Thymoquinone Alleviates Cadmium Induced Stress in Germinated Lens culinaris Seeds by Reducing Oxidative Stress and Increasing Antioxidative Activities.

This study investigated the effect of thymoquinone on seeds germination and young seedlings of lentils under cadmium (Cd) stress (300 µM). Three different concentrations (10 µM, 1 µM, and 0.1 µM) of thymoquinone were applied. Our results indicated that thymoquinone has a positive effect on several physiological and biochemical parameters on seeds germination and young seedlings of lentils under Cd stress, which led to enhancing their growth. A significant increase in shoot and root length, fresh and dry weight, and chlorophyll content was observed in the treated plants compared to the control plants. However, the thymoquinone treatment significantly reduced malondialdehyde (MDA) and hydrogen peroxide (H2O2) contents compared to untreated roots and seedlings under Cd-stress. Nevertheless, our results show that the thymoquinone significantly improved the activities of enzymes involved in antioxidant response, including superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), thioredoxin reductase (TrxR), and ascorbate peroxidase (APX). We have also studied the activities of isocitrate dehydrogenase (ICDH) and malate dehydrogenase (MDH); ICDH was increased significantly in roots and seedlings in the presence of different doses of thymoquinone. However, the activity MDH was increased only in roots. Our results suggest that the application of thymoquinone could mitigate cadmium induced oxidative stress.

Insecticidal Activities of Atriplex halimus L., Salvia rosmarinus Spenn. and Cuminum cyminum L. against Dactylopius opuntiae (Cockerell) under Laboratory and Greenhouse Conditions.

The wild cochineal Dactylopius opuntiae (Hemiptera: Dactylopiidae) is one of the major insect pests of the prickly pear Opuntia ficus-indica (L.) in Morocco, a well-known fruit and vegetable crop of arid and semi-arid regions around the world. The present study investigated the insecticidal potential of six extracts (three aqueous and three hydroalcoholic (MeOH/H2O, 20/80 (v/v)) from Atriplex halimus (leaves), Salvia rosmarinus (leaves) and Cuminum cyminum (seeds) to control nymphs and adult females of D. opuntiae under laboratory and greenhouse conditions. Out of the tested samples, A. halimus aqueous extract showed the highest activity, inducing mortality rates of 67.04% (after 4 days) and 85% (after 8 days) on nymphs and adult females of D. opuntiae, respectively, at a concentration of 5% under laboratory conditions. It also showed the highest mortality rate of nymphs with 100% (4 days after application) and 83.75% of adult females (7 days after the second application) at a concentration of 5% when combined with black soap at 10 g/L under greenhouse conditions. The difference in the toxicity of plant species of the study was correlated with their saponin content. A total of 36 of these triterpene glucosides were suggested after a comprehensive LC-MSn profiling of the most active extract, A. halimus, in addition to phytoecdysones and glycosylated phenolic acids and flavonoids. These findings provided evidence that the aqueous leaf extract of A. halimus could be incorporated in the management of the wild cochineal as an alternative to chemical insecticides.

Box-Behnken Design: Wet Process Optimization for Saponins Removal From Chenopodium quinoa Seeds and the Study of Its Effect on Nutritional Properties.

The pseudocereal grain, Quinoa (Chenopodium quinoa Willd.), has a great nutritional value due to its high contents of proteins, fiber, minerals, and vitamins. However, saponins naturally present outside the grains represent an obstacle to their consumption as human food. Before consumption, the grains are subjected to various treatments, which alter their nutritional value. In an attempt to eliminate the maximum of saponins using the wet process, while minimizing the washing conditions and preserving the nutritional quality, we explored the effects of several parameters, including volume of water, treatment time, soaking time, number of washing, and water temperature, followed by an optimization process using Box-Behnken Design, and finally, the impact of this process on the physicochemical and techno-functional properties of six quinoa genotypes seeds was evaluated. As a result, the variation of the treatment time, volume, and temperature of the water positively affected the saponins leaching. According to the quadratic model, the maximum percentages of eliminated saponins (96.53%-96.77%) were found at a temperature of 50°C, treatment times from 60 to 69 min, and water volumes from 6.99 to 7.50 mL per gram of seeds. The optimized method did not affect the proteins and microelements content (Zn, Mn, B, Mo), while a slight decrease of macro-elements (K, P, Ca, S, Mg) was noted in the level of some genotypes. On the other hand, a significant improvement of the techno-functional properties such as water and oil holding capacity was noted, with a sharp drop-in emulsifying activity in all genotypes without affecting the standard values of pH (6.4-6.8) and moisture content (10%-11%) of the seeds. Hence, the optimized method showed to be a more potential method for saponins removal than the currently used dry method.

