1.Expression of CD44v6 protein in human breast carcinoma and its relevance for prognosis
Lin-Xiang SHI ; Hai-Bao TONG ; Qing LI ; Al ET
China Oncology 2001;0(05):-
Purpose:To study the expression of CD44v6 protein in breast carcinoma and its prognostic significance. Methods:100 cases of formalin-fixed paraffin-embeded female breast invasive ductal carcinoma tissues were retrospectively analyzed using EnVision~(TM) immunohistochemical method with the monoclonal antibody CD44v6.Statistical analysis was based on the Log-rank test and Cox analysis.Results:Sixty-six of 100 cancer tissues expressed CD44v6.Positive staining was mainly on the cell membranes.There was significant correlation between CD44v6 immunoreactivity and lymph node me- tastasis and TNM stage.The 5-and 10-year survival rates were 82.76% and 78.37% of patients with CD44v6 low-expres- sion tumors,and 64.1% and 49.88% of those with CD44v6 high-expression tumors,respectively;the difference between the two groups of patients was significant(P
2.Clinical anti-ischemic effects of trimetazidine in the treatment of stable angina
Zhen-Lin DAI ; Bao-Xiang DUAN ; Jian-Chun LI ;
Chinese Journal of Clinical Pharmacology and Therapeutics 1999;0(04):-
Aim To evaluate the antianginal efficacy of trimetazidine in combination with other regular anti-ischemic drugs in the treatment of stable angina. Methods Twenty-two male cases with stable,effort-induced angina and positive exercise ECG test were treated with trimetazidine for 12 weeks.Exercise ECG test was examined again in the end of the study. Results There were obviously increased in exercise tolerance,total exercise workload after treatment(P
3.Study on traceability system of genuine medicinal materials.
Bao-Sheng LIAO ; Jing-Yuan SONG ; Cai-Xiang XIE ; Jian-Ping HAN ; Shi-Lin CHEN
China Journal of Chinese Materia Medica 2014;39(20):3881-3888
Genuine medicinal materials with special characteristics of Traditional Chinese Medicine (TCM), is recognized as high quality medicine. Both ancient records and modern research considered that the origin is an important reason for the formation of genuine medicinal materials. However, blindly transplanting of genuine medicinal materials has led to the quality decline and counterfeit medicines appeared in production or sale progress, which may increase the risk of accidents in TCM. Frequent accidents emerged in Chinese herbal affects its export. What's more, it is a great threat to the medication safety in TCM clinical. There is an urgent need to implement traceability systems of TCM, which could provide convenient information record and traceability of TCM circulation. This paper reviews a variety of technical methods for genuine medicinal materials traceability, and proposed the establishment of genuine medicinal materials traceability system based on two-dimensional code and network database.
Databases, Factual
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Drugs, Chinese Herbal
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chemistry
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economics
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standards
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Medicine, Chinese Traditional
4.PID1 based connection of insulin resistance to hepatocellular carcinogenesis
Ming XIANG ; Qian-Qian XU ; Sen-Lin LI ; Bao-Tian WANG ; Ya-Li TUO
Chinese Journal of Pharmacology and Toxicology 2018;32(4):316-316
OBJECTIVE To investigate the effect of phosphotyrosine interaction domain containing 1 (PID1, NYGGF4) onpromotion of IR and HCC, and explore its underlying mechanisms. METHODS Lentivirus were used to mediate the knockdown of PID1 in HFD induced IR mouse model as well as ob/ob mice. Intraperitoneal glucose and insulin tolerance were performed 4 weeks after lentivirus injection. Hydrodynamics-based transfection was applied to induce the liver specific overexpression of PID1. Flow cytometry was exerted to detect the proportion and function of immune cells.qRT-PCR and Western blot were used to detect the expression of downstream pathways of PID1. Liquid chromatography-mass spectrometry (LC-MS) and co-immunoprecipitation (Co-IP) were conducted to identify proteins interacting with PID1.Chromatin immunoprecipitation(ChIP)was operated to measure the modification of H3K4me3 of PID1 promoter.RESULTS PID1 restriction improved insulin resistance,hyperglycemia and fatty liver. Conversely, hepatic knockdown of PID1 attenuated liver xenografted tumor growth. Moreover,PID1 liver-specific protooncogenes via hydrodynamics-based transfection established a primary hepatocellular carcinoma mouse model,induced an immunosuppressive environment,with the reduction of CD3+,CD4+,CD8+T cells,retarded maturation of dendritic cells(DCs),pronounced differentiation of regulatory T cells(Tregs),and recruitment of MDSC.In addition,PID1 overexpression activated prolifer-ation related genes, promoted anti-inflammatory genes, suppressed pro-inflammatory genes, induced glycolysis and lipid metabolism genes to facilitate tumorigenesis in liver. Importantly, PID1 exerted its tumor-promoting function through binding to epidermal growth factor receptor(EGFR)and activation of downstream KRAS/ERK pathway.As such,PID1 exist trimethylation of histone H3 at lysine 4(H3K4me3) modification and IR up-regulated the expression of PID1 by activation the H3K4me3 modification. CONCLUSION PID1 is a new gene that exerts both liver cancer-promoting and insulin resistance inducing function.IR accelerates liver cancer development and progression partially dependent on the activation of PID1.
