Displaying publications 81 - 100 of 170 in total

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  1. Ismail NH, Nik Jaafar NR, Woon LS, Mohd Ali M, Dahlan R, Baharuddin ANAP
    Front Psychiatry, 2022;13:989079.
    PMID: 36762292 DOI: 10.3389/fpsyt.2022.989079
    BACKGROUND: The Beck Anxiety Inventory (BAI) is a common tool for screening anxiety symptoms. In Malaysia, the Malay-version 21-item BAI has been previously validated in the Malaysian adult population. However, information regarding its reliability and validity among adolescents below 18 years old is still lacking. The objective of this study is to investigate the psychometric properties of the Malay-version BAI in this population.

    METHODS: The Malay versions of the BAI and the Depression, Anxiety, and Stress Scale (DASS) were administered among a sample of lower secondary school students (n = 329, age range: 13-14 years) in Selangor, Malaysia. Cronbach's alpha value for the internal consistency of the Malay-version BAI was determined. The correlation coefficient between the BAI score and DASS anxiety subscale score was calculated to examine convergent validity. The factor structure of the Malay-version BAI was identified by exploratory factor analysis (EFA) using principal axis factoring.

    RESULTS: The study included 329 respondents, who were predominantly female (58.7%) and Malay (79.9%). The mean Malay-version BAI score was 14.46 (SD = 12.39). The Malay-version BAI showed a high level of internal consistency (Cronbach's alpha = 0.948) and convergent validity with the DASS anxiety subscale score (r = 0.80, p < 0.001). The EFA suggested a one-factor solution, with the factor loading of all items on the single factor ranging between 0.48 and 0.81.

    CONCLUSION: The Malay-version BAI demonstrated good psychometric properties. It can be a valid and reliable screening instrument for anxiety among Malaysian adolescents.

  2. Ismail NH, Ibrahim SF, Mokhtar MH, Yahaya A, Zulkefli AF, Ankasha SJ, et al.
    Front Endocrinol (Lausanne), 2023;14:1031066.
    PMID: 36923220 DOI: 10.3389/fendo.2023.1031066
    INTRODUCTION: Vulvovaginal atrophy (VVA) is a common condition in post-menopausal women. Symptoms of VVA include dyspareunia, vaginal dryness, vaginal and/or vulvar itching, burning and soreness, dysuria and vaginal bleeding accompanying sexual activity. These symptoms are physiological responses to hypoestrogenicity, inducing atrophy of the vagina epithelia and sudden reduction in mucous production. Prevailing therapy for VVA is hormone replacement therapy (HRT), notably estrogen, progesterone or a combination of the two. However, using HRT is associated with an increased incidence of breast and endometrial cancer, venous thromboembolism in the lungs and legs, stroke and cardiovascular complications.

    METHODS: This study evaluated Malaysian Gelam honey as a nutraceutical alternative to estrogen HRT (ERT) in alleviating VVA. A total of 24 female 8-weekold Sprague Dawley rats underwent bilateral oophorectomy. A minimum of 14 days elapsed from the time of surgery and administration of the first dose of Gelam honey to allow the female hormones to subside to a stable baseline and complete recovery from surgery. Vaginal tissues were harvested following a 2-week administration of Gelam honey, the harvested vagina tissue underwent immunohistochemistry (IHC) analysis for protein localization and qPCR for mRNA expression analysis.

    RESULTS: Results indicated that Gelam honey administration had increased the localization of Aqp1, Aqp5, CFTR and Muc1 proteins in vaginal tissue compared to the menopause group. The effect of Gelam honey on the protein expressions is summarized as Aqp1>CFTR>Aqp5>Muc1.

    DISCUSSION: Gene expression analysis reveals Gelam honey had no effect on Aqp1 and CFTR genes. Gelam honey had up-regulated Aqp5 gene expression. However, its expression was lower than in the ERT+Ovx group. Additionally, Gelam honey up-regulated Muc1 in the vagina, with an expression level higher than those observed either in the ERT+Ovx or SC groups. Gelam honey exhibits a weak estrogenic effect on the genes and proteins responsible for regulating water in the vaginal tissue (Aqp1, Aqp5 and CFTR). In contrast, Gelam honey exhibits a strong estrogenic ability in influencing gene and protein expression for the sialic acid Muc1. Muc1 is associated with mucous production at the vaginal epithelial layer. In conclusion, the protein and gene expression changes in the vagina by Gelam honey had reduced the occurrence of vaginal atrophy in surgically-induced menopause models.

