Displaying publications 21 - 35 of 35 in total

Abstract:
Sort:
  1. Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies
    Taha M, Sultan S, Imran S, Rahim F, Zaman K, Wadood A, et al.
    Bioorg Med Chem, 2019 09 15;27(18):4081-4088.
    PMID: 31378594 DOI: 10.1016/j.bmc.2019.07.035
    In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.
  2. Fulltext Enhancement of mechanical and corrosion resistance properties of electrodeposited Ni-P-TiC composite coatings
    Fayyaz O, Khan A, Shakoor RA, Hasan A, Yusuf MM, Montemor MF, et al.
    Sci Rep, 2021 Mar 05;11(1):5327.
    PMID: 33674680 DOI: 10.1038/s41598-021-84716-6
    In the present study, the effect of concentration of titanium carbide (TiC) particles on the structural, mechanical, and electrochemical properties of Ni-P composite coatings was investigated. Various amounts of TiC particles (0, 0.5, 1.0, 1.5, and 2.0 g L-1) were co-electrodeposited in the Ni-P matrix under optimized conditions and then characterized by employing various techniques. The structural analysis of prepared coatings indicates uniform, compact, and nodular structured coatings without any noticeable defects. Vickers microhardness and nanoindentation results demonstrate the increase in the hardness with an increasing amount of TiC particles attaining its terminal value (593HV100) at the concentration of 1.5 g L-1. Further increase in the concentration of TiC particles results in a decrease in hardness, which can be ascribed to their accumulation in the Ni-P matrix. The electrochemical results indicate the improvement in corrosion protection efficiency of coatings with an increasing amount of TiC particles reaching to ~ 92% at 2.0 g L-1, which can be ascribed to a reduction in the active area of the Ni-P matrix by the presence of inactive ceramic particles. The favorable structural, mechanical, and corrosion protection characteristics of Ni-P-TiC composite coatings suggest their potential applications in many industrial applications.
  3. Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin -induced diabetic albino wistar rats
    Taha M, Imran S, Salahuddin M, Iqbal N, Rahim F, Uddin N, et al.
    Bioorg Chem, 2021 05;110:104808.
    PMID: 33756236 DOI: 10.1016/j.bioorg.2021.104808
    We have synthesized new hybrid class of indole bearing sulfonamide scaffolds (1-17) as α-glucosidase inhibitors. All scaffolds were found to be active except scaffold 17 and exhibited IC50 values ranging from 1.60 to 51.20 µM in comparison with standard acarbose (IC50 = 42.45 µM). Among the synthesized hybrid class scaffolds 16 was the most potent analogue with IC50 value 1.60 μM, showing many folds better potency as compared to standard acarbose. Whereas, synthesized scaffolds 1-15 showed good α-glucosidase inhibitory potential. Based on α-glucosidase inhibitory effect, Scaffold 16 was chosen due to highest activity in vitro for further evaluation of antidiabetic activity in Streptozotocin induced diabetic rats. The Scaffold 16 exhibited significant antidiabetic activity. All analogues were characterized through 1H, 13CNMR and HR MS. Structure-activity relationship of synthesized analogues was established and confirmed through molecular docking study.
  4. Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives
    Taha M, Tariq Javid M, Imran S, Selvaraj M, Chigurupati S, Ullah H, et al.
    Bioorg Chem, 2017 10;74:179-186.
    PMID: 28826047 DOI: 10.1016/j.bioorg.2017.08.003
    α-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as 1HNMR and EI-MS and screened for α-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding α-amylase inhibitory potential with IC50 values ranges between 0.002±0.60 and 42.31±0.17μM which is many folds better than standard acarbose having IC50 value 53.02±0.12μM. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent α-amylase inhibitors for further investigation. Structure activity relationship has been established.
  5. Fulltext Factors Contributing to Chronic Kidney Disease following COVID-19 Diagnosis in Pre-Vaccinated Hospitalized Patients
    Ramatillah DL, Michael M, Khan K, Natasya N, Sinaga E, Hartuti S, et al.
    Vaccines (Basel), 2023 Feb 13;11(2).
    PMID: 36851310 DOI: 10.3390/vaccines11020433
