Displaying publications 1 - 20 of 36 in total

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  1. Manukaran MN, Ahmad H, Abdullah I
    Med J Malaysia, 1983 Mar;38(1):71-3.
    PMID: 6633343
    A case of amoebiasis with colonic perforation and ruptured liver abscess is reported. It is rare for both these complications to occur in the same patient. The management is described and the literature reviewed
  2. Bukhari SN, Lauro G, Jantan I, Fei Chee C, Amjad MW, Bifulco G, et al.
    Future Med Chem, 2016 Oct;8(16):1953-1967.
    PMID: 27654499
    In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A2, lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages.
  3. Abdella M, Lahiri C, Abdullah I, Anwar A
    Med Chem, 2024;20(2):130-139.
    PMID: 37612861 DOI: 10.2174/1573406419666230823104300
    BACKGROUND: Infectious diseases are the second leading cause of deaths worldwide. Pathogenic bacteria have been developing tremendous resistance against antibiotics which has placed an additional burden on healthcare systems. Gallic acid belongs to a naturally occurring phenolic class of compounds and is known to possess a wide spectrum of antimicrobial activities.

    AIMS & OBJECTIVES: In this study, we synthesized thirteen derivatives of gallic acid and evaluated their antibacterial potential against seven multi-drug resistant bacteria, as well as cytotoxic effects against human embryonic kidney cell line in vitro. Methods: 13 compounds were successfully synthesized with moderate to good yield and evaluated. Synthesized derivatives were characterized by using nuclear magnetic resonance spectroscopy, mass spectrometry, and Fourier transformation infrared spectroscopy. Antibacterial activity was determined using microdilution while cytotoxicyt was assessed using MTT assay.

    RESULTS: The results of antibacterial assay showed that seven out of thirteen compounds exhibited antibacterial effects with compound 6 and 13 being most potent against Staphylococcus aureus (MIC 56 μg/mL) and Salmonella enterica (MIC 475 μg/mL) respectively. On the other hand, most of these compounds showed lower cytotoxicity against human embryonic kidney cells (HEK 293), with IC50 values ranging from over 700 μg/mL.

    CONCLUSION: Notably, compound 13 was found to be non-toxic at concentrations as high as 5000 μg/mL. These findings suggest that the present synthetic derivatives of gallic acid hold potential for further studies in the development of potent antibacterial agents.

