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Selective COX-2 inhibitor,NS-398,suppresses cellular proliferation in human hepatocellular carcinoma cell lines via cell cycle arrest 被引量:27
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作者 Ji Yeon Baek Wonhee Hur +2 位作者 Jin Sang Wang Si Hyun Bae Seung Kew Yoon 《World Journal of Gastroenterology》 SCIE CAS CSCD 2007年第8期1175-1181,共7页
AIM: To investigate the growth inhibitory mechanism of NS-398, a selective cyclooxygenase-2 (COX-2) inhibitor, in two hepatocellular carcinoma (HCC) cell lines (HepG2 and Huh7). METHODS: HepG2 and Huh7 cells were trea... AIM: To investigate the growth inhibitory mechanism of NS-398, a selective cyclooxygenase-2 (COX-2) inhibitor, in two hepatocellular carcinoma (HCC) cell lines (HepG2 and Huh7). METHODS: HepG2 and Huh7 cells were treated with NS-398. Its effects on cell viability, cell proliferation, cell cycles, and gene expression were respectively evaluated by water-soluble tetrazolium salt (WST-1) assay, 4’-6-diamidino-2-phenylindole (DAPI) staining, flow cytometer analysis, and Western blotting, with dimethyl sulfoxide (DMSO) as positive control. RESULTS: NS-398 showed dose- and time-dependent growth-inhibitory effects on the two cell lines. Proliferating cell nuclear antigen (PCNA) expressions in HepG2 and Huh7 cells, particularly in Huh7 cells were inhibited in a time- and dose-independent manner. NS-398 caused cell cycle arrest in the G1 phase with cell accumulation in the sub-G1 phase in HepG2 and Huh7 cell lines. No evidence of apoptosis was observed in two cell lines. CONCLUSION: NS-398 reduces cell proliferation by inducing cell cycle arrest in HepG2 and Huh7 cell lines, and COX-2 inhibitors may have potent chemoprevention effects on human hepatocellular carcinoma. 展开更多
关键词 selective cyclooxygenase 2 inhibitor Cell growth Cell cycle Hepatocellular carcinoma cells
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Opioid-sparing effect of selective cyclooxygenase-2 inhibitors on surgical outcomes after open colorectal surgery within an enhanced recovery after surgery protocol 被引量:7
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作者 Varut Lohsiriwat 《World Journal of Gastrointestinal Oncology》 SCIE CAS 2016年第7期543-549,共7页
AIM: To evaluate the opioid-sparing effect of selective cyclooxygenase-2(COX-2) inhibitors on short-term surgical outcomes after open colorectal surgery.METHODS: Patients undergoing open colorectal resection within an... AIM: To evaluate the opioid-sparing effect of selective cyclooxygenase-2(COX-2) inhibitors on short-term surgical outcomes after open colorectal surgery.METHODS: Patients undergoing open colorectal resection within an enhanced recovery after surgery protocol from 2011 to 2015 were reviewed. Patients with combined general anesthesia and epidural anesthesia, and those with acute colonic obstruction or perforation were excluded. Patients receiving selective COX-2 inhibitor were compared with well-matched individuals without such a drug. Outcome measures included numeric pain score and morphine milligram equivalent(MME) consumption on postoperative day(POD) 1-3, gastrointestinal recovery(time to tolerate solid diet and time to defecate), complications and length of postoperative stay.RESULTS: There were 75 patients in each group. Pain score on POD 1-3 was not significantly different between two groups. However, MME consumption and MME consumption per kilogram body weight on POD 1-3 was significantly less in patients receiving a selective COX-2 inhibitor(P < 0.001). Median MME consumption per kilogram body weight on POD 1-3 was 0.09, 0.06 and nil, respectively in patients receiving a selective COX-2 inhibitor and 0.22, 0.25 and 0.07, respectively in the comparative group(P < 0.001), representing at least 59% opioidreduction. Patients prescribing a selective COX-2 inhibitor had a shorter median time to resumption of solid diet [1(IQR 1-2) d vs 2(IQR 2-3) d; P < 0.001] and time to first defecation [2(IQR 2-3) d vs 3(IQR 3-4) d; P < 0.001]. There was no significant difference in overall postoperative complications between two groups. However, median postoperative stay was significantly 1-d shorter in patients prescribing a selective COX-2 inhibitor [4(IQR 3-5) d vs 5(IQR 4-6) d; P < 0.001]. CONCLUSION: Perioperative administration of oral selective COX-2 inhibitors significantly decreased intravenous opioid consumption, shortened time to gastrointestinal recovery and reduced hospital stay after open colorectal surgery. 展开更多
关键词 selective CYCLOOXYGENASE-2 inhibitor Outcome Colon SURGERY Rectal SURGERY Enhanced recovery AFTER SURGERY OPIOID ILEUS NON-STEROIDAL anti-inflammatory drug Pain
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A Convenient Synthesis of the Substituted 2,3-Diarylindole the Potent Selective COX-2 Inhibitors
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作者 WenHuiHU ZonRuGUO 《Chinese Chemical Letters》 SCIE CAS CSCD 2002年第4期296-298,共3页
Phenyl sulfone-containing 2, 3-diarylindole derivatives were designed and identified to be selective COX-2 inhibitors. A convenient synthetic route was also developed for the synthesis of the novel inhibitors.
