State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650201, People's Republic of China; University of the Chinese Academy of Science, Beijing 100049, People's Republic of China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650201, People's Republic of China.
Bioorg Chem. 2021 Jul;112:104977. doi: 10.1016/j.bioorg.2021.104977. Epub 2021 May 7.
Previously, we have demonstrated the antiadipogenic benefits of Ganoderma triterpenoids (GTs), which indicated GTs have potential therapeutic implications for obesity. In this study, the EtOAc extract of Ganoderma applanatum was further phytochemically investigated for searching new antiadipogenic agents, which led to the isolation of a total of 15 highly oxygenated lanostane triterpenoids, including 9 new compounds (1-9) and 6 known analogues (10-15). Structurally, ganodapplanoic acids A and B (1, 2) are two rearranged 6/6/5/6-fused lanostane-type triterpenoids with an unusual C-13/C-15 oxygen bridge moiety. In addition, the EtOAc extract (GAE) and isolates (1-4,6-15) were assayed for their antiadipogenic effects in 3T3-L1 adipocytes. The results revealed that compound 9 effectively repressed adipogenesis through down-regulating the expression of major proteins (PPARγ, CEBPβ and FAS) involving differentiation and adipogenesis in 3T3-L1 adipocytes. Thus, the present study further demonstrated the antiadipogenic potential of GTs and provided a possible perspective for obesity treatment.
先前，我们已经证实了灵芝三萜（GTs）的抗脂肪生成作用，这表明 GTs 可能对肥胖症具有治疗意义。在这项研究中，进一步对灵芝的乙酸乙酯提取物进行了植物化学研究，以寻找新的抗脂肪生成剂，从而分离出了总共 15 种高度氧化的羊毛甾烷三萜，包括 9 种新化合物（1-9）和 6 种已知类似物（10-15）。结构上，灵芝酸 A 和 B（1、2）是两种具有不寻常的 C-13/C-15 氧桥部分的重排 6/6/5/6 融合羊毛甾烷型三萜。此外，还测定了乙酸乙酯提取物（GAE）和分离物（1-4、6-15）在 3T3-L1 脂肪细胞中的抗脂肪生成作用。结果表明，化合物 9 通过下调参与 3T3-L1 脂肪细胞分化和脂肪生成的主要蛋白（PPARγ、CEBPβ 和 FAS）的表达，有效抑制脂肪生成。因此，本研究进一步证实了 GTs 的抗脂肪生成潜力，并为肥胖症的治疗提供了可能的视角。