Crataegus oxyacantha Extract as a Biostimulant to Enhance Tolerance to Salinity in Tomato Plants.

Salinity is a severe abiotic problem that has harmful impacts on agriculture. Recently, biostimulants were defined as bioprotectant materials that promote plant growth and improve productivity under various stress conditions. In this study, we investigated the effect of Crataegus oxyacantha extract as a biostimulant on tomato plants (Solanum lycopersicum) grown under salt stress. Concentrations of 20 mg/L, 30 mg/L, and 70 mg/L of C. oxyacantha extract were applied to tomato plants that were grown under salt stress. The results indicated that plants that were treated with C. oxyacantha extract had a higher ability to tolerate salt stress, as demonstrated by a significant (p < 0.05) increase in plant growth and photosynthetic pigment contents, in addition to a significant increase in tomato soluble sugars and amino acids compared to the control plants. In the stressed tomato plants, malondialdehyde increased and then decreased significantly with the different concentrations of C. oxyacantha extract. Furthermore, there was a significant improvement in the antioxidant enzyme activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione S-transferase (GST), and glutathione reductase (GR) in the stressed plants, especially after treatment with 70 mg/L of the extract. Overall, our results suggest that C. oxyacantha extract could be a promising biostimulant for treating tomato plants under salinity stress.

Eichhornia crassipes (Mart.) Solms: A Comprehensive Review of Its Chemical Composition, Traditional Use, and Value-Added Products.

Eichhornia crassipes (Mart.) Solms, commonly known as water hyacinth, is one of the world's most invasive aquatic plants of the Pontederiaceae family occurring in tropical and subtropical regions of the world. Although, E. crassipes causes significant ecological and socioeconomic issues such as a high loss in water resources, it has multipurpose applications since it is famous for many industrial applications such as bioenergy, biofertilizer production, wastewater treatment (absorption of heavy metals), and animal feed. Furthermore, E. crassipes is rich in diverse bioactive secondary metabolites including sterols, alkaloids, phenolics, flavonoids, tannins, and saponins. These secondary metabolites are well known for a wide array of therapeutic properties. The findings of this review suggest that extracts and some isolated compounds from E. crassipes possess some pharmacological activities including anticancer, antioxidant, anti-inflammatory, antimicrobial, skin whitening, neuroprotective, and hepatoprotective activities, among other biological activities such as allelopathic, larvicidal, and insecticidal activities. The present review comprehensively summarizes the chemical composition of E. crassipes, reported to date, along with its traditional uses and pharmacological and biological activities.

Phenolics from Medicinal and Aromatic Plants: Characterisation and Potential as Biostimulants and Bioprotectants.

Biostimulants and bioprotectants are derived from natural sources and can enhance crop growth and protect crops from pests and pathogens, respectively. They have attracted much attention in the past few decades and contribute to a more sustainable and eco-friendly agricultural system. Despite not having been explored extensively, plant extracts and their component secondary metabolites, including phenolic compounds have been shown to have biostimulant effects on plants, including enhancement of growth attributes and yield, as well as bioprotectant effects, including antimicrobial, insecticidal, herbicidal and nematicidal effects. Medicinal and aromatic plants are widely distributed all over the world and are abundant sources of phenolic compounds. This paper reviews the characterisation of phenolic compounds and extracts from medicinal and aromatic plants, including a brief overview of their extraction, phytochemical screening and methods of analysis. The second part of the review highlights the potential for use of phenolic compounds and extracts as biostimulants and bioprotectants in agriculture as well as some of the challenges related to their use.

Functional properties of chitosan derivatives obtained through Maillard reaction: A novel promising food preservative.

