Bioprospecting for antituberculosis natural products – A review

There has been an increase in the reported cases of tuberculosis, a disease caused by Mycobacterium tuberculosis, which is still currently affecting most of the world’s population, especially in resource-limited countries. The search for novel antitubercular chemotherapeutics from underexplored natural sources is therefore of paramount importance. The renewed interest in studies related to natural products, driven partly by the growing incidence of MDR-TB, has increased the prospects of discovering new antitubercular drug leads. This is because most of the currently available chemotherapeutics such as rifampicin and capreomycin used in the treatment of TB were derived from natural products, which are proven to be an abundant source of novel drugs used to treat many diseases. To meet the global need for novel antibiotics from natural sources, various strategies for high-throughput screening have been designed and implemented. This review highlights the current antitubercular drug discovery strategies from natural sources.

Presence of short and cyclic peptides in Acacia and Ziziphus honeys may potentiate their medicinal values

Acacia honey is characterized by high nutritional, antioxidant, antibacterial and immuno-modulatory values. This work investigated the presence of short and cyclic peptides in Acacia and Ziziphus honey samples. Acacia honey samples (Acacia tortilis and Acacia hamulosa) and three Ziziphus honeys (Ziziphus spina-christi) were screened for their short and cyclic peptide contents using the LC-MS and the chemical structure databases. Moreover, the total protein content was determined using the Bradford method. The A. tortilis honey contained three short peptides; HWCC, DSST, and ECH, and the A. hamulosa honey sample contained five short peptides and one cyclic peptide. The short peptides of the A. hamulosa honey were Ac-GMGHG-OH (Ac-MGGHG-OH), Boc-R(Aloc)2-C(Pal)-OH, H-C (1)-NEt2·H-C (1)-NEt2, APAP (AAPP), and GAFQ (deamino-2-pyrid-4-yl-glycyl-dl-alanyl-dl-norvalyl-dl-asparagine). The cyclic peptide of the A. hamulosa honey was cyclo[Aad-RGD-d-F] (cyclo[Aad-Arg-Gly-Asp-d-Phe]). The Ziziphus honey was characterized by the presence of either Almiramide B or Auristatin-6-AQ. A. tortilis, A. hamulosa, and Ziziphus honeys are characterized by the presence of short and cyclic peptides which may contribute to their medicinal values.

Electrochemical determination of atenolol and propranolol using a carbon paste sensor modified with natural ilmenite

In this study, a simple voltammetric method was reported for independent determination of propranolol (PROP) and atenolol (ATN) in pharmaceutical tablets using carbon paste electrode modified with natural Ilmenite (CPE-I). The analytical performance of the modified sensor was evaluated using the square wave voltammetry and cyclic voltammetry for determination of both β(beta) blockers in 0.1 mol L−1 of sulfuric acid solution (H2SO4). The signal obtained with modified carbon paste electrode in 0.1 mol L−1 of H2SO4 showed a good electrocatalytic activity toward the oxidations of PROP and ATN compared with the bare one. The enhanced oxidation peak current response can be attributed to the catalytic effect of the ilmenite nanomaterial incorporated into the carbon paste electrode. Under optimal condition, good linear calibration curves were obtained ranging from 0.20 to 8.9 mmol L−1 for PROP and 2.0 to 9.9 µmol L−1 for ATN, with detection limits of 80 and 0.31 µmol L−1, respectively. The CPE-I sensor had good repeatability and reproducibility (RSD ≤ 3.2%) and high sensitivity for the detection of both ATN and PROP. The proposed sensor was applied for detection of these drugs in pharmaceutical tablets. The obtained results indicate that the voltammetric CPE-I sensor could be an alternative method for the routine quality control of the β blockers in complex matrices.

The structural chemistry of zinc(ii) and nickel(ii) dithiocarbamate complexes

Dithiocarbamate complexes are of immense interest due to their diverse structural properties and extensive application in various areas. They possess two sulfur atoms that often act as the binding sites for metal coordination in a monodentate, bidentate, or anisodentate fashion. These different coordination modes enhance the possibility for complex formation and make them useful in different areas especially in biomedical fields. A synergy exists in the metal ions and dithiocarbamate moieties, which tends to exert better properties than the respective individual components of the complex. These improved properties have also been attributed to the presence of the C–S bonds. Zinc and nickel ions have been majorly found to bind to the dithiocarbamate in bidentate modes, and consequently different geometries have resulted from this interaction. The aim of this review is to present some studies on the synthesis, structural chemistry, and the relevance of zinc and nickel dithiocarbamates complexes especially in biological systems.

Dynamics of λ-cyhalothrin disappearance and expression of selected P450 genes in bees depending on the ambient temperature

Temperature has a significant influence on the action of pyrethroids, and their effect increases with decreasing ambient temperature. Using gas chromatography, we assessed the degradation rate of λ-cyhalothrin, active ingredients (AI) of Karate Zeon 050 CS from pyrethroid group, in bees incubated for 48 h under different temperature conditions. With RT-qPCR method, we studied expression levels of selected cytochrome P450 genes after exposure to the plant protection product (PPP). The half-life of λ-cyhalothrin decreased from 43.32 to 17.33 h in the temperature range of 21–31°C. In animals incubated at 16°C, the AI half-life was even shorter and amounted to 10.19 h. The increase in temperature increased the expression of Cyp9Q1, Cyp9Q2, and Cyp9Q3 in the group of control bees. We showed a two-fold statistically significant increase in gene expression after treatment with PPP bees. The obtained results indicate that honey bees are characterized by susceptibility to pyrethroids that vary depending on the ambient temperature. This may be due to the different expressions of genes responsible for the detoxification of these PPPs at different temperatures.

