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An Indian traditional medicinal plant, Boerhaavia diffusa (Punarnava), is reported for its diuretic activity and helps in impaired kidney function. The present study indicates that alkaloids, carbohydrates, saponins, phytosterols, flavonoids, and glycosides are absent in the petroleum ether extract and present chiefly in the methanolic extract of roots. The phytosterols were found to be present in the ethyl acetate extract, while other phytochemical constituents, that is, alkaloids, carbohydrates, saponins, flavonoids, and glycosides, were absent. From high‐performance thin‐layer chromatography, the results indicated that out of all the three extracts and two marketed formulations, ethyl acetate root extract (LEA) has the highest amount of Boeravinone B content. Further, different root extracts of B. diffusa and two marketed formulations were evaluated on the human embryonic kidney cell line to understand pharmacological safety. From the results, it was observed that LEA and petroleum ether root extracts showed a higher percentage of cell survival and a better safety profile up to the dose of 1 mg/mL. The overall results indicated that further preclinical evaluation of B. diffusa is needed to understand the mechanism behind nephroprotective potential which can further expedite the drug discovery process of nephroprotective molecules. [ABSTRACT FROM AUTHOR]

Pseudomonas aeruginosa easily adapts to newer environments and acquires several genome flexibilities to overcome the effect of antibiotics during therapeutics, especially in cystic fibrosis patients. During adaptation to the host system, the bacteria employ various tactics including virulence factor production and biofilm formation to escape from the host immune system and resist antibiotics. Hence, identifying alternative strategies to combat recalcitrant pathogens is imperative for the successful elimination of drugresistant microbes. In this context, this study portrays the anti-virulence efficacy of umbelliferone (UMB) against P. aeruginosa. UMB (7-hydroxy coumarin) is pervasively found among the plant family of Umbelliferae and Asteraceae. The UMB impeded biofilm formation in the P. aeruginosa reference strain and clinical isolates on polystyrene and glass surfaces at the concentration of 125 µg/ml. Global proteomic analysis of UMB-treated cells revealed the downregulation of major virulence-associated proteins such as RhlR, LasA, AlgL, FliD, Tpx, HtpG, KatA, FusA1, Tsf, PhzM, PhzB2, CarB, DctP, MtnA, and MscL. A functional interaction study, gene ontology, and KEGG pathway analysis revealed that UMB could modulate the global regulators, enzymes, co-factors, and transcription factors related to quorum sensing (QS), stress tolerance, siderophore production, motility, and microcolony formation. In vitro biochemical assays further affirmed the anti-virulence efficacy of UMB by reducing pyocyanin, protease, elastase, and catalase production in various strains of P. aeruginosa. Besides the antibiofilm activity, UMB-treated cells exhibited enhanced antibiotic susceptibility to various antibiotics including amikacin, kanamycin, tobramycin, ciprofloxacin, and cefotaxime Furthermore, in vitro cytotoxicity analysis revealed the biocompatibility of UMB, and the IC50 value was determined to be 249.85 µg/ml on the HepG2 cell line. Altogether, the study substantiates the anti-virulence efficacy of UMB against P. aeruginosa, and the proteomic analysis reveals the differential expression of the regulators related to QS, stress response, and motility factors. [ABSTRACT FROM AUTHOR]

A series of thiophene derivatives substituted at 2, 3 and 5 positions were designed and synthesized using 2,3-disubstituted thiophene aldehyde and alcohol as key building blocks. Invitro cytotoxicity assessed against PC-3, DU145 (prostate), A549 (lung), HT29, HCT116 (colon), MCF7, MDAMB231 (breast), B16F10 (melanoma) NCI (Colorectal) cancer cell lines by conducting (MTT) assay of thiophene derivatives. Most of these synthesized compounds showed anti-cancer activity, compound 5b showed good cytotoxicity with IC50 = 2.61 ± 0.34 µM on HT29 cell line. Also, the key property of cell migration was observed while treating cells with 5b. The Cell cycle arrest at G2/M phase was observed by 5b on HT29 cell line which inhibited tubulin polymerization with IC50 value of 8.21 ± 0.30 μM. Moreover, binding pose with co-crystal ligand and interaction with colchicine binding site of 5b was established by molecular docking studies. Hence this scaffold can be developed as anti-cancer agents that target tubulin polymerization. [ABSTRACT FROM AUTHOR]

