The lipophilic derivative of thalidomide (4-(1,3-dioxo-1,3-dihydro-2
-isoindol-2-yl)-
-(4-ethoxyphenyl)methylidenebenzohydrazide,
) was synthesized to enhance its characteristics and efficacy. ...Earlier studies have proved the immunomodulatory and anti-inflammatory effects of
. In this study the interaction between bovine serum albumin (BSA) and
was studied using a multi-spectroscopic approach which included UV spectrophotometry, spectrofluorimetry and three dimensional spectrofluorometric and molecular docking studies. Static quenching was involved in quenching the fluorescence of BSA by
, because a complex formation occurred between the
and BSA. The binding constant decreased with higher temperature and was in the range of 2.5 × 10⁵-4.8 × 10³ L mol
suggesting an unstable complex at higher temperatures. A single binding site was observed and the the site probe experiments showed site II (sub-domain IIIA) of BSA as the binding site for
. The negative values of ∆G⁰, ∆H⁰ and ∆S⁰ at (298/303/308 K) indicated spontaneous binding between
and BSA as well as the interaction was enthalpy driven and van der Waals forces and hydrogen bonding were involved in the interaction. The docking results and the results from the experimental studies are complimentary to each other and confirm that
binds at site II (sub-domain IIIA) of BSA.
The binding interaction between bovine serum albumin (BSA) and roflumilast (ROF) was explored in this study. The binding of drugs to albumin plays a vital role in their pharmacokinetics and ...pharmacodynamics in vivo. The mechanisms involved in the interaction between BSA and ROF was studied using multi-spectroscopic experimental and computational approaches.
Spectrofluorometric experiments were used to determine the method of quenching involved and the conformational changes in the BSA. UV-visible spectroscopy synchronous and three-dimensional fluorescence spectroscopy were used to further explore the binding interaction mechanism.
The results suggested that the intrinsic fluorescence of BSA was quenched due to the formation of a static complex between ROF and BSA. Conformational changes in BSA were determined based on its interaction with ROF. The thermodynamic results suggested that the interaction between ROF and BSA was spontaneous and a hydrophobic interaction occurred between them. Site I of BSA was suggested as the site of interaction between ROF and BSA based on the site marker experiments.
The molecular simulation results and the experimental outcomes were complimentary to each other and helped to identify the binding site and nature of bonds involved in the interaction between ROF and BSA.
Diagnosis of COVID-19 infection in cancer patients is critical to co-manage their underlying disease and infection appropriately. Our study aimed at evaluating the sensitivity and specificity of ...screening patients with cancer for COVID-19 infection.
All oncology patients receiving care at Department of Oncology at King Abdulaziz Medical City in Riyadh were screened using the acute respiratory infection (ARI) survey. Nasopharyngeal and throat swap for polymerase chain reaction (PCR) testing for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) was performed on patients who have high ARI score (i.e. ≥ 4), or any patient requiring elective/emergency hospitalization, undergoing a procedure as well as screening asymptomatic patients receiving chemotherapy between April 1st and July 30, 2020. Institutional Review Board approval was obtained. Descriptive and inferential analyses were done and sensitivity, specificity, positive and negative predictive values (PPV and NPV) were calculated considering the COVID-19 PCR as the gold standard.
During the study period, a total of 473 patients were included with a median age was 56 years (14–104), 51% were female, 73% had solid tumors, and 66% received treatment within the last 3 months. These patients underwent 688 PCR tests along with ARI survey screening. Testing was done in the outpatient, inpatient, and emergency department setting in 41%, 40% and 19% of the patients, respectively. Majority of tests were screening of asymptomatic patients and only 23% were tested for suspected infections with ARI ≥ 4. A total of 54 patients (8%) had positive PCR for COVID-19 infection. The prevalence of infection varied from month to month ranging from 1.09% in April up to 19.70% in June and correlated with the average daily and active case load at a national level. The diagnostic yield of the ARI score also correlated with infection burden nationally. The PPV and NPV of the ARI as a screening tool was 18.24% (0–31.8) and 95.6% (86.36–98.86%) with the PPN fluctuating considerably in parallel with the prevalence of COVID-19 result. Similarly, the sensitivity and specificity of the ARI were 55.77% (0–70.59) and 79.4 (69.19–92), respectively.
The yield of screening asymptomatic patients with cancer varies based on the community burden of COVID-19 infection. As universal screening can cause delays to patient care, it should be tailored based on the individual patient risks and infection burden in the region.
The FT-Raman and FT-IR spectra of N-(adamantan-1-yl)-1,2,3,4-tetrahydroisoquinoline-2-carbothioamide were recorded and investigated. The DFT/M06-2X/6-311++G(d,p) method was used to compute the ...vibrational wavenumbers. The effect of solvents (water, carbon tetrachloride and chloroform) on the dipole moment and polarizability has been evaluated. UV–Vis spectrum of the title compound was recorded and compared with the theoretical spectrum calculated by TD-DFT approach. To investigate the movement of electrons within the system when excited, the difference of the excited and ground state densities has also been plotted. The molecular docking studies reveals that the investigated compound may exhibit HIV-1 Protease inhibitory activity.
