1. The in vitro stability and proteolytic enzyme of synthesized protamine-analog peptide R15
Journal of International Pharmaceutical Research 2018;45(4):295-300
Objective: To establish an ultra performance liquid chromatography(UPLC)method for determination of prot- amine peptide analogul(R15),and investigate the metabolism in biological samples of R15 in vitro by the method. Methods: Chro- matographic separation was performed by pumping the mobile phase into a BioBasic C 18 (2.1 mm×100 mm,5 μm). The mobile phase was composed of 0.05% trifluoroacetic acid-water and 0.05% trifluoroacetic acid acetonitrile(98:2,V/V),using 10% trifluoroacetic ac- id-acetonitrile-water as precipitant. The stability of R15 in rat whole blood,liver and kidney homogenate was studied. Results: The in- tra-and inter-batch relative standard deviations (RSD)were less than 15%,the relative errors (RE)were in the range of ±15%. The range of calibration curve was 25-1000 μg/ml with a good correlation coefficient. The extraction recoveries of R15 were 99.43-100.43%. R15 was stable under various experimental storage conditions. Half-lives of R15 in rat liver,rat kidneys,rat blood,beagle dog blood and human blood were 27.4 min,9.1 min,15.6 min,11.9 min and 21.0 min,respectively. Compared with the control group without inhibi- tor,the inhibitory rates of EDTA,pepstatin and benzamidine HCl protease inhibitor in the experimental group was 92.7%,41.3% and 33.0%,respectively. Protamine analogue peptide was mainly metabolized by metal carboxyl peptidases. Compared with the control group,AEBSF,leupeptin and trypsin protease inhibitors had significant difference,but the inhibitory rate was low. Conclusion: The method is specific,sensitive,accurate and reliable. The metabolism of R15 in rat kidney is the fastest. The degradation of R15 in whole blood is possibly related to metal carboxypeptidase.
2.The Study on the Relationship between Diet Intake and Impaired Glucose Metabolism in Adult Residents in Guangxi
Zheng-Zhu TANG ; Xing-Le CHEN ; Zhao-Yong HUANG
Chinese Journal of Prevention and Control of Chronic Diseases 2006;0(06):-
Objective To explore the relationship between diet intake and diabetes mellitus(DM) and impaired fasting glucose (IFG) in adult residents in Guangxi,so as to provide scientific basis for dietary prevention.Methods 2 281 people(1 020 from urban areas and 1 261 from rural areas) aged 18 years and above were selected from 4 cities and 4 countrysides in Guangxi through a multistage stratified random sampling.The investigation included the meal investigation,medical examination and blood assay. Results Total 37 people(26 from urban and 11 from rural) suffered from DM and 26 people(15 from urban and 11 from rural) had IFG,the general prevalence rate of Impaired Glucose Metabolism(IGM) was 2.8%(4.0% for urban and 1.7% for rural);It showed that the prevalence of IGM in city was obviously higher than that in the countryside(P
3.Analysis of position of one-piece soft intraocular lens after implantation of intraocular lens with Pentacam
Chun-lei, LIU ; Fang, HUANG ; A-yong, YU ; Shuang-qian ZHU ; Yi-le, XU ; Qin-mei, WANG
Chinese Journal of Experimental Ophthalmology 2011;29(10):913-917
Background The aspheric intraocular lenses(IOLs)can reduce ocular spherical aberration to some degree.However,the clinical effect depends more on the IOL proper alignment.It becomes more important to study the IOL position in eye,Objective This study was to analyze the position alteration of IOL after phacoemulsification combined with implantation of one-piece soft IOLs.Methods In this prospective control study,80 eyes of 40 patients with age-related cataract were enrolled.The phacoemulsification with IOL implantation was performed in all the eyes.Decentration and tilt of IOL in the nasal superior,superior temporal,inferior temporal and nasal inferior quadrants(the intersection point of the system optical axis and the IOL maximum cross plane were regarded as the ordinate origin)were measured by rotating Scheimpflug camera(Pentacam Oculus)in 3 months postoperatively under the mydriasis condition.Written informed consent was obtained from each subject prior to this trial.Results In the right eye group,the IOL decentered toward temporal in 26 eyes(65%)and infratemporal in 16 eyes(40%).IOLs tilted temporally in the horizontal plane in 37 eyes(92.5%)and tilted inferiorly in the vertical plane in 34 eyes(85.0%).In the left eye group,IOLs decentered temporally 33 eyes(82.5%)and 20 IOLs (50%)infratemporally,IOLs tilted temporally in the horizontal plane in 37 eye(92.5%)and 36 IOLs(90%)tilted inferiorly in the vertical plane.There was no statistical difference for the intercomparsion of horizontal/vertical decentration in various quadrant in the right eye(F =0.221,0.792,P>0.05).The obvious elevated horizontal decentration was found in the supertemporal and infratemporal quadrants compared with supernasal quadrant in the left eyes but there was no significant difference in the vertical decentration among 3 quadrants(F=0.576,P>0.05).Decentrations were positively correlated with the tilt in both horizontal and vertical plane(right eye horizontal plane:r=0.374,P=0.002;right eye vertical plane:r=0.402,P=0.001 ;left eye horizontal plane:r=0.377,P=0.002;left eye vertical plane:r=0.347,P=0.002).Conclusions The one-piece soft IOLs(Adapt AO)decenter toward temporal mostly in 3 months after surgery,especially infratemporally in the eye.And the optical axis of the IOL tilt toward infratemperol mostly in both right and left eyes.The decentration and tilt are consisted in the corresponding direction between the right and left eyes.The position of the IOLs showed mirror symmetry between right and left eyes.The IOLs decentration show the positively correlation to tilt whatever in horizontal and vertical plane.
