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Journal of Forensic Medicine 2021;37(5):736-738
4.Design, synthesis and biological evaluation of novel 4-substituted-3-nitrobenzamide derivatives.
Qi-Feng ZHU ; Yong-Xiang GONG ; Jin-Qing ZHONG ; Li-Fei LIU ; Xu-Fei LI ; Xu-Yang ZHAO
Acta Pharmaceutica Sinica 2014;49(8):1143-1149
A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.
Antineoplastic Agents
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chemical synthesis
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pharmacology
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Benzamides
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chemical synthesis
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pharmacology
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Cell Line, Tumor
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Cell Proliferation
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Drug Design
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HL-60 Cells
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Humans
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Inhibitory Concentration 50
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Structure-Activity Relationship
5.Treatment of Chemotherapy Related Leukocytopenia by Oral Administration of Multiple Leucogenic Drugs Combined with G-CSF: an Experimental Study.
Xi-ping ZHANG ; Xiang ZHANG ; Hong-jian YANG ; De-hong ZOU ; Xiang-ming HE ; Xing-fei YU ; Yong-feng LI
Chinese Journal of Integrated Traditional and Western Medicine 2015;35(7):860-865
OBJECTIVETo evaluate efficacies of three commonly used oral drugs including Berbamine Hydrochloride Tablet (B), Qijiao Shengbai Capsule (Q), and Leucogen Tablet (L) (by single drug, two drugs or three drugs) combined with granulocyte colony-stimulating factor (G-CSF) for treat ment of chemotherapy related leukocytopenia in mice.
METHODSTotally 156 Kunming male mice were divided into the normal control group (A, n=24), the model group (B, n=24), the G-CSF group (C, n =24), the G-CSF+Q group (D, n=12), G-CSF+ B (E, n=12), the G-CSF+L group (F, n=12), the G-CSF + Q + B group (G, n=12), the G-CSF + Q + L group (H, n=12), the G-CSF + L + B group (I, n=12), and the G-CSF + L + Q + B (J, n=12). Mouse models of chemotherapy related leukocytopenia were established by intraperitoneal injection of cyclophosphamide (CTX). A G-CSF group was set up as a positive control. Mice were treated by a single oral drug, a single oral drug combined with G-CSF, and two or three drugs combined with G-CSF respectively, and the death rate calculated. Hemocytes [such as white blood cells (WBC) and its classification, red blood cells (RBC), platelet (PLT), hemoglobin (Hb)] were calculated by hematology analyzer. Mice were anatomized and important organs weighed. Organ indices were calculated.
RESULTSThere was no statistical difference in the mortality rate among all groups (P > 0.05). Compared with Group B, WBC was elevated in all other groups (P < 0.01). WBC and PLT were elevated most in Group J, Hb and RBC were also increased at the same time (P < 0.05, P < 0. 01). Compared with Group B, RBC increased in Group E, F, G, I, and J (P < 0.01); Hb obviously increased in Group C, E, F, H, I, and J (P<0.01). Compared with Group B and D, the promotion of erythroid hematopoiesis by G-CSF could be elevated in any group contained drug B and L (P < 0.05, P < 0.01). The spleen index of model mice could be significantly improved in Group C, D, and G (P < 0.01). The thymus index of model mice could be significantly improved in Group H (P < 0.05).
CONCLUSIONSThe best scheme to treat mice with chemotherapy related leukopenia or decreased three blood series was to administrate three commonly oral drugs combined with G-CSF. Authors speculated that G-CSF and Q might have a certain effect on CTX induced immune inhibition.
Administration, Oral ; Animals ; Blood Platelets ; Cyclophosphamide ; Drug-Related Side Effects and Adverse Reactions ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; Erythrocyte Count ; Granulocyte Colony-Stimulating Factor ; metabolism ; Hematopoiesis ; Hemoglobins ; Leukocyte Count ; Leukocytes ; Leukopenia ; chemically induced ; drug therapy ; Male ; Mice ; Pharmaceutical Preparations
6.The effect of Connexin43 downregulation on biological functions of HUVEC.
