Department of Microbial and Biochemical Pharmacy, College of Pharmacy, Jinan University, Guangzhou, 510632, People's Republic of China.
Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, 510632, People's Republic of China.
J Nat Med. 2022 Sep;76(4):849-856. doi: 10.1007/s11418-022-01630-5. Epub 2022 May 31.
Two new clerodane diterpenoids (1 and 2), a new pyran-2-one derivative (3), along with five known compounds (4‒8), were isolated from Croton crassifolius. Notably, crassifolin X (1) is a novel clerodane diterpenoid, characterized with a peculiar δ-lactone core being formed between C-1 and C-4. Their structures, including absolute configurations, were established on the basis of spectroscopic methods (UV, IR, HRESIMS and NMR), and circular dichroism experiments. In addition, all compounds were evaluated for their anti-neuroinflammatory activities based on the expression of TNF-α and IL-6 levels on LPS-induced BV2 cells, and compounds 1‒3 and 5 showed potential anti-neuroinflammatory activity.
从大籽柳中分离得到了两个新的 clerodane 二萜（1 和 2）、一个新的吡喃-2-酮衍生物（3）以及五个已知化合物（4-8）。值得注意的是，cras-sifolin X（1）是一种新型 clerodane 二萜，其特征在于 C-1 和 C-4 之间形成了一个独特的 δ-内酯核。基于光谱方法（UV、IR、HRESIMS 和 NMR）和圆二色谱实验确定了它们的结构，包括绝对构型。此外，根据 LPS 诱导的 BV2 细胞中 TNF-α 和 IL-6 水平的表达，评估了所有化合物的抗神经炎症活性，化合物 1-3 和 5 表现出潜在的抗神经炎症活性。
