Potent Free Radical Scavenging Activity Research Articles

Tangerine fruit peel extract mediated biogenic synthesized silver nanoparticles and their potential antimicrobial, antioxidant, and cytotoxic assessments

Abstract The utilization of plant bioactive composites has concerned substantial attention due to their possible use in the development of novel antibiotics, containing the environmentally sustainable synthesis of nanoparticles. In the current study, a green and eco-friendly process was employed to synthesize silver nanoparticles (Ag-NPs) and to evaluate their anti-bacterial, anti-oxidant, and anti-cancer potentials. The characterization of the Ag-NPs involved UV-vis spectroscopy, Fourier-transform infrared spectroscopy (FTIR), energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM). The UV-vis spectrum of Ag-NPs was 437 nm. The FTIR absorption peaks detected at 685.48 cm−1 confirmed their characteristics. The FESEM displayed that Ag-NPs have an average size of 30 nm. The TEM revealed that the Ag-NPs have an irregular spherical shape with 16 nm size distribution. The XRD results provided a strong indication that the green synthesized Ag-NPs was of high purity with crystalline nature. The anti-bacterial properties were investigated at different concentrations for both the ethanolic tangerine peel extract and Ag-NPs. The results of anti-bacterial activity showed that 100 µg·mL−1 was potent concentration, but the Ag-NPs were more effective than the ethanolic tangerine peel extract. For the ethanolic extract, the inhibition zone was 17.50 ± 0.20 mm for K. pneumoniae and 14.40 ± 0.20 mm for B. cereus. For the Ag-NPs, the inhibition zone was 25.50 mm for K. pneumoniae and 20.50 mm for B. cereus. Furthermore, the antioxidant examination revealed more potent free radical scavenging activity of the Ag-NPs than the ethanolic peel extract alone. The ethanolic extract ranged 46–77% while the Ag-NPs ranged 57–88%. Additionally, the anti-proliferative of the Ag-NPs against the lung cancer cell line (A549) was more potent than the ethanolic extract alone. The cytotoxic activity was 90.03% and 78.50%, respectively. The anti-proliferative effect of Ag-NPs is attributed to cell death, induced apoptosis, and enhanced generation of reactive oxygen species. Our findings highlight the potential and further utilization of Ag-NPs in medicinal applications particularly for cancer therapeutics.

Exploring the Potential of Novel 4-Thiazolidinone Derivatives as Dual Anti-inflammatory and Antioxidant Agents: Synthesis, Pharmacological Activity and Docking Analysis

A series of 4-thiazolidinone was synthesized and characterized by means of TLC, melting point, and spectral data like IR, 1H NMR, and Mass spectra. The anti-inflammatory activity of the synthesized compounds was determined via in vivo studies. The antioxidant properties of the synthesized compounds were determined by carrageenan-induced rat paw edema model. The synthesized compounds (A1-A14) showed significant anti-inflammatory and antioxidant activities. The most promising results for both antioxidant and antiinflammatory activity were exhibited by compound A8 which may emerge as a potent anti-inflammatory agent with potential free radical scavenging activity. Molecular docking studies were carried out to determine the interaction of compounds into the active site of COX-2 inhibitor (PDB ID: 3LN1), which suggested compound A8 to have the best docking score by showing interactions with ASP483 and LYS478.

Bioassay-guided fractionation and in vitro and in silico biological activities of 2,4-di-tert-butylphenol isolated from Nocardiopsis sp. strain LC-8