4.A novel biologic for the treatment of moderate to severe asthma:Tezepelumab
Guo-Zhu BAI ; Xi-Le MU ; Ru-Han A ; Yang-Tao WU ; Yong-Xia BAI
The Chinese Journal of Clinical Pharmacology 2024;40(5):741-744
Tezepelumab(AMG 157/MEDI9929)is a human monoclonal antibody against the epithelial cell-derived cytokine thymic stromal lymphopoietin(TSLP).It is primarily used to treat moderate to severe asthma,particularly in patients with a non-eosinophilic inflammatory phenotype,whose asthma remains uncontrolled despite the use of long-acting beta-agonists and moderate to high doses of inhaled glucocorticoids.This article will summarise the mechanism of action,clinical trial efficacy and safety and tolerability of Tezepelumab in order to provide a comprehensive understanding of the drug and inform clinical work.
5.A novel method for testing sterility of injections based on biothermodynamics.
Dan GAO ; Dan GAO ; Yong-Shen REN ; Dan YAN ; Cong-En ZHANG ; Zhu-Yun YAN ; Yin XIONG ; Li-Na MA ; Le-Le ZHANG ; Xiao-He XIAO
Acta Pharmaceutica Sinica 2014;49(3):385-391
This study aims at trying to establish a novel method of sterility test for injections based on biothermodynamics, in order to overcome the deficiencies of routine sterility tests such as long detecting cycle, low sensitivity and prone to misjudgments. A biothermodynamics method was adopted to rapidly detect the microorganism contamination of injections by monitoring the heat metabolism during the growth of microbe. The growth rate equal to or greater than zero and the heat power difference of P(i) and P(0) with three folds higher than the noise of baseline were chosen as indexes to study the heat change rule of microbe. In this way, the effectiveness of the new method to detect strains required by conventional sterility test or in injection samples was also investigated. Results showed that the Gram-positive bacteria, Gram-negative bacteria and fungi demanded by sterility testing methodology could be detected by biothermodynamics method within 10 hours, with the sensitivity lower than 100 CFU x mL(-1). Meanwhile, this method was successfully applied to the sterility test of Compound Yinchen injection (FFYC), Shuanghuanglian powder injection (SHL) and Compound Triamcinolone injection (TAND) which were sterilized with different degrees. Therefore, the biothermodynamics method, with advantages of fast detection and high sensitivity, could be a complementary solution for conventional sterility tests.
Anti-Inflammatory Agents
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administration & dosage
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chemistry
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Drug Contamination
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Drugs, Chinese Herbal
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administration & dosage
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chemistry
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Fungi
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isolation & purification
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Gram-Negative Bacteria
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isolation & purification
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Gram-Positive Bacteria
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isolation & purification
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Hot Temperature
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Injections
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Microbiological Techniques
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methods
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Sensitivity and Specificity
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Sterilization
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Triamcinolone
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administration & dosage
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chemistry
6.Treatment of orbital venous malformations with intralesional injection of bleomycin lipiodol emulsion
Yong CHEN ; Yan-Hao LI ; Xiao-Feng HE ; Wei LU ; Qing-Le ZENG ; Jian-Bo ZHAO ; Qiao-Hua ZHU ;
Chinese Journal of Radiology 1999;0(10):-
5 mm and ≤8 mm in 4 cases.The mean value was 4.2 mm. Four patients noticed reduction in their vision and two had diplopia.Those patients were examined by CT or MR.Direct venography was performed in each patient.After the diagnosis of OVM was confirmed, intralesional injection of BLE was performed.The efficacy of the treatment and complications were observed during the following 8 to 42 months(mean 23 months).Results The BLE were successfully injected in all the patients.All patients had resolution of proptosis and diplopia.Three patients gained improvement of visual acuity.The periorbital swelling occurred in all patients after operation and resolved within 1 week without special treatment.Other complications,such as orbital hemorrhage and periorbital scar,were not observed during following-up.Conclusion Intralesional injection with BLE is convenient,safe and efficient for the treatment of OVM.
