Coinage metal-ethylene complexes of sterically demanding 1,10-phenanthroline ligands.

Phenanthroline-based ligands with bulky aryl groups flanking the metal binding pocket enabled the synthesis and detailed investigation of ethylene complexes of copper(I), silver(I), and gold(I), including structural data of [{2,9-bis(2,4,6-triisopropylphenyl)-1,10-phenanthroline}M(C2H4)][SbF6] (M = Cu, Ag, Au), Additionally, a related copper(I)-ethylene complex with a highly fluorinated ligand is also reported. Gold(I) affects the ethylene moiety significantly as evident from the notable upfield coordination shifts of ethylene carbon signals in the NMR and lengthening of the ethylene CC bond length. Silver(I) forms the weakest bond with ethylene in this series of isoleptic, group 11 metal-ethylene complexes. Preliminary catalytic investigations underscore the potential of copper complexes, particularly those with weakly coordinating supporting ligands, as effective catalysts for C(sp3)-H functionalization through trifluoromethyl carbene insertion.

Synthesis and Investigations of the Antitumor Effects of First-Row Transition Metal(II) Complexes Supported by Two Fluorinated and Non-Fluorinated ß-Diketonates.

The 3d transition metal (Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II)) complexes, supported by anions of sterically demanding ß-diketones, 1,3-dimesitylpropane-1,3-dione (HLMes) and 1,3-bis(3,5-bis(trifluoromethyl)phenyl)-3-hydroxyprop-2-en-1-one (HLCF3), were synthesized and evaluated for their antitumor activity. To assess the biological effects of substituents on phenyl moieties, we also synthesized and investigated the analogous metal(II) complexes of the anion of the less bulky 1,3-diphenylpropane-1,3-dione (HLPh) ligand. The compounds [Cu(LCF3)2], [Cu(LMes)2] and ([Zn(LMes)2]) were characterized by X-ray crystallography. The [Cu(LCF3)2] crystallizes with an apical molecule of solvent (THF) and features a rare square pyramidal geometry at the Cu(II) center. The copper(II) and zinc(II) complexes of diketonate ligands, derived from the deprotonated 1,3-dimesitylpropane-1,3-dione (HLMes), adopt a square planar or a tetrahedral geometry at the metal, respectively. We evaluated the antitumor properties of the newly synthesized (Mn(II), Fe(II), Co(II), Ni(II), Cu(II) and Zn(II)) complexes against a series of human tumor cell lines derived from different solid tumors. Except for iron derivatives, cellular studies revealed noteworthy antitumor properties, even towards cancer cells endowed with poor sensitivity to the reference drug cisplatin.

Synthesis and cytotoxicity studies of Cu(I) and Ag(I) complexes based on sterically hindered ß-diketonates with different degrees of fluorination.

Design, synthesis, and in vitro antitumor properties of Cu(I) and Ag(I) phosphane complexes supported by the anions of sterically hindered ß-diketone ligands, 1,3-dimesitylpropane-1,3-dione (HLMes) and 1,3-bis(3,5-bis(trifluoromethyl)phenyl)-3-hydroxyprop-2-en-1-one (HLCF3) featuring trifluoromethyl or methyl groups on the phenyl moieties have been reported. In order to compare the biological effects of substituents on the phenyl moieties, the analogous copper(I) and silver(I) complexes of the anion of the parent 1,3-diphenylpropane-1,3-dione (HLPh) ligand were also synthesized and included in the study. In the syntheses of the Cu(I) and Ag(I) complexes, the phosphane coligands triphenylphosphine (PPh3) and 1,3,5-triaza-7-phosphaadamantane (PTA) were used to stabilize silver and copper in the +1 oxidation state, preventing the metal ion reduction to Ag(0) or oxidation to Cu(II), respectively. X-ray crystal structures of HLCF3 and the metal adducts [Cu(LCF3)(PPh3)2] and [Ag(LPh)(PPh3)2] are also presented. The antitumor properties of both classes of metal complexes were evaluated against a series of human tumor cell lines derived from different solid tumors, by means of both 2D and 3D cell viability studies. They display noteworthy antitumor properties and are more potent than cisplatin in inhibiting cancer cell growth.

