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Amylase producing actinobacteria were isolated and characterized from terrestrial environment. There are a limited number of reports investigating the marine environment; hence, in the present study, four marine enzymes were tested for their amylase production ability. On starch agar plates, the Streptomyces rochei strain showed a higher hydrolytic zone (24 mm) than the other isolates. Growth under optimized culture conditions using Plackett-Burman’s experimental design led to a 1.7, 9.8, 7.7, and 3.12-fold increase for the isolates S. griseorubens, S. rochei, S. parvus, and Streptomyces sp., respectively, in the specific activity measurement. When applying the Box-Behnken design on S. rochei using the most significant parameters (starch, K2HPO4, pH, and temperature), there was a 12.22-fold increase in the specific activity measurement 7.37 U/mg. The α-amylase was partially purified, and its molecular weight was determined using sodium dodecyl sulfate-polyacrylamide gel electrophoresis. α-Amylase was particularly active at pH 6 and 65°C. The purified enzyme was most active at 65°C and pH 6, thermal stability of 70°C for 40 min, and salt concentration of 1 M with Km and Vmax of 6.58 mg/ml and 21.93 μmol/ml/min, respectively. The α-amylase was improved by adding Cu+2, Zn+2, and Fe+2 (152.21%, 207.24%, and 111.89%). Increased production of α-amylase enzyme by S. rochei KR108310 leads to production of significant industrial products.

AIM AND OBJECTIVE The aim of this cross-sectional population-based clinical study was to assess the effect of single use of three different mouthrinses on the level of salivary Streptococcus mutans of 8 to 10-year-old Saudi children. MATERIALS AND METHODS Convenient samples of 52 Saudi children aged 8-10 years were randomly allocated into four groups of 13 each. Saliva samples were collected to assess the level of S. mutans at baseline before rinsing with the assigned mouthrinse or control. Three mouthrinses, Avalon Avohex, Listerine Miswak, and Optima Aloe Dent Mouthrinse, were randomly distributed to the children. Each participant was instructed to rinse for 2 minutes using 10 mL of the assigned mouthrinse. Saliva samples were collected after rinsing and colony forming unit (CFU) of S. mutans per mL of saliva was calculated. Statistical analysis was performed to compare S. mutans count at baselines and postintervention values of each experimental group and control using paired t-test and one-way ANOVA. All statistical analyses were set at a significance level of p 0.05) in bacterial count was seen in Avalon Avohex group. CONCLUSION A single-time rinse of chlorhexidine extract mouthrinse for 2 minutes effectively reduced the number of S. mutans of 8 to 10-year-old Saudi children. CLINICAL SIGNIFICANCE Rinsing with chlorhexidine extract mouthrinse should be considered as a potential method in prevention of dental caries in children.

Biosynthesis methods employing microorganisms have emerged as an eco-friendly, clean, and viable alternative to chemical and physical processes. The present study reports the synthesis of copper oxide nanoparticles (CuONPs) using cell-free culture supernatant of marine Streptomyces sp. MHM38. For the optimized production of CuONPs, the influence of some parameters, such as the concentration of copper sulfate (CuSO4), reaction time, filtrate to substrate ratio, and pH, was studied. 5 mM of CuSO4 was optimal for nanoparticle (NP) production. Well-defined CuONP formation occurred after 60 min of incubation when an equal volume of filtrate (cell-free supernatant) to substrate (CuSO4 solution) was added. UV-visible spectroscopy analysis of CuONPs exhibited a peak at 550 nm, which corresponds to the surface plasmon resonance of CuONPs. Most of the particles were spherical and were 1.72–13.49 nm when measured using a transmission electron microscope. The antimicrobial activity of CuONPs was determined using a well diffusion method against Enterococcus faecalis ATCC 29212, Salmonella typhimurium ATCC 14028, Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8939, fungi (Rhizoctonia solani, Fusarium solani, and Aspergillus niger), and yeast (Candida albicans ATCC 10237). The highest antimicrobial activities were recorded against Candida albicans ATCC 10237, whereas Salmonella typhimurium ATCC 14028 and Escherichia coli ATCC 8939 showed the less activity. The biochemical findings of the CuONP groups were significant ( p < 0.05 ) with diminished levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), total and direct bilirubin, urea, and creatinine compared with the paracetamol group. Nonenzymatic and enzymatic antioxidants of the CuONP groups were significantly elevated ( p < 0.05 ) in SOD and GSH levels, and exceptionally low nitric oxide (NO) and malondialdehyde (MAD) levels were found for the paracetamol group. The histopathological examination of the CuONP groups assured the impact of improving CuONPs against paracetamol-induced liver damage.