关键词 Nonsteroidal anti-inflammatory drugs (NSAIDs) selective COX-2 inhibitors substituted 2 3-diarylindole pharmacophore.
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Selective Cyclooxygenase-2 Inhibitors: Design and Synthesis
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作者 Xin Sheng LEI Zong Ru GUO +1 位作者 Ling Bo QU Qi Qing ZHU(Institute of Materia Medica. Chinese Academy of Medical SciencesAnd Peking Union Medical College. Beijing 100050) 《Chinese Chemical Letters》 SCIE CAS CSCD 1999年第6期469-472,共4页
The discovery of COX-2 provides a novel target developing more effective NSAIDs with fewer side effects. On the basis of results from the structure-activity relationships (SAR) of selective COX-2 inhibitors, we have d... The discovery of COX-2 provides a novel target developing more effective NSAIDs with fewer side effects. On the basis of results from the structure-activity relationships (SAR) of selective COX-2 inhibitors, we have designed and synthesized some promising compounds. 展开更多
关键词 CYCLOOXYGENASE cyclooxygenase-2 inhibitor selective
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Health Related Quality of Life among Osteoarthritis Patients: A Comparison of Traditional Non-Steroidal Anti-Inflammatory Drugs and Selective COX-2 Inhibitors in the United Arab Emirates Using the SF-36
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作者 Mohammed Hassanein Mohammed Shamssain Nageeb Hassan 《Pharmacology & Pharmacy》 2015年第4期232-240,共9页
Objectives: Osteoarthritis (OA) has a dramatic impact on patients’ health related quality of life (HRQoL). Chronic use of analgesics and anti-inflammatory medications for pain management may improve symptoms but on l... Objectives: Osteoarthritis (OA) has a dramatic impact on patients’ health related quality of life (HRQoL). Chronic use of analgesics and anti-inflammatory medications for pain management may improve symptoms but on long term may affect HRQoL negatively. The objective of the present study was to compare the impact of two different classes of analgesics, traditional non-steroidal anti-inflammatory drugs (NSAIDs) and selective cyclo-oxygenase-2 (COX-2) inhibitors on HRQoL among osteoarthritis patients using the SF-36 questionnaire. Methods: Clinic based cross-sectional study conducted at Al-Qassimi Hospital, Sharjah, United Arab Emirates (UAE), over a period of six months. Ethical Approval was obtained from the ethics committee at Al-Qassimi Clinical Research Center. Total of 200 osteoarthritis patients fulfilling the inclusion and exclusion criteria were involved in the study. Patients’ demographics were collected from their medical records. The Medical Outcome Study Short-Form 36 (SF-36) questionnaire was used to measure patients’ HRQoL. SF-36 data were scored using health outcomes scoring software 4.5. Results: Mean age of the subjects was 62.19 ± 9.81 years with females constituting 151 (75.5%) of the patients. In general, females scored lower in most of the HRQoL domains compared