New prenylated flavanones from Erythrina abyssinica with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity.
As the insulin and leptin signaling pathway can be regulated by PTP1B, it has been suggested that compounds that reduce PTP1B activity or expression levels can be used for treating type 2 diabetes and obesity. In the course of our screening efforts on new PTP1B inhibitors, six new flavanones ( 1- 6) with dihydrofuran moiety and two known flavanones ( 7 and 8) were isolated from the stem bark of Erythrina abyssinica (Leguminosae). Their structures were elucidated on the basis of spectroscopic (including UV, CD, MS, 1D, and 2D NMR) and physicochemical analyses. With the exception of 3 and 5, the compounds inhibited PTP1B activity in an IN VITRO assay with IC (50) values ranging from 15.2 +/- 1.2 to 19.6 +/- 2.3 microM, whereas RK-682 as a positive control displayed an IC (50) value of 4.7 +/- 0.5 microM.
Cui
Long
L
Korea Research Institute of Bioscience and Biotechnology (KRIBB), Daejeon, Korea.
Lee
Hyun Sun
HS
Ndinteh
Derek Tantoh
DT
Mbafor
Joseph Tanyi
JT
Kim
Young Ho
YH
Le
Thi Van
TV
Nguyen
Phi Hung
PH
Oh
Won Keun
WK
D004353:Drug Evaluation, Preclinical; D004895:Erythrina / Q000737:chemistry*; D044950:Flavanones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*
D044950:Flavanones; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1