- Application of a nano-structured molecularly imprinted polymer as an efficient modifier for the design of captopril drug selective sensor: Mechanism study and quantitative determination. [Journal Article]
- MSMater Sci Eng C Mater Biol Appl 2019 Jan 01; 94:879-885
- In the present study, electrochemical studies and potentiometric determination of captopril (CAP) drug were presented using a glassy carbon electrode (GCE) and carbon paste electrode (CPE), respectiv...
In the present study, electrochemical studies and potentiometric determination of captopril (CAP) drug were presented using a glassy carbon electrode (GCE) and carbon paste electrode (CPE), respectively; which is modified with a synthetic nano-structured molecularly imprinted polymer (MIP). CAP-MIP sample with an average particle size of 95 nm was synthesized using a precipitation polymerization method. The electrochemical behavior of CAP was studied on a MIP modified GCE, in an aqueous solution at pH 3.0. The electron transfer coefficient (α) was determined for the CAP drug, using electrochemical approaches. The prepared CAP-MIP was also used as a modifier in a CPE to design a selective CAP sensor, before its potentiometric determination. The modified CPE exhibits a good electrochemical response with a Nernstian slope of 59.15 ± 1.5 mV per decade over a wide linearity in the concentration range of 3.0 × 10-9-1.0 × 10-1 mol L-1. The cyclic voltammetry results were in good agreement with the electrochemical studies for the 1H+/1e- process. The designed electrode indicates a reasonable selectivity for CAP over other studied drugs such as ibuprofen, paracetamol, acyclovir, pyrazinamide, dimenhydrinate, and naproxen as well as with an excellent applicability in some pharmaceutical products.
- Treatment modalities for hip and knee osteoarthritis: A systematic review of safety. [Journal Article]
- JOJ Orthop Surg (Hong Kong) 2018 May-Aug; 26(3):2309499018808669
- Current guidelines on the management of hip and knee osteoarthritis (OA) do not compare safety of treatment modalities. We therefore systematically reviewed 20 studies investigating mortality and ser...
Current guidelines on the management of hip and knee osteoarthritis (OA) do not compare safety of treatment modalities. We therefore systematically reviewed 20 studies investigating mortality and serious complications of both medical and surgical treatments for hip and knee OA using PubMed, Scopus, Web of Knowledge and Google Scholar. Mortality was the highest for naproxen (hazard ratio (HR) = 3 (1.9, 4.6)) and lowest for total hip replacement (relative risk (RR) = 0.7 (0.7, 0.7)). Highest gastrointestinal complications were reported for diclofenac (odds ratio (OR) = 4.77 (3.94, 5.76)) and lowest for total knee replacement (HR = 0.6 (0.49, 0.75)). Ibuprofen had the highest renal complications (OR = 2.32 (1.45, 3.71)), whereas celecoxib had the highest cardiovascular risk (OR = 2.26 (1, 5.1)) and lowest was for tramadol (RR = 1.1 (0.87, 1.4)). Results show that medical management of hip and knee OA, particularly with non-steroidal anti-inflammatory drugs, may carry higher mortality compared to surgery. Careful consideration should be given to medical management taking into account known co-morbidities.
- Studying drug-drug interaction through chromatographic analysis of two mixtures offering antimicrobial synergism. [Journal Article]
- JCJ Chromatogr B Analyt Technol Biomed Life Sci 2018 Nov 03; 1104:1-10
- Micellar mobile phase was utilized for the separation and quantification of two antimicrobial mixtures with some analgesics that were found to augment their antimicrobial activity, namely; cefotaxime...
Micellar mobile phase was utilized for the separation and quantification of two antimicrobial mixtures with some analgesics that were found to augment their antimicrobial activity, namely; cefotaxime sodium (CFX) with ibuprofen (IBU) and naproxen (NPX) (mixture Ι), and azithromycin dihydrate (AZT) with diclofenac sodium (DIC) (mixture ΙΙ). Both mixtures were analyzed using a C18 column operated at 50 °C using a mobile phase composed of sodium dodecyl sulphate (SDS), an organic modifier; (1-propanol or acetonitrile), and 0.3% triethylamine (TEA), adjusting pH to the required value with 2 M orthro-phosphoric acid, accompanied with UV detection. The proposed method was subjected to full validation procedure and was applied to determine the concentration of the studied antibiotics in homogenized liver, kidney and heart rat tissue samples, with or without the co-administered non steroidal anti-inflammatory drugs.
- Sunburn Recall Reaction and Mucositis Secondary to Methotrexate Toxicity. [Journal Article]
- SSkinmed 2018; 16(5):340-341
- A 59-year-old Native American female presented with a 4-day history of malaise, abdominal pain, nausea, jaundice, and a "sunburn-like rash" on the upper chest and back despite lack of recent sun expo...
