A Promising Drug Candidate as Potent Therapeutic Approach for Neuroinflammation and Its In Silico Justification of Chalcone Congeners: a Comprehensive Review
Multiple genetic, environmental, and immunological variables cause neuropsychiatric disorders (NPDs). The induced inflammatory immune response is also connected to the severity and treatment outcomes of various NPDs. These reactions also significantly impact numerous brain functions such as GABAergi...
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| Veröffentlicht in: | Molecular neurobiology 2024-04, Vol.61 (4), p.1873-1891 |
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| creator | Karati, Dipanjan Mukherjee, Swarupananda Roy, Souvik |
| description | Multiple genetic, environmental, and immunological variables cause neuropsychiatric disorders (NPDs). The induced inflammatory immune response is also connected to the severity and treatment outcomes of various NPDs. These reactions also significantly impact numerous brain functions such as GABAergic signaling and neurotransmitter synthesis through inflammatory cytokines and chemokines. Chalcones (1,3-diaryl-2-propen-1-ones) and their heterocyclic counterparts are flavonoids with various biological characteristics including anti-inflammatory activity. Several pure chalcones have been clinically authorized or studied in humans. Chalcones are favored for their diagnostic and therapeutic efficacy in neuroinflammation due to their tiny molecular size, easy manufacturing, and flexibility for changes to adjust lipophilicity ideal for BBB penetrability. These compounds reached an acceptable plasma concentration and were well-tolerated in clinical testing. As a result, they are attracting increasing attention from scientists. However, chalcones’ therapeutic potential remains largely untapped. This paper is aimed at highlighting the causes of neuroinflammation, more potent chalcone congeners, their mechanisms of action, and relevant structure–activity relationships.
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| doi_str_mv | 10.1007/s12035-023-03632-0 |
| format | Article |
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Graphical Abstract</description><subject>Anti-inflammatory agents</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Brain research</subject><subject>Cell Biology</subject><subject>Chalcone - pharmacology</subject><subject>Chalcones - pharmacology</subject><subject>Chemokines</subject><subject>Clinical outcomes</subject><subject>Congeners</subject><subject>Cytokines</subject><subject>Drug development</subject><subject>Flavonoids</subject><subject>Flavonoids - pharmacology</subject><subject>Humans</subject><subject>Immune response</subject><subject>Inflammation</subject><subject>Kinases</subject><subject>Leukocytes</subject><subject>Mental disorders</subject><subject>Neurobiology</subject><subject>Neuroinflammatory Diseases</subject><subject>Neurology</subject><subject>Neurosciences</subject><subject>Pathogenesis</subject><subject>Pharmaceutical sciences</subject><subject>Proteins</subject><subject>Structure-Activity Relationship</subject><subject>γ-Aminobutyric acid</subject><issn>0893-7648</issn><issn>1559-1182</issn><issn>1559-1182</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc1u1DAUhS0EosPAC7BAltiwCb228-OwG4W_qSqooKwjx7mecZXYqZ0U8TB91xpSQGLBxpZ1v3Nsn0PIcwavGUB1GhkHUWTARQaiFDyDB2TDiqLOGJP8IdmArEVWlbk8IU9ivALgnEH1mJyISkISFxtyu6MXwY82Wnegb8NyoI1yve3VjFRFeuFndDO9PGJQEy6z1XQ3TcErfaTGB_oJl-CtM4MaRzVb72hS0_0c6d7Rr3aw2tOzJc7WWL3OvaHNUQ3aO6SNdwd0GOIbqtJhnAIe0UV7g_QL3lj8_pQ8MmqI-Ox-35Jv799dNh-z888f9s3uPNOCl3PGTafzupOm7njX5VBKJpDlXdGjKoQQUILsjJEVLxH7lEJfgwFtyr7oRMLElrxafdPXrheMc5sS0TgMyqFfYstllfOySKEn9OU_6JVfgkuvawWAEHnFZZ4ovlI6-BgDmnYKdlThR8ug_Vleu5bXpvLaX-WldUte3Fsv3Yj9H8nvthIgViCmUYou_L37P7Z3-YymNg</recordid><startdate>20240401</startdate><enddate>20240401</enddate><creator>Karati, Dipanjan</creator><creator>Mukherjee, Swarupananda</creator><creator>Roy, Souvik</creator><general>Springer US</general><general>Springer Nature B.V</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>7QR</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>K9.