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Product name: Albiflorin
Synonym name:
Catalogue No.: BP0134
Cas No.: 39011-90-0
Formula: C23H28O11
Mol Weight: 480.466
Botanical Source: Paeonia lactiflora Pall.
Physical Description:
Type of Compound: Monoterpenoids
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.
Description:
Albiflorin has anti-inflammatory, and antidepressant-like effects. Albiflorin may reduce or prevent osteoblast degeneration in osteoporosis, and may promote the recovery of bone marrow hemopoietic function in a myelosuppressed mouse model, it has neuroprotective effect on primary hippocampal cells against β-amyloid induced toxicity.
References:
Fitoterapia. 2013 Sep;89:33-41.
Protective effect of albiflorin against oxidative-stress-mediated toxicity in osteoblast-like MC3T3-E1 cells.
Albiflorin isolated from Paeoniae Radix was investigated for its ability to protect against antimycin A-induced osteoblast toxicity in the MC3T3-E1 cell line.
METHODS AND RESULTS:
MC3T3-E1 cells showed significantly reduced viability, increased apoptosis and lactate dehydrogenase release, elevated ROS/RNS levels, and decreased mitochondrial function after exposure to antimycin A. Pretreatment with Albiflorin reversed the loss of cell viability in antimycin A-treated cultures. Similarly, pretreatment with Albiflorin before antimycin A resulted in decreased apoptosis and lactate dehydrogenase release, decreased ROS/RNS levels, and increased mitochondrial function compared to antimycin A-treated cultures. In addition, Albiflorin increased the mineralization reduced by antimycin A. Albiflorin reduced antimycin A-induced mitochondrial cytochrome c loss and cardiolipin peroxidation, conferring protection against ROS. These results confirmed the crucial role of cytochrome c and cardiolipin in the underlying mechanistic action of Albiflorin. Therefore, the results suggest that Albiflorin enhances mitochondrial function to suppress antimycin A-induced oxidative damage via the preservation of cytochrome c and cardiolipin.
CONCLUSIONS:
All of these data indicate that Albiflorin may reduce or prevent osteoblast degeneration in osteoporosis.
Evid-based. Compl. Alt. , 2016, 2016(15):1-8.
Paeoniflorin and Albiflorin Attenuate Neuropathic Pain via MAPK Pathway in Chronic Constriction Injury Rats
Neuropathic pain remains as the most frequent cause of suffering and disability around the world. The isomers paeoniflorin (PF) and Albiflorin (AF) are major constituents extracted from the roots of Paeonia (P.) lactiflora Pall. Neuroprotective effect of PF has been demonstrated in animal models of neuropathologies. However, only a few studies are related to the biological activities of AF and no report has been published on analgesic properties of AF about neuropathic pain to date.
METHODS AND RESULTS:
The aim of this study was to compare the effects of AF and PF against CCI-induced neuropathic pain in rat and explore the underlying mechanism. We had found that both PF and AF could inhibit the activation of p38 mitogen-activated protein kinase (p38 MAPK) pathway in spinal microglia and subsequent upregulated proinflammatory cytokines (interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α)). AF further displayed remarkable effects on inhibiting the activation of astrocytes, suppressing the overelevated expression of phosphorylation of c-Jun N-terminal kinases (p-JNK) in astrocytes, and decreasing the content of chemokine CXCL1 in the spinal cord.
CONCLUSIONS:
These results suggest that both PF and AF are potential therapeutic agents for neuropathic pain, which merit further investigation.
HPLC of Albiflorin
NMR of Albiflorin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
196.4800
-1.5000
-1.5000
Low
No
No
No
No
No
No
No
Albiflorin is an important natural monoterpene glycoside, first isolated from the roots of the traditional Chinese medicine Paeonia lactiflora Pall. As one of the main active ingredients in peony, peony lactone glycosides have attracted widespread attention in the field of natural product pharmacology in recent years due to their unique chemical structure and diverse bioactivity. Research shows that peony lactone glycosides not only have significant neuroprotective effects but also exhibit multiple pharmacological effects including anti-inflammation, antioxidant, antidepressant-like, and bone metabolism regulation. Its potential application value in neurodegenerative diseases, osteoporosis, and inflammation-related diseases makes it an important candidate molecule for natural drug development and new drug research.
This paper aims to systematically review the chemical structure and physicochemical properties of peony lactone glycosides, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics. Combined with its related disease targets, it explores its clinical application prospects and future development directions, providing a theoretical foundation and reference for further research and development.
