Spectral analysis and Antibacterial activity of the bioactive principles of Sargassum tenerrimum J. Agardh collected from the Red sea, Jazan, Kingdom of Saudi Arabia

Seaweeds are a major marine resource that can be explored to develop novel pharmaceutical molecules. The present study showed the presence of unique bioactive components in the petroleum ether extract (PEE) and methanolic extract (ME) of Sargassum tenerrimum. The gas chromatography-mass spectrometry analysis suggested that the PEE of S. tenerrimum contained antibacterial biomolecules: hexadecanoic acid, methyl ester, 17-pentatriacontene, dasycarpidan-1-methanol, and acetate (ester). However, the ME of S. tenerrimum exhibited better antibacterial effect than the PEE due to the presence of the bioactive compounds 1,2-benzenedicarboxylic acid, diisooctyl ester, tetratetracontane, 1-docosene, 1,2-benzenediol, and benzoic acid. Thus, promising antibacterial molecules can be isolated from S. tenerrimum for better therapeutic use.

Nutraceutical and Functional Foods in Treatment of Anemia

WHO database mentions that the global anemia-affected population is 24.8%. To name a few conditions in which compromisation of the red blood corpuscles and hemoglobin occurs are iron deficiency anemia, gestational anemia, anemia due to malaria and parasitism, hemolytic anemia, sickle cell anemia. The line of treatment in case of anemia involves administration of iron supplements, plasmapheresis, steroids, blood transfusion at regular intervals, and lifestyle changes. The systematic approach applied for the pharmaceutical molecules should be equally inculcated in the case of nutraceuticals. The traditional system when woven carefully with the novel drug delivery system will give effective nutrient delivery. Functional foods have inherent nutritional value. Nutraceuticals and functional food cannot cure the anemic condition, but help the patient lead life almost like a normal individual.

Tween® Preserves Enzyme Activity and Stability in PLGA Nanoparticles

Enzymes, as natural and potentially long-term treatment options, have become one of the most sought-after pharmaceutical molecules to be delivered with nanoparticles (NPs); however, their instability during formulation often leads to underwhelming results. Various molecules, including the Tween® polysorbate series, have demonstrated enzyme activity protection but are often used uncontrolled without optimization. Here, poly(lactic-co-glycolic) acid (PLGA) NPs loaded with β-glucosidase (β-Glu) solutions containing Tween® 20, 60, or 80 were compared. Mixing the enzyme with Tween® pre-formulation had no effect on particle size or physical characteristics, but increased the amount of enzyme loaded. More importantly, NPs made with Tween® 20:enzyme solutions maintained significantly higher enzyme activity. Therefore, Tween® 20:enzyme solutions ranging from 60:1 to 2419:1 mol:mol were further analyzed. Isothermal titration calorimetry analysis demonstrated low affinity and unquantifiable binding between Tween® 20 and β-Glu. Incorporating these solutions in NPs showed no effect on size, zeta potential, or morphology. The amount of enzyme and Tween® 20 in the NPs was constant for all samples, but a trend towards higher activity with higher molar rapports of Tween® 20:β-Glu was observed. Finally, a burst release from NPs in the first hour with Tween®:β-Glu solutions was the same as free enzyme, but the enzyme remained active longer in solution. These results highlight the importance of stabilizers during NP formulation and how optimizing their use to stabilize an enzyme can help researchers design more efficient and effective enzyme loaded NPs.

Microwave-Assisted, One-Pot Synthesis of Doxycycline under Heterogeneous Catalysis in Water

The selective synthesis of active pharmaceutical molecules is a challenging issue, particularly when attempting to make the reactions even more sustainable. The present work focuses on the microwave-assisted hydrogenolysis of oxytetracycline to selectively produce α-doxycycline. Although the combination of microwave irradiation and a heterogeneous rhodium catalyst provided good conversions, the selective synthesis of active α-doxycycline was only achieved when an oxytetracycline-cyclodextrin complex was used as the starting material, giving the desired product at 34.0% yield in a one-step reaction under very mild conditions.

