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Single-trial extraction of event-related potentials (ERPs) and classification of visual stimuli by ensemble use of discrete wavelet transform with Huffman coding and machine learning techniques

Amin HU, Ullah R, Reza MF, Malik AS

J Neuroeng Rehabil, 2023 Jun 02;20(1):70.
PMID: 37269019 DOI: 10.1186/s12984-023-01179-8

BACKGROUND: Presentation of visual stimuli can induce changes in EEG signals that are typically detectable by averaging together data from multiple trials for individual participant analysis as well as for groups or conditions analysis of multiple participants. This study proposes a new method based on the discrete wavelet transform with Huffman coding and machine learning for single-trial analysis of evenal (ERPs) and classification of different visual events in the visual object detection task.
METHODS: EEG single trials are decomposed with discrete wavelet transform (DWT) up to the [Formula: see text] level of decomposition using a biorthogonal B-spline wavelet. The coefficients of DWT in each trial are thresholded to discard sparse wavelet coefficients, while the quality of the signal is well maintained. The remaining optimum coefficients in each trial are encoded into bitstreams using Huffman coding, and the codewords are represented as a feature of the ERP signal. The performance of this method is tested with real visual ERPs of sixty-eight subjects.
RESULTS: The proposed method significantly discards the spontaneous EEG activity, extracts the single-trial visual ERPs, represents the ERP waveform into a compact bitstream as a feature, and achieves promising results in classifying the visual objects with classification performance metrics: accuracies 93.60[Formula: see text], sensitivities 93.55[Formula: see text], specificities 94.85[Formula: see text], precisions 92.50[Formula: see text], and area under the curve (AUC) 0.93[Formula: see text] using SVM and k-NN machine learning classifiers.
CONCLUSION: The proposed method suggests that the joint use of discrete wavelet transform (DWT) with Huffman coding has the potential to efficiently extract ERPs from background EEG for studying evoked responses in single-trial ERPs and classifying visual stimuli. The proposed approach has O(N) time complexity and could be implemented in real-time systems, such as the brain-computer interface (BCI), where fast detection of mental events is desired to smoothly operate a machine with minds.
Tracking of EEG activity using motion estimation to understand brain wiring

Nisar H, Malik AS, Ullah R, Shim SO, Bawakid A, Khan MB, et al.

Adv Exp Med Biol, 2015;823:159-74.
PMID: 25381107 DOI: 10.1007/978-3-319-10984-8_9

The fundamental step in brain research deals with recording electroencephalogram (EEG) signals and then investigating the recorded signals quantitatively. Topographic EEG (visual spatial representation of EEG signal) is commonly referred to as brain topomaps or brain EEG maps. In this chapter, full search full search block motion estimation algorithm has been employed to track the brain activity in brain topomaps to understand the mechanism of brain wiring. The behavior of EEG topomaps is examined throughout a particular brain activation with respect to time. Motion vectors are used to track the brain activation over the scalp during the activation period. Using motion estimation it is possible to track the path from the starting point of activation to the final point of activation. Thus it is possible to track the path of a signal across various lobes.
Vasodilator effect of Phlomis bracteosa constituents is mediated through dual endothelium-dependent and endothelium-independent pathways

Khan AU, Ullah R, Khan A, Mustafa MR, Hussain J, Murugan DD, et al.

Clin Exp Hypertens, 2012;34(2):132-9.
PMID: 21967029 DOI: 10.3109/10641963.2011.601383

This study describes the vasorelaxant potential of some pure compounds isolated from Phlomis bracteosa L. marrubiin, phlomeoic acid, and two new constituents labeled as RA and RB. In rat thoracic aortic rings denuded of endothelium, marrubiin, phlomeoic acid, RA, and RB caused relaxation of high K(+) (80 mM) and phenylephrine (1 μM)-induced contractions at the concentration range of 1.0-1000 μg/mL. Marrubiin, phlomeoic acid, RA, and RB concentration dependently (3.0-10 μg/mL) shifted the Ca(++) curves to the right obtained in Ca(++)-free medium. The vasodilator effect of marrubiin, phlomeoic acid, RA, and RB was partially blocked by N(ω)-nitro-L-arginine methyl ester in endothelium-intact aorta preparations. These results reveal that P. bracteosa constituents: marrubiin, phlomeoic acid, RA, and RB exhibit vasodilator action occurred via a combination of endothelium-independent Ca(++) antagonism and endothelium-dependent N(ω)-nitro-L-arginine methyl ester-sensitive nitric oxide-modulating mechanism.
Fulltext Isolation, Structure Elucidation and In Silico Prediction of Potential Drug-Like Flavonoids from Onosma chitralicum Targeted towards Functionally Important Proteins of Drug-Resistant Bad Bugs

Khan SA, Khan SU, Fozia, Ullah N, Shah M, Ullah R, et al.

