Up to date,in literature,it is still debated the role of anti-tumor necrosis factors(TNF)-α treatments in hepatitis C virus(HCV) patients.TNF-α performs a lot of functions,it is an important pro-inflammatory cytokin...Up to date,in literature,it is still debated the role of anti-tumor necrosis factors(TNF)-α treatments in hepatitis C virus(HCV) patients.TNF-α performs a lot of functions,it is an important pro-inflammatory cytokine and it is involved in the host's immunity.Since TNF-α is implicated in the apoptotic signaling pathway of hepatocytes infected by HCV,anti TNF-α therapy may increase the risk of viral replication or their reactivation.However the treatment of anti TNF-α could have a healthful role because TNF-α appears to be engaged in the pathogenesis of liver fibrosis,inducing apoptotic pathways.We describe the case of a patient with plaquetype psoriasis and concomitant chronic HCV,who was treated successfully with anti-TNF agents simultaneously to cyclosporine without sign of reactivation of HCV and increase of liver enzymes.Our personal experience shows that anti-TNF-α agents are not only effective but also safe.Furthermore the combination therapy of cyclosporine and anti-TNF-α appears to be well-tolerated and able to reduce the amount of liver enzymes as well as HCV-viral-load.However systematic,large-scale studies with long follow-ups will be needed to confirm our results,in association with close liver function monitoring.展开更多
Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,...Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil（5-FU） in most cancer cells tested.Furthermore,6f could selectively inhibit tumor cells,but not non-tumor cell proliferation.This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.展开更多
Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cell...Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cells tested. Furthermore, 5e induced tumor cell apoptosis, which was accompanied by lower Bcl-2 expression, but with higher Bax and caspase 3 expression activities in cancer cells.展开更多
Novel 2-aminoimidazolone derivatives were synthesized.Most compounds displayed strong anticancer activities against human carcinoma cells in vitro.Compounds 8a,8b and 8j exhibited optimal activity superior to 5-FU in ...Novel 2-aminoimidazolone derivatives were synthesized.Most compounds displayed strong anticancer activities against human carcinoma cells in vitro.Compounds 8a,8b and 8j exhibited optimal activity superior to 5-FU in most cancer cells tested.Especially,the lC_（50）s of 8b（12.6-21.5μmol/L） against five tumor cells were 1 -4 fold less than those of 5-FU（18.4-56.1μmol/L） in vitro.Furthermore,comp以ound 8b could induce SMMC-7721 cell apoptosis in a dose-dependent manner.Therefore,our novel findings may provide a new framework for the design of new 2-aminoimidazolone derivatives for the treatment of cancer.展开更多
作为重要的天然药物产物,姜黄素(Curcumin)分离自Curcuma longa L.,具有多个方面的活性,包括抗氧化、抗感染和抗炎作用。最近的研究提示姜黄素可能具有一定的抗肿瘤活性,但其活性和作用机制有待深入研究。为考察姜黄素对抗肿瘤药物杀伤...作为重要的天然药物产物,姜黄素(Curcumin)分离自Curcuma longa L.,具有多个方面的活性,包括抗氧化、抗感染和抗炎作用。最近的研究提示姜黄素可能具有一定的抗肿瘤活性,但其活性和作用机制有待深入研究。为考察姜黄素对抗肿瘤药物杀伤肺癌细胞的影响,用肺癌细胞系A549、H460、H1299以及H358使用姜黄素预处理后,分别使用抗肿瘤药物吉非替尼(Gefitinib)、舒尼替尼(Sunitinib)、吉西他滨(Gemcitabine)和紫杉醇(Paclitaxel)处理上述肺癌细胞,检测其抑制率;并计算IC50值。CCK-8实验结果显示,姜黄素能够上调抗肿瘤药物对肺癌细胞的杀伤作用,显著下调其IC50值。说明姜黄素具有增加肿瘤细胞对化疗药物敏感性的作用,具有潜在逆转化疗耐药的价值。展开更多
文摘Up to date,in literature,it is still debated the role of anti-tumor necrosis factors(TNF)-α treatments in hepatitis C virus(HCV) patients.TNF-α performs a lot of functions,it is an important pro-inflammatory cytokine and it is involved in the host's immunity.Since TNF-α is implicated in the apoptotic signaling pathway of hepatocytes infected by HCV,anti TNF-α therapy may increase the risk of viral replication or their reactivation.However the treatment of anti TNF-α could have a healthful role because TNF-α appears to be engaged in the pathogenesis of liver fibrosis,inducing apoptotic pathways.We describe the case of a patient with plaquetype psoriasis and concomitant chronic HCV,who was treated successfully with anti-TNF agents simultaneously to cyclosporine without sign of reactivation of HCV and increase of liver enzymes.Our personal experience shows that anti-TNF-α agents are not only effective but also safe.Furthermore the combination therapy of cyclosporine and anti-TNF-α appears to be well-tolerated and able to reduce the amount of liver enzymes as well as HCV-viral-load.However systematic,large-scale studies with long follow-ups will be needed to confirm our results,in association with close liver function monitoring.