  4. Rosli NA, Ahmad I, Anuar FH, Abdullah I
    Carbohydr Polym, 2019 Jun 01;213:50-58.
    PMID: 30879689 DOI: 10.1016/j.carbpol.2019.02.074
    In this study, modified agave cellulose fibre combined by graft copolymerisation with methylmethacrylate was tested as a potential reinforcement for polylactic acid (PLA)-natural rubber/liquid natural rubber blends. Mechanical, morphological, thermal, wetting, and biodegradation characterisations were performed to assess the influence of cellulose-graft-polymethylmethacrylate (cell-g-PMMA) content on the properties of biocomposites. The addition of cell-g-PMMA improved the mechanical properties of the composites because of the chemical interaction between PLA and PMMA. Thermal stability decreased slightly upon cell-g-PMMA addition because of the low thermal stability of PMMA. A soil burial test revealed that the degradation of composites decreased with an increase in the cell-g-PMMA content. However, the weight loss after burial, which directly affected the water absorption capacity, was still higher for the cell-g-PMMA composites than for the polymer alone.
  5. Abdullah I, Chee CF, Lee YK, Thunuguntla SSR, Satish Reddy K, Nellore K, et al.
    Bioorg Med Chem, 2015 Aug 01;23(15):4669-4680.
    PMID: 26088338 DOI: 10.1016/j.bmc.2015.05.051
    Poly (ADP-ribose) polymerases (PARPs) play diverse roles in various cellular processes that involve DNA repair and programmed cell death. Amongst these polymerases is PARP-1 which is the key DNA damage-sensing enzyme that acts as an initiator for the DNA repair mechanism. Dihydroorotate dehydrogenase (DHODH) is an enzyme in the pyrimidine biosynthetic pathway which is an important target for anti-hyperproliferative and anti-inflammatory drug design. Since these enzymes share a common role in the DNA replication and repair mechanisms, it may be beneficial to target both PARP-1 and DHODH in attempts to design new anti-cancer agents. Benzimidazole derivatives have shown a wide variety of pharmacological activities including PARP and DHODH inhibition. We hereby report the design, synthesis and bioactivities of a series of benzimidazole derivatives as inhibitors of both the PARP-1 and DHODH enzymes.
  6. Saleem F, Mehmood R, Mehar S, Khan MTJ, Khan ZU, Ashraf M, et al.
    Antioxidants (Basel), 2019 Jul 19;8(7).
    PMID: 31331076 DOI: 10.3390/antiox8070231
    Members of genus Pteris have their established role in the traditional herbal medicine system. In the pursuit to identify its biologically active constituents, the specie Pteris cretica L. (P. cretica) was selected for the bioassay-guided isolation. Two new maleates (F9 and CB18) were identified from the chloroform extract and the structures of the isolates were elucidated through their spectroscopic data. The putative targets, that potentially interact with both of these isolates, were identified through reverse docking by using in silico tools PharmMapper and ReverseScreen3D. On the basis of reverse docking results, both isolates were screened for their antioxidant, acetylcholinesterase (AChE) inhibition, α-glucosidase (GluE) inhibition and antibacterial activities. Both isolates depicted moderate potential for the selected activities. Furthermore, docking studies of both isolates were also studied to investigate the binding mode with respective targets followed by molecular dynamics simulations and binding free energies. Thereby, the current study embodies the poly-pharmacological potential of P. cretica.
  7. Tehami M, Imam HT, Abdullah I, Hosford J, Wong XJ, Rahman NA, et al.
    ACS Sustain Chem Eng, 2024 Feb 19;12(7):2678-2685.
    PMID: 38389905 DOI: 10.1021/acssuschemeng.3c06758
    1,4-Benzoxazines are important motifs in many pharmaceuticals and can be formed by a reaction sequence involving the oxidation of o-aminophenols to their corresponding quinone imine followed by an in situ inverse electron demand Diels-Alder (IEDDA) cycloaddition with a suitable dienophile. Reported herein is the development of a reaction sequence that employs horseradish peroxidase to catalyze the oxidation of the aminophenols prior to the IEDDA as a more sustainable alternative to the use of conventional stoichiometric oxidants. The synthesis of 10 example benzoxazines is demonstrated in this "one-pot, two-step" procedure with yields between 42% and 92%. The green chemistry metrics, including the E-factor and generalized reaction mass efficiency, for this biocatalytic reaction were compared against the conventional chemical approach. It was found that the reported biocatalytic route was approximately twice as green by these measures.
  8. Anwar A, Ma'amor A, Mahmud HNME, Basirun WJ, Abdullah I
    Turk J Chem, 2022;46(3):730-746.
    PMID: 37720623 DOI: 10.55730/1300-0527.3363
