Publications by authors named "M Arif A Aziz"

1,749 Publications

  • Page 1 of 1

3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I & TOP II isomerases inhibitors.

Bioorg Chem 2021 Feb 15;110:104698. Epub 2021 Feb 15.

Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, New Minia, Minia, Egypt. Electronic address:

We report herein design and synthesis of a new series of 3,7-bis-benzylidenes of ciprofloxacin. Most of the target compounds revealed good cytotoxic activity; the most potent 4e and 4i achieved strong broad spectrum antiproliferative activity with comparable activity to Doxorubicin with IC (M) of 1.21 ± 0.02, 0.87 ± 0.04, 1.21 ± 0.02; 0.41 ± 0.02, 0.57 ± 0.06, 1.31 ± 0.04 and 1.26 ± 0.01, 1.79 ± 0.04, 0.63 ± 0.01 against leukemia cancer cell line HL-60 (TB), colon cancer cell line HCT-116 and breast cancer cell line MCF7, respectively. Moreover, the most potent derivative 4i induced apoptosis at G2/M phase Investigating the mechanism of action of compounds 4e, 4 h and 4i exhibited promising dual TOP Iα and TOP IIB % inhibition comparable to Camptothecin and Etoposide; respectively. Docking of 4e, 4 h and 4i into the active site of topo I and II proteins compared to Camptothein and Etoposide revealed acceptable binding score and augmented enzyme assay data. Hence, 4e and 4i are promising targeted antiproliferative dual acting TOP Iα TOP IIB inhibitors that require further optimization.
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http://dx.doi.org/10.1016/j.bioorg.2021.104698DOI Listing
February 2021

Acute biliary pancreatitis has better outcomes but increased resource utilization compared to acute alcohol-induced pancreatitis: insights from a nationwide study.

Ann Gastroenterol 2021 7;34(2):253-261. Epub 2020 Dec 7.

Department of Gastroenterology, University of Utah, Salt Lake City, UT (Douglas G. Adler), USA.

Background: The differences in outcomes between acute biliary pancreatitis (ABP) and acute alcohol-induced pancreatitis (AAP) have not been well studied. We sought to examine the differences between ABP and AAP as regards to in-hospital outcomes and resource utilization, using a large nationwide database.

Methods: We queried the National Inpatient Sample databases 2016 and 2017 using the International Classification of Diseases, 10th revision, Clinical Modification (ICD-10-CM) coding system to identify the patients with a primary diagnosis of AAP and ABP. The primary outcome was all-cause in-hospital mortality. Secondary outcomes were hospital length of stay (LOS), hospitalization charge/cost, shock, acute kidney injury (AKI), intensive care unit (ICU) admission, and home discharge. Analysis was performed with STATA software.

Results: There was no significant difference in mortality between patients with AAP and ABP (0.42% vs. 0.82%, adjusted odds ratio [aOR] 0.95, 95% confidence interval [CI] 0.69-1.31; P=0.79). Patients with ABP had a significantly longer LOS (+0.48 days, P<0.001). Patients with ABP had significantly higher adjusted mean hospitalization charges ($+19,958, P<0.001) and costs ($+4,848, P<0.001). Patients with ABP had a significantly lower likelihood of shock (aOR 0.75, 95%CI 0.59-0.95; P=0.02), AKI (aOR 0.76, 95%CI 0.71-0.82; P<0.001) or ICU admission (aOR 0.74, 95%CI 0.62-0.88; P=0.001). They were more likely to be discharged home (aOR 1.26, 95%CI 1.18-1.34; P<0.001).

Conclusion: Although there was no difference in all-cause mortality, patients with ABP had better hospitalization outcomes but greater resource utilization.
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http://dx.doi.org/10.20524/aog.2020.0559DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7903563PMC
December 2020

Cytotoxicity and Apoptosis Effects of Curcumin Analogue (2E,6E)-2,6-Bis(2,3-Dimethoxybenzylidine) Cyclohexanone (DMCH) on Human Colon Cancer Cells HT29 and SW620 In Vitro.

Molecules 2021 Feb 26;26(5). Epub 2021 Feb 26.

Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, University Putra Malaysia, UPM, Serdang 43400, Selangor, Malaysia.

Colorectal cancer (CRC) is the third most common type of cancer worldwide and a leading cause of cancer death. According to the Malaysian National Cancer Registry Report 2012-2016, colorectal cancer was the second most common cancer in Malaysia after breast cancer. Recent treatments for colon cancer cases have caused side effects and recurrence in patients. One of the alternative ways to fight cancer is by using natural products. Curcumin is a compound of the rhizomes of that possesses a broad range of pharmacological activities. Curcumin has been studied for decades but due to its low bioavailability, its usage as a therapeutic agent has been compromised. This has led to the development of a chemically synthesized curcuminoid analogue, (2E,6E)-2,6-bis(2,3-dimethoxybenzylidine) cyclohexanone (DMCH), to overcome the drawbacks. This study aims to examine the potential of DMCH for cytotoxicity, apoptosis induction, and activation of apoptosis-related proteins on the colon cancer cell lines HT29 and SW620. The cytotoxic activity of DMCH was evaluated using the [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) cell viability assay on both of the cell lines, HT29 and SW620. To determine the mode of cell death, an acridine orange/propidium iodide (AO/PI) assay was conducted, followed by Annexin V/FITC, cell cycle analysis, and JC-1 assay using a flow cytometer. A proteome profiler angiogenesis assay was conducted to determine the protein expression. The inhibitory concentration (IC) of DMCH in SW620 and HT29 was 7.50 ± 1.19 and 9.80 ± 0.55 µg/mL, respectively. The treated cells displayed morphological features characteristic of apoptosis. The flow cytometry analysis confirmed that DMCH induced apoptosis as shown by an increase in the sub-G0/G1 population and an increase in the early apoptosis and late apoptosis populations compared with untreated cells. A higher number of apoptotic cells were observed on treated SW620 cells as compared to HT29 cells. Human apoptosis proteome profiler analysis revealed upregulation of Bax and Bad proteins and downregulation of Livin proteins in both the HT29 and SW620 cell lines. Collectively, DMCH induced cell death via apoptosis, and the effect was more pronounced on SW620 metastatic colon cancer cells, suggesting its potential effects as an antimetastatic agent targeting colon cancer cells.
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http://dx.doi.org/10.3390/molecules26051261DOI Listing
February 2021

Iodide promotes bisphenol A (BPA) halogenation during chlorination: Evidence from 30 X-BPAs (X = Cl, Br, and I).

