1.Research progress of natural products for the treatment of hyperuricemia and gout
Zhi-jiao ZHANG ; Rui-peng LIANG ; Tong ZHAO ; Shu-jing XU ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(6):1679-1688
Although current synthetic anti-gout drugs have significant therapeutic effects in reducing serum uric acid levels, they have serious side effects such as allergic reactions and liver and kidney damage. Natural products with a wide range of uric acid-lowering and high safety have played a critical role in anti-gout drug discovery and development. This paper reviews the natural products with uric acid-lowering or anti-gout pharmacological effects and the investigation on their mechanisms of action, to provide information for drug discovery and development.
2.A preliminary study of the relationship of MR delayed enhancement with cardiac troponin Ⅰ in hypertrophic cardiomyopathy
Jun-Yan SUN ; Zhao-Qi ZHANG ; Yi HE ; Teng-Yong JIANG ; Yu LI ; Zhan-Ming FAN ; Yong-Mei WANG ;
Chinese Journal of Radiology 2001;0(08):-
Objective To study the relationship of MR delayed enhancement with cardiac troponin I in hypertrophic cardiomyopathy(HCM)and to evaluate their values on assessing HCM condition and prognosis.Methods Thirty-five HCM patients who were diagnosed by echocardiography were enrolled.All patients were performed MR scan and cTn Ⅰ test of blood.The relationships of MR delayed enhancement, myocardial hypertrophy and cTn Ⅰ were analyzed.Results(1)DE was found in 25 of total 35 HCM patients(71.4%).19 of 35 HCM patients(54.3%)had abnormal increased eTn Ⅰ value.The medians of cTn Ⅰ in patients with DE and without DE(110,5 ?g/ml,respectively)had statistics significance (P
3.Effect of portal vein blocking on permeability of the intestinal mucosa in pigs
Jian-Yong ZHAO ; Jia-Hong DONG ; Guo-Qing ZHAN ; Huai-Zhi WANG ; Zhan-Yu YANG
Journal of Third Military Medical University 2001;23(4):432-433
Objective To study the effect of portal vein blocking on the permeability of the intestinal mucosa in pigs. Methods Healthy Rongchang pigs were divided into 3 groups: ① sham operation group(SO), ② portal vein clamping for 45 min group (PVC-45'), ③ portal vein clamping for 60 min group (PVC-60'). Urine lactulose/mannitol(L/M) ratio was measured after portal vein blocking. Results The L/M ratio was increased significantly (P<0.05) in PVC-45' and 60' groups than in SO group, with that of PVC-60' higher than that of PVC-45' group, but not significantly. Conclusion The increase of intestinal mucosal permeability after portal vein blocking is an early and important index for the damage of the intestinal mucosa barrier.
4.Advances in the research of HIV-1 envelope glycoprotein gp120 inhibitors
Ming-hui XIE ; Zhao WANG ; Yan-ying SUN ; Xiang-yi JIANG ; Peng ZHAN ; Xin-yong LIU ; Dong-wei KANG
Acta Pharmaceutica Sinica 2023;58(3):616-628
From the process of human immunodeficiency virus-1 (HIV-1) invading cells, the combination of gp120 and CD4 is the first step for HIV-1 to invade cells. Interfering with this process can prevent HIV from recognizing target cells and inhibit virus replication. Therefore, HIV-1 gp120 is an important part of the HIV-1 life cycle. Fostesavir, a phosphatate prodrug derived from the gp120 inhibitor BMS-626529 modified by the prodrug strategy, was approved for the treatment of adult patients with multidrug resistant HIV-1 infection by the US FDA and the European Medicines Agency in 2020 and 2021, respectively. In this review, we focus on the research progress of small molecule inhibitors targeting the interaction of gp120-CD4 from the perspective of medicinal chemistry, in order to provide reference for the subsequent research of gp120 inhibitors.
