Inhibition Of Lipid Peroxidation Research Articles

How do taurine and ergothioneine additives improve the parameters of high- and low-quality turkey semen during liquid preservation?

Abstract The study aimed to examine the parameters of turkey ejaculates (n=40) of high and low quality (HQ and LQ, respectively), preserved with the addition of taurine (TAU; 5 mM, 10 mM) and ergothioneine (EGT; 5 mM, 10 mM) for 48 h at 5°C in a liquid state. The motility, plasma membrane integrity (PMI), mitochondrial function, apoptotic and necrotic spermatozoa percentage, and sperm cells that generated NO were determined after 2, 24, and 48 h of storage. The preserved semen was also analysed for the activity of superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT), glutathione (GSH) content, and malondialdehyde (MDA) production. Taurine, in both doses, may improve the antioxidant status of stored turkey semen as well as sperm motility, viability and functionality regardless of ejaculate quality, as manifested by increased SOD and CAT activities, reduced MDA levels, and enhanced sperm characteristics i.e. plasma membrane integrity (PMI), mitochondrial membrane potential (MMP), total motility (TMOT), and progressive motility (PMOT). In turn, the addition of EGT increased GSH content in the external environment and suppressed lipid peroxidation in turkey spermatozoa, in particular those from low-quality (LQ) ejaculates. However, it appears that EGT could deliver more satisfactory results when added at lower concentrations.

Physicochemical and stability analysis of mung bean protein hydrolysates with lipid peroxidation inhibition

This study investigated mung bean protein hydrolysates (MBPH) produced using neutral protease, examining their physicochemical properties, stability, and lipid peroxidation inhibition capabilities. The research revealed that MBPH molecular weight ranged from 17 to 26 kDa and perform various functions, including catalytic, nutrient storage, and binding. Stability assessments showed that MBPH are stable at 45 °C and pH of 7.5 but are light-sensitive and unstable in solution or when combined with sugars. Additionally, increased concentrations of digestive enzymes reduce MBPH stability. Antioxidant tests in vitro and in Caenorhabditis elegans confirmed MBPH's ability to neutralizing radicals, enhance antioxidant enzyme activities, and reduce lipid peroxidation, thereby protecting against oxidative damage. Furthermore, in vivo experiments showed that MBPH extend the lifespan of worms and reduced their body lipid content, indicating potential benefits in mitigating cholesterol-related damage. This research demonstrates the potential of MBPH in inhibiting lipid peroxidation.

Asiatic acid mitigates testosterone-induced benign prostatic hyperplasia in rats via activation of PPAR-γ.

Prostate enlargement due to benign prostate hyperplasia (BPH) is a common, progressive disorder in elderly males with increasing prevalence. It causes devastating lower urinary tract symptoms with no satisfactory medication. Asiatic acid (AA), a natural pentacyclic triterpenoid, is known to have antiproliferative, antioxidant, and anti-inflammatory activities. The aim of this study was to evaluate the possible preventive activities of AA against BPH induced by testosterone in rats. Finasteride (0.5 mg/kg) was used as a reference drug. AA (10 or 20 mg/kg) administration inhibited the rise in prostatic weight and index induced by testosterone. Histopathological staining proved that AA mitigated the pathological features of BPH induced by testosterone, which was reflected as lower glandular epithelial in AA-treated groups. Also, the administration of AA along with testosterone restored the redox valance by inhibiting lipid peroxidation, and MDA production, and restoring the activities of superoxide dismutase (SOD) and catalase (CAT) activities. Also, AA reduced prostate interleukin-6 (IL-6), cyclooxygenase-2 (COX-2), tumor necrosis factor-alpha (TNF-α), and nuclear factor-kappa B (NF-κB) protein expression. In addition, AA modulated mRNA expression of Bax and Bcl-2 in favor of apoptosis. The effects of AA (20 mg/kg) were comparable to those of finasteride. Further, AA ameliorated the rise in insulin-like growth factor 1 receptor (IGF-1R) mRNA expression. This was associated with the enhancement of the prostatic content of PPAR-γ. It can be concluded that AA mitigated the features of BPH induced by testosterone in rats. This involves antioxidant, anti-inflammatory and pro-apototic activities of AA as well as its ability to down-regulate IGF-1R expression and enhance PPAR-γ concentration in prostatic tissues.

