Displaying publications 101 - 120 of 186 in total

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  1. Fulltext Community pharmacists' skills and practice regarding dispensing fiscalized substances: a cross-sectional survey
    El-Dahiyat F, Jairoun AA, Al-Hemyari SS, Shahwan M, Jairoun M, Zyoud SH, et al.
    Front Pharmacol, 2023;14:1237306.
    PMID: 37719848 DOI: 10.3389/fphar.2023.1237306
    Background: The use of drugs containing fiscalized substances is essential in different medical areas, including pain management, obstetric emergencies, and the treatment of mental disorders. However, due to their potential for abuse and negative health effects, the dispensing of these substances demands pharmacists with the requisite skills and practice. Objective: This study assesses the skills and practices of pharmacy personnel in the United Arab Emirates (UAE) regarding the dispensing of tramadol, a medication containing fiscalized substances, in community pharmacies. Methodology: A cross-sectional study was conducted. Community Pharmacies were chosen via random sampling, and seven well-trained final year pharmacy students visited them and conducted face-to-face interviews. The survey tool covered items highlighting the demographic data of the subjects, and items on the practice and skills regarding dispensing the fiscalized substances. The content validity ratio values of all tool questions were more than 0.78, suggesting acceptable validity and the Cronbach's α of 0.75 showed as acceptable internal reliability. The primary outcome measures of interest were the skills and practice regarding dispensing Fiscalized substances. Results: A total of 612 pharmacists were recruited in the study. The average practice score was 80%. There was a statistically significant association (p < 0.05) between practices about dispensing fiscalized substances and gender, age group, pharmacy type, work experience, university of graduation, and receiving training on epilepsy and antiepileptic drugs. Conclusion: The results implied that competency and experience are vital factors for the dispensing of tramadol. Contextually, the majority of the pharmacists evidently have the requisite competencies to provide high-quality and proper medical care, with regards to dispensing tramadol, which will minimize drug abuse and medication errors, and assist outpatients to manage their drugs containing fiscalized substances.
  2. Sodium alginate encapsulated iron oxide decorated with thymoquinone nanocomposite induces apoptosis in human breast cancer cells via PI3K-Akt-mTOR pathway
    Alzahrani B, Elderdery AY, Alsrhani A, Alzerwi NAN, Althobiti MM, Elkhalifa AME, et al.
    Int J Biol Macromol, 2023 Jul 31;244:125054.
    PMID: 37245766 DOI: 10.1016/j.ijbiomac.2023.125054
    The present study investigated the cytotoxicity and proapoptotic properties of iron oxide-sodium-alginate-thymoquinone nanocomposites against breast cancer MDA-MB-231 cells in vitro and in silico. This study used chemical synthesis to formulate the nanocomposite. Electron microscopies such as scanning (SEM) and transmission (TEM), Fourier transform infrared (FT-IR), Ultraviolet-Visible, Photoluminescence spectroscopy, selected area (electron) diffraction (SAED), energy dispersive X-ray analysis (EDX), and X-ray diffraction studies (XRD) were used to characterize the synthesized ISAT-NCs and the average size of them was found to be 55 nm. To evaluate the cytotoxic, antiproliferative, and apoptotic potentials of ISAT-NCs on MDA-MB-231 cells, MTT assays, FACS-based cell cycle studies, annexin-V-PI staining, ELISA, and qRT-PCR were used. PI3K-Akt-mTOR receptors and thymoquinone were predicted using in-silico docking studies. Cell proliferation is reduced in MDA-MB-231 cells due to ISAT-NC cytotoxicity. As a result of FACS analysis, ISAT-NCs had nuclear damage, ROS production, and elevated annexin-V levels, which resulted in cell cycle arrest in the S phase. The ISAT-NCs in MDA-MB-231 cells were found to downregulate PI3K-Akt-mTOR regulatory pathways in the presence of inhibitors of PI3K-Akt-mTOR, showing that these regulatory pathways are involved in apoptotic cell death. We also predicted the molecular interaction between thymoquinone and PI3K-Akt-mTOR receptor proteins using in-silico docking studies which also support PI3K-Akt-mTOR signaling inhibition by ISAT-NCs in MDA-MB-231 cells. As a result of this study, we can conclude that ISAT-NCs inhibit the PI3K-Akt-mTOR pathway in breast cancer cell lines, causing apoptotic cell death.
  3. Therapeutic Potential of Albumin Nanoparticles Encapsulated Visnagin in MDA-MB-468 Triple-Negative Breast Cancer Cells
    Alsrhani A, Elderdery AY, Alzahrani B, Alzerwi NAN, Althobiti MM, Rayzah M, et al.
