School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, PR China.
Tianjin University of Science and Technology, Tianjin, PR China.
Biomed Pharmacother. 2021 Jul;139:111630. doi: 10.1016/j.biopha.2021.111630. Epub 2021 May 1.
Cardiac fibrosis occurs in ischemic and non-ischemic heart failure, hereditary cardiomyopathy, diabetes and aging. Energy metabolism, which serves a crucial function in the course and treatment of cardiovascular diseases, might have therapeutic benefits for myocardial fibrosis. Ginsenoside Rb3 (G-Rb3) is one of the main components of Ginseng and exhibits poor oral bioavailability but still exerts regulate energy metabolism effects in some diseases. Therefore, the study investigated the effect of chitosan (CS) @ sodium tripolyphosphate (TPP) nanoparticles conjugation with ginsenoside Rb3 (NpRb3) on myocardial fibrosis and studied its possible mechanisms. The results showed that NpRb3 directly participates in the remodeling of myocardial energy metabolism and the regulation of perixisome proliferation-activated receptor alpha (PPARα), thereby improving the degree of myocardial fibrosis. The study also verifies the protective effect of NpRb3 on energy metabolism and mitochondrial function by targeting the PPARα pathway. Therefore, the prepared nanodrug carrier may be a potential solution for the delivery of G-Rb3, which is a promising platform for oral treatment of myocardial fibrosis.
心脏纤维化发生于缺血性和非缺血性心力衰竭、遗传性心肌病、糖尿病和衰老中。能量代谢在心血管疾病的发生和治疗中起着至关重要的作用，可能对心肌纤维化具有治疗益处。人参皂苷 Rb3（G-Rb3）是人参的主要成分之一，口服生物利用度差，但在某些疾病中仍能发挥调节能量代谢的作用。因此，本研究探讨了壳聚糖（CS）@三聚磷酸钠（TPP）纳米粒子与人参皂苷 Rb3 缀合物（NpRb3）对心肌纤维化的影响，并研究了其可能的机制。结果表明，NpRb3 直接参与心肌能量代谢的重塑和过氧化物酶体增殖物激活受体α（PPARα）的调节，从而改善心肌纤维化程度。该研究还通过靶向过氧化物酶体增殖物激活受体α（PPARα）通路验证了 NpRb3 对能量代谢和线粒体功能的保护作用。因此，所制备的纳米药物载体可能是 G-Rb3 递药的一种有前途的解决方案，为口服治疗心肌纤维化提供了一个有前景的平台。
