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Fulltext The antibacterial efficacy of silver diamine fluoride (SDF) is not modulated by potassium iodide (KI) supplements: A study on in-situ plaque biofilms using viability real-time PCR with propidium monoazide

Abdullah N, Al Marzooq F, Mohamad S, Abd Rahman N, Rani KGA, Chi Ngo H, et al.

PLoS One, 2020;15(11):e0241519.
PMID: 33141868 DOI: 10.1371/journal.pone.0241519

Silver diamine fluoride (SDF) is commonly used to arrest caries lesions, especially in early childhood caries. Recently, it was suggested that SDF can be combined with potassium iodide (KI) to minimize the discoloration of demineralized dentine associated with SDF application. However, the antibacterial efficacy of SDF alone or combined with KI on in-situ biofilm is unknown. Hence, we compared the anti-plaque biofilm efficacy of two different commercially available SDF solutions, with or without KI, using an in-situ biofilm, analysed using viability real-time PCR with propidium monoazide (PMA). Appliance-borne in-situ biofilm samples (n = 90) were grown for a period of 6 h in five healthy subjects who repeated the experiment on three separate occasions, using a validated, novel, intraoral device. The relative anti-biofilm efficacy of two SDF formulations; 38.0% Topamine (SDFT) and 31.3%, Riva Star (SDFR), KI alone, and KI in combination with SDFR (SDFR+KI) was compared. The experiments were performed by applying an optimized volume of the agents onto the biofilm for 1min, mimicking the standard clinical procedure. Afterwards the viability of the residual biofilm bacteria was quantified using viability real-time PCR with PMA, then the percentage of viable from total bacteria was calculated. Both SDF formulations (SDFT and SDFR) exhibited potent antibacterial activities against the in-situ biofilm; however, there was non-significant difference in their efficacy. KI alone did not demonstrate any antibacterial effect, and there was non-significant difference in the antibacterial efficacy of SDF alone compared to SDF with KI, (SDFT v SDFR/KI). Thus, we conclude that the antibacterial efficacy of SDF against plaque biofilms is not modulated by KI supplements. Viability real-time PCR with PMA was successfully used to analyze the viability of naturally grown oral biofilm; thus, the same method can be used to test the antimicrobial effect of other agents on oral biofilms in future research.
Effect of irradiance on the emission of short-lived halocarbons from three common tropical marine microalgae

Lim YK, Keng FS, Phang SM, Sturges WT, Malin G, Abd Rahman N

PeerJ, 2019;7:e6758.
PMID: 31041152 DOI: 10.7717/peerj.6758

Marine algae have been reported as important sources of biogenic volatile halocarbons that are emitted into the atmosphere. These compounds are linked to destruction of the ozone layer, thus contributing to climate change. There may be mutual interactions between the halocarbon emission and the environment. In this study, the effect of irradiance on the emission of halocarbons from selected microalgae was investigated. Using controlled laboratory experiments, three tropical marine microalgae cultures, Synechococcus sp. UMACC 371 (cyanophyte), Parachlorella sp. UMACC 245 (chlorophyte) and Amphora sp. UMACC 370 (diatom) were exposed to irradiance of 0, 40 and 120 µmol photons m-2s-1. Stress in the microalgal cultures was indicated by the photosynthetic performance (Fv/Fm, maximum quantum yield). An increase in halocarbon emissions was observed at 120 µmol photons m-2s-1, together with a decrease in Fv/Fm. This was most evident in the release of CH3I by Amphora sp. Synechococcus sp. was observed to be the most affected by irradiance as shown by the increase in emissions of most halocarbons except for CHBr3 and CHBr2Cl. High positive correlation between Fv/Fm and halocarbon emission rates was observed in Synechococcus sp. for CH2Br2. No clear trends in correlation could be observed for the other halocarbons in the other two microalgal species. This suggests that other mechanisms like mitochondria respiration may contribute to halocarbon production, in addition to photosynthetic performance.
REPLY TO THE LETTER TO THE EDITOR: EARLY DETECTION OF HIGH-FREQUENCY PRESBYCUSIS AMONG NORMAL HEARING INDIVIDUALS

Aziz A, Md Daud MK, Nik Othman NA, Abd Rahman N

Otol Neurotol, 2021 02 01;42(2):345-346.
PMID: 33273310 DOI: 10.1097/MAO.0000000000002908
Computational-aided design: minimal peptide sequence to block dengue virus transmission into cells

