COUMARINS: A UNIQUE SCAFFOLD WITH VERSATILE BIOLOGICAL BEHAVIOR

Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study

Effect of obesity and metabolic syndrome on severity, quality of life, sleep quality and inflammatory markers in patients of asthma in India

Introduction: The study aimed to compare the effect of obesity with and without metabolic syndrome on asthma severity, quality of life, sleep quality, sleep disordered breathing and inflammatory markers as compared to non-obese asthma patients. Material and methods: 60 asthma patients recruited for the study were divided equally into non-obese (NOA), obese without metabolic syndrome (OANMS) and obese with metabolic syndrome (OAMS) groups. Study cohorts were assessed for severity of asthma, quality of life and quality of sleep using questionnaires and inflammatory markers (FENO, hs-CRP, IL-5, IL-6 and leptin). Institutional ethical committee approved the study. Results: The results suggests OAMS patients may be a subtype of asthmatics having significantly severe asthma (p < 0.05), poor quality of life (p < 0.05), high risk of OSA (p < 0.05), decreased lung volumes (FRC) (p < 0.05), higher levels of inflammatory markers (leptin and IL-6) (p < 0.05), and high incidence of sleep disordered breathing (p < 0.05) in comparison to NOA and OANMS patients. Conclusions: The present study has shown that obese asthmatics especially with metabolic syndrome represent a subtype of asthmatic population. Hence, the treatment of metabolic syndrome may be necessary in addition to asthma to achieve optimal control.  INTRODUCTION: The study aimed to compare the effect of obesity with and without metabolic syndrome on asthma severity, quality of life, sleep quality, sleep disordered breathing and inflammatory markers as compared to non-obese asthma patients. MATERIAL AND METHODS: 60 asthma patients recruited for the study were divided equally into non-obese (NOA), obese without metabolic syndrome (OANMS) and obese with metabolic syndrome (OAMS) groups. Study cohorts were assessed for severity of asthma, quality of life and quality of sleep using questionnaires and inflammatory markers (FENO, hs-CRP, IL-5, IL-6 and leptin). Institutional ethical committee approved the study. RESULTS: The results suggests OAMS patients may be a subtype of asthmatics having significantly severe asthma (p < 0.05), poor quality of life (p  < 0.05), high risk of OSA (p < 0.05), decreased lung volumes (FRC) (p < 0.05), higher levels of inflammatory markers (leptin and IL-6) (p  < 0.05), and high incidence of sleep disordered breathing (p < 0.05) in comparison to NOA and OANMS patients. CONCLUSIONS: The present study has shown that obese asthmatics especially with metabolic syndrome represent a subtype of asthmatic population. Hence, the treatment of metabolic syndrome may be necessary in addition to asthma to achieve optimal control.

Bronchoscopy in immediate diagnosis of smear negative tuberculosis

Wstęp: Gruźlica jest poważnym problemem zdrowia publicznego. Prawie u 30% chorych na gruźlicę bezpośrednie badanie plwociny na prątki jest ujemne. Prowadzi to do niezamierzonych opóźnień w leczeniu tych przypadków. W niniejszym badaniu zaplanowano ocenę roli bronchoskopii w szybkim rozpoznaniu gruźlicy u tych chorych.Materiał i metody: Niniejsze badanie jest retrospektywną analizą 132 chorych z podejrzeniem gruźlicy, u których nie stwierdzono prątków w bezpośrednim badaniu plwociny i którzy zostali poddani bronchoskopii w okresie 2002–2013.Gruźlicę rozpoznawano na podstawie stwierdzenia prątków w wydzielinie oskrzelowej lub w płukaniu oskrzelowo-pęcherzykowym względnie w materiale uzyskanym z biopsji. Rozpoznawano również gruźlicę na podstawie stwierdzenia martwicy serowatej w materiale z biopsji.Wyniki: Wynik niniejszego badania wykazał, że w wyniku bronchoskopii było możliwe ustalenie rozpoznania w 68,2% przypadków, w których badanie plwociny było negatywne. Potwierdzenie uzyskano po stwierdzeniu prątków w wydzielinie oskrzelowej lub płukaniu oskrzelowo-pęcherzykowym w 51,5% przypadków a na podstawie badania materiału z biopsji w 16,5%.Wnioski: Wyniki niniejszego badania wskazują na ważne miejsce bronchoskopii w szybkiej diagnostyce gruźlicy u chorych z ujemnym bezpośrednim badaniem plwociny. Pozwala to na uniknięcie opóźnień w rozpoznawaniu gruźlicy i nas zybkie podjęcie odpowiedniego leczenia.Background: Tuberculosis is a major public health problem. Almost 30% of cases of tuberculosis are known to be sputum smear negative. There is a diagnostic dilemma in such cases leading to inadvertent delays in management of these cases. The present study was planned to assess the role of bronchoscopy in immediate diagnosis of smear negative pulmonary tuberculosis.Material and methods: The present study is a retrospective analysis of 132 sputum smear negative tuberculosis suspects who underwent bronchoscopic evaluation during the period 2002–2013. The diagnosis of tuberculosis was based on the finding of bacilli in aspirate or in tissue biopsy or the demonstration of caseous necrosis on tissue biopsy.Results: The present study showed that bronchoscopy could lead to immediate, accurate diagnosis in 68.2% of suspected smear negative cases. Bronchial aspirate and bronchoalveolar lavage alone were diagnostic in 51.5% of such cases while tissue biopsy added to the yield in another 16.5% cases.Conclusions: The results of the present study suggests an important place of bronchoscopy in immediate diagnosis of suspected smear negative tuberculosis, thus avoiding inadvertent delays in diagnosing and instituting appropriate treatment

