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Fulltext The Kuwait National Primary Immunodeficiency Registry 2004-2018

Al-Herz W, Al-Ahmad M, Al-Khabaz A, Husain A, Sadek A, Othman Y

Front Immunol, 2019;10:1754.
PMID: 31396239 DOI: 10.3389/fimmu.2019.01754

Objective: To present the report from the Kuwait National Primary Immunodeficiency Registry between 2004 and 2018. Methods: The patients were followed prospectively between January 2004 and December 2018 and their collected data included sociodemographic, diagnosis, clinical presentation, laboratory tests, and treatment. Results: A total of 314 PID patients (165 males and 149 females) were registered during the study period. Most of the patients (n = 287, 91.4%) were Kuwaiti nationals and the prevalence among Kuwaitis was 20.27/100,000 with a cumulative incidence of 24.96/100,000 Kuwaitis. The distribution of the patients according to PID categories was as follow: immunodeficiencies affecting cellular and humoral immunity, 100 patients (31.8%); combined immunodeficiencies with associated syndromic features, 68 patients (21.7%); predominantly antibody deficiencies, 56 patients (17.8%); diseases of immune dysregulation, 47 patients (15%); congenital defects of phagocyte number or function, 20 patients (6.4%); autoinflammatory disorders, 1 patient (0.3%); and complement deficiencies, 22 patients (7%). The mean age of the patients at onset of symptoms was 26 months while the mean age at diagnosis was 53 months and the mean delay in diagnosis was 27 months. Most of the patients (n = 272, 86%) had onset of symptoms before the age of 5 years. Parental consanguinity rate within the registered patients was 78% and a positive family history of PID was noticed in 50% of the patients. Genetic testing was performed in 69% of the patients with an overall diagnostic yield of 90%. Mutations were identified in 46 different genes and more than 90% of the reported genetic defects were transmitted by an autosomal recessive pattern. Intravenous immunoglobulins and stem cell transplantation were used in 58% and 25% of the patients, respectively. There were 81 deaths (26%) among the registered patients with a mean age of death of 25 months. Conclusions: PID is not infrequent in Kuwait and the reported prevalence is the highest in the literature with increased proportion of more severe forms. Collaborative efforts including introduction of newborn screening should be implemented to diagnose such cases earlier and improve the quality of life and prevent premature deaths.
Investigations into the therapeutic effects of aerial and stem parts of Buxus papillosa C.K. Schneid.: In vitro chemical, biological and toxicological perspectives

Saleem H, Htar TT, Naidu R, Ahmad I, Zengin G, Ahmad M, et al.

J Pharm Biomed Anal, 2019 Mar 20;166:128-138.
PMID: 30640043 DOI: 10.1016/j.jpba.2019.01.007

In this study, different solvent extracts (methanol, dichloromethane and n-hexane) from aerial and stem parts of Buxus papillosa C.K. Schneid (Buxaceae) were investigated for a panoply of bioassays. Biological profiles were established by determining antioxidant and enzyme inhibition profiles. Toxicity was tested using MTT cell viability assay on five different human cancer cell lines i.e, MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480. For chemical fingerprinting, total bioactive contents and UHPLC-MS secondary metabolites profile were determined. Generally, both aerial and stem methanol extracts had highest total bioactive contents, radical scavenging and reducing power potential. DCM and n-hexane extracts were found to be most active for total antioxidant and metal chelating activity. The UHPLC-MS analysis of methanol extracts revealed the presence of several phenolic, flavonoid, alkaloid, saponin and depsipeptide derivatives. All the extracts were significantly active against butyrylcholinesterase, whereas moderate inhibition was observed for acetylcholinesterase, α-glucosidase and urease. Similarly, a considerable level of cytotoxicity was observed against all the tested cell lines with IC50 values ranging from 26 to 225.9 μg/mL. Aerial methanol and stem n-hexane extracts were found to be most cytotoxic. Principal component analysis was also performed to find any possible correlation between biological activities and total bioactive contents. On the basis of our findings, B. papillosa may be considered as promising source of bioactive molecules.
Production of high quality biodiesel from novel non-edible Raphnus raphanistrum L. seed oil using copper modified montmorillonite clay catalyst

Munir M, Ahmad M, Rehan M, Saeed M, Lam SS, Nizami AS, et al.