    Molecules, 2023 Apr 04;28(7).
    PMID: 37049991 DOI: 10.3390/molecules28073228
    Breast cancer is among the most recurrent malignancies, and its prevalence is rising. With only a few treatment options available, there is an immediate need to search for better alternatives. In this regard, nanotechnology has been applied to develop potential chemotherapeutic techniques, particularly for cancer therapy. Specifically, albumin-based nanoparticles are a developing platform for the administration of diverse chemotherapy drugs owing to their biocompatibility and non-toxicity. Visnagin, a naturally derived furanochromone, treats cancers, epilepsy, angina, coughs, and inflammatory illnesses. In the current study, the synthesis and characterization of albumin visnagin (AV) nanoparticles (NPs) using a variety of techniques such as transmission electron microscopy, UV-visible, Fourier transform infrared, energy dispersive X-ray composition analysis, field emission scanning electron microscopy, photoluminescence, X-Ray diffraction, and dynamic light scattering analyses have been carried out. The MTT test, dual AO/EB, DCFH-DA, Annexin-V-FITC/PI, Propidium iodide staining techniques as well as analysis of apoptotic proteins, antioxidant enzymes, and PI3K/Akt/mTOR signaling analysis was performed to examine the NPs' efficacy to suppress MDA-MB-468 cell lines. The NPs decreased cell viability increased the amount of ROS in the cells, disrupted membrane integrity, decreased the level of antioxidant enzymes, induced cell cycle arrest, and activated the PI3K/Akt/mTOR signaling cascade, ultimately leading to cell death. Thus, AV NPs possesses huge potential to be employed as a strong anticancer therapy alternative.
  4. Fulltext Structural, Optical, Antibacterial, and Anticancer Properties of Cerium Oxide Nanoparticles Prepared by Green Synthesis Using Morinda citrifolia Leaves Extract
    Elderdery AY, Alzahrani B, Alabdulsalam AA, Hamza SMA, Elkhalifa AME, Alhamidi AH, et al.
    Bioinorg Chem Appl, 2022;2022:6835625.
    PMID: 36212986 DOI: 10.1155/2022/6835625
    Currently, new advancements in the area of nanotechnology opened up new prospects in the field of medicine that could provide us with a solution for numerous medical complications. Although a several varieties of nanoparticles is being explored to be used as nanomedicines, cerium oxide nanoparticles (CeO2 NPs) are the most attractive due to their biocompatibility and their switchable oxidation state (+3 and +4) or in other words the ability to act as prooxidant and antioxidant depending on the pH condition. Green synthesis of nanoparticles is preferred to make it more economical, eco-friendly, and less toxic. The aim of our study here is to formulate the CeO2 NPs (CeO2 NPs) using Morinda citrifolia (Noni) leaf extract and study its optical, structural, antibacterial, and anticancer abilities. Their optical and structural characterization was accomplished by employing X-ray diffractography (XRD), TEM, EDAX, FTIR, UV-vis, and photoluminescence assays. Our CeO2 NPs expressed strong antibacterial effects against Gram-positive S. aureus and S. pneumonia in addition to Gram-negative E. coli and K. pneumonia when compared with amoxicillin. The anticancer properties of the green synthesized CeO2 NPs against human acute lymphoblastic leukemia (ALL) MOLT-4 cells were further explored by the meticulous study of their ability to diminish cancer cell viability (cytotoxicity), accelerate apoptosis, escalate intracellular reactive oxygen species (ROS) accumulation, decline the mitochondria membrane potential (MMP) level, modify the cell adhesion, and shoot up the activation of proapoptotic markers, caspase-3, -8, and -9, in the tumor cells. Altogether, the outcomes demonstrated that our green synthesized CeO2 NPs are an excellent candidate for alternative cancer therapy.
  5. Fulltext Examining the Impacts of Coronavirus Disease 2019 Mitigation Policies on Health Outcomes of Older Adults: Lessons Learned From Six High-Income or Middle-Income Countries
    Pushpalata Zanwar P, Perianayagam A, Zazdravnykh E, Omar Z, Vinod Joseph KJ, Santos FH, et al.
    Public Policy Aging Rep, 2022;32(4):121-130.
    PMID: 36349280 DOI: 10.1093/ppar/prac023
  6. Fulltext Anti-sperm Antibody Positivity in Men with Varicocele: A Systematic Review and Meta-Analysis
    Falcone M, Bocu K, Keskin H, Solorzano Vazquez JF, Banthia R, Mahendran T, et al.
