Abstract

Bee bread (BB) is a beehive product generated upon fermentation of pollen combined with flower nectar and glandular secretions. The potential application of BB is related to its nutritional and functional components, including phenolic compounds. This is the first prospective study on palynological parameters, phenolics, antioxidant, and antibacterial activity of Chilean bee bread in vitro. The tested material exhibited high levels of phenolics (1340±186 mg GAE/100 g BB) and showed antioxidant capacity as determined by the FRAP (51±2 μmol Trolox equivalent/g BB) and ORAC-FL (643±64 μmol Trolox equivalent/g BB) and antibacterial activity against Streptococcus pyogenes. Furthermore, the phenolic acids and flavonoids was determined using liquid chromatography-mass spectrometry, and the concentration was determined using liquid chromatography with diode array detection. Kaempferol, quercetin, ferulic acid, and rutin were the main phenolics found. This study demonstrates the bioactive potential of Chilean BB and supports the evidence that this bee product is a promising source of antioxidants and antimicrobial compounds.

:  Pyrazolic hybrids appended with naphthalene, p-chlorobenzene, o-phenol and toluene have been synthesized using Claisen Schmidt condensation reaction of 1-benzyl-3,5-dimethyl-1H-pyrazole-4-carbaldehyde. All compounds were characterized by various spectroscopic techniques. Compound (E)-3-(1-benzyl-3,5-dimethyl-1H-pyrazol-4-yl)-1-(4-chlorophenyl)prop-2-en-1-one crystallizes in monoclinic crystal system with C2/c space group. These synthesized compounds were tested for cytotoxic activity and among these compounds 4b and 5a shows prominent cytotoxic activity against triple-negative breast cancer (TNBC) cells MDA-MB-231 with IC50 values 47.72 µM and 24.25 µM respectively. Distinguishing morphological changes were noticed in MDA-MB-231 cells treated with pyrazole hybrids contributing to apoptosis action. To get more insight into cytotoxic activity, in silico molecular docking of these compounds were performed and the results suggested that (E)-3-(1-benzyl-3,5-dimethyl-1H-pyrazol-4-yl)-1-(p-tolyl)prop-2-en-1-one and 1-(1'-benzyl-5-(4-chlorophenyl)-3',5'-dimethyl-3,4-dihydro-1'H,2H-[3,4'-bipyrazol]-2-yl)ethan-1-one binds to the prominent domain of Akt2 indicating their potential ability as Akt2 inhibitor. Moreover, from in silico ADME studies clearly demonstrated that these compounds may be regarded as a drug candidate for sub-lingual absorption based on log p values (2.157- 4.924). These compounds also show promising antitubercular activity. The overall results suggest that pyrazolic hybrids with substitution at less sterically hindered positions have appealing potent cytotoxic activity and antituberculosis activity due to which they may act as multidrug candidate.

Bacterial infections that cause chronic wounds provide a challenge to healthcare worldwide because they frequently impede healing and cause a variety of problems. In this study, loaded with tungsten oxide (WO3), Magnesium oxide (MgO), and graphene oxide (GO) on chitosan (CS) membrane, an inexpensive polymer casting method was successfully prepared for wound healing applications. All fabricated composites were characterized by X-ray powder diffraction (XRD), Fourier transforms infrared spectroscopy (FTIR), and thermogravimetric analysis (TGA). A scanning electron microscope (SEM) was used to study the synthesized film samples’ morphology as well as their microstructure. The formed WO3/MgO@CS shows a great enhancement in the UV-Vis analysis with a highly intense peak at 401 nm and a narrow band gap (3.69 eV) compared to pure CS. The enhanced electron-hole pair separation rate is responsible for the WO3/MgO/GO@CS scaffold's antibacterial activity. Additionally, human lung cells were used to determine the average cell viability of nanocomposite scaffolds and reached 121 % of WO3/MgO/GO@CS nanocomposite, and the IC50 value was found to be 1654 µg/mL. The ability of the scaffold to inhibit the bacteria has been tested against both E.coli and S. aureus. The 4th sample showed an inhibition zone of 11.5±0.5 mm and 13.5±0.5 mm, respectively.