Environ Res, 2021 02;193:110398.
PMID: 33127396 DOI: 10.1016/j.envres.2020.110398

This study focused on producing high quality and yield of biodiesel from novel non-edible seed oil of abundantly available wild Raphnus raphanistrum L. using an efficient, recyclable and eco-friendly copper modified montmorillonite (MMT) clay catalyst. The maximum biodiesel yield of 83% was obtained by base catalyzed transesterification process under optimum operating conditions of methanol to oil ratio of 15:1, reaction temperature of 150 °C, reaction time of 5 h and catalyst loading of 3.5%. The synthesized catalyst and biodiesel were characterized for their structural features and chemical compositions using various state-of-the-art techniques, including x-ray diffraction, scanning electron microscopy, energy dispersive x-ray spectroscopy, Fourier transform infrared spectroscopy, nuclear magnetic resonance (1H, 13C) and gas chromatography-mass spectroscopy. The fuel properties of the biodiesel were estimated including kinematic viscosity (4.36 cSt), density (0.8312 kg/L), flash point (72 °C), acid value (0.172 mgKOH/g) and sulphur content (0.0002 wt.%). These properties were compared and found in good agreement with the International Biodiesel Standards of American (ASTM-951, 6751), European Committee (EN-14214) and China GB/T 20828 (2007). The catalyst was re-used in five consecutive transesterification reactions without losing much catalytic efficiency. Overall, non-edible Raphnus raphanistrum L.. seed oil and Cu doped MMT clay catalyst appeared to be highly active, stable, and cheap contenders for future biofuel industry. However, detailed life cycle assessment (LCA) studies of Raphnus raphanistrum L. seed oil biodiesel are highly recommended to assess the technical, ecological, social and economic challenges.
Fulltext Comparison of doxorubicin anticancer drug loading on different metal oxide nanoparticles

Javed KR, Ahmad M, Ali S, Butt MZ, Nafees M, Butt AR, et al.

Medicine (Baltimore), 2015 Mar;94(11):e617.
PMID: 25789952 DOI: 10.1097/MD.0000000000000617

Nanomaterials are being vigorously investigated for their use in anticancer drug delivery regimes or as biomarkers agents and are considered to be a candidate to provide a way to combat severe weaknesses of anticancer drug pharmacokinetics, such as their nonspecificity. Because of this weakness, a bigger proportion of the drug-loaded nanomaterials flow toward healthy tissues and result in undesirable side effects. It is very important to evaluate drug loading and release efficiency of various nanomaterials to find out true pharmacokinetics of these drugs.This observational study aims to evaluate various surface functionalized and naked nanomaterials for their drug loading capability and consequently strengthens the Reporting of Observational Studies in Epidemiology (STROBE). We analyzed naked and coated nanoparticles of transition metal oxides for their further loading with doxorubicin, a representative water-soluble anticancer drug.Various uncoated and polyethylene glycol-coated metal oxide nanoparticles were synthesized and loaded with anticancer drug using simple stirring of the nanoparticles in a saturated aqueous solution of the drug. Results showed that surface-coated nanoparticles have higher drug-loading capabilities; however, certain naked metal oxide nanoparticles, such as cobalt oxide nanoparticles, can load a sufficient amount of drug.
On the indirect environmental outcomes of COVID-19: short-term revival with futuristic long-term implications

Irfan M, Ahmad M, Fareed Z, Iqbal N, Sharif A, Wu H

Int J Environ Health Res, 2021 Jan 15.
PMID: 33448868 DOI: 10.1080/09603123.2021.1874888

