Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents.

An analogous library of 2-substituted quinoline compounds was synthesized with the aim to identify a potential drug candidate to treat visceral leishmaniasis. These molecules were tested for their in vitro and in vivo biological activity against Leishmania donovani. Metabolic stability of these compounds was also improved through the introduction of halogen substituents. Compound (26g), found to be the most active; exhibited an IC50 value of 0.2 µM and >180 fold selectivity. The hydrochloride salt of (26g) showed 84.26 ± 4.44 percent inhibition at 50 mg/kg × 5 days (twice daily, oral route) dose in L. donovani/hamster model. The efficacy was well correlated with the PK data observed which indicating that the compound is well distributed.

Cereal non-cellulosic polysaccharides: structure and function relationship - an overview.

The non-cellulosic polysaccharides present in cereals (2-8%) are mostly arabinoxylans, (1 --> 3),(1 --> 4)-beta -glucans, pectins and arabinogalactans. Of these, the arabinoxylans are known to absorb large amounts of water and influence significantly the water balance, rheological properties of dough, and the retrogradation of starch and bread quality. (1 --> 3),(1 --> 4)-beta -glucans are known as biological response modifiers (BMS) as they are believed to modulate the immune response. Cereal Pectins and arabinogalactans form a very small amount and do not contribute substantially to the functionality of noncellulosic polysaccharides. Detailed structural investigations on cereal hetero xylans using modern techniques were initiated in the 1990s and still pose a challenge to carbohydrate chemists because of their structural complexity. Nutritionally, they are classified under "unavailable carbohydrates" (dietary fiber) along with lignin and cellulose and are known to have beneficial effects in alleviating disease symptoms such as diabetes, atherosclerosis, and colon cancer. In this review isolation, purification, characterization, structural elucidation, functional, and nutritional attributes of cereal heteroxylans are covered with particular emphasis on recently characterized finger millet arabinoxylans.

Hemicelluloses of ragi (finger millet, Eleusine coracana, Indaf-15): isolation and purification of an alkali-extractable arabinoxylan from native and malted hemicellulose B.

Hemicelluloses (A and B) were isolated from an Indo-African hybrid variety of finger millet (ragi, Eleusine coracana) by extracting the starch-free residue with 10% sodium hydroxide under a continuous stream of nitrogen, and changes in their sugar composition during malting for 96 h were studied. Hemicellulose B, obtained in higher yield from both native (N) and malted (M) flours, was found to be completely soluble in water, richer in uronic acid, and more viscogenic than hemicelullose A. Fractional precipitation of hemicellulose B by ammonium sulfate resulted in four precipitable fractions (F-60, F-70, F-80, and F-100) and a nonprecipitable (NP) fraction varying in their yield and arabinose, xylose, galactose, and glucose contents. A progressive increase in the pentose-to-hexose ratio (P:H) from 0.42:1.0 in F-60 to 1.94:1.0 in NP was observed in native hemicellulose B fractions; however, in malted hemicellulose B the P:H ratio increased from 0.43:1.0 in F-60 to 1.56:1.0 in F-80 and then decreased to 1.13:1.0 in NP. The major fraction, F-70 (N, 44.5%; M, 38.5%), was separated into eight subfractions on DEAE-cellulose by successive elution with water, ammonium carbonate (AC) (0.1, 0.2, and 0.3 M AC), and sodium hydroxide (0.1 and 0.2 M) differing in their yield and neutral sugar composition. The purity of the major glucuronoarabinoxylan fraction (0.1 M AC eluted) was ascertained by Sepharose CL-4B, HPSEC, cellulose acetate, and capillary electrophoresis methods. A significant decrease in the molecular mass of arabinoxylan from 1200 to 1120 kDa upon malting for 96 h is an indication of cell wall degradation by the inducible cell wall degrading enzymes.

Structural analysis of arabinoxylans isolated from native and malted finger millet (Eleusine coracana, ragi).

Structural elucidation of purified arabinoxylans isolated from finger millet and its malt by methylation, GLC-MS, periodate oxidation, Smith degradation, NMR, IR, optical rotation, and oligosaccharide analysis indicated that the backbone was a 1,4-beta-D-xylan, with the majority of the residues substituted at C-3. The major oligosaccharide generated by endo xylanase treatment was homogeneous with a molecular weight of 1865 Da corresponding to 14 pentose residues as determined by MALDI-TOF-MS and gel filtration on Biogel P-2. The structural analysis of this oligosaccharide showed that it contained 8 xylose and 6 arabinose residues, substituted at C-3 (monosubstituted) and at both C-2 and C-3 (disubstituted).

An integrated process for purification of lysozyme, ovalbumin, and ovomucoid from hen egg white.

This article describes an integrated process for simultaneous purification of lysozyme, ovalbumin, and ovomucoid from hen egg white. The crude egg white extract was passed through a cation exchanger Streamline trade mark SP and the bound lysozyme was eluted with 5% ammonium carbonate, pH 9.0, containing 1 M NaCl after elution of avidin. This partially purified lysozyme was further purified 639-fold on dye-linked cellulose beads. Ovalbumin and ovomucoid did not bind to Streamline SP. Ovalbumin could be precipitated from this unbound fraction by 5% trichloroacetic acid, and ovomucoid was removed from the supernatant by precipitation with ethanol. The yields of lysozyme, ovomucoid, and ovalbumin were 77, 94, and 98%, respectively. All the purified proteins showed single bands on sodium dodecyl sulfate polyacrylamide gel electrophoresis. All the steps are easily scalable, and the process described here can be used for large-scale simultaneous purification of these proteins in the pure form.

Evaluation of the antioxidant properties of free and bound phenolic acids from native and malted finger millet (ragi, Eleusine coracana Indaf-15).

Free and bound phenolic acids were isolated from native and malted finger millet (ragi, Eleusine coracana Indaf-15), and their antioxidant properties were evaluated. Protocatechuic, gallic, and caffeic acids were found to be the major free phenolic acids. A 3-fold decrease was observed in protocatechuic acid content, whereas the decrease was marginal in the case of caffeic acid upon 96 h of malting. However, the contents of other free phenolic acids such as gallic, vanillic, coumaric, and ferulic acids increased. Ferulic, caffeic, and coumaric acids were found to be the major bound phenolic acids, and a 2-fold decrease was observed in their contents upon 96 h of malting. The antioxidant activity of a free phenolic acid mixture was found to be higher compared to that of a bound phenolic acid mixture. An increase in antioxidant activity coefficient was observed in the case of free phenolic acids from 770.0 +/- 7.8 to 1686.0 +/- 16.0, whereas the same was decreased from 570.0 +/- 6.0 to 448.0 +/- 4.5 in bound phenolic acids upon 96 h of malting. Therefore, the antioxidant capacity of phenolic acids changes during the malting of ragi.