Potent Antioxidant Activity Research Articles

Abstract 7309: Edible mushroom derived antioxidant, vialinin A, prevents melanoma growth and invasion

Abstract Melanoma is the second leading invasive cancer with a greater capacity to invade and metastasize. Increased oxidative stress has been shown to be involved in melanoma growth and spread. Several antioxidants, vitamins, and other phytochemicals have been shown to prevent melanoma cancer growth. However, the chemopreventive efficacy of vialinin-A, an edible mushroom-derived p-terphenyl antioxidant, on cancer growth and invasion is unknown. We, therefore, hypothesized that with its potent anti-oxidative and anti-inflammatory actions, vialinin-A could prevent melanoma cell growth and invasion. B16-F10 melanoma cells were treated without or with various concentrations of vialinin-A. The cell viability was determined by MTT assay and apoptosis by annexin-V staining. Our results suggest that vialinin-A prevents melanoma cell growth in a dose-dependent manner. Vialinin-A also prevents the invasion and migration of melanoma cells. Further, vialinin-A prevents the generation of reactive oxygen species and promotes apoptosis of B16-F10 cells. In addition, vialinin-A increases the activation of caspase-3 and cleavage of PARP protein. Vialinin-A also regulated the expression of various anti-apoptotic, pro-apoptotic, and inflammatory markers in melanoma cells. In conclusion, our results suggest that vialinin-A, through regulating oxidative stress-modulated apoptotic pathways, could prevent melanoma cell growth and invasion and has potential chemopreventive properties. Citation Format: Alexandria Vo, Amber Zafar. Edible mushroom derived antioxidant, vialinin A, prevents melanoma growth and invasion [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 7309.

Gamma globulin binding of hinokiflavone with anti-osteoporosis effects: A mechanistic study

Oxidative stress can trigger apoptosis and associated reduction of osteoblast activity. Hinokiflavone (HNK) with a biflavonoid-based structure might show potent antioxidant activity. However, before the application of this compound as a promising therapeutic bioactive material, its interaction with blood proteins should be investigated to further reveal its pharmacokinetic and pharmacodynamic properties. Therefore, in this paper, the interaction of HNK with γ-globulin, one of the main blood proteins, was assessed. Then, the antioxidant properties of HNK against H2O2-induced osteoblast cytotoxicity in MC3T3-E1 cells were assessed. It was shown that HNK can potentially bind to γ-globulin mostly with the aid of hydrophilic forces, with a slight effect on the protein structure. It was then determined that HNK significantly recovered cell survival and alkaline phosphatase (ALP) activity and collagen-I content in MC3T3-E1 cells exposed to H2O2. In addition, HNK decreased the production of intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) in MC3T3-E1 cells triggered by H2O2. Finally, HNK was shown to control the apoptosis induction in MC3T3-E1 cells triggered by H2O2 mediated by regulation of Bax, Bcl-2 and caspase-3. Taken together, these data demonstrated that HNK with promising blood protein binding properties can show significant protective effects in MC3T3-E1 cells mediated by inhibition of osteoblast dysfunction, oxidative stress, and apoptosis.

Antioxidant and enzyme inhibitory potentials of phytochemicals isolated from Dioclea reflexa (Hook F.) stem: in-vitro and in-silico studies

The objective of the study was to isolate and characterize phytochemicals from the stem extract of D. reflexa and investigate their biochemical activities. Five flavonoids together with two terpenoids, were isolated. Their structures were identified using 1D and 2D nuclear magnetic resonance (NMR) and mass spectroscopic techniques in combination with circular dichroism (CD) spectroscopy, as well as comparisons with published data. The in vitro reactive oxygen species scavenging potential of the compounds was investigated. The lipoxygenase and urease inhibitory potential of the compounds were tested using in vitro and in silico methods. Compound 1 and 2 exhibited potent antioxidant activity with lower IC50 values of 38.5 ± 0.25 and 39.5± 0.14 μM respectively compared with the standard used (BHA IC50 value = 39.5± 0.14) in DPPH assay. Compound 1 and 2 also exhibit good reducing ability and superoxide radical scavenging activity reflected by IC50 value 44.6 ± 0.30 and 48.5 ± 0.16 respectively compared with BHA (IC50 45.6 ± 0.54). Compound 2 and 3 showed significant inhibitory effect against urease with IC50 values 26.2 ± 0.29 μM and 36.5 ± 0.37 μM respectively, while compound 4 with IC50 value 33.3 ± 0.74 μM is the most active against lipoxygenase. All the seven compounds showed varying degrees of binding affinity against the targets with compounds 1–5 having the better docking score compared with the co-crystalized ligands of both lipoxygenase and urease. The density functional theory reveals the replicate of the transitional state between the compounds and their respective receptor and stability of the compounds was predicted from the energy gap (ELUMO – EHOMO). These compounds are potential drug against stomach ulcers, inflammation and oxidative stress associated diseases. It is also worth mentioning that the complete assignments of NMR data 1 and 2 were reported for the first time in this study.

