Abstract
Heliopsis longipes roots have been widely used in Mexican traditional medicine to relieve pain, mainly, toothaches. Previous studies have shown that affinin, the major alkamide of these roots, induces potent antinociceptive and anti-inflammatory activities. However, the effect of H. longipes root extracts and affinin on the cardiovascular system have not been investigated so far. In the present study, we demonstrated that the dichloromethane and ethanolic extracts of H. longipes roots, and affinin, isolated from these roots, produce a concentration-dependent vasodilation of rat aorta. Affinin-induced vasorelaxation was partly dependent on the presence of endothelium and was significantly blocked in the presence of inhibitors of NO, H2S, and CO synthesis (NG-nitro-l-arginine methyl ester (l-NAME), dl-propargylglycine (PAG), and chromium mesoporphyrin (CrMP), respectively); K+ channel blockers (glibenclamide (Gli) and tetraethyl ammonium (TEA)), and guanylate cyclase and cyclooxygenase inhibitors (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) and indomethacin (INDO), respectively). Our results demonstrate, for the first time, that affinin induces vasodilation by mechanisms that involve gasotransmitters, and prostacyclin signaling pathways. These findings indicate that this natural alkamide has therapeutic potential in the treatment of cardiovascular diseases.
Highlights
Several pharmacological studies have demonstrated that affinin displays analgesic (ED50 = 1 mg/kg intraperitoneal (i.p.) in mice) [5,16], antinociceptive (ED50 = 6.98 mg/kg per os (p.o.); ED50 = 36 ± 5 mg/kg i.p. in mice) [6,26], anti-inflammatory (90–180 μM in macrophage cell line) [18], anxiolytic (3–30 mg/kg i.p. in mice) [6], and diuretic (800 mg/kg p.o. in mice) [27] properties
Phytochemical Study of the Dichloromethane Extract Obtained from H. longipes Roots and Isolation of Affinin
Our results indicated that affinin is able to activate the nitric oxide (NO)/cGMP, carbon monoxide (CO)/cGMP, H2S/KATP, and PGI2/cAMP signaling pathways, and considering that the triggering of these four signaling pInat.thJ.wMaoly
Summary
Several pharmacological studies have demonstrated that affinin displays analgesic (ED50 = 1 mg/kg intraperitoneal (i.p.) in mice) [5,16], antinociceptive (ED50 = 6.98 mg/kg per os (p.o.); ED50 = 36 ± 5 mg/kg i.p. in mice) [6,26], anti-inflammatory (90–180 μM in macrophage cell line) [18], anxiolytic (3–30 mg/kg i.p. in mice) [6], and diuretic (800 mg/kg p.o. in mice) [27] properties Some of these pharmacological activities have been reported for crude organic extracts of H. longipes roots [5,6,26,28,29,30,31]
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