7.Investigation of ulinastatin on protection of organ functions in patients with severe disease
Fei WU ; Xiao-Yun YU ; Yong LEI ; Jian-Ming ZHU ; Yan GAO ; Wen ZHU ; Ai-Rong LI ; Xiao-zhen WAN ; Mei-cheng LE
Chinese Journal of Integrated Traditional and Western Medicine in Intensive and Critical Care 2006;0(05):-
Objective To study the mechanism and protection of ulinastatin on organ functions in patients with severe disease.Methods Sixty patients in the intensive care unit(ICU)from October 2005 to July 2007 were randomly divided into a control group and an ulinastatin treatment group(each 30 cases).The patients in the control group received the conventional therapy,and the cases in the other treatment group accepted ulinastatin and conventional therapy.According to the disease situations,ulinastatin was administered 200-400 kU once,2-4 times a day,sequentially for 5-7 days.On the day of admission and 3, 5,and 7 days after admission in ICU respectively,blood samples were obtained for measuring alanine aminotransferase(ALT),aspartate aminotransferase(AST),creatinine(Cr),blood urea nitrogen(BUN), activated partial thromboplastin time(APTT),fibrinogen(FIB)and oxygenation index(PaO_2/FiO_2); whether breathing machine or hematodialysis was used and the end results were recorded.Results The rate of usage of breathing machine(23.3%),the incidences of hepatosis(3.3%)and renal dysfunction(10.0%) and fatality(3.3%)in ulinastatin treatment group were obviously lower than those of the control group (63.3%,23.3%,46.7%,10.0%,P0.05).Only one patient received bematodialysis in control group.Conclusion Ulinastatin can protect liver,renal and lung functions markedly and lower the incidence of multiple organ dysfunction syndrome and mortality in patients with severe disease.
8.Vinculin and the androgen receptor in prostate cancer: expressions and correlations.
Li-yong ZHU ; Kuang-biao ZHONG ; Shen-xiu LU ; Le-ye HE
National Journal of Andrology 2010;16(9):794-798
OBJECTIVETo investigate the expressions of vinculin (VCL) and the androgen receptor (AR) in benign prostatic hyperplasia (BPH) and prostate cancer (PCa) and analyze their relationship with the clinical stage and pathological grade of PCa and the level of PSA.
METHODSWe detected the expressions of VCL and AR in 18 cases of BPH and 38 cases of PCa by immunohistochemistry, analyzed the differences of VCL and AR expressions in BPH and PCa in different clinical stages and pathological grades of PCa, compared the primary levels of PSA, and studied their correlations.
RESULTSThe positive rate of VCL was significantly higher in PCa than in BPH tissues (P < 0.05), while that of AR showed no significant differences between the two groups (P > 0.05). Both the expressions of VCL and AR were closely related with the clinical stage and pathological grade of PCa (P < 0.05), but not with the PSA level (P > 0.05). There was a positive correlation between the expressions of VCL and AR in PCa tissues (r = 0.489, P < 0.05).
CONCLUSIONVCL is expressed differently in BPH and PCa, which may serve as an indicator for the differential diagnosis of benign and malignant prostate diseases. The expressions of AR and VCL are gradually reduced with the progression of PCa, with a positive correlation between them, and could be used jointly to evaluate the progression and prognosis of PCa.
Aged ; Aged, 80 and over ; Humans ; Male ; Middle Aged ; Prostatic Hyperplasia ; metabolism ; pathology ; Prostatic Neoplasms ; metabolism ; pathology ; Receptors, Androgen ; metabolism ; Vinculin ; metabolism
9.Expression and significance of P-gp/mdr1 mRNA, MRP and LRP in non-Hodgkin's lymphoma.
Le LI ; Li-ping SU ; Li MA ; Jin ZHAO ; Lei ZHU ; Yong-an ZHOU
Chinese Journal of Oncology 2009;31(3):199-202
OBJECTIVETo explore the expression and clinical significance of P-glycoprotein (P-gp)/mdr1mRNA, multidrug resistance-associated protein (MRP) and lung resistance protein (LRP) in newly diagnosed non-Hodgkin's lymphoma.
