Displaying publications 201 - 220 of 292 in total

Abstract:
Sort:
  1. Fulltext Induction, Multiplication, and Evaluation of Antioxidant Activity of Polyalthia bullata Callus, a Woody Medicinal Plant
    Kamarul Zaman MA, Azzeme AM, Ramle IK, Normanshah N, Ramli SN, Shaharuddin NA, et al.
    Plants (Basel), 2020 Dec 14;9(12).
    PMID: 33327608 DOI: 10.3390/plants9121772
    Polyalthia bullata is an endangered medicinal plant species. Hence, establishment of P. bullata callus culture is hoped to assist in mass production of secondary metabolites. Leaf and midrib were explants for callus induction. Both of them were cultured on Murashige and Skoog (MS) and Woody Plant Medium (WPM) containing different types and concentrations of auxins (2,4-dichlorophenoxyacetic acid (2,4-D), α-naphthaleneacetic acid (NAA), picloram, and dicamba). The callus produced was further multiplied on MS and WPM supplemented with different concentrations of 2,4-D, NAA, picloram, dicamba, indole-3-acetic acid (IAA), and indole-3-butyric acid (IBA) media. The quantification of total phenolic content (TPC), total flavonoid content (TFC) and antioxidant capacity was further carried out on P. bullata callus, and the results were subjected to correlation analysis. Among the media, the WPM + 16.56 µM picloram (53.33 ± 22.06%) was the best for callus induction while MS + 30 µM dicamba was the best for callus multiplication. The TPC, TFC, and EC50 of DPPH scavenging activity were determined at 0.657 ± 0.07 mg GAE/g FW, 0.491 ± 0.03 mg QE/g, and 85.59 ± 6.09 µg/mL in P. bullata callus, respectively. The positive correlation between DPPH scavenging activity with TPC was determined at r = 0.869, and that of TFC was at r = 0.904. Hence, the P. bullata callus has an ability to accumulate antioxidants. It therefore can be a medium for secondary metabolites production.
  2. Fulltext Ageing in Pgc-1β-/- mice modelling mitochondrial dysfunction induces differential expression of a range of genes regulating ventricular electrophysiology
    Edling CE, Fazmin IT, Chadda KR, Ahmad S, Valli H, Grace AA, et al.
    Biosci Rep, 2019 04 30;39(4).
    PMID: 30914453 DOI: 10.1042/BSR20190127
    Mice deficient in mitochondrial promoter peroxisome proliferator activated receptor-γ co-activator-1β (Pgc-1β-/- ) is a valuable model for metabolic diseases and has been found to present with several pathologies including ventricular arrhythmia. In the present study, our aim was to shed light on the molecular mechanisms behind the observed arrhythmic substrate by studying how the expression of selected genes critical for cardiac function differs in wild-type (WT) compared with Pgc-1β knockout mice and young compared with aged mice. We found that a clear majority of genes are down-regulated in the Pgc-1β-/- ventricular tissue compared with the WT. Although most individual genes are not significantly differentially expressed, a pattern is apparent when the genes are grouped according to their functional properties. Genes encoding proteins relating to ATPase activity, potassium ion channels relating to repolarisation and resting membrane potential, and genes encoding proteins in the cAMP pathway are found to be significantly down-regulated in the Pgc-1β deficient mice. On the contrary, the pacemaker channel genes Hcn3 and Hcn4 are up-regulated in subsets of the Pgc-1β deficient tissue. Furthermore, we found that with age, especially in the Pgc-1β-/- genotype, most genes are up-regulated including genes relating to the resting membrane potential, calcium homeostasis, the cAMP pathway, and most of the tested adrenoceptors. In conclusion, we here demonstrate how a complex pattern of many modest changes at gene level may explain major functional differences of the action potential related to ageing and mitochondrial dysfunction.
  3. Fulltext Isolation of Antidiabetic Withanolides from Withania coagulans Dunal and Their In Vitro and In Silico Validation
    Maher S, Choudhary MI, Saleem F, Rasheed S, Waheed I, Halim SA, et al.
    Biology (Basel), 2020 Jul 30;9(8).
    PMID: 32751610 DOI: 10.3390/biology9080197
    Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC50 = 66.7 ± 3.6 µM, followed by compound 4 (IC50: 407 ± 4.5 µM) and compound 2 (IC50: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans.
  4. New naphthalene derivative for cost-effective AChE inhibitors for Alzheimer's treatment: In silico identification, in vitro and in vivo validation
    Anwar F, Saleem U, Ahmad B, Ashraf M, Rehman AU, Froeyen M, et al.
    Comput Biol Chem, 2020 Dec;89:107378.
    PMID: 33002716 DOI: 10.1016/j.compbiolchem.2020.107378
    Neurodegenerative diseases have complex etiology and pose a challenge to scientists to develop simple and cost-effective synthetic compounds as potential drug candidates for such diseases. Here, we report an extension of our previously published in silico screening, where we selected four new compounds as AChE inhibitors. Further, based on favorable binding possess, MD simulation and MMGBSA, two most promising compounds (3a and 3b) were selected, keeping in view the ease of synthesis and cost-effectiveness. Due to the critical role of BChE, LOX and α-glucosidase in neurodegeneration, the selected compounds were also screened against these enzymes. The IC50 values of 3a against AChE and BChE found to be 12.53 and 352.42 μM, respectively. Moderate to slight inhibitions of 45.26 % and 28.68 % were presented by 3a against LOX and α-glucosidase, respectively, at 0.5 mM. Insignificant inhibitions were observed with 3b against the four selected enzymes. Further, in vivo trial demonstrated that 3a could significantly diminish AChE levels in the mice brain as compared to the control. These findings were in agreement with the histopathological analysis of the brain tissues. The results corroborate that selected compounds could serve as a potential lead for further development and optimization as AChE inhibitors to achieve cost-effective anti-Alzheimer's drugs.
  5. New class of acetylcholinesterase inhibitors from the stem bark of Knema laurina and their structural insights
    Akhtar MN, Lam KW, Abas F, Maulidiani, Ahmad S, Shah SA, et al.
    Bioorg Med Chem Lett, 2011 Jul 1;21(13):4097-103.
    PMID: 21641207 DOI: 10.1016/j.bmcl.2011.04.065
    Bioassay-guided extraction of the stem bark of Knema laurina showed the acetylcholinesterase (AChE) inhibitory activity of DCM and hexane fractions. Further repeated column chromatography of hexane and DCM fractions resulted in the isolation and purification of five alkenyl phenol and salicylic acid derivatives. New compounds, (+)-2-hydroxy-6-(10'-hydroxypentadec-8'(E)-enyl)benzoic acid (1) and 3-pentadec-10'(Z)-enylphenol (2), along with known 3-heptadec-10'(Z)-enylphenol (3), 2-hydroxy-6-(pentadec-10'(Z)-enyl)benzoic acid (4), and 2-hydroxy-6-(10'(Z)-heptadecenyl)benzoic acid (5) were isolated from the stem bark of this plant. Compounds (1-5) were tested for their acetylcholinesterase inhibitory activity. The structures of these compounds were elucidated by the 1D and 2D NMR spectroscopy, mass spectrometry and chemical derivatizations. Compound 5 showed strong acetylcholinesterase inhibitory activity with IC(50) of 0.573 ± 0.0260 μM. Docking studies of compound 5 indicated that the phenolic compound with an elongated side chain could possibly penetrate deep into the active site of the enzyme and arrange itself through π-π interaction, H-bonding, and hydrophobic contacts with some critical residues along the complex geometry of the active gorge.
  6. Fulltext Factors Associated with Happiness among Malaysian Elderly
    Shah SA, Safian N, Ahmad S, Wan Ibadullah WAH, Mohammad ZB, Nurumal SR, et al.
    Int J Environ Res Public Health, 2021 04 06;18(7).
    PMID: 33917528 DOI: 10.3390/ijerph18073831