Arumugam AC, Agharbaoui FE, Khazali AS, Yusof R, Abd Rahman N, Ahmad Fuaad AAH

J Biomol Struct Dyn, 2020 Dec 31.
PMID: 33382015 DOI: 10.1080/07391102.2020.1866074

Dengue virus (DV) infection is one of the main public health concerns, affecting approximately 390 million people worldwide, as reported by the World Health Organization. Yet, there is no antiviral treatment for DV infection. Therefore, the development of potent and nontoxic anti-DV, as a complement for the existing treatment strategies, is urgently needed. Herein, we investigate a series of small peptides inhibitors of DV antiviral activity targeting the entry process as the promising strategy to block DV infection. The peptides were designed based on our previously reported peptide sequence, DN58opt (TWWCFYFCRRHHPFWFFYRHN), to identify minimal effective inhibitory sequence through molecular docking and dynamics studies. The in silico designed peptides were synthesized using conventional Fmoc solid-phase peptide synthesis chemistry, purified by RP-HPLC and characterized using LCMS. Later, they were screened for their antiviral activity. One of the peptides, AC 001, was able to reduce about 40% of DV plaque formation. This observation correlates well with the molecular mechanics-Poisson-Boltzmann surface area (MM-PBSA) analysis - AC 001 showed the most favorable binding affinity through 60 ns simulations. Pairwise residue decomposition analysis has revealed four key residues that contributed to the binding of these peptides into the DV2 E protein pocket. This work identifies the minimal peptide sequence required to inhibit DV replication and explains the behavior observed on an atomic level using computational study.Communicated by Ramaswamy H. Sarma.
Fulltext Extended high frequency hearing loss in tinnitus-positive chronic suppurative otitis media patient

Mohd Salehuddin NS, Md Daud MK, Nik Othman NA, Abd Rahman N

Laryngoscope Investig Otolaryngol, 2021 Oct;6(5):1137-1141.
PMID: 34667858 DOI: 10.1002/lio2.651

Objectives: To determine the association between extended high frequency hearing loss and tinnitus in normal cochlear function based on a conventional audiometry chronic suppurative otitis media (CSOM) patient.
Design and methods: A cross-sectional study was conducted on 220 ears diagnosed as having CSOM with an equal number of tinnitus and without tinnitus groups. Only those with normal cochlear function based on conventional pure tone audiometry (250 Hz to 8 kHz) were included. They were further tested for hearing at extended high frequencies of up to 16 kHz. The severity of tinnitus was tested using a tinnitus questionnaire.
Results: The prevalence of extended high frequency hearing loss in the normal cochlear function CSOM patients with tinnitus was 81.8% (95% CI 74.5%, 89.1%), whereas the prevalence in the tinnitus negative group was 30.0% (95% CI 21.3%, 38.7%). There was a significant association between extended high frequency hearing loss and tinnitus in CSOM patients (P
Fulltext Synthesis, Biological Evaluation and Molecular Modelling of 2'-Hydroxychalcones as Acetylcholinesterase Inhibitors

Sukumaran SD, Chee CF, Viswanathan G, Buckle MJ, Othman R, Abd Rahman N, et al.

Molecules, 2016 Jul 22;21(7).
PMID: 27455222 DOI: 10.3390/molecules21070955

A series of 2'-hydroxy- and 2'-hydroxy-4',6'-dimethoxychalcones was synthesised and evaluated as inhibitors of human acetylcholinesterase (AChE). The majority of the compounds were found to show some activity, with the most active compounds having IC50 values of 40-85 µM. Higher activities were generally observed for compounds with methoxy substituents in the A ring and halogen substituents in the B ring. Kinetic studies on the most active compounds showed that they act as mixed-type inhibitors, in agreement with the results of molecular modelling studies, which suggested that they interact with residues in the peripheral anionic site and the gorge region of AChE.
Fulltext Suppression of Staphylococcus aureus biofilm formation and virulence by a benzimidazole derivative, UM-C162

