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℃
Arhat grosvenorii IIa2 (Mogaside II A2) is a triterpene glycoside natural product isolated from Siraitia grosvenorii, which has attracted much attention due to its significant sweetness and multiple biological activities. As a non sugar natural sweetener, Arhat fruit glycoside IIa2 is much sweeter than traditional sucrose, and has low calorie characteristics. It is suitable for diabetes patients and people who lose weight as a sugar substitute. In recent years, with the in-depth development of natural product pharmacology, the potential applications of Arhat fruit glycoside IIa2 in the fields of anti-oxidation, anti diabetes and anti-cancer have been gradually revealed, showing a broad medicinal prospect.
The purpose of this paper is to systematically review the chemical structure and physicochemical properties, plant sources and extraction methods of Arhat fruit glycoside IIa2, combine with the latest pharmacological activity research, deeply explore its mechanism of action and molecular targets, evaluate its pharmaceutical properties and pharmacokinetic characteristics, and look forward to its clinical application potential, providing theoretical basis and reference for subsequent basic research and clinical transformation.
Arhat fruit glycoside IIa2 is a triterpene glycoside compound with the molecular formula of C42H70O14 and the molecular weight of 801.0240. Its core structure is a tetracyclic triterpenoid nucleus, connecting multiple sugar residues to form a highly polar glycoside structure. The LogP value of this compound is 2.6066, indicating that it has moderate lipid solubility, which is beneficial for cell membrane penetration. The total polar surface area (TPSA) is 239.2200, indicating strong polarity characteristics that are favorable for water solubility and interaction with biomolecules.
The water solubility of Arhat fruit glycoside IIa2 is low, about 0.0468 mg/mL, which challenges its absorption and distribution in vivo. The low permeability of the blood-brain barrier suggests its limited role in the central nervous system. The negative result of hERG channel inhibition experiment indicates a low risk of cardiac toxicity. The Ames mutagenicity test result is 0, indicating that the compound has no significant mutagenicity and good safety.
The polysaccharide based modification of chemical structure not only endows it with high sweetness, but also significantly affects its biological activity and pharmacokinetic properties. The structural hydroxyl groups provide a theoretical basis for its antioxidant activity, while the presence of sugar groups may affect its binding affinity with target proteins.
Arhat IIa2 is mainly found in Siraitia grosvenorii fruits. Siraitia grosvenorii is a cucurbitaceae plant, which is native to Guangxi, Guizhou and other places in China. It is widely cultivated because of its sweet taste and medicinal value. The fruit of Momordica grosvenorii contains many triterpene glycosides, among which Arhat grosvenorii IIa2 is one of the main sweet ingredients.
Traditional extraction methods often use water extraction and alcohol precipitation. The specific process includes: crushing the dried Siraitia grosvenorii fruit, extracting it with hot water or ethanol solution, and then removing impurities and non sugar components through filtration, concentration, alcohol precipitation and other steps. High performance liquid chromatography (HPLC) combined with mass spectrometry (MS) is widely used in the separation, purification and quantitative analysis of Arhat 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, and reduced the risk of thermal degradation during the extraction process. In addition, the combination of countercurrent chromatography and high performance liquid chromatography has effectively achieved the high-purity separation of Arhat IIa2, providing a reliable material basis for its pharmacological research and preparation development.
Arhat IIa2 has significant antioxidant capacity. In vitro studies have shown that the compound can effectively scavenge free radicals such as DPPH, ABTS, and superoxide anion radicals, reducing oxidative stress damage to cells. Its multi hydroxyl structure serves as an electron donor, which can stabilize free radicals and block oxidative chain reactions.
In vivo experiments, Arhat fruit glycoside IIa2 reduces the content of lipid peroxidation products (such as malondialdehyde MDA) and alleviates tissue damage related to oxidative stress by regulating the activity of antioxidant enzyme systems (such as superoxide dismutase SOD, glutathione peroxidase GSH Px), showing the potential to protect cardiovascular, cerebrovascular, liver and other target organs.
As a metabolic disease, diabetes has a complex pathogenesis, involving insulin resistance, pancreatic beta cell dysfunction and glucose metabolism disorder. Arhat fruit glycoside IIa2 has shown the role of regulating blood glucose in many in vitro and in vivo experiments.
Research shows that Arhat fruit glycoside IIa2 can activate AMPK (5 'AMP activated protein kinase) signaling pathway, promote glucose uptake and lipid metabolism, and improve insulin sensitivity. In addition, the compound has an inhibitory effect on sodium glucose cotransporter 2 (SGLT2), reducing renal reabsorption of glucose, promoting urinary glucose excretion, and thus lowering blood glucose levels.
In the pancreatic cell model, Arhat 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. In addition, Arhat fruit glycoside IIa2 may also regulate glucose metabolism and neuroendocrine function by regulating estrogen receptor beta (ESR2) and monoamine oxidase A (MAOA) and other targets, and reduce the complications of diabetes.
