1.Study on the Standardization of Similarity Evaluation Method of Chromatographic Fingerprints (Part Ⅱ)
Runtao TIAN ; Peishan XIE ; Yun YANG
Traditional Chinese Drug Research & Clinical Pharmacology 1993;0(02):-
Objective To study the standardization of similarity evaluation method of chromatographic fingerprints. Methods HPLC and computer simulation method were used to analyze the content variation pattern of the characteristic compounds, the construction method of standard fingerprints and the statistical meanings of similarity evaluation respectively. Results The content distribution of characteristic compounds should obey normal probability. It is recommended that content information and median algorism should be used to generate reference fingerprints. The confidence factor of similarity coefficient also should be tested. Conclusion The process of compound sampling, establishment of criteria and result test are described and standardized from statistical aspect.
2.Autophagy and myocardial ischemia/reperfusion injury
Youbin LIU ; Shusen YANG ; Ying FAN ; Runtao GAN
Chinese Journal of Pathophysiology 2009;25(12):2478-2482
Autophagy is a lysosome-dependent degradative pathway which is characterized by cytoplasmic vacuolization. However, it is not just a simple degradative pathway. Research shows that autophagy is related to many diseases, such as neurodegenerative disease, malignant tumor, ageing, pathogenic microorganism infection, myocardial ischemia/reperfusion injury and so on. Autophagy exactly exists in myocardial ischemia/reperfusion injury, and it becomes a new research hotspot. This review will focus on the occurrence and development of autophagy and its role, signal transduction and research status in myocardial ischemia/reperfusion injury.
3.Method of Radix Scutellariae proccessed with wine and its HPLC fingerprint
Yun YANG ; Weisheng FENG ; Yongju WEN ; Zhenhua ZHU ; Runtao TIAN
Chinese Traditional Patent Medicine 1992;0(05):-
AIM: To investigate the processing and HPLC fingerprint of Radix Scutellariae processed with wine,and to set up appropriate quanlity control standard. METHODS: chromatographic condition of HPLC-UV fingerprint consisted of Hypersil C_18 column(200 mm?5.0 mm,5 ?m),mixture of methanol,0.4% phosphoric acid and acetonitrile as a mobile phase in a gradient mode.Flow rate was 1.0 mL/min and detection wavelength was set at 277 nm. RESULTS: There were no evident differences among fingerprints of Radix Scutellariae that was normatively processed from the production areas. CONCLUSION: The process is feasible,and can be used to provide a basis for quanlity control of Radix Scutellariae.
4.Colon-targeted delivery system of dexamethasone-angelica sinensis polysaccharides prodrug in rats
Xinyou LIU ; Siyuan ZHOU ; Jianfeng CHENG ; Yuhua RAN ; Zenghui TENG ; Runtao YANG ; Xi YANG ; Qibing MEI
Chinese Journal of Clinical Pharmacology and Therapeutics 2002;0(05):-
AIM: To explore the transport and delivery of active drug from dexamethasone-angelica sinensis polysaccharides prodrug in the gastrointestinal tract of rats. METHODS: Dexamethasone and the prodrug were orally administered to rats at the dose of 1.96 mg?kg~ -1 (calculated by carried dexamethasone). The drugs in the plasma and contents of different parts of the rats' gastrointestinal tract were determined by high performance liquid chromatography (HPLC). RESULTS: Dexamethasone carried by the prodrug was mainly released in the contents and mucosa of cecum and colon after oral administration of the prodrug. The absorption of released dexamethasone was reduced significantly. The peak time, peak concentration and AUC were 7.2 h , 42 ?g?L~ -1 and 334 ?g?h?L~ -1 , respectively. However, free dexamethasone was found mainly in the contents and mucosa of the stomach, proximal and distal small intestine after oral administration. The peak time, peak concentration and AUC were 2.2 h, 2 120 ?g?L~ -1 and 11 875 ?g?h?L~ -1 , respectively. CONCLUSION: Dexamethasone can be specifically delivered to the cecum and colon by using dexamethasone- angelica sinensis polysaccharides prodrug. The absorption of dexamethasone was reduced significantly and the drug concentration in colon was increased significantly. The prodrug has a potential in the treatment of colitis.
