ABSTRACT
Boron containing compound (BCC) offers the potential further development for therapy against malignant cancers.We successfully synthesized a new compound based on curcumin structure (curcumin analogue) containing boronatoms, namely, CCB-2 and revealed its cytotoxic activities on various cancer cell lines. The compound was simplysynthesized based on aldol condensation using acetone and 4-formylphenyl boronic acid resulted a symmetry CCB-2.The compound was then tested for cytotoxic activities in several cell lines. CCB-2 demonstrated cytotoxic effect onMCF-7/HER-2, MCF-7, RAW 264.7, and 4T1 with IC50 value of 12 µM, 54 µM, 26 µM, and < 10 µM, respectively,while less toxic in fibroblast cells. This compound performed superior cytotoxic against highly metastatic cancer cell,4T1. In addition, CCB-2 induced cells accumulation in G2/M phase, but decreased the accumulation of intracellularReactive oxygen species level in 4T1 cells. All the data suggest that this new compound is promising to be developedas anti-cancer agent rather than for Boron Neutron Capture Therapy-based cancer therapy
ABSTRACT
Objective To investigate the effects of friedelin (terpenoid) and 8-hydroxyisocapnolactone-2-3-diol (coumarin) with concentration 10 μM, 30 μM, and 100 μM on inhibiting mast cells (MCs) degranulation. Methods The investigation was performed in vitro by administering each compound into rat peritoneal MCs and rat basophilic leukemia-2H3 cells followed by activation with 50 μg/mL of compound 48/80 or 1 μM of ionomycin. The concentration of histamine released from each group was measured by a high-performance liquid chromatography-fluorometry system with post-column derivatization using o-phthalaldehyde. Results 8-Hydroxyisocapnolactone-2-3-diol inhibited degranulation of compound 48/80 activated-rat peritoneal MCs with the histamine release percentages of 74.57%, 72.21% and 51.79% when the 10 μM, 30 μM and 100 μM concentrations were used, respectively. Where as about 81% histamine was released by the control group. Degranulation inhibition ability was also observed in ionomycin-activated rat basophilic leukemia-2H3 cells. In contrast, friedelin failed to inhibit degranulation in either cell type. The inhibition of 8-hydroxyisocapnolactone-2-3-diol was not related to the depletion of histamine synthesis as implied by the total histamine measurement. Conclusions These results exhibit the promising of 8-hydroxyisocapnolactone-2-3-diol is a potential parent structure for developing a MCs stabilizer.
ABSTRACT
OBJECTIVE@#To investigate the effects of friedelin (terpenoid) and 8-hydroxyisocapnolactone-2-3-diol (coumarin) with concentration 10 μM, 30 μM, and 100 μM on inhibiting mast cells (MCs) degranulation.@*METHODS@#The investigation was performed in vitro by administering each compound into rat peritoneal MCs and rat basophilic leukemia-2H3 cells followed by activation with 50 μg/mL of compound 48/80 or 1 μM of ionomycin. The concentration of histamine released from each group was measured by a high-performance liquid chromatography-fluorometry system with post-column derivatization using o-phthalaldehyde.@*RESULTS@#8-Hydroxyisocapnolactone-2-3-diol inhibited degranulation of compound 48/80 activated-rat peritoneal MCs with the histamine release percentages of 74.57%, 72.21% and 51.79% when the 10 μM, 30 μM and 100 μM concentrations were used, respectively. Where as about 81% histamine was released by the control group. Degranulation inhibition ability was also observed in ionomycin-activated rat basophilic leukemia-2H3 cells. In contrast, friedelin failed to inhibit degranulation in either cell type. The inhibition of 8-hydroxyisocapnolactone-2-3-diol was not related to the depletion of histamine synthesis as implied by the total histamine measurement.@*CONCLUSIONS@#These results exhibit the promising of 8-hydroxyisocapnolactone-2-3-diol is a potential parent structure for developing a MCs stabilizer.