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吸湿链霉菌亚种代谢物提取物的14K和36K组分对体外疟原虫具有抗疟活性。

Fractions 14 and 36K of Metabolite Extract subsp. Hygroscopicus Have Antimalarial Activities Against in vitro.

作者信息

Fitri Loeki Enggar, Endharti Agustina Tri, Abidah Hafshah Yasmina, Khotimah Alif Raudhah Husnul, Endrawati Heni

机构信息

Department of Parasitology, Faculty of Medicine, Universitas Brawijaya, Malang, Indonesia.

Malaria Research Group, Faculty of Medicine, Universitas Brawijaya, Malang, Indonesia.

出版信息

Infect Drug Resist. 2023 May 12;16:2973-2985. doi: 10.2147/IDR.S400538. eCollection 2023.

Abstract

PURPOSE

The study was conducted to investigate the effectivity and the cytotoxicity of fractions 14 and 36K of metabolite extract of subsp. Hygroscopicus as an antimalarial compounds against in vitro.

METHODS

Fractions 14 and 36K of metabolite extract of subsp. Hygroscopicus produced by the fractionation process utilizing the Flash Column Chromatography (FCC) BUCHI Reveleris PREP. culture was used to assess the antimalarial activity of fractions 14 and 36K. Parasite densities and the ability of parasite growth were determined under microscopic. The cytotoxicity of the fractions was assessed using MTT assays on the MCF-7 cell line.

RESULTS

subsp. Hygroscopicus fractions 14 and 36K have antimalarial activity against , with fraction 14 having the more potent activity. The percentage of -infected erythrocytes was decreased as well as the increase of fraction concentration. Fraction 14 has the highest inhibition of parasite growth at a concentration of 156,25 μg/mL, with an inhibition percentage of 67.73% (R = 0.953, p = 0.000). IC of fractions 14 and 36K were found at 10.63 μg/mL and 135,91 μg/mL, respectively. The fractions caused morphological damage in almost all asexual stages of the parasite. Both fractions were not toxic against MCF-7, indicating that the fractions have a safe active metabolite.

CONCLUSION

Fractions 14 and 36K of metabolite extract subsp. Hygroscopicus contains non-toxic compounds that could damage the morphology and inhibit the growth of in vitro.

摘要

目的

本研究旨在调查吸水链霉菌亚种代谢物提取物的14号和36K组分作为抗疟化合物在体外的有效性和细胞毒性。

方法

利用快速柱色谱法(FCC)BUCHI Reveleris PREP对吸水链霉菌亚种代谢物提取物进行分馏,得到14号和36K组分。使用疟原虫培养物评估14号和36K组分的抗疟活性。在显微镜下测定寄生虫密度和寄生虫生长能力。使用MTT法在MCF-7细胞系上评估这些组分的细胞毒性。

结果

吸水链霉菌亚种的14号和36K组分对疟原虫具有抗疟活性,其中14号组分活性更强。随着组分浓度的增加,感染疟原虫的红细胞百分比降低。14号组分在浓度为156.25μg/mL时对寄生虫生长的抑制作用最强,抑制率为67.73%(R = 0.953,p = 0.000)。14号和36K组分的半数抑制浓度(IC)分别为10.63μg/mL和135.91μg/mL。这些组分在疟原虫几乎所有无性阶段都造成了形态损伤。两种组分对MCF-7均无毒性,表明这些组分具有安全的活性代谢物。

结论

吸水链霉菌亚种代谢物提取物的14号和36K组分含有无毒化合物,可在体外破坏疟原虫形态并抑制其生长。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/34f1/10187656/d1a378ddec8d/IDR-16-2973-g0001.jpg

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