Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies
Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the...
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| Veröffentlicht in: | International journal of biological macromolecules 2024-12, Vol.282 (Pt 1), p.136660, Article 136660 |
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| container_issue | Pt 1 |
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| container_title | International journal of biological macromolecules |
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| creator | Kumar, Sumit Kumar, Dharmender Upadhyay, Charu Bansal, Meenakshi Rathi, Brijesh Singh, Priyamvada |
| description | Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the resulting CNC-CXN nano-conjugate. Elemental analysis, powder X-ray, SEM, AFM, Infrared, and solid-state NMR spectroscopic techniques confirmed the composition of novel CNC-CXN nano-conjugate. Next, CNC-CXN nano-conjugate did not exhibit apparent cytotoxic effects on the sensitive Vero E6 cell line up to a concentration of 4.66 μg/μl. The CNC-CXN nano-conjugate was also evaluated for its preliminary efficacy on Plasmodium falciparum (3D7) malaria parasite and showed a 50 % inhibitory concentration value of 0.02 μg/μl. Overall, the selectivity index (SI) of the CNC-CXN nano-conjugate significantly improved to 233, indicating its suitability for further validation studies in animal models.
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•Biodegradable CNCs were conjugated with Calxinin (CXN) via click chemistry.•CNC-CXN nano-conjugate showed improved thermal stability and structural integrity.•CNC-CXN displayed low cytotoxicity up to 4.66 μg/μl on Vero E6 cells.•High antiplasmodial activity against P. falciparum with a selectivity index of 233. |
| doi_str_mv | 10.1016/j.ijbiomac.2024.136660 |
| format | Article |
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[Display omitted]
•Biodegradable CNCs were conjugated with Calxinin (CXN) via click chemistry.•CNC-CXN nano-conjugate showed improved thermal stability and structural integrity.•CNC-CXN displayed low cytotoxicity up to 4.66 μg/μl on Vero E6 cells.•High antiplasmodial activity against P. falciparum with a selectivity index of 233.</description><identifier>ISSN: 0141-8130</identifier><identifier>ISSN: 1879-0003</identifier><identifier>EISSN: 1879-0003</identifier><identifier>DOI: 10.1016/j.ijbiomac.2024.136660</identifier><identifier>PMID: 39427789</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Animals ; antimalarials ; Antimalarials - chemical synthesis ; Antimalarials - chemistry ; Antimalarials - pharmacology ; biocompatibility ; biodegradability ; cell lines ; cellulose ; Cellulose - chemistry ; Cellulose - pharmacology ; Cellulose nanocrystals ; Chlorocebus aethiops ; Click chemistry ; cytotoxicity ; Functionalization ; malaria ; Nano-conjugate ; nanocrystals ; Nanoparticles - chemistry ; parasites ; Plasmodium falciparum ; Plasmodium falciparum - drug effects ; spectroscopy ; Vero Cells ; X-radiation</subject><ispartof>International journal of biological macromolecules, 2024-12, Vol.282 (Pt 1), p.136660, Article 136660</ispartof><rights>2024 Elsevier B.V.</rights><rights>Copyright © 2024 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c278t-cf69858d6fe47d62b3f4cbce0acbae5a18d9ffe3cada95f1e17ed5a14eca72d63</cites><orcidid>0000-0002-3759-1057</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0141813024074683$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/39427789$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumar, Sumit</creatorcontrib><creatorcontrib>Kumar, Dharmender</creatorcontrib><creatorcontrib>Upadhyay, Charu</creatorcontrib><creatorcontrib>Bansal, Meenakshi</creatorcontrib><creatorcontrib>Rathi, Brijesh</creatorcontrib><creatorcontrib>Singh, Priyamvada</creatorcontrib><title>Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies</title><title>International journal of biological macromolecules</title><addtitle>Int J Biol Macromol</addtitle><description>Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the resulting CNC-CXN nano-conjugate. Elemental analysis, powder X-ray, SEM, AFM, Infrared, and solid-state NMR spectroscopic techniques confirmed the composition of novel CNC-CXN nano-conjugate. Next, CNC-CXN nano-conjugate did not exhibit apparent cytotoxic effects on the sensitive Vero E6 cell line up to a concentration of 4.66 μg/μl. The CNC-CXN nano-conjugate was also evaluated for its preliminary efficacy on Plasmodium falciparum (3D7) malaria parasite and showed a 50 % inhibitory concentration value of 0.02 μg/μl. Overall, the selectivity index (SI) of the CNC-CXN nano-conjugate significantly improved to 233, indicating its suitability for further validation studies in animal models.
