Synthesis and Characterization of Folic Acid Conjugated Gemcitabine Tethered Silver Nanoparticles (FA-GEM-AgNPs) for Targeted Delivery.

BACKGROUND: Silver nanoparticles (AgNPs) have attracted considerable interest in the medical industry due to their physicochemical properties, small size, and surface plasmon behavior. Their smaller particle size and instability in blood circulation leads to toxicity due to its aggregation as Ag+ ions and accumulation at the deepseated organ. In the present study, we aimed at reducing the toxicity of AgNPs by conjugation with an anticancer drug GEM and to improve their internalization through folate receptors-mediated endocytosis by capping the nanoparticles with folic acid (FA). METHODS: One-pot facile synthesis of FA capped silver nanoparticles (FA-AgNPs) has been achieved by using FA as a reducing agent. FA-AgNPs were mixed with Gemcitabine (GEM) to obtain tethered FA-GEM-AgNPs. Nanoparticles were characterized by Dynamic Light Scattering (DLS), UV-Visible spectroscopy, Transmission Electron Microscopy (TEM), Energy Dispersive X-ray Analysis (EDAX), Selected Area Electron Diffraction (SAED), and Atomic Absorption Spectroscopy (AAS). The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was carried out to determine the cytotoxic effect of the prepared nanoformulations. The apoptotic cell death induced by FA-GEM-AgNPs in breast cancer cells were monitored with Acridine orange (AO)/Ethidium Bromide (EtBr) staining. CONCLUSION: Compared to GEM and AgNPs, FA-GEM-AgNPs showed enhanced cytotoxic effect and internalization in MDA-MB-453 breast cancer cell line. FA-GEM-AgNPs could be an ideal candidate for targeting cancer cells via folate receptor-mediated endocytosis.

Protective effect of wild Corni fructus methanolic extract against acute alcoholic liver injury in mice.

BACKGROUND: In Chinese folk medicine, Corni fructus (C. fructus) has traditionally been used to improve liver function, although the mechanism underlying its activity remains unclear. The aim of the present study was to evaluate the protective effects of wild C. fructus methanolic extract against acute alcoholic liver injury. METHODS: Alcohol was administered to mice for three consecutive days, either alone or in combination with C. fructus methanolic extract (50, 100, or 200 mg/kg body weight/d). Serum and liver tissue were collected from the animals and subjected to biochemical and histopathological analyses. RESULTS: C. fructus significantly alleviated alcohol-induced liver injury by reducing serum alanine aminotransferase, aspartate aminotransferase, and thiobarbituric acid reactive species, inhibiting hydroxyl radicals (•OH), and increasing total superoxide dismutase, glutathione peroxidase, and glutathione in the liver (P < 0.05). In addition, the C. fructus treatment inhibited the expression and activity of cytochrome P450 2E1 (P < 0.05). CONCLUSIONS: C. fructus could be a promising natural substance for ameliorating acute alcohol-induced oxidative stress and hepatic injury.

Barringtonia acutangula improves the biochemical parameters in diabetic rats.

AIM: This study was aimed at evaluating the anti-diabetic activity of the ethanol and aqueous extracts of the leaf material of Barringtonia acutangula in a diabetic animal model. METHODS: The ethanolic and aqueous extracts (250 and 500 mg·kg(-1) body weight) of the leaves of B. acutangula were assessed for antidiabetic activity in a streptozotocin (STZ)-induced diabetes animal model following 21 days of treatment. Glibenclamide (0.6 mg·kg(-1) p.o.) was used as a positive control. The hematological parameters, such as blood glucose level, urea, creatinin, cholesterol, HDL-C, and LDL-C levels were examined. RESULTS: An acute toxicity study (5 000 mg·kg(-1), p.o.) did not produce any symptoms of toxicity. Significant reductions in blood glucose level, and serum total cholesterol and triglyceride levels were noted in animals treated with the extract. The high density lipoprotein-cholesterol (HDLC) level was found to increase as compared with the diabetic control group. CONCLUSION: These results suggest that the leaf aqueous and ethanolic extracts of B. acutangula have anti-diabetic effects. The aqueous extract of B. acutangula produced a similar effect when compared with the ethanol extract. It is proposed that consumption of B. acutangula in some form like tea may help the management of diabetes.

Anti-ulcer activity of Ficus religiosa leaf ethanolic extract.

OBJECTIVE: To evaluate the anti-ulcer activity and acute toxicity of Ficus religiosa (F. religiosa) leaf ethanolic extract in animal models. METHODS: Anti-ulcer activity of F. religiosa ethanolic extract (250 and 500 mg/kg body weight) was studied on stress induced ulcer animal models. Ranitidine was used as standard. The anti-ulcer activity of F. religiosa was evaluated with the help of ulcer area and histopatholgical examination. Preliminary phyto-chemical screening and acute toxicity studies of F. religiosa also carried out. RESULTS: Results showed that the extract treatments prevented ulcer area and gastric secretion in a dose-dependent manner. Administration of 2 000 mg/kg extract did not show any acute toxicity in albino mice. Preliminary phytochemical analysis identified the presence of flavonoids in the ethanolic extract of F. religiosa. CONCLUSIONS: The extract is non-toxic even at relatively high concentrations. The anti-ulcer activity is probably due to the presence of flavanoids.