Chemodiversity of Arctic Plant Dryas oxyodonta: LC-MS Profile and Antioxidant Activity

Dryas oxyodonta Yuz. is a perennial evergreen shrub from the Rosaceae family. D. oxyodonta thrives in subalpine and subarctic regions, as well as in highlands spanning from Central Asia to Siberia and Mongolia. Owing to a lack of information on its chemical composition, we conducted qualitative and quantitative chromatographic analyses on extracts from the leaves and flowers of D. oxyodonta sourced from various Siberian habitats. Employing high-performance liquid chromatography with photodiode-array detection and electrospray ionization triple-quadrupole mass spectrometric detection, we identified 40 compounds, encompassing gallotannins, hydroxycinnamates, procyanidins, catechins, flavonoids, and triterpenes. All Siberian populations of D. oxyodonta exhibited a notable abundance of phenolic compounds. Furthermore, we identified rare glycosides, such as sexangularetin and corniculatusin, as potential markers of the chemodiversity within the Dryas genus. Extracts from the flowers and leaves were effective scavengers of free radicals, including DPPH•, ABTS•+−, O2•−, and •OH radicals. Our findings unequivocally establish D. oxyodonta as a rich source of phenolic compounds with potent antioxidant activity, suggesting its potential utility in developing novel functional products.

Evaluation of antioxidant, antidiabetic and antiobesity potential of phenylpropanoids (PPs): Structure-activity relationship and insight into action mechanisms against dual digestive enzymes by comprehensive technologies

Phenylpropanoids (PPs), a group of natural compounds characterized by one or more C6-C3 units, have exhibited considerable potential in addressing metabolic disease. However, the comprehensive investigation on the relationship of compound structures and involved activity, along with the action mechanisms on the drug target is absent. This study aimed to evaluate the antioxidant and inhibitory activities of 16 PPs against two digestive enzymes, including α-glucosidase and pancreatic lipase, explore the structure–activity relationships and elucidate the mechanisms underlying enzyme inhibition. The findings revealed the similarities in the rules governing antioxidant and enzyme inhibitory activities of PPs. Specifically, the introduction of hydroxyl groups generally exerted positive effects on the activities, while the further methoxylation and glycosylation were observed to be unfavorable. Among the studied PPs, esculetin exhibited the most potent antioxidant activity and dual enzymes inhibition potential, displaying IC50 values of 0.017 and 0.0428 mM for DPPH and ABTS radicals scavenging, as well as 1.36 and 6.67 mM for α-glucosidase and lipase inhibition, respectively. Quantification analysis indicated esculetin bound on both α-glucosidase and lipase successfully by a mixed-type mode. Further analyses by UV–Vis, FT-IR, fluorescence spectra, surface hydrophobicity, SEM, and molecular docking elucidated that esculetin could bind on the catalytic or non-catalytic sites of enzymes to form complex, impacting the normal spatial conformation for hydrolyzing the substrate, thus exhibiting the weakened activity. These results may shed light on the utilization value of natural PPs for the management of hyperglycemia and hyperlipemia, and afford the theoretical basis for designing drugs with stronger inhibition against the dual digestive enzymes based on esculetin.