Abstract

We present the inhibitory properties of the R. pompana anthocyanin fraction (RPAF) and its major constituents on alpha-glucosidase (AG), pancreatic lipase (PL), HMG-CoA reductase, and ornithine decarboxylase (ODC). The effect of RPAF was also evaluated in ICR male mice subjected to oral glucose tolerance test (OGTT) and hypercaloric/atherogenic diet for 30 days. RP-HPLC/MS profiling revealed that RPAF contained five major anthocyanins and induced slight inhibition on PL and HMG-CoA reductase (IC₅₀, 245–338 μg mL⁻¹) whereas strong activity on AG and ODC (IC₅₀, 130–133 μg mL⁻¹) was observed. Kinetic studies and molecular docking with pelargonidin-3-O-rutinoside (P3R) on ODC, revealed changes in K_m (0.9514–0.9746 mM) and V_max (1.96–2.32 μmol mg⁻¹ min⁻¹) suggesting mixed inhibition and molecular interaction with two active sites of ODC. P3R showed antiproliferative activity (IC_50, 46.5 μM) and decreased polyamine accumulation in DLD-1 cells. The results of OGTT confirmed that RPAF regulates postprandial glucose levels in diabetic animals which experienced a significant glucose depletion (30 %; p<0.001) from 30 to 120 min post-treatment. Prolonged supplementation of RPAF caused significant decrease (p<0.001) in plasma glucose, total cholesterol, LDL-c and triglycerides as well as significant increase (p<0.001) of HDL-c compared with normoglycemic untreated animals.

Abstract

Synthesis of new anticancer candidates with protein kinases inhibitory potency is a major goal of pharmaceutical science and synthetic research. This current work represents the synthesis of a series of substituted benzoate-thiazolidinones. Most prepared thiazolidinones were evaluated in vitro for their potential anticancer activity against three cell lines by MTT assay, and they found to be more effective against cancer cell lines with no harm toward normal cells. Thiazolidinones 5 c and 5 h were further evaluated to be kinase inhibitors against EGFR showing effective inhibitory impact (with IC₅₀ value; 0.2±0.009 and 0.098±0.004 μM, for 5 c and 5 h, respectively). Furthermore, 5 c and 5 h have effects on cell cycle and apoptosis induction capability in HepG2 cell lines by DNA-flow cytometry analysis and annexin V-FITC apoptosis assay, respectively. The results showed that they have effect of disrupting the cell cycle and causing cell mortality by apoptosis in the treated cells. Moreover, molecular docking studies showed better binding patterns for 5 c and 5 h with the active site of the epidermal growth factor receptor (EGFR) protein kinase (PDB code 1M17). Finally, toxicity risk and physicochemical characterization by Osiris method was performed on most of the compounds, revealing excellent properties as possible drugs.

Front Cover. The berries of Rhamnus pompana are a traditionally consumed by people of the northeastern highlands of Puebla-Mexico as a result of Nahuatl inheritance. These fruits contained five anthocyanins with the capacity to reduce the levels of plasma glucose, cholesterol and triglycerides in mice. Same compounds were able to decrease the specific activity of key enzymes including human ornithine decarboxylase and avoided polyamine accumulation in DLD-1 cancer cells, as reported by Y. Pechaeco-Hernández et al. in their research article at 10.1002/cbdv.202301034.

Abstract

Background: Parkinson's disease (PD) is a common progressive neurodegenerative and the prevailing treatments are ineffective in the early stages of the disease. Therefore, other strategies must be devised to halt the steady decrease of dopaminergic neurons in the brain. In Parkinson's disease, a dysregulated ACE/Ang II/AT1R axis in the brain causes free radical damage, apoptosis, and neuronal destruction. Current PD treatments only alleviate symptoms and do not reverse the degradation mechanism of dopaminergic neurons. As a result, it is critical to discover alternate, dependable medicines for the treatment of Parkinson's disease. Method: In the present study, homology modelling of MAS receptor, in silico docking and molecular dynamic studies (MDS) were employed to determine the efficacy of flavonoids as MASR activators. Result: The flavonoids Pterosupin and Amentoflavone exhibited best binding and therefore, the stability of these complexes were evaluated with MDS studies. The Pterosupin-MASR complex demonstrated better stability, stronger interactions and minimal fluctuation than the Amentoflavone-MASR complex. Conclusion: The data from the present study indicated that the flavonoid Pterosupin possesses better binding, favourable pharmacokinetic properties and stability. However, subsequent in vitro and in vivo assessments are necessary to validate its efficacy.

