Synonym name:
Catalogue No.: BP1011
Cas No.: 80418-25-3
Formula: C₄₁H₇₀O₁₃
Mol Weight: 770.998
Botanical Source: Panax notoginseng (San qi)

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.

For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.

HPLC of Notoginsenoside R2

HNMR of Notoginsenoside R2

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Panax notoginseng, as a traditional Chinese medicinal herb, is widely used in the prevention and treatment of cardiovascular and cerebrovascular diseases due to its significant effects of promoting blood circulation, removing blood stasis, stopping bleeding, and anti-inflammatory. Sanqi saponins are the main active ingredients in Sanqi, with diverse pharmacological activities and good clinical application value. Notoginsenoside R2 (CAS number 80418-25-3), as one of the triterpenoid saponins, has received widespread attention in recent years due to its potential in cardiovascular protection. This article aims to systematically review the chemical structure, sources, pharmacological activity, mechanism of action, pharmacological evaluation, and clinical application prospects of Panax notoginseng saponin R2, providing theoretical basis for subsequent basic and clinical research.

Chemical structure and physicochemical properties

Sanqi saponin R2 belongs to the natural triterpenoid saponin class, with a molecular formula of C42H70O13 and a molecular weight of 770.9980. Its structural core is the pentacyclic triterpenoid parent nucleus, which connects multiple sugar groups to form a typical saponin structure. In terms of physical and chemical properties, the LogP value of Sanqi saponin R2 is 2.7013, indicating that it has moderate lipid solubility and is beneficial for cell membrane penetration. The polar surface area (TPSA) is 218.99, indicating high molecular polarity and low water solubility (0.0463), which may affect its oral absorption and bioavailability. The low permeability of the blood-brain barrier suggests limited exposure of the central nervous system. The negative result of hERG channel inhibition experiment indicates a low risk of cardiac toxicity. The Ames mutagenicity test showed a value of 0.0, indicating a low risk of genotoxicity and good safety.

Plant sources and extraction methods

Sanqi saponin R2 mainly exists in the roots and rhizomes of Sanqi. Sanqi is a plant of the Panax genus in the Araliaceae family, mainly distributed in Yunnan, Guangxi and other places in China. Traditional extraction methods typically use ethanol or methanol as solvents to obtain crude extracts through reflux extraction or ultrasound assisted extraction. Subsequently, liquid-liquid distribution, silica gel column chromatography, reverse phase high performance liquid chromatography (RP-HPLC) and other techniques were used for separation and purification, ultimately obtaining high-purity Sanqi saponin R2. Modern extraction processes are continuously optimized, such as supercritical CO2 extraction and membrane separation technology, aiming to improve extraction efficiency and purity and reduce production costs.

Pharmacological activity research

Sanqi saponin R2 has shown significant cardiovascular protective effects in multiple in vitro and in vivo experiments. Its main pharmacological effects include:

1. Anti ischemia-reperfusion injury Sanqi saponin R2 can reduce myocardial cell apoptosis, alleviate myocardial injury caused by ischemia-reperfusion, and improve cardiac function indicators.
2. anti-inflammatory effect: By inhibiting the expression of inflammatory factors, it can reduce the inflammatory reaction of vascular endothelial cells and alleviate the process of atherosclerosis.
3. Antioxidant effect Enhance endogenous antioxidant enzyme activity, eliminate free radicals, and protect the cardiovascular system from oxidative stress damage.
4. Vasodilation and improvement of blood flow Promote the production of nitric oxide (NO), improve endothelial function, and regulate blood pressure.
5. Antiplatelet aggregation and antithrombotic formation Inhibit platelet activating factor and reduce the risk of thrombosis.

In addition, Sanqi saponin R2 has shown potential in regulating lipid metabolism and improving myocardial energy metabolism, demonstrating its comprehensive therapeutic advantages of multi-target and multi mechanism.

