Studies On The Active Compounds And Quality Control Of Hedyotis Uncinella Hook. Et Arn.

Hedyotis uncinella Hook.et Arn.,commonly known as“Dui Zuo Ye”in traditional Chinese medicine,is mainly scattered in Hainan,Guangdong,Hunan,Guizhou and Yunnan Provinces in mainland China.The whole plant is widely used in Guizhou Province for the treatment of cancer,rheumatism,dysentery,diarrhea,snakebites and hepatitis.Furthermore,there is a pharmaceutical tablet made of H.uncinella extraction named“Jie Du Zhi Xie Pian”in the market to treat diarrhea and abdomen pain.In order to figure out the bioactive compounds and establish a quality control method of this remedy,a phytochemical study on the whole plants of H.uncinella has been implemented.The dichloromethane-extract?100 g?and EtOAc-extract?70 g?were subjected to silica gel column?mesh 200–300?,MCI gel,Sephadex LH-20,HPLC and prep-HPLC,resulting in 41 compounds.Their structures were identified on the basis of the ¹H-NMR,¹³C-NMR,2D-NMR and ESI-MS spectra.41 compounds were identified as 10 lignans,12 aromatic compounds,4 coumarins,3 triterpenes and sterides,and 12other compounds.Except compounds DZY-27^DZY-29,all of the compounds were isolated from H.uncinella for the first time.This study examined the effects of 37 compounds on TNF-?mediated NF-?B activity in the human cervical carcinoma cell line HeLa.Results showed that DZY-9??7R,8S?-balanophonin?,DZY-27?ursolic acid?and DZY-28?oleanolic acid?dose-dependently inhibited TNF-?mediated NF-?B activation.MTT results showed that inhibition of NF-?B activation of these 3 compounds was not caused by toxicity.This study choosed Riemerella anatipestifer CI1410,Staphylococcus aureus CI0809,Streptococcus suis CI1407,Escherichia coli CI1401,Pseudomonas aeruginosa CI1011,Aeromonas hydrophila CI1004,Salmonella gallinarum CI0812,Streptococcus agalactiae CI1302,Vibrio Parahemolyticus CI1456,Staphylococcus epidermidis CI1112 and Enterococcus faecalis CI1102 to examine antimicrobial activities of 37compounds.The positive control was ciprofloxacin,using the broth dilution method.Experiments results showed that DZY-19 had obvious antimicrobial activity on A.hydrophila CI100 and DZY-33 had obvious antimicrobial activity on R.anatipestifer CI1410.Ursolic acid and oleanolic acid were chosen as the index compounds of this remedy.Content of ursolic acid and oleanolic acid in this remedy,along with methodological study,was detected by HPLC.Results of methodological study demonstrated that content determination method was satisfactory.A simple,reliable and precious quality control method was successfully established based on the results.