Molecules, 2021 Apr 02;26(7).
PMID: 33918531 DOI: 10.3390/molecules26072048

Admittedly, the disastrous emergence of drug resistance in prokaryotic and eukaryotic human pathogens has created an urgent need to develop novel chemotherapeutic agents. Onosma chitralicum is a source of traditional medicine with cooling, laxative, and anthelmintic effects. The objective of the current research was to analyze the biological potential of Onosma chitralicum, and to isolate and characterize the chemical constituents of the plant. The crude extracts of the plant prepared with different solvents, such as aqueous, hexane, chloroform, ethyl acetate, and butanol, were subjected to antimicrobial activities. Results corroborate that crude (methanol), EtoAc, and n-C6H14 fractions were more active against bacterial strains. Among these fractions, the EtoAc fraction was found more potent. The EtoAc fraction was the most active against the selected microbes, which was subjected to successive column chromatography, and the resultant compounds 1 to 7 were isolated. Different techniques, such as UV, IR, and NMR, were used to characterize the structures of the isolated compounds 1-7. All the isolated pure compounds (1-7) were tested for their antimicrobial potential. Compounds 1 (4',8-dimethoxy-7-hydroxyisoflavone), 6 (5,3',3-trihydroxy-7,4'-dimethoxyflavanone), and 7 (5',7,8-trihydroxy-6,3',4'-trimethoxyflavanone) were found to be more active against Staphylococcus aureus and Salmonella Typhi. Compound 1 inhibited S. typhi and S. aureus to 10 ± 0.21 mm and 10 ± 0.45 mm, whereas compound 6 showed inhibition to 10 ± 0.77 mm and 9 ± 0.20 mm, respectively. Compound 7 inhibited S. aureus to 6 ± 0.36 mm. Compounds 6 and 7 showed significant antibacterial potential, and the structure-activity relationship also justifies their binding to the bacterial enzymes, i.e., beta-hydroxyacyl dehydratase (HadAB complex) and tyrosyl-tRNA synthetase. Both bacterial enzymes are potential drug targets. Further, the isolated compounds were found to be active against the tested fungal strains. Whereas docking identified compound 7, the best binder to the lanosterol 14α-demethylase (an essential fungal cell membrane synthesizing enzyme), reported as an antifungal fluconazole binding enzyme. Based on our isolation-linked preliminary structure-activity relationship (SAR) data, we conclude that O. chitralicum can be a good source of natural compounds for drug development against some potential enzyme targets.
Fulltext DC-GAN-based synthetic X-ray images augmentation for increasing the performance of EfficientNet for COVID-19 detection

Shah PM, Ullah H, Ullah R, Shah D, Wang Y, Islam SU, et al.

Expert Syst, 2021 Oct 19.
PMID: 34898799 DOI: 10.1111/exsy.12823

Currently, many deep learning models are being used to classify COVID-19 and normal cases from chest X-rays. However, the available data (X-rays) for COVID-19 is limited to train a robust deep-learning model. Researchers have used data augmentation techniques to tackle this issue by increasing the numbers of samples through flipping, translation, and rotation. However, by adopting this strategy, the model compromises for the learning of high-dimensional features for a given problem. Hence, there are high chances of overfitting. In this paper, we used deep-convolutional generative adversarial networks algorithm to address this issue, which generates synthetic images for all the classes (Normal, Pneumonia, and COVID-19). To validate whether the generated images are accurate, we used the k-mean clustering technique with three clusters (Normal, Pneumonia, and COVID-19). We only selected the X-ray images classified in the correct clusters for training. In this way, we formed a synthetic dataset with three classes. The generated dataset was then fed to The EfficientNetB4 for training. The experiments achieved promising results of 95% in terms of area under the curve (AUC). To validate that our network has learned discriminated features associated with lung in the X-rays, we used the Grad-CAM technique to visualize the underlying pattern, which leads the network to its final decision.
Fulltext Seed germination ecology of Conyza sumatrensis populations stemming from different habitats and implications for management

Xu Y, Ye J, Khalofah A, Zuan ATK, Ullah R, El-Shehawi AM

PLoS One, 2021;16(12):e0260674.
PMID: 34855863 DOI: 10.1371/journal.pone.0260674

Conyza sumatrensis (Retz.) E. H. Walker is an obnoxious weed, emerging as an invasive species globally. Seed germination biology of four populations of the species stemming from arid, semi-arid, temperate, and humid regions was determined in this study. Seed germination was recorded under six different environmental cues (i.e., light/dark periods, constant and alternating day and night temperatures, pH, salinity, and osmotic potential levels) in separate experiment for each cue. Populations were main factor, whereas levels of each environmental cue were considered as sub-factor. The impact of seed burial depths on seedling emergence was inferred in a greenhouse pot experiment. Seed germination was recorded daily and four germination indices, i.e., seed germination percentage, mean germination time, time to reach 50% germination, and mean daily germination were computed. Tested populations and levels of different environmental cues had significant impact on various seed germination indices. Overall, seeds stemming from arid and semi-arid regions had higher seed germination potential under stressful and benign environmental conditions compared to temperate and humid populations. Seed of all populations required a definite light period for germination and 12 hours alternating light and dark period resulted in the highest seed germination. Seed germination of all populations occurred under 5-30°C constant and all tested alternate day and night temperatures. However, the highest seed germination was recorded under 20°C. Seeds of arid and semi-arid populations exhibited higher germination under increased temperature, salinity and osmotic potential levels indicating that maternal environment strongly affected germination traits of the tested populations. The highest seed germination of the tested populations was noted under neutral pH, while higher and lower pH than neutral had negative impact on seed germination. Arid and semi-arid populations exhibited higher seed germination under increased pH compared to temperate and humid populations. Seed burial depth had a significant effect on the seedling emergence of all tested populations. An initial increase was noted in seedling emergence percentage with increasing soil depth. However, a steep decline was recorded after 2 cm seed burial depth. These results indicate that maternal environment strongly mediates germination traits of different populations. Lower emergence from >4 cm seed burial depth warrants that deep burial of seeds and subsequent zero or minimum soil disturbance could aid the management of the species in agricultural habitats. However, management strategies should be developed for other habitats to halt the spread of the species.
Fulltext Epidemiology and phylogeny of Haemonchus contortus through internal transcribed spacer 2 gene in small ruminants

Ahmad N, Khan SA, Majid HA, Ali R, Ullah R, Bari A, et al.