This review provides an insight about the functional properties of chitosan obtained through Maillard reaction to enhance the shelf life and food quality. Maillard reaction is a promising and safe method to obtain commercial water-soluble chitosan's through Schiff base linkage and Amadori or Heyns rearrangement. Likewise, chitosan derivatives exert an enhanced antimicrobial, antioxidant, and emulsifying properties due to the development of Maillard reaction products (MRPs) like reductones and melanoidins. Additionally, the application of chitosan-MRPs effectively inhibited the microbial spoilage, reduced lipid oxidative, and extended the shelf life and the quality of fresh food products. Therefore, understand the potential of chitosan-MRPs derivatives as a functional biomaterial to improve the postharvest quality and extending the shelf life of food products will scale up its application as a food preservative.

Chemically degraded soil rehabilitation process using medicinal and aromatic plants: review.

In recent decades, the increasing number of degraded lands worldwide makes their rehabilitation essential and crucial. Various techniques have emerged to fulfill these needs but most of them are expensive and difficult to be applied. Revegetation is a cost effective, environmental friendly, and aesthetically pleasing approach suitable for degraded areas. However, the use of edible crops, especially for areas with heavy metals (HM) contamination, is not ecologically suitable because the HM may enter the food chain. Alternatively, non-edible, fast-growing, deep-rooting, and metal-stabilizing plants with high biomass, which can produce high-value products hold a great potential and have been regarded as potential candidates of edible crops. This current review presents the benefits of using aromatic and medicinal plants (AMPs) and their associated microorganisms for revegetation of degraded sites as they are high-value economic crops. We discussed the effect of various stress on productivity of secondary metabolites in AMPs in addition to the potential health risk with human consumption of these plants and their products. A focus was also given to the effect of HM stress on the essential oil (EO) content of certain AMPs. Reported data showed that AMPs growing on HM-contaminated soils are safe products to use as they are not significantly contaminated themselves by HM.

A Polyphenol-Rich Extract From Entada abyssinica Reduces Oxidative Damage in Cryopreserved Ram Semen.

The Splinter bean, Entada abyssinica, is widely used in folk medicine. In the current work, we profiled the secondary metabolites from E. abyssinica bark extract using LC-MS and investigated its effect on cryopreserved ram semen. Twenty-eight compounds, including tannins and gallic acid derivatives that prevailed in the extract, were tentatively identified. Results showed that the quality of the post-thawed semen showed a significant improvement when the extract was added to the extender at a concentration of 375 µg/mL. The progressive motility and plasma membrane integrity of sperm cells were significantly increased in the post-thawed semen; however, the total antioxidant capacity (TAC) was insignificantly increased. A significant decrease in the concentration of hydrogen peroxide was detected as well. No significant changes were observed in activities of lactate dehydrogenase (LDH), alanine aminotransaminase (ALT), and aspartate transaminase (AST) within the treated samples. Intact sperm percentage was significantly increased, while apoptotic and necrotic sperm percentages were reduced significantly. Molecular docking of some individual components from the extract revealed their potential to interfere with the apoptosis cascade in which Bcl-2 is involved. In conclusion, Entada abyssinica appears to be useful for cryopreservation presumably owing to its polyphenol content that has potent antioxidant capacity scavenging reactive oxygen species (ROS), enhancing the endogenous antioxidant system and inhibiting lipid peroxidation.

A Polyphenols-Rich Extract from Moricandia sinaica Boiss. Exhibits Analgesic, Anti-Inflammatory and Antipyretic Activities In Vivo.

