1.The in vitro anti-atherosclerotic activity of compound IMB-1680.
Tingting FENG ; Yongzhen LI ; Ni LI ; Chang LIU ; Xiao WANG ; Yanni XU ; Shuyi SI
Acta Pharmaceutica Sinica 2014;49(5):602-7
In the previous study, a high-throughput screening method was established to find the antagonists of CD36. In the present study, a new compound named IMB-1680 was found using this method. The anti-atherosclerotic activities of IMB-1680 were then evaluated. Dose-dependent activities of IMB-1680 were detected by using Sf9 [hCD36] and CHO [hCD36] models. Fluorescence microscopic photography and flow cytometry were used to analyze uptake of mLDL. Foam cell test with RAW264.7 macrophages was used to examine lipid accumulation. The results showed that IMB-1680 inhibited CD36 activity with IC50 of 2.80 and 8.79 micromol x L(-1) in Sf9[hCD36] and CHO [hCD36] cells, respectively. Fluorescence microscopic photography and flow cytometry revealed that IMB-1680 could significantly reduce DiI-AcLDL uptake. Meanwhile, IMB-1680 also could reduce lipids accumulation in RAW264.7 macrophages. In all, the data indicated that IMB-1680 might be a potent effective anti-atherosclerotic leading compound.
2.The in vitro anti-atherosclerotic activity of compound IMB-1680.
Ting-Ting FENG ; Yong-Zhen LI ; Ni LI ; Chang LIU ; Xiao WANG ; Yan-Ni XU ; Shu-Yi SI
Acta Pharmaceutica Sinica 2014;49(5):602-607
In the previous study, a high-throughput screening method was established to find the antagonists of CD36. In the present study, a new compound named IMB-1680 was found using this method. The anti-atherosclerotic activities of IMB-1680 were then evaluated. Dose-dependent activities of IMB-1680 were detected by using Sf9 [hCD36] and CHO [hCD36] models. Fluorescence microscopic photography and flow cytometry were used to analyze uptake of mLDL. Foam cell test with RAW264.7 macrophages was used to examine lipid accumulation. The results showed that IMB-1680 inhibited CD36 activity with IC50 of 2.80 and 8.79 micromol x L(-1) in Sf9[hCD36] and CHO [hCD36] cells, respectively. Fluorescence microscopic photography and flow cytometry revealed that IMB-1680 could significantly reduce DiI-AcLDL uptake. Meanwhile, IMB-1680 also could reduce lipids accumulation in RAW264.7 macrophages. In all, the data indicated that IMB-1680 might be a potent effective anti-atherosclerotic leading compound.
Animals
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CD36 Antigens
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antagonists & inhibitors
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genetics
;
metabolism
;
CHO Cells
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Cells, Cultured
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Cricetulus
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Dose-Response Relationship, Drug
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Foam Cells
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cytology
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High-Throughput Screening Assays
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Humans
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Lipoproteins, LDL
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metabolism
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Macrophages
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cytology
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metabolism
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Mice
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Molecular Structure
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Plasmids
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Receptors, Scavenger
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antagonists & inhibitors
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Sf9 Cells
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Spodoptera
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Transfection
3.Test and verify of piping cleaning effect in infusion solution productive process
Xiao-Fang WU ; Fu-Yu HUANG ; Chang-Si FENG ; Liu-Hua PAN
Journal of Pharmaceutical Practice 2001;19(2):83-85
OBJECTIVE:To test and verify the piping cleaning effect in infusion solution productive process.METHODS:Targets of final washing water of pipe were determined.RESULTS:Targets of final washing water of pipe were that electrical conductivity of entrance of pipe was equal to that of exit of pipe essentially,limitation of bacteria and endotoxin were as follows:<50CFU/ml,<0.25EU/ml.CONCLUSIONS:According to the clean rules laid down by pharmaceutical Factory of Shanquan,Jinan,The desired cleaning effect of the pipe of infusion solution can be achieved.
4.Insulin protects isolated hearts from ischemia/reperfusion injury: cross-talk between PI3-K/Akt and JNKs.
