Pharmaceutical Chemistry Journal最新文献

The current study highlights the systematic quality by design-assisted creation of an efficient analytical technique for the estimation of embelin and vilangin in Vidanga (Embelia ribes) tablets. Response surface methodology in the design of experiments was used to identify key material attributes and critical process parameters that influence the designated critical analytical attributes. Separation was achieved on the X-Bridge (100 × 2.1 mm, 2 μm). The effects of acetonitrile content (v/v), flow rate, and column temperature on the retention times of the two drugs and their resolution, number of theoretical plates, and tailing factor were investigated and optimized. The optimal chromatographic conditions within the design space were found to be an isocratic mobile phase consisting of buffer and methanol (57.77:42.33, v/v) with a flow rate of 0.2 mL/min and a run time of 3 min. The retention times of embelin and vilangin were found to be 1.31- and 1.7-min. Different validation parameters were established, and the approach was validated in agreement with ICH and FDA requirements. Data analysis using statistical methods has revealed that the method is reliable, accurate, and robust.

Cryptotanshinone (CPT), which is an important active ingredient of herbs, has shown great value for research. In particular, CPT exerts antitumor effects on various types of cancer; however, there are relatively few studies of CPT on gastric cancer cells. The objectives of this study were to investigate how CPT affects apoptosis in 5-fluorouracil-resistant SGC-7901 gastric cancer cells (SGC-7901/5-FU cells) and the molecular mechanism underlying its action. In this study, SGC-7901/5-FU cells were treated with 5-fluorouracil (5-FU) and CPT and the viability of the cells was assessed by CCK8 assay. Additionally, cellular apoptosis rates were evaluated using immunofluorescence and flow cytometry. Related gene expression was evaluated using Quantitative Real-time PCR methods and Western Blot, respectively. CPT inhibited SGC-7901/5-FU cell growth. The immunofluorescence results showed that CPT caused nuclear shrinkage in the cells. Quantitative Real-time PCR and Western Blot results also showed CPT decreased the expression of Mcl-1, Bcl-xl and Bcl-2 levels, and increased the expression of Bax. We demonstrated that CPT can inhibit the growth of SGC-7901/5-FU cells, and the mechanism may be related to the inhibition of the JAK2/STAT3 pathway. Additionally, CPT increased the inhibitory effect of 5-fluorouracil on SGC-7901/5-FU cells, an effect that correlated with changes in cellular resistance.

The world faces a grave threat from antimicrobial resistance. Currently, many bacterial and fungal infections cannot be treated with the majority of well-known antibiotics. Biosynthesized silver nanoparticles (AgNPs) were achieved by a novel, simple green chemistry procedure to counter microbial familiarity using Taraxacum officinale aqueous extract as a reducing agent. The current study was carried out to explore the efficacy of AgNPs by aqueous extract of Taraxacum officinale followed by physicochemical characterization including ultraviolet-visible spectrophotometry (UV-Vis), scanning electron microscopy (SEM), transmission electron microscopy (TEM), x-ray diffractometer (XRD), and Fourier-transform infrared spectroscopy (FTIR). Antibacterial and antifungal activities of the aqueous extracts AgNPs were assessed using the seeding technique and the tube diluton technique respectively. The UV-Vis distinctive spectral peak was observed at 445 nm. SEM showed a particle size range of 100 nm at 30,000 × magnification whereas TEM showed the spherical shape (100 nm) of nanoparticles. XRD confirmed the crystalline structure of the AgNPs, whereas FTIR validated the phytochemicals in their capping, stabilization, and synthesis of AgNPs. Antibacterial assay of synthesized NPs showed significant action against Escherichia coli, Staphylococcus aureus, and Klebsiella pneumoniae. Similarly, the antifungal activity of synthesized AgNPs showed significant action against Aspergillus flavus, Aspergillus niger, Alternaria alternata, and Fusarium oxysporum. These results suggest that the aqueous extract AgNPs of T. officinale could provide a safer alternative to conventional antibacterial and antifungal agents.

Platelet activating factor (PAF) is a potent lipid mediator involved in inflammation, among other pathophysiological conditions. Bioactive compounds from foods have been suggested to suppress inflammation as well as regulate PAF biosynthesis. Phenolics, such as resveratrol and tyrosol, and their acetylated derivatives, inhibited PAF biosynthetic enzymes’ activity, namely acetyl-coenzyme A: lyso–platelet-activating factor acetyltransferases (lysoPAF-AT), and 1-alkyl-2-acetyl-sn-glycerol cholinephosphotransferase (PAF-CPT) under inflammatory stimuli. This study investigates whether resveratrol and tyrosol lipophilic derivatives are capable of affecting the activity of the two isoforms of lysoPAF-AT along with the activity of PAF-CPT compared with the initial compounds under basal conditions. The derivatives were chemically synthesized and the experiments were conducted either with or without pre-incubation of homogenized U-937 cells and the phenolics and the enzyme activities were determined. Pre-incubation experiments resulted in lower half inhibitory concentration (IC₅₀) than those without pre-incubation, reaching a 5-fold difference between them. Moreover, there were differences among parent compounds and their derivatives, suggesting a dependence on the differently substituted groups of the phenolics. PAF-CPT tends to be less phenolic structure dependent than lysoPAF-ATC, whereas the other isoform, lysoPAF-ATE, was less sensitive in general. Resveratrol and its derivatives were more potent than the tyrosolic compounds, regardless of the enzyme test or the conditions of the experiment. The use of phenolic lipophilic derivatives in pharmaceuticals and in food preparation may overcome the limitations of natural phenolics with regard to their weak solubility and stability in a lipophilic environment.

