1.Research progress on the function of angiotensin Ⅱ receptors in tumor
Yanchun ZHANG ; Jinpei ZHOU ; Xiaoming WU
Chinese Pharmacological Bulletin 1986;0(04):-
AngiotensinⅡ is a biologically activated peptide of the rennin-angiotensin system(RAS).Beside constracting vascular and regulating blood pressure,AngⅡplays an important role in the development of tumor,inflammation and angiogenesis.The expression and major intracellular signaling pathways of AngⅡ and AngⅡ receptors in tumor are reviewed.
2.Effect of Folic Acid on the Homocysteine level and Flow-mediated Vasodilation and Cognitive Function in the Treatment of Elderly Patients with Cerebral Infarction
Heting LUO ; Jinpei ZHANG ; Yi ZHANG ; Yanchen WANG ; Xiaojun LU
China Pharmacy 2015;(27):3789-3790,3791
OBJECTIVE:To discuss the effect of folic acid on the homocysteine(Hcy)and flow-mediated vasodilation and cog-nitove function in the treatment of elderly patients with cerebral infarction. METHODS:The data of 198 elderly patients with cere-bral infarction was randomly divided into the observation group and the control group by different medication. Control group was treated with conventional treatment;based on the treatment of control group,observation group was orally treated with Folic acid tabelts 5 mg,once a day. The treatment course of 2 groups was 8 weeks. The Hcy level and flow-mediated vasodilation(FMD)be-fore and after treatment,mini-mental state examination (MMSE) score and incidence of adverse reactions in 2 groups were ob-served. RESULTS:After treatment,Hcy level in observation group was significantly lower than before and control group,FMD was significantly higher than before and control group(P<0.01). MMSE score in observation group was significantly higher than control group(P<0.01). There were no obvious adverse reactions in 2 groups during treatment. CONCLUSIONS:Based on the con-ventional treatment,folic acid can effectively reduce the Hcy level of elderly patients with cerebral infarction,improve the cogni-tive function and reduce the brain tissue damage,with good safety.
3.The correlation of cerebral perfusion characteristics and cognitive function on patients with unipolar and bipolar depression
Erni JI ; Nianhong GUAN ; Houliang WANG ; Jinpei ZHANG ; Ying PENG
Chinese Journal of Behavioral Medicine and Brain Science 2011;20(4):330-332
Objective To analyze the correlation of cerebral perfusion characteristics and cognitive function on patients with unipolar and bipolar depression. Methods The r-CBF imaging was detected by SPECT forall subjects. Evaluated cognitive function of subjects using WAIS-CR and WMA, and analysed data using SPSS.Results Data showed that some regions in the brain, e.g. temporal lobe, frontal lobe, hippocampus, and basal ganglia, had significant alterations of r-CBF in depressed patients as compared with healthy controls (P < 0. 05 ).Compared with UPD, BPD showed increased perfusion in basal ganglia ( 0,22.73%; 4.54%, 36. 36% ) (P <0.05 ). Furthermore there was no significant different incognitive deficits between UPD and BPD(P > 0. 05 ) , and correlations between cognitive impairment and hypoperfusion of rCBF (P < 0. 05 ). Conclusion There be exist difference in r-CBF between UPD and BPD. The perfusion of r-CBF in BPD is significantly increased than that in UPD,and it suggest that hyperperfusion in basal ganglia may be the biological basis when bipolar depression turning to manic.
4.Advances in indoleamine 2, 3-dioxygenase 1 inhibitors
Yulan CHENG ; Jinxia MEN ; Jinpei ZHOU ; Huibin ZHANG
Journal of China Pharmaceutical University 2017;48(3):361-370
Indoleamine 2,3-dioxygenase 1 (IDO1) is the rate-limiting enzyme which catalyses the metabolism of L-tryptophan(L-Trp) in the kynurenine pathway.It is overexpressed in many tumor cells and antigen presenting cells.This enzyme inhibits local immune response and supports tumor cells to evade immune surveillance by depleting L-Trp and producing kynurenine metabolites,thus,it is an important target for cancer immunotherapy.There are several IDO1 inhibitors with different scarfold under investigation,three of which have already entered clinical stage.The role of IDO1 in tumor immune tolerance and the research progress on IDO1 inhibitors in recent years are summarized in this paper.