Acinetobacter baumannii has become a major challenge to clinicians worldwide due to its high epidemic potential and acquisition of antimicrobial resistance. This work aimed at investigating antimicrobial resistance determinants and their context in four extensively drug-resistant (XDR) NDM-producing A. baumannii clinical isolates collected between July and October 2020 from Kasr Al-Ainy Hospital, Cairo, Egypt. A total of 20 A. baumannii were collected and screened for acquired carbapenemases (blaNDM, blaVIM and blaIMP) using PCR. Four NDM producer A. baumannii isolates were identified and selected for whole-genome sequencing, in silico multilocus sequence typing, and resistome analysis. Antimicrobial susceptibility profiles were determined using disk diffusion and broth microdilution tests. All blaNDM-positive A. baumannii isolates were XDR. Three isolates belonged to high-risk international clones (IC), namely, IC2 corresponding to ST570Pas/1701Oxf (M20) and IC9 corresponding to ST85Pas/ST1089Oxf (M02 and M11). For the first time, we report blaNDM-1 gene on the chromosome of an A. baumannii strain that belongs to sequence type ST164Pas/ST1418Oxf. Together with AphA6, blaNDM-1 was bracketed by two copies of ISAba14 in ST85Pas isolates possibly facilitating co-transfer of amikacin and carbapenem resistance. A novel blaADC allele (blaADC-257) with an upstream ISAba1 element was identified in M19 (ST/CC164Pas and ST1418Oxf/CC234Oxf). blaADC genes harbored by M02 and M11 were uniquely interrupted by IS1008. Tn2006-associated blaOXA-23 was carried by M20. blaOXA-94 genes were preceded by ISAba1 element in M02 and M11. AbGRI3 was carried by M20 hosting the resistance genes aph(3`)-Ia, aac(6`)-Ib`, catB8, ant(3``)-Ia, sul1, armA, msr(E), and mph(E). Nonsynonymous mutations were identified in the quinolone resistance determining regions (gyrA and parC) of all isolates. Resistance to colistin in M19 was accompanied by missense mutations in lpxACD and pmrABC genes. The current study provided an insight into the genomic background of XDR phenotype in A. baumannii recovered from patients in Egypt. WGS revealed strong association between resistance genes and diverse mobile genetic elements with novel insertion sites and genetic organizations.

The aim of this cross-sectional population-based clinical study was to assess the effect of single use of three different mouthrinses on the level of salivaryConvenient samples of 52 Saudi children aged 8-10 years were randomly allocated into four groups of 13 each. Saliva samples were collected to assess the level ofAll test groups showed a reduction in salivaryA single-time rinse of chlorhexidine extract mouthrinse for 2 minutes effectively reduced the number ofRinsing with chlorhexidine extract mouthrinse should be considered as a potential method in prevention of dental caries in children.

Neonatal sepsis is a great challenge for clinicians and infection control practitioners, especially in facilities with limited resources. Carbapenem-resistant Klebsiella pneumoniae (CRKP) is rapidly increasing and carriages a major threat to neonates. We aimed to examine phenotypes causing neonatal late onset sepsis (NLOS) in comparison with neonatal early onset sepsis (NEOS) with further investigations of genotypes, and genetic relatedness of CRKP in neonatal late-onset sepsis. Our study included 88 neonates diagnosed with sepsis: 58 with (NLOS) and 30 with (NEOS) from November 2015 to April 2016, at neonatal intensive care unit (NICU) of Cairo University Hospital. K. pneumoniae was the most common encountered pathogen in the NLOS group (37.9%) with a mean sepsis score of 6.39 when compared to the NEOS group (p < 0.05). In Klebsiella group, C-reactive protein and interleukin-6 levels were significantly high (p ˂ 0.001) and 56.5% of the isolates were meropenem resistant. The most prevalent carbapenemase gene was OXA-48 which was identified in 14/23 (60.8%) followed by NDM-1 which was identified in 12/23 (52.2%) as detected by multiplex PCR. Coexistence of both carbapenemases was found in 52.2% (12/23). The blaKPC, blaIMP, and blaVIM genes were not harbored in the isolates. By investigating the genetic relatedness of CRKP by pulsed-field gel electrophoresis, 23 isolates of K. pneumoniae revealed various pulsed-field gel electrophoresis (PFGE) patterns, demonstrating that the isolates were non-clonal. Awareness of the existing phenotypes and genotypes is important for proper treatment and infection control practices.

WOS: 000491263700054 The compound 2-methoxy-4,6-diphenylnicotinonitrile was characterized by using experimental FT-IR, Laser-Raman, H-1 and (CNMR)-C-13 spectra and UV-Vis. spectroscopic analysis methods. To support experimental structural, vibrational, chemical shift and electronic records, the theoretical analyses were performed at the DFT/B3LYP method with the 6-311++G(2d,2p) basis set. The pi center dot center dot center dot pi, N center dot center dot center dot pi, N center dot center dot center dot H, C center dot center dot center dot H and O center dot center dot center dot H interactions within crystal packing of the compound, which aren't taken into account within the experimental single crystal X-Ray diffraction study, were investigated in detail with Hirshfeld surface analyses and their related 2D fingerprint plots. The highest occupied molecular orbital (HOMO), the lowest unoccupied molecular orbital (LUMO) and their associated parameters were used to explain intra-molecular charge transfer and global reactivity properties of the compound with the computational level of theory. Non-linear optical (NLO) profile of the title compound including pi electron systems such as aromatic and cyano groups was determined by considering the static polarizability (alpha) and the static first-order hyperpolarizability (beta) values. Molecular docking analysis was performed to determine intermolecular interactions between a Mps1/TTK protein kinase inhibitor with the title compound. Deanship of Scientific Research at King Saud UniversityDeanship of Scientific Research at King Saud University [RGP-163] The authors extend their appreciation to the Deanship of Scientific Research at King Saud University for funding the work through the research group project No. RGP-163.