Unleashing the most effective oral health education intervention technique for improving the oral hygiene status and oral health knowledge in visually impaired young individuals: A systematic review and meta-analysis.

Appropriate oral health education (OHE) plays a vital role in prevention of oral diseases and would bridge the gap between dentists and visually impaired individuals. Hence, this systematic review was planned with an aim to evaluate effectiveness of various OHE techniques on the oral hygiene status and oral health knowledge of visually impaired young individuals. An electronic search extended to September 30, 2020 was conducted on PubMed, Wiley, ProQuest, ScienceDirect, Cochrane library, EBSCO, and Google Scholar. Two independent reviewers assessed the studies using a two-stage process; data were extracted according to PRISMA statement. Risk of bias assessment of selected studies was executed according to the study designs. Meta-analysis using the random-effects model was conducted for the outcomes for all oral health education techniques using STATASE 16.1 software. Hand and electronic search identified 3829 articles. After screening for titles and duplicates, 37 articles were retrieved, which were screened through abstract and full text. Of the 37 articles, 17 articles were included for qualitative synthesis, and out of that, 13 were for meta-analysis. Ten variations in oral health education (OHE) techniques were used in the included 17 studies to impart oral health education to visually impaired young individuals. Overall, all OHE techniques demonstrated a positive impact on oral hygiene status. The pooled overall cumulative mean difference of the oral hygiene status after imparting education in ATP, Audio, and Braille was 1.33 [1.06, 1.59], 1.76 [1.11, 2.42], and 1.96 [1.40, 2.55], respectively. An appropriate OHE technique boosts confidence in visually impaired young individuals, making the learning process an enjoyable experience. Use of either Braille or the ATP OHE technique was found to be a reliable and useful method to improve oral hygiene of visually impaired young individuals.

Assessment of knowledge and awareness regarding intellectual property rights among the health-care professionals in Belagavi city: A cross-sectional study.

BACKGROUND: Intellectual property rights (IPRs) are increasingly becoming significant for sustainable growth of today's knowledge-based society. An inappropriate knowledge regarding IPR can fail to reserve rights for one's intellectual creation. Hence this study was planned with an aim to assess knowledge, awareness, and practices regarding intellectual property rights in India amongst the health-care professionals in Belagavi city. MATERIALS AND METHODS: A descriptive cross-sectional study was conducted among the postgraduate students and faculty of six health-care professional institutions in Belagavi, Karnataka. A total of 724 responses were recorded using convenient sampling. Data was collected using self-administered validated questionnaire which included demographic details and total 20 questions pertaining to knowledge, awareness, and practices regarding IPR. Two-point Likert scale was used. Descriptive statistics, Mann-Whitney U-test, and Chi-square test were applied. RESULTS: A total of 724 responses were recorded, 411 from postgraduate students and 313 from faculty of 6 health-care professional institutions. It was observed that 24.3% and 39.3% of postgraduate students and faculty participants, respectively, had maximum knowledge while 35.5% of faculty and 27.5% of postgraduate students had maximum awareness regarding IPR in India. Only 17.6% and 10.2% of faculty and postgraduate students had previously attended workshops on IPR. CONCLUSION: The present study identified that both faculty and postgraduate students of health-care profession have less knowledge and awareness regarding IPR. However, both knowledge and awareness regarding IPR were better among faculty when compared to postgraduate students. Thus, the academic community requires a higher level of sensitization and exposure to IPR in India.

Severity of drug resistance and co-existence of Enterococcus faecalis in diabetic foot ulcer infections.

