Marine and Plant Research Laboratory of Ghana, Department of Chemistry, School of Physical and Mathematical Sciences, University of Ghana, P.O. Box LG 56, Legon-Accra, Ghana.
Department of Parasitology, Noguchi Memorial Institute for Medical Research, University of Ghana, P.O. Box LG 581, Legon-Accra, Ghana.
Mar Drugs. 2018 Dec 24;17(1):9. doi: 10.3390/md17010009.
A new alkaloid paenidigyamycin A () was obtained from the novel Ghanaian sp. isolated from the mangrove rhizosphere soils of the tree growing in the wetlands of the Digya National Park, Ghana. Compound was isolated on HPLC at t = 37.0 min and its structure determined by MS, 1D, and 2D-NMR data. When tested against , (IC 0.75 µM) was just as effective as amphotericin B (IC 0.31 µM). Against , (IC 7.02 µM) was twenty-two times less active than amphotericin B (IC 0.32 µM), reinforcing the unique effectiveness of against . For , (IC 0.78 µM) was ten times more active than the laboratory standard (IC 8.20 µM). The IC of 9.08 µM for against 3d7 compared to artesunate (IC 36 nM) was not strong, but this result suggests the possibility of using the paenidigyamycin scaffold for the development of potent antimalarial drugs. Against cercariae, showed high anticercaricidal activity compared to artesunate. The minimal lethal concentration (MLC) and minimal effective concentration (MEC) of the compound were 25 and 6.25 µM, respectively, while artesunate was needed in higher quantities to produce such results. However, (IC > 100 µM) was not active against .
从生长在加纳 Digya 国家公园湿地的红树林根系土壤中分离到的新型加纳链霉菌中获得了一种新的生物碱帕尼迪吉霉素 A()。化合物在 HPLC 上于 t = 37.0 min 时被分离出来,其结构通过 MS、1D 和 2D-NMR 数据确定。当测试对时,(IC 0.75 µM)与两性霉素 B(IC 0.31 µM)一样有效。对(IC 7.02 µM)的活性比两性霉素 B(IC 0.32 µM)低二十二倍,这进一步证实了对的独特有效性。对于,(IC 0.78 µM)比实验室标准(IC 8.20 µM)活性高十倍。对 3d7 的 IC 9.08 µM 与青蒿琥酯(IC 36 nM)相比并不强,但这一结果表明有可能利用帕尼迪吉霉素骨架来开发有效的抗疟药物。与青蒿琥酯相比,对尾蚴显示出高抗尾蚴活性。该化合物的最小致死浓度(MLC)和最小有效浓度(MEC)分别为 25 和 6.25 µM,而青蒿琥酯则需要更高的浓度才能产生类似的效果。然而,(IC > 100 µM)对无效。