Design and Synthesis of Novel Quinic Acid Derivatives: <i>In Vitro</i> Cytotoxicity and Anticancer Effect on Glioblastoma
Akshaya Murugesan, Suvi Holmstedt, Kenna C Brown, Alisa Koivuporras, Ana S. Macedo, Nga T. T. Nguyen, Pedro Fonte, Patrícia Rijo, Olli Yli‐Harja, Nuno R. Candeias, Meenakshisundaram Kandhavelu
Abstract
Aim: 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. Methodology & results: Sixteen novel QA derivatives and QA-16 encapsulated poly (lactic-co-glycolic acid) nanoparticles (QA-16-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-16 have 90% inhibition with the IC50 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. Conclusion: QA-16 and QA-16-NPs shows similar cytotoxicity effect, providing the opportunity to use QA-16 as a potential chemotherapeutic agent.