Abstract
The seeds of Strychnos nux-vomica L., 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 from Strychnos nux-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.
Highlights
Strychnos nux-vomica, a seed of Strychnos nux-vomica L. (Loganiaceae), can effectively ease pain and diminish inflammation
Cytotoxic effect of brucine was evaluated, and it did not affect the cell viability at all concentrations used (0.058–0.46 mg/L). These findings indicate that brucine could suppress Prostaglandin E2 (PGE2) production in LPS-stimulated RAW264.7 cell line
Dulbecco’s modified Eagle’s medium (DMEM) and dimethyl sulfoxide (DMSO) were purchased from Hyclone (Logan, UT, USA), 5% Formalin physiological saline solution was purchased from Xilong Scientific Co., Ltd. (Guangzhou, China), Yunnan Baiyao powder was purchased from Yunnan Baiyao Co., Ltd. (Kunming, China), Prostaglandin E2 (PGE2) ELISA Kit was purchased from Cusabio Biotech Co., Ltd. (Wuhan, China)
Summary
Strychnos nux-vomica, a seed of Strychnos nux-vomica L. (Loganiaceae), can effectively ease pain and diminish inflammation. (Loganiaceae), can effectively ease pain and diminish inflammation. It has been widely used in the treatment of rheumatism and related inflammatory diseases by oral administration in traditional Chinese medicine [1–5]. It is a major ingredient in many finished herbal products, including “maqian-zi-san”, “shu-feng-ding-tong-pian”, and “fei-bu-wan” [6]. It usually leads to violent convulsion, great rise of blood pressure and even lethal poisoning at too high a dosage via oral administration [7]. A novel steady and continuous administration should be designed to avoid oral toxicity. Transdermal drug delivery system is an administration method through skin absorption, which can cotnhteinraupoeutsilcyddoesaligveeirs dverruygcsloasnedtoetnhseutorexisctdeoasdaygep[l8a]s.mAanodvreulgstceaodnyceantdracotinotnin[u9o]u. Ianjotrhiesffseecntsive,eSctorymchpnoons ennutxo-vfoSmtircyachconmospnousexd-voofmmicaan[y10c–o1m2p].oSniegnntsifiocfapnltalyn,tsitihs ansoat small molecsuuliatrabwleefiogrhtrtawnsidtherm39a4l .d4e6liDveary. [M11e].anwhile, it is a kind of white crystalline powder, which can considerabBlryucdinisesoislvaeminajoerthefafnecotilvaencdomotphoenrenotrgofanStircyschonlvosenutsx-[v1o3m]i.caTh[1e0r–e1f2o].reS,igbnriuficainnetlyis, iat hparsoma ising drug wsmhiaclhl mcaonlecbuelaurswedeifgohrt twraitnhs3d9e4r.m46aDl da.eMliveearnywshyilset,eimt i.s Ianktihned sotfuwdyh,itae ncroyvsetallblinruecpinowe dgeerl,twrahnicshdermal delivecraynscyosntseimderwabalsy ddiesvsoellvoepiende.thTahneoltahnedraoptheeur toircgaalneicffseocltvsenfotsr[a1n3]t.iT-ihneflreafmorme, bartuocriyneanisda parnoamlgiseisniga were evaluadttrreaudngsbdwyerhmthicaehl adcdeajlnuivvebareynutssyaesrdttehmfroitrwistar(saAndAsedv)eemrlmoopaedlded.leTelhixvepeertyhriemrsayepsnteeutm,tit.chaIelnmeftfhoeeuctsssetfuoedrayra, nsawti-neinlolfvilanemlgmbterausttcoir(nMye aEgnSedTl ) and the foramnaallgiensitaeswt.ere evaluated by the adjuvant arthritis (AA) model experiment, the mouse ear swelling test (MEST) and the formalin test
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