Current Bioactive Compounds - Volume 16, Issue 4, 2020

Background: Quinazolines and quinazolinones constitute a major class of biologically active molecules both from natural and synthetic sources. We will limit this review to compounds possessing the 4(3H)-quinazolinone skeleton, which is found in compounds displaying significant biological and pharmacological properties. The molecular design of potential lead compound is still a key line of approach for the discovery and development of new chemical entities. A combination of two or more chemical moieties into one is a common approach of operation and this can most likely result in the improvement of pharmacological activity and removal of unwanted side effects. Methods: We undertake search for peer-reviewed and research literature on quinazolinone moiety using different tools of literature survey. The quality of superior papers was assess using standard tools. The distinctiveness of screened papers was shorted and high-quality content was reorganiz and written in own language. Results: The review will be expressed in two main sections, the first section will be related to synthetic procedures and the second section includes the biological importance of Quinazoline derivatives. Total hundred (100) to one hundred and ten (110) research papers ware searched. Out of these, seventy-eight papers were included in the review, the majority of research papers were from international journals. Fifty fours papers defined the different synthetic schemes considering the general strategies using orthosubstituted anilines such as 2-aminobenzoic acid (anthranilic acid) and its analogues, or isatoic anhydride as starting materials, which are condensed with acid chlorides, imidates or aldehydes. Microwave irradiation was also proven to be very useful to improve the yields, and in particular, it has been successfully applied to the Niementowski procedure involving the fusion of anthranilic acid with formamide. The remaining part of the review focuses on biological importance of the 4(3H)-quinazolinone scaffold as therapeutic agents and a broad range of activities like antibacterial, antifungal, antiviral, anticonvulsant, antitumor, antihypertensive, analgesic and anti-inflammatory agents has been highlighted. Conclusion: The present review focuses on simplified, efficient and widespread literature of the methods of synthesis and diverse pharmacological activities of quinazoline and its derivatives have been highlighted.

Background: Croton species are widely spread around the world, and present a varied chemical composition distributed in many classes of secondary metabolites, such as terpenoides, alkaloids, phenolic compounds and phenylpropanoids. These compounds can be obtained by different extraction methods, and more recently, with supercritical fluids. The crude and isolated extracts may have applications due to their biological activities in animals and humans. Methods: The text was written based on literature data from 1996 onwards. Results: The research showed in a concise way the botanical and taxonomic aspects of Croton and the success of its application is in studies related to the biological activities of the plant parts. It was also related to the chemical composition of its extracts and isolated compounds, obtained by many methods. Conclusion: In summary, the review feature studies reported the use of extracts and isolated Croton compounds due to their biological effects with antioxidant, antimicrobial, anti-inflammatory, neuroprotective, antitumor, anticancer, cytotoxic, insecticidal and allelopathic activities, with potential application in food, cosmetics, pharmaceuticals, and agrochemicals products.

Background: Nitric oxide (NO) is known for decades to play a crucial role in many physiological processes: this includes acting as an anti-microbial mediator/agent, vasodilator, inhibitor of platelet aggregation, immune modulator, and tissue regeneration via regulation of epidermal cell migration, collagen deposition and cytokine/chemokine microenvironment, making it a key player in wound healing. Methods: In order to demonstrate the therapeutic benefits as well as the safety of a NO wound irrigation solution, a broad literature review summarizing efficacy and safety data was conducted. Results: Beneficial effects on wound healing have been demonstrated in several non-clinical and clinical studies. The combination of NO and wound rinsing seems to be a promising approach in terms of improved wound healing of chronic wounds. Conclusion: Based on the results, no safety concerns are expected for a daily 15 minutes use of a NOgenerating rinsing solution system for wound irrigation of diabetic foot ulcers in adults.

