Displaying publications 1 - 20 of 91 in total

Abstract:
Sort:
  1. Majid Shah S, Ullah F, Ayaz M, Sadiq A, Hussain S, Ali Shah AU, et al.
    Steroids, 2019 08;148:56-62.
    PMID: 31085212 DOI: 10.1016/j.steroids.2019.05.001
    The current study was aimed to evaluate the anti-leishmanial potentials of β-sitosterol isolated from Ifloga spicata. The anti-leishmanial potential of β-sitosterol is well documented against Leishmania donovani and Leishmania amazonensis but unexplored against Leishmania tropica. Structure of the compound was elucidated by FT-IR, mass spectrometry and multinuclear (1H and 13C) magnetic resonance spectroscopy. The compound was evaluated for its anti-leishmanial potentials against L. tropica KWH23 using in vitro anti-promastigote, DNA interaction, apoptosis, docking studies against leishmanolysin (GP63) and trypanothione reductase (TR) receptors using MOE 2016 software. β-sitosterol exhibited significant activity against leishmania promastigotes with IC50 values of 9.2 ± 0.06 μg/mL. The standard drug glucantaime showed IC50 of 5.33 ± 0.07 µg/mL. Further mechanistic studies including DNA targeting and apoptosis induction via acridine orange assay exhibited promising anti-leishmanial potentials for β-sitosterol. Molecular docking with leishmanolysin (GP63) and trypanothione reductase (TR) receptors displayed the binding scores of β-sitosterol with targets TR and GP63 were -7.659 and -6.966 respectively. The low binding energies -61.54 (for TR) and -33.24 (for GP63) indicate that it strongly bind to the active sites of target receptors. The results confirmed that β-sitosterol have considerable anti-leishmanial potentials and need further studies as potential natural anti-leishmanial agent against L. tropica.
  2. Hussain S, Ghopa WAW, Singh SSK, Azman AH, Abdullah S, Harun Z, et al.
    Materials (Basel), 2022 Jul 14;15(14).
    PMID: 35888355 DOI: 10.3390/ma15144888
    Vibration fatigue characteristics are critical for rotating machinery components such as turbine rotor blades. Lattice structures are gaining popularity in engineering applications due to their unique ability to reduce weight and improve the mechanical properties. This study is an experimental investigation of octet-truss lattice structure utilization in turbine rotor blades for weight reduction and to improve vibration fatigue characteristics. One completely solid and three lattice infilled blades with variable strut thickness were manufactured via additive manufacturing. Both free and forced experimental vibration analyses were performed on the blades to investigate their modal and vibration fatigue characteristics. The blades were subjected to random vibration using a vibration shaker. The response was measured using a triaxial accelerometer in terms of vibration acceleration time histories in the X, Y, and Z directions. Results indicate a weight reduction of up to 24.91% and enhancement in the first natural frequency of up to 5.29% were achieved using lattice infilled blades. The fatigue life of the blades was investigated using three frequency domain approaches, namely, Lalanne, Dirlik and narrow band. The fatigue life results indicate that the 0.25 mm lattice blade exhibits the highest fatigue life, while the solid blade exhibits the lowest fatigue life of all four blades. The fatigue life of the 0.25 mm lattice blade was 1822-, 1802-, and 1819- fold higher compared to that of the solid blade, using the Lalanne, Dirlik, and narrow-band approaches, respectively. These results can serve as the first step towards the utilization of lattice structures in turbine blades, with thermal analysis as the next step. Therefore, apart from being light weight, the octet-truss lattice infilled blades exhibited superior vibration fatigue characteristics to vibration loads, thereby making them a potential replacement for solid blades in turbine rotors.
  3. Syed-Hussain SS, Howe L, Pomroy WE, West DM, Hardcastle M, Williamson NB
    Vet Parasitol, 2015 Mar 15;208(3-4):150-8.
    PMID: 25638717 DOI: 10.1016/j.vetpar.2014.12.036
    Recent reports indicate N. caninum has a possible role in causing abortions in sheep in New Zealand. Knowledge about the mode of transmission of neosporosis in sheep in New Zealand is limited. This study aimed to determine the rate of vertical transmission that would occur in lambs born from experimentally inoculated ewes and to determine if previous inoculation would protect the lambs from N. caninum infection. A group of 50 ewes was divided into 2 groups with one group being inoculated with 5×10(6) N. caninum tachyzoites prior to pregnancy in Year 1. In Year 2, each of these groups was subdivided into 2 groups with one from each original group being inoculated with 1×10(7) N. caninum tachyzoites on Day 120 of gestation. Inoculation of N. caninum tachyzoites into ewes prior to mating resulted in no congenital transmission in lambs born in Year 1 but without further inoculation, 7 out of 11 lambs in Year 2 were positive for N. caninum infection. Ewes that were inoculated in both years resulted in all 12 lambs born in Year 2 being positive for N. caninum infection. This indicates that previous inoculation in Year 1 did not result in any vertical transmission in that year but did not provide any protection against vertical transmission in Year 2. These results suggest that vertical transmission occurs readily once the ewe is infected.
  4. Zulkipli AF, Islam T, Mohd Taib NA, Dahlui M, Bhoo-Pathy N, Al-Sadat N, et al.
    Integr Cancer Ther, 2018 06;17(2):312-321.
    PMID: 29218996 DOI: 10.1177/1534735417745248
    BACKGROUND: The use of complementary and alternative medicine (CAM) has increased and little is known on CAM use during the initial period. Therefore, the aim was to determine prevalence of CAM use among newly diagnosed breast cancer patients prior to seeking conventional treatment.