    The oxidation of ethylbenzene (EB) using tert-butyl hydroperoxide as the oxidizing agent was carried out in presence of gold nanoparticles (3 nm) supported on zinc oxide in acetonitrile solution. A higher selectivity towards acetophenone (ACP) as the major product, and a moderate selectivity towards other products such as 1-phenylethanol (PE), benzaldehyde (BZL), and benzoic acid (BzA) were observed using the prepared Au/ZnO nanocatalysts at 100 °C for 24 h. It is suggested the reaction produces an intermediate product, which is dimethylethyl-1-phenylethyl peroxide through a radical mechanism. A small amount of benzaldehyde was observed because benzaldehyde went autoxidation to form benzoic acid with the presence of oxidation agent of TBHP during reaction. The factors affecting the catalytic activity such as gold loading, calcination treatment at 300°C, type of solvent, reaction time, reaction temperature, oxidant to substrate molar ratio, catalyst weight, and solvent volume were studied. The gold nanoparticle catalyst synthesized by deposition precipitation method using urea was characterized by XRD, HRTEM, ATR-IR, XRF, and BET and offers a very selective reaction pathway for the oxidation of ethylbenzene.
  9. Hussain AI, Rathore HA, Sattar MZ, Chatha SA, Sarker SD, Gilani AH
    J Ethnopharmacol, 2014 Aug 8;155(1):54-66.
    PMID: 24936768 DOI: 10.1016/j.jep.2014.06.011
    Citrullus colocynthis (L.) Schrad is a valuable cucurbit plant, widely distributed in the desert areas of the world. Citrullus colocynthis fruits are usually recognized for its wide range of medicinal uses as well as pharmaceutical and nutraceutical potential. This review aims to appraise the published information on the ethnobotanical knowledge, phytochemistry, ethnopharmacology, nutraceutical potential and safety studies of Citrullus colocynthis (bitter apple) fruit, with critical analysis on the gaps and potential for future studies.
  10. Dala Ali AHH, Harun SN, Othman N, Ibrahim B, Abdulbagi OE, Abdullah I, et al.
    Antibiotics (Basel), 2023 Aug 10;12(8).
    PMID: 37627725 DOI: 10.3390/antibiotics12081305
    In the management of sepsis, providing adequate empiric antimicrobial therapy is one of the most important pillars of sepsis management. Therefore, it is important to evaluate the adequacy of empiric antimicrobial therapy (EAMT) in sepsis patients admitted to intensive care units (ICU) and to identify the determinants of inadequate EAMT. The aim of this study was to evaluate the adequacy of empiric antimicrobial therapy in patients admitted to the ICU with sepsis or septic shock, and the determinants of inadequate EAMT. The data of patients admitted to the ICU units due to sepsis or septic shock in two tertiary healthcare facilities in Al-Madinah Al-Munawwarah were retrospectively reviewed. The current study used logistic regression analysis and artificial neural network (ANN) analysis to identify determinants of inadequate empiric antimicrobial therapy, and evaluated the performance of these two approaches in predicting the inadequacy of EAMT. The findings of this study showed that fifty-three per cent of patients received inadequate EAMT. Determinants for inadequate EAMT were APACHE II score, multidrug-resistance organism (MDRO) infections, surgical history (lower limb amputation), and comorbidity (coronary artery disease). ANN performed as well as or better than logistic regression in predicating inadequate EAMT, as the receiver operating characteristic area under the curve (ROC-AUC) of the ANN model was higher when compared with the logistic regression model (LRM): 0.895 vs. 0.854. In addition, the ANN model performed better than LRM in predicting inadequate EAMT in terms of classification accuracy. In addition, ANN analysis revealed that the most important determinants of EAMT adequacy were the APACHE II score and MDRO. In conclusion, more than half of the patients received inadequate EAMT. Determinants of inadequate EAMT were APACHE II score, MDRO infections, comorbidity, and surgical history. This provides valuable inputs to improve the prescription of empiric antimicrobials in Saudi Arabia going forward. In addition, our study demonstrated the potential utility of applying artificial neural network analysis in the prediction of outcomes in healthcare research.
  11. Mirza MU, Saadabadi A, Vanmeert M, Salo-Ahen OMH, Abdullah I, Claes S, et al.
    Eur J Pharm Sci, 2020 Dec 01;155:105537.
    PMID: 32890663 DOI: 10.1016/j.ejps.2020.105537
    Chemokine receptors are key regulators of cell migration in terms of immunity and inflammation. Among these, CCR5 and CXCR4 play pivotal roles in cancer metastasis and HIV-1 transmission and infection. They act as essential co-receptors for HIV and furnish a route to the cell entry. In particular, inhibition of either CCR5 or CXCR4 leads very often the virus to shift to a more virulent dual-tropic strain. Therefore, dual receptor inhibition might improve the therapeutic strategies against HIV. In this study, we aimed to discover selective CCR5, CXCR4, and dual CCR5/CXCR4 antagonists using both receptor- and ligand-based computational methods. We employed this approach to fully incorporate the interaction attributes of the binding pocket together with molecular dynamics (MD) simulations and binding free energy calculations. The best hits were evaluated for their anti-HIV-1 activity against CXCR4- and CCR5-specific NL4.3 and BaL strains. Moreover, the Ca2+ mobilization assay was used to evaluate their antagonistic activity. From the 27 tested compounds, three were identified as inhibitors: compounds 27 (CCR5), 6 (CXCR4) and 3 (dual) with IC50 values ranging from 10.64 to 64.56 μM. The binding mode analysis suggests that the active compounds form a salt bridge with the glutamates and π-stacking interactions with the aromatic side chains binding site residues of the respective co-receptor. The presented hierarchical virtual screening approach provides essential aspects in identifying potential antagonists in terms of selectivity against a specific co-receptor. The compounds having multiple heterocyclic nitrogen atoms proved to be relatively more specific towards CXCR4 inhibition as compared to CCR5. The identified compounds serve as a starting point for further development of HIV entry inhibitors through synthesis and quantitative structure-activity relationship studies.