Background: Microalgae are the source of various compounds with high potentials for being used in different industries. The production of such compounds can be raised under extreme conditions. In the present study, four cyanobacteria and one coccoid green alga were examined which were isolated from hot springs in high background radiation areas in Ramsar, a city in the north of Iran. Methods: Cadmium adsorption from aqueous solution, response towards cadmium stress, antioxidant activity, total phenolic compound and drought tolerance were investigated in these microalgae. Results: The results showed that these extremophile microalgae contain valuable biological compounds which can be useful in remediation of heavy metals from contaminated water and soils and pharmaceutical applications. The unicellular cyanobacterium, Chroococidiopsis thermalis IBRC-M50002, was the best strain with the highest biological activity in various testes such as cadmium adsorption (225 mg g-1), cadmium tolerance stress (100 mg ml-1), antioxidant activity (IC50= 18 μg mg-1) and total phenol content (100 μg ml-1). The coccoid green algae Grasiella emersonii IBRC-M50001, also exhibited significant antioxidant activity (IC50=10 μg mg-1) and total phenol compound (116 μg ml-1), but its cadmium adsorption, tolerance at cadmium stress and desiccation were lower than Chroococidiopsis thermalis. Conclusion: HBRAs microalgae, isolated from extreme conditions, are useful microorganisms for the production of bioactive substances and natural antioxidants. In other words, they exhibited high capacity to be used in pharmaceutical, industrial and commercial applications.

Background: Triclopyr(Dow-503), whose commercial name was green grass, was an internal absorption and selective novel herbicide, developed by Dow agricultural sciences using the basic structure of 2,4-D. Triclopyr was suitable for preventing broadleaf weeds for removing shrubs, maintaining fireproof lines, raising pine trees and forest areas. Moreover, it could be used in paddy fields to prevent some broad-leaved weeds at the dose of 150-500g/hm. Methods: Two novel Triclopyr derivatives were synthesized based on the structure of commerical herbicide Triclopyr. Their structures were confirmed by 1H NMR melting point and elemental analysis. The preliminary bioassay were also evaluated. Results: The preliminary bioassay results showed that the title compounds had some herbicidal activities at the dosage of 150 g/hm2.The compound 1 and 2 show the 100% inhibition against three kinds of test weeds. Further test revealed that compound 2 showed the 100% inhibition against the Amaranthus. The safety test for crop revealed that the compound 2 was safe for paddy at the dosage of 150 g/hm2. Conclusion: The two compounds can be used as the leading compounds with certain optimized value.

Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of novel scaffolds are described by variation in therapeutic effects of parent molecule. The structure variants were characterized by using a blend of spectroscopic 1H NMR, 13C NMR, IR, Mass and chromatographic techniques. Results: When tested for in vitro antibacterial and anticancer activities, several of these compounds showed good activities. The target compounds 9b, 9a and 9e exhibited a high degree of anticancer activity against human colon cancer cell line Caco-2 and human breast cancer cell line MDAMB231. Further, 9a, 9b, 9d, and 9h showed better activity towards four medically relevant organisms; Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Klebsiella Species compared to CPF. In the present investigation, cheminfomatics tools Molinspiration, 2003 and MolSoft, 2007 for the prediction of insilico molecular properties and drug likeness for the target compounds 9a-h was evaluated and positive results were observed. Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antibacterial/ anticancer agents.

