Torres Fernando, Robledo Sara M, Quiñones Wiston, Escobar Gustavo, Archbold Rosendo, Correa Edwin, Gil Juan Fernando, Arbeláez Natalia, Murillo Javier, Echeverri Fernando
Group of Organic Chemistry Natural Products, Institute of Chemistry, Universidad de Antioquia, Medellin, Colombia.
PECET-Facultad de Medicina Universidad de Antioquia, Program of Study and Control of Tropical Diseases, Faculty of Medicine, Universidad de Antioquia, Medellin, Colombia.
Front Pharmacol. 2020 Dec 24;11:584668. doi: 10.3389/fphar.2020.584668. eCollection 2020.
Through bioguided assays, the leishmanicidal and trypanocidal effects of an ethanol extract, seven fractions, and two pure substances obtained from Amshoff sawdust were established. The effectiveness of the two metabolites was confirmed in a hamster model of cutaneous Leishmaniasis by and in Balb/c mice infected by . , 3,5-dimethoxystilbene was the most active against amastigotes, with a median lethal concentration (LC) of 4.18 μg/ml (17.40 μM) and a selectivity index of 3.55, but showed moderate activity for , with a median effective concentration (EC) value of 27.7 μg/ml (115.36 μM). Flavanone pinostrobin, meanwhile, showed high activity against with an EC of 13.61 μg/ml (50.39 μM), as well as for with an EC of 18.2 μg/ml (67.38 μM). The animal model assay of cutaneous Leishmaniasis showed that 50% of the hamsters treated with pinostrobin were definitively cured the cutaneous ulcer, and 40% showed an improvement, with a reduction in the size of the of 84-87%. Moreover, Balb/c mice experimentally infected with and treated for 25 days with pinostrobin experienced a reduction in their parasitemia by 71%. These results demonstrate the high potential of Amshoff against cutaneous Leishmaniasis and American trypanosomiasis and indicate the pharmacological potential of waste from the wood industry, which has tons of potentially useful chemicals for the development of new medicines.
通过生物导向分析，确定了从阿姆肖夫木屑中获得的乙醇提取物、七个馏分和两种纯物质的杀利什曼原虫和杀锥虫作用。在皮肤利什曼病的仓鼠模型以及感染了[具体寄生虫名称缺失]的Balb/c小鼠中证实了这两种代谢物的有效性。[具体信息缺失]，3,5 - 二甲氧基芪对无鞭毛体最具活性，中位致死浓度（LC）为4.18μg/ml（17.40μM），选择性指数为3.55，但对[具体寄生虫名称缺失]显示出中等活性，中位有效浓度（EC）值为27.7μg/ml（115.36μM）。同时，黄酮类化合物松属素对[具体寄生虫名称缺失]表现出高活性，EC为13.61μg/ml（50.39μM），对[具体寄生虫名称缺失]的EC为18.2μg/ml（67.38μM）。皮肤利什曼病的动物模型试验表明，用松属素治疗的仓鼠中有50%的皮肤溃疡得到彻底治愈，40%有改善，溃疡大小减少了84 - 87%。此外，实验感染[具体寄生虫名称缺失]并用松属素治疗25天的Balb/c小鼠的寄生虫血症降低了71%。这些结果证明了阿姆肖夫对皮肤利什曼病和美洲锥虫病具有很高的潜力，并表明木材工业废料的药理潜力，其含有数吨可能对开发新药有用的化学物质。
