1. Target screening and antihyperglycemic activity on SGLT2 and α-glucosidase in vitro and in vivo of TSG from Polygonum multiflorum
Chinese Traditional and Herbal Drugs 2019;50(18):4378-4383
Objective: To study the mechanism that TSG can reduce plasma glucose level by inhibiting sodium-dependent glucose cotransporters 2 (SGLT2) and α-glucosidase in vitro and in vivo. Methods: Molecular docking method was used to study the binding affinities of TSG and diabetes related targets. The structures of targets were taken from Protein Data Bank or references. 1-NBDG and PNPG were used as the substrates for the inhibition assays of TSG against SGLT2 and α-glucosidase respectively in vitro. The antihyperglycemic activity of TSG was operated by oral glucose tolerance test (OGTT) and urinary glucose excretion (UGE) test in rats. Results: TSG was identified as the inhibitors of SGLT2 with the docking score of -9.35 less than -9.79 of dapagliflozin as the positive control and α-glucosidase with the docking score of -5.44 compared to -5.58 of acarbose as the positive control. TSG showed the inhibitory rate of 21.6% at the dose of 10 μmol/L against SGLT2 and 32.5% at the dose of 100 μmol/L in vitro test. Compared with model group, the group of 120 mg/kg dose had significant difference (P < 0.05) but the overall effect was not as strong as dapagliflozin in OGTT and UGE test. The result of rat in vivo test showed that glucose inhibition rate of TSG (120 mg/kg) was (9.3 ± 1.0)%, urinary glucose content was (435.5 ± 84.0) mg/kg, which showed certain hypoglycemic effect. Conclusion: TSG exhibited antiglycemic activity through inhibiting SGLT2 and α-glucosidase, which was considered to be a new lead compound of dual target inhibitors.
2.PDS Ⅱ absorbable suture netting for chest wall reconstruction: report of 23 cases
Bo YE ; Jian FENG ; Ming CHENG ; Jicheng TANTAI ; Yong CHENG ; Heng ZHAO ; Jianxin SHI
Chinese Journal of Thoracic and Cardiovascular Surgery 2013;29(10):595-596,613
Objective Explore a new method which application absorbable suture netting for chest wall reconstruction and observe the clinical effect.Methods For 23 cases of part of the rib resection,support the soft tissue using absorbable suture netting and observe the postoperative results.Results 23 patients have the postoperative respiratory stability and no abnormal breathing and chest wall collapse happened.And this method has a good effect to support the Chest wall.Conclusion Chest wall reconstruction using absorbable suture netting has the following advantages:easily obtained,easy to learn to promote,low prices and postoperative respiratory stability.We believe this method is a new technology deserved to be promoted in our country.
3.Genotyping of HBV DNA in Shenzhen and clinical manifestations.
Jian-yi DAI ; Zhi-lin SHI ; Yong DAI ; Hong DU ; De-heng CHEN ; Sha-yan WANG
Chinese Journal of Hepatology 2004;12(4):199-200
OBJECTIVETo detect HBV DNA and its genotypes.
METHODSThe 6 isoforms of HBV DNA was detected out using of different probes by Polymerase Chain Reaction and Nucleic Acid hybridization.
RESULTSOf 150 HBV DNA positive patients who lived in Shenzhen, 50 samples (33%) are type B, 36 samples (24%) are type C, 13 samples (9%) are type D, 3 samples is type F, 1 sample is type A, 48 samples (31%) are mixed type. The ALT value was significantly higher in genotype B than in genotype C. HBe positivity were higher in genotype B than genotype C. HBeAg positivity were higher in genotype C than in genotype B. There are not obvious relations between genotype and age or sex.
CONCLUSIONIn the detected samples, the major genotype of HBV DNA is type B, several are type C, D. The type E haven't been found. There are some relations between all kinds of genotypes and the severity of hepatitis B.
Adult ; DNA, Viral ; analysis ; Female ; Genotype ; Hepatitis B ; virology ; Hepatitis B virus ; classification ; genetics ; Humans ; Male ; Middle Aged ; Polymerase Chain Reaction
4.Study on the effects of different extent of cleft malformation on speech in patients with cleft palate.
