Notoginsenoside R1 is a major active saponin component isolated from Panax notoginseng and is a key bioactive compound in many traditional Chinese medicine formulations[1]. Notoginsenoside R1 can improve the recovery of neurological function following cerebral ischemia-reperfusion injury[2]. Notoginsenoside R1 can be used to study its protective effects on vascular endothelial cells and nerve cells[3]. Notoginsenoside R1 also has potential pharmacological activities in improving cardiac repair after myocardial infarction, alleviating cognitive deficits in a diabetes-induced Alzheimer's disease model, and regulating glucose and lipid metabolism[4].
In vitro, treatment of hepatocellular carcinoma cell lines HepG2 and MHCC97H with Notoginsenoside R1 (0-150μM) for 72 hours significantly reduced cell viability and induced an increase in caspase-3 activity, indicating Notoginsenoside R1 promotion of tumor cell apoptosis[5]. Pretreatment of H9C2 cardiomyocytes and primary cardiomyocytes with Notoginsenoside R1 (100μM) for 30 minutes, followed by treatment with H₂O₂ (350μM) or oxygen-glucose deprivation (OGD), significantly inhibited the accumulation of reactive oxygen species (ROS) and mitochondrial superoxide generation, while also reducing cell apoptosis[6].
In vivo, oral pretreatment of neonatal rats with Notoginsenoside R1 (12.5-50mg/kg) from postnatal day 2 to day 7, followed by exposure to 3% sevoflurane for 6 hours, significantly reduced neuronal apoptosis in the CA1, CA3, and DG regions of the hippocampus[7]. Intraperitoneal injection of Notoginsenoside R1 (25mg/kg) 30 minutes before myocardial ischemia (every 2 hours; a total of 3 times) significantly reduced the myocardial infarction area and decreased the levels of plasma myocardial injury markers cTnI and CK-MB[8].
References:
[1] Guo S, Xi X, Li J. Notoginsenoside R1: A systematic review of its pharmacological properties. Pharmazie. 2019 Nov 1;74(11):641-647.
[2] Tong Q, Zhu PC, Zhuang Z, et al. Notoginsenoside R1 for Organs Ischemia/Reperfusion Injury: A Preclinical Systematic Review. Front Pharmacol. 2019 Oct 17;10:1204.
[3] Zhu T, Xie WJ, Wang L, et al. Notoginsenoside R1 activates the NAMPT-NAD+-SIRT1 cascade to promote postischemic angiogenesis by modulating Notch signaling. Biomed Pharmacother. 2021 Aug;140:111693.
[4] Wen C, Liao X, Ye X, et al. Pharmacokinetics and Biological Activities of Notoginsenoside R1: A Systematical Review. Am J Chin Med. 2025;53(1):205-249.
[5] Li H, Zhu J, Xu YW, et al. Notoginsenoside R1-loaded mesoporous silica nanoparticles targeting the site of injury through inflammatory cells improves heart repair after myocardial infarction. Redox Biol. 2022 Aug;54:102384.
[6] Li H, Zhu J, Xu YW, et al. Notoginsenoside R1-loaded mesoporous silica nanoparticles targeting the site of injury through inflammatory cells improves heart repair after myocardial infarction. Redox Biol. 2022 Aug;54:10238.
[7] Zhang Y, Zhao Y, Ran Y, et al. Notoginsenoside R1 attenuates sevoflurane-induced neurotoxicity. Transl Neurosci. 2020 Jun 22;11(1):215-226.
[8] Zeng JJ, Shi HQ, Ren FF, et al. Notoginsenoside R1 protects against myocardial ischemia/reperfusion injury in mice via suppressing TAK1-JNK/p38 signaling. Acta Pharmacol Sin. 2023 Jul;44(7):1366-1379.
Notoginsenoside R1一种从Panax notoginseng中分离得到的主要活性皂苷成分，是多种中药制剂的关键生物活性化合物[1]。Notoginsenoside R1可改善脑缺血再灌注损伤后的神经功能恢复[2]。Notoginsenoside R1可用于研究其对血管内皮细胞和神经细胞的保护作用[3]。Notoginsenoside R1还具有改善心肌梗死后的心脏修复、减轻糖尿病阿尔茨海默病模型中的认知缺陷以及调节糖脂代谢的潜在药理活性[4]。
在体外，Notoginsenoside R1（0-150μM）处理肝癌细胞系HepG2和MHCC97H 72小时，显著降低细胞活力并诱导caspase-3活性升高，表明其促进肿瘤细胞凋亡[5]。Notoginsenoside R1（100μM）预处理H9C2心肌细胞及原代心肌细胞30分钟，随后以H₂O₂（350μM）或氧糖剥夺（OGD）处理，显著抑制活性氧（ROS）积累和线粒体超氧化物生成，同时减少细胞凋亡[6]。
在体内，Notoginsenoside R1（12.5-50mg/kg）从出生后第2天至第7天口服预处理新生大鼠，随后以3%七氟醚暴露6小时，Notoginsenoside R1显著减轻海马CA1、CA3和DG区域的神经元凋亡[7]。Notoginsenoside R1（25mg/kg）于心肌缺血前30分钟开始腹腔注射（每2小时一次；共3次），Notoginsenoside R1显著降低心肌梗死面积，并降低血浆心肌损伤标志物cTnI和CK-MB水平[8]。