Butylphthalide inhibits ferroptosis and ameliorates cerebral Ischaemia–Reperfusion injury in rats by activating the Nrf2/HO-1 signalling pathway

This study aims to investigate whether butylphthalide can inhibit ferroptosis and ameliorate cerebral ischaemia–reperfusion (I/R) injury in rats by activating the nuclear factor erythroid 2-related factor 2 (Nrf2) / heme oxygenase-1 (HO-1) signalling pathway, known for its antioxidative and cytoprotective properties. Middle cerebral artery occlusion reperfusion (MCAO/R) rat models were established. Male rats were randomly divided into five groups: a sham-operated group (sham), MCAO/R group, MCAO/R ​+ ​ML385 (Nrf2-specific inhibitor) group, MCAO/R ​+ ​NBP (butylphthalide) group and MCAO/R ​+ ​ML385 ​+ ​NBP group. The effect of butylphthalide on cerebral I/R injury was evaluated using neurological deficit scores. The expression levels of Nrf2, HO-1, glutathione peroxidase 4 (GPX4), acyl-CoA synthetase long-chain family member 4 (ACSL4) and transferrin receptor 1 (TfR1) protein were detected using Western blot. Moreover, the expression levels of GPX4, HO-1 and TfR1 mRNA were determined through real-time fluorescence quantitative reverse transcription polymerase chain reaction. The distribution of Nrf2, HO-1, GPX4 and TfR1 was detected using immunohistochemical staining. The levels of iron and related lipid peroxidation indexes, such as reduced glutathione, reactive oxygen species, malondialdehyde and nitric oxide, were measured using a kit. The changes in mitochondria were observed through transmission electron microscopy. Butylphthalide treatment significantly improved neurological dysfunction, reduced cerebral infarction volume and mitigated histopathological damage in MCAO/R rats. It induced the nuclear translocation of Nrf2 and upregulated HO-1 expression, which was attenuated by ML385. Butylphthalide also attenuated lipid peroxidation, iron accumulation and mitochondrial damage induced by MCAO/R. The expression of GPX4, ACSL4 and TfR1 proteins, as well as their mRNA levels, was modulated through butylphthalide treatment, with improvements observed in mitochondrial morphology. Butylphthalide exerts neuroprotective effects by attenuating neurological dysfunction and ferroptosis in MCAO/R rats through the activation of the Nrf2/HO-1 pathway and inhibition of lipid peroxidation and iron accumulation.

The Effect of ZnCl2 Concentrations and Heating Methods on the Chlorophyll, Phenolic, Andrographolide Content and Antioxidant Activity of Sambiloto (Andrographis paniculata) Simplicia Powder

The drying process in Sambiloto simplicia production causes the degradation of chlorophyll as the major compound. However, the stability of chlorophyll can be enhanced by forming a metallochlorophyll complex with zinc (Zn) metal. This research aims to produce Zn-rich Sambiloto simplicia powder to produce high stability of chlorophyll. Sambiloto simplicia powder was prepared through sorting, grinding, sieving, and mixing with ZnCl2 solution at concentrations of 0, 200, 300, 400, and 500 ppm, followed by heating (using either oven or an autoclave) and drying. The analysis included determination of total chlorophyll, phenolic, flavonoid, zinc, and andrographolide content. DPPH and FTC assays were employed to evaluate antioxidant activity. The results showed that increasing ZnCl2 concentration up to 300 ppm enhances chlorophyll, phenolic, flavonoid, zinc, and andrographolide content. Higher concentrations of ZnCl2 in the oven resulted in decreased lipid peroxidation inhibition (LPI) of Sambiloto simplicia powder, whereas using an autoclave led to increased LPI. Furthermore, higher ZnCl2 concentrations, up to 400 ppm, corresponded to increased DPPH radical scavenging activity. Lipid peroxidation inhibition activity correlated with andrographolide, zinc, and total phenolic contents. Conversely, DPPH radical scavenging activity strongly correlated with total phenolic, total flavonoid, Zn, chlorophyll, andrographolide content.