Effects of gossypin on acetaminophen-induced hepatotoxicity in mice

Liver injury from paracetamol (acetaminophen) (APAP) is common worldwide. To prevent intoxication with a drug with high poisoning, treatment can be made possible with an easily accessible and harmless substance. This study aimed to investigate the hepatoprotective ef-fects of Gossypin (GOS) in mice exposed to an overdose of APAP -the possible mechanism of action. Specifically, serum [alanine aminotransferase (ALT), aspartate transaminase (AST), and hepatic biochemical parameters (glutathione (GSH), malondialdehyde (MDA) and super-oxide dismutase (SOD)] were evaluated. Protein and mRNA levels of inflammatory, apoptot-ic, and cytochrome factors, including TNF-α, IL-1β, IL-6, NF-kB, and CYP2E1, were ana-lyzed using real-time PCR. Pretreatment with GOS significantly reduced APAP-induced he-patic injury via oxidative stress. Along with potent antioxidant activity, GOS promoted APAP hepatic detoxification by regulating AST, ALT, GSH, MDA, and SOD activities and mRNA levels of the cytochrome CYP2E1 gene. The anti-inflammatory activity of GOS in-creases its production. TNF-α, IL-1β and IL-6, through possible NF-kB blockade, are also responsible for its hepatoprotective effect. Taken together, GOS has the potential to be devel-oped as a preventive agent to be administered to patients suffering from APAP overdose.

A study on the anti-senescent effects of flavones derived from Prinsepia utilis Royle seed residue

Ethnopharmacological relevancePrinsepia utilis Royle, also known as the Anas fruit, is a unique perennial woody oil plant from Yunnan Province, China. In the ancient texts of Dongba sutras and Yunnan Southern Materia Medica, it has been documented that the local Naxi, Tibetan, and Mosuo communities extensively utilize the root and leaf fruits of green thorns for various purposes. These include treating mild-to-moderate specific dermatitis, moisturising the skin, providing protection against UV damage, aiding childbirth in pregnant women, safeguarding stomach health, reducing the risk of arteriosclerosis, and delaying aging. Aim of the studyIn this study, leftover residues from oil extraction were efficiently reused, and flavonoids were identified during subsequent extraction and separation processes. The anti-senescent effects of flavonoids in P. utilis Royle have not been systematically studied. Therefore, the objective of this study was to explore the anti-senescent properties of the flavonoids obtained from P. utilis Royle. MethodsFirst, HPLC and other analytical techniques were used to identify the components of the P. utilis Royle flavonoid (PURF). Next, DPPH, hydroxyl radicals, superoxide anion O2−, collagenase, and elastase were initially detected using in vitro biochemical assays. To examine its antioxidant properties, a zebrafish model was used, and to confirm its anti-senescent effects, a d-galactose-induced mouse aging model was employed. The anti-senescent mechanism of PURF was examined using a natural senescence HFF model. Furthermore, the anti-senescent target was confirmed using a 3D full T-Skin™ model. ResultsIn vitro biochemical assays demonstrated that flavones exhibited potent antioxidant activity and anti-senescent potential by inhibiting DPPH, hydroxyl radicals, superoxide anion O2−, collagenase, and elastase. It significantly enhanced the antioxidant effect on zebrafish while suppressing ROS and inflammatory injury, up-regulating COL1A1, COL3A1, AMPK, and mTOR gene expression and down-regulating MMP-9, TGF-β, p21, and p16 gene expression suggesting its potential anti-senescent ability. Findings from the D-galactose-induced aging mouse model showed that PURF greatly increased SOD levels, while simultaneously decreasing HYP and MDA levels. In addition, when PURF was given to the HFF cell and 3D full T-Skin™ model, consistent trends were observed in gene and protein expression, with up-regulation of COL1A1, COL3A1, AMPK, and mTOR genes and down-regulation of TGF-β, MMP-1, MMP-9, p21, and p16 genes. Therefore, these preliminary findings indicate that flavones can modulate AMPK/mTOR/TGF-β signalling pathways to exert its influence. ConclusionThe kernel residue of natural P. utilis Royle oil extracted from Yunnan province was previously considered agricultural waste, but we successfully extracted and isolated its flavonoid components. Our preliminary studies demonstrated its potential as an environmentally friendly anti-senescent raw material.

Enzyme-Assisted Ultrasonic Extraction and Antioxidant Activities of Polysaccharides from Schizochytrium limacinum Meal.