Kong C, Chee CF, Richter K, Thomas N, Abd Rahman N, Nathan S

Sci Rep, 2018 02 09;8(1):2758.
PMID: 29426873 DOI: 10.1038/s41598-018-21141-2

Staphylococcus aureus is a major cause of nosocomial infections and secretes a diverse spectrum of virulence determinants as well as forms biofilm. The emergence of antibiotic-resistant S. aureus highlights the need for alternative forms of therapeutics other than conventional antibiotics. One route to meet this need is screening small molecule derivatives for potential anti-infective activity. Using a previously optimized C. elegans - S. aureus small molecule screen, we identified a benzimidazole derivative, UM-C162, which rescued nematodes from a S. aureus infection. UM-C162 prevented the formation of biofilm in a dose-dependent manner without interfering with bacterial viability. To examine the effect of UM-C162 on the expression of S. aureus virulence genes, a genome-wide transcriptome analysis was performed on UM-C162-treated pathogen. Our data indicated that the genes associated with biofilm formation, particularly those involved in bacterial attachment, were suppressed in UM-C162-treated bacteria. Additionally, a set of genes encoding vital S. aureus virulence factors were also down-regulated in the presence of UM-C162. Further biochemical analysis validated that UM-C162-mediated disruption of S. aureus hemolysins, proteases and clumping factors production. Collectively, our findings propose that UM-C162 is a promising compound that can be further developed as an anti-virulence agent to control S. aureus infections.
Fulltext Measuring Pro-Environmental Behavior Triggered by Environmental Values

Ahmat Zainuri N, Abd-Rahman N, Halim L, Chan MY, Mohd Bazari NN

Int J Environ Res Public Health, 2022 Nov 30;19(23).
PMID: 36498088 DOI: 10.3390/ijerph192316013

Pro-environmental behavior in addressing climate change is influenced by multi-dimensional factors-knowledge, values, intention and sociodemographic background. Correlational studies between environmental values and environmental behaviors have not been able to determine values or behaviors that need to be given priority in future interventions. Therefore, this study firstly determined the environmental values and pro-environmental behavior that are easy or difficult to embrace by 152 respondents with low socioeconomic background. Secondly, we identified the extent pro-environmental behavior is triggered by environmental values. This survey study employs the Rasch analysis model. The respondents had difficulty in associating themselves with biospheric values however readily demonstrated consideration toward altruistic values, especially related to concerns for future generations. In terms of environmental conservation behavior, the respondents were not willing to relinquish comfort easily, such as giving up self-driving and taking public transportation or reducing usage of electricity. In addition, adults of low socioeconomic background find it difficult to endorse statements such as getting involved in campaigns related to environmental conservation. Thus, younger family members must be educated about conservation behaviors such as environmental campaigns commonly offered at schools, and these youngsters can be encouraged to extend their role by educating their parents.
Fulltext Evaluation of the current bacteriological profile and antibiotic sensitivity pattern in chronic suppurative otitis media

Wan Draman WNA, Md Daud MK, Mohamad H, Hassan SA, Abd Rahman N

Laryngoscope Investig Otolaryngol, 2021 Dec;6(6):1300-1306.
PMID: 34938866 DOI: 10.1002/lio2.682

OBJECTIVE: To determine the current microbiological profile of chronic suppurative otitis media (CSOM), their antimicrobial sensitivity, their resistance pattern to locally available antibiotics and the appropriate antibiotic against isolated microorganisms causing CSOM.
METHODS: This cross-sectional study involved 91 ear swab specimens obtained from patients clinically diagnosed with active CSOM. Swabs were cultured for microbial identification according to a standard protocol. We performed antibiotic susceptibility testing, using the modified Kirby-Bauer disc diffusion method, and the diameter of the inhibition zone was interpreted based Clinical Laboratory Standards Institute guidelines.
RESULTS: Microbial growth was seen in 85 (93.4%) samples, but 6 (6.6%) samples had no growth. Among the samples with growth, 63 (69.2%) were monomicrobial, 13 (14.3%) were polymicrobial, and 9 (9.9%) were of mixed growth with more than three microorganisms. The most common bacteria isolated was Pseudomonas aeruginosa (32.6%) followed by Staphylococcus aureus (16.9%) and Klebsiella spp. (5.6%). The most sensitive antibiotics against P aeruginosa were ceftazidime, meropenem, piperacillin-tazobactam, and cefepime. S aureus showed the highest sensitivity toward rifampin, cefoxitin, and fusidic acid.
CONCLUSIONS: The bacteriological profile of CSOM showed a high prevalence of P aeruginosa, followed by S aureus and Klebsiella spp. with different distributions in different age groups. We observed a declining pattern of their antibiotic sensitivity. It is important to be aware of the current trend of the bacteriological profiles and to revise the antibiotic regime according to both the sensitivity and age groups.Level of Evidence: NA.
Halocarbon emissions by selected tropical seaweeds exposed to different temperatures

Keng FS, Phang SM, Abd Rahman N, Yeong HY, Malin G, Leedham Elvidge E, et al.

