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山奈酚-3-O-Β-D-葡萄糖醛酸苷在 LPS 刺激的 RAW264.7 细胞和小鼠模型中表现出潜在的抗炎作用。

Kaempferol-3-o-β-d-glucuronate exhibit potential anti-inflammatory effect in LPS stimulated RAW 264.7 cells and mice model.

机构信息

Academy of Scientific and Innovative Research, CSIR-Indian Institute of Integrative Medicines, Jammu Tawi, Jammu and Kashmir, India; Inflammation Pharmacology Division, CSIR-Indian Institute of Integrative Medicine, Jammu Tawi, Jammu and Kashmir, India.

Natural Product Chemistry, CSIR-Indian Institute of Integrative Medicines, Jammu Tawi, Jammu and Kashmir, India.

出版信息

Int Immunopharmacol. 2018 Apr;57:62-71. doi: 10.1016/j.intimp.2018.01.041. Epub 2018 Feb 22.

Abstract

Kaempferol-3-O-β-d-glucuronide (K3G) having various pharmacological effects was explored for its anti-inflammatory effect in LPS induced RAW 264.7 cells and mice model. K3G significantly inhibited various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. It upregulated the secretion of anti-inflammatory cytokine IL-10. K3G is found to reduce inflammation when studied for parameters like phagocytic index, carrageenan induced paw edema in mice and organ weight. It reduced inflammation in a dose dependent manner both in-vitro and in-vivo. Further molecular insights into the study reveal that K3G blocks the phosphorylation of NF-kB which is key regulator of inflammation, thereby exhibiting anti-inflammatory potential. Hence, this study permits further investigation to develop K3G as anti-inflammatory drug.

摘要

山柰酚-3-O-β-D-葡萄糖醛酸苷(K3G)具有多种药理作用,研究其在 LPS 诱导的 RAW264.7 细胞和小鼠模型中的抗炎作用。K3G 显著抑制各种促炎介质,如 IL-1β、NO、PGE2 和 LTB4。它上调抗炎细胞因子 IL-10 的分泌。研究发现,K3G 可降低吞噬指数、角叉菜胶诱导的小鼠足肿胀和器官重量等参数的炎症。它在体外和体内均呈剂量依赖性降低炎症。进一步的分子研究表明,K3G 阻断了 NF-κB 的磷酸化,NF-κB 是炎症的关键调节剂,从而表现出抗炎潜力。因此,本研究允许进一步研究将 K3G 开发为抗炎药物。

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