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体内的丙烯酸微球。II. 聚丙酰胺微粒中L-天冬酰胺酶对大鼠的影响。

Acrylic microspheres in vivo. II. The effect in rat of L-asparaginase given in microparticles of polyacrylamide.

作者信息

Edman P, Sjöholm I

出版信息

J Pharmacol Exp Ther. 1979 Dec;211(3):663-7.

PMID:512928
Abstract

L-Asparaginase was immobilized in spherical microparticles of polyacrylamide. Particles of three different sizes, mean diameter 0.34, 18 and 36 micron, respectively, were used. The Michaelis constant Km, for L-asparaginase, immobilized in small particles (0.34 micron), is virtually the same as in solution. L-Asparaginase in microparticles was also more stable than free enzyme after storage for 140 days at +4 and +37 degrees C. After an i.v. injection of 200 I.U./kg into rat, the plasma L-asparagine fell to very low values (less than 10 nmol/ml), but was normalized again after 4 to 5 days with both the native and immobilized enzymes. After an i.p. injection of 1000 I.U./kg into rats, the microparticles containing L-asparaginase lowered the plasma L-asparagine level for a substantially longer period of time than L-asparaginase in free solution. Normal L-asparagine level was thus reached on day 14 after the injection with immobilized enzyme. However, L-asparaginase activity was still present in the abdominal lymph nodes after this period of time.

摘要

L-天冬酰胺酶被固定在聚丙烯酰胺的球形微粒中。使用了三种不同尺寸的微粒,平均直径分别为0.34微米、18微米和36微米。固定在小颗粒(0.34微米)中的L-天冬酰胺酶的米氏常数Km与溶液中的几乎相同。在4℃和37℃储存140天后,微粒中的L-天冬酰胺酶也比游离酶更稳定。给大鼠静脉注射200国际单位/千克后,血浆L-天冬酰胺降至非常低的值(低于10纳摩尔/毫升),但使用天然酶和固定化酶4至5天后又恢复正常。给大鼠腹腔注射1000国际单位/千克后,含L-天冬酰胺酶的微粒使血浆L-天冬酰胺水平降低的时间比游离溶液中的L-天冬酰胺酶长得多。因此,注射固定化酶后第14天达到正常L-天冬酰胺水平。然而,这段时间后腹部淋巴结中仍存在L-天冬酰胺酶活性。

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