Enzymatic synthesis of fructose ester from mango kernel fat

317-321Fructose ester as a biosurfactant was successfully synthesized from the fatty acid fraction (olein fraction) of Mango Kernel Fat (MKF). The synthesis was carried out by reaction of sugar and fatty acid fraction in presence of the enzyme lipase from Candida rugosa which acted as a biocatalyst. Phosphate buffer (pH 7.0) was used as the reaction medium to realise maximum enzymatic action. The product was separated from the reaction medium by liquid- liquid extraction. Maximum conversion (36.52 %) was achieved at fructose to olein fraction molar ratio of 1 : 10 (mol/L), with the lipase concentration of 4g/L, at a temperature of 30oC at the end of 3 days. The presence of an ester band in the synthesized ester was confirmed by Fourier Transform Infrared (FTIR) analysis. Identity of the product was further confirmed by NMR studies and a colour identity test for the ester group

Design and Optimization of a Novel Method for Extraction of Genistein

Genistein, an isoflavone, has been demonstrated to promote the health of human beings by reducing the incidence of specific chronic diseases, namely, cancer and atherosclerosis. The present investigation explores a novel method of extraction of genistein from soy source which consists of a bioconversion reaction using fermentation by microorganism namely Streptomyces roseolus NRRL B-5424. In situ bioconversion of genistein glycoside to aglycone was carried out by the microbe. Such methodology has not been reported hitherto. Optimization of upstream and downstream parameters was done for maximum extraction of genistein. Genistein was isolated in a powder form by column chromatography and preparative thin layer chromatography and was characterized using massspectrometry, nuclear magnetic resonance and infrared spectroscopy and its purity determined using high performance liquid chromatography. Genistein was extracted with 91.04% purity and extraction efficiency was 67.01%

Trouble-Free Multicomponent Method for Combinatorial Synthesis of 2‑Amino-4-phenyl-5‑<i>H</i>‑indeno[1,2‑<i>d</i>]pyrimidine-5-one and Their Screening against Cancer Cell Lines

The present study describes an alkaline water–ethanol mediated series of combinatorial synthesis of 2-amino-4-phenyl-5-<i>H</i>-indeno­[1,2<i>d</i>]­pyrimidine-5-one derivatives through sequential multicomponent reaction of 1,3indandione, aromatic aldehydes, and guanidine hydrochloride along with their anticancer evaluation. The effect of sequential addition of the components in the configuration of the desired product has been studied by UV–visible absorption spectroscopy. The synthetic method obeys most of the green chemistry principles in regard to high atom economy and greener, nontoxic, and noncarcinogenic solvent system (water–ethanol). The selected synthesized compounds have been screened against the human breast cancer cell line MCF7, human colon cancer cell line HT29, and normal viro monkey cell line, out of which 2-amino-4-(4-meth­oxy­phenyl)-5<i>H</i>-indeno­[1,2-<i>d</i>]­pyrimidin-5-one showed significant potency toward human breast cancer cell line (MCF7)

Development and Evaluation of Lorazepam Microemulsions for Parenteral Delivery

The objective of this investigation was to develop lorazepam (LZM) microemulsions as an alternative to the conventional cosolvent based formulation. Solubility of LZM in various oils and Tween 80 was determined. The ternary diagram was plotted to identify area of microemulsion existence and a suitable composition was identified to achieve desired LZM concentration. The LZM microemulsions were evaluated for compatibility with parenteral fluids, globule size, in vitro hemolysis and stability of LZM. Capmul MCM demonstrated highest solubilizing potential for LZM and was used as an oily phase. LZM microemulsions were compatible with parenteral dilution fluids and exhibited mean globule size less than 200 nm. The in vitro hemolysis studies indicated that microemulsions were well tolerated by erythrocytes. The LZM microemulsions containing amino acids exhibited good physical and chemical stability when subjected to refrigeration for 6 months

Downscaling Drug Nanosuspension Production: Processing Aspects and Physicochemical Characterization

In this study, scaling down nanosuspension production to 10 mg of drug compound and evaluation of the nanosuspensions to 1 mg of drug compound per test were investigated. Media milling of seven model drug compounds (cinnarizine–indomethacin–itraconazole–loviride–mebendazole–naproxen–phenytoin) was evaluated in a 96-well plate setup (10, 20, and 30 mg) and a glass-vial-based system in a planetary mill (10, 100, and 1,000 mg). Physicochemical properties evaluated on 1 mg of drug compound were drug content (high-performance liquid chromatography), size [dynamic light scattering (DLS)], morphology (scanning electron microscopy), thermal characteristics (differential scanning calorimetry), and X-ray powder diffraction (XRPD). Scaling down nanosuspension production to 10 mg of drug compound was feasible for the seven model compounds using both designs, the planetary mill design being more robust. Similar results were obtained for both designs upon milling 10 mg of drug compound. Drug content determination was precise and accurate. DLS was the method of choice for size measurements. Morphology evaluation and thermal analysis were feasible, although sample preparation had a big influence on the results. XRPD in capillary mode was successfully performed, both in the suspended state and after freeze-drying in the capillary. Results obtained for the latter were superior. Both the production and the physicochemical evaluation of nanosuspensions can be successfully downscaled, enabling nanosuspension screening applications in preclinical development settings