In this study, an actinomycete strain was isolated from freshwater soil sediments to produce bioactive metabolite with a broad array of biological activities. Initially, preliminary antibacterial screening of isolate was performed by perpendicular streak method which showed the growth inhibition of all tested bacterial pathogens. Based on the culture characteristics, morphological identification, and 16S rRNA gene sequencing, the isolate was identified as Nocardiopsis sp. strain LC-8. Ethyl acetate extract of strain LC-8 showed potential antibacterial activity against tested bacterial pathogens with a maximum zone of inhibition of 16.98±0.57 mm against Staphylococcus aureus. After column chromatography, fraction 2 (F2) of the extract exhibited prominent growth inhibition activity against all tested bacterial and fungal pathogens. Antioxidant activity of F2 showed potent free radical scavenging activity with low IC50 values (DPPH - 278.15±0.35 μg/mL, ABTS - 367.55±1.13 μg/mL, and FRAP - 347.48±1.35 μg/mL). Total phenolic content of F2 was quantified as 362.44±1.25 mg gallic acid equivalent/gram extract. As per spectral analyses, the isolated compound from F2 was identified as 2,4-di-tert-butylphenol which further induced cytotoxic (IC50 value - 17.5±1.5 μg/mL) and apoptosis activity against MCF-7 cells. Molecular interaction studies of 2,4-di-tert-butylphenol with target proteins of pathogens and cancer cells displayed good docking score values. Finally, molecular dynamics simulation was performed to determine the stable structure of the protein-ligand system and effectiveness of 2,4-di-tert-butylphenol against the target protein. In conclusion, Nocardiopsis sp. strain LC-8 may act as a promising source for the production of 2,4-di-tert-butylphenol aiding diverse therapeutic roles.

Insights into free radicals scavenging, α-Amylase inhibition, cytotoxic and antifibrotic activities unveiled by Peganum harmala extracts

BackgroundPeganum harmala L. is used in traditional medicine to treat several health ailments. Hence, the present work aimed to investigate the DPPH free radical scavenging, α-amylase, cytotoxic, and antifibrotic effects of the hydrophilic extract and fixed oil obtained from P. harmala seeds.MethodsThe hydrophilic extract and fixed oil of P. harmala were assessed for their abilities to scavenge DPPH free radicals and inhibit α-amylase using reference bioassays. The cytotoxicity was assessed on several cancer and normal cell lines, including B16F1, Caco-2, COLO205, HeLa, Hep 3B and Hep G2, MCF-7, and HEK-293 T cells. The MTS assay was used to evaluate the antifibrotic capabilities utilizing the human hepatic stellate (LX-2) cell line.ResultsP. harmala plant fixed oil has potent DPPH free radical scavenging activity with an IC50 dose of 79.43 ± 0.08 µg/ml. Besides, the hydrophilic extract has a poor anti-α-amylase effect compared with the antidiabetic drug Acarbose, with IC50 doses of 398 ± 0.59 and 25.11 ± 1.22 µg/ml, respectively. In addition, the growth of MCF-7, Hep3B, HepG2, HeLa, COLO205, CaCo2, B16F1, and HeK293t was inhibited by P. harmala hydrophilic extract with IC50 doses of 121.34 ± 1.71, 268.3 ± 0.75, 297.20 ± 1.00, 155.60 ± 1.14, 150.01 ± 0.51, 308.35 ± 0.53, 597.93 ± 1.36, and 5.38 ± 0.99 µg/ml, respectively. In addition, at 1000 µg/ml, 5-Fluorouracil reduced fibrosis cells by 0.089%, while the hydrophilic extract decreased the number of LX-2 cells by 5.81%.ConclusionP. harmala plant-fixed oil exhibits potential antioxidant properties. While the hydrophilic extract showed limited effectiveness as an anti-α-amylase agent and demonstrated notable cytotoxic effects against various tested cancer cell lines. Furthermore, this extract significantly reduces the number of LX-2 fibrotic cells. These findings emphasize the therapeutic potential of these products in managing various health disorders and warrant further investigation into their mechanisms of action and clinical applications.

Investigation of in vitro biological activity of young Hordeum vulgare leaf in correlation with its bioactive compounds.

Young shoots of cereals are widely regarded as superfoods with health benefits attributed to their potential antioxidant activity and antioxidant-related effects (e.g. anticancer). The current study aimed to examine the chemical characteristics of Hordeum vulgare methanolic and aqueous extracts and assess their antioxidant activity using the DDPH and ORAC. Furthermore, the inhibitory effect of xanthine oxidase was screened. TLC bioautography was employed to determine the polarity of the compounds present in the extracts that exhibited the most potent free radical scavenging activity. Total flavonoid content of the methanolic and aqueous extracts was 0.14mgQE/g and 0.012mgQE/g, respectively. The antioxidant activity of the methanolic extract was found to be more potent, with a value of 0.97 ± 0.13mmolTE/g than the aqueous extract which had no activity. This study presents novel findings on the xanthine inhibitory activity of H. vulgare. The methanolic extract demonstrated moderate inhibition of xanthine oxidase with a value of 23.24%. The results of our study were compared with the phytochemical and pharmacological analysis of Triticum aestivum, and further comparison was made with the data reported in the literature. Inconsistencies were observed in the chemical and pharmacological properties of H. vulgare, which could be a result of using herbal material harvested in different vegetative phases and various methods used for extraction. The findings of our study indicate that the timing of the harvest and extraction method may play crucial role in attaining the optimal phytochemical composition of H. vulgare, hence enhancing its pharmacological activity.