J Hazard Mater 2021 Feb 20;414:125461. Epub 2021 Feb 20.

School of Environmental Science and Engineering, Tianjin University, Tianjin 300072, China. Electronic address:

As a well known endocrine-disrupting and model chemical, bisphenol A (BPA) may pose a serious threat to human health, since it and its disinfection by-products (DBPs) have been detected in drinking water, urine, human colostrum, adipose tissue, and placenta samples. Although chlorinated BPAs (Cl-BPAs) and iodinated BPAs (I-BPAs) have been well studied, brominated BPAs (Br-BPAs), and mixed halogenated DBPs like bromo-iodo-BPAs (Br-I-BPAs), and bromo-chloro-iodo-BPAs (Cl-Br-I-BPAs) are less well understood. Notably, the role of iodide (I) during chlorination is not well understood, since the studies of the I-DBPs mainly focus on their genotoxicity and cytotoxicity. To understand the formation mechanisms of halogenated bisphenol A (HBPs) during chlorination with bromide (Br) and/or I, and the role of I during chlorination, three set of reactions were performed in the laboratory ("BPA + chlorine + Br", "BPA + chlorine + I" and "BPA + chlorine + Br +I" assigned as group A, B and C respectively). Thirty HBPs were identified and 18 of them were never reported before. I increases the transformation rate of BPA into HBPs as I-BPAs act as intermediate HBPs during chlorination that easily react with HClO/ClO and HBrO/BrO to form Cl-BPAs and Br-BPAs. HIO/IO showed higher reactivity towards BPA and HBPs than that of HBrO/BrO and HClO/ClO. The recycling of I was observed in the reactions of "BPA + chlorine + I" and "BPA + chlorine + Br +I", which may explain why I can induce BPA to transform into HBPs and suggests that I may act as a catalyst during the BPA chlorination reactions. The reaction pathways are proposed which present the reactions of BPA and HBPs with HClO/ClO, HBrO/BrO, and HIO/IO, as well as the recycling of I. This study describes the potential DBP formation and transformation mechanisms of BPA and its 16 alternatives, as well as the role of I on the transformation of phenol compounds during chlorination.
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http://dx.doi.org/10.1016/j.jhazmat.2021.125461DOI Listing
February 2021

Green carbonaceous material‒fibrous silica-titania composite photocatalysts for enhanced degradation of toxic 2-chlorophenol.

J Hazard Mater 2021 Feb 24;414:125524. Epub 2021 Feb 24.

School of Chemical and Energy Engineering, Faculty of Engineering, Universiti Teknologi Malaysia, 81310 UTM Johor Bahru, Johor, Malaysia; Centre of Hydrogen Energy, Institute of Future Energy, 81310 UTM Johor Bahru, Johor, Malaysia.

In this work, fibrous silica-titania (FST) was successfully prepared by the microemulsion method prior to the addition of three types of carbonaceous materials: graphitic-carbon nitride, g-C3N4 (CN), graphene nanoplatelets (GN), and multi-wall carbon nanotubes, MWCNT (CNT), via a solid-state microwave irradiation technique. The catalysts were characterized using XRD, FESEM, TEM, FTIR, UV-Vis DRS, N2 adsorption-desorption, XPS and ESR, while their photoactivity was examined on the degradation of toxic 2-chlorophenol (2-CP). The result demonstrated that the initial reaction rate was in the following order: CNFST (5.1 × 10 mM min) > GNFST (2.5 × 10 mM min) > CNTFST (2.3 × 10 mM min). The best performance was due to the polymeric structure of g-C3N4 with a good dispersion of C and N on the surface FST. This dispersion contributed towards an appropriate quantity of defect sites, as a consequence of the greater interaction between g-C3N4 and the FST support, that led to narrowed of band gap energy (2.98 eV to 2.10 eV). The effect of scavenger and ESR studies confirmed that the photodegradation over CNFST occurred via a Z-scheme mechanism. It is noteworthy that the addition of green carbonaceous materials on the FST markedly enhanced the photodegradation of toxic 2-CP.
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http://dx.doi.org/10.1016/j.jhazmat.2021.125524DOI Listing
February 2021

Enhancing the performance of micro-biosensors by functionally graded geometrical and material parameters.

Arch Appl Mech 2021 Feb 20:1-15. Epub 2021 Feb 20.

Faculty of Engineering, Helwan University, P.O. Box 11718, Mataria, Cairo, Egypt.

Most recently, the whole world is struggling against the virulent pandemic COVID-19. Due to the unbounded global spread of the disease, having biosensors with high performance such as high sensitivity and accuracy is of utmost importance. In this paper, the effects of various parameters on the behaviors of micro-biosensors are investigated in order to enhance their performance. These parameters are related to the geometry and material, and they are assumed to be gradually changing in the longitudinal direction of the biosensor according to a power law. Therefore, they are called functionally graded geometrical and material parameters. Another aspect is when considering microcantilever-based biosensors, the main behavior parameter is the deflection at the free end. In the analyses, the influences of the surface stress and van der Waals intermolecular forces are taken into account. Also, the total energy of the beam, which is the combination of the van der Waals energy and the elastic strain energy, is accomplished. In addition, the equivalent force causing the deflection is also evaluated using Castigliano method for two cases. These cases account for a concentrated force at the free end and a distributed load along the biosensor, respectively. Since the governing equations account for the size dependency and the considered parameters are functions of the position, the solution is too complex to be achieved analytically, and therefore, numerical methods are applied. For uniform biosensors made of homogeneous materials, or in other words when all parameters are not varying with the position, the obtained results are compared with those in the literature, and good agreement is obtained. On the other hand, the performance, which include sensitivity and limit of detection, of functionally graded biosensors can be enhanced by proper choices of the considered parameters and the corresponding exponent of the gradation function.
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http://dx.doi.org/10.1007/s00419-021-01900-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7895744PMC
February 2021

A Lower Tidal Volume Regimen during One-lung Ventilation for Lung Resection Surgery Is Not Associated with Reduced Postoperative Pulmonary Complications.

Anesthesiology 2021 Feb 26. Epub 2021 Feb 26.

Background: Protective ventilation may improve outcomes after major surgery. However, in the context of one-lung ventilation, such a strategy is incompletely defined. The authors hypothesized that a putative one-lung protective ventilation regimen would be independently associated with decreased odds of pulmonary complications after thoracic surgery.