to males and there was significant difference between the two groups in the mental health (p = 0.005) & mental component (p = 0.042) domains. Compared to selective COX-2 inhibitors, patients on NSAIDs scored higher on all domains of SF-36 except physical functioning. There was significant difference in mental health domain for patients treated with NSAIDs (p = 0.02). Celecoxib was only better than NSAIDs in osteoarthritis patients with more than one musculoskeletal disorders in the domain of bodily pain (p = 0.009). Conclusion: NSAIDs-treated patients did not differ significantly from celecoxib-treated patients in all domains of the SF-36 except for the mental health domain. 展开更多
关键词 OSTEOARTHRITIS Health Related Quality of Life Short Form-36 TRADITIONAL NONSTEROIDAL ANTI-INFLAMMATORY Drugs selective COX-2 inhibitorS
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选择性COX-2抑制剂引起心血管风险的研究进展
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作者 黄勇 李頔 +3 位作者 王娜 冉娅娟 雷筱梅(综述) 钱妍(审校) 《西南医科大学学报》 2024年第1期87-92,共6页
非甾体抗炎药(non-steroid anti-inflammatory drugs,NSAIDs)是一种有效的、广泛使用的抗炎镇痛药物,其对环氧合酶(cyclo-oxygenase,COX)亚型(COX-1、COX-2)的抑制作用将引起不同的反应,选择性COX-2抑制剂将显著增加不良心血管事件的风... 非甾体抗炎药(non-steroid anti-inflammatory drugs,NSAIDs)是一种有效的、广泛使用的抗炎镇痛药物,其对环氧合酶(cyclo-oxygenase,COX)亚型(COX-1、COX-2)的抑制作用将引起不同的反应,选择性COX-2抑制剂将显著增加不良心血管事件的风险,随着此类药物使用的增加和临床循证证据的积累,其带来的心血管风险引起了越来越多学者的关注。笔者通过归纳分析最新发表文献对选择性COX-2抑制剂引起心血管风险的研究进行综述,以期辅助临床合理用药,减少不良反应,提高用药安全性。 展开更多
关键词 非甾体类抗炎药 环氧合酶 选择性环氧合酶-2抑制剂 心血管风险
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c-Fos enhances the survival of thymocytes during positive selection by upregulating Bcl-2 被引量:2
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作者 Xiaoming Wang Yafeng Zhang +2 位作者 Gang Xiao Xiang Gao Xiaolong Liu 《Cell Research》 SCIE CAS CSCD 2009年第3期340-347,共8页
T cells are derived from progenitor thymocytes, of which only a minority receive the appropriate TCR signal, undergo positive selection and mature. Owing to the very short lifespan of thymocytes, the prerequisite for ... T cells are derived from progenitor thymocytes, of which only a minority receive the appropriate TCR signal, undergo positive selection and mature. Owing to the very short lifespan of thymocytes, the prerequisite for posi- tive selection is survival. TCR signal-induced Bcl-2 expression is believed to play a dominant role in the survival of positively selecting thymocytes, but how Bcl-2 is directly regulated is unknown. Here we report that the immediate early gene (IEG) c-Fos can stimulate the expression of Bcl-2, depending on a specific AP-l-binding site in the Bcl-2 promoter. In c-Fos transgenic (Fos-Tg) mice, c-Fos binds to this site and promotes the expression of Bcl-2. As a result, Fos-Tg thymocytes exhibited enhanced survival, and more mature single-positive (SP) thymocytes were generated, even on a unique TCR background. The TCR repertoire remained normal in Fos-Tg mice. Our results identified c-Fos as the mediator of the stimulatory effect of TCR signaling on Bcl-2 expression. Therefore, c-Fos, as an IEG, because of its early response ability, can quickly rescue the survival of short-lived thymocytes during positive selection. Our results provide novel insight into the mechanism regulating the survival of positively selecting thymocytes. 展开更多
