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Product name: Pinostrobin
Synonym name:
Catalogue No.: SBP00113
Cas No.: 480-37-5
Formula: C16H14O4
Mol Weight: 270.28
Botanical Source:
Physical Description:
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 Pinostrobin
HNMR of Pinostrobin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
55.7600
3.0696
3.0082
.1208
6.2087
35.3773
High
90.1714
2.5904
No
No
Yes
No
Yes
No
0.6
Yes
No
Yes
No
Qilosonin (Pinostrobin), also known as Josone, is a natural flavonoid compound with the molecular formula C16H14O4 and CAS number 480-37-5. As an important member of flavonoid compounds, colosonin has attracted attention for its diverse biological activities, especially showing significant potential in anti-cancer, antioxidant, antiviral, and neuroprotective fields. In recent years, with in-depth research into the pharmacological mechanisms of natural products, colosonin has become a hot topic in drug development and disease treatment research due to its oral activity and good safety profile. Notably, as an effective PCSK9 inhibitor, colosonin can regulate lipid metabolism, suggesting its potential application value in the prevention and treatment of cardiovascular and cerebrovascular diseases. In addition, colosonin shows promising therapeutic prospects in various pathological conditions such as viral infections, leukemia, cirrhosis, and neurological diseases. This paper will systematically review the chemical structure and physicochemical properties of colosonein, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, and finally explore its clinical application prospects and future development directions.
Viclosones belong to the flavanone subclass of flavonoids. Their chemical structure features a typical C6-C3-C6 backbone, containing two benzene rings (A and B rings) and a central tricyclic structure (C ring). Viclosone has a molecular weight of 270.2840, and its molecular structure contains hydroxyl and methoxy substituents, giving it certain polarity and biological activity. Its LogP value is 3.0696, indicating that colosonin has moderate lipid solubility, which benefits cell membrane permeability and oral absorption. The polar surface area (TPSA) is 55.76 Ų, indicating moderate molecular polarity that supports interactions with multiple biological targets.
Cobulasonin has relatively low water solubility (0.1208 mg/mL), which somewhat limits its bioavailability, but its high blood-brain barrier permeability (BBB) gives it a unique advantage in treating neurological diseases. Importantly, cobloson does not show hERG channel inhibitory activity, suggesting a low risk of cardiotoxicity. The Ames test result was 0.6, indicating a low genotoxicity risk and a solid safety foundation.
Cobroson is widely found in various plants, especially in Pinaceae and certain legumes. Typical plant sources include Pinus spp., Dalbergia spp., and others. Its distribution in plants is not limited to wood, but also found in bark, leaves, and roots.
Traditional extraction methods mainly use organic solvent extraction methods, such as methanol, ethanol, ethyl acetate, etc., combined with ultrasound-assisted extraction or reflux extraction technologies to improve extraction efficiency. In recent years, supercritical CO2 extraction and microwave-assisted extraction technologies have also been applied to efficiently extract colosin, significantly improving yield and purity. The crude extract after extraction is usually purified using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other methods to ensure high-purity colosonin samples for pharmacological research.
Vicusonin exhibits significant antitumor activity across various cancer models. In vitro studies have shown that colosonin can inhibit the proliferation of various cancer cell lines, including breast cancer, lung cancer, liver cancer, and leukemia cells. Its anti-cancer mechanisms mainly involve inducing cell cycle arrest, promoting apoptosis, and inhibiting tumor cell migration and invasion. Vilosonin exerts its anticancer effects by regulating multiple signaling pathways, such as PI3K/Akt, MAPK, and NF-κB pathways. Additionally, coloson can enhance the sensitivity of chemotherapy drugs, demonstrating potential adjunctive therapeutic value.
As a natural flavonoid compound, colosonin has powerful antioxidant properties. Its antioxidant effects are mainly achieved by scavenging free radicals, inhibiting lipid peroxidation, and regulating endogenous antioxidant enzyme systems. Viclosone can activate the NFE2L2/NRF2 signaling pathway, promoting the expression of downstream antioxidant enzymes such as SOD1, SOD2, CAT, GPX1, and HMOX1, thereby enhancing the cells' resistance to oxidative stress. Additionally, the regulation of MMP1 and MMP3 by colosinin helps slow tissue damage and inflammatory responses.
Ballison exhibits activity in inhibiting viral replication and transmission across various viral infection models. Research shows that coloson can interfere with the viral life cycle, including the invasion, replication, and assembly processes. Its antiviral mechanism may involve regulating the immune responses of host cells and directly acting on virus-related enzyme activities. Ballsonin has shown certain inhibitory effects against influenza viruses, hepatitis B viruses, and certain coronavirus strains, suggesting its potential as a broad-spectrum antiviral drug.
