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Ali Yousaf,1 Shafida Abd Hamid,1 Noraslinda M Bunnori,1 AA Ishola2 1Kulliyyah of Science, 2Kulliyyah of Medicine, International Islamic University Malaysia, Bandar Indera Mahkota, Malaysia Abstract: Research on the therapeutic applications of calixarene derivatives is an emerging area of interest. The anticancer activity of various functionalized calixarenes has been reported by several research groups. Due to their superior geometric shape, calixarenes can accommodate drug molecules by forming inclusion complexes. Controlled release of anticancer drugs by calixarenes might help in targeted chemotherapy. This review summarizes the anticancer potential of the calixarenes and their drug loading properties. The potential use of calixarenes in chemoradiotherapy is also highlighted in brief. Keywords: cancer, chemotherapy, calixarenes

Currently, Malaysia has substantially increased its reputation as a country developed for palm-based lignocellulosic biomass. Lignocellulosic palm biomass is composed of cellulose, hemicellulose and lignin, as well as other minor components. The presence of highly cellulose content in palm biomass is potentially converted to nanocellulose, which is a promising bio-polymer that useful for various industrial applications, such as personal cares, chemicals, foods, pharmaceuticals and bio-composites. Nanocellulose possesses many advantages, such as nano-scale dimension, high strength and modulus, large surface area, unique optical properties, etc. This amazing characteristic and wide application prospects have attracted significant interest from both research scientists and industrialists. In this study, we will discuss basic chemistry of palm-based biomass, complex structure of lignocellulose and its recalcitrant. Furthermore, comparison study of all chemical pretreatments to unlock the polysaccharide and depolymerisation of palm-based cellulose into nanocellulose will discuss herein. [ABSTRACT FROM AUTHOR]

Cerium and tungsten co-doped TiO2 photocatalyst composite material has been fabricated by using a facile sol-gel method. The composite was coated on ITO film via electrophoretic deposition method. In order to understand the morphology, structure and optical properties, the composite material was characterized with X-ray diffraction, scanning electron microscope, UV-vis and Fourier transform infrared spectroscopy. The results showed a uniformly distributed porous composite film on ITO substrate. Cerium and tungsten as oxides are dispersed on the substrate. A significant photocurrent was developed under solar simulator irradiation and the value was observed higher as compared with pure TiO2 film electrodes. [ABSTRACT FROM AUTHOR]

Background: Patients requiring medications during discharge are at risk of discharge medication errors that potentially cause readmission due to medication-related events. Objective: The objective of this study was to develop interventions to reduce percentage of patients with one or more medication errors during discharge. Methods: A pharmacist-led quality improvement (QI) program over 6 months was conducted in medical wards at a tertiary public hospital. Percentage of patients discharge with one or more medication errors was reviewed in the pre-intervention and four main improvements were developed: increase the ratio of pharmacist to patient, prioritize discharge prescription order within office hours, complete discharge medication reconciliation by ward pharmacist, set up a Centralized Discharge Medication Pre-packing Unit. Percentage of patients with one or more medication errors in both pre- and post-intervention phase were monitored using process control chart. Results: With the implementation of the QI program, the percentage of patients with one or more medication errors during discharge that were corrected by pharmacists significantly increased from 77.6% to 95.9% (p