关键词 C-FOS bcl-2 SURVIVAL thymocyte development positive selection
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选择性Bcl-2抑制剂Venetoclax的研究进展 被引量:1
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作者 李晓娟 李莎 解红霞 《内蒙古医科大学学报》 2017年第3期283-287,共5页
慢性淋巴细胞白血病(chronic lymphocytic leukemia,CLL)是一种成熟B淋巴细胞克隆增殖性肿瘤,以淋巴细胞在外周血、骨髓、脾脏和淋巴结聚集为特征。目前的标准治疗方案是氟达拉滨+环磷酰胺+利妥昔单抗的FCR方案。作为首个靶向药物,B细... 慢性淋巴细胞白血病(chronic lymphocytic leukemia,CLL)是一种成熟B淋巴细胞克隆增殖性肿瘤,以淋巴细胞在外周血、骨髓、脾脏和淋巴结聚集为特征。目前的标准治疗方案是氟达拉滨+环磷酰胺+利妥昔单抗的FCR方案。作为首个靶向药物,B细胞受体信号通路抑制剂极大的改变了CLL的治疗。Venetoclax是由Abb Vie公司和Genentech/Roche公司合作研发的口服选择性抗凋亡蛋白Bcl-2抑制剂,现已被FDA批准用于17p染色体缺失的CLL病人。它是唯BH3蛋白(Bcl-2蛋白家族成员)的类似物,可以重建恶性肿瘤细胞的凋亡通路。目前,Venetoclax与其他药物联合治疗CLL的Ⅰ-Ⅲ期临床试验、单用或联合其他药物治疗非霍奇金淋巴瘤和急性白血病的Ⅰ/Ⅱ期临床试验也在进行当中。本文叙述了Venetoclax全方面的研究进展。 展开更多
关键词 慢性淋巴细胞白血病 选择性bcl-2抑制剂 B细胞受体信号通路抑制剂
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DYRK1A suppression restrains Mcl-1 expression and sensitizes NSCLC cells to Bd-2 inhibitors 被引量:3
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作者 Yangling Li Dongmei Zhou +5 位作者 Shuang Xu Mingjun Rao Zuoyan Zhang Linwen Wu Chong Zhang Nengming Lin 《Cancer Biology & Medicine》 SCIE CAS CSCD 2020年第2期387-400,共14页
Objective:Mcl-1 overexpression confers acquired resistance to Bcl-2 inhibitors in non-small cell lung cancer(NSCLC),but no direct Mcl-1 inhibitor is currently available for clinical use.Thus,novel therapeutic strategi... Objective:Mcl-1 overexpression confers acquired resistance to Bcl-2 inhibitors in non-small cell lung cancer(NSCLC),but no direct Mcl-1 inhibitor is currently available for clinical use.Thus,novel therapeutic strategies are urgently needed to target Mcl-1 and sensitize the anti-NSCLC activity of Bcl-2 inhibitors.Methods:Cell proliferation was measured using sulforhodamine B and colony formation assays,and apoptosis was detected with Annexin V-FITC staining.Gene expression was manipulated using siRNAs and plasmids.Real-time PCR and Western blot were used to measure mRNA and protein levels.Immunoprecipitation and immunofluorescence were used to analyze co-localization o f dual specificity tyrosine-phosphorylation-regulated kinase 1A(DYRK1A)and Mcl-1.Results:Suppression of DYRK1A resulted in reduced Mcl-1 expression in NSCLC cells,whereas overexpression of DYRK1A significantly increased Mcl-1 expression.Suppression of DYRK1A did not alter Mcl-1 mRNA levels,but did result in an accelerated degradation o f Mcl-1 protein in NSCLC cells.Furthermore,DYRK1A mediated proteasome-dependent degradation o f Mcl-1 in NSCLC cells,and DYRK1A co-localized with Mcl-1 in NSCLC cells and was co-expressed with Mcl-1 in tumor samples from lung cancer patients,suggesting that Mcl-1 may be a novel DYRK1A substrate.We showed that combined therapy with harmine and Bcl-2 antagonists significantly inhibited cell proliferation and induced apoptosis in NSCLC cell lines as well as primary NSCLC cells.Conclusions:Mcl-1 is a novel DYRK1A substrate,and the role of DYRK1A in promoting Mcl-1 stability makes it an attractive target for decreasing Bcl-2 inhibitor resistance. 展开更多