In this study, the aerial parts of Moricandia sinaica were evaluated for their in vivo analgesic, anti-inflammatory and antipyretic activities. The analgesic activities were examined using acetic acid-induced writhing, the hot plate test and the tail flick method. The anti-inflammatory and the antipyretic activities were evaluated using carrageenan-induced paw edema in rats and brewer's yeast-induced pyrexia in mice, respectively. The aqueous fraction of the methanol extract (MS-3) showed to be the most bioactive among the other investigated fractions. At the dose of 500 mg/kg, the fraction (MS-3) showed a significant percentage inhibition of the carrageenan-induced edema by 52.4% (p < 0.05). In addition, MS-3 exhibited a significant inhibition of acetic acid-induced writhes by 44.4% and 61.5% (p < 0.001) at 250-mg/kg and 500-mg/kg doses, respectively. At 120 min post-treatment, the rat groups treated with MS-3 displayed statistically significant reduction in rectal temperature (p < 0.001) by 1.7 °C and 2.2 °C at 250- and 500-mg/kg doses, respectively. The phytochemical composition of the fraction (MS-3) was characterized by high-performance liquid chromatography-mass spectrometry (HPLC-PDA-MS/MS). Molecular docking studies demonstrated that the polyphenols identified in MS-3 revealed good binding energy upon docking to some target proteins involved in pain response and inflammation, such as the cannabinoid receptors CB1 and CB2, the fatty acid amide hydrolase (FAAH) and the cyclooxygenase COX-1 and COX-2 enzymes. Based on the findings from the present work, it could be concluded that the aerial parts extract of M. sinaica exerts potential analgesic, anti-inflammatory and antipyretic effects in rats.

Impact of Washingtonia robusta Leaves on Gamma Irradiation-Induced Hepatotoxicity in Rats and Correlation with STING Pathway and Phenolic Composition.

Exposure to ionizing radiation usually results in cellular oxidative damage and may induce liver toxicity. The efficiency of the ethanol extracts of Washingtonia filifera (EWF) and Washingtonia robusta (EWR) leaves in alleviating γ-radiation-induced oxidative hepatotoxicity was herein explored. Proximate and macronutrient composition of the leaves was determined to establish reliable quality control criteria. Colorimetric estimation of total phenolic (TPC) and flavonoid (TFC) contents revealed their occurrence in larger amounts in EWR. In vitro evaluation of the antioxidant capacity by 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant power (FRAP) assays confirmed higher efficiency of EWR designating a close correlation with phenolic composition. Four phenolics, viz., naringenin, kaempferol, quercetin, and gallic acid, were isolated from EWR. In vivo assessment of the extracts' antioxidant potential was performed on γ-irradiated (7.5 Gy) female rats. EWR was found more efficient in restoring the elevated liver index, ALT, albumin, cholesterol, and reactive oxygen species (ROS) levels. Both extracts ameliorated the increase in the stimulator of interferon gene (STING) expression. Bioactivity was confirmed by immuno-histochemical examination of inflammatory and apoptotic biomarkers (TNF-α, IL-6 and caspase-3) and histopathological architecture. In addition, the interactions of the isolated compounds with STING were assessed in silico by molecular docking. Therefore, Washingtonia robusta leaves might be suggested as a valuable nutritional supplement to alleviate radiotherapy-induced hepatotoxicity.

Variations of Saponins, Minerals and Total Phenolic Compounds Due to Processing and Cooking of Quinoa (Chenopodium quinoa Willd.) Seeds.

Quinoa (Chenopodium quinoa Willd.) is a grain of great nutritional interest that gained international importance during the last decade. Before its consumption, this grain goes through many processes that can alter its nutritional value. Here we report the effect of processing (polishing and milling) and cooking (boiling and steaming) on the saponin content, mineral profile of 14 elements using Inductively Coupled Plasma-Optical Emission Spectrometry (ICP-OES), protein content, and total phenolic compound. The polishing caused an average drop in the saponin content from 1.7% to 0.46% but induced important losses in mineral content (K, Mg, Ca, Zn, Co, Cu, Fe, Mn, and Ni), and phenolic compounds. However, the greatest nutritional degradation happened after milling due to the elimination of seed teguments and embryos, where over 50% of many minerals, 60% of protein content, and almost the totality of phenolic compounds, were lost. Cooking effect was less important than processing, but some significant losses were attested. Boiling caused a loss of up to 40% for some minerals like K, B, and Mo because of their hydrosolubility, and 88% of the polyphenols, while steaming allowed a better retention of those nutrients. Consuming polished quinoa instead of semolina and using steaming instead of boiling are trade-offs consumer needs to make to get optimal benefits from quinoa virtues.

Thymus algeriensis and Thymus fontanesii: Chemical Composition, In Vivo Antiinflammatory, Pain Killing and Antipyretic Activities: A Comprehensive Comparison.