Front Vet Sci, 2024;11:1380203.
PMID: 38655530 DOI: 10.3389/fvets.2024.1380203

INTRODUCTION: Haemonchus contortus (H. contortus) is a blood-feeding nematode causing infectious disease haemonchosis in small ruminants of tropical and subtropical regions around the world. This study aimed to explore the prevalence and phylogeny of H. contortus in small ruminants using the internal transcribed spacer-2 (ITS-2) gene. In addition, a comprehensive review of the available literature on the status of H. contortus in Pakistan was conducted.
METHODS: Fecal samples were collected from sheep and goats (n = 180). Microscopically positive samples were subjected to DNA extraction followed by PCR using species-specific primers.
RESULTS: The overall prevalence of H. contortus was 25.55% in small ruminants. The prevalence of H. contortus was significantly associated with months and area. The highest occurrence of haemonchosis was documented in July (38.70%), whereas the lowest occurred in December (11.11%), with significant difference. The prevalence was highest in the Ghamkol camp (29.4%) and lowest in the arid zone of the Small Ruminant Research Institute (17.5%) (p = 0.01). The results of the systematic review revealed the highest prevalence of haemonchosis (34.4%) in Khyber Pakhtunkhwa (p = 0.001).
DISCUSSION: Phylogenetic analysis revealed a close relationship between H. contortus and isolates from Asia (China, India, Iran, Bangladesh, Malaysia, and Mongolia) and European countries (Italy and the United Kingdom). It has been concluded that H. contortus is prevalent in small ruminants of Kohat district and all over Pakistan, which could be a potential threat to food-producing animals, farmers, dairy, and the meat industry. Phylogenetic analysis indicates that H. contortus isolates share close phylogenetic relationships with species from Asia and Europe.
Fulltext Isolation, Characterization and Neuroprotective Activity of Folecitin: An In Vivo Study

Farooq U, Khan T, Shah SA, Hossain MS, Ali Y, Ullah R, et al.

Life (Basel), 2021 Aug 12;11(8).
PMID: 34440569 DOI: 10.3390/life11080825

Neurodegenerative diseases (NDs) extend the global health burden. Consumption of alcohol as well as maternal exposure to ethanol can damage several neuronal functions and cause cognition and behavioral abnormalities. Ethanol induces oxidative stress that is linked to the development of NDs. Treatment options for NDs are yet scarce, and natural product-based treatments could facilitate ND management since plants possess plenty of bioactive metabolites, including flavonoids, which typically demonstrate antioxidant and anti-inflammatory properties. Hypericum oblongifolium is an important traditional medicinal plant used for hepatitis, gastric ulcer, external wounds, and other gastrointestinal disorders. However, it also possesses multiple bioactive compounds and antioxidant properties, but the evaluation of isolated pure compounds for neuroprotective efficacy has not been done yet. Therefore, in the current study, we aim to isolate and characterize the bioactive flavonoid folecitin and evaluate its neuroprotective activity against ethanol-induced oxidative-stress-mediated neurodegeneration in the hippocampus of postnatal day 7 (PND-7) rat pups. A single dose of ethanol (5 g/kg body weight) was intraperitoneally administered after the birth of rat pups on PND-7. This caused oxidative stress accompanied by the activation of phosphorylated-c-Jun N-terminal kinase (p-JNK), nod-like receptor family pyrin domain containing 3 (NLRP3), apoptosis-associated speck-like protein (ASC), and cysteine-aspartic acid protease-1 (caspase-1) proteins to form a complex called the NLRP3-inflammasome, which converts pro-interleukin 1 beta (IL-1B) to activate IL-1B and induce widespread neuroinflammation and neurodegeneration. In contrast, co-administration of folecitin (30 mg/kg body weight) reduced ethanol-induced oxidative stress, inhibited p-JNK, and deactivated the NLRP3-inflammasome complex. Furthermore, folecitin administration reduced neuroinflammatory and neurodegenerative protein markers, including decreased caspase-3, BCL-2-associated X protein (BAX), B cell CLL/lymphoma 2 (BCL-2), and poly (ADP-ribose) polymerase-1 (PARP-1) expression in the immature rat brain. These findings conclude that folecitin is a flavone compound, and it might be a novel, natural and safe agent to curb oxidative stress and its downstream harmful effects, including inflammasome activation, neuroinflammation, and neurodegeneration. Further evaluation in a dose-dependent manner would be worth it in order to find a suitable dose regimen for NDs.
Fulltext A new strategy for taste masking of azithromycin antibiotic: development, characterization, and evaluation of azithromycin titanium nanohybrid for masking of bitter taste using physisorption and panel testing studies

Amin F, Khan S, Shah SMH, Rahim H, Hussain Z, Sohail M, et al.

