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New Eremophilane Sesquiterpenes from the Roots of Ligularia fischeri

✍ Scribed by Meicai Deng; Weiwei Dong; Wei Jiao; Runhua Lu

Publisher
John Wiley and Sons
Year
2009
Tongue
German
Weight
189 KB
Volume
92
Category
Article
ISSN
0018-019X

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✦ Synopsis

Abstract

magnified image

New eremophilane sesquiterpenes, (3__β__,6__β__,8__α__,10__β__)‐3‐acetyl‐6,8,10‐trihydroxyeremophil‐7(11)‐eno‐12,8‐lactone (1), (3__β__,6__β__,8__β__,10__β__)‐3‐acetyl‐8,10‐dihydroxy‐6‐(2‐methyl‐1‐oxobutoxy) eremophil‐7(11)‐eno‐12,8‐lactone (2), (3__β__,6__β__,10__β__)‐ and (3__β__,6__β__,10__α__)‐3‐acetyl‐6,10‐dihydroxyeremophila‐7(11),8‐dieno‐12,8‐lactone (3 and 4, resp.), and a dinoreremophilane derivative, (3a__R__,4__R__,5__S__,7a__S__)‐2‐acetyl‐3a,4,5,6,7,7a‐hexahydro‐7a‐hydroxy‐1__H__‐inden‐5‐yl acetate (5), were isolated from the roots of Ligularia fischeri. Their structures were elucidated by spectroscopic methods including 1D and 2D NMR spectra, and the structure of 1 was further confirmed by a single‐crystal X‐ray diffraction experiment. Among the isolated compounds, lactone 1 exhibited inhibitory activity towards PTP1B with an IC~50~ value of 1.34 μM in vivo. The other compounds were inactive.

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