The aim of this study is to identify and highlight the positive and negative indirect environmental impacts of COVID-19, with a particular focus on the most affected economies (USA, China, Spain, and Italy). In this respect, the empirical and theoretical dimensions of the contents of those impacts are analyzed. Research findings reveal a significant relationship between contingency actions and positive indirect impacts such as air quality improvements, clean beaches, and the decline in environmental noise. Besides, negative indirect impacts also exist, such as the rise in waste level and curtailment in recycling, further threatening the physical spaces (land and water), besides air. It is expected that global businesses will revive in the near future (though slowly), but the reduction in greenhouse gas emissions during this short time span is not a sustainable way of environmental mitigation. Thus, long-term mitigation policies should be strengthened to cope with the undesirable deterioration of the environment. Research findings provide an up-to-date glimpse of the pandemic from the perspectives of current and future indirect environmental impacts and the post-pandemic situation. Finally, it is suggested to invent and prepare action plans to induce a sustainable economic and environmental future in the post-pandemic world scenario.
Fulltext Crystal structure of 4-meth-oxy-N-[(pyrrolidin-1-yl)carbo-thio-yl]benzamide

Suhud K, Heng LY, Hasbullah SA, Ahmad M, Kassim MB

Acta Crystallogr E Crystallogr Commun, 2015 Apr 1;71(Pt 4):o225-6.
PMID: 26029426 DOI: 10.1107/S2056989015003813

In the title compound, C13H16N2O2S, the pyrrolidine ring has a twisted conformation on the central -CH2-CH2- bond. Its mean plane is inclined to the 4-meth-oxy-benzoyl ring by 72.79 (15)°. In the crystal, mol-ecules are linked by N-H⋯O and C-H⋯O hydrogen bonds to the same O-atom acceptor, forming chains along [001]. The chains are linked via slipped parallel π-π inter-actions [inter-centroid distance = 3.7578 (13) Å], forming undulating slabs parallel to (100).
Vision impairment and cognitive function among urban-dwelling malaysians aged 55 years and over from the Malaysian Elders Longitudinal Research (MELoR) study

Effendi-Tenang I, Tan MP, Khaliddin N, Jamaluddin Ahmad M, Amir NN, Kamaruzzaman SB, et al.

Arch Gerontol Geriatr, 2020 06 26;90:104165.
PMID: 32650156 DOI: 10.1016/j.archger.2020.104165

INTRODUCTION: Published literature on vision impairment and cognitive function amongst older Malaysians remains scarce. This study investigates the association between vision impairment and cognitive function in an older Malaysian population.
METHODS: Subjects aged 55 years and above from the Malaysian Elders Longitudinal Research (MELoR) study with available information on vision and Montreal Cognitive Assessment (MoCA) scores were included. Data were obtained through a home-based interview and hospital-based health check by trained researchers. Visual acuity (VA) was assessed with logMAR score with vision impairment defined as VA 6/18 or worse in the better-seeing eye. Cognition was evaluated using the MoCA-Blind scoring procedure. Those with a MoCA-Blind score of <19/22 were considered to have cognitive impairment.
RESULTS: Data was available for 1144 participants, mean (SD) age = 68.57 (±7.23) years. Vision impairment was present in 143 (12.5 %) and 758 (66.3 %) had MoCA-Blind score of <19. Subjects with vision impairment were less likely to have a MoCA-Blind score of ≥19 (16.8 % vs 36.2 %, p < 0.001). Vision impairment was associated with poorer MoCA-Blind scores after adjustments for age, gender, and ethnicity (β = 2.064; 95 % CI, -1.282 to 3.320; P = 0.003). In those who had > 6 years of education attainment, vision impairment was associated with a significant reduction of cognitive function and remained so after adjustment for age and gender (β = 1.863; 95 % CI, 1.081-3.209; P = 0.025).
CONCLUSION: Our results suggest that vision impairment correlates with cognitive decline. Therefore, maintaining good vision is an important interventional strategy for preventing cognitive decline in older adults.
Enhanced halophilic lipase secretion by Marinobacter litoralis SW-45 and its potential fatty acid esters release

Musa H, Hafiz Kasim F, Nagoor Gunny AA, Gopinath SCB, Azmier Ahmad M

J Basic Microbiol, 2019 Jan;59(1):87-100.
PMID: 30270443 DOI: 10.1002/jobm.201800382

