1.Design,synthesis,and evaluation of fluoroquinolone derivatives as microRNA-21 small-molecule inhibitors
Hei YUAN-YUAN ; Wang SI ; Xi XIAO-XIAO ; Wang HAI-PENG ; Guo YUANXU ; Xin MINHANG ; Jiang CONGSHAN ; Lu SHEMIN ; Zhang SAN-QI
Journal of Pharmaceutical Analysis 2022;12(4):653-663
MicroRNA-21(miRNA-21)is highly expressed in various tumors.Small-molecule inhibition of miRNA-21 is considered to be an attractive novel cancer therapeutic strategy.In this study,fluoroquinolone de-rivatives Al-A43 were synthesized and used as miRNA-21 inhibitors.Compound A36 showed the most potent inhibitory activity and specificity for miRNA-21 in a dual-luciferase reporter assay in HeLa cells.Compound A36 significantly reduced the expression of mature miRNA-21 and increased the protein expression of miRNA-21 target genes,including programmed cell death protein 4(PDCD4)and phos-phatase and tensin homology deleted on chromosome ten(PTEN),at 10 uM in HeLa cells.The Cell Counting Kit-8 assay(CCK-8)was used to evaluate the antiproliferative activity of A36;the results showed that the IC50 value range of A36 against six tumor cell lines was between 1.76 and 13.0 μM.Meanwhile,A36 did not display cytotoxicity in BEAS-2B cells(lung epithelial cells from a healthy human donor).Furthermore,A36 significantly induced apoptosis,arrested cells at the G0/G1 phase,and inhibited cell-colony formation in HeLa cells.In addition,mRNA deep sequencing showed that treatment with A36 could generate 171 dysregulated mRNAs in HeLa cells,while the expression of miRNA-21 target gene dual-specificity phosphatase 5(DUSP5)was significantly upregulated at both the mRNA and protein levels.Collectively,these findings demonstrated that A36 is a novel miRNA-21 inhibitor.
2.Analysis of Chemical Components in Supernatant and Precipitate of Sanajon Oral Liquid Based on UPLC-Q-TOF-MSE Technology
Hao-zhou HUANG ; Min QIU ; Jin-fa TANG ; Meng-Qi LI ; Hai-yan LIU ; San-hu FAN ; Peng TAN ; Li HAN ; Jun-zhi LIN ; Ding-kun ZHANG
Chinese Journal of Experimental Traditional Medical Formulae 2020;26(14):143-151
Objective:To analyze the main chemical components in the supernatant and precipitate of Sanajon oral liquid, so as to provide basis for establishing its quality standard and precipitation control technology. Method:UPLC-Q-TOF-MSE was used to analyze the chemical components in the supernatant and precipitate of this oral liquid. The analysis was performed on Waters ACQUITY UPLC BEH C18 column (2.1 mm×100 mm, 1.7 μm) with the mobile phase of 0.1% formic acid solution (A) and acetonitrile (B) for gradient elution (0-1 min, 2%B; 1-2 min, 2%-5%B; 2-4 min, 5%-7%B; 4-6 min, 7%-24%B; 6-10 min, 24%-42%B; 10-12 min, 42%-54%B; 12-15 min, 54%-76%B; 15-18 min, 76%-100%B), the flow rate was set to 0.3 mL·min-1, the column temperature was 30 ℃, the injection volume was 2 µL. The mass spectrographic analysis was used with electrospray ionization (ESI), sample MS data was acquired by time-dependent MSE in negative ion mode, the collection range was
3.Pharmaceutical mechanism and control strategy for storage of ellagic acid stably in traditional Chinese medicine oral liquid
Hao-zhou HUANG ; Jun-zhi LIN ; Xi-chuan WEI ; Hong-yan MA ; Hai-yan LIU ; San-hu FAN ; Wen-quan ZOU ; Li HAN ; Ding-kun ZHANG
Acta Pharmaceutica Sinica 2019;54(4):737-745
Ellagic acid is ubiquitous in plants and is considered as a potential candidate for antioxidant and antineoplastic drugs. However, ellagic acid has poor solubility and precipitates easily even after initial solubilization. Improvement of its bioavailability has been a concern of pharmaceutical industry. It was found that storage in Sanlejiang oral liquid at low temperature keeps its stability. Ellagic acid is anomalous in a way that is easily soluble at low temperatures but precipitates at high temperatures. In order to reveal the mechanism of this phenomenon and develop precipitation prevention and control strategies, ellagic acid in Sanlejiang oral liquid was stored at high, medium and low temperatures for three months. The changes of composition and phase state of the whole system during storage were systematically tracked and studied by means of precipitation amount or morphology, HPLC chemical profile of supernatant
4. North China bariatric & metabolic surgery clinical database registry report(2018)
Yang LIU ; Meng-yi LI ; Song-hai ZHANG ; San-yuan HU ; Ri-xing BAI ; Neng-wei ZHANG ; Zhong-tao ZHANG
Chinese Journal of Practical Surgery 2019;39(02):149-154
