Free Radical Scavenging Activity Research Articles

Unveiling flavonoids in Alpinia species indigenous to Thailand and their relevance with radical scavenging potential and α-glucosidase inhibitory activities

The rhizomes of plants in the genus Alpinia (Zingiberaceae) have been used as food, spices, and traditional medicine in Thailand. The crude ethanolic extracts from the fresh rhizomes of selected Alpinia species, including A. galanga var. galanga, A. galanga var. pyramidata, A. oxymitra, and A. siamensis, were proposed to be explored for their active principles and in vitro antioxidant and antidiabetic performance. The fresh rhizomes were extracted with 95% ethanol using a Soxhlet apparatus, and crude extracts were subsequently analyzed for amounts of flavonoids using quercetin and kaempferol as chemical markers by high-performance liquid chromatography. All flavonoid-containing extracts were evaluated for their antioxidant and antidiabetic effects using free radical scavenging and α-glucosidase inhibitory tests. The results demonstrated that the examined extracts included active flavonoid markers, predominantly quercetin, which ranged from 11.05% to 13.79% w/w and was approximately 10 times more prevalent than kaempferol. Extracts that consisted of these active flavonoids exhibited strong antioxidant and α-glucosidase inhibitory activities. Pearson’s correlation study was used to determine the association between flavonoid quantity and possessed activities. The findings indicated a substantial correlation between quercetin levels and free radical scavenging activity. This work implies that raw ethanolic extracts from the fresh rhizomes of these rare Alpinia plants have the potential to be developed into functional nourishment and remedies that could benefit diabetics in alternative ways.

Untying the antimicrobial and antioxidant potential of silver nanoparticles fabricated from Typhonium trilobatum (L.) Schott

Understanding the properties of silver nanoparticles (AgNPs) is noteworthy for the development of novel antimicrobial agents. Here AgNPs were procured through a sustainable, effortless, simple and lucrative process by using natural reducing agents from aqueous leaf extract of Typhonium trilobatum (L.) Schott. The study mainly aims at the determination of antibacterial and antioxidant activity of the bio-fabricated AgNPs. The synthesis of nanoparticles (NPs) was initially confirmed by UV–vis spectroscopy. The AgNPs were spherical with diameter ranges between 30 and 90 nm, negatively charged at −29.6 mV, crystalline in nature and surrounded by different active functional groups as evident by FTIR spectra analysis. The presence of phenolic compounds such as gallic acid and catechin were confirmed through HPLC analysis, providing insights into the bio-reduction mechanism which facilitate the conversion of Ag+ to AgNPs. Antimicrobial properties of the synthesized AgNPs were assessed against four Gram-negative and two Gram-positive bacteria with maximum zone of inhibition against Staphylococcus aureus (20±3.00 mm) and Micrococcus luteus (20±1.73 mm). The antibacterial potential of AgNPs is primarily linked with the increased cell membrane permeability of AgNPs treated bacterial cells (E. coli, S. aureus and M. luteus) as evident by measuring increased conductivity and elevated extracellular DNA concentration due to the disruption of bacterial cell membrane. Synthesized AgNPs exhibited antioxidant properties with IC50 value of 239.50 mg/L in free radical scavenging activity and IC50 value of 213.23 mg/L in superoxide scavenging activity. To the best of our knowledge, this is the earliest report of biosynthesis and physico-chemical characterization of AgNPs using T. trilobatum leaf extract having efficient antioxidant and antibacterial activity against some bacteria. These plant-mediated AgNPs might offer a promising solution in antibiotic resistance—a growing global health threat.

Small Steps to the Big Picture for Health-Promoting Applications Through the Use of Chickweed (Stellaria media): InVitro, In Silico, and Pharmacological Network Approaches.