An approach was made to enhance the halophilic lipase secretion by a newly isolated moderate halophilic Marinobacter litoralis SW-45, through the statistical optimization of Plackett-Burman (PB) experimental design and the Face Centered Central Composite Design (FCCCD). Initially, PB statistical design was used to screen the medium components and process parameters, while the One-factor-at-a-time technique was availed to find the optimum level of significant parameters. It was found that MgSO4 · 7H2 O, NaCl, agitation speed, FeSO4 · 7H2 O, yeast extract and KCl positively influence the halophilic lipase production, whereas temperature, carbon source (maltose), inducer (olive oil), inoculum size, and casein-peptone had a negative effect on enzyme production. The optimum level of halophilic lipase production was obtained at 3.0 g L-1 maltose, 1% (v/v) olive oil, 30 °C growth temperature and 4% inoculum volume (v/v). Further optimization by FCCCD was revealed 1.7 folds improvement in the halophilic lipase production from 0.603 U ml-1 to 1.0307 U ml-1 . Functional and biochemical characterizations displayed that the lipase was significantly active and stable in the pH ranges of 7.0-9.5, temperature (30-50 °C), and NaCl concentration (0-21%). The lipase was maximally active at pH 8.0, 12% (w/v) NaCl, and 50 °C temperature. Besides, M. litoralis SW-45 lipase was found to possess the promising industrial potential to be utilized as a biocatalyst for the esterification.
Fulltext Association between reduced visual-motor integration performance and socioeconomic factors among preschool children in Malaysia: A cross-sectional study

Hairol MI, Nordin N, P'ng J, Sharanjeet-Kaur S, Narayanasamy S, Mohd-Ali M, et al.

PLoS One, 2021;16(3):e0246846.
PMID: 33657109 DOI: 10.1371/journal.pone.0246846

Visual-motor integration (VMI) is related to children's academic performance and school readiness. VMI scores measured using the Beery-Bucktenicka Developmental Test of Visual-Motor Integration (Beery-VMI) can differ due to differences in cultural and socioeconomic backgrounds. This study compared the VMI scores of Malaysian preschoolers with the corresponding US norms and determined the association between their VMI scores and socioeconomic factors. A cross-sectional study was conducted among 435 preschoolers (mean age: 5.95±0.47 years; age range: 5.08-6.83 years) from randomly selected public and private preschools. VMI scores were measured using Beery-VMI in the preschools' classrooms. Information on the socioeconomic characteristics of the preschoolers was obtained using a parent-report questionnaire. One sample t-test was used to compare their VMI scores with the corresponding US norms. Multivariate logistic regression models were used to explore the influence of socioeconomic factors on the preschoolers' VMI scores. Overall, Malaysian preschoolers' VMI performance was similar to the US standardized norms (p>0.05). Children from low-income families were twice likely to obtain lower than average VMI scores than those from higher-income families (OR = 2.47, 95%CI 1.05, 5.86). Children enrolled at public preschools were more likely to obtain a lower than average VMI score than those who enrolled at private preschools (OR = 2.60, 95%CI 1.12, 6.06). Children who started preschool at the age of six were more likely to obtain lower than average VMI scores than those who started at an earlier age (OR = 4.66, 95%CI 1.97, 11.04). Low maternal education level was also associated with lower than average VMI score (OR = 2.60, 95%CI 1.12, 6.06). Malaysian preschoolers' Beery-VMI performance compared well to their US counterparts. Some socioeconomic factors were associated with reduced VMI scores. Those from disadvantaged socioeconomic backgrounds are more likely to have reduced VMI performance, potentially adversely affecting their school readiness, cognitive performance, and future academic achievements.
Synthesis, characterization and antimicrobial activity of norfloxacin based acetohydrazides

Walayat K, Ahmad M, Rasul A, Aslam S, Anjum MN, Sultan S, et al.

Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):855-860.
PMID: 32863262

The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon. Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work, norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the treatment with hydrazine hydrate to result in corresponding acetohydrazide 3. A range of substituted benzaldehydes were reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.
Synthesis, molecular docking and anti-diabetic studies of novel benzimidazole-pyrazoline hybrid molecules

Ibraheem F, Ahmad M, Ashfaq UA, Aslam S, Khan ZA, Sultan S

Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):847-854.
PMID: 32863261

Pyrazoline and benzimidazoles derivatives have been widely studied due to their potential applications in the medicinal field. In this research project, we have hybridized these two heterocyclic systems in the same molecule. A new series of compounds, 2-((3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)methyl)-1H-benzo[d]imidazole (5a-i) were synthesized through a multistep reaction. In the first step, chalcones 3a-i were prepared by coupling of various acetophenones and benzaldehydes under alkaline conditions. These chalcones were cyclized with hydrazine hydrate to form a series of pyrazolines which were finally coupled with 2-chloromethyl-1H-benzimidazole to get a new series of titled hybrid molecules. The structures of these compounds were elucidated by spectral (1H NMR and 13C NMR) analysis. The anti-diabetic potential of these compounds was studied by screening them for their α-glucosidase inhibition activity. The SAR was established through molecular docking analysis. Compound 5d appeared as effective inhibitor with IC50 = 50.06μM as compared to reference drug (acarbose) having IC50 = 58.8μM.
Fulltext Perceptions and Acceptability of a Smartphone App Intervention (ChildSafe) in Malaysia: Qualitative Exploratory Study

Yong TSM, Perialathan K, Ahmad M, Juatan N, Abdul Majid L, Johari MZ

JMIR Pediatr Parent, 2021 Jun 01;4(2):e24156.
PMID: 34061039 DOI: 10.2196/24156

BACKGROUND: Home is a vulnerable place for accidental child injuries. Unintentional injuries are a leading cause of death, hospitalization, and disabilities. These injuries are considered preventable and if not tackled, they will continue to be a persisting problem. Smartphones have become increasingly important in our everyday life and is an important tool not only for communication but also for other purposes-they have apps that can be used for various purposes. Therefore, an app-based intervention (ChildSafe) was developed to assess and reduce child injury at home.
OBJECTIVE: This study aimed to evaluate the acceptance of the ChildSafe smartphone app intervention by parents/guardians.
METHODS: This study was conducted using a qualitative exploratory approach on selected participants of the ChildSafe intervention app study. A total of 27 semistructured in-depth interviews were carried out among parents or guardians who have at least one child between the age of 0 and 59 months in the area of Sungai Buloh, Selangor, between November 2017 and March 2018. Interview questions were developed from the consolidated framework for implementation research (CFIR). Interviews were recorded, transcribed verbatim, and data were thematically analyzed guided by CFIR.
RESULTS: The study revealed users' perception on usability, feasibility, and acceptability toward the ChildSafe app. Three CFIR domains were identified: intervention characteristics, inner setting, and characteristics of individuals. A total of 5 constructs were revealed under intervention characteristics: evidence strength and quality, relative advantage, adaptability, trialability, and design quality and packaging; 2 under inner setting: implementation climate and readiness for implementation; and 4 under characteristics of individuals: knowledge and beliefs about the intervention, self-efficacy, individual stage of change, and other personal attributes. In general, participants felt the app is extremely useful and effective, easy to use, and purposeful in achieving home safety assessment via reminders. The app replaces the need for participants to search for information on home safety and dangers, as the app itself was designed as a tool to assess for this specific purpose. Even at the nascent stage and despite its limitations, the app has prompted users to consider and make changes around their own home. However, future versions of the app should be expanded to make it more attractive to users as it lacks interactive feedback and additional features.
CONCLUSIONS: Parents/guardians are accepting the use of the ChildSafe app to prevent child injury at home. However, further expansion and improvements are needed to increase the acceptability of this app by parents/guardians.
Fulltext A new record of Fannia pusio (Wiedemann) (Diptera:Fanniidae) from Malaysia

Omar B, Kurahashi H, Jeffery J, Yasohdha N, Lau SY, John MC, et al.

