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  1. Hambali IU, Abdullah FFJB, Bhutto KR, Mohd Azmi ML, Wahid AH, Zakaria Z, et al.
    Trop Anim Health Prod, 2019 May;51(4):781-789.
    PMID: 30449009 DOI: 10.1007/s11250-018-1755-8
    Mastitis is the inflammation of the mammary gland due to microbial infiltration causing a reduced mammary function. This study aims at developing a vaccine using Malaysian local isolate of Staphylococcus aureus and evaluating serum amyloid A, Interleukin-10, IgM and IgG responses periodically. Four bacterin concentrations (106, 107, 108 and 109 cfu/ml of the local isolate of S. aureus) were adjuvanted with aluminium potassium sulphate. Thirty cows grouped into 4 treatment groups (G-) were vaccinated (2 ml) intramuscularly, with a fifth G-A as control. The mean concentration (MC) of serum amyloid A (SAA) was significantly different (sig-d) (p ˂ 0.05) in G-D at 0 h post vaccination (PV), 3 h PV, 24 h PV, weeks 1, 2, 3 and 4 PV (6-, 15-, 5-, 12-, 11-, 4- and 11-fold increased (FI) respectively). The MC of serum amyloid A was also sig-d in G-E at 0 h PV, weeks 1, 2 and 4 PV (3, 8, 5 and 8 FI respectively). The MC of IL-10 was sig-d in G-D and C at 3 h PV and week 2 PV (5 and 2 FI respectively). The IgM MC was sig-d in G-B and C at 3 h PV (5 and 6 FI respectively), at 24 h PV (5 and 9 FI respectively), at week 3 PV(2 and 2 FI respectively) and week 4 PV (3 and 4 FI respectively). The MC of IgG was sig-d in G-E at 0 h, 3 h and week 3 PV(5, 6 and 2 FI respectively) and in G-D at weeks 1-4 (3, 3, 3 and 5 FI respectively). In conclusion, elevated levels of SAA, IgG and IL-10 in G-D(108) informed our choice of best dosage which can be used to evoke immunity in cows.
  2. Mohd Abd Razak MR, Norahmad NA, Md Jelas NH, Jusoh B, Muhammad A, Mohmad Misnan N, et al.
    BMC Res Notes, 2019 Apr 03;12(1):206.
    PMID: 30944031 DOI: 10.1186/s13104-019-4242-z
    OBJECTIVE: The purpose of this study was to profile and identify the endothelial cell biology related genes that are affected by dengue virus infection in the liver tissue of AG129 mice, with and without Carica papaya leaf juice treatment.

    RESULTS: The dengue fever mouse model was established by intraperitoneal inoculation of dengue virus, New Guinea C strain at 2 × 106 PFU. Daily oral administration of 1000 mg/kg freeze-dried C. papaya leaf juice (FCPLJ) was done starting from day 1 to day 3 post infection. The RNA was extracted from liver tissues harvested on day 4 post infection. The expression levels of 84 genes related to mouse endothelial cell biology were determined by qRT-PCR technique. Dengue virus infection upregulated 15 genes and downregulated two genes in the liver of AG129 mice. The FCPLJ treatment upregulated monocyte chemoattractant protein 1 and downregulated intercellular adhesion molecule 1, integrin beta 3 and fibronectin 1 genes during dengue virus infection. The data showed the potential effect of FCPLJ treatment on the expression profile of endothelial cell biology related genes in the liver of dengue virus infected-AG129 mice. Further proteomic studies are needed to determine the functional roles of the genes affected by FCPLJ treatment.

  3. Othman A, Goggin KA, Tahir NI, Brodrick E, Singh R, Sambanthamurthi R, et al.
    BMC Res Notes, 2019 Apr 16;12(1):229.
    PMID: 30992056 DOI: 10.1186/s13104-019-4263-7
    OBJECTIVE: The addition of residual oils such as palm fibre oil (PFO) and sludge palm oil (SPO) to crude palm oil (CPO) can be problematic within supply chains. PFO is thought to aggravate the accumulation of monochloropropanediols (MCPDs) in CPO, whilst SPO is an acidic by-product of CPO milling and is not fit for human consumption. Traditional targeted techniques to detect such additives are costly, time-consuming and require highly trained operators. Therefore, we seek to assess the use of gas chromatography-ion mobility spectrometry (GC-IMS) for rapid, cost-effective screening of CPO for the presence of characteristic PFO and SPO volatile organic compound (VOC) fingerprints.

