Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies
Biocompatible tryptophan-derived copper (1) and zinc (2) complexes with norharmane (beta-carboline) were designed, synthesized, characterized, and evaluated for the potential anticancer activity in vitro and in vivo. The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cance...
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| Veröffentlicht in: | Molecules (Basel, Switzerland) Switzerland), 2021-03, Vol.26 (6), p.1606, Article 1606 |
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| creator | Alharbi, Walaa Hassan, Iftekhar Khan, Rais Ahmad Parveen, Shazia Alharbi, Khadijah H. Bin Sharfan, Ibtisam I. Alhazza, Ibrahim M. Ebaid, Hossam Alsalme, Ali |
| description | Biocompatible tryptophan-derived copper (1) and zinc (2) complexes with norharmane (beta-carboline) were designed, synthesized, characterized, and evaluated for the potential anticancer activity in vitro and in vivo. The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of 1 against MCF7 cells with an IC50 value of 7.8 +/- 0.4 mu M compared to 2 (less active, IC50 similar to 20 mu M). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of 1. |
| doi_str_mv | 10.3390/molecules26061606 |
| format | Article |
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The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of 1 against MCF7 cells with an IC50 value of 7.8 +/- 0.4 mu M compared to 2 (less active, IC50 similar to 20 mu M). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of 1.</description><identifier>ISSN: 1420-3049</identifier><identifier>EISSN: 1420-3049</identifier><identifier>DOI: 10.3390/molecules26061606</identifier><identifier>PMID: 33799355</identifier><language>eng</language><publisher>BASEL: Mdpi</publisher><subject>Animals ; Antineoplastic Agents - pharmacology ; Antitumor activity ; Biochemistry & Molecular Biology ; Biocompatibility ; Breast cancer ; Breast Neoplasms - drug therapy ; Breast Neoplasms - metabolism ; Cancer therapies ; Carbolines - pharmacology ; Cell Line ; Cell Line, Tumor ; Chemistry ; Chemistry, Multidisciplinary ; Comet assay ; Comet Assay - methods ; Copper ; Copper - pharmacology ; copper complex ; Copper compounds ; Cyclin-dependent kinases ; Cytotoxicity ; Damage detection ; Deoxyribonucleic acid ; DNA ; DNA damage ; DNA Damage - drug effects ; Drugs ; FDA approval ; Female ; Free radicals ; Geometry ; Glutathione - metabolism ; HEK293 Cells ; Hep G2 Cells ; Hepatocytes ; Histopathology ; Humans ; In vivo methods and tests ; in vivo toxicity ; Kinases ; Life Sciences & Biomedicine ; Ligands ; Lipid peroxidation ; Lipid Peroxidation - drug effects ; Lipids ; Liver ; Liver cancer ; MCF-7 Cells ; MCF7 cells ; MTT assay ; Oxidative stress ; Oxidative Stress - drug effects ; Peroxidation ; Physical Sciences ; Rats ; Reactive Oxygen Species - metabolism ; ROS ; Science & Technology ; Selectivity ; Tryptophan ; Tryptophan - pharmacology ; Tumors ; Zinc - pharmacology</subject><ispartof>Molecules (Basel, Switzerland), 2021-03, Vol.26 (6), p.1606, Article 1606</ispartof><rights>2021. This work is licensed under http://creativecommons.org/licenses/by/3.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2021 by the authors. 2021</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>8</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000645392100001</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c493t-b7a4da600ec1ec1e2cda55c20fd6273f859761d80b6993546e1ef9884b6566e93</citedby><cites>FETCH-LOGICAL-c493t-b7a4da600ec1ec1e2cda55c20fd6273f859761d80b6993546e1ef9884b6566e93</cites><orcidid>0000-0001-6993-9954 ; 0000-0003-3301-6562 ; 0000-0002-4106-3011 ; 0000-0002-2213-2958 ; 0000-0002-7599-8464 ; 0000-0003-0897-2296</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001361/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001361/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,315,729,782,786,866,887,2106,2118,27933,27934,39267,53800,53802</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33799355$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Alharbi, Walaa</creatorcontrib><creatorcontrib>Hassan, Iftekhar</creatorcontrib><creatorcontrib>Khan, Rais Ahmad</creatorcontrib><creatorcontrib>Parveen, Shazia</creatorcontrib><creatorcontrib>Alharbi, Khadijah H.