两性霉素B与N-D-鸟氨酰两性霉素B甲酯的体外和体内比较
In vitro and in vivo comparisons of amphotericin B and N-D-ornithyl amphotericin B methyl ester.
作者信息
Kobayashi G S, Little J R, Medoff G
出版信息
Antimicrob Agents Chemother. 1985 Mar;27(3):302-5. doi: 10.1128/AAC.27.3.302.
Abstract
N-D-Ornithyl amphotericin B methyl ester (N-D-ornithyl AmE) has a lower toxicity for animals than does amphotericin B (AmB), and peak serum levels can be achieved that are fourfold higher than those obtained with an equivalent dose of AmB. However, N-D-ornithyl AmE has one-fourth the in vitro activity and between one-fifth and one-eighth the in vivo activity of AmB. N-D-ornithyl AmE and the corresponding lysyl derivative also lack the immunoadjuvant effects of AmB.
摘要
N-D-鸟氨酰两性霉素B甲酯（N-D-ornithyl AmE）对动物的毒性低于两性霉素B（AmB），并且可以达到比等量AmB更高四倍的血清峰值水平。然而，N-D-鸟氨酰两性霉素B甲酯的体外活性仅为两性霉素B的四分之一，体内活性则为两性霉素B的五分之一至八分之一。N-D-鸟氨酰两性霉素B甲酯和相应的赖氨酰衍生物也缺乏两性霉素B的免疫佐剂作用。
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