    World J Mens Health, 2025 Jan;43(1):60-69.
    PMID: 38606868 DOI: 10.5534/wjmh.240003
    PURPOSE: Despite the significant role of varicocele in the pathogenesis of male infertility, its association with anti-sperm antibodies (ASA) remains controversial. This systematic review and meta-analysis (SRMA) aims to investigate the frequency of ASA positivity in men with varicocele.

    MATERIALS AND METHODS: This SRMA is conducted in accordance with the Meta-analysis of Observational Studies in Epidemiology guidelines. We investigated the frequency of ASA positivity in ejaculates or serum of men with varicocele as compared to men without varicocele (controls). A literature search was performed using the Scopus and PubMed databases following the Population Exposure Comparison Outcome, Study Design model. Data extracted from eligible studies were meta-analyzed and expressed as odds ratios (ORs) and confidence intervals (CIs).

    RESULTS: Out of 151 abstracts identified during the initial screening, 6 articles met the inclusion criteria and were included in the meta-analysis. Using mixed antiglobulin reaction (MAR) assay, 61 out of the 153 (39.8%) patients with varicocele tested positive for ASA in their ejaculates as compared to 22 out of the 129 control subjects (17%, OR=4.34 [95% CI: 1.09-17.28]; p=0.04). Using direct or indirect immunobead test, 30 out of 60 cases diagnosed with varicocele (50%) had shown ASA positivity in their ejaculates as compared to 16 out of 104 controls (15.4%, OR=3.57 [95% CI: 0.81-15.68]; p=0.09). Using enzyme-linked immunosorbent assay (ELISA), out of 89 varicocele patients, 33 (37.1%) tested positive for serum ASA as compared to 9 out of 57 participants in the control group (15.8%, OR=7.87 [95% CI: 2.39-25.89]; p<0.01).

    CONCLUSIONS: This SRMA indicates that ASA positivity is significantly higher among men with varicocele when tested by direct method (MAR) or indirect method (ELISA). This data suggests an immunological pathology in infertile men with varicocele and may have implications for the management of these patients.

  7. Fulltext Evaluation of Sechium edule fruit attenuation impact on the cardiomyopathy of the STZ-induced diabetic rats
    Mohammad FS, Das U, Samanta SK, Irfan Z, Gopinath SC, Mostafa MAH, et al.
    Heliyon, 2024 May 15;10(9):e30440.
    PMID: 38742087 DOI: 10.1016/j.heliyon.2024.e30440
    Sechium edule, commonly known as chayote is known for its low glycemic index, high fiber content, and rich nutritional profile, which suggests it may be beneficial for individuals with diabetes. While research specifically examining the impact of chayote on diabetes is limited, this study screened its biological impacts by using different biomarkers on streptozotocin-induced diabetic (STZ-ID) rats. The ethanolic extract of the Sechium edule fruits was assessed for different phytochemical, biochemical, and anti-diabetic properties. In the results, chayote extract had high phenolic and flavonoid contents respectively (39.25 ± 0.65 mg/mL and 12.16 ± 0.50 mg/mL). These high phenolic and flavonoid contents showed high implications on STZ-ID rats. Altogether 200 and 400 mg/kg of the extract considerably reduced the blood sugar level and enhanced the lipid profile of the STZ-ID rats. Additionally, they have decreased blood urea and serum creatinine levels. Besides, the levels of SGOT, SGPT, LDH, sodium, and potassium ions were significantly lowered after the administration period. More importantly, the electrocardiogram (ECG) parameters such as QT, RR, and QTc which were prolonged in the diabetic rats were downregulated after 35 days of administration of S. edule extract (400 mg/kg). And, the histological examination of the pancreas and kidney showed marked improvement in structural features of 200 and 400 mg/kg groups when compared to the diabetic control group. Where the increase in the glucose levels was positively correlated with QT, RR, and QTc (r2 = 0.76, r2 = 0.76, and r2 = 0.43) which means that ECG could significantly reflect the diabetes glucose levels. In conclusion, our findings showed that the fruit extract exerts a high potential to reduce artifacts secondary to diabetes which can be strongly suggested for diabetic candidates. However, there is a need to study the molecular mechanisms of the extract in combating artifacts secondary to diabetes in experimental animals.
  8. Unveiling dynamics of nitrogen content and selected nitrogen heterocycles in thrombin inhibitors: a ceteris paribus approach
    Masand VH, Al-Hussain S, Alzahrani AY, Al-Mutairi AA, Sultan Alqahtani A, Samad A, et al.
