Synthesis of (4R)-thiazolidine carboxylic acid and evaluation of antioxidant potential.

We report here the synthesis as well as antioxidant activity of a series of 2-aryl thiazolidine-4-carboxylic acids, including two novel derivatives. They were synthesized by nucleophilic cyclic condensation of L-cysteine hydrochloride with a range of aromatic aldehydes. Their in vitro antioxidant activity was evaluated by DPPH radical scavenging assay. It was observed that the aromatic substituent at C-2 of thiazolidine ring effects the antioxidant potential of the thiazolidine derivatives. The nature and position of the substituents on aromatic ring were correlated with antioxidant activity. Compounds with -OCH3 group on aromatic ring showed a better radical scavenging property than the other groups such as -Cl, -F, and -NO2. The presence of phenyl ring thus enhanced radical scavenging activity.

Molecular docking, synthesis and biological evaluation of phenacyl derivatives of 9-aminoacridine as anti-Alzheimer's agent.

Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder mainly characterized by progressive deterioration of memory and impaired cognitive function. The most promising approach for symptomatic relief of AD is to inhibit acetylcholinesterase (AChE). On the basis of this approach in-house library of 9-aminoacridine derivatives were constructed and allowed to docked against human acetylcholinesterase (hAChE) (PDB ID: 4EY7), using MOE 2018.01 and PyRx 0.9.2 (AutoDock Vina). Top ranked and best fitted molecules were synthesized by targeting the 9-amino group of aminoacridine with substituted phenacyl halides. Anti-Alzheimer's potential was checked by in vitro AChE inhibition, antioxidant activity (DPPH scavenging ability) and fibril disaggregation. Subjected ligands suggested as promising multitargeted candidate with pronounced results in term of IC50 values (AChE inhibition 2.400-26.138µM), however, none of them showed potential towards fibril inhibition.

Potential nutraceutical benefits of basmati rice bran oil as analgesic, anti-inflammatory and anti-arthritis.

Numerous nutraceutical applications have been explored during the last decades. The present study is based on extraction of oil from super kernel basmati rice which has shown effective analgesic, anti- inflammatory, and anti-arthiritic activities. The feeding experiments on male Wister rats and female Sprague-dawley (SD) rats have elaborated the therapeutic value of variety of bioactive components including γ-oryzanol present in the oil.

Synthesis, Characterization and evaluation of antioxidant potential of 2, 6-diphenylpiperidine-4-one compounds and their novel imine derivatives.

In search of potent molecules having antioxidant activity the present work was designed to synthesize 2, 6-diphenylpiperidine-4-one compounds (1a and 1b) and their imine derivatives (2a, 2b, 3a, and 3b). Compounds 1a and 1b were synthesized by Mannich condensation reaction. The method was found to be simple, convenient with high yield and products were easily separated. Compounds 1a and 1b serves as an intermediate for the preparation of highly functionalized novel imine derivatives. Oxime (2a, 2b) and carbothioamide (3a, 3b) derivatives of 1a and 1b compounds were produced by condensation reaction with hydroxyl amine hydrochloride and thiosemicarbazide respectively. These compounds were characterized by IR, EI-mass and 1HNMR spectroscopy. The antioxidant activity of compounds was analyzed by 1, 1- dipheny1-2-picrylhydrazyl (DPPH) assay method. It was found that substituted aryl derivatives containing phenol and methoxy groups (1b, 2b and 3b) showed better antioxidant activity (IC50 values rang from 1.84-4.53µg/ml) than unsubstituted aryl derivative (1a, 2a and 3a) (IC50 rang from 6.46-11.13µg/ml). Compound 1b exhibited excellent antioxidant activity (IC50 1.84±0.15µg/ml) comparable to standard ascorbic acid (IC501.65± 0.16µg/ml).

Purple Wheat: Food Development, Anthocyanin Stability, and Potential Health Benefits.

Colored wheats such as black, blue, or purple wheat are receiving a great interest as healthy food ingredients due to their potential health-enhancing attributes. Purple wheat is an anthocyanin-pigmented grain that holds huge potential in food applications since wheat is the preferred source of energy and protein in human diet. Purple wheat is currently processed into a variety of foods with potent antioxidant properties, which have been demonstrated by in vitro studies. However, the health impacts of purple wheat foods in humans still require further investigations. Meanwhile, anthocyanins are vulnerable molecules that require special stabilization treatments during food preparation and processing. A number of stabilization methods such as co-pigmentation, self-association, encapsulation, metal binding, and adjusting processing conditions have been suggested as a means to diminish the loss of anthocyanins in processed foods and dietary supplements. The present review was intended to provide insights about purple wheat food product development and its roles in human health. In addition, methods for stabilizing anthocyanins during processing were briefly discussed.

The Impact of Innovative Plant Sources (Cordia myxa L. Fruit (Assyrian Plum) and Phoenix dactylifera L. Biowaste (Date Pit)) on the Physicochemical, Microstructural, Nutritional, and Sensorial Properties of Gluten-Free Biscuits.

The gluten-free products available on the markets are deficient in bioactive compounds and high in cost. The present study is designed to develop gluten-free biscuits with enhanced nutritional properties. The gluten-free biscuits are formulated with rice flour (RF) incorporated with Assyrian plum fruit flour (APF) and bio-waste date-pit flour (DPF) according to the following ratios; RF:DPF:APF (100:0:0)/T0, (90:5:5)/T1, (80:10:10)/T2, and (70:15:15)/T3. The results demonstrate that flour blends with different concentrations of APF and DPF incorporated in RF have high contents of protein, damaged starch, crude fiber, ash, phytochemicals, and antioxidants in contrast to 100% RF, which shows the lowest values for all these parameters. The pasting properties of the flour blends reveals that the values of peak, final, breakdown, and setback viscosities reduce from T1 to T3. Similarly, a differential scanning calorimeter reveals that the phase transition temperature of the flour blends decreases with the increasing amylose content. Moreover, the scanning electron microscopy of the biscuit samples shows a positive contribution of APF and DPF for the development of the desired compactness of the structure due to the leaching of amylose content from the starch. The total phenol content (TPC) and total flavonoid content (TFC) increase from 38.43 to 132.20 mg GAE/100 g DW and 18.67 to 87.27 mg CE/100 g DW, respectively. Similarly, the antioxidant activities of biscuits improved. The protein and fiber contents of the biscuits increased from 10.20 to 14.73% and 0.69 to 12.25%, respectively. The biscuits prepared from T3 resulted in a firmer texture with a reduced spread ratio. However, the formulation of T1 and T2 biscuit samples contributed to desirable physical and sensory properties. Therefore, the addition of DPF and APF to RF is a sustainable way to make gluten-free biscuits as they provide adequate amylose, damaged starch, and fiber content to overcome the essential role of gluten in the baked product with nutraceutical properties.