2.Design, synthesis and evaluation of phenoxyacetic acid-based PTP1B inhibitors
Jin-ying TIAN ; Jun-zheng LIU ; Shu-en ZHANG ; Xiao-lin ZHANG ; Fei YE ; Zhi-yan XIAO
Acta Pharmaceutica Sinica 2023;58(12):3684-3690
Protein tyrosine phosphatase (PTP) 1B is a potential therapeutic target for type 2 diabetes. Phosphotyrosine (pTyr) mimetics still dominate the currently available PTP1B inhibitors. The phenoxyacetic acid moiety was taken as a pTyr mimetic herein and phenoxyacetic acid-based compounds
3.Role of podocyte injury signaling pathway in steroid-resistant nephrotic syndrome and research progress in traditional Chinese medicine intervention.
Wen-Xia YU ; Wen YAN ; En-Lai DAI ; Wen-Xuan TIAN ; Wen-Jing DANG
China Journal of Chinese Materia Medica 2023;48(12):3246-3254
As one of the main diseases leading to end-stage renal disease, steroid-resistant nephrotic syndrome(SRNS) can cause serious complications such as infection. Without effective control, this disease can further lead to the malignant development of the renal function, bringing serious social and economic burdens. As previously reported, the formation of SRNS is mostly related to the podocyte injury in the body, i.e., the injury of glomerular visceral epithelial cells. Phosphatidylinositol 3-kinase(PI3K)/protein kinase B(Akt) signaling pathway, nuclear transcription factor-κB(NF-κB) signaling pathway, mammalian target of rapamycin(mTOR)/adenosine monophosphate(AMP)-activated protein kinase(AMPK), transforming growth factor(TGF)-β1/Smads, and other signaling pathways are classical signaling pathways related to podocyte injury. By regulating the expression of signaling pathways, podocyte injury can be intervened to improve the adhesion between podocyte foot processes and glomerular basement membrane and promote the function of podocytes, thereby alleviating the clinical symptoms of SRNS. Through the literature review, traditional Chinese medicine(TCM) has unique advantages and an important role in intervening in podocyte injury. In the intervention in podocyte injury, TCM, by virtue of multi-target and multi-pathway role, can regulate and intervene in podocyte injury in many ways, alleviate the clinical symptoms of SRNS, and interfere with the progress of SRNS, reflecting the unique advantages of TCM. On the other hand, TCM can directly or indirectly inhibit podocyte injury by regulating the above signaling pathways, which can not only promote the effect of hormones and immunosuppressants and shorten the course of treatment, but also reduce the toxic and side effects caused by various hormones and immunosuppressants to exert the advantages of small side effects and low price of TCM. This article reviewed TCM in the treatment of SRNS by interfering with podocyte injury-related signaling pathways and is expected to provide a reference for the in-depth study of TCM in the treatment of SRNS, as well as a theoretical basis and a new direction for the clinical application of TCM to shorten the course of treatment of SRNS and delay the progression to end-stage renal disease.
Humans
;
Podocytes
;
Nephrotic Syndrome/genetics*
;
Medicine, Chinese Traditional
;
Phosphatidylinositol 3-Kinases/genetics*
;
Signal Transduction
;
NF-kappa B
;
AMP-Activated Protein Kinases
;
Hormones
4.Effect of Rehmanniae Radix on depression-like behavior and hippocampal monoamine neurotransmitters of chronic unpredictable mild stress model rats.
Ping TIAN ; Wei ZHANG ; Kai-Yan LI ; Hong-Wei LI ; Kai MA ; De-En HAN
China Journal of Chinese Materia Medica 2022;47(17):4691-4697
To investigate the effect of Rehmanniae Radix on depression-like behavior and monoamine neurotransmitters of chronic unpredictable mild stress(CUMS) model rats. CUMS combined with isolated feeding was used to induce the depression model of rats. The depression-like behavior of rats was evaluated by sucrose preference test, open field test, and forced swim test. Hematoxylin-Eosin(HE) staining was used to investigate the pathological changes of neurons in the CA1 and CA3 area of hippocampus. Ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS) was used to detect the contents of 5-hydroxytryptamine(5-HT), 5-hydroxyindoleacetic acid(5-HIAA), dopamine(DA), 3,4-dihydroxyphenylacetic acid(DOPAC), homovanillic acid(HVA), norepinephrine(NE), and 3-methoxy-4-hydroxyphenyl glycol(MHPG) in rats. Western blot was used to detect the protein expressions of tryptophan hydroxylase 2(TPH2), serotonin transporter(SERT), and monoamine oxidase A(MAO-A) in the hippocampus of rats. Compared with the normal group, depressive-like behavior of rats was obvious in the model group. The arrangements of neurons in the CA1 and CA3 area of hippocampus were loose and disorderly. The levels of 5-HT, 5-HIAA, and 5-HT/5-HIAA in the hippocampal area were decreased(P<0.01). The protein expression of TPH2 was decreased(P<0.01), but those of SERT and MAO-A were increased(P<0.01). In the Rehmanniae Radix groups with 1.8 g·kg~(-1) and 7.2 g·kg~(-1), the depression-like behavior of CUMS rats and pathological changes of neurons in CA1, CA3 area of hippocampus were improved. The protein expression of TPH2(P<0.05, P<0.01) was increased, and those of SERT and MAO-A were down-regulated(P<0.05, P<0.01). The levels of 5-HT, 5-HIAA, and 5-HT/5-HIAA in hippocampus were increased(P<0.05, P<0.01). The changes in DA, DOPAC, HVA, DA/(DOPAC +HVA), NE, DHPG, and NE/DHPG were not statistically significant. The results suggested that Rehmanniae Radix improved depression-like behavior of CUMS rats, and the mechanism might be related to the regulation of synthesis, transportation, and metabolism of 5-HT neurotransmitter in the hippocampus.
