Objective： To assess the anti-invasive effect of DDB and its possible active mechanism in human hepatocellular carcinoma MHCC97-H with high metastasis potential. Methods： MTT assay was used to evaluate the cytotoxic...Objective： To assess the anti-invasive effect of DDB and its possible active mechanism in human hepatocellular carcinoma MHCC97-H with high metastasis potential. Methods： MTT assay was used to evaluate the cytotoxicity of DDB to MHCC97-H cells and the anti-adhesion of DDB on MHCC97-H cells to laminin （LN） and fibronectin （FN）. The anti-invasive effect of DDB was detected by the transwell chamber experiment. VEGF, nm23-H1 and uPAR mRNA transcriptions were determined by RT-PCR assay. The secretion and expression of a-fetal protein （AFP） were analyzed by ELISA and flow cytometry, respectively. Results： DDB at non-cytotoxic concentrations （10, 50 and 100 μmol/L） obviously inhibited the adhesion of MHCC97-H on LN and FN. In the transwell chamber experiment, the inhibition rates of the invasion of DDB 50 and 100 μmol/L on MHCC97-H cells were 25.8% and 32.3%, respectively. By RT-PCR assay, DDB 50 and 100 μmol/L decreased VEGF, nm23-H1 and uPAR mRNA expressions in MHCC97-H cells. The ELISA assay showed that 50, 100 and 200 μmol/L DDB decreased the AFP secretion of MHCC97-H cells, the inhibitory rates were 16.5%, 17.5% and 48.5%, respectively. DDB also decreased the expression of AFP in MHCC97-H cells by flow cytometry assay. Conclusion： DDB, an anti-hepatitis drug, at non-cytotoxic concentrations showed significant anti-invasion effect in human hepatocellular carcinoma MHCC97-H cells, and the inhibition of VEGF, nm23-H1 and uPAR expression should contribute to the anti-invasion property of DDB.展开更多
Objective： To study the effect of oral administration of dimethyl dimethoxy biphenyl dicarboxylate （DDB） on adjusting angiogeneic/inflammatory mediators and ameliorating the pathology of bones in rats with collagen...Objective： To study the effect of oral administration of dimethyl dimethoxy biphenyl dicarboxylate （DDB） on adjusting angiogeneic/inflammatory mediators and ameliorating the pathology of bones in rats with collagen-induced arthritis （CIA）. Methods： Wistar rat model of CIA was set up using bovine collagen type H. Fifty rats were divided into five groups randomly： normal, CIA model, DDB treatment, methotrexate （MTX） treatment, and combined DDB＋MTX treatment. Ankle joints of rats were imaged with digital X-ray machine to show the destruction of joints. Fore and hind paw and knee joints were removed above the ankle joint then processed for haematoxylin and eosin staining. Plasma levels of vascular endothelial growth factor （VEGF）, platelet derived growth factor, interleukin-8 （IL-8）, IL-4, tumor necrosis factor α （TNF-α）, and cyclooxygenase-2 （COX-2） were quantified by enzyme-linked immunosorbent assay. Nitric oxide levels were detected by Griess reagent. Results： Compared with the CIA model group, a remarkable reduction in various angiogenic （VEGF and IL-8） and inflammatory mediators （TNF-α, IL-4 and COX-2） after treatment with DDB either alone or combined with MTX （P〈0.05 or P〈0.01）. Histopathological and X-ray findings were confirmatory to the observed DDB anti-arthritic effect. The DDB-treated group showed amelioration in signs of arthritis which appeared essentially similar to normal. Conclusion： Our data shed light on the therapeutic efficacy of DDB in experimental rheumatoid arthritis （RA） compared with a choice drug （MTX） and it may be offered as a second-line drug in the treatment of RA.展开更多