Synthetic and natural spiroxindoles are important anti-inflammatory, antibacterial, antileishmanial, and anticancer agents. In this study, we prepared a spiroxindole derivative and evaluated the preliminary results of its biological activity including anti-inflammatory, antileishmanial, and cytotoxic activity against 3T3 and Hela cell lines. By adopting the 1,3-dipolar cycloaddition reaction, we were able to successfully combine olefin, isatin, and an amino acid to form the desired spiroxindole analog 4 (yield, up to 94%). To elucidate the chemical structure of 4, the X-ray single crystal diffraction technique was employed, and the electronic and NMR spectra of 4 were calculated using the B3LYP/6-311G(d,p) method. The calculated 1H and 13C NMR chemical shifts aligned well with the experimental data. Compound 4 was then evaluated for its anti-inflammatory, antileishmanial, and cytotoxic activity against 3T3 and Hela cell lines. This spiroxindole pyrothiazole (IC50 = 65.9 ± 6.6 μM) showed weak anti-inflammatory activity compared to the test standard, ibuprofen (IC50 = 11.2 ± 1.9 μM), and moderate anticancer activity against Hela cell lines compared to doxorubicin (IC50 = 1.2 ± 0.4 μM vs IC50 = 11.2 ± 0.3 μM for 4). Compound 4 also appeared as an effective antileishmanial agent (IC50 = 39.8 ± 0.43 μM) when tested in vitro.

Background: Because of the ability of their bioactive metabolites production, many researchers were attracted to investigate and isolating marine actinomycetes from unique location with a unique environment. Information on antimicrobial activity and antifouling agents by Streptomyces sp. from the Ras Garib area, Gulf of Suez, Egypt is limited. One of the metabolites produced by the actinomycetes was biosurfactant. This paper describes the possibility of marine actinomycetes isolates for the production of biosurfactants, In addition to the possibility of using it as antimicrobial and antifouling agents.Results: Marine actinobacterial isolates RG3 and RG8 had emulsification indexes of 76 and 68%, respectively. The two marine actinobacterial isolates were identified using 16srDNA as Streptomyces althioticus RG3 and Streptomyces californicus RG8, and submitted in the database of genetic information with accession number MW661230 and MW661234, respectively. Biosurfactants were stable at 10% NaCl, in case of Streptomyces althioticus RG3 and stable at 10%–15% NaCl in the case of Streptomyces californicus RG8. A temperature of 35℃ was suitable for the stability of biosurfactants produced by both strains. Both strains produced the most biosurfactant when exposed to alkaline conditions. We characterized the biosurfactants produced by both strains including features such as the chemical composition of the biosurfactants and FTIR analysis. The antimicrobial activity of biosurfactants extract evaluated using a well diffusion method against Vibrio alginolyticus MK170250, Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 4027, and Staphylococcus aureus ATTC 25923. Streptomyces althioticus RG3 biosurfactants have been shown to have better antimicrobial activity than Streptomyces californicus RG8, indicating that they may be used in pharmaceutical industries and in the manufacture of antifouling products.Conclusions: Streptomyces althioticus RG3 and Streptomyces californicus RG8, isolated from Ras Garib, Gulf of Suez, Egypt, were able to develop very stable biosurfactants under stress conditions, which could be useful in a variety of industries such as pharmaceuticals and antifouling manufacturing.

Amylase is an industrial enzyme that is used in the food and biofuel industries. We screened four actinomycetes strains for amylase biosynthesis. The Streptomyces rochei strain had a larger hydrolytic zone (24 mm) on starch agar plates, than the other isolates. Plackett-Burman’s experimental design was implemented to optimize the conditions for amylase production by the selected strains. Growth under optimized culture conditions led to 1.7, 9.8, 7.7, and 3.12 -fold increases for the isolates S. griseorubens, S. rochei, S. parvus, and Streptomyces sp., respectively, in the specific activity measurement in comparison with growth under primary conditions. When applying the Box-Behnken design on S. rochei using the most significant parameters starch, K2HPO4, pH, and temperature, there was a 12.22-fold increase in the specific activity measurement: 7.37 U/mg. The optimal fermentation medium formula was kept at 30.6°C for seven days. The amylase from S. rochei was partially purified, and its molecular weight was determined using Sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The molecular weight was found to be 45, 43, and 53 kDa. Amylase was particularly active at pH 6 and 65°C. The purified enzyme was most active at 65°C and a pH of 6, thermal stability of 70°C for 40 min and salt concentration of 1 M with a Km and Vmax of 6.58 mg/ml and 21.93 mg/ml/min, respectively. The amylase improved by adding Cu + 2, Zn + 2, and Fe + 2 (152.21%, 207.24%, and 111.89%). Increased production of amylase enzyme by Streptomyces rochei KR108310 attracts the production of industrially significant products.