Enzymatic browning is of concern as it can affect food safety and quality. In this study, an effective and safe tyrosinase inhibitor and anti-browning agent, methyl 4-pyridyl ketone thiosemicarbazone (4-PT), was synthesised and characterised using Fourier-transform infrared (FTIR) spectroscopy, CHNS elemental analysis, and proton ( 1 H) and carbon-13 ( 13 C) nuclear magnetic resonance (NMR) spectroscopy. The vibrational frequencies of 4-PT were studied theoretically using vibrational energy distribution analysis (VEDA). Density functional theory (DFT) was applied to elucidate its chemical properties, including the Mulliken atomic charges, molecular electrostatic potential (MEP), quantum theory of atoms in molecules (QTAIM) and reduced density gradient non-covalent interactions (RDG-NCIs). Moreover, 4-PT was compared with kojic acid in terms of its effectiveness as a tyrosinase inhibitor and anti-browning agent. The toxicity and physicochemical properties of 4-PT were predicted via ADME evaluation, which proved that 4-PT is safer than kojic acid. Experimentally, 4-PT (IC50 = 5.82 μM, browning index (10 days) = 0.292 ± 0.002) was proven to be an effective tyrosinase inhibitor and anti-browning agent compared to kojic acid (IC50 = 128.17 μM, browning index (10 days) = 0.332 ± 0.002). Furthermore, kinetic analyses indicated that the type of tyrosinase inhibition is a mixed inhibition, with K m and V max values of 0.85 mM and 2.78 E-09 μM/s, respectively. Finally, the mechanism of 4-PT for tyrosinase inhibition was proven by 1D, second derivative and 2D IR spectroscopy, molecular docking and molecular dynamic simulation approaches., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Mohammad Norazmi Ahmad reports financial support was provided by Malaysian Ministry of Higher Education. Mohammad Norazmi Ahmad reports financial support was provided by Royal Society of Chemistry., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Antimicrobial drug resistance (AMR) is a severe global threat to public health. The increasing emergence of drug-resistant bacteria requires the discovery of novel antibacterial agents. Quinoline derivatives have previously been reported to exhibit antimalarial, antiviral, antitumor, antiulcer, antioxidant and, most interestingly, antibacterial properties. In this study, we evaluated the binding affinity of three newly designed hydroxyquinolines derived from sulfanilamide ( 1 ), 4-amino benzoic acid ( 2 ) and sulfanilic acid ( 3 ) towards five bacterial protein targets (PDB ID: 1JIJ, 3VOB, 1ZI0, 6F86, 4CJN). The three derivatives were designed considering the amino acid residues identified at the active site of each protein involved in the binding of each co-crystallized ligand and drug-likeness properties. The ligands displayed binding energy values with the target proteins ranging from -2.17 to -8.45 kcal/mol. Compounds ( 1 ) and ( 3 ) showed the best binding scores towards 1ZI0/3VOB and 1JIJ/4CJN, respectively, which may serve as new antibiotic scaffolds. Our in silico results suggest that sulfanilamide ( 1 ) or sulfanilic acid ( 3 ) hydroxyquinoline derivatives have the potential to be developed as bacterial inhibitors, particularly MRSA inhibitors. But before that, it must go through the proper preclinical and clinical trials for further scientific validation. Further experimental studies are warranted to explore the antibacterial potential of these compounds through preclinical and clinical studies.Communicated by Ramaswamy H. Sarma.

In addition to environmental concerns, the presence of microorganisms in plastic food packaging can be hazardous to human health. In this work, cinnamon nanoparticles incorporated with red seaweed ( Kappaphycus alvarezii ) biopolymer films were fabricated using a solvent casting method. Cinnamon was used as a filler to enhance the properties of the films at different concentrations (1, 3, 5, and 7% w / w ) by incorporating it into the matrix network. The physico-chemical, thermal, mechanical, and antimicrobial properties of the cinnamon biopolymer films were obtained using dynamic light scattering (DLS), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transmission infrared spectroscopy (FT-IR), water contact angle (WCA) measurement, thermogravimetric analysis (TGA), mechanical testing, and antimicrobial testing, respectively. The results showed that the addition of cinnamon nanoparticles to the film improved the morphological, mechanical, thermal, wettability, and antibacterial properties of the nanocomposite films. The cinnamon particles were successfully reduced to nano-sized particles with an average diameter between 1 nm and 100 nm. The hydrophobicity of the film increased as the concentration of cinnamon nanoparticles incorporated into the seaweed matrix increased. The tensile and thermal properties of the cinnamon seaweed biopolymer film were significantly improved with the presence of cinnamon nanoparticles. The biopolymer films exhibited good inhibitory activity at 7% cinnamon nanoparticles against Escherichia coli ( E. coli ), Staphylococcus aureus ( S. aureus ), and Salmonella bacteria with inhibition zone diameters of 11.39, 10.27, and 12.46 mm, indicating the effective antimicrobial activity of the biopolymer film. The functional properties of the fabricated biopolymer film were enhanced with the addition of cinnamon nanoparticles.

Tyrosine kinase overexpression could result in an unfavourable consequence of cancer progression in the body. A number of kinase inhibitor drugs targeting various cancer-related protein kinases have been developed and proven successful in clinical therapy. Benzimidazole is one of the most studied scaffolds in the search for effective anticancer drugs. The association of various functional groups and the structural design of the compounds may influence the binding towards the receptor. Despite numerous publications on the design, synthesis and biological assays of benzimidazole derivatives, their inhibitory activities against epidermal growth factor receptor (EGFR), a receptor tyrosine kinase (RTK), have not been specifically analysed. This review covers recent research reports on the anticancer activity of benzimidazole derivatives focusing on EGFR expression cell lines, based on their structure-activity relationship study. We believe it would aid researchers to envision the challenges and explore benzimidazole's potentials as tyrosine kinase inhibitors., (© 2021 John Wiley & Sons A/S.)