Bei LI ; Bing SHI ; Qian ZHENG ; Tian MENG ; Heng YIN ; Yong LU
West China Journal of Stomatology 2007;25(1):55-57
OBJECTIVETo investigate the relation between different extents of cleft malformation with the speech characteristics in patients with cleft palate.
METHODSThe formant frequency of vowel [i] of 46 incomplete cleft palate patients (ICCP group) and 56 complete cleft palate patients (CCP group) before and after cleft palate repair, as well as 30 normal people (C group), were measured and analyzed on spectrogram.
RESULTSThe comparison of F1 between C group and CCP, ICCP before surgery showed no difference. So did the comparison of F1 between C group and CCP, ICCP after surgery. The comparison of F2 between C group and CCP, ICCP before surgery showed significant difference. The value of the C group was the highest. The value of the ICCP was higher than that of CCP. So did the comparison of F2 between C group and CCP, ICCP after surgery. The comparison of F3 between C group and CCP, ICCP(including before and after surgery) was similar to the results of F2 between the three groups. The comparison of F1 between before and after surgery in ICCP group showed no difference. However, the same kind of comparison of F2 and F3 showed significant differences: Both the values after surgery were higher than those before surgery. The comparison of Fl, F2 and F3 between before and after surgery in CCP group was similar to that in ICCP group.
CONCLUSIONThe extent of the cleft malformation is closely related to the status of the speech in patients with cleft palate. With the malformation more severe, the tongue will move backward more obviously, the elevation of the soft palate after cleft palate repair will be less active. Two ways are recommended for those patients with CCP: (1) Early interceptive orthodontic treatment to reduce the extent of palate malformation; (2) The hard palate repair can be performed prior to the soft palate repair. Patients with severe cleft lip and palate can have hard palate repaired while accepting the early cleft lip repair.
Cleft Lip ; Cleft Palate ; Female ; Humans ; Male ; Palate, Hard ; Speech
5.¹H-NMR based metabonomic approach to evaluate anti-coagulant effect of Danggui Sini decoction.
Hua ZHENG ; Xia QIN ; Hui SONG ; Chao-lin TANG ; Jun-xiang RUAN ; Hong-ye ZHANG ; Shi-yin LU ; Yong-hong LIANG ; Zhi-heng SU
China Journal of Chinese Materia Medica 2015;40(20):4088-4093
To study the anti-coagulant effect and influence of danggui Sini decoction (DSD) on rat's plasma endogenous metabolites by animal experiment and ¹H-NMR based metabolomics method. After intragastric administration of Danggui Sini Decoction for 7 days, Plasma thrombin time (TT) was measured. Rat plasma metabolic fingerprint in two groups was analyzed using ¹H-NMR, based on which the principal component analysis( PCA) and orthogonal partial least-squares discriminant analysis(OPLS-DA) models for metabonomic analysis. Potential biomarkers were screened by using variable importance in the projection (VIP) and T test. DSD could prolong TT of the rat significantly (P < 0.05). Compared with control group, six kinds of endogenous metabolites in DSD group change significantly (P < 0.05), among which isobutyrate, carnitine and phenylalanine content had an upward trend (P < 0.01) and lysine, Histidine and cholesterol content had a downward trend (P < 0.05). It is likely that carnitine, phenylalanine, Histidine and cholesterol are the potential metabolic markers in the anti-coagulant process and DSD affects the platelet aggregation and the expression of tissue factor and fiber protease by regulating the energy, amino acid and lipid metabolism.
Animals
;
Anticoagulants
;
chemistry
;
Blood Coagulation
;
drug effects
;
Drugs, Chinese Herbal
;
chemistry
;
Female
;
Male
;
Metabolomics
;
methods
;
Proton Magnetic Resonance Spectroscopy
;
methods
;
Rats
6.Hyperglycemia inhibited taurine transport and taurine transporter gene expression in cultured rat cardiomyocytes.
Yan-rong SHI ; Lin GAO ; Shu-heng WANG ; Yong-zheng PANG ; Chaoshu TANG
Chinese Journal of Applied Physiology 2003;19(2):132-136
AIMTo investigate the alterations of taurine transport, and taurine transporter (TAUT) mRNA by hyperglycemia in cultured rat cardiomyocytes.
