Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences , University of Basel , Klingelbergstrasse 50 , 4056 Basel , Switzerland.
Department of Pharmacognosy, School of Pharmacy , Mashhad University of Medical Sciences , Mashhad , Iran.
J Nat Prod. 2019 Apr 26;82(4):958-969. doi: 10.1021/acs.jnatprod.8b01031. Epub 2019 Mar 27.
In a screening of Iranian plants for antiprotozoal activity a dichlomethane extract from the aerial parts of Helichrysum oocephalum showed in vitro antiprotozoal activity against Plasmodium falciparum and Leishmania donovani, with IC values of 4.01 ± 0.50 and 5.08 ± 0.07 μg/mL, respectively. The activity in the extract was tracked by HPLC-based activity profiling, and subsequent targeted preparative isolation afforded 24 compounds, including pyrones 22-24, phloroglucinol derivatives 12-19, and compounds containing both structural motifs (1-11, 20, and 21). Of these, 15 compounds were new natural products. The in vitro antiprotozoal activity of isolates was determined. Compound 3 showed good potency and selectivity in vitro against L. donovani (IC 1.79 ± 0.17 μM; SI 53).
在对伊朗植物进行抗原生动物活性筛选时，发现从 Helichrysum oocephalum 的地上部分提取的二氯甲烷提取物对疟原虫和利什曼原虫具有体外抗原生动物活性，IC 值分别为 4.01 ± 0.50 和 5.08 ± 0.07 μg/mL。提取物中的活性通过基于 HPLC 的活性分析进行跟踪，随后进行的靶向制备分离得到 24 种化合物，包括吡喃酮 22-24、间苯三酚衍生物 12-19 和同时含有这两种结构基序的化合物（1-11、20 和 21）。其中，15 种化合物为新的天然产物。测定了分离物的体外抗原生动物活性。化合物 3 对利什曼原虫（IC 1.79 ± 0.17 μM；SI 53）具有良好的体外活性和选择性。