Drug Des Devel Ther, 2018;12:3855-3866.
PMID: 30510401 DOI: 10.2147/DDDT.S183534

Background: The obnoxious bitter taste of orally taken antibiotics is one of the biggest problems in the treatment of children. The pediatric population cannot tolerate the bitter taste of drugs and vomit out which ultimately leads to suboptimal therapeutic value, grimace and mental stress so it is the challenging task for the formulation scientists to formulate a palatable formulation particularly to overcome address the issue.
Purpose of study: The study aimed to mask and evaluate the unpleasant bitter taste of azithro-mycin (AZ) in the dry suspension dosage form by physisorption technique.
Materials and methods: AZ was selected as an adsorbent and titanium dioxide nanoparticles as adsorbate. The AZ nanohybrids (AZN) were prepared by treating fixed amount of adsorbent with a varied amount of adsorbate, prepared separately by dispersing it in an aqueous medium. The mixture was sonicated, stirred followed by filtration and drying. The AZN produced were characterized by various techniques including scanning electron microscopy (SEM), energy dispersive X-rays (EDX), powder X-ray diffraction (PXRD), HPLC and Fourier-transformed infrared (FTIR). The optimized nanohybrid was blended with other excipients to get stable and taste masked dry suspension dosage form.
Results: The results confirmed the adsorption of titanium dioxide nanoparticles on the surface of AZ. The fabricated optimized formulation was subjected for taste masking by panel testing and accelerated stability studies. The results showed a remarkable improvement in bitter taste masking, inhibiting throat bite without affecting the dissolution rate. The product showed an excellent stability both in dry and reconstituted suspension. The optimized formulation of AZN and was found stable when subjected to physical and chemical stability studies, this is because of short and single step process which interns limits the exposure of the product to various environmental factors that could potentially affect the stability of the product. The dissolution rate of the optimized formulation of AZN was compared with its marketed counterpart, showing the same dissolution rate compared to its marketed formulation.
Conclusion: The current study concludes that, by fabricating AZ-titanium nanohybrids using physisorption can effectively mask the bitter taste of the drug. The palatability and stability of azithromycin formulation was potentially enhanced without affecting its dissolution rate.
Fulltext Hepatoprotective Potential of Pomegranate in Curbing the Incidence of Acute Liver Injury by Alleviating Oxidative Stress and Inflammatory Response

Ali H, Jahan A, Samrana S, Ali A, Ali S, Kabir N, et al.

Front Pharmacol, 2021;12:694607.
PMID: 34899284 DOI: 10.3389/fphar.2021.694607

Hepatitis is an inflammatory disease of the liver and is considered one of the leading causes of death worldwide. Due to its scavenging activity, Punica granatum may be used for the treatment and prevention of liver diseases. The current study investigated the protective mechanism underlying the effects of pomegranate against a rat model of carbon tetrachloride-induced liver injury. Intraperitoneal injection of CCl4 resulted in liver inflammation, oxidative stress, and accumulation of lipid in hepatocytes. CCl4 induced a downregulation of superoxide dismutase (SOD), glutathione (GSH), and melonaldehyde (MDA). Pomegranate protection was assessed in terms of biochemical parameters, histopathology, and immunohistochemistry. Promegranate administration decreased inflammation, elevated serum enzymes and ROS production, and countered the debilitating effects caused by CCl4. In addition, CCl4-induced histological changes were absent in the crude pomegranate extract group, which also enhanced the scavenging activity of reactive oxygen species by enhancing the antioxidant defense mechanism as confirmed by detecting MDA, SOD, and GSH expressions. The migration of CD68+ macrophages was halted at the injured area of the central vein and the number of macrophages was reduced to the normal control by the crude extract compared to the positive control silymarin group. Likewise, protective effects of ethylacetate and the aqueous fraction of the crude extract were also observed. However, the butanol and n-hexane fractions displayed increased levels of ALT, AST, and ALP as compared to silymarin. About 25% damage to hepatocytes was observed in the butanol and n-hexane group by histopathological examination, which is a little better compared to the CCl4-treated group. The crude extract and its ethyl acetate and aqueous fractions may be accountable for the hepatoprotective potential of Punica granatum, which was further confirmed by in vivo experiments. Together, these findings confirm that pomegranate exerts hepatoprotective activity against CCl4-induced oxidative stress and liver damage.
Fulltext Linking Corporate Social Responsibility to Workplace Deviant Behaviors: Mediating Role of Job Satisfaction

Memon KR, Zada M, Ghani B, Ullah R, Azim MT, Mubarik MS, et al.

