Design and synthesis of novel quinic acid derivatives : in vitro cytotoxicity and anticancer effect on glioblastoma
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Future medicinal chemistry - 12(2020), 21 vom: 30. Nov., Seite 1891-1910 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Murugesan, Akshaya [VerfasserIn] |
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| Links: |
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| Themen: |
058C04BGYI |
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| Anmerkungen: |
Date Completed 02.08.2021 Date Revised 02.08.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2020-0194 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM316929905 |
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| 100 | 1 | |a Murugesan, Akshaya |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Design and synthesis of novel quinic acid derivatives |b in vitro cytotoxicity and anticancer effect on glioblastoma |
| 264 | 1 | |c 2020 | |
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| 500 | |a Date Completed 02.08.2021 | ||
| 500 | |a Date Revised 02.08.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
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| 650 | 4 | |a chemotherapeutic drugs | |
| 650 | 4 | |a cytotoxicity | |
| 650 | 4 | |a glioblastoma | |
| 650 | 4 | |a nanoparticle | |
| 650 | 4 | |a quinic acid | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
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| 700 | 1 | |a Holmstedt, Suvi |e verfasserin |4 aut | |
| 700 | 1 | |a Brown, Kenna C |e verfasserin |4 aut | |
| 700 | 1 | |a Koivuporras, Alisa |e verfasserin |4 aut | |
| 700 | 1 | |a Macedo, Ana S |e verfasserin |4 aut | |
| 700 | 1 | |a Nguyen, Nga |e verfasserin |4 aut | |
| 700 | 1 | |a Fonte, Pedro |e verfasserin |4 aut | |
| 700 | 1 | |a Rijo, Patrícia |e verfasserin |4 aut | |
| 700 | 1 | |a Yli-Harja, Olli |e verfasserin |4 aut | |
| 700 | 1 | |a Candeias, Nuno R |e verfasserin |4 aut | |
| 700 | 1 | |a Kandhavelu, Meenakshisundaram |e verfasserin |4 aut | |
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