Phytochemistry, 2021 Oct;190:112869.
PMID: 34274551 DOI: 10.1016/j.phytochem.2021.112869

Four tropical seaweeds, Gracilaria manilaensis Yamamoto & Trono, Ulva reticulata Forsskål, Kappaphycus alvarezii (Doty) L.M.Liao and Turbinaria conoides (J.Agardh) Kützing, collected from various habitats throughout Malaysia, were subjected to temperatures of 40, 35, 30, 25 and 20 °C in the laboratory. An exposure range of 21-38 °C is reported for Malaysian waters. The effect of the temperature exposures on the halocarbon emissions of the seaweeds were determined 4 and 28 h after treatment. The emission rates for a suite of six halocarbons commonly emitted by seaweeds, bromoform (CHBr3), dibromomethane (CH2Br2), diiodomethane (CH2I2), iodomethane (CH3I), dibromochloromethane (CHBr2Cl) and dichlorobromomethane (CHBrCl2), were measured using a cryogenic purge-and-trap sample preparation system coupled to a gas chromatography-mass spectrometry. The emission rate of CHBr3 was the highest of the six halocarbons for all the seaweeds under all the temperatures tested, followed by CH2Br2, and CH2I2. The emission rates were affected by temperature change and exposure duration, but overall responses were unique to each seaweed species. Larger decreases in the emissions of CHBr3, CH2Br2, CH2I2 and CHBr2Cl were found for K. alvarezii and T. conoides after 4 h at 40 °C. In both cases there was a >90% (p
Fulltext Determining food safety in canned food using fuzzy logic based on sulphur dioxide, benzoic acid and sorbic acid concentration

Mavani NR, Mohd Ali J, Hussain MA, Abd Rahman N, Hashim H

Heliyon, 2024 Feb 29;10(4):e26273.
PMID: 38384537 DOI: 10.1016/j.heliyon.2024.e26273

Canned food market demand has arisen due to the higher need for instant and ready-to-eat food. Food preservatives are often added to canned and processed foods to prolong their shelf life and help to sustain the quality, taste, color, and food texture. However, excessive usage of such food preservatives can lead to various diseases and health issues including palpitations, allergies, and cancer. Therefore, food preservative detection in food samples is essential for safe consumption and health well-being. This paper proposed a fuzzy logic framework to determine the safety of food products based on the concentration of sulphur dioxide (SD), benzoic acid (BA), and sorbic acid (SA) in five different food categories as referred to the Food Acts 1983 and Food Regulations 1985 in Malaysia. The fuzzy logic framework comprises of Mamdani inference system design with 90 fuzzy rules, 15 and 5 membership functions for both the input and output parameters respectively. 50 random values and 10 lab analysis results based on the industrial samples were used to validate the developed algorithms in ensuring the safety of the food products. The membership functions generated for the three inputs (SD, BA, and SA) during the fuzzification steps are based on the maximum allowable limit from the food acts. The defuzzification of fuzzy logic gave an average output value of 0.1565, 0.1350, 0.1150, 0.1100, and 0.1550 for chicken curry with potatoes, satay sauce, sardine in tomato sauce, anchovies paste, and sardine spread accordingly. Results obtained from the fuzzy logic framework concluded that all the industrial samples are safe to be eaten and comply with the Sixth Schedule, Regulation 20 in both Acts.
Fulltext Estimation of soil erodibility in Peninsular Malaysia: A case study using multiple linear regression and artificial neural networks

Rehman MA, Abd Rahman N, Ibrahim ANH, Kamal NA, Ahmad A

Heliyon, 2024 Apr 15;10(7):e28854.
PMID: 38576554 DOI: 10.1016/j.heliyon.2024.e28854

