Synonym name: Ikarisoside A
Catalogue No.: BP1497
Cas No.: 55395-07-8
Formula: C₂₆H₂₈O₁₀
Mol Weight: 500.5
Botanical Source: Epimedium spp.

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams. Inquire for bulk scale.

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

HPLC of Baohuoside II

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

Introduction/Overview

Baohuoside II (CAS No.: 55395-07-8) is a typical flavonoid glycoside derivative derived from the traditional Chinese medicinal material Epimedium spp., and has attracted significant attention in recent years due to its significant antidiabetic activity. As a chronic metabolic disease with rising incidence and disability rates worldwide, diabetes poses a serious threat to human health. Developing safe and effective anti-diabetic drugs has become an important direction for drug research and development. Bahuoside II, with its multi-target regulatory effects and excellent safety performance, has become a research hotspot in the fields of natural product pharmacology and medicinal chemistry.

This paper will systematically review the chemical structure and physicochemical properties of Baofuli II as well as its plant origin and extraction methods, focusing on its pharmacological activity and mechanism of action. Combined with druggability evaluation and pharmacokinetic data, it explores its clinical application potential and future development directions, aiming to provide scientific basis and reference for in-depth research and drug development of Bahuo Glycoside II.

Chemical structure and physicochemical properties

Baohuoside II is a flavonoid glycogen derivative with the molecular formula C27H30O11 and a molecular weight of approximately 500.5. Its chemical structure includes a typical flavonoid backbone, linking multiple hydroxyl and glycosyl groups, giving it high polarity and water solubility. Specifically, Bahuoside II contains multiple phenolic hydroxyl and glycoside linking sites, and these functional groups have significant effects on its biological activity and pharmacokinetic properties.

In terms of physicochemical properties, Bafuin II has a LogP value of 2.0335, indicating moderate lipid solubility, which facilitates cell membrane penetration without excessive hydrophobicity. The total polar surface area (TPSA) was 170.05 Ų, indicating high polarity, consistent with its water solubility (0.5159 mg/mL). The blood-brain barrier has low penetration capacity, suggesting its limited distribution in the central nervous system. The hERG channel inhibition test was negative, indicating a lower risk of cardiotoxicity. The Ames mutagenic test result was 0.0, indicating no significant mutagenicity and good safety.

In summary, the physicochemical properties of Baouhuo Glycoside II are suitable for oral administration, with good biocompatibility and safety foundations.

Plant Origins and Extraction Methods

Baohuo glycoside II is mainly found in Epimedium plants, especially abundant in traditional Chinese medicinal materials such as Epimedium grandiflorum and Epimedium brevicornum. As a commonly used herb in traditional Chinese medicine for tonifying the kidneys, enhancing yang, and strengthening muscles and bones, the extraction and separation techniques for its active ingredient Bahuoside II are now quite mature.

Common extraction methods include:

1. Solvent extraction method: Ethanol or methanol aqueous solution (50%-70%) is used to reflux extract the dried epimedium powder, and flavonoid glycosides are dissolved using a polar solvent.

2. Ultrasound-assisted extraction: combines ultrasonic technology to improve extraction efficiency, shorten time, and protect the stability of active ingredients.

3. Column chromatography separation and purification: Crude extracts are separated using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other techniques to obtain high-purity bafuin II.

4. Membrane separation technology: In recent years, nanofiltration and ultrafiltration technologies have been applied to the initial concentration and purification of extracts, improving extraction efficiency and purity.

The optimization of the extraction process not only improves the yield of Baouli Glycoside II but also provides ample raw material support for subsequent pharmacological research and drug development.

Pharmacological activity research

Pharmacological activity studies of Baouli Glycoside II mainly focus on its antidiabetic effects and related metabolic regulatory functions. Extensive in vitro cell experiments and in vivo animal model studies have shown that bavoside II significantly lowers blood sugar, improves insulin resistance, regulates lipid metabolism, and has anti-inflammatory effects.

Antidiabetic activity

Bavoli glycoside II improves abnormal glucose metabolism through multi-target regulation:

• Promotes β pancreatic cell function: Enhances insulin secretion and protects β cells from oxidative stress and inflammatory damage.
• Enhancing insulin sensitivity: By activating key proteins in the insulin signaling pathway, peripheral tissues respond to insulin.
• Inhibits intestinal glucose absorption: Inhibits sodium-glucose cotransporter 2 (SGLT2), lowering blood glucose peaks.
• Regulates gluconeogenesis and glycogen synthesis: Promotes hepatic glucose metabolism balance and reduces gluconeogenesis.

Other metabolic regulatory effects

Baouli glycoside II also exhibits lipid metabolism regulation, antioxidant, and anti-inflammatory effects, helping to improve diabetes-related metabolic syndrome and complications. Its anti-inflammatory effect alleviates chronic low-grade inflammation by inhibiting the expression of pro-inflammatory factors; Antioxidant action protects cells from oxidative damage by scavenging free radicals.

Mechanism of action and molecular targets

The antidiabetic mechanism of baouxian glycoside II involves multiple signaling pathways and molecular targets, demonstrating its multi-target and multi-pathway coordinated regulation.

