Design and synthesis of novel quinic acid derivatives: in vitro cytotoxicity and anticancer effect on glioblastoma

Akshaya Murugesan, Suvi Holmstedt, Kenna C. Brown, Alisa Koivuporras, Ana S. Macedo, Nga Nguyen, Pedro Fonte, Patricia Rijo, Olli Yli-Harja, Nuno R. Candeias, Meenakshisundaram Kandhavelu

Research output: Contribution to journalArticleScientificpeer-review

1 Citation (Scopus)

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 mu M and 28.22 mu M 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 opportunity to use QA-16 as a potential chemotherapeutic agent.

Original languageEnglish
Pages (from-to)1891-1910
Number of pages20
JournalFUTURE MEDICINAL CHEMISTRY
Volume12
Issue number21
DOIs
Publication statusPublished - 2020
Publication typeA1 Journal article-refereed

Keywords

  • chemotherapeutic drugs
  • cytotoxicity
  • glioblastoma
  • nanoparticle
  • PLGA
  • quinic acid
  • NANOPARTICLES
  • TEMOZOLOMIDE
  • DELIVERY
  • CHEMOTHERAPY
  • INHIBITORS
  • DEPENDS
  • KINASE
  • CELLS

Publication forum classification

  • Publication forum level 1

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