3,4-Dihydroxyphenylacetic Acid/pharmacology*
;
Animals
;
Antidepressive Agents/therapeutic use*
;
Chromatography, Liquid
;
Depression/drug therapy*
;
Disease Models, Animal
;
Dopamine
;
Eosine Yellowish-(YS)/pharmacology*
;
Hematoxylin/pharmacology*
;
Hippocampus/metabolism*
;
Homovanillic Acid/pharmacology*
;
Hydroxyindoleacetic Acid/metabolism*
;
Methoxyhydroxyphenylglycol/pharmacology*
;
Monoamine Oxidase/metabolism*
;
Neurotransmitter Agents/metabolism*
;
Norepinephrine/pharmacology*
;
Plant Extracts
;
Rats
;
Rehmannia/chemistry*
;
Serotonin/metabolism*
;
Serotonin Plasma Membrane Transport Proteins/pharmacology*
;
Stress, Psychological/metabolism*
;
Tandem Mass Spectrometry
;
Tryptophan Hydroxylase/metabolism*
5.Exploring an Integrative Therapy for Treating COVID-19: A Randomized Controlled Trial.
Jia-Bo WANG ; Zhong-Xia WANG ; Jing JING ; Peng ZHAO ; Jing-Hui DONG ; Yong-Feng ZHOU ; Guang YANG ; Ming NIU ; Xu ZHAO ; Tian-Jun JIANG ; Jing-Feng BI ; Zhe XU ; Ping ZHANG ; Dan WU ; Zhao-Fang BAI ; Yu-Ming GUO ; Si-Miao YU ; Yong-Qiang SUN ; Zi-Teng ZHANG ; Xiao-Yan ZHAN ; Peng-Yan LI ; Jin-Biao DING ; Peng-Fei ZHAO ; Xue-Ai SONG ; Jian-Yuan TANG ; Dong-Chu HE ; Zhu CHEN ; En-Qiang QIN ; Rui-Lin WANG ; Xiao-He XIAO
Chinese journal of integrative medicine 2020;26(9):648-655
OBJECTIVES:
To develop a new Chinese medicine (CM)-based drug and to evaluate its safety and effect for suppressing acute respiratory distress syndrome (ARDS) in COVID-19 patients.
METHODS:
A putative ARDS-suppressing drug Keguan-1 was first developed and then evaluated by a randomized, controlled two-arm trial. The two arms of the trial consist of a control therapy (alpha interferon inhalation, 50 µg twice daily; and lopinavir/ritonavir, 400 and 100 mg twice daily, respectively) and a testing therapy (control therapy plus Keguan-1 19.4 g twice daily) by random number table at 1:1 ratio with 24 cases each group. After 2-week treatment, adverse events, time to fever resolution, ARDS development, and lung injury on newly diagnosed COVID-19 patients were assessed.
RESULTS:
An analysis of the data from the first 30 participants showed that the control arm and the testing arm did not exhibit any significant differences in terms of adverse events. Based on this result, the study was expanded to include a total of 48 participants (24 cases each arm). The results show that compared with the control arm, the testing arm exhibited a significant improvement in time to fever resolution (P=0.035), and a significant reduction in the development of ARDS (P=0.048).
CONCLUSIONS
Keguan-1-based integrative therapy was safe and superior to the standard therapy in suppressing the development of ARDS in COVID-19 patients. (Trial registration No. NCT04251871 at www.clinicaltrials.gov ).