Viclosin has excellent neuroprotective functions, mainly by reducing oxidative stress and inflammatory responses in nerve cells, and inhibiting apoptosis. Its high blood-brain barrier permeability enables effective action on the central nervous system. Vilosonin activates the NRF2 signaling pathway, enhances antioxidant defenses, reduces neuroinflammation, and improves cognitive function. In models of neurodegenerative diseases such as Parkinson's and Alzheimer's, colosonin has shown potential to slow pathological progression.
As an effective inhibitor of PCSK9, colosonin can lower plasma low-density lipoprotein cholesterol (LDL-C) levels and has potential cardiovascular and cerebrovascular protective effects. Moreover, in cirrhosis and inflammatory diseases, it shows promising therapeutic prospects by modulating immune responses and suppressing the release of inflammatory mediators.
The multiple biological activities of colosonin are attributed to its regulatory effects on various molecular targets. Its main mechanisms of action include:
PCSK9 inhibition
PCSK9 (proproprotein-converting enzyme lysolysin 9) is a key enzyme regulating cholesterol metabolism, and its overexpression is closely linked to atherosclerosis and cardiovascular diseases. Vilosannin directly inhibits the catalytic activity of PCSK9, reduces the degradation of LDL receptors, promotes the clearance of LDL-C, and exerts lipid-lowering and cardiovascular protective effects.
Activation of antioxidant signaling pathways
Vilosonin activates NFE2L2/NRF2 transcription factors, promotes the expression of downstream antioxidant enzymes (SOD1, SOD2, CAT, GPX1, HMOX1), enhances cellular antioxidant defenses, and reduces oxidative stress damage.
Matrix metalloproteinase (MMP) regulation
Cobloson regulates the expression of MMP1 and MMP3, influences extracellular matrix remodeling, and inhibits tumor cell invasion and inflammatory responses.
Regulation of apoptosis and proliferation
By modulating signaling pathways such as PI3K/Akt, MAPK, and NF-κB, colosinin promotes cancer cell apoptosis and inhibits proliferation and migration.
Antiviral mechanism
Viclosin may inhibit viral replication and transmission by interfering with virus-related enzyme activity and enhancing host immune responses.
Neuroprotective mechanisms
In addition to antioxidants, coloson also protects neurons from damage by inhibiting the release of inflammatory factors and regulating neurotransmitter balance.
Vicuson has good druggability characteristics. Its molecular weight of 270.2840 and LogP of 3.0696 comply with the Lipinski rule, indicating good oral bioavailability. TPSA is 55.76 Ų, which facilitates cell membrane penetration and blood-brain barrier penetration, supporting its application in the treatment of central nervous system diseases. Although water solubility is relatively low, formulation technology can improve its dissolution and absorption.
In terms of safety, coloson did not show hERG channel inhibition, reducing the risk of cardiotoxicity. Ames test results showed low genotoxicity and good safety. Pharmacokinetic studies show that colosonin is rapidly absorbed orally, with a shorter peak plasma concentration and wide distribution, especially high concentrations in brain tissue, meeting its neuroprotective requirements. Metabolism mainly occurs through hepatic enzyme systems, and the safety of metabolites still requires further evaluation. Excretion mainly involves the kidneys and bile.
With its multi-target and multi-mechanism pharmacological activity, Qiussonin demonstrates broad clinical application potential. Its research in anti-cancer, antiviral, neuroprotection, and cardiovascular disease prevention and treatment is deepening, and it is expected to become a new natural drug or lead compound in the future.
In the field of anti-cancer treatment, colosonin can serve as an adjunct chemotherapy drug to enhance efficacy and reduce side effects. In antiviral therapy, colosonin is expected to be developed as a broad-spectrum antiviral drug, especially offering new treatment strategies for emerging viral infections. In the treatment of neurological diseases such as Alzheimer's and Parkinson's, the high brain penetration and neuroprotective effects of colosonein provide strong support for clinical translation. In cardiovascular and cerebrovascular diseases, ballsonin lowers blood lipids and prevents atherosclerosis by inhibiting PCSK9, showing promising application prospects.
Future research should focus on preclinical safety evaluation, pharmacokinetic optimization, and dosage form development of cocosonin, combined with modern drug design technologies to conduct structural modification and derivatives studies to improve bioavailability and targetability. At the same time, in-depth analysis of its molecular mechanisms and conducting clinical trials to verify its efficacy and safety are key to advancing the clinical application of colosonine.
As a natural flavonoid compound, colosonin has become a hot topic in natural product pharmacology research due to its diverse pharmacological activities and good druggability. Its multiple mechanisms of action—including anti-cancer, antioxidant, antiviral, and neuroprotective effects—provide new ideas and strategies for treating various major diseases. In the future, with advances in drug development technology and deeper clinical research, covesonin is expected to become an important natural drug resource, contributing greater value to human health.
Shenshuai
Wenjing
Hedandan