</creatorcontrib><creatorcontrib>Bin Sharfan, Ibtisam I.</creatorcontrib><creatorcontrib>Alhazza, Ibrahim M.</creatorcontrib><creatorcontrib>Ebaid, Hossam</creatorcontrib><creatorcontrib>Alsalme, Ali</creatorcontrib><title>Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies</title><title>Molecules (Basel, Switzerland)</title><addtitle>MOLECULES</addtitle><addtitle>Molecules</addtitle><description>Biocompatible tryptophan-derived copper (1) and zinc (2) complexes with norharmane (beta-carboline) were designed, synthesized, characterized, and evaluated for the potential anticancer activity in vitro and in vivo. The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of 1 against MCF7 cells with an IC50 value of 7.8 +/- 0.4 mu M compared to 2 (less active, IC50 similar to 20 mu M). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of 1.</description><subject>Animals</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antitumor activity</subject><subject>Biochemistry & Molecular Biology</subject><subject>Biocompatibility</subject><subject>Breast cancer</subject><subject>Breast Neoplasms - drug therapy</subject><subject>Breast Neoplasms - metabolism</subject><subject>Cancer therapies</subject><subject>Carbolines - pharmacology</subject><subject>Cell Line</subject><subject>Cell Line, Tumor</subject><subject>Chemistry</subject><subject>Chemistry, Multidisciplinary</subject><subject>Comet assay</subject><subject>Comet Assay - methods</subject><subject>Copper</subject><subject>Copper - pharmacology</subject><subject>copper complex</subject><subject>Copper compounds</subject><subject>Cyclin-dependent kinases</subject><subject>Cytotoxicity</subject><subject>Damage detection</subject><subject>Deoxyribonucleic acid</subject><subject>DNA</subject><subject>DNA damage</subject><subject>DNA Damage - drug effects</subject><subject>Drugs</subject><subject>FDA approval</subject><subject>Female</subject><subject>Free radicals</subject><subject>Geometry</subject><subject>Glutathione - metabolism</subject><subject>HEK293 Cells</subject><subject>Hep G2 Cells</subject><subject>Hepatocytes</subject><subject>Histopathology</subject><subject>Humans</subject><subject>In vivo methods and tests</subject><subject>in vivo toxicity</subject><subject>Kinases</subject><subject>Life Sciences & Biomedicine</subject><subject>Ligands</subject><subject>Lipid peroxidation</subject><subject>Lipid Peroxidation - drug effects</subject><subject>Lipids</subject><subject>Liver</subject><subject>Liver cancer</subject><subject>MCF-7 Cells</subject><subject>MCF7 cells</subject><subject>MTT assay</subject><subject>Oxidative stress</subject><subject>Oxidative Stress - drug effects</subject><subject>Peroxidation</subject><subject>Physical Sciences</subject><subject>Rats</subject><subject>Reactive Oxygen Species - metabolism</subject><subject>ROS</subject><subject>Science & Technology</subject><subject>Selectivity</subject><subject>Tryptophan</subject><subject>Tryptophan - 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drug effects</topic><topic>Lipids</topic><topic>Liver</topic><topic>Liver cancer</topic><topic>MCF-7 Cells</topic><topic>MCF7 cells</topic><topic>MTT assay</topic><topic>Oxidative stress</topic><topic>Oxidative Stress - drug effects</topic><topic>Peroxidation</topic><topic>Physical Sciences</topic><topic>Rats</topic><topic>Reactive Oxygen Species - metabolism</topic><topic>ROS</topic><topic>Science & Technology</topic><topic>Selectivity</topic><topic>Tryptophan</topic><topic>Tryptophan - pharmacology</topic><topic>Tumors</topic><topic>Zinc - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Alharbi, Walaa</creatorcontrib><creatorcontrib>Hassan, Iftekhar</creatorcontrib><creatorcontrib>Khan, Rais Ahmad</creatorcontrib><creatorcontrib>Parveen, Shazia</creatorcontrib><creatorcontrib>Alharbi, Khadijah H.