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首页> 外文期刊>British journal of anaesthesia >Antinociceptive curcuminoid, KMS4034, effects on inflammatory and neuropathic pain likely via modulating TRPV1 in mice.
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Antinociceptive curcuminoid, KMS4034, effects on inflammatory and neuropathic pain likely via modulating TRPV1 in mice.

机译：抗矫直性姜黄素，KMS4034，对炎症和神经病疼痛的影响可能通过调节小鼠调节TRPV1。

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Curcumin, the active ingredient of turmeric (Curcuma longa), has a wide range of beneficial effects including anti-inflammation and analgesia. However, poor bioavailability of curcumin hinders its clinical application. To overcome this limitation, we modified the structure of curcumin and synthesized new derivatives with favourable pharmacokinetic profiles. Recently, curcumin has been shown to have an antagonizing effect on transient receptor potential vanilloid type 1 (TRPV1) ion channels. We investigated the antinociceptive activity of KMS4034 which had the most favourable pharmacokinetics among the tested curcumin derivatives.To evaluate the mechanism of the antinociceptive effects of KMS4034, capsaicin (I(CAP))- and heat (I(heat))-induced currents in TRPV1 expressing HEK293 cells were observed after the application of KMS4034. Nociceptive behavioural measurement using the hot-plate test, formalin test, and chronic constriction injury (CCI) model were evaluated in mice. Also, calcitonin gene-related peptide (CGRP) was stained immunohistochemically in the L4/5 dorsal horns in mice with neuropathic pain.I(CAP) (P<0.01) and I(heat) (P<0.05) of TRPV1 were significantly blocked by 10 μM KMS4034. Behaviourally, noticeable antinociceptive effects after 10 mg kg(-1) of KMS4034 treatment were observed in the first (P<0.05) and second phases (P<0.05) of the formalin and hot-plate tests. The mechanical threshold of CCI mice treated with 10 mg kg(-1) KMS4034 was significantly increased compared with control. Immunohistochemical CGRP expression was decreased in the lamina I-II of the lumbar dorsal horns in KMS4034-treated CCI mice compared with the control (P<0.05).KMS4034 may be an effective analgesic for various pain conditions.
机译：姜黄素，姜黄（姜黄Longa）的活性成分，具有广泛的有益效果，包括抗炎和镇痛。然而，姜黄素的生物利用度差阻碍了其临床应用。为了克服这种限制，我们将姜黄素和合成的新衍生物的结构进行了良好的药代动力学谱。最近，已经显示姜黄素对瞬时受体潜在的潜在香草型1（TRPV1）离子通道具有拮抗作用。我们研究了KMS4034的抗血巧活性，其在测试的姜黄素衍生物中具有最有利的药代动力学。可以评估KMS4034，辣椒素（I（帽））和热（I（热））诱导电流在施用KMS4034后观察到表达HEK293细胞的TRPV1。在小鼠中评估了使用热板测试，福尔马林试验和慢性收缩损伤（CCI）模型的伤害行为测量。此外，Calcitonin基因相关肽（CGRP）在具有神经病疼痛的小鼠的L4 / 5背角中染色免疫组织化学.I（帽）（P <0.01）和I（热量）（P <0.05）TRPV1显着阻止通过10μmkms4034。在福尔马林和热板测试的第一种（P <0.05）和第二阶段（P <0.05）中观察到10mg kg（-1）KMS4034处理后的行为，明显的抗血质效应。与对照相比，用10mg kg（-1）KMS4034处理的CCI小鼠的机械阈值显着增加。在KMS4034处理的CCI小鼠中，腰部背角的椎间膜I-II中的免疫组织化学CGRP表达减少（P <0.05）.kms4034可以是各种疼痛条件的有效镇痛。

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