Anti-Angiogenic and Anti-Proliferative Activity of 4-2-(5-bromo-1H-indol-2-carbonyl)-N-(4-methoxyphenyl) Hydrazine-1-carbothioamide: Ex-vivo and in vitro Study.

Angiogenesis, the formation of new blood vessels, stimulates tumor growth and spread by delivering oxygen and nutrients, and is a key component of metastasis. This work aimed to evaluate the anti-angiogenic properties of a new synthesized compound. Rat aorta angiogenesis assay was used to evaluate the ability of the carbothioamide derivative to inhibit blood vessels sprouting. The tetrazolium (MTT) assay was used to evaluate the anti-proliferative effect of the synthetic compound on human umbilical vein endothelial cell line (HUVECs) and A549 lung cancer cells line. The (2, 2-diphenyl-1-picrylhydrazyl) DPPH was used to investigate the free radical scavenging action. The study showed that the compound has anti-angiogenic activity with IC50 56.9 µg/mL, moreover the compound managed to inhibit the proliferation of HUVECs and A549 cells (IC50 76.3 µg/mL and 45.5 µg/mL, respectively), and The IC50 concentration for free radical scavenging activity of the compound was 27.8 µg/ml. The study concluded that the compound has significant anti-angiogenic activity may be related to its significant anti-proliferative effect against HUVECs, these pharmacological effect may attributed to its potent free radical scavenging activity.

Chitosan/rutin multifunctional hydrogel with tunable adhesion, anti-inflammatory and antibacterial properties for skin wound healing

Effective wound care remains a significant challenge due to the need for infection prevention, inflammation reduction, and minimal tissue damage during dressing changes. To tackle these issues, we have developed a multifunctional hydrogel (CHI/CPBA/RU), composed of chitosan (CHI) modified with 4-carboxyphenylboronic acid (CPBA) and the natural flavonoid, rutin (RU). This design endows the hydrogel with body temperature-responsive adhesion and low temperature-triggered detachment, thus enabling painless removal during dressing changes. The CHI/CPBA/RU hydrogels exhibit excellent biocompatibility, maintaining over 97 % viability of L929 cells. They also demonstrate potent intracellular free radical scavenging activity, with scavenging ratios ranging from 53 % to 70 %. Additionally, these hydrogels show anti-inflammatory effects by inhibiting pro-inflammatory cytokines (TNF-α, IL-6, and iNOS) and increasing anti-inflammatory markers (Arg1 and CD206) in RAW 264.7 macrophages. Notably, they possess robust antimicrobial properties, inhibiting over 99.9 % of the growth of Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus growth. In vivo testing on a murine full-thickness skin defect model shows that the hydrogel significantly accelerates wound healing by reducing inflammation, increasing collagen deposition, and promoting angiogenesis, achieving 98 % healing by day 10 compared to 78 % in the control group. These attributes make the polysaccharide-based hydrogel a promising material for advanced wound care.

