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In this manuscript, the resource distribution, pharmacological activity, pharma-cokinetics of sinomenine and the structure, synthesis, biological activity and mechanism of sinomenine derivatives reported from 2000 to December 2023 were reviewed. The lit-erature was retrieved through Web of Science, PubMed, Science Direct, SciFiner Scholar and other websites. Sinomenine belongs to isoquinoline alkaloids and was extracted from the Chinese herb Sinomenium acutum root. In Asian countries such as China and Japan, it is commonly prescribed as a treatment for rheumatoid arthritis. In addition, sinomenine also has sedative, analgesic, anti-inflammatory, immunosuppressive, neuroprotective, an-ti-drug dependence, anti-tumor and other biological activities. Sinomenine limited its ap-plication prospects because of its large dosage, poor epidermal permeability and short half-life. To overcome these defects, new sinomenine derivatives have been synthesized. Based on the comprehensive analysis of relevant literature at home and abroad, this paper reviews the recent progress in the study of sinomenine's pharmacological effects and structural modifications. Future research on sinomenine will focus on improving its thera-peutic effect, and developing new drug preparations and structural modifications. It is hoped that this review will help to better understand the research progress of sinomenine and provide constructive suggestions for further research of sinomenine.
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http://dx.doi.org/10.2174/0109298673323738240830055548 | DOI Listing |
Nat Prod Res
August 2025
School of Pharmacy, Anhui College of Traditional Chinese Medicine, Wuhu, China.
The herbal formula Qing-Luo-Yin (QLY) shows potential in activating PPARγ. This study investigated how this property contributed to its anti-rheumatic effects. Some mice with antigen-induced arthritis (AA) were orally treated with QLY and/or PPARγ antagonist/agonist (T0070907/rosiglitazone).
View Article and Find Full Text PDFJ Nanobiotechnology
August 2025
Department of Anesthesiology, Yuebei People's Hospital, Shantou University Medical College, No. 133, South Huimin Road, Shaoguan, 512026, Guangdong Province, P. R. China.
Background: Diabetic peripheral neuropathy (DPN) is one of the most prevalent and debilitating complications of diabetes, marked by chronic neuroinflammation, immune dysregulation, and progressive neuronal degeneration. Current treatments offer limited efficacy, largely focusing on symptomatic relief rather than addressing the underlying disease mechanisms. There is a critical need for disease-modifying therapies that target the molecular basis of DPN.
View Article and Find Full Text PDFJ Biochem Mol Toxicol
September 2025
Nephrology Department, Hubei Provincial Hospital of Traditional Chinese Medicine, Wuhan, Hubei, China.
Diabetic kidney disease (DKD) is a common complication of diabetes, often characterized by podocyte injury, proteinuria, and eventual renal failure. Sinomenine hydrochloride (SH), an active component derived from traditional Chinese medicine, is clinically effective in treating kidney diseases. This study investigates the protective effects of SH on podocytes under high-glucose conditions and its mechanism of action.
View Article and Find Full Text PDFBioorg Med Chem Lett
December 2025
The Fourth Affiliated Hospital of Jiangsu University, Zhenjiang 212001, China. Electronic address:
Sinomenine possesses potent suppression on the nuclear factor kappa-B (NF-κB) pathway. The phenylpropanoid moiety was introduced into sinomenine for building dual-structure sinomenine hybrid derivatives. The software AutoDock Vina was used to dock the sinomenine hybrid derivatives with 3 key proteins (1VKX, 4KIK and 6YMN) of NF-κB activation, and the virtually screened derivatives were tested via molecular dynamics simulation.
View Article and Find Full Text PDFPhytother Res
July 2025
Department of Gastroenterology, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, People's Republic of China.
Liver fibrosis, a pivotal pathological feature in the progression of chronic liver injury, currently lacks effective therapies. Sinomenine (SIN), a bioactive alkaloid derived from traditional Chinese medicine, demonstrates diverse pharmacological properties. However, its therapeutic potential and mechanisms in liver fibrosis remain inadequately characterized.
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