Building a database of TRPA1 agonists derived from traditional Chinese medicine and elucidation of its pharmacological mechanism
| Project/Area Number |
15K21538
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Natural medicines
Pain science
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| Research Institution | Hyogo University of Health Sciences |
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Principal Investigator |
Wang Shenglan 兵庫医療大学, 薬学部, 助教 (50714359)
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
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| Keywords | TRPA1 / 漢方薬 / 疼痛 |
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| Outline of Final Research Achievements |
Using flexstation calcium assay, we screened 27 natural compounds derived from traditional Chinese medicines. Four compounds were identified to activate TRPA1 channel with the higher EC50 values and lower responses. The agonistic effects of these compounds on TRPA1 could be inhibited by HC030031, a selective TRPA1 antagonist, in TRPA1 expressing human X cells and dorsal root ganglion (DRG) neurons. Further studies showed that these compounds induced the desensitization of TRPA1 channel and the analgesic effects on rat pain models. In addition, we identified two compounds (evodiamine and rutaecarpine) which activated TRPV1 channel. Evodiamine partially activated TRPV1 and inhibited TRPV1 activation through competitive partial antagonism and channel desensitization.
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Report
(3 results)
Research Products
(4 results)
