Product name: Siraitic acid B
Synonym name:
Catalogue No.: BP2037
Cas No.: 183374-16-5
Formula: C₂₉H₄₂O₅
Mol Weight: 470.65
Botanical Source: Siraitiae Radix
Physical Description:
Type of Compound: Triterpenoids

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle

Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.

The product could be supplied from milligrams to grams
Inquire for bulk scale.

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

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

Introduction/Overview

Siraitic acid B is a cucurbitane triterpenoid compound extracted from the root of Siraitia grosvenorii. In recent years, it has attracted extensive attention due to its significant biological activity, especially its potential application in the field of anti diabetes. As a metabolic disease with high incidence worldwide, diabetes seriously threatens human health. Developing safe and effective natural product drugs has become an important direction of current research. With its unique chemical structure and multi-target regulation ability, Arhat B has shown multiple pharmacological effects such as regulating blood glucose metabolism and improving insulin sensitivity, and has become a hot spot in the research of natural anti diabetes drugs.

This article will systematically review the chemical structure, physical and chemical properties, plant sources and extraction methods of Arhat fruit acid B, focus on its pharmacological activity and mechanism of action, analyze its pharmacokinetic characteristics in combination with pharmaceutical parameters, and finally explore its clinical application prospects and future research directions, providing theoretical support and research reference for natural product pharmacology and diabetes treatment.

Chemical structure and physicochemical properties

Arhat fruit acid B belongs to cucurbitane triterpene with molecular formula of C_30H_46O_5 and molecular weight of 470.65. Its structural core is a typical pentacyclic cucurbitane skeleton, containing multiple hydroxyl and carboxyl functional groups, endowing it with strong polarity and biological activity. According to the database information of CAS No. 183374-16-5, the LogP value of Arhat B is 4.5117, which shows that it has good fat solubility and is conducive to penetrating the cell membrane, but its water solubility is low (0.0054 mg/mL), which may limit its oral absorption and bioavailability.

The topological polar surface area (TPSA) is 80.67 Å ², indicating that the molecule has moderate polarity, which may affect its binding affinity with biological targets. The low permeability of the blood-brain barrier suggests its limited role in the central nervous system, reducing potential central side effects. The hERG channel inhibition test was negative, indicating that the heart toxicity risk of Arhat fruit acid B was low. The Ames mutagenicity test result is 0, indicating that it has no significant genotoxicity and meets the basic requirements for safe drug use.

Plant sources and extraction methods

Arhat B is mainly extracted from the root of Momordica grosvenorii. Momordica grosvenorii is the fruit of the gourd plant Siraitia grosvenorii, which is widely used in traditional Chinese medicine to moisten the lung, relieve cough, clear heat, detoxify and reduce sugar. Although the fruit is the main medicinal part, the root contains abundant triterpenes, especially cucurbitane triterpenes such as Arhat fruit acid ethyl, which are the important source of its active ingredients.

The extraction process usually uses organic solvent extraction combined with column chromatography separation. The specific steps include:

1. Raw material pretreatment: The roots of Siraitia grosvenorii were dried and crushed to select the appropriate particle size.
2. Solvent extraction Ethanol or methanol are often used as extractants, and extraction is carried out for several hours at room temperature or reflux conditions.
3. Concentrated separation After vacuum concentration, the extract is separated and purified using silica gel column chromatography or high-performance liquid chromatography (HPLC).
4. Structural Identification Confirm the structure of the compound through nuclear magnetic resonance (NMR), mass spectrometry (MS), and infrared spectroscopy (IR).

In recent years, the application of ultrasonic assisted extraction and microwave assisted extraction technology has improved the extraction efficiency and purity of Arhat B, and promoted its large-scale production and in-depth research.

Pharmacological activity research

The pharmacological activity of Arhat fruit acid B mainly focuses on the anti diabetes effect, in addition, it also shows certain anti-inflammatory, antioxidant and other auxiliary effects, and the comprehensive effect is helpful to improve diabetes and its complications.

Anti diabetes effect

Many in vitro and in vivo studies have confirmed that siraite b can significantly reduce blood glucose levels and improve insulin resistance. Its main manifestations are:

• Promote glucose uptake Enhance the absorption of glucose by skeletal muscle and adipocytes, and improve glucose metabolism disorders.
• Regulating the insulin signaling pathway Promote the signaling of insulin receptor substrate 1 (IRS1) and protein kinase B (AKT1), and enhance insulin sensitivity.
• Inhibit gluconeogenesis Reduce liver glucose production and alleviate blood sugar burden.
• Protecting pancreatic beta cells Slow down cell apoptosis and maintain insulin secretion function.

Other pharmacological effects

Arhat B also has antioxidant activity, which can clear free radicals and reduce the damage of oxidative stress to islet cells. In addition, its anti-inflammatory effect alleviates chronic inflammation related to diabetes by inhibiting the release of inflammatory factors.

Mechanism of action and molecular targets

The anti diabetes effect of Arhat fruit acid B involves multiple signaling pathways and key targets, which reflects the characteristics of multi target and multi pathway coordinated regulation.

