Current Bioactive Compounds - Online First

Plant extracts containing polysaccharides, flavonoids, and chelated calcium compounds are effective for the complex therapy of osteomyelitis. In this study, the content of target components in the extracts of seven Saussurea DC species was studied, and their osteogenic and hematopoietic activities in model osteomyelitis were investigated.

The content of chelidonic acid by high-performance liquid chromatography, flavonoids by spectrophotometric method, polysaccharides by gravimetric method, and calcium by automatic analyzer in extracts was determined. Biological experiments were carried out on rats using the model of experimental osteomyelitis.

The largest amount of calcium (3-4 mmol/l) in S. controversa, S. salicifolia, and S. frolowii, chelidonic acid (122 mg/g) in S. controversa, and flavonoids (63-74 mg/g) and polysaccharides (218-251 mg/g) in S.frolowii and S. parviflora extracts was found. In the model osteomyelitis, the studied extracts stimulated bone marrow hematopoiesis, and the total number of bone marrow cells increased after treatment with S. controversa extract by 50% and with S. parviflora and S. daurica extracts by 28% compared to the control. After treatment with Saussurea extracts, the intensity of inflammation in the bone tissue decreased, and regenerative processes intensified. Moreover, the area of mature bone tissue increased by 72% after treatment with S. controversa and S. parviflora extracts, indicating the successful completion of the bone regeneration process.

Plants of the genus Saussurea (S. controversa DC, S. parviflora (Poir.) DC, S. frolovii Ledeb., S. daurica Adams., and S. salicifolia (L.) DC) showed osteogenic and hematopoietic efficacy in the osteomyelitis model of rats. Extracts and biologically active components of these plants can expand the arsenal of sources for the complex therapy of osteomyelitis.

Paracetamol overdose can lead to severe liver damage due to the formation of toxic metabolites. Casimiora edulis, rich in polyphenols and flavonoids, and silymarin, a known liver protectant, may help mitigate this damage.

This study aims to characterize the main phytoconstituents of Casimiora edulis leaves and evaluate their hepatoprotective activity.

Leaves of Casimiora edulis were extracted with methanol. The total flavonoid and phenolic acid contents in the methanol extract were identified using HPLC. The hepatoprotective effects were assessed in 30 mice divided into five groups, treated with paracetamol to induce liver damage, and administered Casimiora edulis extract or silymarin at different doses. Blood and liver samples were collected to measure biochemical markers, oxidative stress indicators, inflammatory markers, and gene expression. Histopathological examination of liver tissues was also performed.

HPLC analysis revealed a rich polyphenolic profile, with gallic acid (1905.83 µg/g) and diadzein (7039.18 µg/g) as predominant compounds. Paracetamol administration significantly increased TC, TG, liver enzyme levels (ALT, AST, LDH, ALP), MDA, IL-6, TNF-α, and CYP2E1, while decreasing HDL-c, SOD, GSH, and CAT levels, as well as BcL-2 and P53 gene expression, indicating hepatotoxicity. Treatment with Casimiora edulis extract and silymarin significantly mitigated these adverse effects, improving plasma lipid profiles, liver enzyme levels, oxidative stress biomarkers, inflammatory mediators, and gene expression. In addition, Casimiora edulis extract and silymarin significantly improve liver histopathological scores in paracetamol-treated mice. Despite severe congestion and necrosis, the liver maintained its typical structure with central veins and hepatocyte cords, highlighting the potential therapeutic benefits of these treatments.

Casimiora edulis extract and silymarin demonstrate significant hepatoprotective effects against paracetamol-induced liver damage. Their rich polyphenolic and flavonoid content effectively mitigates oxidative stress and inflammation, improving biochemical markers and preserving liver structure. These findings highlight their potential as therapeutic agents for liver health.

This study explores the therapeutic potential of Bixa orellana (B. orellana), focusing on its bioactive compounds and antioxidant effects. Phytochemical analysis combined with network pharmacology was employed to investigate its multi-targeted therapeutic potential against oxidative stress.

