1.Terpenoids and sterols from Ricinus communis and their activities against diabetes.
Shen-Hua LI ; Qing DENG ; Li ZHU ; Chun-Hua LAI ; Heng-Shan WANG ; Qin-Gang TAN
China Journal of Chinese Materia Medica 2014;39(3):448-452
Seven terpenoids and three sterols were isolated from the methanol extracts of the aerial parts of Ricinus communis by chromatography methods and their structures were identified by spectra analysis as ficusic acid( 1), phytol(2), callyspinol(3) , lupeol(4), 30-norlupan-3beta-ol-20-one(5) , lup-20(29)-en-3beta,15alpha-diol(6) , acetylaleuritolic acid( 7), stigmast4-en-3-one(8) , stig-mast-4-en-6beta-ol-3-one(9) , and stigmast4-en-3,6-dione(10). Compounds 1-3 and 5-10 were obtained from this species for the first time and 5 and 6 showed significant inhibitive activity and good selectivity against 11beta-HSD of mouse and human in vitro. [Key words] Ricinus communis; terpenoids; sterols; 11beta-HSD
11-beta-Hydroxysteroid Dehydrogenase Type 1
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antagonists & inhibitors
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11-beta-Hydroxysteroid Dehydrogenase Type 2
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antagonists & inhibitors
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Animals
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Diabetes Mellitus
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drug therapy
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enzymology
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Humans
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Hypoglycemic Agents
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pharmacology
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therapeutic use
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Inhibitory Concentration 50
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Mice
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Ricinus
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chemistry
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Sterols
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pharmacology
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therapeutic use
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Terpenes
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pharmacology
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therapeutic use
2.Quality control of clinical data management based on EDC.
Hong-xia LIU ; Ying-hua LV ; Mao-sheng ZHOU ; Qing-heng MENG ; Jun-chao CHEN ; Ying-chun HE ; Qing-shan ZHENG
Acta Pharmaceutica Sinica 2015;50(11):1470-1473
With the wide application of electronic data management (EDC), the data management is shifting to a new mode. In order to recognize the advantages of EDC, we choose 20 representative registered clinical trials, which involve 5 404 subjects and 321 sites. We found that EDC has many beneficial impacts on the course of clinical trial data management, including the process of data collection, data cleaning, data quality control and clinical trial decision-making. The result also provides a reference for the adoption of EDC in clinical trials.
Clinical Trials as Topic
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Data Collection
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standards
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Information Storage and Retrieval
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standards
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Quality Control
3.Effects of genistein on expression of TGF-beta1 and intracellular free Ca2+ concentration in fibroblasts derived from human hypertrophic scar.
Chuan CAO ; Shi-Rong LI ; Xia DAI ; Zhi FENG ; Shan XIA ; Yan-Qing CHEN ; Heng YAO
Chinese Journal of Plastic Surgery 2008;24(5):335-338
OBJECTIVETo observe the effects of Genistein on TGF-beta1 expression and the intracellular free Ca2+ concentration in human hypertrophic scar fibroblasts, and to discuss the mechanism of the anti-fibrosis effect.
METHODSFibroblasts were derived from human hypertrophic scar tissue and cultured in vitro. Genistein in different concentrations (25, 50, 100 micromol/L) was administrated to the fibroblasts, respectively. After 48 hours of co-culture, the expression of TGF-beta1 mRNA and protein were examined by RT-PCR and Western-Blot assay respectively. The intracellular free Ca2+ concentration in hypertrophic scar fibroblasts pretreated by Genistein was determined by laser confocal scanning microscopy with or without the stimulation of bFGF.
RESULTSGenistein inhibited the expression of TGF-beta1 in hypertrophic scar fibroblasts on a concentration-dependent manner. bFGF significantly elevated the intracellular free Ca2+ concentration, however its stimulating effect was remarkably alleviated when the fibroblasts were pre-treated by Genistein.
CONCLUSIONSGenistein can reduce the expression of TGF-beta1 and block the accumulation of intracellular free calcium induced by growth factors. It maybe one of the possible mechanisms of Genistein's antifibrosis effect.
Calcium ; analysis ; Cells, Cultured ; Cicatrix, Hypertrophic ; metabolism ; Fibroblasts ; drug effects ; metabolism ; Genistein ; pharmacology ; Humans ; Transforming Growth Factor beta1 ; metabolism
4.Study on between magnetic resonance venography and digital subtraction angiography on the inferior vena cava obstructive interface morphology of Budd-Chiari syndrome.