Iberis amara L. belongs to the family of Brassicaceae, which is native to Southern Europe. It is a bloomer cultivated as an ornamental and medicinal plant. Iberis amara has pharmacological effects such as antioxidant, anti-insect, anti-inflammatory, anti-microbial, antiallergic, and anti-cancer effects. This plant is rich in essential oil, fatty oil, amines, glucosinolates, cucurbitacins, and flavonoids. Botanical description, medicine uses, the chemical compositions, and biological activities of Iberis amara are summarized in the present review. Iberis amara is an available and promising medicinal plant for pharmaceutical industries. The purpose of this review is to systematically describe the botanical characteristics, the chemical compositions, and biological activities of Iberis amara, hereby providing a scientific basis for the development of this plant in pharmaceutical applications.

5-Hydroxy-6-methyluracil (5-OH-6-MU) was shown to form a 1:1 complex with N-acetylcysteine (N-AC), i.e., the compounds interacted in an equimolar ratio. The temperature dependence of the stability constant was studied in the range 291-316 K. The thermodynamic parameters of the complexation process were determined. Aprocedure for the synthesis of the 5-OH-6-MU…N-AC complex was developed based on the results. The toxicity and antihypoxic activity of the complex were subsequently studied. The synthesized compound at a dose of 500 mg/kg in mice had low toxicity and antihypoxic activity significantly superior to those of the reference drugs (5-OH-6-MU and N-AC).

Fatigue is a physiological phenomenon experienced by the human body when it undergoes prolonged physical and mental exertion, which can have detrimental effects on both health and work productivity. Previous research has demonstrated that arctigenin (ArcG) has the ability to enhance the physical performance of mice during exercise. In this study, five ArcG derivatives containing different dipeptides coupled via an ethoxy linker were synthesized and tested for their activities to improve exercise performance in mice. All of the derivatives extended the exhaustion distance of mice in the running wheel test. Derivative Z-B-4 exhibited the highest activity, showing that the mice ran a distance 1.3-fold greater than that of the ArcG group and 3.4-fold greater than that of the sport control group. Furthermore, Z-B-4 was found to increase the concentrations of superoxide dismutase (SOD) and catalase (CAT), while simultaneously decreasing levels of lactic acid (LA) and blood urea nitrogen (BUN) during exercise. This study provides new references and promising lead compounds for the development of antifatigue agents.

The purpose of this work is to investigate the physical stability of a ternary amorphous system (Ibuprofen, Caffeine, Polyvinylpyrrolidone (PVP K30)) generated by co-milling technique at room temperature, as well as the intermolecular interactions that could contribute to physical stabilization of amorphous ibuprofen (a poorly water-soluble drug). The milled mixtures were characterized by x-ray diffraction (XRD), infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electronic microscopy (SEM). As shown by XRD results, amorphous Ibuprofen maintains its physical stability even after exposure to high humidity levels (RH = 75%, T = 40°C) for 6 months. FTIR results highlighted the establishment of hydrogen bonds in the binary and ternary systems involving the carboxylic group of Ibuprofen. At higher amounts (more than 75%), the polyvinylpyrrolidone has totally amorphized drug/caffeine mixtures and inhibited polymorphic transition of Caffeine (Form II ≥ Form I) which occurred at higher temperatures. Thus, this polymer has shown an ability to stabilize amorphous solid dispersion (Ibuprofen: Caffeine) and preserve the chemical structure of each molecule.

A comparative study of reagents obtained from hemolymph of Atlantic and Asian horseshoe crabs proved the reliability of bacterial endotoxin determination. It is noted that the enzymatic activity of amebocyte lysate may differ in relation to standard endotoxin and natural endotoxin.

We aimed to investigate the underlying function and mechanism of E1231 against diabetic cardiomyopathy (DCM). H9c2 cells were exposed to either 33 mmol/L mannitol or an identical concentration of glucose (high glucose, HG) in vitro. In vivo, diabetes mellitus (DM) mice were induced by injection of 60 mg/kg streptozotocin intraperitoneally. E1231 was used to treat cells (5 mmol/L) or animals (40 mg/kg), and subsequent assays were conducted to determine its effect on DCM-associated manifestations. Western blot was employed to evaluate protein expressions of the silent information regulator 1 (SIRT1), peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α), and nuclear factor erythroid 2-related factor 2 (Nrf2). In vitro, treatment with E1231 significantly reduced oxidative stress and apoptosis induced by HG via activating the SIRT1-PGC-1α/Nrf2 pathway in H9c2 cells, compared to cardiomyocytes under HG conditions. In vivo, DM mice showed up-regulated SIRT1, PGC-1α, and Nrf2 expression, with protection against cardiac fibrosis, dysfunction, and oxidative stress impairment. The study demonstrated that E1231 alleviates cardiac dysfunction via activating the SIRT1-PGC-1α signaling pathway in DCM, leading to the activation of Nrf2. Therefore, E1231 has the potential to facilitate the treatment of DCM.