Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Antwerp University, Antwerp, Belgium.
Parasitol Res. 2014 Aug;113(8):2925-32. doi: 10.1007/s00436-014-3954-1. Epub 2014 Jun 7.
The search for new therapeutic agents from natural sources has been a constant for the treatment of diseases such as leishmaniasis. Herein, in vitro and in vivo pharmacological activities of pure major phenolic constituents (caffeic acid, chlorogenic acid, ferulic acid, quercetin, and rosmarinic acid) from Pluchea carolinensis against Leishmania amazonensis are presented. Pure compounds showed inhibitory activity against promastigotes (IC50 = 0.2-0.9 μg/mL) and intracellular amastigotes (IC50 = 1.3-2.9 μg/mL). Four of them were selected after testing against macrophages of BALB/c mice: caffeic acid, ferulic acid, quercetin, and rosmarinic acid, with selective indices of 11, 17, 10, and 20, respectively. Ferulic acid, rosmarinic acid, and caffeic acid controlled lesion size development and parasite burden in footpads from BALB/c experimentally infected mice, after five injections of compounds by intralesional route at 30 mg/kg every 4 days. Pure compounds from P. carolinensis demonstrated antileishmanial properties.
从天然来源寻找新的治疗剂一直是治疗利什曼病等疾病的一个不变目标。本文报道了从假泽兰属植物中提取的主要酚类纯成分（咖啡酸、绿原酸、阿魏酸、槲皮素和迷迭香酸）的体外和体内抗亚马逊利什曼原虫的药理学活性。纯化合物对前鞭毛体（IC50=0.2-0.9μg/mL）和内体无鞭毛体（IC50=1.3-2.9μg/mL）均具有抑制活性。在对 BALB/c 小鼠巨噬细胞进行测试后，选择了四种化合物进行后续研究：咖啡酸、阿魏酸、槲皮素和迷迭香酸，其选择性指数分别为 11、17、10 和 20。阿魏酸、迷迭香酸和咖啡酸通过在 30mg/kg 剂量下经皮内注射给药，每 4 天 1 次，共注射 5 次，控制了 BALB/c 实验感染小鼠后足垫病变大小的发展和寄生虫负荷。假泽兰属植物中的纯化合物具有抗利什曼原虫的特性。
