Crinamine from Crinum asiaticum var. japonicum inhibits hypoxia inducible factor-1 activity but not activity of hypoxia inducible factor-2.
In a search for natural product inhibitors of hypoxia inducible factor-1 (HIF-1) function, crinamine (1), a crinane type alkaloid, showed potent dose dependent inhibition (IC50 = 2.7 microM) of HIF-1alpha in a cell-based reporter gene assay. Crinamine (1) was isolated from the aerial parts of Crinum asiaticum var. japonicum together with lycorine (2), norgalanthamine (3) and epinorgalanthamine (4). The other components (2-4) showed no significant inhibition of HIF-1alpha induced transcriptional activity.
Kim
Young Ho
YH
College of Pharmacy, Chungnam National University, Daejeon, Korea. yhk@cnu.ac.kr
Park
Eun Jung
EJ
Park
Mi Hyun
MH
Badarch
Uranchimeg
U
Woldemichael
Girma Moges
GM
Beutler
John Albert
JA
D047151:Amaryllidaceae Alkaloids / Q000494:pharmacology*; D051792:Basic Helix-Loop-Helix Proteins; D045744:Cell Line, Tumor; D031407:Crinum / Q000737:chemistry*; D006801:Humans; D051793:Hypoxia-Inducible Factor 1 / Q000037:antagonists & inhibitors*; D007212:Indolizines / Q000494:pharmacology*; D052247:Nitric Oxide Synthase Type II / Q000502:physiology; D014157:Transcription Factors / Q000037:antagonists & inhibitors*; D000099162:Endothelial PAS Domain-Containing Protein 1
D047151:Amaryllidaceae Alkaloids; D051792:Basic Helix-Loop-Helix Proteins; D051793:Hypoxia-Inducible Factor 1; D007212:Indolizines; D052247:Nitric Oxide Synthase Type II; D014157:Transcription Factors; D000099162:Endothelial PAS Domain-Containing Protein 1; C411129:crinamine