Administration, Inhalation
;
Adult
;
China
;
Coronavirus Infections
;
diagnosis
;
drug therapy
;
mortality
;
Dose-Response Relationship, Drug
;
Drug Administration Schedule
;
Drugs, Chinese Herbal
;
administration & dosage
;
Female
;
Follow-Up Studies
;
Humans
;
Integrative Medicine
;
Interferon-alpha
;
administration & dosage
;
Lopinavir
;
administration & dosage
;
Male
;
Middle Aged
;
Pandemics
;
Pneumonia, Viral
;
diagnosis
;
drug therapy
;
mortality
;
Risk Assessment
;
Severe Acute Respiratory Syndrome
;
diagnosis
;
drug therapy
;
mortality
;
Severity of Illness Index
;
Survival Rate
6.Application of colonoscopic tattooing with India ink for localization of colorectal lesions in laparoscopic surgery
Hai-Yan HE ; Xiao-Wen XU ; Bei-Li CAI ; Jia CHEN ; Na ZHU ; Ling-Yun TIAN ; Cheng-Li GUO ; Li-Qiang HAO ; Hao WANG ; En-Da YU
China Journal of Endoscopy 2018;24(6):93-96
Objective?To investigate the use of submucosal injection of India ink for localization of colorectal lesions in laparoscopic surgery, and to evaluate its efficiency and safety.?Methods?A retrospective study of 146 patients with colorectal lesions from January 2015 to November 2017, who underwent preoperative colonoscopic marking with India ink and subsequently received laparoscopic colectomy was conducted. 1.0 ml of physiologic saline solution was first injected into the submucosa to produce an artificial submucosal elevation, and then 0.2 ml of 1 : 10 diluted India ink followed with another 1ml of physiologic saline solution was injected. Operation time, success rate, complications, location efficiency, and postoperative pathology were evaluated.?Results?The India ink tattooing was easily applied for all patients without complication. At laparoscopic surgery, all lesions could be clearly visualized. No ink diffusion, leakage, and local inflammatory responses were observed. The surgical margins of all samples were tumor negative.?Conclusion?Preoperative submucosal tattooing with India ink is recommended as an easy, safe and economical procedure.
7.Study on the ARIMA model application to predict echinococcosis cases in China
En-Li TAN ; Zheng-Feng WANG ; Wen-Ce ZHOU ; Shi-Zhu LI ; Yan LU ; Lin AI ; Yu-Chun CAI ; Xue-Jiao TENG ; Shun-Xian ZHANG ; Zhi-Sheng DANG ; Chun-Li YANG ; Jia-Xu CHEN ; Wei HU ; Xiao-Nong ZHOU ; Li-Guang TIAN
Chinese Journal of Schistosomiasis Control 2018;30(1):47-53
Objective To predict the monthly reported echinococcosis cases in China with the autoregressive integrated mov-ing average(ARIMA)model,so as to provide a reference for prevention and control of echinococcosis. Methods SPSS 24.0 software was used to construct the ARIMA models based on the monthly reported echinococcosis cases of time series from 2007 to 2015 and 2007 to 2014,respectively,and the accuracies of the two ARIMA models were compared. Results The model based on the data of the monthly reported cases of echinococcosis in China from 2007 to 2015 was ARIMA(1,0,0)(1,1, 0)12,the relative error among reported cases and predicted cases was-13.97%,AR(1)=0.367(t=3.816,P<0.001),SAR (1)=-0.328(t=-3.361,P=0.001),and Ljung-Box Q=14.119(df=16,P=0.590).The model based on the data of the monthly reported cases of echinococcosis in China from 2007 to 2014 was ARIMA(1,0,0)(1,0,1)12,the relative error among reported cases and predicted cases was 0.56%,AR(1)=0.413(t=4.244,P<0.001),SAR(1)=0.809(t=9.584, P<0.001),SMA(1)=0.356(t=2.278,P=0.025),and Ljung-Box Q=18.924(df=15,P=0.217).Conclusions The different time series may have different ARIMA models as for the same infectious diseases.It is needed to be further verified that the more data are accumulated,the shorter time of predication is,and the smaller the average of the relative error is.The estab-lishment and prediction of an ARIMA model is a dynamic process that needs to be adjusted and optimized continuously accord-ing to the accumulated data,meantime,we should give full consideration to the intensity of the work related to infectious diseas-es reported(such as disease census and special investigation).
8.Quantitative analysis of 16 components in Cyclocarya paliurus leaf by UPLC-QE-Orbitrap-MS.
