Aspergillus flavus originated pure compound as a potential antibacterial.

PROBLEM BACKGROUND: Penicillin was the first and most famous fungal secondary metabolite used as broad spectrum antibiotic that revolutionarised pharmaceutical research and also saved millions of lives. The over optimistic belief in 1967 that sufficient antibiotics had been discovered to defeat infectious diseases was quickly crashed with the appearance of multidrug resistant (MDR) bacteria in 1990s. This has posed a serious threat to mankind. Although scientists are making efforts to synthesize and discover new antibiotics there are not enough new drugs in pharmaceutical pipeline to beat the pace at which MDR bacteria are emerging. In view of this there is an urgent and serious medical need for new bioactive compounds to be discovered to treat infections caused by MDR pathogens. The present study is aimed to investigate the antibacterial potential of Aspergillus flavus originated compounds that may act as drug leads to treat future infections. METHODOLOGY: Among the 6 isolated fungal strains from the rhizosphere of Mentha piperetta, one was processed for isolation of secondary metabolites on the basis of preliminary antibacterial testing. Observation of morphological and microscopic features helped in identification of the fungal strain as Aspergillus flavus. Potato Dextrose Agar (PDA) medium was used for fungal growth while Czapec Yeast Broth (CYB) medium was used for production of fungal metabolites. Column chromatography technique was utilized for purification of compound from crude fungal extract and the mass of the compound was determined using Liquid Chromatography Mass Spectrometry (LCMS) method. Structure elucidation of the pure compound was performed using 500 Varian Nuclear Magnetic Resonance (NMR) machine. Docking was performed using Glide SP algorithm. Agar well diffusion method was used to determine the invitro antibacterial potential of the compound against two MDR bacterial strains i.e. Staphylococcus aureus and Proteus vulgaris. For this a total of 4 dose concentrations i.e. (100, 250, 500, 1000 µg mL- 1) of the compound were prepared and applied to bacterial strains on Mueller Hinton agar using tetracycline as control. RESULTS: The chemical name of the purified compound from A. flavus was determined as (2E)-3-[(3S, 4R)-8-hydroxy-3, 4-dimethyl-1-oxo-3, 4-dihydro-1H-2- benzopyran-7-yl] prop-2-enoic acid with the formula C14H14O5 and exact mass of 262.08. The in-Silico analysis showed that this compound has the potential to inhibit the binding pocket of S. aureus TyrRS (1JII) with docking score of - 8.67 Kcal mole- 1. The results obtained from invitro experiments were encouraging as at 1000 µg mL- 1 the compound showed 58.8% inhibition against S. aureus and 28% inhibition against P. vulgaris. CONCLUSIONS: The pure compound with formula C14H14O5 and exact mass of 262 exhibited antibacterial potential both insilico and invitro against both Gram negative and Gram positive bacteria. The compound was more active against S. aureus in comparison to P. vulgaris. From the obtained results it is concluded that this compound can be used as potent antibacterial candidate but further studies will be needed prior to its use as antibiotic.

Antimicrobial and antioxidant activities of silver nanoparticles synthesized by novel biogenic method using mixed reductants.

A novel method, for the synthesis of silver nanoparticles that are eco-friendly by means of mixed reductants method, has been developed. The combined extract of Mentha viridis plant and Prunus domestica gum were used as reducing agents for the synthesis of silver nanoparticles of the size less than 40 nm in diameter. The effect of time and concentration on the formation of silver nanoparticles were also monitored. The silver nanoparticles formed were verified by surface Plasmon spectra using single and double beam UV-Vis spectrophotometer. The XRD technique and scanning electron microscopy were performed to analyze the crystalline structure, crystallite size and morphology. The synthesized silver nanoparticles were tested against different bacterial and fungus strains. The silver nanoparticles showed good inhibition in antimicrobial study and low MIC for bacterial strains. The antioxidant assay was performed to check the scavenging activity. In DPPH, the silver nanoparticles showed good scavenging activity and were found close to that of ascorbic acid.

