School of Chemistry and Molecular Bioscience, Faculty of Science Medicine and Health, University of Wollongong, Wollongong, NSW, 2522, Australia.
Department of Veterinary Physiology, Biochemistry and Pharmacology University of Jos, Jos Plateau State, Nigeria.
BMC Complement Med Ther. 2021 Sep 13;21(1):231. doi: 10.1186/s12906-021-03406-y.
Neorautanenia mitis, Hydnora abyssinica, and Senna surattensis are medicinal plants with a variety of traditional uses. In this study, we sought to isolate the bioactive compounds responsible for some of these activities, and to uncover their other potential medicinal properties.
The DCM and ethanol extracts of the roots of N. mitis and H. abyssinica, and the leaves of S. surattensis were prepared and their phytochemical components were isolated and purified using chromatographic methods. These extracts and their pure phytochemical components were evaluated in in-vitro models for their inhibitory activities against Plasmodium falciparum, Trypanosoma brucei rhodesiense, Mycobacterium tuberculosis, α-amylase (AA), and α-glucosidase (AG).
Rautandiol B had significant inhibitory activities against two strains of Plasmodium falciparum showing a high safety ratio (SR) and IC values of 0.40 ± 0.07 μM (SR - 108) and 0.74 ± 0.29 μM (SR - 133) against TM4/8.2 and K1CB1, respectively. While (-)-2-isopentenyl-3-hydroxy-8-9-methylenedioxypterocarpan showed the highest inhibitory activity against T. brucei rhodesiense with an IC value of 4.87 ± 0.49 μM (SR > 5.83). All crude extracts showed inhibitory activities against AA and AG, with three of the most active phytochemical components; rautandiol A, catechin, and dolineon, having only modest activities against AG with IC values of 0.28 mM, 0.36 mM and 0.66 mM, respectively.
These studies have led to the identification of lead compounds with potential for future drug development, including Rautandiol B, as a potential lead compound against Plasmodium falciparum. The relatively higher inhibitory activities of the crude extracts against AG and AA over their isolated components could be due to the synergistic effects between their phytochemical components. These crude extracts could potentially serve as alternative inhibitors of AG and AA and as therapeutics for diabetes.
Neorautanenia mitis、Hydnora abyssinica 和 Senna surattensis 是具有多种传统用途的药用植物。在这项研究中，我们试图分离出负责其中一些活性的生物活性化合物，并发现它们的其他潜在药用特性。
从 N. mitis 和 H. abyssinica 的根部以及 S. surattensis 的叶子中提取 DCM 和乙醇提取物，并使用色谱方法分离和纯化其植物化学成分。评估这些提取物及其纯植物化学成分在体外模型中对恶性疟原虫、布氏锥虫罗得西亚、结核分枝杆菌、α-淀粉酶 (AA) 和 α-葡萄糖苷酶 (AG) 的抑制活性。
Rautandiol B 对两种恶性疟原虫株表现出显著的抑制活性，安全性比（SR）高，对 TM4/8.2 和 K1CB1 的 IC 值分别为 0.40±0.07μM（SR-108）和 0.74±0.29μM（SR-133）。而（-）-2-异戊烯基-3-羟基-8-9-亚甲二氧基紫檀烷对布氏锥虫罗得西亚显示出最高的抑制活性，IC 值为 4.87±0.49μM（SR>5.83）。所有粗提取物均对 AA 和 AG 具有抑制活性，其中三种最活跃的植物化学成分；rautandiol A、儿茶素和 dolineon，对 AG 的抑制活性仅适度，IC 值分别为 0.28mM、0.36mM 和 0.66mM。
这些研究导致了具有潜在未来药物开发前景的先导化合物的鉴定，包括 Rautandiol B，作为抗恶性疟原虫的潜在先导化合物。粗提取物对 AG 和 AA 的抑制活性相对高于其分离成分，这可能是由于其植物化学成分之间的协同作用。这些粗提取物可能是 AG 和 AA 的替代抑制剂，并可作为糖尿病的治疗方法。