    METHODS: This is a cross-sectional study involved interviewing newly diagnosed breast cancer patients in the University Malaya Medical Centre (UMMC) using a structured questionnaire. Eligible respondents were interviewedduring a routine clinical visit.

    RESULTS: A total of 400 patients were interviewed, of whom 139 (34.8%) were CAM users. Dietary supplementation (n = 107, 77.0%) was the most frequently used type of CAM, followed by spiritual healing (n = 40, 28.8%) and traditional Chinese medicine (n = 32, 23.0%). Malay ethnic group (n = 61, 43.9%) was the largest group of CAM users, followed by Chinese (n = 57, 41.0%) and Indian (n = 20, 14.4%). Majority of these CAM users (n = 87, 73.1%) did not disclose the use of CAM to their doctors. Most of them used remedies based on the recommendation of family and friends. Malay ethnicity and patients with 3 or more comorbidities were more likely to use CAM.

    CONCLUSION: There is substantial use of CAM among breast cancer patients in UMMC prior to seeking hospital treatment, and the most popular CAM modality is dietary supplements. Since, the majority of CAM users do not disclose the use of CAM to their physicians, therefore health care providers should ensure that those patients who are likely to use CAM are appropriately counseled and advised.

  5. Rahim F, Ullah K, Ullah H, Wadood A, Taha M, Ur Rehman A, et al.
    Bioorg Chem, 2015 Feb;58:81-7.
    PMID: 25528720 DOI: 10.1016/j.bioorg.2014.12.001
    A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and (1)H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46±0.008 and 312.79±0.06 μM when compared with the standard acarbose (IC50, 38.25±0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46±0.008, 37.78±0.05, 28.91±0.0, 38.12±0.04, 37.43±0.03, 36.89±0.06 and 37.11±0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking.
  6. Lee YL, Zaini AA, Idris AN, Abdullah RA, Wong JS, Hong JS, et al.
    J Paediatr Child Health, 2023 Jul;59(7):879-884.
    PMID: 37066819 DOI: 10.1111/jpc.16405
    AIMS: Knowledge on the spectrum of thyroid disorders amongst Turner syndrome (TS) patients in Southeast Asia is limited. This study aimed to evaluate the prevalence of thyroid autoimmunity, the spectrum of autoimmune thyroid disease and association with age and karyotype amongst Malaysian TS girls.

    METHODS: A cross-sectional study was conducted at 11 paediatric endocrine units in Malaysia. Blood samples for antithyroglobulin antibodies, antithyroid peroxidase antibodies and thyroid function test were obtained. In patients with pre-existing thyroid disease, information on clinical and biochemical thyroid status was obtained from medical records.