Xin LU ; Kai XU ; Qing-qiao ZHANG ; Chun YANG ; Shao-dong LI ; Jiang-shan LI ; Yu-tao RONG ; Mao-heng ZHU
Chinese Journal of Hepatology 2011;19(12):923-926
OBJECTIVETo evaluate magnetic resonance venography (MRV) in diagnosing obstructive interface morphology of Budd-Chiari syndrome(BCS).
METHODSMRV examination was performed on 44 cases of BCS, and the images of obstructive interface morphology of the inferior vena cava were reviewed by two radiologists.
RESULTSIn all 44 cases, there were 37 cases with complete obstruction and 7 with incomplete obstruction. MRV showed 4 cases with membrane with hole of incomplete obstruction. The morphologies MRV demonstrated that the proximal part of the 37 cases with complete obstruction were mainly divided into the cone type (36 cases) and the planum type (1 case). Besides, the type of distal end of obstruction were the cone type (30 cases), the planum type (4 cases) and the irregular type (3 cases). The overall sensitivity, specificity, positive and negative predictive values for the diagnosis of MRV were respectively 100%%, 57.1%, 92.5% and 100% as compared to the DSA.
CONCLUSIONThe examination of MRV is capable of revealing the obstructive interface morphology of the inferior vena cava, especially for the distal end of obstruction. MRV can provide guidelines in interventional treatment of Budd-Chiari syndrome.
Adult ; Aged ; Angiography, Digital Subtraction ; Budd-Chiari Syndrome ; diagnostic imaging ; pathology ; Female ; Humans ; Magnetic Resonance Imaging ; Male ; Middle Aged ; Vena Cava, Inferior ; diagnostic imaging ; pathology ; Young Adult
5.A multicenter, phase III trial of hemocoagulase Agkistrodon: hemostasis, coagulation, and safety in patients undergoing abdominal surgery.
Jun-min WEI ; Ming-wei ZHU ; Zhong-tao ZHANG ; Zhen-geng JIA ; Xiao-dong HE ; Yuan-lian WAN ; Shan WANG ; Dian-rong XIU ; Yun TANG ; Jie LI ; Jing-yong XU ; Qing-shan HENG
Chinese Medical Journal 2010;123(5):589-593
BACKGROUNDHemocoagulase Agkistrodon for injection is a single component thrombin which has passed phases I and II clinical trials. The purpose of this phase III clinical trial was to evaluate the effect of Hemocoagulase Agkistrodon on hemostasis and coagulation in abdominal skin and subcutaneous incisions and to assess the safety of this agent in surgical patients.
METHODSThis is a phase III, prospective, randomized, double-blind, and controlled multicenter clinical trial including 432 consecutive patients randomized into either a study group (injected with hemocoagulase Agkistrodon at 2 U, n = 324) or a control group (injected with hemocoagulase Atrox, n = 108). The hemostatic time, hemorrhagic volume, hemorrhagic volume per unit area, blood coagulation, and adverse events were measured and compared between the two groups.
RESULTSThe mean hemostatic time in the study group was (36.8 +/- 18.7) seconds; the hemorrhagic volume was (3.77 +/- 3.93) g; and the hemorrhagic volume per unit area was (0.091 +/- 0.125) g/cm(2). In the control group, the corresponding values were (38.1 +/- 19.7) seconds, (4.00 +/- 4.75) g, and (0.095 +/- 0.101) g/cm(2), respectively. No significant difference in values existed between the two groups (P > 0.05). Blood coagulation results and hepatic and renal function were also similar between the two groups. Adverse events were reported in two cases, but were deemed non-drug-related.
CONCLUSIONSHemocoagulase Agkistrodon has good hemostatic and coagulative function and is safe for the use of arresting capillary hemorrhage that occurs while incising the abdomen during surgery.
Abdomen ; surgery ; Adolescent ; Adult ; Aged ; Agkistrodon ; Animals ; Batroxobin ; adverse effects ; pharmacology ; Blood Coagulation ; drug effects ; Double-Blind Method ; Evidence-Based Medicine ; Female ; Hemostasis ; drug effects ; Hemostatics ; pharmacology ; Humans ; Male ; Middle Aged ; Prospective Studies
6.Effect of dangua recipe on glycolipid metabolism and VCAM-1 and its mRNA expression level in Apo E(-/-) mice with diabetes mellitus.