Background: A green and efficient synthetic methodology for a wide family of Nacylhydrazones (yields: 42-76%) using microwave irradiation is described, as well as their full characterization. Their potential antineoplastic activity was evaluated in vitro via EMSA by testing protein- DNA interactions. Among the 11 compounds tested, N-acylhydrazone derivative 5 bearing a hydroxyl group, showed the highest affinity to bind and inhibit the hnRNP K KH3 domain. Docking simulations of compound 5 showed three possible modes of interaction between the KH3 domain of hnRNP K protein and compound predict. The N-acylhydrazones are knows as powerful chemical entities for Medicinal Chemistry, since it has been identified in a huge number of hit and lead compounds that act on various types of molecular targets, including in tumorigenesis processes. Objective: We evaluated their potential ability to inhibit the KH3 domain of the hnRNP K protein binding to single stranded DNA (ssDNA). Furthermore, a docking simulation was performed for the newly synthetized compounds to evaluate their interactions between proteins and N-acylhydrazine derivative. Methods: The N-acylhydrazone derivatives were synthetized through three reaction steps, from a simple and commercial substrate, using microwave irradiation as a green energy source. The N-acylhydrazone derivatives ability to bind with the hnRNP K protein was evaluated via EMSA by testing protein-DNA interactions. The docking simulations were performed in a Gold 5.2.2 software using 100 conformers, 10.000 operations, 95 mutations and 95 crossovers. Results: Eleven new N-acylhydrazone derivatives were synthetized using microwave showing yields between 42% and 76%. Among the eleven compounds tested, compound 5 was shown to be most capable to prevent the natural binding of hnRNP K protein to the oligonucleotide. Regarding the docking simulation, compound 5 can bind to the main binding residues of KH3 domain and compete with the natural ligand ssDNA of this protein. Conclusion: A green and efficient synthetic methodology for a wide family of N-acylhydrazones (yields: 42-76%) using microwave irradiation is described, as well as their full characterization. Their potential antineoplastic activity was evaluated in vitro via EMSA by testing protein-DNA interactions. Among the 11 compounds tested, N-acylhydrazone derivative 5 bearing a hydroxyl group, showed the highest affinity to bind and inhibit the hnRNP K KH3 domain. Docking simulations of compound 5 showed three possible modes of interaction between the KH3 domain of hnRNP K protein and compound predict.

Background: In the present study, a series of substituted naringenin derivatives was synthesized by Claisen–Schmidt reaction using grinding technique. Methods: Synthesized compounds were characterized on the basis of Fourier-Transform Infrared Spectroscopy (FTIR), proton Nuclear Magnetic Resonance (1H NMR), Mass Spectroscopy (MS) and elemental analysis. These derivatives were screened for anticancer activity on breast (MCF-7) and colon (HT-29) cell lines using Sulforhodamine B (SRB) colorimetric assay. Results: Results displayed improved inhibitory concentration (IC50) values of naringenin derivatives. IC50 values of 3(4-chlorobenzylidene)-5,7-dihydroxy-2(4-hydroxyphenyl)chroman-4-one are 10.35 μM (MCF-7) & 12.03 μM (HT-29), which is most potent compound in the series. These finding confirms the suitability of 3-substituted naringenin in improving the anticancer effect. Conclusion: Due to the intense interest in the development of drugs capable of inhibiting cancerous cells, naringenin derivatives may represent important precursor molecules for the therapeutic armamentarium of colon and breast cancer. Further structural modification in these structures will be of interest and may result in compounds having a better anticancer activity.

Background: Biosynthesis of nanoparticles from aqueous leaf extract of ‘Selaginella bryopteris’ is a green chemistry approach and is considered to be one of the most efficient methods as it is devoid of toxic chemicals as well as provides natural capping agents for the stabilization of synthesized nanoparticles. ‘S.bryopteris’ also known as ‘Sanjeevani’ (in India), is thought to be prospective natural resource that possesses extraordinary pharmaceutical potential. Objective: S. bryopteris is exclusively native to India and has already been known for its expression of stress-associated genes and high levels of protective metabolites of sugars, phenolic compounds, and polyols. Its potential as an antibacterial agent is being elucidated. Methods: Different leaf extract volumes, silver nitrate (AgNO3) concentrations, and reaction time were investigated separately and the optimal conditions for the synthesis of AgNPs were suggested. The resulting AgNPs were characterized by various techniques like Ultraviolet-Visible (UV-Vis) Spectroscopy, Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and XRay Diffraction (XRD). Antibacterial assays were carried out by using both agar disk and well diffusion method. Result: The AgNPs synthesized in this process were found to have efficient antimicrobial activity against both Gram-positive as well as Gram-negative bacteria. The antibacterial efficacy of S. bryopteris was consciously tried on uropathogenic Escherichia coli (Gram-negative bacteria) and Bacillus megaterium (Gram-positive bacteria) which have the self-limiting food poisoning potential along with opportunistic uropathogenic bacterial strains namely Proteus mirabilis (Gram-negative bacteria) and a non-pathogenic Micrococcus luteus (Gram-positive bacteria) for comparison. Conclusion: S. bryopteris mediated silver nanoparticles’ synthesis is attempted for being cost-effective, eco-friendly and safe for human therapeutics.