Methods: The authors merged Society of Thoracic Surgeons Database and Multicenter Perioperative Outcomes Group intraoperative data for lung resection procedures using one-lung ventilation across five institutions from 2012 to 2016. They defined one-lung protective ventilation as the combination of both median tidal volume 5 ml/kg or lower predicted body weight and positive end-expiratory pressure 5 cm H2O or greater. The primary outcome was a composite of 30-day major postoperative pulmonary complications.

Results: A total of 3,232 cases were available for analysis. Tidal volumes decreased modestly during the study period (6.7 to 6.0 ml/kg; P < 0.001), and positive end-expiratory pressure increased from 4 to 5 cm H2O (P < 0.001). Despite increasing adoption of a "protective ventilation" strategy (5.7% in 2012 vs. 17.9% in 2016), the prevalence of pulmonary complications did not change significantly (11.4 to 15.7%; P = 0.147). In a propensity score matched cohort (381 matched pairs), protective ventilation (mean tidal volume 6.4 vs. 4.4 ml/kg) was not associated with a reduction in pulmonary complications (adjusted odds ratio, 0.86; 95% CI, 0.56 to 1.32). In an unmatched cohort, the authors were unable to define a specific alternative combination of positive end-expiratory pressure and tidal volume that was associated with decreased risk of pulmonary complications.

Conclusions: In this multicenter retrospective observational analysis of patients undergoing one-lung ventilation during thoracic surgery, the authors did not detect an independent association between a low tidal volume lung-protective ventilation regimen and a composite of postoperative pulmonary complications.

Editor’s Perspective:
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http://dx.doi.org/10.1097/ALN.0000000000003729DOI Listing
February 2021

Tocilizumab in Hospitalized Patients with Severe Covid-19 Pneumonia.

N Engl J Med 2021 Feb 25. Epub 2021 Feb 25.

From Baylor College of Medicine, Houston (I.O.R.); James J. Peters Veterans Affairs Medical Center, Bronx, and Icahn School of Medicine at Mount Sinai, New York - both in New York (N.B.); eStudy Site, Chula Vista (M.W.), Genentech, South San Francisco (M.B., L.T.), and the University of California, San Diego, La Jolla (A.M.) - all in California; Hackensack Meridian School of Medicine and Hacksensack University Medical Center, Hackensack, NJ (R.C.G.); Intermountain Healthcare, Salt Lake City (B.D.H.); Royal Free Hospital (S.B.) and Imperial College London (N.C., T.Y.), London, Leeds Teaching Hospitals NHS Trust and National Institute for Health Research-Leeds Biomedical Research Centre, Leeds (S.S.), North Manchester General Hospital, Manchester (A.U.), and Roche Products, Welwyn Garden City (S.D., E.G., B.M., H.S.) - all in the United Kingdom; the University of Massachusetts Medical School-Baystate, Springfield (D.S.); Rush University Medical Center, Chicago (M.S.A.); Denver Health Medical Center, Denver (I.S.D.), and the University of Colorado, Anschutz School of Medicine, Aurora (I.S.D.); University Health Network, Toronto (L.D.S.); Hospital Universitario HM Sanchinarro, Centro Integral, Oncológico Clara Campal and Departamento de Ciencias Médicas Clínicas, Facultad de Medicina, Universidad CEU San Pablo, Madrid (A.C.G.); and the University of Miami Miller School of Medicine, Miami (D.J.D.L.Z.).

Background: Coronavirus disease 2019 (Covid-19) is associated with immune dysregulation and hyperinflammation, including elevated interleukin-6 levels. The use of tocilizumab, a monoclonal antibody against the interleukin-6 receptor, has resulted in better outcomes in patients with severe Covid-19 pneumonia in case reports and retrospective observational cohort studies. Data are needed from randomized, placebo-controlled trials.

Methods: In this phase 3 trial, we randomly assigned patients who were hospitalized with severe Covid-19 pneumonia in a 2:1 ratio receive a single intravenous infusion of tocilizumab (at a dose of 8 mg per kilogram of body weight) or placebo. Approximately one quarter of the participants received a second dose of tocilizumab or placebo 8 to 24 hours after the first dose. The primary outcome was clinical status at day 28 on an ordinal scale ranging from 1 (discharged or ready for discharge) to 7 (death) in the modified intention-to-treat population, which included all the patients who had received at least one dose of tocilizumab or placebo.

Results: Of the 452 patients who underwent randomization, 438 (294 in the tocilizumab group and 144 in the placebo group) were included in the primary and secondary analyses. The median value for clinical status on the ordinal scale at day 28 was 1.0 (95% confidence interval [CI], 1.0 to 1.0) in the tocilizumab group and 2.0 (non-ICU hospitalization without supplemental oxygen) (95% CI, 1.0 to 4.0) in the placebo group (between-group difference, -1.0; 95% CI, -2.5 to 0; P = 0.31 by the van Elteren test). In the safety population, serious adverse events occurred in 103 of 295 patients (34.9%) in the tocilizumab group and in 55 of 143 patients (38.5%) in the placebo group. Mortality at day 28 was 19.7% in the tocilizumab group and 19.4% in the placebo group (weighted difference, 0.3 percentage points (95% CI, -7.6 to 8.2; nominal P = 0.94).

Conclusions: In this randomized trial involving hospitalized patients with severe Covid-19 pneumonia, the use of tocilizumab did not result in significantly better clinical status or lower mortality than placebo at 28 days. (Funded by F. Hoffmann-La Roche and the Department of Health and Human Services; COVACTA ClinicalTrials.gov number, NCT04320615.).
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http://dx.doi.org/10.1056/NEJMoa2028700DOI Listing
February 2021

An exceptionally giant left atrial myxoma: a case report and literature review.

Eur Heart J Case Rep 2020 Dec 13;4(6):1-7. Epub 2020 Dec 13.

Cardiac Center Sharjah, Al-Qassimi Hospital, Ministry of Health and Prevention (MOHAP), Sharjah, United Arab Emirates.

Background: Cardiac myxomas are considered the most common benign heart tumours. The clinical manifestations mainly depend on the size of the tumour. They usually vary from asymptomatic, mild non-specific symptoms, to severe obstructive cardiac and systemic findings. We describe herein a significantly large left atrial myxoma in a patient misdiagnosed with respiratory asthma.