关键词 DYRK1A MCL-1 NSCLC COMBINATION bcl-2 inhibitor
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环氧酶-2抑制剂对关节炎大鼠小肠黏膜的影响
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作者 陈楠 丁瑞峰 +2 位作者 黎敏 吴昆 贺清 《中国现代医学杂志》 CAS 北大核心 2023年第8期37-42,共6页
目的探讨环氧酶-2抑制剂对关节炎大鼠小肠黏膜的影响。方法将32只雄性SD大鼠随机分为空白对照组、造模对照组、空白给药组和造模给药组,造模对照组、造模给药组给予弗氏完全佐剂右后足跖注射,空白对照组、空白给药组注射等量生理盐水。... 目的探讨环氧酶-2抑制剂对关节炎大鼠小肠黏膜的影响。方法将32只雄性SD大鼠随机分为空白对照组、造模对照组、空白给药组和造模给药组,造模对照组、造模给药组给予弗氏完全佐剂右后足跖注射,空白对照组、空白给药组注射等量生理盐水。1周后造模给药组、空白给药组给予选择性环氧酶-2抑制剂塞来昔布(溶于1%甲基纤维素)灌胃28 d,空白对照组、造模对照组给予等量溶剂。处死大鼠后观察小肠黏膜大体损伤、病理评分,酶联免疫吸附试验检测末段小肠前列腺素浓度。结果造模对照组与造模给药组模型复制第7天的足周径比较,差异无统计学意义(P>0.05),但两组分别与空白对照组和空白给药组比较,差异有统计学意义(P<0.05),空白对照组与空白给药组比较,差异无统计学意义(P>0.05)。空白对照组与造模对照组小肠黏膜损伤面积比较,差异有统计学意义(P<0.05),空白给药组与空白对照组比较,差异有统计学意义(P<0.05)。造模对照组、空白给药组和造模给药组组间小肠黏膜病理评分比较,差异无统计学意义(P>0.05),且空白对照组与其他3组比较,差异有统计学意义(P<0.05)。造模对照组、造模给药组小肠前列腺素浓度较空白对照组降低(P<0.05),造模对照组较空白给药组降低(P<0.05)。结论塞来昔布可致大鼠小肠黏膜损伤;佐剂性关节炎大鼠存在小肠黏膜损伤,塞来昔布可增加其小肠黏膜损伤面积,但不增加损伤程度;塞来昔布对关节炎大鼠与正常大鼠的小肠黏膜损伤相似;小肠黏膜前列腺素浓度下降可能与全身炎症所致小肠损伤有关,但可能不是COX-2抑制剂小肠损伤的主要或起始事件。 展开更多
关键词 佐剂性关节炎 小肠黏膜 选择性环氧酶-2抑制剂 损伤 前列腺素
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Anti-apoptotic protein BCL-XL as a therapeutic vulnerability in gastric cancer
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作者 Yumin Wei Liping Zhang +9 位作者 Chao Wang Zefeng Li Mingjie Luo Guomin Xie Xingjiu Yang Mengyuan Li Shuyue Ren Dongbing Zhao Ran Gao Jia-Nan Gong 《Animal Models and Experimental Medicine》 CAS CSCD 2023年第3期245-254,共10页
Background: New therapeutic targets are needed to improve the outcomes for gastric cancer(GC) patients with advanced disease. Evasion of programmed cell death(apoptosis) is a hallmark of cancer cells and direct induct... Background: New therapeutic targets are needed to improve the outcomes for gastric cancer(GC) patients with advanced disease. Evasion of programmed cell death(apoptosis) is a hallmark of cancer cells and direct induction of apoptosis by targeting the pro-survival BCL2 family proteins represents a promising therapeutic strategy for cancer treatment. Therefore, understanding the molecular mechanisms underpinning cancer cell survival could provide a molecular basis for potential therapeutic interventions. Method: Here we explored the role of BCL2L1 and the encoded anti-apoptotic BCL-XL in GC. Using Droplet Digital PCR(ddPCR) technology to investigate the DNA amplification of BCL2L1 in GC samples and GC cell lines, the sensitivity of GC cell lines to selective BCL-XL inhibitors A1155463 and A1331852, pan-inhibitor ABT-263, and VHL-based PROTAC-BCL-XL was analyzed using(CellTiter-Glo) CTG assay in vitro. Western Blot(WB) was