Zinc oxide nanoparticles cause hepatotoxicity in rare minnow (Gobiocypris rarus) via ROS-mediated oxidative stress and apoptosis activation and inhibition of lipid peroxidation

Zinc oxide nanoparticles (ZnO NPs) measuring 30 ± 10 nm in diameter are utilized in various applications, including batteries, plastics, ceramics, cosmetics, flame retardants, and food. However, their potential impact and risk on aquatic ecosystems remain unclear. This study examined the hepatotoxic effects of dietary ZnO NPs in rare minnow. Three hundred rare minnows were fed diets containing 0 mg/kg, 20 mg/kg and 60 mg/kg of ZnO NPs for 60 days, with hepatotoxicity assessments at 15-day intervals. The histological data showed that ZnO NPs severely damage liver tissues, causing cytoplasmic vacuolization and irregular or missing nuclei. The treatment groups showed a significant rise in the liver injury index (P < 0.05). Moreover, there was a notable increase in zinc accumulation in the ZnO NPs groups compared to the control group (P < 0.05). ZnO NPs also reduced body weight and hepato-somatic index (HSI) in rare minnows. The enzyme activity results showed elevated levels of reactive oxygen species (ROS), total cholesterol (T-CHO), triglyceride (TG), acetyl Coa carboxylase (ACC), and fatty acid synthase (FAS) in the ZnO NPs fed groups, while total antioxidant capacity (T-AOC) and malondialdehyde (MDA) decreased. Further investigation found that accumulation of ZnO NPs in the liver tissues up-regulated the levels of genes related to antioxidant (mn-sod, cat and nf-κb), pro-apoptotic (bax) and lipogenesis (gpat3, dgat1a and dgat1b), while down-regulating genes associated with lipid catabolism (cpt1 and tpi1). These findings suggest that dietary ZnO NPs cause hepatotoxicity by inducing oxidative stress through ROS, triggering apoptosis, and inhibiting lipid peroxidation. The results indicate that ZnO NPs may pose a significant threat to aquatic animals and ecosystems.

Evaluation of Proximate, Phytochemicals, Antioxidant Capacity, Enzymatic Inhibition, and Anti-Inflammatory Properties of Avocado Seed Meal as Potential Feed Additive

This study examined the proximate composition, phytochemical profile, antioxidant capacity, enzymatic inhibition, and anti-inflammatory properties of avocado seed meal. The proximate analysis revealed that avocado seed meal is rich in protein (17.32%), fat (15.33%), and carbohydrates (48.73%), with moderate levels of moisture (10.26%), ash (2.39%), and crude fiber (5.97%). Phytochemical analysis indicated high contents of phenols (111.56 mg/g), saponins (96.94 mg/g) and flavonoids (66.66 mg/g), but lower levels of alkaloids (14.60 mg/g), tannins (1.17 mg/g), and steroids (0.89 mg/g). The antioxidant properties assessed showed significant DPPH (50.05%) and FRAP (63.04%) free radical scavenging activities, though lower inhibition of lipid peroxidation (34.88%) and vitamin C content (0.03 mg/g). Enzymatic inhibition assays demonstrated alpha-lipase, alpha-glucosidase, and alpha-amylase inhibition rates of 31.46%, 27.56%, and 50.88%, respectively. Anti-inflammatory properties were also notable, with 24.02% albumin denaturation inhibition and 37.99% antiprotease activity. These findings suggest that avocado seed meal holds considerable potential for nutritional and therapeutic applications as natural feed supplement for livestock and humans.

Berberine Inhibits Ferroptosis and Stabilizes Atherosclerotic Plaque through NRF2/SLC7A11/GPX4 Pathway.

