A simple access to N-(un)substituted isoquinolin-1(2H)-ones: unusual formation of regioisomeric isoquinolin-1(4H)-ones.

A ligand/additive/Pd-free Cu-mediated coupling/cyclization strategy afforded the first practical, one-pot and general approach towards synthesis of N-(un)substituted isoquinolin-1(2H)-ones. Both the catalyst and the solvent used are recyclable. The use of the Cu reagent in excess led to the unusual formation of regioisomeric and uncommon isoquinolin-1(4H)-ones.

Anti-hyperlipidemic activity of Cucumis melo fruit peel extracts in high cholesterol diet induced hyperlipidemia in rats.

Abstract Cucumis melo Linn. (Cucurbitaceae) fruits have been used, traditionally in Indian traditional system of medicine, for the treatment of various disorders such as liver tonic, cardioprotective, antidiabetic, antiobesity, etc. The aim of the present study was to investigate the possible anti-hyperlipidemic activity of Cucumis melo fruit peel (CMFP) methanolic and aqueous extract in high cholesterol diet induced hyperlipidemia in rats. Treatment with CMFP methanolic and aqueous extract showed significant (P<0.01) reduction in gain in body weight, serum lipid profile like total cholesterol (TC), triglyceride (TG), low density lipoprotein cholesterol (LDL-C) level, atherogenic index and increased the serum high density lipoprotein cholesterol (HDL-C) levels in 28 days treatment when compared to the hyperlipidemic control group. The fecal excretion of bile acids and sterols was further increased upon treatment with CMFP methanolic and aqueous extract and standard drug. Administration of methanolic extract of CMFP at a dose of 500 mg/kg showed higher antihyperlipidemic activity as compared to other extract treated groups. The results concluded that CMFP methanolic extract (500 mg/kg) have potent antihyperlipidemic activity in high cholesterol diet induced hyperlipidemia model and which is equipotent activity when compared with atorvastatin treated group.

Novel solvent-free gelucire extract of Plumbago zeylanica using non-everted rat intestinal sac method for improved therapeutic efficacy of plumbagin.

INTRODUCTION: Various shortcomings of the available methods of extraction of plumbagin from Plumbago zeylanica using non-edible organic solvents coupled with the poor aqueous solubility and low bioavailability called for extracting plumbagin in a water soluble form via a single step technique using hydrophilic lipid Gelucire 44/14. METHODS: Gelucire extract of P. zeylanica (GPZ) was prepared and evaluated for extraction efficiency, High-performance thin layer chromatography (HPTLC) and thermal analysis. In vitro intestinal absorption and bioavailability of plumbagin from GPZ in comparison with that of aqueous (APZ), ethanolic extract (EPZ) and standard plumbagin studied using non-everted rat intestinal sac model. RESULTS: The GPZ showed significantly higher extraction efficiency (3.24±0.12% w/w) compared to ethanolic (EPZ) and aqueous (APZ) extraction, 2.48±0.16% w/w and 0.07±0.02% w/w respectively. GPZ displayed significantly higher Q(30min) (cumulative percentage absorption of plumbagin in 30 min) and lower t(40%) (time required for 40% w/w drug absorption). The flux and apparent permeability coefficient in duodenum and ileum were 2, 3 and 6 fold higher than EPZ, standard plumbagin and APZ respectively. DISCUSSION: Improved therapeutic efficacy of plumbagin may be due to the micellar solubilization and consequent enhanced partitioning of plumbagin through intestinal by Gelucire which was reflected in the in vivo anti-inflammatory study conducted in rats. CONCLUSION: Thus extraction using Gelucire can be proclaimed as an efficient, economic and solvent-free technique for extraction of plumbagin and can be utilized for various clinically important water insoluble phytoconstituents in order to improve their biopharmaceutical properties.

Huge mediastinal mass with minimal symptoms: thymolipoma.

A 35-year-old Indian working in Dubai had come to India for his annual vacation. He presented with a shortness of breath and mild chest discomfort of 3 months duration. Routine investigations gave normal results, except for his chest x-ray that showed homogenous opacity in the right mid and lower zones. Chest CT scan revealed a huge mass with fat and soft tissue involving the anterior mediastinum predominantly on the right side extending into the pericardiac region. The mass was pushing the right hemidiaphragm inferiorly and was compressing the right lung superiorly with atelectasis. The patient underwent surgical excision of the mass and recovered uneventfully. Gross specimen showed an encapsulated mass weighing 2.585 kg. Histopathological examination revealed lobules of mature adipose tissue interspersed with islands of mature thymic tissue and prominent Hassal's corpuscles suggesting thymolipoma. There was no evidence of malignancy.