Key Laboratory of Natural Products Research and Development of Li Folk Medicine of Hainan Province, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou, Hainan 571101, China; Key Laboratory of Conservation and Utilization of Tropical Agro-bioresources of Hainan Province, Hainan Academy of Tropical Agricultural Resources, Haikou, Hainan 571101, China.
Key Laboratory of Natural Products Research and Development of Li Folk Medicine of Hainan Province, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou, Hainan 571101, China; Key Laboratory of Conservation and Utilization of Tropical Agro-bioresources of Hainan Province, Hainan Academy of Tropical Agricultural Resources, Haikou, Hainan 571101, China.
Fitoterapia. 2023 Sep;169:105582. doi: 10.1016/j.fitote.2023.105582. Epub 2023 Jun 17.
Four new compounds ((±)-1-3), including one pair of enantiomers ((±)-1), along with 11 known bibenzyls (4-14) were isolated from Dendrobium nobile. The structures of the new compounds were elucidated by spectroscopic methods including 1D and 2D NMR as well as HRESIMS. The configurations of (±)-1 were established via the electronic circular dichroism (ECD) calculations. Compounds (+)-1 and 13 displayed pronounced α-glucosidase inhibitory activities with IC values of 16.7 ± 2.3 and 13.4 ± 0.2 μM, respectively, which were comparable to that of genistein (IC, 8.54 ± 0.69 μM). Kinetic studies revealed that (+)-1 and 13 were non-competitive inhibitors against α-glucosidase and molecular docking simulations illuminated their interactions with α-glucosidase. All the isolates were also evaluated for their anti-inflammatory activities. Compounds 4, 5, and 11 exhibited superior inhibition activity with IC values ranging from 9.2 to 13.8 μM to that of quercetin (IC, 16.3 ± 1.1 μM).
从铁皮石斛中分离得到 4 个新化合物((±)-1-3),包括 1 对对映异构体((±)-1),以及 11 个已知的联苄类化合物(4-14)。通过 1D 和 2D NMR 以及 HRESIMS 等光谱方法阐明了新化合物的结构。通过电子圆二色性(ECD)计算确定了(±)-1 的构型。化合物(+)-1 和 13 对α-葡萄糖苷酶表现出显著的抑制活性,IC 值分别为 16.7±2.3 和 13.4±0.2 μM,与染料木素(IC,8.54±0.69 μM)相当。动力学研究表明,(+)-1 和 13 是 α-葡萄糖苷酶的非竞争性抑制剂,分子对接模拟揭示了它们与 α-葡萄糖苷酶的相互作用。所有分离物也进行了抗炎活性评估。化合物 4、5 和 11 对 α-葡萄糖苷酶的抑制活性优于槲皮素(IC,16.3±1.1 μM),IC 值范围为 9.2-13.8 μM。