Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells
Abstract Curcumin has demonstrated potential cytotoxicity across various cell lines despite its poor bioavailability and rapid metabolism. Therefore, our group have synthesized curcuminoid analogues with piperidone derivatives, FLDP-5 and FLDP-8 to overcome these limitations. In this study, the anal...
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2022-07-01
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| Series: | Scientific Reports |
| Online Access: | https://doi.org/10.1038/s41598-022-16274-4 |
| _version_ | 1818015118869397504 |
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| author | Nur Syahirah Che Razali Kok Wai Lam Nor Fadilah Rajab A. Rahman A. Jamal Nurul Farahana Kamaluddin Kok Meng Chan |
| author_facet | Nur Syahirah Che Razali Kok Wai Lam Nor Fadilah Rajab A. Rahman A. Jamal Nurul Farahana Kamaluddin Kok Meng Chan |
| author_sort | Nur Syahirah Che Razali |
| collection | DOAJ |
| description | Abstract Curcumin has demonstrated potential cytotoxicity across various cell lines despite its poor bioavailability and rapid metabolism. Therefore, our group have synthesized curcuminoid analogues with piperidone derivatives, FLDP-5 and FLDP-8 to overcome these limitations. In this study, the analogues were assessed on LN-18 human glioblastoma cells in comparison to curcumin. Results from cytotoxicity assessment showed that FLDP-5 and FLDP-8 curcuminoid analogues caused death in LN-18 cells in a concentration-dependent manner after 24-h treatment with much lower IC50 values of 2.5 µM and 4 µM respectively, which were more potent compared to curcumin with IC50 of 31 µM. Moreover, a significant increase (p < 0.05) in the level of superoxide anion and hydrogen peroxide upon 2-h and 6-h treatment confirmed the oxidative stress involvement in the cell death process induced by these analogues. These analogues also showed potent anti-migratory effects through inhibition of LN-18 cells’ migration and invasion. In addition, cell cycle analysis showed that these analogues are capable of inducing significant (p < 0.05) S-phase cell cycle arrest during the 24-h treatment as compared to untreated, which explained the reduced proliferation indicated by MTT assay. In conclusion, these curcuminoid analogues exhibit potent anti-cancer effects with anti-proliferative and anti-migratory properties towards LN-18 cells as compared to curcumin. |
| first_indexed | 2024-04-14T06:52:48Z |
| format | Article |
| id | doaj.art-e4e3cc0d2d5e48809206806d4b379242 |
| institution | Directory Open Access Journal |
| issn | 2045-2322 |
| language | English |
| last_indexed | 2024-04-14T06:52:48Z |
| publishDate | 2022-07-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Scientific Reports |
| spelling | doaj.art-e4e3cc0d2d5e48809206806d4b3792422022-12-22T02:06:58ZengNature PortfolioScientific Reports2045-23222022-07-0112111710.1038/s41598-022-16274-4Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cellsNur Syahirah Che Razali0Kok Wai Lam1Nor Fadilah Rajab2A. Rahman A. Jamal3Nurul Farahana Kamaluddin4Kok Meng Chan5Center for Toxicology and Health Risk Studies, Faculty of Health Sciences, Universiti Kebangsaan MalaysiaCenter for Drug and Herbal Development, Faculty of Pharmacy, Universiti Kebangsaan MalaysiaCenter for Healthy Ageing and Wellness, Faculty of Health Sciences, Universiti Kebangsaan MalaysiaUKM Medical Molecular Biology Institute, UKM Medical CentreCenter for Toxicology and Health Risk Studies, Faculty of Health Sciences, Universiti Kebangsaan MalaysiaCenter for Toxicology and Health Risk Studies, Faculty of Health Sciences, Universiti Kebangsaan MalaysiaAbstract Curcumin has demonstrated potential cytotoxicity across various cell lines despite its poor bioavailability and rapid metabolism. Therefore, our group have synthesized curcuminoid analogues with piperidone derivatives, FLDP-5 and FLDP-8 to overcome these limitations. In this study, the analogues were assessed on LN-18 human glioblastoma cells in comparison to curcumin. Results from cytotoxicity assessment showed that FLDP-5 and FLDP-8 curcuminoid analogues caused death in LN-18 cells in a concentration-dependent manner after 24-h treatment with much lower IC50 values of 2.5 µM and 4 µM respectively, which were more potent compared to curcumin with IC50 of 31 µM. Moreover, a significant increase (p < 0.05) in the level of superoxide anion and hydrogen peroxide upon 2-h and 6-h treatment confirmed the oxidative stress involvement in the cell death process induced by these analogues. These analogues also showed potent anti-migratory effects through inhibition of LN-18 cells’ migration and invasion. In addition, cell cycle analysis showed that these analogues are capable of inducing significant (p < 0.05) S-phase cell cycle arrest during the 24-h treatment as compared to untreated, which explained the reduced proliferation indicated by MTT assay. In conclusion, these curcuminoid analogues exhibit potent anti-cancer effects with anti-proliferative and anti-migratory properties towards LN-18 cells as compared to curcumin.https://doi.org/10.1038/s41598-022-16274-4 |
| spellingShingle | Nur Syahirah Che Razali Kok Wai Lam Nor Fadilah Rajab A. Rahman A. Jamal Nurul Farahana Kamaluddin Kok Meng Chan Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells Scientific Reports |
| title | Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells |
| title_full | Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells |
| title_fullStr | Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells |
| title_full_unstemmed | Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells |
| title_short | Curcumin piperidone derivatives induce anti-proliferative and anti-migratory effects in LN-18 human glioblastoma cells |
| title_sort | curcumin piperidone derivatives induce anti proliferative and anti migratory effects in ln 18 human glioblastoma cells |
| url | https://doi.org/10.1038/s41598-022-16274-4 |
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