used to detect the protein expression of BCL2 family members in GC cell lines and the manner in which PROTAC-BCL-XL kills GC cells. Coimmunoprecipitation(Co-IP) was used to investigate the mechanism of A1331852 and ABT-263 kills GC cell lines. DDPCR, WB, and real-time PCR(RTPCR) were used to investigate the correlation between DNA, RNA, protein levels, and drug activity. Results: The functional assay showed that a subset of GC cell lines relies on BCL-XL for survival. In gastric cancer cell lines, BCL-XL inhibitors A1155463 and A1331852 are more sensitive than the pan BCL2 family inhibitor ABT-263, indicating that ABT-263 is not an optimal inhibitor of BCL-XL. VHL-based PROTAC-BCL-XL DT2216 appears to be active in GC cells. DT2216 induces apoptosis of gastric cancer cells in a time-and dose-dependent manner through the proteasome pathway. Statistical analysis showed that the BCL-XL protein level predicts the response of GC cells to BCL-XL targeting therapy and BCL2L1 gene CNVs do not reliably predict BCL-XL expression.Conclusion: We identified BCL-XL as a promising therapeutic target in a subset of GC cases with high levels of BCL-XL protein expression. Functionally, we demonstrated that both selective BCL-XL inhibitors and VHL-based PROTAC BCL-XL can potently kill GC cells that are reliant on BCL-XL for survival. However, we found that BCL2L1 copy number variations(CNVs) cannot reliably predict BCL-XL expression, but the BCL-XL protein level serves as a useful biomarker for predicting the sensitivity of GC cells to BCL-XL-targeting compounds. Taken together, our study pinpointed BCL-XL as potential druggable target for specific subsets of GC. 展开更多
关键词 apoptosis BCL2L1(bcl-XL) gastric cancer(GC) PROTAC-bcl-XL selective bcl-XL inhibitors
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二芳基取代-1,2,4-三唑类化合物的合成及其抗炎活性研究 被引量:6
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作者 徐进宜 姚和权 +6 位作者 曾翼 华维一 吴晓明 王秋娟 胡松 吴雪丰 岳攀 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2005年第12期2254-2258,共5页
以选择性环氧化酶-2(COX-2)抑制剂Celecoxib为先导,根据其构效关系和分子模拟研究结果,应用生物电子等排原理等药物设计方法,设计合成了19个结构全新的二芳基取代-1,2,4-三唑类衍生物,其结构经IR,1H NMR,MS和元素分析确证.初步的药理试... 以选择性环氧化酶-2(COX-2)抑制剂Celecoxib为先导,根据其构效关系和分子模拟研究结果,应用生物电子等排原理等药物设计方法,设计合成了19个结构全新的二芳基取代-1,2,4-三唑类衍生物,其结构经IR,1H NMR,MS和元素分析确证.初步的药理试验结果表明,部分目标化合物具有一定的抗炎活性. 展开更多
关键词 1 2 4-三唑类衍生物 合成 选择性环氧化酶-2抑制剂 抗炎
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环氧合酶-2在大鼠酒精性肝损伤中的作用 被引量:6
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作者 易辉 王新 +1 位作者 苗继延 樊代明 《解放军医学杂志》 CAS CSCD 北大核心 2003年第4期340-342,F003,共4页
为探讨环氧合酶 2 (COX 2 )在大鼠酒精性肝损伤中的作用 ,将大鼠随机分为 3组。正常组 :予以玉米油 +葡萄糖液灌胃 ;模型组 :玉米油 +酒精灌胃 ;处理组 :玉米油 +酒精 +塞莱昔布 (celecoxib,为COX 2选择性抑制剂)灌胃。 3周后处死大鼠 ... 为探讨环氧合酶 2 (COX 2 )在大鼠酒精性肝损伤中的作用 ,将大鼠随机分为 3组。正常组 :予以玉米油 +葡萄糖液灌胃 ;模型组 :玉米油 +酒精灌胃 ;处理组 :玉米油 +酒精 +塞莱昔布 (celecoxib,为COX 2选择性抑制剂)灌胃。 3周后处死大鼠 ,然后进行大鼠肝组织切片HE染色、脂肪染色及COX 2免疫组化染色 ;血清AST、ALT水平、血浆及肝组织匀浆谷胱甘肽 S转移酶 (GST)活性测定。结果发现 ,模型组脂肪染色明显加重 ,AST升高 ,肝GST活性降低 ,COX 2表达增加 ;而处理组比模型组脂肪染色减轻 ,AST下降 ,GST活性上升 ,肝组织中COX 2表达明显减少。提示使用选择性COX 2抑制剂能减轻大鼠酒精性肝损伤 ,证实COX 2参与了大鼠酒精性肝损伤过程。 展开更多
