过氧化物酶体增殖物激活受体配体与纳米颗粒技术在代谢性脂肪性肝炎治疗中的应用
Application of PPAR Ligands and Nanoparticle Technology in Metabolic Steatohepatitis Treatment.
作者信息
Vu Hung Thai, Nguyen Vien Duc, Ikenaga Hiroko, Matsubara Tsutomu
机构信息
Department of Anatomy and Regenerative Biology, Graduate School of Medicine, Osaka Metropolitan University, Osaka 545-8585, Osaka, Japan.
Department of Hepatology, Graduate School of Medicine, Osaka Metropolitan University, Osaka 545-8585, Osaka, Japan.
出版信息
Biomedicines. 2024 Aug 16;12(8):1876. doi: 10.3390/biomedicines12081876.
Metabolic dysfunction-associated steatotic liver disease/steatohepatitis (MASLD/MASH) is a major disease worldwide whose effective treatment is challenging. Peroxisome proliferator-activated receptors (PPARs) belong to the nuclear receptor superfamily and function as ligand-activated transcription factors. To date, three distinct subtypes of PPARs have been characterized: PPARα, PPARβ/δ, and PPARγ. PPARα and PPARγ are crucial regulators of lipid metabolism that modulate the transcription of genes involved in fatty acid (FA), bile acid, and cholesterol metabolism. Many PPAR agonists, including natural (FAs, eicosanoids, and phospholipids) and synthetic (fibrate, thiazolidinedione, glitazar, and elafibranor) agonists, have been developed. Furthermore, recent advancements in nanoparticles (NPs) have led to the development of new strategies for MASLD/MASH therapy. This review discusses the applications of specific cell-targeted NPs and highlights the potential of PPARα- and PPARγ-targeted NP drug delivery systems for MASLD/MASH treatment.
代谢功能障碍相关脂肪性肝病/脂肪性肝炎(MASLD/MASH)是一种全球性的主要疾病,其有效治疗具有挑战性。过氧化物酶体增殖物激活受体(PPARs)属于核受体超家族,作为配体激活的转录因子发挥作用。迄今为止,已鉴定出三种不同的PPAR亚型:PPARα、PPARβ/δ和PPARγ。PPARα和PPARγ是脂质代谢的关键调节因子,可调节参与脂肪酸(FA)、胆汁酸和胆固醇代谢的基因转录。已经开发了许多PPAR激动剂,包括天然(FA、类花生酸和磷脂)和合成(贝特类、噻唑烷二酮类、格列他唑和依拉非尼)激动剂。此外,纳米颗粒(NPs)的最新进展带来了MASLD/MASH治疗新策略的发展。本综述讨论了特定细胞靶向NPs的应用,并强调了PPARα和PPARγ靶向NP药物递送系统在MASLD/MASH治疗中的潜力。