OBJECTIVE: To report an overview of bariatric & metabolic surgery performed in 2018 in North China. METHODS: Based on prospective and observational North China Bariatric & Metabolic Surgery Clinical Database(NC-BMD), the study of evaluating the number and the type of bariatric &metabolic surgery procedures was performed in North China. Demographic characteristic, obesityrelated diseases and operational information were also analyzed. RESULTS: In 2018, 17 centers from 7 regions in North China contributed a total of 728 registration data. Valid data were analyzed from 16 centers. The patients' median (minimum, maximum) BMI pre-surgery was 38.4(24.7,95.2). The overall proportion of female patients was 74.7%, and mean±SD age was(32.5±8.29) years, while male patients was 25.3%, and mean±SD age was (32.7±9.90) years. According the data 93.9% laparoscopic sleeve gastrectomy(LSG), 4.4% laparoscopic Roux-en-Y gastric bypass (LRYGB) and 1.7% other operation types. 29.2% of patients had a history of type 2 diabetes, 69.4% had sleep apnea, and 22.6% had polycystic ovary syndrome before operation. CONCLUSION: The establishment of NC-BMD has laid a solid foundation for data registration in North China. Based on current data, LSG is the mainstream of bariatric and metabolic surgery in North China this year.
5.Expression and significance of microRNA-130a and microRNA-130b in serum of patients with liver cirrhosis
Xu-Lei HUO ; San-Qiang LI ; Xin-Jie QIAO ; Shan-Long WANG ; Yong-Yong ZHANG ; Ying SONG ; Fang-Yu CAI ; Hai-Kuan SUN ; Yi-Jiong ZHANG ; Qian TI
The Chinese Journal of Clinical Pharmacology 2018;34(1):3-5
Objective To study the expression and significance of microRNA-130a(miR-130a) and miR-130b in cirrhosis' serum.Methods The elbow vein blood of 15 cases of healthy subjects and 15 cases of patients with cirrhosis were collected and were divided into treatment group and control group respectively.Reverse transcription-polymerase chain reaction was used to detect the expression of miR-130a and miR-130b in serum.Results The relative expression of miR-130a in treatment group and control goup were (1.57 ±0.36)and (1.40 ± 0.46) and the relative expression of miR-130b in serum in treatment group and control group were (2.18 ± 0.60) and (1.64 ±0.26).The differences were statistically significant(P <0.05 or P <0.01).Conclusion The expression level of miR-130a and miR-130b in cirrhosis' serum is significantly higher than those in healthy person.It is likely to be used as a diagnostic marker for cirrhosis.
6.Clinical application of modified electroconvulsive therapy in psychiatric inpatients
Qian WANG ; Yan LI ; yun Yun LI ; na Yan KOU ; san Hai ZHANG ; xing Hong ZHANG
Journal of Xinxiang Medical College 2017;34(11):978-981
Objective To investigate the clinical application of modified electroconvulsive therapy (MECT),and provide the references for more standardized and rational use of MECT.Methods A retrospective study was performed by stratified random sampling method.The clinical data of 1 330 psychiatric inpatients from January 2006 to December 2015 in Henan Psychiatric Hospital were analyzed retrospectively,and the clinical application of MECT was investigated,including the proportion of psychiatric inpatients receiving MECT,the situation of combined use of MECT and antipsychotic drugs,and the routine examination results before and after MECT.Results The proportion of receiving MECT in schizophrenic patients was the highest,it is 11.36% (81/713),the second was depressive episode (5.61%,12/214),followed by dissociative conversion disorder (5.56%,2/36),bipolar disorder (5.34%,7/131),organic mental disorder (3.23 %,1/31) and other mental disorders (2.93%,6/205).There were significant differences in the distribution of various mental disorders between the non electroshock group and the electroshock group (x2 =21.728,P < 0.05).The proportion of the patients without electric shock and the patients with single drug,two drugs,triple therapy or quadruple therapy was 0.92%,17.43 %,56.88%,21.10% and 3.67%,respectively.The proportion of the patients with two or more antipsychotic drugs was 81.65% in the electroshock group.The antipsychotics were olanzapine (28.44%),clozapine (27.52%),quetiapine (26.61%) and risperidone (24.77 %) according to the drugs used frequently in the electroshock group.The results of routine blood test were compared among the time points of before treatment,the 1st,2nd,3 rd week of MECT and 1 week after MECT in the shock group,which showed that there was significant difference in white blood cell count (F =2.570,P < 0.05);but there was no significant difference in the levels of platelet,hemoglobin and red blood cell (P > 0.05);the level of white blood cell returned to normal within two weeks in 93.33% patients with increased white blood count.The myocardial enzymes and liver function tests were not perfect during the treatment of MECT and after treatment.There was no long-term systematic evaluation of cognitive function and quality of life in patients with electroconvulsive shock.Conclusions The probability of using MECT in the patients with schizophrenia is more than that in the patients with depression.MECT is used in combination with two or more antipsychotic drugs.MECT may cause a short increase in white blood cells,but the white blood cell level in most patients can recover to normal levels after symptomatic treatment.The clinical data for treatment and prognosis in patients with MECT are inadequate,so it is necessary to improve the medical record.
