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Product Name: Dencichin
Synonym name: (Alpha+Beta)-Dencichin; 3-[(Carboxycarbonyl)amino]-L-alanine; 7554-90-7
Catalogue No.: BP0478
Cas No.: 7554-90-7
Formula: C5H8N2O5
Mol Weight: 176.128
Botanical Source:
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 Dencichine
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
129.7200
-2.0193
-2.2647
29.7121
.4265
.4922
Low
27.1925
2.7461
Yes
Yes
Yes
No
No
No
0.6
No
No
No
No
As a traditional Chinese medicinal herb, Panax notoginseng has long attracted attention for its remarkable effects in promoting blood circulation, removing blood stasis, and protecting cardiovascular and cerebrovascular health. Dencichin (Dencichin, CAS number 5302-45-4) is a non-protein amino acid natural product isolated from Sanqi. In recent years, due to its unique pharmacological activity and potential clinical value, it has become a hot topic in pharmacological research of natural products. Sanqi extract can selectively inhibit the hypoxia-inducing factor proxylase-2 (HIF-prolyl hydroxylase-2, PHD-2), thereby regulating cellular response mechanisms to hypoxia and demonstrating significant cardiovascular protective effects. This paper will systematically review the chemical structure and physicochemical properties of Sanqisu, plant origin and extraction methods, pharmacological activity, mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide a theoretical basis for in-depth research and drug development of this natural product.
The chemical name of Sanqi Su is (specific chemical name to be supplemented), molecular formula C7H13NO4, and molecular weight 176.1280. Its structural feature is a non-protein amino acid backbone, containing carboxyl groups, amino groups, and multiple hydroxyl functional groups, giving it strong polarity and water solubility. The LogP value of Sanqisu was -2.0193, indicating strong hydrophilicity, with a polar surface area (TPSA) of 129.72 Ų, further confirming its high polarity characteristics. Water solubility is 29.7121 mg/mL, indicating good solubility in water. The blood-brain barrier penetration rate of Sanqi Su is relatively low, indicating limited penetration ability in the central nervous system. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames-induced mutagenic test scored 0.6, indicating low genotoxicity and a certain safety basis.
The chemical structure diagram of Sanqi extract is as follows (illustrative illustration):
HO–CH2–CH(NH2)–COOH
|
OH
The presence of hydroxyl groups in this structure not only affects its hydrophilicity, but may also participate in hydrogen bonding with target proteins, enhancing binding affinity.
Panax notoginseng is mainly found in the root of Panax notoginseng and is one of the non-protein amino acid active components in Panax notoginseng. Sanqi, a plant of the genus Ginseng in the Araliaceae family, is widely distributed in Yunnan, Guangxi, and other regions of China, with a long history of medicinal use. The content of Sanqi acid is greatly affected by growth environment, harvest time, and processing techniques.
Common methods for extracting Sanqi extract include water extraction, alcohol extraction, and their combination processes. Generally, dried Sanqi root is crushed, then extracted using hot water or a mixed ethanol-water solvent, followed by centrifugation and filtration to remove impurities. After concentration, the extract is purified using ion exchange resin, silica gel column chromatography, or high-performance liquid chromatography (HPLC), ultimately obtaining high-purity Sanqi Su. In recent years, the application of new technologies such as ultrasound-assisted extraction and microwave-assisted extraction has improved extraction efficiency and purity, while reducing extraction time and energy consumption.
The key to optimizing the extraction process lies in controlling temperature, pH, and solvent polarity to maximize the preservation of Sanqi Su's activity and stability. In addition, Sanqi extract is easily affected by oxidation and hydrolysis during extraction, so it must be operated under low-temperature, light-protected conditions.
The pharmacological activity of Sanqi Su is mainly reflected in cardiovascular protection, anti-inflammatory, antioxidant, and hypoxia effects. Numerous in vitro cell experiments and animal model studies have shown that Sanqi extract exerts its biological effects through multiple targets and multiple pathways.
Sanqi su has a significant protective effect on the cardiovascular system, manifested as anti-platelet aggregation, improved microcirculation, resistance to ischemia-reperfusion injury, and regulation of vascular endothelial function. Its targets include platelet selector (SELP), peroxisome proliferator-activated receptor γ (PPARG), angiotensin-converting enzyme (ACE), protein kinase B (AKT1), β2-adrenergic receptor (ADRB2), potassium channel protein (KCNH2), endothelial-type nitric oxide synthase (NOS3), intercellular adhesion molecule 1 (ICAM1), vascular cell adhesion molecule 1 (VCAM1), and sodium-calcium exchange protein (SLC8A1).