    RESULTS: Lab-pressed CPO and commercial dispatch tank (DT) CPO were spiked with PFO and SPO, respectively. Both additives were detectable at concentrations of 1% and 10% (w/w) in spiked lab-pressed CPO, via seven PFO-associated VOCs and 21 SPO-associated VOCs. DT controls could not be distinguished from PFO-spiked DT CPO, suggesting these samples may have already contained low levels of PFO. DT controls were free of SPO. SPO was detected in all SPO-spiked dispatch tank samples by all 21 of the previously distinguished VOCs and had a significant fingerprint consisting of four spectral regions.

  4. Awaluddin SMB, Ying Ying C, Yoep N, Paiwai F, Lodz NA, Muhammad EN, et al.
    Asia Pac J Public Health, 2019 Nov;31(8_suppl):57S-64S.
    PMID: 31523984 DOI: 10.1177/1010539519872642
    Parental protective factors do play an important role in preventing Internet addiction. A self-administered questionnaire was used to measure health risk behaviors among Malaysian adolescents. The prevalence of Internet addiction was significantly higher among adolescents with perceived lack of parental supervision (30.1% [95% confidence interval (CI) = 28.7-31.4]) and lack of parental connectedness (30.1% [95% CI = 28.5-31.7]), compared with their counterparts. Adolescents who perceived a lack of parental supervision, respect for privacy, connectedness, and bonding were more likely to have Internet addiction: (adjusted odds ratio [aOR] = 1.39; 95% CI = 1.27-1.52), (aOR = 1.23; 95% CI = 1.16-1.31), (aOR = 1.09; 95% CI = 1.02-1.16), (aOR = 1.06; 95% CI = 1.00-1.12), respectively. Among girls, Internet addiction was associated with those who perceived lack in all 4 parental factors, while among boys, those who perceived lack of parental supervision and respect for privacy were more prone to Internet addiction.
  5. Rahim F, Zaman K, Taha M, Ullah H, Ghufran M, Wadood A, et al.
    Bioorg Chem, 2020 01;94:103394.
    PMID: 31699396 DOI: 10.1016/j.bioorg.2019.103394
    Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50 = 2.20 ± 0.1to 88.60 ± 1.70 µM) when compared with standard drug acarbose (IC50 = 38.45 ± 0.80 µM). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.
  6. Jummaat F, Adnan AS, Ab Hamid SA, Hor JN, Nik Mustofar NN, Muhammad Asri NA, et al.
    J Obstet Gynaecol, 2021 Jan;41(1):38-43.
    PMID: 33124936 DOI: 10.1080/01443615.2019.1679731
    Preeclampsia patients have frequently been found to experience hyperuricaemia and this may result in poor outcomes compared to those with normal uric acid levels. This study aimed to determine the relationship of hyperuricaemia in pre-eclampsia patients with foetal and maternal outcomes. This prospective cohort study involved 79 patients in a tertiary centre from year 2016 to 2018. Blood samples were taken antenatally and at the 6th week, post-delivery for renal function including serum uric acid level. Our findings indicate that there was a higher incidence of poor maternal and foetal outcomes in the hyperuricaemia group than the normal uric acid group. Serum uric acid has been shown to be a significant predictor for low birth weight and premature delivery in preeclampsia patients. It was also found that there was a significant negative correlation between uric acid level and antenatal creatinine clearance (rs = -0.338, p = .002). The assessment of the serum uric acid level seems to be important to ensure better outcomes in patients with preeclampsia.Impact statementWhat is already known on this subject? Preeclampsia is a serious pregnancy-related complication and remains as one of the most important cause of maternal and foetal morbidity and mortality, affecting 2-8% in all pregnancy. Many studies have established the association between hyperuricaemia and preeclampsia. Besides, numerous studies have found that hyperuricaemia contributed to adverse maternal and foetal outcomes.What the results of this study add? There was a significant increase in adverse foetal and maternal outcomes in the hyperuricaemia group compared to the normal uric acid group. This study revealed that serum uric acid remains a significant predictor for low birth weight and premature delivery in preeclampsia patients.What the implications are of these findings for clinical practice and/or further research? Hyperuricaemia does not merely become an indicator for the severity of disease in preeclampsia patients but also indicates adverse foetal outcomes. Large population-based studies are required to establish the absolute maternal and foetal outcomes in patients with hyperuricaemia. Besides, further studies are recommended on long-term implication of hyperuricaemia which is not limited to only during antenatal period.
  7. Mohammed M, Muhammad S, Mohammed FZ, Mustapha S, Sha'aban A, Sani NY, et al.
    J Racial Ethn Health Disparities, 2021 10;8(5):1267-1272.
    PMID: 33051749 DOI: 10.1007/s40615-020-00888-3
    BACKGROUND: The novel coronavirus disease (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) was first reported in China and later spread rapidly to other parts of the world, including Africa. Africa was projected to be devastated by COVID-19. There is currently limited data regarding regional predictors of mortality among patients with COVID-19. This study aimed to evaluate the independent risk factors associated with mortality among patients with COVID-19 in Africa.

