Souza Julia M, de Carvalho Érica A A, Candido Ana Carolina B B, de Mendonça Rafael P, Fernanda da Silva Maria, Parreira Renato L T, Dias Fernanda G G, Ambrósio Sérgio R, Arantes Andrea T, da Silva Filho Ademar A, Nascimento Aline N, Costa Monique R, Sairre Mirela I, Veneziani Rodrigo C S, Magalhães Lizandra G
Núcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, Brazil.
Pós Graduação em Ciência Animal, Universidade de Franca, Franca, Brazil.
Front Vet Sci. 2020 Dec 10;7:527. doi: 10.3389/fvets.2020.00527. eCollection 2020.
The efficacy of Licochalcone A (LicoA) and its two analogs were reported against and , and in experimental model of . Initially, LicoA and its analogs were screened against promastigote forms of . LicoA was the most active compound, with IC values of 20.26 and 3.88 μM at 24 and 48 h, respectively. Against amastigote forms, the IC value of LicoA was 36.84 μM at 48 h. In the next step, the effectivity of LicoA was evaluated against promastigote and amastigote forms of . Results demonstrated that LicoA exhibited leishmanicidal activity against promastigote forms with IC values of 41.10 and 12.47 μM at 24 and 48 h, respectively; against amastigote forms the IC value was 29.58 μM at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC value was 123.21 μM at 48 h and showed about 30% of hemolytic activity at concentration of 400 μM. infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL).
据报道，甘草查尔酮A（LicoA）及其两种类似物对[具体病症1]和[具体病症2]以及在[具体实验模型]的实验模型中具有疗效。最初，对LicoA及其类似物针对[某种寄生虫]的前鞭毛体形式进行了筛选。LicoA是最具活性的化合物，在24小时和48小时时的IC值分别为20.26和3.88μM。针对无鞭毛体形式而言，LicoA在48小时时的IC值为3�.84μM。在下一步中，评估了LicoA对[另一种寄生虫]的前鞭毛体和无鞭毛体形式的有效性。结果表明，LicoA对前鞭毛体形式表现出杀利什曼原虫活性，在24小时和48小时时的IC值分别为41.10和12.47μM；对无鞭毛体形式而言，在48小时时的IC值为29.58μM。细胞毒性评估表明，LicoA对小鼠腹膜巨噬细胞表现出中度的哺乳动物细胞毒性；在48小时时的CC值为123.21μM，在400μM浓度下表现出约30%的溶血活性。连续八天以50mg/kg的剂量用LicoA治疗感染的仓鼠，与阴性对照组相比，能够分别显著降低肝脏和脾脏中的寄生虫负荷，降低幅度分别为43.67%和39.81%。这些发现表明，查尔酮型黄酮类化合物可能是一类有前途的天然产物，有望用于寻找能够治疗犬内脏利什曼病（CVL）的新型、安全且有效的化合物。