Case Summary: A 54-year-old lady, was diagnosed previously with asthma, presented with a history of dyspnoea on exertion, palpitations, and mild peripheral oedema. Chest X-ray suggested pulmonary congestion. Due to high suspicion of cardiac issues, transthoracic echocardiography was done revealing giant left atrial mass. Consequently, the mass was approached and excised surgically through the inverted T biatrial incision. Grossly, the mass measured 10 × 8 × 6 cm, and it had a smooth surface and was filled with gelatinous material. The histopathology confirmed benign myxoma without malignant features.

Discussion: Our article mainly focuses on the diagnostic challenges of a patient with atrial myxoma. The major discrepancy between the tumour size and the severity of the patient's symptoms should draw physicians' attention to consider atrial myxoma over a long list of differentials, in order to take immediate action to reduce the mortality and improve the overall prognosis.
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http://dx.doi.org/10.1093/ehjcr/ytaa401DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7891267PMC
December 2020

Transmission of Antimicrobial-Resistant Staphylococcus aureus Clonal Complex 9 between Pigs and Humans, United States.

Emerg Infect Dis 2021 Mar;27(3):740-748

Transmission of livestock-associated Staphylococcus aureus clonal complex 9 (LA-SA CC9) between pigs raised on industrial hog operations (IHOs) and humans in the United States is poorly understood. We analyzed whole-genome sequences from 32 international S. aureus CC9 isolates and 49 LA-SA CC9 isolates from IHO pigs and humans who work on or live near IHOs in 10 pig-producing counties in North Carolina, USA. Bioinformatic analysis of sequence data from the 81 isolates demonstrated 3 major LA-SA CC9 clades. North Carolina isolates all fell within a single clade (C3). High-resolution phylogenetic analysis of C3 revealed 2 subclades of intermingled IHO pig and human isolates differing by 0-34 single-nucleotide polymorphisms. Our findings suggest that LA-SA CC9 from pigs and humans share a common source and provide evidence of transmission of antimicrobial-resistant LA-SA CC9 between IHO pigs and humans who work on or live near IHOs in North Carolina.
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http://dx.doi.org/10.3201/eid2703.191775DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7920674PMC
March 2021

A High-Performance Asymmetric Supercapacitor Based on Tungsten Oxide Nanoplates and Highly Reduced Graphene Oxide Electrodes.

Chemistry 2021 Feb 20. Epub 2021 Feb 20.

Johannes Gutenberg University: Johannes Gutenberg Universitat Mainz, Chemistry, GERMANY.

Tungsten oxide/graphene hybrid-materials are attractive semiconductors for energy-related applications. Herein, we report an asymmetric supercapacitor (ASC, HRG//m-WO 3 ASC), fabricated from monoclinic tungsten oxide (m-WO 3 ) nanoplates as a negative-electrode and highly reduced graphene oxide (HRG) as a positive-electrode material. The supercapacitor performance of the prepared electrodes was evaluated in an aqueous-electrolyte (1M H 2 SO 4 ) using three- and two- electrode systems. The HRG//m-WO 3 ASC exhibits a maximum specific capacitance of 389 F/g at a current density of 0.5 A/g, with an associated high energy density of 93 Wh/kg at a power density of 500 W/kg in a wide 1.6 V operating potential window. In addition, the HRG//m-WO 3 ASC displays long-term cycling-stability, maintaining ~92% of the original specific capacitance after 5000 galvanostatic charge-discharge cycles. The m-WO 3 nanoplates were prepared hydrothermally while HRG was synthesized by a modified Hummers method.
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http://dx.doi.org/10.1002/chem.202005156DOI Listing
February 2021

Following ISAPS Recommendations, Does it Really Help?

Aesthetic Plast Surg 2021 Feb 17. Epub 2021 Feb 17.

Plastic & Reconstructive Surgery Department, Ain Shams University, Cairo, Egypt.

Background: The demand for abdominoplasty procedures has increased in surgical centres as a result of patient preference and economic concerns. The International Society of Aesthetic Plastic Surgery (ISAPS) published the Facility Accreditation Guideline on 22 October 2018. It is a list of recommendations that aim to reduce the incidence of complications and increase safety standards.

Objectives: The objective of this work was to detect the effects of the ISAPS guidelines on the morbidity associated with abdominoplasty procedures in day care surgical centres.

Methods: The authors performed a retrospective study. Data regarding complications of abdominoplasty were collected from medical records of the last 350 cases of abdominoplasty performed in December 2018. The complications and their incidences were compared with similar previously published data of abdominoplasty operations performed by other authors and in surgical centres before initiation of the ISAPS Facility Accreditation Guideline.

Results: In all cases, we achieved a significant reduction in skin and adipose tissue with improvement in body shape. The incidence of major and minor post-operative complications was lower than that reported in other literature.

Conclusions: This report shows that abdominoplasty is a safe procedure with low complication rates, which are even lower when the ISAPS Facility Accreditation Guideline is followed together with national, regional, state and other legal requirements.

Level Of Evidence Iv: This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266 .
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http://dx.doi.org/10.1007/s00266-021-02174-xDOI Listing
February 2021

Cost-effectiveness of pertuzumab and trastuzumab biosimilar combination therapy as initial treatment for HER2-positive metastatic breast cancer in Singapore.

Expert Rev Pharmacoecon Outcomes Res 2021 Feb 17:1-8. Epub 2021 Feb 17.

Agency for Care Effectiveness (ACE), Ministry of Health , Singapore.

Background: This study evaluates the cost-effectiveness of pertuzumab with trastuzumab biosimilar and docetaxel as initial treatment for HER2-positive metastatic breast cancer (MBC) in Singapore.

Methods: A partitioned survival model with three health states was developed to evaluate the cost-effectiveness of trastuzumab biosimilar and docetaxel with or without pertuzumab from a healthcare system perspective over a 15-year time horizon for patients with HER2-positive MBC. Key clinical inputs were derived from the CLEOPATRA trial. Health state utilities were derived from the literature and direct medical costs were obtained from local public healthcare institutions.

Results: The base-case resulted in an incremental cost-effectiveness ratio (ICER) of SGD366,658 (USD272,244) per quality-adjusted life-year (QALY) gained. One-way sensitivity analyses showed that the ICER was sensitive to utilities in the progression-free state, price of pertuzumab and time horizon. When the price for trastuzumab reference biologic (branded) was applied, the ICER was even higher (SGD426,996 [USD317,045]/QALY).

