ABSTRACT
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.
ABSTRACT
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.
Subject(s)
Antiviral Agents/chemical synthesis , Antiviral Agents/pharmacology , Dideoxynucleosides/chemical synthesis , Dideoxynucleosides/pharmacology , Herpesvirus 1, Human/chemistry , Organoselenium Compounds/chemical synthesis , Organoselenium Compounds/pharmacology , Simplexvirus/drug effects , Thymidine Kinase/chemistry , Thymidine Kinase/pharmacology , Antiviral Agents/chemistry , Dideoxynucleosides/chemistry , Herpesvirus 1, Human/drug effects , Molecular Structure , Nucleic Acid Conformation , Organoselenium Compounds/chemistry , Phosphorylation , StereoisomerismABSTRACT
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.
