分離自中藥遠志之具有正腎上腺素轉運子抑制活性之化合物   全文下載

Norepinephrine Transporter Inhibitors from Polygala tenuifolia

本論文使用正腎上腺素轉運子結合分析指引化合物分離及純化，自中藥遠志水抽物之具有正腎上腺素轉運子抑制活性之分劃層分離出兩個活性皂素polygalasaponin XXvIII (1) 和3-O-β-D-glucopyranosyl presenegenin 28-[O-β-D-galatopyranosyl（1 → 4）-β-D-xylopyranosyl-（1 → 4）-α-L-rhamnopyranosyl（1 → 2）-β-D-fucopyranosyl] ester (2)；五個xanthone 醣?分別為neolancerin (3)、polygalaxanthone IX (4)、sibiricaxanthone (5)、polygalaxanthone III (6) 和 7-O-methylmangiferin (7)；五個酚性醣?分別為tenuifoliside A (8)、sibiricoses A3 (9)、A5 (10)、A6 (11) 及 3’,6-disinapoyl sucrose (12)；一三?類化合物，tenuifolin (13)；以及methyl sinapoate (14) 和腺?(15)。上述化合物均藉由一維及二維核磁共振光譜和質譜分析確認其構造。其中化合物1 和2顯示在4.53、3.95 μM 濃度下可以透過阻斷正腎上腺素轉運子抑制正腎上腺素再吸收，其抑制率分別為77% 和28%。"

Using norepinephrine transporter binding assay-directed fractionation, polygalasaponin XXVIII (1) and 3-O-β-D-glucopyranosyl presenegenin 28-[O-β-D-galatopyranosyl(1→4)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl(1→2)-β-D-fucopyranosyl] ester (2), together with five xanthone glycosides, neolancerin (3), polygalaxanthone IX (4), sibiricaxanthone (5), polygalaxanthone III (6), and 7-O-methylmangiferin (7), five phenolic glycosides, tenuifoliside A (8), sibiricoses A3 (9), A5 (10), A6 (11) and 3’,6-disinapoyl sucrose (12), a triterpenoid, tenuifolin (13), methyl sinapoate (14), and adenosine (15) were isolated from the active fraction of an aqueous extract of the roots of Polygala tenuifolia. Their structures were elucidated by extensive NMR and mass spectroscopic analyses. Compounds 1 and 2 were shown to inhibit norepinephrine reuptake through blocking norepinephrine transport by 77% and 28% in the norepinephrine transporter binding assay at concentrations of 4.53 μM and 3.95 μM, respectively.