    Expert Opin Drug Discov, 2024 Aug;19(8):991-1009.
    PMID: 38898679 DOI: 10.1080/17460441.2024.2368743
    BACKGROUND: Despite the progress in comprehending molecular design principles and biochemical processes associated with thrombin inhibition, there is a crucial need to optimize efforts and curtail the recurrence of synthesis-testing cycles. Nitrogen and N-heterocycles are key features of many anti-thrombin drugs. Hence, a pragmatic analysis of nitrogen and N-heterocycles in thrombin inhibitors is important throughout the drug discovery pipeline. In the present work, the authors present an analysis with a specific focus on understanding the occurrence and distribution of nitrogen and selected N-heterocycles in the realm of thrombin inhibitors.

    RESEARCH DESIGN AND METHODS: A dataset comprising 4359 thrombin inhibitors is used to scrutinize various categories of nitrogen atoms such as ring, non-ring, aromatic, and non-aromatic. In addition, selected aromatic and aliphatic N-heterocycles have been analyzed.

    RESULTS: The analysis indicates that ~62% of thrombin inhibitors possess five or fewer nitrogen atoms. Substituted N-heterocycles have a high occurrence, like pyrrolidine (23.24%), pyridine (20.56%), piperidine (16.10%), thiazole (9.61%), imidazole (7.36%), etc. in thrombin inhibitors.

    CONCLUSIONS: The majority of active thrombin inhibitors contain nitrogen atoms close to 5 and a combination of N-heterocycles like pyrrolidine, pyridine, piperidine, etc. This analysis provides crucial insights to optimize the transformation of lead compounds into potential anti-thrombin inhibitors.

  9. Fulltext Impact of Varicocele Repair on Assisted Reproductive Technique Outcomes in Infertile Men: A Systematic Review and Meta-Analysis
    Palani A, Cannarella R, Saleh R, Salvio G, Harraz AM, Crafa A, et al.
    World J Mens Health, 2025 Apr;43(2):344-358.
    PMID: 39344117 DOI: 10.5534/wjmh.240132
    PURPOSE: In this systematic review and meta-analysis, we investigated assisted reproductive technology (ART) success in infertile men with clinical varicocele and abnormal semen parameters who underwent varicocele repair (VR) before the ART procedure as compared to those who did not.

    MATERIALS AND METHODS: A comprehensive search of the Scopus, PubMed, Embase, and Cochrane Library databases was conducted using a specific query string to identify studies examining the impact of VR on ART outcomes, including fertilization rate, clinical pregnancy, pregnancy loss, and live-birth rate, until October 2023. Outcomes were analyzed based on the type of ART. Studies on VR in infertile men with non-obstructive azoospermia and those who underwent ART only due to female factor infertility were excluded from the study.

    RESULTS: Out of 1,554 articles reviewed, only 9 met the inclusion criteria for the study. All the included articles were observational studies. The variability in study quality in the included literature resulted in a moderate overall risk of bias. Data analysis showed that for intrauterine insemination, there was no difference in the clinical pregnancy rate (odds ratio [OR] 1.01, 95% confidence interval [CI]: 0.42, 2.45; p=0.97). However, for intracytoplasmic sperm injection (ICSI), men with VR showed a significant improvement in fertilization rate (mean difference 10.9, 95% CI: 5.94, 15.89; p<0.01), clinical pregnancy rate (OR 1.38, 95% CI: 1.07, 1.78; p=0.01) and live-birth rate (OR 2.07, 95% CI: 1.45, 2.97; p<0.01), compared to men who did not undergo VR.

    CONCLUSIONS: The findings of this systematic review and meta-analysis suggest that VR has a positive impact on pregnancy and live birth rates after ICSI. However, biases like small sample sizes and heterogeneous populations highlight the need for larger, well-designed prospective studies to validate these findings.

  10. Surface water quality index forecasting using multivariate complementing approach reinforced with locally weighted linear regression model
    Hai T, Ahmadianfar I, Halder B, Heddam S, Al-Areeq AM, Demir V, et al.
    Environ Sci Pollut Res Int, 2024 May;31(22):32382-32406.