关键词 环氧合酶-2 大鼠 酒精性肝损伤 作用 免疫组化
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选择性COX-2抑制剂对胃癌细胞株BGC-823增殖和凋亡的影响 被引量:9
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作者 李乾 彭杰 张桂英 《中南大学学报(医学版)》 CAS CSCD 北大核心 2008年第12期1123-1128,共6页
目的:观察塞来昔布对胃癌细胞株BGC-823细胞增殖和凋亡的影响,寻找安全有效的治疗胃癌的化疗药物。方法:常规培养胃癌细胞株BGC-823至80%融合,加入不同浓度塞来昔布继续培养,采用噻唑蓝(MTT)比色法观察其对胃癌BGC-823细胞生长的影响。... 目的:观察塞来昔布对胃癌细胞株BGC-823细胞增殖和凋亡的影响,寻找安全有效的治疗胃癌的化疗药物。方法:常规培养胃癌细胞株BGC-823至80%融合,加入不同浓度塞来昔布继续培养,采用噻唑蓝(MTT)比色法观察其对胃癌BGC-823细胞生长的影响。流式细胞仪检测细胞周期和细胞凋亡情况。RT-PCR技术检测p21和Fas的表达。结果:MTT比色法显示体外不同浓度塞来昔布均能抑制胃癌BGC-823细胞生长,呈浓度和时间依赖性,各浓度组间比较有显著差异(P<0.05)。流式细胞仪检测发现在0~100μmol/L内,随浓度增加G1期细胞数增加,S期细胞数减少;RT-PCR显示塞来昔布干预后胃癌BGC-823细胞p21和Fas的表达增强且呈浓度依赖性,各浓度组间比较,差异有统计学意义(P<0.05)。结论:体外塞来昔布抑制胃癌BGC-823细胞增殖和促进其凋亡,可能与p21上调阻止细胞周期进展和促进Fas表达诱导细胞凋亡有关。 展开更多
关键词 选择性环氧化酶-2 塞来昔布 细胞增殖 细胞凋亡 BCC-823细胞系
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环氧合酶-2在CCl_4诱导大鼠肝纤维化形成中的作用 被引量:5
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作者 涂传涛 郭津生 +1 位作者 方国汀 王吉耀 《复旦学报(医学版)》 CAS CSCD 北大核心 2006年第5期587-591,共5页
目的探讨环氧合酶-2(cyclooxygenase-2,COX-2)在四氯化碳(CCl4)诱导大鼠肝纤维化形成过程中的作用。方法用50%CCl4经腹腔注射,每周2次共8周诱导雄性S-D大鼠肝纤维化模型。将S-D大鼠随机分3组:正常对照组给橄榄油腹腔注射;罗非昔布组在C... 目的探讨环氧合酶-2(cyclooxygenase-2,COX-2)在四氯化碳(CCl4)诱导大鼠肝纤维化形成过程中的作用。方法用50%CCl4经腹腔注射,每周2次共8周诱导雄性S-D大鼠肝纤维化模型。将S-D大鼠随机分3组:正常对照组给橄榄油腹腔注射;罗非昔布组在CCl4诱导肝纤维化模型的同时给予选择性COX-2抑制剂罗非昔布(按10 mg.d-1.kg-1体重溶于10 mL生理盐水中灌胃);模型对照组在CCl4诱导肝纤维化模型的同时给予同等体积的生理盐水灌胃。第8周末处死大鼠,病理组织学观察肝纤维化严重程度并评分,并通过Masson三色染色法将胶原染成蓝色,用图像分析仪自动分析胶原面积。用Western blot检测肝组织COX-2表达和Ⅳ型胶原。计数肝窦内α-SMA阳性的细胞数来观察肝星状细胞的活化。结果与肝纤维化模型组相比,罗非昔布干预组肝组织纤维化严重程度明显减轻(平均积分分别为:4.00±0.00vs2.89±0.60,P<0.05)、胶原面积也减少(分别为:30.7±8.9vs23.5±6.5,P<0.05)、肝窦内平均α-SMA阳性细胞数明显减少(分别为:12.5±1.3vs7.4±1.4,P<0.01);Western blot分析提示:与肝纤维化模型组相比,罗非昔布能降低Ⅳ型胶原表达、对COX-2表达无明显影响。结论COX-2在肝纤维化的形成过程中发挥重要作用,选择性COX-2抑制剂罗非昔布具有减轻或阻止肝纤维生成的作用。 展开更多
关键词 肝纤维生成 肝纤维化 环氧合酶-2 肝星状细胞 选择性环氧合酶-2抑制剂 Ⅳ型胶原
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中长期使用特异性COX-2抑制剂对大鼠左心室重塑的影响 被引量:4
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作者 梁子敬 王舒茵 +3 位作者 曾量波 叶政 卢鉴财 郑贵星 《广东医学》 CAS CSCD 北大核心 2009年第9期1235-1237,共3页
目的通过观察大鼠慢性压力负荷性心肌肥厚过程中左心室重塑2个时间点使用特异性COX-2抑制剂Celecoxib前后左心室质量指数(LVMI)、心脏重/体重比值和炎症标记物的变化,以了解中长期使用特异性COX-2抑制剂对左心室重塑的作用。方法将40只... 目的通过观察大鼠慢性压力负荷性心肌肥厚过程中左心室重塑2个时间点使用特异性COX-2抑制剂Celecoxib前后左心室质量指数(LVMI)、心脏重/体重比值和炎症标记物的变化,以了解中长期使用特异性COX-2抑制剂对左心室重塑的作用。方法将40只雄性SD大鼠随机分成5组:假手术组、手术20周组、Cele-coxib20周组、手术24周组、Celecoxib24周组。手术组及Celecoxib组均按照腹主动脉缩窄法制作压力负荷性心肌肥厚大鼠模型,在造模16周后,用Celecoxib10mg/kg,均匀混入饲料中喂服Celecoxib组大鼠,分别连续喂养4周和8周。在造模20周及24周时,观察大鼠左心室质量指数和炎症标记物TNF-α、TGF-β、PGE2、CRP、UA变化。结果手术组20和24周LVMI、TNF-α、PGE2、CRP、UA较假手术组均有升高(P<0.01,P<0.05);Celecoxib24周组LVMI及心脏重/体重比值、TNF-α、TGF-β、PGE2、CRP、UA均较手术组有下降(P<0.01,P<0.05)。结论炎症参与了心肌重塑的过程,特异性COX-2抑制剂Celecoxib可能通过抗细胞因子起到延缓左心室重塑发展。 展开更多
关键词 左心室重塑 特异性COX-2抑制剂 炎症标记物
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选择性环氧合酶-2(COX-2)非甾体抗炎药的安全性与有效性 被引量:22
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作者 胡曦丹 王卓 《药学服务与研究》 CAS 2016年第2期81-85,共5页