Hai-Tao LIU ; Hai-Feng ZHANG ; Rui SI ; Quan-Jiang ZHANG ; Kun-Ru ZHANG ; Wen-Yi GUO ; Hai-Chang WANG ; Feng GAO
Acta Physiologica Sinica 2007;59(5):651-659
Our previous results have demonstrated that insulin reduces myocardial ischemia/reperfusion (MI/R) injury and increases the postischemic myocardial functions via activating the cellular survival signaling, i.e., phosphatidylinositol 3-kinase (PI3-K)-Akt-endothelial nitric oxide synthase (eNOS)-nitric oxide (NO) cascade. However, it remains largely controversial whether c-Jun NH2-terminal kinase (JNK) is involved in the effects of insulin on MI/R injury. Therefore, the aims of the present study were to investigate the role of JNK, especially the cross-talk between JNK and previously expatiated Akt signaling, in the protective effect of insulin on I/R myocardium. Isolated hearts from adult Sprague-Dawley rats were subjected to 30 min of regional ischemia and followed by 2 or 4 h of reperfusion (n=6). The hearts were pretreated with PI3-K inhibitor LY294002, or phosphorylated-JNK inhibitor SP600125, respectively, then perfused retrogradely with insulin, and the mechanical functions of hearts, including the heart rate (HR), left ventricular developed pressure (LVDP) and instantaneous first derivation of left ventricular pressure (+/-LVdp/dt(max)) were measured. At the end of reperfusion, the infarct size (IS) and apoptotic index (AI) were examined. MI/R caused significant cardiac dysfunction and myocardial apoptosis (strong TUNEL-positive staining). Compared with the control group, insulin treatment in MI/R rats exerted protective effects as evidenced by reduced myocardial IS [(28.9 +/- 2.0)% vs (45.0 +/- 4.0) %, n=6, P<0.01], inhibited cardiomyocyte apoptosis [decreased AI: (16.0 +/- 0.7) % vs (27.6 +/- 1.3) %, n=6, P<0.01] and improved recovery of cardiac systolic/diastolic function (including LVDP and +/-LVdp/dt(max)) at the end of reperfusion. Moreover, insulin resulted in 1.7-fold and 1.5-fold increases in Akt and JNK phosphorylation in I/R myocardium, respectively (n=6, P<0.05). Inhibition of Akt activation with LY294002 abolished, and inhibition of JNK activation with SP600125 enhanced the cardioprotection by insulin, respectively. And the abolishment by LY294002 could be partly converted by SP600125 pretreatment. In addition, SP600125 also decreased the Akt phosphorylation (n=6, P<0.05). These results demonstrate that insulin simultaneously activates both Akt and JNK, and the latter further increases the phosphorylation of Akt which attenuates MI/R injury and improves heart function; this cross-talk between Akt and JNK in the insulin signaling is involved in insulin-induced cardioprotective effect.
Animals
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Apoptosis
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Heart
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Insulin
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metabolism
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JNK Mitogen-Activated Protein Kinases
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MAP Kinase Signaling System
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Myocardial Infarction
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Myocardial Ischemia
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Myocardial Reperfusion Injury
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Myocardium
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Myocytes, Cardiac
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Nitric Oxide Synthase Type III
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Phosphatidylinositol 3-Kinase
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metabolism
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Phosphatidylinositol 3-Kinases
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metabolism
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Phosphorylation
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Proto-Oncogene Proteins c-akt
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Rats
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Rats, Sprague-Dawley
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Reperfusion Injury
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Signal Transduction
5.The effect of autogenous vein cuff and injection of cerebral cell growth peptide on the recovery of injured facial nerve.
Si-yuan HAN ; Yong-feng GUO ; Yu-xin WANG ; Chang-fu SUN
Chinese Journal of Plastic Surgery 2003;19(6):420-422
OBJECTIVETo study the effect of autogenous vein cuff and injection of cerebral cell growth peptide on the recovery of the injured facial nerve.
METHODSThe injured facial nerve was anastomosed and covered with an autogenous vein cuff. Cerebral cell growth peptide was then injected to it. The different repairing methods were evaluated and compared with electromyography and observing functional recovery of the mimetic muscles.
RESULTSThe new repairing method accelerated the recovery of the injured facial nerve. The recovery period of mimetic muscle function was significant shorter than the traditional method (P < 0.01). The recovery period of I-stage repairing was significant shorter than that of II--stage repairing (P < 0.01). The conduction velocity of the repaired facial nerves had no obvious differences between the new repairing method and the traditional method (P > 0.05).
CONCLUSIONApplication of the autogenous vein cuff to cover the nerve anastomosis and injection of cerebral cell growth peptide is a promising method for facial nerve repairing.
Adolescent ; Adult ; Aged ; Child ; Facial Nerve ; physiopathology ; Facial Nerve Injuries ; physiopathology ; surgery ; Female ; Growth Substances ; administration & dosage ; Humans ; Male ; Middle Aged ; Neural Conduction ; Veins ; transplantation
6.Fetal/maternal multi-parameter monitor.
