Antibacterial,antifungal and in vivo anticancer activities of chitin-binding lectins from Tomato (Solanum lycopersicum) fruits

A mixture of chitin-binding lectins from Tomato (Solanum lycopersicum) fruits, designated as Tomato chitin-binding lectins (TCLs), was isolated through affinity chromatography using an acetylated chitin column. Molecular weights of TCLs were determined to be 30 to 115 KDa which possessed mild toxicity with an LC₅₀ value of 521 µg/ml examined by the brine shrimp nauplii toxicity assay. Strong antibacterial activity of TCLs was found against Escherichia coli, Staphylococcus aureus and Shigella boydii at a concentration of 500 µg/ml by using disc diffusion method. Minimum inhibitory concentrations (MIC) of TCLs against Staphylococcus aureus and Escherichia coli were found to be 200 µg/ml and 140 µg/ml, respectively whereas minimum bactericidal concentrations (MBC) against the same bacterial species were 840 and 600 µg/ml, respectively. TCLs also exerted antibiofilm activity (53.32% at 250 μg/ml) against Escherichia coli. Strong antifungal activity of TCLs against Aspergillus niger was found at 600 µg/ml whereas the lectin mixture agglutinated A. niger spores at 200 µg/ml. TCLs exhibited 19.63% and 59.91% anti-proliferative activity against Ehrlich ascites carcinoma (EAC) cells in vivo in Swiss albino mice when intraperitonealy injected at doses 1.0 mg/kg/day and 2.0 mg/kg/day, respectively for five consecutive days. Morphological changes of apoptosis in EAC cells under fluorescence microscope and alteration of the expression of apoptosis-related genes (Fas, Caspase 8 and Caspase 3) had also been observed. MTT assay showed 27.61%, 38.74% and 49.23% of in vitro anticancer activity of the tomato lectins at concentrations of 37.5, 75 and 150 µg/ml, respectively.     

Synthesis of silver nanoparticles using root extract of Duchesnea indica and assessment of its biological activities

Treatment of microbial infections and inflammatory conditions have many challenges in terms of efficacy and safety issues. Novel approaches such as nanoparticles based drug delivery system have shown promising results to solve some of these problems. The aim of this study was to exploit the efficacy of the synthesized silver nanoparticles. In this study, silver nanoparticles (AgNPs) were biosynthesized using root extract (aqueous) of Duchesnea indica. They were characterized using different techniques such as, ultraviolet–visible (UV–Vis) spectrophotometry, transmission and scanning electron microscopy (TEM and SEM), X-ray diffractometer (XRD), energy dispersive X-ray spectroscopy (EDX), fourier-transform infrared spectroscopy (FTIR) and zetasizer. The UV–Vis spectra gave a characteristic peak at 423 nm; XRD confirmed its crystalline structure; FTIR confirmed the involvement of phytochemicals in their capping and reduction; TEM images confirmed their spherical shape with average width of 20.49 nm and average area of 319.25 nm². Various biological activities were performed on these NPs, such as antimicrobial, anti-inflammatory, analgesic and muscle relaxant, which showed significant results as follow. Among bacterial strains, Salmonella typhi (MIC: 0.01 mg/ml) and Escherichia coli (MIC: 0.01 mg/ml), while among that of fungal Microsporum canis (MIC: 0.53 mg/ml) and Alternaria alternata (MIC: 0.51 mg/ml) were most susceptible. The AgNPs showed maximum anti-inflammatory activity (46.15 and 56.85%) at 20 mg/kg after 3 and 5 h of drug administration, comparable to that of standard. In-vivo model exhibited concentration dependent inhibition of both COX-2 and 5-LOX enzymes. Similarly, it exhibited maximum analgesic activity (54.24%) at 20 mg/kg dose after 60 min. of pain induction. Furthermore, they depicted maximum muscle relaxation (P < 0.01) after 60 and 90 min of drug administration. Above results suggest that these AgNPs can be studied further for the development of more effective and safe formulations.     

