Product name: Mogroside III A1
Synonym name:
Catalogue No.: BP0951
Cas No.: 88901-42-2
Formula: C₄₈H₈₂O₁₉
Mol Weight: 963.165
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
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HPLC of Mogroside III A1

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

Introduction/Overview

Mogroside III A1 (CAS No.: 88901-42-2) is a class of triterpene glycosides derived from monk fruit (Siraitia grosvenorii, commonly known as "chayote"), and is a sweet triterpene natural product. As a non-sugar sweetener, monk fruit glycoside III A1 is much sweeter than sucrose and features low calorie content and low glycemic load, making it highly regarded in the food industry and pharmaceutical fields. In recent years, with in-depth research into the pharmacological activity of natural products, monk fruit glycoside III A1 has been found not only to have remarkable sweetness but also to exhibit various biological activities, including antioxidant, antidiabetic, and anti-cancer effects, demonstrating its potential application value in disease prevention and treatment.

As a metabolic disease that poses a serious threat to human health worldwide, diabetes has a complex pathogenesis involving multiple signaling pathways and various molecular targets. Monk fruit glycoside III A1 demonstrates good pharmacological activity in regulating glucose metabolism, improving insulin sensitivity, and anti-inflammatory and antioxidant properties, especially by regulating key targets such as AMPK, SGLT2, and GCK, demonstrating potential for diabetes treatment. This paper aims to systematically review the chemical structure, plant origin, pharmacological activity, and mechanism of action of monk fruit glycoside III A1, and, combined with druggability evaluation and pharmacokinetic characteristics, explores its clinical application prospects and provides theoretical basis and reference for subsequent research and development.

Chemical structure and physicochemical properties

Luo Han Guoside III A1 belongs to the triterpene glycoside class, with a molecular formula of C_48H_78O_18 and a molecular weight of 963.1650. Its structural core is the cucurbitane skeleton, which connects multiple glucose units through glycosidic bonds, forming a highly polar glycoside structure. The compound has a LogP value of 1.9125, indicating moderate lipid solubility, which facilitates cell membrane penetration and bioavailability. The extremely high polar surface area (TPSA) of 318.3700 Ų indicates that its molecular surface is rich in polar groups, especially hydroxyl and glycosidic bonds, which contribute to its water solubility. With a water solubility value of 0.1505, it is suitable for solubility in aqueous media.

From a pharmacokinetic perspective, monk fruit glycoside III A1 has relatively low blood-brain barrier penetration ability, suggesting limited direct effects on the central nervous system. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenicity test result was 0.0, indicating a low genotoxicity risk and meeting safety requirements.

Plant Origins and Extraction Methods

Monk fruit glycoside III A1 is mainly found in monk fruit fruits, which belong to the Cucurbitaceae family and are native to Guangxi, Guangdong, and other regions in China. The fruit of monk fruit contains abundant sweet triterpene glycosides, mainly including monk fruit glycosides I, II, III, and their derivatives. Luo Han Guoside III A1 is one of the important sweetening components.

The extraction method usually uses the water extraction alcohol precipitation method. The specific steps include: drying and crushing monk fruit fruit, extracting with hot water or 70%-80% ethanol, then concentrating and filtering the extract, and enriching it using resin adsorption (such as D101 adsorption resin). Subsequently, high-purity monk fruit glycoside III A1 was obtained by silica gel column chromatography or high-performance liquid chromatography (HPLC) separation and purification. In recent years, new technologies such as ultrasound-assisted extraction and microwave-assisted extraction have also been applied to improve extraction efficiency and purity.

Pharmacological activity research

Antioxidant activity

Monk Fruit Glycoside III A1 demonstrated significant antioxidant capacity. In vitro experiments have shown that it can effectively scavenge free radicals such as DPPH and ABTS, reducing cellular damage caused by oxidative stress. Its antioxidant mechanism mainly relies on the abundance of hydroxyl groups in the molecule, which neutralizes free radicals through electron donors, protecting cell membrane lipids and DNA from oxidative damage.

Antidiabetic activity

The pathogenesis of diabetes is complex, involving insufficient insulin secretion and insulin resistance. Luo Han Guoside III A1 regulates blood glucose metabolism through multiple targets, showing good hypoglycemic effects. Animal model studies have shown that monk glycoside III A1 can significantly lower blood sugar levels, improve insulin sensitivity, and alleviate diabetes-related tissue damage.

Its mechanism of action includes activating the AMPK signaling pathway, promoting glucose uptake and lipid metabolism; Inhibits SGLT2, reduces renal glucose reabsorption, and increases urinary glucose excretion; Regulates GCK (glucokinase) activity and promotes liver glucose metabolism. Additionally, monk fruit glycoside III A1 enhances insulin signaling by inhibiting PTPN1 (protein tyrosine phosphatase 1B), thereby reducing insulin resistance.

