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来自博韦假茉莉（爵床科）叶片的生物碱提取物：具有抗疟原虫、抗氧化及红细胞存活活性。

Alkaloidal Extracts from P. Beauv. (Avicenniaceae) Leaf: An Antiplasmodial, Antioxidant, and Erythrocyte Viable.

作者信息

Ahmed Mustapha A, Ameyaw Elvis O, Armah Francis A, Fynn Patrick M, Asiamah Isaac, Ghartey-Kwansah George, Zoiku Felix K, Ofori-Attah Ebenezer, Adokoh Christian K

机构信息

Department of Biomedical Sciences, School of Allied Health Sciences, University of Cape Coast, Cape Coast, Ghana.

Small Animal Teaching Hospital, SVM, CBAS, University of Ghana, Legon, Accra, Ghana.

出版信息

Adv Pharmacol Pharm Sci. 2024 Jan 9;2024:4541581. doi: 10.1155/2024/4541581. eCollection 2024.

DOI:10.1155/2024/4541581
PMID:38235482
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10791479/
Abstract

BACKGROUND

The emergence of drug-resistant parasites impedes disease management and eradication efforts. Hence, a reinvigorated attempt to search for potent lead compounds in the mangroves is imperative.

AIM

This study evaluates antiplasmodial activity, antioxidant properties, and cytotoxicity of leaf alkaloidal extracts.

METHODS

The leaves were macerated with 70% ethanol to obtain a total crude extract. Dichloromethane and chloroform-isopropanol (3 : 1, v/v) were used to extract the crude alkaloids and quaternary alkaloids from the total crude. The antiplasmodial activities of the alkaloidal extracts were performed against 3D7 chloroquine-sensitive clone via the SYBR Green I fluorescence assay with artesunate serving as the reference drug. The alkaloidal extracts were further evaluated for antioxidant properties via the total antioxidant capacity (TAC), the total glutathione concentration (GSH), the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, and the ferric-reducing antioxidant power (FRAP) methods. The cytotoxic activity of the alkaloidal extracts was tested on erythrocytes using a 3-(4,5-dimethylthiazol-2-yl)-5-diphenyltetrazolium bromide-MTT assay with little modification. The phytocompounds in the alkaloidal extracts were identified via gas chromatography-mass spectrometry (GC-MS) techniques.

RESULTS

The total crude extract showed good antiplasmodial activity (IC = 11.890 g/mL). The crude and quaternary alkaloidal extracts demonstrated promising antiplasmodial effects with IC values of 6.217 and 6.285 g/mL, respectively. The total crude and alkaloidal extracts showed good antioxidant properties with negligible cytotoxicity on erythrocytes with good selectivity indices. The GC-MS spectral analysis of crude alkaloidal extracts gave indole and isoquinoline alkaloids and several other compounds. Dexrazoxane was found to be the main compound predicted, with an 86% peak area in the quaternary alkaloidal extract.

CONCLUSION

The crude and quaternary alkaloidal extracts exhibited antiplasmodial activities and ability to inhibit oxidative stress with negligible toxicity on erythrocytes. This may be good characteristics to avoid oxidative stress related to infection in the treatment of malaria.

摘要

背景

耐药寄生虫的出现阻碍了疾病管理和根除工作。因此，迫切需要重新努力在红树林中寻找有效的先导化合物。

目的

本研究评估叶生物碱提取物的抗疟活性、抗氧化特性和细胞毒性。

方法

将叶子用70%乙醇浸渍以获得总粗提物。用二氯甲烷和氯仿 - 异丙醇（3∶1，v/v）从总粗提物中提取粗生物碱和季铵生物碱。通过SYBR Green I荧光测定法，以青蒿琥酯作为参比药物，对生物碱提取物针对3D7氯喹敏感克隆进行抗疟活性测试。通过总抗氧化能力（TAC）、总谷胱甘肽浓度（GSH）、DPPH（2,2 - 二苯基 - 1 - 苦基肼）测定法和铁还原抗氧化能力（FRAP）方法进一步评估生物碱提取物的抗氧化特性。对生物碱提取物的细胞毒性在红细胞上使用3 -（4,5 - 二甲基噻唑 - 2 - 基）- 5 - 二苯基四氮唑溴盐 - MTT测定法进行测试，仅做了少许修改。通过气相色谱 - 质谱（GC - MS）技术鉴定生物碱提取物中的植物化合物。

结果

总粗提物显示出良好的抗疟活性（IC = 11.890 μg/mL）。粗生物碱提取物和季铵生物碱提取物表现出有前景的抗疟效果，IC值分别为6.217和6.285 μg/mL。总粗提物和生物碱提取物显示出良好的抗氧化特性，对红细胞的细胞毒性可忽略不计，具有良好的选择性指数。粗生物碱提取物的GC - MS光谱分析给出了吲哚和异喹啉生物碱以及其他几种化合物。发现右丙亚胺是预测的主要化合物，在季铵生物碱提取物中的峰面积为86%。

结论

粗生物碱提取物和季铵生物碱提取物表现出抗疟活性以及抑制氧化应激的能力，对红细胞的毒性可忽略不计。这可能是在疟疾治疗中避免与感染相关的氧化应激的良好特性。

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