Design, Synthesis and Biological Activities of Some phthalimides Derivatives

Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties. Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The Nitric oxide and Ferric reducing antioxidant properties (FRAP) were determined by spectrophochemical method. Results: The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50 = 15 ± 2 µg/mL) against Nitric oxide inhibition. Compounds 3 (FRAP = 205±8 µg/ML) and 6 (FRAP = 118±1 µg/ML) were found to exhibit higher FRAP analysis results which were comparable to the results obtained for serine. (FRAP = 202±7 µg/ML). Conclusion: The considerable activity of the compounds shown by its Nitric oxide and Ferric reducing antioxidant properties (FRAP) makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

Antifungal and Anti-Inflammatory Potential of Bupleurum rigidum subsp. paniculatum (Brot.) H.Wolff Essential Oil

Fungal infections remain a major health concern with aromatic plants and their metabolites standing out as promising antifungal agents. The present study aims to assess, for the first time, the antifungal and anti-inflammatory potential of Bupleurum subsp. paniculatum (Brot.) H.Wolff essential oil from Portugal. The oil obtained by hydrodistillation and characterized by GC-MS, showed high amounts of monoterpene hydrocarbons, namely α-pinene (29.0–36.0%), β–pinene (26.1–30.7%) and limonene (10.5–13.5%). The antifungal potential was assessed, according to CLSI guidelines, against several clinical and collection strains. The essential oil showed a broad fungicidal effect being more potent against Cryptococcus neoformans and dermatophytes. Moreover, a significant germ tube inhibition was observed in Candida albicans as well as a disruption of mature biofilms, thus pointing out an effect of the oil against relevant virulent factors. Furthermore, fungal ultrastructural modifications were detected through transmission electron microscopy, highlighting the nefarious effect of the oil. Of relevance, the oil also evidenced anti-inflammatory activity through nitric oxide inhibition in macrophages activated with lipopolysaccharide. In addition, the essential oil’s bioactive concentrations did not present toxicity towards macrophages. Overall, the present study confirmed the bioactive potential of B. rigidum subsp. paniculatum essential oil, thus paving the way for the development of effective drugs presenting concomitantly antifungal and anti-inflammatory properties.

Heat-Killed Lactic Acid Bacteria Inhibit Nitric Oxide Production via Inducible Nitric Oxide Synthase and Cyclooxygenase-2 in RAW 264.7 Cells

Heat-killed lactic acid bacteria perform immunomodulatory functions and are advantageous as probiotics, considering their long product shelf-life, easy storage, and convenient transportation. In this study, we aimed to develop appropriate heat treatments for industrial preparation of probiotics with antioxidant activity. Among 75 heat-killed strains, Lactococcus lactis MG5125 revealed the highest nitric oxide inhibition (86.2%), followed by Lactobacillus acidophilus MG4559 (86.0%), Lactobacillus plantarum MG5270 (85.7%), Lactobacillus fermentum MG4510 (85.3%), L. plantarum MG5239 (83.9%), L. plantarum MG5289 (83.2%), and L. plantarum MG5203 (81.8%). Moreover, the heat-killed selected strains markedly inhibited lipopolysaccharide-induced nitric oxide synthase and cyclooxygenase-2 expression. The use of heat-killed bacteria with intact bio-functionality can elongate the shelf-life and simplify the food processing steps of probiotic foods, given their high stability. The antioxidant and immune-modulatory activities of the heat-killed strains selected in this study indicate a strong potential for their utilization probiotic products manufacturing.

Nitric oxide inhibition assay and the respective target identification of an aptamer designed to control atherosclerosis

Introduction: Aptamers are emerging newer therapeutics and diagnostics can be designed to bind any kind of target proteins. Vascular endothelial damage by the excess amount of nitric oxide production in systemic circulation leads to the secretion of inflammatory chemoattractant and cell adhesion, which is the prime pro-atherogenic events in the formation of plagues at atrial intimal layers due to oxidation – sensitive mechanisms. Nitric oxide inhibition assay is one of the valuable qualitative anti-atherosclerosis matrices. Methods: In this research, Nitric oxide inhibition efficiency of a ssDNA aptamer on cell lines was studied and the respective targets of that aptamer were identified by network analysis. The aptamer used here was originally designed for Selectin P Ligand Protein to control atherogenic process. 20 nM of aptamer solution in LipofectamineTM 2000 shows the highest level of 70.5 % inhibition of nitric oxide liberation on 24 hours cultured medium of Lipopolysaccharide stimulated murine macrophage RAW 264.7 cell lines. Results: Protein interaction network analysis on the nitric oxide synthesis pathway interactors and the molecular docking analysis with network resulted proteins such as AKT Serine/Threonine Kinase 1, Calmodulin, Estrogen Receptor 1, and Nitric Oxide Synthase-3 confirms that the G – quadruplex Model of 18-mer sequence effectively binds on the active sites of Estrogen Receptor 1, and Nitric Oxide Synthase-3. Conclusion : The aptamer designed for atherosclerotic target have also exert significant nitric oxide inhibition to control the atherogenic events through the proteins, AKT1, NOS3 and ESR1.

Antioxidant, anti-inflammatory and cytotoxic activities of the unsaponifiable fraction of extra virgin olive oil

The health benefits of olive oil are well-known. In this study, the unsaponifiable fraction of extra virgin olive oil (Unsap) was investigated for reducing power capacity, ferric reducing antioxidant power, fer-rous chelating activity and nitric oxide inhibition. The present study was also designed to evaluate the in vitro cytotoxic effect of the Unsap against human carcinoma cells. The anti-inflammatory potential of Unsap has been determined via the inhibition of Human Cyclooxygenases. The results showed that Unsap is efficient for ferric reducing antioxidant power and nitric oxide inhibition. Unsap has a selective effect as anti-inflammatory agent. The results showed moderate to good in vitro antitumor activities of Unsap against human liver, lung and pancreas cancer cells with IC50 ranging from 19.6 to 30.4 μg/mL and good selectivity index (≥ 2). In conclusion, Unsap represents a promising and safe antitumor and antioxidant material that supports the need for further investigation.

Evaluation of In-Vitro Antioxidant Activity of Root Bark Extracts of Ventilago Maderspatana Gaertn

Ventilago maderspatana Gaertn. is a plant having enormous biomedical potential. It is a plant in the Indian system of medicine having a plethora of properties and applications and The root barks powder of Ventilago maderspatana Gaertn. have many properties and applications like it are used as a stomachic, tonic, carminative, stimulant. It is also useful in the treatment of weakness and fever. For further investigations of activities like anti-oxidant activity, In-vitro anti-oxidant studies were done on root bark extracts of Ventilago maderspatana Gaertn. (Family Rhamnaceae) by using standard methods like Lipid peroxidation Assay, Estimation of total anti-oxidant capacity (TAC), Hydroxyl radical scavenging activity, Nitric oxide inhibition radical activity by p-Nitroso dimethyl aniline method, and ABTS Radical scavenging method. The root barks of plant Ventilago maderspatana Gaertn. Were subjected to cold maceration process in 3-liter Round bottom flask using ethanol and distilled water and nature and yield was noted and stored at 40C in the refrigerator until further use and both the extracts were labelled as Ventilago maderspatana Gaertn. Root Bark aqueous (VMRBA) and Ventilago maderspatana Gaertn. Root Bark Ethanolic (VMRBE) for convenient identification. Ethanolic extract of Root Bark showed the more potent anti-oxidant activity than aqueous Root Bark extract of Ventilago maderspatana Gaertn.