Background: Immunomodulators could alter the activity of the immune system. Most of the synthetic chemotherapeutic agents are immune suppressants and produce side effects. Immunomodulators derived from plants are used as general adaptogens and immune strengtheners without undesired effects. Methods: Present study established the mode of immunostimulatory action of punarnavine alkaloid (PA) isolated from Boerhaavia diffusa Linn. root by examining various parameters. PA was separated from B. diffusa and its acute toxicity was studied by up-down regulation method. Immunomodulatory activity of PA was determined in Albino mice by observing its effect on organ weight (liver, spleen, thymus and kidney), expression of cytokines, bone marrow cellularity and alpha-esterase positive cells. Plaque Forming Assay (PFA), Delayed Type Hypersensitivity (DTH), and phagocytosis activity were also carried out to support the effect of PA. PA did not exhibit any toxic effect in mice. Results: In DTH study, the foot pad thickness due to influx of mononuclear cells at the site of inoculation was distinctly increased in PA treated mice. PA enhanced the phagocytic activity of the polymorphonuclear cells by increasing the engulfment of the Candida cells thereby stimulating a non-specific immune response. PFA confirmed that PA treatment could elevate the humoral immune response due to the synthesis of antibody which in turn is responsible for the enhancement of macrophages and Blymphocyte subsets. The significant increase in the number of α-esterase positive cells and bone marrow cellularity due to immunomodulatory effect indicated the proliferation of stem cells. Different organ weight was also markedly improved by PA treatment compared to SRBC sensitized group. Further, in real time PCR studies treatment of PA significantly increased IL- 7, IL- 10, IL-12a and IL-12b mRNA gene expression. Conclusion: From the above findings it can be concluded that PA could be developed as a potent immunomodulatory agent.

Background: Diet-disease linkages are getting immense attention of the scientific fraternity. In this regard, red cabbage was assessed against hypercholesterolemic and related oxidative damage. Nowadays, plant bioactives are gaining immense attention among the masses to mitigate lifestyle related malfunctions. Considering phytochemistry and cost-effectiveness, the current project was designed to probe the bioefficacy red cabbage against hypercholesterolemic diet related oxidative stress in the liver. Methods: The red cabbage and its aqueous extract were tested on male white New Zealand rabbits for 12 weeks. Two studies were conducted based on dietary regimens; normal and hypercholesterolemic diet (1% cholesterol). At termination, overnight fasted rabbits were sacrificed to assess serum specific and tissues biomarkers of hepatic oxidative stress alongside, hepatosomatic index and histopathology were studied. Results: In hypercholesterolemic diet induced oxidative stressed rabbits, the supplementation of red cabbage and its aqueous extract suppressed the leakage of liver functioning enzymes in sera up to 15.63 and 12.70% (alanine transaminase), 13.88 and 9.55% (alkaline phosphatase), 12.96 and 8.82% (γ-glutamyl transferase) and 10.77 and 6.15% (total bilirubin). Besides, the respective diets also portrayed considerable reduction in hepatic lipid peroxidation up to 29.60 and 23.63% thus improved endogenous antioxidant enzymes; superoxide dismutase (17.97 and 15.92%) and catalase (24.39 and 20.98%). Furthermore, hepatosomatic index expounded a significant impact of treatments on oxidative stressed rabbits alongside mild degree of fibrotic and necrotic changes in their hepatic parenchyma was rectified by red cabbage, whereas red cabbage extract demonstrated slower rate of amelioration. Conclusion: In the nutshell, dietary inclusions based on red cabbage have shown higher restorative potential against hepatic oxidative stress as compared to red cabbage aqueous extract.

