CAS: 96087-21-7; 6,7,12B,13-Tetrahydro-4H-[1,3]Dioxolo[4',5':7,8]Isoquinolino[3,2-A][1,3]Dioxolo[4,5-G]Isoquinoline Hydrochloride

📜盐酸小檗碱置于platinum(Iv) Oxide 氢气,三溴化硼,溶剂黄146,Cesium Fluoride体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,20.0~95.0 °C,405.3 Kpa 条件下,反应 36.0H,反应生成 盐酸人血草碱
参考文献:Cytotoxicity Evaluation Of Natural Coptisine And Synthesis Of Coptisine From Berberine
标题:Cytotoxicity Evaluation Of Natural Coptisine And Synthesis Of Coptisine From Berberine
摘要:The Crude Extract (80% Meoh In Water) Of Chelidonii Herba Exhibited Very Interesting Cytotoxicity Against Brine Shrimp (Artemia Salina Leach) Nauplii And Cultured Human Tumour Cell In Vitro,The Colon Carcinoma Ht 29 (144 H Treatment). Fractionation Of The Crude Extract And Bioassay-Guided Procedures Showed That The Cytotoxic And,The Antitumour Activities. Were Concentrated In The Basic Extract. On The Basis Of Ir,Ms And H-1 NMR The Compound Responsible Of The Cytotoxic Activity Was Determined To Be Coptisine. Cytotoxicity Evaluation Of-Coptisine Was Next Extended To-A Panel Of Human And Murine Cell Lines In Comparison With The Established Antitumour Drugs Mitoxantrone,Doxorubicin (D. X) And Cisplatin. (Cddp). Coptisine Was Cytotoxic On Lovo And Ht 29 And Less Potent On L-1210,And It Was Partially Crossresistant On The Human Tumour Colon Cell Line Resistant To Dx,Lovo/dx,Whereas It Was Not Significantly Crossresistant On The Murine Leukaemia Cell Line Resistant To. Cd. Dp,L-1210/cddp. Coptisine Alkaloid Was Then Synthesised In Gram Amount From Commercial Berberine. A Four-Step Synthetic Route Was Elaborated. The Overall Yield Was About 8-10%. The Structural Identity Of Synthetic Coptisine Was Verified By Ir And NMR Methods. A Comparison Of The Cytotoxic Effects On The Human Tumour Colon Cell Line Lovo And On The Murine Leukaemia L1210 Showed,For Both Natural And Synthetic Coptisines,A Comparable Cytotoxic Activity More Evident Against-Ht 29 Cell Line And Lovo. Cell Line,While The Activity Was Lower Against The L1210 Cell Line. (C) 2001 Editions Scientifiques Et Medicales. Elsevier Sas.
DOI:10.1016/s0014-827X(01)01121-1