Stellaria media L., also called chickweed, is widespread in all parts of the world. In the present study, we investigated the biological properties and chemical profiles of different extracts (ethyl acetate, ethanol, ethanol/water, and water) of S. media. The chemical profiles were examined using UHPLC/MS/MS technique. Regarding the biological properties, antioxidant properties as well as enzyme-inhibiting and cytotoxic effects of the extracts were demonstrated by invitro methods. To obtain further information about the structure-ability relationship, network pharmacology and molecular docking were also performed. Twelve phenolic compounds were identified in the extracts and most of them were flavonoids (apigenin, kaempferol derivatives, etc.). The water extract showed the best free radical scavenging activity, while the ethanol was the most active in reducing power tests. When inhibiting AChE, the ethyl acetate extract showed the best inhibitory effect. The water extract has a good cytotoxic effect on HepG2 (cell viability: 33.9% at a concentration of 100 g/mL). The analysis, performed using the STRING database, included these 45 cancer-associated targets. The identified hub genes were TP53, CDKN2A, PTEN, KRAS, and HRAS. In molecular docking analysis, acacetin-O-hexoside-O-deoxyhexoside and napigenin-7-O-hexoside exhibit remarkable binding energies with proteins. Consequently, S. media can be potential raw materials for designing functional formulations in the pharmaceutical, nutraceutical, and cosmeceutical industries.

Comparative assessment of antioxidant and antiglycation properties of Leucas species

Abstract BACKGROUND: The genus Leucas is an aromatic plant and belongs to the Lamiaceae family. They are rich in secondary metabolites. The benefits of Leucas in curing many ailments such as coughs, colds, diarrhea, diabetes, inflammation, and skin diseases have made it an Ayurvedic component. Hence, the present study aims to evaluate the phytochemical, antioxidant, and antiglycation properties of methanol and aqueous extract from three Leucas species, viz, Leucas aspera Link, Leucas zeylanica (L.) W.T.Aiton, and Leucas longifolia Benth. METHODS: Dry powders of the whole part of three species of Leucas were extracted with methanol and aqueous solution. Qualitative analysis of secondary metabolites such as flavonoids, phenolics, alkaloids, glycosides, terpenoids, and tannins was performed by using standard phytochemical procedures. Total phenol, flavonoid, and alkaloid contents were estimated by spectrophotometric methods. The superoxide radical scavenging activity, 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, hydrogen peroxide radical scavenging activity, and ferric-reducing power methods are in vitro models. Bovine serum albumin glycation assay was used to evaluate the in vitro antiglycation activity of extracts. RESULTS: The highest percentage of extraction yield was observed in the methanolic extract of all Leucas species compared to the aqueous extract. The preliminary phytochemical tests reveal the presence of various bioactive secondary metabolites such as phenols, flavonoids, alkaloids, steroids, terpenoids, and glycosides. These extracts show that L. aspera has high DPPH activity, superoxide radical scavenging activity, hydrogen peroxide radical scavenging activity, and ferric-reducing antioxidant power compared to L. zeylanica and L. longifolia. The methanolic and aqueous extract of L. aspera exhibited more significant inhibitory (96.70 ± 1.78 and 90.33 ± 1.65%) effects on advanced glycation end products formation in bovine serum albumin glycation systems compared to standard aminoguanidine (99.45 ± 1.37%) than L. zeylanica and L. longifolia. The methanol extract of L. aspera is rich in phenols, flavonoids, and alkaloids and has strong antiglycation and antioxidant properties. CONCLUSION: The strong antiglycation and antioxidant activity of all three Leucas species suggests its possible role in combating diseases associated with diabetic complications and oxidative stress.

Evaluation of the Free Radical Scavenging Activities and Antibacterial Activities of the Extracts of Lindernia ruellioides (Colsmann) Pennell

Evaluation of the Free Radical Scavenging Activities and Antibacterial Activities of the Extracts of Lindernia ruellioides (Colsmann) Pennell

Antidiabetic Potential of Mangifera Indica: Insights from In Vitro and In Vivo Studies