Enzyme-assisted ultrasonic extraction (EAUE) was utilized and optimized for extracting polysaccharides from Schizochytrium limacinum meal (SLMPs) via the response surface methodology. The optimal EAUE conditions were determined as follows: enzyme concentration at 5.18%, ultrasonic temperature at 53 °C, ultrasonic duration of 40 min, ultrasonic power at 60 W, and a liquid-to-material ratio of 34 mL/g, achieving a polysaccharide extraction yield of 11.86 ± 0.61%. The purified polysaccharide component, SLMP1-1, isolated using DEAE Sepharose Fast Flow and Sephadex G-100 columns, exhibited potent antioxidant activity. SLMP1-1, with a molecular weight of 25.5 kDa, comprises glucose, mannose, arabinose, and galactose in a molar ratio of 16.39:14.75:1:693.03. 1H NMR analysis revealed the α configuration of SLMP1-1. Antioxidant assessments, including DPPH, ABTS, and ferric ion reduction assays, were detected with inhibitory values at 21.82-82.98%, 38.21-98.46%, and 3.30-20.30% at 0.2-1.0 mg/mL. This confirmed the effective antioxidant capacity of SLMP1-1, which is notably enhanced post oral and gastric digestion. The findings suggest that polysaccharides extracted from Schizochytrium limacinum meal hold significant promise as natural antioxidants.

Anti-inflammatory, Antioxidative, and Moisturizing Effects of Oxyceros horridus Lour. Ethanol Extract in Human Keratinocytes via the p38 Signaling Pathway.

Skin is the largest and outermost organ in the human body; it serves as a vital defense mechanism against various external threats. Therefore, it is crucial to maintain its health through protection against harmful substances and adequate moisture levels. This study investigates the anti-inflammatory, antioxidant, and moisturizing properties of Oxyceros horridus Lour. (Oh-EE) in human keratinocytes. Oh-EE demonstrates potent antioxidant activity and effectively protects against oxidative stress induced by external stimuli such as UVB radiation and H2O2. Additionally, it exhibits significant anti-inflammatory effects proven by its ability to downregulate the expression of pro-inflammatory cytokines, namely COX-2 and IL-6. The study also explores the involvement of the AP-1 pathway, highlighting the ability of Oh-EE to suppress the expression of p38 and its upstream regulator, MKK3/6, under UVB-induced conditions. Interestingly, Oh-EE can activate the AP-1 pathway in the absence of external triggers. Furthermore, Oh-EE enhances skin moisture by upregulating the expression of key genes involved in skin hydration, namely HAS3 and FLG. These findings underscore the potential of Oh-EE as a versatile ingredient in skincare formulations, providing a range of skin benefits. Further research is warranted to comprehensively understand the underlying mechanisms through which Oh-EE exerts its effects.

Superior performance of biocomposite nanoparticles PLGA-RES in protecting oocytes against vitrification stimuli.

Irreversible cryogenic damage caused by oocyte vitrification limits its widespread use in female fertility preservation. In recent years, nanoparticles (NPs) have gained great attention as potential alternatives in protecting oocytes against cryoinjuries. In this paper, a novel composite nanoparticle, poly (lactic-co-glycolic acid)-resveratrol (PLGA-RES) was designed to improve the biocompatibility and sustained release properties by encapsulating natural antioxidant RES into PLGA NPs. Firstly, biotoxicity and oxidation resistance of PLGA-RES were determined, and the results showed that PLGA-RES had nontoxic effect on oocyte survival during in vitro maturation (IVM) (97.08% ± 0.24% vs. 98.89% ± 1.11%, p > 0.05). Notably, PLGA-RES even increased maturation (65.10% ± 4.11% vs. 52.85% ± 2.87%, p < 0.05) and blastocyst rate (56.13% ± 1.36% vs. 40.91% ± 5.85%, p < 0.05). Moreover, the reduced reactive oxygen species (ROS) level (13.49 ± 2.30 vs. 34.07 ± 3.30, p < 0.01), increased glutathione (GSH) (44.13 ± 1.57 vs. 37.62 ± 1.79, p < 0.01) and elevated mitochondrial membrane potential (MMP) levels (43.10 ± 1.81 vs. 28.52 ± 1.25, p < 0.01) were observed in oocytes treated with PLGA-RES when compared with that of the control group. Subsequently, the role of PLGA-RES played in oocytes during vitrification was systematically evaluated. The results showed that the addition of PLGA-RES during vitrification and thawing significantly improved the survival rate (80.42% ± 1.97% vs. 75.37% ± 1.3%, p < 0.05). Meanwhile, increased GSH (15.09 ± 0.86 vs. 14.51 ± 0.78, p < 0.01) and mitochondrial membrane potential (22.56 ± 3.15 vs. 6.79 ± 0.60, p < 0.01), decreased reactive oxygen species levels (52.11 ± 2.95 vs. 75.41 ± 7.23, p < 0.05) and reduced mitochondrial abnormality distribution rate (25.00% ± 0.29% vs. 33.33% ± 1.15%, p < 0.01) were assessed in vitrified MII oocytes treated with PLGA-RES. Furthermore, transcriptomic analyses demonstrated that PLGA-RES participated in endocytosis and PI3K/AKT/mTOR pathway regulation, which was verified by the rescued expression of ARRB2 and ULK3 protein after PLGA-RES treatment. In conclusion, PLGA-RES exhibited potent antioxidant activity, and could be used as an efficacious strategy to improve the quality of vitrified oocytes.