METHODS3H-taurine measured the amount of taurine uptake. TAUT mRNA consents were measured using quantitative RT-PCR.
RESULTSThe cellular uptake amounts of taurine in seven groups increased with incubation time, and near to be saturated after 5 min. The uptake amount of 10, 20, and 30 mmol/L glucose groups was obviously lower than that of the control group (P < 0.05 or P < 0.01). In 30 mmmol/L glucose, taurine release obviously was decreased, as compared with that of the control. Exposure of cells to 10, 20, and 30 mmmol/L glucose decreased taurine uptake in a concentration-dependent fashion. Exposure to hyperglycemia did not affect the Km of the TAUT, but the apparent Vmax were significantly decreased (P < 0.05). In 20 and 30 mmmol/L groups, TAUT mRNA contents of myocardial cells were significantly reduced, as compared with the control group (P < 0.05).
CONCLUSIONThe data suggests that there are dysfunction of taurine uptake and downregulation of TAUT gene expression by glucose in cultured rat cardiomyocytes.
Animals ; Cells, Cultured ; Glucose ; pharmacology ; Hyperglycemia ; metabolism ; Membrane Glycoproteins ; genetics ; metabolism ; Membrane Transport Proteins ; genetics ; metabolism ; Myocytes, Cardiac ; drug effects ; metabolism ; RNA, Messenger ; genetics ; Rats ; Rats, Sprague-Dawley ; Taurine ; metabolism
7.Clinical research of effect of Yishen Yangnao capsule on vascular dementia.
Wen-jie XU ; Zong-heng LI ; Yong-mei SHI ; Yi-huai ZOU
China Journal of Chinese Materia Medica 2007;32(8):732-735
OBJECTIVETo find a good way to diagnose VD, value the effect of Yishen Yangnao capsule on VD and try to find some rules of changes in Chinese medicine syndromes.
METHODPatients were randomly divided into treating group and western medicine comparison group. It's the phase III clinical research of Rishen Yangnao capsule curing VD, judging the validity and security of it, using dukexi slice as comparison drug. Some of the patients did the examination of P300.
RESULTThe total validity of Yishen Yangnao capsule is 56.3% (contract team is 60.0%). The improve rate of ADL is 0.1069% (contract team is 0.1134%). The scores of Chinese medicine syndrome descend.
CONCLUSIONYishen Yangnao capsule has the same effect as dukexi slice in curing VD at the side of intelligence situation and life ability.
Activities of Daily Living ; Aged ; Almitrine ; therapeutic use ; Capsules ; Dementia, Vascular ; drug therapy ; physiopathology ; Drug Combinations ; Drugs, Chinese Herbal ; isolation & purification ; therapeutic use ; Event-Related Potentials, P300 ; Female ; Humans ; Male ; Medicine, Chinese Traditional ; methods ; Middle Aged ; Neuroprotective Agents ; isolation & purification ; therapeutic use ; Phytotherapy ; Treatment Outcome ; Yohimbine ; therapeutic use
8.Association of the common genetic variant upstream of INSIG2 gene with obesity related phenotypes in Chinese children and adolescents.
Hai-Jun WANG ; Heng ZHANG ; Shi-Wei ZHANG ; Yong-Ping PAN ; Jun MA
Biomedical and Environmental Sciences 2008;21(6):528-536
OBJECTIVETo study the association between the rs7566605 variant of INSIG2 and obesity-related phenotypes in Chinese children and adolescents.
METHODSThe study sample consisted of two independent cohorts of Chinese children and adolescents. Anthropometric indices, lipids, blood pressure, fasting glucose, insulin and percentage of fat mass were determined. PCR with restriction fragment length polymorphism analysis was performed for genotyping the rs7566605 variant.
RESULTSIn each of the two independent cohorts, no significant association was observed between rs7566605 and obesity under additive, dominant or recessive model. We also did not detect any difference in the genotype frequency between all the obese children and controls. Furthermore, we did not find evidence of an association between body composition indices and metabolic phenotypes in all children. However, the triglyceride level of CC homozygotes was significantly higher than that of GG+GC genotypes in obese children (P=0.022). Additionally, we observed a non-significant trend of severe obesity in a post-hoc test.