5.Related risk factors analysis of pancreatic fistula after radical resection of gastric cancer and establishment of risk prediction scoring model
Ping'an DING ; Zhidong ZHANG ; Peigang YANG ; Yuan TIAN ; Shixin ZHAN ; Honghai GUO ; Yang LIU ; Dong WANG ; Yong LI ; Qun ZHAO
Cancer Research and Clinic 2021;33(2):104-108
Objective:To investigate the risk factors of pancreatic fistula after radical resection of gastric cancer, and to establish a risk prediction scoring model for pancreatic fistula.Methods:The clinico-pathological data of 312 patients with gastric cancer admitted to the Fourth Hospital of Hebei Medical University from January 2019 to January 2020 were retrospectively analyzed. Multiple factor logistic regression model was used to analyze the risk factors of pancreatic fistula after radical resection of gastric cancer, and a risk prediction scoring model based on the risk factors was established. Hosmer-Lemeshow test was used to detect the goodness of fit of regression equation, and receiver operating characteristics (ROC) curve was used to evaluate the distinction degree of regression equation.Results:Among 312 patients with gastric cancer, 27 cases (8.65%) had pancreatic fistula after radical resection of gastric cancer. Multiple factor logistic regression analysis showed that male patients ( OR = 5.312, 95% CI 1.532-18.420, P = 0.008), age ≥ 60 years old ( OR = 4.928, 95% CI 1.493-16.250, P = 0.009), preoperative diabetes mellitus ( OR = 3.062, 95% CI 1.091-8.589, P = 0.034), lesion location in the gastric body-gastric antrum ( OR = 3.121, 95% CI 1.052-9.251, P = 0.040), intraoperative omental bursa resection ( OR = 6.209, 95% CI 2.084-18.478, P = 0.001), intraoperative lymph node dissection at D2+ station ( OR = 3.114, 95% CI 1.044-9.281, P = 0.042), intraoperative combined organ resection ( OR = 5.063, 95% CI 1.473-17.400, P = 0.010), preoperative TNM stage Ⅲ ( OR = 4.973, 95% CI 1.189-20.792, P = 0.028) were independent risk factors for pancreatic fistula after radical resection of gastric cancer. A risk prediction equation of pancreatic fistula after radical resection of patients with gastric cancer was established: P = -8.619+1.670X 1+1.595X 2+1.119X 3+1.138X 4+1.826X 5+1.136X 6+1.622X 7+1.604X 8; factor X was set as a binomial assignment (0 or 1); X1-X8 were listed as follows respectively: gender (the male was 1), age (≥60 years old was 1), preoperative diabetes history (yes was 1), lesion location (gastric body-gastric antrum was 1), intraoperative resection of omental bursa or not (yes was 1), intraoperative lymph node dissection at D2+ station or not (yes was 1), intraoperative combined organ resection or not (yes was 1), preoperative TNM stage (stage Ⅲ was 1). The goodness of fit of regression equation was high ( P = 0.395). The area under the curve of ROC by using risk prediction scoring model to judge pancreatic fistula was 0.916 (95% CI 0.872-0.960, P<0.01). The probability of pancreatic fistula in patients with score ≥ 5 was 40.90%, and the probability of pancreatic fistula in patients with score < 5 was 3.35%. Conclusions:The occurrence of pancreatic fistula after radical resection of gastric cancer is closely related to a variety of risk factors. By establishing a risk prediction scoring model for pancreatic fistula after radical resection of gastric cancer, it is helpful to effectively identify patients with high risk of pancreatic fistula after radical surgery during the perioperative period.
6.Research progress and medicinal chemistry strategies of URAT1 inhibitors
Xiao-yu SHI ; Tong ZHAO ; Jian ZHANG ; Rui-peng LIANG ; Zhi-jiao ZHANG ; Xin-yong LIU ; Peng ZHAN
Acta Pharmaceutica Sinica 2022;57(10):2960-2971
The urate transporter 1 (URAT1) which controls urate reabsorption is a membrane transporter in the apical membrane of human renal proximal tubule epithelial cells. It was found that about 90% of patients suffer from hyperuricemia due to insufficient uric acid excretion. Therefore, the development of URAT1 inhibitors that can reduce the level of serum uric acid
7.Apoptosis of human gastric cancer cells induced by omega-3 polyunsaturated fatty acids.
Yong YIN ; Wen-Hua ZHAN ; Jun-Sheng PENG ; Zong-Gang ZHAO
Chinese Journal of Gastrointestinal Surgery 2007;10(6):570-573
OBJECTIVETo investigate the effect of omega-3 polyunsaturated fatty acids(omega-3PUFAs) on the apoptosis of human gastric cancer cell line SGC-7901 and to explore the potential mechanisms.
METHODSCells were treated with eicosapentaenoic acid (20:5 omega-3,EPA) or docosahexaenoic acid (22:6 omega-3, DHA) at concentrations of 10, 20 and 40 microg/ml. Cell growth and apoptosis were analyzed with MTT assay, cell morphology, DNA electrophoresis and flow cytometry. Mitochondrial membrane potential ( triangle right psi mt) was measured by fluorescent probe rhodamine 123. The distribution of cytochrome C in mitochondria and cytosol was determined by enzyme-linked immunoadsorbent assay. The composition of mitochondrial membrane phospholipid(MMP)was examined by gas chromatography.
RESULTSBoth EPA and DHA markedly inhibited the SGC-7901 cell growth and induced apoptosis in a time- and dose-dependent manner. After incubation of the cells with 40 microg/ml EPA or DHA for 24 hours, the level of Deltapsimt siginificantly decreased (P<0.001), and cytochrome C largely released into cytosol from mitochondria. The proportions of EPA and DHA in MMP rapidly elevated while that of arachidonic acid sharply decreased.
CONCLUSIONSomega-3PUFAs inhibit the growth of gastric cancer cells through promoting apoptosis. Compositional and functional alterations in mitochondrial membrane may be an important initiator of apoptosis induced by omega-3PUFAs.
Apoptosis ; drug effects ; Cell Line, Tumor ; Cytochromes c ; metabolism ; Fatty Acids, Omega-3 ; pharmacology ; Humans ; Membrane Potential, Mitochondrial ; Mitochondria ; metabolism ; pathology ; Stomach Neoplasms ; metabolism
8.Clinical observation on the paraumbilical skin flaps application in the repair of the wounds of 39 patients with severe burns.