    Happiness is an essential component to experience healthy ageing. Hence, understanding the factors that contribute to happiness is important. This study aimed to determine the factors associated with happiness among the elderly population in Malaysia. In this study, 1204 respondents were recruited from urban and rural areas in Selangor. A face-to-face interview was conducted using the Bahasa Malaysia version of the Japan Gerontological Evaluation Study questionnaire. The inclusion criteria include Malaysians who are 60-years old and above and can converse in the Malaysian language. Those who encounter less than seven scores for the Abbreviated Mental Test were excluded from the study. Among the 1204 respondents, 953 (79.2%) were happy. Sociodemographic characteristics showed that being a men, age of 60 to 74 years, and living in urban areas were significantly associated with happiness. A logistic regression model showed that locality (aOR 1.61), income category (Bottom 40% aOR 0.49; Middle-class group 40% aOR 1.40), social engagement (active aOR 1.77; less active aOR 1.25), receiving emotional support (aOR 2.11) and handgrip strength (aOR 1.02) were significantly associated with happiness. Thus, ensuring the elderly population in receiving emotional support and active social engagement among them can enhance their happiness level.
  7. Fulltext Antimutagenic, Cytoprotective and Antioxidant Properties of Ficus deltoidea Aqueous Extract In Vitro
    Ooi TC, Ibrahim FW, Ahmad S, Chan KM, Leong LM, Mohammad N, et al.
    Molecules, 2021 May 29;26(11).
    PMID: 34072474 DOI: 10.3390/molecules26113287
    Ficus deltoidea var. deltoidea is used as traditional medicine for diabetes, inflammation, and nociception. However, the antimutagenic potential and cytoprotective effects of this plant remain unknown. In this study, the mutagenic and antimutagenic activities of F. deltoidea aqueous extract (FDD) on both Salmonella typhimurium TA 98 and TA 100 strains were assessed using Salmonella mutagenicity assay (Ames test). Then, the cytoprotective potential of FDD on menadione-induced oxidative stress was determined in a V79 mouse lung fibroblast cell line. The ferric-reducing antioxidant power (FRAP) assay was conducted to evaluate FDD antioxidant capacity. Results showed that FDD (up to 50 mg/mL) did not exhibit a mutagenic effect on either TA 98 or TA 100 strains. Notably, FDD decreased the revertant colony count induced by 2-aminoanthracene in both strains in the presence of metabolic activation (p < 0.05). Additionally, pretreatment of FDD (50 and 100 µg/mL) demonstrated remarkable protection against menadione-induced oxidative stress in V79 cells significantly by decreasing superoxide anion level (p < 0.05). FDD at all concentrations tested (12.5-100 µg/mL) exhibited antioxidant power, suggesting the cytoprotective effect of FDD could be partly attributed to its antioxidant properties. This report highlights that F. deltoidea may provide a chemopreventive effect on mutagenic and oxidative stress inducers.
  8. Fulltext Discovery of HIV entry inhibitors via a hybrid CXCR4 and CCR5 receptor pharmacophore-based virtual screening approach
    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.
  9. Fulltext Toxicity Evaluation of the Naphthalen-2-yl 3,5-Dinitrobenzoate: A Drug Candidate for Alzheimer Disease
    Anwar F, Saleem U, Rehman AU, Ahmad B, Froeyen M, Mirza MU, et al.
    Front Pharmacol, 2021;12:607026.
    PMID: 34040515 DOI: 10.3389/fphar.2021.607026
    The presented study was designed to probe the toxicity potential of newly identified compound naphthalen-2-yl 3,5-dinitrobenzoate (SF1). Acute, subacute toxicity and teratogenicity studies were performed as per Organization of economic cooperation and development (OECD) 425, 407, and 414 test guidelines, respectively. An oral dose of 2000 mg/kg to rats for acute toxicity. Furthermore, 5, 10, 20, and 40 mg/kg doses were administered once daily for 28 days in subacute toxicity study. Teratogenicity study was performed with 40 mg/kg due to its excellent anti-Alzheimer results at this dose. SF1 induced a significant rise in Alkaline Phosphatases (ALP), bilirubin, white blood cells (WBC), and lymphocyte levels with a decrease in platelet count. Furthermore, the reduction in urea, uric acid, and aspartate transaminase (AST) levels and an increase in total protein levels were measured in subacute toxicity. SF1 increased spermatogenesis at 5 and 10 mg/kg doses. Teratogenicity study depicted no resorptions, early abortions, cleft palate, spina bifida and any skeletal abnormalities in the fetuses. Oxidative stress markers (Superoxide dismutase (SOD), Catalase (CAT), and glutathione (GSH) were increased in all the experiments, whereas the effect on melanoaldehyde Malondialdehyde (MDA) levels was variable. Histopathology further corroborated these results with no change in the architectures of selected organs. Consequently, a 2000 mg/kg dose of SF1 tends to induce minor liver dysfunction along with immunomodulation, and it is well below its LD