Comparative analysis of phytochemical profile,antioxidant and anti-inflammatory activity from Hibiscus manihot L. flower

Hibiscus manihot L. is a kind of healthy plant with edible value and health benefits, which possesses multiple pharmacological activities that are closely related to antioxidant and anti-inflammatory activities. The dynamic changes of main active components and biological activities in Hibiscus manihot L. flower (HMLF) during its flowering period were systematically studied to determine the appropriate harvest time. Chemopreventive efficacies of the investigated HMLF extracts, by means of their anti-inflammatory and antioxidant activities, were assessed. The sample harvested on early August had the supreme total flavonoid content, total phenolic content and the strongest antioxidant activity (DPPH radical scavenging activity (IC₅₀ 0.160 mg/mL), ABTS radical scavenging activity (1.570 mmol/g Trolox), reducing power (IC₅₀ 0.101 mg/mL) and FRAP (3.644 mmol FeSO₄/g)). The results of principal component analysis indicated that the primary active components included hyperin, isoquercetin, hibifolin and quercetin-3′-O-glucoside, which were strongly associated with the antioxidant activity in the early August sample, while neochlorogenic acid, chlorogenic acid and caffeic acid were associated with the anti-inflammatory activity. The extracts significantly inhibited lipopolysaccharide-induced nitric oxide production in RAW264.7 cells, especially the samples harvested around August, which was only 3.569 μΜ with the inhibition ratio of>50%. This study indicated that HMLF harvested on the early August possessed the highest antioxidant and anti-inflammatory potential and could be used as high bioactive resources for healthy production.     

Antimicrobial and anti-inflammatory activities of Piper porphyrophyllum (Fam. Piperaceae)

The crude extracts and isolated compounds of Piper porphyrophyllum (Piperaceae) were evaluated for antibacterial and anti-inflammatory activities. The ethyl acetate extract and 3′,4′,5,7-tetramethoxyflavone exhibited the highest activity against Staphylococcus aureus giving values of MIC = 62.5 and 250 μg/mL, respectively. 5-Hydroxy-7-methoxyflavanone and 4′,5-dihydroxy-3′,7-dimethoxyflavone were active against Pseudomonas aeruginosa, both with MIC value 125 μg/mL. The hexane extract and 4′,5-dihydroxy-3′,7-dimethoxyflavone gave the highest anti-inflammatory activity in in vitro quantitative lipoxygenase inhibition assay with inhibitory activity of (IE) 99.72% and 91.81%, respectively.     

Modiolin and phthalide derivatives from the endophytic fungus Microsphaeropsis arundinis PSU-G18

One new modiolin, microsphaerodiolin (1), and seven new phthalides, microsphaerophthalides A-G (2-8), together with 12 known compounds were isolated from the endophytic fungus Microsphaeropsis arundinis PSU-G18. Their structures were elucidated by spectroscopic methods. The new 3-oxygenated phthalides are rare natural products. The known 1-(2,5-dihydroxyphenyl)-2-buten-1-one exhibited significant antifungal activity against Microsporum gypseum SH-MU-4 with an MIC value of 8 μg/mL, moderate antimalarial activity with an IC₅₀ value of 9.63 μg/mL and strong radical scavenging potency with the IC₅₀ value of 0.018 mg/mL. The new compounds 2 and 6 showed moderately antifungal activity against M. gypseum SH-MU-4 and Cryptococcus neoformans, respectively, with equal MIC values of 64 μg/mL.     

Anti-inflammatory and antibacterial activity study of some novel quinazolinones

Anti-inflammatory and antibacterial activities of some novel quinazolinones were determined. Evaluation of anti-inflammatory activity of test compounds was performed using carrageenan induced paw edema in rats. Oral administration of test compounds 25 mg/kg and 50 mg/kg reduced the paw edema significantly (P < 0.05) in a dose dependent manner compared to carrageenan induced rats. The test compounds were also screened for their antibacterial activity against the strains of Staphylococcus aureus and Escherichia coli at the concentrations of 200 μg/ml and 1 mg/ml. The test compounds showed better activity as that of the standard lincomycin at the tested higher concentration against S. aureus. None of the compounds exhibit comparable activity to that of the standard ceftazidime against E. coli.     