Cai-zhen ZHANG ; Xiao-feng MU ; Xian-xiang XU ; Fei QIU ; Jun-sheng LIN ; Yong DIAO
Acta Pharmaceutica Sinica 2015;50(3):298-304
Connexin43 has been shown to play a pivotal role in wound healing process. Wound repair is enhanced by acute downregulation of connexin43, by increasing proliferation and migration of keratinocyte and fibroblast. Angiogenesis is also a central feature of wound repair, but little is known about the effects of connexin43 modulation on functions of endothelial cells. We used connexin43 specific small interference RNA (siRNA) to reduce the expression of connexin43 in human umbilical vein endothelial cell (HUVEC), and investigated the effects of connexin43 downregulation on intercellular communication, viability, proliferation, migration and angiogenic activity of HUVEC. Treatment of siRNA markedly reduced the expression of connexin43 by -80% in HUVEC (P < 0.05), and decreased the intercellular communication by -65% (P < 0.05). The viability, proliferation, migration and angiogenic activity of HUVEC decreased significantly (P < 0.05), compared with that of the normal cells. The results suggest that temporally downregulation of connexin43 expression at early stage of wound to inhibit the abnormal angiogenesis characterized with leaky and inflamed blood vessels, maybe a prerequisite for coordinated normal healing process.
Cell Movement
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Cell Proliferation
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Cell Survival
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Connexin 43
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metabolism
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Down-Regulation
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Human Umbilical Vein Endothelial Cells
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cytology
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Humans
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Neovascularization, Physiologic
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Umbilical Veins
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cytology
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Wound Healing
7.Combined anti-tumor therapeutic effect of targeted gene, hyperthermia, radionuclide brachytherapy in breast carcinoma
Dao-zhen, CHEN ; Qiu-sha, TANG ; Jing-ying, XIANG ; Fei, XU ; Li, ZHANG ; Jun-feng, WANG
Chinese Journal of Nuclear Medicine 2011;31(2):82-86
Objective To investigate the antitumor therapeutic effect of combined therapy of magnetic induction heating by nano-magnetic particles, herpes simplex virus thymidine kinase gene(HSV-tk suicide gene) and internal radiation in mice bearing MCF-7 breast carcinoma. Methods The transfection reagents, plasmids heat shock protein-HSV-tk (pHSP-HSV-tk), ferroso-ferric oxide nano-magnetic fluid flow and 188Re-ganciclovir-bovine serum albumin-nanopaticles (GCV-BSA-NP) were prepared. The heating experiments in vivo were carried out using ferroso-ferric oxide nano-magnetic fluid flow. Sixty mice tumor models bearing MCF-7 breast carcinoma were established and randomly divided into six groups. Group A was the control group, B was gene transfection therapy group, C was hyperthermia group, D was gene transfection therapy combined with radionuclide brachytherapy group, E was gene therapy combined with hyperthermia group, and F was gene therapy, hyperthermia combined with radionuclide brachytherapy group. The tumor growth, tumor mass and histopathological changes were evaluated. The expression of HSV-tk in the groups of B, D, E and F was detected by RT-PCR. Poisson distribution and one-way analysis of variance (ANOVA) were used for statistical analysis by SPSS 10.0 software. Results In the animal heating experiments, the temperature of tumor increased up to 39.6 ℃, 43.2 ℃, and 48.1 ℃ quickly with different injected doses (2, 4 and 6 mg respectively) of nano-magnetic particles and maintained for 40 min. The temperature of tumor tissue reduced to 36.8 ℃, 37.5 ℃ and 37.8 ℃ in 10 min when alternating magnetic field (AMF) stopped. The tumor mass in Groups C ((452.50 ±30.29) mg), D ((240.98 ±35.32)mg), E((231.87 ±27.41) mg) and F ((141.55 ±23.78) mg) were much lower than that in Group A ((719.12±22.65) mg) (F=800.07, P<0. 01), with the most significant treatment effect in Group F.The tumor mass in Group B((684.05 ±24.02) mg) was higher than that in Group D (t =32. 805, P <0. 05). Semi-quantitative RT-PCR analysis showed that the expression of HSV-tk in Groups B and D (0.33 ±0. 13 and 0. 46 ±0.12) was significantly different from that in Groups E and F (0.66 ±0.13 and 0.74 ±0. 11)(F = 21. 573, P < 0.05). Conclusion Combined use of hyperthermia, gene therapy and radionuclide brachytherapy could effectively depress the growth of MCF-7 breast carcinoma, thus possessing treatment potential for this tumor.
