QOPN Grupo Química Orgánica de Productos Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia.
PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia, Calle 70 No. 52-21, Postal Code 0500100, Medellín, Colombia.
Bioorg Med Chem. 2019 Jan 1;27(1):153-160. doi: 10.1016/j.bmc.2018.11.030. Epub 2018 Nov 22.
We describe the in vitro activity of two natural isomeric ent-beyerene diterpenes, several derivatives and synthetic intermediates. Beyerenols 1 and 2 showed EC of 4.6 ± 9.4 and 5.3 ± 9.4 μg/mL against amastigotes of L. (V) brazilensis, with SI of 5.1 and 7.7, respectively. Beyerenol 1 was synthesized from stevioside. In vivo experiments with bereyenols showed cure in 50% of hamsters infected with L. (V) brazilensis topically applied as Cream I (beyerenol 1, 0.81%, w/w) and Cream III (beyerenol 2, 1.96%, w/w). These results suggest that beyerenols are potential candidates for cutaneous leishmaniasis chemotherapy by topical application. In vitro assays of amastigotes of L. (V) brazilensis showed EC of 1.1 ± 0.1 and 1.3 ± 0.04 μg/mL, with SI of 3.1 and 3.5 for hydrazone intermediates 10 and 11, respectively.
我们描述了两种天然对映贝壳杉烯二萜，一些衍生物和合成中间体的体外活性。贝雷醇 1 和 2 对 L.（V）巴西利什曼原虫的无鞭毛体的 EC 分别为 4.6±9.4 和 5.3±9.4μg/mL，SI 分别为 5.1 和 7.7。贝雷醇 1 是由甜菊糖苷合成的。贝雷醇 1（0.81%，w/w）和贝雷醇 2（1.96%，w/w）作为乳膏 I 和乳膏 III 局部应用于感染 L.（V）巴西利什曼原虫的仓鼠体内，有 50%的治愈效果。这些结果表明，贝雷醇类化合物是局部应用治疗皮肤利什曼病的潜在候选药物。体外试验表明，L.（V）巴西利什曼原虫的无鞭毛体对中间产物 10 和 11 的 EC 分别为 1.1±0.1 和 1.3±0.04μg/mL，SI 分别为 3.1 和 3.5。
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