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•Molecular properties of C20H26N2S, having tetrahydroisoquinoline, carbothiomide and adamantane moieties.•Effect of the solvents on the dipole moment and polarizability has been investigated.•Total electron density difference between ground and excited states have been plotted.•Molecular Docking studies reveal, C20H26N2S as a potential inhibitor of HIV-1 Protease.
The present study describes the development of a novel analytical approach that can reduce by 50-fold the consumption of organic solvents in the charge transfer (CT)-based spectrophotometric ...analysis. The proposed approach employed 96-microwell assay plates for carrying out the reaction. The CT reaction between the electron-donating analyte and electron-accepting reagent was performed in microwells (200-μL of organic solvent) and the color signals were measured with a microwell-plate reader. Optimum conditions for the proposed approach were established for two antihypertensive drugs, namely ramipril (RML) and lisinopril (LSL) as model compounds for the electron-donating analytes, and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) as a π-electron acceptor. Under the optimum conditions, Beer's law was obeyed in the concentration range of 6-100 and 6-60 μg mL-1 for RML and LSL, respectively. The limits of detection were 0.97 and 1.10 μg mL-1 for RML and LSL, respectively. The precision of the methods was satisfactory; the values of relative standard deviations did not exceed 1.1 %. The proposed approach was successfully applied to the analysis of pharmaceutical dosage forms with good accuracy and precision. The results were comparable with those of the reported methods. The approach described herein is of great practical value in pharmaceutical analysis because it reduces the exposure of analysts to the toxic effects of organic solvents, lowers the analysis cost by 50-fold, and it has a high throughput property. Although the approach was validated for RML and LSL, the same methodology could be used for any electron-donating analyte for which a CT-reaction can be performed.
U radu je opisan razvoj novog analitičkog pristupa koji 50 puta smanjuje potrošnju organskih otapala u spektrofotometrijskoj analizi na bazi prijenosa naboja (CT). Predložena metoda koristi ploče s 96 jažica za izvođenje analize. CT reakcije između elektron-donora i elektron-akceptora izvode se u jažicama s 200-μL organskog otapala. Promjene boje mjere se pomoću posebnog mikročitača za ploče s jažicama. Određeni su optimalni uvjeti za dva antihipertenzivna lijeka, ramipril (RML) i lizinopril (LSL) koji su upotrebljeni kao modelni spojevi za elektron-donorske analite, i 2,3-diklor-5,6-dicijano-1,4-benzokinon (DDQ) kao π-elektronski akceptor. U optimalnim uvjetima Beerov zakon je vrijedio u koncentracijskom području 6-100 i 6-60 μg mL-1 za RML, odnosno LSL. Granice detekcije bile su 0,97 i 1,1 μg mL-1 za RML, odnosno LSL. Preciznost metode bila je zadovoljavajuća, a relativna standardna devijacija bila je manja od 1,1 %. Predložena metoda uspješno je primijenjena za analizu doziranih farmaceutskih pripravaka koji sadrže ispitivane lijekove, uz dobru točnost i preciznost. Rezultati predložene metode usporedivi su s rezultatima poznatih metoda. Postupak opisan u ovom radu vrlo je praktičan: analitičari su manje izloženi toksičnim učincima organskih otapala, troškovi analize smanjeni su 50 puta, a također ju odlikuje visoka propusnost. Iako je postupak validiran za RML i LSL, ista metoda može se upotrijebiti za elektron-donirajući analit koji ulazi u CT reakciju.
Saudi lung cancer management guidelines 2017 Jazieh, Abdul Rahman; Al Kattan, Khaled; Bamousa, Ahmed ...
Annals of thoracic medicine,
10/2017, Letnik:
12, Številka:
4
Journal Article
Recenzirano
Odprti dostop
Lung cancer management is getting more complex due to the rapid advances in all aspects of diagnostic and therapeutic options. Developing guidelines is critical to help practitioners provide standard ...of care.
The Saudi Lung Cancer Guidelines Committee (SLCGC) multidisciplinary members from different specialties and from various regions and healthcare sectors of the country reviewed and updated all lung cancer guidelines with appropriate labeling of level of evidence. Supporting documents to help healthcare professionals were developed.
Detailed lung cancer management guidelines were finalized with appropriate resources for systemic therapy and short reviews highlighting important issues. Stage based disease management recommendation were included. A summary explanation for complex topics were included in addition to tables of approved systemic therapy.
A multidisciplinary lung cancer guidelines was developed and will be disseminated across the country.
Geochemical study of groundwater from a structurally deformed granitic terrain near Hyderabad (India) was carried out to understand and evaluate the hydrogeochemical processes and quality of ...groundwater. Several trace elements (Fe, Mn, Be, Al, V, Cr, Co, Ni, Cu, Zn, As, Sr, Mo, Cd, Sb, Ba, Pb, U) along with major ions and minor elements were precisely estimated in shallow and drilled wells to know the suitability of water for drinking and irrigation purposes. Analytical data shows that pH and major ion chemistry in dug wells and bore wells do not vary significantly, while some trace elements (Fe, Mn, Al, Be, Co, Pb, U and Zn) vary in dug wells and bore wells, which can be attributed to differential mineral weathering and dissolution/precipitation reactions along fractures/joints. Although the water is not potable, it was found to be suitable for irrigation with little danger in the development of harmful level of exchangeable sodium. It is inferred that the chemical composition of the groundwater in this region is likely to have its origin from silicate weathering reactions and dissolution/precipitation processes supported by rainfall and groundwater flow.