9.Effect of splenectomy on mortality and brain water content of rats with brain injury
Mei LI ; Fei LI ; Lijun ZHANG ; Zhi CHEN ; Xiang ZHANG ; Youan SHAN ; Jiangkai LIN ; Gang ZHU ; Zhiyong YIN ; Hua FENG
Chinese Journal of Trauma 2010;26(1):9-12
Objective To observe the effect of splenectomy on mortality and brain water content of rats with brain injury so as to explore novel way for better clinical management of patients with severe traumatic brain injury. Methods Adult male SD rats were randomly divided into three groups, ie, sham operation on brain and spleen (Group A, n = 23), experimental brain trauma & sham operation on spleen (Group B, n =48) and experimental brain injury & splenectomy (Group C, n = 47). Modified Feeney' s method was used to create the animal model of experimental brain trauma, Longa' s scale was applied to evaluate the neurologic defect. Mortality within seven days following brain injury was calculat-ed. In the meantime, the brain water content was detected at days 1 (n = 8), 2 (n = 8), 3 (n = 8) and 7 (n = 7) after brain injury in each group, Results No statistical difference of Longs' s scale was found between Group B and Group C (P > 0.05). The mortalities within seven days after brain injury were 0%, 35.42 and 14.89% in Groups A, B and C respectively, with statistical difference between groups (P<0.05). The brain water content of Groups B and C at days 1, 2, 3 and 7 were (81.98±0.35)% & (81.78±0.41)%, (82.58±0.63)% & (81.81±0.48)% (P<0.05),(82.54±0.54)% & (81.52±0.84)% (P<0.05) and (81.50±0.41)% & (81.21±0.36)% (P>0.05) respectively. Conclusion Splenectomy can effectively reduce brain water content and significantly decrease mortality in rata with brain injury.
10.Reduction and internal fixation for atlantoaxial dislocation with posterior screw-rod fixation system
Bin NI ; Fengjin ZHOU ; Xiang GUO ; Jian YANG ; Songkai LI ; Zhuangchen ZHU ; Feng ZHANG ; Jinshui CHEN ; Fei WANG ; Jun LIU
Chinese Journal of Trauma 2010;26(8):691-694
Objective To evaluate the outcome of posterior screw-rod fixation system in reduction and internal fixation of atlantoaxial dislocation. Methods A retrospective study was done on 27 patients with atlantoaxial instability including 18 male and 9 female (at age range of 13-51 years, mean 31 years) from January 2007 to May 2009. There were 11 patients with chronic odontoid fractures, five with isolated bone odontoid, seven with transverse ligament rupture of atlas and four with rheumatoid arthritis. Skeletal reduction was performed in all the patients. The anterior atlantodens interval (ADI)ranged from 8 mm to 15 mm, average 11 mm. All the patients underwent an intraoperative reduction by posterior C1 lateral mass and C2 pedicle screws with rod fixation. According to American Spine Injury Association (ASIA) impairment scale, there were eight patients at grade B, 15 at grade C and four at grade D. Results All patients were followed up for 6-24 months (average 13 months), which showed that the neck symptoms were improved, with bony union. The ADI was reduced to 2-4 mm (average 2.8 mm)postoperatively. Postoperative ASIA scale was grade C in four patients, grade D in 12 and grade E in 11.There were no neurologic or vascular complications occurred, or no failure of the internal fixtors, pseudarthrosis or instability. Conclusion Posterior screw-rod fixation system has advantages of simple procedures, few complications and good results and can be used for intraoperative reduction of atlantoaxial dislocation.