Characterization of palm date varieties (Phoenix dactylifera L.) growing in Saudi Arabia: Phenotypic diversity estimated by fruit and seed traits

In order to determine the variation and the degree of diversity among the most well-known Saudi date palm (Phoenix dactylifera L.), this study applied various widely detectible fruit and seed features. The properties of the fruit and seeds were described using ten phenotypic traits. Eighteen date palm varieties from six production sites were used in this study (Ḥaʼil, Al-Madina, Al-Hassa, Al-Qassim, Kharaj, Najran). The data was analysed by Pearson r correlation. The principal components analysis (PCA) and UPGMA clustering were used to analyse the data set. According to PCA, the results showed significant variation among the analysed varieties. Our data shows that seed ratio varies among all varieties. The mean seed weight ratio varies between 4 and 13%. Varieties ‘Raziz’, ‘Lubab’ and ‘Wasily’ demonstrate higher seed ratio (over 10%). Whereas, Fankha depicts a 5 and 4% fresh and dry seed ratio. The statistical analysis indicates that the seed ratio in all 18 varieties is comparable in fresh and dry fruits. The result suggests variation among the numerous features due to dissimilarities and heterogeneity. However, the obtained results also propose the clustering and grouping of closely related features, e.g., weights of fresh and dry fruits. Eventually, it is suggested to conduct additional research on Saudi date palms utilizing more phenotypic traits in order to have a better understanding of the pack of morphological descriptors

Cytoplasmic amino acid profiles of clinical and ATCC 29213 strains of Staphylococcus aureus harvested at different growth phases

Staphylococcus aureus strains are a great contributor to both hospital acquired infections as well as community acquired infections. The objective of the present investigation was to compare potential differences in cytoplasmic amino acid levels between clinical and ATCC 29213 strains of S. aureus. The two strains were grown under ideal conditions to mid-exponential and stationary growth phases, after which they were harvested to analyze their amino acid profiles. Initially, the amino acid patterns of both strains were compared at the mid-exponential phase when grown in controlled conditions. At the mid-exponential phase, both strains shared common features in cytoplasmic amino acid levels, with glutamic acid, aspartic acid, proline, and alanine identified as key amino acids. However, the concentration profiles of seven amino acids exhibited major variances between the strains, even though the total cytoplasmic levels of amino acids did not alter significantly. At the stationary phase, the magnitudes of the amino acids abundant in the mid-exponential phase were altered. Aspartic acid became the most abundant amino acid in both strains accounting for 44% and 59% of the total amino acids in the clinical and ATCC 29213 strains, respectively. Lysine was the second most abundant amino acid in both strains, accounting for 16% of the total cytoplasmic amino acids, followed by glutamic acid, the concentration of which was significantly higher in the clinical strain than in the ATCC 29213 strain. Interestingly, histidine was clearly present in the clinical strain but was virtually lacking in the ATCC 29213 strain. This study reveals the dynamic diversity of amino acid levels among strains, which is an essential step toward illustrating the variability in S. aureus cytoplasmic amino acid profiles and could be significant in explaining variances among strains of S. aureus

Phytochemical Analysis, Antioxidant, and Antimicrobial Activities of Ducrosia flabellifolia: A Combined Experimental and Computational Approaches

Ducrosia flabellifolia Boiss. is a rare desert plant known to be a promising source of bioactive compounds. In this paper, we report for the first time the phytochemical composition and biological activities of D. flabellifolia hydroalcoholic extract by using liquid chromatography-electrospray tandem mass spectrometry (ESI-MS/MS) technique. The results obtained showed the richness of the tested extract in phenols, tannins, and flavonoids. Twenty-three phytoconstituents were identified, represented mainly by chlorogenic acid, followed by ferulic acid, caffeic acid, and sinapic acid. The tested hydroalcoholic extract was able to inhibit the growth of all tested bacteria and yeast on agar Petri dishes at 3 mg/disc with mean growth inhibition zone ranging from 8.00 ± 0.00 mm for Enterococcus cloacae (E. cloacae) to 36.33 ± 0.58 mm for Staphylococcus epidermidis. Minimal inhibitory concentration ranged from 12.5 mg/mL to 200 mg/mL and the hydroalcoholic extract from D. flabellifolia exhibited a bacteriostatic and fungistatic character. In addition, D. flabellifolia hydroalcoholic extract possessed a good ability to scavenge different free radicals as compared to standard molecules. Molecular docking studies on the identified phyto-compounds in bacterial, fungal, and human peroxiredoxin 5 receptors were performed to corroborate the in vitro results, which revealed good binding profiles on the examined protein targets. A standard atomistic 100 ns dynamic simulation investigation was used to further evaluate the interaction stability of the promising phytocompounds, and the results showed conformational stability in the binding cavity. The obtained results highlighted the medicinal use of D. flabellifolia as source of bioactive compounds, as antioxidant, antibacterial, and antifungal agent