Soil erodibility (K) is an essential component in estimating soil loss indicating the soil's susceptibility to detach and transport. Data Computing and processing methods, such as artificial neural networks (ANNs) and multiple linear regression (MLR), have proven to be helpful in the development of predictive models for natural hazards. The present case study aims to assess the efficiency of MLR and ANN models to forecast soil erodibility in Peninsular Malaysia. A total of 103 samples were collected from various sites and K values were calculated using the Tew equation developed for Malaysian soil. From several extracted parameters, the outcomes of correlation and principal component analysis (PCA) revealed the influencing factors to be used in the development of ANN and MLR models. Based on the correlation and PCA results, two sets of influencing factors were employed to develop predictive models. Two MLR (MLR-1 and MLR-2) models and four neural networks (NN-1, NN-2, NN-3, and NN-4) optimized using Levenberg-Marquardt (LM) and scaled conjugate gradient (SCG) were developed and evaluated. The model performance validation was conducted using the coefficient of determination (R2), mean squared error (MSE), root mean squared error (RMSE), and Nash-Sutcliffe efficiency coefficient (NSE). The analysis showed that ANN models outperformed MLR models. The R2 values of 0.446 (MLR-1), 0.430 (MLR-2), 0.894 (NN-1), 0.855 (NN-2), 0.940 (NN-3), and 0.826 (NN-4); MSE values of 0.0000306 (MLR-1), 0.0000315 (MLR-2), 0.0000158 (NN-1), 0.0000261 (NN-2), 0.0000318 (NN-3), and 0.0000216 (NN-4) suggested the higher accuracy and lower modelling error of ANN models as compared with MLR. This study could provide an empirical basis and methodological support for K factor estimation in the region.
Fulltext Dental anomalies and facial profile abnormality of the non-syndromic cleft lip and palate children in Kelantan

Abd Rahman N, Abdullah N, Samsudin AR, Naing Mohd Ayub Sadiq L

Malays J Med Sci, 2004 Jul;11(2):41-51.
PMID: 22973126

This study was done to determine the prevalence of dental anomalies and facial profile abnormality and its association with the non-syndromic cleft lip and palate (CLP) as compared to the non-cleft children. A comparative cross sectional study was conducted where the case group consist of 98 non-syndromic CLP children-unilateral (UCLP) and bilateral (BCLP) who attended the Combined Clinic at Kota Bharu Dental Clinic (KBDC) while the comparison group comprised of 109 non-cleft children who attended the outpatient clinic at KBDC. Their ages were between 3 to 12 years old. Clinical oral and facial profile examinations were carried out to look for dental anomalies (morphology, number and alignment of teeth) and facial profile abnormality. The prevalence of anomalies in morphology of teeth in CLP (24.5%) and non-cleft (10.1%), number of teeth in CLP (44.9%) and non-cleft (7.3%), mal-alignment in CLP (79.6%) and non-cleft (27.5%) and facial profile abnormality in CLP (26.5%) and non-cleft (9.1 %). There was a significant association between CLP and anomalies in morphology, number, mal-alignment and abnormality in facial profile; (p < 0.05). Therefore, there was a high prevalence and risk of dental anomalies and facial profile abnormality in the CLP children compared to the non-cleft children.
The anomalous origin and branches of the obturator artery with its clinical implications

Jusoh AR, Abd Rahman N, Abd Latiff A, Othman F, Das S, Abd Ghafar N, et al.

Rom J Morphol Embryol, 2010;51(1):163-6.
PMID: 20191138

The obturator artery (OA) originates from the internal iliac artery. Variation in the origin of the OA may be asymptomatic in individuals and occasionally be detected during routine cadaveric dissections or autopsies. In the present study, we observed the origin and the branching pattern of the OA on 34 lower limbs (17 right sides and 17 left sides) irrespective of sex. The bifurcation of the common iliac artery into internal and external iliac from the sacral ala varied between 4.3-5.3 cm. The distance of the origin of the anterior division of internal iliac artery from the bifurcation of common iliac artery varied between 1-6 cm. The distance of the origin of the posterior division of the internal iliac artery from the point of bifurcation of the common iliac artery varied between 0-6 cm. Out of 34 lower limbs studied, two specimens (5.8%) showed anomalous origin of the OA originating from the posterior division of the internal iliac artery. Of these two, one limb belonged to the right side while the other was from the left side. The anomalous OA gave off an inferior vesical branch to the prostate in both the specimens. No other associated anomalies regarding the origin or branching pattern of the OA were observed. Prior knowledge of the anatomical variations may be beneficial for vascular surgeons ligating the internal iliac artery or its branches and the radiologists interpreting angiograms of the pelvic region.
Fulltext Halocarbon emissions by selected tropical seaweeds: species-specific and compound-specific responses under changing pH

Mithoo-Singh PK, Keng FS, Phang SM, Leedham Elvidge EC, Sturges WT, Malin G, et al.

