Li K, Vaughan G M, Reiter R J
Endocr Res. 1987;13(1):43-8. doi: 10.1080/07435808709023661.
A single injection of either 5 or 10 mg/kg 8-methoxypsoralen (8-MOP) was given intraperitoneally to male rats at the end of the 14 h light phase (at 2000 h). Two h later (at 2200 h), when the normal nocturnal surge of N-acetyltransferase (NAT) activity and melatonin content in the pineal gland had begun in vehicle-injected controls, mean pineal NAT after the 10 mg/kg 8-MOP was 1.8-fold higher than that after vehicle, though pineal melatonin content did not differ between vehicle- and drug-injected rats. By 4 h into the dark period (at 2400 h), the NAT activity in both 8-MOP injected groups of rats was greater than that in vehicle treated animals; again, however, 8-MOP treatment did not influence the pineal melatonin content. At 0200 h (6 h into the dark period), the difference between the NAT activity in pineals of rats treated with 5 mg/kg 8-MOP and the vehicle was not statistically significant, but the animals that received 10 mg/kg drug still had statistically elevated levels of the serotonin acetylating enzyme. At 0200 h the pineal melatonin levels were equivalent among the three treatment groups. Rats given 5mg/kg 8-MOP always had NAT values intermediate between those of rats injected with vehicle and those that received 10 mg/kg 8-MOP suggesting that the NAT response to the drug was dose related. These results show that the pineal response to psoralen involves an elevation of NAT activity without a commensurate change in the melatonin content of the gland.
在光照期14小时结束时(2000时),给雄性大鼠腹腔注射5或10毫克/千克的8-甲氧基补骨脂素(8-MOP)。两小时后(2200时),当注射赋形剂的对照大鼠开始出现松果体中N-乙酰转移酶(NAT)活性和褪黑素含量的正常夜间激增时,注射10毫克/千克8-MOP后松果体NAT比注射赋形剂后高1.8倍,不过注射赋形剂和药物的大鼠之间松果体褪黑素含量没有差异。到黑暗期4小时时(2400时),两个注射8-MOP的大鼠组中的NAT活性均高于接受赋形剂处理的动物;然而,8-MOP处理仍未影响松果体褪黑素含量。在0200时(黑暗期6小时),注射5毫克/千克8-MOP的大鼠松果体中NAT活性与注射赋形剂的大鼠之间的差异无统计学意义,但接受10毫克/千克药物的动物中血清素乙酰化酶水平仍有统计学意义的升高。在0200时,三个处理组之间松果体褪黑素水平相当。注射5毫克/千克8-MOP的大鼠的NAT值始终介于注射赋形剂的大鼠和接受10毫克/千克8-MOP的大鼠之间,这表明对该药物的NAT反应与剂量相关。这些结果表明,松果体对补骨脂素的反应涉及NAT活性升高,而腺体中褪黑素含量没有相应变化。