| Summary: | 碩士 === 國立高雄大學 === 生命科學系碩士班 === 108 === Saussurea costus belonging to the asteraceae family is a perennial herb. It is reported to have been used to treat many ailments such as ulcer, cancer, inflammatory and liver disease. The purpose of this study is looking for the new compounds from the roots of S. costus. Chromatographic separation of the EtOAc extract of S. costus using column and HPLC resulted in the purification of four new sesquiterpenoids, designated as saucostunoids F–I (1–4) and eleven known sesquiterpenoids,4α-hydroxyeudesm-11-en-12-
al (5), 7α,12-dihydroxy-eudesm-4(15),11(13)-diene (6), ilicic acid (7), 6α-hydroxycostic acid methyl ester (8), arbusculin E methyl ester (9), 4α-methoxy-6α-hydroxycostic acid methyl ester (10), magnolialide (11), santamarine (12), reynosin (13),1,4-epoxyeudesman-
olid (14) and costunolide (15). Structural modifications of costunolide were reacted by allylic oxidation and Michael addition. The purpose of this study explored the change of the oxidation state and α-methylene-γ-lactone for the anti-breast cancer activity. This investigation led to the isolation of five new compounds 15d and 15f‒15i and four known compounds 15a‒15c and 15e. The structures of these isolated compounds and their derivatives were elucidated by a combination of NMR, MS, IR and UV-vis data and by comparison with reported data in literatures. The in vitro anti-triple negative breast cancer (MDA-MB-231) activities of compounds 1‒15 and derivatives 15a‒15i were evaluated. Compounds 1, 13, 15a and 15b showed significant inhibition against MDA-MB-231 with IC50 values of 20.80, 20.66, 13.25 and 9.28 μM, respectively. The results of these derivatives showed that α-methylene-γ-lactone is a active functional group.
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