Uses
Angiotensin-converting enzyme 2 (ACE2) is an enzyme that is cardioprotective and renoprotective. Resorcinolnaphthalein increases the activity of ACE2 in vitro (EC50 = 19.5 μM). Activation of ACE2 in rats produces a decrease in blood pressure and improvement in cardiac function. In spontaneously hypertensive rats it produces a reversal of myocardial, perivascular, and renal fibrosis.[Cayman Chemical]
Biological Activity
resorcinolnaphthalein is an angiotensin-converting enzyme 2 (ace2) activator [1].angiotensin-converting enzyme 2 (ace2) has been involved in hydrolyzing angiotensin ii and opposing its actions, and plays a protective role in the pathogenesis of pulmonary arterial hypertension (pah) [2]. targeted disruption of ace2 in mice results in a severe cardiac contractility defect, increased angiotensin ii levels, and upregulation of hypoxia-induced genes in the heart [2].
in vitro
resorcinolnaphthalein enhanced ace2 activity in a dose-dependent manner [1].
in vivo
resorcinolnaphthalein caused significant activation of ace2 in both normal and diseased rats in 7 days after treatment. treatment with resorcinolnaphthalein prevented high pap, right ventricular hypertrophy and neointimal formation. resorcinolnaphthalein caused an improved endothelia-dependent vasorelaxation and decreased in proinflammatory cytokines, such as tnf-α, mcp-1, il-6, and increased in anti-inflammatory cytokine il-10 in the early stage of the pathogenesis [3]. resorcinolnaphthalein can specifically and effectively enhanced ace2 activity in rats [4]. ace2 activation by resorcinolnaphthalein showed effects on pulmonary endothelial dysfunction and neointimal formation during the development of severe pah in rats [4].
References
[1] prada j a h, ferreira a j, katovich m j, et al. structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents[j]. hypertension, 2008, 51(5): 1312-1317.
[2] crackower m a, sarao r, oudit g y, et al. angiotensin-converting enzyme 2 is an essential regulator of heart function[j]. nature, 2002, 417(6891): 822-828.
[3] haber p k, ye m, wysocki j, et al. angiotensin-converting enzyme 2–independent action of presumed angiotensin-converting enzyme 2 activatorsnovelty and significance[j]. hypertension, 2014, 63(4): 774-782.
[4] li g, liu y, zhu y, et al. ace2 activation confers endothelial protection and attenuates neointimal lesions in prevention of severe pulmonary arterial hypertension in rats[j]. lung, 2013, 191(4): 327-336.
