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Synonym name: Broussochalcone B
Catalogue No.: BP0238
Cas No.: 28448-85-3
Formula: C20H20O4
Mol Weight: 324.376
Botanical Source: Broussonetia papyrifera
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.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
HPLC of Bavachalcone
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
77.7600
3.7000
3.3000
Low
No
No
No
No
No
No
Psoralea Chalcone (CAS No.: 28448-85-3) is a natural chalcone compound derived from the traditional Chinese medicine Psoralea corylifolia L. As an important secondary metabolite of plant flavonoids, psoralea chalcone has attracted widespread attention in pharmacology and natural product chemistry due to its multi-target and multi-pathway bioactivity. In recent years, psoralea chalcone has demonstrated significant pharmacological potential in anticancer, anti-inflammation, neuroprotection, and bone metabolism regulation, especially in the mechanisms of inducing tumor cell apoptosis, autophagy, and regulating inflammatory responses. In addition, the regulation of atherosclerosis-related targets by psoralea chalcone also suggests its promising application in cardiovascular disease prevention and treatment. This paper provides a systematic review of the chemical structure and physicochemical properties of Psoralea chalcone, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and clinical application prospects, aiming to provide theoretical basis and reference for in-depth research and new drug development of this natural product.
Psoralea chalcone belongs to the chalcone class of compounds, with a molecular formula of C20H20O5 and a molecular weight of 324.37. Its structural features include a typical α, β-unsaturated carbonyl system, connecting two aromatic rings, containing multiple hydroxyl substituents, which imparts strong biological activity. Psoralea chalcone has a LogP value of 3.7, indicating moderate lipid solubility, which facilitates cell membrane penetration. Its polar surface area (TPSA) is 77.76 Ų, and it has 4 hydrogen bond acceptors, indicating that it possesses certain hydrophilicity and binding ability in intermolecular interactions. According to pharmacokinetic predictions, psoralea chalcone has low blood-brain barrier permeability, low risk of hepatotoxicity, and no significant cardiotoxicity or hERG channel inhibition. Ames-induced mutagenic test results are negative, indicating good safety and promising drug potential.
Psoralea chalcone is mainly found in the roots and seeds of Psoralea corylifolia L. Psoralea, as a traditional Chinese medicinal herb, is widely used to treat osteoporosis, skin diseases, and immune-related conditions. Common methods for extracting psoralea chalcone include solvent extraction, liquid-liquid distribution, and chromatographic separation. Generally, ethanol or methanol is used as extraction solvents, and extraction efficiency is improved through ultrasound-assisted extraction or reflux extraction. The crude extract is purified using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other techniques, ultimately yielding high-purity psoralea chalcone. In recent years, supercritical fluid extraction and membrane separation technologies have also been introduced to improve extraction efficiency and purity, reduce the use of organic solvents, and align with the concept of green chemistry.
Psoralea chalcone exhibits significant antiproliferative and pro-apoptotic effects across various tumor cell lines. Research shows that psoralea chalcone can induce autophagy and apoptosis in HepG2 liver cancer cells, inhibit cell proliferation, suggesting its potential antitumor activity. Its anti-cancer mechanism involves regulation of multiple signaling pathways, including inhibiting the PI3K/Akt pathway, activating AMPK signaling, and modulating the expression of Bcl-2 family proteins to promote programmed cell death. Additionally, psoralea chalcone can regulate the NF-κB signaling pathway, weaken the inflammatory microenvironment of tumor cells, and enhance its anti-cancer effects.
Neuroinflammation is the pathological basis of various neurological diseases. Psoralea chalcone exerts significant anti-inflammatory effects by inhibiting the NF-κB signaling pathway, reducing the expression of pro-inflammatory factors such as TNF-α and IL-1β. Animal model studies have shown that psoralea chalcone can improve depressive-like behaviors, suggesting its potential in antidepressant treatment. This action may be closely related to its regulation of neuroinflammation and neurotransmitter balance.
Psoralea chalcone interferes with the ERK and Akt signaling pathways, inhibiting osteoclast differentiation and activity, and reducing bone loss during bone resorption. It can also downregulate the expression of transcription factors c-Fos and NFATc1, both key regulators of osteoclast formation, demonstrating the potential of psoralea chalcone in the prevention and treatment of osteoporosis and related bone metabolic diseases.
Psoralea chalcone regulates various atherosclerosis-related targets such as AMPK, EHMT2, MCL1, BCL2, RECQ1, LOX-1, ABCA1, and IDO1. By activating the AMPK signaling pathway, psoralea chalcone promotes lipid metabolism and energy homeostasis, suppresses inflammatory responses, and slows the progression of atherosclerosis. At the same time, its inhibitory effect on LOX-1 receptors reduces oxidized low-density lipoprotein (oxLDL)-mediated vascular endothelial injury, protecting vascular function.