Synthesis and characterization of some tetrazoles and their prospective for aerobic micro-fouling mitigation

Two series of tetrazole derivatives of the type N-(1H-tetrazol-5-yl)-1-(aryl)methanimine (101–106) and 1-(4-alkoxyphenyl)-N-(1H-tetrazol-5-yl)methanimine (107–111) were synthesized and characterized via conventional tools of analysis (elemental analysis, FT-IR and ¹H NMR spectroscopy). These two synthesized series were biologically evaluated for their potentials against some microbial biofilm causing strains (micro bio-foulants). Biological activities were evaluated by MIC values and cell viability percentages of them. In case of compounds (107–111), 107 was the most potent antimicrobial one, where its MIC values were 10.666667 µg/ml; 12.82222 µg/ml and 21.43666 µg/ml for Staphylococcus aureus, Escherichia coli and Candida albicans respectively, whereas compound 106, (of group 101–106), MIC values were 16 µg/ml for all the tested microorganisms. Viability assay showed that 107 activity percentages were 96.99456%, 92.32886% and 89.09558% against Gm +ve bacteria, Gm −ve bacteria and yeast respectively, whereas 106 activity percentages were 95.255569%, 90.204675% and 86.710956% against Gm +ve bacteria, Gm −ve bacteria and yeast respectively. Two antimicrobial mode of actions were proposed and discussed depending on the two evaluated tetrazole groups.     

Isolation,Identification and Pharmacological Effects of Mandragora autumnalis Fruit Flavonoids Fraction

Since ancient times, Mandragora autumnalis has been used as a traditional medicinal plant for the treatment of numerous ailments. In light of this, the current study was designed to isolate and identify the chemical constituents of the flavonoids fraction from M. autumnalis ripe fruit (FFM), and evaluate its DPPH scavenging, anti-lipase, cytotoxicity, antimicrobial and antidiabetic effects. An ethyl acetate extract of M. autumnalis was subjected to a sequence of silica gel column chromatography using different eluents with various polarities. The chemical structures of the isolated compounds were identified using different spectral techniques, including ¹H NMR and ¹³C NMR. FFM’s anti-diabetic activity was assessed using a glucose transporter-4 (GLUT4) translocation assay, as well as an inhibition against α-amylase and α-glucosidase using standard biochemical assays. The FFM anti-lipase effect against porcine pancreatic lipase was also evaluated. Moreover, FFM free radical scavenging activity using the DPPH test and antimicrobial properties against eight microbial strains using the micro-dilution method were also assessed. Four flavonoid aglycones were separated from FFM and their chemical structures were identified. The structures of the isolated compounds were established as kaempferol 1, luteolin 2, myricetin 3 and (+)-taxifolin 4, based on NMR spectroscopic analyses. The cytotoxicity test results showed high cell viability (at least 90%) for up to 1 mg/mL concentration of FFM, which is considered to be safe. A dose-dependent increase in GLUT4 translocation was significantly shown (p < 0.05) when the muscle cells were treated with FFM up to 0.5 mg/mL. Moreover, FFM revealed potent α-amylase, α-glucosidase, DPPH scavenging and porcine pancreatic lipase inhibitory activities compared with the positive controls, with IC₅₀ values of 72.44 ± 0.89, 39.81 ± 0.74, 5.37 ± 0.41 and 39.81 ± 1.23 µg/mL, respectively. In addition, FFM inhibited the growth of all of the tested bacterial and fungal strains and showed the greatest antibacterial activity against the K. pneumoniae strain with a MIC value of 0.135 µg/mL. The four flavonoid molecules that constitute the FFM have been shown to have medicinal promise. Further in vivo testing and formulation design are needed to corroborate these findings, which are integral to the pharmaceutical and food supplement industries.     

Synthesis of indole-based oxadiazoles and their interaction with bacterial peptidoglycan and SARS-CoV-2 main protease: In vitro,molecular docking and in silico ADME/Tox study

In the present study, Indole-based-oxadiazole (1A-17A) compounds were successfully synthesized. The structures of all synthesized compounds were fully characterized by different sophisticated spectroscopic techniques such 1H NMR, 13C NMR, and HREI-MS. Further, the synthesized compounds were explored to investigate their broad-spectrum antibacterial and antibiofilm potential against multidrug resistant Pseudomonas aeruginosa (MDR-PA) and methicillin resistant Staphylococcus aureus (MRSA). The compounds possessed a broad spectrum of antibacterial activity having MIC values of values 1–8 mg/ml against the tested microorganisms. Compound A6 and A7 shows maximum antibacterial activity against MDR-PA, whereas A6, A7 and A11 shows highest activity against MRSA. Furthermore, antibiofilm assay shows that A6, A7 and A11 showed maximum inhibition of biofilm formation and it was found that at 4 mg/ml; A6, A7 and A11 inhibit MRSA biofilm formation by 81.1, 77.5 and 75.9%, respectively; whereas in case of P. aeruginosa; A6 and A7 showed maximum biofilm inhibition and inhibit biofilm formation by 81.5 and 73.7%, respectively. Molecular docking study showed that compounds A6, A7, A8, A10, and A11 had high binding affinity to bacterial peptidoglycan, indicating their potential inhibitory activity against tested bacteria, whereas A6 and A11 were found to be the most effective inhibitors of SARS CoV-2 main protease (3CLpro), with a binding affinity of ? 7.78 kcal/mol. Furthermore, SwissADME and pkCSM-pharmacokinetics online tools was applied to calculate the ADME/Tox profile of the synthesized compounds and the toxicity of these chemicals was found to be low. The Lipinski, Veber, Ghose, and Consensus LogP criteria were also used to predict drug-likeness levels of the compounds. Our findings imply that the synthesized compounds could be a useful for the preventing and treating biofilm-related microbial infection as well as SARS-CoV2 infections.     