5.Pharmacokinetics of loganin, ferulic acid and stilbene glucoside in Bushen Tongluo formula in vivo.
Xiang-dan LIU ; Pan HUANG ; Yue-hua LU ; Ming MA ; Ri-bao ZHOU ; Lin-xiang YUAN ; Xin-jun PENG
China Journal of Chinese Materia Medica 2015;40(12):2428-2434
To study the pharmacokinetics characteristic of loganin, ferulic acid and stilbene glucoside in rat plasma after oral administration of Bushen Tongluo formula. The plasma samples were treated by using liquid-liquid extraction technique, the concentrations were determined by HPLC-UV. Johnson spherigel C18 column (4.6 mm x 250 mm, 5 μm) was adopted and eluted with the of mobile phase of methanol-water containing 0.01% glacial acetic acid in a gradient mode, with the flow rate at 1.0 mL x min(-1), column temperature at 30 degrees C and injection volume of 10 μL. According to the findings, loganin was determined at 235 nm, ferulic acid and stilbene glucoside were determined at 320 nm, with the sample size of 10 μL. The pharmacokinetic parameters of loganin, ferulic acid and stilbene glucoside were calculated by DAS 2. 0 software as follows: C(max) was (0.369 ± 0.042), (0.387 ± 0.071), (0.233 ± 0.044) mg x L(-1); t(max) was (0.226 ± 0.022), (0.282 ± 0.031), (0.233 ± 0.044) h; t(½β) was (6.89 ± 0.20), (10.73 ± 0.11), (6.93 ± 0.09) h; AUC(0-∞) was (1.91 ± 0.36), (3.22 ± 0.52), (1.52 ± 0.33) mg x h x L(-1); AUCO(0-t) was (1.62 ± 0.33), (2.58 ± 0.43), (1.30 ± 0.30) mg x h x L(-1); CL was (20.2 ± 4.0), (1.39 ± 0.23), (31.7 ± 6.9) L x h(-1) x kg(-1), respectively. The results showed that after the oral administration with Bushen Tongluo formula, loganin, ferulic acid and stilbene glucoside showed concentration-time curves in conformity with the two compartment model, with a rapid absorption, loganin and stilbene glucoside was excreted at a moderate speed, and ferulic acid was excreted slowly (but with the highest bioavailability). Bushen Tongluo formula can main maintain plasma concentration with three administrations everyday and so is suitable to be made into common oral preparation.
Administration, Oral
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Animals
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Biological Availability
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Coumaric Acids
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administration & dosage
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blood
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pharmacokinetics
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Drugs, Chinese Herbal
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administration & dosage
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analysis
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pharmacokinetics
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Glucosides
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administration & dosage
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blood
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pharmacokinetics
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Iridoids
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administration & dosage
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blood
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pharmacokinetics
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Male
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Rats
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Rats, Sprague-Dawley
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Stilbenes
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administration & dosage
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blood
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pharmacokinetics
6.Synthesis and antitumor activity of S-hexyl(heptyl) substituted ethanethioate derivatives.
Jia-Chen WEN ; Tao JIANG ; Yu BAO ; Xian-Jun LIN ; Wan-Qiao WANG ; Dan LIU ; Lin-Xiang ZHAO
Acta Pharmaceutica Sinica 2014;49(3):352-358
To simplify the macrocyclic fragment and to modify the zinc binding group of the natural product apicidin, two series of S-hexyl (heptyl) ethanethioate derivatives were designed and synthesized. Twenty-six compounds were synthesized and confirmed with 1H NMR, IR, MS and HR-MS spectrum, which were not reported. Take vorinostat as control, their antiporliferative activities against cancer cell lines, MCF-7 and HL-60, were tested with MTT assay or trypan blue staining method. Generally in both series it was found that, the chiral carbon atom at 7 position is not necessary, compounds II-1, II-3, II-6 and II-13 showed good activity on HL-60 cells in vitro, with the IC50 values less than 10 micromol x L(-1). II-7 and II-8 showed stronger activity against MCF-7 than Vorinostat, with the IC50 of 3.19 and 6.29 micromol x L(-1), respectively.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Cell Proliferation
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drug effects
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Drug Screening Assays, Antitumor
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HL-60 Cells
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Histone Deacetylase Inhibitors
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chemical synthesis
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chemistry
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pharmacology
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Humans
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Inhibitory Concentration 50
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MCF-7 Cells
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Peptides, Cyclic
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chemical synthesis
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chemistry
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pharmacology
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Structure-Activity Relationship
7.Effects of Hedyotis diffusa Willd injection on the proliferation of RPMI 8226 cells.
