COH-203, a novel microtubule inhibitor, exhibits potent anti-tumor activity via p53-dependent senescence in hepatocellular carcinoma.

5-(3-Hydroxy-4-methoxyphenyl)-4-(3,4,5-trimethoxyphenyl)-3H-1,2-dithiol-3-one (COH-203) is a novel synthesized analogue of combretastatin A-4 that can be classified as a microtubule inhibitor. In this study, we evaluated the anti-hepatoma effect of COH-203 in vitro and in vivo and explored the underlying molecular mechanisms. COH-203 was shown to be more effective in inhibiting the proliferation of liver cancer cells compared with normal liver cells.

Amyloid β 3-10 DNA vaccination suggests a potential new treatment for Alzheimer's disease in BALB/c mice.

Background: Amyloid β(1-42) (Aβ(42)) peptide vaccination has been proved to be effective in reducing amyloid burden in brain and improving cognitive function in Alzheimer's disease (AD) mouse models. But the phase II trial of Aβ(42) peptide vaccine was halted because of T cell-mediated meningoencephalitis. In this study, a DNA vaccine, p(Aβ(3-10))(10)-CpG, was constructed to test whether it would induce predominant T(H)2 immune response upon immunization of BALB/c mice.

Improving memory and decreasing cognitive impairment in Tg-APPswe/PSEN1dE9 mice with Aβ3-10 repeat fragment plasmid by reducing Aβ deposition and inflammatory response.

The present study aimed to investigate the effects of Aβ3-10 repeat fragment plasmid for the treatment of Tg-APPswe/PSEN1dE9 (Tg) mice. The plasmid pcDNA3.1-(Aβ3-10)10-CpG was constructed and intramuscularly injected into 12-month-old Tg mice.

Design and synthesis of biphenyl derivatives as mushroom tyrosinase inhibitors.

Two new series of biphenyls, analogs of aglycone of natural product fortuneanoside E, were prepared using Suzuki-Miyaura cross-coupling and selective magnesium iodide demethylation/debenzylation, and their mushroom tyrosinase inhibitory activity was evaluated. Most of the 4-hydroxy-3,5-dimethoxyphenyl biphenyl compounds (series II, 20-36) were in general more active than 3,4,5-trimethoxyphenyl biphenyl compounds (series I, 1-19). Structure-activity relationships study showed that monosaccharide substituents, such as glucose, were not necessary and the presence of 4-hydroxy-3,5-dimethoxyphenyl moiety was crucial for inhibitory activity.

In vitro effects of erythromycin on RANKL and nuclear factor-kappa B by human TNF-alpha stimulated Jurkat cells.

The receptor activator of NF-kappaB ligand (RANKL) and its signal downstream nuclear factor-kappaB (NF-kappaB) are critical regulators for immune responses as well as bone remodeling. The present study aimed to examine the effects of erythromycin (EM) on the activation of RANKL, correlation with NF-kappaB expression, proliferation and apoptosis of human Jurkat T cells. Jurkat T cells were pretreated with 100 pmol/l tumor necrosis factor-alpha (TNF-alpha) for 1 h followed by various concentrations of EM for 24 h.

Synthesis of (+/-) homoisoflavanone and corresponding homoisoflavane.

The total synthesis of racemic 3-(4'-methoxybenzyl)-7,8-methylenedioxy-chroman-4-one, a homoisoflavanone with antimycobacterial activity isolated recently from Chlorophytum inornatum, was described. During this research, the first approach for the conversion of homoisoflavonoids into homoisoflavanes was also developed.

Synthesis and antiproliferative in-vitro activity of natural flavans and related compounds.

The total synthesis of natural flavan racemates (+/-) 1, (+/-) 2 and natural flavones 3, 4 had thus been achieved. A straightforward synthetic procedure of flavans via the Pd-C catalyzed hydrogenation/hydrogenolysis of corresponding flavones was developed. Furthermore, the antiproliferative activities of racemic flavans (+/-) 1, (+/-) 2, flavones 3, 4, and five synthetic intermediates toward human SGC-7901, BEL-7402, HeLa, and HL-60 cell lines in vitro were evaluated by MTT assay, and the racemic flavans (+/-) 1 were found to have significant antiproliferative activity against all four cell lines.

Synthesis and anti-proliferative in-vitro activity of two natural dihydrostilbenes and their analogues.

A total synthetic route for two natural dihydrostilbenes with significant cytotoxicity toward human cancer cell lines, (3-(2-(7-methoxybenzo[d][1,3]dioxol-5-yl)ethyl)phenol 1a and 6-(3-hydroxyphenethyl)benzo[d][1,3]dioxol-4-ol 1b), which were isolated from Bulbophyllum odoratissimum Lindl, was developed via Wittig-Horner reaction. The natural products 1a and 1b were obtained in 28% and 20% overall yield, respectively. Additionally, nine analogues, 1c-1k, of the two natural dihydrostilbenes were synthesized and evaluated for their anti-proliferative activity against human SGC-7901, KB and HT-1080 cell lines by MTT assay.

Involvement of mitochondria and caspase pathways in N-demethyl-clarithromycin-induced apoptosis in human cervical cancer HeLa cell.

Aim: To study the mechanisms by which N-demethyl-clarithromycin (NDC) induces human cervical cancer HeLa cell apoptosis in vitro.

Methods: The viability of N-demethyl-clarithromycin-induced HeLa cells was measured by MTT assay. Apoptotic cells with condensed nuclei were visualized by phase contrast microscopy.