Peony lactone glycoside (CAS No.: 39011-90-0) is a monoterpene glycoside compound with a molecular formula of C23H28O11 and a molecular weight of approximately 480.46. Its structure includes the β-D-glucoside portion, secondary alcohol groups, bridging structure, benzoate, γ-lactone ring, and monoterpene skeleton, reflecting the complex structural characteristics of natural products. This molecule has 11 hydrogen bond acceptors and is highly polar, with a calculated topological pole surface area (TPSA) of 196.48 Ų and a LogP value of about -1.5, indicating good water solubility but low lipid solubility.
From a molecular structure perspective, the γ-lactone ring and benzoate group of peony lactone provides a key chemical basis for its biological activity, while the glycoside component influences its pharmacokinetic properties and in vivo distribution. Although a low LogP indicates insufficient lipid solubility, studies confirm that peony lactone glycosides can cross the blood-brain barrier, suggesting that their molecular structure may enable effective distribution in the central nervous system through specific transport mechanisms or metabolic transformation.
In terms of physicochemical properties, peony lactone glycosides do not show significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition. Ames mutagenic test results are negative, indicating good safety and promising drug potential.
Peony lactoside is mainly found in the root of peony (Paeonia lactiflora Pall.) and is one of the important components of total peony glycosides. As a traditional Chinese medicinal material, peony is widely used in clinical TCM and has effects such as activating blood circulation and removing blood stasis, relieving pain, and regulating immunity. The content of peony lactone glycosides is influenced by variety, harvest time, and growing environment.
The extraction method mostly uses solvent extraction combined with separation and purification technology. The commonly used extraction solvents are ethanol or methanol aqueous solutions, with extraction processes including hot reflux extraction, ultrasound-assisted extraction, and microwave-assisted extraction. The extract is purified by concentration, liquid-liquid distribution, and column chromatography (such as silica gel columns and reversed-phase C18 columns), and finally performed qualitative and quantitative analysis by high-performance liquid chromatography (HPLC).
In recent years, supercritical fluid extraction and membrane separation technologies have also been applied to the extraction and purification of peony lactone glycosides, improving extraction efficiency and purity, reducing the use of organic solvents, and aligning with the concept of green chemistry. Moreover, research on biosynthetic pathways provides a theoretical basis for large-scale production of peony lactone glycosides through future biosynthesis or genetic engineering methods.
Peony lactone glycosides, as monoterpene glycosides capable of crossing the blood-brain barrier, exhibit significant neuroprotective activity. Multiple in vitro and in vivo experiments have shown that peony lactone glycosides can counteract β-amyloid (Aβ)-induced neurotoxicity, alleviate hippocampal neurons' apoptosis and dysfunction, suggesting their potential value in neurodegenerative diseases such as Alzheimer's. Its neuroprotective effects are closely related to antioxidant, anti-inflammatory, and neurotransmitter system regulation.
Peony lactone glycosides can significantly inhibit the release of inflammatory mediators such as tumor necrosis factor α (TNF-α), interleukin-6 (IL-6), and nitric oxide (NO), thereby reducing inflammatory responses. Its anti-inflammatory mechanism involves inhibition of the nuclear factor κB (NF-κB) signaling pathway and downregulation of the expression of inflammation-related enzymes such as COX-2 and iNOS. In terms of antioxidant properties, peony lactone glycosides enhance intracellular antioxidant enzyme activity (such as superoxide dismutase SOD, glutathione peroxidase GSH-Px), reduce the generation of reactive oxygen species (ROS), and protect cells from oxidative damage.
Clinical and animal model studies have shown that peony lactone glycosides have antidepressant-like activity. It may improve neuronal function and neuroplasticity by regulating neurotransmitter levels in the central nervous system (such as serotonin, 5-HT, dopamine DA, and norepinephrine NE), thereby alleviating depressive symptoms. In addition, peony lactone glycosides help exert their antidepressant effects by inhibiting neuroinflammation.
The study found that peony lactone glycosides can reduce osteoblast degeneration and promote bone formation in osteoporosis models. Its restoration of hematopoietic function in bone marrow suppression mouse models also indicates its positive role in regulating the bone marrow microenvironment. This effect may be related to its anti-inflammatory and antioxidant capabilities, improving the bone metabolic microenvironment and promoting the survival and function of bone cells.
In addition, peony lactone glycosides also show certain pain-relieving effects, possibly by regulating inflammatory responses and neural pathways. Its multi-target and multi-mechanism pharmacological properties offer broad possibilities for its application in various diseases.
The pharmacological effects of peony lactone glycosides involve multiple signaling pathways and molecular targets, reflecting their multi-target regulation characteristics.