A 59-year-old Native American female presented with a 4-day history of malaise, abdominal pain, nausea, jaundice, and a "sunburn-like rash" on the upper chest and back despite lack of recent sun exposure (Figure 1). Medical history was significant for a twenty-year history of universal vitiligo and a five-year history of rheumatoid arthritis (RA) treated with methotrexate (MTX), adalimumab, prednisone, and naproxen sodium. Cutaneous examination revealed hemorrhagic crusting of upper and lower lips (Figure 2), scleral icterus, diffuse jaundice of the skin, and well-demarcated erythematous patches on mid-upper back and anterior neck. The patient had a few scattered erythematous papules with whitish center on bilateral extensor surfaces of the upper extremities and scattered petechiae on both the trunk and upper extremities.
- Expanding the applicability of cork as extraction phase for disposable pipette extraction in multiresidue analysis of pharmaceuticals in urine samples. [Journal Article]
- JCJ Chromatogr B Analyt Technol Biomed Life Sci 2018 Dec 01; 1102-1103:159-166
- In this paper, cork is proposed as a natural and renewable material for the extraction phase in disposable pipette extraction to be applied in the multiresidue determination of pharmaceuticals in hum...
In this paper, cork is proposed as a natural and renewable material for the extraction phase in disposable pipette extraction to be applied in the multiresidue determination of pharmaceuticals in human urine by HPLC with diode array detection. The compounds carbamazepine, losartan, ketoprofen, 17‑β‑estradiol, naproxen, diazepam, 17‑α‑ethinylestradiol, estrone, diclofenac and ibuprofen were studied. A known amount (5 mg) of cork, with a size of 200 mesh, was inserted into a pipette tip. The method optimization was carried out with univariate and multivariate approaches. The optimized conditions were sample pH adjusted to 3, urine dilution factor of 40 (158 μL of urine diluted in 6.142 mL of ultrapure water), 9 extraction cycles each performed with 700 μL of sample, and extraction time of 10 s per cycle. Desorption was performed with 85 μL of methanol applying 6 cycles of 10 s each using the same solvent aliquot. For the clean-up step, 4 cycles were carried out each with 200 μL of methanol. The limits of quantification varied from 5 to 10 μg L-1 with determination coefficients higher than 0.9919 for the calibration curves for all the analytes. Intra-day and inter-day precision and relative recovery from urine samples donated by two volunteers were assessed based on three spiked concentrations. The analyte relative recoveries ranged from 65 to 117% (n = 3) for the two samples. Intra-day precision ranged from 1.2 to 17% (n = 3) and inter-day precision varied from 11 to 21% (n = 9).
- New benzimidazothiazole derivatives as anti-inflammatory, antitumor active agents: Synthesis, in-vitro and in-vivo screening and molecular modeling studies. [Journal Article]
- BCBioorg Chem 2018 Oct 24; 83:250-261
- A new series of benzimidazothiazole derivatives has been synthesized. The structure of the products was confirmed by spectroscopic techniques such as IR, NMR and mass spectroscopy. The tested compoun...
A new series of benzimidazothiazole derivatives has been synthesized. The structure of the products was confirmed by spectroscopic techniques such as IR, NMR and mass spectroscopy. The tested compounds were evaluated for their anti-inflammatory activity either in vitro through the COX enzyme inhibition assay, or in vivo through carrageenan paw edema technique. Results revealed that compound 25 and 29 represented the most active ones among the entire series with % inhibition 72.19, 72.07 for COX-1, and 87.46, 87.38 for COX-2, respectively. Interestingly, all synthesized compounds exhibited IC50 values less than both reference drugs celecoxib and naproxen, indicating their superior potency. For compound 25, it showed about 340 and 198 times more potent than celecoxib and naproxen respectively as COX-1 inhibitor (IC50 value 0.044 vs. 15.000 and 8.700 µM), and 10 and 115 times more potent than the same drugs as COX-2 inhibitor (IC50 value 4.52 vs. 40.00 and 520.00 nM). The antitumor activity of the products was also evaluated and the results obtained are consistent with those obtained by the anti-inflammatory screening where compounds 25 and 29 proved to be the most active ones among the other compounds with %GI ranging from 31.5 to 62.5% and they exhibited the lowest IC50 values as well. The ADMET analysis of the tested compounds was also performed in addition to the molecular modeling studies that included flexible alignment, surface and electrostatic maps in addition to the Lipinisk's rule of five.
- Risk of acute myocardial infarction during use of individual NSAIDs: A nested case-control study from the SOS project. [Journal Article]
- PlosPLoS One 2018; 13(11):e0204746
- CONCLUSIONS: The relative risk estimates of AMI differed slightly between 28 individual NSAIDs. The relative risk was highest for ketorolac and was correlated with COX-2 potency, but not restricted to coxibs.
- Uptake and accumulation of emerging contaminants in soil and plant treated with wastewater under real-world environmental conditions in the Al Hayer area (Saudi Arabia). [Journal Article]
- STSci Total Environ 2018 Oct 17; 652:562-572
- In arid and semi-arid areas the use of treated wastewater for crop irrigation and other agricultural practices, such as the use of pesticides, increase the number of emerging contaminants (ECs) in cr...