CONCLUSIONINSIG2 rs7566605 variant is not associated Chinese childhood obesity in two independent cohorts. Further study is needed to verify the effect of rs7566605 on triglyceride in obese children.
Adipose Tissue ; Adolescent ; Asian Continental Ancestry Group ; ethnology ; genetics ; Body Mass Index ; Child ; China ; Cohort Studies ; Female ; Genetic Variation ; genetics ; Humans ; Intracellular Signaling Peptides and Proteins ; genetics ; Male ; Membrane Proteins ; genetics ; Obesity ; ethnology ; genetics ; Phenotype ; Risk Factors ; Young Adult
9.Reconstructive vascular operation for kinking of internal carotid artery.
Ji-Yue WANG ; Ji-Heng HAO ; Shi-Gang ZHANG ; Li-Yong ZHANG ; Wei-Dong LIU ; Kai LIN
Chinese Journal of Surgery 2011;49(2):109-112
OBJECTIVETo evaluate and summarize the possibility and experience of reconstructive vascular operation for kinking of internal carotid artery.
METHODSReconstructive vascular operation was performed on 5 patients with symptomatic kinking of internal carotid artery between July 2008 and June 2009. There were 2 male and 3 female patients, age ranged from 53 to 68 years (mean 62 years). Cutting the internal carotid artery at the bifurcation, mobilizing and stretching the internal carotid artery, then anastomosing the internal and common carotid artery. Two of them underwent endarterectomy simultaneously.
RESULTSFor the 5 patients, postoperative recovery went smoothly and symptoms were well improved. Except that mild high perfusion syndrome happened in 1 patient, no other obvious complications. Kinking of internal carotid artery had been stretched in the postoperative CT angiography. In the 5-16-month follow-up, no transient ischemic attack or cerebral infarction happened, and no restenosis appeared.
CONCLUSIONSReconstructive vascular operation is an effective surgical approach to kinking and coiling of the internal carotid artery. For some risk exists, all-round evaluation should be performed before operation, and operative indication should be strictly controlled.
Aged ; Carotid Artery, Internal ; Carotid Stenosis ; surgery ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Retrospective Studies ; Treatment Outcome ; Vascular Surgical Procedures ; adverse effects ; methods
10.Inhibition of puerarin on sodium-dependent glucose cotransporters 2 to promote urinary glucose excretion
heng Yong SHI ; ying Ying DENG ; ping Ji LIU ; hu En ZHANG
Drug Evaluation Research 2017;40(10):1408-1413
Objective To study that puerarin can prevent the renal glucose reabsorbtion process and promote urinary glucose excretion by inhibiting sodium-dependent glucose cotransporters 2 (SGLT2) to reduce plasma glucose in diabetes rats.Methods Molecular docking was carried out on puerarin and the obtained SGLT2 complexes through homology modeling method with dapagliflozin as positive control.Chinese hamster ovary (CHO) cells stably expressing human SGLT2 and [14C]-MethylD-glucopyranoside ([14C]-AMG) as the substrate were used in vitro for the transport assays and IC50 for SGLT2.The antihyperglycemic activity ofpuerarin was operated by oral glucose tolerance test (OGTT) and urinary glucose excretion (UGE) test in rats.Results Puerarin was identified as the substrate of SGLT2 through molecular docking,but the overall effect was not as strong asdapagliflozin.In vitro experiments showed that puerarin can strongly inhibit hSGLT2,the maximum effect was about 84% with the half inhibitory concentration (IC50) of 0.40 mol/L.OGTT results showed that glucose inhibition rates of puerarin 10,30,60 and 120 mg/kg doses were 5.1%,6.5%,16%,and 22% respectively,in a dose-dependent manner.In the UGE experiment,the urine sugar increased with the increase of puerarin dose.Compared with model group,the 30,60,and 120 mg/kg dose groups had significant difference (P < 0.05 and 0.01).Conclusion Puerarin exhibited antiglycemic activity through inhibiting SGLT2 and was considered to be a new lead compound of SGLT2 inhibitors.