Current Chemical Biology - Volume 18, Issue 2, 2024

Leukemic stem cells are considered to be the main cause of treatment failure and disease recurrence due to their resistance to most common therapies. Apoptosis induction is one of the highly effective methods for treating cancer. Ciprofloxacin is among the compounds whose antitumor effects have been confirmed.

In this study, we investigated the anti-proliferative effect and induction of apoptosis by one of the derivatives of this family called 1-Cyclopropyl-6-fluoro-7-[4-(2-{[(1R,2S,5R)- 2-isopropyl-5-methylcyclohexyl]oxy}-2-oxoethyl)-piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (ICH-CP) on NB4 cell line as an in vitro model of Acute promyelocytic leukemia (APL). NB4 cells were treated using the ICH-CP combination in various concentrations.

The viability of NB4 cells was evaluated by MTT assay, and their morphology of apoptosis was examined by fluorescence microscopy. Flow cytometry and Annexin V/PI staining were used to quantify apoptosis. Finally, the expression of three genes, Bax, Bcl-2, and Survivin was inquired by real-time PCR.

According to the results, ICH-CP was able to destroy about 60% of NB4 cells in a dose and time-dependent manner. Light microscopy and fluorescence microscopy studies on treated cells confirmed the induction of apoptosis. Also, the real-time PCR analysis showed that ICH-CP induces apoptosis in the NB4 cell line via the down-regulation of Survivin and Bcl-2, in contrast to the up-regulation of the Bax gene.

Based on the present data, it seems that the novel compound can be a good candidate for the treatment of acute myeloid leukemia. Furthermore, it is recommended to evaluate the qualification of ICH-CP as an adjunctive agent for other cancer cell lines.

Nanoparticles (NPs) are reliable biological tools for curative purposes through their application in nanomedicine. The present study synthesized and characterized silver nanoparticles (AgNPs) from Tetrapetra tetrapleura fruit. The investigation aims to examine the antidiabetic effect of the AgNPs using in vitro and in vivo models.

Briefly, the synthesized AgNPs were confirmed by the application of ultraviolet-visible (UV-Vis) spectroscopy, and five other techniques, viz; transmission electron microscopy (TEM) techniques, Fourier transform infrared (FTIR) spectroscopy, energy dispersive X-ray spectroscopy (EDX), X-ray diffraction analysis (XRD) and scanning electron microscope (SEM). The in vitro model assay investigated the scavenging effect of AgNPS on 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion (O2ˉ), hydroxyl anion (^-OH), ferric reducing antioxidant power (FRAP), and α-amylase/α-glucosidase inhibitory activity. The in vivo model involving rats-induced type-2 diabetes with streptozotocin (STZ) was divided into six (6) groups of seven (7) rats each to assess antioxidative parameters.

The AgNPs scavenged free radicals (DPPH) and moderately inhibited (O2ˉ), hydroxyl anion (^-OH), reduced ferric to ferrous ions, and inhibited both α-amylase and α-glucosidase activity with increasing concentrations. Similarly, AgNPs ameliorated oxidative stress imposed by type 2 diabetes on the rats’ tissues significantly (p < 0.05), depleting total cholesterol, low-density lipoprotein (LDL), and increased total protein composite and high-density lipoprotein (HDL) contents. The AgNPs enhanced catalase and superoxide dismutase, reduced glutathione (GSH), and, concomitantly, decreased malondialdehyde (MDA) levels in the tissue homogenate.

These findings provide scientific evidence for the first time, finding the application of a biogenic compound synthesized from T. tetrapleura fruit in the treatment of type 2 diabetes.

The allelopathic effects of the essential oils of M. piperita and C. coronarium on seed germination of two wheat species qualify them as bio-herbicides.

In order to search for natural plant-based products that may have herbicidal action, we selected two plant species, M. piperita and C. coronarium, to evaluate the allelopathic potential of their essential oils on wheat seed germination of two wheat species.