This study aimed to investigate the chemical composition, and evaluate the antioxidant, anti-inflammatory, anti-pyretic, and the analgesic properties of methanol extracts from the leaves of Thymus algeriensis and Thymus fontanesii (Lamiaceae). Thirty-five secondary metabolites were characterized in both extracts using HPLC-PDA-ESI-MS/MS. Phenolic acids, mainly rosmarinic acid and its derivatives, dominated the T. algeriensis extract, while the phenolic diterpene carnosol and the methylated flavonoid salvigenin, prevailed in T. fontanesii extract. Molecular docking study was carried out to estimate the anti-inflammatory potential and the binding affinities of some individual secondary metabolites from both extracts to the main enzymes involved in the inflammation pathway. In vitro enzyme inhibitory assays and in vivo assays were used to investigate the antioxidant and anti-inflammatory activities of the extracts. Results revealed that both studied Thymus species exhibited antioxidant, anti-inflammatory, analgesic, and antipyretic effects. They showed to be a more potent antioxidant than ascorbic acid and more selective against cyclooxygenase (COX-2) than diclofenac and indomethacin. Relatively, the T. fontanesii extract was more potent as COX-2 inhibitor than T. algeriensis. In conclusion, Thymus algeriensis and Thymus fontanesii may be interesting candidates for the treatment of inflammation and oxidative stress-related disorders.

An Insight into Saponins from Quinoa (Chenopodium quinoa Willd): A Review.

Saponins are an important group found in Chenopodium quinoa. They represent an obstacle for the use of quinoa as food for humans and animal feeds because of their bitter taste and toxic effects, which necessitates their elimination. Several saponins elimination methods have been examined to leach the saponins from the quinoa seeds; the wet technique remains the most used at both laboratory and industrial levels. Dry methods (heat treatment, extrusion, roasting, or mechanical abrasion) and genetic methods have also been evaluated. The extraction of quinoa saponins can be carried out by several methods; conventional technologies such as maceration and Soxhlet are the most utilized methods. However, recent research has focused on technologies to improve the efficiency of extraction. At least 40 saponin structures from quinoa have been isolated in the past 30 years, the derived molecular entities essentially being phytolaccagenic, oleanolic and serjanic acids, hederagenin, 3ß,23,30 trihydroxy olean-12-en-28-oic acid, 3ß-hydroxy-27-oxo-olean-12en-28-oic acid, and 3ß,23,30 trihydroxy olean-12-en-28-oic acid. These metabolites exhibit a wide range of biological activities, such as molluscicidal, antifungal, anti-inflammatory, hemolytic, and cytotoxic properties.

Polyphenols from Salix tetrasperma Impair Virulence and Inhibit Quorum Sensing of Pseudomonas aeruginosa.

Bacterial resistance represents one of the emerging obstacles in plants, animals, and humans that impairs treatment with antibacterial agents. Targeting of the bacterial quorum sensing system is one of the strategies to overcome this problem. Recently, research has been focused on natural and food components which can function as quorum sensing inhibitors. In this study, a methanol extract from Salix tetrasperma stem bark was phytochemically profiled by LC-MS analysis. This resulted in the identification of 38 secondary metabolites with (epi)catechin-(epi)catechin, epicatechin, tremulacin, salicortin, and trichocarposide as the major constituents. The extracts of both stem bark and the previously profiled flower of S. tetrasperma were tested for anti-quorum sensing activity in a common and widely distributed pathogen Pseudomonas aeruginosa. The natural products inhibited swimming and swarming motilities, as well as proteolytic and hemolytic activities in a dose-dependent manner. Molecular docking of the constituents from both extracts against the quorum sensing controlling systems Lasl/LasR, rhll/rhlR, and PQS/MvfR showed that epicatechin, (epi)catechin-(epi)catechin, p-hydroxy benzoyl galloyl glucose, p-hydroxy benzoyl protocatechuic acid glucose, and caffeoylmalic acid could be the main active components. This study supports the importance of secondary metabolites, especially polyphenols, as quorum sensing inhibitors.

Combining a QSAR Approach and Structural Analysis to Derive an SAR Map of Lyn Kinase Inhibition.