Profile characterization and biological activities of cold pressed Garden Cress (Lepidium sativum) seed oil

Lepidium sativum is cultivated mainly for the edible oil from its seeds, and considered as an unutilized and neglected crop despite its important properties. Its oil fraction is used to produce soap and stabilize linseed oil when it is mixed with wild mustard seed oil. Once converted into fatty acid methyl esters, it represents a good substitute for imported petroleum diesel after alkaline transesterification reaction. In the current study, Lepidium sativum seeds cultivated in Tunisia and the physicochemical properties and nutrient profile of its cold pressed seed oil were investigated. The antioxidant, antibacterial, and anti-inflammatory activities of the above oil were also assessed. Lepidium sativum seed oil was abundant in both linolenic (35.59 ± 1.9%) and oleic (21.14 ± 0.63%) acids, and high amounts of β-sitosterol (42.57 ± 2.96 mg/100 g), campesterol (20.04 ± 1.4 mg/100 g) and Δ 5,24 stigmastadienol (11.82 ± 0.45 mg/100 g) were detected. The total tocopherol content of Lepidium sativum seed oil reached 136.83 ± 7.6 mg/100 g with a predominance of γ-tocopherol (86.23%). Its seed oil exhibited an IC₅₀ of 10.33 ± 0.05 mg/mL and a radical scavenging activity of 415.6 ± 40 Trolox Equivalent Antioxidant Capacity (TEAC) for the DPPH and the ABTS assays, respectively. While the thermal analysis proved a high thermal stability of Lepidium sativum seed oil, that of eight bacteria and one fungal strain showed no noticeable bacterial or antifungal effects. It was also revealed that Lepidium sativum seed oil held a remarkable anti-inflammatory activity. Hence, the obtained results evidenced remarkable chemical, antioxidant and anti-inflammatory properties of Lepidium sativum seed oil, which might potentially be promising for enhancing human health and preventing age-related diseases.     

Chemical Profile,Antimicrobial and Antioxidant Activity Assessment of the Crude Extract and Its Main Flavonoids from Tartary Buckwheat Sprouts

The purpose of this study was to investigate the major flavonoids content and bioactivities of Tartary buckwheat sprouts. The crude methanol extract (ME) of Tartary buckwheat sprouts was abundant in flavonoids, and six major flavonoids, including isoorientin, vitexin, isovitexin, rutin, quercetin, and kaemferol were successfully determined from the sprouts by the high-performance liquid chromatography (HPLC) method. Generally, the flavonoid content of buckwheat sprouts was in the order of rutin > quercetin > isovitexin > vitexin> isoorientin > kaemferol. The highest rutin content of the ME and sprout cultures was 89.81 mg/g and 31.50 mg/g, respectively. Antibacterial activity results indicated the ME displayed notable inhibitory activity against the five tested bacteria, and its minimum inhibitory concentration (MIC) values ranged from 0.8 mg/mL to 3.2 mg/mL. Among the six flavonoids, quercetin was the most active compound, which exhibited strong activity against all tested bacteria except for E. coli and S. epidermidis, with its MIC values ranging from 0.2 mg/mL to 0.4 mg/mL. For the antifungal activity assay, the ME of Tartary buckwheat sprouts and four flavonoids could significantly inhibit the spore germination of two pathogenic fungi, and their inhibitory efficiency was concentration dependent. Quercetin was the most active one, which significantly inhibited the spore germination of F. oxysporum f. sp. vasinfectum and F. oxysporum f. sp. cucumerinum, and its median effective inhibitory concentration (IC₅₀) value was 42.36 and 32.85 µg/mL, respectively. The antioxidant activity results showed that quercetin, kaemferol, and rutin displayed excellent antioxidant activity in the DPPH radical scavenging test, and their IC₅₀ value was calculated as 5.60, 16.23, and 27.95 µg/mL, respectively. This is the first report on the antimicrobial activity of the crude extract of Tartary buckwheat sprouts. These results indicated that the methanol extract of Tartary buckwheat sprouts could be used as a potential antimicrobial or antioxidant agent in the future.     

