ABSTRACT
OBJECTIVE： To design and synthesize N-aroyl substituted indoline-3-acetic acid derivatives and evaluate their in vitro hypoglycemic activity. METHODS： Using indoline derivative 2-[5-（benzyloxy）-1-（4-chlorobenzoyl）-2-methyl-1H-inclol-3-yl]acetic acid （GY3） as leading compound， 4-（benzyloxy）phenyl hydrazine hydrochloride and methyl 4-oxopentanoate as raw material， 8 kinds of N-aroyl （3-hydroxybenzoyl， 3-cyanobenzoyl， 4-nitrobenzoyl， 4-methylsulfonylbenzoyl， 4-acetamidobenzoyl， 3-acetylaminobenzoyl， isoniacyl and pyridine-2-formyl） substituted indoline-3-acetic acid derivatives were synthesized via 4 steps reactions： Fischer indole cyclization， reduction， amidation and hydrolyzation. The human hepatoma HepG2 cell lines were used to investigate the glucose consumption activity of the target compounds. RESULTS： Totally 8 various N-aroyl substituted indoline-3-acetic acids were synthesized and their structures were confirmed by mass spectrum（MS）， nuclear magnetic resonance 1H-NMR and 13C spectrum. Under the condition of 1.0 μmol/L， the percentage of glucose- promoting consumption of the synthesized compounds on HepG2 cells was 5.4％-9.1％. 2-[（2R， 3S）-5-benzyloxy-2-methyl-1-（4-methylsulfonyl benzoyl）-2，3-dihydro-indole-3-yl] acetic acid showed the best hypoglycemic activity. The percentage of glucose- promoting consumption was （9.1±1.81）％， which was close to that of positive control metformin [（10.58±1.68）％]， but less potent than that of leading compound GY3[（12.15±0.78）％]. CONCLUSIONS： Different electron-withdrawing substituents are introduced into N-aroyl aromatic rings of dihydroindole compounds， such as cyano， nitro， methyl sulfonyl； hypoglycemic activity decreases in varying degrees and is weaker than halogen substituents.
ABSTRACT
Objective To explore the clinical application value of blood routine examination in judgment of the activity of inflammatory bowel diseases.Methods 102 patients with inflammatory bowel disease were selected as the main research objects,60 healthy persons in the same period were selected as the control group,all of the subjects were received routine testing of blood,C-reactive protein and erythrocyte sedimentation rate,and the relationships between disease and blood routine indexes were compared.Results In UC group,the PLT,WBC RDW index levels of remission were higher than those of the control group,the differences were statistically significant(t =6.75,8.21,5.73,all P ＜0.05).In patients with UC,the HGB,HCTand MPV index levels were lower than those in the remission patients and the control group,the differences were statistically significant(t =8.12,11.03,6.72,9.35,10.23,8.71,all P ＜0.05).But the PLT index was higher than that of patients in remission,the RDW and WBC indexes were higher than those in the control group and the remission period,there were statistically significant differences (t =7.59,8.51,6.03,all P ＜ 0.05).The routine blood indexes of the relief patients of CD group had significant differences compared with the control group(t =6.17,7.29,9.01,10.35,8.27,7.69,8.01,9.91,allP ＜ 0.05),the HCT,MCV,HGB and MPV indexes were lower than those of the control group,the differences were statistically significant (t =9.01,10.35,8.27,9.9i,all P ＜ 0.05),the WBC,PLT,N and RDW indexes were higher than those of the control group,the differences were statistically significant (t =6.17,7.29,7.69,8.01,all P ＜ 0.05).In UC group,the HGB,HCT,MCV and MPV indexes were lower than those in the remission patients and the control group,there were statistically significant differences(t =8.19,6.97,7.53,9.02,all P ＜ 0.05).But the PLT,RDW,WBC and N indexes were higher than those in the remission patients and the control group,the differences were statistically significant (t =9.81,7.94,8.36,7.61,P ＜ 0.05).In the active patients of CD group,the WBC and N indexes were significantly higher than those of UC group,the differences were statistically significant (t =8.15,9.07,all P ＜ 0.05).In the remission patients of CD group,the PLT index was significandy higher than that in the remission patients of UC group,the difference was statistically significant (t =10.35,P ＜ 0.05).Conclusion Indexes of blood routine has obvious significance in activity of inflammatory bowel disease,and it is significant correlation with inflammation index,which can be used as one of the routine clinical method to determine the activity of inflammatory bowel diseases.