穿心莲内酯潜在的抗银屑病作用:与外用皮质类固醇的比较研究

Indira Dharmasamitha, Luh Made Mas Rusyati, Dyah Kanya Wati, I Made Agus Gelgel Wirasuta
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引用次数: 0

摘要

背景:穿心莲内酯(Andrographolide,AP)是一种生物活性抗炎化合物,可抑制 NF-κB、TNF-α 和白细胞介素 IL-6。目前,AP 与地塞米松针对 NF-κB 受体的分子对接模拟显示,AP 的能量高于地塞米松。这成为治疗银屑病的一种潜在方法:本手稿报告了桑比洛托 AP 与外用类固醇相比在治疗银屑病方面的有效性:本研究对 AP 的含量及其代谢物杂质、凝胶配方、分子对接、体内皮肤毒性研究和体内抗银屑病活性进行了 TLC 分析。这是一项综合了室内研究和体内研究的研究。通过多变量统计分析(PCA)对这项体内研究进行了分析,以阐明穿心莲内酯衍生物与几种靶蛋白之间的数据星座关系。干预为期七天。对PASI评分、分子参数(IL-6、IL-17、VEGF和TNF-a水平)以及组织病理学结果进行了评估:分子对接结果显示,穿心莲内酯与IL-6、NF-kB和TNF-α的结合亲和力较高,与皮质类固醇的结合亲和力相当。在体内研究中,我们发现有几个参数在统计学上与干预有显著差异,包括最终的 PASI 评分(p = 0.017)、发红(p = 0.017)、鳞屑(p = 0.040)、厚度(p = 0.023)、银屑病组织病理学总评分(p = 0.037)、角质层评分(p = 0.018):结论:Emulgel AP 0.1%可降低抗炎剂,而抗炎剂对银屑病的发展至关重要。
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The Potential Anti-psoriatic Effects of Andrographolide: A Comparative Study to Topical Corticosteroids.

Background: Andrographolide (AP), a bioactive anti-inflammatory compound of Sambiloto, inhibits NF-κB, TNF-α, and interleukin IL-6. Nowadays, molecular docking simulation between AP and dexamethasone against NF-κB receptor presented the energy AP higher than dexamethasone. This becomes a potential treatment for psoriasis.

Objective: This manuscript reported the effectiveness of AP from Sambiloto in treating psoriasis compared to topical steroids.

Methods: This study conducted TLC analysis of AP content and its metabolite impurities, emulgel formulation, molecular docking, in-silico skin toxicity study, and in-vivo anti-psoriatic activity. This was a combination study of an in-silico study and an in-vivo study. This in-silico study was analyzed through multivariate statistical analysis (PCA) to elucidate the data constellation relationship of andrographolide derivatives with several target proteins. The intervention was performed in seven days. The PASI score, molecular parameters (IL-6, IL-17, VEGF, and TNF-a levels), and histopathological findings were assessed.

Results: Molecular docking results revealed andrographolide to exhibit a relatively high binding affinity towards IL-6, NF-kB, and TNF-α which is comparable to the corticosteroids, andrographolide also shares similar residue interaction profile with each of the respective protein's native ligand. In the in-vivo study, we found several parameters statistically significantly different regarding the intervention, including final PASI score (p = 0.017), redness (p = 0.017), scale (p = 0.040), thickness (p = 0.023), total histopathology of psoriasis score (p = 0.037), keratin layer score (p = 0.018).

Conclusion: Emulgel AP 0.1% could lower the anti-inflammatory agent, which is vital to psoriasis progression.

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