Research Progress of Triptolide Against Fibrosis

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL

Drug Design, Development and Therapy Pub Date : 2024-07-25 DOI:10.2147/dddt.s467929

Minmin Jiang, Yongxia Xie, Ping Wang, Mengyu Du, Ying Wang, Shuxun Yan

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引用次数: 0

Abstract

Abstract: Fibrosis leads to organ failure and death, which is the final stage of many chronic diseases. Triptolide (TPL) is a terpenoid extracted from the traditional Chinese medicine Tripterygium wilfordii Hook. F (TwHF). Triptolide and its derivatives (Omtriptolide, Minnelide, (5R)-5-hydroxytriptolide) have been proven to have a variety of pharmacological effects. This study comprehensively reviewed the antifibrotic mechanism of TPL and its derivatives, and discussed the application of advanced nanoparticles (NPs) drug delivery system in the treatment of fibrotic diseases by TPL. The results show that TPL can inhibit immune inflammatory response, relieve oxidative stress and endoplasmic reticulum stress (ERS), regulate collagen deposition and inhibit myofibroblast production to play an anti-fibrosis effect and reduce organ injury. A low dose of TPL has no obvious toxicity. Under pathological conditions, a toxic dose of TPL has a protective effect on organs. The emergence of TPL derivatives (especially Minnelide) and NPs drug delivery systems promotes the anti-fibrosis effect of TPL and reduces its toxicity, which may be the main direction of anti-fibrosis research in the future.

Keywords: triptolide, derivatives, anti-fibrosis, nanoparticles

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曲托列特抗纤维化的研究进展

摘要：纤维化导致器官衰竭和死亡，是许多慢性疾病的最后阶段。Triptolide（TPL）是从传统中药Tripterygium wilfordii Hook.F（TwHF）中提取的一种萜类化合物。经证实，曲托内酯及其衍生物（奥曲托内酯、明内酯、（5R）-5-羟基曲托内酯）具有多种药理作用。本研究全面综述了TPL及其衍生物的抗纤维化机理，探讨了先进的纳米颗粒（NPs）给药系统在TPL治疗纤维化疾病中的应用。结果表明，TPL能抑制免疫炎症反应、缓解氧化应激和内质网应激（ERS）、调节胶原沉积和抑制肌成纤维细胞生成，从而起到抗纤维化和减轻器官损伤的作用。小剂量 TPL 无明显毒性。在病理条件下，毒性剂量的 TPL 对器官有保护作用。三苯氧胺衍生物（尤其是明奈里德）和纳米粒子给药系统的出现，促进了三苯氧胺抗纤维化作用的发挥，降低了其毒性，可能是今后抗纤维化研究的主要方向。

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来源期刊

Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

9.00

自引率

0.00%

发文量

382

审稿时长

>12 weeks

期刊介绍： Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.