Laportea aestuans (L.) Chew 提取物的抗疟研究和植物化学分析

Kolade O. Faloye, S. Oguntimehin, S. A. Adesida, K. Olufolabo, O. I. Bello, Israel A. Oguntimehin, Jeremiah P. Ugwo, Tolulope B. Babaagba, Blessing I. Okunribido, J. Aladesanmi
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摘要

本研究利用化学抑制和治疗模型验证了Laportea aestuans提取物的抗疟功效,确定了其最活跃的部分,并对活跃部分进行了化学分析。用 80% 的甲醇萃取 L. aestuans(LA)的气生部分,并通过给每组 5 只小鼠口服 100、200、400 和 800 mg/kg 的萃取物,检测其化学抑制和治疗抗疟活性。然后将提取物悬浮于水中,用二氯甲烷进行分馏,得到二氯甲烷(DLA)和水(ALA)馏分。随后对这些馏分(10、20、40 和 80 毫克/千克)进行抗疟活性测试,并对活性最高的馏分进行气相色谱-质谱分析。结果发现毒性水平高于 2000 毫克/千克。在为期四天的化学抑制性抗疟试验中,所记录的活性呈剂量依赖性,最高可达 400 毫克/千克。其活性明显低于氯喹。最低剂量为 100 毫克/千克时,提取物的抗疟活性为 42%。在治疗试验中,LA 提取物的活性呈剂量依赖性,明显高于阴性对照组。DLA和ALA馏分在所有剂量下都具有相当的治疗活性。在 10 毫克/千克的剂量下,ALA 和 DLA 的清除率分别为 81.25 ± 1.84 和 87.45 ± 1.35,明显高于阴性对照(0.00 ± 0.00),明显低于阳性对照(94.93 ± 0.26)。化学成分分析表明,二氯甲烷馏分中含有非极性和中等极性成分。LA 提取物具有良好的抗疟活性,支持将其作为一种抗疟药物用于民族医药中。
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Antimalarial Studies and Phytochemical Profiling of Laportea aestuans (L.) Chew Extractives
This study validated the antimalarial efficacy of Laportea aestuans extract using chemosuppressive and curative models, identified its most active fraction, and performed chemical profiling of the active fraction. The aerial part of L. aestuans (LA) was extracted with 80% methanol and assayed for its chemosuppressive and curative antimalarial activities through the oral administration of the extract (100, 200, 400 and 800 mg/kg) to groups consisting of five mice each. The extract was thereafter suspended in water and partitioned with dichloromethane to afford the dichloromethane (DLA) and aqueous (ALA) fractions. The fractions (10, 20, 40, and 80 mg/kg) were thereafter tested for their antimalarial activity followed by GC-MS analysis of the most active fraction. The toxicity level was found to be above 2000 mg/kg. The activity recorded for the four-day chemosuppressive antimalarial tests showed a dose-dependent activity up to 400 mg/kg. The activity was significantly lower than that of chloroquine. The antimalarial activity of the extract at the lowest dose of 100 mg/kg was 42%. In the curative test, the extract of LA gave a dose-dependent activity that was significantly higher than the negative control. The DLA and ALA fractions gave a comparable curative activity across all doses. At 10 mg/kg, ALA and DLA gave percentage clearance of 81.25 ± 1.84 and 87.45 ± 1.35, respectively, which were significantly higher than that of the negative control (0.00 ± 0.00) and significantly lower than that of the positive control (94.93 ± 0.26). The chemical profiling revealed the presence of non-polar and medium-polar constituents in the dichloromethane fraction. The good antimalarial activity elicited by LA extractives supports its usage in ethnomedicine as an antimalarial agent.
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