Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.
Fitoterapia. 2023 Jun;167:105493. doi: 10.1016/j.fitote.2023.105493. Epub 2023 Apr 5.
In present study, three series of 2,6-dihalogenated stilbene derivatives were designed, synthesized, and assayed for anti-inflammatory and cytotoxic activities. All 62 compounds showed potential anti-inflammatory activity in zebrafish model in vivo, and the installation of halogens and pyridines led to significant improved effects. Among them, DHS2u and DHS3u with the substitution of pyridine showed more higher effects than positive drug indomethacin at 20 μM with inhibitory rate of 94.59% and 90.54%, respectively. Besides, DHS3g bearing 2,5-dimethoxy exhibited potent cytotoxic activity against K562 cells with IC values 3.12 μM along with a suitable selectivity on normal cell viability. These results showed that 2,6-dihalogenated stilbenes could serve as a bright starting point for the further development as anti-inflammatory and antitumor agents.
在本研究中，设计、合成并评估了三组 2,6-二卤代二苯乙烯衍生物的抗炎和细胞毒性活性。所有 62 种化合物在体内斑马鱼模型中均显示出潜在的抗炎活性，卤素和吡啶的引入导致显著改善了效果。其中，DHS2u 和 DHS3u 带有吡啶取代基，其抑制率分别为 94.59%和 90.54%，在 20 μM 时的效果比阳性药物吲哚美辛更好。此外，带有 2,5-二甲氧基的 DHS3g 对 K562 细胞表现出强烈的细胞毒性活性，IC 值为 3.12 μM，同时对正常细胞活力具有适当的选择性。这些结果表明，2,6-二卤代二苯乙烯可以作为进一步开发抗炎和抗肿瘤药物的良好起点。
