Design and synthesis of novel quinic acid derivatives: in vitro cytotoxicity and anticancer effect on glioblastoma-Reference-Cited by-同舟云学术

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

Published:2020-11 Issue:21 Volume:12 Page:1891-1910
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Murugesan Akshaya¹²³,Holmstedt Suvi⁴,Brown Kenna C¹,Koivuporras Alisa⁴,Macedo Ana S⁵,Nguyen Nga¹,Fonte Pedro⁶⁷⁸,Rijo Patrícia⁹¹⁰,Yli-Harja Olli¹¹¹²,Candeias Nuno R⁴⁵,Kandhavelu Meenakshisundaram¹²³^ORCID

Affiliation:

1. Molecular Signaling Lab, Faculty of Medicine & Health Technology, Tampere University, Finland

2. BioMeditech & Tays Cancer Center, Tampere University Hospital, P.O. Box 553, 33101, Tampere, Finland

3. Department of Biotechnology, Lady Doak College, Thallakulam, Madurai, 625002, India

4. Faculty of Engineering & Natural Sciences, Tampere University, 33101, Tampere, Finland

5. LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193, Aveiro, Portugal

6. Center for Marine Sciences (CCMAR), University of Algarve, Gambelas Campus, 8005-139, Faro, Portugal

7. Department of Chemistry & Pharmacy, Faculty of Sciences & Technology, University of Algarve, Gambelas Campus, 8005-139, Faro, Portugal

8. iBB – Institute for Bioengineering & Biosciences, Department of Bioengineering, Instituto Superior Técnico, Universidade de Lisboa, 1049-001, Lisboa, Portugal

9. Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024, Lisboa, Portugal

10. Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003, Lisboa, Portugal

11. Computational Systems Biology Group, Faculty of Medicine & Health Technology, Tampere University, P.O. Box 553, 33101, Tampere, Finland

12. Institute for Systems Biology, 1441N 34th Street, Seattle, WA 98103-8904, USA

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.

Funder

Suomen Kulttuurirahasto

Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa

Academy of Finland

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2020-0194

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