Kaushik Naveen K, Bagavan Asokan, Rahuman Abdul A, Zahir Abdul A, Kamaraj Chinnaperumal, Elango Gandhi, Jayaseelan Chidambaram, Kirthi Arivarasan V, Santhoshkumar Thirunavukkarasu, Marimuthu Sampath, Rajakumar Govindasamy, Tiwari Santosh K, Sahal Dinkar
Malaria Research Group, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Marg, New Delhi, 110067, India.
Department of Bioscience & Biotechnology, Banasthali University, P.O. Banasthali Vidyapith, Rajasthan, 304 022, India.
Malar J. 2015 Feb 7;14:65. doi: 10.1186/s12936-015-0564-z.
Development of resistance against the frontline anti-malarial drugs has created an alarming situation, which requires intensive drug discovery to develop new, more effective, affordable and accessible anti-malarial agents.
Inspired by their ethnobotanical reputation for being effective against febrile diseases, antiplasmodial potential of ethyl acetate extracts (EAE) and methanol extracts (ME) of 17 medicinal plants collected from the Eastern Ghats of South India and Buchpora, North India were explored against Plasmodium falciparum in vitro using the SYBR Green assay. The results were validated both by confirmation that the fall in fluorescence signal was not due to quenching effects mediated by phytochemical extracts and by Giemsa-stained microscopy.
Using EAE or ME, promising antiplasmodial activity (IC₅₀ Pf3D7 ≤ 20 μg/ml), was seen in Aerva lanata (Whole aerial parts-EAE), Anisomeles malabarica (Leaf-EAE), Anogeissus latifolia (bark-EAE), Cassia alata (leaves-EAE), Glycyrrhiza glabra (root-EAE), Juglans regia (seed-ME), Psidium guajava (leaf-ME and EAE) and Solanum xanthocarpum (Whole aerial parts-EAE). EAEs from leaves of Couroupita guianensis, Euphorbia hirta, Pergularia daemia, Tinospora cordifolia and Tridax procumbens as also ME from Ricinus communis (leaf and seed) showed good antiplasmodial activity (Pf 3D7 IC₅₀ 21 - 40 μg/ml). Moderate activity (Pf 3D7 IC₅₀: 40-60 μg/mL) was shown by the leaf EAEs of Cardiospermum halicacabum, Indigofera tinctoria and Ricinus communis while the remaining extracts showed marginal (Pf 3D7 IC₅₀ 60 to >100 μg/ml) activities. The promising extracts showed good resistance indices (0.41 - 1.4) against the chloroquine resistant INDO strain of P. falciparum and good selectivity indices (3 to > 22.2) when tested against the HeLa cell line.
These results provide validity to the traditional medicinal usage of some of these plants and further make a case for activity-guided purification of new pharmacophores against malaria.
对一线抗疟药物产生耐药性的情况已引发警报,这需要大力开展药物研发以开发新型、更有效、可负担且可及的抗疟药物。
受这些植物在民族植物学上对治疗发热性疾病有效的声誉启发,对从印度南部东高止山脉和印度北部布乔波拉采集的17种药用植物的乙酸乙酯提取物(EAE)和甲醇提取物(ME)针对恶性疟原虫的体外抗疟潜力进行了探索,采用SYBR Green检测法。通过确认荧光信号的下降不是由植物化学提取物介导的淬灭效应导致以及吉姆萨染色显微镜检查对结果进行了验证。
使用EAE或ME时,在翅果草(全地上部分 - EAE)、马拉巴罗勒(叶 - EAE)、大叶藤黄(树皮 - EAE)、翅荚决明(叶 - EAE)、光果甘草(根 - EAE)、胡桃(种子 - ME)、番石榴(叶 - ME和EAE)和刺天茄(全地上部分 - EAE)中观察到了有前景的抗疟活性(IC₅₀ Pf3D7≤20μg/ml)。圭亚那炮弹树、大戟、白首乌、心叶地锦和三叶鬼针草叶的EAE以及蓖麻(叶和种子)的ME显示出良好的抗疟活性(Pf 3D7 IC₅₀ 21 - 40μg/ml)。倒地铃叶、木蓝叶和蓖麻叶的EAE表现出中等活性(Pf 3D7 IC₅₀:40 - 60μg/mL),而其余提取物表现出边缘活性(Pf 3D7 IC₅₀ 60至>100μg/ml))。有前景的提取物对氯喹耐药的恶性疟原虫INDO株显示出良好的耐药指数(0.41 - 1.4),并且在针对HeLa细胞系进行测试时显示出良好的选择性指数(3至>22.2)。
这些结果为其中一些植物的传统药用价值提供了有效性依据,并进一步证明了针对疟疾对新药效团进行活性导向纯化的必要性。