SYNTHESIS AND INVESTIGATION OF ANTHELMINTIC, ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY OF 3,3-DIPHENYL PROPANAMIDE DERIVATIVES

Objective: A novel series of substituted 3,3-diphenyl propanamide derivatives (I-VIII) were synthesized by reacting 3,3-diphenyl propanoyl chloride with different amines/amino acids, and all the derivatives were investigated for anthelmintic, antibacterial, and antifungal activity.Methods: All the compounds were characterized by infrared (IR) and1H- nuclear magnetic resonance spectrometry data. The synthesized derivatives were investigated for their anthelmintic activity employing housefly worms method and earthworm species model. The antibacterial and antifungal activity was performed employing cup plate method.Results: The synthesized compounds (VII and VIII) exhibited maximum anthelmintic activity as compared with standard drug albendazole at doses of 50 and 100 mg/mL, due to minimal paralyzing and death time in both housefly and earthworm models. The compounds (IV, VII, and VIII) at 50 μg/mL exhibited maximum activity against Gram-negative bacterial strains, namely, Escherichia coli, Pseudomonas aeruginosa as compared with ciprofloxacin and same compounds exhibited maximum antifungal activity against Candida albicans and Aspergillus niger in comparison with standard drug griseofulvin at 50 μg/mL.Conclusion: The synthesized compounds bearing amino acid moiety in their structure (VII-VIII) exhibited impressive anthelmintic activity in comparison with albendazole. This suggests that amino acid/peptide derivative of diphenyl propanamides can act as great anthelmintic agents. Further, the research can be performed to design potent antimicrobial diphenyl propanamide derivatives.Â

DESIGN AND DEVELOPMENT OF LOSARTAN POTASSIUM FLOATING DRUG DELIVERY SYSTEMS

Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner's ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type

Wpływ otyłości i zespołu metabolicznego na ciężkość choroby, jakość życia, jakość snu i markery zapalenia u chorych na astmę w Indiach

  WSTĘP: Celem badania było porównanie ciężkości astmy, jakości życia, jakości snu, zaburzeń oddychania w czasie snu i markerów zapalenia u chorych na astmę z otyłością, z lub bez zespołu metabolicznego z analogicznymi parametrami w grupie chorych na astmę bez otyłości. MATERIAŁ I METODY: Do badania włączono 60 chorych na astmę, których podzielono na równe pod względem liczebności grupy chorych bez otyłości (NOA non-obese), otyłych bez zespołu metabolicznego (OANMS, obese without metabolic syndrome) oraz otyłych z zespołem metabolicznym (OAMS, obese with metabolic syndrome). Przedmiotem oceny była ciężkość astmy, jakość życia oraz jakość snu za pomocą kwestionariuszy i stężenia markerów zapalenia (FENO, hs-CRP, IL-5, IL-6 i leptyna). Badanie uzyskało aprobatę komisji etycznej odpowiedniej dla instytucji. WYNIKI: Wyniki badań wskazują, że chorzy z grupy OAMS mogą reprezentować podtyp astmy o istotnie cięższym przebiegu (p < 0,05), gorszej jakości życia (p < 0,05), większym ryzyku obturacyjnego bezdechu podczas snu (p < 0,05), z obniżoną czynnościową pojemnością zalegającą (FRC) (p < 0,05), wyższymi stężeniami markerów zapalenia (leptyna i IL-6) (p < 0,05) oraz częstszym występowaniem zaburzeń oddychania podczas snu (p < 0,05) w porównaniu z grupami NOA i OANMS. WNIOSKI: W badaniu wykazano, że otyli chorzy na astmę, a szczególnie z zespołem metabolicznym, stanowią szczególny podtyp. Z tego powodu leczenie zespołu metabolicznego wraz z odpowiednim leczeniem astmy może być niezbędne w celu uzyskania optymalnej kontroli choroby.