Influence of mica mineral on flame retardancy and mechanical properties of intumescent flame retardant polypropylene composites

In many plastic applications, improvement of the flame retardancy is a very significant topic. Polypropylene (PP) is used in many applications such as housing industry due to its cost performance efficiency. Enhancement of flame retardancy properties of PP is necessary in many applications. In this study, the investigation focuses on the synergistic effect of mica mineral and IFR in enhancing the flame retardancy properties of PP in order to achieve cost competitive solution, so as to provide that different/various ratios of IFR and mica mineral were added into PP to compose 30 wt% of the total mass of the polymeric compounds. The synergistic effect of mica mineral with IFR in PP was investigated by limiting oxygen index (LOI), glow wire test (GWT), UL-94 test, thermal gravimetric analyses (TGA), and mechanical tests. The results from LOI, UL 94, and GWT tests indicated that mica added to PP/IFR compound has a synergistic flame retardancy effects with the IFR system. When the content of mica was 6 wt%, LOI value of PP compound reaches to 34.9% and becomes V-0 rating (3.2 mm) in UL 94 flammability tests and compounds pass GWT tests both at 750 and 850°C.

Effect of synthesis and activation methods on the character of CoMo/ultrastable Y-zeolite catalysts

The properties of three types of CoMo/USY catalysts with different synthesized methods have been studied. The sequential and co-impregnation methods followed by activation using calcination and reduction process have been conducted. The properties of the catalysts were examined using Fourier-transform-infrared (FTIR) spectroscopy, X-ray diffraction (XRD) with refinement, and surface area analyzer (SAA). The FTIR spectrum study revealed the enhanced intensity of its Bronsted acid site, and the XRD diffractogram pattern verified the composition of pure metals, oxides, and alloys in the catalyst. The SAA demonstrated the mesoporous features of the catalyst. Scanning electron microscopy showed an irregular particle morphology. Additional analysis using the transmission electron microscopy indicated that the metal has successfully impregnated without damaging the USY structure.

Qualitative and semi-quantitative assessment of anthocyanins in Tibetan hulless barley from different geographical locations by UPLC-QTOF-MS and their antioxidant capacities

Tibetan hulless barley (“qingke” in Chinese) is a valuable food in Tibet. Purple qingke (PQK) and black qingke (BQK), two special pigmented types of hulless barley, have traditionally been widely cultivated and consumed in Tibet for thousands of years. The composition and contents of anthocyanins of two cultivars are unknown. This study aimed to explore the composition and contents of anthocyanins of two cultivars and their antioxidant capacities. Six anthocyanins were identified by ultra-performance liquid chromatography-quadrupole-time of flight mass spectrometry from barley, most of the anthocyanins were acylated by malonyl group. The total anthocyanin contents ranged from 141 to 2,304 μg/g in PQK and from 248.7 to 2902.9 μg/g in BQK. Furthermore, qingke has strong antioxidant activity against DPPH, ABTS˙+, and FRAP. Qingke may be useful for treating or preventing diseases caused by the overproduction of radicals.

Utilization and simulation of innovative new binuclear Co(ii), Ni(ii), Cu(ii), and Zn(ii) diimine Schiff base complexes in sterilization and coronavirus resistance (Covid-19)

This article aimed at the synthesis and molecular docking assessment of new diimine Schiff base ligand, namely 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxyvinyl)hydrazono) methyl)-6-methoxyphenol (methoxy-diim), via the condensation of 1-(4-chloro-phenyl)-2-hydrazino-ethenol compound with 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxy vinyl) hydrazono)methyl)-6-methoxyphenol in acetic acid as well as the preparation of new binuclear complexes of Co(ii), Ni(ii), Cu(ii), and Zn(ii). The following synthesized complexes were prepared in a ratio of 2:1 (metal/ligand). The 1H-NMR, UV-Vis, and FTIR spectroscopic data; molar conductivity measurements; and microanalytical, XRD, TGA/DTG, and biological studies were carried out to determine the molecular structure of these complexes. According to the spectroscopic analysis, the two central metal ions were coordinated with the diamine ligand via the nitrogen of the hydrazine and oxygen of the hydroxyl groups for the first metal ions and via the nitrogen of the hydrazine and oxygen of the phenol group for the second metal ions. Molecular docking for the free ligand was carried out against the breast cancer 3hb5-oxidoreductase and the 4o1v-protein binding kidney cancer and COVID-19 protease, and good results were obtained.

Full spectrum and genetic algorithm-selected spectrum-based chemometric methods for simultaneous determination of azilsartan medoxomil, chlorthalidone, and azilsartan: Development, validation, and application on commercial dosage form

Five various chemometric methods were established for the simultaneous determination of azilsartan medoxomil (AZM) and chlorthalidone in the presence of azilsartan which is the core impurity of AZM. The full spectrum-based chemometric techniques, namely partial least squares (PLS), principal component regression, and artificial neural networks (ANN), were among the applied methods. Besides, the ANN and PLS were the other two methods that were extended by genetic algorithm procedure (GA-PLS and GA-ANN) as a wavelength selection procedure. The models were developed by applying a multilevel multifactor experimental design. The predictive power of the suggested models was evaluated through a validation set containing nine mixtures with different ratios of the three analytes. For the analysis of Edarbyclor® tablets, all the proposed procedures were applied and the best results were achieved in the case of ANN, GA-ANN, and GA-PLS methods. The findings of the three methods were revealed as the quantitative tool for the analysis of the three components without any intrusion from the co-formulated excipient and without prior separation procedures. Moreover, the GA impact on strengthening the predictive power of ANN- and PLS-based models was also highlighted.