Center for Research and Technology Transfer (CRETECH), Vietnam Academy of Sciences and Technology, Hanoi 10072, Vietnam.
Graduate School for International Development and Cooperation (IDEC), Hiroshima University, Higashi-Hiroshima 739-8529, Japan.
Molecules. 2019 Oct 29;24(21):3899. doi: 10.3390/molecules24213899.
The root of L. has been shown to possess anti-gout and anti-diabetic properties, but the compounds responsible for these pharmaceutical effects have not yet been reported. In this study, we aimed to isolate and purify active components from the root of , and to evaluate their anti-radical, anti-gout and anti-diabetic capacities. From the ethyl acetate (EtOAc) extract, two compounds, chrysophanol () and physcion (), were isolated by column chromatography with an elution of hexane and EtOAc at a 9:1 ratio. Their structures were identified by spectrometric techniques including gas chromatography-mass spectrometry (GC-MS), electrospray ionization-mass spectrometry (ESI-MS), X-ray diffraction analyses and nuclear magnetic resonance (NMR). The results of bioassays indicated that () showed stronger activities than (). For antioxidant activity, () and () exhibited remarkable DPPH radical scavenging capacity (IC = 9.8 and 12.1 µg/mL), which was about two times stronger than BHT (IC = 19.4 µg/mL). The anti-gout property of () and () were comparable to the positive control allopurinol, these compounds exerted strong inhibition against the activity of xanthine oxidase (IC = 36.4 and 45.0 µg/mL, respectively). In the anti-diabetic assay, () and () displayed considerable inhibitory ability on α-glucosidase, their IC values (IC = 20.1 and 18.9 µg/mL, respectively) were higher than that of standard acarbose (IC = 143.4 µg/mL). Findings of this study highlight that () and () may be promising agents to treat gout and diabetes, which may greatly contribute to the medicinal properties of root.
黄连的根已被证明具有抗痛风和抗糖尿病的特性,但负责这些药物作用的化合物尚未被报道。在这项研究中,我们旨在从黄连的根中分离和纯化活性成分,并评估它们的抗自由基、抗痛风和抗糖尿病能力。从乙酸乙酯(EtOAc)提取物中,通过柱层析用正己烷和 EtOAc 的 9:1 比例洗脱,分离出两种化合物,大黄酚()和大黄素()。它们的结构通过包括气相色谱-质谱联用(GC-MS)、电喷雾电离质谱(ESI-MS)、X 射线衍射分析和核磁共振(NMR)在内的光谱技术来鉴定。生物测定结果表明,()比()具有更强的活性。对于抗氧化活性,()和()表现出显著的 DPPH 自由基清除能力(IC = 9.8 和 12.1 µg/mL),大约是 BHT(IC = 19.4 µg/mL)的两倍。()和()的抗痛风性质与阳性对照别嘌呤醇相当,这些化合物对黄嘌呤氧化酶的活性表现出强烈的抑制作用(IC = 36.4 和 45.0 µg/mL,分别)。在抗糖尿病测定中,()和()对α-葡萄糖苷酶表现出相当大的抑制能力,其 IC 值(IC = 20.1 和 18.9 µg/mL,分别)高于标准阿卡波糖(IC = 143.4 µg/mL)。本研究的结果表明,()和()可能是治疗痛风和糖尿病的有前途的药物,这可能极大地促进黄连根的药用特性。