Notoginsenoside R1 (NR1), the main bioactive component in panaxnotoginseng, is reported to have some neuronal protective, antihypertensive effects. NR1 significantly reduce blood pressure in SHR (spontaneously hypertensive rats) and induce nitric oxide (NO) generation through increasing the phosphorylation of iNOS (inducible nitric oxide synthase) [3]. R1 is a novel cardioprotective agent that can attenuate adverse cardiac dysfunction, hypertrophy, and associated disorders, such as fibrosis. R1-supressed cardiac dysfunction, atherosclerotic lesions, and inflammatory cytokine accumulation in the myocardium can be partially inhibited by CCR2 (CC chemokine receptor 2) translation in bone marrow cells[4]. In addition, retinal vascular degeneration, reduced retinal thickness, and impaired retinal function in db/db mice were all dramatically attenuated by oral treatment with NGR1 (30 mg/kg) for 12 weeks. NGR1 pretreatment also significantly inhibited apoptosis, markedly suppressed the VEGF expression, markedly increased PEDF expression and markedly inhibited oxidative stress and inflammation in rat retinal Müller cells (rMC-1) subjected to high glucose (HG) and in the retinas of db/db mice[5].
Notoginsenoside R1/三七皂甙 R1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Adult primary cardiomyocytes
100 μmol/L
NGR1 reduced H2O2-induced apoptosis in adult primary cardiomyocytes, enhanced cell viability, and reduced mitochondrial ROS accumulation.
Redox Biol. 2022 Aug;54:102384.
Primary cardiomyocytes
100 μmol/L
NGR1 protected primary cardiomyocytes from H2O2 and OGD-induced oxidative stress injury and reduced apoptosis.
Redox Biol. 2022 Aug;54:102384.
H9C2 cells
100 μmol/L
30 minutes
NGR1 protected H9C2 cells from H2O2-induced oxidative stress injury, reduced apoptosis, decreased ROS levels, increased SOD activity, and reduced mitochondrial ROS accumulation and oxidative DNA damage.
Redox Biol. 2022 Aug;54:102384.
U87 cells
100 μM and 200 μM
24 hours
To evaluate the effect of NGR1 on U87 cell viability, results showed that NGR1 significantly inhibited U87 cell viability.
Neuro Oncol. 2024 Aug 5;26(8):1438-1452.
LN18 cells
100 μM and 200 μM
24 hours
To evaluate the effect of NGR1 on LN18 cell viability, results showed that NGR1 significantly inhibited LN18 cell viability.
Neuro Oncol. 2024 Aug 5;26(8):1438-1452.
Bone marrow mesenchymal stem cells (MSCs)
0.1 µM, 1 µM, 10 µM, 100 µM
24 hours, 48 hours, 72 hours
Promoted MSC proliferation and protected MSCs against H2O2-induced apoptosis
Stem Cell Res Ther. 2024 Nov 13;15(1):419.
Murine neonatal cardiomyocytes (CMs)
25 μM
24 hours
To evaluate the protective effect of NG-R1 on hypoxia/reoxygenation-induced apoptosis. Results showed that NG-R1 significantly inhibited apoptosis, reduced LDH release, and improved cell viability.
Acta Pharmacol Sin. 2023 Jul;44(7):1366-1379.
3D intestinal organoid model
100 μM
4 days
Increased Lgr5+ cells and budding rates
Acta Pharmacol Sin. 2024 Jul;45(7):1451-1465.
NCM460 human intestinal epithelial cells
100 μM
24 hours
Promoted wound healing and reduced cell apoptosis
Acta Pharmacol Sin. 2024 Jul;45(7):1451-1465.
MDA-MB-231 cells
75-150 mmol/L
24 hours
Inhibited proliferation, migration, and invasion in MDA-MB-231 cells
Chin Med J (Engl). 2021 Jan 20;134(5):546-554.
MCF-7 cells
148.9 mmol/L
24 hours
Inhibited proliferation, migration, invasion, and angiogenesis, and promoted cell cycle arrest and apoptosis in MCF-7 cells
Chin Med J (Engl). 2021 Jan 20;134(5):546-554.
Notoginsenoside R1/三七皂甙 R1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57/BL6 mice
Myocardial ischemia/reperfusion injury model
Intraperitoneal injection
25 mg/kg
Every 2 hours for a total of 3 times, starting 30 minutes before ischemic surgery
To evaluate the protective effect of NG-R1 on myocardial ischemia/reperfusion injury. Results showed that NG-R1 significantly reduced myocardial infarction area, alleviated myocardial cell damage, and improved cardiac function.
Acta Pharmacol Sin. 2023 Jul;44(7):1366-1379.
C57BL/6 mice
Myocardial infarction model
Caudal vein injection
267 ng/kg MSN-NGR1
Single dose
MSN-NGR1-CD11b antibody nanoparticles improved cardiac function after myocardial infarction by enhancing the activation of AKT and MAPK signaling pathways and the nuclear translocation of YAP, reducing infarct size and collagen deposition, promoting angiogenesis, and regulating macrophage phenotype and inflammatory factors.
Redox Biol. 2022 Aug;54:102384.
C57BL/6 mice
DSS-induced colitis model
Oral
25, 50, 125 mg/kg/d
Once per day for 10 days
Dose-dependently ameliorated mucosal inflammation and enhanced epithelial repair evidenced by increased tight junction proteins, mucus production and reduced permeability in colitis mice
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