Product name: Magnesium Salvianolate B
Synonym name: Magnesium lithospermate B; 154334-65-3
Catalogue No.: BP1529
Cas No.: 122021-74-3
Formula: C₃₆H₂₈MgO₁₆
Mol Weight: 740.909
Botanical Source:
Physical Description: Powder
Type of Compound: Phenylpropanoids

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
The product could be supplied from milligrams to grams. Inquire for bulk scale.
We provide solution to improve the water-solubility of compounds, thereby facilitating the variety of activity tests and clinic uses.

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

HPLC of Magnesium Salvianolate B

HNMR of Magnesium Salvianolate B

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

Introduction/Overview

Cardiovascular disease (CVD) is the leading cause of death and disability worldwide, with a complex pathogenesis involving multiple pathophysiological processes such as oxidative stress, inflammatory response, cell apoptosis, metabolic disorders, and endothelial dysfunction. Although modern medicine has made significant progress in the prevention and treatment of CVD, existing drugs still have problems such as side effects, drug resistance, and difficulty in fully intervening in multi-target therapy. Therefore, discovering efficient, multi-target, and low toxicity natural products from the treasure trove of traditional medicine has become an important strategy for new drug development. Danshen (Salvia miltiorrhiza)（Salvia miltiorrhiza Bunge, as a classic Chinese medicine for promoting blood circulation, removing blood stasis, and relieving pain, is considered one of the core substances that exert cardiovascular protective effects due to its water-soluble phenolic acid components. Salvianolic acid B (Sal B) is the most abundant and active representative component among them. However, the poor stability and low oral bioavailability of salvianolic acid B itself limit its clinical application. Magnesium Salvianolate B, as a magnesium ion chelate of salvianolic acid B, not only improves the stability and solubility of the original compound, but also exhibits unique and powerful pharmacological activity in multiple studies. This article aims to systematically review the chemical properties, pharmacological effects, molecular mechanisms, and pharmacological properties of magnesium salt of salvianolic acid B, providing scientific basis for its deep development and clinical application.

Chemical structure and physicochemical properties

Danshensu B magnesium salt (CAS number: 122021-74-3) is a salt formed by Danshensu B and magnesium ions. Danshensu B itself is a polyphenolic acid compound composed of three molecules of danshensu and one molecule of caffeic acid connected by ester bonds. Its magnesium salt form has a molecular weight of 718.6200. This structure endows the molecule with abundant phenolic hydroxyl and carboxyl groups, resulting in a theoretical topological polar surface area (TPSA) of up to 278.0400 Å ², which explains its relatively hydrophilic properties. The calculated LogP value is 2.4687, indicating that it has a certain degree of lipophilicity, but overall it still belongs to amphiphilic molecules. The experimentally measured water solubility is approximately 0.1268 mg/mL. Compared to salvianolic acid B, the formation of magnesium salt significantly improves its solubility and chemical stability in physiological environments, which is crucial for its formulation development and in vivo absorption. Preliminary predictions of its pharmacological properties indicate that its ability to penetrate the blood-brain barrier is relatively low, suggesting that its direct action may be limited, but this may not necessarily be a disadvantage for its main effect on the peripheral cardiovascular system. Importantly, its hERG inhibition risk prediction was negative ("no"), and the Ames test predicted a value of 0.0 (indicating no mutagenicity), providing preliminary favorable evidence for its cardiovascular safety.

Plant sources and extraction methods

The direct plant source of magnesium salt of salvianolic acid B is Danshen（Salvia miltiorrhiza Bunge's roots and rhizomes, commonly known as "Danshen". The extraction of water-soluble phenolic acid components in Danshen is mainly carried out by reflux extraction or percolation extraction using water or different concentrations of alcohols (such as ethanol and methanol). In industry, in order to enrich salvianolic acid B and prepare its magnesium salt, the following process route is usually adopted: first, the raw material of Danshen is extracted by water or alcohol, and the extract is filtered and concentrated. Then, it is enriched and purified through macroporous adsorption resin columns (such as AB-8, HPD-100, etc.), and eluted with water and different concentrations of ethanol gradient to collect the fraction rich in salvianolic acid B. Subsequently, an appropriate amount of soluble magnesium salts (such as magnesium chloride and magnesium sulfate) are added to the purified solution of salvianolic acid B. The reaction is carried out under specific pH and temperature conditions to combine salvianolic acid B with magnesium ions to form a precipitate or complex. After filtration, washing, drying, and other steps, crude salvianolic acid B magnesium salt can be obtained. Further refinement can be achieved through recrystallization or preparative chromatography techniques. This process not only achieves standardization of active ingredients, but also improves the physicochemical properties of raw materials through salt formation.

