New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect

A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreve...
Ausführliche Beschreibung

Gespeichert in:

Autor*in:	Gustavo Moreno-Quintero [verfasserIn] Emmanuel Betancur-Zapata [verfasserIn] Angie Herrera-Ramírez [verfasserIn] Wilson Cardona-Galeano [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2023

Schlagwörter:	5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer

Übergeordnetes Werk:	In: Pharmaceutics - MDPI AG, 2010, 15(2023), 4, p 1221
Übergeordnetes Werk:	volume:15 ; year:2023 ; number:4, p 1221

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/pharmaceutics15041221

Katalog-ID:	DOAJ089791223

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allfields	10.3390/pharmaceutics15041221 doi (DE-627)DOAJ089791223 (DE-599)DOAJ2ee688f88b394c439bca57a00e1dad9f DE-627 ger DE-627 rakwb eng RS1-441 Gustavo Moreno-Quintero verfasserin aut New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research. 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer Pharmacy and materia medica Emmanuel Betancur-Zapata verfasserin aut Angie Herrera-Ramírez verfasserin aut Wilson Cardona-Galeano verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 4, p 1221 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:4, p 1221 https://doi.org/10.3390/pharmaceutics15041221 kostenfrei https://doaj.org/article/2ee688f88b394c439bca57a00e1dad9f kostenfrei https://www.mdpi.com/1999-4923/15/4/1221 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 15 2023 4, p 1221
spelling	10.3390/pharmaceutics15041221 doi (DE-627)DOAJ089791223 (DE-599)DOAJ2ee688f88b394c439bca57a00e1dad9f DE-627 ger DE-627 rakwb eng RS1-441 Gustavo Moreno-Quintero verfasserin aut New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research. 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer Pharmacy and materia medica Emmanuel Betancur-Zapata verfasserin aut Angie Herrera-Ramírez verfasserin aut Wilson Cardona-Galeano verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 4, p 1221 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:4, p 1221 https://doi.org/10.3390/pharmaceutics15041221 kostenfrei https://doaj.org/article/2ee688f88b394c439bca57a00e1dad9f kostenfrei https://www.mdpi.com/1999-4923/15/4/1221 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 15 2023 4, p 1221
allfields_unstemmed	10.3390/pharmaceutics15041221 doi (DE-627)DOAJ089791223 (DE-599)DOAJ2ee688f88b394c439bca57a00e1dad9f DE-627 ger DE-627 rakwb eng RS1-441 Gustavo Moreno-Quintero verfasserin aut New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research. 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer Pharmacy and materia medica Emmanuel Betancur-Zapata verfasserin aut Angie Herrera-Ramírez verfasserin aut Wilson Cardona-Galeano verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 4, p 1221 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:4, p 1221 https://doi.org/10.3390/pharmaceutics15041221 kostenfrei https://doaj.org/article/2ee688f88b394c439bca57a00e1dad9f kostenfrei https://www.mdpi.com/1999-4923/15/4/1221 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 15 2023 4, p 1221
allfieldsGer	10.3390/pharmaceutics15041221 doi (DE-627)DOAJ089791223 (DE-599)DOAJ2ee688f88b394c439bca57a00e1dad9f DE-627 ger DE-627 rakwb eng RS1-441 Gustavo Moreno-Quintero verfasserin aut New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research. 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer Pharmacy and materia medica Emmanuel Betancur-Zapata verfasserin aut Angie Herrera-Ramírez verfasserin aut Wilson Cardona-Galeano verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 4, p 1221 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:4, p 1221 https://doi.org/10.3390/pharmaceutics15041221 kostenfrei https://doaj.org/article/2ee688f88b394c439bca57a00e1dad9f kostenfrei https://www.mdpi.com/1999-4923/15/4/1221 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 15 2023 4, p 1221
allfieldsSound	10.3390/pharmaceutics15041221 doi (DE-627)DOAJ089791223 (DE-599)DOAJ2ee688f88b394c439bca57a00e1dad9f DE-627 ger DE-627 rakwb eng RS1-441 Gustavo Moreno-Quintero verfasserin aut New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research. 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer Pharmacy and materia medica Emmanuel Betancur-Zapata verfasserin aut Angie Herrera-Ramírez verfasserin aut Wilson Cardona-Galeano verfasserin aut In Pharmaceutics MDPI AG, 2010 15(2023), 4, p 1221 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:15 year:2023 number:4, p 1221 https://doi.org/10.3390/pharmaceutics15041221 kostenfrei https://doaj.org/article/2ee688f88b394c439bca57a00e1dad9f kostenfrei https://www.mdpi.com/1999-4923/15/4/1221 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 15 2023 4, p 1221
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callnumber-first	R - Medicine
author	Gustavo Moreno-Quintero
spellingShingle	Gustavo Moreno-Quintero misc RS1-441 misc 5-FU misc curcumin misc hybrid misc cytotoxicity misc antiproliferative misc colorectal cancer misc Pharmacy and materia medica New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect
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topic_title	RS1-441 New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect 5-FU curcumin hybrid cytotoxicity antiproliferative colorectal cancer
topic	misc RS1-441 misc 5-FU misc curcumin misc hybrid misc cytotoxicity misc antiproliferative misc colorectal cancer misc Pharmacy and materia medica
topic_unstemmed	misc RS1-441 misc 5-FU misc curcumin misc hybrid misc cytotoxicity misc antiproliferative misc colorectal cancer misc Pharmacy and materia medica
topic_browse	misc RS1-441 misc 5-FU misc curcumin misc hybrid misc cytotoxicity misc antiproliferative misc colorectal cancer misc Pharmacy and materia medica
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title	New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect
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title_full	New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect
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title_sort	new hybrid scaffolds based on 5-fu/curcumin: synthesis, cytotoxic, antiproliferative and pro-apoptotic effect
callnumber	RS1-441
title_auth	New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect
abstract	A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research.
abstractGer	A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research.
abstract_unstemmed	A series of 5-FU-Curcumin hybrids were synthesized, and their structures were elucidated by spectroscopic analysis. The synthesized hybrid compounds were evaluated in different colorectal cancer cell lines (SW480 and SW620) and in non-malignant cells (HaCaT and CHO-K1), to determine their chemopreventive potential. Hybrids <b<6a</b< and <b<6d</b< presented the best IC<sub<50</sub< value against the SW480 cell line with results of 17.37 ± 1.16 µM and 2.43 ± 0.33 µM, respectively. Similarly, compounds <b<6d</b< and <b<6e</b< presented IC<sub<50</sub< results of 7.51 ± 1.47 µM and 14.52 ± 1.31 µM, respectively, against the SW620 cell line. These compounds were more cytotoxic and selective than curcumin alone, the reference drug 5-fluorouracil (5-FU), and the equimolar mixture of curcumin and 5-FU. In addition, hybrids <b<6a</b< and <b<6d</b< (in SW480) and compounds <b<6d</b< and <b<6e</b< (in SW620) induced cell cycle arrest in S-phase, and, compounds <b<6d</b< and <b<6e</b< caused a significant increase in the sub-G0/G1 phase population in both cell lines. Hybrid <b<6e</b< was also observed to induce apoptosis of SW620 cells with a respective increase in executioner caspases 3 and 7. Taken together, these results suggest that the hybrids could actively act on a colorectal cancer model, making them a privileged scaffold that could be used in future research.
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title_short	New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect
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up_date	2024-07-04T00:40:00.810Z
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New Hybrid Scaffolds Based on 5-FU/Curcumin: Synthesis, Cytotoxic, Antiproliferative and Pro-Apoptotic Effect

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