A Novel Non-Coding RNA CsiR Regulates the Ciprofloxacin Resistance in Proteus vulgaris by Interacting with emrB mRNA.

Bacterial non-coding RNAs (ncRNAs) play important regulatory roles in various physiological metabolic pathways. In this study, a novel ncRNA CsiR (ciprofloxacin stress-induced ncRNA) involved in the regulation of ciprofloxacin resistance in the foodborne multidrug-resistant Proteus vulgaris (P. vulgaris) strain P3M was identified. The survival rate of the CsiR-deficient strain was higher than that of the wild-type strain P3M under the ciprofloxacin treatment condition, indicating that CsiR played a negative regulatory role, and its target gene emrB was identified through further target prediction, quantitative real-time PCR (qRT-PCR), and microscale thermophoresis (MST). Further studies showed that the interaction between CsiR and emrB mRNA affected the stability of the latter at the post-transcriptional level to a large degree, and ultimately affected the ciprofloxacin resistance of P3M. Notably, the base-pairing sites between CsiR and emrB mRNAs were highly conserved in other sequenced P. vulgaris strains, suggesting that this regulatory mechanism may be ubiquitous in this species. To the best of our knowledge, this is the first identification of a novel ncRNA involved in the regulation of ciprofloxacin resistance in P. vulgaris species, which lays a solid foundation for comprehensively expounding the antibiotic resistance mechanism of P. vulgaris.

New pyrimidine and pyrazole-based compounds as potential EGFR inhibitors: Synthesis, anticancer, antimicrobial evaluation and computational studies.

This study was focused on the synthesis of new pyrimidines 4a,b, 5a,b and pyrazoles 6a, b as ATP mimicking tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). The new compounds were assessed as cytotoxic candidates against human breast cancer cells (MCF-7) and hepatocellular carcinoma cells (HepG-2). All the new compounds appeared as more potent cytotoxic agents than erlotinib, while only compound 4a exhibited more potency than 5-flourouracil and 4b analogue was equipotent to it. Accordingly, the kinase suppression effect of 4a and 4b was further evaluated against EGFRWT, EGFRL858R and EGFRT790M. Both pyrimidine analogues 4a and 4b displayed outstanding inhibitory activity against EGFRWT and its two mutated isoforms EGFRL858R and EGFRT790M in comparing to erlotinib and osimertinib as reference drugs. Additionally, all the new analogues were subjected to antimicrobial assay. Interestingly, both 4a and 4b represented the most promising activity of wide spectrum antimicrobial effect against the examined microbes in comparison to gentamycin and ketoconazole as standard drugs. Moreover, docking results proved the good binding interactions of the compounds 4a and 4b with EGFRWT and EGFRT790M which were in accordance with the results of the in vitro enzyme assay. Additional in silico ADMET studies were performed for the new derivatives which represented their good oral absorption, good drug-likeness properties and low toxicity risks in human.

Characterization of Proteus vulgaris Strain P3M, a Foodborne Multidrug-Resistant Bacterium Isolated from Penaeus vannamei in China.

Proteus vulgaris is an important foodborne opportunistic pathogen, both environmentally and clinically. The use of appropriate antibiotics has significant therapeutic effects, but has led to the emergence and spread of drug-resistant strains. In this study, a P. vulgaris strain, designated "P3M," was isolated from Penaeus vannamei in Tianjin, China. The whole genome of P3M was sequenced, generating detailed information, including the key genes involved in important metabolic pathways and their physiological functions. A total of 218 antibiotic resistance genes (ARGs) were predicted in the genome. The determination of various minimum inhibitory concentrations indicated that P3M is a multidrug-resistant (MDR) bacterium, with significant resistance to 16 antibiotics in seven categories. Determination of fractional inhibitory concentration index showed that the combination of ciprofloxacin plus tetracycline exhibited synergistic antimicrobial activity. Bioinformatics and phylogenetic analyses detected the presence of two two-component systems that mediate multidrug resistance and several mobile genetic elements involved in the horizontal transfer of ARGs in P3M. P. vulgaris strains represent a serious challenge to clinicians and infection control teams for its ubiquity worldwide and close relevance with human life. To the best of our knowledge, we report the first isolation and characterization of an important foodborne MDR P. vulgaris strain, and this study will provide necessary theoretical basis for the selection and clinical use of the appropriate antibiotics.