5.Advances in antidiabetic small molecule ABHD6 inhibitors
Lianghui SI ; Hui MA ; Jinpei ZHOU ; Huibin ZHANG
Journal of China Pharmaceutical University 2017;48(2):125-134
Type 2 diabetes,a glucose and lipid metabolism disorder accompanied by chronic multiple organ damage,has become a huge threat to human health,α/β hydrolase domain-6 (ABHD6) regulates the insulin release negatively by hydrolyzing monoacylglycerol.Small molecule ABHD6 inhibitors have been proven to lower bloodglucose and regulates energy homeostasis,which is a potential candidate for the treatment of type 2 diabetes.This paper introduced the ABHD6 signaling pathway and its mechanism,then reviewed the progress of small molecule ABHD6 inhibitors with different structures in recent years,and analyzed the structure activity relationship.
6.The utility of Liebowitz Social Anxiety Scale in the patients with social anxiety disorder in Chinese
Jiyang PAN ; Jihui ZHANG ; Ping MA ; Huajun LIANG ; Houliang WANG ; Jiong TAO ; Shenglin WEN ; Jinpei ZHANG
Chinese Journal of Nervous and Mental Diseases 2006;32(3):206-210
Background During the past two decades, a number of rating scales were developed to facilitate diagnosis and assessment of subjects with social anxiety disorder. One of the most commonly used scales for the assessment of social anxiety disorder is the Liebowitz social anxiety scale (LSAS). The LSAS is widely used in epidemiologic investigations and clinical researches,and its assessment in the pharmacotherapy efficacy for social anxiety disorder is superior to any other scale. So we designed this study to explore the validity and reliability of the LSAS in Chinese patients with social anxiety disorder and normal control, and to find the difference of the scores between the patients self -report version and clinician-administered version. Methods Fifty five patients meeting the DSM-Ⅳ diagnostic criteria for social anxiety disorder and 168 normal controls who were screened from 222 college students were rated by LSAS, social phobia scale and self-made General Information Forms. Results The Cronbath α of LSAS for the patients and the normal controls was 0.83 and 0.77, respectively. The 4-week test-retest reliability for total scores and its factors scores of LSAS in 31 normal controls were ranging from 0.68 to 0.79. The ROC area under curve value in discriminating the patients from normal controls was 0.87±0.03; the total score of 35 was considered to be the best cut-off score for LSAS, then its sensitivity was 0.77 and its specificity was 0.81; and no significant difference between the self-report version and clinician-administered version. Conclusions The LSAS is good in internal consistency and test-retest reliability, and has high sensitivity and specificity in discriminating the patients and the controls. There is no significant difference in the total score and each factor scores of LSAS between self-report version and clinician-administered version.
7.Influence of stigma on QOL of patients with mental disorders
Ying ZHOU ; Shengmao PAN ; Chunyang ZHAO ; Jiankui LIN ; Yajie LI ; Jinpei ZHANG ; Lianqi LIU
Chongqing Medicine 2015;(10):1349-1351
Objective To investigate the influence of stigma on QOL of patients with mental disorders.Methods By using Link stigma series scale and schizophrenic quality of life scale,we assessed and analyzed 406 psychiatric patients′stigma and QOL, as well as the correlation and influence between them.Results The score of perceived devaluation-discrimination dimension of the stigma scale had positive correlation with total score of QOL,score of psycho-social dimension and score of motivation and energy dimension (P <0.05).The scores of challenge dimension and separation dimension in the stigma scale had positive correlation with motivation and energy dimension of the QOL scale (P <0.05).Regression analysis showed that stigma did not have influence on QOL of patients with mental disorders.Conclusion Stigma in psychiatric patients has no significant influence on QOL,but correla-tion relationship exists between them.The higher score of perceived devaluation-discrimination dimension,challenge dimension and separation dimension of stigma scale,the poor QOL the patient would have.
