1.Diagnostic value of carotid artery intima-media thickness and plaque formation for coronary heart disease
Nairong DUAN ; Jinling GUAN ; Fang ZHAO ; Yi CAO
Chinese Journal of Primary Medicine and Pharmacy 2012;19(20):3056-3057
ObjectiveTo investigate the relationship between carotid intima-media thickness (IMT)and plaque extent of carotid artery with coronary heart disease (CHD).Methods 131 inpatients were divided into 3 groups,in which 54 cases of coronary heart disease group,46 cases of risk group with coronary heart disease,31 cases of control group.The carotid wall IMT,plaque length and thickness was measured by Color Doppler ultrasound.The obtained data using SPSS 17.0 software for statistical processing.ResultsCarotid intimal thickening and the incidence had no significant difference between the group of coronary heart disease and risk group with coronary heart disease risk( all P > 0.05),carotid artery IMT and incidence rate between the above two groups and the control group had statistical differene( t =3.26,3.48,all P < 0.05 ),and the three groups of carotid artery plaque score and plaque classification were statistically significant( F =4.28,P < 0.05 ).ConclusionCarotid IMT and plaque formation was the independent risk factor of CHD,and it could predict the occurrence and development of CHD,especially in carotid artery plaque specificity is higher,in the primary hospital could be used as the auxiliary examination method of CHD.
2.Bioequivalence of Metoprolol Tartrate Tablets in healthy volunteers
Jing WANG ; Liangqing FU ; Yongbiao GUAN ; Yi FANG ; Zeyuan LIU
Chinese Journal of Clinical Pharmacology and Therapeutics 2004;0(09):-
AIM: To study the bioequivalence of domestic and imported Metoprolol Tartrate Tablets in Chinese healthy volunteers.METHODS: According to the rule published by SFDA,the serum concentration of 20 selected volunteers among 18 to 40 years old was determined by HPLC-fluorescence detection after giving domestic and imported Metoprolol Tartrate Tablets 0.1g,and the pharmacokinetic parameters were calculated by DAS software.RESULTS: The method of HPLC-fluorescence detection to study the pharmakokinetics of Metoprolol Tartrate was sensitive,reliable,accurate and reasonable.The main pharmakokinetics parameters of domestic and imported Metoprolol Tartrate Tablets were T_(max):(1.11)?(0.36 h) and(1.39)?(0.65 h) respectively;C_(max):(269.20)?(87.15)(?g?L~(-1)) and(262.03)?(75.52)(?g?L~(-1)) respectively;AUC_(0-12h):(1088.91)?(510.52)(?g?L~(-1)?h) and(1098.29)?5(55.14)(?g?L~(-1)?h) respectively.The relative bioavailability of domestic Metoprolol Tartrate Tablets was(100.09)%.CONCLUSION: The domestic and imported Metoprolol Tartrate Tablets was bioequivalents.
3.Pharmacokinetics and biodistribution of 11C-HupA in the normal animal
Jin, YAN ; Yi-hui, GUAN ; Fang-ping, XUE ; Zheng-wei, ZHANG ; Ping, LIU ; Xiang-tong, LIN
Chinese Journal of Nuclear Medicine 2009;29(2):109-112
Objective HupA is one of the potential drugs which can be used to treat Alzheimer's disease(AD).The aim of this study was to explore the pharmacokinetics and biodistribution of HupA in vivo by using 11C-HupA.Methods A total of 25 SD rats were studied.They were divided into 5 groups (5 rats in each group).All had intravenous injection of 22 MBq(in0.2 ml)11C-HupA through tail vein.Dynamic im-aging Was acquired from 5 to 90 minutes after injection.Venous blood and organ activities were collected at 5,15,30,60.and 90 minutes after injection.Percentage activity of injected dose per gram of tissue(%ID/g)was calculated to characterize the biodistribution of tracer in different brain regions: frontal,apical, temporal,occipital,cerebellum,hippocampus,striatum,thalamencephalon, and brain stem, Variance analysis using SPSS 11.5 software was performed and compared among the study groups.Results 11C-HupA was character-istic for its quick clearance from blood,with half time T1/2 of (14.61±1.77) min,and clearance rate (CL)macokinetics of 11C-HupA in rats corresponded to a one-compartment model.with an activity curve(area 11C-HupA distribution in different brain regions,being greater in cerebral cortex,hippocampus,hypothala-mus and brain stem. Conclusions Pharmacokinetic study of 11C-HupA in brain was fast.convenient and showed high specificity and sensitivity.Its ability to quantitatively evaluate brain function and its character-istic distribution in mice provided some evidence for monitoring therapy in AD patients.
