Product name: Chrysin
Synonym name: Chrysinic acid
Catalogue No.: BP0346
Cas No.: 480-40-0
Formula: C₁₅H₁₀O₄
Mol Weight: 254.241
Botanical Source: Oroxylum indicum（L.）Vent.
Physical Description:
Type of Compound: Flavonoids

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 Chrysin

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

Introduction/Overview

Natural products have long been an important source of innovative drug discovery, among which flavonoids have attracted much attention due to their broad biological activity and low toxicity. Chrysin, also known as 5,7-dihydroxyflavone, is a typical dihydroxyflavone compound with a CAS number of 480-40-0. It was initially recognized for its presence in natural products such as propolis and exhibited various pharmacological activities including antioxidant, anti-inflammatory, and anti-tumor effects. In recent years, with the in-depth understanding of the mechanism of complex diseases such as tumors and neurodegenerative diseases, the potential of chrysin as a multi-target regulator has become increasingly prominent. Especially in the research of hormone related tumors such as breast cancer, its characteristics as an estrogen blocker have aroused widespread interest in the pharmacological community. This article aims to systematically review the chemical properties, plant sources, pharmacological activities, molecular mechanisms of action, pharmacological evaluation, and clinical application prospects of poplar extract, in order to provide comprehensive scientific references for the in-depth development and transformation research of this natural product.

Chemical structure and physicochemical properties

The molecular formula of poplar extract is C ₁₅ H ₁₀ O ₄, with a molecular weight of 254.2410 g/mol. Its basic skeleton is flavonoids (2-phenylchromenone), with one phenolic hydroxyl group at each of the 5th and 7th positions of the A ring, which is the key pharmacophore for its antioxidant activity. This structure makes it a representative member of dihydroxyflavones and 7-hydroxyflavonols.

In terms of physical and chemical properties, Baiyangsu exhibits typical flavonoid compound characteristics. Its lipid water partition coefficient (LogP) is 2.7293, indicating that it has moderate lipophilicity, which is beneficial for transmembrane transport, but may also affect its dispersion in the aqueous phase. The theoretical polar surface area (TPSA) is 70.6700 Å ², reflecting the area occupied by polar groups (mainly two hydroxyl groups) in the molecule. The water solubility is poor, about 0.0377 mg/mL, which to some extent limits its bioavailability. In addition, the predictive model shows that its blood-brain barrier permeability is low, suggesting that it may not easily enter the central nervous system. In the early safety screening, the Ames test result of Baiyangsu was 0.6 (usually considered negative if less than 2), indicating a low risk of mutagenicity and no significant inhibitory effect on hERG potassium channels, suggesting a low potential risk of arrhythmia.

Plant sources and extraction methods

Poplar extract is widely distributed in nature and mainly exists in various plants and bee products. Its classic plant sources include plants of the Wisteria genus, such as the wood butterfly Oroxylum indicum Bark and seeds of poplar trees, bark of poplar trees, and passion fruit（Passiflora Spp.) and some mushrooms. In addition, propolis, especially poplar type propolis, is one of the most abundant and well-known natural sources of poplar extract, which is also the origin of its name "poplar extract".

Organic solvent extraction is commonly used to extract lignin from raw materials. Common solvents include methanol, ethanol, ethyl acetate, etc. The typical extraction process is to heat and reflux the dried and crushed plant materials or propolis with an appropriate solvent or ultrasound assisted extraction, followed by filtration and concentration to obtain crude extract. Further purification relies on chromatographic techniques such as silica gel column chromatography, high-performance liquid chromatography (HPLC), etc. to obtain high-purity poplar extract monomers. With the development of green chemistry, modern technologies such as supercritical fluid extraction (such as CO ₂ extraction) have also been explored to improve extraction efficiency and selectivity. Research on biosynthetic pathways has shown that paeoniflorin is catalyzed by a series of enzymes such as chalcone synthase from phenylalanine in plants, laying the foundation for future large-scale production through synthetic biology strategies.

Pharmacological activity research

Numerous in vitro and in vivo studies have confirmed that paeoniflorin has diverse pharmacological activities, providing support for its multifaceted therapeutic potential.

