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在口腔状细胞癌模型中的Piper cernuum物质的抗癌活性和分子标

Thaíssa Queiróz Machado¹, Maria Emanuelle Damazio Lima², Rafael Carriello da Silva³

¹Postgraduate Program in Applied Science for Health Products, Faculty of Pharmacy, Fluminense Federal University, Niteroi 24241-000, RJ, Brazil.

|July 29, 2023

概括

Piper cernuum (PCLd) 的二甲分离是一种无毒的,有前途的抗癌剂,用于口腔状细胞癌 (OSCC). 它通过通过新型化合物和阿波芬类化合物诱导亡来降低异常并增加生存率.

科学领域:

药理学药理学是指药理学的学科.
自然产品化学化学
在瘤学瘤学.

背景情况:

口腔状细胞癌 (OSCC) 是一个重大的全球健康挑战,死亡率高.
开发用于OSCC的新型治疗剂至关重要.
派珀植物属表现出多样化的生物活动,包括潜在的抗癌特性.

研究的目的:

评估Piper cernuum二甲分离 (PCLd) 作为化学诱导的小鼠口腔状细胞癌 (OSCC) 的潜在治疗方法的疗效和安全性.
识别和描述PCLd中负责抗癌作用的活性化合物.
为了研究所观察到的抗癌活性背后的分子机制.

主要方法:

在小鼠PCLd的慢性毒性评估.
在小鼠中化学诱导OSCC,然后进行PCLd治疗.
染色学净化PCLd以分离活性分数 (09.07和14.05).
亡试验 (胺暴露,DNA碎片化,卡斯巴-3/7激活) 和血液溶解试验.
用于化合物识别的LC-DAD-MS/MS分析.
在基分子对接研究中预测潜在的药物点.

主要成果:

在老鼠慢性治疗期间,PCLd没有显示出毒性.
在化学诱导的OSCC模型中,PCLd显著降低了口腔异型症和增加了生存率.
净化分数09.07和14.05通过诱导亡,表现出强烈和选择性的细胞毒性活性.
分数14.05含有阿波芬类化合物,新描述在P. cernuum中,与细胞毒性作用相关.
在分析中确定了潜在的分子标,包括受体 (AR),CHK1,CK2,DYRK1A,EHMT2,LXRβ和VEGFR2.

结论:

Piper cernuum 分数,特别是PCLd,显示出作为OSCC的抗癌剂的显著临床前潜力.
来自P. cernuum的新型化合物和阿波芬类化合物通过亡诱导癌细胞死亡.
这些发现需要进一步调查P. cernuum衍生物作为新型OSCC疗法的候选者.

关键词:

在GNPS的GNPS系统中.这是一种N-甲基可克劳林.这种植物是Piperaceae.这是一种抗瘤药物.灭症 (apoptosis) 是一种死亡的过程.亚西米洛宾 (Asimilobine) 是一种可怕的药物.大胆的 boldine 是一个字体.可克劳林 (Coclaurine) 是一种可克劳林 (Coclaurine) 的成分.这是一种异基氨酸 (isocorydine).口腔癌是指口腔癌的发生.

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