Study On The Chemical Constituents,Anti-bacterial And Anti-inflammatory Activities Of Stephania Longa Lour

Stephania longa Lour.,a perennial herbaceous vine plant belonging to the genus Stephania（Menispermaceae）,which is widely distributed in tropical areas of Asia and Africa.In China,it is mainly found in southern areas,including Guangdong,Guangxi,Hainan and Taiwan.As a traditional Chinese herbal medicine,it has the functions of removing fever,clearing detoxification,reducing swelling and promoting urination,along with dispelling cold and dredging venation.The results of modern pharmacological experiments showed that S.longa possessed some excellent pharmacological activities,including anti-inflammatory,analgesia and sedation.Preliminary studies of our research group have proven that the ethanol extract of S.longa had positive therapeutic effect on prostatic hyperplasia and ulcerative colitis.In order to further elucidate its pharmacodynamic material basis,this study would conduct a systematic study on chemical constituents of S.longa.Methods:The air-dried aerial part of S.longa was smashed into powder and extracted with 95%ethanol for 24 hours at room temperature,repeated three times.The total extracts were evaporated under reduced pressure to yield a extracta sicca,and the extracta sicca was separated and purified by silica gel column chromatography,ODS column chromatography,and preparative high performance liquid chromatography（HPLC）,then,the structures of the isolated compounds were identified according to their physical and chemical properties and spectral techniques such as UV,IR,1D-NMR,2D-NMR,HR-ESI-MS,ECD and so on.Finally,the anti-bacterial and anti-inflammatory activities of the isolated compounds were evaluated in vitro.Result:In this paper,19 compounds were isolated from 95%ethanol extract of S.longa by various chromatographic methods,and their structures were identified by plenty of modern spectroscopic methods.These compounds including:stephalonester A（SL-1）,stephalonester B（SL-2）,stephalonine Q（SL-3）,stephalonine R（SL-4）,and stephalonine S（SL-5）,cephatonine（SL-6）,stephalonine E（SL-7）,longanone（SL-8）,prostephabyssine（SL-9）,isolonganone（SL-10）,eletefine（SL-11）,aurantiamide（SL-12）,（2S）-3-O-Octadeca-9Z,12Z,15Z-trienoylglyceryl-O-β-D-galactopyranoside（SL-13）,N-cinnamoyltyramine（SL-14）,p-hydroxyphenethyl trans-ferulate（SL-15）,dibutyl-phthalate（SL-16）,ferulic acid（SL-17）,4-hydroxybenzaldehyde（SL-18）and（-）-Loliolide（SL-19）.Among the above compounds,compounds SL-1～SL-5 are new alkaloid compounds,compounds SL-12～SL-19 are all known compounds,but they are isolated from S.longa for the first time.The result of anti-bacterial experiment in vitro showed that compound SL-11 not only could significantly inhibited S.aureus with the IC₅₀value of 50μg/m L in 24 h,but also effectively inhibited P.aeruginosa and E.coli with the IC₅₀values of 100μg/m L and 200μg/m L in 24 h,respectively.In addition,compounds SL-6,SL-8 and SL-9 exhibited significant inhibition against TNF-αand IL-6 production of RAW 264.7macrophages stimulated by LPS in vitro,which suggested that they possessed excellent anti-inflammatory activity.Furthermore,compounds SL-6,SL-8 and SL-9 suppressed TNF-αproduction with IC₅₀values of16.44μM,19.22μM,and 15.86μM,respectively.Besides,compounds SL-6,SL-8 and SL-9 showed inhibitory effects on IL-6 production with IC₅₀values of 39.12μM,6.54μM,and 30.44μM,respectively.Conclusion:In this paper,a total of 19 compounds were isolated and identified,including 5 new alkaloid compounds SL-1～SL-5,and 8 known compounds SL-12～SL-19 which were isolated from S.longa for the first time.Among all of compounds,compound SL-11 possessed moderate anti-bacterial activity,and compounds SL-6,SL-8 and SL-9 had significant anti-inflammatory activities.