7.Diffusion tensor imaging study of white matter fiber in patients with schizophrenia episode in early adulthood
liang Ben LI ; feng Yong YANG ; xing Hong ZHANG ; san Hai ZHANG ; qiang Wen LI ; Dai ZHANG ; xian Lu LYU
Journal of Xinxiang Medical College 2017;34(11):974-977
Objective To explore the structure changes of white matter of the patients with schizophrenia episode in early adulthood by diffusion tensor imaging(DTI) and in order to provide a structural neuroimaging basis for understanding the pathology of schizophrenia.Methods Twenty-six patients with schizophrenia episode in early adulthood in the Second Affiliated Hospital of Xinxiang Medical University from July 2012 to March 2014 were selected as study group and twenty-eight healthy subjects whose age,sex,education were matched with study group were selected as control group.All subjects received structural magnetic resonance imaging and DTI scans.The fractional anisotropy (FA) and the mean diffusivity (MD) of the white matter of the same encephalic region were compared between the two groups by voxel-based analyses.Results The FA values of the right anterior cingulate gyrusthe,genu of corpus callosum,the right limb of internal capsule,the bilateral external capsule,the bilateral posterior of coronal radiate,the right anterior coronal radiate of patients in the study group were significantly lower than those in the control group (P < 0.05).The MD values of the bilateral limbs of internal capsule,the right cingulate gyrus,left superior longitudinal tract,corpus callosum and right anterior coronal radiate of patients in the study group were significantly higher than those in the control group (P < 0.05).Conclusion Schizophrenia patients who episode in early adulthood exist widespread microstructural damage of white matter.These changes may be related to the pathological change of schizophrenia.
8.Expression and significance of cytochrome P4502E1 of alcoholic liver injury in mice
Xin-Jie QIAO ; San-Qiang LI ; Xu-Lei HUO ; Xiao-Ping LI ; Yi-Jiong ZHANG ; Hai-Kuan SUN ; Shan-Long WANG ; Yong-Yong ZHANG ; Qing LU ; Fan-Zhu MENG
The Chinese Journal of Clinical Pharmacology 2017;33(16):1561-1563
Objective To study the dynamic changes of cytochrome P4502E1 (CYP2E1) in alcohol-induced liver injury in mice and its sig nificance.Methods Fifty male mice were randomly divided into modelgroup (n =40) and control group (n =10).The model of alcoholic liver injury was established by continuous infusion of 56 ° Erguotou at 10 mL · kg-1 for 4 weeks.At the time of 1,2,3,4 weeks,to take 10 mice,eye blood for serum aspartate aminotransferase (AST) activity determina tion.Followed by cervical dislocation of mice,the number of CYP2E1positive cells in mice liver were detected by immunohistochemical SP method.Results The activity of hepatic AST enzyme in model group were (126 ±24),(967 ±30),(1010 ±35) and (206 ±23) U · L-1 in 1st,2nd,3rd and 4th weeks,respectively.Compared with the control group (112 ±22) U · L-1,the activity of hepatic AST enzyme in the model group increased continuouslyfrom 1st to 3rd weeks and reached the peak at 3rd week with significantly (P < 0.01),which was decreased at the 4th week,but still higher than the control group with significantly (P <0.05).The number of CYP2E1 positive cells per square millimeter were (3.2 ±0.8),(8.4 ± 1.1),(13.2 ± 1.3),and (4.6±0.8) cell · mm-2 in 1st,2nd,3rd and 4th weeks.Compared with the control group (2.8 ±0.5) cell ·mm-2,the number were obviously increased in 1st,2nd and 3rd weeks and represented statistically significant (P <0.01)while the number of the 4th week decreased but still with statistically significant(P <0.05).Conclusion The expression of CYP2E1 was increased first and then decreased in alcohol-induced liver injury model,which was consistent with the trend of serum AST enzyme activity.The dynamic changes in expression may be associated with damage and repair of the hver.
9.Cryptosporidium spp., Giardia intestinalis, and Enterocytozoon bieneusi in Captive Non-Human Primates in Qinling Mountains.
