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阿洛酮糖还原酶抑制剂的研究进展：基于构树水提物对细胞毒性的对比研究及其与银纳米粒子（NPs）的分子对接评价。

Aldose reductase inhibitor form Cassia glauca: A comparative study of cytotoxic activity with Ag nanoparticles (NPs) and molecular docking evaluation.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, October 6 University, Giza, Egypt.

Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

出版信息

PLoS One. 2020 Oct 16;15(10):e0240856. doi: 10.1371/journal.pone.0240856. eCollection 2020.

DOI:10.1371/journal.pone.0240856
PMID:33064762
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7567391/
Abstract

UPLC-MS/MS profiling of Cassia glauca leaves extract revealed the identification of 10 flavonoids. Kaempferol 3-O-β-D-rutinoside was isolated and studied for its cytotoxic activity. It showed high cytotoxic effects against MCF-7 (IC50 of 4.6±0.038 μg/ml) and HepG-2 (IC50 of 8.2±0.024 μg/ml) cancer cell lines, compared to the leaves extracts, their Ag nanoparticles, and doxorubicin. Moreover, Kaempferol 3-O-β-D-rutinoside exerted a synergistic cytotoxic effect with doxorubicin on MCF-7 cell lines. It was discovered as kinases and aldose reductase inhibitor while rationalizing its cytotoxic activity through molecular docking study. Thus, it is expected that the cardiotoxic effects of doxorubicin can be also decreased by using Kaempferol 3-O-β-D-rutinoside due to its aldose reductase inhibitory effect. These findings suggested that Kaempferol 3-O-β-D-rutinoside could be used in combination with chemotherapeutic drugs to increase the sensitivity to their cytotoxic activity and protect against their side effects.

摘要

UPLC-MS/MS 分析显示，决明子叶提取物中含有 10 种类黄酮。分离并研究了山柰酚 3-O-β-D-芦丁糖苷的细胞毒性。与叶提取物、其银纳米粒子和阿霉素相比，它对 MCF-7（IC50 为 4.6±0.038 μg/ml）和 HepG-2（IC50 为 8.2±0.024 μg/ml）癌细胞系表现出高细胞毒性作用。此外，山柰酚 3-O-β-D-芦丁糖苷对 MCF-7 细胞系与阿霉素表现出协同细胞毒性作用。它被发现是一种激酶和醛糖还原酶抑制剂，通过分子对接研究来解释其细胞毒性作用。因此，由于其醛糖还原酶抑制作用，预计使用山柰酚 3-O-β-D-芦丁糖苷也可以降低阿霉素的心脏毒性作用。这些发现表明，山柰酚 3-O-β-D-芦丁糖苷可以与化疗药物联合使用，以提高其对细胞毒性作用的敏感性，并防止其副作用。

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