Jiangsu Key Laboratory of Bioactive Natural Product Research, State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
J Agric Food Chem. 2023 Sep 27;71(38):14000-14012. doi: 10.1021/acs.jafc.3c02926. Epub 2023 Sep 13.
Sarglaroids A-H (-), eight new lindenane dimers, and a monomer sarglaroid I (), along with fourteen known analogues (-), were isolated from the roots of The planar structures and the absolute configurations were elucidated by HR-MS, NMR, ECD calculations, and X-ray diffraction crystallography. Sarglaroid A () was identified as a rare 8,9- lindenane dimer with a unique 5/5/5 tricyclic system. The biological evaluation showed that compounds and potently inhibited NO production with IC values at 19.8 ± 1.06 and 10.7 ± 0.25 μM, respectively, and had no cytotoxicity to RAW264.7 cells. Compound significantly inhibited the LPS-/ATP-induced IL-1β release by inactivating the NLRP3 inflammasome through inhibiting the initiation and assembly by affecting the K efflux. Compounds and inhibited the proliferation of MCF-7 and MDA-MB-231 with IC values ranging from 5.4 to 10.2 μM.
从白皮松根部分离得到了 Sarglaroids A-H(-)、八个新的贝壳杉烷二聚体和一个单体 Sarglaroid I(),以及 14 个已知类似物(-)。通过高分辨质谱、NMR、ECD 计算和 X 射线衍射晶体学确定了它们的平面结构和绝对构型。Sarglaroid A()被鉴定为一种罕见的 8,9-贝壳杉烷二聚体,具有独特的 5/5/5 三环系统。生物评价表明,化合物和强烈抑制了 NO 的产生,IC 值分别为 19.8±1.06 和 10.7±0.25 μM,对 RAW264.7 细胞没有细胞毒性。化合物通过抑制 NLRP3 炎性小体的起始和组装,通过影响 K 外流来失活,显著抑制了 LPS-/ATP 诱导的 IL-1β释放。化合物和抑制 MCF-7 和 MDA-MB-231 的增殖,IC 值范围为 5.4 至 10.2 μM。