5.Evaluation of the preventive effect of DL0805-2 against monocrotaline induced rat pulmonary arterial hypertension
Di CHEN ; Tian-yi YUAN ; Yu-cai CHEN ; Hui-fang ZHANG ; Zi-ran NIU ; Lian-hua FANG ; Guan-hua DU
Acta Pharmaceutica Sinica 2021;56(1):208-216
In the treatment of hypertensive crisis, the novel Rho kinase inhibitor DL0805-2 can rapidly lower systematic blood pressure, reduce pulmonary artery pressure, and has a significant protective effect on lung injury. This experiment intends to evaluate the efficacy of DL0805-2 against pulmonary arterial hypertension (PAH) and preliminarily reveals its underlying mechanism. Animal welfare and experimental procedures are in accordance with the provision of the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences. Sprague Dawley (SD) rats were randomly divided into DL0805-2 low, medium, and high dose groups (1, 3, and 10 mg·kg-1), bosentan positive control group, model group, and blank control group. The drug was administered daily on the 7th day after model establishment by monocrotaline injection. On the 25th day of the experiment, relevant indicators were examined to observe the therapeutic effect of DL0805-2 on pulmonary hypertension. DL0805-2 significantly relieved the abnormal changes in the physiological parameters related to PAH induced by monocrotaline, including reducing right ventricular systolic pressure, alleviating cardiac damage caused by pressure overload, and reducing the levels of endothelin-1 and inflammatory factors in lung tissues. DL0805-2 also attenuated pulmonary arteries remodeling. It was preliminarily discovered that DL0805-2 exerts preventive and therapeutic effect on PAH through Rho-kinase pathway. Our results suggested that DL0805-2 had good therapeutic effects on monocrotaline-induced PAH rat model. It intervened early in the disease process, effectively prevented the development of the disease, and reduced the mortality of the diseased animals. The mechanism is related to Rho-kinase pathway.
6.Curcumin,from health product to medicine
Tian-Yi YUAN ; Di CHEN ; Lian-Hua FANG ; Guan-Hua DU
Chinese Journal of Pharmacology and Toxicology 2018;32(4):328-328
Curcumin is the principal curcuminoid of the rhizomes of Curcuma longa(turmeric,Jiang Huang), which has more than 6000 years of application history in India and other Asian countries. At present,curcumin is sold as an herbal supplement,cosmetics ingredient,food flavoring,and food coloring. In China curcumin is mainly used in food, while in western countries it has been regarded as a health care product and is contained in the British Pharmacopoeia (2017), United States Pharmacopeia (40) and European Pharmacopoeia (8.7th ed.). Curcumin has been proved to have multiple pharmacology effects including anti-fibrosis, anti-tumor, anti-inflammation effects and so on. As its broad biological activities, it is applicated in a lot of diseases such as hyperlipidemia, infection and cancer. Among them, the anti-cancer effect of curcumin is the most attractive. In the treatment of cancer and related diseases, curcumin has been tested in phase I and II clinical trials in several research centers across the world and has been approved by the U.S.FDA into the phase III clinical trial.It has been listed as the third generation of cancer chemoprevention agent by the U.S.National Cancer Institute.Curcumin has been proved to inhibit the proliferation of a variety of tumor cells through regulating a variety of tran-scription factors(NF-κB,AP-1,etc),mitogen-activated protein kinase(MAPK),growth factor receptor ki-nase(PDGFR,VEGFR,etc)and cyclooxygenase.It plays an important role in the cell cycle and further to inhibit proliferation.Curcumin can also inhibit the migration of tumor cells by activating caspase and in-ducing tumor cell apoptosis.However,curcumin still needs researches to confirm its effects and mecha-nisms and find its exact indications. There is still a long way to go to make curcumin better applied in clinical practice in the further.
