Evaluation of Mongolian compound library for potential antimalarial and anti-Toxoplasma agents

Evaluation of Mongolian compound library for potential antimalarial and anti-Toxoplasma agents
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蒙古化合物库潜在抗疟和抗弓形虫药物的评价

DOI:
10.1016/j.parint.2021.102424
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发表时间:
2021
影响因子:
1.9
通讯作者:
Nishikawa Yoshifumi
Nishikawa Yoshifumi
中科院分区:
医学3区
文献类型:
--
作者:
Banzragchgarav Orkhon;Ariefta Nanang R.;Murata Toshihiro;Myagmarsuren Punsantsogvoo;Battsetseg Badgar;Battur Banzragch;Batkhuu Javzan;Nishikawa Yoshifumi

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对蒙古族化合物库中的179个化合物进行了体外抑制恶性疟原虫和弓形虫生长的活性研究,其中Brachangobinan A的半数抑制浓度(IC_(50))为2.62 μM,选择性指数(SI)为27.91; 2-(2′-羟基-5 ′-O-甲基苯基)-5-(2″,5 ″-二羟基苯基)恶唑(IC 503.58 μM和SI 24.66);金磺素(IC 503.78 μM和SI 15.26); 4,11-二-O-没食子酰基岩白菜素2-(2′,5 ′-二羟基苯基)-5-(2″-羟基苯基)恶唑(IC 506.94 μM,SI 11.48)。恶性疟原虫增殖此外,麦黄酮(IC_(50)为12.94 μM,SI > 23.40)也被认为是T的潜在抑制剂。生殖道增殖我们的研究结果代表了一个很好的起点,从蒙古化合物开发新的抗疟疾和抗弓形虫疗法。
179 compounds in a Mongolian compound library were investigated for their inhibitory effect on thein vitrogrowth ofPlasmodium falciparumand Toxoplasma gondii.Among these compounds, brachangobinan A at a half-maximal inhibition concentration (IC50) of 2.62 μM and a selectivity index (SI) of 27.91; 2-(2′-hydroxy-5′-O-methylphenyl)-5-(2″,5″-dihydroxyphenyl)oxazole (IC503.58 μM and SI 24.66); chrysosplenetin (IC503.78 μM and SI 15.26); 4,11-di-O-galloylbergenin (IC503.87 μM and SI 13.38); and 2-(2′,5′-dihydroxyphenyl)-5-(2″-hydroxyphenyl)oxazole (IC506.94 μM and SI 11.48) were identified as potential inhibitors ofP. falciparummultiplication. Additionally, tricin (IC5012.94 μM and SI > 23.40) was identified as a potential inhibitor ofT. gondiimultiplication. Our findings represent a good starting point for developing novel antimalarial and anti-Toxoplasmatherapeutics from Mongolian compounds.