OBJECTIVETo observe the effect of 2-methoxycinnamaldehyde (isolated from fraction A of Guizhi Tang) on activity of COX and PGE2 release in rat cerebral microvascular endothelial cells (rCMEC) stimulated by IL-1.

METHODrCMEC were cultured, and identified by immunohistochemistry for von Willebrand factor (VIII factor, a marker for all endothelial cells) in cytoplasm of the cells. Different concentrations of 2-methoxycinnamaldehyde were added respectively and incubated for 3 hours, then stimulated for another 12 hours by IL-1. Activities of COX-1 and COX-2 in rCMEC, and production of PGE2 in the conditioned media were measured by ELISA.

RESULTPositive immunostaining for VIII factor was present diffusely in the cytoplasm of > 90% rCMEC. After being exposed to 30 ng x mL(-1) IL, the activity of COX-2 in rCMEC and the production of PGE2 in conditioned media were higher than those of control group, while there was no difference on activity of COX-1 in the two groups. 2-methoxycinnamaldehyde could down-regulate them in concentration-dependently, and significant differences on the activity of COX-2 and amount of PGE2 were showed in 200 microg x mL(-1) concentration.

CONCLUSION2-methoxycinnamaldehyde can affect the PGE2 release in rCMEC induced by IL-1, which might be related with its inhibition on the activity of COX-2.

Acrolein ; administration & dosage ; analogs & derivatives ; isolation & purification ; pharmacology ; Animals ; Brain ; blood supply ; Cells, Cultured ; Cyclooxygenase 1 ; metabolism ; Cyclooxygenase 2 ; metabolism ; Dinoprostone ; metabolism ; Dose-Response Relationship, Drug ; Drug Combinations ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Endothelial Cells ; cytology ; metabolism ; Interleukin-1 ; antagonists & inhibitors ; Male ; Microcirculation ; cytology ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley

As antibiotic drug resistance has become one of the most serious threats to global public health, there is a pressing need to look for new effective therapeutic drugs. Flavonoids are a large class of chemicals widely exist in plants, and have such effects as direct antibiotics, synergistic antibiotics and inhibition of bacterial activity. In this article, we made a summary for the advance in studies on the antibacterial effects of flavonoids and their mechanism.
Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Bacteria ; drug effects ; Drug Synergism ; Flavonoids ; chemistry ; pharmacology ; Humans