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Antinociceptive curcuminoid, KMS4034, effects on inflammatory and neuropathic pain likely via modulating TRPV1 in mice

Authors
Lee, J. Y.Shin, T. J.Choi, J. M.Seo, K. S.Kim, H. J.Yoon, T. G.Lee, Y. S.Han, H.Chung, H. J.Oh, Y.Jung, S. J.Shin, K. J.
Issue Date
10월-2013
Publisher
ELSEVIER SCI LTD
Keywords
calcitonin gene-related peptide, curcuminoid synthesis, pain; inflammatory; neuropathic, TRPV1 receptor; nociceptive
Citation
BRITISH JOURNAL OF ANAESTHESIA, v.111, no.4, pp.667 - 672
Indexed
SCIE
SCOPUS
Journal Title
BRITISH JOURNAL OF ANAESTHESIA
Volume
111
Number
4
Start Page
667
End Page
672
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/102029
DOI
10.1093/bja/aet176
ISSN
0007-0912
Abstract
Background. 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. Methods. 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. Results. I-CAP, (P<0.01) and I-heat (P<0.05) of TRPV1 were significantly blocked by 10 mu M 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). Conclusions. KMS4034 may be an effective analgesic for various pain conditions.
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