    METHODS: A total of 1028 confirmed cases of COVID-19 from Africa with definite survival outcomes were identified retrospectively from an open-access individual-level worldwide COVID-19 database. The live version of the dataset is available at https://github.com/beoutbreakprepared/nCoV2019 . Multivariable logistic regression was conducted to determine the risk factors that independently predict mortality among patients with COVID-19 in Africa.

    RESULTS: Of the 1028 cases included in study, 432 (42.0%) were females with a median (interquartile range, IQR) age of 50 (24) years. Older age (adjusted odds ratio {aOR} 1.06; [95% confidence intervals {95% CI}, 1.04-1.08]), presence of chronic disease (aOR 9.63; [95% CI, 3.84-24.15]), travel history (aOR 2.44; [95% CI, 1.26-4.72]), as well as locations of Central Africa (aOR 0.14; [95% CI, 0.03-0.72]) and West Africa (aOR 0.12; [95% CI, 0.04-0.32]) were identified as the independent risk factors significantly associated with increased mortality among the patients with COVID-19.

    CONCLUSIONS: The COVID-19 pandemic is evolving gradually in Africa. Among patients with COVID-19 in Africa, older age, presence of chronic disease, travel history, and the locations of Central Africa and West Africa were associated with increased mortality. A regional response should prioritize strategies that will protect these populations. Also, conducting a further in-depth study could provide more insights into additional factors predictive of mortality in COVID-19 patients.