Losartan: Comprehensive Profile Al-Majed, Abdul-Rahman A; Assiri, Ebrahim; Khalil, Nasr Y ...
Profiles of drug substances, excipients, and related methodology,
2015, Letnik:
40
Journal Article
Recenzirano
Losartan (Cozaar™) is an angiotensin II receptor antagonist with antihypertensive activity. It is used in the management of hypertension and heart failure. Nomenclature, formulae, elemental analysis, ...and appearance of the drug are included in this review. The uses, applications, and the variety of synthetic pathways of this drug are outlined. Physical characteristics including: ionization constant, solubility, X-ray powder diffraction pattern, thermal methods of analysis, UV spectrum, IR spectrum, mass spectrum with fragmentation patterns, and NMR (1H and 13C) spectra of losartan together with the corresponding figures and/or tables are all produced. This profile also includes the monograph of British Pharmacopoeia, together with several reported analytical methods including: spectrophotometric, electrochemical, chromatographic, and capillary electrophoretic methods. The stability, the pharmacokinetic behavior and the pharmacology of the drug are also provided.
A highly sensitive competitive enzyme immunoassay (EIA) has been developed and validated for the determination of the plasma level of 2′-deoxycytidine (dCyd), the potential prognostic marker for ...breast cancer chemotherapy. This assay employed a monoclonal antibody that recognizes dCyd with a high specificity, and 5′-succinyl-dCyd (5′sdCyd) conjugate of bovine serum albumin (5′sdCyd–BSA) immobilized onto microplate wells as a solid phase. The assay involved a competitive binding reaction between dCyd, in plasma sample, and the immobilized 5′sdCyd–BSA for the binding sites of the anti-dCyd antibody. The bound antibody was quantified with horseradish peroxidase-labeled anti-immunoglobulin second antibody and 3,3′,5,5′-tetramethylbenzidine as a peroxidase substrate. The concentration of dCyd in the sample was quantified by its ability to inhibit the binding of the antibody to the immobilized 5′sdCyd–BSA and subsequently the color formation in the assay. The assay limit of detection was 8
nM and the effective working range at relative standard deviations (R.S.D.s) of ≤10% was 20–800
nM. No cross-reactivity from the structurally related nucleobases, nucleosides, and nucleotides was observed in the proposed assay. Mean analytical recovery of added dCyd was 98–100
±
3.2–8.2%. The precision of the assay was satisfactory; R.S.D. was 3.4–4.2 and 4.3–8.9% for intra- and inter-assay precision, respectively. The proposed EIA was compared favorably with HPLC method in its ability to accurately measure dCyd spiked into plasma samples. The analytical procedure is convenient, and one can analyze 200 samples per working day, facilitating the processing of large-number batch of samples. The proposed EIA is expected to contribute in further evaluation of dCyd as a prognostic marker for breast cancer chemotherapy and elucidation of the role of dCyd in various biological and biochemical systems.
Dependence on antipsycotic drugs like aripriprazole (ARI) is increasing at alarming rate, hence, this study was undertaken to support the hypothesis that supplementation of Citrus paradisi ...(Grapefruit) juice having high concentration of polyphenols might potentiate and synergize the therapeutic effect of ARI, by increasing its bioavailability and inherent antioxidant potential. These benefits together might decrease the daily dosage of the ARI and thus alleviate the possible side effects of drug.
In this study the antioxidant and anti-inflammatory potential of ARI alone and in combination with GFJ was evaluated for hydrogen peroxide (H
O
) induced oxidative stress in mice. Seventy mice (4 weeks old), were randomly divided into seven groups. Group I: Control; Group II: H
O
treated; Group III; ARI treated; Group IV GFJ treated; Group V: GFJ and H
O
treated; Group VI; ARI and H
O
treated; Group VII; ARI, GFJ and H
O
treated. Serum levels of alanine aminotransferase (ALT), blood urea nitrogen (BUN), creatinine kinase (CK), creatinine and total protein were measured. Furthermore, pro-inflammatory cytokines Interleukin (IL)-1α, IL-2, IL-10 and tumor necrosis factor-α (TNF-α) concentrations were also measured.
The mice group that was treated with ARI, GFJ or combination of the two showed significant improvement in the H
O
altered parameters with the combination group showing more significant improvement than the ARI and GFJ alone groups indicating a synergistic and potentiating effect of the antioxidant and anti-inflammatory potential of GFJ on ARI.
Supplementing GFJ to ARI might increase an anti-oxidative potential of ARI due to inherent antioxidant and anti-inflammatory activity of GFJ and thus could alleviate the possible dosage dependent side effects of ARI.
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