Kai MA ; Ping TIAN ; Di-Wen ZHANG ; Hong-Yan ZHOU ; Wei SUN ; Yan-Yan WANG ; De-En HAN
China Journal of Chinese Materia Medica 2018;43(20):4077-4083
Modern research showed that components in the dried leaf of Cyclocarya paliurus. had various biological activities. The current quality control research was focused on content determination of polysaccharides and flavonoids, while there were less research on quantitative analysis of terpenes and phenolic acids. In this paper, the contents of 16 components of 3 kinds in C. paliurus leaf were determined by UPLC-QE-Orbitrap-MS. The results were as following: good linear relationship of 16 analytes existed within the studied concentration rages (²>0.996), and RSDs were of <3.0% in the precision test and replicate test, with the average recovery rates 95.20%-104.4%, respectively. The results indicatod that the method is simple and accurate, which can be used for the comprehensive quality evaluation of C. paliurus leaf. The established method was applied to determine the contents of 12 batches of C. paliurus leaf from different areas, and the 16 analvtes contents in the samples could be different from several times to dozens times, which indicated that there might be significant quality difference in C. paliurus leaf from different areas.
Flavonoids
;
analysis
;
Juglandaceae
;
chemistry
;
Phytochemicals
;
analysis
;
Plant Leaves
;
chemistry
;
Polysaccharides
;
analysis
9.Effect of group mind-games and group counseling on training burnout among soldiers stationed on plateau for the first time
Kui DING ; Quan-Chao LI ; En-Li QUAN ; Yong-Bin WANG ; Yan WANG ; Xin-Zhen MENG ; Tian QIN
Military Medical Sciences 2017;41(10):845-849
Objective To explore the effect of group mind-games and group counseling on training burnout among soldiers who quickly marched to the plateau for the first time .Methods Totally 399 soldiers who quickly marched to the plateau for the first time were divided randomly into to the control group ( n=201 ) and test group ( n=198 ) .The test group had particinated in group mind-games and psychological counseling twice a week for a total of 5 weeks, while the control group received no counseling .Soldier training fatigue questionnairs were used to compare the difference between the two groups before and after group mind-games and psychological counseling .Results ①The total scores of training burnout and the scores of all the factors of soldiers before counseling in the two groups was of no statistical significance (P>0.05). After counseling , the total scores of training burnout and the scores of all factors in test group were remarkably lower than those in control group,and the difference was of statistical significance (P<0.05).The total scores of training burnout and the scores of physical and psychologica exhaustion and alienaties decreased significantly after training in test group ( P<0.05), but the change was of no statistical significance in control group (P>0.05).②Soldiers who had served 1 to 2 years or over 9 years had significant difference in the scores of training burnout , physical and psychologica exhaustion ( P<0.05).Soldiers who had served 3 to 8 years had significant difference in the scores of training and the scores of each factor after counseling(P<0.05).Conclusion Group mind-games and psychological counseling can effectively help alleviate the training burnout of soldiers who quickly march to the plateau for the first time.
10.A cross-sectional investigation on the control effect of varicella vaccination on the outbreak of varicella in Minhang District of Shanghai
Xia TIAN ; ci En WANG ; Yan DU ; song Jin CUI ; li Dong XU
Fudan University Journal of Medical Sciences 2017;44(5):608-611
Objective To analyze the changes of varicella outbreak in Minhang District before and after practicing "the varicella emergency vaccination implementation program (2013-2014 trial version),Shanghai",and to evaluate the effects of live attenuated vaccine against varicella.Methods We used cross-sectional investigation to collect monitoring data of vaticella outbreak recorded in "China Information System for Disease Control and Prevention".The observation periods before and after the implementation of the program were during 2012-01-01 to 2013-06-30 and during 2013-07-01 to 2014-12-31.Results Before the implementation of the program,14 cases of varicella epidemic were reported in Minhang District.All cases were up to the outbreaks in the epidemic,the longest duration was 82 days,the average duration continued was 50.86 days (912/14),the average cumulative generation was 2.42 generations (50.86/21),the total number of people was 159,the total incidence rate was 1.26% (159/12 625),the class incidence rate was 9.09% (159/1 750),the average number of people was 11.36 (159/14),the average number of class was 3.21 (45/14).After the implementation of the program,169 cases of the varicella epidemic were reported in Minhang District,only 22 cases rose to the outbreaks in the epidemic,the longest duration was 66 days,the average duration continued was 41.32 days (909/22),the average cumulative generation was 1.97 generations (41.32/21),the total number of people was 200,the total incidence rate was 1.10% (200/18 200),the class incidence rate was 8.38% (200/2 387),the average number of people was 9.09 (200/22),the average number of class was 2.50 (55/22);Although the varicella epidemic in the total outbreaks had significantly increased in Minhang District before and after emergency implementation,but the varicella outbreak in the varicella epidemic significantly decreased,the total incidence rate,the class incidence rate,the longest duration,the average duration,the average cumulative generation,the average number of people and the average number of class had decreased in varying degrees.There is statistical difference between the average duration before and after the implementation (x2 =4.06,P<0.05).Conclusions Emergency vaccination of varicella vaccine in high risk population can effectively control the spread of epidemic situation and reduce the possibility of secondary transmission.

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