Abstract

Apilarnil is 3–7 days old drone larvae. It is an organic bee product known to be rich in protein. In this study, the biological activities of Apilarnil were determined by its antioxidant and enzyme inhibition effects. Antioxidant activities were determined by Fe³⁺, Cu²⁺, Fe³⁺-TPTZ ((2,4,6-tris(2-pyridyl)-s-triazine), reducing ability and 1,1-diphenyl-2-picrylhydrazyl (DPPH⋅) scavenging assays. Also, its enzyme inhibition effects were tested against carbonic anhydrase I and II isoenzymes (hCA I, hCA II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Antioxidant activity of Apilarnil was generally lower than the standard molecules in the applied methods. In DPPH⋅ radical scavenging assay, Apilarnil exhibited higher radical scavenging than some standards. Enzyme inhibition results towards hCA I (IC₅₀: 14.2 μg/mL), hCA II: (IC₅₀: 11.5 μg/mL), AChE (IC₅₀: 22.1 μg/mL), BChE (IC₅₀: 16.1 μg/mL) were calculated. In addition, the quantity of 53 different phytochemical compounds of Apilarnil was determined by a validated method by LC/MS/MS. Compounds with the highest concentrations (mg analyte/g dry extract) were determined as quinic acid (1091.045), fumaric acid (48.714), aconitic acid (47.218), kaempferol (39.946), and quercetin (27.508). As a result, it was determined that Apilarnil had effective antioxidant profile when compared to standard antioxidants.

Abstract

Chondroitin synthesis was performed using the recombinant Escherichia coli(C2987) strain created by transforming the plasmid pETM6-PACF-vgb, which carries the genes responsible for chondroitin synthesis, kfoA, kfoC, kfoF, and the Vitreoscilla hemoglobin gene (vgb). Then, Microbial chondroitin sulfate (MCS)’s antioxidant, anticholinesterase, and antibacterial activity were compared with commercial chondroitin sulfate (CCS). The antioxidant studies revealed that the MCS and CCS samples could be potential targets for scavenging radicals and cupric ion reduction. MCS demonstrated better antioxidant properties in the ABTS assay with the IC50 value of 0.66 mg than CCS. MCS showed 2.5-fold for DPPH and almost 5-fold for ABTS⋅+ (with a value of 3.85 mg/mL) better activity than the CCS. However, the compounds were not active for cholinesterase enzyme inhibitions. In the antibacterial assay, the Minimum inhibitory concentration (MIC) values of MCS against S. aureus, E. aerogenes, E. coli, P. aeruginosa, and K. pneumoniae (0.12, 0.18, 0.12, 0.18, and 0.18 g/mL, respectively) were found to be greater than that of CCS (0.42, 0.48, 0.36, 0.36, and 0.36 g/mL, respectively). This study demonstrates that MCS is a potent pharmacological agent due to its physicochemical properties, and its usability as a therapeutic-preventive agent will shed light on future studies.

Abstract

This work describes a new hair dyeing methodology using a chemical reaction between geniposide, an iridoid glycoside extracted from the fruit of Genipa americana (geniposide extract, GE) and the amine group of hair keratin. The influence of reaction conditions (pH, temperature, and extract concentration) on the staining of hair fibers, color development, fiber morphology, and mechanical hair properties of black and white human hair samples, was evaluated before and after GE dyeing treatment. Eye contact safety of GE was also studied using HET-CAM. The treatment of white hair fibers using GE at 20 mg mL⁻¹, temperature of 80 °C and pH 5.5 presented the greatest color change (ΔE=54.0). The higher pH influence was observed at pH 10.0 on white hair tresses (ΔE=6.8), using an GE concentration of 20 mg mL⁻¹ and room temperature (25 °C). Treated samples showed marked changes on mechanical and morphological properties. The HET-CAM did not show any change, thus demonstrating that using GE is safe. In conclusion, the temperature and concentration of the extract were the variables that mostly influenced the color and hair damage. A new approach for hair dyeing was established where iridoids may potentially be useful as a natural hair dyeing.