PeerJ, 2017;5:e2918.
PMID: 28149690 DOI: 10.7717/peerj.2918

Five tropical seaweeds, Kappaphycus alvarezii (Doty) Doty ex P.C. Silva, Padina australis Hauck, Sargassum binderi Sonder ex J. Agardh (syn. S. aquifolium (Turner) C. Agardh), Sargassum siliquosum J. Agardh and Turbinaria conoides (J. Agardh) Kützing, were incubated in seawater of pH 8.0, 7.8 (ambient), 7.6, 7.4 and 7.2, to study the effects of changing seawater pH on halocarbon emissions. Eight halocarbon species known to be emitted by seaweeds were investigated: bromoform (CHBr3), dibro-momethane (CH2Br2), iodomethane (CH3I), diiodomethane (CH2I2), bromoiodomethane (CH2BrI), bromochlorometh-ane (CH2BrCl), bromodichloromethane (CHBrCl2), and dibro-mochloromethane (CHBr2Cl). These very short-lived halocarbon gases are believed to contribute to stratospheric halogen concentrations if released in the tropics. It was observed that the seaweeds emit all eight halocarbons assayed, with the exception of K. alvarezii and S. binderi for CH2I2 and CH3I respectively, which were not measurable at the achievable limit of detection. The effect of pH on halocarbon emission by the seaweeds was shown to be species-specific and compound specific. The highest percentage changes in emissions for the halocarbons of interest were observed at the lower pH levels of 7.2 and 7.4 especially in Padina australis and Sargassum spp., showing that lower seawater pH causes elevated emissions of some halocarbon compounds. In general the seaweed least affected by pH change in terms of types of halocarbon emission, was P. australis. The commercially farmed seaweed K. alvarezii was very sensitive to pH change as shown by the high increases in most of the compounds in all pH levels relative to ambient. In terms of percentage decrease in maximum quantum yield of photosynthesis (Fv∕Fm) prior to and after incubation, there were no significant correlations with the various pH levels tested for all seaweeds. The correlation between percentage decrease in the maximum quantum yield of photosynthesis (Fv∕Fm) and halocarbon emission rates, was significant only for CH2BrCl emission by P. australis (r = 0.47; p ≤ 0.04), implying that photosynthesis may not be closely linked to halocarbon emissions by the seaweeds studied. Bromine was the largest contributor to the total mass of halogen emitted for all the seaweeds at all pH. The highest total amount of bromine emitted by K. alvarezii (an average of 98% of total mass of halogens) and the increase in the total amount of chlorine with decreasing seawater pH fuels concern for the expanding seaweed farming activities in the ASEAN region.
Fulltext Cell-based influenza vaccine: current production, halal status assessment, and recommendations towards Islamic-compliant manufacturing

Zulkarnain NN, Anuar N, Abd Rahman N, Sheikh Abdullah SR, Alias MN, Yaacob M, et al.

Hum Vaccin Immunother, 2021 07 03;17(7):2158-2168.
PMID: 33539195 DOI: 10.1080/21645515.2020.1865044

Influenza virus is a life-threatening pathogen that infects millions of people every year, with annual mortality in the hundreds of thousands. The scenario for controlling infection has worsened with increasing numbers of vaccine hesitancy cases reported worldwide due to objections on safety, religious and other grounds. Uses of haram (impermissible) and mashbooh (doubtful) ingredients in vaccine production has raised doubts among Muslim consumers and consequently stimulated serious vaccine hesitancy. To address this major problem, we have reviewed and recommended some alternatives appropriate for manufacturing cell-based influenza vaccine which comply with Islamic laws and consumers' needs. Intensive assessments of current influenza vaccine production in both scientific and Islamic views have led to the identification of four main ingredients deemed impermissible in novel sharia-compliant (approved by Islamic laws) vaccine manufacturing. Only some of these impermissible components could be replaced with halal (permissible) alternatives, while others remain impermissible due to unavailability and unsuitability.
Fulltext Thioguanine-based DENV-2 NS2B/NS3 protease inhibitors: Virtual screening, synthesis, biological evaluation and molecular modelling

Hariono M, Choi SB, Roslim RF, Nawi MS, Tan ML, Kamarulzaman EE, et al.

