Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People's Republic of China.
Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People's Republic of China.
Bioorg Chem. 2021 Sep;114:105091. doi: 10.1016/j.bioorg.2021.105091. Epub 2021 Jun 13.
Five new acetylenic phenol derivatives (1-4 and 7), one new benzofuran derivative (8), one new naphthol derivative (9), and two known analogues (5 and 6), were isolated and identified from an endophytic fungus Daldinia sp. TJ403-LS1 that was isolated from the medicinally valuable plant Anoectochilus roxburghii. Their structures were elucidated by means of extensive spectroscopic analyses and electronic circular dichroism (ECD) calculations. In addition, compound 1 exhibited remarkable immunosuppressive activity against LPS and anti-CD3/anti-CD28 mAbs activated murine splenocytes proliferation with the same IC values of 0.06 μM and BChE inhibitory activity with an IC value of 6.93 ± 0.71 μM, and compounds 6, 8 and 9 showed excellent BChE inhibitory activity with IC values of 16.00 ± 0.30, 23.33 ± 0.55, and 15.53 ± 0.39 μM, respectively (positive drug neostigmine, IC = 49.60 ± 6.10 μM), highlighting the promising potentials to be designed and developed as immunosuppressive and BChE inhibitory agents.
从药用植物铁皮石斛内生真菌 Daldinia sp. TJ403-LS1 中分离得到了 5 个新的炔酚衍生物（1-4 和 7）、1 个新的苯并呋喃衍生物（8）、1 个新的萘酚衍生物（9）和 2 个已知类似物（5 和 6）。通过广泛的光谱分析和电子圆二色性（ECD）计算确定了它们的结构。此外，化合物 1 对 LPS 和抗 CD3/抗 CD28 mAbs 激活的小鼠脾细胞增殖具有显著的免疫抑制活性，IC 值相同为 0.06 μM，对 BChE 的抑制活性为 6.93±0.71 μM，化合物 6、8 和 9 对 BChE 具有优异的抑制活性，IC 值分别为 16.00±0.30、23.33±0.55 和 15.53±0.39 μM（阳性药物新斯的明，IC=49.60±6.10 μM），具有作为免疫抑制剂和 BChE 抑制剂的设计和开发潜力。