Conclusion: Although trastuzumab biosimilar reduced the cost of the pertuzumab combination regimen, the ICER remained high and was not cost effective in Singapore's context. As pertuzumab contributed 80% of the overall combination treatment cost, price reductions for pertuzumab will be required to improve the cost-effectiveness of combination treatment to an acceptable level.
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http://dx.doi.org/10.1080/14737167.2021.1880323DOI Listing
February 2021

Cost-effectiveness of olaparib maintenance therapy when used with and without restriction by BRCA1/2 mutation status for platinum-sensitive relapsed ovarian cancer.

Expert Rev Pharmacoecon Outcomes Res 2021 Feb 16. Epub 2021 Feb 16.

Agency for Care Effectiveness, Ministry of Health , Singapore.

Objectives: To determine whether olaparib maintenance therapy, used with and without restriction by mutation status, is cost-effective at the population level for platinum-sensitive relapsed ovarian cancer in Singapore.

Methods: : A partitioned survival model compared three management strategies: 1) treat all patients with olaparib; 2) test for germline mutation, followed by targeted olaparib use in mutation carriers only; 3) observe all patients. Mature overall survival (OS) data from Study 19 and a 15-year time horizon were used and direct medical costs were applied. Sensitivity analyses were conducted to explore uncertainties.

Results: : Treating all patients with olaparib was the most costly and effective strategy, followed by targeted olaparib use, and observation of all patients. Base-case incremental cost-effectiveness ratios (ICERs) for all-olaparib and targeted use strategies were SGD133,394 (USD100,926) and SGD115,736 (USD87,566) per quality-adjusted life year (QALY) gained, respectively, compared to observation. ICERs were most sensitive to the cost of olaparib, time horizon and discount rate for outcomes. When these parameters were varied, ICERs remained above SGD92,000 (USD69,607)/QALY.

Conclusions: : At the current price, olaparib is not cost-effective when used with or without restriction by mutation status in Singapore, despite taking into account potential OS improvement over a long-time horizon.
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http://dx.doi.org/10.1080/14737167.2021.1890587DOI Listing
February 2021

DAMPs as Double-edged Swords in Sepsis.

Antioxid Redox Signal 2021 Feb 15. Epub 2021 Feb 15.

Northwell Health Feinstein Institutes for Medical Research, 88982, Center for Immunology and Inflammation , Manhasset, New York, United States.

Significance: Sepsis is defined as life-threatening organ dysfunction caused by dysregulated host response to infection. This leads to an uncontrolled inflammatory response at the onset of infection, followed by immunosuppression. The development of a specific treatment modality for sepsis is still challenging, reflecting our inadequate understanding of its pathophysiology. Understanding the mechanism and transition of the early hyperinflammation to late stage of immunosuppression in sepsis is critical for developing sepsis therapeutics. Recent Advances: Damage-associated molecular patterns (DAMPs) are intracellular molecules and released upon tissue injury and cell death in sepsis. DAMPs are recognized by pattern recognition receptors to initiate inflammatory cascades. DAMPs not only elicit an inflammatory response, but also they subsequently induce immunosuppression, both are equally important for exacerbating sepsis. Recent advances on a new DAMP, extracellular cold-inducible RNA-binding protein for fueling inflammation and immunosuppression in sepsis have added a new avenue into the dual functions of DAMPs in sepsis.

Critical Issues: The molecular modification of DAMPs and their binding to pattern recognition receptors transit dynamically by the cellular environment in pathophysiologic conditions. Correlation between the dynamic changes of the impacts of DAMPs and the clinical outcomes in sepsis still lack adequate understanding. Here, we focus on the impacts of DAMPs that cause inflammation as well as induce immunosuppression in sepsis. We further discuss the therapeutic potential by targeting DAMPs to attenuate inflammation and immunosuppression for mitigating sepsis.

Future Directions: Uncovering pathways of the transition from inflammation to immunosuppression of DAMPs is a potential therapeutic avenue for mitigating sepsis.
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http://dx.doi.org/10.1089/ars.2021.0008DOI Listing
February 2021

Polymorphic variants INSIG2 rs6726538, HLA-DRB1 rs9272143, and GCNT1P5 rs7780883 contribute to the susceptibility of cervical cancer in the Bangladeshi women.

Cancer Med 2021 Feb 14. Epub 2021 Feb 14.

Department of Pharmacy, Noakhali Science and Technology University, Noakhali, Bangladesh.

Objective: Cervical cancer is a gynecological health problem, affecting nearly 500,000 women each year worldwide. Genome-wide association studies have revealed multiple susceptible genes and their polymorphisms for cervical carcinoma risk. We have carried out this case-control study to investigate the association of INSIG2 rs6726538 (A; T), HLA-DRB1 rs9272143 (T; C), and GCNT1P5 rs7780883 (G; A) with cervical cancer.

Methods: The present study recruited 234 cervical cancer patients as cases and 212 healthy females as controls. We have applied the tetra-primer amplification refractory mutation system polymerase chain reaction (T-ARMS-PCR) method for genotyping.

Results: The SNP rs6726538 was significantly associated with increased risk of cervical cancer in all genetic models (AT vs. AA: OR = 3.30, 95% CI = 2.19-4.97, p < 0.0001; TT vs. AA: OR = 8.72, 95% CI = 3.87-19.7, p < 0.0001; AT+TT vs. AA: OR = 3.87, 95% CI = 2.61-5.73, p < 0.0001; T vs. A: OR = 2.97, 95% CI = 2.20-4.01, p < 0.0001) except the recessive model which showed a significantly reduced risk (TT vs. AA+AT: OR = 0.20, 95% CI = 0.09-0.44, p = 0.0001). rs9272143 showed significantly reduced risk for the additive model 1, dominant model, and allelic model (TC vs. TT: OR = 0.46, 95% CI = 0.31-0.70, p = 0.0004; TC+CC vs. TT: OR = 0.47 95% CI = 0.32-0.70, p = 0.0002; C vs. T: OR = 0.56, 95% CI = 0.40-0.78, p = 0.0006, respectively). The third variant, rs7780883, was significantly associated with increased risk in additive model 2, dominant, and allelic models (AA vs. GG: OR = 5.08, 95% CI = 2.45-10.5, p < 0.0001; GA+AA vs. GG: OR = 1.54, 95% CI = 1.06-2.24, p = 0.0237; A vs. G: OR = 1.88, 95% CI = 1.34-2.52, p < 0.0001, consecutively), whereas recessive model reduced the risk of cervical cancer (AA vs. GG+GA: OR = 0.20, 95% CI = 0.09-0.41, p < 0.0001). Other models of these SNPs were not associated with cervical cancer. All significant associations for three SNPs withstand after Bonferroni correction except the additive model 2 of rs7780883.