    In this study, we aim to evaluate the factors that may contribute to the development of chronic kidney disease following COVID-19 infection among hospitalized patients in two private hospitals in Jakarta, Indonesia. This is a retrospective cohort study between March 2020 and September 2021. Patient selection was conducted with a convenience sampling. All patients (n = 378) meeting the inclusion criteria during the study period were enrolled. Various sociodemographic, laboratory test, and diagnostic parameters were measured before the determination of their correlation with the outcome of COVID-19 infection. In this study, all pre-vaccinated patients with COVID-19 had no history of chronic kidney disease (CKD) prior to hospital admission. From this number, approximately 75.7% of the patients developed CKD following COVID-19 diagnosis. Overall, significant correlations were established between the clinical outcome and the CKD status (p = 0.001). Interestingly, there was a significant correlation between serum creatinine level, glomerular filtration rate (GFR), and CKD (p < 0.0001). Oxygen saturation (p = 0.03), admission to the intensive care unit (ICU) (p < 0.0001), and sepsis (p = 0.005) were factors that were significantly correlated with CKD status. Additionally, the type of antibiotic agent used was significantly correlated with CKD (p = 0.011). While 82.1% of patients with CKD survived, the survival rate worsened if the patients had complications from hyperuricemia (p = 0.010). The patients who received levofloxacin and ceftriaxone had the highest (100%) survival rate after approximately 50 days of treatment. The patients who received the antiviral agent combination isoprinosine + oseltamivir + ivermectin fared better (100%) as compared to those who received isoprinosine + favipiravir (8%). Factors, such as hyperuricemia and the antibiotic agent used, contributed to CKD following COVID-19 hospitalization. Interestingly, the patients who received levofloxacin + ceftriaxone and the patients without sepsis fared the best. Overall, patients who develop CKD following COVID-19 hospitalization have a low survival rate.
  6. Global and regional mortality statistics of nipah virus from 1994 to 2023: a comprehensive systematic review and meta-analysis
    Vasudevan SS, Subash A, Mehta F, Kandrikar TY, Desai R, Khan K, et al.
    Pathog Glob Health, 2024 Jul 20.
    PMID: 39030703 DOI: 10.1080/20477724.2024.2380131
    The mortality rate of Nipah virus (NiV) can vary in different regions, and its pattern across timelines has yet to be assessed. The primary objective is to perform a comparative analysis of mortality rates across different timelines and countries. Articles reporting NiV mortality from inception to November 2023 were analyzed in PubMed, Ovid Embase, Scopus, and Web of Science databases. A meta-analysis utilizing random-effects models determined the mortality rate secondary to NiV complications. The initial search strategy yielded 1213 records, of which 36 articles met the inclusion criteria, comprising 2736 NiV patients. The Global mortality rate of the Nipah virus in the 2014-2023 decade was 80.1% (CI: 68.7-88.1%), indicating a significant 24% increase compared to the preceding decade (2004-2013) with a mortality rate of 54.1% (CI: 35.5-71.6%). Among the countries analyzed for overall mortality from 1994-2023, India experienced the highest mortality rate at 82.7% (CI: 74.6-88.6%), followed by Bangladesh at 62.1% (CI: 45.6-76.2%), Philippines at 52.9% (CI: 30-74.5%), Malaysia at 28.9% (CI: 21.4-37.9%), and Singapore at 21% (CI: 8-45%). Subgroup analysis revealed that India consistently had the highest mortality rate for the past two decades (91.7% and 89.3%). The primary complication leading to mortality was encephalitis, accounting for 95% of cases. This systematic review and meta-analysis revealed a noteworthy surge in NiV mortality rates, particularly in the current decade (2014-2023). The escalation, with India reporting a concerning level of mortality of 89.3-91.7% in the past decades, signifies a pressing public health challenge.
  7. A review of heavy metals pollution in riverine sediment from various Asian and European countries: Distribution, sources, and environmental risk
    Zeb M, Khan K, Younas M, Farooqi A, Cao X, Kavil YN, et al.
    Mar Pollut Bull, 2024 Sep;206:116775.
    PMID: 39121593 DOI: 10.1016/j.marpolbul.2024.116775
