Bokesch Heidi Rose, Gardella Roberta Scott, Rabe Daniel Christopher, Bottaro Donald Paul, Linehan William Marston, McMahon James Brislin, McKee Tawnya Carlene
SAIC-Frederick, Inc., NCI-Frederick, Frederick, MD 21702, USA.
Chem Pharm Bull (Tokyo). 2011;59(9):1178-9. doi: 10.1248/cpb.59.1178.
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.
从胡椒科植物蒌叶（Piper sarmentosum ROXB.）的根和茎中分离得到了一种新的三甲氧基肉桂酰基-2-吡咯烷酮生物碱——蒌叶酰胺（1），以及已知化合物荜茇宁（2）和3,4,5-三甲氧基肉桂酸（3）。通过光谱分析并将其光谱数据与文献报道的值进行比较确定了这些化合物的结构。测试了这些化合物调节缺氧诱导因子-2（HIF-2）转录活性的能力，化合物1、2和3均表现出HIF-2抑制活性，其EC₅₀值分别为14.0、4.8和60.6 μM。