Crataeva adansonii is a medicinal plant and many folklore uses of this plant are well known to us. Pharmacognostic studies like finding extractive values and nutritional values play a vital role in the determination of adulterated or exhausted drugs. It lays down parameters for authentication and standardization of drugs. The cytotoxic study helps in the evaluation of a drug for its toxicity, which is determined by the prevention of growth and replication. Such drugs can be used to treat cancer, multiple sclerosis and rheumatoid arthritis. During the present study ethanolic extracts of leaf and bark parts of C. adansonii were evaluated through cytotoxic activity. Brine shrimp larvae assay was conducted for this purpose. Extractive values of leaf and bark parts were estimated using n-hexane, chloroform, ethanol, methanol, water, and ether as a solvent. 10g of plant powder was dissolved in 200 ml solvent during various extract preparations Fluorescence study was conducted after treating the powder drug with different reagents including ethanol, methanol, acetic acid, n-hexane, HCl, nitric acid, carrageenan, glacial acetic acid, diethyl ether and picric acid and change in coloration was observed. Distinct fluorescence was exhibited by the drug under the normal daylight and UV-radiations of short wavelength (256nm) and long wavelength (365nm). Both the leaf and bark parts showed maximum extractive values in water (23% and 15% respectively) followed by methanol (15% and 6% respectively. The leaf part showed greater extractive values as compared to the bark. The cytotoxic study revealed that the ethanolic extract crude drugs of each part dose-dependently exhibited cytotoxic activity. At higher concentration (100-1000 µg/ml) the leaf and bark ethanolic extracts showed cytotoxicity and at lower concentration (10 µg/ml) very low cytotoxic effect was observed (Figure 4). The LC50 values for crude leaf extract were found to be 5.34 and for that of stem bark extract, it was 7.44 ug/ml. This study manifests that the selected plant can be helpful in the preparation of novel pharmaceuticals. The pharmacognostic evaluation of this important medicinal drug will be supportive in the detection of adulteration and drug quality control. [ABSTRACT FROM AUTHOR]

Recently, Ag/ZnO nanocomposite (Ag/ZnONC) has been known as one of effective antimicrobial agents. However, its interesting aspects could cause several health effects. This problem can be rectified by capping its surface via the addition of a biomolecule which form a "bio-capped layer" around the particles and prevent them from interacting human cells. In this study, a new fabrication of bio-capped Ag/ZnONCs in various amounts of silver has been reported. Stable and spherical bio-capped Ag/ZnONCs were produced using extract which acts as a reducing and capping agent. The physicochemical, properties of the fabricated NCs was characterized by UV-Vis, XRD, DLS, zeta potential, SEM, XRD, EDX, and FTIR, antioxidant activity. In addition, the mechanism of fabrication has been suggested. Our method of fabrication could be an eco-friendly technique and considered as an alternative to other techniques such as electro- and photo-chemical, chemical, and physical techniques. Our results show that the as-synthesized Ag/ZnONCs possess antioxidant activity and the secondary metabolites of the extract adsorbed on the NC reacts with DPPH. Moreover, the cytotoxicity of bio-capped Ag/ZnONCs (0.15% of Ag) to treat cell lines was evaluated by using cell viability test of human A549 cell line. The obtained results demonstrated that concentrations of up to 0.1 mg/mL of bio-capped Ag/ZnONCs induced no significant harmful to the cells. Hence, the present study proved that the fabricated NCs have the potential to use in industrial and pharmacological applications. [ABSTRACT FROM AUTHOR]