Echinacea purpurea root extract mitigates hepatotoxicity, genotoxicity, and ultrastructural changes induced by hexavalent chromium via oxidative stress suppression

Environmental and occupational exposure to hexavalent chromium (CrVI) is mostly renowned as a possible hepatotoxic in mammals. Echinacea purpurea (L.) Moench, a phenolic-rich plant, is recurrently used for its therapeutic properties. Therefore, this investigation was done to explore whether E. purpurea (EP) root extract would have any potential health benefits against an acute dose of CrVI-induced oxidative damage and hepatotoxicity. Results revealed that GC–MS analysis of EP root extract has 26 identified components with a significant amount of total phenolic and flavonoid contents. Twenty-four Male Wistar rats were divided into four groups: control, EP (50 mg/kg BW/day for 21 days), CrVI (15 mg/kg BW as a single intraperitoneal dosage), and EP + CrVI, respectively. Rats treated with CrVI displayed a remarkable rise in oxidative stress markers (TBARS, H2O2, PCC), bilirubin, and lactate dehydrogenase activity, and a marked decrease in enzymatic and non-enzymatic antioxidants, transaminases, and alkaline phosphatase activities, and serum protein level. Also, CrVI administration induced apoptosis and inflammation in addition to histological and ultrastructural abnormalities in the liver tissue. The examined parameters were improved significantly in rats pretreated with EP and then intoxicated with CrVI. Conclusively, EP had a potent antioxidant activity and could be used in the modulation of CrVI-induced hepatotoxicity.

Astaxanthin treatment reduces kidney damage and facilitates antioxidant recovery in lithium-intoxicated rats

ObjectiveThis study aimed to evaluate the protective effects of astaxanthin against lithium-induced nephrotoxicity, focusing on histopathological changes, oxidative stress modulation, and alteration in the expression of key proteins related to apoptosis and inflammation. MethodsIn this study, 56 male rats were utilized and divided into experimental groups subjected to lithium-induced nephrotoxicity, with and without astaxanthin treatment, over 14 and 28 days. The parameters assessed included oxidative stress markers (MDA, GSH, SOD), protein expression levels of BCL-2, BAX, TNF- α, PI3K, NF-κ B-p65, IL-1β, and comprehensive histopathological examinations to evaluate the integrity of renal tissue. ResultsLithium exposure led to significant renal damage, as evidenced by histological distortions in renal architecture, increased oxidative stress indicated by elevated MDA levels, and dysregulated expressions of apoptotic and inflammatory proteins. Notably, histopathological analysis revealed glomerular and tubular degeneration in lithium-treated groups. Astaxanthin treatment effectively mitigated these effects, demonstrating its efficacy in reducing lipid peroxidation, rebalancing apoptotic proteins, suppressing pro-inflammatory cytokines, and preserving renal histological structure. The concurrent use of lithium and astaxanthin showed a considerable amelioration of lithium-induced damage, suggesting astaxanthin's role in attenuating the nephrotoxic effects of lithium, both at a molecular and structural level. ConclusionAstaxanthin demonstrates significant renoprotective effects against lithium-induced nephrotoxicity, suggesting its utility as an effective adjunctive therapy. Through its potent antioxidative, anti-inflammatory, and anti-apoptotic actions, astaxanthin effectively reduces renal damage associated with lithium treatment, underscoring its potential for enhancing renal health in patients receiving lithium therapy.