  3. Taha M, Naz H, Rasheed S, Ismail NH, Rahman AA, Yousuf S, et al.
    Molecules, 2014 Jan 21;19(1):1286-301.
    PMID: 24451249 DOI: 10.3390/molecules19011286
    A series of 4-methoxybenzoylhydrazones 1-30 was synthesized and the structures of the synthetic derivatives elucidated by spectroscopic methods. The compounds showed a varying degree of antiglycation activity, with IC50 values ranging between 216.52 and 748.71 µM, when compared to a rutin standard (IC50=294.46±1.50 µM). Compounds 1 (IC50=216.52±4.2 µM), 3 (IC50=289.58±2.64 µM), 6 (IC50=227.75±0.53 µM), 7 (IC50=242.53±6.1) and 11 (IC50=287.79±1.59) all showed more activity that the standard, and these compounds have the potential to serve as possible leads for drugs to inhibit protein glycation in diabetic patients. A preliminary SAR study was performed.
  4. Ismail A, Ismail NH, Abu Kassim NYM, Lestari W, Ismail AF, Sukotjo C
    Dent J (Basel), 2021 Dec 14;9(12).
    PMID: 34940048 DOI: 10.3390/dj9120151
    PURPOSE: Coronavirus disease 19 (COVID-19) has affected dental education in Malaysia. However, studies on dental students' knowledge, perception, and behaviors with regards to COVID-19 are very limited. Thus, this study aims to determine the knowledge status, perceived risk, and preventive behaviors of dental students in Malaysia regarding COVID-19.

    METHODS: A cross-sectional study was conducted among students from 13 dental schools across Malaysia using online questionnaires.

    RESULTS: From 355 respondents, 93.5% obtained a high score of knowledge of COVID-19. Female respondents scored higher than males in perceived risks and preventive behaviors. Chinese respondents scored highest in knowledge, while Malay respondents had the highest perceived risk score. The mean preventive behavior score did not vary across ethnicity. On-campus students scored higher in knowledge and perceived risk whereas off-campus students practiced more preventive behaviors. Clinical students' knowledge score was higher than preclinical students. Final year students scored higher in knowledge and perceived risk compared to their juniors.

    CONCLUSION: The majority of dental students have good knowledge and a high perceived risk of COVID-19, and they practiced most of the preventive behaviors. However, the latest information on this disease should be incorporated into dental schools' curriculums and updated periodically.

  5. Taha M, Ismail NH, Jamil W, Yousuf S, Jaafar FM, Ali MI, et al.
    Molecules, 2013 Sep 05;18(9):10912-29.
    PMID: 24013406 DOI: 10.3390/molecules180910912
    2,4-Dimethylbenzoylhydrazones 1-30 were synthesized by condensation reactions of 2,4-dimethylbenzoylhydrazide with various aromatic aldehydes and characterized. The assigned structures of compounds 10, 15 and 22 were further supported by single-crystal X-ray diffraction data. The synthesized compounds were evaluated for their in vitro DPPH radical scavenging activity. They exerted varying degree of scavenging activity toward DPPH radical with IC₅₀ values between 25.6-190 µM. Compounds 1, 4, 2, 3, 7, and 6 have IC₅₀ values of 25.6, 28.1, 29.3, 29.8, 30.0 and 30.1 µM respectively, showing better activity than an n-propyl gallate standard (IC₅₀ value = 30.30 µM). For super oxide anion scavenging activity compounds 1, 2 and 3 with IC₅₀ values of 98.3, 102.6, and 105.6, respectively, also showed better activity than the n-propyl gallate standard (IC₅₀ value = 106.34 µM).
  6. Taha M, Ismail NH, Aziza AN, Shah SA, Yousuf S
    Acta Crystallogr Sect E Struct Rep Online, 2013 Feb 01;69(Pt 2):o245.
    PMID: 23424524 DOI: 10.1107/S160053681300127X
    In the title compound, C(29)H(21)O(3)P, a coumarin-substitued ylid, the P atom is linked to three benzene rings and a planar coumarin moiety via a methyl-enecarbonyl group. The bond lengths in the P=C-C=O fragment clearly indicate a delocalized system involving the olefinic and carbonyl bonds. The mol-ecular structure is stabilized by an intra-molecular C-H⋯O inter-action that results in an S7 graph-set ring motif. In the crystal, mol-ecules are linked into a three-dimensional framework by C-H⋯O hydrogen bonds.
  7. Abd Mutalib N, Syed Mohamad SA, Jusril NA, Hasbullah NI, Mohd Amin MCI, Ismail NH
    Pharmaceuticals (Basel), 2023 May 07;16(5).
    PMID: 37242494 DOI: 10.3390/ph16050712
    BACKGROUND: In recent years, the potential role of probiotics has become prominent in the discoveries of neurotherapy against neurodegenerative diseases, such as Alzheimer's and Parkinson's diseases. Lactic acid bacteria (LAB) exhibit neuroprotective properties and exert their effects via various mechanisms of actions. This review aimed to evaluate the effects of LAB on neuroprotection reported in the literature.

