所选天然产物对恶性疟原虫硫氧还蛋白还原酶（PfTrxR）和谷胱甘肽还原酶（PfGR）的抗疟活性及结合亲和力的测定
Determination of antiplasmodial activity and binding affinity of selected natural products towards PfTrxR and PfGR.
作者信息
Munigunti Ranjith, Becker Katja, Brun Reto, Calderón Angela I
机构信息
Department of Pharmacal Sciences, 4306 Walker Building, Auburn University, Auburn, AL, USA.
出版信息
Nat Prod Commun. 2013 Aug;8(8):1135-6.
In our study, the binding affinities of selected natural products towards PfTrxR, PfGR, human TrxR and human GR were determined using a mass spectrometry based ligand binding assay. The in vitro antimalarial activity and cytotoxicity of these ligands were also determined. Catharanthine, 11-(OH)-coronaridine, hernagine, vobasine and hispolone displayed antiplasmodial activity against PfK1 (IC50 = 0.996-3.63 microg/mL).
在我们的研究中，使用基于质谱的配体结合测定法测定了所选天然产物对恶性疟原虫硫氧还蛋白还原酶（PfTrxR）、恶性疟原虫谷胱甘肽还原酶（PfGR）、人硫氧还蛋白还原酶和人谷胱甘肽还原酶的结合亲和力。还测定了这些配体的体外抗疟活性和细胞毒性。长春花碱、11-（羟基）-萝芙木碱、赫那精、沃巴碱和组蛋白对恶性疟原虫K1株显示出抗疟活性（半数抑制浓度[IC50]=0.996-3.63微克/毫升）。
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