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罗哌卡因和利多卡因抑制未转化的培养成人人类成纤维细胞、内皮细胞和角质形成细胞的增殖。

Ropivacaine and lidocaine inhibit proliferation of non-transformed cultured adult human fibroblasts, endothelial cells and keratinocytes.

作者信息

Martinsson T, Haegerstrand A, Dalsgaard C J

机构信息

Astra Pain Control, Preclinical Research & Development, Södertälje, Sweden.

出版信息

Agents Actions. 1993 Sep;40(1-2):78-85. doi: 10.1007/BF01976755.

Abstract

Local anaesthetics are known to affect a variety of cell functions, many of which are involved in the inflammatory response. Local anaesthetics have also been shown to influence cell proliferation. The aim of this study was to examine the effect of two local anaesthetics (ropivacaine and lidocaine) on cell proliferation of cultured human fibroblasts, vascular endothelial cells and epithelial cells, i.e. keratinocytes, as earlier studies have not included primary human cell types. Significant inhibition of fibroblast proliferation was observed with concentrations of 50 microM ropivacaine or 100 microM lidocaine in 1% newborn calf serum and 500 microM ropivacaine or lidocaine in 10% newborn calf serum. The proliferation of endothelial cells was significantly inhibited by 1 mM ropivacaine in 5% human serum and 500 microM ropivacaine or 100 microM lidocaine in 40% human serum. Significant inhibition was not obtained with lidocaine when these cells were cultured in 5% HS. Significant inhibition of keratinocytes was obtained with 100 microM ropivacaine and 500 microM lidocaine. The effective concentrations are within the range of therapeutical concentrations in vivo and there seems to be a general correlation between the local anaesthetic potency and the inhibiting effect on cell proliferation. This suggest a mechanism by which local anaesthetics may exhibit anti-hyperproliferative effects in clinical situations.

摘要

已知局部麻醉药会影响多种细胞功能,其中许多功能都参与炎症反应。局部麻醉药也已被证明会影响细胞增殖。本研究的目的是检验两种局部麻醉药(罗哌卡因和利多卡因)对培养的人成纤维细胞、血管内皮细胞和上皮细胞(即角质形成细胞)增殖的影响,因为早期研究未纳入原代人细胞类型。在含1%新生小牛血清的培养基中,50微摩尔/升的罗哌卡因或100微摩尔/升的利多卡因,以及在含10%新生小牛血清的培养基中,500微摩尔/升的罗哌卡因或利多卡因,均可观察到对成纤维细胞增殖的显著抑制。在含5%人血清的培养基中,1毫摩尔/升的罗哌卡因,以及在含40%人血清的培养基中,500微摩尔/升的罗哌卡因或100微摩尔/升的利多卡因,均可显著抑制内皮细胞的增殖。当这些细胞在含5%人血清的培养基中培养时,利多卡因未产生显著抑制作用。100微摩尔/升的罗哌卡因和500微摩尔/升的利多卡因可显著抑制角质形成细胞的增殖。有效浓度在体内治疗浓度范围内,并且局部麻醉药的效力与对细胞增殖的抑制作用之间似乎存在普遍关联。这提示了一种机制,通过该机制局部麻醉药在临床情况下可能表现出抗增殖作用。

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