1. AMPK signaling pathway

5 'AMP activated protein kinase (AMPK) is a core regulatory factor in cellular energy metabolism. B siraite can activate AMPK (including PRKAA1 subunit), promote glucose uptake and lipid metabolism, inhibit gluconeogenesis, and improve insulin sensitivity.

2. SGLT2 inhibition

Sodium glucose cotransporter 2 (SGLT2) is a key target for renal glucose reabsorption. Arhat B showed inhibitory effect on SGLT2, promoted urine glucose excretion and reduced blood glucose level.

3. Insulin signaling pathway

By regulating insulin receptor substrate 1 (IRS1), protein kinase B (AKT1) and PI3K regulatory subunit (PIK3R1), Arhat B enhances insulin signal transduction, promotes the translocation of glucose transporter 4 (SLC2A4) to the cell membrane, and improves the glucose uptake of cells.

4. Regulation of nuclear receptor PPAR γ

Peroxisome proliferator activated receptor gamma (PPARG) is involved in regulating lipid and glucose metabolism. Arhat B can improve insulin resistance and regulate the balance of lipid metabolism by activating PPARG.

5. DPP4 inhibition

Dipeptidyl peptidase 4 (DPP4) participates in the degradation of glucagon like peptide-1 (GLP-1) and affects insulin secretion. Arhat fruit acid B inhibits DPP4 activity, prolongs the action time of GLP-1, and promotes insulin secretion.

To sum up, Arhat B fructate can regulate glucose metabolism and insulin function through multi target and multi pathway synergy, and exert its anti diabetes effect.

Evaluation of drug properties and pharmacokinetics

The pharmaceutical evaluation of Arhat B is based on its physicochemical properties and pharmacokinetics in vivo.

Physical and chemical property analysis

• Molecular weight 470.65 Within the appropriate range of drug molecular weight.
• LogP 4.5117 It shows good lipid solubility, which is beneficial for cell membrane penetration, but too high may affect water solubility and oral absorption.
• TPSA 80.67 ŲModerate polarity facilitates target binding.
• Very low water solubility (0.0054 mg/mL)To limit its oral bioavailability, it is necessary to improve dissolution through formulation optimization.
• Low permeability of blood-brain barrier Reduce the risk of central nervous system side effects.
• No hERG channel inhibition Good cardiac safety.
• No mutagenicity The safety is relatively high.

Pharmacokinetic characteristics

At present, the pharmacokinetic study on Arhat B is relatively limited, but based on its structure and physical and chemical properties, it is speculated that:

• Oral absorption is limited, and new drug delivery systems such as nanocarriers or liposomes may be needed to improve bioavailability.
• The distribution in vivo tends to peripheral tissues, especially liver and muscle, which is in line with its anti diabetes target.
• The metabolic pathway may involve the liver cytochrome P450 enzyme system, and further research is needed on its metabolites and metabolic kinetics.
• The excretion pathway is not yet clear, and it is speculated that bile and urine are the main excretions.

In the future, systematic pharmacokinetic and toxicological studies need to be conducted to clarify its in vivo behavior and safe dose range, laying the foundation for clinical development.

Clinical application prospects and prospects

As a natural cucurbitane triterpene, Arhat fruit acid B has a multi-target anti diabetes activity, showing good clinical application potential. Its advantages lie in:

• Multi-target effect It can comprehensively regulate glucose metabolism and is suitable for the treatment of diabetes with complex pathological conditions.
• High security No obvious cardiac toxicity or genotoxicity, suitable for long-term use.
• Natural source Easy to extract and develop on a large scale.

However, at present, Arhat B is still in the basic research stage, and the data of preclinical research and clinical trials are still lacking. Future research directions should include:

• Optimize extraction and purification processes to improve yield and purity.
• Develop new drug delivery systems to improve oral bioavailability.
• Conduct systematic pharmacokinetic, toxicological, and pharmacodynamic studies to determine safe and effective doses.
• Design a multicenter, randomized, double-blind clinical trial to validate its clinical efficacy and safety.
• To explore the potential of its combination with existing anti diabetes drugs and evaluate the synergistic effect.

In addition, in view of its anti-inflammatory and antioxidant properties, the application of Arhat B in diabetes complications such as diabetes nephropathy and neuropathy is also worth further exploration.

Conclusion

As a natural product of cucurbitane triterpenoids extracted from the root of Arhat grosvenorii, Momordica acid B shows a broad application prospect in the field of anti diabetes due to its unique chemical structure and multi-target regulatory ability. It comprehensively improves glucose metabolism disorders through multiple mechanisms such as activating AMPK, inhibiting SGLT2, regulating insulin signaling pathway, and PPAR γ, and has good safety and potential for drug development.

Although most of the current studies focus on in vitro and animal models, the clinical transformation of Arhat B still faces challenges such as low bioavailability and unclear pharmacokinetics. In the future, it is necessary to strengthen the optimization of pharmaceutical preparations, systematic pharmacokinetic research and clinical verification, so as to promote it to become a safe and effective natural anti diabetes drug.

In conclusion, Arhat B not only enriches the research scope of diabetes natural drugs, but also provides an important molecular basis for the development of multi-target treatment strategies, which has important scientific value and application prospects.