Novel bibenzyl compound Ae exhibits anti-agiogenic activity in HUVECs in vitro and zebrafish in vivo
[Display omitted] •Our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity in zebrafish in vivo.•Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro.•The anti-angiogenic activity of compound Ae is connecte...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2024-09, Vol.111, p.117866, Article 117866 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Guan, Li Zhang, Shengjie Song, Pengfei Xia, Yanxin Zheng, Xinle Li, Weize |
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•Our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity in zebrafish in vivo.•Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro.•The anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway.
The inhibition of angiogenesis has been considered as an attractive method for the discovery of potential anti-cancer drugs. Herein, we report our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity(the lowest effective concentration is to 0.62–1.25 μM) in zebrafish in vivo and showed a concentration-dependent inhibition of inter-segmental blood vessels (ISVs) compared to control. Further, Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro. Moreover, qRT-PCR analysis revealed that the anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway. Molecular docking studies revealed that compound Ae had an interaction with the angiopoietin-2 receptor(TEK) and VEGFR2. Additionally, analysis of the ADMET prediction data indicated that compound Ae possessed favorable physicochemical properties, drug-likeness, and synthetic accessibility. In conclusion, compound Ae had remarkable anti-angiogenic activity and could be served as an candidate for cancer therapy. |
| doi_str_mv | 10.1016/j.bmc.2024.117866 |
| format | Article |
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•Our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity in zebrafish in vivo.•Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro.•The anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway.
The inhibition of angiogenesis has been considered as an attractive method for the discovery of potential anti-cancer drugs. Herein, we report our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity(the lowest effective concentration is to 0.62–1.25 μM) in zebrafish in vivo and showed a concentration-dependent inhibition of inter-segmental blood vessels (ISVs) compared to control. Further, Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro. Moreover, qRT-PCR analysis revealed that the anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway. Molecular docking studies revealed that compound Ae had an interaction with the angiopoietin-2 receptor(TEK) and VEGFR2. Additionally, analysis of the ADMET prediction data indicated that compound Ae possessed favorable physicochemical properties, drug-likeness, and synthetic accessibility. In conclusion, compound Ae had remarkable anti-angiogenic activity and could be served as an candidate for cancer therapy.</description><identifier>ISSN: 0968-0896</identifier><identifier>ISSN: 1464-3391</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2024.117866</identifier><identifier>PMID: 39096785</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Angiogenesis Inhibitors - chemical synthesis ; Angiogenesis Inhibitors - chemistry ; Angiogenesis Inhibitors - pharmacology ; Animals ; Anti-angiogenesis ; Anticancer ; Bibenzyl ; Bibenzyls - chemical synthesis ; Bibenzyls - chemistry ; Bibenzyls - pharmacology ; Cell Movement - drug effects ; Cell Proliferation - drug effects ; Dose-Response Relationship, Drug ; Human Umbilical Vein Endothelial Cells - drug effects ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Receptor, TIE-2 - antagonists & inhibitors ; Receptor, TIE-2 - metabolism ; Structure-Activity Relationship ; Transgenic zebrafish model ; Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors ; Vascular Endothelial Growth Factor Receptor-2 - metabolism ; Zebrafish</subject><ispartof>Bioorganic & medicinal chemistry, 2024-09, Vol.111, p.117866, Article 117866</ispartof><rights>2024 Elsevier Ltd</rights><rights>Copyright © 2024 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c235t-e906a1e6a7df48f3eb71fa7356eed218f2082f78dce5fc0ac2af6c2c7a2ed03b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0968089624002803$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/39096785$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Guan, Li</creatorcontrib><creatorcontrib>Zhang, Shengjie</creatorcontrib><creatorcontrib>Song, Pengfei</creatorcontrib><creatorcontrib>Xia, Yanxin</creatorcontrib><creatorcontrib>Zheng, Xinle</creatorcontrib><creatorcontrib>Li, Weize</creatorcontrib><title>Novel bibenzyl compound Ae exhibits anti-agiogenic activity in HUVECs in vitro and zebrafish in vivo</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
•Our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity in zebrafish in vivo.•Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro.•The anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway.
