Friedman Y, Park S, Levasseur S, Burke G
Biochim Biophys Acta. 1977 Dec 22;500(2):291-303. doi: 10.1016/0304-4165(77)90021-6.
When spermidine, putrescine or 1,3-diaminopropane was injected (12.5 mumol/100 g body weight) into rats 1 h before thyrotropin, ornithine decarboxylase activity was increased by 75--150% over control levels. However, when greater than or equal to 75 mumol polyamine/100 g body weight was injected, thyrotropin-activated activity was inhibited by 70--95%. Multiple polyamine injections inhibited goitrogen-induced activity and gland weight increase by approx 35%. The polyamines also inhibited thyrotropin-activated rat thyroid ornithine decarboxylase in vitro in a dose-related fashion, with 50% inhibition occurring at 2--5 . 10(-4)M. The inhibition was not due to a direct effect on the enzyme. No stimulation was seen with low concentrations of polyamine. The polyamines had no effect on in vitro thyroid protein/RNA synthesis or glucose oxidation but had a biphasic effect on plasma membrane adenylate cyclase activity. A protein inhibitor to thyroid ornithine decarboxylase was generated in vivo by multiple injections of the polyamines into rats and in vitro by incubating bovine thyroid slices with 2--10 mM polyamine. The inhibitor was non-dialyzable, destroyed by boiling, and its formation was blocked in a dose-related fashion by cycloheximide. We conclude that: (1) thyroid ornithine decarboxylase is subject not only to positive control, but is also negatively regulated by its end-products, the polyamines, which induce a protein inhibitor to ornithine decarboxylase; (2) since gland growth is also inhibited under these conditions, the polyamine effect on thyroid ornithine decarboxylase may be biologically significant.
在促甲状腺素注射前1小时,给大鼠注射亚精胺、腐胺或1,3 - 二氨基丙烷(12.5 μmol/100 g体重),鸟氨酸脱羧酶活性比对照水平增加75% - 150%。然而,当注射大于或等于75 μmol多胺/100 g体重时,促甲状腺素激活的活性被抑制70% - 95%。多次注射多胺可使致甲状腺肿物质诱导的活性及腺体重量增加受到约35%的抑制。多胺在体外也以剂量相关方式抑制促甲状腺素激活的大鼠甲状腺鸟氨酸脱羧酶,在2 - 5×10⁻⁴M时出现50%的抑制。这种抑制并非由于对该酶的直接作用。低浓度多胺未观察到刺激作用。多胺对体外甲状腺蛋白质/RNA合成或葡萄糖氧化无影响,但对质膜腺苷酸环化酶活性有双相作用。通过多次给大鼠注射多胺在体内以及用2 - 10 mM多胺孵育牛甲状腺切片在体外产生了一种甲状腺鸟氨酸脱羧酶的蛋白质抑制剂。该抑制剂不可透析,煮沸可破坏,其形成被环己酰亚胺以剂量相关方式阻断。我们得出结论:(1)甲状腺鸟氨酸脱羧酶不仅受到正向调控,还受到其终产物多胺的负向调控,多胺诱导一种鸟氨酸脱羧酶的蛋白质抑制剂;(2)由于在这些条件下腺体生长也受到抑制,多胺对甲状腺鸟氨酸脱羧酶的作用可能具有生物学意义。