    METHODS: A database search on Google Scholar, PubMed, and Science Direct revealed a total of 467 references, of which 25 were included in this review based on inclusion criteria which comprises 7 in vitro, 16 in vivo, and 2 clinical studies.

    RESULTS: From the studies, LAB treatment alone or in probiotics formulations demonstrated significant neuroprotective activities. In animals and humans, LAB probiotics supplementation has improved memory and cognitive performance mainly via antioxidant and anti-inflammatory pathways.

    CONCLUSIONS: Despite promising findings, due to limited studies available in the literature, further studies still need to be explored regarding synergistic effects, efficacy, and optimum dosage of LAB oral bacteriotherapy as treatment or prevention against neurodegenerative diseases.

  8. Abduh MY, Norazmi-Lokman NH, Syahnon M, Roslan GAG, Ismail NH, Abol-Munafi AB
    Data Brief, 2020 Dec;33:106557.
    PMID: 33304955 DOI: 10.1016/j.dib.2020.106557
    Despite having high economical value and declining wild population, the aquaculture of the Malaysian mahseer (Tor tambroides) is still way behind. Crucial information such as on its sexual dimorphism is scarce thus making its broodstock management in captivity challenging. The first step in studying fish sexual dimorphism is by observing and identifying the morphological differences between each sex. Thus, this article collected and described morphometric measurements data of broodstock reared in captive conditions. The broodstock were reared and raised in captivity for five years since they were bought from a local commercial supplier while they were five-inch fingerlings. Seven conventional and 21 Truss network morphometric measurements were taken from 27 male (TL: 53.88 ± 2.86 cm; W: 1.82 ± 0.23 kg) and 27 female (TL: 53.97 ± 3.62 cm; W: 1.86 ± 0.35 kg) T. tambroides broodstocks using digital image analysis. Photograph of the fish broodstocks were captured and the morphometric measurements were conducted using imageJ freeware. Statistical analysis was later conducted on the morphometric data to identify the morphological differences between the broodstocks. This dataset will not only aid the sex identification of this species but also in stock population studies thus accelerating the development of T. tambroides aquaculture while improving its conservation efforts.
  9. Chandradevan M, Simoh S, Mediani A, Ismail NH, Ismail IS, Abas F
    PMID: 32047522 DOI: 10.1155/2020/3238561
    This study aimed to determine the total phenolic content, DPPH scavenging, α-glucosidase, and nitric oxide (NO) inhibition of Gynura procumbens and Cleome gynandra extracts obtained with five different ethanolic concentrations. The findings showed that the 100% ethanolic extract of G. procumbens had the highest phenolic content and the lowest IC50 values for DPPH scavenging and NO inhibition activity compared to the properties of the other extracts. For C. gynandra, the 20% and 100% ethanolic extracts had comparably high total phenolic contents, and the latter possessed the lowest IC50 value in the NO inhibition assay. In addition, the 20% ethanolic extract of C. gynandra had the lowest IC50 value in the DPPH scavenging assay. However, none of the extracts from either herb had the ability to inhibit α-glucosidase enzyme. Pearson correlation analysis indicated a strong relationship between the phenolic content and DPPH scavenging activity in both herb extracts. A moderately strong relationship was also observed between the phenolic content and NO inhibition in G. procumbens extracts and not in C. gynandra extracts. The UHPLC-ESI-Orbitrap-MS revealed major phenolics from the groups of hydroxycinnamic acids, hydroxybenzoic acids, and flavonoid derivatives from both herbs, which could be the key contributors to their bioactivities. Among the identified metabolites, 24 metabolites were tentatively assigned for the first time from both species of studied herbs. These two herbs could be recommended as prospective natural products with valuable medicinal properties.
