中可能具有治疗价值。
