人直肠黏膜中前列腺素合成酶的抑制作用。
Inhibition of prostaglandin synthetase in human rectal mucosa.
作者信息
Hawkey C J, Lo Casto M
出版信息
Gut. 1983 Mar;24(3):213-7. doi: 10.1136/gut.24.3.213.
Abstract
Miniaturised methods have been used to construct dose-response curves for the effects of inhibitory drugs on prostaglandin synthesis using individual rectal biopsies obtained from patients with ulcerative colitis. The potency of different drugs has been compared. Sulphasalazine, 5 amino salicylic acid (5-ASA) and N-acetyl 5-ASA inhibited prostaglandin synthesis at high concentration, but sulphapyridine and prednisolone did not. Indomethacin and flurbiprofen were considerably more potent inhibitors. These data imply that sulphasalazine does not act by simple inhibition of prostaglandin synthesis but leave open the possibility that sulphasalazine or 5-ASA may be inhibitors of the synthesis of related lipoxygenase products.
摘要
已采用小型化方法，利用从溃疡性结肠炎患者获取的单个直肠活检组织，构建了抑制性药物对前列腺素合成影响的剂量反应曲线。比较了不同药物的效力。柳氮磺胺吡啶、5-氨基水杨酸（5-ASA）和N-乙酰5-ASA在高浓度时抑制前列腺素合成，但磺胺吡啶和泼尼松龙则无此作用。吲哚美辛和氟比洛芬是效力更强的抑制剂。这些数据表明，柳氮磺胺吡啶并非通过简单抑制前列腺素合成起作用，但柳氮磺胺吡啶或5-ASA有可能是相关脂氧合酶产物合成的抑制剂。
相似文献
1
Inhibition of prostaglandin synthetase in human rectal mucosa.人直肠黏膜中前列腺素合成酶的抑制作用。
Gut. 1983 Mar;24(3):213-7. doi: 10.1136/gut.24.3.213.
2
Inhibition of leucocyte motility by drugs used in ulcerative colitis.溃疡性结肠炎用药对白细胞运动的抑制作用。
Gut. 1981 Aug;22(8):642-7. doi: 10.1136/gut.22.8.642.
3
Prostaglandin catabolism and ulcerative colitis: effect of sulphasalazine, 5-aminosalicylic acid and other drugs.前列腺素分解代谢与溃疡性结肠炎：柳氮磺胺吡啶、5-氨基水杨酸及其他药物的作用
Braz J Med Biol Res. 1990;23(12):1323-34.
4
Role of prostaglandins in ulcerative colitis. Enhanced production during active disease and inhibition by sulfasalazine.前列腺素在溃疡性结肠炎中的作用。疾病活动期前列腺素生成增加及柳氮磺胺吡啶对其的抑制作用。
Gastroenterology. 1978 Oct;75(4):638-40.
5
Ulcerative colitis: effect of sulphasalazine, its metabolites and indomethacin on the ability of human colonic mucosa to metabolize prostaglandins in vitro.溃疡性结肠炎：柳氮磺胺吡啶、其代谢产物及吲哚美辛对人结肠黏膜体外代谢前列腺素能力的影响。
Br J Pharmacol. 1982 May;76(1):157-61. doi: 10.1111/j.1476-5381.1982.tb09201.x.
6
Role of platelet-activating factor in ulcerative colitis. Enhanced production during active disease and inhibition by sulfasalazine and prednisolone.血小板活化因子在溃疡性结肠炎中的作用。活动期疾病期间产生增加，柳氮磺胺吡啶和泼尼松龙可抑制其产生。
Gastroenterology. 1988 Nov;95(5):1167-72. doi: 10.1016/0016-5085(88)90346-0.
7
Increased suppressor cell activity in inflammatory bowel disease.炎症性肠病中抑制性细胞活性增加。
Gut. 1981 Dec;22(12):1025-30. doi: 10.1136/gut.22.12.1025.
8
Enhanced formation of sulfidopeptide-leukotrienes in ulcerative colitis and Crohn's disease: inhibition by sulfasalazine and 5-aminosalicylic acid.溃疡性结肠炎和克罗恩病中硫肽白三烯生成增加：柳氮磺胺吡啶和5-氨基水杨酸的抑制作用
Agents Actions. 1986 Jun;18(3-4):381-3. doi: 10.1007/BF01965001.
9
Sulphasalazine and derivatives, natural killer activity and ulcerative colitis.柳氮磺胺吡啶及其衍生物、自然杀伤细胞活性与溃疡性结肠炎
Clin Sci (Lond). 1985 Aug;69(2):177-84. doi: 10.1042/cs0690177.
10
Sulphasalazine, sulphapyridine or 5-aminosalicylic acid--which is the active moiety in rheumatoid arthritis?柳氮磺吡啶、磺胺吡啶或5-氨基水杨酸——类风湿关节炎中的活性成分是哪一种？
Br J Rheumatol. 1995 Nov;34 Suppl 2:16-9.
引用本文的文献
1
Synthesis and Characterization of 5-Aminosalicylic Acid Based Poly(anhydride-esters) by Solution Polymerization.通过溶液聚合合成及表征基于5-氨基水杨酸的聚（酸酐-酯）
J Polym Sci A Polym Chem. 2010 Dec 15;48(24):6003-6008. doi: 10.1002/pola.24381.
2
Medical influences, surgical outcomes: role of common medications on the risk of perforation from untreated diverticular disease.医学影响，手术结果：常见药物在未治疗的憩室疾病穿孔风险中的作用。
World J Gastroenterol. 2013 Sep 28;19(36):5947-52. doi: 10.3748/wjg.v19.i36.5947.