    RESULTS: Ninety-seven TS patients with a mean age of 13.4 ± 4.8 years were recruited. Thyroid autoimmunity was found in 43.8% of TS patients. Nineteen per cent of those with thyroid autoimmunity had autoimmune thyroid disease (Hashimoto thyroiditis in 7.3% and hyperthyroidism in 1% of total population). Patients with isochromosome X and patients with 45,X mosaicism or other X chromosomal abnormalities were more prone to have thyroid autoimmunity compared to those with 45,X karyotype (OR 5.09, 95% CI 1.54-16.88, P = 0.008 and OR 3.41, 95% CI 1.32-8.82, P = 0.01 respectively). The prevalence of thyroid autoimmunity increased with age (33.3% for age 0-9.9 years; 46.8% for age 10-19.9 years and 57.1% age for 20-29.9 years) with autoimmune thyroid disease detected in 14.3% during adulthood.

    CONCLUSION: Thyroid autoimmunity was significantly associated with the non 45,X karyotype group, particularly isochromosome X. Annual screening of thyroid function should be carried out upon diagnosis of TS until adulthood with more frequent monitoring recommended in the presence of thyroid autoimmunity.

  7. Wang C, Tee M, Roy AE, Fardin MA, Srichokchatchawan W, Habib HA, et al.
    PLoS One, 2021;16(2):e0246824.
    PMID: 33571297 DOI: 10.1371/journal.pone.0246824
    The coronavirus disease (COVID-19) pandemic has impacted the economy, livelihood, and physical and mental well-being of people worldwide. This study aimed to compare the mental health status during the pandemic in the general population of seven middle income countries (MICs) in Asia (China, Iran, Malaysia, Pakistan, Philippines, Thailand, and Vietnam). All the countries used the Impact of Event Scale-Revised (IES-R) and Depression, Anxiety and Stress Scale (DASS-21) to measure mental health. There were 4479 Asians completed the questionnaire with demographic characteristics, physical symptoms and health service utilization, contact history, knowledge and concern, precautionary measure, and rated their mental health with the IES-R and DASS-21. Descriptive statistics, One-Way analysis of variance (ANOVA), and linear regression were used to identify protective and risk factors associated with mental health parameters. There were significant differences in IES-R and DASS-21 scores between 7 MICs (p<0.05). Thailand had all the highest scores of IES-R, DASS-21 stress, anxiety, and depression scores whereas Vietnam had all the lowest scores. The risk factors for adverse mental health during the COVID-19 pandemic include age <30 years, high education background, single and separated status, discrimination by other countries and contact with people with COVID-19 (p<0.05). The protective factors for mental health include male gender, staying with children or more than 6 people in the same household, employment, confidence in doctors, high perceived likelihood of survival, and spending less time on health information (p<0.05). This comparative study among 7 MICs enhanced the understanding of metal health in the general population during the COVID-19 pandemic.
  8. Chee ZJ, Chang CYM, Cheong JY, Malek FHBA, Hussain S, de Vries M, et al.
    Int J Psychophysiol, 2024 May;199:112328.
    PMID: 38458383 DOI: 10.1016/j.ijpsycho.2024.112328
    According to the arousal-mood hypothesis, changes in arousal and mood when exposed to auditory stimulation underlie the detrimental effects or improvements in cognitive performance. Findings supporting or against this hypothesis are, however, often based on subjective ratings of arousal rather than autonomic/physiological indices of arousal. To assess the arousal-mood hypothesis, we carried out a systematic review of the literature on 31 studies investigating cardiac, electrodermal, and pupillometry measures when exposed to different types of auditory stimulation (music, ambient noise, white noise, and binaural beats) in relation to cognitive performance. Our review suggests that the effects of music, noise, or binaural beats on cardiac, electrodermal, and pupillometry measures in relation to cognitive performance are either mixed or insufficient to draw conclusions. Importantly, the evidence for or against the arousal-mood hypothesis is at best indirect because autonomic arousal and cognitive performance are often considered separately. Future research is needed to directly evaluate the effects of auditory stimulation on autonomic arousal and cognitive performance holistically.
  9. Ali S, Osman NA, Razak A, Hussain S, Wan Abas WA
    Eur J Phys Rehabil Med, 2015 Feb;51(1):31-7.
    PMID: 24963603
    Lower limb amputee's are greatly affected in dealing with the environmental barriers such as ramps and stairs and reported high interface pressure between the residual limb and socket/liner. Interface pressure between the residual limb and socket/liner can affect the satisfaction and use of the prosthesis. Until now, little attention has been paid to interface pressure between socket and stump during ramp negotiation and its effect on amputee's satisfaction.
  10. Chan PW, Hussain S, Ghani NH, Debruyne JA, Liam CK
    PMID: 12693597
    A pilot study to evaluate the direct cost of treating 51 adults and 50 children with bronchial asthma was conducted. All aspects of the medical care provided over a 6-month period were considered. The mean treatment costs per month were US dollars 22.97 (adults) and US dollars 15.56 (children). The cost of maintenance therapy accounted for 55.5% and 73.4% of the total direct cost treatment for adults and children respectively. Only 27 (52.9%) adults and 17 (34.0%) children paid for their inhaled prophylactic drugs, amounting to 12.3% of the total maintenance therapy costs. Thirteen (25.4%) adults and 9 (18.0%) children were using alternative therapy at a monthly cost of US dollars 41.50 and US dollars 16.77 respectively. A substantial proportion of the direct cost of asthma treatment is heavily subsidized in Malaysia. Adequate attention to the allocation of the health budget, to ensure the optimal provision of health care, is warranted.
  11. Islam T, Bhoo-Pathy N, Su TT, Majid HA, Nahar AM, Ng CG, et al.
    BMJ Open, 2015 Oct 26;5(10):e008643.
    PMID: 26503386 DOI: 10.1136/bmjopen-2015-008643
    INTRODUCTION: Over recent decades, the burden of breast cancer has been increasing at an alarming rate in Asia. Prognostic research findings from Western countries may not readily be adapted to Asia, as the outcome of breast cancer depends on a multitude of factors ranging from genetic, clinical and histological predictors, to lifestyle and social predictors. The primary aim of this study is to determine the impact of lifestyle (eg, nutrition, physical activity), mental and sociocultural condition, on the overall survival and quality of life (QoL) among multiethnic Malaysian women following diagnosis of breast cancer. This study aims to advance the evidence on prognostic factors of breast cancer within the Asian setting. The findings may guide management of patients with breast cancer not only during active treatment but also during the survivorship period.

