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    During the screening of natural anti-inflammatory agent, we identified some C21-steroidal pregnane sapogenins or the derivatives to inhibit TLR2, TLR3, and TLR4-initiatedinflammatory responses respectively. Treatment with active compounds 10, 2j and 3p failed to impact tumor necrosis factor-α (TNF-α) induced nucleus translocation of NF-κB p65 subunit. However, these compounds regulated distinct canonical or non-canonical NF-κB family members. Ectopic expression of TNF receptor associated factor 6 (TRAF6) abrogated the inhibitory activity of the compounds on production of pro-inflammatory cytokines downstream of TLR4. These results suggested that compounds 10, 2j, and 3p suppressed TLR-initiated innate immunity through TRAF6 with differential regulation of NF-κB family proteins. Copyright © 2017 Elsevier Ltd. All rights reserved.

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    Lie-Jun Huang, Shao-Ru Chen, Chun-Mao Yuan, Wei Gu, Bao-Jian Guo, Yi-Tao Wang, Ying Wang, Xiao-Jiang Hao. C21-steroidal pregnane sapogenins and their derivatives as anti-inflammatory agents. Bioorganic & medicinal chemistry. 2017 Jul 01;25(13):3512-3524

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    PMID: 28506585

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