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.

Background: Atractylis gummifera is a cosmopolitan species that is particularly abundant in the Mediterranean regions. It has been used to treat many diseases, including intestinal parasites, ulcers, snakebite poisoning, hydrops and drowsiness. As part of our research program on natural compounds with biological activities, the objective of this study was to determine for the first time the chemical composition and biological activities of essential oils of Atractylis gummifera during beginning of the vegetative cycle (March), beginning of the flowering stage (April) and full bloom (May/June). Methods: The essential oils were obtained by means of hydrodistillation and its components were analyzed using gas chromatography and mass spectrometry (GC/MS). The antioxidant properties were evaluated using two different methods i) Radical scavenging activity (DPPH) and ii) β-carotene bleaching assay. Whereas, the antifungal activity of the essential oils was investigated against five plant fungi. The fumigation toxicity of essential oils was evaluated against adults of Bactrocera oleae better known as the olive fly. Results: The essential oil produced from the plant taken at the beginning of the vegetative cycle (March) had a high level of non-terpenic aliphatic compounds. On the other hand, the essential oil obtained during the period from the beginning of the flowering stage (April) showed that its proportion of non-terpene compounds decreased and that of sesquiterpene compounds increased. Finally, the essential oils obtained during the period from full bloom (May/June) consisted mainly of acetylene compounds such as carlina oxide and 13-methoxy carlina oxide. The results showed that essential oils from plants at full bloom presented interesting antioxidant and antifungal properties, while essential oil produced from plants at the beginning of the vegetative cycle (Mars) and at the beginning of the flowering stage (April) had better insecticidal activity. Conclusion: The data presented here constitutes new findings in the field of the chemical characterization and biological potential of A. gummifera.

Background: 1,2,4-Triazoles are important five-membered heterocyclic scaffolds due to their extensive biological activities. These products have been an area of growing interest to many researchers around the world as of their diverse biological activities including antifungal and antibacterial activity against broad spectrum of microbial pathogens. Methods: A series of 2-((1H-1,2,4-triazol-1-yl)methyl) derivatives was designed, synthesized and evaluated as antifungal agents against five plant pathogenic fungi (Alternaria tennis, Botryodiplodia theobromae, Fusarium moniliforme, Fusarium oxysporum and Helminthosporium turcicum) to meet the urgent need of new antifungal agents with improved activity and broader spectrum. In silico studies including pharmacophore modeling, virtual screening, drug-likeness analysis and ADMET prediction were examined. In addition, the elucidation of the activity is based on the molecular docking to the active site of the Sterol 14α-Demethylase Cytochrome P450 (CYP51) was investigated. Results: The results of antifungal activity indicated that the compounds containing tert or sec-butyl as hydrophobic substituents on a phenyl ring significantly increased the activity (compounds 4, 5 and 6) with EC50 in the range of 8-84 mg/L of all tested fungi. The pharmacophore modeling produced an accurate projecting model (Hypo 1) from these derivatives. The superlative Hypo1 consists of three features counting two hydrogen bond acceptors (HBA) and one hydrophobic (HYD). The docking results showed approximately a similar binding degree at the active sites of the fungal enzyme (CYP51) as a standard fungicide penconazole. Conclusion: According to data obtained, some derivatives, especially those with tert or sec-butyl substituents on the phenyl ring, were more potent against phytopathogenic fungi. These compounds (e.g., 4, 5, and 6) should develop into new potential fungicides as a desirable activity.