    METHODS: This hospital-based prospective cohort study will comprise patients with breast cancer (18 years and above), managed in the University Malaya Medical Centre (UMMC). We aim to recruit 1000 cancer survivors over a 6-year period. Data collection will occur at baseline (within 3 months of diagnosis), 6 months, and 1, 3 and 5 years following diagnosis. The primary outcomes are disease-free survival and overall survival, and secondary outcome is QoL. Factors measured are demographic and socioeconomic factors, lifestyle factors (eg, dietary intake, physical activity), anthropometry measurements (eg, height, weight, waist, hip circumference, body fat analysis), psychosocial aspects, and complementary and alternative medicine (CAM) usage.

    ETHICS AND DISSEMINATION: This protocol was approved by the UMMC Ethical Committee in January 2012. All participants are required to provide written informed consent. The findings from our cohort study will be disseminated via scientific publication as well as presentation to stakeholders including the patients, clinicians, the public and policymakers, via appropriate avenues.

  12. Fleming KA, Horton S, Wilson ML, Atun R, DeStigter K, Flanigan J, et al.
    Lancet, 2021 Nov 27;398(10315):1997-2050.
    PMID: 34626542 DOI: 10.1016/S0140-6736(21)00673-5
  13. Alam MK, Abutayyem H, Alzabni KMD, Almuhyi NHS, Alsabilah KAS, Alkubaydan FST, et al.
    Cureus, 2023 Aug;15(8):e44243.
    PMID: 37645665 DOI: 10.7759/cureus.44243
    The literature on the impact of temporomandibular disorders (TMDs) on orthodontic management or vice versa lacks clarity. This study presents a review that aims to evaluate the influence of TMDs on orthodontic management and explore the association between TMDs and various aspects of orthodontic treatment. A systematic search was conducted across multiple databases to identify relevant articles documenting the correlation between TMD incidence and orthodontic treatment to achieve the objectives. The selection process followed predefined criteria, and the selected studies underwent bias assessment using the AXIS tool and Cochrane risk of bias (RoB) tool. Among the articles identified, nine studies were deemed suitable for inclusion in the review. The findings from the subsequent meta-analysis indicated a significant overall effect, suggesting that orthodontic treatment may increase the risk of developing TMD. Furthermore, the analysis revealed that patients with TMD had higher odds of experiencing orthodontic issues than those without TMD. Subgroup analysis further demonstrated that orthodontic treatment could have a negative impact on the psychological well-being of TMD patients, while its effect on TMD incidence was found to be negligible. The results highlight the need for additional research to gain a better understanding of the underlying mechanisms and develop appropriate interventions aimed at minimizing the risk of TMD in patients undergoing orthodontic treatment. Clinicians should be aware of TMD as a potential complication of orthodontic treatment and implement appropriate monitoring strategies.
  14. GBD 2019 Lip, Oral, and Pharyngeal Cancer Collaborators, Cunha ARD, Compton K, Xu R, Mishra R, Drangsholt MT, et al.
    JAMA Oncol, 2023 Oct 01;9(10):1401-1416.
    PMID: 37676656 DOI: 10.1001/jamaoncol.2023.2960
    IMPORTANCE: Lip, oral, and pharyngeal cancers are important contributors to cancer burden worldwide, and a comprehensive evaluation of their burden globally, regionally, and nationally is crucial for effective policy planning.

