Anti-fatigue activity screening of novel positive allosteric modulators on AMPA receptor / 中国药理学通报

Aim To explore the novel anti-fatigue a-gents targeting AMPA receptor. Methods Three ben-zoic acids of different methoxy substitutions were em-ployed, including piperonylic acid, 3,4,5-trimethoxy benzoic acid and 3,4-dimethoxy benzoic acid, which as mother nucleus and cyclic aliphatic amine or pheny-lpiperazine derivatives were introduced to modify the nitrogen atoms connecting to amino bonds. Forty-three compounds were synthesized and identified by 1 H-NMR. MTT assay, then pentobarbital induced hypno-sis experiment and mice burden swimming experiment were applied respectively to evaluate the new synthesized compounds’ cytotoxicity, CNS excitability and anti-fatigue activity. Results Compound 2j had low cytotoxicity,presenting certain central excitability and significant advantages on anti-fatigue. Conclusion The further development of compounds 2j with good anti-fatigue activities could be cultivated in further study.

Screening of Gongshisong's Active Sites for Anti-sports Fatigue / 中国药房

OBJECTIVE:To screen Gongshisong's active sites for anti-sports fatigue. METHODS:Gongshisong extract was prepared with 80% ethanol extraction technology,and extracted with petroleum ether,chloroform,ethyl acetate and n-butyl alco-hol after dispersed with water to obtain the extract. 70 mice were randomly divided into blank control group(1% sodium carboxy-methylcellulose,CMC-Na),positive control group [Rhodiola wallichiana capsules,590 mg/(kg·d)],petroleum ether,chloro-form,ethyl acetate and n-butyl alcohol extracts and aqueous layer of Gongshisong groups(TS,TL,TY,TZ,TW groups). Gong-shisong extracts groups was given relevant medicine 2.5 g(crude drug)/(kg·d),ig,for consecutive 7 days. Exhaustion time of bur-den swimming test was detected. 70 mice were grouped according to above method,and the contents of liver glycogen,muscle gly-cogen and the coefficient of liver were tested in mice. 80 mice were grouped according to above method,and model group was es-tablished additionally(1% CMC-Na). The contents of lactic acid(LA),creatine kinase(CK)and urea nitrogen(BUN)in serum of mice were determined after 90 minutes of unburden swimming. RESULTS:Compared with blank control group,exhaustion time of burden swimming mice in TS,TY and TZ groups prolonged;the content of liver glycogen increased in TY,TZ and TW groups;the content of muscle glycogen increased in TS and TW groups;the contents of BUN,LA and CK in mice increased in model group (P<0.05 or P<0.01). Compared with model group,the serum content of BUN in mice decreased in TS and TY groups;that of LA in mice decreased in TZ and TW groups;that of CK in mice decreased in TS group (P<0.05 or P<0.01). CONCLUSIONS:The petroleum ether and n-butanol extract site and water layer of Gongshisong are good anti-fatigue active sites.