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Article in English | WPRIM | ID: wpr-881086


Natural product bufotenine (5) which could be isolated from Venenum Bufonis, has been widely used as a tool in central nervous system (CNS) studies. We present here its quaternary ammonium salt (6) which was synthesized with high yields using 5-benzyloxyindole as raw materials, and we firstly discover its analgesic effects in vivo. The analgesic evaluation showed that compounds 5 and 6 had stronger effects on the behavior of formalin induced pain in mice. Moreover, the combination of compound 6 and morphine has a synergistic effect. We intended to explain the molecular mechanism of this effect. Therefore, 36 analgesic-related targets (including 15 G protein-coupled receptors, 6 enzymes, 13 ion channels, and 2 others) were systemically evaluated using reverse docking. The results indicate that bufotenine and its derivatives are closely related to acetyl cholinesterase (AChE) or α

Article in Chinese | WPRIM | ID: wpr-921533


Objective To evaluate the effects of antiretroviral therapy(ART)for the prevention of mother-to-child transmission(PMTCT)of acquired immune deficiency syndrome(AIDS)on the growth and development of 18-month-old children born by human immunodeficiency virus(HIV)-positive pregnant women in Lingshan County,Guangxi Zhuang Autonomous Region,and provide scientific evidence for improving the ART medication plan for PMTCT.Methods Lingshan County,ranking the first in the HIV-epidemic counties of Guangxi,was selected as the research site.According to the design of retrospective case-control study,we assigned all the subjects into the case group and the control group:(1)The case group included the HIV-positive pregnant women who had received ART for PMTCT and their HIV-negative infants in Lingshan County from 2010 to 2017.The historical cards and PMTCT data of them were collected from the national PMTCT database.(2)The control group included the healthy pregnant women and their healthy babies born in the Lingshan Maternity and Infant Hospital in 2017,and the children's growth and development data were collected.The stunted growth in children was defined as at least one of the three main indicators of body height,body weight,and head circumference below the normal range.Results The number of HIV-positive mothers and their infants in the case group was 391 and 368,respectively,and 87.21%(341/391)and 95.38%(351/368)of mothers and infants respectively received ART medication.The HIV positive rate,mortality rate,and mother-to-child transmission rate of 18-month-old children were 1.36%(5/368),4.35%(16/368),and 2.01%(5/249),respectively.The incidence of stunted growth of 18-month-old children in the case group and the control group was 42.12%(155/368)and 23.06%(101/438),respectively,with significant difference(

Case-Control Studies , China/epidemiology , Female , Growth and Development , HIV , HIV Infections/prevention & control , Humans , Infant , Infectious Disease Transmission, Vertical/prevention & control , Mothers , Pregnancy , Pregnancy Complications, Infectious/drug therapy , Retrospective Studies
Article in English | WPRIM | ID: wpr-810980


OBJECTIVE: We aimed to investigate the ability of readout-segmented echo-planar imaging (rs-EPI)-based diffusion tensor imaging (DTI) in assessing the microstructural change of extraocular muscles (EOMs) and optic nerves in patients with thyroid-associated orbitopathy (TAO) as well as in evaluating disease activity.MATERIALS AND METHODS: We enrolled 35 TAO patients and 22 healthy controls (HCs) who underwent pre-treatment rs-EPI-based DTI. Mean, axial, and radial diffusivity (MD, AD, and RD) and fractional anisotropy (FA) of the medial and lateral EOMs and optic nerve for each orbit were calculated and compared between TAO and HC groups and between active and inactive TAO groups. Factors such as age, sex, disease duration, mediation, and smoking history between groups were also compared. Logistic regression analysis was used to evaluate the predictive value of significant variables for disease activity.RESULTS: Disease duration was significantly shorter in active TAOs than in inactive ones (p < 0.001). TAO patients showed significantly lower FA and higher MD, AD, and RD than HCs for both medial and lateral EOMs (p < 0.001), but not the AD value of lateral EOMs (p = 0.619). Active patients had significantly higher FA, MD, and AD than inactive patients for medial EOMs (p < 0.005), whereas only FA differed significantly in the lateral EOMs (p = 0.018). The MD, AD, and RD of optic nerves were significantly lower in TAO patients than HCs (p < 0.05), except for FA (p = 0.129). Multivariate analysis showed that the MD of medial EOMs and disease duration were significant predictors for disease activity. The combination of these two parameters showed optimal diagnostic efficiency for disease activity (area under the curve, 0.855; sensitivity, 68.4%; specificity, 96.9%).CONCLUSION: rs-EPI-based DTI is promising in assessing microstructural changes of EOMs and optic nerves and can help to indicate the disease activity of TAO, especially through the MD of medial EOMs.

