Ayers Sloan, Zink Deborah L, Mohn Kenneth, Powell Joanne Staats, Brown Christine M, Murphy Terry, Brand Robert, Pretorius Seef, Stevenson Dennis, Thompson Donald, Singh Sheo B
Natural Products Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Planta Med. 2007 Mar;73(3):296-7. doi: 10.1055/s-2007-967124. Epub 2007 Feb 16.
Two known aporphine alkaloids, (S)-dicentrine (1) and (S)-neolitsine (2), have been isolated from the MeOH extract of the aerial parts of Cissampelos capensis (Menispermaceae). The structures of these compounds were elucidated by NMR and MS analysis and comparison to literature data. These compounds were isolated by bioassay-guided fractionation using the Haemonchus contortus larval development assay. Compounds 1 and 2 exhibited EC90 values (concentration at which 90% loss of larval motility is observed) of 6.3 and 6.4 microg/mL, respectively. In an IN VIVO assay, administration of 1 resulted in 67% reduction of worm counts in mice at 25 mg/kg when dosed orally.
从南非锡生藤（防己科）地上部分的甲醇提取物中分离出了两种已知的阿朴啡生物碱，即（S）-双苄基异喹啉（1）和（S）-新木姜子碱（2）。通过核磁共振（NMR）和质谱（MS）分析并与文献数据对比，阐明了这些化合物的结构。这些化合物是通过生物测定导向的分级分离法，利用捻转血矛线虫幼虫发育试验分离得到的。化合物1和2的EC90值（观察到幼虫运动能力丧失90%时的浓度）分别为6.3和6.4微克/毫升。在一项体内试验中，口服给药时，化合物1以25毫克/千克的剂量给药，可使小鼠体内的蠕虫数量减少67%。