Chemical profiling of Aristolochia tagala Cham. leaf extracts by GC-MS analysis and evaluation of its antibacterial activity

Aristolochia tagala Cham. (Aristolochiaceae) is an underexplored medicinal plant traditionally used to treat snakebites, stomachaches, and poisonous bites. In this study, chemical profiling of the petroleum ether, chloroform, ethyl acetate, methanol, and hydro-alcoholic extracts of the plant was investigated by gas chromatography-mass spectrometry. The antibacterial activity of the plant was tested against ten bacterial strains using the agar disc diffusion and microdilution method. In total, forty two compounds were identified from the extracts with neophytadiene, palmitic acid, phytol, trans-δ9-octadecenoic acid, phytyl palmitate, phytyl tetradecanoate, ergost-5-en-3-ol, (3beta,24r)-,z,z-8,10-hexadecadien-1-ol, stigmasterol, and tetrapentacontane as major phytoconstituents. The hydro-alcoholic extract possessed maximum total phenolics (52.58 ± 06 mg GAE/g), total flavonoids (48.66 ± 91 QRE/g), total flavanols (67.20 ± 64 QRE/g) and vitamin E content (31.26 ± 0.05 mg ATE/g). For antibacterial activity, hydro-alcoholic extract of Aristolochia tagala effectively controlled the growth of bacterial strains such as Proteus valgaris (26.3 mm) and Pseudomonas aeruginosa (19.33 mm) and the same extract showed notable minimum inhibitory concentration (MIC) against the growth of bacteria like Escherichia coli (10.93 μg/ml) and Enterobacter aerogenes (43.7 μg/ml). It was determined that, hydro-alcoholic and methanolic extracts Aristolochia tagala leaf found to have a number of bioactive compounds with significant antibacterial activity against the pathogenic bacteria. Further investigations are necessary to isolate and characterize bioactives and to evaluate its therapeutic potential.     

Multifunctional approaches to provide potential pharmacophores for the pharmacy shelf: Heracleum sphondylium L. subsp. ternatum (Velen.) Brummitt.

Heracleum sphondylium L. subsp. ternatum (Velen.) Brummitt. commonly known as “hogweed” is traditionally used to manage several human ailments. This investigation assessed, for the first time, the enzyme inhibitory properties, antioxidant activity, phytochemical profile, antimutagenic, and antimicrobial potential of the ethyl acetate, methanol, and water extracts of H. sphondylium. We also established the possible interactions of identified phenolic compounds with cholinesterases, amylase, glucosidase, and tyrosinase using in silico docking studies. Chlorogenic acid was found in high amounts in the methanol extract of H. sphondylium. The methanol extract was an effective inhibitor of acetylcholinesterase (1.70 mg galantamine equivalent (GALAE)/g extract) while the ethyl acetate extract showed pronounced inhibitory action against butyrylcholinesterase (1.77 mg GALAE/g extract). The extracts exhibited low inhibition against amylase (0.12-0.84 mmol acarbose equivalent (ACAE)/g extract) and a more pronounced inhibition against glucosidase (2.29–3.65 mmol ACAE/g extract). In silico results showed that rutin and quercetin (-70.4 and -72.2 Kcal/mol, for rutin and quercetin respectively) docked to the enzymatic cavity of acetylcholinesterase but these phenolic compounds showed less affinity with butyrylcholinesterase (-15.0 and -5.2 Kcal/mol, for rutin and quercetin respectively). The extracts did not induce any mutations on the bacterial strains, while they have excellent antimutagenic capacity against well-known mutagens (inhibition values 98%, 97% and 96%). The methanol extract (0.78 mg/ml) showed moderate antifungal activity while the ethyl acetate extract (0.78–3.12 mg/ml) showed weak to moderate antimicrobial activity. This study provides valuable baseline data which might serve for the development of future pharmacophores for the management of human ailments.     