The assessment and control of microbial contamination in health care facilities is presently a mandatory and vital part of strategies to prevent and control hospital-acquired infections. This study aims to assess the bioburden with two passive sampling methods (30 ventilations grids swabs and 16 electrostatic dust collectors (EDCs)) at Clinical Pathology Services. The fungal burden was characterized through molecular tools, antifungal resistance, and the mycotoxins and cytotoxicity profile. Total bacteria presented the highest prevalence in both matrixes, whereas Gram-bacteria presented the lowest. Swabs presented a higher prevalence (27.6%) for fungal burden. Chrysonilia sitophila presented the highest prevalence in swabs, whereas for EDCs, C. sitophila and Mucor sp. were the most prevalent. Concerning Aspergillus genera on swabs, section Flavi was the one with the highest prevalence (58.02%), whereas, for EDCs, section Versicolores was the only section observed (100%). Aspergillus section Fumigati was detected in 10 swabs and 7 EDC samples and Aspergillus section Versicolores was detected in one EDC sample. Fungal growth on azole-supplemented media was observed in eight EDC samples. No mycotoxins were detected in any of the samples. A low cytotoxic effect was observed in two sites upon incubation of collected samples with A549 and SK cells and in two other sites upon incubation of collected samples with SK cells only. A medium cytotoxic effect was observed with one EDC sample upon incubation with A549 cells. This study reinforces the need of determination of the azole resistance profile for fungal species and allowed a preliminary risk characterization regarding the cytotoxicity. An intervention including the use of a ultraviolet with wavelength between 200 nm and 280 nm (UVC)—emitting device and an increased maintenance and cleaning of the central heating, ventilation, and air conditioning (HVAC) systems should be ensured to promote the reduction of microbial contamination.

Desalination of seawater is becoming an important means to address the increasing scarcity of freshwater resources in the world. Seawater has been used as drinking water in the health, food, and medical fields and various beneficial effects have been suggested, although not confirmed. Given the presence of 63 minerals and trace elements in drinking desalinated seawater (63 DSW), we evaluated their effects on the behavior of tumorigenic and nontumorigenic cells through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and annexin-V-fluorescein isothiocyanate/propidium iodide staining. Our results showed that cell viability and proliferation in the presence of 63 DSW were significantly greater than in mineral water and in the presence of fetal bovine serum in a dose-dependent manner. Furthermore, 63 DSW showed no toxic effect on murine embryonic fibroblast (NIH-3T3) and murine melanoma (B16-F10) cells. In another assay, we also showed that pre-treatment of non-adherent THP-1 cells with 63 DSW reduces apoptosis incidence, suggesting a protective effect against cell death. We conclude that cell viability and proliferation were improved by the mineral components of 63 DSW and this effect can guide further studies on health effects associated with DSW consumption. [ABSTRACT FROM AUTHOR]

Biosynthesis of novel therapeutic nano‐scale materials for biomedical and pharmaceutical applications has been enormously developed, since last decade. Herein, the authors report an ecological way of synthesising the platinum nanoparticles (PtNPs) using Streptomyces sp. for the first time. The produced PtNPs exhibited the face centred cubic system. The fourier transform infrared spectrum revealed the existence of amino acids in proteins which serves as an essential reductant for the formation of PtNPs. The spherical morphology of the PtNPs with an average size of 20–50 nm was observed from topographical images of atomic force microscopy and field emission scanning electron microscopy. The X‐ray fluorescence spectrum confirms the presence of PtNPs with higher purity. The PtNPs size was further confirmed with transmission electron microscopy analysis and the particles were found to exist in the same size regime. Additionally, PtNPs showed the characteristic surface plasmon resonance peak at 262 nm. Dynamic light scattering studies report that 97.2% of particles were <100 nm, with an average particle diameter of about 45 nm. Furthermore, 3‐(4, 5‐dimethyl‐2‐thiazolyl)‐2, 5‐diphenyl‐tetrazolium assay based in vitro cytotoxicity analysis was conducted for the PtNPs, which showed the inhibitory concentration (IC50) at 31.2 µg/ml against Michigan Cancer Foundation‐7 breast cancer cells. [ABSTRACT FROM AUTHOR]

Highlights: [•] Two dinuclear platinum complexes have been synthesized. [•] Chloride substitution by thiourea and glutathione in water–DMF medium has been studied. [•] An unusual medium was applied due to extremely low solubility of the complexes in water. [•] Trypan blue exclusion tests have been undertaken to estimate cytotoxicity of the complexes. [Copyright &y& Elsevier]

