Functional Water Foundation, 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141-0021, Japan.
Bioscience Associates, Tokyo, Japan.
J Antibiot (Tokyo). 2018 Mar;71(4):417-424. doi: 10.1038/s41429-017-0017-8. Epub 2018 Feb 5.
On the occasion of the 60th anniversary of the discovery (1957) of kanamycin (KM), a series of research achievements on KM and its semisynthetic derivative Arbekacin (ABK) are outlined. KM was first used clinically in 1958 and was appreciated for its remarkable curing effect on various bacterial infections, especially tuberculosis. ABK is a KM derivative rationally semisynthesized to overcome KM resistance due to enzymatic phosphorylation and acetylation. Since its approval in 1990 as an anti-MRSA drug, ABK has been and still is effectively used in chemotherapy because MRSA rarely develops high ABK-resistance. Research that illuminated the unique features of ABK enabling it to resist the development of resistance by MRSA are also described.
在发现卡那霉素（KM）60 周年之际（1957 年），概述了一系列关于 KM 及其半合成衍生物阿贝卡星（ABK）的研究成果。KM 于 1958 年首次在临床上使用，因其对各种细菌感染，特别是结核病的显著疗效而受到赞誉。ABK 是一种通过合理半合成的 KM 衍生物，可克服由于酶磷酸化和乙酰化引起的 KM 耐药性。自 1990 年作为抗耐甲氧西林金黄色葡萄球菌（MRSA）药物获得批准以来，ABK 一直在化疗中得到有效应用，因为 MRSA 很少产生高 ABK 耐药性。本文还描述了阐明 ABK 独特特征的研究，使其能够抵抗 MRSA 产生耐药性。
