Pharmaceutical Chemistry Journal最新文献

UV spectrophotometric determination of salicylic acid in several multicomponent drugs using an ethylcellulose-based sorbent for solid-phase extraction (SPE) for sample preparation was shown to be selective. Selective binding of the analyte to sorbent active sites and stepwise elution successively with purified water and NaOH solution (0.1 M) during SPE eliminated interference of other active pharmaceutical ingredients of multicomponent drugs during identification and quantitation of salicylic acid by UV spectrophotometry. Use of the ethylcellulose sorbent made it possible to improve the metrological parameters and decrease systematic error of the quantitative procedure by an average of 47%.

4-(3-Acyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)benzoic acids were synthesized by three- component reactions of acylpyruvic acid methyl esters, aromatic aldehydes, and 4-aminobenzoic acid (PABA). The structures of the compounds were determined using IR, PMR, and ¹³C NMR spectroscopy. Pronounced analgesic activity of the synthesized compounds was revealed. An aroyl substituent in the 3-position of the heterocycle was shown to increase the analgesic activity. All studied compounds were practically nontoxic.

The anti-inflammatory activity of 17 derivatives of 5-N-arylaminocarbonyl-6-aryl-4-methyl-1,2,3,6-tetrahydropyrimidine-2-thiones was studied. The molecular structure of one of them was established. Ten compounds that inhibited the inflammatory reaction in experimental animals in the range 56-81% were identified.

The present study aimed to study the effect of caffeic acid (CA) on diabetic cardiac complications associated with Type-I diabetes mellitus (DM) in rats. Type-I DM in rats was induced by streptozotocin (STZ) injection once only [45 mg/kg, i.v]. The animals were divided into four groups, and treatment was given for 8 weeks with CA [25 mg/kg, PO and 50 mg/kg, PO] in two specified diabetic groups. After 8 weeks, serum and urine were collected and various serum and urine parameters were estimated. Animals were then sacrificed, and their hearts were removed for estimation of histopathological and oxidative parameters. STZ-induced diabetic rats showed significantly decreased albumin levels and increased MDA, collagen, and decreased activates of SOD and glutathione in their diabetic hearts. In the diabetic control, rats showed significantly increased serum cardiac parameters of CK, CRP, and LDH and also increased serum lipid profile parameters of LDL, cholesterol, and TG. Treatment with CA 25 mg/kg and 50 mg/kg showed significantly decreased CK, CRP, and LDH in diabetic-treated rats and decreased UA. Additionally, significantly decreased MDA, collagen, and increased activities of SOD and GSH were seen in the diabetic-treated rats. Histopathological findings also supported the beneficial effect of CA on the left ventricle of the heart. The present study revealed that the beneficial effects of CA on diabetic cardiovascular complications may be via anti-oxidative and anti-inflammatory actions.

Lung cancer is the leading cause of cancer death worldwide and curcumin is a natural polyphenol product with a diversity of antitumor activities. However, its clinical utility is limited due to its relatively low instability and poor bioavailability. This study evaluates the antitumor activity and the underlying mechanism of eight new curcumin analogs in A549 cells. Cell proliferation, migration and apoptosis were examined, respectively, through MTT assay, clone formation, wound healing, transwell, JC-1 staining, Bcl-2 activity, and caspase 3 activity. Protein levels of TGF-βR, MEK, and ERK were determined via western blotting. The binding mode of the ligand and the receptor was simulated by molecular docking studies. Compound A7 was found as the most potent analog (IC₅₀ = 25.78 μM) compared to curcumin (IC₅₀ = 42.30 μM). A7 exposure suppressed A549 cell migration and induced apoptosis with significant differences. Western blot and molecular docking studies demonstrated that the potential mechanism may relate to regulating the TGF-βR/MEK/ERK signaling pathway. Therefore, inhibiting this signaling pathway may provide a potential therapeutic strategy for lung cancer.

Cancer is still one of the greatest threats to human health. Marine fungi are abundant in constituents that can cause various bioactivities for many purposes. Compounds are the basis of drug development, leading to more studies on exploring these bioactive items. In this study, 9 compounds were isolated from Penicillium terrigenum. Four compounds isolated from the Trichocomaceae family, two compounds isolated from the Penicillium genus, as well as the other compounds, were all isolated from this strain for the first time. Compounds PTL-1 - PTL-6 were initially screened for antiproliferative activity on liver and lung cancer cells using the MTT assay in vitro. The results showed that the 6 compounds exhibited different antiproliferative activities. From the results, PTL-2, 7-ethylcamptothecin significantly inhibited the proliferation of cancer cells, highlighting it as a potential drug or lead compound.

The Heckel and Kawakita equations are the most common mathematical models used in modern studies of the pressing process to evaluate the mechanical properties of tablets. However, these classical models do not take into account the whole spectrum of processes occurring during interparticle interaction, which necessitates the development of new approaches to modeling the tableting process. For this reason, a rather large number of direct- pressing models have now been developed. The choice of the optimal equation for each specific case has become a nontrivial problem. Currently used mathematical descriptions of the direct-pressing process were analyzed in the present study.

An HPLC method for the quantitative determination of the rosmarinic acid content in leaves of peppermint (Mentha piperita L.) was developed. The content of the dominant phenylpropanoid rosmarinic acid in leaves of M. piperita varied from 2.01 ± 0.03% to 5.54 ± 0.05%. The error of a single determination of the rosmarinic acid content in M. piperita leaves was ±9.66% at a confidence probability of 95%.

The goal of the current research was to create an easy-to-understand, precise, and affordable UV-spectrophotometric method for measuring pirfenidone in bulk, in commercial formulations, and in nanoparticle form. The stock solution of pirfenidone was made using a phosphate buffer with a pH of 7.4, and the highest absorbance wavelength in the absorption spectrum was then identified. The standard curve was developed by preparing various working standard solutions from the aforementioned solution by dilution with the same diluents. This technique was also validated in accordance with International Council for Harmonization (ICH) guidelines. Pirfenidone showed the maximum absorptivity at 311 nm and the linearity range was found to be 10 – 50 μg/mL (R² = 0.998). The limit of detection (LOD) and limit of quantification (LOQ) were 6.1140 μg/mL and 18.527 μg/mL respectively. The validity of all other parameters was determined to be acceptable. It was decided that the precision and accuracy were satisfactory. The developed processes were validated based on ICH standards. All of the validation parameters were found to be acceptable when compared with the standard values. Therefore, the suggested technique for pirfenidone determination in bulk drug and pharmaceutical formulation assays is applicable to everyday activities. The estimation of pirfenidone in pure form, commercial formulations, and nanoparticles was performed using an easy process that did not involve any potentially dangerous chemicals.

The reaction of p-aminophenol with acetic anhydride under microwave irradiation in the presence of H-clinoptilolite was studied to continue the search for effective, economically favorable, and environmentally friendly methods for synthesizing acetaminophen (paracetamol). The proposed system, which provided a rapid synthesis of the most important drug with a high yield and purity, was demonstrated to be efficient.