The authors have withdrawn this preprint due to author disagreement.

Tarek A Yousef,1,2 Essam Ezzeldin,3,4 Hatem A Abdel-Aziz,5 Mohamed H Al-Agamy,6,7 Gamal AE Mostafa3,5 1College of Science, Chemistry Department, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Kingdom of Saudi Arabia; 2Department of Toxic and Narcotic Drug, Forensic Medicine, Mansoura Laboratory, Medicolegal Organization, Ministry of Justice, Mansoura, Egypt; 3Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 4Bioavailability Laboratory, Central Laboratory, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 5Applied Organic Chemistry Department, National Research Center, Cairo 12622, Egypt; 6Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 7Department of Microbiology and Immunology, Faculty of Pharmacy, Al-Azhar University, Cairo, EgyptCorrespondence: Gamal AE Mostafa Email gmostafa@ksu.edu.saBackground: Electron donor–acceptor interactions are important molecular reactions for the activity of pharmacological compounds. The aim of the study is to develop a charge transfer (CT) complex: synthesis, characterization, antimicrobial activity, and theoretical study.Method and Results: A solid CT complex of neostigmine (NSG) with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) was synthesized and characterized by infrared spectra, NMR, and UV–visible spectroscopy. The results confirm the formation of a CT complex. The stability of the CT complex between NSG and DDQ in acetonitrile was determined in solution via spectrophotometric measurement, ie, by calculating the formation constant, molar extinction coefficient, and different spectroscopic parameters. The stoichiometry of the formed NSG–DDQ complex was determined using Job’s method. The absorption band of the NSG–DDQ complex can be used for the quantification of NSG.Conclusion: The DFT geometry optimization of NSG, DDQ, and the CT complex and the UV comparative study of both theoretical and experimental structures are presented. The experimental results confirm the charge transfer structure. The bacterial study shows that the NSG–DDQ complex has good antibacterial activity against both Gram-positive and Gram-negative bacteria as well as antifungal activity against Candida albicans.Keywords: charge transfer complex, neostigmine, DDQ, synthesis, spectroscopic, characterization, antimicrobial activity, theoretical study

Reem I Al-Wabli,1 Alwah R Al-Ghamdi,1 Hazem A Ghabbour,2 Mohamed H Al-Agamy,3,4 Mohamed I Attia1,5 1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 2Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; 3Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 4Microbiology and Immunology Department, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt; 5Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza 12622, Egypt Background: The incidence of fungal infections is a growing serious global health burden. There is an urgent medical demand to acquire new antifungal drug-like compounds having azole nuclei to get rid of the drawbacks of the currently available azole antifungal agents. Methods: The target compounds 5a-r were synthesized in a four-step reaction sequence using the appropriate acetophenone derivative as a starting material. The antifungal potential of the title compounds was assessed using DIZ and MIC assays according to the reported standard procedures. Results: The newly synthesized oximino esters 5a-r were identified with the aid of various spectroscopic approaches. Their assigned chemical structures were confirmed via single-crystal X-ray structure of compound 5o. The molecular structure of compound 5o was crystallized in the triclinic, P-1, a=9.898 (3) Å, b=10.433 (3) Å, c=11.677 (4) Å, α=86.886 (6)°, β=87.071 (7)°, γ=64.385 (6)°, V=1,085.2 (6) Å3, Z=2. The synthesized compounds 5a-r were in vitro evaluated for antifungal potential against four fungal strains. Compounds 5l and 5m bearing a trifluoromethylphenyl moiety showed the best anti-Candida albicans activity with minimum inhibitory concentration (MIC) value of 0.148 µmol/mL, while compound 5b displayed the best activity toward Candida tropicalis with MIC value of 0.289 µmol/mL. Compounds 5o and 5l were the most active congeners against Candida parapsilosis and Aspergillus niger, respectively. Conclusion: Single-crystal X-ray analysis of compound 5o confirmed without doubt the assigned chemical structures of the title compounds as well as confirmed the (E)-configuration of their oximino group. Compounds 5b, 5l, 5m, and 5o emerged as the most active compounds against the tested fungi and they could be considered as new antifungal lead candidates. Keywords: crystal structure, imidazole, benzodioxole, ester, antifungal

