Product name: Lactiflorin
Synonym name:
Catalogue No.: BP4407
Cas No.: 1361049-59-3
Formula: C₂₃H₂₆O₁₀
Mol Weight: 462.451
Botanical Source:
Type of Compound:

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 Lactiflorin

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

Introduction/Overview

Lactiflorin, CAS number 1361049-59-3, is a monoterpene glycoside natural product isolated from plants of the Peony genus. As an organic heteropolycyclic compound, peony neoglycosides have a unique chemical structure and diverse biological activities, especially showing significant pharmacological effects in kidney protection and anti-inflammatory fields. In recent years, with in-depth research into the pharmacological mechanisms of natural products, peony neoglycosides have gradually become one of the hotspots in natural drug development due to their multi-target regulatory capabilities and superior safety. This paper will systematically review the chemical structure and physicochemical properties of peony neoglycosides, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, and explore their clinical application prospects and research prospects, aiming to provide scientific basis for in-depth research and clinical translation of this compound.

Chemical structure and physicochemical properties

The chemical formula of peony neoglycoside is C23H26O10, with a molecular weight of 462.4510. Its structure belongs to the monoterpene glycoside class, containing an organic heteropenate structure, specifically including bridging compounds, benzoates, cyclic ketones, and cyclochlorone functional groups. These structural features give it strong biological activity and good water solubility (0.4544), with a LogP value of 0.3479, indicating moderate lipophilicity, which is beneficial for distribution in the body but has a lower blood-brain barrier penetration ability. Its topological pole surface area (TPSA) is 140.98 Ų, indicating high polarity, which may affect membrane permeability and oral absorption. The hERG channel inhibition test results were negative, indicating that peony neoglycoside carries a relatively low cardiotoxicity risk; The Ames test value was 1.2, indicating low mutagenicity and good safety.

Plant Origins and Extraction Methods

Peony neoglycosides are mainly found in plants of the Peony genus, especially in some traditional Chinese medicinal materials such as White Peony (Paeonia lactiflora Pall.), where their content is relatively abundant. Its extraction usually uses solvent extraction methods, with commonly used solvents including ethanol, water, or their mixed solvent systems. The extraction process generally includes the following steps:

1. Raw material crushing: Dry peony rhizomes are ground into fine powder to increase the solvent contact area.
2. Leaching: Use 70%-95% ethanol or water for reflux extraction, temperature controlled at 60-80°C, for about 2-4 hours.
3. Filtration and concentration: After filtering the extract, vacuum concentration is used to remove the solvent.
4. Separation and purification: Further purification of peony neoglycosides is performed using liquid chromatography (such as high-performance liquid chromatography (HPLC) or column chromatography techniques.

In recent years, ultrasound-assisted extraction and microwave-assisted extraction technologies have also been applied to the extraction of peony neoglycosides, significantly improving extraction efficiency and purity. In addition, the application of modern separation technologies such as countercurrent chromatography and preparative HPLC provides effective means to obtain high-purity peony neoglycosides.

Pharmacological activity research

The pharmacological activity of peony neoglycosides mainly focuses on kidney protection and anti-inflammatory effects. Numerous in vivo and in vitro experiments have shown that peony neoglycoside can significantly reduce kidney damage, improve kidney function indicators, suppress inflammatory responses, and reduce tissue inflammatory damage.

Kidney protective effects

Peony neoglycoside has shown protective effects in various kidney disease models, including acute kidney injury (AKI), chronic kidney disease (CKD), and diabetic nephropathy (DKD). Its mechanism of action involves antioxidant, anti-inflammatory, anti-fibrotic, and apoptosis regulation, among other aspects. For example, in the renal ischemia-reperfusion injury model, peony neoglycoside can reduce the formation of oxidative stress products, inhibit apoptosis of renal tubular epithelial cells, and promote renal tissue repair. In the diabetic nephropathy model, peony neoglycoside alleviates glomerular sclerosis and basement membrane thickening by regulating glycolipid metabolism and inhibiting inflammatory factor expression.

Anti-inflammatory effects

The anti-inflammatory effects of peony neoglycosides have been validated in various inflammation models. It can significantly downregulate the expression of pro-inflammatory cytokines such as IL-6 and TNF-α, inhibit activation of inflammatory signaling pathways, and reduce the release of inflammatory mediators. In vitro cell experiments showed that peony neoglycoside inhibits the activation of macrophages and other immune cells, reducing the expression of genes related to inflammation responses.

In addition, peony neoglycosides also show certain alleviating effects on disease models such as neuroinflammation, arthritis, and intestinal inflammation, suggesting broad anti-inflammatory potential.

Mechanism of action and molecular targets

The multi-target mechanism of peony neoglycosides forms the basis of its pharmacological activity. By regulating multiple signaling pathways and key molecules, peony neoglycosides exert their renal protective and anti-inflammatory effects.