The genes encoding aminoglycoside resistance in Enterococcus faecalis may promote collateral aminoglycoside resistance in polymicrobial wounds. We studied a total of 100 diabetic foot ulcer samples for infection and found 60 samples to be polymicrobial, 5 to be monomicrobial, and 35 samples to be culture negative. A total of 65 E. faecalis isolates were screened for six genes coding for aminoglycoside resistance, antibiotic resistance patterns, and biofilm production. Infectious Diseases Society of America/International Working Group on the Diabetic Foot system was used to classify the wound ulcers. Majority of the subjects with culture-positive wound were recommended conservative management, while 14 subjects underwent amputation. Enterococcal isolates showed higher resistance for erythromycin, tetracycline, and ciprofloxacin. Isolates from grade 3 ulcer showed higher frequency of aac(6')-Ie-aph(2″)-Ia, while all the isolates were negative for aph(2″)-Ib, aph(2″)-Ic, and aph(2″)-Id. The isolates from grade 3 ulcers showed higher resistance to aminoglycosides as well as teicoplanin and chloramphenicol. All the 39 biofilm producers were obtained from polymicrobial wound and showed higher resistance when compared to biofilm non-producers. Higher frequency of isolates carrying aac(6')-Ie-aph(2″)-Ia in polymicrobial community showing resistance to key antibiotics suggests widespread distribution of aminoglycoside-resistant E. faecalis and their role in worsening diabetic foot ulcers.

Virulence determinants in clinical Staphylococcus aureus from monomicrobial and polymicrobial infections of diabetic foot ulcers.

Antibiotic resistance in Staphylococcus aureus is a major public health concern, and methicillin-resistant S. aureus has emerged as an important pathogen. We characterized S. aureus isolates from monomicrobial and polymicrobial wound infections from 200 diabetic individuals with foot ulcers to understand their underlying diversity and pathogenicity. Staphylococcal cassette chromosome mec typing was performed, and genes coding for production of biofilm, Panton-Valentine leukocidin, toxic shock syndrome toxin and leukotoxins DE and M were screened. Biofilm production was also quantified by the tissue culture plate method. Strains were genotyped using multilocus sequence typing, multiple-locus variable number tandem repeat analysis and repetitive sequence PCR methods. Polymicrobial infections were present in 115 samples, 61 samples showed monomicrobial infection and 24 samples were culture negative. Polymicrobial infections were significantly higher in patients with previous amputation history. Of the 86 samples infected with S. aureus, virulence genes were found in 81 isolates, and 41 isolates possessed more than one virulence gene. Strains which contained pvl gene alone or luk-DE alone were significantly higher in polymicrobial wounds. Based on biofilm production, 18.6 % of isolates were classified as high, 24.4 % as moderate and 57 % as low biofilm producers. Genotyping of 30 strains revealed 10 different sequence types with a strong association among sequence types, specific virulence markers and antibiotic resistance profiles. Moreover, isolates from monomicrobial and polymicrobial wounds differed significantly in their virulence potential and the sequence types to which they belonged, and these are helpful in mapping the evolution of the identified strains of S. aureus.

Modulation of genetic clusters for synthesis of bioactive molecules in fungal endophytes: A review.

Novel drugs with unique and targeted mode of action are very much need of the hour to treat and manage severe multidrug infections and other life-threatening complications. Though natural molecules have proved to be effective and environmentally safe, the relative paucity of discovery of new drugs has forced us to lean towards synthetic chemistry for developing novel drug molecules. Plants and microbes are the major resources that we rely upon in our pursuit towards discovery of novel compounds of pharmacological importance with less toxicity. Endophytes, an eclectic group of microbes having the potential to chemically bridge the gap between plants and microbes, have attracted the most attention due to their relatively high metabolic versatility. Since continuous large scale supply of major metabolites from microfungi and especially endophytes is severely impeded by the phenomenon of attenuation in axenic cultures, the major challenge is to understand the regulatory mechanisms in operation that drive the expression of metabolic gene clusters of pharmaceutical importance. This review is focused on the major regulatory elements that operate in filamentous fungi and various combinatorial multi-disciplinary approaches involving bioinformatics, molecular biology, and metabolomics that could aid in large scale synthesis of important lead molecules.