Recently, drug delivery systems based on nanoparticles for cancer treatment have become the centre of attention for researchers to design and fabricate drug carriers for anti-cancer drugs due to the lack of tumour-targeting activity in conventional pharmaceuticals. Poly(caprolactone)- b -poly(ethylene glycol) (PCL-PEG)-based micelles have attracted significant attention as a potential drug carrier intended for human use. Since their first discovery, the Food and Drug Administration (FDA)-approved polymers have been studied extensively for various biomedical applications, specifically cancer therapy. The application of PCL-PEG micelles in different cancer therapies has been recorded in countless research studies for their efficacy as drug cargos. However, systematic studies on the effectiveness of PCL-PEG micelles of specific cancers for pharmaceutical applications are still lacking. As breast cancer is reported as the most prevalent cancer worldwide, we aim to systematically review all available literature that has published research findings on the PCL-PEG-based micelles as drug cargo for therapy. We further discussed the preparation method and the anti-tumour efficacy of the micelles. Using a prearranged search string, Scopus and Science Direct were selected as the databases for the systematic searching strategy. Only eight of the 314 articles met the inclusion requirements and were used for data synthesis. From the review, all studies reported the efficiency of PCL-PEG-based micelles, which act as drug cargo for breast cancer therapy.

Patchouli extracts and oils extracted from Pogostemon cablin are essential raw material for the perfume and cosmetics industries, in addition to being used as a natural additive for food flavoring. Steam distillation is a standard method used for plant extraction. However, this method causes thermal degradation of some essential components of the oil. In this study, patchouli was extracted with supercritical carbon dioxide (SC-CO 2 ) under different conditions of pressure (10-30 MPa) and temperature (40-80 °C). The chemical components of the crude extracted oil and the functional group were characterized using gas chromatography-mass spectrometry (GC-MS) and Fourier Transform Infrared Spectroscopy (FT-IR). The extraction with supercritical carbon dioxide was shown to provide a higher yield (12.41%) at a pressure of 20 MPa and a temperature of 80 °C. Patchouli alcohol, Azulene, δ-Guaiene, and Seychellene are the main bioactive compounds that GC-MS results have identified. FTIR spectra showed alcohol, aldehyde, and aromatic ring bond stretching peaks. Extraction of patchouli with supercritical carbon dioxide provided a higher yield and a better quality of the crude patchouli oil., Competing Interests: The authors declare no conflict of interest.

In the past decade, electrospun nanofibers made of biodegradable polymers have been used for different biomedical applications due to their flexible features in terms of surface area to volume ratio, pores, and fiber size, as well as their highly tunable surface properties. Recently, interest is growing in the use of supramolecular structures in combination with electrospun nanofibers for the fabrication of bioactive platforms with improved in vitro responses, to be used for innovative therapeutic treatments. Herein, sulfonatocalix[4]arene (SCX4) was synthesized from p - tert -butyl-calix[4]arene and embedded in electrospun nanofibers made of polycaprolactone (PCL) and gelatin (GEL). The supramolecular structure of SCX4 and its efficient entrapment into electrospun fibers was confirmed by NMR spectroscopy and FTIR analysis, respectively. SEM analysis supported via image analysis enabled the investigation of the fiber morphology at the sub-micrometric scale, showing a drastic reduction in fiber diameters in the presence of SCX4: 267 ± 14 nm (without SCX) to 115 ± 5 nm (3% SCX4). Moreover, it was demonstrated that SCX4 significantly contributes to the hydrophilic properties of the fiber surface, as was confirmed by the reduction in contact angles from 54 ± 1.4° to 31 ± 5.5° as the SCX4 amount increased, while no effects on thermal stability were recognized, as was confirmed by TGA analyses. In vitro tests also confirmed that SCX4 is not cytotoxic, but plays a supporting role in L929 interactions, as was validated by the cell viability of PGC15% after 7 days, with respect to the control. These preliminary but promising data suggest their use for the fabrication of innovative platforms able to bind SCX4 to bioactive compounds and molecules for different therapeutic applications, from molecular recognition to controlled drug delivery.

Targeted drug delivery system improves the efficiency and safety of the therapeutic agents by managing the pharmacokinetics and pharmacodynamics of drugs. Currently, numerous drug carrier systems have been developed with different sizes, architectures and characteristics surface properties. Among different systems, macromolecules have a wide range of applications in targeted drug delivery system. The optimal drug loading potential, smooth drug releasing ability and biocompatibility are the distinguishing features that ensure the drugs delivery ability of macromolecules. This review briefly introduces some of the most commonly studied macromolecules which have been recommended as drugs delivery vehicles.

