1.Effects of irbesartan and perindopril on pressure overload-induced cardiac hypertrophy in rats
Qingjun JIANG ; Geng XU ; Youfa ZHU
Chinese Journal of Pathophysiology 1989;0(05):-
AIM: To observe the effects of irbesartan and perindopril on pressure-overload cardiac hypertrophy in rats. METHODS: 40 male adult Sprague Dawley rats were divided into 5 groups. One was sham operation group, other four were aortic banding groups. One week after operation, all rats were gavaged with normal saline, perindopril, irbesartan or combination of perindopril and irbesartan. Morphometric determination, calcineurin (CaN) expression, CaN and sarcoplasmic reticulum (SR) Ca 2+-ATPase activity were performed at the end of 6 weeks of drug intervention. RESULTS: Left ventricular mass index (LVMI), transverse diameter of myocardical cell (TDM), CaN activity were remarkably decreased after drug intervention and this decrease was most remarkable in the combination group. SR Ca 2+-ATPase activity increased after drug intervention, especially in the combination group. CaN expression in myocardium were remarkably decreased after drug intervention. LVMI was positively correlated with TDM and CaN, negatively correlated with SR Ca 2+-ATPase. CONCLUSION: Both irbesartan and perindopril decrease CaN activity, increase SR Ca 2+-ATPase activity and combination of them has synergic effects on regressing of ventricular hypertrophy.
2.Preliminary Application of Magnetic Resonance/Digital Subtraction Angiography 3D Fusion Imaging
Yijie CHANG ; Zhiquan TANG ; Hongwei XU ; Youfa YUAN ; Ying HAN
Chinese Medical Equipment Journal 2003;0(10):-
Objective To evaluate the clinical application value of MR/DSA- 3D fusion software. Method Fusion imaging was made with fusion software after performing MR and DSA examinations on nine cerebrovascular diseases sufferers. Results The fusion image of six sufferers could display the exact part having pathological changes to cerebral vessel and specify the relationship between the tissue of pathological changes and cerebral vessel, offering a scientific basis for clinics and the fusion images of three sufferers were not ideal. Conclusion MRDSA-3D fusion software can provide image with high diagnostic accuracy and treatment precision.
3.Synthesis and druggability study of triptolide stearate
Zhiqin FU ; Youfa XU ; Bingchen CHEN ; Dan CHENG ; Juanjuan MA ; Jianming CHEN
Journal of Pharmaceutical Practice 2017;35(2):141-145
Objective To synthesize a lipophilic prodrug of triptolide (TP) and improve its druggability .Methods Trip-tolidestearate (TP-SA)was synthesized via the DMAP-catalyzed DCC method and identified by MS ,1H-NMR and 13C-NMR. The shake-flask method was used to study the oil/water partition coefficient .The preparations of TP and TP-SA liposomes and emulsions were compared .Their encapsulation efficiency and stability were investigated .Results TP-SA was synthesized suc-cessfully .Its log P in octanol/water system was 2 .33 .It was difficult to prepare TP liposome or emulsion .By contrast ,TP-SA liposome and emulsion can be prepared successfully with the same formulation process .The particle size of TP-SA lipo-somes were about 90 nm and TP-SA emulsions were about 110 nm .The encapsulation efficiency was above 95% .Their stabili-ty were studied at 4℃ and 25℃ .The preparation parameters ,such as particle size and encapsulation efficiency ,had no signif-icant change in a week .Conclusion Triptolide stearate enhanced drug lipophilicity .Its druggability was improved significant-ly .These data can be used for the TP related drug design and development .
4.Research progress on tumor-targeting paclitaxel prodrugs
Dan CHENG ; Youfa XU ; Zhiqin FU ; Jianming CHEN
Journal of Pharmaceutical Practice 2018;36(1):1-8
Paclitaxel is a natural compound with efficient broad-spectrum antitumor activity .However ,the clinical ap-plication has been limited owing to the undesirable drawbacks ,such as the poor water-solubility ,cardiovascular toxicity and neurotoxicity .The design of paclitaxel prodrugs is an effective measure which can improve the drug's druggability ,alleviate its toxicity adverse effect and enhance its antitumor effect .With the in-depth research of prodrugs ,tumor-targeting paclitaxel pro-drugs which using the excessive receptors ,specific enzymes ,transporters ,reactive oxide species ,glutathione in tumor tissues as well as acidosis and hypoxia in tumors as specific targets ,have made great progress .The relevant literature about paclitaxel prodrugs were reviewed in this paper ,which targeted to the specific pathological and physiological features of tumor microenvi-ronment in recent years.