The antioxidant activity of B. orellana flower extract was determined using DPPH assays. High-performance thin-layer chromatography (HPTLC) and liquid chromatography-mass spectrometry (LC-MS) were performed to profile key bioactive constituents. Network pharmacology analysis linked to these phytochemicals was performed to determine its role in oxidative stress and associated complications.

The results showed a significant DPPH activity of the flower extract of B. orellana. HPTLC profiling showed several major and minor metabolites at different Rf values, while LC-MS profiling revealed quercetin, kaempferol, genestin, etc, as key components of the flower extract. In network pharmacology analysis, quercetin showed a significant interaction with genes like TP53, NOS2, and CAT, while kaempferol targeted SOD2 and NFE2L2, both crucial in oxidative stress regulation. The results highlight the multi-targeted approach of B. orellana flower extract compounds in modulating oxidative stress pathways.

This comprehensive approach revealed multiple molecular pathways influenced by B. orellana compounds, providing a strong foundation for their therapeutic potential in oxidative stress-related diseases.

The use of plant extracts in the biosynthesis of nanoparticles has garnered attention in recent years due to the rapid, ecological, and economical production protocol. The current study aimed to biosynthesize silver nanoparticles (AgNPs) of Hypochaeris radicata L. extract.

These nanoparticles were characterized by UV-Vis, Fourier Transform Infrared Spectroscopy (FTIR), and X-Ray Diffraction (XRD) to determine their size and composition. The bioactivity was assessed by the determination of their antimicrobial effect using the well diffusion method and their cytotoxicity by hemolysis method.

The results showed that AgNPs have been successfully synthesized and exhibit a surface plasmon resonance spectrum with an absorption maximum at 420 nm. FTIR affirmed the role of H. radicata L. as a reducing and capping agent of silver ions and XRD revealed their crystalline nature. Interestingly, the synthesized AgNPs exhibited significant antimicrobial effects particularly against Escherichia coli and Aspergillus niger with inhibition zones of 20.5 and 19 mm, respectively. The cytotoxicity test confirmed the non-toxic characteristics of the synthesized AgNPs.

The bio-ingredients present in the plant extract were effective for the synthesis of Ag nanoparticles with significant biological efficacy.

Tetrazole-based compounds are of significant interest due to their potential pharmacological applications. The current study focuses on the synthesis and analysis of such a compound.

This research aims to synthesize the title compound N-(3-methyl-1-phenyl-2-(1H-tetrazol-1-yl) butyl) acetamide, analyze its crystal structure, perform computational studies, and evaluate its potential pharmacological activities and it’s in silico and in vitro supports, specifically antidiabetic and anti-inflammatory properties.

The title compound, C14H19N5O, was synthesized, and its crystal structure was confirmed using single-crystal X-ray diffraction analysis by default parameters. Density Functional Theory (DFT) calculations were performed using the Gaussian 09W software package with the B3LYP/6-311++G (d,p) method to optimize the compound's structure and calculate its HOMO-LUMO energy gap, Molecular Electrostatic Potential (MEP), and Mulliken charge distribution. In vitro, antidiabetic and anti-inflammatory activities were assessed and compared with standard drugs by using reported protocols. Additionally, molecular docking studies were conducted with enzymes related to diabetes and inflammation with default parameters, and Auto-Dock 4.2 software was used.

The X-ray diffraction analysis confirmed the crystal structure, and the Density Functional Theory (DFT) calculations provided insights into the molecular properties of the compound. Molecular docking experiments with relevant enzymes further supported the significant antidiabetic and anti-inflammatory activities demonstrated in the in vitro tests.

The synthesized tetrazole-based compound exhibits promising antidiabetic and anti-inflammatory activities, supported by both experimental and theoretical studies, suggesting its potential for further pharmacological investigation.