Pharmacological activity research

Numerous preclinical studies have confirmed that magnesium salt of salvianolic acid B has broad and powerful cardiovascular protection and other related pharmacological activities.

1. Cardioprotective effect In animal models of myocardial ischemia/reperfusion injury and doxorubicin induced cardiomyopathy, magnesium salvianolic acid B can significantly reduce myocardial infarction area, inhibit myocardial enzyme release, and improve cardiac function. Its function is closely related to reducing oxidative stress damage and inhibiting myocardial cell apoptosis.
2. Anti atherosclerosis This compound can inhibit the inflammatory response of endothelial cells, reduce monocyte adhesion and migration; Downregulate abnormal proliferation and migration of vascular smooth muscle cells; At the same time, it can regulate lipid metabolism and reduce the level of oxidized low-density lipoprotein, thus inhibiting the formation and development of atherosclerotic plaque in multiple links.
3. Improving endothelial function and anti thrombotic effects Danshensu B magnesium salt can promote the release of nitric oxide from endothelial cells, dilate blood vessels, and improve endothelial dependent vasodilation function. At the same time, it can inhibit platelet activation and aggregation, and regulate the fibrinolytic system (such as affecting SERPINE1/PAI-1), demonstrating potential for anti thrombotic effects.
4. anti-fibrotic In models of cardiac, vascular, and renal fibrosis, magnesium salvianolic acid B exhibits inhibitory effects on fibroblast activation and reduces extracellular matrix deposition, which helps to delay the progression of organ fibrosis.
5. Neuroprotective effect Although its blood-brain barrier permeability is low, some studies suggest that it may have indirect effects such as peripheral anti-inflammatory and antioxidant effects, or direct effects with trace amounts entering the brain, which may have a certain protective effect on cerebral ischemic injury and Alzheimer's disease models (involving BACE1 targets).
6. Other activities The study also suggests that it has certain value in improving insulin resistance (involving PTPN1, AKR1B1 targets) and potential anti-tumor adjuvant effects.

Mechanism of action and molecular targets

The multiple pharmacological activities of magnesium salt of salvianolic acid B stem from its diverse regulation of cellular signaling networks, and its mechanism of action involves multiple key molecular targets:

• Energy metabolism and cell survival regulator: AMPK (PRKAA1)Activation of AMPK is one of the core mechanisms of magnesium salvianolic acid B. As a cellular energy sensor, AMPK activation can promote fatty acid oxidation, glucose uptake, and improve myocardial energy metabolism; Simultaneously inhibiting mTOR and other pathways, reducing endoplasmic reticulum stress, and upregulating downstream anti apoptotic proteins such as Bcl-2 (targets)BCL2）To jointly promote the survival of cells under stress.
• Key Node of Inflammation and Stress Response: TLR4 Danshensu B magnesium salt can inhibit the overactivation of Toll like receptor 4 (TLR4) and its downstream NF - κ B signaling pathway, effectively reducing the production of pro-inflammatory factors such as tumor necrosis factor - α and interleukin-6. This is an important molecular basis for its anti-inflammatory, endothelial and myocardial protective effects.
• Regulator of oxidation-reduction and apoptosis Its rich phenolic hydroxyl structure makes it a powerful antioxidant, capable of directly scavenging reactive oxygen species. In addition, it can upregulate endogenous antioxidant systems (such as the Nrf2/HO-1 pathway). In the apoptotic pathway, in addition to regulating the AMPK-Bcl-2 axis, protein kinase C may also be regulated（PRKCA）Waiting for signaling molecules to inhibit the activation of mitochondrial apoptosis pathways.
• Metabolic disease-related targets Protein tyrosine phosphatase 1B（PTPN1）Inhibition helps to enhance insulin signaling sensitivity and improve glucose metabolism. Aldose reductase（AKR1B1）The inhibition of β - lactamase is helpful to reduce the stress of polyol pathway in the complications of diabetes.
• Other specific targets In the context of neurodegenerative diseases, it affects β - secretase activity（BACE1）Inhibition may reduce the production of β - amyloid protein. Compared with estrogen receptor β（ESR2）The interaction may mediate some vascular protective effects. Deopurine/Depyrimidine endonuclease 1（APEX1）The impact may involve DNA damage repair. And for plasminogen activator inhibitor-1（SERPINE1）If it is downregulated, it is directly related to its pro fibrinolysis and anti thrombotic activity.