    PMID: 38653893 DOI: 10.1007/s11356-024-33027-0
    River water quality management and monitoring are essential responsibilities for communities near rivers. Government decision-makers should monitor important quality factors like temperature, dissolved oxygen (DO), pH, and biochemical oxygen demand (BOD). Among water quality parameters, the BOD throughout 5 days is an important index that must be detected by devoting a significant amount of time and effort, which is a source of significant concern in both academic and commercial settings. The traditional experimental and statistical methods cannot give enough accuracy or solve the problem for a long time to detect something. This study used a unique hybrid model called MVMD-LWLR, which introduced an innovative method for forecasting BOD in the Klang River, Malaysia. The hybrid model combines a locally weighted linear regression (LWLR) model with a wavelet-based kernel function, along with multivariate variational mode decomposition (MVMD) for the decomposition of input variables. In addition, categorical boosting (Catboost) feature selection was used to discover and extract significant input variables. This combination of MVMD-LWLR and Catboost is the first use of such a complete model for predicting BOD levels in the given river environment. In addition, an optimization process was used to improve the performance of the model. This process utilized the gradient-based optimization (GBO) approach to fine-tune the parameters and better the overall accuracy of predicting BOD levels. To assess the robustness of the proposed method, we compared it to other popular models such as kernel ridge (KRidge) regression, LASSO, elastic net, and gaussian process regression (GPR). Several metrics, comprising root-mean-square error (RMSE), R (correlation coefficient), U95% (uncertainty coefficient at 95% level), and NSE (Nash-Sutcliffe efficiency), as well as visual interpretation, were used to evaluate the predictive efficacy of hybrid models. Extensive testing revealed that, in forecasting the BOD parameter, the MVMD-LWLR model outperformed its competitors. Consequently, for BOD forecasting, the suggested MVMD-LWLR optimized with the GBO algorithm yields encouraging and reliable results, with increased forecasting accuracy and minimal error.
  11. Polyphenolic profiling of Ipomoea carnea Jacq. by HPLC-DAD and its implications in oxidative stress and cancer
    Khan MZI, Zahra SS, Ahmed M, Fatima H, Mirza B, Haq IU, et al.
    Nat Prod Res, 2019 Jul;33(14):2099-2104.
    PMID: 29873254 DOI: 10.1080/14786419.2018.1482551
    Ipomoea carnea Jacq. is an important folklore medicinal plant, assessed for its underexplored biological potential. Antioxidant, cytotoxic, antiproliferative and polyphenolic profile of whole plant was evaluated using various techniques. Maximum extract recovery (29% w/w), phenolic [13.54 ± 0.27 μg GAE/mg dry weight (DW)] and flavonoid (2.11 ± 0.10 μg QE /mg DW) content were recorded in methanol-distilled water (1:1) flower extract. HPLC-DAD analysis quantified substantial amount of six different polyphenols ranging from 0.081 to 37.95 μg/mg extract. Maximum total antioxidant and reducing potential were documented in methanol-distilled water and acetone-distilled water flower extracts (42.62 ± 0.47 and 24.38 ± 0.39 μg AAE/mg DW) respectively. Ethanol-chloroform root extract manifested highest free radical scavenging (IC50 of 61.22 μg/mL) while 94.64% of the extracts showed cytotoxicity against brine shrimps. Ethanol leaf extract exhibited remarkable activity against THP-1 cell line (IC50 = 8 ± 0.05 μg/mL) and protein kinases (31 mm phenotype bald zone).
  12. Staff and ambient radiation dose resulting from therapeutic nuclear medicine procedures
    Alkhorayef M, Sulieman A, Mohamed-Ahmed M, Al-Mohammed HI, Alkhomashi N, Sam AK, et al.
    Appl Radiat Isot, 2018 Nov;141:270-274.
    PMID: 30145016 DOI: 10.1016/j.apradiso.2018.07.014
    With associated cure rates in excess of 90%, targeted 131I radioactive iodine therapy has clearly improved thyroid cancer survival. Thus said, potential radiation risks to staff represent a particular concern, current study seeking to determine the radiation exposure of staff from 131I patients during hospitalization, also estimating accumulated dose and related risk to staff during preparation of the radioactive iodine. In present study made over the three-month period 1st February to 1st May 2017, a total of 69 patient treatments were investigated (comprising a cohort of 46 females and 23 males), this being a patient treatment load typically reflective of the workload at the particular centre for such treatments. The patients were administered sodium iodide 131I, retained in capsules containing activities ranging from 370 to 5550 MBq at the time of calibration, radioiodine activity depends on many factors such as gender, clinical indication, body mass index and age. The staff radiation dose arising from each patient treatment was measured on three consecutive days subsequent to capsule administration. In units of µSv, the mean and dose-rates range at distances from the patients of 5 cm, 1 m and 2 m were 209 ± 73 (165-294), 6.8 ± 2 (5.3-9.5) and 0.9 ± 0.3 (0.7-1.2). The annual dose (also measured in units of µSv), based on annual records of doses, for medical physicists, technologists and nurses were 604, 680 and 1000 µSv respectively. In regard to current practice and workload, staff exposures were all found to be below the annual dose limit for radiation workers.
