Vasorelaxant and antihypertensive effects of neferine. - GreenMedInfo Summary
Vasorelaxant and Antihypertensive Effects of Neferine in Rats: An In Vitro and In Vivo Study.
Planta Med. 2020 May ;86(7):496-504. Epub 2020 Mar 27. PMID: 32219782
The present study was performed to examine the antihypertensive effect of neferine in hypertensive rats and its relaxant mechanisms in isolated rat thoracic aorta. The antihypertensive effect was evaluated by tail-cuff methods on N-nitro-L-arginine methyl ester (L-NAME) (40 mg/kg BW) 4-week hypertensive-induced hypertensive rats. The vasorelaxant effect and its mechanisms were studied by the organ bath technique in the thoracic aorta isolated from normotensive rats. The results indicated that the treatment of neferine (1 mg/kg and 10 mg/kg) markedly decreased the systolic blood pressure (SBP) when compared with the hypertension group (137.75 ± 10.14 mmHg and 132.23 ± 9.5 mmHg, respectively, p < 0.001), without affecting the heart rate. Moreover, neferine (10 - 10 M) exhibited concentration-dependent vasorelaxation in endothelium-intact rings (Evalues = 98.95 ± 0.66% and pD = 7.93 ± 0.28) and endothelium-denuded rings (Evalues = 90.61 ± 1.91% and pD = 6.85 ± 0.36). The effects of neferine were reduced by pre-incubation with L-NAME and 1H-[1,2,4]oxadiazolo[4,3-a] quinoxalin-1-one (ODQ) but not with pre-incubation with indomethacin and Kchannel blockers. Neferine attenuated the contractions induced by phenylephrine and caffeine in a Ca-free solution and also inhibited in CaCl- and phenylephrine-induced contracted rings. Our study suggests that neferine exhibited hypertensive potential, induced vasorelaxation through the endothelium nitric oxide synthase (eNOS)/nitric oxide (NO)/soluble guanylyl cyclase (sGC) pathway and involved the modulation of Cainflux through Cachannels and intracellular Carelease from the sarcoplasmic reticulum.