Xian-Pei HENG ; Liang LI ; Su-Ping HUANG ; Yan CHEN ; Miao-Xian LIN ; Huai-Shan ZHUANG ; Qun-Fang YAN ; Liu-Qing YANG ; Ling CHEN ; Qing LIN ; Xin-Ling CHENG ; Min-Ling CHEN ; Yi-Chu CHEN ; Yuan-Long LAN ; Zhi-Ta WANG ; Shu-Hong YAO ; Zhi-San ZHANG
Chinese Journal of Integrated Traditional and Western Medicine 2014;34(9):1086-1095
OBJECTIVETo study the effect of Dangua Recipe (DGR) on glycolipid metabolism, vascular cell adhesion molecule-1 (VCAM-1) and its mRNA expression level of transgenic Apo E(-/-) mouse with spontaneous atherosclerosis, thus revealing its partial mechanism for curing diabetes mellitus (DM) with angiopathy.
METHODSDiabetic model was prepared by peritoneally injecting streptozotocin (STZ) to Apo E(-/-) mouse. Totally 32 modeled mice were stratified by body weight, and then divided into 4 groups referring to blood glucose levels from low to high by random digit table, i.e., the model group (MOD, fed with sterile water, at the daily dose of 15 mL/kg), the DGR group (fed with DGR at the daily dose of 15 mL/kg), the combination group (COM, fed with DGR at the daily dose of 15 mL/kg and pioglitazone at the daily dose of 4.3 mg/kg), and the pioglitazone group (PIO, at the daily dose of 4.3 mg/kg), 8 in each group. Another 8 normal glucose C57 mouse of the same age and strain were recruited as the control group. All interventions lasted for 12 weeks by gastrogavage. The fasting blood glucose (FBG), body weight, food intake, water intake, skin temperature, the length of tail, and the degree of fatty liver were monitored. The hemoglobin A1c (HbA1c), total cholesterol (TC), and LDL-C were determined. Endothelin-1 (ET-1) was determined by radioimmunoassay. Nitrogen monoxidum (NO) was determined by nitrate reductase. The kidney tissue VCAM-1 level was analyzed with ELISA. The expression of VCAM-1 mRNA in the kidney tissue was detected with real time quantitative PCR.
RESULTSCompared with the control group, the body weight and food intake decreased, water intake increased in all the other model groups (P < 0.05). Besides, the curve of blood glucose was higher in all the other model groups than in the control group (P < 0.01). Compared with the model group, the body weight increased; levels of HbAlc, TC, LDL-C, ET-1, and VCAM-1 were significantly lower; and skin temperature was higher in the DGR group (P < 0.05, P < 0.01). Compared with the PIO group, body weight, the increment of body weight, FBG, TC, and LDL-C were lower (P < 0.05, P < 0.01); food intake and water intake increased more and the tail length was longer in the DRG group (P < 0.01). There was no statistical difference in the level of NO among groups. The degree of fatty liver in the model group was significantly severer than that in the control group (P < 0.05). It was obviously alleviated in the DGR group (P < 0.05) when compared with the model group and the PIO group (P < 0.05, P < 0.01). But it was severer in the PIO group than in the model group (P < 0.01). The degree of fatty liver in the combination group ranged between that of the DGR group and the PIO group (P < 0.05). The level of VCAM-1 mRNA expression was significantly lower in the DGR group than in the model group, the PIO group, and the combination group (P < 0.05).
CONCLUSIONSDGR had effect in lowering blood glucose and blood lipids, and fighting against fatty liver of transgenic Apo E(-/-) mouse with spontaneous atherosclerosis. DGR played an effective role in preventing and treating DM with angiopathy by comprehensively regulating glycolipid metabolism and promoting the vascular function.
Animals ; Apolipoproteins E ; genetics ; Blood Glucose ; metabolism ; Diabetes Mellitus, Experimental ; blood ; drug therapy ; Diabetic Angiopathies ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; Lipids ; blood ; Male ; Mice ; Mice, Knockout ; RNA, Messenger ; genetics ; Random Allocation ; Thiazolidinediones ; pharmacology ; Vascular Cell Adhesion Molecule-1 ; genetics ; metabolism
7.Percutaneous radiofrequency ablation combined with other minimally invasive treatments for recurrent hepatocellular carcinoma after hepatectomy.
Li XU ; Peng LI ; Min-shan CHEN ; Xiong-hao PANG ; Heng-jun GAO ; Zhen-wei PENG ; Hui-hong LIANG ; Yao-jun ZHANG ; Jin-qing LI
Chinese Journal of Surgery 2008;46(21):1617-1620
OBJECTIVETo evaluate the efficacy and safety of percutaneous radiofrequency ablation (PRFA) and combined with other minimally invasive treatments for recurrent hepatocellular carcinoma (RHCC) after hepatectomy.