Background: Diabetes mellitus is a chronic endocrine disorder characterized by elevated blood glucose levels. Owing to the adverse side effects of synthetic drugs, natural products attract research interest because of their fewer side effects and prominent efficacy. In the present study, we examined the antidiabetic effects of the seeds of Mangifera indica. Materials & Methods: Phytochemical analysis (quantitative and free radical scavenging activity), in vitro enzymatic assays, and in vivo antidiabetic studies were performed on the hydroalcoholic extract of M. indica. Additionally, an immunohistochemistry approach was utilized to illustrate the alteration of the cellular architecture in the pancreatic islets of extract-treated diabetic rats. Results: The hydroalcoholic extract exhibited good phenolic and flavonoid contents, prominent radical scavenging ability, and antidiabetic activity in an in vitro enzymatic assay. At a dose of 200 mg/kg body weight, the hydroalcoholic extract significantly decreased the blood glucose and HbA1c levels and substantially improved the serum marker levels (GLU, ALB, UREA, CREA, CHOL, TG, SGPT, SGOT, TP, HDL, and ALP). The immunohistological study revealed 40% regeneration of pancreatic β-cells upon extract treatment. Conclusion: The hydroalcoholic extract has prominent antidiabetic activity, as evidenced by both in vitro and in vivo studies, by modulating the cellular composition and regenerating the β-cells of the pancreatic islet.

Aquo-ethanolic extract of Lilii Bulbus attenuates dexamethasone-induced muscle loss and enhances muscle strength in experimental mice

Traditionally, Lilium lancifolium bulb is known for its ability to nourish yin, nourish the lungs, clear the heart, soothe coughs, reduce irritability, and calm the mind. In Oriental Medicine, it is categorized as a tonic remedy for alleviating symptoms of fatigue and enhancing the strength of bones and muscles.In this study, we aimed to validate the effectiveness of the aquo-ethanolic extract of Lilli Bulbus (LBE) in a dexamethasone (DEX)-induced muscle atrophy model, both in vitro and in vivo, and elucidate its mechanism of action through muscle transcriptome analysis. The effects of LBE on the viability and myotube density of C2C12 myoblasts and differentiated C2C12 myotubes with and without DEX treatment were investigated. LBE pretreatment protected C2C12 myoblast cells and increased the muscle density of C2C12 myotubes in response to DEX. LBE showed potent free radical scavenging activities in cell-free biochemical assays as well as antioxidant activity in C2C12 myoblasts. LBE also exhibited protective effects in an experimental animal model of DEX-induced muscle atrophy, showing muscular function and motor coordination recovery. Transcriptomic analysis of three different muscle tissues from mice with DEX-induced muscle atrophy showed that the regulation of the extracellular matrix was perturbed by glucocorticoid treatment, and this perturbation was reversed by LBE treatment.Collectively, LBE alleviated skeletal muscle loss and maintained muscle function from the chronic toxicity of DEX by protecting muscle cells from various stressful conditions, as well as DEX itself, inhibiting muscle protein degradation, and preserving the muscle tissue microenvironment.

In-vitro Evaluation of Free Radical Scavenging Activities and Inflammatory Markers from LPS-Induced MH-S Cells by Xanthium strumarium L.

<i>In-vitro</i> Evaluation of Free Radical Scavenging Activities and Inflammatory Markers from LPS-Induced MH-S Cells by <i>Xanthium strumarium</i> L.

Optimization of enzymatic-assisted extraction of polyphenol from cashew nut testa by using cellulase and pectinase

A significant amount of cashew nut testa is removed during the processing of cashew kernels, resulting in many negative environmental impacts. The objective of this study was to valorize the cashew nut testa by enzymatic-assisted extraction of polyphenol using a mixture of cellulase and pectinase. A central composite design was employed to analyze the effects of extraction temperature from 41.6°C to 58.4°C, extraction pH from pH 3.2 to pH 4.8, and enzyme concentration from 0.03% to 0.37% (v/w) on extraction efficiency. A second-order response surface model was constructed to elucidate the effects of these independent variables on the response values of total phenolic content (TPC) and free radical scavenging activities [2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis-3- ethylbenzothiazoline-6-sulfonic acid (ABTS) assays]. Regression analysis results showed that 91%, 88%, and 92% variations of the response variables of TPC, DPPH and ABTS scavenging activities can be explained by the models, respectively. Under optimal conditions, the predicted value for TPC was 164.26 (mg GAE/g DW), and the free radical scavenging activities according to DPPH and ABTS assays were 936.52 (µmol TE/g DW) and 1591.47 (µmol TE/g DW), respectively. The experimental results were consistent with the predicted values, demonstrating the suitability of the quadratic model and the success of the response surface method for optimizing the polyphenol extraction from cashew nut testa by using the enzyme mixture.