Biosurfactant derived from probiotic Lactobacillus acidophilus exhibits broad-spectrum antibiofilm activity and inhibits the quorum sensing-regulated virulence

Antimicrobial resistance by pathogenic bacteria has become a global risk to human health in recent years. The most promising approach to combating antimicrobial resistance is to target virulent traits of bacteria. In the present study, a biosurfactant derived from the probiotic strain Lactobacillus acidophilus was tested against three Gram-negative bacteria to evaluate its inhibitory potential on their biofilms, and whether it affected the virulence factors controlled by quorum sensing (QS). A reduction in the virulence factors of Chromobacterium violaceum (violacein production), Serratia marcescens (prodigiosin production) and Pseudomonas aeruginosa (pyocyanin, total protease, LasB elastase and LasA protease production) was observed at different sub-MIC concentrations in a dose-dependent manner. Biofilm development was reduced by 65.76%, 70.64% and 58.12% at the highest sub-MIC levels for C. violaceum, P. aeruginosa and S. marcescens, respectively. Biofilm formation on glass surfaces exhibited significant reduction, with less bacterial aggregation and reduced formation of extracellular polymeric materials. Additionally, swimming motility and exopolysaccharides (EPS) production were shown to be reduced in the presence of the L. acidophilus-derived biosurfactant. Furthermore, molecular docking analysis performed on compounds identified through gas chromatography–mass spectrometry (GC-MS) analysis of QS and biofilm proteins yielded further insights into the mechanism underlying the anti-QS activity. Therefore, the present study has clearly demonstrated that a biosurfactant derived from L. acidophilus can significantly inhibit virulence factors of Gram-negative pathogenic bacteria. This could provide an effective method to inhibit the formation of biofilms and QS in Gram-negative bacteria

Chemical Composition and the Anticancer, Antimicrobial, and Antioxidant Properties of Acacia Honey from the Hail Region: The in vitro and in silico Investigation

In consideration of the emergence of novel drug-resistant microbial strains and the increase in the incidences of various cancers throughout the world, honey could be utilized as a great alternative source of potent bioactive compounds. In this context, this study pioneers in reporting the phytochemical profiling and the antimicrobial, antioxidant, and anticancer properties of Acacia honey (AH) from the Hail region of Saudi Arabia, assessed using in vitro and molecular docking approaches. The phytochemical profiling based on high-resolution liquid chromatography-mass spectrometry (HR-LCMS) revealed eight compounds and three small peptide-like proteins as the constituents. The honey samples exhibited promising antioxidant activities (DPPH-IC50 = 0.670 mg/mL; ABTS-IC50 = 1.056 mg/mL; β-carotene-IC50 > 5 mg/mL). In the well-diffusion assay, a high mean growth inhibition zone (mGIZ) was observed against Staphylococcus aureus (48.33 ± 1.53 mm), Escherichia coli ATCC 10536 (38.33 ± 1.53 mm), and Staphylococcus epidermidis ATCC 12228 (39.33 ± 1.15 mm). The microdilution assay revealed that low concentrations of AH could inhibit the growth of almost all the evaluated bacterial and fungal strains, with the minimal bactericidal concentration values (MBCs) ranging from 75 mg/mL to 300 mg/mL. On the contrary, high AH concentrations were required to kill the tested microorganisms, with the minimal bactericidal concentration values (MBCs) ranging from approximately 300 mg/mL to over 600 mg/mL and the minimal fungicidal concentration values (MFCs) of approximately 600 mg/mL. The AH exhibited effective anticancer activity in a dose-dependent manner against breast (MCF-7), colon (HCT-116), and lung (A549) cancer cell lines, with the corresponding IC50 values of 5.053 μg/mL, 5.382 μg/mL, and 6.728 μg/mL, respectively. The in silico investigation revealed that the observed antimicrobial, antioxidant, and anticancer activities of the constituent compounds of AH are thermodynamically feasible, particularly those of the tripeptides (Asp-Trp-His and Trp-Arg-Ala) and aminocyclitol glycoside. The overall results highlighted the potential of AH as a source of bioactive compounds with significant antimicrobial, antioxidant, and anticancer activities, which could imply further pharmacological applications of AH

Deciphering the Molecular Mechanism Responsible for Efficiently Inhibiting Metastasis of Human Non-Small Cell Lung and Colorectal Cancer Cells Targeting the Matrix Metalloproteinases by Selaginella repanda

