AIM: To demonstrate the effects of telmisartan on the proliferation and apoptosis of U937 cells.METHODS: The proliferation ability of the U937 cells was assessed by CCK-8 assay and colony formation test with methylcellulose.The CD11b expression rate of the U937 cells was identified by flow cytometry.The apoptotic rate was analyzed by flow cytometry with Annexin V-PI double staining and Hoechst 33342 staining.The protein levels of cleaved PARP and cleaved caspase-3 were determined by Western blot.RESULTS: The results of CCK-8 assay confirmed that the viability of U937 cells was inhibited by telmisartan.The colony formation capacity of U937 cells was also significantly inhibited by telmisartan.The differentiation of U937 cells was induced by telmisartan with the expression of CD11b.The results of flow cytometry analysis with Annexin V-PI double staining and Hoechst 33342 staining identified that the apoptosis of U937 cells was induced by telmisartan in dose-dependent and time-dependent manners with the up-regulation of cleaved PARP and cleaved caspase-3 proteins.CONCLUSION: Telmisartan inhibits the proliferation and induces the differentiation of U937 cells.Telmisartan also induces the apoptosis of U937 cells through the caspase pathway.

Aim: To study the synthesis and anti-inflammatory activity of p-(sulfamyl) benzylidene-linked hetero-cyclic ketone derivatives. Methods: A series of p-(sulfamyl) benzylidene-linked heterocyclic ketone derivatives were synthesized. Anti-inflammatory activity was evaluated against xylene-induced ear oedema in mice and against carrageenan-induced paw oedema in rats. Gastrointestinal side effects in the rats were also examined after continu-ous introgastric administration of these compounds once daily for 7 days. Results: Twelve compounds( LHZ-101-LHZ-112) were synthesized and their structures were confirmed by IR, ~1H NMR, MS and elemental analysis. LHZ-105, LHZ-106 and LHZ-111 exhibited marked anti-inflammatory activity in xylene-induced mice ear swelling model. LHZ-106 and LHZ-111 showed significant anti-inflammatory activity in carrageenan-induced rat paw ede-ma model. LHZ-105, LHZ-106 and LHZ-111 had less gastrointestinal side effects than diclofenac sodium and CI-1004. Conclusion: These results suggest that some of these compounds have the potential for anti-inflammatory activity with few gastrointestinal side effects.