Alanazi, Mohammed/0000-0002-0483-8113; Gokce, Halil/0000-0003-2258-859X; , Nuri/0000-0001-8742-0160; Al-agamy, Mohamed/0000-0001-9868-0355 WOS: 000456717300009 Molecular structure analysis, vibrational and electronic spectroscopic studies and thermochemical features of (11R,12 S)-16-aminotetracyclo[6.6.2.0(2,7).0(9,14)]hexadeca-2(7),3,5,9(14),10,12-hexaen-15-ol were investigated via both theoretical and experimental techniques. Experimental investigations were made by using FT-IR, Raman, H-1 and C-13 NMR and UV-Vis. spectroscopies. To support experimental evidences, molecular electronic structure computations were obtained with the DFT/B3LYP method at the 6-311G++(3d,3p) basis set. 2D and 3D Hirshfeld surfaces studies were performed to understand non-bonding intermolecular interactions in solid phase crystal packing of the compound. MEP surface analysis was performed to investigate nucleophilic and electrophilic reactive sites of the compound. The highest occupied molecular orbitals (HOMOs) and lowest unoccupied molecular orbitals (LUMO) analyses were theoretically used for determination of electronic transitions corresponding to UV-Vis. electronic absorption wavelengths. Enzyme-ligand interactions between the compound with BACE1 (Beta-Secretase1) inhibitor were determined via molecular docking study. Deanship of Scientific Research at King Saud UniversityDeanship of Scientific Research at King Saud University [RGP-163] The authors extend their appreciation to the Deanship of Scientific Research at King Saud University for funding the work through the research group project No. RGP-163.

Introduction Serratia marcescens is a significant hospital-acquired pathogen, and many outbreaks of S. marcescens infection have been reported in neonates. We report a sudden breakout of S. marcescens harboring the bla IMP-4 and bla VIM-2 metallo-β-lactamase (MBL) genes that occurred from March to August 2015 in the neonatal intensive care unit of Cairo University Hospital, Cairo, Egypt. Methods During the study period, 40 nonduplicate clinical isolates of S. marcescens were collected from blood culture samples. Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry was used to identify each isolate. Then, minimum inhibitory concentrations of different antibiotics were assessed by the Vitek 2 compact system. Screening of the MBL genes bla IMP, bla VIM, bla SIM-1, bla SPM-1, and bla GIM-1 as well as the carbapenemase genes KPC, NDM, OXA-48, SME-1, and SME-2 were evaluated. Pulsed field gel electrophoresis was preformed to detect the genetic relationship of the isolates. Results Analysis showed that 37.5% of the S. marcescens clinical isolates were resistant to meropenem (minimum inhibitory concentrations ≥ 2 µg/mL), and bla IMP-4 and bla VIM-2 were the most prevalent MBL genes (42.5% and 37.5%, respectively). None of the other investigated genes were observed. Pulsed field gel electrophoresis typing revealed two discrete clones; 33/40 (82.5%) were pulsotype A and 7/40 (17.5%) were pulsotype B. Conclusion Here, we report for the first time the detection of MBL-producing S. marcescens isolates, particularly IMP-4 and VIM-2 recovered from inpatients with bacteremias from the intensive care unit at Cairo University Hospital.

Fungal infections are a growing health threat to mankind. The development of novel potent antifungal agents is a challenge to overcome the resistance to the available antifungal medications. The current report focuses on the synthesis and spectroscopic characterization of a new imidazole-bearing antifungal agent. The vibrational characteristics of the title compound are explored using Fourier transform infrared and Raman spectroscopy with the aid of density functional theory. Highest occupied and lowest unoccupied molecular orbital investigations and natural bond orbital analysis of the title molecule are performed to investigate the possible intermolecular delocalisation or hyper-conjugation, and the possible interactions with the target protein. Single crystal X-ray analysis confirms the assigned (E)-configuration of the imine double bond structure of the title compound. The molecular structure of the title compound is crystallised in a monoclinic space group, namely, P21/c, a = 10.7007 (4) A, b = 7.3072 (3) A, c = 24.9088 (8) A, β = 97.178 (2)°, V = 1932.41 (12) A3 and Z = 4. The antifungal potential of the title compound is in vitro assessed against four fungal strains. In addition, molecular docking of the title molecule predicts its binding orientation in the active site of the target protein.

This study assessed the wound healing potential and antimicrobial activity of henna, pomegranate and myrrh extract formulations and their blend in excision, and dead space wound models in rats in comparison to a marketed ointment (gentamycin). The natural extracts were used in ointment formulations alone or in a combination of three extracts at a total concentration of 15% w/w in medications. The percent of wound contraction in case of henna, myrrh, pomegranate, the blend and gentamycin (10 mg/kg) were 85.90–98.5%, 88.35–99.52%, 93.55–100%, 97.30–100%, and 90.25–100% from days 16 to 20, respectively. The blended formulation showed the highest increase in the percent of wound contraction and decrease in the epithelisation period compared to other formulations and showed comparable results to the standard ointment. The histological studies of excision biopsy at day 24 showed healed skin structures with normal epithelisation, the restoration of adnexa and fibrosis within the dermis in all of the formulation- and gentamycin-treated groups while the control group lagged behind in the formation of the amount of ground substance in the granulation tissue. The formulations showed antimicrobial activity against Candida, Staphylococcus aureus, mucous membrane infections and E. coli topical infections. The study proved the wound healing potential and antimicrobial activity of the herbal extract. Keywords: Wound healing, Henna, Pomegranate, Myrrh, Hydrophilic ointment, Herbal extract

