State Key Laboratory of Phytochemistry and Plant Resources in West China, Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, PR China; University of Chinese Academy of Sciences, Beijing 100049, PR China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Institute of Botany, Chinese Academy of Sciences, Kunming 650201, PR China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming 650201, PR China.
Fitoterapia. 2018 Jul;128:57-65. doi: 10.1016/j.fitote.2018.03.009. Epub 2018 Apr 8.
Ten new (1-10) and ten known (11-20) diterpenoids involving ent-atisane, ent-seco-atisane, ent-kaurane and ent-seco-kaurane types were isolated from Sapium insigne under the guidance of LCMS-IT-TOF analyses. Their structures were characterized by extensive spectroscopic analyses (HRESIMS, UV, IR, 1D and 2D NMR). A putative biosynthetic pathway was proposed for ent-seco-atisane diterpenoids. Their inhibitory activities on α-glucosidase in vitro were tested for the first time. Compound 4 showed moderate inhibitory effect on α-glucosidase with an IC value of 0.34 mM via a noncompetitive inhibition mechanism (K = 0.27 mM). The preliminary structure-activity relationships of the ent-atisane diterpenoids inhibiting α-glucosidase were discussed.
在 LCMS-IT-TOF 分析的指导下，从乌桕中分离得到了 10 个新的（1-10）和 10 个已知的（11-20）二萜类化合物，涉及 ent-atisane、ent-seco-atisane、ent-kaurane 和 ent-seco-kaurane 型。通过广泛的光谱分析（HRESIMS、UV、IR、1D 和 2D NMR）确定了它们的结构。提出了 ent-seco-atisane 二萜的可能生物合成途径。首次测试了它们在体外对α-葡萄糖苷酶的抑制活性。化合物 4 通过非竞争性抑制机制（K 值为 0.27 mM）对α-葡萄糖苷酶表现出中等抑制作用，IC 值为 0.34 mM。讨论了抑制α-葡萄糖苷酶的 ent-atisane 二萜的初步结构-活性关系。