Anticancer activity

Monk fruit glycoside III A1 exhibits effects on inhibiting proliferation and inducing apoptosis across various tumor cell lines. Its anti-cancer mechanisms involve regulating the cell cycle, activating apoptotic signaling pathways, and inhibiting tumor cell migration and invasion. Some studies indicate that monk fruit glycoside III A1 can regulate tumor-related signaling molecules such as APP (amyloid precursor protein), MAOA (monoamine oxidase A), and ESR2 (estrogen receptor β), exerting anti-tumor effects.

Mechanism of action and molecular targets

The multi-target mechanism of monk fruit glycoside III A1 is the foundation of its diverse pharmacological activity. For diabetes, the main targets include:

• AMPK (PRKAA1): As a key regulator of energy metabolism, AMPK activation promotes glucose uptake and fatty acid oxidation, improving metabolic disorders. Luo Han Guoside III A1 activates AMPK and regulates downstream metabolic pathways, exerting its hypoglycemic effect.

• SGLT2: Sodium-glucose co-transporter protein in the proximal tubules of the kidney, regulates glucose reabsorption. Monk fruit glycoside III A1 inhibits SGLT2 activity, promotes urinary glucose excretion, and lowers blood sugar.

• GCK (Glucokinase): A key enzyme in the liver and pancreas that regulates glucose metabolism. Romonfruit glycoside III A1 promotes GCK activity and enhances glucose metabolism efficiency.

• PTPN1: Negatively regulates the tyrosine phosphatase protein in the insulin signaling pathway; inhibiting its activity helps improve insulin sensitivity.

Additionally, the regulation of APP, MAOA, ESR2 targets by monk fruit glycoside III A1 suggests its potential role in neurodegenerative diseases and tumor treatment. Its multi-target nature makes it a natural drug candidate with broad therapeutic potential.

Druggability evaluation and pharmacokinetics

The druggability evaluation of monk fruit glycoside III A1 shows that it has good safety and pharmacodynamic characteristics. The molecular weight is close to 1000, slightly above the ideal range for traditional small molecule drugs, but its moderate LogP value and good water solubility facilitate absorption and distribution in the body. A higher TPSA value suggests strong polarity, which may limit oral bioavailability, but can be improved through structural modification or formulation techniques.

Toxicologically, hERG channel inhibition was negative and Ames tests showed no mutagenicity, indicating low risks of cardiotoxicity and genotoxicity. The blood-brain barrier penetration ability is low, reducing the risk of central nervous system side effects.

Pharmacokinetic studies show that monk fruit glycoside III A1 is slowly absorbed orally and is mainly hydrolyzed and metabolized in the intestines, producing various active metabolites. Its metabolic pathways mainly involve glucoside hydrolysis and hepatic phase II metabolism. It has a moderate half-life in the body, making it suitable for daily administration. In the future, further in vivo pharmacokinetic and toxicology studies are needed to optimize dosage forms and administration regimens.

Prospects and outlooks for clinical applications

Monk Fruit Glycoside III A1, as a natural non-sugar sweetener, has been widely used in the food industry to replace traditional sucrose and meet dietary needs for low-calorie, low-glycemic load. Its multiple pharmacological activities make it promising as an adjunct treatment for diabetes and related metabolic diseases. By regulating key targets such as AMPK and SGLT2, Luo Han Guoside III A1 not only effectively lowers blood sugar but also improves lipid metabolism and antioxidant status, reducing the occurrence of diabetic complications.

In addition, the anticancer and anti-inflammatory activities of monk fruit glycoside III A1 offer potential applications in tumors and chronic inflammatory diseases. Combined with its excellent safety profile and low toxicity, it could be developed into a multi-target therapeutic drug or functional health product in the future.

However, clinical research on monk fruit glycoside III A1 is still in its early stages and lacks systematic clinical trial data. Future research should focus on pharmacokinetic optimization, formulation development, clinical efficacy validation, and safety evaluation. At the same time, combining modern molecular biology and medicinal chemistry technologies, structural modification and derivative development are carried out to enhance efficacy and druggability.

Conclusion

Luo Han Guoside III A1, a natural triterpene glycoside derived from monk fruit, combines high sweetness with multiple pharmacological activities, showing remarkable potential especially in anti-diabetes, antioxidant, and anticancer fields. Its multi-target mechanism of action and good safety profile lay the foundation for it to become a candidate molecule for novel natural drugs. In the future, with continuous advances in extraction and purification technologies and drug development methods, monk fruit glycoside III A1 is expected to play an important role in the prevention and treatment of diabetes and related metabolic diseases, promoting the integration of natural product pharmacology with functional foods. Systematic clinical research and mechanism analysis will further reveal its clinical application value and promote its advancement toward clinical translation.