METHODSEighty-four patients with RHCC after hepatectomy who were treated with PRFA or combined with other minimally invasive therapies between August 1999 and February 2008 were analyzed retrospectively.
RESULTSThere was no treatment related mortality in the study population, and the morbidity was 2.4% (2/84). The complete ablation rate was 94.0% (79/84), and the 1-, 3- and 5-year overall survival rates were 74.9%, 54.9% and 48.2%, respectively. The 1-, 3- and 5-year overall survival rates of patients with recurrent interval after hepatectomy less than 1 year and over 1 year were 72.1%, 36.2%, 24.2% and 76.8%, 70.6% and 65.1%, respectively (P = 0.040). The 1-, 3- and 5-year overall survival rates of patients with tumor size
CONCLUSIONSPRFA is an effective and safe treatment for RHCC, and tumor size and recurrent interval after hepatectomy are important prognostic factors. Combination with PEI or TACE may improve the efficacy of PRFA for treatment of RHCC.
Adult ; Aged ; Carcinoma, Hepatocellular ; pathology ; surgery ; Catheter Ablation ; Female ; Follow-Up Studies ; Hepatectomy ; methods ; Humans ; Liver Neoplasms ; pathology ; surgery ; Male ; Middle Aged ; Neoplasm Recurrence, Local ; surgery ; Retrospective Studies ; Treatment Outcome
8.Synthesis, bioactivity evaluation of dibenzoyl methane halophenols and their interactions with CAV-1
Heng-jiang LIU ; Ning-ning CHENG ; Meng-ru ZHANG ; Hong-xia YUAN ; Yuan-lin ZHANG ; Xiu-e FENG ; Qing-shan LI
Acta Pharmaceutica Sinica 2021;56(12):3493-3502
Caveolin-1 (CAV-1) is related to inflammation, oxidative damage, and immunity. In order to obtain a series of dibenzoylmethane halophenols with strong anti-inflammatory and antioxidant effects targeting CAV-1, twenty-nine target compounds were therefore synthesized by Baker-Ventaraman rearrangement and demethylation reaction, starting from the substituted benzoyl chloride and
9.Clinical treatment outcomes and their changes in extremely preterm twins: a multicenter retrospective study in Guangdong Province, China.
Bi-Jun SHI ; Ying LI ; Fan WU ; Zhou-Shan FENG ; Qi-Liang CUI ; Chuan-Zhong YANG ; Xiao-Tong YE ; Yi-Heng DAI ; Wei-Yi LIANG ; Xiu-Zhen YE ; Jing MO ; Lu DING ; Ben-Qing WU ; Hong-Xiang CHEN ; Chi-Wang LI ; Zhe ZHANG ; Xiao RONG ; Wei SHEN ; Wei-Min HUANG ; Bing-Yan YANG ; Jun-Feng LYU ; Hui-Wen HUANG ; Le-Ying HUO ; Hong-Ping RAO ; Wen-Kang YAN ; Xue-Jun REN ; Yong YANG ; Fang-Fang WANG ; Dong LIU ; Shi-Guang DIAO ; Xiao-Yan LIU ; Qiong MENG ; Yu WANG ; Bin WANG ; Li-Juan ZHANG ; Yu-Ge HUANG ; Dang AO ; Wei-Zhong LI ; Jie-Ling CHEN ; Yan-Ling CHEN ; Wei LI ; Zhi-Feng CHEN ; Yue-Qin DING ; Xiao-Yu LI ; Yue-Fang HUANG ; Ni-Yang LIN ; Yang-Fan CAI ; Sha-Sha HAN ; Ya JIN ; Guo-Sheng LIU ; Zhong-He WAN ; Yi BAN ; Bo BAI ; Guang-Hong LI ; Yue-Xiu YAN
Chinese Journal of Contemporary Pediatrics 2022;24(1):33-40
OBJECTIVES:
To investigate the clinical treatment outcomes and the changes of the outcomes over time in extremely preterm twins in Guangdong Province, China.
METHODS:
A retrospective analysis was performed for 269 pairs of extremely preterm twins with a gestational age of <28 weeks who were admitted to the department of neonatology in 26 grade A tertiary hospitals in Guangdong Province from January 2008 to December 2017. According to the admission time, they were divided into two groups: 2008-2012 and 2013-2017. Besides, each pair of twins was divided into the heavier infant and the lighter infant subgroups according to birth weight. The perinatal data of mothers and hospitalization data of neonates were collected. The survival rate of twins and the incidence rate of complications were compared between the 2008-2012 and 2013-2017 groups.