</creatorcontrib><creatorcontrib>Bin Sharfan, Ibtisam I.</creatorcontrib><creatorcontrib>Alhazza, Ibrahim M.</creatorcontrib><creatorcontrib>Ebaid, Hossam</creatorcontrib><creatorcontrib>Alsalme, Ali</creatorcontrib><collection>Web of Science Core Collection</collection><collection>Science Citation Index Expanded</collection><collection>Web of Science - 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The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of 1 against MCF7 cells with an IC50 value of 7.8 +/- 0.4 mu M compared to 2 (less active, IC50 similar to 20 mu M). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of 1.</abstract><cop>BASEL</cop><pub>Mdpi</pub><pmid>33799355</pmid><doi>10.3390/molecules26061606</doi><tpages>17</tpages><orcidid>https://orcid.org/0000-0001-6993-9954</orcidid><orcidid>https://orcid.org/0000-0003-3301-6562</orcidid><orcidid>https://orcid.org/0000-0002-4106-3011</orcidid><orcidid>https://orcid.org/0000-0002-2213-2958</orcidid><orcidid>https://orcid.org/0000-0002-7599-8464</orcidid><orcidid>https://orcid.org/0000-0003-0897-2296</orcidid><oa>free_for_read</oa></addata></record> |
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| source | MDPI - Multidisciplinary Digital Publishing Institute; MEDLINE; DOAJ Directory of Open Access Journals; Web of Science - Science Citation Index Expanded - 2021<img src="https://exlibris-pub.s3.amazonaws.com/fromwos-v2.jpg" />; EZB-FREE-00999 freely available EZB journals; PubMed Central; Free Full-Text Journals in Chemistry |
| subjects | Animals Antineoplastic Agents - pharmacology Antitumor activity Biochemistry & Molecular Biology Biocompatibility Breast cancer Breast Neoplasms - drug therapy Breast Neoplasms - metabolism Cancer therapies Carbolines - pharmacology Cell Line Cell Line, Tumor Chemistry Chemistry, Multidisciplinary Comet assay Comet Assay - methods Copper Copper - pharmacology copper complex Copper compounds Cyclin-dependent kinases Cytotoxicity Damage detection Deoxyribonucleic acid DNA DNA damage DNA Damage - drug effects Drugs FDA approval Female Free radicals Geometry Glutathione - metabolism HEK293 Cells Hep G2 Cells Hepatocytes Histopathology Humans In vivo methods and tests in vivo toxicity Kinases Life Sciences & Biomedicine Ligands Lipid peroxidation Lipid Peroxidation - drug effects Lipids Liver Liver cancer MCF-7 Cells MCF7 cells MTT assay Oxidative stress Oxidative Stress - drug effects Peroxidation Physical Sciences Rats Reactive Oxygen Species - metabolism ROS Science & Technology Selectivity Tryptophan Tryptophan - pharmacology Tumors Zinc - pharmacology |
| title | Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-11-29T23%3A42%3A18IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_webof&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Bioactive%20Tryptophan-Based%20Copper%20Complex%20with%20Auxiliary%20%CE%B2-Carboline%20Spectacle%20Potential%20on%20Human%20Breast%20Cancer%20Cells:%20In%20Vitro%20and%20In%20Vivo%20Studies&rft.jtitle=Molecules%20(Basel,%20Switzerland)&rft.au=Alharbi,%20Walaa&rft.date=2021-03-14&rft.volume=26&rft.issue=6&rft.spage=1606&rft.pages=1606-&rft.artnum=1606&rft.issn=1420-3049&rft.eissn=1420-3049&rft_id=info:doi/10.3390/molecules26061606&rft_dat=%3Cproquest_webof%3E2503039988%3C/proquest_webof%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2503039988&rft_id=info:pmid/33799355&rft_doaj_id=oai_doaj_org_article_861863b5479c4d3980e2e1b1125c1c40&rfr_iscdi=true |