To investigate potential mechanisms of anti-atherosclerosis by berberine (BBR) using ApoE-/- mice. Eight 8-week-old C57BL/6J mice were used as a blank control group (normal), and 56 8-week-old AopE-/- mice were fed a high-fat diet for 12 weeks, according to a completely random method, and were divided into the model group, BBR low-dose group (50 mg/kg, BBRL), BBR medium-dose group (100 mg/kg, BBRM), BBR high-dose group (150 mg/kg, BBRH), BBR+nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor group (100 mg/kg BBR+30 mg/kg ML385, BBRM+ML385), NRF2 inhibitor group (30 mg/kg, ML385), and positive control group (2.5 mg/kg, atorvastatin), 8 in each group. After 4 weeks of intragastric administration, samples were collected and serum, aorta, heart and liver tissues were isolated. Biochemical kits were used to detect serum lipid content and the expression levels of malondialdehyde (MDA) and superoxide dismutase (SOD) in all experimental groups. The pathological changes of atherosclerosis (AS) were observed by aorta gross Oil Red O, aortic sinus hematoxylin-eosin (HE) and Masson staining. Liver lipopathy was observed in mice by HE staining. The morphology of mitochondria in aorta cells was observed under transmission electron microscope. Flow cytometry was used to detect reactive oxygen species (ROS) expression in aorta of mice in each group. The content of ferrous ion Fe2+ in serum of mice was detected by biochemical kit. The mRNA and protein relative expression levels of NRF2, glutathione peroxidase 4 (GPX4) and recombinant solute carrier family 7 member 11 (SLC7A11) were detected by quantitative real time polymerase chain reaction (RT-qPCR) and Western blot, respectively. BBRM and BBRH groups delayed the progression of AS and reduced the plaque area (P<0.01). The characteristic morphological changes of ferroptosis were rarely observed in BBR-treated AS mice, and the content of Fe2+ in BBR group was significantly lower than that in the model group (P<0.01). BBR decreased ROS and MDA levels in mouse aorta, increased SOD activity (P<0.01), significantly up-regulated NRF2/SLC7A11/GPX4 protein and mRNA expression levels (P<0.01), and inhibited lipid peroxidation. Compared with the model group, the body weight, blood lipid level and aortic plaque area of ML385 group increased (P<0.01); the morphology of mitochondria showed significant ferroptosis characteristics; the serum Fe2+, MDA and ROS levels increased (P<0.05 or P<0.01), and the activity of SOD decreased (P<0.01). Compared with BBRM group, the iron inhibition effect of BBRM+ML385 group was significantly weakened, and the plaque area significantly increased (P<0.01). Through NRF2/SLC7A11/GPX4 pathway, BBR can resist oxidative stress, inhibit ferroptosis, reduce plaque area, stabilize plaque, and exert anti-AS effects.

Extraction of Bioactive Compounds from Rubus Idaeus Bioresidues: A Full Screening on Phenolic Composition and Bioactive Potential

Abstract Purpose Rubus idaeus cultivation has boosted productivity due to its high nutritional value. In consequence, waste production increased. The discarded biomass, including leaves and aerial components, can be transformed into valuable functional ingredients for industrial applications, such as cosmetics. Studying their bioactivity potential is highly relevant. Methods According to the present idea, the research involved producing extracts from raspberry plant branches and leaves by employing four different techniques: aqueous decoction, aqueous infusion, hydroethanolic maceration, and ultrasound-assisted extraction (UAE). Subsequently, these compounds were screened for their bioactive potential, including antioxidant, antibacterial, anti-inflammatory, and cytotoxic properties. Results The ultrasound-assisted extraction produced extracts rich in phenolic compounds, whereas the infusion and maceration methods resulted in higher flavonol contents. Among the identified phenolic compounds, hydrolyzable tannins, particularly galloyl-bis-HHDP-glucose, were the most dominant ones. Regarding antioxidant potential, the decoction extract was the strongest, while the infusion showed the greatest potential for inhibiting lipid peroxidation. The UAE extract was found to be highly effective as an antibacterial agent. Both infusion and UAE extracts demonstrated the highest anti-inflammatory potential. Conclusion The combination of these results highlights the sample’s bioactive potential and the importance of exploiting bioresidues as unique, sustainable candidates for industrial applications.

Evaluation of the Antioxidant Activity and Phenolic Composition of Different Monofloral and Polyfloral Brazilian Honey Extracts.

This study aimed to evaluate the chemical composition and antioxidant activity of phenolic extracts from monofloral and polyfloral honey samples obtained from different Brazilian regions. The chemical composition (total content of phenolic compounds and flavonoids) of extracts were measured by using colorimetric assays and analyzed by high performance liquid chromatographic (HPLC-DAD). The antioxidant activity was evaluated by chemical and biochemical assays (reducing power assay, 1,1-diphenyl-2-picrylhydrazyl (DPPH⋅) and 2,2-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTS⋅+) scavenger assays. It was also investigated the ability of extracts in attenuate lipid peroxidation induced by Fe2+ in phospholipids. The obtained results clearly demonstrated that the botanical origin and geographical region of honey collection influenced the chemical composition and antioxidant activity of extracts. Furthermore, the samples were constituted by phenolic acids and flavonoids, which p-coumaric acid was predominant among the compounds identified. All samples were able to scavenge free radicals and inhibit lipid peroxidation, and good correlations were obtained between the flavonoid content and honey color. In conclusion, the obtained extracts were constituted by antioxidant compounds, which reinforce the usage of honey in human diets, and demonstrated that the region of honey collection strong influenced in the chemical composition and, consequently, its biological effect.