Evaluation of Total Flavonoids, Total Phenolics Content and in Vitro Antioxidant Activities of Extract of Platycerium bifurcatum Leaf: A Potential Antihypertensive Medicinal Plant

Plant bioactive compounds possess the potential to function as antioxidants, which makes interest in the use of ethnomedicine for treatment or prevention of diseases associated with oxidative stress to be growing. This study evaluated the flavonoid contents, total phenolics and in vitro antioxidant activity of Platycerium bifurcatum leaf extract. The free radical scavenging activity was determined using diphenyl-picrylhydrazyl (DPPH) and nitric oxide assay, and the reducing power by ferric reducing antioxidant power (FRAP) and the total antioxidant capacity assays. The total phenolics content of the extract was 4.7 ± 0.56 mg GAE/g extract and flavonoid contents of the extract was 46.73 ± 2.03 mg QE/g extract. The extarct exhibited a dose dependent nitric oxide and DPPH free radical scavenging capacity, which showed a strong correlation between the antioxidant activity and the flavonoid contents and total phenolics. The appreciable amount of flavonoid contents, total phenolics and its strong antioxidant properties suggested that Platycerium bifurcatum is a promising source of novel lead antioxidants and could be utilized in the treatment of oxidative stress mediated cardiovascular disease like hypertensive and obesity

Encapsulation of Microalgae Tisochrysis lutea Extract in Nanostructured Lipid Carriers (NLCs) and Evaluation of Their Sunscreen, Wound Healing, and Skin Hydration Properties.

Traditional sunscreens have relied on synthetic compounds to protect against harmful ultraviolet (UV) radiation. However, there is increasing interest in utilizing the natural photoprotective properties of microalgae extracts. This approach does not only aim to enhance the stability and efficacy of sun protection formulae but also seeks to reduce the reliance on synthetic sunscreens. This study investigates the encapsulation of Tisochrysis lutea extract (TL) in nanostructured lipid carriers (NLCs) to create a combination (NLC-TL) with enhanced physicochemical stability, antioxidant activity, SPF efficacy, wound healing capacity, and skin hydration. The particle size and ζ-potential were approximately 100 nm and -50 mV, respectively, and both formulations successfully passed the stability tests. The antioxidant activity, measured via DPPH assay, revealed that NLC-TL achieved the highest free radical scavenging activity across all tested concentrations, indicating a synergistic effect. The incorporation of TL in NLCs maintained the sun protection factor (SPF) of a 2% extract solution (1.53 ± 0.13). The wound healing assay indicated that NLC-TLs significantly enhanced wound closure compared to controls and TL alone. Additionally, skin hydration tests on healthy volunteers revealed that NLC-TLs provided superior and sustained hydration effects. These results highlight NLC-TLs' potential as a multifunctional topical agent for cosmetic and therapeutic applications.

Phytochemical characterization and valorization of Quercus ilex (west of Algeria)