Front Psychol, 2021;12:803481.
PMID: 35035376 DOI: 10.3389/fpsyg.2021.803481

The purpose of this article is to present a mechanism through which the deviant work behaviors of employees can be dealt-with positively through corporate good deeds in the form of fulfilling social responsibilities. Based on the spirit of social identity theory and social exchange theory, the study explores the relationships of various deviant behaviors with corporate social responsibility (CSR) through the mediation mechanism of job satisfaction. Data were collected from 385 employees of 40 large manufacturing organizations involved in CSR activities operating in Pakistan. A self-report survey was conducted using a close-ended questionnaire. Data analysis was performed using SEM through Mplus 7. The results reveal that both internal and external CSR contribute to the reduced level of turnover intention, counterproductive work behaviors, and prohibitive voice behaviors. Job satisfaction fully mediates the relationship for internal CSR while partially mediates for external CSR. The study encourages the practitioners to avail approaches that convey the feelings of care, concern, and safety, representing internal CSR practices through diverse HR interventions, organizational support, and justice. They should also keep up the socially responsible behaviors aiming toward the larger community.
Fulltext Aceclofenac nanocrystals with enhanced in vitro, in vivo performance: formulation optimization, characterization, analgesic and acute toxicity studies

Rahim H, Sadiq A, Khan S, Khan MA, Shah SMH, Hussain Z, et al.

Drug Des Devel Ther, 2017;11:2443-2452.
PMID: 28860715 DOI: 10.2147/DDDT.S140626

This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation-ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0.12%, w/w). The characterization of AC was performed using zeta sizer, scanning electron microscopy, transmission electron microscopy, powder X-ray diffraction and differential scanning calorimetry. The saturation solubility of the AC nanocrystals was substantially increased 2.6- and 4.5-fold compared to its unprocessed active pharmaceutical ingredient in stabilizer solution and unprocessed drug. Similarly, the dissolution rate of the AC nanocrystals was substantially enhanced compared to its other counterpart. The results showed that >88% of AC nanocrystals were dissolved in first 10 min compared to unprocessed AC (8.38%), microsuspension (66.65%) and its marketed tablets (17.65%). The in vivo studies of the produced stabilized nanosuspension demonstrated that the Cmax were 4.98- and 2.80-fold while area under curve from time of administration to 24 h (AUC0→24 h) were found 3.88- and 2.10-fold greater when compared with unprocessed drug and its marketed formulation, respectively. The improved antinociceptive activity of AC nanocrystals was shown at much lower doses as compared to unprocessed drug, which is purely because of nanonization which may be attributed to improved solubility and dissolution rate of AC, ultimately resulting in its faster rate of absorption.
Fulltext Experimental and molecular modeling approach to optimize suitable polymers for fabrication of stable fluticasone nanoparticles with enhanced dissolution and antimicrobial activity

Ahmed S, Govender T, Khan I, Rehman NU, Ali W, Shah SMH, et al.

Drug Des Devel Ther, 2018;12:255-269.
PMID: 29440875 DOI: 10.2147/DDDT.S148912

Background and aim: The challenges with current antimicrobial drug therapy and resistance remain a significant global health threat. Nanodrug delivery systems are playing a crucial role in overcoming these challenges and open new avenues for effective antimicrobial therapy. While fluticasone (FLU), a poorly water-soluble corticosteroid, has been reported to have potential antimicrobial activity, approaches to optimize its dissolution profile and antimicrobial activity are lacking in the literature. This study aimed to combine an experimental study with molecular modeling to design stable FLU nanopolymeric particles with enhanced dissolution rates and antimicrobial activity.
Methods: Six different polymers were used to prepare FLU nanopolymeric particles: hydroxyl propyl methylcellulose (HPMC), poly (vinylpyrrolidone) (PVP), poly (vinyl alcohol) (PVA), ethyl cellulose (EC), Eudragit (EUD), and Pluronics®. A low-energy method, nanoprecipitation, was used to prepare the polymeric nanoparticles.
Results and conclusion: The combination of HPMC-PVP and EUD-PVP was found most effective to produce stable FLU nanoparticles, with particle sizes of 250 nm ±2.0 and 280 nm ±4.2 and polydispersity indices of 0.15 nm ±0.01 and 0.25 nm ±0.03, respectively. The molecular modeling studies endorsed the same results, showing highest polymer drug binding free energies for HPMC-PVP-FLU (-35.22 kcal/mol ±0.79) and EUD-PVP-FLU (-25.17 kcal/mol ±1.12). In addition, it was observed that Ethocel® favored a wrapping mechanism around the drug molecules rather than a linear conformation that was witnessed for other individual polymers. The stability studies conducted for 90 days demonstrated that HPMC-PVP-FLU nanoparticles stored at 2°C-8°C and 25°C were more stable. Crystallinity of the processed FLU nanoparticles was confirmed using differential scanning calorimetry, powder X-ray diffraction analysis and TEM. The Fourier transform infrared spectroscopy (FTIR) studies showed that there was no chemical interaction between the drug and chosen polymer system. The HPMC-PVP-FLU nanoparticles also showed enhanced dissolution rate (P<0.05) compared to the unprocessed counterpart. The in vitro antibacterial studies showed that HPMC-PVP-FLU nanoparticles displayed superior effect against gram-positive bacteria compared to the unprocessed FLU and positive control.
Efficacy of pentamidine-loaded chitosan nanoparticles as a novel drug delivery system for Leishmania tropica

Khan RU, Khan M, Sohail A, Ullah R, Iqbal A, Ahmad B, et al.

