Agroprocessing and Natural Products Division, National Institute for Interdisciplinary Science and Technology (CSIR), Trivandrum 695019, India.
J Ethnopharmacol. 2011 Feb 16;133(3):1117-20. doi: 10.1016/j.jep.2010.10.027. Epub 2010 Oct 20.
Seed of Semecarpus anacardium L. is widely used in Indian traditional medicine; Ayurveda and Sidha, for treatment of inflammatory disorders and gout.
The present study was aimed at isolation of a compound for its potential to inhibit xanthine oxidase (XO), over expression of which lead to inflammation and gout.
Activity guided fractionation of S. anacardium seed was conducted using liquid-liquid partition and preparative HPLC. The fractions were evaluated for their XO inhibition and antioxidant activity. The ethyl acetate fraction with the highest XO activity yielded a biflavonoid compound tetrahydroamentoflavone (THA). Lineweaver-Burk (LB) plot for the XO inhibition of THA and allopurinol was constructed from the kinetic data.
IC₅₀ values of THA and allopurinol for XO inhibition were 92 and 100 nM respectively and their corresponding values for K(i) were 0.982 and 0.612 μM respectively.
THA was a potent XO inhibitor which could be considered as a drug candidate or chemopreventive agent, after establishing its pharmacological and clinical evaluation. The study results appear to support the claim of the traditional medicine with respect to the efficacy of S. anacardium seed against inflammation and gout.
麻枫树的种子在印度传统医学中被广泛应用，包括阿育吠陀和悉达医学，用于治疗炎症性疾病和痛风。
本研究旨在分离一种化合物，以评估其抑制黄嘌呤氧化酶（XO）的潜力，因为 XO 的过度表达会导致炎症和痛风。
采用液-液萃取和制备高效液相色谱法对麻枫树种子进行活性导向分离。评估各馏分对 XO 的抑制作用和抗氧化活性。对具有最高 XO 活性的乙酸乙酯馏分进行进一步研究，得到双黄酮化合物四氢荛花素（THA）。根据动力学数据，构建 THA 和别嘌呤醇对 XO 抑制的Lineweaver-Burk（LB）图。
THA 和别嘌呤醇对 XO 抑制的 IC₅₀值分别为 92 和 100 nM，其相应的 K(i)值分别为 0.982 和 0.612 μM。
THA 是一种有效的 XO 抑制剂，在进行药理学和临床评估后，可考虑将其作为药物候选物或化学预防剂。该研究结果似乎支持了传统医学关于麻枫树种子在抗炎和痛风方面的疗效的说法。