    50
    . Moreover, it can be safely used in pregnancy owing to its no detectable teratogenicity.
  10. Fulltext Corrigendum to 'Discovery of HIV entry inhibitors via a hybrid CXCR4 and CCR5 receptor pharmacophore-based virtual screening approach' [European Journal of Pharmaceutical Sciences 155 (2020) 105537]
    Mirza MU, Saadabadi A, Vanmeert M, Salo-Ahen OMH, Abdullah I, Claes S, et al.
    Eur J Pharm Sci, 2021 Jul 01;162:105827.
    PMID: 33814256 DOI: 10.1016/j.ejps.2021.105827
  11. Selective dual cholinesterase inhibitors from Aconitum laeve
    Ahmad H, Ahmad S, Shah SAA, Khan HU, Khan FA, Ali M, et al.
    J Asian Nat Prod Res, 2018 Feb;20(2):172-181.
    PMID: 28463565 DOI: 10.1080/10286020.2017.1319820
    New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 μM, 4.53 μM) and BChE (IC50 = 12.23 μM, 9.94 μM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 μM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.
  12. Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum
    Ahmad H, Ahmad S, Shah SAA, Latif A, Ali M, Khan FA, et al.
    Bioorg Med Chem, 2017 07 01;25(13):3368-3376.
    PMID: 28457693 DOI: 10.1016/j.bmc.2017.04.022
    Extensive chromatographic separations performed on the basic (pH=8-10) chloroform soluble fraction of Aconitum heterophyllum resulted in the isolation of three new diterpenoid alkaloids, 6β-Methoxy, 9β-dihydroxylheteratisine (1), 1α,11,13β-trihydroxylhetisine (2), 6,15β-dihydroxylhetisine (3), and the known compounds iso-atisine (4), heteratisine (5), hetisinone (6), 19-epi-isoatisine (7), and atidine (8). Structures of the isolated compounds were established by means of mass and NMR spectroscopy as well as single crystal X-ray crystallography. Compounds 1-8 were screened for their antioxidant and enzyme inhibition activities followed by in silico studies to find out the possible inhibitory mechanism of the tested compounds. This work is the first report demonstrating significant antioxidant and anticholinesterase potentials of diterpenoid alkaloids isolated from a natural source.
  13. Norditerpenoid alkaloids of Delphinium denudatum as cholinesterase inhibitors
    Ahmad H, Ahmad S, Ali M, Latif A, Shah SAA, Naz H, et al.
    Bioorg Chem, 2018 08;78:427-435.
    PMID: 29698893 DOI: 10.1016/j.bioorg.2018.04.008
    Three new norditerpenoids alkaloids, 1β-hydroxy,14β-acetyl condelphine (1), jadwarine-A (2), jadwarine-B (3) along with two known alkaloids isotalatizidine hydrate (4) and dihydropentagynine (5) were isolated from medicinal plant Delphinium denudatum. The structures of natural products 1-5 were established on the basis of HR-EIMS, 1H and 13C NMR (1D & 2D) spectroscopic data as well as by comparison from literature data. The structures of compound 1 and 4 were also confirmed by single crystal X-ray diffraction studies. In-vitro AChE and BChE enzyme inhibitory activities of compounds 1-5 and molecular docking studies were performed to investigate the possible molecular inhibitory mechanism of the isolated natural products. Compound 2, 4 and 5 showed competitive inhibitory effects by inhibiting AChE and BChE, respectively, while 1 and 3 showed non-competitive inhibition. This work is the first report that provides a supporting evidence about the use of constituents of Delphinium denudatum in cerebral dementia and Alzheimer diseases.
  14. Fulltext In silico and in vivo characterization of cabralealactone, solasodin and salvadorin in a rat model: potential anti-inflammatory agents
    Malik A, Arooj M, Butt TT, Zahid S, Zahid F, Jafar TH, et al.
    Drug Des Devel Ther, 2018;12:1431-1443.
    PMID: 29872266 DOI: 10.2147/DDDT.S154169
    Background: The present study investigates the hepato- and DNA-protective effects of standardized extracts of Cleome brachycarpa (cabralealactone), Solanum incanum (solasodin), and Salvadora oleioides (salvadorin) in rats.

