Kirsch G, Köng G M, Wright A D, Kaminsky R
Institute for Pharmaceutical Biology, Technical University of Braunschweig, Mendelssohnstrasse 1, D-38106 Braunschweig, Germany.
J Nat Prod. 2000 Jun;63(6):825-9. doi: 10.1021/np990555b.
From the CH(2)Cl(2) extract of the sponge Hyrtios cf. erecta, collected from Fiji, two new sesterterpenes, 1 and 2, and the known compounds isodehydroluffariellolide (3), homofascaplysin A (4), and fascaplysin (5) were isolated. The structures of 1-5 were established employing 1D and 2D NMR spectroscopy and mass spectrometry. All NMR resonances of fascaplysin (5) have been unambiguously assigned. Evaluation of the biological activity of the extracts and pure compounds toward Plasmodium falciparum, Trypanosoma brucei subsp. rhodesiense, Trypanosoma cruzi, hepatitis A virus (HAV), several other microbial targets, and HIV-1-RT and p56(lck) tyrosine kinase revealed new activities for homofascaplysin (4) and fascaplysin (5), both being potently active in vitro against P. falciparum.
从采自斐济的海绵类动物近似直立管指海绵(Hyrtios cf. erecta)的二氯甲烷提取物中,分离得到了两种新的倍半萜烯(1和2)以及已知化合物异脱氢卢法瑞内酯(3)、高法卡普林A(4)和法卡普林(5)。通过一维和二维核磁共振光谱以及质谱确定了1 - 5的结构。法卡普林(5)的所有核磁共振共振信号都已明确归属。对提取物和纯化合物针对恶性疟原虫、布氏罗得西亚锥虫亚种、克氏锥虫、甲型肝炎病毒(HAV)、其他几种微生物靶点以及HIV - 1逆转录酶和p56(lck)酪氨酸激酶的生物活性进行评估后,发现高法卡普林(4)和法卡普林(5)具有新的活性,二者在体外对恶性疟原虫均具有强效活性。