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Fulltext Philanthotoxin-343 attenuates retinal and optic nerve injury, and protects visual function in rats with N-methyl-D-aspartate-induced excitotoxicity

Fazel MF, Abu IF, Mohamad MHN, Agarwal R, Iezhitsa I, Bakar NS, et al.

PLoS One, 2020;15(7):e0236450.
PMID: 32706792 DOI: 10.1371/journal.pone.0236450

Retinal ganglion cell (RGC) loss and optic neuropathy, both hallmarks of glaucoma, have been shown to involve N-methyl-D-aspartate receptor (NMDAR)-mediated excitotoxicity. This study investigated the neuroprotective effects of Philanthotoxin (PhTX)-343 in NMDA-induced retinal injury to alleviate ensuing visual impairments. Sprague-Dawley rats were divided into three; Group I was intravitreally injected with phosphate buffer saline as the control, Group II was injected with NMDA (160 nM) to induce retinal excitotoxic injury, while Group III was injected with PhTX-343 (160 nM) 24 h prior to excitotoxicity induction with NMDA. Rats were subjected to visual behaviour tests seven days post-treatment and subsequently euthanized. Rat retinas and optic nerves were subjected to H&E and toluidine blue staining, respectively. Histological assessments showed that NMDA exposure resulted in significant loss of retinal cell nuclei and thinning of ganglion cell layer (GCL). PhTX-343 pre-treatment prevented NMDA-induced changes where the RGC layer morphology is similar to the control. The numbers of nuclei in the NMDA group were markedly lower compared to the control (p<0.05). PhTX-343 group had significantly higher numbers of nuclei within 100 μm length and 100 μm2 area of GCL (2.9- and 1.7-fold, respectively) compared to NMDA group (p<0.05). PhTX-343 group also displayed lesser optic nerve fibres degeneration compared to NMDA group which showed vacuolation in all sections. In the visual behaviour test, the NMDA group recorded higher total distance travelled, and lower total immobile time and episodes compared to the control and PhTX-343 groups (p<0.05). Object recognition tests showed that the rats in PhTX-343 group could recognize objects better, whereas the same objects were identified as novel by NMDA rats despite multiple exposures (p<0.05). Visual performances in the PhTX-343 group were all comparable with the control (p>0.05). These findings suggested that PhTX-343 inhibit retinal cell loss, optic nerve damage, and visual impairments in NMDA-induced rats.
Fulltext Modeling of Cu(II) Adsorption from an Aqueous Solution Using an Artificial Neural Network (ANN)

Khan T, Binti Abd Manan TS, Isa MH, Ghanim AAJ, Beddu S, Jusoh H, et al.

Molecules, 2020 Jul 17;25(14).
PMID: 32708928 DOI: 10.3390/molecules25143263

This research optimized the adsorption performance of rice husk char (RHC4) for copper (Cu(II)) from an aqueous solution. Various physicochemical analyses such as Fourier transform infrared spectroscopy (FTIR), field-emission scanning electron microscopy (FESEM), carbon, hydrogen, nitrogen, and sulfur (CHNS) analysis, Brunauer-Emmett-Teller (BET) surface area analysis, bulk density (g/mL), ash content (%), pH, and pHZPC were performed to determine the characteristics of RHC4. The effects of operating variables such as the influences of aqueous pH, contact time, Cu(II) concentration, and doses of RHC4 on adsorption were studied. The maximum adsorption was achieved at 120 min of contact time, pH 6, and at 8 g/L of RHC4 dose. The prediction of percentage Cu(II) adsorption was investigated via an artificial neural network (ANN). The Fletcher-Reeves conjugate gradient backpropagation (BP) algorithm was the best fit among all of the tested algorithms (mean squared error (MSE) of 3.84 and R2 of 0.989). The pseudo-second-order kinetic model fitted well with the experimental data, thus indicating chemical adsorption. The intraparticle analysis showed that the adsorption process proceeded by boundary layer adsorption initially and by intraparticle diffusion at the later stage. The Langmuir and Freundlich isotherm models interpreted well the adsorption capacity and intensity. The thermodynamic parameters indicated that the adsorption of Cu(II) by RHC4 was spontaneous. The RHC4 adsorption capacity is comparable to other agricultural material-based adsorbents, making RHC4 competent for Cu(II) removal from wastewater.
Fulltext Factors Associated with the Perception of Risk and Knowledge of Contracting the SARS-Cov-2 among Adults in Bangladesh: Analysis of Online Surveys

Abir T, Kalimullah NA, Osuagwu UL, Yazdani DMN, Mamun AA, Husain T, et al.

