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评估α-l-古洛糖醛酸对强直性脊柱炎患者 COX-1 和 COX-2 基因表达谱的口服给药效果。

Evaluation of the oral administration of α-l-guluronic acid on COX-1 and COX-2 gene expression profile in ankylosing spondylitis patients.

机构信息

Department of Immunology, International Campus, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.

Department of Immunology, Faculty of Medicine, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.

出版信息

Drug Dev Res. 2021 Apr;82(2):296-301. doi: 10.1002/ddr.21756. Epub 2020 Nov 2.

DOI:10.1002/ddr.21756
PMID:33140463
Abstract

Ankylosing spondylitis (AS) is a chronic autoimmune arthritis disease with a genetic background, affecting the skeletal axis, sacroiliac, and peripheral joints. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the first-line treatment for AS to alleviate the inflammation and pain. Despite the beneficial effect, their use is accompanied by a wide variety of possible side effects in the gastrointestinal and kidneys. The α-l-guluronic acid (G2013) is a new nonsteroidal anti-inflammatory patented (PCT/EP2017/067920) drug, which has shown its anti-inflammatory properties in the previous investigations. The present study revealed the oral administration effect of G2013 on COX-1 and COX-2 gene expression in AS patients. The blood samples of twelve 18-45 years old patients suffering AS and BASDAI >4, and BASFI >4, before and after 12 weeks of treatment with G2013 and 12 blood samples of healthy volunteers were collected and the effect of G2013 on the gene expression of COX-1 and COX-2 enzymes were assessed by Real-Time PCR. The results indicate that G2013 is able to reduce the gene expression level of COX-1 and COX-2 enzymes in treated AS patients compared to healthy control. Statistically significant differences were not observed between the treatment and the healthy control groups. According to the findings, G2013 might be categorized and introduced as a novel NSAID for the treatment of AS.

摘要

强直性脊柱炎(AS)是一种具有遗传背景的慢性自身免疫性关节炎疾病,影响骨骼轴、骶髂关节和外周关节。非甾体抗炎药(NSAIDs)是治疗 AS 的一线药物,可缓解炎症和疼痛。尽管有疗效,但它们在胃肠道和肾脏方面有各种各样的潜在副作用。α-l-古洛糖醛酸(G2013)是一种新的非甾体抗炎专利(PCT/EP2017/067920)药物,在之前的研究中已显示出其抗炎特性。本研究揭示了 G2013 对 AS 患者 COX-1 和 COX-2 基因表达的口服给药效果。在 12 周的 G2013 治疗前后,收集了 12 名年龄在 18-45 岁之间、患有 AS 和 BASDAI >4、BASFI >4 的患者以及 12 名健康志愿者的血液样本,并通过实时 PCR 评估 G2013 对 COX-1 和 COX-2 酶基因表达的影响。结果表明,与健康对照组相比,G2013 能够降低治疗 AS 患者 COX-1 和 COX-2 酶的基因表达水平。治疗组和健康对照组之间未观察到统计学差异。根据这些发现,G2013 可能被归类为治疗 AS 的新型 NSAID。

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