    Materials and methods: Hepatotoxicity was induced with intraperitoneal injection of carbon tetrachloride (CCl4) (1 mL/kg b.wt.) once a week for 12 weeks. The hepato- and DNA protective effects of the extracts in different combinations were compared with that of a standard drug Clavazin (200 mg/kg b.wt.). Tissue alanine aminotransferase, alpha-fetoprotein, tumor necrosis factor alpha (TNF-α), isoprostanes-2α, malondialdehyde, and 8-hydroxydeoxyguanosine, the significant hallmarks of oxidative stress, were studied.

    Results: Histopathological findings of the liver sections from the rat group which received CCl4+cabralealactone, solasodin, and salvadorin demonstrated improved centrilobular hepatocyte regeneration with moderate areas of congestion and infiltration comparable with Clavazin. For in silico study, the identified compounds were subjected to molecular docking with cyclooxygenase-2 and TNF-α followed by a molecular dynamics study, which indicated their potential as anti-inflammatory agents.

    Conclusion: Cabralealactone, solasodin, and salvadorin confer some hepatoprotective and DNA-damage protective effects against CCl4-induced toxicity. They successfully restored the normal architecture of hepatocytes and have the potential to be used as inhibitor to main culprits, that is, cyclooxygenase-2 and TNF-α. They can combat oxidative stress and liver injuries both as mono and combinational therapies. However, combination therapy has more ameliorating effects.

  15. Predictors of postpartum weight retention among urban Malaysian mothers: A prospective cohort study
    Fadzil F, Shamsuddin K, Wan Puteh SE, Mohd Tamil A, Ahmad S, Abdul Hayi NS, et al.
    Obes Res Clin Pract, 2018 06 28;12(6):493-499.
    PMID: 29960869 DOI: 10.1016/j.orcp.2018.06.003
    BACKGROUND: Women of childbearing age are predisposed to becoming overweight or obese. This study determines the mean, prevalence and factors associated with 6 months postpartum weight retention among urban Malaysian mothers.

    METHODS: A prospective cohort study was conducted at baseline (after delivery), 2, 4 and 6 months postpartum. From 638 eligible mothers initially recruited, 420 completed until 6 months. Dependent variable was weight retention, defined as difference between weight at 6 months postpartum and pre-pregnancy weight, and weight retention ≥5kg was considered excessive. Independent variables included socio-demographic, history of pregnancy and delivery, lifestyle, practices and traditional postpartum practices.

    RESULTS: Average age was 29.61±4.71years, majority (83.3%) were Malays, 58.8% (low education), 70.0% (employed), 65.2% (middle income family), 33.8% (primiparous) and 66.7% (normal/instrumental delivery). Average gestational weight gain was 12.90±5.18kg. Mean postpartum weight retention was 3.12±4.76kg, 33.8% retaining ≥5kg. Bivariable analysis showed low income, primiparity, gestational weight gain ≥12kg, less active physically, higher energy, protein, carbohydrate and fat intake in diet, never using hot stone compression and not continuing breastfeeding were significantly associated with higher 6 months postpartum weight retention. From multivariable linear regression analysis, less active physically, higher energy intake in diet, gestational weight gain ≥12kg, not continuing breastfeeding 6 months postpartum and never using hot stone compression could explain 55.1% variation in 6 months postpartum weight retention.