RESULTS:
Compared with the 2008-2012 group, the 2013-2017 group (both the heavier infant and lighter infant subgroups) had lower incidence rates of severe asphyxia and smaller head circumference at birth (P<0.05). The mortality rates of both of the twins, the heavier infant of the twins, and the lighter infant of the twins were lower in the 2013-2017 group compared with the 2008-2012 group (P<0.05). Compared with the 2008-2012 group, the 2013-2017 group (both the heavier infant and lighter infant subgroups) had lower incidence rates of pulmonary hemorrhage, patent ductus arteriosus (PDA), periventricular-intraventricular hemorrhage (P-IVH), and neonatal respiratory distress syndrome (NRDS) and a higher incidence rate of bronchopulmonary dysplasia (P<0.05).
CONCLUSIONS
There is a significant increase in the survival rate over time in extremely preterm twins with a gestational age of <28 weeks in the 26 grade A tertiary hospitals in Guangdong Province. The incidences of severe asphyxia, pulmonary hemorrhage, PDA, P-IVH, and NRDS decrease in both the heavier and lighter infants of the twins, but the incidence of bronchopulmonary dysplasia increases. With the improvement of diagnosis and treatment, the multidisciplinary collaboration between different fields of fetal medicine including prenatal diagnosis, obstetrics, and neonatology is needed in the future to jointly develop management strategies for twin pregnancy.
Bronchopulmonary Dysplasia/epidemiology*
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Female
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Gestational Age
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Humans
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Infant
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Infant, Extremely Premature
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Infant, Newborn
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Pregnancy
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Respiratory Distress Syndrome, Newborn/epidemiology*
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Retrospective Studies
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Treatment Outcome
10.Bis (2-butoxyethyl) Phthalate Delays Puberty Onset by Increasing Oxidative Stress and Apoptosis in Leydig Cells in Rats.
Miao Qing LIU ; Hai Qiong CHEN ; Hai Peng DAI ; Jing Jing LI ; Fu Hong TIAN ; Yi Yan WANG ; Cong De CHEN ; Xiao Heng LI ; Jun Wei LI ; Zhong Rong LI ; Ren Shan GE
Biomedical and Environmental Sciences 2023;36(1):60-75
OBJECTIVE:
This study investigated the effects of bis (2-butoxyethyl) phthalate (BBOP) on the onset of male puberty by affecting Leydig cell development in rats.
METHODS:
Thirty 35-day-old male Sprague-Dawley rats were randomly allocated to five groups mg/kg bw per day that were gavaged for 21 days with BBOP at 0, 10, 100, 250, or 500 mg/kg bw per day. The hormone profiles; Leydig cell morphological metrics; mRNA and protein levels; oxidative stress; and AKT, mTOR, ERK1/2, and GSK3β pathways were assessed.
RESULTS:
BBOP at 250 and/or 500 mg/kg bw per day decreased serum testosterone, luteinizing hormone, and follicle-stimulating hormone levels mg/kg bw per day (P < 0.05). BBOP at 500 mg/kg bw per day decreased Leydig cell number mg/kg bw per day and downregulated Cyp11a1, Insl3, Hsd11b1, and Dhh in the testes, and Lhb and Fshb mRNAs in the pituitary gland (P < 0.05). The malondialdehyde content in the testis significantly increased, while Sod1 and Sod2 mRNAs were markedly down-regulated, by BBOP treatment at 250-500 mg/kg bw per day (P < 0.05). Furthermore, BBOP at 500 mg/kg bw per day decreased AKT1/AKT2, mTOR, and ERK1/2 phosphorylation, and GSK3β and SIRT1 levels mg/kg bw per day (P < 0.05). Finally, BBOP at 100 or 500 μmol/L induced ROS and apoptosis in Leydig cells after 24 h of treatment in vitro (P < 0.05).
CONCLUSION:
BBOP delays puberty onset by increasing oxidative stress and apoptosis in Leydig cells in rats.
UNLABELLED
The graphical abstract is available on the website www.besjournal.com.
Rats
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Male
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Animals
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Leydig Cells/metabolism*
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Testosterone
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Glycogen Synthase Kinase 3 beta/pharmacology*
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Rats, Sprague-Dawley
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Sexual Maturation
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Testis
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Oxidative Stress
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TOR Serine-Threonine Kinases/metabolism*
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Apoptosis