Department of Microbiology, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, Uttar Pradesh, India.
ICAR-Directorate of Medicinal and Aromatic Plants Research, Boriavi, 387310 Anand, Gujarat, India.
J Ethnopharmacol. 2019 May 10;235:489-500. doi: 10.1016/j.jep.2019.02.021. Epub 2019 Feb 11.
The whole plant of Andrographis paniculata (Burm. f.) Wall.ex Nees is used traditionally in different forms by the local people of Asian countries owing to its myriad medicinal properties. Its use as an anthelmintic has been mentioned in literature but has not been well elucidated.
To determine anthelmintic effects of extracts from leaves of A.paniculata against human hookworm species based on a standard assay system and to establish the effects of major active compounds responsible for the effects.
Ovicidal and larvicidal activities of extracts of leaves of A.paniculata in different solvents ethanol (Et), methanol (Met), ethyl acetate (EA) and petroleum ether (PE) was studied against field isolates of Ancylostoma duodenale collected and cultivated from hookworm infected human stool samples by egg hatch and larval motility assays. Major active compounds namely andrographolide (AP1), neoandrographolide (AP2) and andrograpanin (AP3) were estimated quantitatively in all the extracts by high-performance liquid chromatography (HPLC) and mass spectrometry (MS) analysis. Anthelmintic effects (ED, LC) and presence of the marker compounds in each extract was statistically analyzed by principal component analysis (PCA). Further, biological activities of pure compounds of AP1, AP2, AP3 were assessed to validate the results of the study.
Extracts in ethanol and methanol showed highest activity in inhibition of egg hatching with lowest ED values (0.017 and 0.02 mg/mL respectively) while ethyl acetate extract had the highest activity against larval motility (0.001 mg/mL) followed by ethanol (0.019 mg/mL). On HPLC analysis, andrographolide content (%), the major diterpene compound, in Met and Et was 0.85 and 1.43 respectively. On PCA, andrographolide component in the extracts was associated with significant inhibitory effects both on egg hatching and larval motility. Pure compound AP1 also showed significant ovicidal and larvicidal activities at concentrations 0.125 µg/mL and 0.019 mg/mL respectively.
Andrographolide is one of the main phytochemical responsible for significant ovicidal and larvicidal activity against field isolates of A.duodenale from human infections and can be developed as a potential therapeutic choice.
全株穿心莲(Burm. f.)Wall.ex Nees 以不同形式被亚洲国家的当地人传统使用,因为它具有多种药用特性。文献中提到过它作为驱虫剂的用途,但尚未得到充分阐明。
根据标准检测系统,确定穿心莲叶提取物对人体钩虫物种的驱虫作用,并确定负责这些作用的主要活性化合物的作用。
通过卵孵化和幼虫运动检测,研究了不同溶剂乙醇(Et)、甲醇(Met)、乙酸乙酯(EA)和石油醚(PE)提取物对从钩虫感染的人类粪便样本中分离培养的十二指肠钩虫的杀卵和杀幼虫活性。通过高效液相色谱(HPLC)和质谱(MS)分析定量测定所有提取物中的主要活性化合物即穿心莲内酯(AP1)、新穿心莲内酯(AP2)和穿心莲内酯(AP3)。通过主成分分析(PCA)对驱虫效果(ED、LC)和每种提取物中标记化合物的存在进行统计学分析。此外,还评估了 AP1、AP2 和 AP3 纯化合物的生物活性,以验证研究结果。
乙醇和甲醇提取物在抑制卵孵化方面表现出最高的活性,最低 ED 值分别为 0.017 和 0.02mg/mL,而乙酸乙酯提取物对幼虫运动的活性最高(0.001mg/mL),其次是乙醇(0.019mg/mL)。HPLC 分析显示,Met 和 Et 中的主要二萜化合物穿心莲内酯含量(%)分别为 0.85 和 1.43。PCA 结果表明,提取物中的穿心莲内酯成分与对卵孵化和幼虫运动的显著抑制作用相关。纯化合物 AP1 在浓度为 0.125µg/mL 和 0.019mg/mL 时也表现出显著的杀卵和杀幼虫活性。
穿心莲内酯是导致对人体感染的十二指肠钩虫的显著杀卵和杀幼虫活性的主要植物化学物质之一,可开发为潜在的治疗选择。