Xiang ZHANG ; Bao-dong YE ; Sheng-yun LIN
Chinese Journal of Integrated Traditional and Western Medicine 2012;32(12):1658-1662
OBJECTIVETo explore the inhibition of Hedyotis diffusa Willd Injection (HDI) on the proliferation of RPMI 8226 cells and its mechanisms.
METHODSThe inhibition of HDI on the proliferation of RPMI 8226 cells was detected by MTT and the drug concentrations for further researches were screened out. The apoptosis rate was detected using Annexin V-PI of flow cytometry. The cell cycle distribution was detected by PI. The expressions of adhesion molecule FITC-CD44 and PE-CD49d were detected. The IL-6 and VEGF concentrations of cell supernatants were tested by ELISA. The mRNA expressions of Bax, Bcl-2, Caspase-3, Survivin, IL-6, and VEGF were detected by RT-PCR.
RESULTSHDI could inhibit the proliferation of RPMI 8226 cells. Meanwhile, it induced their early apoptosis, arresting them at G1 phase in a concentration-dependent manner. The VEGF concentrations were down-regulated after acted by 0, 20, 40, and 60 microL/mL HDI in a dose-dependent manner (P< 0.01). The IL-6 content increased (P<0.01). The expressions of CD44 and CD49d were up-regulated in a concentration-dependent manner. After acted by 40 microL/mL HDI, the Survivin mRNA level was significantly downregulated (P<0.01), the mRNA levels of Bcl-2, IL-6, and VEGF were significantly up-regulated (P<0.01), but the up-regulation of Bax and Caspase-3 mRNA levels were not so obvious (P>0.05).
CONCLUSIONSHDI could inhibit the proliferation of RPMI 8226 cells. Its mechanisms might be correlated with early apoptosis induction, G1 phase arresting, VEGF secretion lowering, and Survivin mRNA transcription level down-regulating.
Apoptosis ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Hedyotis ; Humans ; Inhibitor of Apoptosis Proteins ; metabolism ; Interleukin-6 ; metabolism ; Vascular Endothelial Growth Factor A ; metabolism
8.Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles.
Zhi-zhong ZUO ; Hang ZHONG ; Ting CAI ; Yu BAO ; Zhi-qiang LIU ; Dan LIU ; Lin-xiang ZHAO
Acta Pharmaceutica Sinica 2015;50(7):868-874
Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
Antineoplastic Agents
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chemical synthesis
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chemistry
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Artemisinins
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chemical synthesis
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chemistry
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Breast Neoplasms
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pathology
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Cell Proliferation
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Doxorubicin
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Drug Design
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HL-60 Cells
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drug effects
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Humans
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MCF-7 Cells
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drug effects
9.Research of cranio-occlusional change of skeletal class III malocclusion in permanent dentition treated by the multiloop edgewise arch wire technique.
Chang-wei JIN ; Jiu-xiang LIN ; Bao-hua XU
West China Journal of Stomatology 2004;22(3):216-219
OBJECTIVETo analyze the mechanics in correction of skeletal class III malocclusion with Multiloop Edgewise Arch Wire (MEAW).
METHODS15 patients with skeletal class III malocclusion were treated with MEAW technique. Cephalometric analysis was performed with pre-treatment and post-treatment cephalograms. Paired t-test was conducted to assess the treatment effects.
RESULTSL6-XI decreased by 2.87 mm, L6/MP increased by 8.60 degrees, L1-XI decreased by 2.60 mm, OP/MP increased by 2.33 degrees. Skeleton changed a little. There was no significant change in the soft tissue.
CONCLUSION(1) Dento-alveolar compensation is the main change after the treatment by MEAW technique; (2) The improvement in molar relationship and overjet is achieved with upright and distal movement of the lower posterior teeth; (3) The lower anterior teeth moved lingually and protracted. Occlusal plane is flattened.
Adolescent ; Adult ; Cephalometry ; Dentition, Permanent ; Female ; Humans ; Male ; Malocclusion, Angle Class III ; therapy ; Orthodontic Wires ; Orthodontics, Corrective ; methods