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Product name: Mogroside II A2
Synonym name:
Catalogue No.: BP0949
Cas No.: 88901-45-5
Formula: C42H72O14
Mol Weight: 801.024
Botanical Source: Siraitiae fructus
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.
Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
B. Custom extraction and purification, target Herb Active Ingredients
C. Custom synthesis and semi-synthesis for Natural Active Ingredients
D. CR(contract research), CM(contract manufacture) and PD(process development) services from lab scale, pilot scale to commercial scale(GMP is also available)
E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.
HPLC of Mogroside IIa2
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
239.2200
2.6066
2.6064
.0468
.5656
.6317
Low
72.4149
6.0515
No
No
No
No
No
No
0.0
Yes
No
No
Yes
Mogroside II A2 is a triterpene glycoside natural product isolated from Siraitia grosvenorii, attracting attention for its remarkable sweetness and multiple biological activities. As a non-carbohydrate natural sweetener, monk fruit glycoside IIa2 is much sweeter than traditional sucrose and has low calorie characteristics, making it suitable as a sugar substitute for diabetic patients and those trying to lose weight. In recent years, with the deepening of natural product pharmacology, the potential applications of monk fruit glycoside IIa2 in antioxidant, anti-diabetic, and anti-cancer fields have gradually been revealed, showing broad pharmaceutical prospects.
This paper aims to systematically review the chemical structure and physicochemical properties, plant origin, and extraction methods of monk fruit glycoside IIa2, and, combined with the latest pharmacological activity studies, deeply explore its mechanism of action and molecular targets, evaluate its druggability and pharmacokinetic characteristics, and anticipate its clinical application potential, providing a theoretical basis and reference for subsequent basic research and clinical translation.
Monk fruit glycoside IIa2 belongs to the triterpene glycoside class of compounds, with a molecular formula of C42H70O14 and a molecular weight of 801.0240. Its core structure is a tetracyclic triterpene parent nucleus, connecting multiple glycosyl residues to form a highly polar glycoside structure. The compound has a LogP value of 2.6066, indicating moderate lipid solubility, which facilitates penetration of cell membranes. The total polar surface area (TPSA) is 239.2200, showing strong polar characteristics that favor water solubility and interaction with biological macromolecules.
Luo Han Guoside IIa2 has relatively low water solubility, about 0.0468 mg/mL, which poses certain challenges to its absorption and distribution in the body. The low permeability of the blood-brain barrier suggests its limited role in the central nervous system. The hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity. Ames mutagenicity test results were zero, indicating that this compound has no significant mutagenicity and is relatively safe.
Chemical modification of polysaccharides not only imparts high sweetness but also significantly influences bioactivity and pharmacokinetic properties. The polyhydroxyl groups in its structure provide a theoretical basis for its antioxidant activity, while the presence of glycosyls may affect its binding affinity with target proteins.
Monk fruit glycoside IIa2 is mainly found in monk fruit fruit, a plant of the Cucurbitaceae family, native to Guangxi, Guizhou, and other regions in China. It is widely cultivated for its sweetness and medicinal value. Monk fruit contains various triterpene glycoside compounds, among which monk fruit glycoside IIa2 is one of the main sweeteners.
Traditional extraction methods mostly use water extraction and alcohol precipitation. The specific process includes: crushing the dried monk fruit and extracting it with hot water or ethanol solution, followed by filtering, concentration, and alcohol settling to remove impurities and non-sugar components. High-performance liquid chromatography (HPLC) combined with mass spectrometry (MS) technology is widely used for the isolation, purification, and quantitative analysis of monk fruit glycoside IIa2.
In recent years, the application of ultrasound-assisted extraction, microwave-assisted extraction, and membrane separation technologies has improved extraction efficiency and purity, reducing the risk of thermal degradation during the extraction process. Moreover, the combined use of countercurrent chromatography and high-performance liquid chromatography effectively achieves high-purity separation of monk fruit glycoside IIa2, providing a reliable material foundation for its pharmacological research and formulation development.
Mongol glycoside IIa2 has significant antioxidant capacity. In vitro studies have shown that this compound can effectively scavenge free radicals such as DPPH, ABTS, and superoxide anion free radicals, reducing oxidative stress damage to cells. Its polyhydroxyl structure acts as an electron donor, which can stabilize free radicals and block oxidation chain reactions.
In vivo experiments, monk fruit glycoside IIa2 regulates the activity of antioxidant enzyme systems (such as superoxide dismutase SOD, glutathione peroxidase GSH-Px), reduces lipid peroxidation products (such as malondialdehyde MDA), alleviates oxidative stress-related tissue damage, and demonstrates potential in protecting target organs such as cardiovascular and cerebrovascular systems and liver.
As a metabolic disease, diabetes has a complex pathogenesis, involving insulin resistance, dysfunction of islet β cells, and disorders of glucose metabolism. Monk Fruit Glycoside IIa2 has demonstrated blood sugar regulation effects in multiple in vivo and in vitro experiments.
Research shows that monk fruit glycoside IIa2 can activate the AMPK (5' AMP-activated protein kinase) signaling pathway, promote glucose uptake and lipid metabolism, and improve insulin sensitivity. Additionally, this compound inhibits sodium-glucose co-transporter 2 (SGLT2), reducing renal glucose reabsorption and promoting urinary glucose excretion, thereby lowering blood sugar levels.