    CONCLUSION: Women need to control gestational weight gain, remain physically active, reduce energy intake, breastfeed for at least 6 months and use hot stone compression to prevent high postpartum weight retention.

  16. Synthesis, X-ray crystal and monoamine oxidase inhibitory activity of 4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine 5,5-dioxides: In vitro studies and docking analysis
    Ahmad S, Jalil S, Zaib S, Aslam S, Ahmad M, Rasul A, et al.
    Eur J Pharm Sci, 2019 Apr 01;131:9-22.
    PMID: 30735822 DOI: 10.1016/j.ejps.2019.02.007
    We report the synthesis and biological evaluation of two new series of 2-amino-6-benzyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides and 2-amino-6-methyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides. The synthetic methodology involves a multistep reaction starting with methyl anthranilate which was coupled with methane sulfonyl chloride. The product of the reaction was subjected to N-benzylation and N-methylation reactions followed by ring closure with sodium hydride resulting in the formation of respective 2,1-benzothiazine 2,2-dioxides. These 2,1-benzothiazine precursors were subjected to multicomponent reaction with malononitrile and substituted benzaldehydes for the synthesis of two new series of pyranobenzothiazines (6a-r and 7a-r). The synthesized compounds were screened as selective inhibitors of monoamine oxidase A and monoamine oxidase B. The in vitro results suggested that compound 6d and 7q are the selective inhibitors of monoamine oxidase A, however, the selective and potent inhibitors of monoamine oxidase B included compounds 6h and 7r. Moreover, some dual inhibitors were noticed like 7l having more inhibitory activity towards both the isozymes. Moreover, the binding modes of the selective and potent inhibitors of monoamine oxidase A and B were investigated by molecular docking analysis. The results suggested that the synthetic derivatives may be potential towards the monoamine oxidase isozymes.
  17. Structural probing of HapR to identify potent phytochemicals to control Vibrio cholera through integrated computational approaches
    Tahir Ul Qamar M, Ahmad S, Khan A, Mirza MU, Ahmad S, Abro A, et al.
    Comput Biol Med, 2021 11;138:104929.
    PMID: 34655900 DOI: 10.1016/j.compbiomed.2021.104929
    Cholera is a severe small intestine bacterial disease caused by consumption of water and food contaminated with Vibrio cholera. The disease causes watery diarrhea leading to severe dehydration and even death if left untreated. In the past few decades, V. cholerae has emerged as multidrug-resistant enteric pathogen due to its rapid ability to adapt in detrimental environmental conditions. This research study aimed to design inhibitors of a master virulence gene expression regulator, HapR. HapR is critical in regulating the expression of several set of V. cholera virulence genes, quorum-sensing circuits and biofilm formation. A blind docking strategy was employed to infer the natural binding tendency of diverse phytochemicals extracted from medicinal plants by exposing the whole HapR structure to the screening library. Scoring function criteria was applied to prioritize molecules with strong binding affinity (binding energy 
  18. Fulltext Vaccine hesitancy in East Malaysia (Sabah): A survey of the national COVID-19 immunisation programme
    Jafar A, Mapa MT, Sakke N, Dollah R, Joko EP, Atang C, et al.
    Geospat Health, 2022 01 14;17(s1).
    PMID: 35147010 DOI: 10.4081/gh.2022.1037
    The Malaysian government has introduced the National COVID-19 Immunisation Programme (PICK) as a new mechanism to address the transmission of coronavirus disease 2019 (COVID-19). Unfortunately, the number of PICK registrations is still unsatisfactory and is now even lower. The low level of participation of the Sabah (East Malaysia) population significantly impacts the PICK registrations. Therefore, this study aims to identify the factors that cause vaccine hesitancy among the people of Sabah. This study seeks to identify these trends based on zone and district boundaries. A total of 1024 respondents were sampled in this study. Raw data collected through the survey method were analysed using K-means clustering, principal component analysis (PCA), and spatial analysis. The study discovered that factors including confidence, authority, mainstream media, complacency, social media, and convenience are the top causes of vaccine hesitancy among respondents. This study also revealed that the Sabah population's key variables causing vaccine hesitancy to vary by region (zones and districts). The conclusion is significant as a source of supporting data for stakeholders seeking to identify the Sabah population's constraints in each region and therefore, it would help improve PICK management's performance in Sabah.
  19. Fulltext Unmet Healthcare Needs Among Elderly Malaysians
    Shah SA, Safian N, Ahmad S, Nurumal SR, Mohammad Z, Mansor J, et al.
    J Multidiscip Healthc, 2021;14:2931-2940.
    PMID: 34703245 DOI: 10.2147/JMDH.S326209
    Purpose: Older people often have chronic diseases which require a continuity of care over the long term. Countries undergoing population aging need to ensure that older people are receiving the care they need. This study assesses the prevalence of, reasons for, and factors associated with unmet healthcare needs among older people individuals in Malaysia.