  13. Single-step pyrolysis of phosphoric acid-activated chitin for efficient adsorption of cephalexin antibiotic
    Khanday WA, Ahmed MJ, Okoye PU, Hummadi EH, Hameed BH
    Bioresour Technol, 2019 May;280:255-259.
    PMID: 30772638 DOI: 10.1016/j.biortech.2019.02.003
    Cephalexin (CFX) antibiotic, a potent pharmaceutical water pollutant, was efficiently removed by activated carbon (AC) derived from a single-step pyrolysis of phosphoric acid-activated chitin. Experimental conditions such as temperature, CFX initial concentration, and solution pH were screened in batch adsorption. Phosphoric acid activation of chitin and subsequent pyrolysis tailored the Brunauer-Emmett-Teller surface area, total pore volume, and average pore diameter to 1199.02 m2/g, 0.641 cm3/g, and 21.37 Å, respectively. The Langmuir isotherm adequately described the equilibrium data for CFX adsorption on chitin-AC, with an R2 of 0.99 and a monolayer capacity of 245.19 mg/g at 50 °C. Chitin-AC showed higher adsorption capacity compared with other ACs derived from industrial and agricultural precursors. When activated by phosphoric acid, chitin-AC featured functional multi-sites for vast antibiotic adsorption treatment. Overall, chitin-AC could be a promising adsorbent for removal of CFX.
  14. Non-linear relationship between tourism, economic growth, urbanization, and environmental degradation: evidence from smooth transition models
    Raza SA, Qureshi MA, Ahmed M, Qaiser S, Ali R, Ahmed F
    Environ Sci Pollut Res Int, 2021 Jan;28(2):1426-1442.
    PMID: 32840747 DOI: 10.1007/s11356-020-10179-3
    The study aims to analyze two objectives: first is to explore the non-linear relationship between tourism development, economic growth, urbanization, and environmental degradation, and also to analyze the threshold level of the contribution of tourism development on environmental degradation in top tourist arrival destinations. We applied the newly proposed econometric method panel smooth transition regression (PSTR) framework with two regimes on yearly panel data from 1995 to 2017. Findings suggest that the relationship between tourism development and environmental degradation is non-linear and regime dependent. Furthermore, the findings indicated that the relationship above the threshold level is negative and significant, while below the threshold, tourism development is positive and significant effect on environmental degradation. Tourism development and environmental degradation also exhibit the inverted U-shape relationship meaning that at a particular point, increase in tourism development increases in environmental degradation but after a particular point, increase in tourism development decreases the environmental degradation. The economic growth and urbanization also portray a non-linear and regime-dependent relationship with environmental degradation. The study assists policies and empirical information.
  15. Fulltext In vivo assessment of reversing Cisplatin-Induced nephrotoxicity using Jatropha mollissima crude extract and its potential cytotoxicity
    Omer Iqbal M, Bashir Yahya E, Andleeb S, Masood Ahmed M, Umar Javaid M, Shakeel W, et al.
    Saudi J Biol Sci, 2021 Dec;28(12):7373-7378.
    PMID: 34867040 DOI: 10.1016/j.sjbs.2021.08.057
    Jatropha mollissima is one of the ancient plants that known in Africa, Asia and Latin America for its high medicinal value. Previously we showed that the ethanolic leaves extract of J. mollissima was able to reverse the aminoglycoside antibiotics induced nephrotoxicity in only two weeks of administration. Here, we evaluated the phytochemicals, antioxidant and in vivo cytotoxicity of the ethanolic leaves extract in addition to the ability of reversing Cisplatin-induced nephrotoxicity in wistar albino rats. The results of phytochemical analysis showed the presence of flavonoids, phenols, tannins and saponins, with significantly high antioxidant activity. The treated rats did not show any cytotoxic signs; no anatomical, physiological and/or histopathological changes compared with the control group. Kidney, spleen and liver tissues appeared normal after two weeks administration of the maximum dose, with a possible alteration in distal tubules, proximal tubules and glomerulus of the kidney tissues. The results of nephrotoxicity and kidney function suggest promising potential for J. mollissima in kidney damage treatment.
  16. Fulltext Expression of survivin and its clinicopathological correlations in invasive ductal carcinoma of the breast
    Al-Joudi FS, Iskandar ZA, Hasnan J, Rusli J, Kamal Y, Imran AK, et al.