New Mononuclear and Binuclear Cu(II), Co(II), Ni(II), and Zn(II) Thiosemicarbazone Complexes with Potential Biological Activity: Antimicrobial and Molecular Docking Study.

Herein, we report the synthesis of eight new mononuclear and binuclear Co2+, Ni2+, Cu2+, and Zn2+ methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and its metal complexes was fully characterized by elemental analysis, spectroscopic techniques (NMR, FTIR, UV-Vis), molar conductivity, thermogravimetric analysis (TG), and thermal differential analysis (DrTGA). The spectral and analytical data revealed that the obtained thiosemicarbazone-metal complexes have octahedral geometry around the metal center, except for the Zn2+-thiosemicarbazone complexes, which showed a tetrahedral geometry. The antibacterial and antifungal activities of the MTSC ligand and its (Co2+, Ni2+, Cu2+, and Zn2+) metal complexes were also investigated. Interestingly, the antibacterial activity of MTSC- metal complexes against examined bacteria was higher than that of the MTSC alone, which indicates that metal complexation improved the antibacterial activity of the parent ligand. Among different metal complexes, the MTSC- mono- and binuclear Cu2+ complexes showed significant antibacterial activity against Bacillus subtilis and Proteus vulgaris, better than that of the standard gentamycin drug. The in silico molecular docking study has revealed that the MTSC ligand could be a potential inhibitor for the oxidoreductase protein.

Alginate-gum acacia based sponges as potential wound dressings for exuding and bleeding wounds.

The improper management of wound exudates can expose the wound to bacterial invasion, skin maceration etc. thereby resulting in prolonged wound healing. Biopolymers are characterized by hydrophilic functional groups which when employed for the development of wound dressings promote the wound dressings capability to absorb a high amount of wound exudates. Alginate-gum acacia sponges were prepared from a combination of biopolymers such as sodium alginate and gum acacia in varying amounts with carbopol via crosslinking with 1 and 2% CaCl2. The prepared sponges were loaded with a combination of ampicillin and norfloxacin. In vitro antibacterial analysis revealed that the antibacterial activity of the loaded antibiotics was retained and the sponges were effective against gram-positive and gram-negative bacteria. The sponges displayed rapid and high absorption capability in the range of 1022-2419% at pH 5.5 simulating wound exudates, and 2268-5042% at pH 7.4 simulating blood within a period of 1-3 h. Furthermore, the whole blood clotting studies further revealed low absorbance values when compared to the control revealing the good clotting capability of the sponges. The unique features of the sponges revealed their potential application for the management of infected, high exuding and bleeding wounds.

Phytochemical Profile, Antimicrobial, Cytotoxic, and Antioxidant Activities of Fresh and Air-Dried Satureja nabateorum Essential Oils.

