蒽环霉素对磷脂酶A2活性的影响和在大鼠胃粘膜前列腺素E2生产。
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Grataroli R, Leonardi J, Chautan M,拉丰H, Nalbone G
蒽环霉素对磷脂酶A2活性的影响和在大鼠胃粘膜前列腺素E2生产。
生物化学杂志。1993年8月3;46 (3):349 - 55。
- PubMed ID
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8347160 (在PubMed]
- 文摘
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本研究的目的是调查在老鼠的影响三个蒽环霉素,pirarubicin、阿霉素、表阿霉素在胃前列腺素E2 (PGE2)代谢和磷脂酶A2 (PLA2 EC 3.1.1.4)活动。膜的前体水平,花生四烯酸,膜的稳定性进行了分析脂肪酸的组成。酶的活动参与的营业额膜磷脂,如溶血磷脂酶(EC 3.1.1.5 LPase)和酰coa lysophosphatidylcholine:酰基转移酶(EC 2.3.1.23 ACLAT)和脂质氢过氧化物的解毒,selenium-dependent谷胱甘肽过氧化物酶(EC 1.11.1.9氧化酶)测定注射药物后连续4天。Pirarubicin不产生任何这些活动,但阿霉素和盐酸表柔比星的变化产生PGE2和PLA2的活动减少,LPase ACLAT。氧化酶活力并没有改变任何的药物。PLA2活性的下降似乎并没有与膜脂质成分的变化是因为总磷脂含量不变。P / S(多不饱和/饱和)比率增加阿霉素组和减少表阿霉素组和未饱和指数适度修改。花生四烯酸增加阿霉素组。体外、PLA2活性并不是抑制三种药物在微摩尔的范围。显著抑制观察为pirarubicin 2.5毫米和1.0毫米阿霉素和盐酸表柔比星。 The Lineweaver-Burk representation showed that these inhibitions were of an uncompetitive type. Pirarubicin may therefore be considered to be an anthracycline without marked side-effects on gastric mucosa. However, the in vitro inhibition of PLA2 activity by anthracyclines does not fully explain the in vitro decrease in PLA2 specific activity observed after doxorubicin and epirubicin treatment, and in this context membrane structure modifications unconnected with the lipid composition can not be excluded. In vivo these phenomena may affect PGE2 synthesis, whose level was lower in the doxorubicin and epirubicin groups than in control group.