[Display omitted]
•Biodegradable CNCs were conjugated with Calxinin (CXN) via click chemistry.•CNC-CXN nano-conjugate showed improved thermal stability and structural integrity.•CNC-CXN displayed low cytotoxicity up to 4.66 μg/μl on Vero E6 cells.•High antiplasmodial activity against P. falciparum with a selectivity index of 233.</description><subject>Animals</subject><subject>antimalarials</subject><subject>Antimalarials - chemical synthesis</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - pharmacology</subject><subject>biocompatibility</subject><subject>biodegradability</subject><subject>cell lines</subject><subject>cellulose</subject><subject>Cellulose - chemistry</subject><subject>Cellulose - pharmacology</subject><subject>Cellulose nanocrystals</subject><subject>Chlorocebus aethiops</subject><subject>Click chemistry</subject><subject>cytotoxicity</subject><subject>Functionalization</subject><subject>malaria</subject><subject>Nano-conjugate</subject><subject>nanocrystals</subject><subject>Nanoparticles - chemistry</subject><subject>parasites</subject><subject>Plasmodium falciparum</subject><subject>Plasmodium falciparum - drug effects</subject><subject>spectroscopy</subject><subject>Vero Cells</subject><subject>X-radiation</subject><issn>0141-8130</issn><issn>1879-0003</issn><issn>1879-0003</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkUFv1DAQhS0EokvhL1Q-cmgWO3EchxOoogWpEgfaszWxJ6xXib3YDmg594fXq91yLacZjd57Y89HyAVna864_LBdu-3gwgxmXbNarHkjpWQvyIqrrq8YY81LsmJc8Erxhp2RNylty1S2XL0mZ00v6q5T_Yo8XC_eZBc8TO4vHBoaRmpwmpYpJKQefDBxnzJMif5xeUOB7kJGnyn47GaYIDqYqAnzLizefqQ_9j5vMLl0Sc0GIpiM8RR9WTyWlmdP4aczxZXyYh2mt-TVWPLx3amek_vrL3dXX6vb7zffrj7fVqbuVK7MKHvVKitHFJ2V9dCMwgwGGZgBsAWubD-O2Biw0LcjR96hLWOBBrrayuacvD_m7mL4tWDKenbp8FfwGJakG96KWrS8r_9DypVqRN-KIpVHqYkhpYij3sVymLjXnOkDLL3VT7D0AZY-wirGi9OOZZjR_rM90SmCT0cBlqP8dhh1Mg69QesimqxtcM_teATmOq4h</recordid><startdate>202412</startdate><enddate>202412</enddate><creator>Kumar, Sumit</creator><creator>Kumar, Dharmender</creator><creator>Upadhyay, Charu</creator><creator>Bansal, Meenakshi</creator><creator>Rathi, Brijesh</creator><creator>Singh, Priyamvada</creator><general>Elsevier 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>7X8</scope><scope>7S9</scope><scope>L.6</scope><orcidid>https://orcid.org/0000-0002-3759-1057</orcidid></search><sort><creationdate>202412</creationdate><title>Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies</title><author>Kumar, Sumit ; Kumar, Dharmender ; Upadhyay, Charu ; Bansal, Meenakshi ; Rathi, Brijesh ; Singh, Priyamvada</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c278t-cf69858d6fe47d62b3f4cbce0acbae5a18d9ffe3cada95f1e17ed5a14eca72d63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Animals</topic><topic>antimalarials</topic><topic>Antimalarials - chemical synthesis</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - pharmacology</topic><topic>biocompatibility</topic><topic>biodegradability</topic><topic>cell lines</topic><topic>cellulose</topic><topic>Cellulose - chemistry</topic><topic>Cellulose - pharmacology</topic><topic>Cellulose nanocrystals</topic><topic>Chlorocebus aethiops</topic><topic>Click chemistry</topic><topic>cytotoxicity</topic><topic>Functionalization</topic><topic>malaria</topic><topic>Nano-conjugate</topic><topic>nanocrystals</topic><topic>Nanoparticles - chemistry</topic><topic>parasites</topic><topic>Plasmodium falciparum</topic><topic>Plasmodium falciparum - drug effects</topic><topic>spectroscopy</topic><topic>Vero Cells</topic><topic>X-radiation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumar, Sumit</creatorcontrib><creatorcontrib>Kumar, Dharmender</creatorcontrib><creatorcontrib>Upadhyay, Charu</creatorcontrib><creatorcontrib>Bansal, Meenakshi</creatorcontrib><creatorcontrib>Rathi, Brijesh</creatorcontrib><creatorcontrib>Singh, Priyamvada</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><collection>AGRICOLA</collection><collection>AGRICOLA - Academic</collection><jtitle>International journal of biological macromolecules</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kumar, Sumit</au><au>Kumar, Dharmender</au><au>Upadhyay, Charu</au><au>Bansal, Meenakshi</au><au>Rathi, Brijesh</au><au>Singh, Priyamvada</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies</atitle><jtitle>International journal of biological macromolecules</jtitle><addtitle>Int J Biol Macromol</addtitle><date>2024-12</date><risdate>2024</risdate><volume>282</volume><issue>Pt 1</issue><spage>136660</spage><pages>136660-</pages><artnum>136660</artnum><issn>0141-8130</issn><issn>1879-0003</issn><eissn>1879-0003</eissn><abstract>Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the resulting CNC-CXN nano-conjugate. Elemental analysis, powder X-ray, SEM, AFM, Infrared, and solid-state NMR spectroscopic techniques confirmed the composition of novel CNC-CXN nano-conjugate. Next, CNC-CXN nano-conjugate did not exhibit apparent cytotoxic effects on the sensitive Vero E6 cell line up to a concentration of 4.66 μg/μl. The CNC-CXN nano-conjugate was also evaluated for its preliminary efficacy on Plasmodium falciparum (3D7) malaria parasite and showed a 50 % inhibitory concentration value of 0.02 μg/μl. Overall, the selectivity index (SI) of the CNC-CXN nano-conjugate significantly improved to 233, indicating its suitability for further validation studies in animal models.
[Display omitted]
•Biodegradable CNCs were conjugated with Calxinin (CXN) via click chemistry.•CNC-CXN nano-conjugate showed improved thermal stability and structural integrity.•CNC-CXN displayed low cytotoxicity up to 4.66 μg/μl on Vero E6 cells.•High antiplasmodial activity against P. falciparum with a selectivity index of 233.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>39427789</pmid><doi>10.1016/j.ijbiomac.2024.136660</doi><orcidid>https://orcid.org/0000-0002-3759-1057</orcidid></addata></record> |
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| subjects | Animals antimalarials Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology biocompatibility biodegradability cell lines cellulose Cellulose - chemistry Cellulose - pharmacology Cellulose nanocrystals Chlorocebus aethiops Click chemistry cytotoxicity Functionalization malaria Nano-conjugate nanocrystals Nanoparticles - chemistry parasites Plasmodium falciparum Plasmodium falciparum - drug effects spectroscopy Vero Cells X-radiation |
| title | Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies |
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