| Innate immunity of human body is quite important to anti-bacterial, anti-viral andanti-tumor. Toll-like receptors (TLRs) are key receptors of innate immunity. TLRs and itsagonist ligand binding activation of innate immune cells and the further adjustment to acquireimmune systems. Recently, TLRs were discovered in the occurrence and development ofcancer also play an important role. TLRs agonists are used as immunomodulators (immunoadjuvants) and cytotoxic drugs in cancer immunotherapy. TLRs agonists are usually complexnatural compounds that derived from bacteria, viruses and other pathogens, such astri-acylated lipopeptide(PAM3), zymosan, bacterial lipopolysaccharide (LPS) and so on. Lastcentury, scientists found that the small molecule compounds that synthetic miaow thiazolequinoline can also combined with TLRs, Imiquimod, resiquimod, and confirmed thesecompounds which could antitumor and antiviral.We present the new anticancer thiochroman ketones study to e xamine its non-cytotoxicconcentrations whether activation of macrophages, indicating TLRs agonist effects. Theresults showed that: the new thiochromanones with similar effect of LPS, can regulatemacrophage functions, which suggesting that it may be a new molecule agonists of TLRs. Forthe study targets thiochroman ketones provide avant-garde ideas, we selected RAW264.7,Hela, HEPG-2, MCF-7, MKN-28as experimental objects. It detected that the newthiochromanones could immune activation, which can significantly stimulated RAW264.7production of NO, increase the phagocytic activity, increased cytokine TNF-α and IL-6release can be activated murine macrophage RAW264.7cells. It also showed a goodanti-metastasis effect, but its anti-transfer mechanism has not been clearly yet, which requiresfurther study. |