Recent Advancements and Developments in the Biological Importance of Pyrimido[4,5‐b]Quinoline Scaffolds

AbstractThis study highlights the biological efficiency of pyrimido[4,5‐b]quinolines as inhibitors of cancer cell growth and antioxidants and anti‐inflammatory properties, etc. Recent research studies have revealed their promising biological activity to inhibit the growth of many disease‐causing yeasts, fungi, and bacteria. The structural composition greatly affects the biological effectiveness, as these compounds exceed the value of some standard compounds against pathogenic microbes. The antioxidant potential of these derivatives is also explored. Several glycosylated and non‐glycosylated derivatives exhibited potent free radical scavenging activity and protected against DNA damage, exceeding reference standards in some cases. Furthermore, the review examines the anti‐inflammatory and analgesic properties of pyrimidoquinoline derivatives. Studies suggest their efficacy is comparable to known drugs like diclofenac and aspirin in carrageenan‐induced paw edema and hot plate tests. Pyrimidoquinoline derivatives also demonstrate promising anticancer activity. While some have minimal effects, others exhibit notable activity against various human cancer cell lines. This review documents over two decades of research, covering the period from 2000 to 2024. Overall, pyrimidoquinoline derivatives signify an auspicious class of compounds with therapeutic potential across various areas. Further research is necessary to elucidate their mechanisms of action, optimize their efficacy and selectivity, and assess their safety profiles for clinical development.

Evaluation of structural parameters of monoclinic nanocrystalline CuO and study of sunlight-driven photocatalytic dye degradation, antimicrobial and antioxidant potential

Highly pure, crystalline and spherical-shaped Copper oxide nanoparticles (NPs) have been synthesized via facile chemical coprecipitation. Various models including the Scherrer, Monshi-Scherrer, Williamson-Hall, Size-Strain Plot and Halder-Wagner method have been applied to study the crystal structure characteristics. The lattice parameters associated with the monoclinic crystal lattice of CuO NPs were estimated to be a = 4.69 Å, b = 3.41 Å, c = 5.14 Å and β = 99.87(degree), unit cell volume V = 81.35Å3 and cell density dx = 6.49 g/cm3. The photocatalytic dye degradation proficiency at 20 mg/l CuO concentration and 120 min sunlight exposure results the order of percentage dye degradation Malachite Green (88.4%) > Crystal Violet (70.8%) > Eosin Yellow (70.2%) > Methylene Blue (54.08%) dyes. The antimicrobial activity assessment was done against the broad-spectrum pathogenic microbes unveiled the exceptional microbial controlling capability of CuO NPs. Furthermore, the antioxidant activity test demonstrated the potential free radical scavenging activity of CuO NPs with an IC50 value of 47.733 µg/ml. Highlights Synthesis of pure and spherical shaped nanocrystalline CuO was done by using low cost and facile chemical coprecipitation method. XRD, FTIR, FESEM, EDX, UV-Vis, and Raman spectroscopic techniques were used for characterization purpose. The structural and crystallographic parameters of monoclinic crystal structure of CuO NPs were evaluated successfully. The photocatalytic performance of CuO NPs follow the percentage dye degradation order as MG (88.4%) > CV (70.8%) > EY (70.20%) > MB (54.08%) after 120 minutes of sunlight exposure. CuO NPs exhibit promising antifungal activity against COVID-19 associated Pulmonary Aspergillosis (CAPA) causing pathogenic fung. CuO NPs show potential DPPH free radical scavenging activity with an IC50 value of 47.733 µg/ml.

Multifaceted chemical and bioactive features of Ag@TiO2 and Ag@SeO2 core/shell nanoparticles biosynthesized using Beta vulgaris L. extract

Due to increasing concerns about environmental impact and toxicity, developing green and sustainable methods for nanoparticle synthesis is attracting significant interest. This work reports the successful green synthesis of silver (Ag), silver-titanium dioxide (Ag@TiO2), and silver-selenium dioxide (Ag@SeO2) nanoparticles (NPs) using Beta vulgaris L. extract. Characterization by XRD, SEM, TEM, and EDX confirmed the successful formation of uniformly distributed spherical NPs with controlled size (25 ± 4.9 nm) and desired elemental composition. All synthesized NPs and the B. vulgaris extract exhibited potent free radical scavenging activity, indicating significant antioxidant potential. However, Ag@SeO2 displayed lower hemocompatibility compared to other NPs, while Ag@SeO2 and the extract demonstrated reduced inflammation in a carrageenan-induced paw edema animal model. Interestingly, Ag@TiO2 and Ag@SeO2 exhibited strong antifungal activity against Rhizoctonia solani and Sclerotia sclerotium, as evidenced by TEM and FTIR analyses. Generally, the findings suggest that B. vulgaris-derived NPs possess diverse biological activities with potential applications in various fields such as medicine and agriculture. Ag@TiO2 and Ag@SeO2, in particular, warrant further investigation for their potential as novel bioactive agents.