Yao-sheng LU ; Hui-jin WANG ; Guang-chang LIU ; Si-hua WANG ; Jing-bo RONG ; Ge LIANG ; Jun-feng PAN
Chinese Journal of Medical Instrumentation 2002;26(2):100-102
A fetal/maternal multi-parameter monitor is introduced here in the paper. It can monitor the vital signs of a fetus and his/her mother in a same screen synchronously. It is more useful in obstetric clinics. Its other functions include management of patient file, computer-assistant analyses.
Adult
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Automatic Data Processing
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instrumentation
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Electrocardiography, Ambulatory
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instrumentation
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Equipment Design
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Female
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Fetal Monitoring
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instrumentation
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Heart Rate, Fetal
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Humans
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Microcomputers
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Monitoring, Ambulatory
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instrumentation
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Pregnancy
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Signal Processing, Computer-Assisted
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Software
7.Relationships between the gene polymorphisms of drug metabolizing enzymes and the outcome of the first induction chemotherapy in patients with de novo acute myeloid leukemia.
Na WANG ; Jun-Ling HAN ; Ying-Chang MI ; Zhi-Jian XIAO ; Si-Zhou FENG ; Yu-Ling ZHOU ; Jian-Xiang WANG ; Ming-Zhe HAN
Journal of Experimental Hematology 2011;19(2):327-331
The objective of this study was to investigate the correlation between the gene polymorphisms of drug metabolizing enzymes and the outcome of the first induction chemotherapy in patients with de novo acute myeloid leukemia (AML). 113 de novo AML patients were enrolled in this study. The genotypes of 11 single nucleotide polymorphisms (SNP) in drug metabolizing enzymes were detected by the SNPstream(®) Genotyping System. The correlation between the distribution of genotypes and the complete remission rate of first induction chemotherapy was analyzed by logical regression. The results showed that patients with variant genotype of CYP2D6 (rs16947) had a lower complete remission (CR) rate, as compared to those with wild type (p = 0.033, OR = 0.32, 95%CI 0.112 - 0.915); meanwhile the patients with variant genotype of GSTO2 (rs156697) had a higher CR rate as compared to those with wild type (p = 0.011, OR = 3.023, 95%CI 1.289 - 7.089). Combined analysis of the above polymorphisms, showed that patients with variant genotype of CYP2D6 and wild genotype of GSTO2 (V + W) had lower CR rates in comparison to patients with wild genotypes of both polymorphisms (p = 0.017, OR = 0.183, 95%CI 0.045 - 0.735). It is concluded that CYP2D6 (rs16947) and GSTO2 (rs156697) polymorphisms are independent factors influencing CR rates of the first induction chemotherapy in de novo AML patients.
Adolescent
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Adult
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Aged
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Antineoplastic Agents
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therapeutic use
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Child
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Cytochrome P-450 CYP2D6
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genetics
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Female
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Genotype
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Glutathione Transferase
;
genetics
;
Humans
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Leukemia, Myeloid, Acute
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drug therapy
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enzymology
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genetics
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Male
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Middle Aged
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Polymorphism, Single Nucleotide
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Remission Induction
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Treatment Outcome
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Young Adult
8.Study on the mechanism of acupoint sticking therapy with Chuan fuling for treatment of asthma model rats.
Xi-xiong XIANG ; Jing-ying ZHANG ; Yin-mei SI ; Chang-yu LIU ; Yan-fang LU ; Xiao-ying LIU ; Wang-xi CAI ; Han-ge FENG
Chinese Acupuncture & Moxibustion 2009;29(9):739-743
OBJECTIVETo investigate the mechanism of the acupoint sticking therapy with Chuanfuling for preventing and treating asthma.
METHODSThirty male SD rats were randomly divided into a control group (normal saline, p.i. +no acupoint sticking+ normal saline, spray inhalation), model group (normal saline with ovalbumin, p.i. +no acupoint sticking+ normal saline with ovalbumin, spray inhalation), and acupoint sticking group (normal saline with ovalbumin, p.i. +acupoint sticking with Chuan fuling+normal saline with ovalbumin, spray inhalation), 10 rats in each group. The incubation period of nodding breath, symptom of asthmatic attack, expression level of interleukin-4 mRNA (IL-4 mRNA) and interferon-gamma mRNA (IF-gamma mRNA), as well as pathological changes on the middle leaf of right lung, were observed in each group.
RESULTS(1) Comparing with the control group, the model group was showed that the expression level of IL-4 mRNA in the peripheral blood cells (PBMC) was increased, while hyperemia, edema and eosinocyte (EOS) invasion of lung tissue was more serious (P < 0.01). (2) Comparing with the model group, the acupoint sticking group was showed that the expression level of IL-4 mRNA in PBMC was decreased, the incubation period of nodding breath was prolonged for induced asthma on the fifth and seventh time with lower frequency, while in the lung tissue EOS invasion was reduced (P < 0.05), but there were no significant changes on the hyperemia and edema (P > 0.05).