Bioprospecting Dodonaea viscosa Jacq.; a traditional medicinal plant for antioxidant,cytotoxic, antidiabetic and antimicrobial potential

Purpose of studyDodonaea viscosa Jacq. is an ethnomedicinal plant that has been extensively used for the treatment of gout, rheumatism and pain. Current study was undertaken to mine its antioxidant, antimicrobial, cytotoxic and antidiabetic potential. Chromogenic assays were employed to establish plant’s multimode antioxidant profile whereas HPLC fingerprinting was performed to quantify polyphenols. Standard brine shrimp lethality, MTT and SRB assays proved its cytotoxicity potential.ResultsAmong all the extracts (flower, leaf, stem and root), maximum extract recovery (22% w/w), gallic acid equivalent total phenolic content (20.11 ± 0.11 ug GAE/mg DW), ascorbic acid equivalent total antioxidant capacity (22.5 ± 0.07 µg/mg DW) and total reducing power (31.1 ± 1.13 µg/mg DW) were recorded in the distilled water + acetone extract of leaf. The acetone extract of leaf showed maximum quercetin equivalent total flavonoid content (4.78 ± 0.13 µg/mg DW). HPLC-DAD analysis revealed significant amount of rutin, vanillic acid, coumaric acid, ferulic acid, gallic acid, syringic acid, cinnamic acid, gentisic acid, catechin, caffeic acid, apigenin and myricetin in the different plant parts. Maximum scavenging potential was exhibited by methanol + ethyl acetate stem extract (IC₅₀ = 23.8 µg/ml). The highest antibacterial potential was found in flower (85.7%) and root (71.4%) extracts. The ethanol + ethyl acetate (1:1) leaf extract showed noteworthy toxicity against brine shrimps (LC₅₀ = 95.46 µg/ml) while a notable antiproliferative activity against THP-1 (IC₅₀ = 3.4 µg/ml) and Hep G2 (IC₅₀ = 20 µg/ml) cell lines was shown by ethanol + ethyl acetate extracts (1:1) of stem and root, respectively. A moderate inhibition of α-amylase enzyme was observed in all parts of the plant.ConclusionThe results of the present study suggest D. viscosa as a potential source of antioxidant, anticancer and α-amylase inhibitory phytochemicals.     

Antimicrobial and cytotoxicity properties of biosynthesized gold and silver nanoparticles using D. brittonii aqueous extract

Recently, the production of nanoparticles using biological resources has gained considerable attention due to their application for animal and human well-being. In this study, we used a green synthesis to fabricate gold and silver nanoparticles by reducing HAuCl₄ and AgNO₃ into AuNPs and AgNPs, respectively, using Dudleya brittonii (DB) extract. The physio-chemical properties of the synthesized nanoparticles were analyzed using a UV–vis spectrophotometer, FESEM, EDX, HR-TEM, AFM and FT-IR. Furthermore, the antimicrobial and cytotoxicity activities of DB-AuNPs and DB-AgNPs against livestock pathogenic bacteria and different cell lines, as well as anti-oxidant activity, were investigated. DB synthesized AuNPs and AgNPs were mostly spherical with a few triangular rods and sizes ranging of 5–25 nm and 10–40 nm, respectively. The in vitro antibacterial and antifungal studies demonstrated the DB-AuNPs and DB-AgNPs have good antibacterial activity against E. coli and other livestock pathogens, including Y. pseudotuberculosis and S. typhi. Cell studies revealed that the higher concentrations of both DB-AuNPs and DB-AgNPs (1 µg/ml to 1 mg/ml) showed potent cytotoxicity in chicken cells after 24 hrs, whereas the middle and lower concentrations of DB-AuNPs and DB-AgNPs did not show cytotoxicity in selected cell lines after 24 hrs. In addition, the DB synthesized AuNPs and AgNPs exhibited good free scavenging activity in a dose-dependent manner. Therefore, the biosynthesized nanoparticles can be utilized by the livestock industry to develop an effective source against livestock microbial infections.     

