Advanced

Ursolic Acid Inhibits Acid Sphingomyelinase in Intestinal Cells.

Zhang, Ping LU ; Cheng, Yajun LU and Duan, Rui-Dong LU (2012) In Phytotherapy Research
Abstract
Ursolic acid (UA) has antiinflammatory and anticancer effects on mammalian cells. Increase in acid sphingomyelinase (SMase) is associated with several inflammatory diseases including inflammatory bowel diseases. The enzyme has become a target for drug discovery. The present study examined the roles of UA on acid SMase in intestinal cells. We found that UA specifically inhibited acid SMase activity in both human colon cancer Caco-2 cells and rat nontransformed IEC-6 intestinal cells in a dose-dependent manner, with 50% inhibition occurred at 30 μM for Caco-2 cells and less than 20 μM for IEC-6 cells. In comparison with some chemicals known to inhibit acid SMase, UA appeared most effective. The decreased acid SMase activity was not... (More)
Ursolic acid (UA) has antiinflammatory and anticancer effects on mammalian cells. Increase in acid sphingomyelinase (SMase) is associated with several inflammatory diseases including inflammatory bowel diseases. The enzyme has become a target for drug discovery. The present study examined the roles of UA on acid SMase in intestinal cells. We found that UA specifically inhibited acid SMase activity in both human colon cancer Caco-2 cells and rat nontransformed IEC-6 intestinal cells in a dose-dependent manner, with 50% inhibition occurred at 30 μM for Caco-2 cells and less than 20 μM for IEC-6 cells. In comparison with some chemicals known to inhibit acid SMase, UA appeared most effective. The decreased acid SMase activity was not associated with significant accumulation of cellular sphingomyelin but significant increase in phosphatidylcholine, the donor of choline for sphingomyelin synthesis. Western blot analysis showed a decreased enzyme levels in the cells after UA stimulation, but real time quantitative polymerase chain reaction (qPCR) failed to show a parallel reduction of acid SMase mRNA after UA stimulation. Finally, UA had no direct effect on acid SMase activity in cell-free extracts. In conclusion, UA has inhibitory effects on acid SMase synthesis and the effect occurs presumably at posttranslational levels. Copyright © 2012 John Wiley & Sons, Ltd. (Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Phytotherapy Research
publisher
John Wiley & Sons
external identifiers
  • wos:000314581800003
  • pmid:22511398
  • scopus:84873414090
ISSN
1099-1573
DOI
10.1002/ptr.4709
language
English
LU publication?
yes
id
e7c0171c-dcce-4a19-9ba0-1a8d55733dd0 (old id 2519324)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/22511398?dopt=Abstract
date added to LUP
2012-05-06 17:25:15
date last changed
2017-11-05 04:44:03
@article{e7c0171c-dcce-4a19-9ba0-1a8d55733dd0,
  abstract     = {Ursolic acid (UA) has antiinflammatory and anticancer effects on mammalian cells. Increase in acid sphingomyelinase (SMase) is associated with several inflammatory diseases including inflammatory bowel diseases. The enzyme has become a target for drug discovery. The present study examined the roles of UA on acid SMase in intestinal cells. We found that UA specifically inhibited acid SMase activity in both human colon cancer Caco-2 cells and rat nontransformed IEC-6 intestinal cells in a dose-dependent manner, with 50% inhibition occurred at 30 μM for Caco-2 cells and less than 20 μM for IEC-6 cells. In comparison with some chemicals known to inhibit acid SMase, UA appeared most effective. The decreased acid SMase activity was not associated with significant accumulation of cellular sphingomyelin but significant increase in phosphatidylcholine, the donor of choline for sphingomyelin synthesis. Western blot analysis showed a decreased enzyme levels in the cells after UA stimulation, but real time quantitative polymerase chain reaction (qPCR) failed to show a parallel reduction of acid SMase mRNA after UA stimulation. Finally, UA had no direct effect on acid SMase activity in cell-free extracts. In conclusion, UA has inhibitory effects on acid SMase synthesis and the effect occurs presumably at posttranslational levels. Copyright © 2012 John Wiley & Sons, Ltd.},
  author       = {Zhang, Ping and Cheng, Yajun and Duan, Rui-Dong},
  issn         = {1099-1573},
  language     = {eng},
  month        = {04},
  publisher    = {John Wiley & Sons},
  series       = {Phytotherapy Research},
  title        = {Ursolic Acid Inhibits Acid Sphingomyelinase in Intestinal Cells.},
  url          = {http://dx.doi.org/10.1002/ptr.4709},
  year         = {2012},
}