    OBJECTIVE: To analyze the total and risk-attributable burden of lip and oral cavity cancer (LOC) and other pharyngeal cancer (OPC) for 204 countries and territories and by Socio-demographic Index (SDI) using 2019 Global Burden of Diseases, Injuries, and Risk Factors (GBD) Study estimates.

    EVIDENCE REVIEW: The incidence, mortality, and disability-adjusted life years (DALYs) due to LOC and OPC from 1990 to 2019 were estimated using GBD 2019 methods. The GBD 2019 comparative risk assessment framework was used to estimate the proportion of deaths and DALYs for LOC and OPC attributable to smoking, tobacco, and alcohol consumption in 2019.

    FINDINGS: In 2019, 370 000 (95% uncertainty interval [UI], 338 000-401 000) cases and 199 000 (95% UI, 181 000-217 000) deaths for LOC and 167 000 (95% UI, 153 000-180 000) cases and 114 000 (95% UI, 103 000-126 000) deaths for OPC were estimated to occur globally, contributing 5.5 million (95% UI, 5.0-6.0 million) and 3.2 million (95% UI, 2.9-3.6 million) DALYs, respectively. From 1990 to 2019, low-middle and low SDI regions consistently showed the highest age-standardized mortality rates due to LOC and OPC, while the high SDI strata exhibited age-standardized incidence rates decreasing for LOC and increasing for OPC. Globally in 2019, smoking had the greatest contribution to risk-attributable OPC deaths for both sexes (55.8% [95% UI, 49.2%-62.0%] of all OPC deaths in male individuals and 17.4% [95% UI, 13.8%-21.2%] of all OPC deaths in female individuals). Smoking and alcohol both contributed to substantial LOC deaths globally among male individuals (42.3% [95% UI, 35.2%-48.6%] and 40.2% [95% UI, 33.3%-46.8%] of all risk-attributable cancer deaths, respectively), while chewing tobacco contributed to the greatest attributable LOC deaths among female individuals (27.6% [95% UI, 21.5%-33.8%]), driven by high risk-attributable burden in South and Southeast Asia.

    CONCLUSIONS AND RELEVANCE: In this systematic analysis, disparities in LOC and OPC burden existed across the SDI spectrum, and a considerable percentage of burden was attributable to tobacco and alcohol use. These estimates can contribute to an understanding of the distribution and disparities in LOC and OPC burden globally and support cancer control planning efforts.

