Petrelli Riccardo, Ranjbarian Farahnaz, Dall'Acqua Stefano, Papa Fabrizio, Iannarelli Romilde, Ngahang Kamte Stephane L, Vittori Sauro, Benelli Giovanni, Maggi Filippo, Hofer Anders, Cappellacci Loredana
School of Pharmacy, University of Camerino, Camerino, Italy.
Department of Medical Biochemistry and Biophysics, Umeå University, Umeå, Sweden.
Parasitol Int. 2017 Apr;66(2):146-151. doi: 10.1016/j.parint.2017.01.001. Epub 2017 Jan 10.
Among natural products, sesquiterpenes have shown promising inhibitory effects against bloodstream forms of Trypanosoma brucei, the protozoan parasite causing human African trypanosomiasis (HAT). Smyrnium olusatrum (Apiaceae), also known as Alexanders or wild celery, is a neglected horticultural crop characterized by oxygenated sesquiterpenes containing a furan ring. In the present work we explored the potential of its essential oils obtained from different organs and the main oxygenated sesquiterpenes, namely isofuranodiene, germacrone and β-acetoxyfuranoeudesm-4(15)-ene, as inhibitors of Trypanosoma brucei. All essential oils effectively inhibited the growth of parasite showing IC values of 1.9-4.0μg/ml. Among the main essential oil constituents, isofuranodiene exhibited a significant and selective inhibitory activity against T. brucei (IC of 0.6μg/ml, SI=30), with β-acetoxyfuranoeudesm-4(15)-ene giving a moderate potentiating effect. These results shed light on the possible application of isofuranodiene as an antiprotozoal agent to be included in combination treatments aimed not only at curing patients but also at preventing the diffusion of HAT.
在天然产物中，倍半萜烯已显示出对布氏锥虫血液型有良好的抑制作用，布氏锥虫是引起人类非洲锥虫病（HAT）的原生动物寄生虫。香芹（伞形科），也称为亚历山大草或野芹菜，是一种被忽视的园艺作物，其特征是含有呋喃环的氧化倍半萜烯。在本研究中，我们探索了从不同器官获得的其精油以及主要的氧化倍半萜烯，即异呋喃二烯、吉马酮和β-乙酰氧基呋喃桉叶-4(15)-烯作为布氏锥虫抑制剂的潜力。所有精油均有效抑制寄生虫生长，IC值为1.9-4.0μg/ml。在主要的精油成分中，异呋喃二烯对布氏锥虫表现出显著的选择性抑制活性（IC为0.6μg/ml，SI=30），β-乙酰氧基呋喃桉叶-4(15)-烯有中等程度的增效作用。这些结果揭示了异呋喃二烯作为一种抗原生动物药物的可能应用，可用于联合治疗，不仅旨在治愈患者，还旨在预防HAT的传播。
