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5-羟色胺4受体激动剂Prucalopride对胃癌细胞增殖、迁移、侵袭、凋亡的影响
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作者 刘源 王璐 +1 位作者 马超 武聚山 《山东医药》 CAS 2018年第2期30-32,共3页
目的观察5-羟色胺(5-HT)4受体激动剂Prucalopride对胃癌细胞增殖、迁移、侵袭、凋亡的影响,并探讨其机制。方法将胃癌细胞MKN28随机分为观察组和对照组,分别予以10μmol/L的Prucaloprid及等体积DMSO处理24 h,分别采用CCK8、Transwell、... 目的观察5-羟色胺(5-HT)4受体激动剂Prucalopride对胃癌细胞增殖、迁移、侵袭、凋亡的影响,并探讨其机制。方法将胃癌细胞MKN28随机分为观察组和对照组,分别予以10μmol/L的Prucaloprid及等体积DMSO处理24 h,分别采用CCK8、Transwell、流式细胞术检测细胞增殖(OD值)、迁移和侵袭(穿膜细胞数)及细胞凋亡,用Western blotting法检测细胞凋亡相关蛋白Bcl-2、Bax、活化的Caspase3(Active Caspase3)及PI3K信号通路关键蛋白蛋白激酶B(AKT)、磷酸化AKT(p-AKT)、哺乳动物雷帕霉素靶蛋白(mTOR)、磷酸化mTOR(p-mTOR)、P70。结果两组处理24 h时细胞OD值比较无统计学差异,48、72 h时观察组细胞OD值均低于对照组(P均<0.05);观察组细胞迁移及侵袭个数分别为(150±6)、(59±2)个,均高于对照组的(58±3)、(21±4)个(P均<0.05);观察组细胞凋亡率为26.1%,高于对照组的3.9%(P<0.05)。与对照组比较,观察组抗凋亡蛋白Bcl-2表达量下降(P<0.05),促凋亡蛋白Bax、Active Caspase3及PI3K信号通路蛋白p-AKT、p-mTOR、P70表达量增加(P均<0.05)。结论 Prucalopride可抑制胃癌细胞的增殖、迁移和侵袭,促进胃癌细胞凋亡,并可能通过激活PI3K信号通路发挥该作用。 展开更多
关键词 胃癌 prucalopride 5-羟色胺4受体激动剂 细胞增殖 细胞凋亡 PI3K信号通路
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Prucalopride通过促进自噬抑制胶质瘤细胞U251增殖
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作者 霍会永 刘冰 +5 位作者 曹凌 赵现 曹妍 薛靖 王如科 李军涛 《现代肿瘤医学》 CAS 2018年第9期1340-1344,共5页
目的:研究Prucalopride对胶质瘤U251细胞增殖、自噬、凋亡的影响,并探讨其相关信号通路。方法:通过CCK8检测细胞增殖的变化;Transwell检测迁移和侵袭的变化;细胞流式实验、Western blot检测细胞凋亡的变化;Western blot检测自噬相关蛋白... 目的:研究Prucalopride对胶质瘤U251细胞增殖、自噬、凋亡的影响,并探讨其相关信号通路。方法:通过CCK8检测细胞增殖的变化;Transwell检测迁移和侵袭的变化;细胞流式实验、Western blot检测细胞凋亡的变化;Western blot检测自噬相关蛋白LC3、Beclin1、p62的表达;AKT/m TOR通路相关蛋白的变化。结果:CCK8显示Prucalopride显著抑制U251细胞的增殖(P<0.05);Transwell侵袭实验显示Prucalopride可以抑制脑胶质瘤细胞的迁移和侵袭(P<0.05);细胞流式实验显示Prucalopride促进U251细胞的凋亡(P<0.05),Prucalopride处理后细胞凋亡相关蛋白Bax、Active Caspase3水平升高,Bcl-2表达降低;自噬相关蛋LC3、Beclin1表达上调,p62表达下调;p-AKT蛋白和p-m TOR蛋白水平显著降低。结论:Prucalopride通过抑制AKT/m TOR信号通路激活自噬抑制U251细胞增殖和迁移,促进其凋亡。 展开更多
关键词 prucalopride 脑胶质细胞瘤 自噬 AKT/mTOR信号通路
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Prucalopride-associated acute tubular necrosis 被引量:1
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作者 Vithika Sivabalasundaram Flavio Habal David Cherney 《World Journal of Clinical Cases》 SCIE 2014年第8期380-384,共5页
We report the first case of acute renal failure secondary to prucalopride, a novel agent for the treatment of chronic constipation. The 75 years old male patient was initiated on prucalopride after many failed treatme... We report the first case of acute renal failure secondary to prucalopride, a novel agent for the treatment of chronic constipation. The 75 years old male patient was initiated on prucalopride after many failed treatments for constipation following a Whipple's procedure for pancreatic cancer. Within four months of treatment his creatinine rose from 103 to 285 μmol/L(e GFR 61 decrease to 19 m L/min per 1.73 m2). He was initially treated with prednisone for presumed acute interstitial nephritis as white blood casts were seen on urine microscopy. When no improvement was detected, a core biopsy was performed and revealed interstitial fibrosis and tubular atrophy. The presence of oxalate and calcium phosphate crystals were also noted. These findings suggest acute tubular necrosis which may have been secondary to acute interstitial nephritis or hemodynamic insult. The use of prednisone may have suppressed signs of inflammation and therefore the clinical diagnosis was deemed acute interstitial nephritis causing acute tubular necrosis. There are no previous reports ofprucalopride associated with acute renal failure from the literature, including previous Phase Ⅱ and Ⅲ trials. 展开更多