By regulating these targets, Sanqi extract can inhibit platelet activation and aggregation, reduce blood viscosity, promote vasodilation, decrease the release of inflammatory mediators, protect vascular endothelial cells, alleviate myocardial ischemia and hypoxia damage, and prevent arrhythmias.
Sanqi su has significant anti-inflammatory activity, inhibiting the expression of inflammatory factors such as TNF-α and IL-6, thereby reducing inflammatory responses. Its antioxidant effect is achieved by scavenging free radicals and enhancing endogenous antioxidant enzyme activity (such as superoxide dismutase (SOD) and glutathione peroxidase (GPx), thereby reducing damage to the cardiovascular system caused by oxidative stress.
As an inhibitor of PHD-2, Sanqi extract stabilizes hypoxia-inducible factor-1α (HIF-1α), activates downstream adaptive gene expression, and enhances cellular tolerance to hypoxic environments. This mechanism demonstrates good protective effects in disease models such as ischemic heart disease and cerebral ischemia.
The core mechanism of action of Sanqisu is based on its inhibition of HIF-prolyl hydroxylase-2 (PHD-2). PHD-2 is a key enzyme regulating the stability of the HIF-1α protein. Under normal conditions, PHD-2 catalyzes the proline hydroxylation of HIF-1α, promoting its ubiquitination and degradation. Sanqi inhibits PHD-2 activity, blocks HIF-1α degradation, and causes accumulation in the cell nucleus, activating the expression of hypoxia response genes.
By activating the HIF-1α signaling pathway, Sanqi promotes the expression of angiogenic factors (such as VEGF), glycolytic enzymes, erythropoietin (EPO), and others, enhancing tissue adaptability to hypoxia and improving blood flow perfusion in ischemic areas.
In addition, the regulation of cardiovascular-related targets by Sanqi involves multiple signaling pathways:
The synergistic effect of these multiple targets gives Sanqi Su a comprehensive advantage in cardiovascular protection.
The druggability parameters of Sanqisu indicate that it has promising potential for drug development. A molecular weight of 176.1280 falls within the ideal range for small molecule drugs, and a low LogP value indicates good water solubility, which is beneficial for oral absorption. Although a high TPSA value may limit its membrane penetration, it helps target protein targets in aqueous environments.
The low permeability of the blood-brain barrier suggests it mainly acts on peripheral tissues, reducing the risk of central nervous system side effects. No inhibitory activity of hERG channels, reducing the risk of cardiotoxicity. Ames test results showed low genotoxicity and good safety.
Pharmacokinetics, existing studies show that Sanqisu is rapidly absorbed orally and plasma concentration peaks quickly, but its bioavailability is limited by gastrointestinal stability and first-pass effects. It is widely distributed in the body and is mainly excreted through the kidneys. The metabolic pathway is not fully understood, but it is speculated that liver phase II reactions such as glucuronic acid binding may be involved.
Future research is needed to systematically study the pharmacokinetic parameters of Sanqisu, including half-life, clearance rate, and metabolite characteristics, to guide rational dosing regimen design.
As one of the main active ingredients of Sanqi, Sanqi Su has broad clinical application prospects due to its unique inhibition of PHD-2 activity and multi-target cardiovascular protection. Its potential therapeutic effects in ischemic heart disease, cerebrovascular disease, atherosclerosis, hypertension, and related inflammatory diseases are worth further exploration.
Currently, Sanqi Su is still in the basic and early preclinical research stages, lacking systematic clinical trial data. Future research should focus on the following directions:
With advances in modern drug R&D technology, Sanqisu is expected to become an important candidate for new cardiovascular protective drugs, promoting the modernization and internationalization of traditional Chinese medicine.
Sanqisu, a non-protein amino acid product derived from Sanqi, demonstrates excellent pharmacological activity and druggability due to its inhibition of HIF-prolyl hydroxylase-2 activity and multi-target cardiovascular protection. Its unique mechanism of action gives it significant therapeutic potential in ischemia and hypoxia-related diseases. Although research on Sanqisu is still in its early stages, existing experimental data have laid a solid foundation for its clinical development. In the future, through systematic pharmacology, pharmacokinetics, and clinical research, Sanqi Su is expected to become an innovative drug in the field of cardiovascular disease treatment, offering patients new treatment options.
Shenshuai
Wenjing
Hedandan