  12. Takhi M, Sreenivas K, Reddy CK, Munikumar M, Praveena K, Sudheer P, et al.
    Eur J Med Chem, 2014 Sep 12;84:382-94.
    PMID: 25036796 DOI: 10.1016/j.ejmech.2014.07.036
    A novel and potent series of ene-amides featuring azetidines has been developed as FabI inhibitors active against drug resistant Gram-positive pathogens particularly staphylococcal organisms. Most of the compounds from the series possessed excellent biochemical inhibition of Staphylococcus aureus FabI enzyme and whole cell activity against clinically relevant MRSA, MSSA and MRSE organisms which are responsible for significant morbidity and mortality in community as well as hospital settings. The binding mode of one of the leads, AEA16, in Escherichia coli FabI enzyme was determined unambiguously using X-ray crystallography. The lead compounds displayed good metabolic stability in mice liver microsomes and pharmacokinetic profile in mice. The in vivo efficacy of lead AEA16 has been demonstrated in a lethal murine systemic infection model.
  13. Ilyas S, Tabasum R, Iftikhar A, Nazir M, Hussain A, Hussain A, et al.
    Sci Rep, 2021 01 18;11(1):1708.
    PMID: 33462261 DOI: 10.1038/s41598-020-80579-5
    Ifosfamide is a widely used chemotherapeutic agent having broad-spectrum efficacy against several tumors. However, nephro, hepato, neuro cardio, and hematological toxicities associated with ifosfamide render its use limited. These side effects could range from organ failure to life-threatening situations. The present study aimed to evaluate the attenuating efficiency of Berberis vulgaris root extract (BvRE), a potent nephroprotective, hepatoprotective, and lipid-lowering agent, against ifosfamide-induced toxicities. The study design comprised eight groups of Swiss albino rats to assess different dose regimes of BvRE and ifosfamide. Biochemical analysis of serum (serum albumin, blood urea nitrogen, creatinine, alanine transaminase, aspartate transaminase, alkaline phosphatase, lactate dehydrogenase, total cholesterol, and triglycerides) along with complete blood count was performed. Kidney, liver, brain, and heart tissue homogenates were used to find malondialdehyde, catalase, and glutathione S-transferase levels in addition to the acetylcholinesterase of brain tissue. The results were further validated with the help of the histopathology of the selected organs. HeLa cells were used to assess the effect of BvRE on ifosfamide cytotoxicity in MTT assay. The results revealed that pre- and post-treatment regimens of BvRE, as well as the combination therapy exhibited marked protective effects against ifosfamide-induced nephro, hepato, neuro, and cardiotoxicity. Moreover, ifosfamide depicted a synergistic in vitro cytotoxic effect on HeLa cells in the presence of BvRE. These results corroborate that the combination therapy of ifosfamide with BvRE in cancer treatment can potentiate the anticancer effects of ifosfamide along with the amelioration of its conspicuous side effects.
  14. Abdullah I, AlMojil K, Shehab M
    Diseases, 2022 Nov 09;10(4).
    PMID: 36412596 DOI: 10.3390/diseases10040102
    Inflammatory bowel disease (IBD) is a chronic autoimmune disease with relapse-remission courses. A number of patients may present with a refractory disease with partial or no response to treatment. Others may present with extra-intestinal manifestations that makes the treatment with one biologic challenging. Dual target therapy (DTT), combining biologics and/or small molecule drugs, may offer a chance to achieve remission in these cases and improve patients' quality of life despite the limited evidence regarding this approach. We present a case series of refractory inflammatory bowel disease cases managed with DTT. Seven patients with refractory IBD achieved steroid free, clinical, and endoscopic remission by using DTT. These results support that DTT could be an effective approach in selected patients with refractory IBD or with concomitant extra-intestinal manifestations (EIM). Larger studies, ideally randomized controlled trials, are needed to further support the evidence and confirm the efficacy and safety of DTT for IBD.
  15. Mekzali NW, Chee CW, Abdullah I, Lee YK, Rashid NN, Lee VS, et al.
    Med Chem, 2023;19(9):897-905.
    PMID: 37046198 DOI: 10.2174/1573406419666230410134213
    BACKGROUND: KRAS and p53 are two of the most common genetic alterations associated with colorectal cancer. New drug development targeting these mutated genes in colorectal cancer may serve as a potential treatment avenue to the current regimen.