The aim of this study was to investigate the mechanisms responsible for resistance to antimicrobials in a collection of enterobacterial isolates recovered from two hospitals in Saudi Arabia. A total of six strains isolated from different patients showing high resistance to carbapenems was recovered in 2015 from two different hospitals, with four being Klebsiella pneumoniae and two Enterobacter cloacae. All isolates except one K. pneumoniae were resistant to tigecycline, but only one K. pneumoniae was resistant to colistin. All produced a carbapenemase according to the Carba NP test, and all were positive for the EDTA-disk synergy test for detection of MBL. Using PCR followed by sequencing, the four K. pneumoniae isolates produced the carbapenemase NDM-1, while the two E. cloacae isolates produced the carbapenemase VIM-1. Genotyping analysis by Multilocus Sequence Typing (MLST) showed that three out of the four K. pneumoniae isolates were clonally related. They had been recovered from the same hospital and belonged to Sequence Type (ST) ST152. In contrast, the fourth K. pneumoniae isolate belonged to ST572. Noticeably, the NDM-1-producing K. pneumoniae additionally produced an extended-spectrum ß-lactamase (ESBL) of the CTX-M type, together with OXA-1 and TEM-1. Surprisingly, the three clonally related isolates produced different CTX-M variants, namely, CTX-M-3, CTX-M-57, and CTX-M-82, and coproduced QnrB, which confers quinolone resistance, and the 16S rRNA methylase RmtC, which confers high resistance to all aminoglycosides. The AAC(6′)-Ib acetyltransferase was detected in both K. pneumoniae and E. cloacae. Mating-out assays using Escherichia coli as recipient were successful for all isolates. The blaNDM-1 gene was always identified on a 70-kb plasmid, whereas the blaVIM-1 gene was located on either a 60-kb or a 150-kb plasmid the two E. cloacae isolates, respectively. To the best of our knowledge, this is the first report of the coexistence of an MBL (NDM-1), an ESBL (CTX-M), a 16S rRNA methylase (RmtC), an acetyltransferase (AAC[6′]-Ib), and a quinolone resistance enzyme (QnrB) in K. pneumoniae isolates recovered from different patients during an outbreak in a Saudi Arabian hospital.

Background The incidence of fungal infections is a growing serious global health burden. There is an urgent medical demand to acquire new antifungal drug-like compounds having azole nuclei to get rid of the drawbacks of the currently available azole antifungal agents. Methods The target compounds 5a-r were synthesized in a four-step reaction sequence using the appropriate acetophenone derivative as a starting material. The antifungal potential of the title compounds was assessed using DIZ and MIC assays according to the reported standard procedures. Results The newly synthesized oximino esters 5a-r were identified with the aid of various spectroscopic approaches. Their assigned chemical structures were confirmed via single-crystal X-ray structure of compound 5o. The molecular structure of compound 5o was crystallized in the triclinic, P–1, a=9.898 (3) Å, b=10.433 (3) Å, c=11.677 (4) Å, α =86.886 (6)°, β =87.071 (7)°, γ =64.385 (6)°, V=1,085.2 (6) Å3, Z=2. The synthesized compounds 5a-r were in vitro evaluated for antifungal potential against four fungal strains. Compounds 5l and 5m bearing a trifluoromethylphenyl moiety showed the best anti-Candida albicans activity with minimum inhibitory concentration (MIC) value of 0.148 μmol/mL, while compound 5b displayed the best activity toward Candida tropicalis with MIC value of 0.289 μmol/mL. Compounds 5o and 5l were the most active congeners against Candida parapsilosis and Aspergillus niger, respectively. Conclusion Single-crystal X-ray analysis of compound 5o confirmed without doubt the assigned chemical structures of the title compounds as well as confirmed the (E)-configuration of their oximino group. Compounds 5b, 5l, 5m, and 5o emerged as the most active compounds against the tested fungi and they could be considered as new antifungal lead candidates.