In summary, magnesium salt of salvianolic acid B forms a synergistic network by simultaneously acting on multiple targets such as AMPK, TLR4, BCL2, PTPN1, etc., exerting cardiovascular protective effects from multiple dimensions including energy metabolism, inflammation, oxidation, apoptosis, fibrosis, etc.

Evaluation of drug properties and pharmacokinetics

Although the physicochemical properties of magnesium salt of salvianolic acid B have been improved compared to salvianolic acid B, it still faces challenges in terms of its medicinal properties as a polyphenolic acid compound.

• Absorption, distribution, metabolism, excretion (ADME)After oral administration, magnesium salt of salvianolic acid B may dissociate in the gastrointestinal tract, and its absorption mainly occurs in its prototype or metabolite form. Due to its high polarity and molecular weight, oral bioavailability is generally low. After absorption, it is mainly distributed in organs with abundant blood flow, such as the liver, kidneys, lungs, and heart, but the amount that enters the central nervous system through the blood-brain barrier is very small. In the body, it is prone to extensive phase II metabolic reactions such as glucuronidation and sulfation, generating corresponding complexes. The prototype drug and its metabolites are mainly excreted through the kidneys in urine, with some being excreted through bile and feces.
• Challenges and Strategies in Drug Development Low oral bioavailability is the main bottleneck limiting its clinical translation. To this end, researchers have developed various novel drug delivery systems, including nanocrystals, liposomes, polymer micelles, self microemulsions, etc., aimed at improving their solubility, delaying metabolism, enhancing intestinal absorption, and targeting. In addition, preparing freeze-dried powder injections for intravenous administration is a current effective strategy to avoid first pass effects and achieve rapid onset, which has been applied in some clinical studies.
• safety Preclinical toxicology studies have shown that magnesium salt of salvianolic acid B has good safety within the therapeutic dose range. Its lack of hERG inhibition risk and negative Ames test prediction provide important safety endorsement for its cardiovascular application. However, the potential toxicity of long-term high-dose use still needs to be systematically evaluated.

Clinical application prospects and prospects

The clinical application prospects of magnesium salt of salvianolic acid B are broad, but it needs to be promoted from multiple perspectives:

1. Cardiovascular disease treatment Its most direct application direction is as an auxiliary treatment drug for coronary heart disease, angina pectoris and myocardial infarction, as well as for the prevention and treatment of atherosclerosis, heart failure, diabetes and cardiovascular complications. Based on its multi-target characteristics, it is particularly suitable for CVD patients with complex pathological backgrounds.
2. Development of new formulations: To continue to deepen the research of new drug delivery systems, such as developing oral bioavailability of nanoparticles, or designing intelligent delivery systems targeting atherosclerotic plaque and ischemic myocardium, is the key to improving its efficacy and expanding its application scenarios.
3. Combination therapy strategy Exploring the combined use of magnesium salt of salvianolic acid B with existing standard therapeutic drugs (such as statins, antiplatelet drugs, ACEIs, etc.) may produce synergistic effects and reduce side effects, which has important clinical value.
4. Expand the field of diseases Based on its effect on PTPN1, AKR1B1, BACE1 and other targets, its therapeutic potential in type 2 diabetes and its complications, Alzheimer's disease and other fields deserves further exploration.
5. High quality clinical research At present, large-scale, multicenter, randomized double-blind phase III clinical trials are still needed to confirm its exact efficacy and long-term safety in different CVD indications, and establish a clear dose-response relationship.
6. Deep exploration of the mechanism of action By utilizing techniques such as systems pharmacology, proteomics, metabolomics, and gene editing, we aim to further uncover the full scope of its network pharmacology effects and discover new targets and signaling pathways.

Conclusion

Danshensu B magnesium salt, as a modernized product of traditional Chinese medicine Danshen, has become a star molecule in the development of natural cardiovascular drugs due to its clear chemical structure, multi-target synergistic pharmacological effects, and relatively good safety characteristics. It intervenes in the process of cardiovascular disease from multiple core links such as energy metabolism, oxidative stress, inflammatory response, and cell apoptosis, reflecting the systemic treatment concept of "multi-component multi-target multi pathway". Although there are challenges in developing drug properties such as oral bioavailability, these obstacles are gradually being overcome through modern pharmaceutical technology and in-depth clinical research. In the future, with the continuous deepening of basic and translational research, magnesium salt of salvianolic acid B is expected to move from the laboratory to a wider range of clinical applications, not only providing a new combination of traditional Chinese and Western medicine treatment option for cardiovascular disease patients, but also providing a model for innovative drug development based on natural products.