1.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) .
2.Roles of the cross talk between MAP kinases and Keap1-Nrf2-ARE signaling pathways in chronic obstructive pulmonary disease.
Shujun WANG ; Yajun CHEN ; Shanshan WANG ; Dianlei WANG ; Chenyin WANG ; Lili YANG ; Jinpei CHEN
Acta Pharmaceutica Sinica 2015;50(2):133-40
Chronic obstructive pulmonary disease (COPD), a common preventable and treatable disease, is characterized by airflow limitation that is usually progressive and associated with an enhanced chronic inflammatory response in the airways. Its main pathological manifestations include airway inflammation, mucus hypersecretion, oxidative stress and apoptotic epithelial cells. Recent research suggests that MAP kinases and Keap1-Nrf2-ARE signaling pathway are involved in the pathological process of inflammation and oxidative stress. This review explores the potential role of the cross talk of these signaling pathways in airway inflammation, mucus hypersecretion, oxidative stress and apoptotic epithelial cells. To clarify the roles of cross talk between MAP kinases and Keap1-Nrf2-ARE signaling pathway, we also focus on the drugs related to that in the treatment of COPD, and it provides ideas for more drug research in the treatment of COPD.
3.MRP1 expression and bronchial epithelial function in lipopolysaccharide-induced rat model of chronic obstructive pulmonary disease
Shanshan WANG ; Dianlei WANG ; Xiuhua TAO ; Chenyin WANG ; Jinpei CHEN ; Lili YANG ; Yin CAO
Acta Laboratorium Animalis Scientia Sinica 2014;(3):30-34
Objective To study the impact of establishment of lipopolysaccharide ( LPS )-induced rat model of chronic obstructive pulmonary disease (COPD)on the function of multidrug resistance-associated protein 1(MRP1)in the rat bronchial epithelium .Methods Using intratracheal instillation of LPS to establish COPD rat model .8-week old healthy male Wistar rats were divided into 3 groups (10 rats in each group ):(1) Normal control;(2) Modeling for 14 days after LPS instillation;(3) Modeling for 28 days after LPS instillation.Pulmonary function and the concentration of phenol red in bronchoalveolar lavage fluid ( BALF) and plasma were measured .The ratio of phenol red concentration in BALF/plasma was used as an index of the MRP 1 function in the rat bronchial epithelium and the expression of MRP 1 in the bronchial epi-thelium was also observed by immunohistochemistry .Results Compared with the normal group , the pulmonary functions of the rats in the model groups were significantly reduced along with the modeling progress .After intravenous administration of phenol red, the ratio of phenol red concentration in BALF/plasma was gradually reduced , and the expression of MRP1 in the bronchial epithelium was significantly decreased .Conclusions COPD rat model can be established by intratracheal LPS instillation, and the function of MRP1 in bronchial epithelium was gradually reduced along with the modeling progress .
4.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.
5.Value of nasobiliary cholangiography in the diagnosis of residual common bile duct stones after endoscopic retrograde cholangiopancreatography and related factors of residual common bile duct stones
Dapeng BIAN ; Jinpei DONG ; Haixia NIU ; Yinmo YANG ; Qiushi FENG
Journal of Clinical Hepatology 2021;37(4):868-871
ObjectiveTo investigate the value of nasobiliary cholangiography in the diagnosis of residual common bile duct stones after endoscopic retrograde cholangiopancreatography (ERCP) and the risk factors for residual stones. MethodsA retrospective analysis was performed for the clinical data of the patients who underwent ERCP and nasobiliary cholangiography after endoscopic nasobiliary drainage in Peking University First Hospital from January 1, 2018 to December 31, 2019. The chi-square test was used for comparison of categorical data between groups, and a logistic regression analysis was used to investigate independent risk factors for residual stones. ResultsA total of 366 patients underwent ERCP and nasobiliary cholangiography and 27 patients were suspected to have residual stones, among whom 25 had residual stones confirmed by ERCP. The rate of residual stones after ERCP was 6.8% (25/366), and nasobiliary cholangiography had a positive predictive value of 92.6% (25/27) in predicting residual common bile duct stones. The univariate analysis showed that there were significant differences between the two groups in multiple stones, common bile duct diameter ≥1.5 cm, and mechanical lithotripsy (χ2=5014, 7.651, and 9.670, all P<0.05). The multivariate logistic regression analysis showed that multiple stones (odds ratio [OR]=2713, 95% confidence interval [CI]: 1.002-7.345, P=0.049) and mechanical lithotripsy (OR=9.183, 95% CI: 2.347-35.925, P=0.001) were independent risk factors for residual stones. ConclusionPost-ERCP nasobiliary cholangiography is an effective method to detect residual common bile duct stones. Multiple stones and mechanical lithotripsy during ERCP are independent risk factors for residual stones.
6.Human umbilical cord mesenchymal stem cells differentiate into neuron-like cells after induction with B27-supplemented serum-free medium.
Yunyi LI ; Jinpei YANG ; Guo FU ; Pan ZHOU ; Yang LIU ; Zhizhong LI ; Genlong JIAO
Journal of Southern Medical University 2020;40(9):1340-1345
OBJECTIVE:
To evaluate the capacity and efficiency of human umbilical cord mesenchymal stem cells (HUCMSCs) to differentiate into neuron- like cells after induction with B27- supplemented serum- free medium.
METHODS:
HUCMSCs at passage 4 were cultured for 14 days with serum-containing medium (SCM) (group A), SCM supplemented with 20 ng/mL nerve growth factor (NGF) and 10 ng/mL basic fibroblast growth factor (bFGF) (group B), serum-free medium (SFM) (group C), or SFM supplemented with 20 ng/mL NGF and 10 ng/mL bFGF. The culture medium were changed every 3 days and the growth of the neurospheres was observed using an inverted microscope. The cell markers were analyzed with flow cytometry and the expressions of nestin, neuron- specific enolase (NSE), neurofilament heavy polypeptide (NEFH), and glial fibrillary acidic protein (GFAP) were quantified by quantitative real-time PCR (qRT-PCR) and Western blotting.
RESULTS:
Before induction, HUCMSCs expressed abundant mesenchymal stem cell surface markers including CD29 (99.5%), CD44 (49.6%) and CD105 (77.7%). Neuron-like cells were observed in the cultures on days 7, 10, and 14, and the cell differentiation was the best in group D, followed by groups C, B and A. In all the 4 groups, the cellular expressions of nestin and GFAP gradually lowered while those of NEFH and NSE increased progressively. The expressions of GFAP, NEFH, nestin and NSE were significantly different between group A and the other 3 groups ( < 0.001 or 0.05).
CONCLUSIONS
B27-supplemented SFM effectively induces the differentiation of HUCMSCs into neuron- like cells, and the supplementation with cytokines (NGF and bFGF) strongly promotes the cell differentiation.