Conclusion: Our study concludes that INSIG2 rs6726538, HLA-DRB1 rs9272143, and GCNT1P5 rs7780883 polymorphisms may contribute to the development of cervical cancer in the Bangladeshi population.
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http://dx.doi.org/10.1002/cam4.3782DOI Listing
February 2021

Ghrelin as an Anti-Sepsis Peptide: Review.

Front Immunol 2020 28;11:610363. Epub 2021 Jan 28.

Laboratory of Diabetes, Obesity, and Other Metabolic Disorders, The Feinstein Institutes for Medical Research, Manhasset, NY, United States.

Sepsis continues to produce widespread inflammation, illness, and death, prompting intensive research aimed at uncovering causes and therapies. In this article, we focus on ghrelin, an endogenous peptide with promise as a potent anti-inflammatory agent. Ghrelin was discovered, tracked, and isolated from stomach cells based on its ability to stimulate release of growth hormone. It also stimulates appetite and is shown to be anti-inflammatory in a wide range of tissues. The anti-inflammatory effects mediated by ghrelin are a result of both the stimulation of anti-inflammatory processes and an inhibition of pro-inflammatory forces. Anti-inflammatory processes are promoted in a broad range of tissues including the hypothalamus and vagus nerve as well as in a broad range of immune cells. Aged rodents have reduced levels of growth hormone (GH) and diminished immune responses; ghrelin administration boosts GH levels and immune response. The anti-inflammatory functions of ghrelin, well displayed in preclinical animal models of sepsis, are just being charted in patients, with expectations that ghrelin and growth hormone might improve outcomes in patients with sepsis.
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http://dx.doi.org/10.3389/fimmu.2020.610363DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7876230PMC
January 2021

Family planning perspectives and practices of married adolescent girls in rural Upper Egypt.

Eur J Contracept Reprod Health Care 2021 Feb 12:1-7. Epub 2021 Feb 12.

Department of Public Health and Community Medicine, Assiut University, Assiut, Egypt.

Objectives: The aims of the study were to explore the contraceptive practices of married adolescent girls in rural Upper Egypt and identify the determinants of their ever use of modern contraception.

Methods: The study was a household survey of 729 married adolescent girls in 23 villages of two governorates in Upper Egypt. Listing and enumeration of all households in the selected villages were performed prior to data collection, to recruit married adolescent girls below 20 years of age. The girls were interviewed using a structured questionnaire.

Results: Only 6% of married adolescent girls were using a modern contraceptive method; 10.6% had ever used a modern contraceptive method, mostly a short-acting method. Considerable proportions of participants believed that using contraception would reduce a woman's fertility and that women should not delay their first pregnancy (34% and 54.3%, respectively); only 50.2% believed that contraception could be used for birth spacing. Predictors of the ever use of a modern method of contraception among married adolescent girls were: accepting that contraception could be used for birth spacing (B = 1.82,  < .001), older age (B = 0.42,  < .01), better reproductive health knowledge (B = 0.23,  < .05) and sharing in contraceptive decision making (B = 0.55,  < .05).

Conclusion: Married adolescent girls' current use and ever use of modern contraception were very low in rural Upper Egypt. Changing the social norms to create the desire to delay first childbirth, improving adolescent girls' reproductive health knowledge, correcting myths about contraception and building girls' agency to use contraception may increase their contraceptive use.
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http://dx.doi.org/10.1080/13625187.2021.1879781DOI Listing
February 2021

Development, synthesis, and biological evaluation of sulfonyl-α-l-amino acids as potential anti-Helicobacter pylori and IMPDH inhibitors.

Arch Pharm (Weinheim) 2021 Feb 12:e2000385. Epub 2021 Feb 12.

Chemistry of Natural Compounds Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza, Egypt.

Inosine 5'-monophosphate dehydrogenase (IMPDH) catalyzes a crucial step in the biosynthesis of DNA and RNA, and it has been exploited as a promising target for antimicrobial therapy. The present study discusses the development and synthesis of a series of sulfonyl-α-l-amino acids coupled with the anisamide scaffold and evaluates their activities as anti-Helicobacter pylori and IMPDH inhibitors. Twenty derivatives were synthesized and their structures were established by high-resolution mass spectrometry and  H and C nuclear magnetic resonance measurements. Four compounds (6, 10, 11, and 21) were found to be the most potent and selective molecules in the series with minimum inhibitory concentration (MIC) values <17 µM, which were selected to test their inhibitory activities against HpIMPDH and human (h)IMPDH2 enzymes. In all tests, amoxicillin and clarithromycin were used as reference drugs. Compounds 6 and 10 were found to have a promising activity against the HpIMPDH enzyme, with IC  = 2.42 and 2.56 µM, respectively. Moreover, the four compounds were found to be less active and safer against hIMPDH2 than the reference drugs, with IC  > 17.17 µM, which makes sure that their selectivity is toward HpIMPDH and reverse to that of amoxicillin and clarithromycin. Also, the synergistic antibacterial activity of compounds 6, 10, amoxicillin, and clarithromycin was investigated in vitro. The combination of amoxicillin/compound 6 (2:1 by weight) exhibited a significant antibacterial activity against H. pylori, with MIC = 0.12 µg/ml. The molecular docking study and ADMET analysis of the most active compounds were used to elucidate the mode-of-action mechanism.
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http://dx.doi.org/10.1002/ardp.202000385DOI Listing
February 2021

Multifunctional Hydroxyapatite/Silver Nanoparticles/Cotton Gauze for Antimicrobial and Biomedical Applications.

Nanomaterials (Basel) 2021 Feb 8;11(2). Epub 2021 Feb 8.

Chemistry Department, Faculty of Science, Helwan University, Helwan, Cairo 11795, Egypt.