The inhibition of angiogenesis has been considered as an attractive method for the discovery of potential anti-cancer drugs. Herein, we report our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity(the lowest effective concentration is to 0.62–1.25 μM) in zebrafish in vivo and showed a concentration-dependent inhibition of inter-segmental blood vessels (ISVs) compared to control. Further, Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro. Moreover, qRT-PCR analysis revealed that the anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway. Molecular docking studies revealed that compound Ae had an interaction with the angiopoietin-2 receptor(TEK) and VEGFR2. Additionally, analysis of the ADMET prediction data indicated that compound Ae possessed favorable physicochemical properties, drug-likeness, and synthetic accessibility. In conclusion, compound Ae had remarkable anti-angiogenic activity and could be served as an candidate for cancer therapy.</description><subject>Angiogenesis Inhibitors - chemical synthesis</subject><subject>Angiogenesis Inhibitors - chemistry</subject><subject>Angiogenesis Inhibitors - pharmacology</subject><subject>Animals</subject><subject>Anti-angiogenesis</subject><subject>Anticancer</subject><subject>Bibenzyl</subject><subject>Bibenzyls - chemical synthesis</subject><subject>Bibenzyls - chemistry</subject><subject>Bibenzyls - pharmacology</subject><subject>Cell Movement - drug effects</subject><subject>Cell Proliferation - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>Human Umbilical Vein Endothelial Cells - drug effects</subject><subject>Humans</subject><subject>Molecular Docking Simulation</subject><subject>Molecular Structure</subject><subject>Receptor, TIE-2 - antagonists & inhibitors</subject><subject>Receptor, TIE-2 - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Transgenic zebrafish model</subject><subject>Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors</subject><subject>Vascular Endothelial Growth Factor Receptor-2 - metabolism</subject><subject>Zebrafish</subject><issn>0968-0896</issn><issn>1464-3391</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kD1v2zAQhomgQeKk_QFdCo5d5PJDJil0Mgw3KWA0S5KVoMhjQkMSXVI2Yv_60lDasdMd7p57gXsQ-kzJnBIqvm3nbW_njLB6TqlUQlygGa1FXXHe0A9oRhqhKqIacY1uct4SUsiGXqFr3pSVVIsZcr_iATrchhaG07HDNva7uB8cXgKGt9fQhjFjM4yhMi8hvsAQLDZ2DIcwHnEY8P3T83qVz12ZpFhQh0_QJuNDfp3Gh_gRXXrTZfj0Xm_R04_14-q-2jzc_VwtN5VlfDFW0BBhKAgjna-V59BK6o3kCwHgGFWeEcW8VM7CwltiLDNeWGalYeAIb_kt-jrl7lL8vYc86j5kC11nBoj7rDlRUjSqlk1B6YTaFHNO4PUuhd6ko6ZEn-XqrS5y9VmunuSWmy_v8fu2B_fv4q_NAnyfAChPHgIknW2AwYILCeyoXQz_if8DqgWLjA</recordid><startdate>20240901</startdate><enddate>20240901</enddate><creator>Guan, Li</creator><creator>Zhang, Shengjie</creator><creator>Song, Pengfei</creator><creator>Xia, Yanxin</creator><creator>Zheng, Xinle</creator><creator>Li, Weize</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20240901</creationdate><title>Novel bibenzyl compound Ae exhibits anti-agiogenic activity in HUVECs in vitro and zebrafish in vivo</title><author>Guan, Li ; Zhang, Shengjie ; Song, Pengfei ; Xia, Yanxin ; Zheng, Xinle ; Li, Weize</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c235t-e906a1e6a7df48f3eb71fa7356eed218f2082f78dce5fc0ac2af6c2c7a2ed03b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Angiogenesis Inhibitors - chemical synthesis</topic><topic>Angiogenesis Inhibitors - chemistry</topic><topic>Angiogenesis Inhibitors - pharmacology</topic><topic>Animals</topic><topic>Anti-angiogenesis</topic><topic>Anticancer</topic><topic>Bibenzyl</topic><topic>Bibenzyls - chemical synthesis</topic><topic>Bibenzyls - chemistry</topic><topic>Bibenzyls - pharmacology</topic><topic>Cell Movement - drug effects</topic><topic>Cell Proliferation - drug effects</topic><topic>Dose-Response