529-51-1
Chemical Structure
Azaleatin
- CAS No.: 529-51-1
- Formula:C16H12O7
- Molecular Weight:316.26
IUPAC Name: 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-5-methoxy-4H-chromen-4-one
InChIKey: RJBAXROZAXAEEM-UHFFFAOYSA-N
SMILES: O=C1C(O)=C(C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(OC)=C13
Biological Activity: Azaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC50 values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections[1][2][3][4][5][6][7][8][9].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Azaleatin | 98.86% | Azaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC50 values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections. | ||||||||||||||||||||
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- [1]. Hassan HM, et al. Cardioprotective potential of azaleatin against sodium arsenite instigated sub-chronic cardiotoxicity via targeting TLR4/MyD88, JAK1/STAT3, and NF-κB in Sprague Dawley rats. J Trace Elem Med Biol. 2025;92:127763.
- [2]. Tsai KC, et al. Pharmacophore-driven identification of human glutaminyl cyclase inhibitors from foods, plants and herbs unveils the bioactive property and potential of Azaleatin in the treatment of Alzheimer's disease. Food Funct. 2022;13(24):12632-12647. Published 2022 Dec 13.
- [3]. Mustafa NF, Cheng KK, Nadri MH, Razali SA, Zakaria II, Salin NH, Amran SI. Discovery of azaleatin as a potential allosteric inhibitor for dengue NS2B-NS3 protease using in vitro and in silico studies. Journal of Biomolecular Structure and Dynamics. 2025 Sep 22;43(14):7759-70.
- [4]. Kamel EM, et al. Deciphering molecular mechanisms underlying the inhibition of β-glucuronidase by xanthones from Centaurium spicatum. Bioorg Chem. 2024;150:107609.
- [5]. Adachi SI, et al. Anti-hyperuricemic effect of isorhamnetin in cultured hepatocytes and model mice: structure-activity relationships of methylquercetins as inhibitors of uric acid production. Cytotechnology. 2019;71(1):181-192.
- [6]. Ganbold M, et al. Antifibrotic effect of methylated quercetin derivatives on TGFβ-induced hepatic stellate cells. Biochem Biophys Rep. 2019;20:100678. Published 2019 Aug 16.
- [7]. Dai L, He J, Miao X, Guo X, Shang X, Wang W, Li B, Wang Y, Pan H, Zhang J. Multiple biological activities of Rhododendron przewalskii Maxim. extracts and UPLC-ESI-Q-TOF/MS characterization of their phytochemical composition. Frontiers in Pharmacology. 2021 Feb 10;12:599778.
- [8]. Ramos LC, Palacios J, Barrientos RE, Gómez J, Castagnini JM, Barba FJ, Tapia A, Paredes A, Cifuentes F, Simirgiotis MJ. UHPLC-MS phenolic fingerprinting, aorta endothelium relaxation effect, antioxidant, and enzyme inhibition activities of azara dentata ruiz & pav berries. Foods. 2023 Feb 2;12(3):643.
- [9]. Boojar FM, Golmohamad S, Tafreshi G. Comparative study on the status of glycation precursors, advanced glycation end products, and cell viability under effects of kaempferol, myricetin, and azaleatin in HGC-27 cell line. Journal of Young Investigators. 2019 Jan 1;36(1).
Keywords