Int J Environ Res Public Health, 2020 Jul 21;17(14).
PMID: 32708161 DOI: 10.3390/ijerph17145252

This study investigated the perception and awareness of risk among adult participants in Bangladesh about Coronavirus Disease 2019 (COVID-19). During the lockdown era in Bangladesh at two different time points, from 26-31 March 2020 (early lockdown) and 11-16 May 2020 (late lockdown), two self-administered online surveys were conducted on 1005 respondents (322 and 683 participants, respectively) via social media. To examine risk perception and knowledge-related factors towards COVID-19, univariate and multiple linear regression models were employed. Scores of mean knowledge (8.4 vs. 8.1, p = 0.022) and perception of risk (11.2 vs. 10.6, p < 0.001) differed significantly between early and late lockdown. There was a significant decrease in perceived risk scores for contracting SARS-Cov-2 [β = -0.85, 95%CI: -1.31, -0.39], while knowledge about SARS-Cov-2 decreased insignificantly [β = -0.22, 95%CI: -0.46, 0.03] in late lockdown compared with early lockdown period. Self-quarantine was a common factor linked to increased perceived risks and knowledge of SARS-Cov-2 during the lockdown period. Any effort to increase public awareness and comprehension of SARS-Cov-2 in Bangladesh will then offer preference to males, who did not practice self-quarantine and are less worried about the propagation of this kind of virus.
Fulltext Multiepitope-Based Subunit Vaccine Design and Evaluation against Respiratory Syncytial Virus Using Reverse Vaccinology Approach

Tahir Ul Qamar M, Shokat Z, Muneer I, Ashfaq UA, Javed H, Anwar F, et al.

Vaccines (Basel), 2020 Jun 08;8(2).
PMID: 32521680 DOI: 10.3390/vaccines8020288

Respiratory syncytial virus (RSV) is primarily associated with respiratory disorders globally. Despite the availability of information, there is still no competitive vaccine available for RSV. Therefore, the present study has been designed to develop a multiepitope-based subunit vaccine (MEV) using a reverse vaccinology approach to curb RSV infections. Briefly, two highly antigenic and conserved proteins of RSV (glycoprotein and fusion protein) were selected and potential epitopes of different categories (B-cell and T-cell) were identified from them. Eminently antigenic and overlapping epitopes, which demonstrated strong associations with their respective human leukocyte antigen (HLA) alleles and depicted collective ~70% coverage of the world's populace, were shortlisted. Finally, 282 amino acids long MEV construct was established by connecting 13 major histocompatibility complex (MHC) class-I with two MHC class-II epitopes with appropriate adjuvant and linkers. Adjuvant and linkers were added to increase the immunogenic stimulation of the MEV. Developed MEV was stable, soluble, non-allergenic, non-toxic, flexible and highly antigenic. Furthermore, molecular docking and molecular dynamics (MD) simulations analyses were carried out. Results have shown a firm and robust binding affinity of MEV with human pathogenic toll-like receptor three (TLR3). The computationally mediated immune response of MEV demonstrated increased interferon-γ production, a significant abundance of immunoglobulin and activation of macrophages which are essential for immune-response against RSV. Moreover, MEV codons were optimized and in silico cloning was performed, to ensure its increased expression. These outcomes proposed that the MEV developed in this study will be a significant candidate against RSV to control and prevent RSV-related disorders if further investigated experimentally.
Fulltext Metabolite Profiles of Red and Yellow Watermelon (Citrullus lanatus) Cultivars Using a 1H-NMR Metabolomics Approach

Sulaiman F, Ahmad Azam A, Ahamad Bustamam MS, Fakurazi S, Abas F, Lee YX, et al.

