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胱氨酸稳定的 Morinda lucida(Benth)叶肽提取物具有抗疟活性,并增强了感染 P. berghei 的小鼠的抗氧化防御系统。

Cysteine-stabilised peptide extract of Morinda lucida (Benth) leaf exhibits antimalarial activity and augments antioxidant defense system in P. berghei-infected mice.

机构信息

Department of Biochemistry, Faculty of Life Sciences, University of Ilorin, Ilorin, Nigeria.

Department of Biochemistry, Faculty of Life Sciences, University of Ilorin, Ilorin, Nigeria.

出版信息

J Ethnopharmacol. 2017 Jul 31;207:118-128. doi: 10.1016/j.jep.2017.06.026. Epub 2017 Jun 20.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Cysteine-stabilised peptides (CSP) are majorly explored for their bioactivities with applications in medicine and agriculture. Morinda lucida leaf is used indigenously for the treatment of malaria; it also contains CSP but the role of CSP in the antimalarial activity of the leaf has not been evaluated.

AIM OF THE STUDY

This study was therefore performed to evaluate the antimalarial activity of partially purified cysteine-stabilised peptide extract (PPCPE) of Morinda lucida leaf and its possible augmentation of the antioxidant systems of liver and erythrocytes in murine malaria.

MATERIALS AND METHODS

PPCPE was prepared from Morinda lucida leaf. The activity of PPCPE was evaluated in vitro against Plasmodium falciparum W2 and its cytotoxicity against a BGM kidney cell line. PPCPE was also evaluated for its antimalarial activity and its effects on selected liver and erythrocyte antioxidant parameters in P. berghei NK65-infected mice.

RESULTS

PPCPE was not active against P. falciparum W2 (IC: >50µg/ml) neither was it cytotoxic (MLD: >1000µg/ml). However, PPCPE was active against P. berghei NK65 in vivo, causing 51.52% reduction in parasitaemia at 31.25mg/Kg body weight on day 4 post-inoculation. PPCPE significantly reduced (P < 0.05) malondialdehyde concentrations in the liver and erythrocyte at higher doses compared to untreated controls. PPCPE increased glutathione concentration and activities of glutathione peroxidase, glutathione reductase, superoxide dismutase and catalase in a dose-dependent manner, which was significant (P < 0.05) at higher doses compared to the untreated controls.

CONCLUSION

The results suggest that PPCPE may require bioactivation in vivo in order to exert its antimalarial effect and that PPCPE may augment the antioxidant defense system to alleviate the reactive oxygen species-mediated complications of malaria.

摘要

民族药理学相关性

半胱氨酸稳定肽(CSP)主要因其生物活性而被广泛研究,这些活性在医学和农业领域有应用。密蒙花的叶子在当地被用于治疗疟疾;它也含有 CSP,但 CSP 在叶子的抗疟活性中的作用尚未得到评估。

研究目的

因此,本研究旨在评估密蒙花叶部分纯化的半胱氨酸稳定肽提取物(PPCPE)的抗疟活性及其对伯氏疟原虫感染小鼠肝和红细胞抗氧化系统的可能增强作用。

材料和方法

PPCPE 是从密蒙花叶中制备的。评估 PPCPE 在体外对恶性疟原虫 W2 的活性及其对 BGM 肾细胞系的细胞毒性。还评估了 PPCPE 在伯氏疟原虫 NK65 感染小鼠中的抗疟活性及其对选定肝和红细胞抗氧化参数的影响。

结果

PPCPE 对恶性疟原虫 W2 没有活性(IC:>50µg/ml),也没有细胞毒性(MLD:>1000µg/ml)。然而,PPCPE 在体内对伯氏疟原虫 NK65 有效,在接种后第 4 天,在 31.25mg/Kg 体重时,寄生虫血症减少了 51.52%。与未处理的对照组相比,PPCPE 在较高剂量下显著降低(P<0.05)肝和红细胞中的丙二醛浓度。PPCPE 以剂量依赖的方式增加谷胱甘肽浓度和谷胱甘肽过氧化物酶、谷胱甘肽还原酶、超氧化物歧化酶和过氧化氢酶的活性,与未处理的对照组相比,在较高剂量下这些变化显著(P<0.05)。

结论

结果表明,PPCPE 可能需要在体内进行生物活化才能发挥其抗疟作用,并且 PPCPE 可能增强抗氧化防御系统,以减轻疟疾引起的活性氧物质介导的并发症。

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