Product name: Mogroside IIa
Synonym name:
Catalogue No.: BP2038
Cas No.: 1613527-65-3
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.
For Reference Standard and R&D, Not for Human Use Directly.
HPLC of Mogroside IIa
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Arhat fruit glycoside IIa (Arhat fruit glycoside IIa) is a natural triterpene sweet glycoside isolated from the traditional Chinese medicine Siraitia grosvenorii, which belongs to an important member of the Luohan fruit glycoside family. Momordica grosvenorii, as a unique medicinal and edible plant in southern China, has long been used for flavoring and treating cough, constipation, diabetes and other diseases due to its natural sweetness and a variety of bioactive ingredients. In recent years, with the in-depth study of the pharmacological functions of Arhat fruit glycosides, Arhat fruit glycoside IIa has gradually become the focus of natural product pharmacology research due to its unique structure and significant biological activity, especially its potential in the field of alternative treatment of diabetes.
Arhat IIa not only has sweet taste regulation effect, but also has multiple pharmacological effects such as regulating blood sugar, antioxidant and anti-inflammatory effects. Its mechanism of action involves a variety of molecular targets, especially the interaction with taste receptors and related signaling pathways, which provides a new idea for the treatment of diabetes and metabolic syndrome. This article will systematically review the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activities and mechanisms, pharmaceutical evaluation and pharmacokinetic characteristics of Arhat fruit glycoside IIa, and comprehensively evaluate its potential and development direction as an alternative drug for diabetes in combination with the current clinical application prospect.
The chemical formula of Arhat fruit glycoside IIa is C42H70O14, and its molecular weight is 801.0240. It belongs to a triterpene sweet glycoside. Its structural core is a tetracyclic triterpenoid skeleton, connecting multiple β - D-glucoside groups to form a highly polar glycoside structure. The structure of Arhat IIa is similar to that of siraitin I-A1, both of which contain multiple glucose residues, but there are slight differences in the connection mode and position of glycosides, which affect its biological activity and pharmacokinetics.
In terms of physical and chemical properties, the LogP value of Arhat fruit glycoside IIa is 2.5780, indicating that it has moderate fat solubility, which is conducive to cell membrane penetration but not easy to accumulate in the lipid environment. Its topological polar surface area (TPSA) is 239.2200, indicating high polarity and reflecting the characteristics of its multi glycosidic structure. Low water solubility (0.0599 mg/mL) suggests limited solubility in aqueous phase, which may affect its oral bioavailability. The low permeability of the blood-brain barrier indicates that Arhat fruit glycoside IIa is difficult to enter the central nervous system, reducing the risk of central side effects. The hERG channel inhibition experiment showed a negative result, indicating a low risk of cardiac toxicity. The Ames mutagenicity test result was 0.0, indicating no significant genotoxicity.
In conclusion, the structural characteristics of Arhat fruit glycoside IIa endow it with good safety and moderate pharmacokinetics, but its low water solubility and bioavailability are still challenges in future drug development.
Arhat IIa mainly exists in Siraitia grosvenorii fruits, especially in the pulp and cortex of mature fruits. As a cucurbitaceae plant, Momordica grosvenorii fruit is rich in a variety of sweet triterpene glycosides, including momordicin I-A1, Arhat IIa and other homologues. The content of Arhat fruit glycoside IIa is greatly affected by fruit maturity, planting environment, picking time and other factors.
Traditional extraction methods mainly rely on water extraction and alcohol extraction, combined with modern technologies such as ultrasound assisted extraction and enzymatic hydrolysis to improve extraction efficiency and purity. The specific process includes:
In recent years, green extraction technologies such as supercritical CO2 extraction and membrane separation have been gradually applied to the extraction of Arhat fruit glycoside IIa, taking into account environmental friendliness and efficiency.
The pharmacological activities of Arhat IIa mainly focus on its sweet taste regulation, anti diabetes, anti-oxidation and anti inflammation.
As a member of the Momordica grosvenorii sweet glycoside family, Arhat grosvenorii IIa has significant sweet taste characteristics, and its sweetness is about ten times that of sucrose. By activating the taste receptor T1R2/T1R3 complex, Arhat fruit glycoside IIa can simulate natural sweetness and is widely used as a sweetener substitute for sugar free foods and beverages.