将120只小鼠随机分为空白组、四氯化碳(CCl_4)组、联苯双酯(DDB)组及低、中、高3个剂量(1.0、2.0、4.0 g/kg)的原药诃子、白狼毒制诃子和茜草制诃子组,共12个组,每组10只。给药7 d后,腹腔注射10 m L/kgCCl_4油溶液,建立小鼠肝损伤模型,...将120只小鼠随机分为空白组、四氯化碳(CCl_4)组、联苯双酯(DDB)组及低、中、高3个剂量(1.0、2.0、4.0 g/kg)的原药诃子、白狼毒制诃子和茜草制诃子组,共12个组,每组10只。给药7 d后,腹腔注射10 m L/kgCCl_4油溶液,建立小鼠肝损伤模型,检测各组血清中谷丙转氨酶(ALT)、谷草转氨酶(AST)活力,肝脏超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH–Px)活力,观察肝脏组织学结构变化。研究结果显示,诃子不同炮制品可减少CCl_4所引起的小鼠肝损伤,显著降低血清ALT、AST活力,提高肝脏SOD、GSH–Px活力,并对肝细胞有一定保护作用;药效表现由强到弱依次为茜草制诃子、白狼毒制诃子、生药诃子,且高剂量的效果优于低剂量。以茜草制诃子高剂量组4.0 g/kg效果最为理想,其作用机制可能与抗氧化性有关。展开更多
目的探讨联苯双酯(DDB)对中波紫外线(UVB)的防护作用及其相关机制研究,为临床应用提供理论依据。方法 DDB和维生素C对照检测五味子甲素衍生物DDB对超氧阴离子(O_2^-)的清除率。MTT法测定DDB、UVB对人永生化角质形成细胞(Ha Ca T)、人真...目的探讨联苯双酯(DDB)对中波紫外线(UVB)的防护作用及其相关机制研究,为临床应用提供理论依据。方法 DDB和维生素C对照检测五味子甲素衍生物DDB对超氧阴离子(O_2^-)的清除率。MTT法测定DDB、UVB对人永生化角质形成细胞(Ha Ca T)、人真皮成纤维细胞(FB)生长的影响及DDB对UVB的防护作用。通过Giemsa染色,从形态学上观察DDB对UVB损伤的防护作用。激光共聚焦观察活性氧簇(ROS)及检测其荧光强度。结果实验结果表明,相同浓度DDB具有强的清除O_2^-的能力;DDB对Ha Ca T、Fb细胞无毒性且可防护UVB损伤。Giemsa染色后,形态学上发现DDB可以明显抑制细胞的凋亡。DDB可抑制Ha Ca T细胞外ROS的生成。结论五味子甲素衍生物DDB对UVB有明显的防护作用,DDB作用机制是通过其抗氧化活性抑制UVB辐射引起的氧化应激及细胞凋亡等,起到紫外线防护作用,有望开发成为有效的抗氧化剂和紫外防护产品。展开更多
目的:探讨联苯双酯所致药品不良反应(adverse drug reaction,ADR)的一般规律及特点,为临床合理用药提供参考。方法:检索中国知网数据库、维普中文科技期刊数据库和万方数据库从建库至2019年6月国内医药期刊公开发表的联苯双酯致ADR的个...目的:探讨联苯双酯所致药品不良反应(adverse drug reaction,ADR)的一般规律及特点,为临床合理用药提供参考。方法:检索中国知网数据库、维普中文科技期刊数据库和万方数据库从建库至2019年6月国内医药期刊公开发表的联苯双酯致ADR的个案报道文献,对相关数据进行统计分析。结果:共收集到联苯双酯致ADR的个案报道文献20篇,获取ADR有效病例47例,48例次。31例报告了性别、年龄的患者中,男性患者所占比例高于女性患者[83.87%(26例)vs.16.13%(5例)];>20~50岁患者居多(21例,占67.74%);原患疾病以各型肝炎为主;ADR发生时间以给药后>7~14 d为主;ADR累及器官和(或)系统以肝胆系统为主,临床表现主要为氨基转移酶升高和黄疸。经停药、对症治疗,患者预后良好,无死亡病例报告。结论:联苯双酯的临床应用广泛且价格便宜,但使用时应严格把握适应证,加强用药监测,保证安全、有效、经济用药。展开更多
文摘Objective： To assess the anti-invasive effect of DDB and its possible active mechanism in human hepatocellular carcinoma MHCC97-H with high metastasis potential. Methods： MTT assay was used to evaluate the cytotoxicity of DDB to MHCC97-H cells and the anti-adhesion of DDB on MHCC97-H cells to laminin （LN） and fibronectin （FN）. The anti-invasive effect of DDB was detected by the transwell chamber experiment. VEGF, nm23-H1 and uPAR mRNA transcriptions were determined by RT-PCR assay. The secretion and expression of a-fetal protein （AFP） were analyzed by ELISA and flow cytometry, respectively. Results： DDB at non-cytotoxic concentrations （10, 50 and 100 μmol/L） obviously inhibited the adhesion of MHCC97-H on LN and FN. In the transwell chamber experiment, the inhibition rates of the invasion of DDB 50 and 100 μmol/L on MHCC97-H cells were 25.8% and 32.3%, respectively. By RT-PCR assay, DDB 50 and 100 μmol/L decreased VEGF, nm23-H1 and uPAR mRNA expressions in MHCC97-H cells. The ELISA assay showed that 50, 100 and 200 μmol/L DDB decreased the AFP secretion of MHCC97-H cells, the inhibitory rates were 16.5%, 17.5% and 48.5%, respectively. DDB also decreased the expression of AFP in MHCC97-H cells by flow cytometry assay. Conclusion： DDB, an anti-hepatitis drug, at non-cytotoxic concentrations showed significant anti-invasion effect in human hepatocellular carcinoma MHCC97-H cells, and the inhibition of VEGF, nm23-H1 and uPAR expression should contribute to the anti-invasion property of DDB.