Selaginella species are known to have antimicrobial, antioxidant, anti-inflammatory, anti-diabetic as well as anticancer effects. However, no study has examined the cytotoxic and anti-metastatic efficacy of Selaginella repanda (S. repanda) to date. Therefore, this study aimed to evaluate the potential anti-metastatic properties of ethanol crude extract of S. repanda in human non-small-cell lung (A-549) and colorectal cancer (HCT-116) cells with possible mechanisms. Effect of S. repanda crude extract on the growth, adhesion, migration and invasion of the A-549 and HCT-116 were investigated. We demonstrated that S. repanda crude extract inhibited cell growth of metastatic cells in a dose and time dependent manner. Incubation of A-549 and HCT-116 cells with 100–500 µg/mL of S. repanda crude extract significantly inhibited cell adhesion to gelatin coated surface. In the migration and invasion assay, S. repanda crude extract also significantly inhibited cellular migration and invasion in both A-549 and HCT-116 cells. Moreover, reverse transcription-polymerase chain reaction, and real-time PCR (RT-PCR) analysis revealed that the activity and mRNA level of matrix metalloproteinase-9 (MMP-9), matrix metalloproteinase-2 (MMP-2) and membrane type 1-matrix metalloproteinase (MT1-MMP) were inhibited. While the activity of tissue inhibitor matrix metalloproteinase 1 (TIMP-1); an inhibitor of MMPs was stimulated by S. repanda crude extract in a concentration-dependent manner. Therefore, the present study not only indicated the inhibition of motility and invasion of malignant cells by S. repanda, but also revealed that such effects were likely associated with the decrease in MMP-2/-9 expression of both A-549 and HCT-116 cells. This further suggests that S. repanda could be used as a potential source of anti-metastasis agent in pharmaceutical development for cancer therapy

Antiviral Effects of Artemisinin and Its Derivatives against SARS-CoV-2 Main Protease: Computational Evidences and Interactions with ACE2 Allelic Variants

Fighting against the emergent coronavirus disease (COVID-19) remains a big challenge at the front of the world communities. Recent research has outlined the potential of various medicinal herbs to counteract the infection. This study aimed to evaluate the interaction of artemisinin, a sesquiterpene lactone extracted from the Artemisia genus, and its derivatives with the SARS-CoV-2 main protease. To assess their potential use against COVID-19, the interactions of the main active principle of Artemisia with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) was investigated through in silico probing. Our results showed that artemesinin and its derivatives manifested good oral absorption and bioavailability scores (0.55). They potently bound to the Mpro site of action—specifically, to its Cys145 residue. The selected compounds established two to three conventional hydrogen bonds with binding affinities ranging between −5.2 and −8.1 kcal/mol. Furthermore, artemisinin interactions with angiotensin converting enzyme 2 (ACE2) were dependent on the ACE2 allelic variants. The best score was recorded with rs961360700. A molecular dynamic simulation showed sufficient stability of the artemisinin–Mpro complex on the trajectory of 100 ns simulation frame. These binding interactions, together with drug-likeness and pharmacokinetic findings, confirmed that artemisinin might inhibit Mpro activity and explain the ethnopharmacological use of the herb and its possible antiviral activity against SARS-CoV-2 infection inducing COVID-19. Nevertheless, it interacted differently with the various ACE2 allelic variants reported to bind with the SARS-CoV-2 spike protein

Histophysiologie du microenvironnement osseux conditionné par l'intoxication au tetradifon et par les métastases osseuses ostéolytiques induites par cellules Wlaker 256/B

