1.A Method for Evaluation of Non-similarity Degrees between Splitting Fractions of Atractylodis Macrocephalae Rhizoma
Linghui LI ; Xiaoku RAN ; Yubin XU ; Deqiang DOU
Chinese Journal of Analytical Chemistry 2014;(3):343-348
Five fractions were split for the chemical components of Atractylodis macrocephalae rhizome by the combination application of various separation methods and the over 90% similarity of HPLC fringerprints within each fractions indicated the good repeatability for the splitting procedure. Further, a term of nonsimilarity degree ( NSD) was introduced to measure the unoverlapping property of the chemical fractions and different statistic analyses, including principal component analysis, cluster analysis, angle cosin analysis, squared euclidean distance and the NSD of peak areas of crude drug were used to qualitatively and quantitatively analyze their unoverlapping property, revealing the NSD among different fractions was calculated above 85%. Among them, the NSD of peak area of crude drug established on the basis of HPLC fingerprints of crude drug is more suitable for the NSD evaluation of chemical splitting fractions of crude drug comparing with other statistical methods and practical for reflecting the real content-activity relationship in the subsequent exploration of effective substances of crude drugs. This research provides a new effective method to evaluate the chemical difference of splitting fractions of Chinese medicine and lay the foundation for exploring the effective and property-flavor substances or of Atractylodes macrocephala Koidz.
2.Effect of lansoprazole on gastric ulceration in rats
Hua XU ; Liping YU ; Jie WEN ; Wen ZHAO ; Yadong HUANG ; Xiaoku LI
Chinese Journal of Pathophysiology 1989;0(06):-
AIM:To investigate the effect of lansoprazole on gastric ulceration in rats. METHODS:Using the gastric ulcer model induced by hemorrhagic shock, restraint water-immersion stress and pylorus-ligature, the protective effect of lansoprazole (iv) on gastric ulceration was observed. RESULTS: Pretreatment with lansoprazole (7.5-60 mg/kg) significantly inhibited the formation of gastric ulcer in the three models in a dose-dependent manner. The autiulcer efficacy of lansoprazole was similar to that of omeprazole in the equal dose, but stronger than that of omeprazole for ulcer induced by water-immersion stress. CONCLUSION: The intravenously administered lansoprazole inhibited formation of experimental gastric ulcer in rats.
3.Synthesis of ferulic acid derivatives and their inhibition of cholinesterase inhibitory activity
Li GUAN ; Xuchao SONG ; Xiaoku WANG ; Ning ZHAO ; Weize LI ; Yang WANG
Journal of China Pharmaceutical University 2022;53(4):433-440
Ferulic acid (FA), a natural product of phenylpropanoids containing phenolic hydroxyl groups, has a wide range of pharmacological activities and some therapeutic effect on Alzheimer's disease (AD).Using FA as the raw material, the ferulic acid carbamate aniline derivatives were first synthesized by 4-step esterification reaction, splicing carbamate active functional groups, hydrolysis reaction and amide condensation.These FA derivatives were evaluated for in vitro cholinesterase inhibition activity by the Ellman method.A total of 15 novel FA derivatives were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and ESI-MS.Cholinesterase activity tests showed that compounds 5c, 5f, 5j, 5g, 5m possessed good acetylcholinesterase inhibition activity.Except for 5l, 5m, almost all compounds have inhibition activity on butyrylcholinesterase, which is much higher than that on acetylcholinesterase.In conclusion, compounds 5c, 5f, 5j and 5g can be used as potential anti-AD inhibitors targeting cholinesterase..