In pancreatic cell models, monk fruit glycoside IIa2 enhances glucokinase (GCK) activity and promotes glucose metabolism. Its inhibitory effect on protein tyrosine phosphatase 1B (PTPN1) helps improve insulin signaling and alleviate insulin resistance. Additionally, monk fruit glycoside IIa2 may regulate glucose metabolism and neuroendocrine functions by regulating targets such as estrogen receptor β (ESR2) and monoamine oxidase A (MAOA), thereby reducing diabetic complications.
Monk fruit glycoside IIa2 exhibits activity in inhibiting proliferation and inducing apoptosis across various cancer cell lines. Its anticancer mechanism involves regulation of multiple signaling pathways, including inhibiting oxidative stress responses in tumor cells, inducing apoptosis in mitochondrial pathways, and blocking the expression of tumor-related signaling molecules such as amyloid precursor protein (APP).
In vitro experiments show that monk fruit glycoside IIa2 can inhibit tumor cell migration and invasion, reducing the potential for tumor metastasis. Its anti-inflammatory and immunomodulatory effects also support its anti-tumor effects. Although current anticancer research mostly focuses on cell and animal models, the safety and multi-target properties of monk fruit side IIa2 as a natural product make it a potential candidate for anticancer drug development.
The pharmacological action of monk fruit glycoside IIa2 depends on its interactions with multiple molecular targets, forming a complex signal regulatory network.
AMPK (PRKAA1): As a key regulator of energy metabolism, AMPK activation promotes glucose uptake and fatty acid oxidation. Romonfruit glycoside IIa2 activates AMPK, improves metabolic disorders, and exerts antidiabetic effects.
SGLT2: In the kidneys, SGLT2 is responsible for glucose reabsorption. Luomonfruit glycoside IIa2 inhibits SGLT2, promotes urinary glucose excretion, and lowers blood sugar.
GCK (Glucose Kinase): A key enzyme regulating glucose metabolism, monk fruit glycoside IIa2 enhances its activity and promotes glucose utilization.
PTPN1 (protein tyrosine phosphatase 1B): negatively regulates the insulin signaling pathway. Monk fruit glycoside IIa2 enhances insulin sensitivity by inhibiting PTPN1.
MAOA (Monoamine Oxidase A): affects neurotransmitter metabolism and may be involved in the regulation of diabetes-related neuropathy.
ESR2 (estrogen receptor β): Regulates metabolic and immune functions; monk fruit glycoside IIa2 may mediate some biological effects through ESR2.
APP (amyloid precursor protein): Related to tumor cell proliferation and migration, monk fruit glycoside IIa2 regulates APP expression and exerts antitumor effects.
The multi-target regulation of these targets demonstrates the potential of monk fruit glycoside IIa2 as a multi-target drug, aiding its therapeutic application in complex diseases such as diabetes and cancer.
The druggability evaluation of monkfruit glycoside IIa2 shows good safety and a low risk of toxic side effects. Its hERG channel inhibition test was negative, reducing the risk of cardiotoxicity; The Ames test showed no mutagenicity, indicating a low risk of genotoxicity.
However, the lower water solubility and higher polarity (TPSA) of monk fruit glycoside IIa2 may limit its oral bioavailability. Its low blood-brain barrier permeability limits its application in central nervous system-related diseases. In the future, improving their pharmacokinetic properties through structural modification or nanocarrier technology will help enhance their clinical application value.
Currently, pharmacokinetic studies on monk fruit glycoside IIa2 are relatively limited. Preliminary data indicate that its distribution in the body is mainly concentrated in the liver and kidneys, and its metabolic pathway may involve glycolysis mediated by glucosidase. Its excretion is mainly completed by the kidneys, with a moderate half-life, supporting the design of routine dosing regimens.
As a natural non-sugary sweetener, monk fruit glycoside IIa2 has been widely used in the food industry, especially suitable as a sugar substitute for diabetic and obese individuals. Its low calorie and high sweetness characteristics meet the modern demand for healthy eating.
In drug development, the antidiabetic, antioxidant, and anticancer activities of monk fruit glycoside IIa2 provide a solid foundation for clinical translation. In the future, through in-depth mechanistic research and preclinical evaluation, it is expected that novel multi-target therapies will be developed, especially in the prevention and treatment of diabetes and its complications.
In addition, monk fruit glycoside IIa2 can be used in combination with existing drugs to exert synergistic effects, reducing drug dosage and side effects. The combination of nanotechnology and drug delivery systems will further enhance its bioavailability and targeting, expanding its clinical application range.
Despite the broad prospects, issues such as pharmacokinetic limitations, formulation development, and large-scale production process optimization still need to be addressed. In the future, multidisciplinary collaboration will promote monk fruit glycoside IIa2 from the laboratory to clinical practice, benefiting a wide range of patients.
Monk Fruit Glycoside IIa2, as a triterpene glycoside derived from monk fruit, demonstrates broad pharmacological potential due to its unique chemical structure and multiple biological activities. Its research achievements in antioxidant, anti-diabetic, and anti-cancer areas provide important examples for natural product pharmacology.
Systematic evaluation of its mechanism of action, multi-target regulation, and druggability characteristics helps guide its clinical application and new drug development. In the future, with advances in extraction and purification technology and deepening pharmacokinetic research, monk fruit glycoside IIa2 is expected to become an important candidate for natural product drug development, providing new strategies and options for the treatment of diabetes and related metabolic diseases.
In summary, monk fruit glycoside IIa2 is not only a high-quality natural sweetener but also a multifunctional medicinal natural product with potential clinical value, worthy of ongoing attention and in-depth exploration in basic research and clinical translation.
Shenshuai
Wenjing
Hedandan
