Division of Chinese Medicine Resources, School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Guangzhou Jinan Biomedicine Research and Development Center, College of Life Science and Technology, Jinan University, Guangzhou 510632, China.
Fitoterapia. 2021 Sep;153:104991. doi: 10.1016/j.fitote.2021.104991. Epub 2021 Jul 13.
Morinda officinalis How was widely applied to alleviate symptom like impotence, menstrual disorders, osteoporosis, and rheumatoid arthritis. To expand resources usage, phytochemistry of the aerial parts was studied and the structures of compounds were elucidated based on NMR, HRESIMS, IR and UV. Moreover, the anti-inflammatory effect and possible mechanism were investigated by Griess kit, RT-qPCR, ELISA, western blot and molecular docking on LPS-induced inflammation in RAW 264.7 cells. Herein, we isolated and identified 16 iridoid derivatives, including seven new iridoids officinaloside A-G (1-7) and nine known iridoids. All the compounds were safe to RAW 264.7 cells. Luckily, compounds 5 and 6 showed inhibitory effect on production of NO, and decreased the expression of inflammatory cytokines at mRNA and protein levels in a dose-dependent way. The possible mechanism of their anti-inflammation may be the affinity interaction between 5 with COX-2 protein, and 6 with iNOS protein. Overall, compounds 5 and 6 exert promising effects in inhibiting inflammatory cytokines, indicating that they could be used as lead compounds for developing health products or clinical practice for inflammation, which provides a scientific basis for further sustainable development and usage of the aerial parts of Morinda officinalis How.
巴戟天被广泛应用于缓解阳痿、月经失调、骨质疏松症和类风湿性关节炎等症状。为了扩大资源利用，对其地上部分的植物化学进行了研究，并根据 NMR、HRESIMS、IR 和 UV 等方法阐明了化合物的结构。此外，通过 LPS 诱导 RAW 264.7 细胞炎症模型中的 Griess 试剂盒、RT-qPCR、ELISA、western blot 和分子对接实验，研究了其抗炎作用及可能的机制。在此，我们分离并鉴定了 16 种裂环烯醚萜类衍生物，包括 7 种新的裂环烯醚萜类化合物 officinaloside A-G（1-7）和 9 种已知的裂环烯醚萜类化合物。所有化合物对 RAW 264.7 细胞均安全。幸运的是，化合物 5 和 6 对 NO 的产生具有抑制作用，并呈剂量依赖性降低炎症细胞因子在 mRNA 和蛋白水平的表达。它们抗炎的可能机制可能是 5 与 COX-2 蛋白、6 与 iNOS 蛋白的亲和力相互作用。总之，化合物 5 和 6 在抑制炎症细胞因子方面表现出有希望的效果，表明它们可作为开发用于炎症的保健品或临床实践的先导化合物，为进一步可持续开发和利用巴戟天地上部分提供了科学依据。