    Singapore Med J, 2007 Jul;48(7):607-14.
    PMID: 17609820
    INTRODUCTION: Survivin is a 16.5-kDa intracellular protein that inhibits apoptosis and regulates cell division, and belongs to the inhibitors of apoptosis gene family. It appears to have an important role in regulating apoptosis at the cell cycle checkpoints. Survivin has been found to have a differential distribution in cancer compared to normal tissue, as it is over-expressed in malignant tumours.
    METHODS: In addition to the demographical analysis of the disease, data from 382 women with invasive ductal carcinoma of the breast were collected from three hospitals in Northeast Malaysia, and analysed for survivin expression by immunohistochemistry.
    RESULTS: Invasive ductal carcinoma of the breast was found to be the most prevalent breast cancer type. Survivin was detected in 260 (68.1 percent) study cases. In addition, significant correlations have been shown between survivin expression on one hand, and tumour size and lymph node involvement on the other hand (p-value is less than 0.05). However, no significant correlations were found with other clinicopathological factors, such as tumour histological grade, tumour side, oestrogen and progesterone receptors. Nuclear expression of survivin was detected in 16.5 percent of the study cases, cytoplasmic expression was detected in 24.1 percent, and 27.5 percent of the cases expressed survivin in both nuclear and cytoplasmic locations simultaneously. The subcellular localisation of survivin was significantly correlated (p is less than 0.001) with the lymph node involvement indicating its value in predicting the aggressiveness of tumour cells, since it increases the resistance to apoptosis and promotes cell proliferation.
    CONCLUSION: This is the fi rst known report on survivin expression in cancer in West Malaysia and Southeast Asia. It emphasises the importance of the detection of survivin in breast cancer to aid in diagnosis, confirm malignancy, and to assess the disease progress and response to therapy.
  17. Fulltext Polyimide biocomposites coated with tantalum pentoxide for stimulation of cell compatibility and enhancement of biointegration for orthopedic implant
    Asadullah S, Ahmed M, Sarfraz S, Zahra M, Asari A, Wahab NHA, et al.
    Heliyon, 2023 Dec;9(12):e23284.
    PMID: 38144283 DOI: 10.1016/j.heliyon.2023.e23284
    Orthopedic implants are an important tool in the treatment of musculoskeletal conditions and helped many patients to improve their quality of life. Various inorganic-organic biocomposites have been broadly investigated particularly in the area of load-bearing orthopedic/dental applications. Polyimide (PI) is a promising organic material and shows excellent mechanical properties, biocompatibility, bio-stability, and its elastic modulus is similar to human bone but it lacks bioactivity, which is very important for cell adhesion and ultimately for bone regeneration. In this research, tantalum pentoxide (Ta2O5) coating was prepared on the surface of PI by polydopamine (PDA) bonding. The results showed that Ta2O5 was evenly coated on the surface of PI, and with the concentration of Ta2O5 in the PDA suspension increased, the content of Ta2O5 particles on the surface of PI increased significantly. In addition, the Ta2O5 coating significantly increased the roughness and hydrophilicity of the PI matrix. Cell experiments showed that PI surface coating Ta2O5 could promote the proliferation, adhesion, and osteogenic differentiation of bone marrow-derived stromal cells (BMSCs). The results demonstrated that fabricating Ta2O5 coating on the surface of PI through PDA bonding could improve the biocompatibility as well as bioactivity of PI, and increase the application potential of PI in the field of bone repair materials.
  18. Acetylsalicylic acid-sulfa drugs conjugates as potential urease inhibitors and anti-inflammatory agents: bio-oriented drug synthesis, molecular docking, and dynamics simulation studies
    Ahmad S, Abdul Qadir M, Ahmed M, Imran M, Yousaf N, Asari A, et al.
    J Biomol Struct Dyn, 2023 Aug 29.