Background: Amongst the quinolone core structures, 8-hydroxyquinoline (8-HQ or quinolinol) stands out as the greatest frequently used therapeutic moietiy. This includes the most critical molecules in medicinal chemistry. Quinolinol remains a broad-spectrum ligand capable of chelating to a large number of metal ions. Method: The synthesized quinolinols Mannich bases were screened for their in vitro antimicrobial activity against Staphylococcus aureus (ATTCC 6538), Escherichia coli (ATTCC 7839), Klebsiella pneumonia (ATCC10131). The antifungal activity of the prepared compounds was assessed against Candida albicans (10231), Aspergillus niger and Penicillium sp. The antioxidant activity of the established compounds was assessed by means of α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method. Results: The antimicrobial outcomes indicated that all the synthesized compounds excluding 5 and 9b displayed reasonable antibacterial activity against Staphylococcus aureus (ATTCC 6538) and Escherichia coli (ATTCC 7839) with an inhibition zones ranging from 13 to 23 mm. However, in the case of Klebsiella pneumonia (ATCC10131) only compound 6 did not show any activity. The results also indicated that compounds 2b and 3 were the most potent antibacterial compounds against the verified strains with minimum inhibitory concentration (MIC) values ranging from 0.05 to 0.5mg/ml. In the antifungal assay, all compounds showed good activity against Candida albicans (10231) except compounds 5 and 9b. However, in the case of Aspergillus niger and Penicillium sp. only compounds 2b and 3 showed good activity. In the antifungal assay, MIC values for compounds 2b and 3 ranged from 0.25 to 2.5 mg/ml against the specified fungal strains. The antioxidant activity was assessed using the DPPH scavenging activity method. The results indicated that 2b was the most active among all tested compounds, with almost double the antioxidant activity as compared with that of trolox (positive control). Conclusion: In this work, we describe the synthesis of new Mannich bases comprising 8-HQ (1) and its derivative (8). The resulted Mannich bases of type 2 were used in transamination reactions with hydrazine and hydrazine derivatives. The structures of the newly synthesized Mannich bases were confirmed based on the NMR spectroscopic data and elemental analysis. Antimicrobial and antioxidant activities were also assessed.

Background: The epidemiological transition is directly associated with dietary shift towards empty calories. In contrary, cabbage fights against oxidative stress mediated health disorders owing to the presence of nutritive constituents and low caloric count. The study aimed to assess the efficacy of red cabbage and its aqueous extract against renal and cardiac oxidative stress in response to hypercaloric diet. Methods: Red cabbage and its aqueous extract were fed to normal rabbits (Study I) and hypercholesterolemic diet (1% cholesterol) induced oxidatively stressed rabbits (Study II) for 12-weeks. Serum specific biomarkers of renal and cardiac oxidative stress including creatinine, urea, creatine kinase (CK), creatine kinase-MB (CK-MB), lactate dehydrogenase (LDH), and aspartate aminotransferase (AST) were measured. Tissues of kidney and heart were employed to assess the activities of superoxide dismutase (SOD) and catalase (CAT) alongside; lipid peroxidation was also studied. Results: Red cabbage extract depicted more decrement (p<0.05) in serum creatinine and urea levels up to 14.45 and 9.01% in oxidatively stressed rabbits (Study II), respectively. In kidney tissues, red cabbage extract showed an obvious reduction in lipid peroxidation up to 24.07% in Study II that ultimately restored SOD (11.38%) and CAT (16.72%) activities. On the other hand, red cabbage demonstrated promising aptitude (p<0.05) in mitigating cardiac compromised condition by down-regulating lipid peroxidation by 16.44%, which considerably decreased the serum levels of CK, CK-MB, LDH and AST. Conclusion: Relatively, red cabbage extract showed a relatively better response in controlling renal oxidative stress as compared to red cabbage; however, vice-versa was observed in case of cardiac oxidative stress.