  15. Godman B, Haque M, Leong T, Allocati E, Kumar S, Islam S, et al.
    Front Public Health, 2021;9:671961.
    PMID: 34249838 DOI: 10.3389/fpubh.2021.671961
    Background: Diabetes mellitus rates continue to rise, which coupled with increasing costs of associated complications has appreciably increased global expenditure in recent years. The risk of complications are enhanced by poor glycaemic control including hypoglycaemia. Long-acting insulin analogues were developed to reduce hypoglycaemia and improve adherence. Their considerably higher costs though have impacted their funding and use. Biosimilars can help reduce medicine costs. However, their introduction has been affected by a number of factors. These include the originator company dropping its price as well as promoting patented higher strength 300 IU/ml insulin glargine. There can also be concerns with different devices between the manufacturers. Objective: To assess current utilisation rates for insulins, especially long-acting insulin analogues, and the rationale for patterns seen, across multiple countries to inform strategies to enhance future utilisation of long-acting insulin analogue biosimilars to benefit all key stakeholders. Our approach: Multiple approaches including assessing the utilisation, expenditure and prices of insulins, including biosimilar insulin glargine, across multiple continents and countries. Results: There was considerable variation in the use of long-acting insulin analogues as a percentage of all insulins prescribed and dispensed across countries and continents. This ranged from limited use of long-acting insulin analogues among African countries compared to routine funding and use across Europe in view of their perceived benefits. Increasing use was also seen among Asian countries including Bangladesh and India for similar reasons. However, concerns with costs and value limited their use across Africa, Brazil and Pakistan. There was though limited use of biosimilar insulin glargine 100 IU/ml compared with other recent biosimilars especially among European countries and Korea. This was principally driven by small price differences in reality between the originator and biosimilars coupled with increasing use of the patented 300 IU/ml formulation. A number of activities were identified to enhance future biosimilar use. These included only reimbursing biosimilar long-acting insulin analogues, introducing prescribing targets and increasing competition among manufacturers including stimulating local production. Conclusions: There are concerns with the availability and use of insulin glargine biosimilars despite lower costs. This can be addressed by multiple activities.
  16. Zolio L, Lim KY, McKenzie JE, Yan MK, Estee M, Hussain SM, et al.
    Osteoarthritis Cartilage, 2021 08;29(8):1096-1116.
    PMID: 33971205 DOI: 10.1016/j.joca.2021.03.021
    OBJECTIVE: To determine the prevalence of neuropathic-like pain (NP) and pain sensitization (PS) defined by self-report questionnaires in knee and hip osteoarthritis, and whether prevalence is potentially explained by disease-severity or affected joint.

    DESIGN: MEDLINE, EMBASE, CINAHL were systematically searched (1990-April 2020) for studies describing the prevalence of NP and PS in knee and hip osteoarthritis using self-report questionnaires. Random-effects meta-analysis was performed. Statistical heterogeneity between studies and sub-groups (affected joint and population source as a proxy for disease severity) was assessed (I2 statistic and the Chi-squared test).

    RESULTS: From 2,706 non-duplicated references, 39 studies were included (2011-2020). Thirty-six studies reported on knee pain and six on hip pain. For knee osteoarthritis, the pooled prevalence of NP was: using PainDETECT, possible NP(score ≥13) 40% (95%CI 32-48%); probable NP(score >18) 20% (95%CI 15-24%); using Self-Report Leeds Assessment of Neuropathic Symptoms and Signs, 32% (95%CI 26-38%); using Douleur Neuropathique (DN4) 41% (95% CI 24-59%). The prevalence of PS using Central Sensitization Inventory (CSI) was 36% (95% CI 12-59%). For hip osteoarthritis, the pooled prevalence of NP was: using PainDETECT, possible NP 29% (95%CI 22-37%%); probable NP 9% (95%CI 6-13%); using DN4 22% (95%CI 12-31%) in one study. The prevalence of possible NP pain was higher at the knee (40%) than the hip (29%) (difference 11% (95% CI 0-22%), P = 0.05).

    CONCLUSIONS: Using self-report questionnaire tools, NP was more prevalent in knee than hip osteoarthritis. The prevalence of NP in knee and hip osteoarthritis were similar for each joint regardless of study population source or tool used. Whether defining NP using self-report questionnaires enables more effective targeted therapy in osteoarthritis requires investigation.