Carotenoid content, phytochemical screening, and antioxidant potential of Kantutay (Lantana camara L.), Katuray (Sesbania grandiflora L.), and Blue Ternate (Clitoria ternatea L.) flowers in the Philippines

Natural product chemistry plays a pivotal role in drug discovery and development. This study investigated the phytochemical profiles and antioxidant capacities of three prominent Philippine plants: Blue ternate (Clitoria ternatea), Kantutay (Lantana camara), and Katuray (Sesbania grandiflora). The primary aim is to provide a comprehensive assessment of their bioactive constituents and evaluate their potential for pharmacological applications. Phytochemical screening identified a diverse array of compounds, including flavonoids, tannins, glycosides, terpenoids, and other major chemical constituent classes, highlighting their therapeutic potential. The pigment analysis revealed substantial variations, with Blue ternate exhibiting the highest concentration, suggesting it as a promising source of carotenoids. Thin Layer Chromatography (TLC) and chlorophyll analysis further revealed distinct compound profiles. Total Phenolic Content (TPC) analysis and the DPPH radical scavenging method marked Blue ternate to have the highest phenolic content and the most potent antioxidant activity among the plant samples. These findings collectively emphasize the significant therapeutic potential of these plants, warranting further exploration for pharmaceutical development.

Ascorbic acid-mediated selenium nanoparticles as potential antihyperuricemic, antioxidant, anticoagulant, and thrombolytic agents

Abstract Selenium (Se) is an important trace element that is involved in controlling oxidative stress and inflammatory disorders. Gouty arthritis is the inflammation and pain within the joints and tissues caused due to the accumulation of monosodium urate (MSU) crystals. This study aimed to investigate the antigout, antioxidant, anticoagulant, and thrombolytic potential of ascorbic acid-mediated Se nanoparticles (A-SeNPs). Different analytical techniques were used to investigate the formation of A-SeNPs. The antigout potential of the nanoparticles was carried out using MSU crystal dissolution, uric acid (UA) degradation assay, and xanthine oxidase inhibition (XOI). A-SeNPs exhibited excellent antihyperurecemic activity in a concentration-dependent manner. It was observed that at the tested concentration of 20 mg·mL−1, the A-SeNPs demonstrated significant breakage and dissolution of MSU crystals and resulted in UA degradation of 67.76%. Similarly, A-SeNPs resulted in 76% XOI with an excellent IC50 of 140 µg·mL−1. Furthermore, considerable antioxidant activity was noted for the A-SeNPs as evaluated with multiple antioxidant assays. Finally, the NPs were found to have significant anticoagulant and thrombolytic potential. Thus, it was concluded that A-SeNPs have potent antihyperuricemic, antioxidant, anticoagulant, and thrombolytic activities, making them an ideal choice for future biomedical applications.

In vitro antimicrobial, antioxidant and molecular study of Nostoc punctiforme isolated from the rice field

Cyanobacteria are photosynthetic prokaryotes and are reservoir of bioactive compounds having substantial antimicrobial and antioxidant activity. They serve as a rich source of structurally novel and biologically active metabolites, holding great potential for various pharmaceutical applications. The aim of this study is to investigate in vitro antimicrobial and antioxidant activities of the extracts of Nostoc punctiforme, a filamentous heterocystous cyanobacterium predominant in the rice fields of Lakhanpur (Bargarh District), Odisha. The heterocystous cyanobacteria was collected from rice field and identified by means of morphological and molecular approach (Nostoc punctiforme Jbr02). Subsequently, in vitro antimicrobial and antioxidant activity was assayed using acetone, methanol, and benzene extract. The cyanobacterial extracts established important antimicrobial actions against bacterial and fungal pathogens with significant MIC values from 62.5 to 500 μg/ml. The methanolic extract displayed better inhibitory activities against both V. Cholerae and P. verrucosun with the MIC value 62.5μg/ml while no such activity was recorded in benzene extract against B. subtilis, A. niger and F. oxysporum pathogens. The antioxidant study, depicted that the methanolic extract showed relatively higher antiradical activity of IC50 542±0.012 μg/ml among the three solvents. The Ferric reducing assay result was also maximum in methanolic extract (0.478±0.78) as compared to benzene and acetone extract. These findings infer that Nostoc punctiforme has potential antimicrobial and antioxidant activity, unveiling its potential as a valuable source of bioactive compounds. Thus, N. punctiforme in specific and cyanobacteria in general are one of the most promising candidates for commercial applications.

Evaluation of antioxidant and antibacterial properties of dehydrocostus lactoneisolated from Echinops kebericho root.

