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Synthesis, Purification, and Selective β2-AR Agonist and Bronchodilatory Effects of Catecholic Tetrahydroisoquinolines from Portulaca oleracea

J Nat Prod. 2019; 
Yang EL, Sun B, Huang ZY, Lin JG, Jiao B, Xiang L.
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Stable Cell Line Development Services This assay was performed according to the protocols of Nanjing GenScript Co.... oleracea (Figure 1) were screened for their β 1-, β 2-, and α 1B-AR agonist activities, at the concentration of 100 μM, according to intracellular calcium fluorescence changes in CHO-K1/Gα15/ADRB1 (Gen- Script, M00269), CHO-K1/Gα15/ADRB2 (GenScript, M00308), and CHO-K1/Gα15/ADRA1B (GenScript, M00260) cell lines that consistently express β 1-, β 2-, and α 1B-AR. Get A Quote

摘要

A green, biomimetic, phosphate-mediated Pictet-Spengler reaction was used in the synthesis of three catecholic tetrahydroisoquinolines, 1, 2, and 12, present in the medicinal plant Portulaca oleracea, as well as their analogues 3-11, 13, and 14, with dopamine hydrochloride and aldehydes as the substrates. AB-8 macroporous resin column chromatography was applied for purification of the products from the one-step high-efficacy synthesis. It eliminated the difficulties in the isolation of catecholic tetrahydroisoquinolines from the aqueous reaction system and unreacted dopamine hydrochloride. Activity screening in CHO-K1/Gα15 cell models consistently expressing α1B-, β1-, or β2-adrenergic receptors indicated t... More

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