Molecules, 2020 Jul 15;25(14).
PMID: 32679913 DOI: 10.3390/molecules25143235

Watermelon, a widely commercialized fruit, is famous for its thirst-quenching property. The broad range of cultivars, which give rise to distinct color and taste, can be attributed to the differences in their chemical profile, especially that of the carotenoids and volatile compounds. In order to understand this distribution properly, water extracts of red and yellow watermelon pulps with predominantly polar metabolites were subjected to proton nuclear magnetic resonance (1H-NMR) analysis. Deuterium oxide (D2O) and deuterated chloroform (CDCl3) solvents were used to capture both polar and non-polar metabolites from the same sample. Thirty-six metabolites, of which six are carotenoids, were identified from the extracts. The clustering of the compounds was determined using unsupervised principal component analysis (PCA) and further grouping was achieved using supervised orthogonal partial least squares discriminant analysis (OPLS-DA). The presence of lycopene, β-carotene, lutein, and prolycopene in the red watermelon plays an important role in its differentiation from the yellow cultivar. A marked difference in metabolite distribution was observed between the NMR solvents used as evidenced from the PCA model. OPLS-DA and relative quantification of the metabolites, on the other hand, helped in uncovering the discriminating metabolites of the red and yellow watermelon cultivars from the same solvent system.
Association between cognitive reserve with cognitive impairment, social and occupational functioning, and quality of life in schizophrenia: A preliminary study in the Malaysian population

Sharip S, Zairani MI, Ing LP, Baharom NN, Asarapoo NS, Rahman NA, et al.

Asian J Psychiatr, 2020 Oct;53:102230.
PMID: 32585635 DOI: 10.1016/j.ajp.2020.102230
Effect of miscentering and low-dose protocols on contrast resolution in computed tomography head examination

Shaffiq Said Rahmat SM, Abdul Karim MK, Che Isa IN, Abd Rahman MA, Noor NM, Hoong NK

Comput Biol Med, 2020 08;123:103840.
PMID: 32658782 DOI: 10.1016/j.compbiomed.2020.103840

BACKGROUND: Unoptimized protocols, including a miscentered position, might affect the outcome of diagnostic in CT examinations. In this study, we investigate the effects of miscentering position during CT head examination on the signal-to-noise ratio (SNR) and contrast-to-noise ratio (CNR).
METHOD: We simulate the CT head examination using a water phantom with a standard protocol (120 kVp/180 mAs) and a low dose protocol (100 kVp/142 mAs). The table height was adjusted to simulate miscentering by 5 cm from the isocenter, where the height was miscentered superiorly (MCS) at 109, 114, 119, and 124 cm, and miscentered inferiorly (MCI) at 99, 94, 89, and 84 cm. Seven circular regions of interest were used, with one drawn at the center, four at the peripheral area of the phantom, and two at the background area of the image.
RESULTS: For the standard protocol, the mean CNR decreased uniformly as table height increased and significantly differed (p
Fulltext Pre-existing chronic medical illnesses and follow up status among active pulmonary tuberculosis cases in a district population

Thai LT, Li YL, Kig TY, Muhammad Afiq R, Shoen CC, Sing HC, et al.

Med J Malaysia, 2020 05;75(3):204-208.
PMID: 32467533

INTRODUCTION: The knowledge of pre-existing medical illnesses and their follow up status among active pulmonary tuberculosis (PTB) subjects can help in tuberculosis (TB) control programme. The aims of our study were to examine: the prevalence of pre-existing chronic medical illnesses, the follow up status of known pre-existing co-morbid and to distinguish between diagnosed and undiagnosed preexisting tuberculosis related chronic medical illnesses among our active PTB subjects.

METHODS: We conducted a retrospective review of demographic and clinical data of active PTB subjects that were diagnosed between January 2015 and June 2017 in the district of Manjung, Perak, Malaysia. Among the 302 TB clinical notes reviewed, 253 patients were included. Subjects below the age of 18 years and whose follow up centres for their medical illnesses that were located outside of Manjung were excluded. Demographic and clinical data were collected using pre-tested data collection form by trained investigators. The data was analysed using SPSS Version 20.0.