The aim of this study was to investigate the mechanisms responsible for resistance to antimicrobials in a collection of enterobacterial isolates recovered from two hospitals in Saudi Arabia. A total of six strains isolated from different patients showing high resistance to carbapenems was recovered in 2015 from two different hospitals, with four being Klebsiella pneumoniae and two Enterobacter cloacae. All isolates except one K. pneumoniae were resistant to tigecycline, but only one K. pneumoniae was resistant to colistin. All produced a carbapenemase according to the Carba NP test, and all were positive for the EDTA-disk synergy test for detection of MBL. Using PCR followed by sequencing, the four K. pneumoniae isolates produced the carbapenemase NDM-1, while the two E. cloacae isolates produced the carbapenemase VIM-1. Genotyping analysis by Multilocus Sequence Typing (MLST) showed that three out of the four K. pneumoniae isolates were clonally related. They had been recovered from the same hospital and belonged to Sequence Type (ST) ST152. In contrast, the fourth K. pneumoniae isolate belonged to ST572. Noticeably, the NDM-1-producing K. pneumoniae additionally produced an extended-spectrum ß-lactamase (ESBL) of the CTX-M type, together with OXA-1 and TEM-1. Surprisingly, the three clonally related isolates produced different CTX-M variants, namely, CTX-M-3, CTX-M-57, and CTX-M-82, and coproduced QnrB, which confers quinolone resistance, and the 16S rRNA methylase RmtC, which confers high resistance to all aminoglycosides. The AAC(6′)-Ib acetyltransferase was detected in both K. pneumoniae and E. cloacae. Mating-out assays using Escherichia coli as recipient were successful for all isolates. The blaNDM-1 gene was always identified on a 70-kb plasmid, whereas the blaVIM-1 gene was located on either a 60-kb or a 150-kb plasmid the two E. cloacae isolates, respectively. To the best of our knowledge, this is the first report of the coexistence of an MBL (NDM-1), an ESBL (CTX-M), a 16S rRNA methylase (RmtC), an acetyltransferase (AAC[6′]-Ib), and a quinolone resistance enzyme (QnrB) in K. pneumoniae isolates recovered from different patients during an outbreak in a Saudi Arabian hospital.

The pathogenic effect of Staphylococci is due to extra-cellular factors and properties such as adherence and biofilm production. The nature of the biofilm and the physiological properties of biofilm-producing bacteria result in an inherent antibiotic resistance and require further investigation. Two hundred and sixty Staphylococcal strains were cultured from 600 clinical specimens obtained from hospitalized patients. Among these, 155 were identified as coagulase-positive (CPS) and 105 as coagulase-negative (CNS) staphylococci. Staphylococcal strains were tested for biofilm production using the tissue culture plate (TCP) method. TCP detection showed that of the 155 CPS, 124 (80%) were biofilm producers, while 63 (60%) of the 105 CNS were biofilm producers. Biofilm-producing strains were scanned by scanning electron microscope (SEM) to confirm biofilm formation, study biofilm production, and examine antibiotic effects on biofilm formation. Disc diffusion method was used to study resistance of planktonic and biofilm-forming cells to antibiotics. Planktonic cells were less resistant to antibiotics than biofilm-forming cells. Microbroth dilution method and a new BioTimer assay were used to determine antibiotic MICs affecting planktonic and biofilm cells. Both methods showed that the MICs for planktonic cells were less than that for biofilm cells. The BioTimer assay was therefore found to be sensitive, accurate, and reliable, with results in agreement with those from the broth dilution method and SEM.

Objectives: To investigate the prevalence, antibiotic resistant profiles, and risk factors of early fecal carriage of Enterococcus faecalis (E. faecalis) and staphylococci among 150 healthy Saudi neonates born in a hospital setting in central Saudi Arabia. Methods. This prospective study was conducted in Al-Bukayriyah General Hospital, Qassim, Saudi Arabia, between June 2012 and January 2013. The E. faecalis and Staphylococcus spp. isolates were identified manually, and Vitek2 system was used for identity confirmation at the species level and minimum inhibitory concentration-susceptibility testing. Results: Enterococcus faecalis (n=73) and Staphylococcus spp. (n=18) were recovered. Unlike staphylococci, E. faecalis colonization did not significantly vary from day one up to 7 days of life, regardless of the type of feeding, but it was relatively higher among vaginally versus cesarean delivery. Both Staphylococcus epidermidis ( S. epidermidis) and Staphylococcus aureus ( S. aureus) carriage increase as the body weight increases, and this difference was significant ( p =0.025) for S. epidermidis . High-level resistance in Gentamycin among E. faecalis isolates was 25% and 11% to Streptomycin. Thirty percent of S. epidermidis were resistant to oxacillin and exhibited multidrug-resistant (MDR) patterns of 5 resistant markers, which were also observed among 2/5 (40%) of Methicillin-resistant Staphylococcus aureus isolates. Conclusion: Enterococcus faecalis did not significantly vary in relation to type of delivery, age up to 7 days, and type of feeding. The neonatal fecal carriage of MDR isolates should be considered as a crucial reservoir to the further spread of antimicrobial resistance genes among hospitals, cross infections, and the community. Saudi Med J 2016; Vol. 37 (3): 280-287 doi: 10.15537/smj.2016.3.13871 How to cite this article El-Kersh TA, Marie MA, Al-Sheikh YA, Al-Agamy MH, Al Bloushy AA. Prevalence and risk factors of early fecal carriage of Enterococcus faecalis and Staphylococcus spp and their antimicrobial resistant patterns among healthy neonates born in a hospital setting in central Saudi Arabia. Saudi Med J 2016; 37: 280-287.

