A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway

Bone destruction in rheumatoid arthritis (RA) leads to significant disability, yet effective treatments are limited. Sinomenine (Sino) demonstrates anti-arthritic and bone-protective effects but requires high doses. In this study, we developed a Sino derivative, SINX, and evaluated its efficacy in R...

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Main Authors: Wan-Yi Guo, Qi-Min Wu, Hao-Feng Zeng, Yu-Lian Chen, Jie Xu, Zhen-Yi Yu, Yong-Kang Shu, Xiao-Nan Yang, Chuan-Hai Zhang, Xi-Zi He, Jia-Ning Mi, Si Chen, Xiao-Man Chen, Jia-Qi Wu, He-Quan Yao, Liang Liu, Hu-Dan Pan
Format: Article
Language:English
Published: Elsevier 2025-05-01
Series:Pharmacological Research
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Online Access:http://www.sciencedirect.com/science/article/pii/S1043661825001112
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author Wan-Yi Guo
Qi-Min Wu
Hao-Feng Zeng
Yu-Lian Chen
Jie Xu
Zhen-Yi Yu
Yong-Kang Shu
Xiao-Nan Yang
Chuan-Hai Zhang
Xi-Zi He
Jia-Ning Mi
Si Chen
Xiao-Man Chen
Jia-Qi Wu
He-Quan Yao
Liang Liu
Hu-Dan Pan
author_facet Wan-Yi Guo
Qi-Min Wu
Hao-Feng Zeng
Yu-Lian Chen
Jie Xu
Zhen-Yi Yu
Yong-Kang Shu
Xiao-Nan Yang
Chuan-Hai Zhang
Xi-Zi He
Jia-Ning Mi
Si Chen
Xiao-Man Chen
Jia-Qi Wu
He-Quan Yao
Liang Liu
Hu-Dan Pan
author_sort Wan-Yi Guo
collection DOAJ
description Bone destruction in rheumatoid arthritis (RA) leads to significant disability, yet effective treatments are limited. Sinomenine (Sino) demonstrates anti-arthritic and bone-protective effects but requires high doses. In this study, we developed a Sino derivative, SINX, and evaluated its efficacy in RA. Safety assessments in mice confirmed its suitability for further study. In vitro, SINX inhibited osteoclast differentiation by reducing TRAP-positive cells, disrupting F-actin ring formation, and suppressing bone resorption pits, alongside downregulating osteoclast-specific genes. It also showed strong anti-inflammatory properties by reducing inflammatory cytokine levels. In vivo, using a collagen-induced arthritis (CIA) mouse model, SINX improved bone integrity by reducing joint inflammation, maintaining trabecular bone density, and preventing erosion. Histological and micro-CT analyses confirmed its effects, including suppressed osteoclast activity and reduced bone resorption-related gene expression. Mechanistically, SINX ameliorated mitochondrial dysfunction, decreased ROS levels, and activated the NRF2/HO-1/NQO1 pathway, enhancing antioxidant defenses. Compared to Sino, SINX achieved similar results at lower doses. These findings highlight the potential of SINX as a safe, effective treatment for RA-related bone destruction.
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spelling doaj-art-9dfd8f882d854791b612c1d777b3242b2025-08-20T02:18:55ZengElsevierPharmacological Research1096-11862025-05-0121510768610.1016/j.phrs.2025.107686A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathwayWan-Yi Guo0Qi-Min Wu1Hao-Feng Zeng2Yu-Lian Chen3Jie Xu4Zhen-Yi Yu5Yong-Kang Shu6Xiao-Nan Yang7Chuan-Hai Zhang8Xi-Zi He9Jia-Ning Mi10Si Chen11Xiao-Man Chen12Jia-Qi Wu13He-Quan Yao14Liang Liu15Hu-Dan Pan16State Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, China; Chinese Medicine Guangdong Laboratory (Hengqin Laboratory), Guangdong-Macao In-Depth Cooperation Zone in Hengqin, 519000, China; State Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Jiangning District, Nanjing 211198, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, China; State Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Jiangning District, Nanjing 211198, ChinaState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, China; Chinese Medicine Guangdong Laboratory (Hengqin Laboratory), Guangdong-Macao In-Depth Cooperation Zone in Hengqin, 519000, China; State Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, MacaoState Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, China; Chinese Medicine Guangdong Laboratory (Hengqin Laboratory), Guangdong-Macao In-Depth Cooperation Zone in Hengqin, 519000, China; State Key Laboratory of Quality Research in Chinese Medicine (Macau University of Science and Technology), Taipa, Macao; Corresponding author at: State Key Laboratory of Traditional Chinese Medicine Syndrome /The Second Clinical College, Guangzhou University of Chinese Medicine, Guangdong Province 510405, China.Bone destruction in rheumatoid arthritis (RA) leads to significant disability, yet effective treatments are limited. Sinomenine (Sino) demonstrates anti-arthritic and bone-protective effects but requires high doses. In this study, we developed a Sino derivative, SINX, and evaluated its efficacy in RA. Safety assessments in mice confirmed its suitability for further study. In vitro, SINX inhibited osteoclast differentiation by reducing TRAP-positive cells, disrupting F-actin ring formation, and suppressing bone resorption pits, alongside downregulating osteoclast-specific genes. It also showed strong anti-inflammatory properties by reducing inflammatory cytokine levels. In vivo, using a collagen-induced arthritis (CIA) mouse model, SINX improved bone integrity by reducing joint inflammation, maintaining trabecular bone density, and preventing erosion. Histological and micro-CT analyses confirmed its effects, including suppressed osteoclast activity and reduced bone resorption-related gene expression. Mechanistically, SINX ameliorated mitochondrial dysfunction, decreased ROS levels, and activated the NRF2/HO-1/NQO1 pathway, enhancing antioxidant defenses. Compared to Sino, SINX achieved similar results at lower doses. These findings highlight the potential of SINX as a safe, effective treatment for RA-related bone destruction.http://www.sciencedirect.com/science/article/pii/S1043661825001112Rheumatoid arthritisReactive oxygen species (ROS)Mitochondrial functionSinomenine derivativesNRF2/HO-1/NQO1
spellingShingle Wan-Yi Guo
Qi-Min Wu
Hao-Feng Zeng
Yu-Lian Chen
Jie Xu
Zhen-Yi Yu
Yong-Kang Shu
Xiao-Nan Yang
Chuan-Hai Zhang
Xi-Zi He
Jia-Ning Mi
Si Chen
Xiao-Man Chen
Jia-Qi Wu
He-Quan Yao
Liang Liu
Hu-Dan Pan
A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
Pharmacological Research
Rheumatoid arthritis
Reactive oxygen species (ROS)
Mitochondrial function
Sinomenine derivatives
NRF2/HO-1/NQO1
title A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
title_full A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
title_fullStr A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
title_full_unstemmed A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
title_short A sinomenine derivative alleviates bone destruction in collagen-induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the NRF2/HO-1/NQO1 signaling pathway
title_sort sinomenine derivative alleviates bone destruction in collagen induced arthritis mice by suppressing mitochondrial dysfunction and oxidative stress via the nrf2 ho 1 nqo1 signaling pathway
topic Rheumatoid arthritis
Reactive oxygen species (ROS)
Mitochondrial function
Sinomenine derivatives
NRF2/HO-1/NQO1
url http://www.sciencedirect.com/science/article/pii/S1043661825001112
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