Calixarene derivatives are reported as potential therapeutic agents. Azo derivatives of calixarenes have not been given much consideration to explore their biomedical applications. In the present study, some azo-based derivatives of calix[4]arene were synthesized and characterized and their antibacterial and antiviral potentials were studied. The mono azo products of sulphanilamide, sulfaguanidine and 2-methyl-4-aminobenzoic acid showed good activity against bacterial strains with minimum inhibition concentration values ranging from 0.97 to 62.5 μg/mL. For mono azo products, the diazotized salt was applied as a limiting reagent. The use of calix[4]arene and sodium acetate trihydrate in 1:3 (molar ratio) helped in partial substitution. Molecular docking was performed to see the interaction of the designed compounds with two bacterial and one viral (neuraminidase) receptor. Some of the derivatives showed good interaction with the active site of bacterial and neuraminidase enzymes through hydrogen, hydrophobic and pi-pi interactions, and could inhibit the activity of the selected enzymes.

Recent outbreaks of highly pathogenic influenza strains have highlighted the need to develop new anti-influenza drugs. Here, we report an in silico study of carvone derivatives to analyze their binding modes with neuraminidase (NA) active sites. Two proposed carvone analogues, CV(A) and CV(B), with 36 designed ligands were predicted to inhibit NA (PDB ID: 3TI6) using molecular docking. The design is based on structural resemblance with the commercial inhibitor, oseltamivir (OTV), ligand polarity, and amino acid residues in the NA active sites. Docking simulations revealed that ligand A18 has the lowest energy binding (∆G bind ) value of -8.30 kcal mol -1 , comparable to OTV with ∆G bind of -8.72 kcal mol -1 . A18 formed seven hydrogen bonds (H-bonds) at residues Arg292, Arg371, Asp151, Trp178, Glu227, and Tyr406, while eight H-bonds were formed by OTV with amino acids Arg118, Arg292, Arg371, Glu119, Asp151, and Arg152. Molecular dynamics (MD) simulation was conducted to compare the stability between ligand A18 and OTV with NA. Our simulation study showed that the A18-NA complex is as stable as the OTV-NA complex during the MD simulation of 50 ns through the analysis of RMSD, RMSF, total energy, hydrogen bonding, and MM/PBSA free energy calculations.

A new naturally occurring dibenzylbutyrolactone lignan named isocubebinic ether has been isolated from Knema patentinervia. The structure was established by spectroscopic methods, which include Ultraviolet, Infrared, Nuclear Magnetic Resonance and Mass Spectrometry. The compound showed activity in the stimulation of glucose uptake by 3T3-L1 adipocytes.

Topoisomerases are nuclear enzymes that regulate topology of DNA by facilitating the temporary cleavage and ligation cycle of DNA. Among all forms of topoisomerases, TOP-IIA is extensively associated with cell proliferation and therefore is an important therapeutic target in diseases that involved cellular proliferation such as cancers. Nearly half of present-day antitumor regimens contain at least one prescription that act as a topoisomerase inhibitor. Generally, tumor cells show divergent expression of TOP-IIA compared to normal cells. The remarkable expression of TOP-IIA in various carcinomas provides a significant biomarker toward understanding the nature of malignancy. TOP-IIA expression and amplification studies help in diagnosing cancer and to observe the disease progression, overall survival (OS) of patients, and response to therapy. This review highlights the research output and analysis in exploring the standing of TOP-IIA in various carcinomas. As some reports show contradiction within the same field of interest, the outline of that may help to induce researchers for further investigation and clarification. To the best of our knowledge, this is the first overview briefly summarizing the prognostic feature of TOP-IIA in various types of cancer.

The lack of stability is a challenge for most heterogeneous catalysts. During operations, the agglomeration of particles may block the active sites of the catalyst, which is believed to contribute to its instability. Recently, titanium oxide (TiO2) was introduced as an alternative support material for heterogeneous catalyst due to the effect of its high surface area stabilizing the catalysts in its mesoporous structure. TiO2 supported metal catalysts have attracted interest due to TiO2 nanoparticles high activity for various reduction and oxidation reactions at low pressures and temperatures. Furthermore, TiO2 was found to be a good metal oxide catalyst support due to the strong metal support interaction, chemical stability, and acid-base property. The aforementioned properties make heterogeneous TiO2 supported catalysts show a high potential in photocatalyst-related applications, electrodes for wet solar cells, synthesis of fine chemicals, and others. This review focuses on TiO2 as a support material for heterogeneous catalysts and its potential applications.