  8. Elhusseiny KM, Abd-Elhay FA, Kamel MG, Abd El Hamid Hassan HH, Muhammad El Tanany HH, Hong HT, et al.
    Ann Oncol, 2018 Nov;29 Suppl 9:ix104.
    PMID: 32177708 DOI: 10.1093/annonc/mdy438.035
  9. Andriani Y, Chaudhry GE, Oksal E, Pangestika I, Ramli NM, Mohamad H, et al.
    J Adv Pharm Technol Res, 2020 3 11;11(1):30-35.
    PMID: 32154156 DOI: 10.4103/japtr.JAPTR_164_19
    Atherosclerosis is a leading cause of death worldwide. The adverse side effects of currently available drugs urge to find more effective and safe remedial agents. Alternative candidates from natural resources are of great consequence in the emerging of new drugs. Pandanus tectorius (Pandanaceae) was traditionally used in Ayurvedic medicine to cure certain diseases. Thus, the current study conducted to elucidate the potency of P. tectorius fruit as antiatherosclerosis and antihypercholesterolemia agents through the regulation of high density lipoprotein (HDL) receptor (scavenger receptor [SR]-B1) gene expression and 3-hydroxy-3-methylglutaryl coenzyme A reductase reductase (HMGCR) in vitro, respectively. The P. tectorius fruit was noncytotoxic against the HepG2 cell line confirmed by 3-(4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazolium bromide assay. The P. tectorius fruit successfully upregulates the SR-B1 gene expression and downregulate the HMGCR. Moreover, anin vivo study showed that P. tectorius has good activity on the upregulation of HDL and subsequently downregulation of total cholesterol level. Moreover, P. tectorius fruit did not show any increase in toxicity biomarkers serum glutamic oxaloacetic transaminase and serum glutamate pyruvate transaminase in vivo. These results found that P. tectorius fruits have potency as the preventive agent for hypercholesterolemia and atherosclerosis via SR-B1 and HMGCR mechanisms of action.
  10. Taha M, Sain AA, Ali M, Anouar EH, Rahim F, Ismail NH, et al.
    Bioorg Chem, 2020 06;99:103819.
    PMID: 32325334 DOI: 10.1016/j.bioorg.2020.103819
    Leishmaniasis has affected a wider part of population around the globe. Most often, the existing regiments to battle against leishmaniasis are inadequate and limited. In our ongoing efforts to develop new leishmanicidal agents, we have synthesized a series of novel and symmetrical bis-Schiff base-disulfide hybrids 1-27. Intermediate disulfide was synthesized from corresponding 2-aminothiol followed by reacting the coupled adduct with various aromatic aldehydes. All these compounds showed outstanding inhibition when compared with standard (Table 1). Out of twenty seven analogues, twenty two analogues i.e. 1-5, 7-13, 17-21, 23-27 analogues showed excellent inhibitory potential with EC50 values ranging from 0.010 ± 0.00 to 0.096 ± 0.01 μM while five compounds i.e. 6, 14-16, and 22 showed good inhibitory potential with EC50 values ranging from 0.10 ± 0.00 to 0.137 ± 0.01 μM when compared with the standard Amphotericin B. Structure-activity relationship has been established while molecular docking studies were performed to pin the binding interaction of active molecules. This study will help to develop new antileishmanial lead compounds.
  11. Muhammad EN, Abdul Mutalip MH, Hasim MH, Paiwai F, Pan S, Mahmud MAF, et al.
    BMC Infect Dis, 2020 Nov 16;20(1):843.
    PMID: 33198646 DOI: 10.1186/s12879-020-05500-x
    BACKGROUND: Typhoid fever causes global morbidity and mortality and is a significant health burden, particularly in low- and middle-income countries. The direct fecal-oral route is the main transmission mode, but indirect environmental transmission could occur, particularly in urban settings. This study aimed to investigate the burden and trend of typhoid fever, reporting the coverage system between government and private practice and pattern of multidrug-resistant (MDR) typhoid cases in the urban Klang Valley area from 2011 to 2015.

    METHODS: The data from a cross-sectional study retrieved from the e-Notifikasi System, a national reporting system for communicable diseases provided by the Disease Control Division, Ministry of Health Malaysia and secondary data of all the typhoid cases were obtained from the public and private hospitals and laboratories in Klang Valley. Descriptive analysis was performed to examine the sociodemographic characteristics, spatial mapping was conducted to examine trends, and the crude incidence rates of confirmed typhoid cases and percentage of reporting coverage were calculated. Significant differences between MDR and non-MDR Salmonella typhi were determined in the patient's sociodemographic characteristics, which were analyzed using χ2 test. P values

  12. Ninomiya K, Arimura H, Chan WY, Tanaka K, Mizuno S, Muhammad Gowdh NF, et al.
    PLoS One, 2021;16(1):e0244354.
    PMID: 33428651 DOI: 10.1371/journal.pone.0244354
    OBJECTIVES: To propose a novel robust radiogenomics approach to the identification of epidermal growth factor receptor (EGFR) mutations among patients with non-small cell lung cancer (NSCLC) using Betti numbers (BNs).

    MATERIALS AND METHODS: Contrast enhanced computed tomography (CT) images of 194 multi-racial NSCLC patients (79 EGFR mutants and 115 wildtypes) were collected from three different countries using 5 manufacturers' scanners with a variety of scanning parameters. Ninety-nine cases obtained from the University of Malaya Medical Centre (UMMC) in Malaysia were used for training and validation procedures. Forty-one cases collected from the Kyushu University Hospital (KUH) in Japan and fifty-four cases obtained from The Cancer Imaging Archive (TCIA) in America were used for a test procedure. Radiomic features were obtained from BN maps, which represent topologically invariant heterogeneous characteristics of lung cancer on CT images, by applying histogram- and texture-based feature computations. A BN-based signature was determined using support vector machine (SVM) models with the best combination of features that maximized a robustness index (RI) which defined a higher total area under receiver operating characteristics curves (AUCs) and lower difference of AUCs between the training and the validation. The SVM model was built using the signature and optimized in a five-fold cross validation. The BN-based model was compared to conventional original image (OI)- and wavelet-decomposition (WD)-based models with respect to the RI between the validation and the test.

