| Autor: |
Wang Wang, Liangliang Xiong, Yanli Wu, Yirong Zhou, Yutong Li, Mengzhu Zheng, Zhuorui Song, Dejuan Sun, Lixia Chen |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Acta Materia Medica, Vol 1, Iss 2, Pp 224-243 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2737-7946 |
| DOI: |
10.15212/AMM-2022-0008 |
| Popis: |
In our ongoing work on the identification of potent anti-inflammatory agents, we designed and synthesized three series of lathyrane diterpenoid hybrids in which the lathyrane diterpenoid skeleton was hybridized with other anti-inflammatory pharmacophores. Unexpectedly, lathyrane diterpenoid/3-hydroxyflavone hybrids showed more potent anti-inflammatory activity in RAW264.7 cells than did the corresponding parent compounds. Compound 8d1 exhibited potent anti-inflammatory activity with low cytotoxicity (IC50 = 1.55 ± 0.68 μM), and downregulated LPS-induced expression of iNOS and COX-2, as well as IκBα phosphorylation. This compound also inhibited the expression and nuclear translocation of NF-κB, and stimulated autophagy induction. Thus, 8d1’s anti-inflammatory mechanism is associated with inhibition of the NF-κB signaling pathway and increasing autophagy. This compound may serve as a promising anti-inflammatory agent. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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