Novel Pyrazoline‐based Organometallic Compounds Containing Ferrocenyl and Quinoline units: Synthesis,Characterization and Microbial susceptibilities

Some novel pyrazoline‐based organometallic compounds were synthesized as new leads in antimicrobial chemotherapy. The structures of compounds were elucidated by different spectroscopic techniques and elemental analyses. All compounds were investigated for in vitro antimicrobial studies against fifteen ATTC bacterial and fungal strains. The microbial susceptibility of these compounds revealed that all the tested compounds gave good minimum inhibitory concentration (MIC) values against the tested organisms that are either similar or even better than the reference drugs amoxicillin and fluconazole, which gave MIC values 8‐64 μg/ml against bacterial and 64 μg/ml against fungal strains, respectively. Among all compounds, compound ( 4d ) 1‐(5‐(4‐chlorophenyl)‐3‐ferrocenyl‐4,5‐dihydropyrazol‐1‐yl)‐2‐quinolin‐8‐yloxy) ethanone, emerged out the most promising antimicrobial organometallic derivative with MIC values against all the strains ranging from 8‐32 μg/ml. Other compounds gave a range of MIC values between 16‐64 μg/ml against S. bovis, 16‐32 μg/ml against E. coli, and C. tropicalis except compound ( 4d) which gave MIC 8 μg/ml against S. bovis and E. coli, whereas 32 μg/ml against C. tropicalis. Collectively, these compounds gave a lower MIC value between 32‐64 μg/ml against both of the biofilm forming strains namely, P. aeruginosa and S. mutans. The results of microbial susceptibility concluded that these novel organometallic compounds are new leads in antimicrobial chemotherapy and can be very useful for further optimization work on microbial chemotherapy.     

Molecular docking of phenolic compounds and screening of antioxidant and antidiabetic potential of Olea europaea L. Ethanolic leaves extract

Oxidative stress has a crucial role in diabetic pathophysiology, therefore consuming naturally derived antioxidants as a remedial target. This study examines the naturally occurring antioxidant and antidiabetic of Olea europaea L. ethanolic leaves extract. Olea europaea L. leaves were macerated (OLE) by using absolute ethanol. Phytochemical and physiochemical analysis of OLE was screened using standard methods. The antioxidant effects were examined by DPPH (1, 1-diphenyl-2-picrylhydrazil) radical scavenging assay. In vitro antidiabetic was assayed by α-amylase enzyme inhibition study. Ethanolic extraction of OLE by maceration technique, 10% yield. Loss on drying, foreign organic matters and total ash value of OLE showed 2%, 0.2% and 16.5%, respectively. Phytochemical test on OLE confirmed saponin, flavonoid, glycoside, tannin, phenol and carbohydrate presences. The total phenolic and flavonoid contents of OLE is 490 mg GAE/g and 855 mg RUE/g of extract, respectively. OLE (IC₅₀ 38.37 ± 0.26 µg/ml) showed functional DPPH scavenging assay comparable to ascorbic acid (IC₅₀ 30.37 ± 0.17 µg/ml). In the alpha-amylase inhibitory activity, Acarbose showed an IC₅₀ value of 20.06 ± 0.19 µg/ml, while OLE portrayed an IC₅₀ value of 37.99 ± 0.15 µg/ml. The kinetic studies revealed that all samples at high concentrations reacted within a very short time, and a steady state was reached almost immediately. The lowest concentration showed slow kinetic behaviour implied longer periods before the constant state was reached. Molecular docking studies evidenced that most of the phenolic compounds of OLE interact with the active site of Human pancreatic α-amylase through the hydrogen bonding and hydrophobic interaction confirming the alpha-amylase inhibitory effect. The results suggest that Olea europaea L. has been a conceivable natural bioactive source as an antioxidant and an antidiabetic agent.     

Phytochemical profiling and antimicrobial activity of ginger (Zingiber officinale) essential oils against important phytopathogens

