基于透皮成分组的地的米皮质抗银屑病药效学物质基础。

IF 5.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Zhaoyu Wang, Mengting Pi, Ziang Gao, Maobo Du, Liwei Gu, Shuzhi Liu, Shuo Shen
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引用次数: 0

摘要

背景:银屑病是一种慢性炎症性皮肤病,局部药物治疗是首选的治疗方案。然而,目前的治疗受到不良反应、耐药性和经济负担的限制。地黄皮(DC; Dictamnus dasycarpus Turcz.的根皮)在治疗银屑病方面有着悠久的历史,其透皮生物活性成分是局部抗银屑病治疗的药效学基础。方法:在分离金银桃化学成分的基础上,结合超高效液相色谱-四极杆飞行时间质谱(UPLC-Q-TOF-MS)和网络药理学,结合活性验证,研究金银桃透皮成分中抗银屑病的有效成分。结果:经鉴定的化学成分有41种,其中透皮性化合物26种,以生物碱和柠檬素为主。网络药理学分析揭示了核心靶点,包括MMP9和TLR4,以及与炎症和免疫反应相关的多种途径。分子对接研究发现,双胺明、姜甘莫内酯、芦黄素和其他关键的透皮成分对核心靶点表现出高度的结合亲和力。体外验证表明,这些化合物显著抑制银屑病样HaCaT细胞增殖(p < 0.05),下调Ki67 mRNA表达(p < 0.05)。同时,它们显著降低了IL-17A、IL-22、IL-1β、IL-6和IL-8等关键促炎因子的分泌(p < 0.05)。综合比较分析证实,双胺明具有理想的抗银屑病疗效。结论:本研究结果为开发治疗银屑病的DC外用制剂提供了药理物质基础,为探索中药外用药物的药效学物质基础提供了新的研究思路。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Anti-Psoriatic Pharmacodynamic Material Basis of Dictamni Cortex Based on Transdermal Constituents Group.

Background: Psoriasis is a chronic inflammatory skin disorder for which topical medications are the preferred treatment option. However, current therapies are limited by adverse reactions, drug resistance, and economic burdens. Dictamni Cortex (DC; the root bark of Dictamnus dasycarpus Turcz.) has a long history in the treatment of psoriasis, with its transdermal bioactive constituents serving as the pharmacodynamic foundation for topical anti-psoriatic therapy. Methods: Building on the separation of DC's chemical constituents, this study integrated ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and network pharmacology, along with activity verification, to investigate the anti-psoriatic active components among the transdermal constituents of DC. Results: Forty-one chemical constituents were characterized in DC, including 26 transdermally permeable compounds, predominantly alkaloids and limonoids. Network pharmacological analysis revealed core targets, including MMP9 and TLR4, as well as multiple pathways related to inflammatory and immune responses. Molecular docking studies identified dictamnine, jangomolide, rutaevin, and other key transdermal constituents that exhibited high binding affinity to core targets. In vitro validation showed that these compounds significantly suppressed cellular proliferation (p < 0.05) and downregulated Ki67 mRNA expression (p < 0.05) in the psoriasis-like HaCaT cell model. Concurrently, they significantly reduced secretion of key pro-inflammatory cytokines, including IL-17A, IL-22, IL-1β, IL-6, and IL-8 (p < 0.05). Comprehensive comparative analyses confirmed that dictamnine exhibited ideal anti-psoriatic efficacy. Conclusions: These results provide a pharmacological substance basis for the development of external preparations of DC for treating psoriasis and provide novel research concepts for investigating the pharmacodynamic material basis of Traditional Chinese Medicine topical drugs.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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