Trop Biomed, 2022 Dec 01;39(4):511-517.
PMID: 36602209 DOI: 10.47665/tb.39.4.003

The present study compares the in vitro effects of nanoparticles loaded pentamidine drug and conventional pentamidine on Leishmania tropica. Herein, pentamidine-loaded chitosan nanoparticles (PTN-CNPs) have been synthesized through an ionic gelation method with sodium tripolyphosphate (TPP). Next, the physical characteristics of PTN-CNPs were determined through the surface texture, zeta potential, in vitro drug release, drug loading content (DLC), and encapsulation efficacy (EE) and compared its efficacy with free pentamidine (PTN) drug against promastigotes and axenic amastigotes forms of L. tropica in vitro. The PTN-CNPs displayed a spherical shape having a size of 88 nm, an almost negative surface charge (-3.09 mV), EE for PTN entrapment of 86%, and in vitro drug release of 92% after 36 h. In vitro antileishmanial activity of PTN-CNPs and free PTN was performed against Leishmania tropica KWH23 promastigote and axenic amastigote using 3-(4, 5- dimethylthiazol-2-yl)-2, 5-diphenyletetrazolium bromide (MTT) assay. It was observed that the effect of PTN-CNPs and free PTN on both forms of the parasite was dose and time dependent. Free PTN presented low efficacy even at higher dose (40 µg/ml) with 25.6 ± 1.3 and 26.5 ±1.4 mean viability rate of the promastigotes and axenic amastigotes, respectively after 72 hrs incubation. While PTN-CNPs showed strong antileishmanial effects on both forms of parasite with 16 ± 0.4 and 19 ± 0.7 mean viability rate at the same higher concentration (40 µg/ml) after 72 hrs incubation. Half maximal inhibitory concentration (IC50) values of PTN-CNPs toward promastigotes and amastigotes were obtained as 0.1375 µg/ml and 0.1910 µg/ml, respectively. In conclusion, PTN-CNPs effectively inhibited both forms of the L. tropica; however, its effect was more salient on promastigotes. This data indicates that the PTN-CNPs act as a target drug delivery system. However, further research is needed to support its efficacy in animal and human CL.
Fulltext Expediting Multiple Biological Properties of Limonene and α-Pinene: Main Bioactive Compounds of Pistacia lentiscus L., Essential Oils

El Omari N, Mrabti HN, Benali T, Ullah R, Alotaibi A, Abdullah ADI, et al.

Front Biosci (Landmark Ed), 2023 Sep 27;28(9):229.
PMID: 37796709 DOI: 10.31083/j.fbl2809229

BACKGROUND: Screening new natural molecules with pharmacological and/or cosmetic properties remains a highly sought-after area of research. Moreover, essential oils and volatile compounds have recently garnered significant interest as natural substance candidates. In this study, the volatile components of Pistacia lentiscus L. essential oils (PLEOs) isolated from the fruit and its main compounds, alpha-pinene, and limonene, are investigated for antioxidant, antidiabetic, and dermatoprotective activities.
METHODS: In vitro antioxidant activity was investigated using 2,2'-diphenyl-1-picrylhydrazyl (DPPH), fluorescence recovery after photobleaching (FRAP), and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. The antidiabetic and dermatoprotective effects were studied using enzyme inhibitory activities.
RESULTS: Antioxidant tests showed that PLEO has the best activity (ranging from 29.64 ± 3.04 to 73.80 ± 3.96 µg/mL) compared to its main selected molecules (ranging from 74 ± 3.72 to 107.23 ± 5.03 µg/mL). The α-glucosidase and α-amylase assays demonstrated that the elements tested have a promising antidiabetic potential with IC50values ranging from 78.03 ± 2.31 to 116.03 ± 7.42 µg/mL and 74.39 ± 3.08 to 112.35 ± 4.92 µg/mL for the α-glucosidase and α-amylase assays, respectively, compared to the standard drug. For the tyrosinase test, we found that the EOs (IC50 = 57.72 ± 2.86 µg/mL) followed by limonene (IC50 = 74.24 ± 2.06 µg/mL) and α-pinene (IC50 = 97.45 ± 5.22 µg/mL) all exhibited greater inhibitory effects than quercetin (IC50 = 246.90 ± 2.54 µg/mL).
CONCLUSIONS: Our results suggest that the biological activities of PLEO, as well as its main compounds, make them promising candidates for the development of new strategies aimed at improving dermatoprotection and treating diseases associated with diabetes mellitus and oxidative stress.
Fulltext Engineering of Naproxen Loaded Polymer Hybrid Enteric Microspheres for Modified Release Tablets: Development, Characterization, in silico Modelling and in vivo Evaluation

Hameed HA, Khan S, Shahid M, Ullah R, Bari A, Ali SS, et al.

