文献类型：期刊文献

中文题名：藁本内酯治疗运动系统疾病的作用机制及药代动力学研究进展

英文题名：Research progress on mechanisms and pharmacokinetics of ligustilide in treatment of locomotor system diseases

作者：朱芙琴[1];马佳怡[1];张圆圆[1];余琰[1]

第一作者：朱芙琴

机构：[1]甘肃中医药大学,甘肃兰州730000

第一机构：甘肃中医药大学

年份：2024

卷号：49

期号：24

起止页码：6625

中文期刊名：中国中药杂志

外文期刊名：China Journal of Chinese Materia Medica

收录：;北大核心:【北大核心2023】；CSCD:【CSCD2023_2024】；

基金：甘肃省自然科学基金项目(23JRRA1715)。

语种：中文

中文关键词：藁本内酯;药理作用;运动系统疾病;药代动力学

外文关键词：ligustilide;pharmacological effects;locomotor system disease;pharmacokinetics

摘要：藁本内酯是从伞形科植物当归、川芎中提取出来的一种苯酞类化合物,已被证实具有抗炎、抗肿瘤、抗动脉粥样硬化、抗缺血性脑卒中损伤、抗阿尔茨海默病等多种药理活性。近年来,其在治疗运动系统疾病方面显示出巨大潜力。研究显示藁本内酯对多种运动系统疾病,包括骨质疏松症、骨关节炎、股骨头坏死、骨肉瘤、肌肉衰老损伤等具有显著治疗作用。其作用机制包括增强造骨细胞(OBs)分化能力,抑制破骨细胞(OCs)生成能力、下调炎症因子、促进细胞外基质(ECM)合成、改善股骨头局部供血、平衡脂质代谢、抑制骨肉瘤细胞增殖迁移,诱导周期阻滞、加强骨骼肌对糖的利用、调控细胞自噬和凋亡等。但其结构不稳定、水溶性差、生物利用度低等缺陷严重限制其临床应用,目前借助制剂手段,如滴丸、微丸、包合物、脂质体等,改善了其稳定性和水溶性,提高了药物疗效。该文通过对近年来国内外藁本内酯治疗运动系统疾病的作用、作用机制及其单体和制剂的药代动力学研究进行归纳总结,以期为藁本内酯在治疗运动系统疾病方面的进一步开发应用提供参考和指导。
Ligustilide, a phthalide compound extracted from Umbelliferae plants such as Angelica sinensis and Ligusticum chuanxiong, has been proven to possess various pharmacological activities, such as anti-inflammatory, anti-tumor, anti-atherosclerosis, anti-ischemic stroke injury, and anti-Alzheimer′s disease properties. In recent years, it has shown great potential, particularly in the treatment of locomotor system diseases. Studies have shown that ligustilide has significant therapeutic effects on various locomotor system diseases, including osteoporosis, osteoarthritis, femoral head necrosis, osteosarcoma, and muscle aging and injury. Its mechanisms of action include enhancing the differentiation ability of osteoblasts(OBs), inhibiting the formation ability of osteoclasts(OCs), downregulating inflammatory factors, promoting the synthesis of extracellular matrix(ECM), improving local blood supply to the femoral head, balancing lipid metabolism, inhibiting the proliferation and migration of osteosarcoma cells, inducing cell cycle arrest, enhancing glucose utilization in skeletal muscle, and regulating autophagy and apoptosis. However, its clinical application is severely limited by drawbacks such as structural instability, poor water solubility, and low bioavailability. Currently, formulation techniques such as dripping pills, micropills, inclusion complexes, and liposomes are being used to improve its stability and water solubility, thereby enhancing its therapeutic efficacy. This article summarized the effects, mechanisms of action, and pharmacokinetics of ligustilide monomers and preparations in the treatment of locomotor system diseases in China and abroad in recent years, aiming to provide reference and guidance for further development and application of ligustilide in this field.