RESULTS: We identified diabetes mellitus as the most prevalent pre-existing co-morbid (77 cases) and almost 90% (68 cases) of these diabetic subjects were diagnosed prior to active PTB diagnosis. This was followed by Human Immunodeficiency Virus and Hepatitis C infection which accounted for 12.0% (30 cases) of the study populations. Among 132 subjects who had pre-existing chronic medical illnesses, only 74 subjects (29%) were under regular follow up at healthcare facilities in Manjung prior to PTB diagnosis.

CONCLUSION: Overall, our research provides evidence on the existence of wide variation of clinical background among active PTB subjects.
Fulltext Estimating Blood Pressure from the Photoplethysmogram Signal and Demographic Features Using Machine Learning Techniques

Chowdhury MH, Shuzan MNI, Chowdhury MEH, Mahbub ZB, Uddin MM, Khandakar A, et al.

Sensors (Basel), 2020 Jun 01;20(11).
PMID: 32492902 DOI: 10.3390/s20113127

Hypertension is a potentially unsafe health ailment, which can be indicated directly from the blood pressure (BP). Hypertension always leads to other health complications. Continuous monitoring of BP is very important; however, cuff-based BP measurements are discrete and uncomfortable to the user. To address this need, a cuff-less, continuous, and noninvasive BP measurement system is proposed using the photoplethysmograph (PPG) signal and demographic features using machine learning (ML) algorithms. PPG signals were acquired from 219 subjects, which undergo preprocessing and feature extraction steps. Time, frequency, and time-frequency domain features were extracted from the PPG and their derivative signals. Feature selection techniques were used to reduce the computational complexity and to decrease the chance of over-fitting the ML algorithms. The features were then used to train and evaluate ML algorithms. The best regression models were selected for systolic BP (SBP) and diastolic BP (DBP) estimation individually. Gaussian process regression (GPR) along with the ReliefF feature selection algorithm outperforms other algorithms in estimating SBP and DBP with a root mean square error (RMSE) of 6.74 and 3.59, respectively. This ML model can be implemented in hardware systems to continuously monitor BP and avoid any critical health conditions due to sudden changes.
Fulltext Boron-Doped Reduced Graphene Oxide with Tunable Bandgap and Enhanced Surface Plasmon Resonance

Junaid M, Khir MHM, Witjaksono G, Tansu N, Saheed MSM, Kumar P, et al.

Molecules, 2020 Aug 11;25(16).
PMID: 32796504 DOI: 10.3390/molecules25163646

Graphene and its hybrids are being employed as potential materials in light-sensing devices due to their high optical and electronic properties. However, the absence of a bandgap in graphene limits the realization of devices with high performance. In this work, a boron-doped reduced graphene oxide (B-rGO) is proposed to overcome the above problems. Boron doping enhances the conductivity of graphene oxide and creates several defect sites during the reduction process, which can play a vital role in achieving high-sensing performance of light-sensing devices. Initially, the B-rGO is synthesized using a modified microwave-assisted hydrothermal method and later analyzed using standard FESEM, FTIR, XPS, Raman, and XRD techniques. The content of boron in doped rGO was found to be 6.51 at.%. The B-rGO showed a tunable optical bandgap from 2.91 to 3.05 eV in the visible spectrum with an electrical conductivity of 0.816 S/cm. The optical constants obtained from UV-Vis absorption spectra suggested an enhanced surface plasmon resonance (SPR) response for B-rGO in the theoretical study, which was further verified by experimental investigations. The B-rGO with tunable bandgap and enhanced SPR could open up the solution for future high-performance optoelectronic and sensing applications.
Pleiotropic ameliorative effects of ellagitannin geraniin against metabolic syndrome induced by high-fat diet in rats

Cheng HS, Goh BH, Phang SCW, Amanullah MM, Ton SH, Palanisamy UD, et al.