8.Dynamic Study on Soluble Sugar Accumulation and Sucrose Metabolizing Enzyme Activities During Fruit Development of Amomum villosum Lour
Anmin YU ; Min ZHANG ; Jinfen YANG ; Wenhua LIN ; Ping YAN ; Jinpei LIANG ; Ruoting ZHAN
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(7):1497-1504
This study was aimed to discuss the dynamic variation of soluble sugar contents, sucrose metabolizing en-zyme activities and gene expression quantities during the fruits development of A momum villosum, in order to pro-vide the basis of improvement of the fruit yield. Fresh fruits at three different development processes (30 DAF, 60 DAF, 90 DAF) were used to investigate changes of soluble sugar components and sucrose metabolizing enzyme activ-ities by HPLC and UV spectrophotometry. Combining with the high-throughput sequencing expression profile data of three fruit development period, the trends of three key enzymes gene expressed in sugar metabolism were analyzed. The results showed that the fruit sugar components were dominated by fructose, glucose and sucrose. The concentra-tion of hexose (fructose and glucose) gradually decreased in peel. But in seeds the concentration of hexose decreased at first and then increased. The content of sucrose and the net activities of sucrose synthase (synthesizing direction minus decomposing direction) in peel and seeds were gradually increased. The expression trends of key enzyme gene in sugar metabolism examined by RNA-seq quantification showed that sucrose phosphate synthase and sucrose syn-thase gene increased and then kept constant, but the invertase gene expression trend was gradually rising. Conse-quently, sucrose synthase was the key enzyme catalyzing sucrose synthesis and decomposition. The activity of sucrose synthase and sucrose contents in peel and seeds reached the highest peak in the end of fruit mature.
9.Design, synthesis and antiplatelet evaluation of tetramethylpyrazine/chalcone hybrids
Yang GAO ; Wei YIN ; Jingchao LIU ; Fenghua KANG ; Yanlin JIAN ; Jinpei ZHOU ; Zhangjian HUANG ; Yihua ZHANG
Journal of China Pharmaceutical University 2017;48(1):23-30
In order to search for new antiplatelet agents with higher potency, a series of tetramethylpyrazine ( TMP) /chalcone hybrids ( 2-26) were synthesized and evaluated based on the principle of bioisostere and hybrid-ization. They exerted inhibitory activity against adenosine diphosphate ( ADP )-induced and arachidonic acid ( AA)-induced platelet aggregation to varied extent. Among them, compound 8 was the most potent with IC50 of 0. 14 mmol/L on ADP-induced platelet aggregation ( 9. 1 folds of TMP and 10. 5 folds of chalcone ) and 0. 09 mmol/L on AA-induced platelet aggregation ( 8. 8 folds of TMP and 10. 0 folds of chalcone) , which was superior to clinically used anti-platelet drug aspirin ( ASP, IC50 =0. 15 mmol/L) .
10.Advances in small molecule inhibitors of PD-1/PD-L1 immune checkpoint pathway
Jiping TIAN ; Jian ZHANG ; Jinpei ZHOU ; Huibin ZHANG
Journal of China Pharmaceutical University 2019;50(1):1-10
Studies have found that a variety of tumors continue to activate PD-1(programmed cell death protein 1, PD-1)/PD-L1(programmed cell death-ligand 1)signaling pathway by up-regulating PD-L1 expression in tumor cells and microenvironment. The dysfunction of T cells leads to the occurrence of tumor immune escape. Several PD-1/PD-L1 monoclonal antibodies have been marketed to achieve significant clinical efficacy. However, because of the high production cost, the harsh conditions for storage and transportation, and the potential immunogenicity of monoclonal antibody, the seeking for PD-1/PD-L1 small molecule inhibitors has become a hot spot in the development of new drugs. In this paper, the biological mechanisms of PD-1/PD-L1 was introduced in detail. Based on the structural classification, the research progress of PD-1/PD-L1 small molecule inhibitors was reviewed, with a prospect of the development of small molecule inhibitors.