Anisotropy , Diffusion Tensor Imaging , Diffusion , Echo-Planar Imaging , Humans , Logistic Models , Multivariate Analysis , Muscles , Negotiating , Optic Nerve , Orbit , Sensitivity and Specificity , Smoke , Smoking , Troleandomycin
Chinese Journal of Cardiology ; (12): 795-799, 2013.
Article in Chinese | WPRIM | ID: wpr-261466


<p><b>OBJECTIVE</b>To explore the association between CYP11B2 gene polymorphism and essential hypertension, blood pressure level in Chinese Han population by meta-analysis.</p><p><b>METHODS</b>After searching database, the research quality was quantified according to NOS. Genetic model, heterogeneity, publication bias, overall OR/standardized mean difference (SMD) and 95%CI were explored by Stata, 19 studies including 9249 subjects were included in this meta-analysis.</p><p><b>RESULTS</b>Compared to control group, OR(95%CI) of CC vs. TT, CT vs. TT, CC vs. CT in essential hypertensive patients were 1.022(95%CI: 0.879-1.190), 1.108 (95%CI: 0.951-1.291), 1.050(95%CI:0.995-1.109), respectively; SMD (95%CI) was 0.315 (0.066-0.565, P < 0.05) for systolic pressure derived CC vs. TT, and 0.088 (0.014-0.162, P < 0.05) for CT vs.</p><p><b>TT CONCLUSION</b>Individuals with -344C CYP11B2 allele are at higher risk of increased systolic blood pressure, but there is no evidence showing association between CYP11B2 polymorphism and susceptibility of essential hypertension in Chinese Han population.</p>

Asian Continental Ancestry Group , Genetics , Cytochrome P-450 CYP11B2 , Genetics , Essential Hypertension , Genetic Predisposition to Disease , Genotype , Humans , Hypertension , Genetics , Polymorphism, Single Nucleotide
Acta Pharmaceutica Sinica ; (12): 29-33, 2004.
Article in Chinese | WPRIM | ID: wpr-301155


<p><b>AIM</b>To investigate the inhibitory effects of artesunate on angiogenesis.</p><p><b>METHODS</b>The in vitro anti-angiogenic effect of artesunate was tested on models of angiogenesis: proliferation, migration and tube formation of human umbilical vein endothelial (HUVE) cells; The anti-angiogenic effect in vivo was evaluated in nude mice by means of human ovarian cancer HO-8910 implantation and immunohistochemical stainings for microvessel (CD31), vascular endothelial growth factor (VEGF) and VEGF receptor KDR/flk-1.</p><p><b>RESULTS</b>Artesunate significantly inhibited angiogenesis in a concentration-dependent form in range of 0.5-50 mumol.L-1. The IC50 of artesunate for HUVE cells was (21 +/- 3) mumol.L-1. Growth of xenograft tumor was decreased and microvessel density was reduced following drug-treatment with no apparent toxicity to the animals. Artesunate also remarkably lowered VEGF expression on tumor cells and KDR/flk-1 expression on endothelial cells as well as tumor cells.</p><p><b>CONCLUSION</b>Artesunate was shown to inhibit angiogenesis in vitro and in vivo. These findings together with the known low toxicity of artesunate are clues that artesunate may be a promising angiogenesis inhibitor.</p>

Angiogenesis Inhibitors , Pharmacology , Animals , Artemisia , Chemistry , Artemisinins , Pharmacology , Endothelial Cells , Cell Biology , Female , Humans , Male , Mice , Mice, Inbred BALB C , Mice, Nude , Neoplasm Transplantation , Ovarian Neoplasms , Metabolism , Pathology , Receptors, Vascular Endothelial Growth Factor , Sesquiterpenes , Pharmacology , Tumor Cells, Cultured , Umbilical Veins , Cell Biology , Vascular Endothelial Growth Factor Receptor-2