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布比卡因和左旋布比卡因在果蝇翅斑试验中的遗传毒性评估。

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

作者信息

Gürbüzel Mehmet, Karaca Ugur, Karayilan Nermin

机构信息

Department of Biology, Faculty of Arts and Sciences, Erzincan University, 24100, Erzincan, Turkey.

出版信息

Cytotechnology. 2016 Aug;68(4):979-86. doi: 10.1007/s10616-015-9852-2. Epub 2015 Feb 19.

DOI:10.1007/s10616-015-9852-2
PMID:25693764
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4960147/
Abstract

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 Drosophila melanogaster. 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.

摘要

布比卡因和左旋布比卡因是医学实践中常用的氨基酰胺类局部麻醉药。虽然布比卡因由S(-)-布比卡因和R(+)-布比卡因对映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。已知左旋布比卡因比布比卡因更可取,因为它可能导致心血管和神经系统毒性。为了确定这些麻醉药的遗传毒性,我们在黑腹果蝇中使用了翅体细胞突变和重组试验。用布比卡因和左旋布比卡因处理3日龄的反式杂合幼虫。标准杂交分析表明,在幼虫阶段达到毒性剂量之前,布比卡因和左旋布比卡因均未表现出诱变或重组活性。当我们在HB杂交中检测布比卡因和左旋布比卡因时,布比卡因在高浓度(500μg/mL)下未表现出任何遗传毒性,但左旋布比卡因在高浓度(1000μg/mL)下确实表现出遗传毒性——这取决于显著的重组效应。

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