Satureja nabateorum (Danin and Hedge) Bräuchler is a perennial herb in the Lamiaceae family that was discovered and classified in 1998. This green herb is restricted to the mountains overlooking the Dead Sea, specifically in Jordan's southwest, the Edom mountains, and the Tubas mountains in Palestine. Gas chromatography-mass spectrometry (GC-MS) analysis of essential oil (EO) of air-dried and fresh S. nabateorum resulted in the identification of 30 and 42 phytochemicals accounting for 99.56 and 98.64% of the EO, respectively. Thymol (46.07 ± 1.1 and 40.64 ± 1.21%) was the major compound, followed by its biosynthetic precursors γ-terpinene (21.15 ± 1.05% and 20.65 ± 1.12%), and p-cymene (15.02 ± 1.02% and 11.51 ± 0.97%), respectively. Microdilution assay was used to evaluate the antimicrobial property of EOs against Staphylococcus aureus (ATCC 25923), clinical isolate Methicillin-Resistant Staphylococcus aureus (MRSA), Enterococcus faecium (ATCC 700221) Klebsiella pneumoniae (ATCC 13883), Proteus vulgaris (ATCC 700221), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853) and Candida albicans (ATCC-90028). With a MIC of 0.135 µg/mL, the EOs has the most potent antibacterial action against K. pneumonia. Both EOs display good antifungal efficacy against C. albicans, with a MIC value of 0.75 µg/mL, which was better than that of Fluconazole's (positive control, MIC = 1.56 µg/mL). The antioxidant capacity of EOs extracted from air-dried and fresh S. nabateorum was determined using the DPPH assay, with IC50 values of 4.78 ± 0.41 and 5.37 ± 0.40 µg/mL, respectively. The tested EOs showed significant cytotoxicity against Hela, HepG2, and COLO-205 cells, with IC50 values ranging from 82 ± 0.98 to 256 ± 1.95 µg/mL. The current work shows there is a possibility to use the S. nabateorum EOs for various applications.

Establishment and elicitation of transgenic root culture of Plantago lanceolata and evaluation of its anti-bacterial and cytotoxicity activity.

Hairy root induction in Plantago lanceolata was optimized to take advantage of transformed root cultures. The highest frequency of transformation was achieved using leaf explant, A4 strain, pre-cultivation of explant, 150 µM Acetosyringone, 5 min inoculation, half-strength Murashige and Skoog basal medium as co-cultivation, and half-strength Gamborg's basal medium as a selective medium with 3% sucrose. Among the studied compound encompassing gallic acid, catalpol and apigenin, only the production of gallic acid in hairy roots was affected by 20 mg L-1 AgNO3 and 100 mg L-1 chitosan at 24 hr which yielded 7.63, 4.76-fold increase in its content, respectively. The methanolic extracts of hairy roots elicited by 20 mg L-1 AgNO3 exhibited anti-bacterial activity (MIC and MBC = 25 mg mL-1) against Klebsiella pneumoniae, Proteus vulgaris and Salmonella typhi and anti-bacterial potential of non-elicited hairy roots of P. lanceolata (MIC = 25 mg mL-1 and MBC = 35 mg mL-1) were more active against Klebsiella pneumoniae and P. vulgaris than other bacteria. The methanolic extracts of the P. lanceolata hairy roots demonstrated significant cytotoxic activity on colorectal carcinoma cell line (SW-480) with IC50 = 250.65 ± 6.8 µg mL-1 in comparison to human embryonic kidney (HEK-293) with IC50 = 5263.65 ± 4.6 µg mL-1. Plantago lanceolata hairy roots showed important biological activity explaining its role in traditional medicine.

The antibacterial and antihemolytic activities assessment of zinc oxide nanoparticles synthesized using plant extracts and gamma irradiation against the uro-pathogenic multidrug resistant Proteus vulgaris.

