Shangluo Key Research Laboratory of Standardized Planting & Quality Improvement of Bulk Chinese Medicinal Materials College of Biology Pharmacy & Food Engineering, Shangluo University, Shangluo, China.
Qinba Mountains of Bio-Resource Collaborative Innovation Center of Southern Shaanxi Province, Hanzhong, China.
Nat Prod Res. 2024 Dec;38(23):4280-4285. doi: 10.1080/14786419.2023.2273911. Epub 2023 Oct 25.
Two previously undescribed natural cyathane diterpenoids Me-dentifragilin A () and Epi-neocyathin O (), and three known cyathane diterpenoids -, cyathin O, neocyathin P, and cyathin I, were isolated from the rice medium of the CBPFE A06. Their structures were established by NMR spectra, and HR-ESI-MS. Compounds - displayed encouraging neurotrophic activity in PC-12 cells at doses of 5 µM. Meanwhile, - significantly inhibited LPS-induced NO generation in BV2 cells with the IC values ranging from 2.44 ± 0.16 to 4.33 ± 0.32 μM. Western blot analysis showed that and inhibited the expression of genes involved in nitric oxide (NO) production. Molecular docking revealed that five residues of inducible NO synthase (iNOS) are key residues affecting the interaction of and with iNOS. This study enriches the structural diversity of cyathane diterpenes and adds to the evidence that cyathane diterpenes prevent and treat neurodegenerative diseases.
从 CBPFE A06 的大米培养基中分离得到了两个以前未描述的天然杯烷二萜类化合物 Me-dentifragilin A()和 Epi-neocyathin O()，以及三个已知的杯烷二萜类化合物 - ，cyathin O，neocyathin P 和 cyathin I。通过 NMR 光谱和 HR-ESI-MS 确定了它们的结构。化合物 - 在 5 μM 剂量下对 PC-12 细胞表现出令人鼓舞的神经营养活性。同时，- 显著抑制 LPS 诱导的 BV2 细胞中 NO 的产生，IC 值范围为 2.44 ± 0.16 至 4.33 ± 0.32 μM。Western blot 分析表明，和抑制参与一氧化氮 (NO) 产生的基因表达。分子对接表明，诱导型一氧化氮合酶 (iNOS) 的五个残基是影响与 iNOS 相互作用的关键残基。本研究丰富了杯烷二萜的结构多样性，并为杯烷二萜预防和治疗神经退行性疾病提供了证据。