Medical textiles have played an increasingly important protection role in the healthcare industry. This study was aimed at improving the conventional cotton gauze for achieving advanced biomedical specifications (coloration, UV-protection, anti-inflammation, and antimicrobial activities). These features were obtained by modifying the cotton gauze fabrics via in-situ precipitation of hydroxyapatite nanoparticles (HAp NP), followed by in-situ photosynthesis of silver (Ag) NPs with ginger oil as a green reductant with anti-inflammation properties. The HAp-Ag NPs coating provides good UV-protection properties. To further improve the HAp and Ag NPs dispersion and adhesion on the surface, the cotton gauze fabrics were modified by cationization with chitosan, or by partial carboxymethylation (anionic modification). The influence of the cationic and anionic modifications and HAp and Ag NPs deposition on the cotton gauze properties (coloration, UV-protection, antimicrobial activities, and water absorption) was thoroughly assessed. Overall, the results indicate that chemical (anionic and cationic) modification of the cotton gauze enhances HAp and Ag NPs deposition. Chitosan can increase biocompatibility and promotes wound healing properties of cotton gauze. Ag NP deposition onto cotton gauze fabrics brought high antimicrobial activities against Candida albicans, Gram-positive and Gram-negative bacteria, and improved UV protection.
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http://dx.doi.org/10.3390/nano11020429DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7915402PMC
February 2021

The Removal of Selected Inorganics from Municipal Membrane Bioreactor Wastewater Using UF/NF/RO Membranes for Water Reuse Application: A Pilot-Scale Study.

Membranes (Basel) 2021 Feb 6;11(2). Epub 2021 Feb 6.

Environmental Engineering Research Group (EnvERG), Department of Chemical Engineering, Faculty of Engineering and the Built Environment, Cape Peninsula University of Technology, Bellville, P. O. Box 1906, Cape Town 7535, South Africa.

Membrane technology has advanced substantially as a preferred choice for the exclusion of widespread pollutants for reclaiming water from various treatment effluent. Currently, little information is available about Ultrafiltration (UF)/Nanofiltration (NF)/Reverse Osmosis (RO) performance at a pilot scale as a practical engineering application. In this study, the effluent from a full-scale membrane bioreactor (MBR) municipal wastewater treatment works (MWWTWs) was treated with an RO pilot plant. The aim was to evaluate the effect of operating conditions in the removal of selected inorganics as a potential indirect water reuse application. The influent pH, flux, and membrane recovery were the operating conditions varied to measure its influence on the rejection rate. MBR/RO exhibited excellent removal rates (>90%) for all selected inorganics and met the standard requirements for reuse in cooling and irrigation system applications. The UF and NF reduction of inorganics was shown to be limited to meet water standards for some of the reuse applications due to the high Electron Conductivity (EC > 250 μS·cm) levels. The MBR/NF was irrigation and cooling system compliant, while for the MBR/UF, only the cooling system was compliant.
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http://dx.doi.org/10.3390/membranes11020117DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7915294PMC
February 2021

Decline in fish species diversity due to climatic and anthropogenic factors in Hakaluki Haor, an ecologically critical wetland in northeast Bangladesh.

Heliyon 2021 Jan 6;7(1):e05861. Epub 2021 Jan 6.

Department of Aquaculture, Bangladesh Agricultural University, Mymensingh, Bangladesh.

This study evaluates changes in fish species diversity over time in Hakaluki Haor, an ecologically critical wetland in Bangladesh, and the factors affecting this diversity. Fish species diversity data were collected from fishers using participatory rural appraisal tools and the change in the fish species diversity was determined using Shannon-Wiener, Margalef's Richness and Pielou's Evenness indices. Principal component analysis (PCA) was conducted with a dataset of 150 fishers survey to characterize the major factors responsible for the reduction of fish species diversity. Out of 63 fish species, 83% of them were under the available category in 2008 which decreased to 51% in 2018. Fish species diversity indices for all 12 taxonomic orders in 2008 declined remarkably in 2018. The first PCA (climatic change) responsible for the reduced fish species diversity explained 24.05% of the variance and consisted of erratic rainfall (positive correlation coefficient 0.680), heavy rainfall (-0.544), temperature fluctuation (0.561), and siltation (0.503). The second PCA was anthropogenic activity, including the use of harmful fishing gear (0.702), application of urea to harvest fish (0.673), drying beels annually (0.531), and overfishing (0.513). Finally, the third PCA was loaded with the fishermen age (0.719), education (-0.767), and fishing experience (0.695) of the fishers. Deepening of could enhance dry season water availability and shelter the fish. Imposing fisheries regulations to reduce human activities is inevitable to sustain haor fisheries.
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http://dx.doi.org/10.1016/j.heliyon.2020.e05861DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7855352PMC
January 2021

Introduction of typhoid vaccine in the expanded immunization program of Pakistan.

Hum Vaccin Immunother 2021 Jan 31. Epub 2021 Jan 31.

Department of Pharmacy Administration and Clinical Pharmacy, Xi'an Jiaotong University , Xi'an, China.

Worldwide, typhoid infects 11-20 million people each year. In Pakistan, the first extensively drug-resistant (XDR) typhoid was reported in 2016 resulting in an epidemic. To curb this battle of typhoid, the Expanded Program for Immunization (EPI) of Pakistan requested Global Alliance for Vaccines and Immunization (GAVI) for financial assistance. Hence becoming the first country to administer the vaccination against typhoid in children through EPI. To address the possible risk of endemic, it is needed that WHO and the United Nations should recommend all south Asian countries to avail of this golden opportunity provided by GAVI. Finally, the addition of typhoid vaccine in routine immunization will reduce mortalities, morbidities, health expenditure, and increase life expectancy in all low- and middle-income countries.
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http://dx.doi.org/10.1080/21645515.2020.1869496DOI Listing
January 2021

Technological review on thermochemical conversion of COVID-19-related medical wastes.

Resour Conserv Recycl 2021 Apr 15;167:105429. Epub 2021 Jan 15.

Institute of Industrial Science, The University of Tokyo, 4-6-1 Komaba, Meguro-ku, Tokyo 153-8505, Japan.