Key molecular targets

• IL-6 (interleukin-6): Peony neoglycosides inhibit IL-6 expression, reducing the transmission of pro-inflammatory signals and alleviating inflammatory responses.
• STAT3 (Signal Transduction and Transcription Activator 3): As a key transcription factor in the IL-6 signaling pathway, inhibition of STAT3 helps block inflammatory cascades.
• CASP1 (caspase 1): Involved in inflammasome activation, peony neoglycoside reduces the maturation and release of pro-inflammatory cytokines by inhibiting CASP1.
• TRPV1 and TRPA1 (transient receptor potential channels): regulate pain and inflammation responses; peony neoglycosides help alleviate inflammation-related pain by modulating these two ion channels.
• PTGS1 and PTGS2 (cyclooxygenase-1 and -2): involved in the synthesis of inflammatory mediators prostaglandins; peony neoglycosides inhibit their activity and reduce the formation of inflammatory mediators.
• TNF (tumor necrosis factor): As an important pro-inflammatory factor, peony neoglycosides reduce inflammatory responses by downregulating TNF expression.
• NOS2 (induced nitric oxide synthase): regulates inflammation-related nitric oxide production; peony neoglycosides inhibit NOS2 expression and reduce oxidative stress.
• NFKB1 (nuclear factor κB subunit): As a core transcription factor for inflammatory signaling, peony neoglycosides inhibit NFKB1 activation and block inflammatory signaling pathways.

Signal path regulation

Peony neoglycosides exert anti-inflammatory effects by inhibiting the IL-6/STAT3 and NF-κB signaling pathways, reducing the expression and release of pro-inflammatory factors. At the same time, peony neoglycosides regulate the TRPV1/TRPA1 channel, alleviating neuroinflammation and pain. Its inhibitory effect on CASP1 reduces the maturation of cytokine mediated by inflammasomes, further alleviating inflammatory responses.

Additionally, peony neoglycoside promotes antioxidant enzyme expression by regulating oxidative stress-related signaling pathways (such as Nrf2/ARE), protecting kidney cells from oxidative damage.

Druggability evaluation and pharmacokinetics

The druggability parameters of peony neoglycosides indicate that it has good potential for drug development. The molecular weight was moderate (462.45 Da), with a LogP value of 0.3479, indicating good hydrolipid balance, which is beneficial for distribution in the body but has low blood-brain barrier permeability, reducing the risk of adverse reactions to the central nervous system. A high TPSA value (140.98 Ų) suggests strong polarity, which may affect oral absorption, but bioavailability can be optimized through structural modification or formulation techniques.

In terms of safety, the hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity; Ames trial results indicate that it has low mutagenicity and good genetic safety.

Pharmacokinetic studies show that peony neoglycosides are absorbed orally quickly, with a shorter peak plasma concentration, but bioavailability is limited by their polarity and water solubility. In the body, it is mainly metabolized by the liver, whose metabolic products are mostly water-soluble complexes that are easily excreted. Moderate half-life, suitable for daily administration. Future research needs to further clarify its metabolic enzyme system and drug interaction characteristics.

Prospects and outlooks for clinical applications

Peony neoglycosides, with their remarkable renal protective and anti-inflammatory activities, have broad clinical application prospects. Its potential therapeutic value in diabetic nephropathy, acute and chronic kidney injury, and various inflammatory diseases has attracted significant attention in drug development.

Future clinical research should focus on the following aspects:

1. Safety and efficacy evaluation: Systematic Phase I and Phase II clinical trials were conducted to evaluate the safety, tolerability, and preliminary efficacy of peony neoglycosides.
2. Dosage form development and route optimization: Given its high polarity, develop formulations suitable for oral or other administration methods to improve bioavailability.
3. Combination therapy strategy: Explore the synergistic effects of peony neoglycosides with existing nephroprotective or anti-inflammatory drugs to optimize treatment plans.
4. In-depth Mechanism Research: Using multi-omics techniques and systems biology approaches, further elucidating its multi-target mechanisms and uncovering potential indications.
5. Biomarker development: Identify biomarkers related to the efficacy of peony neoglycosides to guide personalized medication.

Moreover, the structural diversity and good safety profile of peony neoglycosides provide a solid foundation for chemical modification and derivative development. In the future, structural optimization can enhance their efficacy and pharmacokinetic properties, promoting the transformation of natural products into innovative drugs.

Conclusion

Peony neoglycosides, a monoterpene glycoside derived from plants of the Peony genus, have a unique chemical structure and significant kidney protection and anti-inflammatory activities. Through multi-target and multi-signal pathway regulation, it exerts a wide range of pharmacological effects, offering good safety and druggability. With the ongoing advancement of pharmacological research on natural products, peony neoglycosides are expected to become a new candidate drug for treating kidney diseases and inflammation-related conditions. However, current research on its clinical application is still in its early stages, urgently requiring systematic pharmacokinetic, toxicological, and clinical trial data support. In the future, through multidisciplinary collaboration and technological innovation, the prospects for drug development and clinical translation of peony neoglycosides are broad and worthy of continued attention and in-depth exploration.