Current Bioactive Compounds - Volume 21, Issue 3, 2025

A 9-aminoacridine derivative has anticancer properties against several types of cancer cells, including colon, breast, pancreatic, lung, and renal cell carcinoma. It triggers apoptosis by stopping the cell cycle in the S phase and inhibits the activity of topoisomerase. So, the present study deals with the synthesis and anti-cancer activity of some of the acridine derivatives.

The novel set of N-(acridin-9-yl)-N-(2-substituted benzoyl) derivatives were synthesized, and these compounds were subjected to docking studies against topoisomerase II and the result of docking studies revealed that all the compounds possessed promising activity against the targeted enzyme. The docking studies revealed that the derivative AB7 showed a good docking score of -8.7 kcal/mol when compared to doxorubicin.

The following derivatives AA2, AA3, AB3, AB7, AB7, AF6, AF10, AP7, AP10, and APZ7 were selected for the synthesis by conventional method and further studies. These compounds weresubjected to an in-vitro cytotoxicity study using the MTT assay method with MCF-7 cell lines. Among the tested compounds, derivative APZ7 substituted with chlorobenzene and pyrrole ring showed a significant IC50 value (46.402 μg/ml), and the compound AP10 substituted with chlorobenzene and pyridine moiety (59.42 μg/ml) exhibited promising inhibition in breast cancer cell line.

The current study suggests that the most effective anticancer compounds are found in the substituted acridine derivative.

Various Mentha species are cultivated all over the world due to their aroma and valuable therapeutic constituents. Along with its traditional use as a food flavor, it is well-established folklore medicine for treating digestive and cardiovascular problems. Mentha spicata L. is a perennial, aromatic herb belonging to the Lamiaceae family. M. spicata leaves have been used in traditional systems of medicines for treating various digestive system disorders since old times.

The present research work encompasses the pharmacognostic study, phytochemical screening and physicochemical parameter estimation of leaves and stem of M. spicata L. for standardization of Mentha plant.

Morpho-anatomical characterization, physicochemical analysis and preliminary phytochemical investigation of leaves and stems were performed. These investigations were done as per WHO guidelines to determine the main diagnostic characteristics for correct identification and standardization of whole plant and powdered drug of M. spicata L.

The dimensions, size, color, and surface texture characteristics of fresh crude drug (leaf and stem) were determined. Compound microscope images of the transverse section (TS) of M. spicata leaf and stem revealed the cellular arrangement and main identification characters. Phytochemical and physicochemical analysis of powdered drugs confirmed the presence of important phytoconstituents such as phytosterol, terpeneoids, phenolic compounds, saponins, volatile oil, etc.

The results obtained are helpful for the characterization of the crude drug. Morpho-anatomical characterization and physicochemical analysis are inexpensive methods and serve as a quality control tool for stem and leaf standardization. The ethanolic and aqueous extract of leaves and stem showed the presence of valuable medicinally active phytoconstituents.

Glycerolates of biogenic elements are of interest because of their pharmacological activity. Some of them are used as active substances in agents for topical application and as biocompatible precursors in sol-gel synthesis of bioactive materials.

In this work, morphostructural feature, ability to hydrolyze, and the pharmacological activity of previously synthesized iron(III) monoglycerolate were studied.

Analytical techniques, including SEM, TEM, XRD, TGA, IR spectroscopy, DLS and ELS, were used. Hemostatic activity was studied in vivo, and primary toxicological studies were carried out on experimental animals. Antimicrobial activity was studied using the agar diffusion method.

When dispersed in glycerol, solid crystalline iron(III) monoglycerolate transforms into an amorphous state, forming aggregates with an average particle size of 250 nm (according to DLS data). It slowly hydrolyzes in water at room temperature, while hydrolysis does not take place in an aqueous glycerol media. Iron(III) monoglycerolate is nontoxic and exhibits pronounced hemostatic activity and low antibacterial activity (relative to the strain S. аureus).

Iron(III) monoglycerolate can be considered a potential hemostatic agent, showing promise for topical application in medical and veterinary practice, as well as a novel biocompatible precursor in the sol-gel synthesis of practically useful substances.

Due to the fact that animal parasitic diseases often occur in the form of mixed infections, it is necessary to use complex drugs with a combination of active substances that act against different classes of helminths. Fenbendazole has a wide spectrum of nematocidal action and is less effective against cestodes. Considering that sheep are often infected with both gastro-intestinal nematodes and cestodes, a complex drug based on fenbendazole, niclosamide with polyvinylpyrrolidone polymer, was developed using mechanochemical technology in order to increase its solubility and bioavailability and reduce the dosages and side effects.

This study aimed to evaluate the influence of mechanochemical technology on the efficacy of complex solid dispersions of anthelmintics against cestodoses and nematodoses.

The influence of different types of mills (roller and planetary mills), levels of energy intensity (20, 40, 60 g), and component ratio (2:20:78; 3:30:67; 4:40:56) during mechanochemical processing was studied on the anthelmintic efficacy of complex solid dispersions of fenbendazole, niclosamide, and polyvinylpyrrolidone in laboratory models of trichinellosis and hymenolepiosis of white mice, and on sheep naturally infected with helminths.

The efficacy of complex solid dispersions obtained in the planetary mill was higher than the activity of dispersions obtained in a roller mill. It showed 87.5, 96.36, 83.77, and 99.39% efficacy, respectively, against experimental trichinellosis, hymenolepiosis of white mice, gastro-intestinal nematode infection and monieziosis of sheep at a ratio of 2:20:78. The basic drug - fenbendazole demonstrated 31.37 and 22.77% activity against experimental trichinellosis and gastro-intestinal nematode infection of sheep. The basic drug, niclosamide, showed 36.37% efficacy against hymenolepiosis in mice and 28.31% against monieziosis in sheep. It was established that with an increase in the energy intensity level of the planetary mill (20, 40, and 60 g), the decrease in the efficacy of solid dispersion occurred from 73.90 to 59.12% against T. spiralis and from 92.73% to 79.81% against H. nana.

The use of mechanochemical technology for the production of solid dispersions of fenbendazole and niclosamide with polyvinylpyrrolidone makes it possible to increase the anthelmintic efficacy by 2.7–3 times compared to the activity of basic substances. It was noted that the complex solid dispersions of anthelmintics obtained in a planetary mill had 7.51–10.17% greater activity in comparison with the samples obtained in a roller mill. The most optimal ratio of active substances was 2:20:78 at a 20 g level of energy intensity of the planetary mill.