Lamien-Meda Aline, Kiendrebeogo Martin, Compaoré Moussa, Meda Roland N T, Bacher Markus, Koenig Karin, Pacher Thomas, Fuehrer Hans-Peter, Noedl Harald, Willcox Merlin, Novak Johannes
Institute of Animal Nutrition and Functional Plant Compounds, University of Veterinary Medicine, Veterinaerplatz 1, A-1210 Vienna, Austria.
Laboratoire de Biochimie et Chimie Appliquées, LABIOCA, University of Ouagadougou, 03 BP 7021 Ouagadougou 03, Burkina Faso.
Phytochemistry. 2015 Nov;119:51-61. doi: 10.1016/j.phytochem.2015.09.006. Epub 2015 Sep 28.
The present study focuses on development of phytochemical methods for quality assessment of two West-African Cochlospermum species (Cochlospermum planchonii and Cochlospermum tinctorium) traditionally used for malaria treatment in Burkina Faso. Antimalarial activity of preparations from dried rhizomes (decoction) was tested against the chloroquine-sensitive Plasmodium strain 3D7 using the histidine-rich protein II (HRP2) drug susceptibility assay and compared with extract preparations using organic solvents of different polarity. Two main apocarotenoids were isolated from rhizomes of C. planchonii and unambiguously identified as dihydrocochloxanthine and cochloxanthine by spectroscopic methods. Comparative HPLC analyses of thirty-nine (39) samples from markets and from collections in natural habitats of both species showed a high variability in the accumulation of cochloxanthines and related carotenoids which were proven to be characteristic for rhizomes of both species and generally absent in leaves. Furthermore, content of total phenolics and antioxidant activities (DPPH and FRAP) as well as haemolytic activity of various extracts was tested. The HPLC method presented here was validated and provides a good separation of both compounds including 10 minor carotenoids. Extracts from both species and pure cochloxanthine offered pronounced antioxidant activities and weak haemolytic activity while, in contrast, dihydrocochloxanthine had a strong haemolytic effect at the highest concentration analysed. However, cochloxanthine as well as dihydrocochloxanthine showed erythroprotective effects against the haemolytic activity of the reference saponin. Moderate antiplasmodial activity between 16 and 63 μg/ml were observed with all tested extracts, and lower IC50 values were obtained with pure dihydrocochloxanthine (IC50=6.9 μg/ml), cochloxanthine (IC50=6.8 μg/ml), the DCM fraction (IC50=2.4 μg/ml) and the ethyl acetate fraction (IC50=11.5μg/ml) derived from a methanolic extract of C. planchonii. This study shows a major variability of carotenoid content and antiplasmodial activity of both C. planchonii and C. tinctorium. The high haemolytic activity of dihydrocochloxanthine (at 100 μg/ml) should be considered as a selection criterion for choosing species phenotypes for treatment.
本研究聚焦于开发植物化学方法,用于评估布基纳法索传统上用于治疗疟疾的两种西非卷柏属植物(普兰雄卷柏和染色卷柏)的质量。使用富含组氨酸蛋白II(HRP2)药物敏感性试验,测试了干燥根茎(煎剂)制剂对氯喹敏感的疟原虫菌株3D7的抗疟活性,并与使用不同极性有机溶剂的提取物制剂进行了比较。从普兰雄卷柏的根茎中分离出两种主要的阿朴胡萝卜素,并通过光谱方法明确鉴定为二氢卷柏黄质和卷柏黄质。对来自市场和两种植物自然栖息地采集的39个样品进行的比较高效液相色谱分析表明,卷柏黄质和相关类胡萝卜素的积累存在高度变异性,这些物质被证明是两种植物根茎的特征性成分,而在叶子中通常不存在。此外,还测试了各种提取物的总酚含量、抗氧化活性(DPPH和FRAP)以及溶血活性。本文提出的高效液相色谱方法经过验证,能够很好地分离这两种化合物,包括10种次要类胡萝卜素。两种植物的提取物和纯卷柏黄质均具有显著的抗氧化活性和较弱的溶血活性,相比之下,二氢卷柏黄质在分析的最高浓度下具有很强的溶血作用。然而,卷柏黄质和二氢卷柏黄质均对参考皂苷的溶血活性表现出红细胞保护作用。所有测试提取物均观察到16至63μg/ml的中度抗疟活性,从普兰雄卷柏甲醇提取物中得到的纯二氢卷柏黄质(IC50=6.9μg/ml)、卷柏黄质(IC50=6.8μg/ml)、二氯甲烷馏分(IC50=2.4μg/ml)和乙酸乙酯馏分(IC50=11.5μg/ml)的IC50值较低。本研究表明,普兰雄卷柏和染色卷柏的类胡萝卜素含量和抗疟活性存在很大变异性。二氢卷柏黄质(100μg/ml时)的高溶血活性应作为选择用于治疗的物种表型的一个选择标准。