  10. Shimbo S, Moon CS, Zhang ZW, Watanabe T, Ismail NH, Ali RM, et al.
    Tohoku J Exp Med, 1996 Oct;180(2):99-114.
    PMID: 9111760
    Nutrient intake was surveyed by the total food duplicate method in 49 adult ethnically Malay women (at the ages of 18 to 47 years and mostly at 30-39 years) working in Kuala Lumpur, Malaysia. Simultaneously, hematological examinations, serum biochemistry, anthropometry and clinical examination were conducted. Nutrient intakes were estimated in reference to the weight of each food item and the standard food composition tables. Lunch was the most substantial meal of the day with rice as a staple food. Compared with the Recommended Dietary Allowance (RDA) values, daily intakes of energy (1,917 kcal as an arithmetic mean), protein (62.2 g), vitamin B1 (0.83 mg) and vitamin B2 (1.18 mg) were sufficient, but intakes of minerals [i.e., calcium (347.8 mg) and iron (12.5 mg)] and some vitamins [i.e., vitamin A (equivalent to 627 micrograms retinol) and niacin (7.84 mg)] were less than RDA. When evaluated on an individual basis, the prevalence of those who took less than 80% RDA was highest for iron (92%), followed by niacin (80%), calcium (57%) and vitamin A (57%). The presence of 7 hypohemoglobinemia cases may be related to the insufficient iron intake. Overweight cases (14 women) were also detected, the prevalence of which increased at advanced ages. Lipid intake was rather high (28% of total food on energy basis), for which the major source was plants with limited contribution from fish/shellfish.
  11. Jaffar FHF, Osman K, Ismail NH, Chin KY, Ibrahim SF
    Tohoku J Exp Med, 2019 07;248(3):169-179.
    PMID: 31353326 DOI: 10.1620/tjem.248.169
    Extensive use of Wi-Fi has contributed to radiofrequency electromagnetic radiation (RF-EMR) pollution in environment. Various studies have been conducted to evaluate the effect of RF-EMR emitted by Wi-Fi transmitter on male reproduction health. However, there are conflicting findings between studies. Thus, this review aims to elucidate the possible effects of 2.45 GHz Wi-Fi exposure on both animal and human male reproductive system. A computerized database search performed through MEDLINE via Ovid and PUBMED with the following set of keywords: 'Wi-Fi or WiFi or wireless fidelity or Wi-Fi router or WiFi router or electromagnetic or radiofrequency radiation' AND 'sperm or spermatozoa or spermatogenesis or semen or seminal plasma or testes or testis or testosterone or male reproduction' had returned 526 articles. Only 17 studies conformed to pre-set inclusion criterion. Additional records identified through Google Scholar and reviewed article further revealed six eligible articles. A total of 23 articles were used for data extraction, including 15 studies on rats, three studies on mice, and five studies on human health. Sperm count, motility and DNA integrity were the most affected parameters when exposed to RF-EMR emitted by Wi-Fi transmitter. Unfortunately, sperm viability and morphology were inconclusive. Structural and/or physiological analyses of the testes showed degenerative changes, reduced testosterone level, increased apoptotic cells, and DNA damage. These effects were mainly due to the elevation of testicular temperature and oxidative stress activity. In conclusion, exposure towards 2.45 GHz RF-EMR emitted by Wi-Fi transmitter is hazardous on the male reproductive system.
  12. Dewi IP, Dachriyanus, Aldi Y, Ismail NH, Hefni D, Susanti M, et al.
    J Ethnopharmacol, 2024 Feb 10;320:117381.
    PMID: 37967776 DOI: 10.1016/j.jep.2023.117381
    ETHNOPHARMACOLOGICAL RELEVANCE: Garcinia cowa Roxb. is called asam kandis in West Sumatra. This plant contains several quinone compounds, including tetraprenyltoluquinone (TPTQ). The bioactivity of this compound has been tested as an anticancer agent. However, reports regarding its anti-inflammatory effects are still limited, especially against coronavirus disease (Covid-19).