    Patients and Methods: This cross-sectional study used data collected during 2018-2020 from 1204 older adults aged 60 and older selected from Selangor state, Malaysia. A comprehensive face-to-face interview based on the Bahasa Malaysia version of the Japan Gerontological Evaluation Study (JAGES-BM) questionnaire was administered to gain information on unmet healthcare needs, socioeconomic factors, health-related factors, and measures of function (activities of daily living, depression, visual impairment, hearing impairment, memory impairment, and walking impairment). Multivariate logistic regression was used to analyze factors associated with their unmet healthcare needs.

    Results: Overall, the percentage of older people respondents with unmet healthcare needs is 6.6%. The most reported reasons for forgoing or delaying healthcare were lack of knowledge about healthcare and financial barriers to care. The inability to travel alone (adjusted odds ratio [aOR] 2.51), being overweight (aOR 1.88), and having self-reported depression (aOR 2.23) were each associated with a higher likelihood of having unmet healthcare needs in their daily life.

    Conclusion: The prevalence of unmet healthcare needs among older people in this part of Malaysia is lower than that reported in some other countries. However, it is possible to further reduce unmet healthcare needs by improving people's knowledge and attitudes about appropriate healthcare utilization, strengthening financial protection measures and providing support to people at high risk of having unmet healthcare needs.

  20. Fulltext Weight perception among non-pregnant urban Malaysian women: is it reliable?
    Fadzil F, Shamsuddin K, Wan Puteh SE, Ahmad S, Abdul Hayi NS, Abdul Samad A, et al.
    Int J Public Health Res, 2015;5(2):637-642.
    MyJurnal
    Introduction: In maternal healthcare, pre-pregnancy weight is used to predict pregnancy outcomes. Since no recorded data on pre-pregnancy weight, perceived weight is used alternatively. This study examines the relationship between perceived and actual weight among non-pregnant urban Malaysian women of childbearing age and identifies differences in perceived and actual weight by selected socio-demographic characteristics.
    Methods: A cross-sectional study was conducted between April and June 2013 among urban Malaysian women attending public health clinics in the Klang Valley. Information on height, perceived current weight and time when their weight was last taken were obtained and actual weight was the average of two measurements (TANITA-HD-323-digital-scale). Socio-demographic data collected were age, ethnicity, education level, marital and employment status and total household income.
    Results: Mean age of 371 women in this study was 28.81±5.65, 82.2% were Malays, 62.8% had tertiary education, over 75% were married and employed, with more than half from middle-income households. Overall, the mean perceived and actual weight was 59.29±11.59 and 59.20±11.90 respectively. Pearson‟s Correlation test showed a very strong positive correlation between perceived and actual weight (r=0.957;p<0.0001), ranging between 0.852 to 0.994 among subgroups; 258 (69.5%) perceived their weight accurately (±2.0 kg of actual weight), 49 (13.2%) under and 64 (17.3%) overestimated their weight.Main outliers were among younger women, Malays, tertiary educated, employed, middle-income and had weight last measured a month or more ago.
    Conclusion: Strong correlation between perceived and actual weight among women in this study reassured weight perception can be used more confidently in patients‟ history taking and future research among urban Malaysian women using public health services.
Related Terms
Filters
Contact Us

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

External Links