1. Antitumor activity This is one of the most in-depth areas of research on poplar extract. Studies have shown that chrysin can inhibit proliferation and promote apoptosis of many cancer cell lines, especially for breast cancer cells. Its activity is not limited to cytotoxicity, but also includes inhibition of cell migration, invasion, and angiogenesis.
2. Antioxidant and anti-inflammatory activities As a polyphenolic compound, poplar extract can effectively scavenge free radicals such as DPPH and ABTS, and upregulate the activity of intracellular antioxidant enzymes such as superoxide dismutase (SOD) and glutathione peroxidase (GPx). In various acute and chronic inflammation models, such as LPS induced RAW264.7 macrophage inflammation and mouse ear swelling model, paeoniflorin exerts anti-inflammatory effects by inhibiting the release of pro-inflammatory factors (such as TNF - α, IL-6, IL-1 β) and the expression of inflammation related enzymes (such as COX-2, iNOS).
3. Liver protection and neuroprotective activity In animal models of liver injury induced by carbon tetrachloride, acetaminophen, etc., paeoniflorin showed hepatoprotective effects by reducing serum transaminase levels and alleviating pathological damage to liver tissue. Its antioxidant and anti-inflammatory properties play a key role in it. In addition, some studies suggest that resveratrol may have protective potential against neurodegenerative disease models such as Alzheimer's disease by inhibiting neuroinflammation and oxidative stress, although its low blood-brain barrier permeability is a challenge.
4. Other activities The study also reported that chrysin has potential activities such as anti anxiety, anti microbial, anti diabetes complications and so on, showing its broad prospects as a pleiotropic molecule.

Mechanism of action and molecular targets

The pharmacological action of chrysin, especially its anti breast cancer activity, is achieved by regulating multiple key signal pathways and molecular targets, which reflects the characteristics of multi target action. The mechanism of action of the mentioned targets can be summarized as follows:

• Hormone receptor regulation Poplar extract is defined as an estrogen blocker. It plays a selective estrogen receptor modulator (SERM) like role mainly by binding to estrogen receptor beta (ESR2), thereby antagonizing the proliferation promoting signal mediated by estrogen receptor alpha (ESR1), which is of great significance in the treatment of hormone receptor positive breast cancer.
• Inducing cell apoptosis and autophagy Poplar extract can upregulate pro apoptotic proteins (such as Bax) and downregulate the expression of anti apoptotic protein Bcl-2 (BCL2), disrupt mitochondrial membrane potential, lead to the release of cytochrome C, activate caspase cascade reaction, and induce cancer cell apoptosis. At the same time, it can also activate AMP activated protein kinase (AMPK, encoded by PRKAA1), an energy receptor that can inhibit the mTOR pathway, thereby inducing protective autophagy or synergizing with apoptosis.
• Inhibition of proliferation and metastasis signals Poplar extract can effectively inhibit the phosphorylation and activation of signal transduction and transcription activator 3 (STAT3). STAT3 is an important oncogenic transcription factor, and its sustained activation is closely related to cell proliferation, survival, and metastasis. Inhibition of the STAT3 pathway can downregulate the expression of downstream target genes such as Cyclin D1 and Survivor. In addition, poplar extract can inhibit the activity of protein kinase C alpha (PRKCA) and reduce the expression of matrix metalloproteinase-2 (MMP2), thereby inhibiting the invasion and metastasis ability of cancer cells.
• Reverse multidrug resistance Chemotherapy for breast cancer often fails due to multidrug resistance (MDR). It has been proved that chrysin is an inhibitor of ATP binding cassette transporters such as P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). By competitively inhibiting the function of these efflux pumps, resveratrol can increase the accumulation of chemotherapy drugs (such as doxorubicin and paclitaxel) in cancer cells, thereby reversing drug resistance.
• Other target interactions Poplar extract has also been reported to inhibit tyrosinase (TYR) activity, which may be related to its antioxidant and potential skin whitening applications. The interaction with microtubule associated protein tau (MAPT) suggests its possible mechanism in regulating tau protein pathological phosphorylation and intervening in the formation of neurofibrillary tangles.

