CN116549447A - 西达苯胺在治疗炎症性肠病中的应用 - Google Patents
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Abstract
本发明公开了西达苯胺在治疗炎症性肠病中的应用，涉及西达苯胺技术领域，其技术方案要点为西达苯胺在治疗炎症性肠病中溃疡性结肠炎和克罗恩病的应用，效果是西达苯胺对于治疗炎症性肠病能够起到有效作用。
Description
技术领域
本发明涉及西达苯胺技术领域，更具体地说，它涉及西达苯胺在治疗炎症性肠病中的应用。
背景技术
炎症性肠病（IBD）是累及回肠、直肠、结肠的慢性特发性肠道炎症性疾病，主要分为溃疡性结肠炎（UC）和克罗恩病（CD），近年来该病的发病率呈整体上升趋势。虽然IBD的直接致死率不高，但并发症多，严重影响患者的生活质量，甚至会诱发癌变。目前认为IBD属于一种自身免疫性疾病，因此临床常用的IBD治疗药物主要为抗炎、免疫抑制剂、生物抗体制剂等。由于这些药物通常伴有肾脏毒性、固醇类依赖性等毒副作用，导致了它们临床应用的局限性。由此研发新型的IBD治疗药物具有广泛的临床需求。
西达苯胺是组蛋白去乙酰化酶抑制剂，对基因表达具有表观遗传学调控作用。目前西达苯胺临床治疗主要用于至少接受过一次全身化疗的复发或难治的外周T细胞淋巴瘤（PTCL）患者。目前西达苯胺注册的相关临床研究主要集中在血液系统肿瘤和乳腺癌肺癌等实体肿瘤中。由于表观遗传学调控对细胞的功能有多种影响，现有理论研究提示组蛋白去乙酰化酶抑制剂能够调控免疫功能，改善免疫亢进状态，缓解自身免疫性反应。但目前有关西达苯胺对IBD的治疗作用尚无相关研究。
发明内容
针对现有技术存在的不足，本发明的目的在于提供西达苯胺在治疗炎症性肠病中的应用。
为实现上述目的，本发明提供了如下技术方案：
西达苯胺在治疗炎症性肠病中溃疡性结肠炎和克罗恩病的应用。
与现有技术相比，本发明具备以下有益效果：
本发明中，西达苯胺对于治疗炎症性肠病能够起到有效作用。
附图说明
图1为本发明在小鼠取材的示意图；
图2为本发明中葡聚糖硫酸钠组小鼠体重变化示意图；
图3为本发明中疾病活动评分的示意图；
图4为本发明中西达苯胺抑制有DSS所致的结肠缩短示意图；
图5为本发明中在小鼠体内注射不同剂量西达苯胺给药的变化示意图；
图6为本发明中西达苯胺缓解DSS所致的脾脏肿大示意图；
图7为本发明中不同剂量组的西达苯胺对小鼠结肠结构较DSS组改善的示意图。
具体实施方式
参照图1至图7。
实施例对本发明提出的西达苯胺在治疗炎症性肠病中的应用做进一步说明。
西达苯胺在治疗炎症性肠病中溃疡性结肠炎和克罗恩病的应用。
小鼠给予2.5%葡聚糖硫酸钠（DSS）水溶液，从第1天至第7天自由饮用以建立炎症性肠病模型。在葡聚糖硫酸钠水溶液饮用前1天，灌胃给予0.3mg/kg或3mg/kg的西达苯胺，每2天给药一次，共给药6次。从第8天起小鼠给予正常饮水，在第10天处死取材（见图1）。期间每天进行体重称量，葡聚糖硫酸钠组小鼠从第6天起体重显著降低，并至第10天持续降低（见图2）。不同剂量的西达苯胺给药能够显著降低葡聚糖硫酸钠引起的体重降低，其中3mg/kg的疗效优于0.3mg/kg的疗效（见图5）。第10天疾病活动评分（DAI）结果显示：葡聚糖硫酸钠组DAI评分约为饮水组的10倍，0.3mg/kg西达苯胺组的DAI评分为饮水组的7.5倍，3.0mg/kg西达苯胺组的DAI评分为饮水组的5倍（见图3），西达苯胺组的DAI评分均显著低于葡聚糖硫酸钠组。上述结果表明西达苯胺灌胃治疗能够显著改善葡聚糖硫酸钠诱导的小鼠炎症性肠病症状，改善体重减轻、腹泻和便血症状。
图4显示西达苯胺可以显著的抑制有DSS所致的结肠长度缩短。图6显示西达苯胺能够显著缓解DSS所致的脾脏肿大。
结肠病理切片HE染色显示：DSS组小鼠的结肠局部腺体结构紊乱，黏膜及黏膜下有大量炎症细胞浸润，黏膜局部糜烂，部分隐窝破坏；而不同剂量组的西达苯胺对小鼠结肠结构较DSS组比均得到了显著改善（见图7）。
以上所述仅是本发明的优选实施方式，本发明的保护范围并不仅局限于上述实施例，凡属于本发明思路下的技术方案均属于本发明的保护范围。应当指出，对于本技术领域的普通技术人员来说，在不脱离本发明原理前提下的若干改进和润饰，这些改进和润饰也应视为本发明的保护范围。
Claims (1)
1.西达苯胺在治疗炎症性肠病中溃疡性结肠炎和克罗恩病的应用。
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103254205A (zh) * | 2009-10-13 | 2013-08-21 | Dac有限公司 | 作为组蛋白脱乙酰酶抑制剂的螺环衍生物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103254205A (zh) * | 2009-10-13 | 2013-08-21 | Dac有限公司 | 作为组蛋白脱乙酰酶抑制剂的螺环衍生物 |
Non-Patent Citations (2)
| Title |
|---|
| CHANG GAO等: "Primary extrasensal nasal-type natural killer/T-cell lymphoma of the sigmoid colon and ıleocecal junction: A case report", TURK J GASTROENTEROL, vol. 31, no. 12, pages 955 - 956 * |
| 蒋少红;马旭东;许云禄;: "组蛋白去乙酰化酶抑制药研究现状", 中国新药与临床杂志, vol. 27, no. 08, pages 598 - 603 * |
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