Shuai Zhi DU ; Guang Hui ZHAO ; Jun Feng SHAO ; Yan Qin FANG ; Ge Ru TIAN ; Long Xian ZHANG ; Rong Jun WANG ; Hai Yan WANG ; Meng QI ; San Ke YU
The Korean Journal of Parasitology 2015;53(4):395-402
Non-human primates (NHPs) are confirmed as reservoirs of Cryptosporidium spp., Giardia intestinalis, and Enterocytozoon bieneusi. In this study, 197 fresh fecal samples from 8 NHP species in Qinling Mountains, northwestern China, were collected and examined using multilocus sequence typing (MLST) method. The results showed that 35 (17.8%) samples were positive for tested parasites, including Cryptosporidium spp. (3.0%), G. intestinalis (2.0%), and E. bieneusi (12.7%). Cryptosporidium spp. were detected in 6 fecal samples of Macaca mulatta, and were identified as C. parvum (n=1) and C. andersoni (n=5). Subtyping analysis showed Cryptosporidium spp. belonged to the C. andersoni MLST subtype (A4, A4, A4, and A1) and C. parvum 60 kDa glycoprotein (gp60) subtype IId A15G2R1. G. intestinalis assemblage E was detected in 3 M. mulatta and 1 Saimiri sciureus. Intra-variations were observed at the triose phosphate isomerase (tpi), beta giardin (bg), and glutamate dehydrogenase (gdh) loci, with 3, 1, and 2 new subtypes found in respective locus. E. bieneusi was found in Cercopithecus neglectus (25.0%), Papio hamadrayas (16.7%), M. mulatta (16.3%), S. sciureus (10%), and Rhinopithecus roxellana (9.5%), with 5 ribosomal internal transcribed spacer (ITS) genotypes: 2 known genotypes (D and BEB6) and 3 novel genotypes (MH, XH, and BSH). These findings indicated the presence of zoonotic potential of Cryptosporidium spp. and E. bieneusi in NHPs in Qinling Mountains. This is the first report of C. andersoni in NHPs. The present study provided basic information for control of cryptosporidiosis, giardiasis, and microsporidiosis in human and animals in this area.
Animals
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China
;
Cryptosporidiosis/*parasitology
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Cryptosporidium/classification/genetics/*isolation & purification
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Enterocytozoon/classification/genetics/*isolation & purification
;
Feces/parasitology
;
Female
;
Genotype
;
Giardia lamblia/classification/genetics/*isolation & purification
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Giardiasis/parasitology/*veterinary
;
Male
;
Microsporidiosis/parasitology/*veterinary
;
Molecular Sequence Data
;
Phylogeny
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Primate Diseases/*parasitology
;
Primates/classification/parasitology
10.Influence of empathy nursing on depressive emotion and life function of glioma patients with depression
Hai-Hua YAN ; San-Tao ZHANG ; Yin-Xian LI ; Li-Xue WANG
Chinese Journal of Modern Nursing 2013;19(19):2267-2269
Objective To study the influence of empathy nursing on depressive emotion and life function of glioma patients with depression.Methods Totals of 94 glioma patients with depression between April 2006 and December 2012 were divided into two groups.Fifty-one cases in the experimental group accepted empathy nursing,while 43 cases in the control group accepted regular nursing.Compared and analyzed the Hamilton depression scale (HAMD) score,nurses' observation scale for inpatient evaluation (NOSIE) score and satisfaction for the nursing job of the two groups.Results Before the intervention,difference of HAMD score between two groups was not statistically significant [(27.1 ± 5.2) vs (26.9 ± 5.0) ; t =0.190,P > 0.05].After the intervention,HAMD score of the experimental group was obviously better than that of the control group [(16.3 ± 2.9) vs (21.1 ± 2.5) ; t =8.618,P < 0.05].Before the intervention,the difference of social competence,social interest,personal hygiene and depression scores between the two groups was not statistically significant [(16.29±3.18),(17.52 ±3.48),(13.98±2.84),(10.24 ±2.12) vs (16.43 ±3.07),(17.56 ±3.63),(14.13 ±2.91),(10.29 ±2.23);t=0.217,0.054,0.252,0.111;P>0.05)].After the intervention,the above ratings of experimental group was significantly better than that of the control group [(9.81±2.08),(8.69±1.87),(6.61 ±1.97),(4.82 ±1.37) vs (13.29 ±1.94),(12.63 ±2.58),(8.84 ± 2.35),(6.98 ± 1.99) ; t =8.382,8.337,4.931,6.016 ; P < 0.05)].The total score of nursing job satisfaction in the experimental group was significantly better than that of the control group [(120.59 ± 9.48) vs (112.78 ± 10.05) ; t =3.852,P < 0.05)].Conclusions Empathy nursing can improve the depressive emotion and life function of glioma patients with depression,which can also improve the satisfaction of patients with the nursing job.

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