Phytochemical composition, antioxidant activity, and cytotoxicity of the aqueous extracts of Dracaena arborea and Bridelia ferruginea: In vitro and in silico studies

Dracaena arborea (DA) and Bridelia ferruginea (BF) are medicinal plants used in the treatment of various ailments such as diabetes, infertility, and sexual dysfunctions. The aim of this work was to characterize these plants chemically and investigate their antioxidant and cytotoxicity in vitro and in silico. The cytotoxicity was determined in PC3, NIH3T3 and BT474 cells, and through hemolysis using erythrocytes. Furthermore, selected compounds from DA and BF were docked against some oxidative stress (Keap1: Kelch-like ECH-associated protein 1 and GST: glutathione S-transferase) and cytotoxicity (PARP10: poly(ADP-ribose) polymerase family member 10 and p90 RSK: p90 ribosomal S6 kinases) proteins to predict the ligand-protein interaction. We found that the total phenolic and flavonoid content in BF was significantly (p < 0.001) higher than that of DA. 16 and 32 phytocompounds were identified in DA and BF, respectively. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS+) free radical scavenging activity, and cupric and ferric reducing power of BF were significantly (p < 0.05–0.001) higher than those of DA. Moreover, the ability of BF to inhibit lipid peroxidation was higher than that of DA. DA dose-dependently decreased the viability of PC3, NIH3T3, and BT474 cells, while BF tended to feed the cells. Drug-Likeness and toxicity prediction of selected compounds found in DA and BF were within the acceptable standards, according to Lipinski's rule. The majority of compounds found in DA and BF exhibited a strong binding affinity with Keap1, GST, PARP10 and p90 RSK, which supports the in vitro results. For instance, Cis-cyclohexane-1,3-diamine from DA showed a binding affinity of -6.73 kcal/mol and interacted with Keap1 through five conventional hydrogen bonds, while Nrf2 (a Keap1 inhibitor) exhibited a binding affinity of -11.82 kcal/mol and interacted with Keap1 via two conventional hydrogen bonds. 1,3-propanediamine, n-methyl identified in BF exhibited a high stability with Keap1 (-5.95 kcal/mol) due to the presence of 6 conventional hydrogen bonds. Among the compounds identified in DA, the best stable ligand interacting with PARP10 was 2-deoxy-alpha-d-ribopyranose (-7.62 kcal/mol), as it was well-matched in the PARP10 pocket through five conventional hydrogen bonds. In parallel, among the compounds present in BF, 2-[(methylamino)methyl]cyclohexanol showed the best binding affinity with PARP10 (-9.80 kcal/mol), which was higher than that of veliparib (-8.26 kcal/mol), used as a reference inhibitor. In conclusion, BF has the possibility to be exploited in the prevention/treatment of oxidative stress-related diseases, while DA could be a potential anticancer agent. This could justify their ethnomedicinal uses.

GA receptor targeted chitosan oligosaccharide polymer nanoparticles improve non-alcoholic fatty liver disease by inhibiting ferroptosis

Excessive iron in the liver may exacerbate Non-alcoholic fatty liver disease (NAFLD) by increasing the risk of liver cell expansion, inflammation and fibrosis. Ferroptosis in liver cells may lead the progression of simple fatty liver degeneration to steatohepatitis (NASH). More and more studies shew that ferroptosis played a crucial role in the pathological process of NAFLD. Based on the mechanism of ferroptosis, this study first synthesized a liver targeted 18-β-Glycyrrhetinic-acid-chitosan oligosaccharide -N-acetylcysteine polymer (GCNp), and further curcumin (Cur) was used as model drug to prepare Cur loaded nanodelivery system (GCNp-Cur NPs). The particle size of GCNp-Cur NPs was 132.5 ± 9.8 nm, PDI was 0.148 ± 0.026 and the potential was 23.8 mV. GCNp-Cur NPs can regulate the GPX4/GSH pathway, inhibit lipid peroxidation, restore cellular oxidative environment, reduce free Fe2+, improve cellular lipid metabolism and iron metabolism, thereby NPs inhibited liver cell ferroptosis through multiple pathways. Additionally, GCNp-Cur NPs could also alleviate liver tissue lipid accumulation and oxidative damage, delaying disease progression, and providing a new method and theoretical basis for the treatment of NAFLD.