    OBJECTIVE: The objective of the present study was to investigate the effects of alkoxy chain length and 1-hydroxy group on anticolorectal cancer activity of a series of 2-bromoalkoxyanthraquinones and corroborate it with their in silico properties.

    METHODS: In vitro anticancer activity of 2-bromoalkoxyanthraquinones was evaluated against HCT116, HT29, and CCD841 CoN cell lines, respectively. Molecular docking was performed to understand the interactions of these compounds with putative p53 and KRAS targets (7B4N and 6P0Z).

    RESULTS: 2-Bromoalkoxyanthraquinones with the 1-hydroxy group were proven to be more active than the corresponding counterparts in anticancer activity. Among the tested compounds, compound 6b with a C3 alkoxy chain exhibited the most promising antiproliferation activity against HCT116 cells (IC50 = 3.83 ± 0.05 μM) and showed high selectivity for HCT116 over CCD841 CoN cells (SI = 45.47). The molecular docking reveals additional hydrogen bonds between the 1-hydroxy group of 6b and the proteins. Compound 6b has adequate lipophilicity (cLogP = 3.27) and ligand efficiency metrics (LE = 0.34; LLE = 2.15) close to the proposed acceptable range for an initial hit.

    CONCLUSION: This work highlights the potential of the 1-hydroxy group and short alkoxy chain on anticolorectal cancer activity of 2-bromoalkoxyanthraquinones. Further optimisation may be warranted for compound 6b as a therapeutic agent against colorectal cancer.

  16. Li H, Khoury M, Bonef B, Alhassan AI, Mughal AJ, Azimah E, et al.
    ACS Appl Mater Interfaces, 2017 Oct 18;9(41):36417-36422.
    PMID: 28960058 DOI: 10.1021/acsami.7b11718
    We demonstrate efficient semipolar (11-22) 550 nm yellow/green InGaN light-emitting diodes (LEDs) with In0.03Ga0.97N barriers on low defect density (11-22) GaN/patterned sapphire templates. The In0.03Ga0.97N barriers were clearly identified, and no InGaN clusters were observed by atom probe tomography measurements. The semipolar (11-22) 550 nm InGaN LEDs (0.1 mm2 size) show an output power of 2.4 mW at 100 mA and a peak external quantum efficiency of 1.3% with a low efficiency drop. In addition, the LEDs exhibit a small blue-shift of only 11 nm as injection current increases from 5 to 100 mA. These results suggest the potential to produce high efficiency semipolar InGaN LEDs with long emission wavelength on large-area sapphire substrates with economical feasibility.
  17. Ghalib, H., Abdullah, I., Daik, R.
    MyJurnal
    Conducting polypyrrole (PPy) nanoparticles were synthesized by chemical oxidative polymerization of pyrrole in aqueous solution containing ferric sulfate (Fe2(SO4)3), anionic surfactants (sodium dodecylbenzene-sulfonate (NaDBS) or sodium dodecyl sulfate (SDS)), 1-pentanol as the oxidant, dopant and co-emulsifier, respectively. The polymerization was carried out at 0 ºC and 25 ºC. Fourier transform infrared spectroscopy (FTIR) and elemental analysis indicated that anionic surfactants were successfully incorporated into the PPy backbone. Incorporation of anionic surfactants caused enhanced electrical conductivity, increased yield, decreased the size of particles as well as improved the thermal stability of the resultant PPy. The presence of anionic surfactant seems to inhibit undesirable side reactions so as to improve the regularity of the PPy backbone. Globular PPy particles were obtained with diameter ranged from 40 to 118 nm as revealed by field emission scanning electron microscopy (FE-SEM) and conductivity of 7.89×10-4 –2.35×10-2 S cm-1, as measured using impedance analyzer. It was found that polymerization at low temperature (0 ºC) produced PPy particles with smaller size and higher conductivity. The sodium dodecyl sulfate-doped PPy (SDS-doped PPy) exhibited higher conductivity than that of the sodium dodecylbenzenesulfonate-doped PPy (NaDBS-doped PPy), due to the bulkiness of NaDBS as compared to SDS.
  18. Bahari HMM, Abdullah I
    Med J Malaysia, 1982 Dec;37(4):316-7.
    PMID: 7167081
    There are many techniques of drainage of a pseudopancreatic cyst. We are describing a new method of drainage by an endoscopic transgastric route.
  19. Navookarasu NT, Rahman AR, Abdullah I
    Int J Clin Pract, 1999 Jan-Feb;53(1):25-30.
    PMID: 10344062
    Despite their proven value in reducing morbidity and mortality in different grades of heart failure, angiotensin converting enzyme (ACE) inhibitors continue to be underused. One reason for this is clinicians' apprehension of first-dose hypotension. We conducted a double-blind, randomised, placebo-controlled parallel group study to investigate the effect of various ACE inhibitors on first-dose hypotension. Eighty unselected patients were randomised into five treatment groups: placebo, captopril 6.25 mg, enalapril 2.5 mg, perindopril 2 mg and lisinopril 2.5 mg. Blood pressure was measured at baseline, half hourly for two hours and hourly for three hours after drug treatment. The maximum drops in mean arterial pressure (in mmHg +/- SD) were placebo 5.89 +/- 2.65, perindopril 5.29 +/- 2.49, enalapril 13.28 +/- 3.31, lisinopril 15.04 +/- 5.74 and captopril 16.76 +/- 5.74 (all p < 0.05 vs placebo except for perindopril). Perindopril, unlike the other ACE inhibitors studied, did not produce first-dose hypotension following its initiation in patients with congestive heart failure.
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