Echinacoside Elicits Endothelium-Dependent Relaxation in Rat Aortic Rings via an NO-cGMP Pathway

Abstract

The aim of this study was to identify and elucidate the vasorelaxant activity of echinacoside, a phenylethanoid glycoside isolated from the medicinal herb Cistanche tubulosa, and its possible underlying mechanism on isolated rat thoracic aortic rings pre-contracted with phenylephrine (PE, 1 microM) and KCl (60 mM). Echinacoside (30-300 microM) exhibited an acute relaxation in endothelium-intact rings in a concentration-dependent manner, while this relaxation was significantly inhibited in endothelium-denuded condition and in the presence of the endothelial nitric oxide synthase (eNOS) inhibitor, N(W)-nitro-L-arginine methyl ester (L-NNA, 100 microM), an unselective soluble guanylate cyclase blocker, methylene blue (10 microM), the selective sGC inhibitor 1 H-[1, 2, 4]oxadiazolo[4,3- A]quinoxalin-1-one (ODQ, 1 microM); in addition, atropine (1 microM), a selective muscarinic receptor antagonist, partially affected the relaxation. However, the cyclooxygenase inhibitor indomethacin (5 microM) had no influence on the action. Echinacoside enhanced the cyclic guanosine monophosphate (cGMP) production in aortic rings contracted with PE. These results indicate for the first time that echinacoside mediates the endothelium-dependent vasodilator action in rat thoracic aortic rings through nitric oxide (NO)-cGMP pathway.

The longevity effect of echinacoside inCaenorhabditis elegansmediated throughdaf-16

“…8,[42][43][44] Echinacoside (ECH) is one such natural polyphenol that is known to possess various important of pharmacological activities including antioxidative, antiinflammatory, neuroprotective, hepatoprotective, and nitric oxide radical-scavenging properties. 3,4) However, to the best of our knowledge, there have been no published in vivo studies addressing its effects on promoting longevity.…”

“…1,2) It has been reported that ECH possess an array of important pharmacological properties such as antioxidative, antiinflammatory, neuroprotective, hepatoprotective, and nitric oxide radical-scavenging activities. 3,4) However, whether ECH can affect longevity in vivo and what are the underlying molecular mechanisms associated with its anti-aging property have not been rigorously tested.…”

Echinacoside induces rat pulmonary artery vasorelaxation by opening the NO-cGMP-PKG-BKCa channels and reducing intracellular Ca2+ levels

“…In rat PASMCs, ECH could reduce intracellular calcium concentration directly. Previous studies have also suggested that ECH could mediate the endothelium-dependent vasodilator action in rat thoracic aortic rings through the NO-cGMP pathway [7] .…”

“…ECH has various desirable pharmacological characteristics, such as antioxidative, anti-inflammatory, neuroprotective, hepatoprotective, and nitric oxide (NO) radical-scavenging properties [6] . It can also elicit endothelium-dependent relaxation in rat thoracic aortic rings and cure cardiovascular diseases [7] . HowEchinacoside induces rat pulmonary artery vasorelaxation by opening the NO-cGMP-PKG-BK Ca channels and reducing intracellular Ca 2+ levels Aim: Sustained pulmonary vasoconstriction as experienced at high altitude can lead to pulmonary hypertension (PH).…”

Phenylethanoid Glycosides: Research Advances in Their Phytochemistry, Pharmacological Activity and Pharmacokinetics

“…In another study, compound 121 appeared an inhibitory effect on DHT-induced secretion of both free and total prostate-specific antigen at all tested concentration in an in vitro model of human prostate epithelium [108]. He et al studied the vasorelaxant activity of 117 and the results highlighted that 117 could evoke a significant endothelium-dependent vasorelaxation action mediated through the NO-cGMP pathway in an isolated rat thoracic aorta ring [109].…”