Trolox, Ferulic, Sinapic, and Cinnamic Acid Derivatives of Proline and GABA with Antioxidant and/or Anti-Inflammatory Properties.

Degenerative conditions, such as neurodegenerative disorders (Alzheimer's disease (AD), Parkinson's disease (PD)) and cardiovascular diseases, are complex, multifactorial disorders whose pathophysiology has not been fully elucidated yet. As a result, the available treatment options cannot eliminate these diseases radically, but only alleviate the symptoms. Both inflammatory processes and oxidation are key factors in the development and evolution of neurodegeneration, while acetylcholinesterase inhibitors are the most used therapeutic options against AD. In this work, following the multi-targeting compound approach, we designed and synthesized a series of proline and gamma-aminobutyric acid (GABA) amides with various acidic moieties that possess an antioxidant and/or anti-inflammatory potency. Proline is the pharmacophore of nootropic drugs (e.g., piracetam) used for memory improvement, while GABA is the main inhibitory neurotransmitter in the central nervous system. The designed molecules were subjected to a preliminary screening of their bioactivity in antioxidant and anti-inflammatory assays, as well as against acetylcholinesterase. Most of the synthesized compounds could inhibit lipid peroxidation (IC50 as low as 8 μΜ) and oxidative protein glycation (inhibition of up to 48%) and reduce the 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH). In addition, all of the compounds were moderate inhibitors of lipoxygenase (LOX) (up to 46% at 100 μΜ) and could decrease carrageenan-induced paw edema in rats by up to 55%. Finally, some of the compounds were moderate acetylcholinesterase inhibitors (IC50 as low as 219 μΜ). The results confirmed the design rationale, indicating that the compounds could be further optimized as multi-targeting molecules directed against degenerative conditions.

Analytical Method Development and Validation for Butylated Hydroxy Toluene by using UV- Visible Spectrophotometric Method

Upon utilizing the Prediction Activity Spectra of Substances (PASS) program, computer-aided predictions were conducted to assess the antioxidant activities. Compounds 1, 3, 4, and 5 underwent evaluation using 1,1-diphenyl-2- picrylhydrazyl (DPPH) and lipid peroxidation assays to confirm the predictions obtained from the PASS program. Notably, compounds 3 and 5 exhibited higher inhibition of the DPPH stable free radical at 10 M compared to the widely recognized standard antioxidant, butylated hydroxytoluene (BHT). Of particular interest, compound 5 demonstrated significant in vitro inhibition of Fe-induced lipid peroxidation in the lipid-rich medium of essential egg yolk (83.99%, IC50 16.07 ± 3.51 μM/mL) in contrast to α-tocopherol (α-ΤΟΗ, 84.6%, IC50 5.6 ± 1.09 μM/mL). Furthermore, the drug-likeness of these BHT analogues was assessed based on Lipinski's "rule-of-five" (RO5), revealing a violation of one parameter (Log P &gt; 5) despite their solubility in protic solvents. The predictive polar surface area (PSA) and absorption percentage (% ABS) data imply a potential capacity for cell membrane penetration. Consequently, these new multipotent antioxidants (MPAOs) hold promise as effective agents for addressing oxidative stress and lipid peroxidation processes.

Recent developments in the design of functional derivatives of edaravone and exploration of their antioxidant activities.

Edaravone, a pyrazalone derivative, is an antioxidant and free radical scavenger used to treat oxidative stress-related diseases. It is a proven drug to mitigate conditions prevailing to oxidative stress by inhibiting lipid peroxidation, reducing inflammation, and thereby preventing endothelial cell death. In recent years, considerable interest has been given by researchers in the derivatization of edaravone by adding varieties of substituents of versatile steric and functional properties to improve its antioxidant and pharmacological activity. This review accounts all the important methods developed for the derivatization of edaravone and the impacts of the structural modifications on the antioxidant activity of the motif.

Azilsartan as a preventive agent against cyclophosphamide-induced testicular injury in male rats.