During the process and operation of the dyes, the wastes produced were commonly found to contain organic and inorganic impurities leading to risks in the ecosystem and biodiversity with the resultant impact on the environment. Improper effluent disposal in aqueous ecosystems leads to reduction of sunlight penetration which in turn diminishes photosynthetic activity, resulting in acute toxic effects on the aquatic flora/fauna and dissolved oxygen concentration. Recently, photodegradation of various synthetic dyes has been studied in terms of their absorbance and the reduction of oxygen content by changes in the concentration of the dye. The advantages that make photocatalytic techniques superior to traditional methods are the ability to remove contaminates in the range of ppb, no generation of polycyclic compounds, higher speed, and lower cost. Semiconductor metal oxides, typically TiO2, ZnO, SnO, NiO, Cu2O, Fe3O4, and also CdS have been utilized as photocatalyst for their nontoxic nature, high photosensitivity, wide band gap and high stability. Various process parameters like photocatalyst dose, pH and initial dye concentrations have been varied and highlighted. Research focused on surface modification of semiconductors and mixed oxide semiconductors by doping them with noble metals (Pt, Pd, Au, and Ag) and organic matter (C, N, Cl, and F) showed enhanced dye degradation compared to corresponding native semiconductors. This paper reviews recent advances in heterogeneous photocatalytic decolorization for the removal of synthetic dyes from water and wastewater. Thus, the main core highlighted in this paper is the critical selection of semiconductors for photocatalysis based on the chemical, physical, and selective nature of the poisoning dyes.

An alkaloid from Maclurodendron porteri has been isolated and characterized. Extraction process was conducted by acid-base extraction method followed by column chromatography. The structure was established by nuclear magnetic resonance spectroscopy and mass spectrometry. The compound was identified as haplophytin B which occurs commonly in the Rutaceae family. However, this is the first time this alkaloid was isolated and reported from the species. The compound showed no inhibition against Staphylococus aureus, Pseudomonas aeruginosa, Bacillus cereus and Escherichia coli and no cytotoxic activity against H199 and A549 cell lines.

A new series of N-sec/tert-butyl 2-arylbenzimidazole derivatives was synthesised in 85-96% yields within 2-3.5 min by condensing ethyl 3-amino-4-butylamino benzoate with various substituted metabisulfite adducts of benzaldehyde under focused microwave irradiation. The benzimidazole analogues were characterised using (1)H NMR, (13)C NMR, high resolution MS and melting points. Evaluation of antiproliferative activity of the benzimidazole analogues against MCF-7 and MDA-MB-231 revealed several compounds with unexpected selective inhibitions of MDA-MB-231 in micromolar range. All analogues were found inactive towards MCF-7. The most potent inhibition against MDA-MB-231 human breast cancer cell line came from the unsubstituted 2-phenylbenzimidazole 10a.

A series of novel 1-(2'-α-O-D-glucopyranosyl ethyl) 2-arylbenzimidazoles has been prepared via one-pot glycosylation of ethyl-1-(2'-hydroxyethyl)-2-arylbenzimidazole-5-carboxylate derivatives. Synthesis of the 2-arylbenzimidazole aglycones from 4-fluoro-3-nitrobenzoic acid was accomplished in four high-yielding steps. The reduction and cyclocondensation steps for the aglycone synthesis proceeded efficiently under microwave irradiation to afford the appropriate benzimidazoles in excellent yields within 2-3 min. Glycosylation of the hydroxyethyl aglycones with the perbenzylated 1-hydroxy- glucopyranose, pretreated with the Appel-Lee reagent, followed by catalytic hydrogenolysis delivered the desired 1-(2'-α-O-D-glucopyranosyl ethyl) 2-aryl-benzimidazoles in a simple and straightforward manner.

A test for assessing pork adulteration in meatballs, using TaqMan probe real-time polymerase chain reaction, was developed. The assay combined porcine-specific primers and TaqMan probe for the detection of a 109 bp fragment of porcine cytochrome b gene. Specificity test with 10 ng DNA of eleven different species yielded a threshold cycle (Ct) of 15.5 ± 0.20 for the pork and negative results for the others. Analysis of beef meatballs with spiked pork showed the assay can determine 100-0.01% contaminated pork with 102% PCR efficiency, high linear regression (r(2) = 0.994) and ≤ 6% relative errors. Residuals analysis revealed a high precision in all determinations. Random analysis of commercial meatballs from pork, beef, chicken, mutton and goat, yielded a Ct between 15.89 ± 0.16 and 16.37 ± 0.22 from pork meatballs and negative results from the others, showing the suitability of the assay to determine pork in commercial meatballs with a high accuracy and precision., (Copyright © 2012 Elsevier Ltd. All rights reserved.)