In arid and semi-arid areas the use of treated wastewater for crop irrigation and other agricultural practices, such as the use of pesticides, increase the number of emerging contaminants (ECs) in crops. Hazards of these practices to human being are largely unknown since there are few studies yet covering a short range of compounds and most of them under non-realistic conditions. This study aims at assessing this problem that will become global soon in an area of Saudi Arabia heavily affected by the reuse of treated wastewater and pesticide in order to ascertain its scale. The novelty of the study relays in the large number of ECs covered and the variety of crops (cabbage, barley, green beans, eggplants, chili, tomato and zucchini) analysed. Extraction procedure developed provided an appropriate extraction yield (up to 50% of the compounds were recovered within a 70-120% range), with good repeatability (relative standard deviations below 20% in most cases) and sensitivity (LOQ < 25 ng g-1) for the model compounds. Determination by liquid chromatography quadrupole time-of-flight (LC-QqTOF-MS) is able to identify >2000 contaminants. Sixty-four ECs were identified in wastewater but of the sixty-four compounds, six pharmaceuticals (atenolol, caffeine, carbamazepine and its metabolites 10,11-epoxycarbamazepine, gemfibrozil, and naproxen) and seven pesticides (acetamiprid, atrazine deethyl, azoxystrobin, bupirimate, diazinon, malathion, pirimicarb and some of their metabolites) were detected in plants. Furhermore, one metabolite of the ibuprofen (not detected in water or soil), the ibuprofen hexoside was also found in plants. Up to our knowledge, this study demonstrate for the first time the accumulation of ECs in crops irrigated with treated wastewater under real non-controlled environmental conditions.
- Naproxen ecotoxicity and biodegradation by Bacillus thuringiensis B1(2015b) strain. [Journal Article]
- EEEcotoxicol Environ Saf 2019 Jan 15; 167:505-512
- High level of naproxen consumption leads to the appearance of this drug in the environment but its possible effects on non-target organisms together with its biodegradation are not well studied. The ...
High level of naproxen consumption leads to the appearance of this drug in the environment but its possible effects on non-target organisms together with its biodegradation are not well studied. The aim of this work was to evaluate naproxen ecotoxicity by using the Microbial Assay for Risk Assessment. Moreover, Bacillus thuringiensis B1(2015b) was tested for both ecotoxicity and the ability of this strain to degrade naproxen in cometabolic conditions. The results indicate that the mean value of microbial toxic concentration estimated by MARA test amounts to 1.66 g/L whereas EC50 of naproxen for B1(2015b) strain was 4.69 g/L. At toxic concentration, Bacillus thuringiensis B1(2015b) showed 16:0 iso 3OH fatty acid presence and an increase in the ratio of total saturated to unsaturated fatty acids. High resistance of the examined strain to naproxen correlated with its ability to degrade this drug in cometabolic conditions. The results of bacterial reverse mutation assay (Ames test) revealed that naproxen at concentrations above 1 g/L showed genotoxic effect but the response was not dose-dependent. Maximal specific naproxen removal rate was observed at pH 6.5 and 30 °C, and in the presence of 0.5 g/L glucose as a growth substrate. Kinetic analysis allowed estimation of the half saturation constant (Ks) and the maximum specific naproxen removal rate (qmax) as 6.86 mg/L and 1.26 mg/L day, respectively. These results indicate that Bacillus thuringiensis B1(2015b) has a high ability to degrade naproxen and is a potential tool for bioremediation.
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- Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective. [Review]
- EJEur J Med Chem 2019 Jan 01; 161:252-276
- Naphthalene, a cytotoxic moiety, is an extensively explored aromatic conjugated system with applications in various pathophysiological conditions viz. anticancer, antimicrobial, anti-inflammatory, an...
Naphthalene, a cytotoxic moiety, is an extensively explored aromatic conjugated system with applications in various pathophysiological conditions viz. anticancer, antimicrobial, anti-inflammatory, antiviral, antitubercular, antihypertensive, antidiabetic, anti-neurodegenerative, antipsychotic, anticonvulsant, antidepressant. Naphthalene epoxides and naphthoquinones are most reactive metabolites of naphthalene and are responsible for the covalent interaction with cysteine amino acid of cellular proteins for cytotoxic nature. Many naphthalene derived bioactive phytoconstituents are present in nature including podophyllotoxins (Etoposide, teniposide), bis-ANS 82, Rifampicin, Justiprocumin A, B, Patentiflorin A. The naphthalene-based molecules, viz. Naphyrone, tolnaftate, naftifine, nafcillin, terbinafine, propranolol, nabumetone, nafimidone, naproxen, duloxetine, lasofoxifene, bedaquiline etc. have also been approved by FDA and are being marketed as therapeutics. Thus, the naphthalene scaffold emerges as an important building block in drug discovery owing to its broad spectrum of biological activities through varying structural modifications. This review incorporates the pharmacological aspects of different types of chemically modified naphthalene-based molecules along with their activity profile. This compiled information may serve as a benchmark for the alteration of existing ligands to design novel potent molecules with lesser side effects.