In the case of Proteus vulgaris infection, the increased occurrence of multidrug-resistance strains has become a critical challenge in the treatment of urinary tract diseases. Therefore, using plant extracts as eco-friendly antibacterial provides an attractive solution to battle bacterial infection. The current study investigates the antibacterial and antihemolytic activity of nine medicinal plant extracts against P. vulgaris. Citrus limon extract at 150 µg/ml exhibited the highest antimicrobial action against P. vulgaris (the inhibition zone diameter; 22.7 mm). Zinc oxide nanoparticles (ZnO NPs) are synthesized using the plant extracts of C. limon, Allium sativum, Sonchus bulbosus, Allium cepa, and Asparagus racemosus. The antibacterial activity of ZnO NPs synthesized using C. limon extract at 150 µg/ml is significantly increased (33.8 mm). ZnO NPs synthesized using A. cepa, A. racemosus, and C. limon plant extracts are effectively protective for human red blood cells. The ZnO NPs synthesized using C. limon extract are characterized using UV-Visible spectroscopy, FTIR, XRD, and TEM. FTIR revealed that the plant extracts may serve as reducing and capping agents of ZnO NPs. XRD spectra confirmed the crystallinity of ZnO NPs. TEM image demonstrated the formation of spherical shapes of ZnO NPs with an average size of 37.05 nm. SEM of P. vulgaris cells treated with ZnO NPs showed cellular morphological damage compared to the untreated cells. ZnO NPs are synthesized by gamma irradiation as a clean and novel method. This study recommended the promising uses of the biosynthesized ZnO NPs using plant extracts as a natural, unique approach, to control the pathogenicity of P. vulgaris.

Bioactive components, antioxidant and antimicrobial activities of Paeonia rockii fruit during development.

In last ten years, much attention focused on tree peony fruit (TPF) for edible oil production despite other potential utilization. The present study identified and quantified 29 bioactive components by liquid chromatography-electrospray ionization-triple quadrupole-mass spectrometry (LC-ESI-QqQ-MS) targeted approach during the development of TPF. Trans-resveratrol, benzoic acid, luteolin, and methyl gallate were selected as predominant chemical markers between seeds and pods through principal component analysis (PCA) and orthogonal partial least square-discriminant analysis (OPLS-DA). Extremely high levels of paeoniflorin (1893 mg/100 g) and trans-resveratrol (1793 mg/100 g) were observed at stage 2 (S2) and S6 in seeds, respectively. Antioxidant activities determined by ABTS+•, DPPH•, and FRAP assays showed significant correlations with total phenolic content (TPC) and total flavonoid content (TFC). The strongest antibacterial effects of pod and seed against Staphylococcus aureus and Proteus vulgaris occurred at initial stages and maturation stages. TPF could be a potential source of bioactive compounds with functional properties.

Novel thiobarbiturates as potent urease inhibitors with potential antibacterial activity: Design, synthesis, radiolabeling and biodistribution study.

Urease enzyme is a virulence factor that helps in colonization and maintenance of highly pathogenic bacteria in human. Hence, the inhibition of urease enzymes is well-established to be a promising approach for preventing deleterious effects of ureolytic bacterial infections. In this work, novel thiobarbiturate derivatives were synthesized and evaluated for their urease inhibitory activity. All tested compounds effectively inhibited the activity of urease enzyme. Compounds 1, 2a, 2b, 4 and 9 displayed remarkable anti-urease activity (IC50 = 8.21-16.95 µM) superior to that of thiourea reference standard (IC50 = 20.04 µM). Moreover, compounds 3a, 3g, 5 and 8 were equipotent to thiourea. Among the tested compounds, morpholine derivative 4 (IC50 = 8.21 µM) was the most potent one, showing 2.5 folds the activity of thiourea. In addition, the antibacterial activity of the synthesized compounds was estimated against both standard strains and clinical isolates of urease producing bacteria. Compound 4 explored the highest potency exceeding that of cephalexin reference drug. Moreover, biodistribution study using radiolabeling approach revealed a remarked uptake of 99mTc-compound 4 into infection induced in mice. Furthermore, a molecular docking analysis revealed proper orientation of title compounds into the urease active site rationalizing their potent anti-urease activity.

Taxonomic identification and bioactive compounds characterization of Psilocybe cubensis DPT1 to probe its antibacterial and mosquito larvicidal competency.

