title: A new hypoxia inducible factor-2 inhibitory pyrrolinone alkaloid from roots and stems of Piper sarmentosum.
abstract: A new trimethoxycinnamoyl-2-pyrrolinone alkaloid, langkamide (1), along with the known compounds piplartine (2) and 3,4,5-trimethoxycinnamic acid (3) were isolated from the roots and stems of the shrub Piper sarmentosum ROXB. The structures were established by spectroscopic analyses and comparison of their spectral data with values reported in the literature. The compounds were tested for their ability to modulate hypoxia inducible factor-2 (HIF-2) transcription activity and all three showed HIF-2 inhibitory activity with EC₅₀ values of 14.0, 4.8, and 60.6 μM, respectively, for compounds 1, 2, and 3.
authors: SAIC-Frederick, Inc., NCI-Frederick, Frederick, MD 21702, USA.
authors: Heidi Rose
authors: HR
authors: Bokesch
authors: Roberta Scott
authors: RS
authors: Gardella
authors: Daniel Christopher
authors: DC
authors: Rabe
authors: Donald Paul
authors: DP
authors: Bottaro
authors: William Marston
authors: WM
authors: Linehan
authors: James Brislin
authors: JB
authors: McMahon
authors: Tawnya Carlene
authors: TC
authors: McKee
mesh_terms: D000470:Alkaloids / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D051792:Basic Helix-Loop-Helix Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D031701:Piper / Q000737:chemistry*; D018517:Plant Roots / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry; D011758:Pyrroles / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D000099162:Endothelial PAS Domain-Containing Protein 1
chemical_list: D000470:Alkaloids; D051792:Basic Helix-Loop-Helix Proteins; D011758:Pyrroles; D000099162:Endothelial PAS Domain-Containing Protein 1; C568982:langkamide; C013231:pyrroline