Objectives: The aim of this cross-sectional in vivo study was to assess the effect of green tea and honey solutions on the level of salivary Streptococcus mutans. Study design: A convenient sample of 30 Saudi boys aged 7–10 years were randomly assigned into 2 groups of 15 each. Saliva sample was collected for analysis of level of S. mutans before rinsing. Commercial honey and green tea were prepared for use and each child was asked to rinse for two minutes using 10 mL of the prepared honey or green tea solutions according to their group. Saliva samples were collected again after rinsing. The collected saliva samples were prepared and colony forming unit (CFU) of S. mutans per mL of saliva was calculated. Results: The mean number of S. mutans before and after rinsing with honey and green tea solutions were 2.28* 108(2.622*108), 5.64 *107(1.03*108), 1.17*109(2.012*109) and 2.59*108 (3.668*108) respectively. A statistically significant reduction in the average number of S. mutans at baseline and post intervention in the children who were assigned to the honey (P=0.001) and green tea (P=0.001) groups was found. Conclusions: A single time mouth rinsing with honey and green tea solutions for two minutes effectively reduced the number of salivary S. mutans of 7–10 years old boys.

The main objective of the present study was to explore different types of surfactants for formulating itraconazole (ITZ) loaded niosomes to improve its skin penetration. These surfactants vary in number and nature of the alkyl chains. The prepared niosomes were characterized in terms of particle size, surface charge, entrapment efficiency, skin penetration and antifungal activity. Brij (BR) 35 niosomes exhibited largest size, while the smallest size was observed in case of Spans and Tweens with tri-alkyl chains. The entrapment efficiency (EE%) of niosomes made of unsaturated alkyl chain surfactants was less than that one with saturated alkyl chain. Furthermore, tri-alkyl chains of niosomes showed higher EE% compared to mono-alkyl chain. Regarding skin permeation, Spans niosomes showed enhancement permeation of ITZ compared to ITZ solution; however, it was less in magnitude than that of Tweens. The niosomes made of tri-alkyl chains tend to accumulate more in stratum corneum (SC) and stripped skin with low amount of ITZ in receptor fluid. The highest amount of ITZ reached receptor fluid was observed in Tween 80 and 60 niosomes. The antifungal activity of ITZ was not compromised when ITZ being loaded into niosomes. It could be concluded that niosomes drug delivery systems are promising carriers for cutaneous targeted delivery of ITZ.

To the Editor,We read with interest a recent report in the present journal on the spread of OXA-48-producing Klebsiella pneumoniae in central Europe [1]. The spread implicates a severe threat to th...

Background Design and synthesis of pyrazole-dimedone derivatives were described by one-pot multicomponent reaction as new antimicrobial agents. These new molecular framework were synthesized in high yields with a broad substrate scope under benign conditions mediated by diethylamine (NHEt2). The molecular structures of the synthesized compounds were assigned based on different spectroscopic techniques (1H-NMR, 13C-NMR, IR, MS, and CHN). Results The synthesized compounds were evaluated for their antibacterial and antifungal activities against S. aureus ATCC 29213, E. faecalis ATCC29212, B. subtilis ATCC 10400, and C. albicans ATCC 2091 using agar Cup plate method. Compound 4b exhibited the best activity against B. subtilis and E. faecalis with MIC = 16 µg/L. Compounds 4e and 4l exhibited the best activity against S. aureus with MIC = 16 µg/L. Compound 4k exhibited the best activity against B. subtilis with MIC = 8 µg/L. Compounds 4o was the most active compounds against C. albicans with MIC = 4 µg/L. Conclusion In-silico predictions were utilized to investigate the structure activity relationship of all the newly synthesized antimicrobial compounds. In this regard, a ligand-based pharmacophore model was developed highlighting the key features required for general antimicrobial activity. While the molecular docking was carried out to predict the most probable inhibition and binding mechanisms of these antibacterial and antifungal agents using the MOE docking suite against few reported target proteins. Electronic supplementary material The online version of this article (10.1186/s13065-018-0399-0) contains supplementary material, which is available to authorized users.

Here, 210 healthy participants including community personnel (70), clinical students (68), and healthcare workers (HCWs) (72) from the eastern region of Saudi Arabia were studied. Sixty-threeStaphylococcus aureusisolates were obtained from the nares of 37% of the community personnel and 26% of the clinical students and HCWs. Methicillin-resistantS. aureus(MRSA) was found in 16% (10 isolates) of the 63 isolates; six were from HCWs. Molecular characterization revealed high clonal diversity among the isolates, with 19 differentspatypes, 12 clonal complexes (CCs), and seven sequence types (STs) detected. The most common strain type was USA900, CC15, and t084, seen in 11 methicillin-susceptibleS. aureus(MSSA) isolates. Moreover, three novelspatypes in six isolates and one novel ST in two isolates were identified, most from HCWs. Interestingly, 29 isolates weremecA positive by PCR, whereas only 10 isolates were MRSA by disk diffusion (cefoxitin resistant). Of the 19 MSSAmecA-positive isolates, 16 were PBP2a negative, leaving three unique isolates from HCWs that weremecA and PBP2a positive yet cefoxitin susceptible. Our findings highlight the importance of phenotypically and genotypically characterizingS. aureusstrains isolated from healthy communities to monitor the risk of possible cross-transmission to hospitalized patients. The identified strains showed a clonal lineage relationship with previously reportedS. aureusand MRSA strains acquired from hospital settings.