文摘Novel furoxan-based nitric oxide-releasing derivatives 6a-p of hydroxylcinnamic acids were synthesized by coupling the carboxyl group of hydroxylcinnamic acids with furoxan through various alkylol amines.Compounds 6a,e-i and m-p displayed more potent anti-tumor activities superior to control 5-fluorouracil（5-FU） in most cancer cells tested.Furthermore,6f could selectively inhibit tumor cells,but not non-tumor cell proliferation.This inhibition was attributed to high levels of NO released in cancer cells and potentially synergistic effect of NO donor moieties and the bioactivity of hydroxylcinnamic acids.
基金support by the Natural Science Foundation of Jiangsu Province in China (NoBK2011389)Applied Research Projects of Nantong City(BK2012085)funded by the Priority Academic Programs Development of Jiangsu Higher Education Institutions(PAPD)
文摘Novel farnesylthiosalicylic acid （PTA） derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b, 5e, 5e and 5f displayed anti-tumor activities superior to FTA in most cancer cells tested. Furthermore, 5e induced tumor cell apoptosis, which was accompanied by lower Bcl-2 expression, but with higher Bax and caspase 3 expression activities in cancer cells.
基金support by the Nature and Science Foundation of Department of Education,Anhui province(No.KJ2013A168)Applied Research Projects of Nantong City(No.BK2012085)a project funded by the Priority Academic Programs Development of Jiangsu Higher Education Institutions(PAPD)
文摘Novel 2-aminoimidazolone derivatives were synthesized.Most compounds displayed strong anticancer activities against human carcinoma cells in vitro.Compounds 8a,8b and 8j exhibited optimal activity superior to 5-FU in most cancer cells tested.Especially,the lC_（50）s of 8b（12.6-21.5μmol/L） against five tumor cells were 1 -4 fold less than those of 5-FU（18.4-56.1μmol/L） in vitro.Furthermore,comp以ound 8b could induce SMMC-7721 cell apoptosis in a dose-dependent manner.Therefore,our novel findings may provide a new framework for the design of new 2-aminoimidazolone derivatives for the treatment of cancer.
文摘作为重要的天然药物产物,姜黄素(Curcumin)分离自Curcuma longa L.,具有多个方面的活性,包括抗氧化、抗感染和抗炎作用。最近的研究提示姜黄素可能具有一定的抗肿瘤活性,但其活性和作用机制有待深入研究。为考察姜黄素对抗肿瘤药物杀伤肺癌细胞的影响,用肺癌细胞系A549、H460、H1299以及H358使用姜黄素预处理后,分别使用抗肿瘤药物吉非替尼(Gefitinib)、舒尼替尼(Sunitinib)、吉西他滨(Gemcitabine)和紫杉醇(Paclitaxel)处理上述肺癌细胞,检测其抑制率;并计算IC50值。CCK-8实验结果显示,姜黄素能够上调抗肿瘤药物对肺癌细胞的杀伤作用,显著下调其IC50值。说明姜黄素具有增加肿瘤细胞对化疗药物敏感性的作用,具有潜在逆转化疗耐药的价值。