Cyclophosphamide (CP) is a popular cancer treatment; however, despite its efficacy, it is known to cause harm to the testicles. To mitigate the reproductive damage caused by CP in male rats, we examined the protective effect of azilsartan (AZ) on CP-induced testicular damage. Thirty Sprague-Dawley male rats were equally divided into three groups: normal control group: received 0.5% CMC suspension for 13 days; induction group: received a single dose of 200 mg/kg of CP on day 6 by intraperitoneal (IP) injection, azilsartan group: received azilsartan (4 mg/kg) orally for 5 days followed by a single dose of 200 mg/kg of (CP) on day 6 by IP injection, then azilsartan administered again for 7 days. Animals were sacrificed on day 14, and sperm characteristics, testosterone levels, and testicular histopathology were evaluated. Induction with CP caused a significant reduction in median value compared to normal control in sperm count (12.0 vs. 22.0 × 106/mm3), sperm motility (30 vs. 90%), abnormal sperm (30.32 vs. 14.43%), dead sperm count (32.43 vs. 10.49 × 106/mm3), DNA fragmentation (21.57 vs. 5.49%); meanwhile, azilsartan prevent these effects on median sperm count (17.0 × 106/mm3), sperm motility (70.0%), abnormal sperm (23.19%), dead sperm count (26.17 × 106/mm3), DNA fragmentation (13.81%), and improved plasmatic testosterone levels compared to the CP group and prevented histopathological alterations of the testes. Azilsartan's mitigation of CP's effects suggests it can prevent male rats' reproductive damage caused by CP. One possible explanation for AZ's protective effects is that it inhibits lipid peroxidation and has antioxidant properties.

Pharmacochemical Study of Multitarget Amino Acids' Hybrids: Design, Synthesis, In vitro, and In silico Studies.

Neuro-inflammation is a complex phenomenon resulting in several disorders. ALOX-5, COX-2, pro-inflammatory enzymes, and amino acid neurotransmitters are tightly correlated to neuro-inflammatory pathologies. Developing drugs that interfere with these targets will offer treatment for various diseases. Herein, we extend our previous research by synthesizing a series of multitarget hybrids of cinnamic acids with amino acids recognized as neurotransmitters. The synthesis was based on an In silico study of a library of cinnamic amide hybrids with glycine, γ- aminobutyric, and L - glutamic acids. Drug-likeness and ADMET properties were subjected to In silico analysis. Cinnamic acids were derived from the corresponding aldehydes by Knoevenagel condensation. The synthesis of the amides followed a two-step reaction with 1- hydroxybenzotriazole monohydrate and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride in dry dichloromethane and the corresponding amino acid ester hydrochloride salt in the presence of N,N,-diisopropyl-Nethylamine. The structure of the synthesized compounds was confirmed spectrophotometrically. The new compounds, such as lipoxygenase, cyclooxygenase-2, lipid peroxidation inhibitors, and antiinflammatories, were tested in vitro. The compounds exhibited LOX inhibition with IC50 values in the low μM region). Compounds 18a, 23b, and 11c are strong lipid peroxidation inhibitors (99%, 78%, and 92%). Compound 28c inhibits SLOX-1 with IC50 =8.5 μM whereas 11a and 22a highly inhibit COX-2 (IC50 6 and 5 μM Hybrids 14c and 17c inhibit both enzymes. Compound 29c showed the highest anti-inflammatory activity (75%). The In silico ADMET properties of 14c and 11a support their drug-likeness.

Ballota acetabulosa (L). Bentham: A First-Time GC-MS Analysis and Antioxidant Potential of its Essential Oil.

