A FLT3-inhibitory constituent from the rhizomes of Anemarrhena asphodeloides.
Bioactivity-guided investigation for the rhizomes of Anemarrhena asphodeloides using the Fms-like tyrosine kinase 3 (FLT3) inhibition assay led to the identification of an active xanthone, mangiferin. Mangiferin was found to inhibit activity of the FLT3 wild type and a mutated form of FLT3 with IC(50) values of 0.7 and 1.2 μM, respectively. Furthermore, this compound was assessed with a small panel of select kinases anaplastic lymphoma kinase (ALK), insulin receptor, and epidermal growth factor receptor) and was also found to be active in ALK assay.
Han
Sun-Young
SY
College of Pharmacy, Gyeongsang National University, Jinju, South Korea.
Chin
Young-Won
YW
D031403:Anemarrhena / Q000737:chemistry*; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D027343:Rhizome / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology*; D051941:fms-Like Tyrosine Kinase 3 / Q000037:antagonists & inhibitors*
D047428:Protein Kinase Inhibitors; D011994:Recombinant Proteins; D044004:Xanthones; C013592:mangiferin; D051941:fms-Like Tyrosine Kinase 3