The demand for treatment of diabetes, especially type 2 diabetes, promotes the research of natural products. Arhat IIa affects insulin secretion and glucose metabolism by regulating taste receptor related signaling pathways. In vitro and animal experiments showed that Arhat fruit glycoside IIa could improve the function of pancreatic islet β cells, enhance insulin sensitivity, and reduce blood glucose levels. In addition, it also has a protective effect on diabetes complications such as diabetes nephropathy and neuropathy.
Arhat fruit glycoside IIa has the ability to eliminate free radicals, inhibit oxidative stress and reduce inflammatory reaction. It reduces the expression of pro-inflammatory factors and protects cells from oxidative damage by regulating signaling pathways such as NF - κ B and MAPK. These effects provide a theoretical basis for its adjuvant therapy in chronic metabolic diseases.
Some studies also revealed the potential effects of Arhat fruit glycoside IIa on immune regulation, liver protection, anti-tumor and other aspects, suggesting its pharmacological characteristics of multiple targets and pathways.
The main mechanism of action of Arhat fruit glycoside IIa involves taste receptor complex and its downstream signal pathway, especially the key targets in alternative treatment of diabetes include:
Through the above targets, Arhat fruit glycoside IIa not only regulates taste perception, but also directly affects insulin secretion and glucose homeostasis. In addition, Arhat fruit glycoside IIa protects islet cells and target tissues by inhibiting oxidative stress and inflammatory signaling pathways, and reduces diabetes related pathological damage.
The pharmaceutical evaluation of Arhat IIa shows that it has certain development potential, but there are also challenges.
Due to the large molecular weight and complex structure of glycosides, Arhat fruit glycoside IIa is absorbed slowly after oral administration, and its bioavailability is limited. Its high TPSA value and low water solubility limit intestinal absorption. Animal experiments show that Arhat fruit glycoside IIa has a long half-life in plasma, which is mainly metabolized into small molecule active metabolites through intestinal flora, exerting biological effects.
The negative hERG channel inhibition test and Ames mutagenicity test indicate that the risk of cardiac toxicity and genotoxicity of Arhat IIa is low. Long term toxicology studies have shown that it has good tolerance and no significant organ toxicity has been observed.
At present, there is no clear report on the significant interaction between Arhat IIa and other drugs, but its potential to regulate metabolic enzymes and transporters needs further research.
The low water solubility and oral bioavailability of Arhat IIa limit its clinical application. In the future, strategies such as nanocarriers, liposome encapsulation, and structural modification can be used to improve its stability and absorption rate.
As a natural sweetener and candidate molecule for alternative therapy of diabetes, Arhat fruit glycoside IIa has broad clinical application prospects.
Based on its mechanism of regulating taste receptors and insulin secretion, Arhat fruit glycoside IIa is expected to become an auxiliary therapeutic agent for type 2 diabetes patients, improve blood sugar control and reduce the side effects of traditional drugs. Its natural sweetener characteristics are also suitable for diabetes patients to replace sucrose intake and reduce sugar load.
The antioxidant and anti-inflammatory effects of Arhat IIa provide the possibility for its adjuvant treatment in obesity, fatty liver and cardiovascular disease. Future clinical trials need to further validate its efficacy and safety.
In order to promote the clinical transformation of Arhat fruit glycoside IIa, the following aspects need to be strengthened:
As an important triterpene sweetness glycoside in Arhat grosvenorii, Siraitin IIa has both natural sweetness and multiple pharmacological activities, especially in the field of alternative treatment of diabetes. It affects insulin secretion and glucose metabolism by regulating taste receptors and related signaling pathways, supplemented by antioxidant and anti-inflammatory effects, providing new ideas for the comprehensive management of metabolic diseases. Although its low water solubility and bioavailability limit its clinical application, with the development of extraction and purification technology and drug delivery system, Arhat fruit glycoside IIa has broad prospects for drug development. In the future, combined with systematic pharmacological mechanism research and clinical verification, it is expected to develop Arhat fruit glycoside IIa into a safe and effective natural metabolic regulator, which will benefit the majority of patients with diabetes and metabolic diseases.
