Habtemariam Solomon, Belai Abebech
Pharmacognosy Research Laboratories & Herbal Analysis Services, Chatham-Maritime, Kent ME4 4TB. United Kingdom.
Enteric Neuroscience Lab, Health Sciences Research Centre, Department of Life Sciences, University of Roehampton London, Whitelands College, Holybourne Avenue, London SW15 4JD. United Kingdom.
Mini Rev Med Chem. 2018;18(3):234-243. doi: 10.2174/1389557517666170120152417.
Inflammatory bowel disease (IBD), commonly represented by ulcerative colitis and Crohn's disease, is a form of chronic inflammatory disorders of the gastrointestinal system. Its current drug treatment includes the use of antibiotics, 5-aminosalicylates, corticosteroids, immune-modifying agents and biologics such as anti-TNF agents and adhesion molecules blockers. These drugs have inherent problems of efficacy as many IBD sufferers need surgical intervention at some stage, high cost especially for the protein-based drugs, loss of efficacy and unwanted side effects. The discovery of novel drugs including those from natural sources that overcome the above mentioned drawbacks of the current therapy is therefore of great interest. While the flavonoid quercetin with proven antiinflammatory effect failed to show activity in vivo, its glycoside rutin has recently proven to possess a significant IBD therapeutic potential in experimental animals. In this communication, the pharmacological and pharmacokinetic profiles of rutin along with its ability to serve as a prodrug that deliver the bioactive quercetin close to the IBD site are discussed. Potential mechanisms of action far beyond antioxidant effects such as suppression of proinflammatory mediators' release and expression of inflammatory proteins (e.g. adhesion molecules, cyclooxygenase, nitric oxide synthase, etc.) are also scrutinized.
炎症性肠病（IBD）通常以溃疡性结肠炎和克罗恩病为代表，是一种胃肠道系统的慢性炎症性疾病。其目前的药物治疗包括使用抗生素、5-氨基水杨酸酯、皮质类固醇、免疫调节剂以及生物制剂，如抗TNF制剂和黏附分子阻滞剂。这些药物存在固有的疗效问题，因为许多IBD患者在某个阶段需要手术干预，成本高昂，尤其是基于蛋白质的药物，还会出现疗效丧失和不良副作用。因此，发现包括来自天然来源的新型药物以克服当前治疗方法的上述缺点具有重大意义。虽然已证实具有抗炎作用的黄酮类化合物槲皮素在体内未显示出活性，但其糖苷芦丁最近已证实在实验动物中具有显著的IBD治疗潜力。在本通讯中，讨论了芦丁的药理和药代动力学概况以及其作为前药在IBD部位附近递送生物活性槲皮素的能力。还仔细研究了远远超出抗氧化作用的潜在作用机制，如抑制促炎介质的释放和炎症蛋白（如黏附分子、环氧化酶、一氧化氮合酶等）的表达。