Nutrition, 2020 08 12;79-80:110973.
PMID: 32916379 DOI: 10.1016/j.nut.2020.110973

OBJECTIVES: Metabolic syndrome (MetS), a multiplex risk factor for cardiovascular disease and type 2 diabetes, is increasingly prevalent worldwide. Ellagitannin geraniin, a polyphenol found in the rind of rambutan (Nephelium lappaceum), has demonstrated therapeutic effects against metabolism dysfunction. The aim of this study was to characterize the metabolic effects and possible mechanism of geraniin in rats with MetS induced by a high-fat diet (HFD).
METHODS: MetS was induced in Sprague Dawley rats on an HFD, followed by a daily oral gavage of geraniin (25 mg/kg) for 4 wk. The outcomes of geraniin-treated rats were compared with those of untreated rats on either a control diet or an HFD and with rats with MetS treated with metformin on a daily basis (200 mg/kg).
RESULTS: The supplementation of geraniin ameliorated multiple metabolic abnormalities caused by HFD, including hypertension, impaired glucose and lipid metabolism, ectopic fat deposition in the visceral fat and liver, and disturbed antioxidant mechanism and inflammatory response. The benefits conferred by geraniin were comparable to metformin. Transcriptomic analysis revealed a profound influence of geraniin on the hepatic expression profiles. The lipid and steroid metabolic processes that were aberrantly activated by HFD were suppressed by geraniin. Based on the differential transcriptomes, geraniin also exerted a significant modulatory effect on the expression of mitochondrial genes, potentially influencing the mitochondrial activity and leading to the observed beneficial effects.
CONCLUSION: Geraniin supplementation mitigated metabolic anomalies of MetS in rats, making it an attractive drug candidate for further investigation.
Fulltext Development of Polyvinylidene Fluoride Membrane by Incorporating Bio-Based Ginger Extract as Additive

Fahrina A, Arahman N, Mulyati S, Aprilia S, Mat Nawi NI, Aqsha A, et al.

Polymers (Basel), 2020 Sep 03;12(9).
PMID: 32899138 DOI: 10.3390/polym12092003

Biofouling on the membrane surface leads to performance deficiencies in membrane filtration. In this study, the application of ginger extract as a bio-based additive to enhance membrane antibiofouling properties was investigated. The extract was dispersed in a dimethyl acetamide (DMAc) solvent together with polyvinylidene fluoride (PVDF) to enhance biofouling resistance of the resulting membrane due to its antibiotic property. The concentrations of the ginger extract in the dope solution were varied in the range of 0-0.1 wt %. The antibacterial property of the resulting membranes was assessed using the Kirby Bauer disc diffusion method. The results show an inhibition zone formed around the PVDF/ginger membrane against Escherichia coli and Staphylococcus aureus demonstrating the efficacy of the residual ginger extract in the membrane matrix to impose the antibiofouling property. The addition of the ginger extract also enhanced the hydrophilicity in the membrane surface by lowering the contact angle from 93° to 85°, which was in good agreement with the increase in the pure water flux of up to 62%.
Fulltext Real-Time Stress Assessment Using Sliding Window Based Convolutional Neural Network

Naqvi SF, Ali SSA, Yahya N, Yasin MA, Hafeez Y, Subhani AR, et al.

Sensors (Basel), 2020 Aug 07;20(16).
PMID: 32784531 DOI: 10.3390/s20164400

Mental stress has been identified as a significant cause of several bodily disorders, such as depression, hypertension, neural and cardiovascular abnormalities. Conventional stress assessment methods are highly subjective and tedious and tend to lack accuracy. Machine-learning (ML)-based computer-aided diagnosis systems can be used to assess the mental state with reasonable accuracy, but they require offline processing and feature extraction, rendering them unsuitable for real-time applications. This paper presents a real-time mental stress assessment approach based on convolutional neural networks (CNNs). The CNN-based approach afforded real-time mental stress assessment with an accuracy as high as 96%, the sensitivity of 95%, and specificity of 97%. The proposed approach is compared with state-of-the-art ML techniques in terms of accuracy, time utilisation, and quality of features.
Nanoparticles Based Intranasal Delivery of Drug to Treat Alzheimer's Disease: A Recent Update

Pandey M, Choudhury H, Verma RK, Chawla V, Bhattamisra SK, Gorain B, et al.

