Aurantiamide (2.5, 5, 10 mg/kg; oral gavage; 3 times, 24 hours apart) improves cognitive impairment in C57BL/6 mice after ischemia/reperfusion (I/R) and cecal ligation and puncture (CLP) in a dose-dependent manner, and inhibits microglial polarization and NLRP3 activation[2].
Aurantiamide (0.5 mg/kg; intraperitoneal injection; once a day, 5 days a week; 4 weeks) significantly reduces mean arterial blood pressure, improves endothelium-dependent vasodilation, upregulates aortic endothelial nitric oxide synthase (eNOS) protein expression and promotes nitric oxide (NO) production in the two-kidney-one-clip (2K-1C) renovascular hypertension model in Sprague-Dawley rats[4].
The metabolic characteristics of Aurantiamide (0.1 mg/kg; oral gavage; single dose) and Aurantiamide acetate (HY-N2905) (0.2 mg/kg; oral gavage; single dose) in rats shows that they have the characteristics of rapid diffusion, wide distribution, and can pass through the blood-brain barrier, with a peak time of 0.5 h. In addition, the decline rate of aurantiamide acetate is faster than that of aurantiamide[5].
| Animal Model: | Male C57BL/6 mice (6-8 weeks old, 20-22 g) + cisplatin-induced, I/R, or CLP-induced acute kidney injury model[1] |
| Dosage: | 2.5, 5, 10 mg/kg (dissolved in 0.5% carboxymethylcellulose + 0.1% Tween 80)
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| Administration: | Oral gavage, three times before the surgery, with a 24 h interval between each administration |
| Result: |
Renal function : Reduced serum creatinine and BUN levels by 30-45% compared to model controls, with the 10 mg/kg dose showing the most pronounced effect.
Histopathology : PAS staining revealed decreased tubular dilation, glycogen deposition, and interstitial fibrosis; immunofluorescence showed reduced KIM1 (renal injury marker) and F4/80+ macrophage infiltration in renal tissues.
Protein expression : Western blot demonstrated dose-dependent inhibition of p-RIPK3, p-MLKL, and p-P65 (NF-κB) in renal lysates, with corresponding reduction in pro-inflammatory cytokines (IL-6, TNF-α) by qPCR.
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| Animal Model: | Male Sprague-Dawley rats (8 weeks old, 230-250 g) + two-kidney one-clip (2K-1C) renovascular hypertension model[4] |
| Dosage: | 0.5 mg/kg (dissolved in DMSO, final concentration 0.1%) |
| Administration: | Intraperitoneal injection, once daily for 5 days/week, total 4 weeks
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| Result: |
Blood pressure : Reduced mean arterial pressure (MAP) by 20-25% compared to hypertensive controls, with significant improvement in endothelium-dependent relaxation to acetylcholine (ACh) and reduced constriction to phenylephrine (Phe).
Vascular function : Organ bath assays showed enhanced ACh-induced vasodilation and attenuated Phe-induced vasoconstriction in aortic rings, correlated with increased eNOS protein expression (1.5-fold by Western blot) and NO production (measured as nitrite/nitrate levels).
Red blood cell deformability : Ektacytometry revealed increased erythrocyte deformability (Elmax) in treated rats, indicating improved blood fluidity and microvascular flow. |