关键词 prucalopride Acute kidney TUBULAR NECROSIS Renal INSUFFICIENCY CONSTIPATION ADVERSE drug event
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Efficacy of Prucalopride in bowel cleansing before colonoscopy:Results of a pilot study
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作者 Vito Domenico Corleto Giulio Antonelli +2 位作者 Chiara Coluccio Lucia D'Alba Emilio di Giulio 《World Journal of Gastrointestinal Endoscopy》 CAS 2017年第11期558-560,共3页
Colonoscopy is a crucial diagnostic instrument for colorectal cancer screening and an adequate bowel preparation is definitely decisive for the success of the procedure. Especially in elderly patients, bowel cleansing... Colonoscopy is a crucial diagnostic instrument for colorectal cancer screening and an adequate bowel preparation is definitely decisive for the success of the procedure. Especially in elderly patients, bowel cleansing is considered a big issue, because it is often poorly tolerated for many reasons(like inability to swallow large volume of liquids or unlikable taste); this can cause a suboptimal preparation that may lead to miss a neoplastic lesion. There is relatively little data about how to improve preparation tolerability. The purpose of our pilot study was to analyze the effect of prucalopride(Resolor~?), a highly selective serotonin 5HT4 receptor agonist used for chronic constipation for its ability to stimulate gastrointestinal peristalsis, undertaken the day before colonoscopy, followed by half volume of polyethylene glycol solution. We found that this can be a good and safe method to achieve an adequate and better-tolerated colon cleansing. 展开更多
关键词 清洁的肠 COLONOSCOPY prucalopride 屏蔽 Colorectal 癌症
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Prucalopride (Motegrity)
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作者 马德翊(编译) 关奇(审校) 《中国药物化学杂志》 CAS CSCD 北大核心 2019年第6期498-498,共1页
Prucalopride是由爱尔兰夏尔(Shire)公司研发的一种用于治疗成人慢性特发性便秘(CIC)的口服药物,于2018年12月14日获得美国FDA批准上市,其商品名为Motegrity[1]。Prucalopride的中文化学名称:4-氨基-5-氯-2,3-二氢-N-[1-(3-甲氧基丙基)... Prucalopride是由爱尔兰夏尔(Shire)公司研发的一种用于治疗成人慢性特发性便秘(CIC)的口服药物,于2018年12月14日获得美国FDA批准上市,其商品名为Motegrity[1]。Prucalopride的中文化学名称:4-氨基-5-氯-2,3-二氢-N-[1-(3-甲氧基丙基)-4-哌啶基]-7-苯并呋喃甲酰胺琥珀酸盐;英文化学名称:butanedioic acid 4-amino-5-chloro-2. 展开更多
关键词 治疗组 安慰剂 prucalopride Motegrity
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Novel therapies for constipation 被引量:6
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作者 Sreedhari Thayalasekeran Hani Ali Her-Hsin Tsai 《World Journal of Gastroenterology》 SCIE CAS 2013年第45期8247-8251,共5页
Constipation is a common medical problem and when standard laxatives fail it can be difficult to treat.Different aetiologies require tailored therapeutic approaches.Simple constipation may only require dietary manipul... Constipation is a common medical problem and when standard laxatives fail it can be difficult to treat.Different aetiologies require tailored therapeutic approaches.Simple constipation may only require dietary manipulation while severe neurological or slow transit constipation may need pharmacologic intervention.Recently new drug therapies have been introduced.PubMed and Ovid were searched for reviews,systematic reviews