Structural Study of a La(III) Complex of a 1,2,3-Triazole Ligand with Antioxidant Activity.

The 1,2,3-triazole derivative 2-(4-chlorophenyl)-5-(pyrrolidin-1-yl)-2H-1,2,3-triazole-4-carboxylic acid with potential anticancer activity was used as a ligand in complex formation with the lanthanum(III) ion. The molecular structure and vibrational spectra of the complex were optimized at three DFT levels, and the scaled IR and Raman spectra were compared to the experimental ones. Several scaling procedures were used. Through a detailed analysis, the structure predicted for the newly synthetized La(III) complex was confirmed by the good accordance of the calculated/experimental IR and Raman spectra. The best DFT method appeared to be M06-2X with the Lanl2mb basis set, followed closely by Lanl2dz. The effect of the lanthanide atom on the molecular structure and atomic charge distribution of the triazole ring was evaluated. The potential free radical scavenging activity of both the ligand and the complex was investigated in several radical-generating model systems. The potential mechanisms of antioxidant action (hydrogen atom transfer (HAT) and single-electron transfer (SET)) were elucidated.

Biological Synthesis of Copper Nanoparticles Using Edible Plant Allium monanthum: Characterization of Antibacterial, Antioxidant, and Anti-Inflammatory Properties Using In Silico Molecular Docking Analysis.

This study prepared copper nanoparticles using an edible leaf extract from A. monanthum (AM-CuNPs) via eco-friendly green synthesis techniques. The size, shape, crystalline nature and functional groups of the synthesized AM-CuNP particles were analyzed by a UV-VIS spectrophotometer and SEM, EDX, TEM, XRD and FT-IR instrumentation. The synthesized AM-CuNPs had spherical shapes with sizes in the range of 30-80 nm and were crystalline in nature. In addition, the AM-CuNPs were synthesized using various bioactive sources, including flavonoids, phenolic acids, alkaloids and sugars that were present in an aqueous broth of A. monanthum. Furthermore, the AM-CuNPs possessed good antibacterial properties against selected major disease-causing pathogenic bacteria, such as E. coli, Salmonella typhi, Pseudomonas aeruginosa and Staphylococcus aureus. The antioxidant activity of AM-CuNPs exhibited potent free radical scavenging activities in DPPH, ABTS and H2O2 radical assays. In addition, in silico analysis of the AM-CuNPs was performed, including ADME prediction, and molecular simulation docking on the secondary metabolites identified in the edible plant extract was used to evaluate their anti-inflammatory applications. In particular, the molecular docking scores showed that alliin, apigenin, isorhamnetin, luteolin and myricetin have sufficient binding energy and top values as inhibitors of the protein target involved in the inflammation signaling cascade.

Relative Free Radical Scavenging, Tyrosinase Inhibitory, and Anti-Inflammatory Potential of the Polar Peel decoctures of distinct Malus Species indigenous to Kashmir

