Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU), Varanasi, 221005, India.
Inflammopharmacology. 2018 Jun;26(3):769-778. doi: 10.1007/s10787-017-0411-7. Epub 2017 Dec 2.
The present study was designed to explore the anti-inflammatory activity of an anti-platelet agent crinumin, by various in vitro and in vivo inflammation models. Firstly, crinumin protein was purified through cation exchange chromatography; then, in vitro activity was estimated by albumin denaturation assay and HRBC membrane stabilization assay. Carrageenan-induced paw oedema and cotton pellet-induced granuloma models were used for in vivo anti-inflammatory activity assessment in rats. In both models, rats were pre-treated for 7 days with crinumin (25-50 µg/ml) and diclofenac sodium (50 µg/ml). Expression of P-selectin (in serum and plasma) through ELISA and NF-κB (in paw and granulomatous tissues) through western blotting was checked. Our results showed that crinumin at both doses (25 or 50 µg/kg of b.w.) significantly (p < 0.05) reduced the paw oedema formation in a dose-dependent manner in the second phase of inflammation and significant (p < 0.05) reduction of wet and dry weight of granuloma was observed indicating the anti-inflammatory potential of crinumin. Crinumin decreased the expression of P-selectin and NF-κB indicating its potential role in decreasing platelet activation and healing inflammation. Histopathological studies additionally proved the efficacy of drug in treating inflammation. The results of the study suggest that the crinumin might have an inhibitory role in atherosclerosis as platelet aggregation and inflammation are the key processes involved in atherosclerotic disorders.
本研究旨在通过各种体外和体内炎症模型探索抗血小板药物 crinumin 的抗炎活性。首先,通过阳离子交换层析纯化 crinumin 蛋白;然后,通过白蛋白变性测定法和 HRBC 膜稳定测定法评估体外活性。在大鼠中使用角叉菜胶诱导的足肿胀和棉籽球诱导的肉芽肿模型评估体内抗炎活性。在这两种模型中,大鼠用 crinumin(25-50μg/ml)和双氯芬酸钠(50μg/ml)预处理 7 天。通过 ELISA 检查血清和血浆中 P-选择素(in serum and plasma)的表达,通过 Western blot 检查 paw 和肉芽肿组织中的 NF-κB(in paw and granulomatous tissues)的表达。我们的结果表明,crinumin 在两种剂量(25 或 50μg/kg 的 b.w.)下均显著(p<0.05)降低了炎症第二期的足肿胀形成,并且观察到肉芽肿的湿重和干重显著(p<0.05)减少,表明 crinumin 具有抗炎潜力。Crinumin 降低了 P-选择素和 NF-κB 的表达,表明其在降低血小板活化和炎症愈合方面的潜在作用。组织病理学研究进一步证明了药物治疗炎症的功效。研究结果表明,crinumin 可能在动脉粥样硬化中具有抑制作用,因为血小板聚集和炎症是动脉粥样硬化紊乱中涉及的关键过程。