Trop Biomed, 2007 Dec;24(2):99-100.
PMID: 18209716

Fannia pusio (Wiedemann) (Diptera: Fanniidae) is newly recorded from Malaysia. This record is based on 1male symbol 1female symbol from Sarawak, east Malaysia and 1male symbol 2female symbol from Selangor, peninsular Malaysia. It is included in the pusio group of Fannia wherein are included Fannia femoralis (Stein), Fannia howardi Malloch, Fannia trimaculata (Stein), Fannia leucosticta (Meigen) and Fannia punctiventris Malloch. The male of Fannia pusio is differentiated from other members of the group by the following features: hind femur with a swelling bearing a number of setae that are usually curled at tip; squamae creamy; tergite 1+2 broadly grey dusted at sides.
Fulltext How deep is deep enough? Analysis of sea turtle eggs nest relocation procedure at Chagar Hutang Turtle Sanctuary

Najwa-Sawawi S, Azman NM, Rusli MU, Ahmad A, Fahmi-Ahmad M, Fadzly N

Saudi J Biol Sci, 2021 Sep;28(9):5053-5060.
PMID: 34466082 DOI: 10.1016/j.sjbs.2021.05.021

Sea turtle eggs incubation involves natural and artificial incubation of eggs, and indeed the depth will be varied and presumably affect the development of hatchlings. For nest relocation, the researcher needs to decide on the depth to incubate the eggs. Sea turtle eggs clutches may vary between 40 and 120 eggs for the green turtle, thus using a single value as the standard procedure might affect the quality of hatchlings. Here we quantify the dimension of the natural (in-situ) nest constructed by the nester and the artificial (ex-situ) built by our ranger during nest relocation. We suggest a linear regression calculation of Y = 0.2366X + 59.3267, better predict a more accurate nest depth based on the number of eggs to imitate the natural nest.
Fulltext Synergetic Effects of Graphene Nanoplatelets/Tapioca Starch on Water-Based Drilling Muds: Enhancements in Rheological and Filtration Characteristics

Ahmad M, Ali I, Bins Safri MS, Bin Mohammad Faiz MAI, Zamir A

Polymers (Basel), 2021 Aug 10;13(16).
PMID: 34451195 DOI: 10.3390/polym13162655

Several borehole problems are encountered during drilling a well due to improper mud design. These problems are directly associated with the rheological and filtration properties of the fluid used during drilling. Thus, it is important to investigate the mud rheological and filtration characteristics of water-based drilling muds (WBMs). Several materials have been examined but due to the higher temperature conditions of wells, such materials have degraded and lost their primary functions. In this research, an attempt was made to prepare a water-based mud by utilizing graphene nano platelets (GNP) in addition to the native tapioca starch at different ratios. The combined effect of starch and graphene nano platelets has been investigated in terms of mud's rheological and filtration parameters, including its plastic viscosity (PV), yield point (YP), fluid loss volume (FLV) and filtercake thickness (FCT). The morphological changes in the filtercake have also been observed using Field Emission Scanning Electron Microscope (FESEM) micrographs. Plastic viscosity was increased from 18-35 cP, 22-31 cP and 21-28 cP for 68 °F, 250 °F and 300 °F, respectively. The yield point was also enhanced from 22-37 lb/100ft2, 26-41 lb/100ft2 and 24-31 lb/100ft2 at the studied range. The fluid loss was dramatically reduced from 14.5-6.5 mL, 17.3-7.5 mL and 36-9.5 mL at 68 °F, 250 °F and 300 °F respectively. Similarly, filtercake thickness was also reduced which was further illustrated by filtercake morphology.
Fulltext Magnetic Properties of Polyvinyl Alcohol and Doxorubicine Loaded Iron Oxide Nanoparticles for Anticancer Drug Delivery Applications

Nadeem M, Ahmad M, Akhtar MS, Shaari A, Riaz S, Naseem S, et al.