&lt;p&gt;&lt;span style="font-family:&amp;quot;Times New Roman&amp;quot;,&amp;quot;serif&amp;quot;;font-size:12pt;line-height:115%;"&gt;&lt;strong&gt;ABSTRACT&lt;/strong&gt;&lt;/span&gt;&lt;/p&gt;&lt;p style="text-align:justify;"&gt;&lt;span style="font-family:&amp;quot;Times New Roman&amp;quot;,&amp;quot;serif&amp;quot;;font-size:12pt;line-height:115%;" lang="EN-US"&gt;This project is part of the promotion of natural resources such as Non-Timber Forest Products (NTFP). In order to assess the economic value of NTFP, this research focuses on the phytochemical analysis of holm oak (&lt;/span&gt;&lt;em&gt;&lt;span style="font-family:&amp;quot;Times New Roman&amp;quot;,&amp;quot;serif&amp;quot;;font-size:12pt;line-height:115%;" lang="EN-US"&gt;Quercus ilex &lt;/span&gt;&lt;/em&gt;&lt;span style="font-family:&amp;quot;Times New Roman&amp;quot;,&amp;quot;serif&amp;quot;;font-size:12pt;line-height:115%;" lang="EN-US"&gt;L.) from the Terni region (Western Algeria). It focused on bioactive substances, particularly polyphenols. The method used consists of extracting the phenolic compounds by two methods which are maceration and ultrasound from the leaves and bark of this species. The quantity of these compounds is assessed spectrometrically and the antioxidant activity of the extracts in vitro using free radical scavenging and total antioxidant capacity assays. The results obtained indicate that maceration offers the best yield for extracting phenolic compounds from the leaves, with a yield of 10.74%. These results also showed that the extracts of holm oak leaves and bark are rich in phenolic compounds and have a content of total phenols (103,014±1,393 and 813.462±1.675 mg EAG/g DM), flavonoids (87.078±6.220 and 949.936±36.394 mg EC/g DM) and condensed tannins (57.194±12.447 and 940.195±20.417 mg EC/g DM). Regarding the antioxidant power, it is evident that all extracts have significant antioxidant capacity, and all have high free radical scavenging activity. The highest inhibition percents are 84.98±7.45% for the leaf extract and 83.15±9.27% for the bark extract. According to these results, holm oak contains a large quantity of polyphenols and antioxidant molecules. This information represents a natural source of antioxidants which remains to be exploited for future use in the agri-food and health sectors, within the broader framework of promoting the biodiversity of Algerian plants (NTFP).&lt;/span&gt;&lt;/p&gt;

Extraction and In Vitro and In Vivo Antioxidant Activity Evaluation of Polyphenols from Lychee Pericarp

Background Finding a new promising plant antioxidant to combat or prevent cardiovascular disease remains a major challenge for researchers. Lychee pericarp, which includes a variety of polyphenols, is a prospective source of botanical antioxidants. Purpose In response to this issue, we assessed the effect of lychee bark extract on oxygen radical scavenging capacity and separate vascular protective ability in vivo. Methods In the current study, the lychee pericarp enrichment product (RLP) was obtained by optimizing an extraction method and separated using modern separation methods. The structure of the isolated compounds was assessed using 1H-NMR, 13C-NMR, and electrospray ionization-mass spectrometry, and the content of polyphenols obtained from the extract was quantified using the area normalization method. In addition, the capacity of RLP to scavenge oxygen radicals in vitro was assessed using the DPPH (1,1-diphenyl-2-picrylhydrazyl) and T-AOC (total antioxidant capacity) techniques. Furthermore, an isoprenaline hydrochloride (ISO)-induced rat model of acute myocardial ischemia was established, and four biochemical indicators were used to assess the effect of lychee bark extract on oxygen radical scavenging capacity and cardiovascular protective ability in vivo. Results RLP extraction produced 11 chemicals, 6 of which were structurally assessed. Quantitative analysis revealed that epicatechin, PC-C(epicatechin-(4β↓8,2β↓O↓7)-epicatechin-(4β↓8)-epicatechin), type A proanthocyanidin trimer, proanthocyanidin A2, and type B proanthocyanidin dimer were the most abundant polyphenols. The in vitro DPPH and T-AOC findings revealed that RLP exhibited strong free radical scavenging activity, approximately 1.5-fold that of vitamin C. The four biochemical indicators confirmed the antioxidant activity and cardiovascular protective ability of RLP in vivo. Conclusion RLP has good in vivo and in vitro antioxidant activity, confirming lychee pericarp as a prospective source of botanical antioxidants.

