title: Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives.
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.
authors.affiliation: College of Chemistry and Materials Engineering, Huaihua University, Huaihua 418000, Hunan, China. 2266@hhtc.edu.cn.
authors.forename: Zi-Jian
authors.initials: ZJ
authors.lastname: Zhao
authors.affiliation: Huaihua No. 3 High School, Huaihua 418000, Hunan, China. zjzhao72@163.com.
authors.forename: Chang
authors.initials: C
authors.lastname: Zhao
authors.affiliation: College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, Hunan, China. xiaojing@hnu.edu.cn.
authors.forename: Jing
authors.initials: J
authors.lastname: Xiao
authors.affiliation: College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, Hunan, China. wjc08071211@163.com.
authors.forename: Jian-Cheng
authors.initials: JC
authors.lastname: Wang
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism / Q000494:pharmacology*; D002470:Cell Survival; D016207:Cytokines / Q000235:genetics / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D015870:Gene Expression / Q000187:drug effects; D008070:Lipopolysaccharides / Q000494:pharmacology; D008297:Male; D051379:Mice; D009019:Morphinans / Q000378:metabolism / Q000494:pharmacology*; D010539:Permeability; D000067996:RAW 264.7 Cells; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000276:immunology / Q000378:metabolism*
chemical_list: D000893:Anti-Inflammatory Agents; D016207:Cytokines; D008070:Lipopolysaccharides; D009019:Morphinans; C009271:sinomenine
keywords: anti-inflammatory; sinomenine-derivative; transdermal permeation