    AIM OF THE STUDY: This study explores the anti-inflammatory effect of TPTQ in silico, in vitro, and in vivo.

    MATERIALS AND METHODS: In silico testing used the Gnina application, opened via Google Colab. The TPTQ structure was docked with the nuclear factor kappa B (NF-ĸB) protein (PDB: 2RAM). In vitro testing began with testing the cytotoxicity of TPTQ against Raw 264.7 cells, using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) method. A phagocytic activity test was carried out using the neutral red uptake method, and interleukin-6 (IL-6) and tumor necrosis factor alpha (TNF-α) secretion tests were carried out using the enzyme-linked immunosorbent assay (ELISA) method. In vivo, tests were carried out on mice by determining cluster of differentiation 8+ (CD8+), natural killer cell (NK cell), and IL-6 parameters, using the ELISA method.

    RESULTS: TPTQ has a lower binding energy than the native ligand and occupies the same active site as the native ligand. TPTQ decreased the phagocytosis index and secretion of IL-6 and TNF-α experimentally in vitro. TPTQ showed significant downregulation of CD8+ and slightly decreased NK cells and IL-6 secretion in vivo.

    CONCLUSION: The potent inhibitory effect of TPTQ on the immune response suggests that TPTQ can be developed as an anti-inflammatory agent, especially in the treatment of Covid-19.

  13. Muhamad NAS, Mohd Mokhtar N, Naim R, Lau WJ, Ismail NH
    Environ Pollut, 2024 Aug 19.
    PMID: 39168437 DOI: 10.1016/j.envpol.2024.124739
    Membrane distillation (MD) is gaining increasing recognition within membrane-based processes for palm oil mill effluent (POME) treatment. This study aims to alter the physicochemical characteristics of polyvinylidene fluoride (PVDF) membranes through the incorporation of bentonite (B) at varying weight concentrations (ranging from 0.25 wt% to 1.0 wt%). Characterization was conducted to evaluate changes in morphology, thermal stability, surface characteristics and wetting properties of the resulting membranes. The resulting membranes were also tested using direct contact membrane distillation (DCMD) with POME as the feed solution, aiming to generate high-purity water. Results indicated that the PVDF-0.3B and PVDF-0.5B membranes achieved the highest water vapor flux. The finger-like structure and macrovoids present in these membranes aid in minimizing mass resistance during vapor transport and enhancing permeate flux. All membranes demonstrated exceptional performance in removing contaminants, eliminating total dissolved solids (TDS) and achieving over 99% rejection of chemical oxygen demand, nitrate nitrogen, color, and turbidity from the feed solution. The permeate water analysis showed that the PVDF-0.3B membrane had superior removal efficiency and met the standards set by the local Department of Environment (DOE). The PVDF-0.3B membrane was chosen as the preferred option because of its consistent flux and high removal efficiency. This study demonstrated that incorporating bentonite into PVDF membranes significantly enhanced their properties and performance for POME treatment.
  14. Dewi IP, Dachriyanus, Aldi Y, Ismail NH, Osman CP, Putra PP, et al.
    J Ethnopharmacol, 2025 Feb 08.
    PMID: 39929399 DOI: 10.1016/j.jep.2025.119380
    ETHNOPHARMACOLOGICAL RELEVANCE: Garcinia cowa Roxb. commonly known as asam kandis in Indonesia and Cha muang in Thailand, has been extensively utilized as traditional medicine. This plant contains compounds such as xanthones, phloroglucinol, depsidones, terpenoids, steroids, and flavonoids. These compounds have been extensively studied for various bioactivities. However, the utilization of this plant as an anti-inflammatory agent is still limited.