and meta-analysis published since 2003 using the terms:constipation,Prucalopride,Linaclotide and Lubiprostone.This review summarizes potential novel therapies identified as effective in the management of chronic constipation.Prucalopride is a selective 5-hydroxytryptamine receptor agonist.The prucalopride study was in patients,largely women with idiopathic constipation showed improved spontaneous complete bowel movement(SCBM)at a dose of 2 mg a day with few adverse events reported.Linaclotide is a 14-amino acid peptide guanylate cyclase-C agonist.The linaclotide study was carried out in patients with irritable bowel syndrome,constipation group(IBS-C).There was significant improvement of bowel evacuation and symptom resolution in patients on the active treatment arm.Lubiprostone activates type-2 chloride channels,increasing intestinal fluid secretion.In the trials of this drug,the lubiprostone arms had a greater mean number of SCBM.The novel therapies,prucalopride,lubiprostone,and linaclotide had very different modes of action yet,all three have been shown to be efficacious and safe in the treatment dose for constipation. 展开更多
关键词 CONSTIPATION prucalopride Linaclotide
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Review of efficacy and safety of laxatives use in geriatrics 被引量:3
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作者 Manhal Izzy Anju Malieckal +1 位作者 Erin Little Sury Anand 《World Journal of Gastrointestinal Pharmacology and Therapeutics》 CAS 2016年第2期334-342,共9页
AIM:To study the efficacy and safety of pharmacolo-gical treatment of constipation in geriatrics.METHODS:Pub Med,MEDLINE,google scholar,and Ovid were searched to identify human studies performed on the use of laxative... AIM:To study the efficacy and safety of pharmacolo-gical treatment of constipation in geriatrics.METHODS:Pub Med,MEDLINE,google scholar,and Ovid were searched to identify human studies performed on the use of laxatives in elderly with constipation,which were conducted between January1990 and January 2013 using the specified keywords.Controlled studies that enrolled geriatric patients with a diagnosis of constipation and addressed the efficacy and/or the safety of pharmacological treatments were included.Studies were excluded from this review if they were non-controlled trials,case series,or case reports.RESULTS:Out of twenty three studies we initially retrieved in our search,only nine studies met the eligibility criteria of being controlled trials within geriatrics.The laxatives examined in the nine studies were senna,lactulose,sorbital,polyethylene glycol(PEG),lubiprostone,linaclotide,and prucalopride.In those studies,senna combinations had a higher efficacy than sorbitol or lactulose as well as,a very good adverse effect profile.PEG was also shown to be safe and effective in geriatric population.Furthermore,it has been shown that PEG is as safe in geriatrics as in general population.New agents like lubiprostone and prucalopride show promising results but the data about these agents in geriatrics are still limited which warrant further investigation.CONCLUSION:Senna combinations and PEG appear to have a more favorable profile over the other traditionally used laxatives in elderly patients with constipation. 展开更多
关键词 Chronic CONSTIPATION LAXATIVES ELDERLY LUBIPROSTONE Linaclotide prucalopride
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