Drug Des Devel Ther, 2020;14:27-41.
PMID: 32021089 DOI: 10.2147/DDDT.S232111

BACKGROUND: Naproxen (NP) is a non-steroidal anti-inflammatory drug with poor aqueous solubility and low oral bioavailability, which may lead to therapeutic failure. NP causes crucial GIT irritation, bleeding, and peptic and duodenal ulcers.
PURPOSE OF THE STUDY: This study aimed to engineer and characterize polymer hybrid enteric microspheres using an integrated (experimental and molecular modelling) approach with further development to solid dosage form with modified drug release kinetics and improved bioavailability.
MATERIALS AND METHODS: NP loaded polymer hybrid enteric microspheres (PHE-Ms) were fabricated by using a modified solvent evaporation technique coupled with molecular modelling (MM) approach. The PHE-Ms were characterized by particle size, distribution, morphology, crystallinity, EE, drug-polymer compatibility, and DSC. The optimized NP loaded PHE-Ms were further subjected to downstream procedures including tablet dosage form development, stability studies and comparative in vitro-in vivo evaluation.
RESULTS: The hydrophobic polymer EUD-L100 and hydrophilic polymer HPMC-E5 delayed and modified drug release at intestinal pH while imparting retardation of NP release at gastric pH to diminish the gastric side effects. The crystallinity of the NP loaded PHE-Ms was established through DSC and P (XRD). The particle size for the developed formulations of PEH-Ms (M1-M5) was in the range from 29.06 ±7.3-74.31 ± 17.7 μm with Span index values of 0.491-0.69, respectively. The produced NP hybrid microspheres demonstrated retarded drug release at pH 1.2 and improved dissolution at pH 6.8. The in vitro drug release patterns were fitted to various release kinetic models and the best-followed model was the Higuchi model with a release exponent "n" value > 0.5. Stability studies at different storage conditions confirmed stability of the NP loaded PHE-Ms based tablets (P<0.05). The molecular modelling (MM) study resulted in adequate binding energy of co-polymer complex SLS-Eudragit-HPMC-Naproxen (-3.9 kcal/mol). In contrast to the NP (unprocessed) and marketed formulations, a significant increase in the Cmax of PHE-MT1 (44.41±4.43) was observed.
CONCLUSION: The current study concludes that developing NP loaded PHE-Ms based tablets could effectively reduce GIT consequences with restored therapeutic effects. The modified release pattern could improve the dissolution rate and enhancement of oral bioavailability. The MM study strengthens the polymer-drug relationship in microspheres.
Fulltext Biogenic Salvia species synthesized silver nanoparticles with catalytic, sensing, antimicrobial, and antioxidant properties

Ihsan S, Gul H, Jamila N, Khan N, Ullah R, Bari A, et al.

Heliyon, 2024 Feb 29;10(4):e25814.
PMID: 38375246 DOI: 10.1016/j.heliyon.2024.e25814

Salvia (Lamiaceae family) is used as a brain tonic to improve cognitive function. The species including S. plebeia and S. moorcroftiana are locally used to cure hepatitis, cough, tumours, hemorrhoids, diarrhoea, common cold, flu, and asthma. To the best of authors' knowledge, no previous study has been conducted on synthesis of S. plebeia and S. moorcroftiana silver nanoparticles (SPAgNPs and SMAgNPs). The study was aimed to synthesize AgNPs from the subject species aqueous and ethanol extracts, and assess catalytic potential in degradation of standard and extracted (from yums, candies, and snacks) dyes, nitrophenols, and antibiotics. The study also aimed at AgNPs as probe in sensing metalloids and heavy metal ions including Pb2+, Cu2+, Fe3+, Ni2+, and Zn2+. From the results, it was found that Salvia aqueous extract afforded stable AgNPs in 1:9 and 1:15 (quantity of aqueous extract and silver nitrate solution concentration) whereas ethanol extract yielded AgNPs in 1:10 (quantity of ethanol extract and silver nitrate solution concentration) reacted in sunlight. The size of SPAgNPs and SMAgNPs determined by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) were 21.7 nm and 19.9 nm, with spherical, cylindrical, and deep hollow morphology. The synthesized AgNPs demonstrated significant potential as catalyst in dyes; Congo red (85 %), methylene blue (75 %), Rhodamine B (<50 %), nitrophenols; ortho-nitrophenol (95-98 %) and para-nitrophenol (95-98 %), dyes extracted from food samples including yums, candies, and snacks. The antibiotics (amoxicillin, doxycycline, levofloxacin) degraded up to 80 %-95 % degradation. Furthermore, the synthesized AgNPs as probe in sensing of Pb2+, Cu2+, and Fe3+ in Kabul river water, due to agglomeration, caused a significant decrease and bathochromic shift of SPR band (430 nm) when analyzed after 30 min. The Pb2+ ions was comparatively more agglomerated and chelated. Thus, the practical applicability of AgNPs in Pb2+ sensing was significant. Based on the results of this research study, the synthesized AgNPs could provide promising efficiency in wastewater treatment containing organic dyes, antibiotics, and heavy metals.
Fulltext Effective Antiplasmodial and Cytotoxic Activities of Synthesized Zinc Oxide Nanoparticles Using Rhazya stricta Leaf Extract

Najoom S, Fozia F, Ahmad I, Wahab A, Ahmad N, Ullah R, et al.

Evid Based Complement Alternat Med, 2021;2021:5586740.
PMID: 34484393 DOI: 10.1155/2021/5586740

