Isolation of betulinic acid, its methyl ester and guaiane sesquiterpenoids with protein tyrosine phosphatase 1B inhibitory activity from the roots of Saussurea lappa C.B.Clarke.
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.
Choi
Ji Young
JY
College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongbuk 712-749, Korea.
Na
Minkyun
M
Hyun Hwang
In
I
Ho Lee
Seung
S
Young Bae
Eun
E
Yeon Kim
Bo
B
Seog Ahn
Jong
J
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D053978:Pentacyclic Triterpenes; D018517:Plant Roots / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D030441:Saussurea / Q000737:chemistry*; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D045789:Sesquiterpenes, Guaiane / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000094062:Betulinic Acid
D004791:Enzyme Inhibitors; D007783:Lactones; D053978:Pentacyclic Triterpenes; D012717:Sesquiterpenes; D045789:Sesquiterpenes, Guaiane; D014315:Triterpenes; C534740:betulinic acid methyl ester; C097581:mokko lactone; C083030:dehydrocostus lactone; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D015107:4-Butyrolactone; D000094062:Betulinic Acid