Isolation of Betulinic Acid, its Methyl Ester and Guaiane Sesquiterpenoids with Protein Tyrosine Phosphatase 1B Inhibitory Activity from the Roots of Saussurea lappa CBClarke

被引:63
作者
Choi, Ji Young [1 ]
Na, MinKyun [1 ]
Hwang, In Hyun [1 ]
Lee, Seung Ho [1 ]
Bae, Eun Young [2 ]
Kim, Bo Yeon [2 ]
Ahn, Jong Seog [2 ]
机构
[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, Gyeongbuk, South Korea
[2] Korea Res Inst Biosci & Biotechnol KRIBB, Taejon 305806, South Korea
关键词
Protein tyrosine phosphatase 1B; Saussurea lappa CBClarke; Betulinic acid; Betulinic acid methyl ester; Mokko lactone; Dehydrocostuslactone; COSTUNOLIDE; DERIVATIVES; RADIX;
D O I
10.3390/molecules14010266
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Activity-guided fractionation of a MeOH extract of the roots of Saussurea lappa C.B.Clarke (Compositae), using an in vitro protein tyrosine phosphatase 1B (PTP1B) inhibition assay, led to the isolation of four active constituents: betulinic acid (1), betulinic acid methyl ester (2), mokko lactone (3) and dehydrocostuslactone (4), along with nine inactive compounds. Our findings indicate that betulinic acid (1) and its methyl ester 2, as well as the two guaiane sesquiterpenoids 3 and 4 are potential lead moieties for the development of new PTP1B inhibitors.
引用
收藏
页码:266 / 272
页数:7
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