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Genotoxic evaluation of bupivacaine and levobupivacaine in the Drosophila wing spot test

机译:果蝇翅斑试验中布比卡因和左旋布比卡因的遗传毒性评价

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摘要

Bupivacaine and levobupivacaine are amino amide local anesthetics commonly used in medical practice. Although bupivacaine consists of a racemic mixture of S (–)-bupivacaine and R (+)-bupivacaine enantiomers, levobupivacaine is comprised of pure S (–)-bupivacaine. It has been known that levobupivacaine is preferable to bupivacaine since it may cause cardiovascular and nervous system toxicity. For determining genotoxicity of these anesthetics, we used the wing somatic mutation and recombination test in Drosophilamelanogaster. Three-day-old trans-heterozygous larvae were treated with bupivacaine and levobupivacaine. Analysis of the standard crosses indicated that bupivacaine and levobupivacaine did not exhibit mutagenic or recombinogenic activity until toxic doses have been reached at the larval stage. When we examined bupivacaine and levobupivacaine in the HB cross, bupivacaine did not exhibit any genotoxicity at high concentrations (500 µg/mL), but levobupivacaine did exert genotoxicity at high concentrations (1000 µg/mL)—depending on the substantial recombinogenic effect.
机译:布比卡因和左旋布比卡因是医学实践中常用的氨基酰胺局部麻醉剂。尽管布比卡因由S(-)-布比卡因和R(+)-布比卡因对映异构体的外消旋混合物组成,但左旋布比卡因由纯S(-)-布比卡因组成。已知左布比卡因比布比卡因更可取,因为它可能引起心血管和神经系统毒性。为了确定这些麻醉剂的遗传毒性,我们在果蝇中使用了机翼的体细胞突变和重组试验。用布比卡因和左旋布比卡因处理三天大的反式杂合子幼虫。对标准杂交的分析表明,在幼虫期达到毒性剂量之前,布比卡因和左旋布比卡因不具有诱变或重组活性。当我们检查HB杂交中的布比卡因和左旋布比卡因时,布比卡因在高浓度(500μg/ mL)时没有表现出任何遗传毒性,而左旋布比卡因在高浓度(1000μg/ mL)时却表现出遗传毒性-取决于实质的重组作用。

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