Psoralea chalcone showed significant inhibitory effects on baculovirus β-secretase 1 (BACE-1) expressed in vitro, suggesting its potential application value in neurodegenerative diseases such as Alzheimer's disease. In addition, psoralea chalcone also exhibits certain antioxidant and immunomodulatory activities, further enriching its pharmacological spectrum.
The multi-target mechanism of psoralea chalcone forms the basis of its pharmacological activity. Its main mechanisms of action include:
Promoting autophagy and apoptosis: Psoralea chalcone activates the AMPK signaling pathway, inducing HepG2 cell autophagy while regulating the expression of Bcl-2 family proteins, promoting mitochondrial-mediated apoptosis.
Inhibition of NF-κB signaling pathway: NF-κB is a key regulator of inflammation and immune responses. Psoralein chalcone exerts anti-inflammatory and antidepressant effects by blocking its activation and reducing pro-inflammatory cytokine expression.
Regulating ERK and Akt signaling pathways: Psoralein chalcone blocks osteoclast differentiation and activation by inhibiting these two signaling pathways, reducing bone resorption.
Regulates transcription factor expression: downregulates c-Fos and NFATc1 expression, inhibiting osteoclast formation.
Regulation of atherosclerosis-related targets: activation of AMPK, regulation of lipid metabolism, and inflammatory response; Inhibits LOX-1-mediated oxidative stress; Regulating ABCA1 promotes cholesterol excretion and slows plaque formation.
Inhibition of BACE-1 activity: blocking abnormal cleavage of β-amyloid protein precursors may slow the pathological progression of Alzheimer's disease.
The synergistic effect of these mechanisms allows psoralea chalcone to demonstrate good therapeutic potential across various disease models.
The druggability parameters of psoralea chalcone indicate that it has good potential for drug development. The molecular weight of 324.37 complies with the Lipinski rule, with a moderate LogP value of 3.7, which facilitates cell membrane permeability. TPSA is 77.76, indicating moderate molecular polarity and favorable bioavailability. It has 4 hydrogen bond receptors, supporting effective binding to target proteins. The blood-brain barrier has a relatively low penetration capacity, suggesting that its direct effect in the central nervous system may be limited, but this also reduces the risk of central toxicity.
Toxicological evaluation showed that psoralea chalcone had a low risk of hepatotoxicity, no significant cardiotoxicity, and no hERG channel inhibition. The Ames test was negative, indicating high safety. Pharmacokinetics: Although systematic studies on metabolism and bioavailability in vivo are still insufficient, studies have shown good oral absorption, stable liver metabolism, and excretion mainly via the kidneys and bile. In the future, further in vivo pharmacokinetics, metabolic kinetics, and toxicology studies are needed to lay the foundation for clinical application.
Psoralea chalcone, as a versatile natural product, has broad clinical application potential. Its anti-proliferative and pro-apoptotic effects in tumor treatment provide important clues for the development of novel anticancer drugs. Especially in solid tumors such as liver cancer, psoralen chalcone may serve as an adjunct therapy to enhance treatment efficacy and reduce chemotherapy toxicity side effects.
In the field of neurological diseases, psoryl chalcone has anti-neuroinflammatory and antidepressant effects and is expected to become a new candidate drug for treating depression and neurodegenerative diseases. Its inhibitory effect on BACE-1 provides new ideas for drug development for Alzheimer's disease.
Additionally, Psoralea chalcone has potential in regulating bone metabolism and preventing and treating atherosclerosis, suggesting its potential for comprehensive treatment of osteoporosis and cardiovascular diseases. It has good safety and druggability, making it suitable for further preclinical and clinical research.
Future research should focus on optimizing the pharmacokinetic properties of psoralea chalcone in vivo, developing formulations, and combining drug strategies, while deeply analyzing its molecular mechanisms to promote clinical translation. Combining modern medicinal chemistry and pharmacological technologies, psoralea chalcone is expected to become an important representative in the development of natural product drugs.
Psoralea chalcone, a natural chalcone compound with multiple biological activities, demonstrates a wide range of pharmacological effects and good safety. Its research achievements in anti-cancer, anti-inflammation, neuroprotection, and bone metabolism regulation provide valuable scientific evidence for the field of natural product pharmacology. Although research on its in vivo pharmacokinetics and clinical applications is still in its early stages, psoralea chalcone has high drug potential due to its unique molecular structure and multi-target regulatory capabilities. In the future, systematic pharmacodynamics, toxicology, and clinical studies are expected to promote psoralea chalcone as a new natural drug or drug-leading compound, providing new strategies and options for the treatment of related diseases.
Shenshuai
Wenjing
Hedandan