    Riverine sediments are important reservoirs of heavy metals, representing both historical and contemporary anthropogenic activity within the watershed. This review has been conducted to examine the distribution of heavy metals in the surface sediment of 52 riverine systems from various Asian and European countries, as well as to determine their sources and environmental risks. The results revealed significant variability in heavy metal contamination in the world's riverine systems, with certain hotspots exhibiting concentrations that exceeded the permissible limits set by environmental quality standards. Among the studied countries, India has the highest levels of chromium (Cr), cobalt (Co), manganese (Mn), nickel (Ni), zinc (Zn), cadmium (Cd), copper (Cu), and lead (Pb) contamination in its riverine systems, followed by Iran > Turkey > Spain > Vietnam > Pakistan > Malaysia > Taiwan > China > Nigeria > Bangladesh > Japan. Heavy metal pollution in the world's riverine systems was quantified using pollution evaluation indices. The Contamination Factor (CF) revealed moderate contamination (1 ≤ CF  Pakistan > Bangladesh > China > Taiwan > Japan and Iron, while the potential risks of ∑non-carcinogenic Pb, Cr, Ni, Cu, Cd, Co, Zn, and Mn for exposed human children and adults through ingestion and dermal contact were significantly influenced between acceptable to high risk, necessitating special attention from pollution control agencies.
  8. Fulltext Viscosine as a Potent and Safe Antipyretic Agent Evaluated by Yeast-Induced Pyrexia Model and Molecular Docking Studies
    Muhammad A, Khan B, Iqbal Z, Khan AZ, Khan I, Khan K, et al.
    ACS Omega, 2019 Sep 03;4(10):14188-14192.
    PMID: 31508540 DOI: 10.1021/acsomega.9b01041
    The antipyretic potential of viscosine, a natural product isolated from the medicinal plant Dodonaea viscosa, was investigated using yeast-induced pyrexia rat model, and its structure-activity relationship was investigated through molecular docking analyses with the target enzymes cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E synthase-1 (mPGES-1). The in vivo antipyretic experiments showed a progressive dose-dependent reduction in body temperatures of the hyperthermic test animals when injected with viscosine. Comparison of docking analyses with target enzymes showed strongest bonding interactions (binding energy -17.34 kcal/mol) of viscosine with the active-site pocket of mPGES-1. These findings suggest that viscosine shows antipyretic properties by reducing the concentration of prostaglandin E2 in brain through its mPGES-1 inhibitory action and make it a potential lead compound for developing effective and safer antipyretic drugs for treating fever and related pathological conditions.
  9. Broadband Nonlinear Photonics in Few-Layer Borophene
    Ma C, Yin P, Khan K, Tareen AK, Huang R, Du J, et al.
    Small, 2021 Jan 27.
    PMID: 33502109 DOI: 10.1002/smll.202006891
    In this paper, 2D borophene is synthesized through a liquid-phase exfoliation. The morphology and structure of as-prepared borophene are systemically analyzed, and the Z-scan is used to measure the nonlinear optical properties. It is found that the saturable absorber (SA) properties of borophene make it serve as an excellent broadband optical switch, which is strongly used for mode-locking in near- and mid-infrared laser systems. Ultrastable pulses with durations as short as 792 and 693 fs are successfully delivered at the central wavelengths of 1063 and 1560 nm, respectively. Furthermore, stable pulses at a wavelength of 1878 nm are demonstrated from a thulium mode-locked fiber laser based on the same borophene SA. This research reveals a significant potential for borophene used in lasers helping extending the frontiers of photonic technologies.
  10. Syntheses, in vitro α-amylase and α-glucosidase dual inhibitory activities of 4-amino-1,2,4-triazole derivatives their molecular docking and kinetic studies
    Yeye EO, Kanwal, Mohammed Khan K, Chigurupati S, Wadood A, Ur Rehman A, et al.
    Bioorg Med Chem, 2020 06 01;28(11):115467.
    PMID: 32327353 DOI: 10.1016/j.bmc.2020.115467
