ABSTRACT
OBJECTIVE：To study spectrum-effect relationship of 11 different solvent extracts from Trollius chinensis against hypoxia/reoxygenation injury of cardiomyocyte . METHODS ：HPLC-MS/MS method was used to establish the fingerprints of 11 different solvent extracts from T. chinensis ，the compounds corresponding to the common peaks were identified by comparing with the substance control and literature information. MTT assay was used to detect the effects of 11 different solvent extracts from T. chinensis on the survival rate of rat myocardial H 9c2 cells injured by hypoxia/reoxygenation. The MDA content ，ROS level in cells and LDH content in the supernatant were detected by ELISA. GRA and PLS method were used to analyze the spectrum-effect relationship between the compounds corresponding to common peak and anti-hypoxia/reoxygenation injury of cardiomyocyte （drug effect）. RESULTS ：There were 22 common peaks in 11 different solvent extracts from T. chinensis ，and 22 compounds were identified. Compared with hypoxia/reoxygenation injury group ，survival rate of hypoxia/reoxygenation injury+S 1-S6，S9 and S 10 groups were increased significantly ，while MDA content ，ROS level and LDH content were decreased significantly （P＜0.05）； ROS level and LDH content of hypoxia/reoxygenation injury+S 8 group w ere decreased significantly （P＜0.05）. The r of GRA analysis of 22 compounds with drug effects were all higher than 0.8. Except for peaks 1，2，7，13，14 and 21，r of PLS analysis of rest peaks with drug effects were higher than 0 发。电话：0431-86058683。E-mial：nml2000@163.com （being positive correlation ）. Top 9 common peaks in the list of contribution rate were peak 6＞11＞4＞5＞8＞9＞12＞10＞15. CONCLUSIONS ：Orientin（peak 6），vitexin（peak 11）， orientin-2″-O-β-L-galacto- pyranosl （peak 4），orientin-2″-O-β-D-Pyrine xylosides （peak 5），quercetin-3-O-glucopyranoside（peak 8），vitexin-2″-O-β-L-galactoside（peak 9），hyperoside（peak 12），vitexin-2″-O-β-D-pyrine xylosides （peak 10），2″-O-（2″′- methylbutyry-loxy）-orientin（peak 15）may be the main components of anti-hypoxia/reoxygenation injury of cardiomyocytes.
ABSTRACT
OBJECTIVE： To synthesize and identify rotundic acid esters derivatives， and to evaluate in vitro antitumor activity. METHODS： Using rotundic acid as raw material， rotundic acid esters derivatives were synthesized by 28-esterification， 3β and 23-position hydroxyl group combined with acid anhydride. The structure of rotundic acid esters derivatives were identified by HRMS， 1H-NMR， 13C-NMR and physicochemical properties. The in vitro antitumor activities were evaluated by MTT assay against paclitaxel （positive control）， rotundic acid and rotundic acid esters derivatives with human cervical cancer cells HeLa， human malignant melanoma cells A375， human lung adenocarcinoma cells SPC-A1 and human liver cancer cells HepG2 （take IC50 as an indicator）. RESULTS： Totally 6 kinds of rotundic acid esters derivatives were synthesized， i.e. rotundic acid methyl ester（compound 1）， 3， 23-O-di（acetyl） rotundic acid methyl ester（compound 2）， 3， 23-O-di（propionyl） rotundic acid methyl ester（compound 3）， 3， 23-O-di（butyryl） rotundic acid methyl ester（compound 4）， 3， 23-O-di（phthaloyl） rotundic acid methyl ester（compound 5） and 3， 23-O-di（succinyl） rotundic acid methyl ester（compound 6）. Compared with paclitaxel， the antitumor activity of compound 5 and compound 6 to Hela， A375， HepG2 and SPC-A1 was similar to it， and there was no significant difference between them （P＞0.05）； the IC50 of rotuntic acid and other compounds decreased with statistical significance （P＜0.05）. CONCLUSIONS： In the study， 6 kinds of rotundic acid esters derivatives are synthesized and compound 5 and compound 6 have significant antitumor activity in vitro， which can provide reference for further study.
ABSTRACT
A target molecule affinity-ultrafiltration liquid chromatography-electrospray ionization tandem mass spectrometric (LC-ESI-MSn) method was established for rapid screening acetylcholinesterase (AChE) inhibitors from total alkaloids of fibraurea recisa Pierre.A total of 12 potential inhibitors were screened from Fibraurea recisa Pierre.and 6 compounds were identified including palmatine,berberine,jatrorrhizine,palmatrubine,7,8-dihydro-8-hydroxyberberine and groenlandicine.The AChE inhibitory activity of these 6 compounds was validated in vitro.Palmatine showed the strongest inhibitory activity for AChE,which was stronger than that of donepezil hydrochloride,demonstrating the potential of palmatine as anti-Alzheimer's drug.This method is simple,rapid,and accurate for directly screening active ingredients which can inhibit AChE from complex extract of traditional Chinese medicines.