In order to search for drugs with excellent anti-inflammatory activities, a series of novel sinomenine derivatives were designed, synthesized, and evaluated for their inhibition activities against NF-κB activation induced by lipopolysaccharide (LPS). Compared with the natural parent sinomenine, compounds 2a-w showed higher activity, while compounds 1a-o showed similar activity against NF-κB. Moreover, a molecular model for the binding between compound 2v and the active site of p50 was provided on the basis of the computational docking results.
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[Preparation of hybrid exosomes based on bovine milk exosomes and liposomes and pharmacodynamic study of sinomenine loaded exosomes in treatment of rheumatoid arthritis].
Zhongguo Zhong Yao Za Zhi
August 2024
College of Pharmacy, Heilongjiang University of Chinese Medicine Harbin 150040, China.
This study investigates the therapeutic effect of hybrid exosomes loaded with sinomenine(SIN) obtained by membrane fusion of milk exosomes with liposomes in collagen-induced arthritis(CIA) rats. Exosomes were isolated from fresh bovine milk by sucrose density gradient centrifugation, while liposomes were prepared using the emulsion solvent evaporation-low temperature curing method. Hybrid exosomes were characterized after membrane fusion through co-incubation: The morphology was detected by transmission electron microscopy, the particle size and potential by nanoparticle size potentiostat, and the expressions of surface characteristic proteins CD63 and TSG101 before and after fusion by Western blot(WB).
View Article and Find Full Text PDFResearch, Development and Pharmacological Activity of Sinomenine and Its Derivatives.
Curr Med Chem
September 2024
Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, P.R. China.
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.
View Article and Find Full Text PDFSinomenine ameliorates bleomycin-induced pulmonary fibrosis by inhibiting the differentiation of fibroblast into myofibroblast.
Heliyon
July 2024
Department of Geriatrics, The Central Hospital of Wuhan, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430014, China.
Idiopathic pulmonary fibrosis (IPF) represents a severe interstitial lung disease characterized by limited therapeutic interventions. Recent study has suggested that sinomenine (SIN), an alkaloid derived from the roots of Sinomenium acutum, demonstrates efficacy in interrupting aerobic glycolysis, a predominant metabolic pathway in myofibroblasts. However, its pharmacological potential in the context of pulmonary fibrosis remains inadequately explored.
View Article and Find Full Text PDF[Sinomenine inhibits PDGF/PDGFR signaling pathway to reduce RA-FLS migration induced by NETs].
Zhongguo Zhong Yao Za Zhi
April 2024
Department of Rheumatology and Immunology, Gulou Clinical College of Nanjing University of Chinese Medicine Nanjing 210008, China.
This study aims to decipher the mechanism of sinomenine in inhibiting platelet-derived growth factor/platelet-derived growth factor receptor(PDGF/PDGFR) signaling pathway in rheumatoid arthritis-fibroblast-like synoviocyte(RA-FLS) migration induced by neutrophil extracellular traps(NETs). RA-FLS was isolated from the synovial tissue of 3 RA patients and cultured. NETs were extracted from the peripheral venous blood of 4 RA patients and 4 healthy control(HC).
View Article and Find Full Text PDFA systematic review: Sinomenine.
Heliyon
May 2024
Sino-Pakistan Center on Traditional Chinese Medicine, School of Pharmaceutical Sciences, Hunan University of Medicine, Huaihua City, Hunan Province, 418000, PR China.
Sinomenine (SIN), an alkaloid derived from the traditional Chinese medicine, , has been used as an anti-inflammatory drug in China for over 30 years. With the continuous increase in research on the pharmacological mechanism of SIN, it has been found that, in addition to the typical rheumatoid arthritis (RA) treatment, SIN can be used as a potentially effective therapeutic drug for anti-tumour, anti-renal, and anti-nervous system diseases. By reviewing a large amount of literature and conducting a summary analysis of the literature pertaining to the pharmacological mechanism of SIN, we completed a review that focused on SIN, found that the current research is insufficient, and offered an outlook for future SIN development.
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