Arhat IIa2 has been shown to inhibit proliferation and induce apoptosis in many cancer cell lines. Its anti-cancer mechanism involves the regulation of multiple signaling pathways, including inhibiting the oxidative stress response of tumor cells, inducing apoptosis through the mitochondrial pathway, and blocking the expression of tumor related signaling molecules such as amyloid precursor protein (APP).
In vitro experiments showed that Arhat fruit glycoside IIa2 could inhibit the migration and invasion of tumor cells and reduce the potential of tumor metastasis. Its anti-inflammatory and immune regulatory effects also provide support for its anti-tumor effects. Although the current anti-cancer research focuses on cell and animal models, the safety and multi-target characteristics of Arhat fruit glycoside IIa2 as a natural product make it a potential candidate for anti-cancer drug development.
The pharmacological effect of Arhat IIa2 depends on its interaction with a variety of 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. Arhat fruit glycoside IIa2 plays an anti diabetes role by activating AMPK, improving metabolic disorder.
SGLT2 SGLT2 in the kidneys is responsible for the reabsorption of glucose. Lohanoside IIa2 inhibits SGLT2, promotes urine glucose excretion, and reduces blood sugar.
GCK (Glucokinase): It is a key enzyme that regulates glucose metabolism. Arhat fruit glycoside IIa2 enhances its activity and promotes glucose utilization.
PTPN1 (protein tyrosine phosphatase 1B): It negatively regulates insulin signaling pathway, and Arhat fruit glycoside IIa2 enhances insulin sensitivity by inhibiting PTPN1.
MAOA (monoamine oxidase A): It affects the metabolism of neurotransmitters and may participate in the regulation of diabetes related neuropathy.
ESR2 (estrogen receptor beta): Regulate metabolism and immune function, and Arhat fruit glycoside IIa2 may mediate some biological effects through ESR2.
APP (amyloid precursor protein): It is related to the proliferation and migration of tumor cells. Arhat fruit glycoside IIa2 regulates the expression of APP and plays an anti-tumor role.
The multiple regulation of these targets reflects the potential of Arhat fruit glycoside IIa2 as a multi target drug, which is helpful for its therapeutic application in complex diseases such as diabetes and cancer.
The pharmaceutical evaluation of Arhat IIa2 shows that it has good safety and low risk of side effects. The hERG channel inhibition experiment was negative, reducing the risk of cardiac toxicity; The Ames test showed no mutagenicity, indicating a low risk of genetic toxicity.
However, the low water solubility and high polarity (TPSA) of Arhat fruit glycoside IIa2 may limit its oral bioavailability. Its low blood-brain barrier permeability limits its application in central nervous system related diseases. Improving its pharmacokinetic properties through structural modification or nanocarrier technology in the future will help enhance its clinical application value.
At present, the pharmacokinetic studies on Arhat fruit glycoside IIa2 are relatively limited. Preliminary data show that its distribution in vivo is mainly concentrated in the liver and kidney, and the metabolic pathway may involve glycosyl cleavage mediated by glucoside hydrolase. Its excretion is mainly completed through the kidneys, with a moderate half-life, supporting the design of daily dosing regimens.
As a natural non sugar sweetener, Arhat fruit glycoside IIa2 has been widely used in the food industry, especially as a sugar substitute for diabetes patients and obese people. Its low calorie and high sweetness characteristics meet the needs of modern healthy eating.
In the field of drug development, the anti diabetes, anti-oxidation and anti-cancer activities of Arhat fruit glycoside IIa2 provide a solid foundation for its clinical transformation. In the future, through in-depth mechanism research and pre clinical evaluation, it is expected to develop new multi target therapeutic drugs, especially in the prevention and treatment of diabetes and its complications.
In addition, Arhat fruit glycoside IIa2 can be used in combination with existing drugs to play a synergistic role and reduce drug dose and side effects. The combination of nanotechnology and drug delivery systems will further enhance their bioavailability and targeting, and expand their clinical application scope.
Despite its promising prospects, there is still a need to address issues such as pharmacokinetic limitations, formulation development, and optimization of large-scale production processes. In the future, multi-disciplinary cross cooperation will promote Arhat fruit glycoside IIa2 from laboratory to clinical, and benefit the majority of patients.
As a triterpene glycoside derived from Arhat grosvenorii, its unique chemical structure and multiple biological activities show a wide range of pharmacological potential. Its research achievements in antioxidant, anti diabetes and anti-cancer provide an important example for natural product pharmacology.
Systematic evaluation of its mechanism of action, multi-target regulation, and pharmacological characteristics can help guide its clinical application and new drug development. In the future, with the progress of extraction and purification technology and the deepening of pharmacokinetics research, Arhat 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.
To sum up, Arhat fruit glycoside IIa2 is not only a high-quality natural sweetener, but also a multi-functional medicinal natural product with potential clinical value, which deserves continuous attention and in-depth exploration in basic research and clinical transformation.
