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黄酮类衍生物的抗炎活性。

Anti-inflammatory activities of flavonoid derivates.

作者信息

Ysrafil Ysrafil, Sapiun Zulfiayu, Slamet Nangsih Sulastri, Mohamad Fihrina, Hartati Hartati, Damiti Sukmawati A, Alexandra Francisca Diana, Rahman Sudarman, Masyeni Sri, Harapan Harapan, Mamada Sukamto S, Bin Emran Talha, Nainu Firzan

机构信息

Department of Pharmacotherapy, Faculty of Medicine, Universitas Palangka Raya, Palangka Raya 73111, Indonesia.

Department of Pharmacy, Politeknik Kesehatan Kementerian Kesehatan Gorontalo, Gorontalo 96135, Indonesia.

出版信息

ADMET DMPK. 2023 Jul 26;11(3):331-359. doi: 10.5599/admet.1918. eCollection 2023.

Abstract

BACKGROUND AND PURPOSE

Flavonoids are a group of phytochemicals found abundantly in various plants. Scientific evidence has revealed that flavonoids display potential biological activities, including their ability to alleviate inflammation. This activity is closely related to their action in blocking the inflammatory cascade and inhibiting the production of pro-inflammatory factors. However, as flavonoids typically have poor bioavailability and pharmacokinetic profile, it is quite challenging to establish these compounds as a drug. Nevertheless, progressive advancements in drug delivery systems, particularly in nanotechnology, have shown promising approaches to overcome such challenges.

REVIEW APPROACH

This narrative review provides an overview of scientific knowledge about the mechanism of action of flavonoids in the mitigation of inflammatory reaction prior to delivering a comprehensive discussion about the opportunity of the nanotechnology-based delivery system in the preparation of the flavonoid-based drug.

KEY RESULTS

Various studies conducted in silico, in vitro, in vivo, and clinical trials have deciphered that the anti-inflammatory activities of flavonoids are closely linked to their ability to modulate various biochemical mediators, enzymes, and signalling pathways involved in the inflammatory processes. This compound could be encapsulated in nanotechnology platforms to increase the solubility, bioavailability, and pharmacological activity of flavonoids as well as reduce the toxic effects of these compounds.

CONCLUSION

In Summary, we conclude that flavonoids and their derivates have given promising results in their development as new anti-inflammatory drug candidates, especially if they formulate in nanoparticles.

摘要

背景与目的

黄酮类化合物是一类在各种植物中大量存在的植物化学物质。科学证据表明,黄酮类化合物具有潜在的生物活性,包括减轻炎症的能力。这种活性与其阻断炎症级联反应和抑制促炎因子产生的作用密切相关。然而,由于黄酮类化合物通常具有较差的生物利用度和药代动力学特征,将这些化合物开发成药物颇具挑战性。尽管如此,药物递送系统,特别是纳米技术的不断进步,已显示出克服此类挑战的有前景的方法。

综述方法

本叙述性综述在全面讨论基于纳米技术的递送系统在制备基于黄酮类化合物的药物方面的机会之前,概述了关于黄酮类化合物减轻炎症反应作用机制的科学知识。

关键结果

在计算机模拟、体外、体内研究及临床试验中开展的多项研究已表明,黄酮类化合物的抗炎活性与其调节参与炎症过程的各种生化介质、酶和信号通路的能力密切相关。该化合物可封装于纳米技术平台,以提高黄酮类化合物的溶解度、生物利用度和药理活性,并降低这些化合物的毒性作用。

结论

总之,我们得出结论,黄酮类化合物及其衍生物在作为新型抗炎候选药物的开发中已取得了有前景的结果,特别是当它们制成纳米颗粒时。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04fa/10567070/722ba9901e5e/ADMET-11-1918-g001.jpg

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