    PMID: 37643014 DOI: 10.1080/07391102.2023.2252083
    To explore the new mode of action and reduce side effects, making conjugates of existing drugs is becoming an attractive tool in the realm of medicinal chemistry. In this work, we exploited this approach and synthesized new conjugates to assess their activities against the enzymes involved in different pathological conditions. Specifically, we design and synthesized conjugates involving acetylsalicylic acid and sulfa drugs, validating the newly crafted conjugates using techniques like IR, 1HNMR, 13CNMR, and elemental analysis. These conjugates underwent assessment for their ability to inhibit cyclooxygenase-2 (COX-2), urease enzymes, and their anti-inflammatory potential. A competitive mode of urease inhibition was observed for acetylsalicylic acid conjugated with sulfanilamide, sulfacetamide, and sulfadiazine with IC50 of 2.49 ± 0.35 µM, 6.21 ± 0.28 µM, and 6.57 ± 0.44 µM, respectively. Remarkably, the acetylsalicylic acid-sulfamethoxazole conjugate exhibited exceptional anti-inflammatory activity, effectively curtailing induced edema by 83.7%, a result akin to the reference anti-inflammatory drug indomethacin's performance (86.8%). Additionally, it demonstrated comparable COX-2 inhibition (75.8%) to the reference selective COX-2 inhibitor celecoxib that exhibited 77.1% inhibition at 10 µM concentration. To deepen our understanding, we employed molecular docking techniques to predict the binding interactions of competitive inhibitors with COX-2 and urease receptors. Additionally, MD simulations were carried out, confirming the stability of inhibitor-target complexes throughout the simulation period, devoid of significant conformational changes. Collectively, our research underscores the potential of coupling approved medicinal compounds to usher in novel categories of pharmacological agents, holding promise for addressing a wide spectrum of pathological disorders involving COX-2 and urease enzymes.Communicated by Ramaswamy H. Sarma.
  19. Synthesis, spectral studies and biological evaluation of 2-aminonicotinic acid metal complexes
    Nawaz M, Abbasi MW, Hisaindee S, Zaki MJ, Abbas HF, Mengting H, et al.
    Spectrochim Acta A Mol Biomol Spectrosc, 2016 May 15;161:39-43.
    PMID: 26945123 DOI: 10.1016/j.saa.2016.02.022
    We synthesized 2-aminonicotinic acid (2-ANA) complexes with metals such as Co(II), Fe(III), Ni(II), Mn(II), Zn(II), Ag(I),Cr(III), Cd(II) and Cu(II) in aqueous media. The complexes were characterized and elucidated using FT-IR, UV-Vis, a fluorescence spectrophotometer and thermo gravimetric analysis (TGA). TGA data showed that the stoichiometry of complexes was 1:2 metal/ligand except for Ag(I) and Mn(II) where the ratio was 1:1. The metal complexes showed varied antibacterial, fungicidal and nematicidal activities. The silver and zinc complexes showed highest activity against Bacillus subtilis and Bacillus licheniformis respectively. Fusarium oxysporum was highly susceptible to nickel and copper complexes whereas Macrophomina phaseolina was completely inert to the complexes. The silver and cadmium complexes were effective against the root-knot nematode Meloidogyne javanica.
  20. Fulltext Combined 3D-QSAR, molecular docking and dynamics simulations studies to model and design TTK inhibitors
    Ashraf N, Asari A, Yousaf N, Ahmad M, Ahmed M, Faisal A, et al.
    Front Chem, 2022;10:1003816.
    PMID: 36405310 DOI: 10.3389/fchem.2022.1003816
    Tyrosine threonine kinase (TTK) is the key component of the spindle assembly checkpoint (SAC) that ensures correct attachment of chromosomes to the mitotic spindle and thereby their precise segregation into daughter cells by phosphorylating specific substrate proteins. The overexpression of TTK has been associated with various human malignancies, including breast, colorectal and thyroid carcinomas. TTK has been validated as a target for drug development, and several TTK inhibitors have been discovered. In this study, ligand and structure-based alignment as well as various partial charge models were used to perform 3D-QSAR modelling on 1H-Pyrrolo[3,2-c] pyridine core containing reported inhibitors of TTK protein using the comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) approaches to design better active compounds. Different statistical methods i.e., correlation coefficient of non-cross validation (r2), correlation coefficient of leave-one-out cross-validation (q2), Fisher's test (F) and bootstrapping were used to validate the developed models. Out of several charge models and alignment-based approaches, Merck Molecular Force Field (MMFF94) charges using structure-based alignment yielded highly predictive CoMFA (q2 = 0.583, Predr2 = 0.751) and CoMSIA (q2 = 0.690, Predr2 = 0.767) models. The models exhibited that electrostatic, steric, HBA, HBD, and hydrophobic fields play a key role in structure activity relationship of these compounds. Using the contour maps information of the best predictive model, new compounds were designed and docked at the TTK active site to predict their plausible binding modes. The structural stability of the TTK complexes with new compounds was confirmed using MD simulations. The simulation studies revealed that all compounds formed stable complexes. Similarly, MM/PBSA method based free energy calculations showed that these compounds bind with reasonably good affinity to the TTK protein. Overall molecular modelling results suggest that newly designed compounds can act as lead compounds for the optimization of TTK inhibitors.
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