1.Roles of G protein-coupled estrogen receptor in the male reproductive system.
Kai-hong CHEN ; Xian ZHANG ; Xue-wu JIANG
National Journal of Andrology 2016;22(2):175-179
The G protein-coupled estrogen receptor (GPER), also known as G protein-coupled receptor 30 (GPR30), was identified in the recent years as a functional membrane receptor different from the classical nuclear estrogen receptors. This receptor is widely expressed in the cortex, cerebellum, hippocampus, heart, lung, liver, skeletal muscle, and the urogenital system. It is responsible for the mediation of nongenomic effects associated with estrogen and its derivatives, participating in the physiological activities of the body. The present study reviews the molecular structure, subcellular localization, signaling pathways, distribution, and function of GPER in the male reproductive system.
Estrogens
;
metabolism
;
Genitalia, Male
;
metabolism
;
Humans
;
Male
;
Molecular Structure
;
Organ Specificity
;
Receptors, Estrogen
;
chemistry
;
physiology
;
Receptors, G-Protein-Coupled
;
chemistry
;
physiology
;
Reproduction
;
physiology
;
Signal Transduction
2.Design, synthesis and cholinesterase inhibitory activity of quinoline-polyamine conjugates.
Wen LUO ; Kai HUANG ; Zhen ZHANG ; Chen HONG ; Chaojie WANG
Acta Pharmaceutica Sinica 2013;48(2):269-75
A series of quinoline-polyamine conjugates (8a-8n) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). Some of these compounds had potent ChEs inhibitory activity with IC50 values at micromolar range. Compound 8n exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 8.78 micromol x L(-1), and compound 8i showed the most potent inhibition on butyrylcholinesterase (BChE) with IC50 value of 1.60 micromol x L(-1) which was slightly better than rivastigmine. The structure-activity relationship revealed that the chain length of polyamine and linker played important roles for inhibitory activity. Molecular modeling studies showed that 8i targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of cholinesterases.
3.A Clinical Observation on Preventive Effect of Spleen-Strengthening and Kidney-Reinforcing Method on Leukopenia Caused by Chemotherapy
Chunyong CHEN ; Kai XU ; Hong DENG ; Diying ZHU
Journal of Guangzhou University of Traditional Chinese Medicine 2000;0(04):-
Objective To observe the effect of spleen-strengthening and kidney-reinforcing method on leukopenia in patients with malignant tumor after chemotherapy.Methods Seventy-one patients with malignant tumor were randomly allocated to Group A(n=37) and Group B (n=34).Group A was treated with spleen-strengthening and kidney-reinforcing herbal medicine and chemotherapy and Group B with chemotherapy only. The treatment course lasted 28 days.Blood routine examination was carried out before chemotherapy and on 7 th,9 th,12 th,15 th,18 th and 21 st day of chemotherapy.Results In Group A,5 cases of leukopenia were found, 3 in degree Ⅰ, 1 in degree Ⅱ and 1 in degree Ⅲ,the incidence being 13.5%; In Group B,25 cases of leukopenia were found, 3 in degree Ⅰ,13 in degree Ⅱ,8 in degree Ⅲ and 1 in degree Ⅳ, the incidence being 73.5%. There was significant difference between the two groups (P
5.The effect of polyethylene terephthalates coated with 58S bioactive glass on graft-bone healing
Yang WU ; Shiyi CHEN ; Jia JIANG ; Hong LI ; Kai GAO
Chinese Journal of Orthopaedics 2012;32(6):576-581
Objective To observe the effect of polyethylene terephthalates (PET) coated with 58S bioactive glass on graft-bone healing.Methods The PET coated with 58S bioactive glass was used in experimental group,and uncoated PET was used as a control.The coating solution was made of 20% bioactive glass powder and 80% gelatin powder (by weight).In our vitro study,4×104/ml MT3T3-E1 cells were cultured in 24-well plates with the coated or uncoated PET,and the MTT and ALP were tested at 1,3,5 days to show the proliferation and the activity of the cells.The SEM and the X-ray photoelectron spectrometer were adopted to analyze the surface characteristics of the fiber.In our vivo study,24 skeletally mature New Zealand white rabbits were randomly divided into two groups,the 58S-PET group and the PET group.Both groups underwent a surgical procedure to establish a tibia-articular tendon-bone healing model.Mechanical examination and histological assay were taken to verify the coating effect in vivo.Results The 58S-PET group showed significantly differences in both the MTT and ALP tests at each time point (3,5 days) compared with the PET group.In the animal experiments,the maximum load increased by time in both groups.At 6 weeks,the load-to-failure was significantly higher in the 58S-PET group [(61.70±6.95) N]than that of the PET group [(45.21±9.78) N].At 12 weeks,the load-to-failure was also significantly higher in the 58S-PET group [(89.25±9.50) N]than that of the PET group [(71.38±6.26) N].In the histological assay,it was found that there was new bone formation in the indistinct interface between the graft and the host bone in both groups at 6,12 weeks,and a stronger binding was seen in the 58S-PET group than in the PET group.Conclusion The 58S-PET could enhance the proliferation and activity of the osteoblast and therefore promote the new bone formation and subsequently leads to a positive effect on tendon-bone healing.