The objectives of this study were to profile ginger essential oils (EOs) phytochemical constituents and antimicrobial activity against important phytopathogens. Ginger EOs was extracted using a modified Clevenger-type apparatus by hydro-distillation then followed by GCMS and headspace analysis of its phytochemical constituents. The phytoconstituents identified were monoterpenes and sesquiterpene hydrocarbons. Food poisoned and disc diffusion techniques were applied to determine the percentage inhibition of fungal mycelial and bacterial growth respectively. The EOs produced mycelial growth inhibition in all the test fungal pathogens after five days of incubation. The MIC and MFC of the EOs on the tested fungi were in the range of 1 μl/ml and 5–6 μl/ml, respectively. The bacterial growth of all the tested isolates was also affected by EOs at 100–500 µl/ml, from weak to strong antibacterial activity. The EOs affected the Xanthomonas oryzae pv. oryzae-strain A isolate most at a higher concentration of 400–500 μl/ml with mean inhibition of 20.66 mm and 22.66 mm respectively, which are found to be effective. The MIC values on the bacterial pathogens were at100 μl/ml. The inhibition zone of positive control (streptomycin) at 15 µg/disc was 25.00 mm and appeared to be efficient. Metabolomics analysis to concurrently quantify variability among multiple compounds in the data sets and identify such compounds responsible for the X. oryzae pv. oryzae-strain-A inhibition were determined. The cross-validated PLS model has shown a strong correlation between ginger EOs and bioactivity. The action of ginger EOs on the cell structure was fully identified using SEM by observing the changes in morphology and integrity of X. oryzae pv. oryzae-strain-A cells. The DMSO treatment (control) showed a normal rod shape cell, while treatment with the ginger EOs showed irregular shape with sunken surfaces, and treatment with antibiotics display abnormal growth of the cells. These findings can, therefore, propose that the ginger EOs could be used as a new antimicrobial agent in suppressing the growth of phytopathogens and as possible new alternatives to synthetic fungicides and bactericides.     

Polarity guided extraction,HPLC based phytochemical quantification,and multimode biological evaluation of Otostegia limbata (Benth.) Boiss

Purpose of studyOtostegia limbata (Benth.) Boiss. (Family: Lamiacae) is an important underexplored ethnomedicinal plant that has been used as antinflammatory, anticancer and antibacterial herbal remedy previously. The present work was aimed to evaluate the antioxidant, antimicrobial, antileishmanial, and anticancer prospective of O. limbata stem and leaf extracts.ResultsThe highest amount of phenolic and flavonoid content was obtained in the methanol-acetone and methanol stem extracts i.e., 53.29 ± 1.33 and 28.64 ± 1.16, respectively with highest DPPH scavenging in MeH stem extract (IC₅₀ = 34.5 ± 1.34 μg/ml). Significant amount of catechin, gallic acid, apigenin and rutin was quantified. A moderate antibacterial and substantial antifungal activity was observed. Cytotoxicity against brine shrimps categorized 21% of stem (3 out of 14 extracts) and 57% (8 out of 14 extracts) of leaf extracts as potent. Substantial cytotoxicity against THP-1 cell line (IC₅₀ = 3.46 ± 0.25 μg/ml) and Leishmania (IC₅₀ = 1.50 ± 0.23 μg/ml) was exhibited by methanol-distilled water leaf extract while noteworthy antiproliferative activity against Hep-G2 (IC₅₀ = 0.44 ± 0.45 μg/ml) was manifested by n-hexane stem extract. Absence of hemolysis in normal RBCs signified plant’s selective cytotoxicity. Methanol-distilled water and chloroform stem extracts displayed prominent protein kinase inhibition and antidiabetic potential of plant.ConclusionThe results of present study recommend O. limbata as a potential source of antifungal, antileishmanial, anticancer, and α-amylase inhibitory agents.     

Anti-Helicobacter pylori Activity of Artemisia ludoviciana subsp. mexicana and Two of Its Bioactive Components,Estafiatin and Eupatilin

Artemisia ludoviciana subsp. mexicana has been traditionally used for the treatment of digestive ailments such as gastritis, whose main etiological agent is Helicobacter pylori. In a previous screening study, the aqueous extract exhibited a good in vitro anti-H. pylori activity. With the aim of determining the efficacy of this species as a treatment for H. pylori related diseases and finding bioactive compounds, its aqueous extract was subjected to solvent partitioning and the fractions obtained were tested for their in vitro anti-H. pylori effect, as well as for their in vivo gastroprotective and anti-inflammatory activities. The aqueous extract showed a MIC = 250 µg/mL. No acute toxicity was induced in mice. A gastroprotection of 69.8 ± 3.8%, as well as anti-inflammatory effects of 47.6 ± 12.4% and 38.8 ± 10.2% (by oral and topical administration, respectively), were attained. Estafiatin and eupatilin were isolated and exhibited anti-H. pylori activity with MBCs of 15.6 and 31.2 µg/mL, respectively. The finding that A. ludoviciana aqueous extract has significant anti-H. pylori, gastroprotective and anti-inflammatory activities is a relevant contribution to the ethnopharmacological knowledge of this species. This work is the first report about the in vivo gastroprotective activity of A. ludoviciana and the anti-H. pylori activity of eupatilin and estafiatin.