Enzymatic synthesis of self-adhesive zein to impart durable hydrophobicity with antioxidant activity to cotton fabrics

In this study, dopamine (DA) was used as the acyl receptor to modify zein through transglutaminase (TGase)-mediated reaction, producing self-adhesive zein (zein-DA complex). The structure of zein-DA complex was characterized by Fourier transform infrared spectrum (FT-IR), 1H nuclear magnetic resonance spectrum (1H NMR), and circular dichroism spectrum (CD), revealing the successful grafting of catechol structure of DA to zein. The results of SDS-PAGE demonstrated that zein-DA complex exhibited great ability of self-polymerization. The zein-DA complex absorbed on the cotton fabric surface imparted hydrophobicity with a water contact angle value (WCA) of 121.34 ± 1.14° to the fabrics. After 5 washing cycles, the WCA still remained 100.28 ± 4.83°, which indicated the fabrics obtained relatively durable hydrophobicity due to the self-adhesion of zein-DA complex. The results of FT-IR, scanning electron microscope (SEM), X-ray photoelectron spectroscopy (XPS), and color reaction tests manifested that much more protein attached on the surface of cotton fabric treated with zein-DA complex after washing compared with that with zein, which verified that the zein-DA complex had strong adhesion properties. Due to the introduction of DA, the relative DPPH free radical scavenging activity of cotton treated with zein-DA complex reached 43.60 ± 0.28 %, which was obviously higher than cotton treated with zein. The functionalized fabrics with zein-DA complex had both hydrophobicity and antioxidant activities.

Therapeutic Potential of Aryl Sulfonamides: Synthesis, Antiproliferative, Antioxidant, Antiparasitic and Molecular Docking Studies

AbstractThis study outlines the synthesis of pyrazine sulfonamides (3 a–3 i) along with halo‐phenyl derivatives (4 a–4 j and 5 a–5 e). The antiproliferative effects were tested against MCF‐7 breast cancer, and colon carcinoma HT‐29, HCT‐116 WT, and HCT‐116 p53 knock‐out mutant cell lines. Compounds 3 b and 3 c were notably active against HCT‐116 WT cells, while 3 e and 3 h were moderately effective against MCF‐7 cells. Among the halo‐phenyl sulfonamides, 4e and 4j were active against MCF‐7 cells, and 5 b was active against HCT‐116 WT cells. The most promising compounds were evaluated against non‐tumorigenic cells, demonstrating cancer selectivity. Compounds 3 b, 3 c, 3 e, 3 h, and 5 b showed dose‐dependent inhibition of colony formation. Compound 3 f exhibited free radical scavenging activity comparable to ascorbic acid. Molecular docking revealed strong binding to thymidylate synthase (3 b, 5 b), Akt‐3 protein kinase (3 e, 3 h, 4 e, 4 j), and tyrosinase (3 f, 3 h). The compounds also exhibited antiparasitic activity against Toxoplasma gondii and Leishmania major, with modifications enhancing selectivity for T. gondii. Substitutions in compounds 4 b and 4 d increased activity against T. gondii while reducing toxicity. Notably, compound 4 f emerged as a T. gondii‐selective lead drug. These findings suggest sulfonamides may help treat complex diseases like cancer and infections.

Synergistic Action of Rutin-Coated Zinc Oxide Nanoparticles: Targeting Biofilm Formation Receptors of Dental Pathogens and Modulating Apoptosis Genes for Enhanced Oral Anticancer Activity.

