title: A Novel Brucine Gel Transdermal Delivery System Designed for Anti-Inflammatory and Analgesic Activities.
abstract: The seeds ofStrychnosnux-vomicaL., as a traditional Chinese medicine, have good anti-inflammatory and analgesic activities. However, it usually leads to gastrointestinal irritation and systemic toxicity via oral administration. In the study, it was discovered that a novel gel transdermal delivery system contained brucine, the main effective component extracted fromStrychnosnux-vomica. Results showed that the brucine gel system inhibited arthritis symptoms and the proliferation of the synoviocytes in the rat adjuvant arthritis model, which indicated its curative effect for rheumatoid arthritis. Meanwhile, it significantly relieved the xylene-induced ear edema in the mouse ear swelling test, which manifested its anti-inflammatory property. Moreover, the brucine gel eased the pain of paw formalin injection in the formalin test, which demonstrated its analgesic effects. In addition, the brucine significantly inhibited lipopolysaccharide (LPS)-induced Prostaglandin E2 (PGE2) production without affecting the viability of cell in vitro anti-inflammatory test, which proved that its anti-inflammatory and analgesic actions were related to inhibition of prostaglandin synthesis. It is suggested that the brucine gel is a promising vehicle for transdermal delivery on the treatment of inflammatory disease.
authors.affiliation: School of Chemistry, Xiangtan University, Xiangtan 411105, China. pingwu@xtu.edu.cn.|Hunan Province Engineering Research Center of Bioactive Substance Discovery of Chinese Medicine, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China. pingwu@xtu.edu.cn.|Key Lab of Environment-Friendly Chemistry and Application in Ministry of Education, Xiangtan University, Xiangtan 411105, China. pingwu@xtu.edu.cn.
authors.forename: Ping
authors.initials: P
authors.lastname: Wu
authors.affiliation: School of Chemistry, Xiangtan University, Xiangtan 411105, China. liangqin@hotmail.com.
authors.forename: Qin
authors.initials: Q
authors.lastname: Liang
authors.affiliation: State Key Laboratory of High Performance Complex Manufacturing, Central South University, Changsha 410083, China. fengpei@csu.edu.cn.
authors.forename: Pei
authors.initials: P
authors.lastname: Feng
authors.affiliation: School of Chemistry, Xiangtan University, Xiangtan 411105, China. lichunyan@xtu.edu.cn.|Key Lab of Environment-Friendly Chemistry and Application in Ministry of Education, Xiangtan University, Xiangtan 411105, China. lichunyan@xtu.edu.cn.
authors.forename: Chunyan
authors.initials: C
authors.lastname: Li
authors.affiliation: School of Chemistry, Xiangtan University, Xiangtan 411105, China. yangchunguang2016@hotmail.com.|Key Lab of Environment-Friendly Chemistry and Application in Ministry of Education, Xiangtan University, Xiangtan 411105, China. yangchunguang2016@hotmail.com.
authors.forename: Chunguang
authors.initials: C
authors.lastname: Yang
authors.affiliation: Joint Surgery Department of the Second People's Hospital of Nanning City, Guangxi Zhuang Autonomous Region, Nanning 530021, China. lianghongsuo@hotmail.com.
authors.forename: Hongsuo
authors.initials: H
authors.lastname: Liang
authors.affiliation: School of Chemistry, Xiangtan University, Xiangtan 411105, China. tanghuaibo@hotmail.com.|Key Lab of Environment-Friendly Chemistry and Application in Ministry of Education, Xiangtan University, Xiangtan 411105, China. tanghuaibo@hotmail.com.
authors.forename: Huaibo
authors.initials: H
authors.lastname: Tang
authors.affiliation: State Key Laboratory of High Performance Complex Manufacturing, Central South University, Changsha 410083, China. tanghuaibo@hotmail.com.
authors.forename: Cijun
authors.initials: C
authors.lastname: Shuai
mesh_terms: D000279:Administration, Cutaneous; D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001169:Arthritis, Experimental / Q000473:pathology; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D015232:Dinoprostone / Q000096:biosynthesis; D004195:Disease Models, Animal; D016503:Drug Delivery Systems / Q000379:methods; D004487:Edema / Q000517:prevention & control; D005557:Formaldehyde; D005782:Gels; D006801:Humans; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D008517:Phytotherapy; D017208:Rats, Wistar; D013331:Strychnine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D031461:Strychnos nux-vomica / Q000737:chemistry; D000070918:Synoviocytes / Q000187:drug effects / Q000473:pathology
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D005782:Gels; D005557:Formaldehyde; C083806:brucine; D013331:Strychnine; D015232:Dinoprostone
keywords: analgesic activities; anti-inflammatory; brucine gel; transdermal delivery