Plasmodium berghei: inhibited incorporation of AMP-8- 3 H into nucleic acids of erythrocyte-free malarial parasites by acridines, phenanthridines, and 8-aminoquinolines |
| |
| Authors: | C H Lantz K Van Dyke |
| |
| Affiliation: | 1. KU Leuven – University of Leuven, Department of Neurosciences, Research Group Experimental ORL, Leuven, Belgium;2. KU Leuven – University of Leuven, Faculty of Psychology and Education Sciences, Parenting and Special Education Research Unit, Leuven, Belgium;1. CHRU de Tours, Centre de référence Maladies Métaboliques ToTeM, Médecine pédiatrique, Hôpital Clocheville, 49, boulevard Béranger, 37000 Tours, France;2. Inserm U1069, Nutrition, Croissance et Cancer, Faculté de médecine, Université François Rabelais de Tours, PRES Centre-Val de Loire Universités, 10, boulevard Tonnellé, 37000 Tours, France;1. Center for Environmental Security, The Biodesign Institute, Security and Defense Systems Initiative, Arizona State University, 781 E. Terrace Mall, Tempe, AZ 85287, USA;2. Department of Environmental Health Sciences, Bloomberg School of Public Health, Johns Hopkins University, Baltimore, MD, USA;1. Key Laboratory for Ultrafine Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237, China;2. Department of Orthopaedics, Jiangwan Hospital, Hongkou District of Shanghai, Shanghai 200434, China;3. Institute of Biomaterials, Department of Materials Science and Engineering, University of Erlangen-Nuremberg, 91058 Erlangen, Germany |
| |
| Abstract: | The ability of several acridine derivatives and various other heterocyclic compounds to inhibit incorporation of radioactivity from exogenous AMP-8-3H into the DNA and RNA of erythrocyte-free malarial parasites (Plasmodium berghei) was studied. The most potent acridine derivative was acriflavin (50% inhibition of RNA between 10−6 and 10−5 M). Acridine orange (50% inhibition of RNA at nearly 10−4 M) and acridine red (50% inhibition of RNA at nearly 10−3 M) were less potent than acriflavin by about 10-and 100-fold, respectively. Another heterocycle, methylene blue NN, approached the potency of acriflavin (50% inhibition of RNA at slightly greater than 10−5 M). Three phenanthridine heterocycles were tested and M &; B 1502 (dimidium butoxide) was found to be the most potent, exerting 50% inhibition of RNA at slightly greater than 10−5 M. Another derivative, M &; B 4250A exerted 50% inhibition of RNA at 10−4 M while a dose midway between 10−4 and 10−3 M was required of M &; B 4180A to cause this magnitude of inhibition. Two 8-aminoquinolines were also studied to determine their inhibitory potency against plasmodial nucleic acid anabolism. Both of these two-ringed heterocycles were relatively lacking in potency, exerting 50% inhibition of RNA at doses somewhat greater than 10−4 M. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