6.Clinical significance of retinal binding protein and cystatin C in blood and urine of patients with chronic kidney disease
Hong LIU ; Chen LU ; Ying LIU ; Kai LIU ; Hua YUE ; Hong JIANG
Clinical Medicine of China 2014;30(5):464-466
Objective To investigate the clinical significance of retinal binding protein (RBP) and Cystatin C in blood and urine in patients with chronic kidney disease (CKD).Methods One hundred and twenty-one patients with CKD in Nephrology Laboratory of The People's Hospital of Xinjiang Uygur Autonomous Region from Aug.2012 to Jan.2013 were served as the case group.Sixty healthy check-up people were considered as control group.Enzyme linked immunosorbent assay was used to detect RBP and Cystatin C in urine,and the immune turbidimetry testing was applied to detect RBP and Cystatin C in blood.The receiveroperating characteristic (ROC) curve and area under curve (AUC) were applied to evaluate the sensibility and diagnostic value of indexes in CKD.Results The positive rate of RBP,Cystatin C in urine and blood were 89.6%,92.6%,52.5%,59.5% respectively of 12 patients in case group,higher than those in control group (all value were 0,P <0.001).ROC curve showed that the sensitivity of urine RBP and Cystatin C were higher than that in blood of case group.AUC of RBP,Cystatin C level in urine and blood were 0.915,0.974,.655,and 0.623 respectively.And 95% confidence interval were 0.877-0.954,0.956-0.992,0.575-0.736,0.543-0.702 respectively,and the differences are statistically significant (P < 0.001).Conclusion The sensitivity of urine cystatin C and RBP are significantly higher than that in blood,which might be served as a diagnostic marker of CKD and can provide important basis for clinical diagnosis.
7.Change of iodine load and thyroid homeostasis induced by ammonium perchlorate in rats.
Hong-Xia, CHEN ; Miao-Hong, DING ; Qin, LIU ; Kai-Liang, PENG
Journal of Huazhong University of Science and Technology (Medical Sciences) 2014;34(5):672-8
Ammonium perchlorate (AP), mainly used as solid propellants, was reported to interfere with homeostasis via competitive inhibition of iodide uptake. However, detailed mechanisms remain to be elucidated. In this study, AP was administered at 0, 130, 260 and 520 mg/kg every day to 24 male SD rats for 13 weeks. The concentrations of iodine in urine, serum thyroid hormones levels, total iodine, relative iodine and total protein, and malondialdehyde (MDA), superoxide dismutase (SOD) and catalase (CAT) activity in thyroid tissues were measured, respectively. Our results showed that high-dose perchlorate induced a significant increase in urinary iodine and serum thyroid stimulating hormone (TSH), with a decrease of total iodine and relative iodine content. Meanwhile, free thyroxine (FT4) was decreased and CAT activity was remarkably increased. Particularly, the CAT activity was increased in a dose-dependent manner. These results suggested that CAT might be enhanced to promote the synthesis of iodine, resulting in elevated urinary iodine level. Furthermore, these findings suggested that iodine in the urine and CAT activity in the thyroid might be used as biomarkers for exposure to AP, associated with thyroid hormone indicators such as TSH, FT4.
9.Observation of injection drug speed in ropivcaine combined spinal epidural anesthesia
Guo-Qiang CHEN ; Jian-Dong WENG ; Wen-Ke YANG ; Yi-Shan HONG ; Huan-Kai ZHANG ;
Chinese Journal of Primary Medicine and Pharmacy 2006;0(10):-
Objective To investigate the effect of ropiyacaine combined with intra-spinal epidural anesthesia by using the same volume but different injection speed on anaesthetic level.Methods 80 cases of patients of ASA~Ⅱdegree suitable to use intra-spinal epidural combined anesthesia for gynecologic operation were selected and ran- domly divided into three groups,0.75 % ropivacaine 2mg(15mg)administered,group A the speed of injection was 10 seconds,group B injection speed was 20 seconds,group C injection speed was 30 seconds,the anaesthetic level reached T_(10).The time of highest level in spinal anesthesia,30 minutes after spinal anesthesia MAP,and number of cases need to add epidural drug were all recorded.Results The best effect of anesthesia was found in group B,the block level of anesthesia was satisfactory,blood dynamic was stable,and there was no need to add epidural drug.Conclusion The speed of 0.75 % ropivacaine 2ml spinal epidural combined with anesthesia was suitable at the speed of 20 seconds.
10.The survey on the traffic capacity of ambulances in Beijing
Jin-Jun ZHANG ; Yong-Chun ZHAO ; Hang LI ; Jin-Bao GUAN ; Kai-Hong CHEN ;
Chinese Journal of Emergency Medicine 2006;0(09):-
Objective To investigate the traffic capacity of ambulances in Beijing,and to explore factors and methods to resolve this problem.Method A survey on all the ambulances on-duty in Beijing from 17th August to 17th September 2006 was conducted by questionnaires.Results The average speed of ambulances in Beijing was 32.07 km/h.There were statistically significant differences in terms of the areas and time, respectively.Conclusions The traffic jam of Beijing was serious.The traffic capacity of ambulances was far from being ideal,which restricted the operation of 120 ambulances.It is difficult to satisfy the needs of Beijing 2008 Olympic games and it is time for the relevant authorities to search for appropriate methods and solve this problem.