Synthesis and Biological Evaluation of Gastroprotective Polymer Conjugates of Aceclofenac

IF 1.7 3区化学 Q3 CHEMISTRY, ORGANIC Current Organic Chemistry Pub Date : 2024-06-24 DOI:10.2174/0113852728301376240604052622

Monika Mishra, Viney Chawla, Pooja A. Chawla

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Abstract

: Nonsteroidal anti-inflammatory drugs account for a sizeable fraction of the drugs prescribed worldwide. If consumed for a long time, they can cause ulcers and life-threatening side effects. Since the acidic group present in NSAIDs is mainly responsible for these side effects, the scientists try to synthesize polymer drug conjugates that avoid these side effects but still retain the potency of the parent drug. Macromolecular drug conjugates of aceclofenac were prepared by employing pectin, β cyclodextrin, deacetylated chitin (chitosan) and albumin (egg and bovine serum). The prepared conjugates were characterized and tested for their antiinflammatory, antinociceptive and antiulcerogenic activity. Further experimentation was undertaken to analyze the behavior of compounds and their stability in hydrolytic conditions. Test compound A1, a pectin conjugate of aceclofenac, exhibited significant antinociceptive and anti-inflammatory activity with a significant decrease in ulcer index (4.45±0.24) as against aceclofenac (8.61±0.40) or vehicle (12.39±0.44) treated group. A novel and safer polymer drug conjugate of aceclofenac has been synthesized and evaluated.

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阿昔洛芬酸胃保护性聚合物共轭物的合成与生物学评价

:非甾体类消炎药占全球处方药的很大一部分。如果长期服用，它们会导致溃疡和危及生命的副作用。由于非甾体抗炎药中的酸性基团是造成这些副作用的主要原因，科学家们试图合成聚合物药物共轭物，以避免这些副作用，但仍保留母药的药效。研究人员利用果胶、β 环糊精、脱乙酰甲壳素（壳聚糖）和白蛋白（鸡蛋和牛血清）制备了醋氯芬酸的大分子药物共轭物。对制备的共轭物进行了表征，并测试了其抗炎、抗痛觉和抗溃疡活性。进一步的实验分析了化合物的行为及其在水解条件下的稳定性。试验化合物 A1 是醋氯芬酸的果胶共轭物，与醋氯芬酸（8.61±0.40）或载体（12.39±0.44）处理组相比，具有显著的抗痛觉和抗炎活性，溃疡指数（4.45±0.24）显著下降。我们合成并评估了一种新型、更安全的醋氯芬酸聚合物药物共轭物。

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来源期刊

Current Organic Chemistry 化学-有机化学

CiteScore

3.70

自引率

7.70%

发文量

审稿时长

1 months

期刊介绍： Current Organic Chemistry aims to provide in-depth/mini reviews on the current progress in various fields related to organic chemistry including bioorganic chemistry, organo-metallic chemistry, asymmetric synthesis, heterocyclic chemistry, natural product chemistry, catalytic and green chemistry, suitable aspects of medicinal chemistry and polymer chemistry, as well as analytical methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by chosen experts who are internationally known for their eminent research contributions. The Journal also accepts high quality research papers focusing on hot topics, highlights and letters besides thematic issues in these fields. Current Organic Chemistry should prove to be of great interest to organic chemists in academia and industry, who wish to keep abreast with recent developments in key fields of organic chemistry.