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2',4'-二羟基-6'-甲氧基-3',5'-二甲氧基查耳酮对人宫颈癌细胞系的增殖抑制、DNA 损伤、细胞周期阻滞和凋亡的影响。

Effects of 2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone from Seeds on Antiproliferative, DNA Damage, Cell Cycle Arrest, and Apoptosis in Human Cervical Cancer Cell Lines.

机构信息

Interdisciplinary Program in Biotechnology, Graduate School, Chiang Mai University, Chiang Mai 50200, Thailand.

Department of Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200, Thailand.

出版信息

Molecules. 2022 Feb 9;27(4):1154. doi: 10.3390/molecules27041154.

Abstract

2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), a natural product derived from A. Cunn. ex DC., was investigated for its inhibitory activities against various cancer cell lines. In this work, we investigated the effects of DMC and available anticervical cancer drugs (5-fluorouracil, cisplatin, and doxorubicin) on three human cervical cancer cell lines (C-33A, HeLa, and SiHa). DMC displayed antiproliferative cervical cancer activity in C-33A, HeLa, and SiHa cells, with IC values of 15.76 ± 1.49, 10.05 ± 0.22, and 18.31 ± 3.10 µM, respectively. DMC presented higher antiproliferative cancer activity in HeLa cells; therefore, we further investigated DMC-induced apoptosis in this cell line, including DNA damage, cell cycle arrest, and apoptosis assays. As a potential anticancer agent, DMC treatment increased DNA damage in cancer cells, observed through fluorescence inverted microscopy and a comet assay. The cell cycle assay showed an increased number of cells in the G/G phase following DMC treatment. Furthermore, DMC treatment-induced apoptosis cell death was approximately three- to four-fold higher compared to the untreated group. Here, DMC represented a compound-induced apoptosis for cell death in the HeLa cervical cancer cell line. Our findings suggest that DMC, a phytochemical agent, is a potential candidate for antiproliferative cervical cancer drug development.

摘要

2',4'-二羟基-6'-甲氧基-3',5'-二甲基查尔酮(DMC)是一种从 A. Cunn. ex DC. 中提取的天然产物,研究了其对各种癌细胞系的抑制活性。在这项工作中,我们研究了 DMC 和现有抗宫颈癌药物(5-氟尿嘧啶、顺铂和阿霉素)对三种人宫颈癌细胞系(C-33A、HeLa 和 SiHa)的影响。DMC 在 C-33A、HeLa 和 SiHa 细胞中显示出抗增殖宫颈癌活性,IC 值分别为 15.76±1.49、10.05±0.22 和 18.31±3.10µM。DMC 在 HeLa 细胞中表现出更高的抗增殖癌症活性;因此,我们进一步研究了 DMC 在该细胞系中诱导的细胞凋亡,包括 DNA 损伤、细胞周期阻滞和凋亡测定。作为一种潜在的抗癌剂,DMC 处理增加了癌细胞中的 DNA 损伤,通过荧光倒置显微镜和彗星试验观察到。细胞周期测定显示 DMC 处理后 G/G 期的细胞数量增加。此外,与未处理组相比,DMC 处理诱导的凋亡细胞死亡增加了约三到四倍。在这里,DMC 代表了化合物诱导的 HeLa 宫颈癌细胞系中细胞死亡的凋亡。我们的研究结果表明,DMC 作为一种植物化学物质,是一种有潜力的抗增殖宫颈癌药物开发候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7eef/8879438/ac3465d21327/molecules-27-01154-g001.jpg

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