Tabefam Marzieh, Farimani Mahdi Moridi, Danton Ombeline, Ramseyer Justine, Kaiser Marcel, Ebrahimi Samad N, Salehi Peyman, Batooli Hossien, Potterat Olivier, Hamburger Matthias
Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, G. C., Evin, Tehran, Iran.
Division of Pharmaceutical Biology, University of Basel, Switzerland.
Planta Med. 2018 Aug;84(12-13):913-919. doi: 10.1055/a-0608-4946. Epub 2018 Apr 26.
As part of a screening for new antiparasitic natural products from Iranian plants, -hexane and ethyl acetate extracts from the aerial parts of were found to exhibit strong inhibitory activity against and . The activity was tracked by high-performance liquid chromatography (HPLC)-based activity profiling. Preparative isolation by a combination of silica gel column chromatography and HPLC afforded 17 diterpenoids (1: -17: ), including 14 abietane-, two icetexane-, and one isopimarane-type derivatives. Among these, (5,10)-11-hydroxy-12-methoxy-20-norabieta-8,11,13-triene (2: ), 12-hydroxy-norabieta-1(10),8,11,13-tetraene-1,11-furan (6: ), and 12-methoxybarbatusol (9: ) were new compounds, the structure of which was established by comprehensive spectroscopic data analysis (one- and two-dimensional nuclear magnetic resonance, high-resolution electrospray ionization mass spectrometry, electronic circular dichroism). The antiprotozoal activity of the isolated compounds was evaluated against , and . Selectivity indexes (SI) were calculated in comparison to cytotoxicity on rat myoblast (L6) cells. Particularly active were 7-ethoxyrosmanol (4: ) with an IC of 0.8 µM against (SI 14.9) and an IC of 1.8 µM (SI 6.9) against , ferruginol (8: ) with an IC of 2.9 µM (SI 19.2) against , and miltiodiol (10: ) with an IC of 0.5 µM (SI 10.5) against . None of the compounds exhibited selective toxicity against (SI ≤ 1.6).
作为从伊朗植物中筛选新型抗寄生虫天然产物的一部分，发现[植物名称]地上部分的正己烷和乙酸乙酯提取物对[寄生虫名称1]和[寄生虫名称2]具有很强的抑制活性。通过基于高效液相色谱（HPLC）的活性分析来追踪该活性。采用硅胶柱色谱和HPLC相结合的方法进行制备分离，得到了17种二萜类化合物（1：[化合物1名称]-17：[化合物17名称]），包括14种松香烷型、2种异贝壳杉烷型和1种异海松烷型衍生物。其中，（5,10）-11-羟基-12-甲氧基-20-降松香-8,11,13-三烯（2：[化合物2名称]）、12-羟基-降松香-1(10),8,11,13-四烯-1,11-呋喃（6：[化合物6名称]）和12-甲氧基巴巴妥醇（9：[化合物9名称]）是新化合物，其结构通过综合光谱数据分析（一维和二维核磁共振、高分辨率电喷雾电离质谱、电子圆二色性）得以确定。对分离得到的化合物针对[寄生虫名称1]、[寄生虫名称2]和[寄生虫名称3]的抗原虫活性进行了评估。与对大鼠成肌细胞（L6）的细胞毒性相比，计算了选择性指数（SI）。特别有活性的是7-乙氧基迷迭香酚（4：[化合物4名称]），对[寄生虫名称1]的IC50为0.8 μM（SI为14.9），对[寄生虫名称2]的IC50为1.8 μM（SI为6.9）；铁锈醇（8：[化合物8名称]）对[寄生虫名称1]的IC50为2.9 μM（SI为19.2）；以及米替多醇（10：[化合物10名称]）对[寄生虫名称2]的IC50为0.5 μM（SI为10.5）。没有一种化合物对[寄生虫名称3]表现出选择性毒性（SI≤1.6）。