CNS Neurol Disord Drug Targets, 2020;19(9):648-662.
PMID: 32819251 DOI: 10.2174/1871527319999200819095620

Alzheimer Association Report (2019) stated that the 6th primary cause of death in the USA is Alzheimer's Disease (AD), which leads to behaviour and cognitive impairment. Nearly 5.8 million peoples of all ages in the USA have suffered from this disease, including 5.6 million elderly populations. The statistics of the progression of this disease is similar to the global scenario. Still, the treatment of AD is limited to a few conventional oral drugs, which often fail to deliver an adequate amount of the drug in the brain. The reduction in the therapeutic efficacy of an anti-AD drug is due to poor solubility, existence to the blood-brain barrier and low permeability. In this context, nasal drug delivery emerges as a promising route for the delivery of large and small molecular drugs for the treatment of AD. This promising pathway delivers the drug directly into the brain via an olfactory route, which leads to the low systemic side effect, enhanced bioavailability, and higher therapeutic efficacy. However, few setbacks, such as mucociliary clearance and poor drug mucosal permeation, limit its translation from the laboratory to the clinic. The above stated limitation could be overcome by the adaption of nanoparticle as a drug delivery carrier, which may lead to prolong delivery of drugs with better permeability and high efficacy. This review highlights the latest work on the development of promising Nanoparticles (NPs) via the intranasal route for the treatment of AD. Additionally, the current update in this article will draw the attention of the researcher working on these fields and facing challenges in practical applicability.
Fulltext 99mTc-sodium phytate is a valid alternative to the gold-standard 99mTc-sulfur colloid in the measurement of gastric emptying among healthy multi-ethnic Asian population: results of a randomized cross-over trial

Mat Nawi N, Tagiling N, Mohd Rohani MF, Wan Zainon WMN, Zanial MS, Wong MS, et al.

BMC Gastroenterol, 2020 Aug 31;20(1):293.
PMID: 32867699 DOI: 10.1186/s12876-020-01426-5

BACKGROUND: It is unclear if the 99mTc-sodium phytate (99mTc-SP) is as reliable as the gold-standard 99mTc-sulfur colloid (99mTc-SC) for gastric emptying scintigraphy (GES). This study is aimed to compare the emptying rates of both radiotracers in a prospective, randomized cross-over trial and to determine the normative data of a healthy multi-ethnic Asian population.
METHODS: Out of the 44 healthy individuals screened, 31 (14 females; mean age: 28.4 ± 7.0 years) were enrolled and underwent GES using the standardized egg-white meal. All participants were randomly assigned to either 99mTc-SP or 99mTc-SC on the first GES session before crossed over to the other formulation after 2 weeks.
RESULTS: Both kits achieved the radiochemical purities of > 95%. The median rate (95th upper normative limit) of gastric emptying, reported as total gastric meal retention between 99mTc-SP and 99mTc-SC, was found to be comparable at all measured time points: 0.5 h [85.0% (96.6%) vs. 82.0% (94.0%)], 1 h [70.0% (86.4%) vs. 65.0% (86.6%)], 2 h [31.0% (55.8%) vs. 25.0% (64.4%)], 3 h [7.0% (26.3%) vs. 5.0% (29.9%)], and 4 h [3.0% (10.3%) vs. 2.0% (9.9%)]; P > 0.05. In addition, both radiotracers correlated well (Kendall's Tau (τ) coefficient = 0.498, P
Fulltext Structure Characterization and Biological Activity of 2-Arylbenzofurans from an Indonesian Plant, Sesbania grandiflora (L.) Pers

Noviany N, Samadi A, Yuliyan N, Hadi S, Aziz M, Purwitasari N, et al.

