A new bioactive steroidal ketone from the South China Sea sponge Xestospongia testudinaria.
A new steroidal ketone (1), with an ergosta-22,25-diene side chain, was obtained from the South China Sea marine sponge Xestospongia testudinaria. The structure of 1 was determined on the basis of detailed spectroscopic analysis and by comparison with literature. Compound 1 exhibited significant inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), a key target for the treatment of type II diabetes and obesity, with an IC50 value of 4.27 ± 0.55 μM, which is comparable with the positive control oleanolic acid (IC50 = 2.63 ± 0.22 μM).
a School of Pharmaceutical Sciences, Wenzhou Medical University , Wenzhou 325035 , China.|b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Wen-Fei
WF
He
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Duo-Qing
DQ
Xue
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Li-Gong
LG
Yao
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Jia
J
Li
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Hai-Li
HL
Liu
b State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203 , China.
Yue-Wei
YW
Guo
D000818:Animals; D002777:Cholestanols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D003924:Diabetes Mellitus, Type 2; D007659:Ketones; D015394:Molecular Structure; D009792:Oceans and Seas; D009828:Oleanolic Acid; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors; D013256:Steroids; D047131:Xestospongia / Q000737:chemistry*
C000608636:(22E,24S)-24-methylcholesta-4,7,22,25-tetraene-3-one; D002777:Cholestanols; D007659:Ketones; D013256:Steroids; D009828:Oleanolic Acid; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
PTP1B inhibitory activity; Petrosiidae; Xestospongia testudinaria; sponge; steroidal ketone