黄嘌呤衍生物对大鼠脑内碱性磷酸酶的抑制作用。
The inhibitory effect of xanthine derivatives on alkaline phosphatase in the rat brain.
作者信息
Sugimura K, Mizutani A
出版信息
Histochemistry. 1979 Jun 18;61(2):131-7. doi: 10.1007/BF00496525.
Histochemical and biochemical studies were carried out on the inhibition of alkaline phosphatase (A1-P) activity in rat cerebral cortex with various methylxanthine derivatives. The histochemical study revealed that A1-P activity was completely inhibited with 2 mM theophylline or aminophylline, only slightly inhibited with 5 mM of xanthine, and no way inhibited even with 5 mM of diprophylline or caffeine. The biochemical study showed that A1-P activity was markedly inhibited by 1 mM theophylline, to 36% of the control value, and equally markedly by 1 mM aminophylline to 26% of the control value. It was only inhibited to 99% of the control value even by 5 mM diprophylline and conversely slightly activated, to 110% of the control value, by caffeine. The relationship between the pharmacological activities of methylxanthine derivatives and A1-P was studied, and the biological role of A1-P in the central nervous system was also discussed.
利用各种甲基黄嘌呤衍生物对大鼠大脑皮层碱性磷酸酶（A1-P）活性的抑制作用进行了组织化学和生物化学研究。组织化学研究表明，2 mM 茶碱或氨茶碱可完全抑制 A1-P 活性，5 mM 黄嘌呤仅轻微抑制该活性，而即使 5 mM 二羟丙茶碱或咖啡因也无法抑制该活性。生物化学研究显示，1 mM 茶碱可显著抑制 A1-P 活性，降至对照值的 36%，1 mM 氨茶碱同样显著抑制，降至对照值的 26%。即使 5 mM 二羟丙茶碱也仅将其抑制至对照值的 99%，相反，咖啡因可使其轻微激活，升至对照值的 110%。研究了甲基黄嘌呤衍生物的药理活性与 A1-P 之间的关系，并讨论了 A1-P 在中枢神经系统中的生物学作用。
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