Background: Date palm (Phoenix dactylifera L.) is a dominant fruit crop in most of the Arabian countries. Date pits, as a major byproduct which remained after consumption of date flesh proved to be valuable source of energy. Methods: Solid State Degradation (SSD) system was used for the preparation of degraded date pits. Date pits degraded with Trichoderma reesei were evaluated for their proximate, chemical composition and antioxidant activity. Results: The crude fiber content of degraded date pits was found to be 20.8 %, ash (2.09%), crude fat (7.2%), protein (5.56%), and total carbohydrate (87.2%). Neutral detergent fiber (NDF) and acid detergent fiber (ADF) was found to be 74.6% and 45.7%, respectively. Monosaccharide composition of fiber showed that the degradation with T. reesei significantly (P<0.05) enhanced the glucose and mannose content of cellulose, hemicellulose and lignin. Pectin, total carbohydrate and mannan oligosaccharide content were also increased in degraded date pits in which galactose and mannose were the major neutral sugars. Among the studied minerals, potassium, calcium, magnesium, sulphur and phosphorus were predominant. The phenolic and flavonoid contents of degraded date pits significantly (P<0.05) increased to 14.230 g Gallic equivalent/100g DW and 11.68 g Rutin equivalent /100g DW. Degraded date pits also showed significant antioxidant activity as evidenced by the results of 2,2-diphenyl-1- picrylhydrazyl(DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline 6 sulphonicacid) (ABTS) and Ferric Reducing Antioxidant Power (FRAP) assays. Conclusion: Biological degradation with T. reesei significantly (P<0.05) improved the nutritional effect of date pits and thereby its potential usage in food industry was greatly improved.

Background: One of the main sources of ROS in stress conditions is the mitochondria. Excessive generation of ROS leads to oxidation of thiol groups of proteins, peroxidation of membrane lipids and swelling of the mitochondria. In this regard, there is a need to search for preparationsadaptogens that increase the body's resistance to stress factors. Perhaps, antioxidants can serve as such adaptogens. This work aims at studying the effect of antioxidant; the potassium anphen in a wide range of concentrations on the functional state of 6 day etiolated pea seedlings mitochondria (Pisum sativum L). Methods: The functional state of mitochondria was studied per rates of mitochondria respiration, by the level of lipid peroxidation and study of fatty acid composition of mitochondrial membranes by chromatography technique. Results: Potassium anphen in concentrations of 10-5 - 10-8 M and 10-13-10-16 prevented the activation of LPO in the mitochondrial membranes of pea seedlings, increased the oxidation rates of NAD-dependent substrates and succinate in the respiratory chain of mitochondria that probably pointed to the anti-stress properties of the drug. Indeed, the treatment of pea seeds with the preparation in concentrations of 10-13 M prevented the inhibition of growth of seedlings in conditions of water deficiency. Conclusion: It is assumed that the dose dependence of the biological effects of potassium anphen and the manifestation of these effects in ultra-low concentrations are due to its ability in water solutions to form a hydrate containing molecular ensembles (structures).

Background: Polygonum maritimum is one of the spontaneous halophyte plants of the Algerian coast. Many studies were carried out to evaluate the contents and the quality of phenolic compounds of this plant around the Mediterranean region. Objective: This paper intends to identify, for the first time, the phenolic compounds from the flower part of P. maritimum. Methods: RP-HPLC-PDA (Reversed Phase-High Performance Liquid Chromatography-Photo Diode Array) material was used for this purpose. Many standards were used and their retention times were stored in a local database. Identification was made on the basis of retention times of retained compounds and those found in the literature, and UV spectra of each peak. Results: This study intends to identify five phenolic acids (gallic, ferulic, sinapic, caffeic and syringic acids), one flavonol (rutin) and one flavanone (naringenin). Conclusion: P. maritimum is an important source of natural bioactive compounds that can be exploited for the benefit of many fields.