PLoS One, 2016;11(6):e0158084.
PMID: 27348436 DOI: 10.1371/journal.pone.0158084

The current study emphasizes the synthesis of iron oxide nanoparticles (IONPs) and impact of hydrophilic polymer polyvinyl alcohol (PVA) coating concentration as well as anticancer drug doxorubicin (DOX) loading on saturation magnetization for target drug delivery applications. Iron oxide nanoparticles particles were synthesized by a reformed version of the co-precipitation method. The coating of polyvinyl alcohol along with doxorubicin loading was carried out by the physical immobilization method. X-ray diffraction confirmed the magnetite (Fe3O4) structure of particles that remained unchanged before and after polyvinyl alcohol coating and drug loading. Microstructure and morphological analysis was carried out by transmission electron microscopy revealing the formation of nanoparticles with an average size of 10 nm with slight variation after coating and drug loading. Transmission electron microscopy, energy dispersive, and Fourier transform infrared spectra further confirmed the conjugation of polymer and doxorubicin with iron oxide nanoparticles. The room temperature superparamagnetic behavior of polymer-coated and drug-loaded magnetite nanoparticles were studied by vibrating sample magnetometer. The variation in saturation magnetization after coating evaluated that a sufficient amount of polyvinyl alcohol would be 3 wt. % regarding the externally controlled movement of IONPs in blood under the influence of applied magnetic field for in-vivo target drug delivery.
Synthesis, characterization, monoamine oxidase inhibition, molecular docking and dynamic simulations of novel 2,1-benzothiazine-2,2-dioxide derivatives

Ahmad S, Zaib S, Jalil S, Shafiq M, Ahmad M, Sultan S, et al.

Bioorg Chem, 2018 10;80:498-510.
PMID: 29996111 DOI: 10.1016/j.bioorg.2018.04.012

In this research work, we report the synthesis and biological evaluation of two new series of 1-benzyl-4-(benzylidenehydrazono)-3,4-dihydro-1H-benzo[c] [1,2]thiazine 2,2-dioxides and 1-benzyl-4-((1-phenylethylidene)hydrazono)-3,4-dihydro-1H-benzo[c][1,2]thiazine 2,2-dioxides. The synthetic plan involves the mesylation of methyl anthranilate with subsequent N-benzylation of the product. The methyl 2-(N-benzylmethylsulfonamido)benzoate was subjected to cyclization reaction in the presence of sodium hydride to obtain 1-benzyl-1H-benzo[c][1,2]thiazin-4(3H)-one 2,2-dioxide which was treated with hydrazine hydrate to get corresponding hydrazone precursor. Finally, the titled compounds were obtained by reaction of hydrazone with various substituted aldehydes and ketones. The synthesized derivatives were subjected to carry out their inhibition activities against monoamine oxidases along with modelling investigations to evaluate their binding interactions and dynamic stability during the docking studies. The inhibition profile of potent compounds was found as competitive for both the isozymes. The compounds were more selective inhibitors of MAO-A as compared to MAO-B. Moreover, drug likeness profile of the derivatives was evaluated to have an additional insight into the physicochemical properties. The molecular dynamic simulations predicted the behaviour of amino acids with the active site residues.
Fulltext Vasorelaxation Study and Tri-Step Infrared Spectroscopy Analysis of Malaysian Local Herbs

Ch'ng YS, Tan CS, Loh YC, Ahmad M, Zaini Asmawi M, Yam MF

J Pharmacopuncture, 2016 Jun;19(2):145-54.
PMID: 27386148 DOI: 10.3831/KPI.2016.19.016

The aim of this paper is to investigate the activities of Malaysian local herbs (Clinacanthus nutans Lindau, Strobilanthes crispus, Murdannia bracteata, Elephantopus scaber Linn., Pereskia bleo, Pereskia grandifolia Haw., Vernonia amygdalina, and Swietenia macrophylla King) for anti-hypertensive and vasorelaxant activity. An infrared (IR) macro-fingerprinting technique consisting of conventional fourier transform IR (FTIR), second-derivative IR (SD-IR), and two-dimensional correlation IR (2D-correlation IR) analyses were used to determine the main constituents and the fingerprints of the Malaysian local herbs.
Vasorelaxation effect of Glycyrrhizae uralensis through the endothelium-dependent Pathway