Bone remodeling is mediated by the osteoclasts and osteoblasts coupling. Xenoestrogens are endocrines disruptors that could interfere with bone remodeling. We have investigated the effect of tetradifon on bone remodeling. We have shown that disturbance of bone remodeling and metabolism were accompanied with a secondary genotoxic effect via oxidative damages. Bone is the main site of metastases for many cancer diseases such as the breast cancer. We have used Walker 256/B to induce bone metastases in rats. In vitro, ATA effects on these cells have provided acceptable results by inducing apoptosis and reducing ROS releasing. In vivo effects of ATA, have been investigated in a designed several model of breast cancer skeletal metastases. ATA did not prevent the bone loss but reduced the oxidative stress damage in the bone microenvironment. Microtomography and histology were used to detect and differentiate bone alterations due to osteolytic with or without ATA treatment. We have also shown that newly metaplastic, osteosclerotic, apposed bone was observed in the periosteal envelope of cancerous and ATA treated group. A hepatorenal bilan of this animal model of bone metastases was investigated. In this study, it seems that in situ inoculation of Walker 256 cells is not associated with renal and hepatic complications.Le remodelage osseux est conditionné par un couplage entre les ostéoclastes et les ostéoblastes. Les xénoestrogènes sont des perturbateurs endocriniens qui peuvent interférer avec le remodelage osseux. Nous nous sommes attachés à étudier l'effet du tetradifon sur le remodelage osseux. Nous avons montré que la perturbation du remodelage et du métabolisme de l'os sont accompagné d'un effet génotoxique secondaire via les dommages oxydatifs. L'os est le site de métastases de plusieurs tumeurs solides tels que le cancer du sein. Nous avons utilisé les cellules Walker 256/B pour induire des métastases osseuses chez le rat. In vitro, le traitement des cellules par l'ATA a apporté des résultats satisfaisants par induction d'apoptose et réduction de l'expression des RLO. Nous avons évalué cet effet, in vivo, sur un modèle animal de métastases osseuses ostéolytiques. L'ATA ne prévient pas la perte osseuse mais elle réduit les dommages oxydatives dans le microenvironnement osseux. La microtomographie et l'histologie ont permis de détecter et de différencier les altérations osseuses induites par métastases ostéolytiques avec ou sans traitement à l'ATA. Nous avons également montré la présence d'os métaplasique, ostéosclérotique, apposé sur les périostes des rats cancéreux et traités à l'ATA. Un bilan hépatorénal du modèle animal de métastases osseuses ostéolytiques a été réalisé. Il parait que l'inoculation in situ des cellules Walker 256 n'avait pas de complications rénales et hépatiques pour cette durée d'étude

Histophysiologie du microenvironnement osseux conditionné par l'intoxication au tetradifon et par les métastases osseuses ostéolytiques induites par cellules Wlaker 256/B

Le remodelage osseux est conditionné par un couplage entre les ostéoclastes et les ostéoblastes. Les xénoestrogènes sont des perturbateurs endocriniens qui peuvent interférer avec le remodelage osseux. Nous nous sommes attachés à étudier l'effet du tetradifon sur le remodelage osseux. Nous avons montré que la perturbation du remodelage et du métabolisme de l'os sont accompagné d'un effet génotoxique secondaire via les dommages oxydatifs. L'os est le site de métastases de plusieurs tumeurs solides tels que le cancer du sein. Nous avons utilisé les cellules Walker 256/B pour induire des métastases osseuses chez le rat. In vitro, le traitement des cellules par l'ATA a apporté des résultats satisfaisants par induction d'apoptose et réduction de l'expression des RLO. Nous avons évalué cet effet, in vivo, sur un modèle animal de métastases osseuses ostéolytiques. L'ATA ne prévient pas la perte osseuse mais elle réduit les dommages oxydatives dans le microenvironnement osseux. La microtomographie et l'histologie ont permis de détecter et de différencier les altérations osseuses induites par métastases ostéolytiques avec ou sans traitement à l'ATA. Nous avons également montré la présence d'os métaplasique, ostéosclérotique, apposé sur les périostes des rats cancéreux et traités à l'ATA. Un bilan hépatorénal du modèle animal de métastases osseuses ostéolytiques a été réalisé. Il parait que l'inoculation in situ des cellules Walker 256 n'avait pas de complications rénales et hépatiques pour cette durée d'étude.Bone remodeling is mediated by the osteoclasts and osteoblasts coupling. Xenoestrogens are endocrines disruptors that could interfere with bone remodeling. We have investigated the effect of tetradifon on bone remodeling. We have shown that disturbance of bone remodeling and metabolism were accompanied with a secondary genotoxic effect via oxidative damages. Bone is the main site of metastases for many cancer diseases such as the breast cancer. We have used Walker 256/B to induce bone metastases in rats. In vitro, ATA effects on these cells have provided acceptable results by inducing apoptosis and reducing ROS releasing. In vivo effects of ATA, have been investigated in a designed several model of breast cancer skeletal metastases. ATA did not prevent the bone loss but reduced the oxidative stress damage in the bone microenvironment. Microtomography and histology were used to detect and differentiate bone alterations due to osteolytic with or without ATA treatment. We have also shown that newly metaplastic, osteosclerotic, apposed bone was observed in the periosteal envelope of cancerous and ATA treated group. A hepatorenal bilan of this animal model of bone metastases was investigated. In this study, it seems that in situ inoculation of Walker 256 cells is not associated with renal and hepatic complications.ANGERS-BU Médecine-Pharmacie (490072105) / SudocSudocFranceF