Oral diseases are often associated with bacterial and fungal pathogens such as Staphylococcus aureus, Streptococcus mutans, Enterococcus faecalis, and Candida albicans. This research explored a novel approach to addressing these pathogens by synthesizing zinc oxide nanoparticles (ZnO NPs) coated with rutin (RT), a plant-derived compound. The synthesized ZnO-RT NPs were comprehensively characterized using UV-Vis spectrophotometer, SEM, and EDAX techniques to confirm their structural composition. The antioxidant potential was assessed through free radical scavenging assays. Additionally, the antimicrobial activity of ZnO-RT NPs was evaluated using a zone of inhibition assay against oral pathogens. Molecular docking studies with the Autodock tool were performed to elucidate the interactions between RT and the receptors of oral pathogens. The findings demonstrated that ZnO-RT NPs exhibited robust free radical scavenging activity. Furthermore, they showed significant antimicrobial activity with a minimal inhibitory concentration of 40 μg/mL against oral pathogens. ZnO-RT NPs also displayed dose-dependent anticancer effects on human oral cancer cells at concentrations of 10, 20, 40, and 80 μg/mL. Mechanistic insights into the anticancer activity on KB cells revealed the upregulation of apoptotic genes. This study underscores the promising potential of ZnO-RT NPs for dental applications due to their strong antioxidant, anticancer, and antimicrobial properties. These nanoparticles offer a hopeful prospect for addressing oral pathogen challenges and enhancing overall oral health.

In Silico and In Vivo Evaluation of Anti-Arthritic Effects of Bakuchiol from Psoralea corylifolia Seeds in Experimental Rat Model.

Rheumatoid arthritis is an autoimmune disease mainly affecting the joints categorized by inflammation, swelling of the synovium and decrease in the joint movement. Bakuchiol, a meroterpene class of natural product present in Psoralea corylifolia known to possess anti-inflammatory effects by a variety of mechanisms. However, its effects in rheumatoid arthritis still remain unclear. In the present investigation, we studied the anti-arthritic effects of bakuchiol via in silico and in vivo experiments. It also showed antioxidant effects measured using DPPH assay where it showed free radical scavenging activity with IC50 value 468.26 μg/ml. Molecular Docking studies carried out on COX-1 (PDB ID: 3 N8Z), COX-2 (PDB ID: 4PH9) and TNF-α (PDB ID: 7JRA), proteins involved in inflammation in arthritis. Bakuchiol showed the maximum binding affinity for TNF-α with binding affinity score is -7.29 kcal/moland less affinity was observed for COX-1 and 2. In vivo antiarthritic effects were studied in arthritic female wistar rats model prepared by intradermal injection of freund's complete adjuvant. Bakuchiol was administered orally at dose of 10,20 and 40 mg/kg for 21 days. Our treatment showed that bakuchiol at 20 and 40 mg/kg exhibited significant anti-inflammatory effects (p<0.001) showed by significant decrease in paw volume, paw diameter, spleen and thymus weight and increase in pain threshold and body weight in arthritic rat model. A significant decrease in hematological parameters such as total leukocyte count (TLC), platelet count, CRP and rheumatoid arthritis factor (RF) and increase in red blood cells count, ESR and hemoglobin further demonstrated that bakuchiol treatment suppresses the progression of adjuvant induced arthritis (AIA) in arthritic rat model. Histological analysis further revealed that bakuchiol ameliorates the pathological manifestations of AIA and reverse the abnormality induced by AIA in rats shown by protection against bone necrosis involved with low influx of inflammatory cells. Therefore, in silico and in vivo results revealed that bakuchiol has the potential to be developed as potent antiarthritic agent.

Multi-functional tyrosinase inhibitors derived from kojic acid and hydroquinone-like diphenols for treatment of hyperpigmentation: Synthesis and in vitro biological evaluation.

A series of multi-functional tyrosinase inhibitors derived from kojic acid (KA) and hydroquinone-like diphenols were designed and synthesized using click chemistry. The in vitro enzymatic assay revealed that all compounds containing a free enolic structure showed excellent activity against tyrosinase (IC50 = 0.14-3.7 µM), being significantly more potent than KA. The most active compounds were catechol (6c) and α-naphthol (6i) analogs with 138- and 96-fold higher potency than KA. On the other hand, all free phenolic compounds (6a-c and 6g-j) derived from aromatic diols showed outstanding free radical scavenging activities superior to KA. Certainly, the α-naphthol derivative 6i with IC50 = 10.1 µM was the most active anti-oxidant, being as potent as quercetin. The SAR analysis indicated that the enolic head of the conjugate molecules mainly contributes to the anti-tyrosinase activity, and the free phenolic part of the molecules can offer anti-oxidant potency. The anti-melanogenic assay of the most promising derivative, 6i, against melanoma (B16F10) cells demonstrated that the prototype compound 6i can significantly reduce the melanin content, more effectively than KA. By using a conjugation strategy, we have improved the tyrosinase inhibitory and radical scavenging activity in the multi-functional agents such as 6i over the parent compound KA, being potentially useful in the treatment of hyperpigmentation and other skin disorders.

