Abstract
Toll-like receptors are identified as an important factor in regulation of expression of pro-inflammatory cytokines and used as an important target in the field of anti-inflammation. SpanrstoloninB (SsnB), a new isocoumarin compound isolated from the tuber of Scirpus yagara, is a Toll-like receptor 2 (TLR2) and TLR4 antagonist and can selectively block TLR2- and TLR4- mediated macrophages inflammatory responses. In this study, ten derivatives (A1–A6, B1–B2, and C1–C2) were synthesized by the structural modification of compounds 1 and 2, of which nine derivatives are new compounds. The n-octanol/water partition coefficients (Kow) of these derivatives were determined by high performance liquid chromatography method, and their anti-inflammatory activities were evaluated of inhibiting the secretion of TNF-α and IL-6 in LPS- or Pam3csk4- induced RAW264.7 cells. Preliminary structure-activity relationship study revealed that methylated, acetylated and butyrylated derivatives (A1–A6) exhibited weaker activities of anti-inflammatory than compound 1 and 2. However, hydrolyzed and isoquinolone derivatives (B1–B2 and C1–C2) had better potential to decrease the levels of TNF-α and IL-6.
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