PLoS One, 2019;14(1):e0210869.
PMID: 30677071 DOI: 10.1371/journal.pone.0210869

Dengue virus Type 2 (DENV-2) is predominant serotype causing major dengue epidemics. There are a number of studies carried out to find its effective antiviral, however to date, there is still no molecule either from peptide or small molecules released as a drug. The present study aims to identify small molecules inhibitor from National Cancer Institute database through virtual screening. One of the hits, D0713 (IC50 = 62 μM) bearing thioguanine scaffold was derivatised into 21 compounds and evaluated for DENV-2 NS2B/NS3 protease inhibitory activity. Compounds 18 and 21 demonstrated the most potent activity with IC50 of 0.38 μM and 16 μM, respectively. Molecular dynamics and MM/PBSA free energy of binding calculation were conducted to study the interaction mechanism of these compounds with the protease. The free energy of binding of 18 calculated by MM/PBSA is -16.10 kcal/mol compared to the known inhibitor, panduratin A (-11.27 kcal/mol), which corroborates well with the experimental observation. Results from molecular dynamics simulations also showed that both 18 and 21 bind in the active site and stabilised by the formation of hydrogen bonds with Asn174.
Fulltext Thymoquinone loaded in nanostructured lipid carrier showed enhanced anticancer activity in 4T1 tumor-bearing mice

Ong YS, Saiful Yazan L, Ng WK, Abdullah R, Mustapha NM, Sapuan S, et al.

Nanomedicine (Lond), 2018 07;13(13):1567-1582.
PMID: 30028248 DOI: 10.2217/nnm-2017-0322

AIM: To investigate the enhancement of anticancer activity of thymoquinone (TQ) by the use of nanostructured lipid carrier (NLC) in 4T1 tumor-bearing female BALB/c mice.
MATERIAL & METHODS: TQ was incorporated into NLC (TQNLC) by using high pressure homogenization. TQNLC and TQ were orally administered to the mice.
RESULTS & CONCLUSION: TQNLC and TQ are potential chemotherapeutic drugs as they exhibited anticancer activity. The use of NLC as a carrier has enhanced the therapeutic property of TQ by increasing the survival rate of mice. The antimetastasis effect of TQNLC and TQ to the lungs was evidence by downregulation of MMP-2. TQNLC and TQ induced apoptosis via modulation of Bcl-2 and caspase-8 in the intrinsic apoptotic pathway.
In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5-HT2 and α1 receptors

Heng HL, Chee CF, Thy CK, Tee JT, Chin SP, Herr DR, et al.

Chem Biol Drug Des, 2019 02;93(2):132-138.
PMID: 30216681 DOI: 10.1111/cbdd.13390

Compounds with activity at serotonin (5-hydroxytryptamine) 5-HT2 and α1 adrenergic receptors have potential for the treatment of central nervous system disorders, drug addiction or overdose. Isolaureline, dicentrine and glaucine enantiomers were synthesized, and their in vitro functional activities at human 5-HT2 and adrenergic α1 receptor subtypes were evaluated. The enantiomers of isolaureline and dicentrine acted as antagonists at 5-HT2 and α1 receptors with (R)-isolaureline showing the greatest potency (pKb = 8.14 at the 5-HT2C receptor). Both (R)- and (S)-glaucine also antagonized α1 receptors, but they behaved very differently to the other compounds at 5-HT2 receptors: (S)-glaucine acted as a partial agonist at all three 5-HT2 receptor subtypes, whereas (R)-glaucine appeared to act as a positive allosteric modulator at the 5-HT2A receptor.
Fulltext Correction: Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists

Heng HL, Chee CF, Chin SP, Ouyang Y, Wang H, Buckle MJC, et al.

Medchemcomm, 2018 03 01;9(3):593-594.
PMID: 30288212 DOI: 10.1039/c8md90012d

[This corrects the article DOI: 10.1039/C7MD00629B.].

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