Use of Baicalin-Conjugated Gold Nanoparticles for Apoptotic Induction of Breast Cancer Cells.

Baicalin (BC) has been used for cancer therapy due to its multiple effects as an anti-cancer drug. However, the effective delivery of this molecule to targeted cells is difficult. Gold nanoparticles (AuNPs) conjugated with thiolated beta cyclodextrin (AuNP-S-ß-CD) were used as a delivery vector in this study. Cell viability tests were evaluated by cell counting kit-8 (CCK) and live/dead cell assay. To demonstrate the proliferation inhibition effect on Michigan Cancer Foundation-7 (MCF-7) cells by BC, we analyzed using Hoechst 33342 staining assay and gel electrophoresis. The S-ß-CD conjugated AuNPs were characterized by transmission electron microscopy (TEM), 1H nuclear magnetic resonance ((1)H NMR), and ultraviolet visible (UV-vis) spectroscopy. AuNP-S-ß-CD with approximately 40 µM of BC loaded by inclusion complex showed an inhibition effect on MCF-7 cells by inducing apoptosis. Apoptosis test results were evaluated by analyzing the expression of typical apoptic markers such as cleaved caspase-3, full length caspase-3, and apaf-1 in western blot assay. These results demonstrated that AuNP-S-ß-CD-BC inhibited the proliferation of cancerous MCF-7 cells by inducing apoptosis. These findings suggested that AuNP-S-ß-CD-BC could be a promising agent for chemotherapeutic usage.

Dietary conjugated linoleic acid reduces lipid peroxidation by increasing oxidative stability in rats.

The antioxidative effect of conjugated linoleic acid (CLA) was examined by determining lipid peroxidation and antioxidative enzyme activities. Male Sprague-Dawley rats were fed one of the experimental diets-normal diet, vitamin E-deficient control diet, 0.5% CLA vitamin E-deficient diet, or 1.5% CLA vitamin E-deficient diet for 5 wk. Hepatic thiobarbituric acid reactive substances (TBARS) were increased in the vitamin E-deficient control group, but they were was significantly lowered in the CLA groups. Similarly, hepatic glutathione peroxidase activity was increased in the vitamin E-deficient diet and reduced by CLA supplementation. In addition, CLA caused a significant decrease in superoxide dismutase activity while having no effect on catalase activity. Analyses of the fatty acid composition revealed that dietary CLA was incorporated into hepatic microsomal membrane dose-dependently. Compared to the vitamin E-deficient control, CLA resulted in significantly higher saturated and monounsaturated fatty acids (palmitic and oleic acids) while lowering levels of oxidation-susceptible polyunsaturated fatty acids (linoleic, linolenic, and arachidonic acids) in both plasma and hepatic membrane. The concentrations of plasma cholesterol and triacylglycerol (TG) were lower in the 1.5% CLA group than in other groups. These results suggest that dietary CLA has antiatherosclerotic and antioxidant activity by increasing oxidative stability in plasma and hepatic membrane in the vitamin E-deficient rats.

Stereoselective synthesis of 4'-selenonucleosides via seleno-Michael reaction as potent antiviral agents.

Based on the hypothesis that the bulky selenium atom, with 4p orbitals, can sterically hinder the approach of a cellular kinase to 5'-OH for phosphorylation, 4'-selenonucleosides with one-carbon homologation were designed and synthesized via a novel seleno-Michael reaction, with the stereoselectivity controlled by steric effects. 5'-Homo-4'-selenonucleosides (n = 2) demonstrated potent antiherpes simplex virus (HSV-1) activity, indicating that the bulky selenium atom might play a key role in preventing phosphorylation by cellular kinases, resulting in no antiviral activity.