• Spectroscopic analysis of 2-(piperidin-1-ylmethyl)isoindoline-1,3-dione, a potent anti-cancer activity. • The complete assignments are performed on the basis of the total energy distribution (TED). • Density of state diagrams for title molecule is analyzed. • The possible electrophilic and nucleophilic sites are identified. A Mannich base molecule of 2-(piperidin-1-ylmethyl)isoindoline-1,3-dione (PPF) has been synthesized using Mannich base condensation reaction. The molecular geometry of PPF molecule was optimized by B3LYP/6-311G(d,p) basis set. The vibrational frequencies have been assigned with the aid of normal coordinate analysis. Total energy distributions (TED) were used to explain each vibrational wavenumber assignments of a molecule. The 1H and 13C NMR spectroscopic analyses were predicted by using gauge independent atomic orbital (GIAO) method. The thermal stability was determined by applying the thermo gravimetric/differential scanning calorimetry (TG/DSC) studies. The HOMO-LUMO energies, population density of states (PDOS), overlap population density of states (OPDOS), reduced density gradient (RDG), Mulliken atomic charges and molecular electrostatic potential (MEP) surface were plotted to investigate the van der Waals, attraction, repulsion, non-covalent and covalent interactions of the compound. The natural bond orbital (NBO) charge analysis was used in explaining the intermolecular charge transfer and resonance stabilization energy of molecule. Besides, the molecular docking studies have been performed. The cytotoxic activity of the PPF molecule has been resolved. Image, graphical abstract [ABSTRACT FROM AUTHOR]

The assessment and control of microbial contamination in health care facilities is presently a mandatory and vital part of strategies to prevent and control hospital-acquired infections. This study aims to assess the bioburden with two passive sampling methods (30 ventilations grids swabs and 16 electrostatic dust collectors (EDCs)) at Clinical Pathology Services. The fungal burden was characterized through molecular tools, antifungal resistance, and the mycotoxins and cytotoxicity profile. Total bacteria presented the highest prevalence in both matrixes, whereas Gram-bacteria presented the lowest. Swabs presented a higher prevalence (27.6%) for fungal burden. Chrysonilia sitophila presented the highest prevalence in swabs, whereas for EDCs, C. sitophila and Mucor sp. were the most prevalent. Concerning Aspergillus genera on swabs, section Flavi was the one with the highest prevalence (58.02%), whereas, for EDCs, section Versicolores was the only section observed (100%). Aspergillus section Fumigati was detected in 10 swabs and 7 EDC samples and Aspergillus section Versicolores was detected in one EDC sample. Fungal growth on azole-supplemented media was observed in eight EDC samples. No mycotoxins were detected in any of the samples. A low cytotoxic effect was observed in two sites upon incubation of collected samples with A549 and SK cells and in two other sites upon incubation of collected samples with SK cells only. A medium cytotoxic effect was observed with one EDC sample upon incubation with A549 cells. This study reinforces the need of determination of the azole resistance profile for fungal species and allowed a preliminary risk characterization regarding the cytotoxicity. An intervention including the use of a ultraviolet with wavelength between 200 nm and 280 nm (UVC)—emitting device and an increased maintenance and cleaning of the central heating, ventilation, and air conditioning (HVAC) systems should be ensured to promote the reduction of microbial contamination. [ABSTRACT FROM AUTHOR]

The prospect of Zr‐based metallic glasses (MGs) in achieving a combination of properties, such as excellent electrochemical properties and extended biocompatibility, has been studied in this work. The combinatorial method (magnetron co‐sputtering) has been adopted to fabricate two novel quaternary MG systems (Zr50Ti32Cu13Ag5 and Zr40Ti37Co12Ni11) with optimized compositions. The structural analysis has been performed by the grazing incidence x‐ray diffraction and high‐resolution transmission electron microscopy to affirm the disordered structure of the MG systems. The electrochemical analysis demonstrates lower corrosion‐ (0.10 and 0.04 μA cm−2), and passive (2.93 and 1.88 μA cm−2) current densities of the MGs. In addition, the MGs are found to have higher charge transfer resistance (4.70 and 7.86 MΩ cm2) compared to the 316L stainless steel (SS) (0.15 MΩ cm2) and cp‐Ti (0.53 MΩ cm2). The electrochemical features are indicative towards higher corrosion‐resistance capabilities of Zr50Ti32Cu13Ag5 and Zr40Ti37Co12Ni11 MGs to prevent adverse biological reactions. Additionally, the cell proliferation analysis manifests higher cell proliferation on the Zr50Ti32Cu13Ag5 and Zr40Ti37Co12Ni11 MGs for the MC3T3‐E1 preosteoblast cells. Besides, the MTS assay analysis strengthens the prediction of cytocompatibility of the MGs. The integration of such unique properties makes these MG systems ideal candidates for biomedical implants. [ABSTRACT FROM AUTHOR]