In the present study, zinc oxide (ZnO) nanoparticles were prepared using ZnCl2.2H2O as a precursor, via green route using leaf extract of Rhazya stricta as capping and reducing agent. The prepared ZnO nanoparticles were examined using UV-visible spectrophotometer (UV-Vis), Fourier transform infrared spectrometer (FT-IR), X-ray diffraction spectrometer (XRD), and scanning electron microscope (SEM). The UV-Vis absorption spectrum at 355 nm showed an absorption peak, which indicates the formation of ZnO NPs. The FT-IR spectra analysis was performed to identify the potential biomolecule of the as-prepared ZnO NPs. The FT-IR spectra showed peaks at 3455, 1438, 883, and 671 cm-1 in the region of 4000-500 cm-1, which indicates -OH, NH, C-H, and M-O groups, respectively. The SEM images showed aggregation of ZnO nanoparticles with an average size of 70-90 nm. The XRD study indicated that the ZnO NPs were crystalline in nature with hexagonal wurtzite structure and broad peaks were observed at 2 theta positions 31.8°, 34.44°, 36.29°, 47.57°, 56.61°, 67.96°, and 69.07°. The synthesized ZnO NPs were found to be good antiplasmodial with a 50% inhibitory concentration (IC50) value of 3.41 μg/mL. It is concluded from the current study that the ZnO NPs exhibited noble antiplasmodial activity, and for the improvement of antiplasmodial medications, it might be used after further in vivo studies.
Fulltext In Silico, Cytotoxic and Antioxidant Potential of Novel Ester, 3-hydroxyoctyl -5- trans-docosenoate Isolated from Anchusa arvensis (L.) M.Bieb. Against HepG-2 Cancer Cells

Hussain S, Ullah F, Ayaz M, Ali Shah SA, Ali Shah AU, Shah SM, et al.

Drug Des Devel Ther, 2019;13:4195-4205.
PMID: 31849451 DOI: 10.2147/DDDT.S228971

Background: Cancer is one of the chronic health conditions worldwide. Various therapeutically active compounds from medicinal plants were the current focus of this research in order to uncover a treatment regimen for cancer. Anchusa arvensis (A. anchusa) (L.) M.Bieb. contains many biologically active compounds.
Methods: In the current study, new ester 3-hydroxyoctyl -5- trans-docosenoate (compound-1) was isolated from the chloroform soluble fraction of A. anchusa using column chromatography. Using MTT assay, the anticancer effect of the compound was determined in human hepatocellular carcinoma cells (HepG-2) compared with normal epithelial cell line (Vero). DPPH and ABTS radical scavenging assays were performed to assess the antioxidant potential. The Molecular Operating Environment (MOE-2016) tool was used against tyrosine kinase.
Results: The structure of the compound was elucidated based on IR, EI, and NMR spectroscopy technique. It exhibited a considerable cytotoxic effect against HepG-2 cell lines with IC50 value of 6.50 ± 0.70 µg/mL in comparison to positive control (doxorubicin) which showed IC50 value of 1.3±0.21 µg/mL. The compound did not show a cytotoxic effect against normal epithelial cell line (Vero). The compound also exhibited significant DPHH scavenging ability with IC50 value of 12 ± 0.80 µg/mL, whereas ascorbic acid, used as positive control, demonstrated activity with IC50 = 05 ± 0.15 µg/mL. Similarly, it showed ABTS radical scavenging ability (IC50 = 130 ± 0.20 µg/mL) compared with the value obtained for ascorbic acid (06 ± 0.85 µg/mL). In docking studies using MOE-2016 tool, it was observed that compound-1 was highly bound to tyrosine kinase by having two hydrogen bonds at the hinge region. This good bonding network by the compound might be one of the reasons for showing significant activity against this enzyme.
Conclusion: Our findings led to the isolation of a new compound from A. anchusa which has significant cytotoxic activity against HepG-2 cell lines with marked antioxidant potential.
Fulltext The impact of PEG-induced drought stress on seed germination and seedling growth of different bread wheat (Triticum aestivum L.) genotypes

Mahpara S, Zainab A, Ullah R, Kausar S, Bilal M, Latif MI, et al.

PLoS One, 2022;17(2):e0262937.
PMID: 35148345 DOI: 10.1371/journal.pone.0262937

Wheat is an important crop, used as staple food in numerous countries around the world. However, wheat productivity is low in the developing world due to several biotic and abiotic stresses, particularly drought stress. Non-availability of drought-tolerant wheat genotypes at different growth stages is the major constraint in improving wheat productivity in the developing world. Therefore, screening/developing drought-tolerant genotypes at different growth stages could improve the productivity of wheat. This study assessed seed germination and seedling growth of eight wheat genotypes under polyethylene glycol (PEG)-induced stress. Two PEG-induced osmotic potentials (i.e., -0.6 and -1.2 MPa) were included in the study along with control (0 MPa). Wheat genotypes included in the study were 'KLR-16', 'B6', 'J10', '716', 'A12', 'Seher', 'KTDH-16', and 'J4'. Data relating to seed germination percentage, root and shoot length, fresh and dry weight of roots and shoot, root/shoot length ratio and chlorophyll content were recorded. The studied parameters were significantly altered by individual and interactive effects of genotypes and PEG-induced osmotic potentials. Seed germination and growth parameters were reduced by osmotic potentials; however, huge differences were noted among genotypes. A reduction of 32.83 to 53.50% was recorded in seed germination, 24.611 to 47.75% in root length, 37.83 to 53.72% in shoot length, and 53.35 to 65.16% in root fresh weight. The genotypes, 'J4', 'KLR-16' and 'KTDH-16', particularly 'J4' better tolerated increasing osmotic potentials compared to the rest of the genotypes included in the study. Principal component analysis segregated these genotypes from the rest of the genotypes included in the study indicated that these can be used in the future studies to improve the drought tolerance of wheat crop. The genotype 'J4' can be used as a breeding material to develop drought resistant wheat genotypes.

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