Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment

Osteoporosis (OP) is a common metabolic disease, that mainly affects skeletal system with the features, including reduction bone density, deterioration bone structure, bone pain and increase risk of bone fracture. In this work, a well-known anti-osteoporosis natural compound named as dihydromyriceti...

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Main Authors: Yanlong Zhong, Shaorong Huang, Peng Luo, Qi Lai, Fengbo Mo, Xinmin Yang, Xiaoyong Zhang, Bin Zhang, Yen Wei, Xiaowei Yang
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/S0264127525005696
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author Yanlong Zhong
Shaorong Huang
Peng Luo
Qi Lai
Fengbo Mo
Xinmin Yang
Xiaoyong Zhang
Bin Zhang
Yen Wei
Xiaowei Yang
author_facet Yanlong Zhong
Shaorong Huang
Peng Luo
Qi Lai
Fengbo Mo
Xinmin Yang
Xiaoyong Zhang
Bin Zhang
Yen Wei
Xiaowei Yang
author_sort Yanlong Zhong
collection DOAJ
description Osteoporosis (OP) is a common metabolic disease, that mainly affects skeletal system with the features, including reduction bone density, deterioration bone structure, bone pain and increase risk of bone fracture. In this work, a well-known anti-osteoporosis natural compound named as dihydromyricetin (DMY) was selected as the model compound to construct a carrier-free bone targeting nanomedicine via a one-step phosphorylation reaction, in which the phenolic groups on DMY were converted into phosphate groups after reacting with phosphorus oxychloride. The resultant phosphorylated DMY (p-DMY) could self-assemble into nanoparticles with excellent water dispersibility and bone targeting capability because of the introduction of hydrophilic phosphate groups. In vitro results demonstrated p-DMY mainly inhibited osteoclast differentiation by blocking NF-κB and MAPK signals in a dose-dependent manner. More interestingly, p-DMY could significantly improve OP treatment efficacy in preventing bone loss and improving the biomechanics of bone tissues as compared with DMY in ovariectomy mice. Therefore, considered the facile synthesis procedure, enhanced OP treatment efficacy as well as negative toxicity of p-DMY, we trust this strategy described in this work should be an elegant tool for construction of natural compounds-based nanomedicines for OP and other metabolic disease treatment.
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spelling doaj-art-337dec8e8a474603a7796b7c76eb7f032025-08-20T03:30:49ZengElsevierMaterials & Design0264-12752025-07-0125511414910.1016/j.matdes.2025.114149Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatmentYanlong Zhong0Shaorong Huang1Peng Luo2Qi Lai3Fengbo Mo4Xinmin Yang5Xiaoyong Zhang6Bin Zhang7Yen Wei8Xiaowei Yang9Orthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, ChinaInstitute of Geriatrics, Jiangxi Provincial People’s Hospital &, the First Affiliated Hospital of Nanchang Medical College, Nanchang 330006 Jiangxi, People's Republic of ChinaOrthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, ChinaOrthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, ChinaOrthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, ChinaOrthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, ChinaDepartment of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, China; Corresponding authors.Orthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Corresponding authors.Department of Chemistry and the Tsinghua Center for Frontier Polymer Research, Tsinghua University, Beijing 100084, ChinaOrthopedic Hospital, the First Affiliated Hospital, Jiangxi Medical College, Nanchang University, No. 17 Yong Wai Zheng Street, Nanchang, Jiangxi 330006, China; Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, China; Corresponding authors.Osteoporosis (OP) is a common metabolic disease, that mainly affects skeletal system with the features, including reduction bone density, deterioration bone structure, bone pain and increase risk of bone fracture. In this work, a well-known anti-osteoporosis natural compound named as dihydromyricetin (DMY) was selected as the model compound to construct a carrier-free bone targeting nanomedicine via a one-step phosphorylation reaction, in which the phenolic groups on DMY were converted into phosphate groups after reacting with phosphorus oxychloride. The resultant phosphorylated DMY (p-DMY) could self-assemble into nanoparticles with excellent water dispersibility and bone targeting capability because of the introduction of hydrophilic phosphate groups. In vitro results demonstrated p-DMY mainly inhibited osteoclast differentiation by blocking NF-κB and MAPK signals in a dose-dependent manner. More interestingly, p-DMY could significantly improve OP treatment efficacy in preventing bone loss and improving the biomechanics of bone tissues as compared with DMY in ovariectomy mice. Therefore, considered the facile synthesis procedure, enhanced OP treatment efficacy as well as negative toxicity of p-DMY, we trust this strategy described in this work should be an elegant tool for construction of natural compounds-based nanomedicines for OP and other metabolic disease treatment.http://www.sciencedirect.com/science/article/pii/S0264127525005696OsteoporosisPhosphorylated dihydromyricetinBone targetingCarrier-free nanomedicineEnhancement of efficacy
spellingShingle Yanlong Zhong
Shaorong Huang
Peng Luo
Qi Lai
Fengbo Mo
Xinmin Yang
Xiaoyong Zhang
Bin Zhang
Yen Wei
Xiaowei Yang
Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
Materials & Design
Osteoporosis
Phosphorylated dihydromyricetin
Bone targeting
Carrier-free nanomedicine
Enhancement of efficacy
title Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
title_full Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
title_fullStr Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
title_full_unstemmed Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
title_short Self-assembly of phosphorylated dihydromyricetin as a carrier-free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
title_sort self assembly of phosphorylated dihydromyricetin as a carrier free bone targeting nanomedicine with enhanced efficacy for osteoporosis treatment
topic Osteoporosis
Phosphorylated dihydromyricetin
Bone targeting
Carrier-free nanomedicine
Enhancement of efficacy
url http://www.sciencedirect.com/science/article/pii/S0264127525005696
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