Echinops kebericho, an endemic plant to Ethiopia, traditionally used to treat infectious as well as noninfectious diseases. The primary objective of this study was isolating dehydrocostus lactone (DHCL) from E. kebericho and evaluating antibacterial activities on selected human pathogenic bacteria. Extraction method used in this study was maceration. Based on the bioassay information methanol extract of the root of E. kebericho was subjected to column chromatography on silica gel by increasing solvent gradients to isolate DHCL. Optimized amount isolation of DHCL was done by dissolving methanol crude extract by hexane followed by recrystallization at room temperature in the dark place. Different concentrations of the extract were subjected by disc diffusion method against tested bacterial species and antioxidant activity test. The phytochemical analysis of E. kebericho revealed a high presence of terpenoids, which are diverse natural compounds known for their antimicrobial and antioxidant properties. This suggests that terpenoids contribute significantly to the pharmacological effects of E. kebericho. In antibacterial testing, Escherichia coli was the most sensitive bacterium among all extracts and concentrations. The methanol extract displayed higher antioxidant activity compared to ethyl acetate and hexane extracts, indicating a higher concentration of antioxidant compounds. Notably, the isolated compound DHCL showed promising activity against tested pathogens and significant antioxidant activity. The higher activity of DHCL compared to the crude extracts suggests its responsibility for the observed effects, indicating that the isolation and purification process may have concentrated its beneficial properties. These findings highlight the potential of E. kebericho and DHCL as sources of bioactive compounds for therapeutic applications. All tested extracts and pure compound showed higher inhibition than positive controls in both bioassay. DHCL the principal bioactive component in the root extract of the plant and it displayed potent antibacterial and antioxidant activity.

Synthesis, Characterization, and Biological Studies of Metal Complexes of Dicoumarol Derivatives of Gatifloxacin

Copper(II) complexes were prepared using gatifloxacin and dicoumarin derivatives to investigate their biological activities and to conduct X-ray studies. The complexes were synthesized through classical thermal methods. Biologically potent ligands were synthesized by the reaction of dicoumarin derivative with different aldehydes in ethanol. Cu(II) complexes were formed by mixing ethanolic solution of ligands and gatifloxacin with metal solutions in a 1:1 mole ratio. The structures of the dicoumarin derivatives and their Cu(II) complexes were analyzed by infrared, 1H NMR, 13C NMR, and mass spectrometry. The thermal behavior of the new mixed ligand Cu(II) complexes was investigated by thermogravimetric, fast atom bombardment (FAB) mass, and X-ray analysis. The iron-reducing antioxidant potential (FRAP) (antioxidant activity) of all compounds was evaluated. All the synthesized compounds were screened for antibacterial activity against Escherichia coli; Pseudomonas aeruginosa; Streptococcus pyogenes; minimum inhibitory concentration values for Candida albicans; and Aspergillus niger were determined using the Luria Broth dilution method. The ligands and their complexes were evaluated for antioxidant and antibacterial activity in vitro. The complexes exhibited better results than their respective counterparts.. KEYWORDS :Antimicrobial, Antioxidant, Fast atom bombardment mass, Thermal analysis, Thermo gravimetric analysis, X-ray.

Toxicity and therapeutical impacts of Bee venom (Apis mellifera L.) on Nile tilapia juvenile (Oreochromisniloticus)

Bee venom (BV) has been widely studied for its therapeutic properties in various medical applications. However, its effects on aquatic organisms, particularly Nile tilapia (Oreochromis niloticus), remain poorly understood, particularly concerning toxicity and therapeutic impacts. This study investigated the effects of bee venom (BV) injection on Nile tilapia (O. niloticus) by examining growth, feed efficiency, biometric parameters, whole-body chemical analysis, and the activity of antioxidant enzymes in the liver. Nile tilapia juveniles were injected with BV at doses of 0, 3, 6, 9, and 12 mg/kg of fish weight. Observations were made on the 14th day post-injection (DPI). No significant differences were found in growth, feed utilization, survival rate, biometric indices, and whole-body composition among the BV dosage groups. Similarly, the activity of intestinal enzymes (amylase, protease, and lipase) showed no significant changes. However, the study revealed a time-dependent response of antioxidant enzymes (SOD, CAT, and GPx) in the liver, with activity peaks on the 4th and 6th DPI. On the 14th DPI, fish injected with BV at doses of 3, 6, and 9 mg/kg exhibited higher antioxidant enzyme activities compared to the control and the highest dosage group (12 mg/kg). These results imply the presence of potential adaptive antioxidant activity and a favorable influence on the health and immune responses of Nile tilapia following BV injection. Notably, the effects appear to vary with the dose, influencing both antioxidant enzyme activities and immunity. Further research is warranted to explore the long-term effects of BV exposure and its potential therapeutic applications in aquaculture.