Anti-Plaque Efficacy of Herbal and 0.2% Chlorhexidine Gluconate Mouthwash: A Comparative Study.

BACKGROUND: Mouthwashes are an adjunct to, not a substitute for, regular brushing and flossing. Chlorohexidine is cationic bis-biguanide broad spectrum antiseptic with both anti-plaque and antibacterial properties. It has side-effects like brownish discoloration of teeth and dorsum of the tongue, taste perturbation, oral mucosal ulceration, etc. To compare the antiplaque efficacy of herbal and chlorohexidine gluconate mouthwash. MATERIALS AND METHODS: A double-blinded parallel, randomized controlled clinical trial was conducted in the Department of Periodontics, MNR Dental College. Totally 100 preclinical dental students were randomized into three groups (0.2% chlorohexidine, Saline and herbal mouthwash). All the groups were made to refrain from their regular mechanical oral hygiene measures and were asked to rinse with given respective mouthwashes for 4 days. The gingival and plaque scores are evaluated on 1(st) day, and 5(th) day, and differences were compared statistically. RESULTS: There was no significant difference in the gingival index (GI) and plaque index (PI) scores of the pre-rinsing scores of three groups and mean age of subjects in the three age groups, suggesting selected population for the three groups was homogenous. Mean GI and PI scores at the post rinsing stage were least for the Group A, followed by B and C. The difference of post rinsing PI and GI scores between Group A and Group B were statistically non-significant, which means anti-gingivitis and plaque inhibiting properties are similar for both. CONCLUSION: Within the limitations of this study chlorhexidine gluconate and herbal mouthwash (Hiora) showed similar anti plaque activity with latter showing no side effects.

Evaluation of Anti-Inflammatory Effects of Curcumin Gel as an Adjunct to Scaling and Root Planing: A Clinical Study.

BACKGROUND: Complete removal of irritants is not possible with mechanical therapy alone. Adjunctive use of systemic administration of antibiotics results in the distribution of drug throughout the body, which can give rise to toxicity. Curcumin (diferuloylmethane), a constituent of Curcuma longa plant, which possess antioxidant, anti-inflammatory, anti-carcinogenic, anti-microbial, anti-hyper algesic and hypocholesterolemic properties. The aim of the present study is to compare the effects of the curcumin gel as an adjunct to subgingival scaling and root planning with the effect achieved using subgingival scaling and root planning alone. MATERIALS AND METHODS: Thirty patients either male or female with chronic localized or generalized periodontitis aged between 25 and 60 years with pocket depth of 5-7 mm affecting at least two nonadjacent sites were included. In the experimental site scaling and root planning was performed, followed by placement of the curcumin gel and periodontal pack application. In the control site, subgingival scaling alone was performed followed by periodontal pack application. Parameters included were: Plaque index (PI), gingival index (GI), probing depth (PD) and clinical attachment loss. These parameters were recorded on day 0, 30 and 45 days. RESULTS: Significant reduction in mean was observed in PI, GI, PD and gain in clinical attachment level were demonstrated in both the groups from baseline to 45 days. However, statistical significant reduction was observed in PI at baseline and 30(th) day and GI at 30(th) day. CONCLUSION: Curcumin can be effectively used along with scaling and root planning. Future research is required to determine the long-term effects of curcumin on a large sample of subjects.

Characteristics of microbial drug resistance and its correlates in chronic diabetic foot ulcer infections.