CONCLUSIONAcupoint sticking for treating asthma of model rats with Chuanfuling can inhibit the expression level of IL-4 mRNA in PBMC, and the release of the inflammatory mediator and cytokine from the EOS to the air passage, in order to reduce the injury of epithelial layer and high reaction on the air passage.
Acupuncture Points ; Animals ; Asthma ; drug therapy ; genetics ; immunology ; Disease Models, Animal ; Drugs, Chinese Herbal ; therapeutic use ; Gene Expression ; drug effects ; Humans ; Interleukin-4 ; genetics ; immunology ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley
9.G protein?coupled estrogen receptor reduces renal ischemia?reperfusion injury by improving diastolic function of renal interlobular artery
Yuechen CHANG ; Ziwei HAN ; Ying ZHOU ; Yang ZHANG ; Ziyi FENG ; Ketao MA ; Zhiqin ZHANG ; Li LI ; Junqiang SI
Chinese Journal of Nephrology 2018;34(11):838-844
Objective To investigate the effect of G protein?coupled estrogen receptor (GPER) on the diastolic function of renal interlobular artery and reduce renal ischemia?reperfusion injury in rats. Methods Female ovariectomized rats were divided into control group; ischemia?reperfusion injury (IRI) group;GPER?specific agonist (G1) intervention group;GPER?specific blocker+GPER?specific agonist (G15+G1) intervention group. Histopathological examination (HE staining), renal function test and Paller score were used to identify the success of the model and the degree of kidney damage. In vitro microvascular pressure diameter measuring instrument was used to detect the relaxation and contraction activity of renal interlobular artery in each group. Immunofluorescence technique was used to observe the expression of GPER on the renal interlobular artery. Westernblotting was used to detect the expression of GPER protein in renal interlobular artery of rats in each group. The NO content was determined by a nitrate reductase method. Results Compared with IRI group, serum BUN, Scr level and Paller score in G1 intervention group were significantly decreased (all P<0.05). The systolic rate of renal interlobar artery was significantly increased [(40.76 ± 1.57)% vs (29.78 ± 1.87)%, P<0.05]. The results of immunofluorescence showed that GPER was expressed in renal interlobular artery smooth muscle cells and endothelial cells, and the expression of IRI group was higher than that of the control group. The expression of G15+G1 intervention group was lower than that of G1 intervention group (all P<0.05). Compared with the IRI group, the NO content in the G1 intervention group increased significantly (all P<0.05). Conclusions During renal ischemia ?reperfusion injury, GPER may regulate the systolic and diastolic activity of the renal interlobar artery by increasing the content of NO, so as to alleviate the renal ischemia?reperfusion injury.
10.Association between single nucleotide polymorphisms of 5'-untranslated region of GPx4 gene and male infertility.
Shu-yuan LIU ; Chang-jun ZHANG ; Xiao-min SI ; Yu-feng YAO ; Lei SHI ; Jin-kun KE ; Liang YU ; Li SHI ; Zhao-qin YANG ; Xiao-qin HUANG ; Hao SUN ; Jia-you CHU
Chinese Journal of Medical Genetics 2011;28(3):270-274
OBJECTIVETo study the association between the single nucleotide polymorphisms (SNPs) of the 5'-untranslated region (5'-UTR) of phospholipid hydroperoxide glutathione peroxidase (GPx4 or PHGPx) gene and oligo- or asthenozoospermic male infertility.
METHODSThe 5'-UTR region of the GPx4 gene was amplified from infertile men and controls using the polymerase chain reaction and was analyzed for polymorphisms by direct sequencing.
RESULTSA total of 9 SNPs were present in the cohort, however there were no significant differences in these 9 SNPs between the case and control groups. According to the results of linkage disequilibrium analysis and haplotype construction, one haplotype (rs757229-rs757230-rs4588110-rs3746165-rs3746166: C-G-G-T-A) was present only in the control men, and significant difference was detected(P< 0.01).
CONCLUSIONThe SNPs of 5'-UTR region of the GPx4 gene might not be associated with oligo- or asthenozoospermic male infertility. However, the haplotype (rs757229-rs757230-rs4588110- rs3746165-rs3746166: C-G-G-T-A) might be a protective haplotype.
5' Untranslated Regions ; genetics ; Adult ; Alleles ; Gene Frequency ; Genotype ; Glutathione Peroxidase ; genetics ; Humans ; Infertility, Male ; genetics ; Linkage Disequilibrium ; genetics ; Male ; Middle Aged ; Polymorphism, Single Nucleotide ; genetics ; Young Adult