评估香豆素肼-腙衍生物在人肝细胞癌细胞系中诱导的细胞毒性和细胞凋亡

Trends in Sciences Pub Date : 2024-05-01 DOI:10.48048/tis.2024.7628

Saisuree Prateeptongkum, N. Duangdee, Wiratchanee Mahavorasirikul

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引用次数: 0

摘要

香豆素和芳基肼基腙因其广泛的生物特性而备受关注。以前的研究表明，香豆素系芳基酰肼-腙对 HepG2 具有很强的活性。在本研究中，我们研究了香豆素衍生物 1 - 3 与香豆素肼-腙混合物 4 和 5 对肝癌 HepG2 和 LH86 细胞系的细胞毒性作用。在测试的香豆素类化合物中，杂交化合物 4 和 5 对 HepG2 表现出极强的活性，IC50 值分别为 17.82 ± 2.79 和 7.87 ± 0.88 𝜇g/mL。杂交 4 对 LH86 细胞株的活性也最强，IC50 值为 48.32 ± 2.64 𝜇g/mL。此外，我们还通过流式细胞仪分析以及 caspase-3 和 caspase-7 的活化，研究了杂交化合物 4 和 5 在 HepG2 细胞中的作用机制。结果表明，杂交化合物 4 和 5 通过诱导细胞凋亡明显抑制了 HepG2 细胞株的增殖。我们报道了香豆素酰肼-腙杂交化合物的制备方法，并评估了它们对肝癌细胞系 HepG2 和 LH86 的作用。这些杂化物对 HepG2 和 LH86 具有很高的药效。流式细胞术和 Caspase-3/7 表达分析表明，混合化合物能诱导 HepG2 细胞凋亡。

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Evaluation of Cytotoxicity and Apoptosis Induced by Coumarin Hydrazide-Hydrazone Derivatives in Human Hepatocellular Carcinoma Cell Line

Coumarin and aryl hydrazide-hydrazone have attracted our attention due to their vast biological properties. Previous studies suggested that coumarin-tethered aryl hydrazide-hydrazone showed potent activities against HepG2. In the present study, we investigated the cytotoxic potency of the coumarin derivatives 1 - 3 to compare with coumarin hydrazine-hydrazone hybrids 4 and 5 against hepatocellular carcinoma HepG2 and LH86 cell lines. Among the tested coumarins, hybrids 4 and 5 showed highly potent activity against HepG2 with IC50 values of 17.82 ± 2.79 and 7.87 ± 0.88 𝜇g/mL, respectively. The hybrid 4 also showed the strongest activity against LH86 cell line with IC50 values of 48.32 ± 2.64 𝜇g/mL. Further, we have studied the mechanism of action of the hybrid compounds 4 and 5 in HepG2 cells via the flow-cytometry analysis and the activation of the caspase-3 and caspase-7. The results showed that hybrids 4 and 5 obviously inhibited the proliferation of HepG2 cell line through inducing apoptosis. HIGHLIGHTS Focusing on coumarin and aryl hydrazide-hydrazone possess significant biological properties. We reported the preparation of coumarin hydrazine-hydrazone hybrids and evaluated their effects against hepatocellular carcinoma cell lines HepG2 and LH86. The hybrid compounds exhibited high potency against HepG2 and LH86. Flow-cytometry and caspase-3/7 expression analysis revealed that the hybrid compounds induced apoptosis in HepG2 cells. GRAPHICAL ABSTRACT

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来源期刊

Trends in Sciences

CiteScore

1.20

自引率

0.00%

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