While virulence factors and the biofilm-forming capabilities of microbes are the key regulators of the wound healing process, the host immune response may also contribute in the events following wound closure or exacerbation of non-closure. We examined samples from diabetic and non-diabetic foot ulcers/wounds for microbial association and tested the microbes for their antibiotic susceptibility and ability to produce biofilms. A total of 1074 bacterial strains were obtained with staphylococci, Pseudomonas, Citrobacter and enterococci as major colonizers in diabetic samples. Though non-diabetic samples had a similar assemblage, the frequency of occurrence of different groups of bacteria was different. Gram-negative bacteria were found to be more prevalent in the diabetic wound environment while Gram-positive bacteria were predominant in non-diabetic ulcers. A higher frequency of monomicrobial infection was observed in samples from non-diabetic individuals when compared to samples from diabetic patients. The prevalence of different groups of bacteria varied when the samples were stratified according to age and sex of the individuals. Several multidrug-resistant strains were observed among the samples tested and most of these strains produced moderate to high levels of biofilms. The weakened immune response in diabetic individuals and synergism among pathogenic micro-organisms may be the critical factors that determine the delicate balance of the wound healing process.

Isolation and partial characterization of delayed releasing starches of Colocasia species from Jharkhand, India.

There is an increasing interest in starch manufactured from edible tubers for controlled delivery of drug. Starches of different cultivars of Colocasia from Jharkhand, North Eastern State of India, were isolated and their morphological, physicochemical, structural properties were studied. The yield of starches was estimated in the range of 6.46-13.75%. All the isolated starches revealed their irregular shape with a diameter of 5-10 µm. There was considerable variation in amylose content, swelling and solubility power, water hydration capacity. FTIR spectra confirmed their carbohydrate nature. Powder studies revealed that these starches possess potential for pharmaceutical industries. In vitro release data revealed the delayed release of all tablets made by using Colocasia starches at pH 6.8 and 7.4 when compared with maize starch. Delayed release of all starches showed there is a great potential to be used these starches as pharmaceutical excipient in sustained release dosage form with minimum modification.

Isolation and physicochemical characterization of sustained releasing starches from Dioscorea of Jharkhand.

Starches were isolated from varieties of Dioscorea (Da1, Da2) grown in Jharkhand state of India and it was characterized in terms of moisture, ash, amylose content, bulk density, tapped density, true density, porosity, Carr's index, Hausner's ratio, swelling power, solubility, water holding capacity, paste clarity. Morphological, thermal and IR spectroscopic studies were also done to characterize the isolated starch. The shape and size of starch granules were round/oval to ellipsoid and 5-10µm. There were considerable differences in powder characteristics, amylose content, ash values, and water holding capacity, swelling and solubility power. Starch from variety Da2 showed high enthalpy of gelatinization temperature as compared to variety Da1. Peaks in FTIR spectra of both starches revealed its carbohydrate nature. In vitro studies revealed that both the starches from Da1 and Da2 can be used in developing sustained release formulations. The result showed that starches from both Dioscorea can be used in pharmaceutical industries as excipients with minimal modifications.

Implications from predictions of HLA-DRB1 binding peptides in the membrane proteins of Corynebacterium diphtheriae.

The aerobic gram positive bacterium Corynebacterium diphtheriae causes diphtheria, a respiratory tract illness characterized by symptoms such as sore throat, low fever, and an adherent membrane on the tonsils, pharynx, and/or nasal cavity. Therefore, it is important to develop preventive vaccines for diphtheria. The availability of the 2,488,635 bp long complete sequence for the C. diphtheriae genome provides an opportunity to understand cell mediated immune response using Computational Biology tools from the bacterial proteome sequence data. We selected 355 membrane proteins from the C. diphtheriae proteome using annotation data to identify potential HLA-DRB1 binding short peptide using modeling, simulations and predictions. This exercise identified 30 short peptides in membrane proteins showing binding capability to HLA-DRB1 alleles. These peptides serve as outline for the understanding of cell mediated immune response to C. diphtheriae. It should be noted that the predicted data to be verified using binding assays for further consideration.