Strigolactones: a plant phytohormone as novel anti-inflammatory agents†,RSC Medicinal Chemistry

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Strigolactones: a plant phytohormone as novel anti-inflammatory agents†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-12-05 00:00:00 , DOI: 10.1039/c7md00461c
Jun-Xia Zheng _{1,

2,

3,

4} , Yu-Shui Han _{3,

4,

5,

6} , Jin-Cai Wang _{3,

4,

5,

6} , Hui Yang _{3,

4,

5,

6} , Hao Kong _{3,

4,

5,

6} , Kang-Jia Liu _{3,

4,

5,

6} , Si-Yu Chen _{3,

4,

5,

6} , Yi-Rui Chen _{4,

7,

8,

9} , Yi-Qun Chang _{3,

4,

5,

6} , Wei-Min Chen _{3,

4,

5,

6} , Jia-Liang Guo _{4,

7,

8,

9} , Ping-Hua Sun _{3,

4,

5,

6}

Affiliation

Strigolactones (SLs) are a novel class of plant hormones with enormous potential for the prevention and treatment of inflammation. To further investigate the anti-inflammatory activities of SLs, a representative SL, GR24, and the reductive products of its D-ring were synthesized and their anti-inflammatory activities were fully evaluated on both in vitro and in vivo models. Among these compounds, the two most active optical isomers (2a and 6a) demonstrated strong inhibitory activity on the release of inflammatory cytokines, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) by blocking the nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways; they also greatly inhibited the migration of neutrophils and macrophages in fluorescent protein labeled zebrafish larvae. These results identified the promising anti-inflammatory effects of SLs, and suggested that both the absolute configuration of SL and the α,β-unsaturated D-ring structure are essential for the observed anti-inflammatory activity.

中文翻译：

Strigolactones：一种植物激素，作为新型抗炎药†

Strigolactones（SLs）是一类新型的植物激素，在预防和治疗炎症方面具有巨大潜力。为了进一步研究SL的抗炎活性，合成了代表性的SL，GR24及其D环的还原产物，并在体外和体内模型中全面评估了它们的抗炎活性。在这些化合物中，两种活性最高的旋光异构体（2a和6a）通过阻断核因子kappa B（NF-κB），对包括一氧化氮（NO），肿瘤坏死因子α（TNF-α）和白细胞介素6（IL-6）在内的炎性细胞因子的释放具有较强的抑制活性。）和丝裂原激活的蛋白激酶（MAPK）信号通路；它们还极大地抑制了中性粒细胞和巨噬细胞在荧光蛋白标记的斑马鱼幼虫中的迁移。这些结果确定了SL的有希望的抗炎作用，并表明SL的绝对构型和α，β-不饱和D环结构对于观察到的抗炎活性都是必不可少的。

更新日期：2017-12-05

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