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乙酸卡可洛尔作为抗癌剂:抗增殖、促凋亡、细胞生长抑制及抗迁移作用

Cacalol Acetate as Anticancer Agent: Antiproliferative, Pro-Apoptotic, Cytostatic, and Anti-Migratory Effects.

作者信息

Rostro-Alonso Gareth Omar, Castillo-Montoya Alejandro Israel, García-Acosta Juan Carlos, Aguilar-Llanos Erick Fernando, Quintas-Granados Laura Itzel, Villegas-Vazquez Edgar Yebrán, García-Aguilar Rosario, Porras-Vázquez Samantha Andrea, Bustamante-Montes Lilia Patricia, Alvarado-Sansininea Jesús J, Jiménez-Estrada Manuel, Cariño-Calvo Lizbeth, Carmen Manuel González-Del, Cortés Hernán, Leyva-Gómez Gerardo, Figueroa-González Gabriela, Reyes-Hernández Octavio Daniel

机构信息

Laboratorio de Farmacogenética, Unidad Multidisciplinaria de Investigación Experimental Zaragoza, Facultad de Estudios Superiores Zaragoza, Universidad Nacional Autónoma de México, Batalla 5 de Mayo s/n Esquina Fuerte de Loreto, Iztapalapa, Mexico City 09230, Mexico.

Laboratorio de Biología Molecular del Cáncer, Unidad Multidisciplinaria de Investigación Experimental Zaragoza, Facultad de Estudios Superiores-Zaragoza, Universidad Nacional Autónoma de México, Iztapalapa, Mexico City 09230, Mexico.

出版信息

Curr Issues Mol Biol. 2024 Aug 23;46(9):9298-9311. doi: 10.3390/cimb46090550.

Abstract

Cacalol (C), a sesquiterpene isolated from , has demonstrated anti-inflammatory and antioxidant activities. Its cytotoxic, antiproliferative, and pro-apoptotic effects have been previously shown in an in vitro breast cancer model. A derivative, cacalol acetate (CA), shows potential in regulating these processes, which has not been previously reported. This study focused on an in vitro cervical cancer model, assessing CA's antiproliferative, pro-apoptotic, cytostatic, and anti-migratory activities using the HeLa cell line. The natural anticancer agent indole-3-carbinol (I3C) was used as a control for comparison. CA demonstrated significant antitumor activities, including inhibiting cell growth, inducing apoptosis, arresting cells in the G2 phase of the cell cycle, and inhibiting cell migration. These effects were notably greater compared to I3C. I3C, while following a similar trend, did not induce Cas-3 expression, suggesting a different apoptotic pathway. Neither CA nor I3C increased p62 and LC3B levels, indicating they do not stimulate autophagy marker expression. Both compounds inhibited HeLa cell migration and induced cell cycle arrest. Despite both holding promise as anticancer agents for cervical cancer, CA's lower cytotoxicity and stronger regulation of tumor phenotypes make it a more promising agent compared to I3C.

摘要

刺蒴麻醇(C)是一种从[植物名称未给出]中分离出的倍半萜,已证明具有抗炎和抗氧化活性。其细胞毒性、抗增殖和促凋亡作用此前已在体外乳腺癌模型中得到证实。一种衍生物,醋酸刺蒴麻醇(CA),在调节这些过程方面显示出潜力,此前尚未见报道。本研究聚焦于体外宫颈癌模型,使用HeLa细胞系评估CA的抗增殖、促凋亡、细胞生长抑制和抗迁移活性。天然抗癌剂吲哚 - 3 - 甲醇(I3C)用作对照进行比较。CA表现出显著的抗肿瘤活性,包括抑制细胞生长、诱导凋亡、使细胞停滞在细胞周期的G2期以及抑制细胞迁移。与I3C相比,这些作用明显更强。I3C虽然呈现类似趋势,但未诱导Caspase - 3表达,表明凋亡途径不同。CA和I3C均未增加p62和LC3B水平,表明它们不会刺激自噬标志物表达。两种化合物均抑制HeLa细胞迁移并诱导细胞周期停滞。尽管两者都有望成为宫颈癌的抗癌药物,但与I3C相比,CA较低的细胞毒性和对肿瘤表型更强的调节作用使其成为更有前景的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b648/11430360/3acd0011c99d/cimb-46-00550-sch001.jpg

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