METHODSmdr1 mRNA of in 41 patients with non-Hodgkin's lymphoma was assayed by semi-quantitative RT-PCR. The expressions of P-gp, MRP and LRP proteins in lymph node viable blasts were identified by flow cytometry. The results were compared with those obtained from control cases, and the correlation of the changes with clinical outcomes was analyzed.
RESULTS(1) Among the 41 cases, the positive expression of P-gp protein was detected in 8 cases, MRP in 7 cases, LRP in 15 cases, and mdr 1 mRNA in 11 cases. (2) The P-gp and LRP levels in NHL were significantly higher than those in control group, but MRP wasn't. The P-gp over-expression was significantly associated with mdr1mRNA (r = 0.396, P = 0.01). No correlation was showed among the expressions of P-gp, MRP and LRP. (3) Patients with P-gp expression had a poorer outcome of chemotherapy than those with P-gp-negative (P = 0.005). P-gp expression was significantly associated with higher clinical stage (P = 0.046) and elevated serum lactate dehydrogenase level (P = 0.032), but not associated with malignant degree (P = 0.298). MRP had no impact on the outcome of chemotherapy (P = 0.212), and wasn't significantly associated with higher clinical stage (P = 0.369), elevated LDH (P = 0.762) and higher malignant degree (P = 0.451). Patients with LRP expression had a poorer outcome of chemotherapy than those LRP-negative (P = 0.012). LRP expression was significantly associated with higher clinical stage (P = 0.0019), elevated LDH (P = 0.02) and higher malignant degree (P = 0.01).
CONCLUSIONThe data of this study indicate that P-gp and LRP expressions but not MRP expression are important in the mechanism of drug resistance associated with a poor clinical outcome in previously untreated NHL.
ATP Binding Cassette Transporter, Sub-Family B ; ATP-Binding Cassette, Sub-Family B, Member 1 ; genetics ; metabolism ; Adolescent ; Adult ; Aged ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Cell Line, Tumor ; Child ; Drug Resistance, Multiple ; Drug Resistance, Neoplasm ; Female ; Humans ; Lactate Dehydrogenases ; blood ; Lymph Nodes ; metabolism ; Lymphoma, Non-Hodgkin ; drug therapy ; metabolism ; pathology ; Male ; Middle Aged ; Multidrug Resistance-Associated Proteins ; metabolism ; Neoplasm Staging ; RNA, Messenger ; metabolism ; Remission Induction ; Vault Ribonucleoprotein Particles ; metabolism ; Young Adult
10.Dietary factors and the risk of neural tube defects: a case-control study in Shanxi province, China.
Zhi-wen LI ; Ai-guo REN ; Le ZHANG ; Zhan-ying GUO ; Yong-sheng JIN ; Zhu LI
Chinese Journal of Epidemiology 2006;27(10):831-835
OBJECTIVEDietary factors that could potentially be related to the risk of birth defects are still unknown in Shanxi province, a region with high prevalence of neural tube defects(NTDs) in China. The main aim of this study was to evaluate the association between NTDs and local dietary factors.
METHODSA population-based case-control study was conducted during 2003-2005 in four selected counties of Shanxi province with 363 NTDs cases ascertained and 523 control babies without any external birth defects.
RESULTSBy multivariate logistic regression analysis, we found the NTDs risk was significantly associated with low consumption of meat and legume, high consumption of pickled vegetables, noncentralized supply of drinking water and drinking tea after adjusting for maternal education level and birth defects history. A significant dose response trend was found between the NTDs risk and the lower frequencies of meat and legume consumption and higher frequency of pickled vegetable consumption, with population attributable risks (PAR) of 69.4%, 22.0% and 18.5%, respectively. Mothers who got their drinking water from river or pond during periconceptional period were more likely to have a NTD-affected pregnancy [OR = 3.42, 95% CI: 1.44-8.09, population attributable risk (PAR) = 4.7%] compared with those who utilized tap or well water. Those who drank tea everyday had an elevated risk of having a NTD-affected pregnancy compared with those who didn't (OR = 4.65, 95% CI: 1.41-15.36, PAR = 2.6%).
CONCLUSIONHigher intake of meat and legume protects a woman from having a NTD-affected pregnancy, and consumption of pickled vegetables, drinking water from river or pond and drinking tea everyday increase the risk of having such a pregnancy in the study population.
Case-Control Studies ; China ; epidemiology ; Diet ; Female ; Humans ; Meat ; Neural Tube Defects ; epidemiology ; Pregnancy ; Risk Factors ; Vegetables ; Water Supply