Takeda K, Kawai S, Kato F, Tetsuka T, Konno K
J Antibiot (Tokyo). 1978 Sep;31(9):884-7. doi: 10.7164/antibiotics.31.884.
The activity of purified prolyl hydroxylase (proline, 2-oxoglutarate dioxygenase, EC 1. 14. 11. 2) was enhanced 3 approximately 8-fold at a low concentration of ferrous ion (1 X 10(-5 M) by addition of bleomycin, a glycopeptide antibiotic with antineoplastic activity and a side effect of producing pulmonary fibrosis. The maximum stimulation was attained at a concentration of 15 microgram/ml bleomycin (about 1 X 10(-5) M), which was approximately equimolar with the ferrous ion, one of the cofactors of this enzyme. Addition of bleomycin to the assay mixture resulted in a change of the optimal concentration of ferrous ion from 2 X 10(-3) M to 1 X 10(-5) M. Changing the order of addition of ferrous ion, enzyme and bleomycin in assay medium before incubation at 37 degrees C, the stimulatory activity was varied. Blemycin A2Cu++(Cu++-chelated bleomycin), which scarcely complexed with Fe++, had no enhancing effects on the enzymatic activity. We discuss the possible reasons as to why the activity of prolyl hydroxylase was enhanced by addition of bleomycin in the assay mixture.
通过添加博来霉素（一种具有抗肿瘤活性且有导致肺纤维化副作用的糖肽类抗生素），纯化的脯氨酰羟化酶（脯氨酸，2-氧代戊二酸双加氧酶，EC 1.14.11.2）的活性在低浓度亚铁离子（1×10⁻⁵ M）下增强了约8倍。在15微克/毫升博来霉素（约1×10⁻⁵ M）的浓度下达到最大刺激效果，该浓度与亚铁离子（此酶的辅因子之一）大致等摩尔。向测定混合物中添加博来霉素导致亚铁离子的最佳浓度从2×10⁻³ M变为1×10⁻⁵ M。在37℃孵育前改变测定介质中亚铁离子、酶和博来霉素的添加顺序，刺激活性会有所变化。几乎不与Fe⁺⁺络合的博来霉素A2Cu⁺⁺（铜离子螯合的博来霉素）对酶活性没有增强作用。我们讨论了在测定混合物中添加博来霉素会增强脯氨酰羟化酶活性的可能原因。