Qiang WANG ; Yu-ling ZHAO ; Quan-bin CAO ; Zhan-jie YANG ; Dian-yong ZHU
Chinese Journal of Burns 2006;22(4):266-268
OBJECTIVETo evaluate the effectiveness of paraumbilical skin flaps for the repair of the severe burn wounds.
METHODSPedicled, island, or free paraumbilical skin flaps, as well as combined transplantation of several kinds of flaps were used to repair the wounds of 39 patients with severe burns. The largest paraumbilical skin flap was 55 x 27 cm(2) in area, with the end approaching the armpit midline of the axilla on the same side, and extending 10cm from the abdominal midline. The survival, color, elasticity of the flaps, degree of deformity resulted from scar contracture, and the condition of donor area were observed.
RESULTSAll the paraumbilical skin flaps survived, without obvious infection subsequent to complete debridement of the wounds. The flaps exhibited good color and elasticity, without scar contracture after 1 to 46 months in 33 patients. No obvious scar formation was observed in the donor area.
CONCLUSIONParaumbilical skin flap is an ideal one for the early repair of deep burn wounds, because it can cover a large area, and can be transferred in different ways according to the area and the position of the wounds.
Adolescent ; Adult ; Burns ; surgery ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Reconstructive Surgical Procedures ; Skin Transplantation ; methods ; Surgical Flaps ; Thorax ; Umbilicus ; Wound Healing
9.The regulation effect of interleukin-1 on expression of cartilage specificity gene Sox9 mRNA in the human intervertebral discs.
Yong ZHAO ; Wen-bo WANG ; Yu LU ; Yun GE ; Zhan-ge YU ; Fei XUE
Chinese Journal of Surgery 2006;44(24):1704-1707
OBJECTIVETo assess the regulating effects of interleukin-1 (IL-1) on gene expression of cartilage specificity gene Sox9 and type II collagen mRNA in the human intervertebral discs.
METHODSRT-PCR were used to investigate the effects of IL-1 on gene expression of Sox9 and type II collagen mRNA in intervertebral discs cells cultures of embryo.
RESULTSThe Sox9 and type II collagen mRNA in intervertebral discs were decreased progressively along with the addition concentrations of IL-1 than the controls. And the mRNA of Sox9 and type II collagen also markedly decreased with the time of culture.
CONCLUSIONSIL-1 could cause dose-dependent and time-dependent inhibition effects on Sox9 and type II collagen gene expression in human intervertebral discs.
Cells, Cultured ; Collagen Type II ; genetics ; Dose-Response Relationship, Drug ; Gene Expression ; drug effects ; High Mobility Group Proteins ; genetics ; Humans ; Interleukin-1 ; pharmacology ; Intervertebral Disc ; cytology ; drug effects ; metabolism ; RNA, Messenger ; genetics ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; SOX9 Transcription Factor ; Time Factors ; Transcription Factors ; genetics
10.Influence of Migu capsule and strengthening spleen prescription on the expression of small intestine VDR mRNA in calf muscle on ovariectomized rats.
Li-Tong WANG ; Yong-Fang ZHAO ; Xiang WANG ; Yu XU ; Yuan-Chuan CHEN ; Hong-Sheng ZHAN
China Journal of Orthopaedics and Traumatology 2009;22(5):367-370
OBJECTIVETo observe the effect of Migu capsule and Strengthening Spleen prescriptions on the expression of vitamin D receptor on small intestine and calf muscle of the rat, while observing whether the Chinese medicine complex prescriptions of different effect such as invigorating the kidney and strengthening the spleen had selectivity to expression of the VDR mRNA.
METHODSCopy the model of osteoporosis by ovariectomy operation, the rats were randomly divided into four groups, pseudo-resection group, model group, Migu capsule group and strengthening Spleen prescriptions group. Drug delivery 12 weeks later from operation, stomach lavage last for 12 weeks. Then, to observe the effect of medicine on the rats' bone mineral density, uterus weight, calf muscle/weight, and the VDR mRNA in small intestine and calf muscle through RT-PCR.
RESULTSMigu capsule enhanced bone mineral density (P<0.05), raised calf muscle/weight (P<0.05), up-regulated expression of calf muscle VDR mRNA in the small intestine (P<0.01). Strengthening Spleen prescriptions remained bone mineral density (P>0.05), up-regulated expression of calf muscle VDR mRNA (P<0.01), there was no obvious difference in uterus weight in Migu capsule group and Strengthening Spleen prescription group.
CONCLUSIONMigu capsule and Strengthening Spleen prescriptions can cure osteoporosis by improving the expression of calf muscle VDR mRNA in the small intestine.
Animals ; Bone Density ; Capsules ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Gene Expression Regulation ; drug effects ; Intestine, Small ; drug effects ; metabolism ; Muscle, Skeletal ; drug effects ; metabolism ; Osteoporosis ; metabolism ; prevention & control ; Ovariectomy ; Prescriptions ; RNA, Messenger ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Receptors, Calcitriol ; genetics ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction ; Spleen ; drug effects ; metabolism