Apple, (Malus domestica, Brokh), is a vital source of phenolic and polyphenolic compounds whose accumulation in the different parts of the fruit depends upon various intrinsic and extrinsic factors. This study aimed to perform a comparative evaluation of phenolics of peels of three red-skinned (“Delicious”, “Maharaji”, “Royal delicious”), and one yellow-skinned (“Golden Delicious”) apple varieties incorporating preliminary secondary metabolite perusal followed by estimation of Total phenol and total flavonoid contents. Secondary phytocompounds being usually polar in nature were extracted from peels via the Soxhlet and hot maceration processes using different menstruum systems of varied polarity. Comparative assessment of Free radical scavenging, anti-pigmentation, and anti-inflammatory properties of all the decoctures was analyzed thereafter.Free radical scavenging capacity was analyzed via 2, 2-diphenyl-1-picrylhydrazyl assay.Tyrosinase inhibitory activity was assessed by studying the in vitro impact of decoctures on the monophenolase and diphenolase reactions of the enzyme tyrosinase. The anti-inflammatory potential of the samples was assessed by inhibition of hypotonicity-induced HRBC membrane lysis. TPC/TFC estimation was analyzed via spectrophotometry. Methanol crude peel extracts of all apple species revealed rich phytochemical content as per TPC/TFC analysis. In a dose-dependent manner, all the crude peel extracts demonstrated considerable free radical scavenging capacity with DPPH assay. Maharaji methanolic decocture revealed potent free radical scavenging activity by showing the lowest IC50 value while Royal delicious acetone extract showed the highest IC50 value when collated with the potent reference antioxidant ascorbic acid with an IC50value of 114.62µg/ml. Polarextract of Malus domestica var Maharaji revealed significant tyrosinase inhibitory activity by revealing IC50 of 8460.65µg/mlon L-Tyrosine substrate and IC50 of 7830.46 µg/ml on L-DOPA substrate. Malus peel compounds turn out to be more effective in diphenolase reaction and kojic acid acts more effectively in the monophenolase one.At various concentrations, the percentage of membrane stabilization for methanolic extracts and the reference NSAID diclofenac sodium was determined.The highest level of membrane stabilization wasshown by methanolic Maharaji and delicious apple peel extracts (83.76 % and 72.32% at a dose of 200 mg/ml respectively) when juxtaposed with standard NSAID showing 98.58 % inhibition at a concentration of 25 mg/ml. Methanol extracts of Malus domestica var Maharaji out performed the other Malus peel extracts in terms of all the parameters analyzed, according to the current study. So, this study is giving the highest pharmaceutical priority to the Malus domestica var Maharaji when it comes to human-health benign bioactive compounds, oxidative stress-related diseases, pigmentation disorders, and inflammatory diseases.

Preliminary Assessment of Phytochemicals and Free Radical Scavenging Activity of Different Plants Collected from the Western Region of Nepal

Medicinal plants produce vital secondary metabolites in curing various diseases and pathological conditions. There are multiple tribes and communities where people are using plants from the medicinal aspect to cure different diseases. The aim of the present study was qualitative and quantitative phytochemical screening, determination of total phenol and total flavonoid content, and free radical scavenging activity of different parts of ethnomedicinally used plants collected from the western region of Nepal. The phytochemical screening of most of the extract showed the presence of phenols, carbohydrates, flavonoids, and glycosides. The ethanolic flower extract of Callicarpa macrophylla showed a higher phenolic content with a value of 195 ± 7.33 µg GAE/mg. Ethyl acetate extract of Elephantopus scaber root revealed the highest amount of flavonoid content with the value of 1692.31 ± 34.79 µg QE/mg of extract, followed by ethanolic flower extract of Callicarpa macrophylla. Ethanolic flower extract of Callicarpa macrophylla showed potent DPPH free radical scavenging activity with a half inhibitory concentration of 7.28 µg/ml. In contrast, Elephantopus scaber ethyl acetate root extract revealed the maximum free extreme scavenging properties among all the ethyl acetate extracts. From the experiment, the free radical scavenging potential of ethanolic flower extract of the Callicarpa macrophylla was comparable with ascorbic acid. This comparable activity may be attributed to higher phenols and flavonoid content in ethanolic extract. The result signifies that the ethanolic extract of Callicarpa macrophylla acts as an antioxidant and may contain a potent bioactive compound which, with further investigation, may lead to a novel compound.

An Overview of Chemistry, Kinetics, Toxicity and Therapeutic Potential of Boldine in Neurological Disorders.

