Key Laboratory of Drug Target Research and Drug Screen, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2A Nan Wei Road, Beijing, 100050, China.
Shandong Province Key Laboratory of Polymorph Drugs, Shandong Yikang Pharmaceutical Co. Ltd, No. 3288, Yikang Avenue, Tengzhou, 277513, China.
Sci Rep. 2020 Oct 20;10(1):17787. doi: 10.1038/s41598-020-74246-y.
Puerarin has shown unique pharmacological effects on myocardial ischemia (MI). Changing the crystal form is an effective approach to improve the cardioprotective effects of puerarin. However, the mechanisms of the new crystal form of puerarin are unclear. In this study, an electrocardiogram, echocardiography, cardiac marker enzymatic activity, oxidative stress indices, and myocardial histology analysis of cardiac tissues were performed to evaluate the cardioprotective effects of the new crystal form of puerarin. Moreover, serum and cardiac tissue metabolomics based on nuclear magnetic resonance (NMR) were used to investigate the potential mechanism of the new crystal form. The results indicated that the new crystal form of puerarin (30 mg/kg) could improve oxidative stress indices, and these improvements were similar to those of the original crystal form of puerarin (120 mg/kg). The new crystal form of puerarin (30 mg/kg) could effectively improve the activities of cardiac marker enzymes, and the improvement effects were better than those of the original crystal form (120 mg/kg). Moreover, metabolomics analysis showed that amino acid metabolism, oxidative stress and energy metabolism were disturbed after MI and could be improved by puerarin. These results demonstrated that the new crystal form of puerarin was effective in treating MI.
葛根素对心肌缺血(MI)具有独特的药理作用。改变晶体形式是提高葛根素心脏保护作用的有效途径。然而,新葛根素晶体形式的机制尚不清楚。在这项研究中,通过心电图、超声心动图、心肌标志物酶活性、氧化应激指标和心肌组织学分析来评估新葛根素晶体形式的心脏保护作用。此外,还基于核磁共振(NMR)进行血清和心肌组织代谢组学研究,以探讨新晶体形式的潜在机制。结果表明,新葛根素晶体形式(30mg/kg)可改善氧化应激指标,其改善作用与原葛根素晶体形式(120mg/kg)相似。新葛根素晶体形式(30mg/kg)可有效改善心肌标志物酶的活性,改善效果优于原晶体形式(120mg/kg)。此外,代谢组学分析表明,MI 后氨基酸代谢、氧化应激和能量代谢受到干扰,葛根素可改善这些代谢紊乱。这些结果表明新葛根素晶体形式在治疗 MI 方面是有效的。