Evaluation of drug properties and pharmacokinetics

Although poplar extract exhibits excellent biological activity in vitro, its pharmacological properties, especially oral bioavailability, are the main bottleneck restricting its clinical translation.

Pharmacokinetic studies have shown that the oral absorption of Baiyangsu is rapid but limited. The main reason is that the first pass effect is significant, and it is easily bound by metabolic enzymes such as UDP glucuronosyltransferase (UGT) in the intestine and liver, generating glucuronide or sulfate conjugates, resulting in a low proportion of prototype drugs entering the systemic circulation. This is also one of the reasons why it predicts low blood-brain barrier permeability. Its poor water solubility also affects its dissolution and absorption in the gastrointestinal tract.

In order to improve its bioavailability, researchers have explored various strategies:
1. Structural modification Synthesize its prodrugs or derivatives, such as preparing phospholipid complexes, amino acid ester derivatives, etc., to improve solubility and metabolic stability.
2. Formulation technology Utilizing nanotechnology, such as the preparation of poplar extract nanocrystals, liposomes, solid lipid nanoparticles, polymer micelles, etc., to enhance their solubility, stability, and targeting by increasing specific surface area, promoting lymphatic absorption, or providing protective carriers.
3. Combined administration Combined with metabolic enzyme inhibitors (such as piperine), it can significantly inhibit the glucuronidation of paeoniflorin, thereby increasing its blood drug concentration.

In terms of toxicology research, existing animal experiments have shown that salicylic acid has good safety at appropriate doses, but the potential toxicity of long-term use at high doses still needs to be systematically evaluated. The negative Ames test and lack of hERG inhibitory properties provide preliminary support for its safety.

Clinical application prospects and prospects

The multi-target pharmacological properties of Baiyangsu provide possibilities for its application in various disease fields, but its development is still in the preclinical or early clinical exploration stage.

1. Cancer adjuvant therapy and chemoprevention As a natural dietary supplement, chrysin has potential in chemoprevention of breast cancer. Its ability to reverse multidrug resistance makes it promising to be used in combination with conventional chemotherapy drugs, improve chemotherapy efficacy, and overcome drug resistance. Future research can focus on developing a combination therapy of poplar extract and standard chemotherapy, and utilizing nano delivery systems to achieve tumor targeting, improve efficacy, and reduce systemic toxicity.
2. Chronic inflammatory diseases: Based on its powerful anti-inflammatory and antioxidant activities, chrysin may be used to treat chronic inflammation related diseases such as arthritis, hepatitis, atherosclerosis, etc.
3. Neuroprotective agent Despite the challenges posed by the blood-brain barrier, poplar extract still has exploratory value in the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease through nasal administration or the development of nano formulations or prodrugs that can penetrate the blood-brain barrier.
4. Functional foods and cosmetics As a safe natural antioxidant, poplar extract has been applied in some health foods and cosmetics for anti-aging, skin protection, and more.

Future research directions should focus on: ① Deeply elucidating its complex network of interactions, especially the interactions between different targets; ② Conduct Good Laboratory Practice (GLP) toxicology studies in compliance with regulations to clarify the safe dosage range; ③ Vigorously promote the development of formulations based on new delivery systems to fundamentally solve the problem of low bioavailability; ④ Design and carry out rigorous clinical trials to verify its effectiveness and safety in specific diseases (such as drug-resistant breast cancer).

Conclusion

Poplar extract, as a widely sourced natural dihydroxyflavonoid, has demonstrated significant drug development value due to its multiple pharmacological activities such as antioxidant, anti-inflammatory, and anti-tumor effects, as well as its unique mechanism of acting on key targets such as AMPK, STAT3, BCL2, estrogen receptor, and multidrug resistance protein. Although its poor solubility and oral bioavailability are currently the main obstacles to clinical translation, this challenge is gradually being overcome through the continuous innovation of modern medicinal chemistry and pharmacy methods. With the deepening understanding of its molecular mechanism and breakthroughs in delivery technology, Populus euphratica is expected to develop from a promising lead compound into an innovative drug or highly effective adjuvant therapy for the prevention and treatment of diseases such as cancer and inflammation, providing a model for the modernization and precision application of natural products.