Mushrooms have an important role in sustainability since they have long been used as valuable food source and traditional medicine around the world. Regrettably, they are among the most rigorously affected populations, along with several plants and animals, due to the destructive activities of mankind. Thus the authentication and conservation of mushroom species are constantly needed to exploit the remarkable potential in them. In this perspective, an attempt has been made to identify and assess the biological attributes of psychedelic mushrooms collected from Kodaikanal, Tamil Nadu, India. The macromorphological features of the psychedelic mushroom DPT1 helped its presumptive identification and the molecular characters depicted by DNA marker revealed its close relationship with the genus Psilocybe. Accordingly, the psychedelic mushroom was identified as Psilocybe cubensis DPT1 and its crude ethyl acetate extract on analysis revealed the occurrence of phytoconstituents like alkaloids, flavonoids, tannins, saponins and carbohydrates. Moreover, it exhibited 80% larvicidal activity against Culex quinquefasciatus mosquito at 800 ppm concentration and an array of antibacterial effects with utmost susceptibility of Proteus vulgaris, and the identification of bioactive compounds by different analytical techniques substantiate that the bioactivities might be due to the presence of phytochemicals. The results of the study indicated that the extract of P. cubensis DPT1 having notable antibacterial and mosquito larvicidal efficacies which could be probed further for the isolation of medicinally important as well as bio-control compounds.

Synthesis, in-Vitro Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles.

Condensation of rhodanine (1) with pyrazol-3(2H)-one derivatives (2a-f) gave 5-substituted-2-thioxo-1,3-thiazolidin-4-one derivatives (3a-f). Reaction of compound (1) with 2-arylmethylidene-malononitrile (4a-d) yielded the unexpected derivatives (5a-d). The latter compounds were subjected to cyclization reactions with malononitrile under different basic conditions, hydroxylamine hydrochloride and/or thiourea to furnish the fused thiazole derivatives (6a-d) and (8-10a-d). Coupling of (1) with diazotized aromatic amines (11a-c) in pyridine afforded the arylhydrazones (12a-c). Fusion of latter compounds with malononitrile afforded the thiazolopyridazine derivatives (13a-c). The structures of the newly synthesized compounds were elucidated via spectral data and elemental analyses. The in-vitro cytotoxic activity of compounds (3a-f) against the cell line MCF-7 was evaluated. Also, the synthesized products were investigated for their antibacterial and antifungal activities against six standard organisms including the G+ bacteria, Staphylococcus aureus and Bacillus subtilis, G- bacteria, Escherichia coli and Proteus vulgaris in addition to fungi, Candida albicans and Aspergillus flavus.

The Effect of Ten Essential Oils on Several Cutaneous Drug-Resistant Microorganisms and Their Cyto/Genotoxic and Antioxidant Properties.

In this study, we determined the antimicrobial activity of ten essential oils (EOs)-oregano, thyme, clove, arborvitae, cassia, lemongrass, melaleuca, eucalyptus, lavender, and clary sage-against drug-resistant microorganisms previously isolated from patients with skin infections. The essential oil compositions were determined using gas chromatography coupled to mass spectrometry (GC/MS). The assayed bacteria included Pseudomonas aeruginosa, Proteus vulgaris, Citrobacter koseri, and Klebsiella pneumoniae. Two drug-resistant yeasts (Candida albicans and Candida parapsilosis) were also involved in our survey. Oregano, thyme, cassia, lemongrass and arborvitae showed very strong antibacterial and antifungal activity against all tested strains. These results show that these essential oils may be effective in preventing the growth of the drug-resistant microorganisms responsible for wound infections. In this study, the genotoxic effects of tested essential oils on healthy human keratinocytes HaCaT were evaluated using the comet assay for the first time. These results revealed that none of the essential oils induced significant DNA damage in vitro after 24 h. Moreover, the treatment of HaCaT cells with essential oils increased the total antioxidant status (TAS) level. The obtained results indicate that EOs could be used as a potential source of safe and potent natural antimicrobial and antioxidant agents in the pharmaceutical and food industries.

Enzyme Inhibitory, Antioxidant And Antibacterial Potentials Of Synthetic Symmetrical And Unsymmetrical Thioureas.