非甾体抗炎药(non-steroidal anti-inflammatory drugs,NSAIDs)作为急性和慢性疼痛管理治疗药物的重要组成部分,在临床使用历史长达100年之久,是世界范围内使用最为广泛的一类药物。所有的非选择性NSAIDs都存在潜在的副作用,尤其是胃肠... 非甾体抗炎药(non-steroidal anti-inflammatory drugs,NSAIDs)作为急性和慢性疼痛管理治疗药物的重要组成部分,在临床使用历史长达100年之久,是世界范围内使用最为广泛的一类药物。所有的非选择性NSAIDs都存在潜在的副作用,尤其是胃肠道和心血管系统的药品不良反应(ARDs)。这都与它们对环氧合酶-1(cyclooxygenase-1,COX-1)和COX-2抑制作用的选择性有关。为了避免与COX-1抑制相关的胃肠道副作用,罗非昔布等选择性COX-2抑制剂应运而生。随着临床应用时间的延长,以及一些最新大型临床试验的结果揭晓,COX-2选择性抑制剂胃肠道的安全性得到了广泛的验证,但其非胃肠道ADRs也越来越令人担忧,尤其是其心血管、肾脏以及过敏等方面的ADRs在近年来逐渐受到关注。本文总结近年来对选择性COX-2抑制剂的有效性及安全性进行评价的文献,以期临床选用时有更多的参考。 展开更多
关键词 消炎药 非甾药 选择性COX-2抑制剂 有效性 安全性
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选择性COX-2抑制剂塞来昔布对肝星状细胞增殖及活化的影响 被引量:6
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作者 唐保东 徐雅 +1 位作者 刘思纯 马博 《胃肠病学和肝病学杂志》 CAS 2007年第5期468-470,共3页
目的通过观察选择性COX-2抑制剂塞来昔布对肝星状细胞增殖及活化的影响,以探讨COX-2在肝纤维化中的作用。方法用不同浓度的选择性COX-2抑制剂塞来昔布作用于体外培养的人肝星状细胞株LI-90,采用MTT法和半定量RT-PCR法检测塞来昔布对肝... 目的通过观察选择性COX-2抑制剂塞来昔布对肝星状细胞增殖及活化的影响,以探讨COX-2在肝纤维化中的作用。方法用不同浓度的选择性COX-2抑制剂塞来昔布作用于体外培养的人肝星状细胞株LI-90,采用MTT法和半定量RT-PCR法检测塞来昔布对肝星状细胞增殖及活化的影响。结果塞来昔布可显著抑制体外培养的肝星状细胞LI-90的增殖和活化,随着药物剂量的增加和时间的延长,肝星状细胞LI-90的增殖和活化明显抑制,呈剂量和时间依赖性。结论塞来昔布对肝星状细胞增殖和活化的抑制作用是研究肝纤维化预防和治疗的重要方向之一。 展开更多
关键词 选择性COX-2抑制剂 肝星状细胞 肝纤维化
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Cox-2选择性抑制剂预防结直肠癌术后复发的作用 被引量:4
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作者 金志明 王天翔 尹路 《上海交通大学学报(医学版)》 CAS CSCD 北大核心 2008年第4期424-426,共3页
目的探讨Cox-2选择性抑制剂预防结直肠癌术后复发的作用。方法52例患者经手术和术后病理证实为结直肠腺癌(不晚于T3N0M0期),免疫组化检测Cox-2表达阳性,随机分为对照组(n=30)和试验组(n=22)。对照组术后2周单纯按folfox-4方案化疗6个疗... 目的探讨Cox-2选择性抑制剂预防结直肠癌术后复发的作用。方法52例患者经手术和术后病理证实为结直肠腺癌(不晚于T3N0M0期),免疫组化检测Cox-2表达阳性,随机分为对照组(n=30)和试验组(n=22)。对照组术后2周单纯按folfox-4方案化疗6个疗程;试验组术后1周起口服塞来昔布(200 mg,qd)持续1年,术后2周后同样按folfox-4方案化疗6个疗程。比较两组患者手术时、术后6个月及术后1年的肠镜活检标本Cox-2、Bcl-2和血管内皮生长因子(VEGF)的表达情况,并比较3年生存率和复发率。结果试验组患者术后1年时Cox-2、Bcl-2和VEGF阴性表达率较6个月时明显增加(P<0.05);对照组患者术后6个月时Cox-2、Bcl-2和VEGF弱表达和阴性表达率与术后1年时比较,差异无统计学意义(P>0.05)。两组患者3年生存率无统计学差异(P>0.05),但试验组患者的3年复发率显著低于对照组(P<0.05)。结论Cox-2选择性抑制剂显著降低Cox-2、Bcl-2和VEGF的表达,并降低结直肠癌术后的3年复发率,有可能成为预防结直肠癌术后复发的一种新方法。 展开更多
关键词 结直肠癌 COX-2选择性抑制剂 生存率 复发率
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MMP-2和ICAM-1在裸鼠体内塞来昔布抑制肝癌组织中的表达 被引量:3
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作者 殷积彬 李宝馨 +4 位作者 谢新玉 刘冰熔 吕志武 关景明 高善玲 《世界华人消化杂志》 CAS 北大核心 2010年第12期1206-1210,共5页
目的:研究机体内部选择性环氧合酶-2(COX-2)抑制剂对肝细胞癌的抑制作用.方法:将三种肝癌细胞株HepG2、BEL-7402和SMMC-7721分别接种于6周龄裸鼠肝脏被膜下;将接种了不同肝癌细胞株的裸鼠分别分为3组,阴性对照组给予生理盐水灌胃,实验... 目的:研究机体内部选择性环氧合酶-2(COX-2)抑制剂对肝细胞癌的抑制作用.方法:将三种肝癌细胞株HepG2、BEL-7402和SMMC-7721分别接种于6周龄裸鼠肝脏被膜下;将接种了不同肝癌细胞株的裸鼠分别分为3组,阴性对照组给予生理盐水灌胃,实验组给予塞来昔布灌胃,阳性对照组进行生理盐水灌胃的同时使用阿霉素腹腔注射;3wk后对裸鼠肝脏肿瘤取材、免疫组织化学法观察肿瘤组织中基质金属蛋白酶-2(MMP-2)及其抑制剂(TIMP-2)以及细胞间黏附因子-1(ICAM-1)的表达.结果:在肝脏被膜下接种了HepG2、BEL-7402和SMMC-7721肝癌细胞株的裸鼠中,应用塞来昔布的裸鼠肿瘤组织中MMP-2的表达下降(P<0.05),MMP-2的表达增加(P<0.05),TIMP-2/MMP-2比值增加.在肝脏被膜下接种了BEL-7402和SMMC-7721肝癌细胞株的裸鼠中,应用塞来昔布的裸鼠肿瘤组织中ICAM-1表达下降.结论:塞来昔布在机体内部可能具有抑制肝癌细胞转移和改善预后的作用. 展开更多
关键词 选择性环氧合酶-2抑制剂 肝癌 基质金属蛋白酶-2 细胞间黏附因子-1
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