COVID-19 pandemic has brought tremendous environmental burden due to huge amount of medical wastes (about 54,000 t/d as of November 22, 2020), including face mask, gloves, clothes, goggles, and sanitizer/disinfectant containers. A proper waste management is urgently required to mitigate the spread of the disease, minimize the environmental impacts, and take their potential advantages for further utilization. This work provides a prospective review on the possible thermochemical treatments for those COVID-19 related medical wastes (CMW), as well as their possible conversion to fuels. The characteristics of each waste are initially analyzed and described, especially their potential as energy source. It is clear that most of CMWs are dominated by plastic polymers. Thermochemical processes, including incineration, torrefaction, pyrolysis, and gasification, are reviewed in terms of applicability for CMW. In addition, the mechanical treatment of CMW into sanitized refuse-derived fuel (SRDF) is also discussed as the preliminary stage before thermochemical conversion. In terms of material flexibility, incineration is practically applicable for all types of CMW, although it has the highest potential to emit the largest amount of CO and other harmful gasses. Furthermore, gasification and pyrolysis are considered promising in terms of energy conversion efficiency and environmental impacts. On the other hand, carbonization faces several technical problems following thermal degradation due to insufficient operating temperature.
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http://dx.doi.org/10.1016/j.resconrec.2021.105429DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7832489PMC
April 2021

Characterization of soy-lignin bonded Rhizophora spp. particleboard as substitute phantom material for radiation dosimetric studies - Investigation of CT number, mass attenuation coefficient and effective atomic number.

Appl Radiat Isot 2021 Jan 21;170:109601. Epub 2021 Jan 21.

School of Industrial Technology, Universiti Sains Malaysia, Penang, 11800, Malaysia.

Experimental particleboards are made from Rhizophora spp. wood trunk with three different percentages of lignin and soy flour (0%, 6% and 12%) as adhesives. The objective was to investigate the equivalence of Rhizophora spp. particleboard as phantom material with human soft tissue using Computed Tomography (CT) number. The linear and mass attenuation coefficient of Rhizophora spp. particleboard at low energy range was also explored using X-ray Fluorescence (XRF) configuration technique. Further characterization of the particleboard was performed to determine the effective atomic number, Z using Energy Dispersive X-Ray (EDX) method. Adhesive-bonded Rhizophora spp. particleboard showed close similarities with water, based on the average CT numbers, electron density calibration curve and the analysis of CT density profile, compared to the binderless particleboard. The effective atomic number obtained from the study indicated that the attenuation properties of all the particleboards at different percentages of adhesives were almost similar to water. The mass attenuation coefficient calculated from XRF configuration technique showed good agreement with water from XCOM database, suggesting its potential as phantom material for radiation study.
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http://dx.doi.org/10.1016/j.apradiso.2021.109601DOI Listing
January 2021

Evaluation of Hepatoprotective Activity of Stem Extract against CCl-Induced Hepatic Damage in Wistar Rats.

Adv Pharmacol Pharm Sci 2021 7;2021:8883040. Epub 2021 Jan 7.

Laboratory of Bioresources Biotechnology Ethnopharmacology and Health, Mohammed First University, Oujda, Morocco.

The present study aims to evaluate the hepatoprotective activity of stem aqueous extract of (AECe) on carbon tetrachloride- (CCl-) induced hepatic damage in Wistar rats. The animals were daily treated with the aqueous extract of at a dose of 250 mg/kg body weight for 14 days. CCl was injected (1 ml/kg, .) two times, on the 7 and 14 days. At the end of the experimental period, all rats were anesthetized to collect blood for the assessment of biochemical parameters and then sacrificed to collect the liver for weighing. Hepatotoxicity was evaluated by measuring the serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), bilirubin (total and direct), malondialdehyde (MDA), total protein (TP), triglycerides (TG), total cholesterol, very low-density lipoprotein (VLDL-c ), low-density lipoprotein (LDL-c), high-density lipoprotein (HDL-c), urea, creatinine, and uric acid. Based on the results obtained in this study, the administration of before exposure to the administration of CCl conferred favorable hepatoprotective effect in rats. The treatment with AECe (250 mg/kg) exhibits a significant hepatoprotective effect by ameliorating CCl-induced alterations of these biochemical parameters. Hence, could be a potential medicinal herb that can be used in the future to prevent liver intoxication.
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http://dx.doi.org/10.1155/2021/8883040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7810557PMC
January 2021

Phytochemical Profiling, In Vitro and In Silico Anti-Microbial and Anti-Cancer Activity Evaluations and Staph GyraseB and -TOP-IIβ Receptor-Docking Studies of Major Constituents of L. Aqueous-Ethanolic Extract and Its Subsequent Fractions: An Approach to Validate Traditional Phytomedicinal Knowledge.

Molecules 2021 Jan 22;26(3). Epub 2021 Jan 22.

Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo 11371, Egypt.

, an edible halophytic plant, is part of the traditional medicine chest in the Mediterranean region for symptomatic relief of diabetes, hypertension, wound healing, burns, infections, and rheumatoid arthritis pain. The current study aimed to characterize phytoconstituents, and the evaluations of the anti-microbial-biofilm, and anti-cancers bioactivities of the plant's mother liquor, i.e., aqueous-ethanolic extract, and its subsequent fractions. The in silico receptors interaction feasibility of major constituents with Staph GyraseB, and human topoisomerase-IIβ (-TOP-IIβ) were conducted to confirm the plant's anti-microbial and anti-cancer biological activities. Thirty-eight secondary metabolites of flavonoids, stilbene, phenolic acids, alkaloids, and coumarin classes identified by LC-ESI-TOF-MS spectrometric analysis, and tiliroside (kaempferol-3-O-(6''''--coumaroyl)-glucoside, 19.8%), zygophyloside-F (12.78%), zygophyloside-G (9.67%), and isorhamnetin-3-O-glucoside (4.75%) were identified as the major constituents. A superior biofilm obliteration activity established the minimum biofilm eradication concentration (MBEC) for the chloroform fraction at 3.9-15.63 µg/mL, as compared to the positive controls (15.63-31.25 µg/mL) against all the microbial strains that produced the biofilm under study, except the . The aqueous-ethanolic extract showed cytotoxic effects with IC values at 3.47, 3.19, and 2.27 µg/mL against MCF-7, HCT-116, and HepG2 cell-lines, respectively, together with the inhibition of TOP-IIβ with IC value at 45.05 ng/mL in comparison to its standard referral inhibitor (staurosporine, IC, 135.33 ng/mL). This conclusively established the anti-cancer activity of the aqueous-ethanolic extract that also validated by in silico receptor-binding predicted energy levels and receptor-site docking feasibility of the major constituents of the plant's extract. The study helped to authenticate some of the traditional phytomedicinal properties of the anti-infectious nature of the plant.
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http://dx.doi.org/10.3390/molecules26030577DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7866194PMC
January 2021