Phytochem Lett, 2020 Feb;35:211-215.
PMID: 32863985 DOI: 10.1016/j.phytol.2019.12.008

A new 2-arylbenzofuran, sesbagrandiflorain C (1), together with four known compounds, 2-(3,4-dihydroxy-2-methoxyphenyl)-4-hydroxy-6-methoxybenzofuran-3-carbaldehyde (2), 2-(4-hydroxy-2-methoxyphenyl)-5,6-dimethoxybenzofuran-3-carboxaldehyde (3), sesbagrandiflorain A (4) and sesbagrandiflorain B (5), have been isolated from the stem bark of an Indonesian plant, Sesbania grandiflora (L.) Pers. The chemical structure of compound 1 was elucidated by UV, IR, MS, and NMR spectroscopic techniques. The proton and carbon NMR resonances of 1 were also compared with the predicted chemical shifts obtained from DFT quantum mechanical calculations with Gaussian. None of the compounds showed antibacterial activity against Bacillus subtilis, Escherichia coli, Mycobacterium smegmatis, Pseudomonas aeruginosa, and Staphylococcus aureus in an agar diffusion assay. However, sesbagrandiflorains A (4) and B (5) exhibited moderate activity against Mycobacterium tuberculosis H37Rv. In addition, compounds 1 - 5 have moderate cytotoxicity against HeLa, HepG2, and MCF-7 cancer cell lines.
Synthesis, characterization, antibacterial, hemolytic and thrombolytic activity evaluation of 5-(3-chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives

Aziz-Ur-Rehman -, Khan SG, Bokhari TH, Anjum F, Akhter N, Rasool S, et al.

Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):871-876.
PMID: 32863264

A novel series of 5-(3-Chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives was efficiently synthesized and screened for antibacterial, hemolytic and thrombolytic activities. The molecule 7c remained the best inhibitor of all selected bacterial strains and furthermore possessed very low toxicity, 8.52±0.31. Compound 7a 7b and 7f showed very good thrombolytic activity relative to Streptokinase employed as reference drug. In addition to low toxicity and moderately good thrombolytic activity, the synthesized compounds possessed excellent to moderate antibacterial activity, relative to ciprofloxacin. All compounds especially 7b and 7f can be consider for further clinical studies and might be helpful in synthesis of new drugs for treatment of cardiovascular diseases.
Fulltext Enhancement of targeted microalgae species growth using aquaculture sludge extracts

Arumugam K, Ahmad MF, Yaacob NS, Ikram WM, Maniyam MN, Abdullah H, et al.

Heliyon, 2020 Jul;6(7):e04556.
PMID: 32775725 DOI: 10.1016/j.heliyon.2020.e04556

Natural growth-promoting nutrients extracted from aquaculture sludge waste can be used to maximise microalgal growth. This study identified the influence of aquaculture sludge extract (SE) on four microalgae species. Conway or Bold's Basal Media (BBM) was supplemented with SE collected from a Sabak Bernam shrimp pond (SB) and Kota Puteri fish pond (KP), and tested using a novel microplate-incubation technique. Five different autoclave extraction treatment parameters were assessed for both collected SE, i.e., 1-h at 105 °C, 2-h at 105 °C, 1-h at 121 °C, 2-h at 121 °C, and 24-h at room temperature (natural extraction). Microalgae culture in the microplates containing control (media) and enriched (media + SE) samples were incubated for nine days, at 25 °C with the light intensity of 33.75 μmol photons m-2 s-1 at 12-h light/dark cycle. The total dissolved nitrogen (TDN) and total dissolved phosphorus (TDP) in KP SE were 44.0-82.0 mg L-1 and 0.96-8.60 mg L-1. TDN (8.0%-515.0%) and TDP (105%-186 %) were relatively higher in KP SE compared to SB SE. The growth of microalgae species Nannochloropsis ocenica showed significant differences (p < 0.05) between the five extraction treatments from SB and the control. However, Chlorella vulgaris, Neochloris conjuncta, and Nephroclamys subsolitaria showed no significant differences (p > 0.05) in SB SE. N. ocenica, C. vulgaris, and N. conjuncta showed significant differences (p < 0.05) between five extraction treatments from KP and the control while N. subsolitaria showed no significant difference (p > 0.05). The specific growth rate (SGR) in the exponential phase of all microalgae species were relatively higher in SB SE compared to KP SE. While the organic matter content of KP SE was relatively higher, there were no significant differences in microalgae growth compared to SB SE. Nonetheless, modified SE did influence microalgae growth compared to the control. This study shows that modified SE could be used as enrichment media for microalgae cultivation.
Fulltext Sale of WHO AWaRe groups antibiotics without a prescription in Pakistan: a simulated client study

Saleem Z, Hassali MA, Godman B, Fatima M, Ahmad Z, Sajid A, et al.