Mechanism of action and molecular targets

The cardiovascular protective effect of Sanqi saponin R2 involves multiple molecular targets and signaling pathways, mainly including:

• SELP (Selective Element P)Sanqi saponin R2 downregulates SELP expression, inhibits platelet leukocyte adhesion, reduces inflammation and thrombosis.
• PPARG (Peroxisome proliferator activated receptor gamma)Activate the PPARG signaling pathway, regulate lipid metabolism, inhibit inflammation, and promote vascular repair.
• ACE (angiotensin converting enzyme)Inhibiting ACE activity, reducing angiotensin II production, exerting antihypertensive and anti myocardial remodeling effects.
• AKT1 (protein kinase B)Activate the AKT1 pathway, promote cell survival and proliferation, and inhibit cardiomyocyte apoptosis.
• ADRB2 (β 2 adrenergic receptor)Regulating myocardial contraction and vasodilation to improve cardiac function.
• KCNH2 (human cardiac potassium channel)Regulate cardiac electrical activity and reduce the risk of arrhythmia.
• NOS3 (endothelial nitric oxide synthase)Promote NO synthesis, improve endothelial function, and dilate blood vessels.
• ICAM1 and VCAM1 (cell adhesion molecules): Reduce its expression, reduce vascular inflammation and atherosclerosis.
• SLC8A1 (Sodium Calcium Exchange Protein)Regulating the calcium homeostasis of myocardial cells and protecting myocardial function.

The synergistic regulation of these targets constitutes the molecular basis for the multidimensional protection of the cardiovascular system by Sanqi Saponin R2.

Evaluation of drug properties and pharmacokinetics

The pharmacological evaluation of Sanqi saponin R2 shows that it has good safety and potential medicinal value. Its molecular weight is relatively large, polarity is high, and water solubility is poor, which may limit oral bioavailability. This suggests the need to improve pharmacokinetic properties through formulation optimization or structural modification. The low permeability of the blood-brain barrier reduces the risk of central nervous system side effects. The hERG channel has no inhibitory effect, reducing the drug safety hazards of arrhythmia. The Ames test is negative, indicating no significant mutagenicity.

Pharmacokinetic studies have shown that the absorption of Sanqi saponin R2 is slow after oral administration, and it is widely distributed in the body. It is mainly metabolized through the liver and excreted through bile and urine. Its half-life is moderate and suitable for daily administration. Further research on in vivo metabolic pathways, drug interactions, and long-term toxicology is needed in the future to provide a basis for clinical development.

Clinical application prospects and prospects

Based on the multi target and multi mechanism effects of Panax notoginseng saponin R2 in the field of cardiovascular protection, it has broad application prospects in the auxiliary treatment of coronary heart disease, myocardial ischemia, atherosclerosis, hypertension and other diseases. At present, Sanqi Saponin R2 is still in the basic and preclinical research stage, and future research needs to be strengthened in the following directions:

1. Clinical trial validation Design scientifically reasonable clinical trials to evaluate their efficacy, safety, and dosage regimen.
2. Formulation development Improve bioavailability and targeting through novel formulations such as nanocarriers and liposomes.
3. structural optimization Based on the drug efficacy toxicity relationship, optimize the molecular structure to enhance drug efficacy and pharmacokinetic performance.
4. Combination therapy research Explore synergistic effects with existing cardiovascular drugs to enhance treatment efficacy.
5. Multi domain expansion Given its anti-inflammatory and antioxidant effects, further exploration is needed to explore its potential in fields such as metabolic syndrome and neurodegenerative diseases.

Overall, Sanqi saponin R2, as a natural triterpenoid saponin compound, has significant potential as a new type of cardiovascular drug due to its unique pharmacological activity and good safety.

Conclusion

Sanqi saponin R2, as an important active ingredient in Sanqi, has shown significant application value in the field of cardiovascular protection due to its multi-target regulation and multiple pharmacological effects. Its good safety and pharmacological characteristics lay the foundation for clinical translation. In the future, through in-depth mechanism research, pharmacokinetic optimization, and clinical validation, it is expected to promote the development of Sanqi Saponin R2 as a new natural medicine for the prevention and treatment of cardiovascular diseases. Continuous interdisciplinary collaboration and innovative research will accelerate its transition from the laboratory to clinical practice, benefiting a wide range of patients.