Chemical composition and potential antioxidant, anti-inflammatory, and analgesic efficacy of Cistus albidus L.

This study aims to assess the chemical composition of the aqueous extract of Cistus albidus L. leaves, as well as the potential of aqueous and hydroethanol extracts of the leaves and seeds as analgesic, anti--inflammatory, and antioxidant agents. The contents of phenolics and inorganic constituents were determined in C. albidus seeds and leaves; antioxidant capacity was assessed by 3 complementary and diverse tests. The carrageenan-induced paw edema technique was used to investigate the anti-inflammatory effect in vivo, and albumin denaturation to evaluate the anti-inflammatory effect in vitro. The acetic acid-induced contortion test, the tail-flick test, and the plantar test were used to assess the analgesic effi cacy in vivo. Chemical analysis was performed by UPLC-MS/MS to quantify several phenolic compounds including catechin (1,627.6 mg kg-1), quercitrin (1,235.8 mg kg-1) and gallic acid (628. 2 mg kg-1). The ICP analysis revealed that potassium and calcium were the main inorganic components in the seeds and leaves of C. albidus. The hydroethanolic extract of the leaves showed the highest content of polyphenols/flavonoids, whereas the highest value of proantho cyanidins was detected in the aqueous extract of the seeds. All extracts showed potent antioxidant activity related to different phenolic compounds (quercetin, gallic acid, astragalin, catechin, and rutin). The aqueous extract of the leaves strongly inhibited paw edema (76.1 %) after 6 h of treatment and showed maximal inhibition of protein denaturation (191.0 µg mL-1 for 50 % inhibition) and analgesic activity in different nociceptive models. The presented data reveal that C. albidus extracts potentially show antioxidant, anti-inflammatory, and analgesic activities that could confirm the traditional use of this plant.

Validating the protective role of orange and tangerine peel extracts foramending food safety against microorganisms’ contamination using molecular docking

Latest studies indicated that agro-food wastes are considered renewable sources of bioactive compounds. This investigation aimed to utilize natural extracts of citrus peels as antimicrobial and anti-aflatoxigenic agents for food safety. The bioactivity of two citrus peels was assessed by total phenolic, flavonoids, and antioxidant activity. Nanoemulsions were manufactured using high-speed homogenization. The mean particle size of the nanoemulsions ranged from 29.41 to 66.41 nm with a polydispersity index of 0.11–0.16. The zeta potential values ranged from −14.27 to −26.74 mV, indicating stability between 81.44% and 99.26%. The orange peel extract showed the highest contents of total phenolic and flavonoids compared to the other extracts and nanoemulsions (39.54 mg GAE/g and 79.54 mg CE/100 g, respectively), which agreed with its potential antioxidant activity performed by DPPH free radical–scavenging and ABTS assays. Chlorogenic, caffeic, ferulic, and catechin were the dominant phenolic acids in the extracts and nanoemulsions, while quercitrin, rutin, and hesperidin were the most abundant flavonoids. Limonene was the major volatile component in both oils; however, it was reduced dramatically from 92.52% to 76.62% in orange peel oil and from 91.79 to 79.12% in tangerine peel oil. Consistent with the differences in phenolics, flavonoids, and volatiles between orange and tangerine peel extracts, the antibacterial properties of orange extracts had more potential than tangerine ones. Gram-positive bacteria were more affected by all the examined extracts than Gram-negative ones. The antifungal activity of orange extract and nanoemulsion on seven fungal strains from Aspergillus spp had more potential than tangerine extracts. Additionally, using a simulated media, the orange peel extract and its nanoemulsion had a more anti-aflatoxigenic influence. Molecular docking confirmed the high inhibitory action of flavonoids, especially hesperidin, on the polyketide synthase (−9.3 kcal/mol) and cytochrome P450 monooxygenase (−10.1 kcal/mol) key enzymes of the aflatoxin biosynthetic mechanism.