BACKGROUND: In this study, 2 symmetrical and 3 unsymmetrical thioureas were synthesized to evaluate their antioxidant, antibacterial, antidiabetic, and anticholinesterase potentials. METHODS: The symmetrical thioureas were synthesized in aqueous media in the presence of sunlight, using amines and CS2 as starting material. The unsymmetrical thioureas were synthesized using amines as a nucleophile to attack the phenyl isothiocyanate (electrophile). The structures of synthesized compounds were confirmed through H1 NMR. The antioxidant potential was determined using DPPH and ABTS assays. The inhibition of glucose-6-phosphatase, alpha amylase, and alpha glucosidase by synthesized compounds was used as an indication of antidiabetic potential. Anticholinesterase potential was determined from the inhibition of acetylcholinesterase and butyrylcholinesterase by the synthesized compounds. RESULTS: The highest inhibition of glucose-6-phosphatase was shown by compound V (03.12 mg of phosphate released). Alpha amylase was most potently inhibited by compound IV with IC50 value of 62 µg/mL while alpha glucosidase by compound III with IC50 value of 75 µg/mL. The enzymes, acetylcholinesterase, and butyrylcholinesterase were potently inhibited by compound III with IC50 of 63 µg/mL and 80 µg/mL respectively. Against DPPH free radical, compound IV was more potent (IC50 = 64 µg/mL) while ABTS was more potently scavenged by compound I with IC50 of 66 µg/mL. The antibacterial spectrum of synthesized compounds was determined against Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Agrobacterium tumefaction and Proteus vulgaris). Compound I and compound II showed maximum activity against A. tumefaction with MIC values of 4.02 and 4.04 µg/mL respectively. Against P. vulgaris, compound V was more active (MIC = 8.94 µg/mL) while against S. aureus, compound IV was more potent with MIC of 4.03 µg/mL. CONCLUSION: From the results, it was concluded that these compounds could be used as antibacterial, antioxidant, and antidiabetic agents. However, further in vivo studies are needed to determine the toxicological effect of these compounds in living bodies. The compounds also have potential to treat neurodegenerative diseases.

Synthesis and characterization of crustin capped titanium dioxide nanoparticles: Photocatalytic, antibacterial, antifungal and insecticidal activities.

Current scenario of bio-nanotechnology, successfully fabrication of ultrafine titanium dioxide nanoparticles (TiO2NPs) using various biological protein sources for the multipurpose targets. The present research report involves synthesis of TiO2NPs using antimicrobial peptide (AMP) crustin (Cr). Crustin previously purified from the blue crab, Portunus pelagicus haemolymph, by blue Sepharose CL-6B matrix assisted affinity column chromatography. Synthesized Cr-TiO2NPs was physico-chemically characterized by UV-Visible spectroscopy (UV-Visible), X-ray Diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), High-resolution transmission electron microscopy (HR-TEM) and zeta potential examination. X-ray diffraction analysis for crystalline nature and phase identification of titanium dioxide nanoparticles was absorbed. Functional groups were found through FTIR ranges between 1620 and 1700 cm-1. HR-TEM analysis showed that the synthesized Cr-TiO2NPs tetragonal shape and sizes ranging from 10 to 50 nm. Finally, the surface charge of the Cr-TiO2NPs was confirmed through zeta potential analysis. Furthermore, the characterized Cr-TiO2NPs exhibited good biofilm inhibition against GPB - S. mutans (Gram Positive Bacteria- Streptococcus mutans), GNB - P. vulgaris (Gram Negative Bacteria- Proteus vulgaris) and fungal Candida albicans. Moreover, photocatalysis demonstrated that the Cr-TiO2NPs was effectively explored the degradation of dyes. The results suggest that Cr-TiO2NPs is an excellent bactericidal, fungicidal and photocatalytic agent that can be supportively used for biomedical and industrial applications.

Synthesis and molecular docking study of some 3,4-dihydrothieno[2,3-d]pyrimidine derivatives as potential antimicrobial agents.

