Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components

The ordered biofunctionalization of hydrothermal nanocarbons played a key role in broadening their advanced biological usages, because the biomacromolecular functions were greatly affected by their direction and biostability. This paper designed novel stable inner-side-out osteoblast membrane bonded...

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Main Authors: Pinyu Ye, Kaiyi Wang, Menglan Shen, Xinran Yu, Sha Liu, Enxu Liu, Gang Chen, Qiaoyan Zhang, Shan Tao, Lupin Qin, Qiming Zhao
Format: Article
Language:English
Published: Elsevier 2025-07-01
Series:Materials & Design
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Online Access:http://www.sciencedirect.com/science/article/pii/S0264127525006318
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author Pinyu Ye
Kaiyi Wang
Menglan Shen
Xinran Yu
Sha Liu
Enxu Liu
Gang Chen
Qiaoyan Zhang
Shan Tao
Lupin Qin
Qiming Zhao
author_facet Pinyu Ye
Kaiyi Wang
Menglan Shen
Xinran Yu
Sha Liu
Enxu Liu
Gang Chen
Qiaoyan Zhang
Shan Tao
Lupin Qin
Qiming Zhao
author_sort Pinyu Ye
collection DOAJ
description The ordered biofunctionalization of hydrothermal nanocarbons played a key role in broadening their advanced biological usages, because the biomacromolecular functions were greatly affected by their direction and biostability. This paper designed novel stable inner-side-out osteoblast membrane bonded hydrothermal magnetic carbonaceous nanospheres (IOM-HMCNs) for screening herbal anti-osteoporotic components targeting to intracellular surface. Bioorthogonal hydrazone chemistry was first used for the directed and covalent immobilization of OMs, in which the cell surface carbohydrates were mildly oxidized into aldose, and linked to hydrazide-functionalized HMCNs through hydrazone bonds. The high stability and inner-side-out OM direction of biocomposite were confirmed by fluorescently labeled assay, immunogold transmission microscopyand the adsorption experiments. IOM-HMCNs successfully identified five specific components, including three novel potential active compounds from Schisandrae chinensis Fructus, which cannot be identified by traditional randomly directed OM bonded HMCNs. Their bioactivity was further validated by osteoblast-based pharmacology and osteoporotic zebrafish tests. Their binding membrane proteins were preliminarily located on insulin-like growth factor receptor 1 and ephrin receptor B4 through molecular docking and western blot analysis. These findings provide a powerful tool for advanced orientable construction of biomaterials through a sustainable route, and also contributed to a comprehensive high-efficiency screening of bioactive compounds from natural products.
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spelling doaj-art-3b46786bcf1e4c008495f09eaedaf84f2025-08-20T02:37:09ZengElsevierMaterials & Design0264-12752025-07-0125511421110.1016/j.matdes.2025.114211Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active componentsPinyu Ye0Kaiyi Wang1Menglan Shen2Xinran Yu3Sha Liu4Enxu Liu5Gang Chen6Qiaoyan Zhang7Shan Tao8Lupin Qin9Qiming Zhao10College of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaDepartment of Chemistry, The University of Hong Kong, Hong Kong SAR 999077, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, ChinaCollege of Pharmaceutical Sciences, Zijingang Campus, Zhejiang University, Hangzhou 310058, ChinaCollege of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, China; Corresponding authors.College of Pharmaceutical Sciences, Fuchun Campus, Zhejiang Chinese Medical University, Hangzhou 311403, China; Corresponding authors.The ordered biofunctionalization of hydrothermal nanocarbons played a key role in broadening their advanced biological usages, because the biomacromolecular functions were greatly affected by their direction and biostability. This paper designed novel stable inner-side-out osteoblast membrane bonded hydrothermal magnetic carbonaceous nanospheres (IOM-HMCNs) for screening herbal anti-osteoporotic components targeting to intracellular surface. Bioorthogonal hydrazone chemistry was first used for the directed and covalent immobilization of OMs, in which the cell surface carbohydrates were mildly oxidized into aldose, and linked to hydrazide-functionalized HMCNs through hydrazone bonds. The high stability and inner-side-out OM direction of biocomposite were confirmed by fluorescently labeled assay, immunogold transmission microscopyand the adsorption experiments. IOM-HMCNs successfully identified five specific components, including three novel potential active compounds from Schisandrae chinensis Fructus, which cannot be identified by traditional randomly directed OM bonded HMCNs. Their bioactivity was further validated by osteoblast-based pharmacology and osteoporotic zebrafish tests. Their binding membrane proteins were preliminarily located on insulin-like growth factor receptor 1 and ephrin receptor B4 through molecular docking and western blot analysis. These findings provide a powerful tool for advanced orientable construction of biomaterials through a sustainable route, and also contributed to a comprehensive high-efficiency screening of bioactive compounds from natural products.http://www.sciencedirect.com/science/article/pii/S0264127525006318Bionic magnetic nanocarbonsBioorthogonal hydrazone bioconjugationCell membrane directionOsteoporosisNatural drug discovery
spellingShingle Pinyu Ye
Kaiyi Wang
Menglan Shen
Xinran Yu
Sha Liu
Enxu Liu
Gang Chen
Qiaoyan Zhang
Shan Tao
Lupin Qin
Qiming Zhao
Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
Materials & Design
Bionic magnetic nanocarbons
Bioorthogonal hydrazone bioconjugation
Cell membrane direction
Osteoporosis
Natural drug discovery
title Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
title_full Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
title_fullStr Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
title_full_unstemmed Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
title_short Covalent biofunctionalization of hydrothermal nanocarbons with inner-side-out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
title_sort covalent biofunctionalization of hydrothermal nanocarbons with inner side out directed cytomembrane by hydrazone bioconjugation for screening herbal active components
topic Bionic magnetic nanocarbons
Bioorthogonal hydrazone bioconjugation
Cell membrane direction
Osteoporosis
Natural drug discovery
url http://www.sciencedirect.com/science/article/pii/S0264127525006318
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