3
Scavenging of reactive oxygen and nitrogen species by the prodrug sulfasalazine and its metabolites 5-aminosalicylic acid and sulfapyridine.前药柳氮磺吡啶及其代谢物 5-氨基水杨酸和磺胺吡啶对活性氧和氮物种的清除作用。
Redox Rep. 2010;15(6):259-67. doi: 10.1179/135100010X12826446921707.
4
Inhibitory effect of flavonoids on the efflux of N-acetyl 5-aminosalicylic acid intracellularly formed in Caco-2 cells.黄酮类化合物对Caco-2细胞内形成的N-乙酰5-氨基水杨酸外排的抑制作用。
J Biomed Biotechnol. 2009;2009:467489. doi: 10.1155/2009/467489. Epub 2009 Aug 13.
5
Mechanism of action of 5-arninosalicylic acid.5-氨基水杨酸的作用机制。
Mediators Inflamm. 1992;1(3):151-65. doi: 10.1155/S0962935192000243.
6
Diclofenac suppositories and acute ischaemic proctitis.双氯芬酸栓剂与急性缺血性直肠炎
Ulster Med J. 2004 May;73(1):63-4.
7
Non-steroidal anti-inflammatory drugs and perforated diverticular disease: a case-control study.非甾体抗炎药与穿孔性憩室病：一项病例对照研究。
Ann R Coll Surg Engl. 2002 Mar;84(2):93-6.
8
Sulphasalazine in the treatment of children with chronic arthritis.柳氮磺胺吡啶治疗儿童慢性关节炎
Clin Rheumatol. 1998;17(5):359-63. doi: 10.1007/BF01450892.
9
Cytokine gene transcription of human colonic intraepithelial lymphocytes costimulated with epithelial cells bearing HLA-DR and its inhibition by 5-aminosalicylic acid.携带HLA - DR的上皮细胞共刺激下人结肠上皮内淋巴细胞的细胞因子基因转录及其受5 - 氨基水杨酸的抑制作用
J Clin Immunol. 1996 Jul;16(4):237-41. doi: 10.1007/BF01541230.
10
Inhibition of leucocyte adhesion molecule upregulation by tumor necrosis factor alpha: a novel mechanism of action of sulphasalazine.肿瘤坏死因子α对白细胞黏附分子上调的抑制作用：柳氮磺胺吡啶的一种新作用机制。
Gut. 1993 Feb;34(2):252-6. doi: 10.1136/gut.34.2.252.
本文引用的文献
1
Rectal mucosal prostaglandin E2 release and its relation to disease activity, electrical potential difference, and treatment in ulcerative colitis.溃疡性结肠炎中直肠黏膜前列腺素E2释放及其与疾病活动、电位差和治疗的关系。
Gut. 1980 Jul;21(7):591-6. doi: 10.1136/gut.21.7.591.
2
Effect of prednisolone on prostaglandin synthesis by rectal mucosa in ulcerative colitis: investigation by laminar flow bioassay and radioimmunoassay.泼尼松龙对溃疡性结肠炎直肠黏膜前列腺素合成的影响：通过层流生物测定法和放射免疫测定法进行的研究。
Gut. 1981 Mar;22(3):190-3. doi: 10.1136/gut.22.3.190.
3
The effect of topical N-acetyl-5-aminosalicylic acid in ulcerative colitis.局部应用N-乙酰-5-氨基水杨酸对溃疡性结肠炎的影响。
Scand J Gastroenterol. 1980;15(6):715-9. doi: 10.3109/00365528009181520.
4
Evidence that prednisolone is inhibitory to the cyclooxygenase activity of human rectal mucosa.有证据表明泼尼松龙对人直肠黏膜的环氧化酶活性具有抑制作用。
Prostaglandins. 1982 Mar;23(3):397-409. doi: 10.1016/0090-6980(82)90085-5.
5
5-Aminosalicylic acid, a co-factor for colonic prostacyclin synthesis?5-氨基水杨酸，结肠前列环素合成的辅助因子？
Lancet. 1981 Aug 1;2(8240):255. doi: 10.1016/s0140-6736(81)90502-x.
6
Distribution studies of salicylazosulfapyridine and its metabolites.柳氮磺胺吡啶及其代谢产物的分布研究。
Gastroenterology. 1973 Feb;64(2):240-5.
7
Assay of prostaglandin-like substances in faeces and their measurement in ulcerative colitis.粪便中前列腺素样物质的测定及其在溃疡性结肠炎中的测量
Prostaglandins. 1976 Mar;11(3):489-97. doi: 10.1016/0090-6980(76)90095-2.
8
Prostaglandins and ulcerative colitis.前列腺素与溃疡性结肠炎
Gastroenterology. 1979 May;76(5 Pt 1):1083.
9
Aspirin-like drugs interfere with arachidonate metabolism by inhibition of the 12-hydroperoxy-5,8,10,14-eicosatetraenoic acid peroxidase activity of the lipoxygenase pathway.阿司匹林样药物通过抑制脂氧合酶途径中12-氢过氧-5,8,10,14-二十碳四烯酸过氧化物酶的活性来干扰花生四烯酸代谢。
Proc Natl Acad Sci U S A. 1979 Aug;76(8):3774-8. doi: 10.1073/pnas.76.8.3774.
10
An experiment to determine the active therapeutic moiety of sulphasalazine.一项确定柳氮磺胺吡啶活性治疗部分的实验。
Lancet. 1977 Oct 29;2(8044):892-5. doi: 10.1016/s0140-6736(77)90831-5.
Zotero 插件