Drug intelligence / Profile preview

xanthomicrol

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Not Formally Established For Pharmaceutical Use
01

Overview

Xanthomicrol is a **plant-derived, trimethoxylated hydroxyflavone** with reported antineoplastic, antiangiogenic, anti-inflammatory, and antimicrobial activity. Mechanistic studies indicate that xanthomicrol induces cytotoxic and antiproliferative effects in malignant cell lines, selectively reducing cancer cell viability with minimal toxicity to normal cells. Its anticancer activities are due to modulation of lipid metabolism, induction of apoptosis, cell cycle arrest at G2/M phase, and inhibition of de novo lipogenesis. In vivo, xanthomicrol has been shown to inhibit tumor growth and angiogenesis, associated with downregulation of the PI3K/Akt pathway and suppression of HIF-1α and VEGF expression. Molecular modeling studies also suggest xanthomicrol may inhibit DNA methyltransferase 1 (DNMT1), similar to decitabine, suggesting potential epigenetic effects[1][2][3][4][5][6].

Other names
4',5-dihydroxy-6,7,8-trimethoxyflavone4H-1-benzopyran-4-one, 5-hydroxy-2-(4-hydroxyphenyl)-6,7,8-trimethoxy-5-hydroxy-2-(4-hydroxyphenyl)-6,7,8-trimethoxychromen-4-one
02

Targets

CCND1 (Cyclin D1)DNMT1 (DNA (cytosine-5)-methyltransferase 1)VEGFA (Vascular endothelial growth factor A)CDKN1A (Cyclin-dependent kinase inhibitor 1A)TP53 (Cellular Tumor Antigen p53 R175H)

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