Unravelling The Bioactivities of Acmella paniculata Extract-Mediated Green Deep Eutectic Solvent of Citric Acid Monohydrate and Glycerol

Plants are important sources of underlying medicinal value properties. The extraction of bioactive compounds from botanical sources using green solvents has gained interest due to its environmental sustainability. This study highlighted the bioactivities potential of Acmella paniculata extract mediated by green deep eutectic solvent (DES) composed of the citric acid monohydrate and glycerol. Acmella paniculata, a local flowering shrub was selected due to its rich medicinal value compounds. The synergistic effect between plant’s bioactive compounds and DES is capable of enhancing bioactivity, making DES a promising plant solvent extractor candidate. The plant extracts were prepared in leaf and flower parts using the centrifugation method. The phytochemical screening for both extracts showed the presence of terpenoids and steroid constituents which have valuable bioactivity functions. The antibacterial activity assessed by disc diffusion assay exhibited higher susceptible bacterial response of E. coli, Salmonella enterica ser. Typhimurium and S. aureus against the flower extract compared to the leaf extract. The DPPH assay was conducted to assess free radical scavenging activity. The flower extract demonstrated radical scavenging activity (RSA) of 75%-77% while the leaf extract demonstrated 65%-69%. The flower extract results showed higher RSA emphasizing its potential as a natural antioxidant. The anti-inflammatory activity was determined by egg albumin denaturation assay, which showed a greater inhibition rate in flower extract than the leaf extract which was up to 95% and 89% respectively. Thus, both extracts possess an in vitro anti-inflammatory effect. Conclusively, flower extract exhibited better bioactivities value than leaf extract in a green DES. Hence, offering a new insight into its application as an effective alternative in natural product-based therapeutics.

Green-synthesis of silver nanoparticles AgNPs from Podocarpus macrophyllus for targeting GBM and LGG brain cancers via NOTCH2 gene interactions

Brain tumors, particularly Glioblastoma Multiforme (GBM) and Low-Grade Gliomas (LGG), present significant clinical challenges due to their aggressive nature and resistance to conventional treatments. Traditional therapies such as surgery, chemotherapy, and radiation are often limited in efficacy, necessitating novel therapeutic strategies. Nanotechnology, particularly the use of silver nanoparticles (Ag NPs), offers a targeted and potentially more effective approach. This study focuses on the green synthesis of Ag NPs using Podocarpus macrophyllus leaf extract as a reducing agent. The synthesized Ag NPs were characterized for their physicochemical properties, demonstrating a controlled particle size of 13 nm as determined by scanning electron microscopy (SEM). Fourier-transform infrared (FTIR) spectroscopy confirmed the presence of functional groups, and energy-dispersive X-ray (EDX) spectroscopy revealed that silver constituted approximately 90% of the nanoparticle composition. The Ag NPs exhibited promising biological activity, including 90% free radical scavenging (antioxidant) activity, 99.15% inhibition of protein denaturation (anti-inflammatory activity), and 90.56% inhibition of alpha-amylase (anti-diabetic activity). Additionally, the nanoparticles displayed significant anti-hemolytic (89.9% inhibition) and antimicrobial activities, with a 20 mm inhibition zone against Staphylococcus species. Computational analyses further indicated that the NOTCH2 gene, which is upregulated in LGG and GBM, may interact with Ag NPs, suggesting their potential in brain cancer therapy. The green synthesis approach offers a sustainable and bioactive method for producing Ag NPs, underscoring their therapeutic promise for treating GBM and LGG.