    Thirty-three 4-amino-1,2,4-triazole derivatives 1-33 were synthesized by reacting 4-amino-1,2,4-triazole with a variety of benzaldehydes. The synthetic molecules were characterized via1H NMR and EI-MS spectroscopic techniques and evaluated for their anti-hyperglycemic potential. Compounds 1-33 exhibited good to moderate in vitro α-amylase and α-glucosidase inhibitory activities in the range of IC50 values 2.01 ± 0.03-6.44 ± 0.16 and 2.09 ± 0.08-6.54 ± 0.10 µM as compared to the standard acarbose (IC50 = 1.92 ± 0.17 µM) and (IC50 = 1.99 ± 0.07 µM), respectively. The limited structure-activity relationship suggested that different substitutions on aryl part of the synthetic compounds are responsible for variable activity. Kinetic study predicted that compounds 1-33 followed mixed and non-competitive type of inhibitions against α-amylase and α-glucosidase enzymes, respectively. In silico studies revealed that both triazole and aryl ring along with different substitutions were playing an important role in the binding interactions of inhibitors within the enzyme pocket. The synthetic molecules were found to have dual inhibitory potential against both enzymes thus they may serve as lead candidates for the drug development and research in the future studies.
  11. Innovations in the synthesis of graphene nanostructures for bio and gas sensors
    Ikram M, Bari MA, Bilal M, Jamal F, Nabgan W, Haider J, et al.
    Biomater Adv, 2023 Feb;145:213234.
    PMID: 36502548 DOI: 10.1016/j.bioadv.2022.213234
    Sensors play a significant role in modern technologies and devices used in industries, hospitals, healthcare, nanotechnology, astronomy, and meteorology. Sensors based upon nanostructured materials have gained special attention due to their high sensitivity, precision accuracy, and feasibility. This review discusses the fabrication of graphene-based biosensors and gas sensors, which have highly efficient performance. Significant developments in the synthesis routes to fabricate graphene-based materials with improved structural and surface properties have boosted their utilization in sensing applications. The higher surface area, better conductivity, tunable structure, and atom-thick morphology of these hybrid materials have made them highly desirable for the fabrication of flexible and stable sensors. Many publications have reported various modification approaches to improve the selectivity of these materials. In the current work, a compact and informative review focusing on the most recent developments in graphene-based biosensors and gas sensors has been designed and delivered. The research community has provided a complete critical analysis of the most robust case studies from the latest fabrication routes to the most complex challenges. Some significant ideas and solutions have been proposed to overcome the limitations regarding the field of biosensors and hazardous gas sensors.
  12. Fulltext Exploring the therapeutic and anti-tumor properties of morusin: a review of recent advances
    Hafeez A, Khan Z, Armaghan M, Khan K, Sönmez Gürer E, Abdull Razis AF, et al.
    Front Mol Biosci, 2023;10:1168298.
    PMID: 37228582 DOI: 10.3389/fmolb.2023.1168298
    Morusin is a natural product that has been isolated from the bark of Morus alba, a species of mulberry tree. It belongs to the flavonoid family of chemicals, which is abundantly present in the plant world and is recognized for its wide range of biological activities. Morusin has a number of biological characteristics, including anti-inflammatory, anti-microbial, neuro-protective, and antioxidant capabilities. Morusin has exhibited anti-tumor properties in many different forms of cancer, including breast, prostate, gastric, hepatocarcinoma, glioblastoma, and pancreatic cancer. Potential of morusin as an alternative treatment method for resistant malignancies needs to be explored in animal models in order to move toward clinical trials. In the recent years several novel findings regarding the therapeutic potential of morusin have been made. This aim of this review is to provide an overview of the present understanding of morusin's beneficial effects on human health as well as provide a comprehensive and up-to-date discussion of morusin's anti-cancer properties with a special focus on in vitro and in vivo studies. This review will aid future research on the creation of polyphenolic medicines in the prenylflavone family, for the management and treatment of cancers.
  13. Fulltext The incidence of acute angle closure in Scotland: a prospective surveillance study
    Chua PY, Day AC, Lai KL, Hall N, Tan LL, Khan K, et al.
    Br J Ophthalmol, 2018 Apr;102(4):539-543.
    PMID: 28794074 DOI: 10.1136/bjophthalmol-2017-310725
    PURPOSE: To estimate the incidence, and describe the clinical features and short-term clinical outcomes of acute angle closure (AAC).

