AIM: To investigate the inhibition of endothelium-dependent in vitro vascul
ar relaxation induced by the total saponins (gensenosides) from Panax notog
inseng (PNS) and the effect of PNS on the cytosolic Ca2+ concentration on c
ultured bovine pulmonary artery endothelial cells. METHODS: The endothelial
-dependent vascular relaxation was assessed using acetylcholine (ACh) or cy
clopiazonic acid (CPA) induced relaxation in endothelium-intact mt aorta. C
ytosolic Ca2+ level was assessed in real time using dynamic digital fluores
cence ratio imaging. RESULTS: In addition to its direct relaxation of the s
mooth muscle cells at high concentrations, PNS, at 100 mg/L having little e
ffect on smooth muscle, caused a marked inhibition of endothelium-dependent
relaxation brought about by PNS. This inhibitory effect was due to its inh
ibition of elevation of cytosolic Ca2+, which is required for the activatio
n of NO generation and release from the vascular endothelial cells. Nifedip
ine has no effect on either the endothelium-dependent relaxation or the cyt
osolic Ca2+ level in the cultured endothelial cells. CONCLUSION: Our findin
gs are consistent with the known action of PNS on receptor-operated Ca2+ ch
annels and support our contention that PNS inhibits endothelium-dependent r
elaxation by preventing the increase of Ca2+ level in endothelial cells via
the receptor-operated Ca2+ channels in the presence of ACh or the non-sele
ctive cation channels opened by CPA.