Human Cancer Cell Lines SGC-7901 Research Articles

Design, synthesis and biological evaluation of 4-piperidin-4-yl-triazole derivatives as novel histone deacetylase inhibitors.

Histone deacetylase is an important member of epigenetics and a well validated target for anti-cancer drug discovery. In this study, we designed and synthesized a series of twenty-one novel hydroxamic acid-based histone deacetylase inhibitors with 4-piperidin-4-yl-triazole as the core skeleton. Most target compounds displayed excellent inhibition rates toward histone deacetylases at the concentration of 1 μM. Among them, the inhibition rates of two compounds MH1-18 and MH1-21 exceeded 90%. Furthermore, these two compounds selectively inhibited the activity of histone deacetylase 6 with low IC50 values. The high potency of them toward histone deacetylase 6 was rationalized by molecular docking studies. We found that MH1-18 and MH1-21 moderately inhibited the proliferation of four human cancer cell lines SGC-7901, NCI-H226, MCF-7, and HL-60. However, MH1-21 showed potent efficacy in suppressing the migration of MCF-7 cells. Results obtained in the current study shed light on designing potent HDAC6 inhibitors as anti-cancer agents.

Transformation of ginsenoside Rh4 and its aglycone from the total saponins of stems and leaves of Panax ginseng by Aspergillus tubingensis

Rare ginsenoside Rh4 and its aglycone are present in low levels in Panax ginseng. This study focused on achieving ginsenoside Rh4 and its aglycone by microbial transformation of the total saponins of stems and leaves of P. ginseng (TSSLG). A total of 78 fungal strains isolated from the rhizosphere soil of P. ginseng, and one of them, Aspergillus tubingensis, was found to be capable of biotransformation of TSSLG to ginsenoside Rh4 and its aglycone with high efficiency, especially the content of ginsenoside Rh4 aglycone was enhanced 100 folds over than that in the original TSSLG. Compared with ginsenoside Rg3 (named ShenYi capsule as antitumor drug in China), ginsenoside Rh4 aglycone exhibited stronger antitumor activity against human cancer cell lines SGC-7901, KB-A-1 and HT-1080. The possible biotransformation pathways of ginsenoside Rh4 and its aglycone were speculated according to the chemical structures. The anticancer binding-target, myeloid cell leukemia 1 protein (MCL-1), was explored using molecular docking analysis and the possible combination mechanism was discussed.

Cytotoxic triterpenoid saponins from Clematis tangutica

Eight previously undescribed oleanane-type triterpenoid saponins, clematangoticosides A-H, together with eight known saponins, were isolated from the whole plants of Clematis tangutica (Maxim.) Korsh. Their structures were elucidated by extensive spectroscopic analysis, in combination with chemical methods (acid hydrolysis and mild alkaline hydrolysis). Clematangoticosides D-G were found to be unusual 23, 28-bidesmosidic glycosides. The cytotoxic activities of all of the isolated saponins were evaluated against the four human cancer cell lines SGC-7901, HepG2, HL-60 and U251MG. Clematoside S, sapindoside B, kalopanax saponin A, and koelreuteria saponin A exhibited cytotoxicity against all of the test cancer cell lines with IC50 values in the range of 1.88–27.20 μM, while clematangoticoside D and F showed selective cytotoxicity against SGC-7901 with IC50 values of 24.22 and 21.35 μM, respectively.