Peony lactone glycosides reduce neuroinflammation and oxidative stress by inhibiting β-amyloid-induced neurotoxicity, protecting neurons. Its mechanism involves inhibition of the NF-κB signaling pathway, reducing the release of pro-inflammatory cytokines, while activating the antioxidant enzyme system to lower ROS levels. In addition, peony lactone glycosides can regulate neurotransmitter metabolism and improve neuronal function.
Peony lactone glycosides inhibit COX-2 and iNOS activity by downregulating the expression of inflammatory mediators such as TNF-α, IL-6, and nitric oxide, thereby reducing inflammatory responses. Its inhibition of the NF-κB pathway is one of the key mechanisms, blocking inflammatory signal transduction and reducing the activation and infiltration of inflammatory cells.
The role of peony lactone glycosides in osteoporosis may be related to regulating osteoblast apoptosis and improving the bone marrow microenvironment. Related targets include bone metabolism regulators and apoptosis-related proteins. Additionally, in bone marrow suppression models, peony lactone glycosides promote the restoration of bone marrow hematopoietic function, suggesting that they may play a role by regulating the microenvironment of bone marrow mesenchymal cells and hematopoietic stem cells.
According to database analysis, peony lactone glycosides have potential associations with various sarcoma-related targets, including tyrosinase (TYR), ATP binding cassette transporter B1 (ABCB1), APEX nucleic acid endonuclease (APEX1), RECQL helilase, phosphatidylinositol phosphatase SYNJ2, selector P (SELP), acidic α-glucosidase (GAA), estrogen receptor α (ESR1), and lectin LGALS1. These targets involve multiple biological processes such as DNA repair, apoptosis, drug resistance, and cell adhesion, suggesting that peony lactone glycosides have potential multi-target regulatory effects in tumor treatment.
The druggability parameters of peony lactone glycosides indicate that it has certain potential for drug development. Its molecular weight is 480.46, slightly above the ideal range for traditional small molecule drugs, but still within acceptable limits. The LogP value was -1.5, indicating strong hydrophilicity, which may affect oral bioavailability, but also benefits in vivo distribution and blood-brain barrier penetration.
The topological pole surface area (TPSA) is 196.48 Ų. The higher polarity may limit its passive diffusion, but the study confirms its ability to penetrate the blood-brain barrier, suggesting a possible active transport mechanism. The number of hydrogen bond receptors is 11, indicating strong intermolecular interaction capability and facilitating binding to targets.
In terms of safety, peony lactone glycosides showed no hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and the Ames mutagenic test was negative, indicating good safety. Pharmacokinetic studies have shown that peony lactone glycosides have good stability and metabolic properties in the body, effectively distributing to the central nervous system.
However, the oral absorption rate and bioavailability of peony lactone glycosides still need further optimization. In the future, their pharmacokinetic performance can be improved through structural modification, drug carrier systems (such as nanoparticles and liposomes), and delivery routes.
Peony lactone glycosides, with their multiple pharmacological activities and excellent safety, show broad clinical application prospects. Its neuroprotective effects make it a potential candidate for treating neurodegenerative diseases such as Alzheimer's and Parkinson's. Its anti-inflammatory and antioxidant properties give it potential applications in inflammatory diseases and immune regulation. Antidepressant effects offer new ideas for adjunctive treatment of neuropsychiatric disorders.
Additionally, peony lactone glycosides regulate bone metabolism in osteoporosis and bone marrow suppressive diseases, suggesting their value in orthopedics and hematological diseases. Its potential role in sarcoma-related targets also provides new research directions for tumor treatment.
Future research should focus on:
Through multidisciplinary collaboration, peony lactone glycosides are expected to become a major breakthrough in the field of natural product pharmacology, providing new drug options for the treatment of related diseases.
Peony lactone glycosides, as a typical natural monoterpene glycoside, demonstrate significant pharmacological potential in neuroprotection, anti-inflammatory, antidepressant, and bone metabolism regulation due to their unique chemical structure and diverse biological activities. It is safe and has certain drug-making advantages, especially showing broad application prospects in areas such as neurological diseases and osteoporosis.
Although significant progress has been made in peony lactone glycosides, further elucidation of molecular mechanisms, optimization of pharmacokinetic properties, and advancement of clinical translation are still needed. In the future, with the continuous development of modern pharmacology, molecular biology, and medicinal chemistry technologies, peony lactone glycosides are expected to become an important representative of natural product drug development, contributing new strength to human health.
Shenshuai
Wenjing
Hedandan
