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Molecules 2016, 21(11), 1520; doi:10.3390/molecules21111520

Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives

1
College of Chemistry and Materials Engineering, Huaihua University, Huaihua 418000, Hunan, China
2
Huaihua No. 3 High School, Huaihua 418000, Hunan, China
3
College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, Hunan, China
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 29 August 2016 / Revised: 7 November 2016 / Accepted: 7 November 2016 / Published: 17 November 2016
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Abstract

Sinomenine is extracted from Sinomenii caulis (a traditional Chinese medicine), and it is used as the active ingredient in rheumatic arthritis treatments. It has been used in clinical applications for decades. However, there are some disadvantages, including low activity in transdermal permeation and a high dosage being clinically required. To overcome these defects, sinomenine was used as a primer, and structural modification was performed. In our study, eight new compounds were screened out by transdermal permeation in vitro and anti-inflammatory response in vitro and in vivo. Compound 1a exhibited the most potent transdermal permeation and anti-inflammatory activity. Based on these results, further development of this compound may be warranted. View Full-Text
Keywords: sinomenine-derivative; transdermal permeation; anti-inflammatory sinomenine-derivative; transdermal permeation; anti-inflammatory
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Zhao, Z.-J.; Zhao, C.; Xiao, J.; Wang, J.-C. Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives. Molecules 2016, 21, 1520.

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