    RESULTS: The BN-based model showed a higher RI of 1.51 compared with the models based on the OI (RI: 1.33) and the WD (RI: 1.29).

    CONCLUSION: The proposed model showed higher robustness than the conventional models in the identification of EGFR mutations among NSCLC patients. The results suggested the robustness of the BN-based approach against variations in image scanner/scanning parameters.

  13. M Hussain FB, Al-Khdhairawi AAQ, Kok Sing H, Muhammad Low AL, Anouar EH, Thomas NF, et al.
    J Nat Prod, 2020 12 24;83(12):3493-3501.
    PMID: 33233893 DOI: 10.1021/acs.jnatprod.9b01105
    Svalbardines A and B (1 and 2) and annularin K (3) were isolated from cultures of Poaceicola sp. E1PB, an endophyte isolated from the petals of Papaver dahlianum from Svalbard, Norway. Svalbardine A (1) is a pyrano[3,2-c]chromen-4-one, a new analogue of citromycetin. Svalbardine B (2) displays an unprecedented carbon skeleton based on a 5'-benzyl-spiro[chroman-3,7'-isochromene]-4,8'-dione core. Annularin K (3) is a hydroxylated derivative of annularin D. The structure of these new polyketides, along with those of known compounds 4-6, was established by spectrometric analysis, including extensive ESI-CID-MS
    n
    processing in the case of svalbardine B (2).
  14. Pervaiz I, Saleem H, Sarfraz M, Imran Tousif M, Khurshid U, Ahmad S, et al.
    Food Res Int, 2020 11;137:109606.
    PMID: 33233202 DOI: 10.1016/j.foodres.2020.109606
    Calligonum polygonoides L. also known as famine food plant, is normally consumed in times of food scarcity in India and Pakistan and also used traditionally in the management of common diseases. The present design aims to provide an insight into the medicinal potential of four solvent extracts of C. polygonoides via an assessment of its phytochemical profile, antioxidant and enzyme inhibitory potential. Phytochemical composition was estimated by deducing total bioactive constituents, UHPLC-MS secondary metabolites profile, and HPLC phenolic quantification. Antioxidant potential was determined via six methods (radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum total antioxidant capacity and metal chelation activity). Enzyme inhibitory potential was assessed against clinical enzymes (acetylcholinesterase -AChE, butyrylcholinesterase -BChE, tyrosinase, and α-amylase). The highest amounts of phenolic contents were found in chloroform extract (76.59 mg GAE/g extract) which may be attributed to its higher radical scavenging, reducing power and tyrosinase inhibition potential. The n-butanol extract containing the maximum amount of flavonoids (55.84 mg RE/g extract) exhibited highest metal chelating capacity. Similarly, the n-hexane extract was found to be most active against AChE (4.65 mg GALAE/g extract), BChE (6.59 mg GALAE/g extract), and α-amylase (0.70 mmol ACAE/g extract) enzymes. Secondary metabolite assessment of the crude methanol extract as determined by UHPLC-MS analysis revealed the presence of 24 (negative ionization mode) and 15 (positive ionization mode) secondary metabolites, with most of them belonging to phenolic, flavonoids, terpene, and alkaloid groups. Moreover, gallic acid and naringenin were the main phenolics quantified by HPLC-PDA analysis in all the tested extracts (except n-butanol extract). PCA statistical analysis was also conducted to establish any possible relationship amongst bioactive contents and biological activities. Overall, the C. polygonoides extracts could be further considered to isolate bioactive enzyme inhibitory and antioxidant natural phytocompounds.
  15. Anirudhan A, Okomoda VT, Mimi Iryani MT, Andriani Y, Abd Wahid ME, Tan MP, et al.
    Fish Shellfish Immunol, 2021 Feb;109:97-105.
    PMID: 33352338 DOI: 10.1016/j.fsi.2020.12.011
    Plants and herbal extracts are indispensable for controlling the spread of disease-causing bacteria, including those that infect aquatic organisms used in aquaculture. The use of plant or herbal extract is expected to be safe for aquatic animals and less harmful to the environment, as opposed to conventional therapeutic alternatives such as antibiotics that promote the occurrence of potential antibiotic-resistant bacteria when used improperly. The efficacy of Pandanus tectorius fruit extract in the regulation of Hsp70 expression, pro-phenoloxidase (ProPO), peroxinectin, penaeidin, crustin and transglutaminase, all immune peptides essential for Vibrio tolerance in white leg shrimp, Penaeus vannamei, was investigated in this study, which included the determination of the safety levels of the extract. Tolerance of shrimp against Vibrio parahaemolyticus, a pathogenic bacteria that causes Acute Hepatopancreas Necrosis Disease (AHPND), was assessed on the basis of median lethal dose challenge survival (LD50 = 106 cells/ml). Mortality was not observed 24 h after exposure of 0.5-6 g/L of the fruit extract, indicating that P. tectorius was not toxic to shrimp at these concentrations. A 24-h incubation of 2-6 g/L of the fruit extract increased shrimp tolerance to V. parahaemolyticus, with survival doubled when the maximum dose tested in this study was used. Concomitant with a rise in survival was the increase in immune-related proteins, with Hsp70, ProPO, peroxinectin, penaeidin, crustin and transglutaminase increased 10, 11, 11, 0.4, 8 and 13-fold respectively. Histological examination of the hepatopancreas and muscle tissues of Vibrio-infected shrimp primed with P. tectorius extract revealed reduced signs of histopathological degeneration, possibly due to the accumulation of Hsp70, a molecular chaperone crucial to cellular protein folding, tissue repair and immune response of living organisms, including Penaeid shrimp.
  16. Taufik Ramli MH, Lodz NA, Abdul Aziz FA, Maw Pin T, Alias N, Abdul Mutalip MH, et al.
    Geriatr Gerontol Int, 2020 Dec;20 Suppl 2:38-42.
    PMID: 33370861 DOI: 10.1111/ggi.14028
    AIMS: As the Malaysian population is aging rapidly, there is an urgent need for an effective management plan for healthy aging, to extend life expectancy and to improve quality of life (QoL). Urinary incontinence (UI), which is common in older persons, is often linked to reduced QoL. This study aimed to determine the effects of UI on QoL among older persons in Malaysia.

