The United Graduate School of Agricultural Sciences, Kagoshima University, Kagoshima, 890-0065, Japan.
Faculty of Agriculture, University of the Ryukyus, Okinawa, 903-0213, Japan.
Naunyn Schmiedebergs Arch Pharmacol. 2020 Feb;393(2):191-201. doi: 10.1007/s00210-019-01721-3. Epub 2019 Sep 4.
We previously reported the antifungal, antioxidant, and vasodilator effects of Ryudai gold (RD) and isolated some potentially active compounds. Here, we aimed to identify other active compounds present in RD and investigate their pharmacological effects, in terms of antioxidant, and inhibitory activities against skin disease-related enzymes, pancreatic α-amylase, and lipase enzymes. The methanol extract of RD rhizomes was subjected to repeated fractionation by silica gel column, Toyopearl HW-40F column, and high-performance liquid chromatography to obtain a pure compound. The isolated compound was characterized by analyzing its spectroscopic data, particularly nuclear magnetic resonance spectra. Inhibitory activities against α-amylase, pancreatic lipase, elastase, collagenase, xanthine oxidase, and tyrosinase were evaluated to investigate its potential antidiabetic, antiobesity, and enzyme inhibitory effects. Antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl-scavenging, reducing power, and 2-deoxyribose degradation assays. The purified compound was recognized as 4-methylene-8-hydroxybisabola-2,10-diene-9-one, a new compound. The content of this compound was 0.068 μmol/g or 0.016 mg/g of dry RG powder. Our results suggested that 4-methylene-8-hydroxybisabola-2,10-diene-9-one exhibited antidiabetic, antiobesity, enzyme inhibitory, and antioxidant activities by inhibiting their respective enzymes activity. 4-methylene-8-hydroxybisabola-2,10-diene-9-one could be a promising candidate therapeutic agent or a lead compound for the development of new synthetic drugs.
我们之前报道了 Ryudai 金（RD）的抗真菌、抗氧化和血管舒张作用，并分离出一些潜在的活性化合物。在这里，我们旨在鉴定 RD 中存在的其他活性化合物，并研究它们在抗氧化、抑制皮肤疾病相关酶、胰腺α-淀粉酶和脂肪酶方面的药理作用。RD 根茎的甲醇提取物通过硅胶柱、Toyopearl HW-40F 柱和高效液相色谱法进行反复分段，以获得纯化合物。通过分析其光谱数据，特别是核磁共振谱，对分离得到的化合物进行了表征。评估了对α-淀粉酶、胰脂肪酶、弹性蛋白酶、胶原酶、黄嘌呤氧化酶和酪氨酸酶的抑制活性，以研究其潜在的抗糖尿病、抗肥胖和酶抑制作用。抗氧化活性通过 2,2-二苯基-1-苦基肼清除、还原能力和 2-脱氧核糖降解测定进行评估。纯化的化合物被鉴定为 4-亚甲基-8-羟基双黄烷-2,10-二烯-9-酮，一种新化合物。该化合物的含量为 0.068μmol/g 或 0.016mg/g 的干 RG 粉。我们的结果表明，4-亚甲基-8-羟基双黄烷-2,10-二烯-9-酮通过抑制各自的酶活性表现出抗糖尿病、抗肥胖、酶抑制和抗氧化活性。4-亚甲基-8-羟基双黄烷-2,10-二烯-9-酮可能是一种有前途的候选治疗剂或新型合成药物开发的先导化合物。