In continuation of our research program aiming at developing new potent antimicrobial agents, new series of substituted 3,4-dihydrothieno[2,3-d]pyrimidines was synthesized. The newly synthesized compounds were preliminary tested for their in vitro activity against six bacterial and three fungal strains using the agar diffusion technique. The results revealed that compounds 7, 8a, 10b, 10d and 11b exhibited half the potency of levofloxacine against the Gram-negative bacterium, Pseudomonas aeruginosa, while compounds 5a, 8b, 10c and 12 displayed half the potency of levofloxacine against Proteus Vulgaris. Whereas, compounds 7, 10b, 10d and 11b showed half the activity of ampicillin against the Gram-positive bacterium, B. subtilis. Most of the compounds showed high antifungal potency. Compounds 3, 6, 7, 9b, 10a, 11a, 11b, 15 and 16 exhibited double the potency of clotrimazole against A. fumigatus. While compounds 3, 4, 5a, 5b, 9b, 10a, 10b, 10c, 13, 15, 16 and 18 displayed double the activity of clotrimazole against R. oryazae. Molecular docking studies of the active compounds with the active site of the B. anthracis DHPS, showed good scoring for various interactions with the active site of the enzyme compared to the co-crystallized ligand.

Chemical Composition and Antimicrobial Activities of Artemisia argyi Lévl. et Vant Essential Oils Extracted by Simultaneous Distillation-Extraction, Subcritical Extraction and Hydrodistillation.

Artemisia argyi Lévl. et Vant essential oil could be used as a good antimicrobial flavouring agent and applied in the food industry. In this study, three methods, including simultaneous distillation-extraction (SDE), subcritical extraction and hydrodistillation, were applied to extract A. argyi essential oil. Compared with subcritical extraction (1%) and hydrodistillation (0.5%), SDE gave a higher yield (1.2%). Components of the essential oils were analysed with gas chromatography-mass spectrometry (GC-MS), and the most abundant ingredients were caryophyllene oxide, neointermedeol, borneol, α-thujone and ß-caryophyllene. These five components accounted for 82.93%, 40.90% and 40.33% for SDE, subcritical extraction, and hydrodistillation, respectively. Based on agar disc diffusion and minimum inhibitory concentration (MIC) assays, SDE oil showed a significant inhibitory effect towards Listeria monocytogenes, Escherichia coli, Proteus vulgaris, Salmonella enteritidis and Aspergillus niger. Furthermore, electron microscope observations (SEM) confirmed that SDE oil could obviously deform cell morphology and destroy the structure of cell walls. Performances showed that SDE was a promising process for extracting A. argyi essential oil with both high yield and antimicrobial activity.

Pyranopyrazoles as efficient antimicrobial agents: Green, one pot and multicomponent approach.

Innovative therapeutic heterocycles having precisely thiadiazolyl-pyranopyrazole fragments were prepared by using the ecofriendly synthetic route. Entire compounds formed in quantitative yields. All the composites tested for their antimicrobial effectiveness against four microbial, two beneficial fungi's and accurately measured the minimum inhibitory concentrations (MIC and MBC/MFC), along with some initial structure activity relationships (SARs) also discussed. From the biological outcomes, the motif 6f provided an outstanding activity against all six pathogens. The possible presence of a nitro substituent on this composite may undoubtedly enhance the activity. In addition, amalgams 6d, 6g and 6l displayed promising antimicrobial results. This may be justified to the presence of electron capture group attached to the benzene ring, while the combinations 6j and 6k were zero effect towards all bacterial strains. The other compounds were excellent to low antimicrobial efficiency. The intriguing point was observed that all the active compounds had in common immense antibacterial effectiveness on Gram-negative bacteria than Gram-positive one and more antifungal activity on A. niger compare to other fungus. All things considered and suggested that this outstanding green synthetic approach is used to develop biological active compounds. On top of that, biological results confirmed that these biologically energetic motifs suitable for additional preclinical examine with the aim of standing novel innovative drugs.