    METHODS: This study was based on data obtained from 3716 Malaysians aged ≥60 years as part of the National Health and Morbidity Survey (NHMS) 2018. QoL was measured using the Control, Autonomy, Self-realization and Pleasure 19-item (CASP-19) questionnaire. UI was measured using the Questionnaire Urinary Incontinence Diagnosis (QUID) score. Association between UI and QoL were examined using linear regression analysis, after controlling socio-demographic variables and comorbidities.

    RESULTS: Overall, the prevalence of UI was 5.2%. By subtypes, the prevalence of stress UI and urge UI were both 2.0%, while that of mixed UI was 1.3%. The UI group rated their lives more negatively in all four domains of QoL compared with non-UI group. Those who were incontinent had lower standardized scores on control and autonomy domains of CASP-19 as well as total score. Results from linear regression analysis indicated that UI had a significantly negative impact on control and autonomy domains of QoL after controlling for socio-demographic factors and comorbidities.

    CONCLUSION: UI contributes to a significant reduction on QoL of older persons. Healthcare providers need to be sensitive in evaluating and discussing UI, particularly with their older patients. Geriatr Gerontol Int 2020; 20: 38-42.

  17. 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.
  18. Sidik SM, Jaffar A, Foo CN, Muhammad NA, Abdul Manaf R, Ismail SIF, et al.
    BMJ Open, 2021 01 12;11(1):e039076.
    PMID: 33436465 DOI: 10.1136/bmjopen-2020-039076
    INTRODUCTION: Pelvic floor muscle training (PFMT) strongly recommended to incontinent pregnant women. The Kegel Exercise Pregnancy Training-app trial is a multicentre cluster-randomised study aims to assess the effectiveness and its cost-effectiveness of the mobile app guidance in PFMT among incontinent pregnant women.