5.Effect of dexamethasone Angelica sinensis polysaccharide prodrug on trinitrobenzene sulfonic acid induced ulcerative colitis in rats
Xinyou LIU ; Siyuan ZHOU ; Jianfeng CHENG ; Zenghui TENG ; Yuhua RAN ; Runtao YANG ; Xi YANG ; Qibing MEI
Chinese Journal of Clinical Pharmacology and Therapeutics 2004;0(07):-
AIM:To explore the therapeutic effect of dexamethasone Angelica sinensis polysaccharide prodrug(DEX-AP) on trinitrobenzene sulfonic acid(TNBS) induced ulcerative colitis(UC) in rats and its side effects.METHODS: The experimental UC rats were induced by clusis of the solution of TNBS in 45% alcoho1(50(mg?ml~(-1))).The UC rats were orally administrated with(0.25)(?mol?kg~(-1)?d~(-1)) DEX and(0.05),(0.25),(1.25)(?mol?kg~(-1)?d~(-1)) DEX-AP(calculated by carried DEX in DEX-AP) for 7 days,respectively.The rats were killed after the amount of peripheral blood lymphocyte was counted,then the spleen,thymus and colon were separated and weighted.After the ulcerative area of colon was calculated,the colonic myeloperoxidase(MPO) activity was determined and parts of colon were paraffin sectioned and examined under light microscope by HE stain.RESULTS: After the UC rats were administrated with different doses of DEX-AP for 7 days,the ulcerative area,the weight and the MPO activity of colon reduced significantly.The reduction of MPO activity was correlated to the dose of DEX-AP and the MPO activity with DEX-AP at the doses of(0.25),(1.25)(?mol?kg~(-1)?d~(-1)) reduced more significantly than that with DEX at the the dose of(0.25)(?mol?kg~(-1)?d~(-1)).The number of peripheral blood lymphocyte,spleen weight and thymus weight of UC rats reduced significantly at the dose of(0.25)(?mol?kg~(-1)?d~(-1)) DEX(P
6.Study of fractional flow reserve guided percutaneous coronary intervention on non-culprit moderate coronary stenosis
Guijia ZHU ; Yangyang LIU ; Yang CAO ; Lin CHEN ; Duirong SUN ; Guo DONG ; Runtao GAN ; Shusen YANG
Chinese Journal of Interventional Cardiology 2014;(10):626-631
Objective To study the feasibility of using fractional flow reserve (FFR) to guide whether to perform coronary revascularization of non-culprit moderate stenosis in patients with unstable angina and estimate their clinical prognosis. Methods This study enrolled unstable angina patients with multivessel disease. First successful stenting of the culprit artery, then the other non-culprit moderate coronary stenosis were randomized into PCI guided by angiography or guided by FFR measurements. Death from any cause, nonfatal myocardial infarction, unplanned hospitalization leading to urgent revascularization and clinical manifestations with angina were followed during the first year. Results 71 patients were included, among them 35 patiens were randomly assigned to angiography-guided PCI and 36 patients to FFR-guided PCI. In FFR-guided PCI group, FFR was successfully measured in all of non-culprit moderate coronary stenosis. In 23 stenosis, the FFR was greater than 0.80, and stents were not placed in these stenosis. In 13 stenosis with FFR<0.8, stent were inplant and FFR was raised≥0.95 after stenting. The percentage of patients who had a primary end-point event was higher in the angiography-guided PCI group than the FFR-guided PCI group (P<0.05). Neither the rate of mortelity from any cause nor the rate of non-fatal myocardial infarction had significant difference between the 2 groups. Related to the target vessels rates of nonfatal myocardial infarction (5.6%vs. 28.6%) and target lesion revascularization (5.6%vs. 31.4%) were statistically different (P<0.01 and P<0.05, respectively). Conclusions In patients with unstable angina, it is safe to use FFR values to guide decisions on the revascularization of angiographically moderate non-culprit stenosis. Routine measurement of FFR in addition to angiographic guidance, as compared with PCI guided by angiography alone, results in a significant reduction in major adverse events at 1 year, particularly in urgent revascularization, and clinical manifestations with angina get better.
7.Change of Caspase-3 and PSD-95 Expression in Hippocampus of Mice with Chronic Ketamine Addiction
Ao DU ; Peng REN ; Bolin HE ; Shuncheng YANG ; Runtao DING ; Ruipeng SHEN ; Yanning LI ; Zhibin DONG ; Yan LU ; Xu WU
Journal of China Medical University 2017;46(3):193-196
Objective To study the changes of hippocampal caspase-3 and PSD-95 expression levels in the mice exposed to ketamine 30 mg/(kg·d)for three months. Methods Forty C57BL/6 mice were randomly divided into two groups,and the chronic ketamine addiction model was established by giving mice a three month course of daily intraperitoneal injections of ketamine. Immunohistochemical study and Western blot-ting were applied to observe the expression of caspase-3 and PSD-95 protein. Results There were more expression of caspase-3 and less of PSD-95 in ketamine group as detected by immuohistochemistry. Western blotting results showed caspase-3 active fragment level significantly increased com-pared to saline group,but PSD-95 protein level was decreased. Conclusion The increased level of caspase-3 protein and reduced expression of PSD-95 are observed after long-term ketamine administration. These findings may provide an evidence for the neurotoxicity in mouse hippocampus of chronic ketamine addition as a recreational drug.
8.Discovery of novel diarylamides as orally active diuretics targeting urea transporters.
Shun ZHANG ; Yan ZHAO ; Shuyuan WANG ; Min LI ; Yue XU ; Jianhua RAN ; Xiaoqiang GENG ; Jinzhao HE ; Jia MENG ; Guangying SHAO ; Hong ZHOU ; Zemei GE ; Guangping CHEN ; Runtao LI ; Baoxue YANG
Acta Pharmaceutica Sinica B 2021;11(1):181-202
Urea transporters (UT) play a vital role in the mechanism of urine concentration and are recognized as novel targets for the development of salt-sparing diuretics. Thus, UT inhibitors are promising for development as novel diuretics. In the present study, a novel UT inhibitor with a diarylamide scaffold was discovered by high-throughput screening. Optimization of the inhibitor led to the identification of a promising preclinical candidate,