Epiberberine chloride

Qingchang Wenzhong Decoction Alleviates DSS-Induced Inflammatory Bowel Disease by Inhibiting M1 Macrophage Polarization In Vitro and In Vivo.[Pubmed:36060126]

Biomed Res Int. 2022 Aug 25;2022:9427076.

BACKGROUND: An imbalance of macrophage M1/M2 polarization significantly influences the pathogenesis of inflammatory bowel disease. Qingchang Wenzhong decoction (QCWZD) has a proven therapeutic effect on patients with inflammatory bowel disease (IBD) and can significantly inhibit the inflammatory response in mice with colitis. However, its effect on macrophages during IBD treatment remains nebulous. Aim of the Study. Explore the mechanism underlying QCWZD effects in a dextran sulfate sodium (DSS)-induced colitis mouse model in vivo and RAW264.7 cell in vitro by observing macrophage polarization dynamics. METHODS: The main active components of QCWZD were determined using high-performance liquid chromatography. Surface marker expression on M1-type macrophages was analyzed using flow cytometry and immunofluorescence. The effect on inducible nitric oxide synthase (iNOS), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-alpha) released by M1 type macrophages was determined using ELSA and RT-PCR. The expression of key proteins in the JAK2/STAT3 signaling pathway was analyzed using western blotting. QCWZD cytotoxicity in macrophages was measured using CCK8 and Annexin V-FITC/PI assays. RESULTS: The main active components of QCWZD were berberine chloride, coptisine chloride, Epiberberine chloride, gallic acid, ginsenoside Rg1, ginsenoside Rb1, indigo, indirubin, notoginsenoside R1, palmatine chloride, and 6-curcumin. QCWZD markedly alleviated DSS-induced colitis in mice, as revealed by the rescued weight loss and disease activity index, attenuated the colonic shortening and mucosal injury associated with the inhibition of M1 macrophage polarization and expression of related cytokines, such as IL-6 and TNF-alpha, in vivo and in vitro. Furthermore, QCWZD decreased the iNOS, JAK2, and STAT3 levels in vivo and in vitro, regulating the JAK2/STAT3 signaling pathway. CONCLUSION: QCWZD administration improves intestinal inflammation by inhibiting M1 macrophage polarization. The JAK2/STAT3 signaling pathway may mediate the effects of QCWZD on M1 macrophage polarization in colitis treatment. This study presents a novel macrophage-mediated therapeutic strategy for the treatment of IBD.

Development and Validation of an UPLC-MS/MS Method for Pharmacokinetic Comparison of Five Alkaloids from JinQi Jiangtang Tablets and Its Monarch Drug Coptidis Rhizoma.[Pubmed:29286316]

Pharmaceutics. 2017 Dec 29;10(1):4.

JinQi Jiangtang (JQJT) tablets, a Chinese patent medicine approved by the State Food and Drug Administration, are composed of Coptidis Rhizoma, Astragali Radix, and Lonicerae Japonicae Flos, and have a significant effect on diabetes. Coptidis Rhizoma is monarch drug in the prescription. The aim of the present study was to investigate and compare the pharmacokinetics of multiple ingredients from JQJT tablets and Coptidis Rhizoma extract (CRE) following oral administration in rats. Five alkaloids: coptisine chloride, Epiberberine chloride, berberine chloride, jatrorrhizine chloride, and palmatine chloride, were simultaneously determined in rat plasma using established and validated ultra-high performance liquid chromatography mass spectrometry (UPLC-MS/MS). Significant pharmacokinetic differences were observed for the five alkaloids after a single administration of CRE and JQJT tablets. Compared with CRE, the C(max) values of palmatine chloride and jatrorrhizine chloride were decreased significantly, the AUC(0-t) values of four alkaloids (all except jatrorrhizine chloride) were notably decreased, and the mean residence times of all five alkaloids were significantly decreased after administration of JQJT tablets. The results indicated that the absorption characteristics of the five alkaloids from Coptidis Rhizoma would be influenced by the compatibility of Astragali Radix or Lonicerae Japonicae Flos from JQJT tablets, such that absorption was inhibited and elimination was accelerated. In conclusion, the developed strategy was suitable for the comparison of five alkaloids from JinQi Jiangtang tablets and its monarch drug, which could be valuable for compatibility studies of traditional Chinese medicines.

[Establishment of the control substance of plant drug and fingerprints of Coptis chinensis].[Pubmed:15663220]

Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 2004 Dec;26(6):622-7.

OBJECTIVE: To establish the control substance of plant drug (CSPD) of Coptis chinensis Franch. and its proton nuclear magnetic resonance (1H NMR) and high performance liquid chromatography (HPLC) fingerprints for the purpose of original identification. METHODS: The CSPD and their 1H NMR and HPLC fingerprints of Coptis chinensis were obtained by standardized procedure. Chemical components were isolated from the CSPD by silica gel column chromatography. By elucidation of their structures, the assignments of the characteristic signals in fingerprints could be achieved. RESULTS; The 1H NMR and HPLC fingerprints of the samples from various sources had wonderful reproducibility and characteristic features. Furthermore, five main compounds were isolated from CSPD and their structures were authenticated by spectral analysis as palmatine chloride, berberine chloride, Epiberberine chloride, coptisine chloride, and jatrorrhizine chloride, respectively. The 1H NMR and HPLC fingerprints of the CSPD of Coptis chinensis showed mainly the characteristic signals of the berberine-type compounds isolated in this work. CONCLUSION: The 1H NMR and HPLC fingerprints of the CSPD of Coptis chinensis exhibit the structures and total composition of the main active constituents in it, and can be used for its original identification and quality evaluation.