Lyn kinase, a member of the Src family of protein tyrosine kinases, is mainly expressed by various hematopoietic cells, neural and adipose tissues. Abnormal Lyn kinase regulation causes various diseases such as cancers. Thus, Lyn represents, a potential target to develop new antitumor drugs. In the present study, using 176 molecules (123 training set molecules and 53 test set molecules) known by their inhibitory activities (IC50) against Lyn kinase, we constructed predictive models by linking their physico-chemical parameters (descriptors) to their biological activity. The models were derived using two different methods: the generalized linear model (GLM) and the artificial neural network (ANN). The ANN Model provided the best prediction precisions with a Square Correlation coefficient R² = 0.92 and a Root of the Mean Square Error RMSE = 0.29. It was able to extrapolate to the test set successfully (R² = 0.91 and RMSE = 0.33). In a second step, we have analyzed the used descriptors within the models as well as the structural features of the molecules in the training set. This analysis resulted in a transparent and informative SAR map that can be very useful for medicinal chemists to design new Lyn kinase inhibitors.

Petroleum sludge bioremediation and its toxicity removal by landfill in gunder semi-arid conditions.

In this investigation, petroleum sludge landfilling was carried out in order to assess the biodegradation degree and the final product quality. The microbial analysis showed a good microorganism proliferation which reinforces the biodegradation process. The total mesophilic and thermophilic microflora evaluated symmetrically as they increased at the intermediate stage and decreased at the final. The C/N and NH4+/NO3-ratios decreased while the polymerization degree increased at the end of the landfilling process. The total polyphenols and total petroleum C6 to C22hydrocarbons were removed by 71.6% and 73% respectively, and that affected the reduction of the phytotoxicity in a positive way. All these changes are in agreement with the efficiency of the biotransformation process and showed that petroleum sludge and filling reduced the toxic organic compounds and led to a stable final product.

Discovering novel 7-azaindole-based series as potent AXL kinase inhibitors.

AXL is a receptor tyrosine kinase that plays a key role in tumor growth and proliferation. The scientific community has validated AXL as therapeutic target in the treatment of cancers for several years now, and several AXL inhibitors have been developed but none of them are approved. In this context, we started to design new kinase inhibitors targeting AXL from the 7-azaindole scaffold well known to interact with the ATP binding site of the kinase. Focused screening and chemical diversification around 7-azaindole scaffold were developed, based on modeling studies and medicinal chemistry rational, leading to the discovery of a new family of hits with potent inhibitory activity against AXL.

Structure-activity relationships study of mTOR kinase inhibition using QSAR and structure-based drug design approaches.

The discovery of clinically relevant inhibitors of mammalian target of rapamycin (mTOR) for anticancer therapy has proved to be a challenging task. The quantitative structure-activity relationship (QSAR) approach is a very useful and widespread technique for ligand-based drug design, which can be used to identify novel and potent mTOR inhibitors. In this study, we performed two-dimensional QSAR tests, and molecular docking validation tests of a series of mTOR ATP-competitive inhibitors to elucidate their structural properties associated with their activity. The QSAR tests were performed using partial least square method with a correlation coefficient of r2=0.799 and a cross-validation of q2=0.714. The chemical library screening was done by associating ligand-based to structure-based approach using the three-dimensional structure of mTOR developed by homology modeling. We were able to select 22 compounds from two databases as inhibitors of the mTOR kinase active site. We believe that the method and applications highlighted in this study will help future efforts toward the design of selective ATP-competitive inhibitors.

Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.

Efforts were made to improve a series of potent dual ABL/SRC inhibitors based on a 7-azaindole core with the aim of developing compounds that demonstrate a wider activity on selected oncogenic kinases. Multi-targeted kinase inhibitors (MTKIs) were then derived, focusing on kinases involved in both angiogenesis and tumorigenesis processes. Antiproliferative activity studies using different cellular models led to the discovery of a lead candidate (6z) that combined both antiangiogenic and antitumoral effects. The activity of 6z was assessed against a panel of kinases and cell lines including solid cancers and leukemia cell models to explore its potential therapeutic applications. With its potency and selectivity for oncogenic kinases, 6z was revealed to be a focused MTKI that should have a bright future in fighting a wide range of cancers.