Tan CS, Ch'ng YS, Loh YC, Zaini Asmawi M, Ahmad M, Yam MF

J Ethnopharmacol, 2017 Mar 06;199:149-160.
PMID: 28161542 DOI: 10.1016/j.jep.2017.02.001

ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrhiza uralensis (G. uralensis) is one of the herbs used in traditional Chinese medicine (TCM) and serves as an envoy medicinal. Since G. uralensis plays a major role in the anti-hypertensive TCM formulae, we believe that G. uralensis might possess vasorelaxation activity.
AIM OF THE STUDY: This study is designed to investigate the vasorelaxation effect of G. uralensis from various extracts and to study its pharmacology effect.
MATERIALS AND METHODS: The vasorelaxation effect of G. uralensis extracts were evaluated on thoracic aortic rings isolated from Sprague Dawley rats.
RESULTS: Among these three extracts of G. uralensis, 50% ethanolic extract (EFG) showed the strongest vasorelaxation activity. EFG caused the relaxation of the aortic rings pre-contracted with phenylephrine either in the presence or absence of endothelium and pre-contracted with potassium chloride in endothelium-intact aortic ring. Nω-nitro-L-arginine methyl ester, methylene blue, or 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one inhibit the vasorelaxation effect of EFG in the presence of endothelium. On the other hand, in the presence of the potassium channel blockers (tetraethylammonium and barium chloride), the vasorelaxation effect of EFG was not affected, but glibenclamide and 4-aminopyridine did inhibit the vasorelaxation effect of EFG. With indomethacin, atropine and propranolol, the vasorelaxation effect by EFG was significantly reduced. EFG was also found to be effective in reducing Ca(2+) release from sarcoplasmic reticulum and the blocking of calcium channels.
CONCLUSIONS: The results obtained suggest that EFG is involved in the NO/sGC/cGMP pathway.
Vasodilatory Effects of Combined Traditional Chinese Medicinal Herbs in Optimized Ratio

Loh YC, Tan CS, Ch'ng YS, Ahmad M, Asmawi MZ, Yam MF

J Med Food, 2017 Mar;20(3):265-278.
PMID: 28296594 DOI: 10.1089/jmf.2016.3836

Recently, a new syndromic disease combination theory of traditional Chinese medicine (TCM) for hypertensive treatment has been introduced. In the wake of this new concept, a new science-based TCM formula that counteracts various syndromes is needed. The objective of this study was to develop such a formula. Five of the most clinically prescribed TCM herbs that work on different syndromes, namely Gastrodia elata, Uncaria rhynchophylla, Pueraria thomsonii, Panax notoginseng, and Alisma orientale, were selected for this study. The fingerprints of these five herbs were analyzed by tri-step Fourier transform infrared spectroscopy. Three different solvents, 95% ethanol, 50% ethanol, and distilled water, were used for the maceration of the herbs and their vasodilatory effects were studied using in vitro precontracted aortic ring model. Among these, the 50% ethanolic extracts of G. elata (GE50) and A. orientale (AO50), and 95% ethanolic extracts of U. rhynchophylla (UR95), P. thomsonii (PT95), and P. notoginseng (PN95) were found to be the most effective for eliciting vasodilation. Thus, these five extracts were used for orthogonal stimulus-response compatibility group studies by using L25 (5(5)) formula. The best combination ratio for GE50, UR95, PT95, PN95, and AO50, which was assigned as Formula 1 (F1), was found at EC0, EC25, EC20, EC20, and EC10, respectively. The vasodilatory effect of the extracts prepared from different extraction methods using F1 ratio was also studied. From the results, the EC50 and Rmax of total 50% ethanolic extract of five herbs using F1 ratio (F1-2) were 0.028 ± 0.005 mg/mL and 101.71% ± 3.64%, with better values than F1 (0.104 ± 0.014 mg/mL and 97.80% ± 3.12%, respectively). In conclusion, the optimum ratio and appropriate extraction method (F1-2) for the new TCM formula were revealed.

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