Boldine is an alkaloid obtained from the medicinal herb Peumus boldus (Mol.) (Chilean boldo tree; boldo) and belongs to the family Monimiaceae. It exhibits a wide range of pharmacological effects such as antioxidant, anticancer, hepatoprotective, neuroprotective, and anti-diabetic properties. There is a dearth of information regarding its pharmacokinetics and toxicity in addition to its potential pharmacological activity. Boldine belongs to the aporphine alkaloid class and possesses lipophilic properties which enable its efficient absorption and distribution throughout the body, including the central nervous system. It exhibits potent free radical scavenging activity, thereby reducing oxidative stress and preventing neuronal damage. Through a variety of neuroprotective mechanisms, including suppression of AChE and BuChE activity, blocking of connexin-43 hemichannels, pannexin 1 channel, reduction of NF-κβ mediated interleukin release, and glutamate excitotoxicity which successfully reduces neuronal damage. These results point to its probable application in reducing neuroinflammation and oxidative stress in epilepsy, Alzheimer's disease (AD), and Parkinson's disease (PD). Moreover, its effects on serotonergic, dopaminergic, opioid, and cholinergic receptors were further investigated in order to determine its applicability for neurobehavioral dysfunctions. The article investigates the pharmacokinetics of boldine and reveals that it has a low oral bioavailability and a short half-life, requiring regular dosage to maintain therapeutic levels. The review studies boldine's potential therapeutic uses and mode of action while summarizing its neuroprotective benefits. Given the favorable results for boldine as a potential neurotherapeutic drug in laboratory animals, more research is required. However, in order to optimise its therapeutic potential, it must be more bioavailable with fewer detrimental side effects.

The Protective Effect of Oxitard on Sperm Function and Antioxidant Status in Rats Exposed to Swimming Stress.

Infertility is a significant public health issue, but its impact on quality of life and treatment efficacy is limited. Modern medicine lacks safe and effective drugs for male infertility, while traditional medicine has explored herbal extracts like Oxitard, which contains multiple extracts and oils. This study aimed to investigate the effects of Oxitard on male rats exposed to swimming (SW) stress. Albino rats weighing 220-250 g were divided into five groups: control, SW stress, and SW treated with Oxitard at low, medium, and high doses of 250, 500, and 750 mg/kg/day, respectively. The rats were subjected to SW stress for 15 days and then assessed for body weight, reproductive organ weight, testosterone, antioxidant status, sperm function, and histological changes in the testes, seminal vesicles, and vas deferens. The results showed that SW stress significantly reduced body weight, seminal vesicle weight, testosterone levels, superoxide dismutase (SOD), catalase (CAT), sperm count, sperm motility, sperm viability, and significantly increased malondialdehyde (MDA) levels. The testes of the SW-stress group rats also showed a significant decrease in spermatogenesis and the number of seminiferous tubules containing sperm. In contrast, treatment with Oxitard, especially at the highest dose, demonstrated potent free radical scavenging activity, recovering antioxidant status, and sperm function. SW stress led to decreased sperm function, antioxidant status, and increased lipid peroxidation (LPO) in male rats. Oxitard treatment, particularly in high doses, showed a potential role as a free radical scavenger in treating oxidative stress (OS)-associated male infertility. Further studies are needed to investigate the individual components of Oxitard and conduct clinical trials in human subjects.

Design, Synthesis, Characterization and Biological Evaluation of Para-Amino Salicylic Acid (PAS) Analogues: An Approach to Repurpose

The ever-emerging microbial resistance has imposed great challenges for the medicinal chemist in designing newer chemical entities, which is a lengthy and time-consuming process. An alternate approach of repurposing older drugs can be undertaken to accelerate the discovery of some newer derivatives with lesser side effects. The work reported in the present paper is an extension of the idea of repurposing older drugs. The study aimed to synthesize a series of ester and amide derivatives (P1-P28) of Para-amino salicylic acid. The antimicrobial evaluation of all the synthesized derivatives was performed via the serial dilution method. The Gram-positive bacteria: Staphylococcus aureus and Bacillus subtilis and Gram-negative bacteria: Escherichia coli and Pseudomonas aeruginosa were used for the antibacterial activity, and Candida albicans were used for the antifungal activity. Ciprofloxacin (antibacterial) and Fluconazole (antifungal) were the standard drugs. The antioxidant evaluation (ester derivatives, P1-P19) was carried out by using the DPPH scavenging method and BHA (butylated hydroxy anisole) was used as the reference. The derivative 5-acetamido-2-(propyl carbamoyl) phenyl acetate (P22) was the most effective antibacterial agent, which may be attributed to the presence of 3-carbon aliphatic alkyl chain. At the same time, 4-methoxy phenyl-4-amino-2-hydroxy benzoate (P15) and 2-chloro phenyl-4-amino-2-hydroxy benzoate (P16) displayed effective antifungal activity. Ethyl-4-amino-2-hydroxy benzoate (P2) demonstrated the most potent free radical scavenging activity. Further, the spectroscopic characterization and physicochemical characterization of the synthesized derivatives have been carried out and were found to be in accord with the assigned structures.

