New Monoterpenoid Indole Hybrids from Gelsemium elegans with Anti-Inflammatory and Osteoclast Inhibitory Activities
New Monoterpenoid Indole Hybrids from Gelsemium elegans with Anti-Inflammatory and Osteoclast Inhibitory Activities
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DOI：
10.1002/cbdv.202301665
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发表时间：
2023-11-27
影响因子：
2.9
通讯作者：
Wei，Xin
中科院分区：
文献类型：
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作者：
Zhang，Pan-Pan;Liang，Jia-Jun;Wei，Xin
从钩吻（Gelsemiumelegans）地上部分分离得到两个新的吲哚生物碱沿着（3-8），即钩吻碱A（1）和B（2）。通过波谱技术鉴定了它们的结构。结构上，化合物1和2具有罕见的笼状gelsedine骨架与双环单萜类化合物的杂合。在LPS诱导的RAW264.7细胞上测试分离的化合物（1-3）的抗炎活性。 在对细胞无毒性的处理浓度下，采用Griess法和酶联免疫吸附试验（ELISA）检测细胞因子一氧化氮（NO）、肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）的水平。结果表明，化合物1 - 3在12.5 ~ 50 μmol/L范围内具有一定的抗炎活性，并呈剂量依赖性。 此外，体外实验还检测了化合物1和2对NF-κB配体受体激活因子（RANKL）诱导破骨细胞形成的抑制作用。 化合物1和2在5μmol/L时对RANKL诱导的破骨细胞生成有明显的抑制作用。本工作报道了新的吲哚单萜类化合物的抗炎和抑制破骨细胞活性，为进一步开展G.优雅
Gelsegansymines A (1) and B (2), two new indole alkaloids along with six known analogues (3–8) were isolated from the aerial parts ofGelsemium elegans. Their structures were elucidated by means of spectroscopic techniques. Structurally, compounds1and2possessed the rare cage‐like gelsedine skeleton hybrid with bicyclic monoterpenoid. The anti‐inflammatory activities of isolated compounds (1–3) were tested on LPS induced RAW264.7 cells. Under the treated concentration without toxicity for cells, the cytokines levels of nitric oxide (NO), tumor necrosis factor‐α(TNF‐α) and interleukin‐6 (IL‐6) were evaluated by Griess method and enzyme‐linked immunosorbent assay (ELISA). The results showed that compounds1–3exhibited anti‐inflammatory activities with dose‐dependent manner range from 12.5 to 50 μmol/L. Furthermore, the inhibitory activities of compounds1and2on receptor activator of NF‐κB ligand (RANKL) induced osteoclast formation were testedin vitro. Compounds1and2at 5μmol/L exhibited the significant inhibitory effect on the osteoclastogenesis induced by RANKL. This work reported the anti‐inflammatory and osteoclast inhibitory activities of new monoterpenoid indole hybrids, which may inspire the further light on the related traditional application research ofG. elegans.