文摘Objective： To study the effect of oral administration of dimethyl dimethoxy biphenyl dicarboxylate （DDB） on adjusting angiogeneic/inflammatory mediators and ameliorating the pathology of bones in rats with collagen-induced arthritis （CIA）. Methods： Wistar rat model of CIA was set up using bovine collagen type H. Fifty rats were divided into five groups randomly： normal, CIA model, DDB treatment, methotrexate （MTX） treatment, and combined DDB＋MTX treatment. Ankle joints of rats were imaged with digital X-ray machine to show the destruction of joints. Fore and hind paw and knee joints were removed above the ankle joint then processed for haematoxylin and eosin staining. Plasma levels of vascular endothelial growth factor （VEGF）, platelet derived growth factor, interleukin-8 （IL-8）, IL-4, tumor necrosis factor α （TNF-α）, and cyclooxygenase-2 （COX-2） were quantified by enzyme-linked immunosorbent assay. Nitric oxide levels were detected by Griess reagent. Results： Compared with the CIA model group, a remarkable reduction in various angiogenic （VEGF and IL-8） and inflammatory mediators （TNF-α, IL-4 and COX-2） after treatment with DDB either alone or combined with MTX （P〈0.05 or P〈0.01）. Histopathological and X-ray findings were confirmatory to the observed DDB anti-arthritic effect. The DDB-treated group showed amelioration in signs of arthritis which appeared essentially similar to normal. Conclusion： Our data shed light on the therapeutic efficacy of DDB in experimental rheumatoid arthritis （RA） compared with a choice drug （MTX） and it may be offered as a second-line drug in the treatment of RA.
文摘目的探讨联苯双酯(DDB)对中波紫外线(UVB)的防护作用及其相关机制研究,为临床应用提供理论依据。方法 DDB和维生素C对照检测五味子甲素衍生物DDB对超氧阴离子(O_2^-)的清除率。MTT法测定DDB、UVB对人永生化角质形成细胞(Ha Ca T)、人真皮成纤维细胞(FB)生长的影响及DDB对UVB的防护作用。通过Giemsa染色,从形态学上观察DDB对UVB损伤的防护作用。激光共聚焦观察活性氧簇(ROS)及检测其荧光强度。结果实验结果表明,相同浓度DDB具有强的清除O_2^-的能力;DDB对Ha Ca T、Fb细胞无毒性且可防护UVB损伤。Giemsa染色后,形态学上发现DDB可以明显抑制细胞的凋亡。DDB可抑制Ha Ca T细胞外ROS的生成。结论五味子甲素衍生物DDB对UVB有明显的防护作用,DDB作用机制是通过其抗氧化活性抑制UVB辐射引起的氧化应激及细胞凋亡等,起到紫外线防护作用,有望开发成为有效的抗氧化剂和紫外防护产品。
文摘目的:探讨联苯双酯所致药品不良反应(adverse drug reaction,ADR)的一般规律及特点,为临床合理用药提供参考。方法:检索中国知网数据库、维普中文科技期刊数据库和万方数据库从建库至2019年6月国内医药期刊公开发表的联苯双酯致ADR的个案报道文献,对相关数据进行统计分析。结果:共收集到联苯双酯致ADR的个案报道文献20篇,获取ADR有效病例47例,48例次。31例报告了性别、年龄的患者中,男性患者所占比例高于女性患者[83.87%(26例)vs.16.13%(5例)];>20~50岁患者居多(21例,占67.74%);原患疾病以各型肝炎为主;ADR发生时间以给药后>7~14 d为主;ADR累及器官和(或)系统以肝胆系统为主,临床表现主要为氨基转移酶升高和黄疸。经停药、对症治疗,患者预后良好,无死亡病例报告。结论:联苯双酯的临床应用广泛且价格便宜,但使用时应严格把握适应证,加强用药监测,保证安全、有效、经济用药。