</scope><scope>P64</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0003-2980-0362</orcidid></search><sort><creationdate>20240401</creationdate><title>A Promising Drug Candidate as Potent Therapeutic Approach for Neuroinflammation and Its In Silico Justification of Chalcone Congeners: a Comprehensive Review</title><author>Karati, Dipanjan ; Mukherjee, Swarupananda ; Roy, Souvik</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c326t-2fbc49b8f9b2bb406813e14b5dea53330608bff8726eed022d90f0cf6d5b34b53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Anti-inflammatory agents</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Brain research</topic><topic>Cell Biology</topic><topic>Chalcone - pharmacology</topic><topic>Chalcones - pharmacology</topic><topic>Chemokines</topic><topic>Clinical outcomes</topic><topic>Congeners</topic><topic>Cytokines</topic><topic>Drug development</topic><topic>Flavonoids</topic><topic>Flavonoids - pharmacology</topic><topic>Humans</topic><topic>Immune response</topic><topic>Inflammation</topic><topic>Kinases</topic><topic>Leukocytes</topic><topic>Mental disorders</topic><topic>Neurobiology</topic><topic>Neuroinflammatory Diseases</topic><topic>Neurology</topic><topic>Neurosciences</topic><topic>Pathogenesis</topic><topic>Pharmaceutical sciences</topic><topic>Proteins</topic><topic>Structure-Activity Relationship</topic><topic>γ-Aminobutyric acid</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Karati, Dipanjan</creatorcontrib><creatorcontrib>Mukherjee, Swarupananda</creatorcontrib><creatorcontrib>Roy, Souvik</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Molecular neurobiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Karati, Dipanjan</au><au>Mukherjee, Swarupananda</au><au>Roy, Souvik</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A Promising Drug Candidate as Potent Therapeutic Approach for Neuroinflammation and Its In Silico Justification of Chalcone Congeners: a Comprehensive Review</atitle><jtitle>Molecular neurobiology</jtitle><stitle>Mol Neurobiol</stitle><addtitle>Mol Neurobiol</addtitle><date>2024-04-01</date><risdate>2024</risdate><volume>61</volume><issue>4</issue><spage>1873</spage><epage>1891</epage><pages>1873-1891</pages><issn>0893-7648</issn><issn>1559-1182</issn><eissn>1559-1182</eissn><abstract>Multiple genetic, environmental, and immunological variables cause neuropsychiatric disorders (NPDs). The induced inflammatory immune response is also connected to the severity and treatment outcomes of various NPDs. These reactions also significantly impact numerous brain functions such as GABAergic signaling and neurotransmitter synthesis through inflammatory cytokines and chemokines. Chalcones (1,3-diaryl-2-propen-1-ones) and their heterocyclic counterparts are flavonoids with various biological characteristics including anti-inflammatory activity. Several pure chalcones have been clinically authorized or studied in humans. Chalcones are favored for their diagnostic and therapeutic efficacy in neuroinflammation due to their tiny molecular size, easy manufacturing, and flexibility for changes to adjust lipophilicity ideal for BBB penetrability. These compounds reached an acceptable plasma concentration and were well-tolerated in clinical testing. As a result, they are attracting increasing attention from scientists. However, chalcones’ therapeutic potential remains largely untapped. This paper is aimed at highlighting the causes of neuroinflammation, more potent chalcone congeners, their mechanisms of action, and relevant structure–activity relationships.
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| subjects | Anti-inflammatory agents Biomedical and Life Sciences Biomedicine Brain research Cell Biology Chalcone - pharmacology Chalcones - pharmacology Chemokines Clinical outcomes Congeners Cytokines Drug development Flavonoids Flavonoids - pharmacology Humans Immune response Inflammation Kinases Leukocytes Mental disorders Neurobiology Neuroinflammatory Diseases Neurology Neurosciences Pathogenesis Pharmaceutical sciences Proteins Structure-Activity Relationship γ-Aminobutyric acid |
| title | A Promising Drug Candidate as Potent Therapeutic Approach for Neuroinflammation and Its In Silico Justification of Chalcone Congeners: a Comprehensive Review |
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