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Molecules-13 December 2019 coptisine
Alkaloids having acetylcholinesterase (AChE) inhibitory activity are commonly found in traditional Chinese medicine (TCM); for example, berberine from Coptis chinensis, galantamine from Lycoris radiata, and huperzine A from Huperzia serrata. In practice of TCM, Stephaniae Tetrandrae Radix (STR) is often combined with Coptidis Rhizoma (CR) or Phellodendri Chinensis Cortex (PCC) as paired herbs during clinical application. Fangchinoline from STR and coptisine and/or berberine from CR and/or PCC are active alkaloids in inhibiting AChE. The traditional usage of paired herbs suggests the synergistic effect of fangchinoline–coptisine or fangchinoline–berberine pairing in AChE inhibition. HPLC was applied to identify the main components in herbal extracts of STR, CR, and PCC, and the AChE inhibition of their main components was determined by Ellman assay. The synergism of herb combination and active component combination was calculated by median-effect principle. Molecular docking was applied to investigate the underlying binding mechanisms of the active components with the AChE protein. It was found that fangchinoline showed AChE inhibitory potency; furthermore, fangchinoline–coptisine/berberine pairs (at ratios of 1:5, 1:2, 1:1, and 2:1) synergistically inhibited AChE; the combination index (CI) at different ratios was less than one when Fa = 0.5, suggesting synergistic inhibition of AChE. Furthermore, the molecular docking simulation supported this enzymatic inhibition. Therefore, fangchinoline–coptisine/berberine pairs, or their parental herbal mixtures, may potentially be developed as a possible therapeutic strategy for Alzheimer’s patients.Keywords: acetylcholinesterase; fangchinoline; coptisine; berberine; synergistic effect
......coptisine (Lot DST170711-003,purity 99%) and epiberberine (Lot DST170711-109, purity 99%) were purchased from from Chengdu Desite Biological Technology Co. Ltd. (Sichuan, China).
原文地址：https://www.mdpi.com/1420-3049/24/24/4567
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Hindawi -Dec18th 2020
Corydalis Rhizoma (CR) is a commonly used traditional Chinese medicine for its potency in activating blood circulation and analgesia. In clinic, CR extracts or components are commonly used in the treatment of myocardial ischemia, rheumatism, and dysmenorrhea with different types of inflammation. However, due to different mechanism of pain and inflammation, the anti-inflammatory property of CR has not been fully revealed. Here, the major chromatographic peaks of CR extracts in different extracting solvents were identified, and the anti-inflammatory activities of CR extracts and its major alkaloids were evaluated in LPS-treated macrophages by determining expressions of proinflammatory cytokines, IκBα and NF-κB. The most abundant alkaloid in CR extract was dehydrocorydaline, having >50% of total alkaloids. Besides, the anti-inflammatory activities of dehydrocorydaline and its related analogues were demonstrated. The anti-inflammatory roles were revealed in LPS-treated cultured macrophages, including (i) inhibiting proinflammatory cytokines release, for example, TNF-α, IL-6; (ii) suppressing mRNA expressions of proinflammatory cytokines; (iii) promoting IκBα expression and suppressing activation of NF-κB transcriptional element; and (iv) reducing the nuclear translocation of NF-κB. The results supported that dehydrocorydaline was the major alkaloid in CR extract, which, together with its analogous, accounted the anti-inflammatory property of CR.
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Columbamine (Lot DST190528-009, purity 99%), coptisine (Lot DST170711-003, purity 99%), glaucine (Lot DST190720-176, purity 99%), dehydrocorydaline (Lot DST190422-025, purity 99%), rotundinum (Lot DST190718-331, purity 99%), canadine (Lot DST180127-065, purity 99%), corydaline (Lot DST190701-102, purity 99%), stylopine (Lot DST180127-158, purity 99%), allocryptopine (Lot DST190322-091, purity 99%), corydalmine (Lot DST190602-726, purity 99%), and isocorypalmine (Lot DST190612-157, purity 99%) were purchased from Chengdu DeSiTe Biological Technology (Chengdu, China).was purchased from Chengdu DeSiTe Biological Technology Co., Ltd. (Sichuan, China)
原文链接：https://doi.org/10.1155/2020/4181696
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