Ballota acetabulosa native to the Mediterranean region, belonging to the Lamiaceae family, holds significance in folk medicine. Externally, it is applied for treating cuts and burns, while internally, it is utilized to alleviate inflammation, suppress cough, and address gastrointestinal issues. This study aimed to investigate the chemical composition of the essential oil of Ballota acetabulosa and to evaluate the antioxidant capacity of the essential oil, as well as the aqueous and ethanolic extracts of the plant. Essential oil analysis was performed using Gas Chromatography- Mass Spectrometry (GC-MS), while 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and inhibition of lipid peroxidation assays were applied to the essential oil, water, and ethanol extracts of the plant. Spathulenol was found to be the predominant constituent of the essential oil, comprising 25.03% of the oil. Compared to the control group (Propyl gallate for DPPH, IC50 0.109; BHT for inhibition of lipid peroxidation, IC50 0.133), the essential oil was found to have insignificant antioxidant activity (IC50 value 10.395 mg/mL for DPPH, 1.051 mg/mL for inhibition of lipid peroxidation). Moreover, ethanolic extract (IC50 value 1.583 mg/mL for DPPH, 0.029 mg/mL for inhibition of lipid peroxidation) exerted more antioxidant activity than aqueous extract (IC50 value 1.9017 mg/mL for DPPH, 0.161 mg/mL for inhibition of lipid peroxidation). Hitherto, this is the earliest report on the composition and activity of the essential oil Ballota acetabulosa. However, further investigation of different antioxidant capacity assays is suggested to highlight potential variations in mechanisms of action and subsequent results. Everything considered, this study advances the comprehension of the chemical composition and possible therapeutic uses of Ballota acetabulosa, highlighting the need for more research into its uses.

In vitro Cytotoxic and Anti-ROS Potentials of the Aerial Part of Pyrrosia lanceolata on A549 Cells and Cell Free Condition

Antioxidants and cancer are somewhat related to each other. The study was designated to evaluate the antioxidant activities of the aerial parts of Pyrosia lanceolata (P. lanceilata, Fam. Polypodiaceae) and their cytotoxic potential in a lung cancer cell line (A549). The extraction of plant material was performed by using methanol (CME), followed by solvent-solvent partitioning with different solvents. The methanol (CME) and its subsequent fractions (pet-ether PEF, chloroform CHF, ethyl acetate EAF and aqueous AQF fractions) confirmed the presence of alkaloids, flavonoids, phenols, tannins and terpenoids at different degrees. The phenolic and flavonoid content were found to be 69.46, 37.93, 64.61, 126.74 and 60.64 mg of GAE/gm and 33.93, 4.11, 45.68, 146.95, and 44.36 mg of CAE/gm of dried CME, PEF, CHF, EAF and AQF, respectively. The overall antioxidant and iron reduction capacities of CME and all the fractions were in the following order: EAF &gt; CHF &gt; CME &gt; AQF &gt; PEF and EAF &gt; CHF &gt; CME &gt; AQF &gt; PEF, respectively. Among the fractions, EAF significantly scavenged DPPH (IC50 of 1.34 μg/ml) and OH radicals (IC50 of 4.38 μg/ml), which closely resembled those of standard BHT (IC50 of 0.9 μg/ml) and CA (IC50 of 2.73 μg/ml), respectively. Moreover, EAF (IC50 of 14.06 μg/ml) demonstrated a similar effect on inhibiting lipid peroxidation when compared to standard CA (IC50 of 13.86 μg/ml). In addition, CHF (24.25%) and EAF (14.9%) showed a potent cytotoxic effect in A549 cells. Our results suggest that P. lanceolata might be a good source of anticancer potential having antioxidant activity. Bangladesh Pharmaceutical Journal 27(2): 137-148, 2024 (July)

Isolation and Characterization of Antioxidant Peptides from Dairy Cow (Bos taurus) Placenta and Their Antioxidant Activities.

Our preliminary study identified dairy cow placenta extract (CPE) as a mixture of peptides with potent antioxidant activity both in vivo and in vitro. However, the specific antioxidant peptides (AOPs) responsible for this activity were not yet identified. In the current study, we employed virtual screening and chromatography techniques to isolate two peptides, ANNGKQWAEVF (CP1) and QPGLPGPAG (CP2), from CPE. These peptides were found to be less stable under extreme conditions such as high temperature, strong acid, strong alkali, and simulated digestive conditions. Nevertheless, under normal physiological conditions, both CP1 and CP2 exhibited significant antioxidant properties, including free-radical scavenging, metal chelating, and the inhibition of lipid peroxidation. They also up-regulated the activities of intracellular antioxidant enzymes in response to hydrogen-peroxide-induced oxidative stress, resulting in reduced MDA levels, a decreased expression of the Keap1 gene and protein, and increased levels of the Nrf2 and HO-1 genes and proteins. Furthermore, CP1 demonstrated superior antioxidant activity compared to CP2. These findings suggest that CP1 and CP2 hold potential for mitigating oxidative stress in vitro and highlight the efficacy of virtual screening as a method for isolating AOPs within CPE.