Hamada H, Hiramatsu M, Edamatsu R, Mori A
Department of Neuroscience, Okayama University Medical School, Japan.
Arch Biochem Biophys. 1993 Oct;306(1):261-6. doi: 10.1006/abbi.1993.1509.
TJ-960 is a Japanese Kampo (traditional herbal) medicine used for the treatment of epilepsy. It's a crude drug, an extract of nine herbs, and consists of many known and unknown components. Among the known components of TJ-960, we found that 5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one (baicalein) might be the most potent scavenger for radicals. In the present study, we examined in vitro the radical scavenging effect of baicalein in detail using electron spin resonance spectrometry. Furthermore, we examined in vivo its effect on the thiobarbituric acid-reactive substances (TBARS) levels and superoxide dismutase in the brain of rats with FeCl3-induced epilepsy and on hippocampal delayed neuronal death in gerbils with transient ischemia. In in vitro experiments, baicalein quenched in a dose-dependent manner 1,1-diphenyl-2-picrylhydrazyl, superoxide, and hydroxyl radicals. In the FeCl3-induced epileptic model, baicalein suppressed the increase in the TBARS level at the FeCl3-injected site. Baicalein also inhibited hippocampal neuronal death induced by 5 min of cerebral ischemia in gerbils. Hence the present study suggested that baicalein is one of the active components in TJ-960, which partially contributes to the antiepileptic and neuronal protective effects of TJ-960, and that the mechanism of its pharmacological action is based upon radical quenching and antioxidative effects.
TJ - 960是一种用于治疗癫痫的日本汉方（传统草药）药。它是一种粗药，由九种草药提取物组成，包含许多已知和未知成分。在TJ - 960的已知成分中，我们发现5,6,7 - 三羟基 - 2 - 苯基 - 4H - 1 - 苯并吡喃 - 4 - 酮（黄芩素）可能是最有效的自由基清除剂。在本研究中，我们使用电子自旋共振光谱法详细研究了黄芩素在体外的自由基清除作用。此外，我们研究了其在体内对氯化铁诱导的癫痫大鼠大脑中硫代巴比妥酸反应性物质（TBARS）水平和超氧化物歧化酶的影响，以及对短暂性脑缺血沙土鼠海马延迟性神经元死亡的影响。在体外实验中，黄芩素以剂量依赖性方式淬灭1,1 - 二苯基 - 2 - 苦基肼、超氧阴离子和羟基自由基。在氯化铁诱导的癫痫模型中，黄芩素抑制了氯化铁注射部位TBARS水平的升高。黄芩素还抑制了沙土鼠5分钟脑缺血诱导的海马神经元死亡。因此，本研究表明黄芩素是TJ - 960中的活性成分之一，它部分有助于TJ - 960的抗癫痫和神经保护作用，并且其药理作用机制基于自由基淬灭和抗氧化作用。