    AIM OF THE STUDY: This study aims to evaluate newly derived compounds from Garcinia cowa Roxb., focusing on their ADMET profiles (Absorption, Distribution, Metabolism, Excretion, and Toxicity) and anti-inflammatory bioactivity. The assessment will be carried out using a combination of in silico and in vitro experiments to determine their pharmacological potential as anti-inflammatory agents.

    MATERIALS AND METHODS: Isolation of compounds from Garcinia cowa Roxb. was carried out using column chromatography, purified with radial chromatography, and recycling HPLC. The compounds' structures were evaluated for their ADMET profiles and anti-inflammatory bioactivity using the NF-ĸB protein (PDB Code: 2RAM) as the target. The in vitro experiment was conducted using Raw 264.7 macrophages cell to assess cytotoxicity, phagocytic activity, IL-6, and TNF-α secretion. The determination of the anti-inflammatory mechanism is carried out by testing the activity of NF-ĸB and IKB-α using the western blot method.

    RESULTS: We successfully analyzed the structure of a new compound from the bark of Garcinia cowa Roxb., named Garciacowanin (NC). In silico analysis suggests that the drug shows promising absorption potential, there are concerns related to its metabolism and toxicity that warrant further investigation during the development process and does not show mutagenic properties based on the negative AMES test results. There is a risk of hepatotoxicity (liver damage) and the drug can also interfere with the hERG II ion channel, which can cause side effects on the heart. The compound can affect the NF-ĸB protein, while in vitro studies have demonstrated its ability to suppress phagocytic activity, as well as the production of IL-6 and TNF-α. Western blot analysis suggests that NC's anti-inflammatory mechanism functions via the NF-ĸB signaling pathway.

    CONCLUSION: NC has the potential to be developed as an anti-inflammatory agent with a mechanism of inhibiting the inflammatory response through the NF-ĸB signaling pathway.

