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首页> 外文期刊>ACS Omega >Chemical Genomic Profiling Unveils the in Vitro and in Vivo Antiplasmodial Mechanism of A?a?? (Euterpe oleracea Mart.) Polyphenols
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Chemical Genomic Profiling Unveils the in Vitro and in Vivo Antiplasmodial Mechanism of A?a?? (Euterpe oleracea Mart.) Polyphenols

机译：化学基因组分析揭示了A？a ??的体外和体内抗疟原虫机制。 （欧亚油菜市场）多酚

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Malaria remains a major detrimental parasitic disease in the developing world, with more than 200 million cases annually. Widespread drug-resistant parasite strains push for the development of novel antimalarial drugs. Plant-derived natural products are key sources of antimalarial molecules. Euterpe oleracea Martius (“a?a??”) originates from Brazil and has anti-inflammatory and antineoplasic properties. Here, we evaluated the antimalarial efficacy of three phenolic fractions of a?a??; total phenolics (1), nonanthocyanin phenolics (2), and total anthocyanins (3). In vitro, fraction 2 moderately inhibited parasite growth in chloroquine-sensitive (HB3) and multiresistant (Dd2) Plasmodium falciparum strains, while none of the fractions was toxic to noncancer cells. Despite the limited activity in vitro, the oral treatment with 20 mg/kg of fraction 1 reduced parasitemia by 89.4% in Plasmodium chabaudi-infected mice and prolonged survival. Contrasting in vitro and in vivo activities of 1 suggest key antiplasmodial roles for polyphenol metabolites rather than the fraction itself. Finally, we performed haploinsufficiency chemical genomic profiling (HIP) utilizing heterozygous Saccharomyces cerevisiae deletion mutants to identify molecular mechanisms of a?a?? fractions. HIP results indicate proteostasis as the main cellular pathway affected by fraction 2. These results open avenues to develop a?a?? polyphenols as potential new antimalarial candidates.
机译：疟疾仍然是发展中国家的主要有害寄生虫病，每年有2亿多病例。广泛耐药的寄生虫菌株推动了新型抗疟药的开发。植物来源的天然产物是抗疟分子的关键来源。 Euterpe oleracea Martius（“ a？a ??”）起源于巴西，具有抗炎和抗肿瘤作用。在这里，我们评估了三种酚类α？a ??的抗疟药的功效。总酚醛（1），非花色素酚（2）和总花青苷（3）。在体外，级分2在氯喹敏感（HB3）和多重耐药（Dd2）恶性疟原虫菌株中适度抑制了寄生虫的生长，而所有级分均对非癌细胞没有毒性。尽管体外活性受到限制，但是用20 mg / kg级分1口服治疗可降低Chabaudi疟原虫感染小鼠的寄生虫病89.4％，并延长了其生存期。 1的体外和体内活性对比表明，多酚代谢物而不是级分本身具有关键的抗血浆作用。最后，我们利用杂合的酿酒酵母缺失突变体进行了单倍不足化学基因组谱分析（HIP），以鉴定α？α？分数。 HIP结果表明蛋白稳定是受到级分2影响的主要细胞途径。这些结果为发展α？多酚是潜在的新型抗疟药候选物。

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