番石榴叶提取物抗β-血红素形成的筛选

S. Abu-Lafi, M. Akkawi, Qassem Abu-Remeleh, P. Lutgen
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引用次数: 3

摘要

背景:疟疾控制是至关重要的,因为不仅在东南亚,而且在非洲,抗疟药耐药性日益增长。开发新颖、安全、有效和负担得起的药物是抗击疟疾的关键。药用植物和一些水果是治疗疟疾药物发现工作的重要来源。目的:研究番石榴水浸提液和水乙醇叶提取物对β-血红素形成的体外抑制作用。方法:采用LC-ESi-MS-PDA全扫描方法,在100 ~ 1200amu的质量范围内对番石榴叶中可能存在的活性次生代谢物进行鉴定。此外,采用基于β-血红素抑制和405nm光密度测量的体外比色半定量分析。结果与讨论:35%乙醇提取番石榴叶的效果表明,浓度在1 ~ 0.4mg/ml范围内的活性优于番石榴水提取物,且与阳性对照相当。经鉴定的黄酮类苷有槲皮素3- O -糖苷、槲皮素-没食子糖苷、桑皮素-3- O -葡糖苷、桑皮素-3- O -阿拉伯糖苷、槲皮素-3- O -阿拉伯糖苷(愈创木黄苷)和鞣花酸。这表明自由血红素与β-血红素形成的络合作用令人鼓舞。
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Screening of guava (Psidium guajava) leaves extracts against β-hematin formation 
Background: Malaria control is crucial as a result of the growing antimalarial drug- resistance not only in South-East Asia but also in Africa. Developing novel, safe, effective, and affordable drugs is a key to combat malaria. Medicinal plants and some fruits are intensive sources in the drug discovery effort to treat malaria. Objective: The main aim of the work is to investigate Guava ( Psidium guajava ) infused water and water-ethanol leaf extracts against β-hematin formation in-vitro . Methodology: To determine the identity of any possible active secondary metabolite in P. guajava leaves, a full scan LC-ESi-MS-PDA was run within a mass range of 100-1200 amu. Moreover, the in-vitro colorimetric semi-quantitative assays that are based on β-hematin inhibition and optical density measurement at 405nm were utilized. Results and discussion: The effect of using 35% ethanol in extracting guava leaves showed that concentrations between 1 and 0.4mg/ml have an activity superior to guava water extract and comparable to the positive control. Among the identified flavonoids glycosides are quercetin 3- O -glycoside, quercetin-galloylhexoside, morin-3- O -lyxoside, morin-3- O -arabinoside, quercein-3- O -arabinoside (guaijaverin) and ellagic acid. This indicates to an encouraging complexation with the free heme over β-hematin formation.
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