Development of multifunctional packaging films based on arginine-modified chitosan/gelatin matrix and betacyanins from weed amaranth (A. hybridus)

Active and intelligent films with antioxidant, antimicrobial, and pH-responsive properties were developed by incorporating betacyanins-rich weed amaranth (A. hybridus) extract (AE) into chitosan/gelatin (Cs/Gn) and arginine-modified chitosan/gelatin (MCs/Gn) blend films. The microstructures, physical and functional properties of Cs/Gn, MCs/Gn, Cs/Gn-AE, and MCs/Gn-AE films were compared. Results showed the addition of AE into MCs/Gn film produced a compact inner microstructure through H-bonding and electrostatic interactions. Meanwhile, AE remarkably changed the colors of the film under alkaline pH mediums. However, AE significantly reduced the water vapor permeability of the films. By comparing different films, MCs/Gn-AE film presented the best UV–vis light and barrier ability as well as the highest mechanical strength. Moreover, MCs/Gn and MCs/Gn-AE films showed stronger microbial growth inhibition than Cs/Gn and Cs/Gn-AE films. Cs/Gn-AE and MCs/Gn-AE films possessed more potent free radical scavenging activity than Cs/Gn and MCs/Gn. Notably, MCs/Gn-AE film is suitable to monitor fish freshness and could be used as novel multifunctional packaging in the seafood industry.

Synthesis and biological evaluation of capsaicin analogues as antioxidant and neuroprotective agents.

Capsaicin and its analogues 3a-3q were designed and synthesized as potential new antioxidant and neuroprotective agents. Many analogues exhibited good antioxidant effects, and some showed more potent free radical scavenging activities than the positive drug quercetin (IC50 = 8.70 ± 1.75 μM for DPPH assay and 13.85 ± 2.87 μM for ABTS assay, respectively). The phenolic hydroxyl of capsaicin analogues was critical in determining antioxidant activity. Among these compounds, 3k displayed the most potent antioxidant activity. Cell vitality tests revealed that the representative compound 3k was good at protecting cells from H2O2-induced oxidative damage at low concentrations (cell viability increased to 90.0 ± 5.5% at 10 μM). In addition, the study demonstrated that 3k could reduce intracellular ROS accumulation and increase GSH levels to prevent H2O2-induced oxidative stress in SY5Y cells. In the mitochondrial membrane potential assay, 3k significantly increased the MMP level of SY5Y cells treated with H2O2 and played an anti-neuronal cell death role. These results provide a promising strategy to develop novel capsaicin analogues as potential antioxidant and neuroprotective agents.

Qualitative and Quantitative Phytochemical Screening and Free Radical Scavenging Activity of Different Parts of Rubus ellipticus Sm.

Free radicals are molecules with reactive unpaired electrons which are produced during cell metabolism and create the oxidative stress inside tissue resulting in tissue damage. The aim of the present study was qualitative and quantitative phytochemical screening, determination of total phenolic and total flavonoid content, and free radical scavenging activity of different parts of ethnomedicinally used Rubus ellipticus Sm. plant. Root, stem, and leaves of Rubus ellipticus Sm. were collected from Annapurna Rural Municipality, Kaski, Western Nepal. Ethyl acetate and ethanol extracts of the plant parts were obtained by subsequent maceration process. The phytochemical screening of most of the extract showed the presence of phenols, carbohydrates, flavonoids, and glycosides. The ethanolic extract of stem showed the higher phenolic content with the value of 343.75 ± 2.21 µg GAE/mg. Ethanolic extract of stem had the highest amount of flavonoid content (1563.17 ± 10.79 µg QE/mg of extract), whereas all the ethyl acetate extracts of root, leaves and stem showed comparable flavonoid content. Ethanolic extracts of leaves showed potent DPPH free radical scavenging activity with IC50 value of 5.03µg/ml while ethyl acetate extract of stem showed the maximum free radical scavenging properties. The result depicted that the ethanolic extract of Rubus ellipticus Sm. showed the potent antioxidant activity by scavenging free radicals.