    METHODS AND ANALYSIS: 370 pregnant women (aged 18 years old and above) will be recruited with International Consultation on Incontinence Questionnaire-Urinary Incontinence-Short Form. Ten clusters (primary care clinics) will be randomly assigned to either PFMT or usual care in a 1:1 ratio by an independent researcher (sealed envelope). The primary outcome will be urinary incontinence, and the secondary outcomes (quality of life; PFMT adherence, psychological status and mobile apps' usability) will be assessed at four measurement time points (t0: baseline) and postintervention (t1: 4 weeks, t2: 8 weeks and t3: 8 weeks postnatal). T-test analysis will determine any significant differences at the baseline between the control and intervention groups. The mixed-model analysis will determine the effectiveness of the intervention at the population-average level for both the primary and secondary outcomes. For the cost-effectiveness analysis, expenditures during the study and 6 months after the intervention will be compared between the groups using the multiway sensitivity analysis. The recruitment planned will be in December 2020, and the planned end of the study will be in August 2021.

    ETHICS AND DISSEMINATION: This study protocol was approved by the Ethics Committee for Research Involving Human Subjects, Universiti Putra Malaysia (JKEUPM-2019-368) and Medical Research and Ethics Committee (MREC), Ministry of Health Malaysia, NMRR-19-412-47116 (IIR) with the ANZCTR registration. This study will obtain informed written consent from all the study participants. The results which conform with the Consolidated Standards of Reporting Trials and the Recommendations for Interventional Trials will be published for dissemination in peer-reviewed journals and conference proceedings.

    TRIAL REGISTRATION NUMBER: ACTRN12619000379112.

  19. Arshad T, Khan KM, Rasool N, Salar U, Hussain S, Asghar H, et al.
    Bioorg Chem, 2017 06;72:21-31.
    PMID: 28346872 DOI: 10.1016/j.bioorg.2017.03.007
    On the basis of previous report on promising α-glucosidase inhibitory activity of 5-bromo-2-aryl benzimidazole derivatives, these derivatives were further screened for urease inhibitory and cytotoxicity activity in order to get more potent and non-cytotoxic potential dual inhibitor for the patients suffering from diabetes as well as peptic ulcer. In this study, all compounds showed varying degree of potency in the range of (IC50=8.15±0.03-354.67±0.19μM) as compared to standard thiourea (IC50=21.25±0.15μM). It is worth mentioning that derivatives 7 (IC50=12.07±0.05μM), 8 (IC50=10.57±0.12μM), 11 (IC50=13.76±0.02μM), 14 (IC50=15.70±0.12μM) and 22 (IC50=8.15±0.03μM) were found to be more potent inhibitors than standard. All compounds were also evaluated for cytotoxicity towards 3T3 mouse fibroblast cell line and found to be completely non-toxic. Previously benzimidazole 1-25 were also showed α-glucosidase inhibitory potential. In silico studies were performed on the lead molecules i.e.2, 7, 8, 11, 14, and 22, in order to rationalize the binding interaction of compounds with the active site of urease enzyme.
  20. Ur-Rehman A, Khan SG, Naqvi SAR, Ahmad M, Akhtar N, Bokhari TH, et al.
    Pak J Pharm Sci, 2021 Jan;34(1(Special)):441-446.
    PMID: 34275792
    A series of new derivatives of 4-(2-chloroethyl)morpholine hydrochloride (5) were efficiently synthesized. Briefly, different aromatic organic acids (1a-f) were refluxed to acquire respective esters (2a-f) using conc. H2SO4 as catalyst. The esters were subjected to nucleophillic substitution by monohydrated hydrazine to acquire hydrazides (3a-f). The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Finally, the derivatives, 6a-f, were prepared by reacting oxadiazoles (4a-f) with 5 using NaH as activator. Structures of all the derivatives were elucidated through 1D-NMR EI-MS and IR spectral data. All these molecules were subjected to antibacterial and hemolytic activities and showed good antibacterial and hemolytic potential relative to the reference standards.
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