7.Puerarin reduces oxidative damage to vascular endothelial cells by improving mitochondrial respiratory function
Shu-chan SUN ; Di-fei GONG ; Tian-yi YUAN ; Shou-bao WANG ; Lian-hua FANG ; Guan-hua DU
Acta Pharmaceutica Sinica 2022;57(5):1352-1360
This study investigated the effect of puerarin on human umbilical vein endothelial cells (HUVEC) injured with hydrogen peroxide (H2O2). HUVEC were divided into three groups: a control group, a model group (H2O2 400 μmol·L-1) and a puerarin-treated group (3, 10, 30 and 100 μmol·L-1). HUVEC were cultured with varied concentration of puerarin for 2 h and treated with H2O2 for another 24 h. Cell proliferation was detected by a CCK-8 assay. The mitochondrial membrane potential was measured by a JC-1 fluorescent probe. A transwell chamber assay was adopted to observe cell migration ability. Mitochondrial respiratory function was measured in a two-chamber titration injection respirometer (Oxygraph-2k). The expression of interleukin-1
8.Research progress in drugs targeting tumor associated macrophage
Li-wen REN ; Yi-hui YANG ; Wan LI ; Yi-zhi ZHANG ; Hong YANG ; Sen ZHANG ; Fang XU ; Yue HAO ; Wan-xin CAO ; Guan-hua DU ; Jin-hua WANG
Acta Pharmaceutica Sinica 2023;58(12):3508-3518
Tumor brings great threat to human public health. In recent years, incidence rate and mortality of tumor were rapidly increased in the world. Anti-tumor therapies have undergone the development of cytotoxic therapy, targeted therapy, and immunotherapy. Among them, tumor immunotherapy is rapidly developed and becomes an important anti-tumor therapy in recent years, although it also brings some related side effects. Tumor microenvironment (TME) is composed of immune cells, vascular vessels, fibroblasts, the extracellular matrix, etc. TME significantly affects the efficacy of immunotherapy. Macrophages in the TME are named as tumor associated macrophages (TAMs). Recently, increasing studies have shown that TAMs play an important role in the regulation of tumor immunity, especially in tumor immune surveillance and immune escape. Currently, more and more anti-tumor immunotherapy strategies targeting TAMs are at the development stage. Based on the important role of TAMs in the TME and their potential as therapeutic targets in tumor immunotherapy, we first reviewed the subtypes and functions of TAMs, as well as the roles of TAMs in tumors. Furthermore, we summarized the research progress on anti-tumor strategies targeting TAMs and the current status of drug targeting TAMs. The current review will provide new ideas and novel insights for tumor immunotherapy.
9.Identification and expression analysis of a full-length cDNA encoding a Kandelia candel tonoplast intrinsic protein.
Wei HUANG ; Xiao-Dong FANG ; Qi-Fen LIN ; Guan-Yi LI ; Wen-Ming ZHAO
Chinese Journal of Biotechnology 2003;19(2):147-152
Soil salinity is an important issue, as most crop plants are low in salt tolerance. Salt tolerance, a complex, multifactorial, and multigenic process, has been known to be a quantitative trait. The identification of the salt stress responsive genes or salt tolerance genes is essential for the breeding programs. Most recent efforts have been focused on the products of structural genes (transport proteins, ion channels, enzymes of solute synthesis) while little attention were paid to the regulatory aspects of these proteins. Since the first aquaporin gene from plants was cloned and functionally expressed in 1993, there has been a growing interest in the molecular biology of MIPs (membrane intrinsic proteins) and their bearing on the biophysics of water flow across plant membranes. In the last decades, studies on Mangroves, a special kind of wood plants, grow in high-salt and flooding conditions have been concentrated almost exclusively on their physiological and ecological characteristics. Kandelia candel, one of the dominant species of mangroves along the Chinese coast, lacks salt glands or salt hairs used for removal of excess salt in other mangroves. This makes K. candel a perfect model to study the molecular mechanism of salt tolerance in mangrove plants. Using cDNA RDA, a cDNA-specific modification of genomic representational difference analysis, a series of salt responsive genes of Kandelia candel were cloned. Among these gene fragments, a 183 bp fragment (termed as SRGKC1) encoding a tonoplast intrinsic protein (TIP) in Kandelia candel (KCTIP1) was identified. Based on the sequence of SRGKC1, two gene specific primers were designed, and the 3' and 5' end of the KCTIP1 gene were obtained using the SMART RACE cDNA Amplification Kit. RACE products were purified from low-melting agarose, and sequenced directly with GSPs as the sequencing primers. A 500-bp fragment corresponding to the 3'end of this gene was obtained using the GSP1 primer, and a 690 bp fragment corresponding to the 5' end of this gene was obtained using the GSP2 primer. Two primers that flank the putative open reading frame (ORF) were designed to obtain the cDNA containing the complete ORF by RACE PCR reaction. The full-length cDNA of