Relationship, Drug</topic><topic>Human Umbilical Vein Endothelial Cells - drug effects</topic><topic>Humans</topic><topic>Molecular Docking Simulation</topic><topic>Molecular Structure</topic><topic>Receptor, TIE-2 - antagonists & inhibitors</topic><topic>Receptor, TIE-2 - metabolism</topic><topic>Structure-Activity Relationship</topic><topic>Transgenic zebrafish model</topic><topic>Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors</topic><topic>Vascular Endothelial Growth Factor Receptor-2 - metabolism</topic><topic>Zebrafish</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Guan, Li</creatorcontrib><creatorcontrib>Zhang, Shengjie</creatorcontrib><creatorcontrib>Song, Pengfei</creatorcontrib><creatorcontrib>Xia, Yanxin</creatorcontrib><creatorcontrib>Zheng, Xinle</creatorcontrib><creatorcontrib>Li, Weize</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Guan, Li</au><au>Zhang, Shengjie</au><au>Song, Pengfei</au><au>Xia, Yanxin</au><au>Zheng, Xinle</au><au>Li, Weize</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel bibenzyl compound Ae exhibits anti-agiogenic activity in HUVECs in vitro and zebrafish in vivo</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2024-09-01</date><risdate>2024</risdate><volume>111</volume><spage>117866</spage><pages>117866-</pages><artnum>117866</artnum><issn>0968-0896</issn><issn>1464-3391</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
•Our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity in zebrafish in vivo.•Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro.•The anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway.
The inhibition of angiogenesis has been considered as an attractive method for the discovery of potential anti-cancer drugs. Herein, we report our new synthesized bibenzyl compound Ae had potent anti-angiogenic activity(the lowest effective concentration is to 0.62–1.25 μM) in zebrafish in vivo and showed a concentration-dependent inhibition of inter-segmental blood vessels (ISVs) compared to control. Further, Ae exhibited the obvious inhibitory activity of proliferation, migration, invasion and tube formation in HUVEC cells in vitro. Moreover, qRT-PCR analysis revealed that the anti-angiogenic activity of compound Ae is connected with the ang-2, tek in ANGPT-TEK pathway and the kdr, kdrl signaling axle in VEGF-VEGFR pathway. Molecular docking studies revealed that compound Ae had an interaction with the angiopoietin-2 receptor(TEK) and VEGFR2. Additionally, analysis of the ADMET prediction data indicated that compound Ae possessed favorable physicochemical properties, drug-likeness, and synthetic accessibility. In conclusion, compound Ae had remarkable anti-angiogenic activity and could be served as an candidate for cancer therapy.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>39096785</pmid><doi>10.1016/j.bmc.2024.117866</doi></addata></record> |
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| subjects | Angiogenesis Inhibitors - chemical synthesis Angiogenesis Inhibitors - chemistry Angiogenesis Inhibitors - pharmacology Animals Anti-angiogenesis Anticancer Bibenzyl Bibenzyls - chemical synthesis Bibenzyls - chemistry Bibenzyls - pharmacology Cell Movement - drug effects Cell Proliferation - drug effects Dose-Response Relationship, Drug Human Umbilical Vein Endothelial Cells - drug effects Humans Molecular Docking Simulation Molecular Structure Receptor, TIE-2 - antagonists & inhibitors Receptor, TIE-2 - metabolism Structure-Activity Relationship Transgenic zebrafish model Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2 - metabolism Zebrafish |
| title | Novel bibenzyl compound Ae exhibits anti-agiogenic activity in HUVECs in vitro and zebrafish in vivo |
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