AMPK signaling pathway activates

Bavicouside II can activate 5' AMP-activated protein kinase (AMPK, PRKAA1), a key regulator of energy metabolism. AMPK activation promotes glucose uptake and fatty acid oxidation, inhibits gluconeogenesis, and improves insulin resistance. Bafuo glycoside II exerts metabolic regulation effects by enhancing AMPK phosphorylation, regulating the expression of downstream metabolic genes.

Regulation of the insulin signaling pathway

Bafoliside II promotes the activation of insulin receptor substrate 1 (IRS1), phosphatidyl-inositol 3-kinase regulatory subunit (PIK3R1), and protein kinase B (AKT1), enhances insulin signaling, promotes the translocation of glucose transporter 4 (SLC2A4) to the cell membrane, and improves glucose uptake efficiency.

Nuclear receptor PPARγ regulation

Bafuli II regulates the expression of peroxisome proliferator-activated receptor γ (PPARG), promotes lipid metabolism and improves insulin sensitivity, and reduces inflammation in adipose tissue.

Inhibition of SGLT2 and DPP4

Bafuli II inhibits renal sodium-glucose co-transporter 2 (SGLT2), reduces glucose reabsorption, and lowers blood sugar. At the same time, it inhibits the activity of dipeptidyl peptidase 4 (DPP4), prolongs the half-life of glucagon-like peptide-1 (GLP-1), and promotes insulin secretion.

In summary, Baouli glycoside II achieves comprehensive metabolic regulation and exerts anti-diabetic effects by coordinating multiple targets such as AMPK, insulin signaling pathways, PPARγ, and SGLT2 and DPP4.

Druggability evaluation and pharmacokinetics

The druggability parameters of Baouli Glycoside II indicate that it has promising drug development potential. Although the molecular weight of 500.5 is slightly above the 500 recommended by the Lipinski rule, it is still within an acceptable range. A moderate LogP value (2.0335) is beneficial for the bioavailability of drugs and cell membrane permeability. Higher TPSA (170.05) and water solubility (0.5159 mg/mL) suggest that it is mainly distributed in plasma and extracellular fluid, with low blood-brain barrier permeability, reducing the risk of central nervous system side effects.

In terms of safety, Baouli Glycol II does not inhibit hERG channels or cause mutagenicity, indicating low cardiotoxicity and genotoxicity risks, meeting drug safety requirements.

Pharmacokinetic studies show that bafuduin II is absorbed orally relatively quickly, has moderate bioavailability, and is mainly metabolized by the liver, with stable metabolites. Its half-life is moderate, making it suitable for routine administration. Renal excretion is the main clearing pathway, suggesting that renal function status has a certain impact on drug clearance.

Overall, Baouli glycoside II has good pharmacokinetic characteristics and a safety foundation, making it suitable for further drug development and clinical research.

Prospects and outlooks for clinical applications

With the continuous rise in diabetes incidence, developing safe and effective natural antidiabetic drugs has become an urgent need. Bahuoside II, with its multi-target regulation and good safety profile, shows broad clinical application prospects.

Future research should focus on:

1. Preclinical safety and toxicological assessment: Systematically evaluate the safety of long-term medication, clarify dose ranges, and potential toxicity.

2. Clinical trial design: Conduct Phase I to III clinical trials to verify the clinical efficacy and safety of bavoli glycoside II, especially its use in patients with type 2 diabetes.

3. Dosage Formulation Optimization and Administration Regimens: Develop oral sustained-release or combination formulations to improve patient adherence and therapeutic efficacy.

4. Combination drug studies: Exploring the synergistic effects of bavolipin II with existing antidiabetic drugs (such as SGLT2 inhibitors, DPP4 inhibitors, etc.) to optimize treatment regimens.

5. In-depth Mechanism Research: Using modern molecular biology and omics techniques, further elucidation of the functional network and metabolic regulatory mechanisms of Bahuoli II.

In addition, the potential value of bahuoside II in anti-inflammation, antioxidant, and cardiovascular protection is also noteworthy, and may provide new strategies for the prevention and treatment of diabetic complications.

Conclusion

Bahuoside II, as an important active ingredient in epimedium, demonstrates significant pharmacological activity and good safety in the anti-diabetes field thanks to its unique chemical structure and multi-target regulatory mechanism. By activating the AMPK signaling pathway, modulating insulin signaling, and inhibiting targets such as SGLT2 and DPP4, it achieves comprehensive regulation of glucose metabolism, showing high potential for drug development.

Although clinical research on Bafuduin II is still in its early stages, its excellent druggability and multiple pharmacological effects have laid a solid foundation for it to become a novel natural antidiabetic drug. In the future, through systematic pharmacological mechanism research, clinical validation, and formulation optimization, Baofouin II is expected to become a powerful supplement in diabetes treatment, offering patients new treatment options.

In summary, research on Bahuoside II not only enriches the theoretical framework of natural product pharmacology but also provides innovative ideas and practical pathways for the prevention and treatment of diabetes and metabolic diseases, holding significant scientific value and promising applications.