  17. Abbas A, Nazir H, Naseer MM, Bolte M, Hussain S, Hafeez N, et al.
    PMID: 24177882 DOI: 10.1016/j.saa.2013.10.023
    A series of new pyrazoline derivatives (1b-4c) bearing N-acyl arms and nine to twelve carbon long alkoxy side chains was synthesized and characterized on the basis of spectroscopic data and microanalysis. The nature of self-assembly to understand the interplay of alkoxy chain crystallization and various supramolecular interactions was investigated using single crystal X-ray diffraction studies. Interesting self-assembled supramolecular structures of 1b and 4c were observed in the crystal lattice owing to various CH⋯O, H⋯H, CH⋯π, lonepair⋯π and π⋯π interactions. Further, all the synthesized compounds (1b-4c) were screened for their in vitro antifungal and anti-inflammatory activities. Compounds 2b, 3b, 2c and 3c showed significant to moderate antifungal activity against Microsporum canis whereas most of the other compounds were found inactive against all the five tested fungal strains. Good anti-inflammatory activity was observed for compounds 1b with IC50 value 331 μM compared to 273 μM for Indomethacine, a standard reference drug. The bio-activity data demonstrates the relationship between lipophilicity, solubility and bioavailability.
  18. Khan KM, Qurban S, Salar U, Taha M, Hussain S, Perveen S, et al.
    Bioorg Chem, 2016 10;68:245-58.
    PMID: 27592296 DOI: 10.1016/j.bioorg.2016.08.010
    Current study based on the synthesis of new thiazole derivatives via "one pot" multicomponent reaction, evaluation of their in vitro α-glucosidase inhibitory activities, and in silico studies. All synthetic compounds were fully characterized by (1)H NMR, (13)C NMR and EIMS. CHN analysis was also performed. These newly synthesized compounds showed activities in the range of IC50=9.06±0.10-82.50±1.70μM as compared to standard acarbose (IC50=38.25±0.12μM). It is worth mentioning that most of the compounds such as 1 (IC50=23.60±0.39μM), 2 (IC50=22.70±0.60μM), 3 (IC50=22.40±0.32μM), 4 (IC50=26.5±0.40μM), 6 (IC50=34.60±0.60μM), 7 (IC50=26.20±0.43μM), 8 (IC50=14.06±0.18μM), 9 (IC50=17.60±0.28μM), 10 (IC50=27.16±0.41μM), 11 (IC50=19.16±0.19μM), 12 (IC50=9.06±0.10μM), 13 (IC50=12.80±0.21μM), 14 (IC50=11.94±0.18μM), 15 (IC50=16.90±0.20μM), 16 (IC50=12.60±0.14μM), 17 (IC50=16.30±0.29μM), and 18 (IC50=32.60±0.61μM) exhibited potent inhibitory potential. Molecular docking study was performed in order to understand the molecular interactions between the molecule and enzyme. Newly identified α-glucosidase inhibitors except few were found to be completely non-toxic.
  19. Rahim F, Ullah H, Javid MT, Wadood A, Taha M, Ashraf M, et al.
    Bioorg Chem, 2015 Oct;62:15-21.
    PMID: 26162519 DOI: 10.1016/j.bioorg.2015.06.006
    A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94μM when compared with the standard acarbose (IC50, 38.25±0.12μM). Compound (8) (IC50, 18.23±0.03μM) and compound (7) (IC50=36.75±0.05μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.
  20. Alomari M, Taha M, Rahim F, Selvaraj M, Iqbal N, Chigurupati S, et al.
    Bioorg Chem, 2021 03;108:104638.
    PMID: 33508679 DOI: 10.1016/j.bioorg.2021.104638
    A series of nineteen (1-19) indole-based-thiadiazole derivatives were synthesized, characterized by 1HNMR, 13C NMR, MS, and screened for α-glucosidase inhibition. All analogs showed varied α-glucosidase inhibitory potential with IC50 value ranged between 0.95 ± 0.05 to 13.60 ± 0.30 µM, when compared with the standard acarbose (IC50 = 1.70 ± 0.10). Analogs 17, 2, 1, 9, 7, 3, 15, 10, 16, and 14 with IC50 values 0.95 ± 0.05, 1.10 ± 0.10, 1.30 ± 0.10, 1.60 ± 0.10, 2.30 ± 0.10, 2.30 ± 0.10, 2.80 ± 0.10, 4.10 ± 0.20 and 4.80 ± 0.20 µM respectively showed highest α-glucosidase inhibition. All other analogs also exhibit excellent inhibitory potential. Structure activity relationships have been established for all compounds primarily based on substitution pattern on the phenyl ring. Through molecular docking study, binding interactions of the most active compounds were confirmed. We further studied the kinetics study of analogs 1, 2, 9 and 17 and found that they are Non-competitive inhibitors.
Filters
Contact Us

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

External Links