Molecular Signaling Lab, Faculty of Medicine & Health Technology, Tampere University, Finland.
BioMeditech & Tays Cancer Center, Tampere University Hospital, P.O. Box 553, 33101, Tampere, Finland.
Future Med Chem. 2020 Nov;12(21):1891-1910. doi: 10.4155/fmc-2020-0194. Epub 2020 Oct 30.
Quinic acid (QA) is a cyclic polyol exhibiting anticancer properties on several cancers. However, potential role of QA derivatives against glioblastoma is not well established. Sixteen novel QA derivatives and QA- encapsulated poly (lactic-co-glycolic acid) nanoparticles (QA--NPs) were screened for their anti-glioblastoma effect using standard cell and molecular biology methods. Presence of a tertiary hydroxy and silylether groups in the lead compound were identified for the antitumor activity. QA- have 90% inhibition with the IC of 10.66 μM and 28.22 μM for LN229 and SNB19, respectively. The induction of apoptosis is faster with the increased fold change of caspase 3/7 and reactive oxygen species. QA- and QA--NPs shows similar cytotoxicity effect, providing the opportunity to use QA- as a potential chemotherapeutic agent.
奎尼酸（QA）是一种环状多元醇，对多种癌症具有抗癌特性。然而，QA 衍生物在神经胶质瘤中的潜在作用尚未得到充分证实。本研究使用标准的细胞和分子生物学方法，筛选了 16 种新型 QA 衍生物和 QA 包裹的聚（乳酸-共-羟基乙酸）纳米颗粒（QA-NPs），以评估它们对神经胶质瘤的抑制作用。研究发现，先导化合物中存在叔羟基和硅醚基团，具有抗肿瘤活性。QA 的 IC 分别为 10.66μM 和 28.22μM，对 LN229 和 SNB19 的抑制率达到 90%。半胱天冬酶 3/7 和活性氧的倍数变化更快诱导了细胞凋亡。QA-和 QA-NPs 表现出相似的细胞毒性作用，为将 QA-作为一种潜在的化疗药物提供了机会。