Echinocandins accelerate the particle transport velocity in the murine tracheal epithelium: dependency on intracellular Ca 2+ stores

The mucociliary clearance of lower airways is modulated by different physiologic stimuli and also by pathophysiologic agents like polluting substances or pharmaceutical molecules. In the present investigation, we measured the particle transport velocity (the PTV) of mouse tracheae as a surrogate for mucociliary clearance. In mouse tracheal preparations, we detected a sustained increase in the PTV under the application of the echinocandins caspofungin, anidulafungin, and micafungin. In further experiments we observed the effects of echinocandins on the PTV were dependent on intracellular Ca 2+ homeostasis. In Ca 2+ -free buffer solutions, the amplitude of the echinocandin-evoked rise in the PTV was significantly reduced relative to in the experiments in Ca 2+ -containing solutions. Depletion of intracellular Ca 2+ stores of the endoplasmic reticulum (ER) by caffeine completely prevented an increase in the PTV with subsequent caspofungin applications. Mitochondrial Ca 2+ stores seemed to be unaffected by echinocandin treatment. We also observed no altered generation of reactive oxygen species under the application of echinocandins as probable mediators of the PTV. Consequently, the observed echinocandin effects on the PTV depend upon the Ca 2+ influx and Ca 2+ contents of the ER. We assume that all three echinocandins may act intracellularly on ER Ca 2+ stores to activate Ca 2+ -dependent signal-transduction cascades, enhancing the PTV.

Phosphorus coordinated Rh single-atom sites on nanodiamond as highly regioselective catalyst for hydroformylation of olefins

Single-atom Rh catalysts present superior activity relative to homogeneous catalyst in olefins hydroformylation, yet with limited success in regioselectivity control. In the present work, we develop a phosphorus coordinated Rh1 single-atom catalyst with nanodiamond as support. Benefiting from this unique structure, the catalyst exhibits excellent activity and regioselectivity in hydroformylation of arylethylenes with wide substrate generality, i.e., with high conversion (>99%) and high regioselectivity (>90%), which is comparable with the homogeneous counterparts. The coordination interaction between Rh1 and surface phosphorus species is clarified by 31P solid-state NMR and X-ray absorption spectroscopy (XAS). Rh single atoms are firmly anchored over nanodiamond through Rh-P bonds, guaranteeing good stability in the hydroformation of styrene even after six runs. Finally, by using this catalyst, two kinds of pharmaceutical molecules, Ibuprofen and Fendiline, are synthesized efficiently with high yields, demonstrating a new prospect of single-atom catalyst in pharmaceutical synthesis.

Sorption of Pharmaceuticals in Aqueous Solution Using Insoluble β-Cyclodextrin Polymers

The present study was aimed at evaluating the ability of insoluble β-cyclodextrin polymers (βCDps) to recover pharmaceuticals from aqueous solutions. Two different β-cyclodextrin polymers, one composed of epichlorohydrin-cross linked β-cyclodextrin and the other a β-cyclodextrin-polyurethane, were prepared by condensation polymerization and addition polymerization of βCD using epichlorohydrin (EP) and diisocyanatohexane (HDI) as cross linking agents, respectively. The contaminants tested were naphthalene, naproxen, nabumetone, 2-naphthol, pyrene and propranolol which represent model pharmaceutical molecules. The adsorption isotherms of the organics and βCDPs were well described by Freundlich isotherm equations. The trapping efficiencies were determined using fluorescence spectroscopy as the analytical technique. Based on the results of this study, it was found that the epichlorohydrin-cross linked β-cyclodextrin polymers were more efficient in adsorption of organic contaminants both in batch and column systems when compared with β-cyclodextrin-polyurethane polymers. Reasons for these differences are discussed.

Sorption of Pharmaceuticals in Aqueous Solution Using Insoluble β-Cyclodextrin Polymers

The present study was aimed at evaluating the ability of insoluble β-cyclodextrin polymers (βCDps) to recover pharmaceuticals from aqueous solutions. Two different β-cyclodextrin polymers, one composed of epichlorohydrin-cross linked β-cyclodextrin and the other a β-cyclodextrin-polyurethane, were prepared by condensation polymerization and addition polymerization of βCD using epichlorohydrin (EP) and diisocyanatohexane (HDI) as cross linking agents, respectively. The contaminants tested were naphthalene, naproxen, nabumetone, 2-naphthol, pyrene and propranolol which represent model pharmaceutical molecules. The adsorption isotherms of the organics and βCDPs were well described by Freundlich isotherm equations. The trapping efficiencies were determined using fluorescence spectroscopy as the analytical technique. Based on the results of this study, it was found that the epichlorohydrin-cross linked β-cyclodextrin polymers were more efficient in adsorption of organic contaminants both in batch and column systems when compared with β-cyclodextrin-polyurethane polymers. Reasons for these differences are discussed.