Vijayarani K Reeta, Govindarajulu Manoj, Ramesh Sindhu, Alturki Mansour, Majrashi Mohammed, Fujihashi Ayaka, Almaghrabi Mohammed, Kirubakaran N, Ren Jun, Babu R Jayachandra, Smith Forrest, Moore Timothy, Dhanasekaran Muralikrishnan
Department of Pharmaceutics, Periyar College of Pharmaceutical Sciences, Tiruchirappalli, India.
Department of Drug Discovery and Development, Harrison School of Pharmacy, Auburn University, Auburn, AL, United States.
Front Pharmacol. 2020 Dec 15;11:551911. doi: 10.3389/fphar.2020.551911. eCollection 2020.
Chronic inflammation is a key culprit factor in the onset and progression of several diseases. Novel and pharmacologically effective therapeutic approaches are needed for new treatment remedy or improved pharmacokinetics and pharmacodynamics for existing synthetic drugs, in particular natural products. Boswellic acids are well-known natural products, with capacity to effectively retard inflammation without severe adverse effects. However, the therapeutic use of Boswellic acids are greatly hindered by its poor pharmacokinetic properties. Co-administration strategies that facilitate the oral absorption and distribution of Boswellic acids should lead to a safe and more effective use of this product prophylactically and therapeutically in inflammatory disorders. In this study, we examined the effect of extract on the absorption and bioavailability of Boswellic acid in rabbits. In addition, we further explored computational pharmacodynamic interactions between and Boswellic acid. extract at 2.5 and 10 mg/kg, increased the bioavailability of Boswellic acid ( < 0.05). Based on our drug-based computational modeling, cytochrome P450 (CYP450)-mediated mechanism was involved in increased bioavailability. These findings confirmed that with Boswellic acid may be administered orally together for effective therapeutic efficacy. Thus, our studies support the application of with Boswellic acid as a novel therapeutic avenue in diseases associated with inflammation.
慢性炎症是多种疾病发生和发展的关键致病因素。对于新的治疗方法或改善现有合成药物(特别是天然产物)的药代动力学和药效学,需要新颖且具有药理活性的治疗方法。乳香酸是著名的天然产物,具有有效减轻炎症且无严重不良反应的能力。然而,乳香酸的治疗应用因其较差的药代动力学性质而受到极大阻碍。促进乳香酸口服吸收和分布的联合给药策略应能使其在炎症性疾病的预防和治疗中更安全、有效地使用。在本研究中,我们研究了[提取物名称]提取物对兔体内乳香酸吸收和生物利用度的影响。此外,我们还进一步探讨了[提取物名称]与乳香酸之间的计算药效学相互作用。2.5毫克/千克和10毫克/千克的[提取物名称]提取物提高了乳香酸的生物利用度(P<0.05)。基于我们的药物计算模型,细胞色素P450(CYP450)介导的机制参与了生物利用度的提高。这些发现证实,[提取物名称]与乳香酸可一起口服给药以获得有效的治疗效果。因此,我们的研究支持将[提取物名称]与乳香酸联合应用作为与炎症相关疾病的一种新型治疗途径。