Liver cancer has become one of the major types of cancer with high mortality and liver cancer is not responsive to the current cytotoxic agents used in chemotherapy. The purpose of this study was to examine the in vitro cytotoxicity of goniothalamin on human hepatoblastoma HepG2 cells and normal liver Chang cells. The cytotoxicity of goniothalamin against HepG2 and liver Chang cell was tested using MTT cell viability assay, LDH leakage assay, cell cycle flow cytometry PI analysis, BrdU proliferation ELISA assay and trypan blue dye exclusion assay. Goniothalamin selectively inhibited HepG2 cells [IC₅₀ = 4.6 (±0.23) µM in the MTT assay; IC₅₀ = 5.20 (±0.01) µM for LDH assay at 72 hours], with less sensitivity in Chang cells [IC₅₀ = 35.0 (±0.09) µM for MTT assay; IC₅₀ = 32.5 (±0.04) µM for LDH assay at 72 hours]. In the trypan blue dye exclusion assay, the Viability Indexes were 52 ± 1.73% for HepG2 cells and 62 ± 4.36% for Chang cells at IC₅₀ after 72 hours. Cytotoxicity of goniothalamin was related to inhibition of DNA synthesis, as revealed by the reduction of BrdU incorporation. At 72 hours, the lowest concentration of goniothalamin (2.3 µL) retained 97.6% of normal liver Chang cells proliferation while it reduced HepG2 cell proliferation to 19.8% as compared to control. Besides, goniothalamin caused accumulation of hypodiploid apoptosis and different degree of G2/M arrested as shown in cell cycle analysis by flow cytometry. Goniothalamin selectively killed liver cancer cell through suppression of proliferation and induction of apoptosis. These results suggest that goniothalamin shows potential cytotoxicity against hepatoblastoma HepG2 cells.

The intercalation of cetirizine into two types of layered double hydroxides, Zn/Al and Mg/Al, has been investigated by the ion exchange method to form CTZAN and CTMAN nanocomposites, respectively. The basal spacing of the nanocomposites were expanded to 31.9 Å for CTZAN and 31.2 Å for CTMAN, suggesting that cetirizine anion was intercalated into Layered double hydroxides (LDHs) and arranged in a tilted bilayer fashion. A Fourier transform infrared spectroscopy (FTIR) study supported the formation of both the nanocomposites, and the intercalated cetirizine is thermally more stable than its counterpart in free state. The loading of cetirizine in the nanocomposite was estimated to be about 57.2% for CTZAN and 60.7% CTMAN. The cetirizine release from the nanocomposites show sustained release manner and the release rate of cetirizine from CTZAN and CTMAN nanocomposites at pH 7.4 is remarkably lower than that at pH 4.8, presumably due to the different release mechanism. The inhibition of histamine release from RBL2H3 cells by the free cetirizine is higher than the intercalated cetirizine both in CTZAN and CTMAN nanocomposites. The viability in human Chang liver cells at 1000 μg/mL for CTZAN and CTMAN nanocomposites are 74.5 and 91.9%, respectively.

An ellagic acid (EA)-zinc layered hydroxide (ZLH) intercalation compound (EAN) was synthesized using zinc oxide as the starting material at two different concentrations of EA: 0.01 and 0.025 mol/L. The resulting EAN have the same basal spacing of 10.4 Å. The cytotoxicity of EAN was determined using a total protein content assay against two normal cell lines (murine fibroblast 3T3 cells and human breast epithelial MCF-10a cells) and two human cancer cell lines (breast cancer MCF-7 cells and liver cancer HepG2 cells). The results suggest that EAN displays cytotoxicity and anti-proliferative activity in MCF-7 and HepG2 cancer cells while impacting less on the growth of normal cells at all concentrations tested. The activities of three caspase enzymes were quantified for both of the cancer cell lines that were treated with the EAN. It was found that caspase-3 and caspase-9, but not caspase-8, were activated, which in turn indicated that apoptosis via the mitochondrial (intrinsic) pathway had taken place. In the MCF-7 and HepG2 cells, the EAN increased DNA fragmentation in a time- and concentration-dependent manner. The morphology of treated cells was also studied, and the EAN-treated HepG2 cells showed more dramatic changes than MCF-7 cells. In addition, we investigated the antimicrobial activity of EAN using minimum inhibitory concentration (MIC) determination by the agar dilution method. It was found that EAN has enhanced antimicrobial activity compared to ellagic acid.