J Pharm Policy Pract, 2020;13:26.
PMID: 32774870 DOI: 10.1186/s40545-020-00233-3

Introduction: Resistant strains of bacteria are rapidly emerging with increasing inappropriate use of antibiotics rendering them less efficacious. Self-purchasing of antibiotics particularly for viral infections is a key driver of inappropriate use, especially in lower- and middle-income countries. There is a particular issue in countries such as Pakistan. Consequently, there is a need to assess current rates of self-purchasing especially for reserve antibiotics to guide future policies.
Aims: Assess the extent of current antibiotic sales without a prescription in urban areas of Pakistan.
Methodology: A multicenter cross-sectional study was conducted in different areas of Punjab, Pakistan using Simulated Client technique. The investigators demanded different predefined antibiotics from WHO AWaRe groups without prescription. Three levels of demand were used to convince the pharmacy staff in order to dispense the antibiotic without a prescription. A data collection form was completed by simulated clients within 15 min of each visit.
Results: Overall 353 pharmacies and medical stores were visited out of which 96.9% pharmacies and medical stores dispensed antibiotics without demanding a prescription (82.7% at demand level 1 and 14.2% at demand level 2), with only 3.1% of pharmacies refusing to dispense antibiotics. The most frequently dispensed antibiotic was ciprofloxacin (22.1%). Surprisingly, even the reserve group antibiotics were also dispensed without a prescription. In only 25.2% visits, pharmacy staff guided patients about the use of antibiotics, and in only 11.0% pharmacists enquired about other medication history.
Conclusion: Currently, antibiotics are easily acquired without a legitimate prescription in Pakistan. There is a need for strict adherence to regulations combined with a multi-dimensional approach to enhance appropriate dispensing of antibiotics and limit any dispensing of WHO restricted antibiotics without a prescription.
Fulltext Phytochemical screening and enzymatic and antioxidant activities of Erythrina suberosa (Roxb) bark

Ahmed Z, Aziz S, Hanif M, Mohiuddin SG, Ali Khan SH, Ahmed R, et al.

J Pharm Bioallied Sci, 2020 04 10;12(2):192-200.
PMID: 32742119 DOI: 10.4103/jpbs.JPBS_222_19

Background: This study aimed to evaluate the phytochemicals screening of Erythrina suberosa (Roxb) bark and to analyze the enzymatic activities of its various organic fractions.
Materials and Methods: Crude methanolic fraction of E. suberosa (Roxb) bark and its respective fractions were screened for the presence of different phytochemicals with different reagents. On the basis of increasing order of polarity, different organic solvents were used to obtain different fractions. Enzymatic studies were performed on crude methanolic extract of the plant. All the assays were performed under standard in vitro conditions.
Results: The phytochemical analysis shows the presence of alkaloids, phenols, triterpenoids, phytosterols, and flavonoids. Phenolic compounds and flavonoids are the major constituents of the plant. In anticholinesterase assay, the percent inhibition of standard drug (eserine) was 91.27 ± 1.17 and the half maximal inhibitory concentration (IC50) was 0.04 ± 0.0001. For α-glucosidase inhibition, the IC50 value for Dichloromethane fraction was 8.45 ± 0.13, for Methanol fraction it was 64.24 ± 0.15, and for aqueous fraction it was 42.62 ± 0.17 as compared with standard IC50 that is 37.42 (acarbose). Furthermore, results show that all fractions have potential against anti-urease enzyme, but DCM fraction of crude aqueous extract has significant IC50 value (45.26 ± 0.13) than other fractions.
Conclusion: Keeping in view all the results, it is evident that the plant can be used in future for formulating effective drugs against many ailments. Secondary metabolites and their derivatives possess different biological activities, for example, .g. flavonoids in cancer, asthma, and Alzheimer. Furthermore, the extracts of this plant can be used in their crude form, which is an addition to the complementary and alternative treatment strategies.

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