    METHODS: Patients with newly diagnosed AAC were identified prospectively over a 12-month period (November 2011 to October 2012) by active surveillance through the Scottish Ophthalmic Surveillance Unit reporting system. Data were collected at case identification and at 6 months follow-up.

    RESULTS: There were 114 cases (108 patients) reported, giving an annual incidence of 2.2 cases (95% CI 1.8 to 2.6) or 2 patients (95% CI 1.7 to 2.4) per 1 00 000 in the whole population in Scotland. Precipitating factors were identified in 40% of cases. Almost one in five cases was associated with topical dilating drops. Best-corrected visual acuity (BCVA) at presentation ranged from 6/6 to perception of light. The mean presenting intraocular pressure (IOP) was 52 mm Hg (SD 11). Almost 30% cases had a delayed presentation of 3 or more days. At 6 months follow-up, 75% had BCVA of 6/12 or better and 30% were found to have glaucoma at follow-up. Delayed presentation (≥3 days) was associated with higher rate of glaucoma at follow-up (22.6% vs 60.8%, p<0.001), worse VA (0.34 vs 0.74 LogMAR, p<0.0001) and need for more topical medication (0.52 vs 1.2, p=0.003) to control IOP.

    CONCLUSION: The incidence of AAC in Scotland is relatively low compared with the Far East countries, but in line with previous European data. Almost one in five cases were associated with pupil dilation for retinal examination.

  14. Mo-based MXenes: Synthesis, properties, and applications
    Hussain I, Amara U, Bibi F, Hanan A, Lakhan MN, Soomro IA, et al.
    Adv Colloid Interface Sci, 2024 Jan 04;324:103077.
    PMID: 38219341 DOI: 10.1016/j.cis.2023.103077
    Ti-MXene allows a range of possibilities to tune their compositional stoichiometry due to their electronic and electrochemical properties. Other than conventionally explored Ti-MXene, there have been ample opportunities for the non-Ti-based MXenes, especially the emerging Mo-based MXenes. Mo-MXenes are established to be remarkable with optoelectronic and electrochemical properties, tuned energy, catalysis, and sensing applications. In this timely review, we systematically discuss the various organized synthesis procedures, associated experimental tunning parameters, physiochemical properties, structural evaluation, stability challenges, key findings, and a wide range of applications of emerging Mo-MXene over Ti-MXenes. We also critically examined the precise control of Mo-MXenes to cater to advanced applications by comprehensively evaluating the summary of recent studies using artificial intelligence and machine learning tools. The critical future perspectives, significant challenges, and possible outlooks for successfully developing and using Mo-MXenes for various practical applications are highlighted.
  15. Fulltext Immunogenicity of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection and Ad26.CoV2.S Vaccination in People Living With Human Immunodeficiency Virus (HIV)
    Khan K, Lustig G, Bernstein M, Archary D, Cele S, Karim F, et al.
    Clin Infect Dis, 2022 Aug 24;75(1):e857-e864.
    PMID: 34893824 DOI: 10.1093/cid/ciab1008
    BACKGROUND: People living with HIV (PLWH) have been reported to have a higher risk of more severe COVID-19 disease and death. We assessed the ability of the Ad26.CoV2.S vaccine to elicit neutralizing activity against the Delta variant in PLWH relative to HIV-negative individuals. We also examined effects of HIV status and suppression on Delta neutralization response in SARS-CoV-2-infected unvaccinated participants.

    METHODS: We enrolled participants who were vaccinated through the SISONKE South African clinical trial of the Ad26.CoV2.S vaccine in healthcare workers (HCWs). PLWH in this group had well-controlled HIV infection. We also enrolled unvaccinated participants previously infected with SARS-CoV-2. Neutralization capacity was assessed by a live virus neutralization assay of the Delta variant.

    RESULTS: Most Ad26.CoV2.S vaccinated HCWs were previously infected with SARS-CoV-2. In this group, Delta variant neutralization was 9-fold higher compared with the infected-only group and 26-fold higher relative to the vaccinated-only group. No decrease in Delta variant neutralization was observed in PLWH relative to HIV-negative participants. In contrast, SARS-CoV-2-infected, unvaccinated PLWH showed 7-fold lower neutralization and a higher frequency of nonresponders, with the highest frequency of nonresponders in people with HIV viremia. Vaccinated-only participants showed low neutralization capacity.

    CONCLUSIONS: The neutralization response of the Delta variant following Ad26.CoV2.S vaccination in PLWH with well-controlled HIV was not inferior to HIV-negative participants, irrespective of past SARS-CoV-2 infection. In SARS-CoV-2-infected and nonvaccinated participants, HIV infection reduced the neutralization response to SARS-CoV-2, with the strongest reduction in HIV viremic individuals.

Related Terms
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links