Parasitic Plants as Vectors for Pathogens

Parasitic plants obtain their nutrition from their hosts. In addition to this direct damage, they cause indirect damage to their hosts by transmitting various plant pathogens. There are some 4,500 species of parasitic plants known; out of them, nearly 60% are root parasites and the rest of them parasitise on the shoot parts. Orobanchaceae and Convolvulaceae are the two mostly studied families of parasitic plants; and the parasitic plants are the chief mode for transmission of the phytoplasmas. The parasitic plants have various modes of obtaining nutrition; however, the information about the mechanism(s) involved in the pathogen transmission by the parasitic plants is limited. The latest biotechnolgical advances, such as metagenomics and high througput sequencing, carry immense promise in understanding the host-parasitic plant-pathogen association in deeper details; and initiatives have indeed been taken. Nevertheless, compared to the other pests hindering crop productivity, parasitic plants have not yet been able to gain the needed attention of the plant scientists. In this chapter, we review and present some of the latest advances in the area of these important plant pests

Structure-based virtual screening methods for the identification of novel phytochemical inhibitors targeting furin protease for the management of COVID-19

The coronavirus disease 2019 (COVID-19), caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, is a highly contagious respiratory disease with widespread societal impact. The symptoms range from cough, fever, and pneumonia to complications affecting various organs, including the heart, kidneys, and nervous system. Despite various ongoing efforts, no effective drug has been developed to stop the spread of the virus. Although various types of medications used to treat bacterial and viral diseases have previously been employed to treat COVID-19 patients, their side effects have also been observed. The way SARS-CoV-2 infects the human body is very specific, as its spike protein plays an important role. The S subunit of virus spike protein cleaved by human proteases, such as furin protein, is an initial and important step for its internalization into a human host. Keeping this context, we attempted to inhibit the furin using phytochemicals that could produce minimal side effects. For this, we screened 408 natural phytochemicals from various plants having antiviral properties, against furin protein, and molecular docking and dynamics simulations were performed. Based on the binding score, the top three compounds (robustaflavone, withanolide, and amentoflavone) were selected for further validation. MM/GBSA energy calculations revealed that withanolide has the lowest binding energy of −57.2 kcal/mol followed by robustaflavone and amentoflavone with a binding energy of −45.2 kcal/mol and −39.68 kcal/mol, respectively. Additionally, ADME analysis showed drug-like properties for these three lead compounds. Hence, these natural compounds robustaflavone, withanolide, and amentoflavone, may have therapeutic potential for the management of SARS-CoV-2 by targeting furin

Forward-central two-particle correlations in p-Pb collisions at root s(NN)=5.02 TeV

Two-particle angular correlations between trigger particles in the forward pseudorapidity range (2.5 2GeV/c. (C) 2015 CERN for the benefit of the ALICE Collaboration. Published by Elsevier B. V.Peer reviewe

Azimuthal anisotropy of charged jet production in root s(NN)=2.76 TeV Pb-Pb collisions

We present measurements of the azimuthal dependence of charged jet production in central and semi-central root s(NN) = 2.76 TeV Pb-Pb collisions with respect to the second harmonic event plane, quantified as nu(ch)(2) (jet). Jet finding is performed employing the anti-k(T) algorithm with a resolution parameter R = 0.2 using charged tracks from the ALICE tracking system. The contribution of the azimuthal anisotropy of the underlying event is taken into account event-by-event. The remaining (statistical) region-to-region fluctuations are removed on an ensemble basis by unfolding the jet spectra for different event plane orientations independently. Significant non-zero nu(ch)(2) (jet) is observed in semi-central collisions (30-50% centrality) for 20 <p(T)(ch) (jet) <90 GeV/c. The azimuthal dependence of the charged jet production is similar to the dependence observed for jets comprising both charged and neutral fragments, and compatible with measurements of the nu(2) of single charged particles at high p(T). Good agreement between the data and predictions from JEWEL, an event generator simulating parton shower evolution in the presence of a dense QCD medium, is found in semi-central collisions. (C) 2015 CERN for the benefit of the ALICE Collaboration. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).Peer reviewe