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Anti-inflammatory activities of isopimara-8(9),15-diene diterpenoids and mode of action of kaempulchraols B-D from Kaempferia pulchra rhizomes.
Journal of Natural Medicines ( IF 2.5 ) Pub Date : 2020-01-31 , DOI: 10.1007/s11418-020-01389-7
Nwet Nwet Win 1 , Besse Hardianti 1, 2 , Hla Ngwe 3 , Yoshihiro Hayakawa 1 , Hiroyuki Morita 1
Affiliation  

Kaempulchraols B–D (2–4), isopimara-8(9),15-diene diterpenoids isolated from Kaempferia pulchra rhizomes collected in Myanmar, were identified as potent NF-κB inhibitors. These compounds were also effective as NO inhibitory agents, with IC50 values of 47.69, 44.97, and 38.17 μM, respectively, without showing any cytotoxicity against LPS-induced RAW264.7 cells. Investigations of the mechanisms of action of 2–4 revealed that they inhibit the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression, with an effective dose of 25 μM. Thus, isopimarane diterpenoids are suggested to be potent inhibitors of NF-κB pathways and could be further explored as potential anti-inflammatory lead compounds.

中文翻译:

Isempimara-8(9),15-diene diterpenoids的抗炎活性和来自Kaempferia pulchra根茎的kaempulchraols BD的作用方式。

从缅甸采集的Kaempferia pulchra根茎中分离得到的Kaempulchraols B–D(2-4),isopimara -8(9),15-二烯二萜类化合物被认为是有效的NF-κB抑制剂。这些化合物也可作为NO抑制剂有效,IC 50值分别为47.69、44.97和38.17μM,而对LPS诱导的RAW264.7细胞没有任何细胞毒性。对2-4作用机制的研究表明,它们以有效剂量25μM抑制NF-κB介导的萤光素酶报告基因的反式激活,IL-6产生和COX-2表达。因此,异匹烷烷二萜被认为是有效的NF-κB信号通路抑制剂,可以作为潜在的抗炎先导化合物进行进一步的研究。
更新日期:2020-01-31
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