KCTIP1, containing a 756 bp open reading frame (ORF), was approximately 1.1 kb; the start codon was located at the nucleotides of 99-101 and stop codon at the nucleotides of 855-857 followed by a poly (A) tail. The KCTIP1 cDNA sequence in this research was released in GenBank with accession number AF521135. Using ExPASy Proteomics tools provided by EMBL, the isoelectric point and MWt of KCTIP1 are estimated as 5.77 and 26.3 kD respectively. Transmembrane prediction analysis revealed the deduced KCTIP1 protein sequence contains six transmembrane regions at amino acid residues of 20 - 42, 57 - 79, 86 - 108, 113 - 135, 142 - 164 and 217 - 239. Two highly conserved asparagine-proline-alanine (NPA) motifs were located at 85 - 87 and 199 - 201 amino acid residues respectively. KCTIP1 is also predicted to contain the Cys residue (Cys 118) that are shown to confer Hg-sensitivity in Arabidopsis gamma-TIP and delta-TIP. Similarity analysis showed that KCTIP1 shared 77% - 79% amino acid sequence identity with the TIPs from Vitis berlandieri, Brassica oleracea and Arabidopsis thaliana. Expression analyses indicated that KCTIP1 had different expression among species of Mangroves. Expressions of KCTIP1 in Kandelia candel, Rhizophora apoculata and Ceriops tagal were suppressed by salt, and were insensitive to salt stress in unknown species of Mangroves. Previous studied showed that salt conditions might result in large and rapid changes in extracellular water potential and serious disturbance to the cytoplasm. In order to compensate for this imbalance, the relative contribution of water channels to flow across the root could thus vary. K. candel is a species that is native to intertial zone of tropical and subtropical coast and is well-adapted to salt conditions. The coordinated down-regulation of aquaporins in this plant may decrease membrane water permeability and thus increase the cellular water conserva- tion during periods of salt stress. The results reported here are consistent with the postulated roles for tonoplast water channels in regulating the hydraulic permeability of the vacuolar membranes and in adjusting the water homeostasis of the protoplasm under various physiological conditions. The identification of KCTIP1 as one of salt-responsive genes implies that intracellular osmotic equilibration is a part of salt-tolerant mechanisms in Mangroves.
Amino Acid Sequence
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Base Sequence
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Blotting, Northern
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DNA, Complementary
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genetics
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Membrane Proteins
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chemistry
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genetics
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Molecular Sequence Data
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Nucleic Acid Amplification Techniques
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Plant Proteins
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chemistry
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genetics
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Rhizophoraceae
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genetics
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Sequence Alignment
10.A study of recompression treatment schedule for treating type I decompression illness with medical hyperbaric chamber pressurized.
Ya-dong GUAN ; Zhen WANG ; Dong-sheng LI ; Yi-qun FANG ; Zhi-qiang HUANG
Chinese Journal of Industrial Hygiene and Occupational Diseases 2011;29(5):374-376
OBJECTIVETo observe the therapic effects of the recompression treatment schedule D2 (breathing 100% oxygen at 0.12 MPa gauge pressure) on the type I decompression illness (DCI) by hyperbaric chamber pressurized with air.
METHODSThe recompression treatment schedule D2 was from the decompression treatment tables of
RESULTSIn the work site group, the pains of joints, arms and legs were released quickly, the therapic effects appeared at (8.1 +/- 8.1) min, the cases were cured with a recompression therapy of basic schedule D2, the total mean time of treatment was (150 +/- 0.0) min. In the hospital group, the pains of joints, arms and legs disappeared slowly, the therapic effects appeared at (115.0 +/- 60.0) min, the cases were cured with a recompression therapy of extended schedule D2, the total mean time of treatment was (270.0 +/- 0.0) min, which was significantly longer than that in the work site group (P<0.01).
CONCLUSIONSThe treatment pressure is 0.12 MPa(gauge pressure) in schedule D2 with medical hyperbaric chamber pressurized with air,which can be used for treatment of type I DCI, the curative effects in the work site group are better than those in the hospital group.
Adult ; Decompression ; methods ; Decompression Sickness ; therapy ; Diving ; Humans ; Hyperbaric Oxygenation ; methods ; Male ; Middle Aged ; Oxygen Inhalation Therapy ; Treatment Outcome