  15. Ali F, Khan KM, Salar U, Iqbal S, Taha M, Ismail NH, et al.
    Bioorg Med Chem, 2016 08 15;24(16):3624-35.
    PMID: 27325448 DOI: 10.1016/j.bmc.2016.06.002
    Dihydropyrimidones 1-37 were synthesized via a 'one-pot' three component reaction according to well-known Biginelli reaction by utilizing Cu(NO3)2·3H2O as catalyst, and screened for their in vitro β-glucuronidase inhibitory activity. It is worth mentioning that amongst the active molecules, compounds 8 (IC50=28.16±.056μM), 9 (IC50=18.16±0.41μM), 10 (IC50=22.14±0.43μM), 13 (IC50=34.16±0.65μM), 14 (IC50=17.60±0.35μM), 15 (IC50=15.19±0.30μM), 16 (IC50=27.16±0.48μM), 17 (IC50=48.16±1.06μM), 22 (IC50=40.16±0.85μM), 23 (IC50=44.16±0.86μM), 24 (IC50=47.16±0.92μM), 25 (IC50=18.19±0.34μM), 26 (IC50=33.14±0.68μM), 27 (IC50=44.16±0.94μM), 28 (IC50=24.16±0.50μM), 29 (IC50=34.24±0.47μM), 31 (IC50=14.11±0.21μM) and 32 (IC50=9.38±0.15μM) found to be more potent than the standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Molecular docking study was conducted to establish the structure-activity relationship (SAR) which demonstrated that a number of structural features of dihydropyrimidone derivatives were involved to exhibit the inhibitory potential. All compounds were characterized by spectroscopic techniques such as (1)H, (13)C NMR, EIMS and HREI-MS.
  16. Zawawi NK, Taha M, Ahmat N, Wadood A, Ismail NH, Rahim F, et al.
    Bioorg Chem, 2016 Feb;64:29-36.
    PMID: 26637946 DOI: 10.1016/j.bioorg.2015.11.006
    Newly synthesized benzimidazole hydrazone derivatives 1-26 were evaluated for their α-glucosidase inhibitory activity. Compounds 1-26 exhibited varying degrees of yeast α-glucosidase inhibitory activity with IC50 values between 8.40 ± 0.76 and 179.71 ± 1.11 μM when compared with standard acarbose. In this assay, seven compounds that showed highest inhibitory effects than the rest of benzimidazole series were identified. All the synthesized compounds were characterized by different spectroscopic methods adequately. We further evaluated the interaction of the active compounds with enzyme with the help of docking studies.
  17. Taha M, Ismail NH, Lalani S, Fatmi MQ, Atia-Tul-Wahab, Siddiqui S, et al.
    Eur J Med Chem, 2015 Mar 6;92:387-400.
    PMID: 25585009 DOI: 10.1016/j.ejmech.2015.01.009
    In an effort to design and synthesize a new class of α-glucosidase inhibitor, we synthesized benzothiazole hybrid having benzohydrazide moiety (5). Compound 5 was reacted with various substituted aryl aldehyde to generate a small library of compounds 6-35. Synthesis of compounds was confirmed by the spectral information. These compounds were screened for their α-glucosidase activity. They showed a varying degree of α-glucosidase inhibition with IC50 values ranging between 5.31 and 53.34 μM. Compounds 6, 7, 9-16, 19, 21-30, 32-35 showed superior activity as compared to standard acarbose (IC50 = 906 ± 6.3 μM). This has identified a new class of α-glucosidase inhibitors. The predicted physico-chemical properties indicated the drug appropriateness for most of these compounds, as they obey Lipinski's rule of five (RO5). A hybrid B3LYP density functional theory (DFT) was employed for energy, minimization of 3D structures for all synthetic compounds using 6-311 + G(d,p) basis sets followed by molecular docking to explore their interactions with human intestinal C- and N-terminal domains of α-glucosidase. All compounds bind to the prospective allosteric site of the C- terminal domain, and consequently, may be considered as mixed inhibitors. It was hypothesized that both the dipole moment and H-bond interactions govern the biological activation of these compounds.
  18. Jamil W, Perveen S, Shah SA, Taha M, Ismail NH, Perveen S, et al.
    Molecules, 2014 Jun 25;19(7):8788-802.
    PMID: 24968334 DOI: 10.3390/molecules19078788
    Phenoxyacetohydrazide Schiff base analogs 1-28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50=9.20±0.32 µM), 5 (IC50=9.47±0.16 µM), 7 (IC50=14.7±0.19 µM), 8 (IC50=15.4±1.56 µM), 11 (IC50=19.6±0.62 µM), 12 (IC50=30.7±1.49 µM), 15 (IC50=12.0±0.16 µM), 21 (IC50=13.7±0.40 µM) and 22 (IC50=22.0±0.14 µM) showed promising β-glucuronidase inhibition activity, better than the standard (D-saccharic acid-1,4-lactone, IC50=48.4±1.25 µM).
  19. Ee GC, Foo CH, Jong VY, Ismail NH, Sukari MA, Taufiq Yap YH, et al.
    Nat Prod Res, 2012;26(9):830-5.
    PMID: 22044165 DOI: 10.1080/14786419.2011.559640
    A detailed chemical study on the stem bark of Garcinia nitida has led to the isolation of five xanthones. They are 1,6-dihydroxy-5-methoxy-6,6-dimethylpyrano[2',3':2,3]-xanthone (1), inophyllin B (2), osajaxanthone (3), 3-isomangostin (4) and rubraxanthone (5). The structures of these compounds were established using mainly 1-D and 2-D NMR spectroscopy ((1)H, (13)C, DEPT, COSY, HMBC and HMQC) while molecular masses were determined via MS techniques; 1 is a new compound.
  20. Taha M, Ismail NH, Imran S, Mohamad MH, Wadood A, Rahim F, et al.
    Bioorg Chem, 2016 Apr;65:100-9.
    PMID: 26894559 DOI: 10.1016/j.bioorg.2016.02.004
    Benzimidazole analogs 1-27 were synthesized, characterized by EI-MS and (1)HNMR and their α-glucosidase inhibitory activities were found out experimentally. Compound 25, 19, 10 and 20 have best inhibitory activities with IC50 values 5.30±0.10, 16.10±0.10, 25.36±0.14 and 29.75±0.19 respectively against α-glucosidase. Compound 6 and 12 has no inhibitory activity against α-glucosidase enzyme among the series. Further studies showed that the compounds are not showing any cytotoxicity effect. The docking studies of the compounds as well as the experimental activities of the compounds correlated well. From the molecular docking studies, it was observed that the top ranked conformation of all the compounds fit well in the active site of the homology model of α-glucosidase.
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