Anthracycline antibiotic pharmacology and metabolism.
Anthracycline antibiotic pharmacology and metabolism.
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蒽环类抗生素药理学和代谢。
DOI：
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发表时间：
1979
期刊：
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通讯作者：
N. Bachur
中科院分区：
文献类型：
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作者：
N. Bachur
蒽环类抗生素显示出与细胞组分的许多相互作用和参与几种代谢途径的证据。抗生素分子中的小的结构变化可以在细胞内定位和相互作用中产生大的变化。迄今为止，我们发现所有的蒽环类抗生素通过微粒体和核电子传递机制的催化作用形成自由基中间体。NADPH细胞色素P-450还原酶催化自由基的形成。自由基中间体（“位点特异性自由基”）可能导致毒性和药物作用。自由基中间体非酶降解为7-脱氧苷元代谢物，这证明了体内自由基的存在。
The anthracycline antibiotics show evidence of numerous interactions with cellular components and participation in several metabolic pathways. Small structural changes in the antibiotic molecule can produce major changes in intracellular localization and interaction. To date, we find that all of the anthracycline antibiotics form free radical intermediates through the catalysis of microsomal and nuclear electron-transport machinery. NADPH cytochrome P-450 reductase catalyzes the free radical formation. The free radical intermediates ("site-specific free radicals") may be causative of both toxicity and pharmaceutic action. The free radical intermediates degrade nonenzymatically to 7-deoxyaglycone metabolites which prove the existence of the free radical in vivo.