Aerials parts of M. piperita and C. Coronarium were subjected to hydrodistillation using a Clevenger-type apparatus to extract essential oils, followed by characterization using gas chromatography coupled with mass spectrometry. Bioassays were conducted with ethanol as the organic solvent, employing three concentrations (0.25, 0.5, and 0.75 μl/ml of oil/ethanol) to assess their effects on the seed and seedling growth of two wheat species.

Under laboratory conditions, extracts of Mentha piperita and Chrysanthemum coronarium oils at varying concentrations (0.25 μl, 0.5 μl, and 0.75 μl) were examined for their effects on two wheat species (Triticum durum L. and Triticum aestivum L.). The yields of the obtained oils were 1.19% and 0.25%, respectively. The chemical composition of the essential oils extracted from M. piperita and C. coronarium was dominated by oxygenated monoterpenes, representing 97.5% and 94.9%, respectively. The tested essential oils strongly inhibit seed germination and seedling growth (root length LR and shoot length LPA) of both wheat species studied. The inhibition increased as the oil concentration increased, although this increase differed between the two species. This study has shown that the tested essential oils possess an interesting inhibitory allelopathic potential.

The findings of this study indicate that the tested essential oils possess promising allelopathic properties, suggesting them as natural bio-herbicides.

Numerous natural products have been successfully developed for clinical use in the treatment of human diseases in almost every therapeutic area.

This work aimed to assess the in-vitro and in-silico α-amylase inhibition activities of carlina oxide and aplotaxene, isolated from the roots of Carthamus caeruleus and Rhaponticum acaule respectively.

The essential oil from C. caeruleus roots was obtained using a Clevenger-type apparatus, and the hexanoic extract from the roots of R. acaule was obtained through maceration. Major components of each plant were separated via column chromatography. The in-vitro α-amylase inhibition activity was evaluated using porcine pancreatic α-amylase, while the molecular docking study was conducted using the Molecular Operating Environment (MOE) with three types of α-amylase: human salivary, pancreatic α-amylase and Aspergillus oryzae α-amylase (PDB: 1Q4N, 5EMY, 7P4W respectively).

The in-vitro α-amylase inhibition results for the essential oil, the hexanoic extract, carlina oxide and aplotaxene showed that carlina oxide exhibited significant activity with IC50 of 0.42 mg/mL. However, the in-silico study showed no interaction between aplotaxene and the three α-amylase enzymes, whereas carlina oxide demonstrated one pi-cation interaction with 5EMY with the amino acid TYR 62 at a distance of 4.70 Å and two pi-H interactions with 7P4W with the amino acid LYS 383 at distances of 4.31 and 4 .03 Å.

In conclusion, carlina oxide has the potential to serve as an alternative agent for α-amylase inhibition, contributing to the reduction of postprandial hyperglycemia.

Acute Kidney Injury (AKI) is a common clinical disease that has a high incidence and mortality rate. Clove, a robust natural source of bioactive chemicals and rich in secondary metabolites, plays a wide range of biological roles.

The present study aimed to assess the ameliorative efficacy of clove extract against acute renal damage induced by folic acid in rats.

Gas Chromatography/Mass Spectrometry (GC/MS) was used to investigate the main components of clove extract. Folic acid, at a dose of 250 mg/kg, was delivered intraperitoneally to rats to induce AKI. Eighteen rats were divided into three groups: control, AKI, and AKI + clove extract (500 mg/kg).

The administration of clove extract significantly restored the levels of creatine, urea, uric acid, sodium, potassium, chloride, creatinine clearance, and microalbumin to nearly normal levels. Also, clove water extract inhibited oxidative stress by decreasing concentrations of Malondialdehyde (MDA) and Nitric Oxide (NO). Furthermore, clove extract elevated the levels of Glutathione-reduced (GSH), Catalase (CAT), and Glutathione S-transferase (GST). Kidney section histology showed notable improvements after the administration of clove extract.

The clove water extract has been found to contain many bioactive components possessing antioxidant and anti-inflammatory properties, effectively protecting against acute renal injury.