de Araújo Maria Elisa Melo Branco, Franco Yollanda Edwirges Moreira, Alberto Thiago Grando, Messias Marcia Cristina Fernandes, Leme Camila Wielewski, Sawaya Alexandra Christine Helena Frankland, Carvalho Patricia de Oliveira
a Laboratory of Multidisciplinary Research , São Francisco University , Bragança Paulista , Brazil.
b Department of Biochemistry , Institute of Biology, State University of Campinas (UNICAMP) , Campinas , Brazil.
J Enzyme Inhib Med Chem. 2017 Dec;32(1):978-985. doi: 10.1080/14756366.2017.1347165.
Studies have reported that flavonoids inhibit xanthine oxidase (XO) activity; however, poor solubility and stability in lipophilic media limit their bioavailability and applications. This study evaluated the kinetic parameters of XO inhibition and partition coefficients of flavonoid esters biosynthesised from hesperidin, naringin, and rutin via enzymatic acylation with hexanoic, octanoic, decanoic, lauric, and oleic acids catalysed by Candida antarctica lipase B (CALB). Quantitative determination by ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) showed higher conversion yields (%) for naringin and rutin esters using acyl donors with 8C and 10C. Rutin decanoate had higher partition coefficients (0.95), and naringin octanoate and naringin decanoate showed greater inhibitory effects on XO (IC of 110.35 and 117.51 μM, respectively). Kinetic analysis showed significant differences (p < .05) between the flavonoids before and after acylation regarding K values, whereas the values for V were the same, implying the competitive nature of XO inhibition.
研究报告称，黄酮类化合物可抑制黄嘌呤氧化酶（XO）的活性；然而，其在亲脂性介质中的低溶解度和稳定性限制了它们的生物利用度及应用。本研究评估了通过南极假丝酵母脂肪酶B（CALB）催化，用己酸、辛酸、癸酸、月桂酸和油酸对橙皮苷、柚皮苷和芦丁进行酶促酰化生物合成的黄酮酯的XO抑制动力学参数和分配系数。通过超高效液相色谱-质谱联用仪（UHPLC-MS）进行的定量测定表明，使用含8个碳和10个碳的酰基供体时，柚皮苷酯和芦丁酯的转化率（%）更高。癸酸芦丁酯具有更高的分配系数（0.95），而辛酸柚皮苷和癸酸柚皮苷对XO表现出更大的抑制作用（IC分别为110.35和117.51 μM）。动力学分析表明，酰化前后黄酮类化合物的K值存在显著差异（p < 0.05），而V值相同，这意味着XO抑制具有竞争性。
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