In a continuing study on discovery of more potent derivatives of sinomenine (1), a clinically available alkaloid for rheumatoid arthritis (RA) treatment, oxidation of sinomenine provided two unique stereoisomers, disinomenines 2 and 3. The structure of 3 was determined by MS, NMR, and X-ray analysis. The formation of 2 and 3 via oxidation of sinomenine by potassium permanganate (KMnO4) exhibited a pH-dependent stereoselectivity. The bioassay results using human synovial sarcoma cells (SW982) showed that 2 inhibited, while 3 stimulated, IL-6 production.
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Exploring the therapeutic potential: sinomenine and melatonin in alkali-induced corneal burns.
Int Ophthalmol
November 2024
Faculty of Medicine, Department of Ophthalmology, Tokat Gaziosmanpaşa University, Tokat, Turkey.
Purpose: This study aimed to investigate the effects of sinomenine and melatonin on corneal alkali burns.
Methods: Twenty-seven female Wistar albino rats, aged 3-6 months and weighing 200-300 g, were used in this study. After the induction of general anesthesia, 2 mol/L sodium hydroxide (NaOH) solution was used to create corneal alkali burns in all experimental animals.
Sinomenine Hydrochloride Regulates the Apoptosis of Endothelial Cells through PPAR-γ to Alleviate PAH.
Int Heart J
September 2024
Department of Respiratory and Critical Care Medicine, The Second Hospital of Hebei Medical University.
Pulmonary arterial hypertension is a progressive heart and lung disease that is caused by irreversible pulmonary vascular remodeling. Sinomenine hydrochloride is an alkaloid that is extracted from sinomenium acutum, which has strong anti-inflammatory effects. In this study, male rats were injected with monocrotaline, and endothelial cells were exposed to hypoxia for 24 hours to induce pulmonary arterial hypertension.
View Article and Find Full Text PDFProtective effect of sinomenine against CCl4-induced acute liver injury through regulation of mitochondrial biogenesis.
Naunyn Schmiedebergs Arch Pharmacol
September 2024
Neurophysiology Research Center, Shahed University, Tehran, Iran.
Carbon tetrachloride (CCl4)-provoked acute liver injury (ALI) is typified by intensified apoptotic, inflammatory, and oxidative changes besides mitochondrial dysfunction. Sinomenine is an active constituent in the medicinal plant Sinomenium acutum. The main objective of this study was to determine sinomenine-induced hepatoprotection following CCl4 challenge with an emphasis on unraveling the contribution of mitochondrial biogenesis-related factors.
View Article and Find Full Text PDFDevelopment of an integrated strategy for comprehensive characterization of Sinomenii Caulis extract and metabolites in rats based on UPLC/Q-TOF-MS.
J Pharm Biomed Anal
October 2024
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address:
Article Synopsis
- Sinomenii Caulis (SC) is a traditional Chinese medicine primarily studied for its therapeutic effects on rheumatoid arthritis, but research has mostly centered on sinomenine rather than exploring other alkaloids.
- This study utilized advanced techniques (UPLC/Q-TOF-MS) to analyze SC's chemical profile and its effects on rats, identifying 114 alkaloid compounds and 324 metabolites in biological samples like plasma and urine.
- The findings highlight various metabolization processes and offer a comprehensive strategy for better understanding the compound diversity in SC, potentially aiding in the discovery of new treatments for rheumatoid arthritis.
Graphene oxide quantum dots-loaded sinomenine hydrochloride nanocomplexes for effective treatment of rheumatoid arthritis via inducing macrophage repolarization and arresting abnormal proliferation of fibroblast-like synoviocytes.
J Nanobiotechnology
July 2024
Institute of Innovation and Applied Research in Chinese Medicine, Department of Rheumatology of First Hospital, Hunan University of Chinese Medicine, Changsha, 410208, Hunan, China.
The characteristic features of the rheumatoid arthritis (RA) microenvironment are synovial inflammation and hyperplasia. Therefore, there is a growing interest in developing a suitable therapeutic strategy for RA that targets the synovial macrophages and fibroblast-like synoviocytes (FLSs). In this study, we used graphene oxide quantum dots (GOQDs) for loading anti-arthritic sinomenine hydrochloride (SIN).
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