Denaturation Of Bovine Serum Albumin Research Articles

Therapeutic evaluation of titanium dioxide nanoparticles based herbal dental varnish derived from rosemary and ginger extracts:A comprehensive investigation into anti-inflammatory and antioxidant properties.

Titanium nanoparticles (NPs) offer promising applications in the treatment and prevention of inflammatory disorders due to their unique physicochemical characteristics. However, additional research is necessary to attain a thorough comprehension and validate the efficacy of this approach in dental practice. This study scrutinizes the anti-inflammatory properties of a dental varnish infused with ginger and rosemary extracts mediated by titanium dioxide (TiO2) nanoparticles. A herbal dental varnish was formulated by integrating ginger and rosemary extracts with titanium dioxide nanoparticles at concentrations of 10, 20, 30, 40, and 50μL. Anti-inflammatory properties were assessed through Bovine Serum Albumin denaturation and membrane stabilization assays, comparing results with a control group. The results reveal concentration-dependent antioxidant and anti-inflammatory properties in the test group when compared to the control group. The BSA assay corroborates increased percent inhibition with rising titanium dioxide nanoparticle concentrations. In line with existing literature, titanium dioxide nanoparticles enhance dental material properties. The bioactive compounds in ginger and rosemary, such as phenolic compounds and terpenes, contribute to anti-inflammatory and antioxidant effects of the varnish. Additionally, the therapeutic potential of titanium dioxide nanoparticles in addressing inflammatory diseases underscores their significance in this formulation.

Green Synthesis of Guilandina bonduc Seed Extract Mediated Silver Nanoparticles and Its Anti-Inflammatory Activity

Green synthesis is a promising approach for the synthesis of silver nanoparticles (AgNPs) that is environmentally friendly and sustainable. In this study, we report a green method for the synthesis of AgNPs using Guilandina bonduc seed extract. The seed extract was used as a reducing and capping agent for the synthesis of AgNPs. The prepared nanoparticles were evaluated for its anti-inflammatory activity using Bovine serum albumin denaturation assay and Egg albumin denaturation assay. The AgNPs also showed significant anti-inflammatory activity in vitro. The results show that the green synthesised silver nanoparticles have excellent anti-inflammatory activity. The results of this study suggest that the green synthesised AgNPs have potential application in the treatment of inflammation. These findings also highlight the potential of Guilandina bonduc seed extract as a source of natural compounds for the green synthesis of AgNPs with biological activity.

EVALUATION OF ANTIDIABETIC, ANTI-INFLAMMATORY, AND ANTIOXIDANT ACTIVITIES OF DIFFERENT FRACTIONS OF ETHANOLIC EXTRACT OF LEAVES OF Bauhinia variegata BY In vitro METHOD AND ISOLATION OF PHYTOCONSTITUENTS

Today, diabetes is a common morbidity, and the occurrence of the disease is attributed to various pathophysiological states of the human body, including inflammation and free radical oxidants. Previous types of research also reported the involvement of free radical oxidants in the development of secondary complications of diabetes. The scavenging of free radicals by antioxidants turns out to be a defense mechanism and can also alter disease states. Therefore, the study was designed to evaluate the properties of Bauhinia variegata L. leaves in controlling diabetes, inflammation, and free radicals. The ethanolic leaf extract was prepared and the extract was then fractionated with solvents, which were further used to perform pharmacological screening by in vitro methods. The IC50 values of the chloroform fraction (BVC) of leaf extract were recorded as the lowest among the test materials for all in vitro studies. The IC50 values of BVC in the study of inhibition of α-amylase and α-glucosidase enzymes were 31.08±1.53 and 25.33±1.52 g/mL, respectively. In the study of inhibition of bovine serum albumin and egg albumin denaturation, BVC showed efficacy with IC50 values of 23.75±1.35 and 28.15±1.32 g/mL, respectively. The fraction showed free radical scavenging activity in DPPH and nitric oxide assay, with IC50 values of 27.78±1.61 and 34.93±1.49 g/mL, respectively. In addition, two pure compounds, namely chrysoeriol and β-amyrin palmitate, were isolated from this bioactive fraction. Thus, the results proved all the claimed pharmacological effects of the leaves of Bauhinia variegata L. and also justified the hypothesis of the current study.

Evaluation of Anti-inflammatory, Antioxidant and Antimicrobial Activity of Pomegranate Peel Extract: An In-vitro Study

Introduction: Pomegranate fruit contains biologically active compounds that provide anti-inflammatory properties. Byproducts of pomegranate and punicalagins inhibit the growth of pathogens while enhancing the growth of beneficial bacteria. The beneficial effects of phenolic compounds are exhibited in scavenging free radicals. Aim: To evaluate the anti-inflammatory, antioxidant, and antimicrobial activity of Pomegranate Peel Extract (PPE). Materials and Methods: The present in-vitro study was designed and carried out at the Nanobiomedicine Laboratort, Department of Pharmacology, Saveetha Dental College and Hospitals, Chennai, Tamil Nadu, India, from June 2021 to August 2021. The anti-inflammatory activity was evaluated using the Egg Albumin Denaturation assay (EA) and Bovine Serum Albumin Denaturation assay (BSA). The measurement of antioxidant activity was conducted using the 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) assay, Hydrogen peroxide radical scavenging (H2O2) assay, and Ferric Reducing Antioxidant Power (FRAP) assay. Antimicrobial activity was evaluated using the agar well diffusion method. The microorganisms used to evaluate the antimicrobial effect of PPE were S. mutans, S.aureus, E.faecalis, and C.albicans. Results were analysed using independent t-tests, Analysis of Variance (ANOVA) and Tukey’s Honestly Significant Difference (HSD). Results: Anti-inflammatory activity was observed with high concentrations of 40 and 50 µL in EA (70.06%±0.15, 78.08%±0.21) and BSA (75.50%±3.90, 80.82%±3.38) assays. Pronounced antioxidant activity of PPE was seen with higher concentrations of 40 and 50 µL in DPPH (88.17%±0.69, 92.50%±1.23), H2O2 (78.22%±0.94, 88.99%±1.03), and FRAP (78.43%±1.25, 88.49%±0.67) assays. The antimicrobial activity was highest at 100 µL for S.mutans (38±2.62 mm), S.aureus (36±3.16 mm), E.faecalis (21±1.48 mm), and C.albicans (23±2.36 mm). Conclusion: The study concluded that PPE has antiinflammatory, antioxidant and antimicrobial properties and these properties are concentration-dependent.

Anti-inflammatory Activities of Sulfated Polysaccharides From Ethanol Crude Extract of Spyrida Species Red Seaweed.

The extracts derived from red seaweed have shown characteristics that may reduce inflammation. The abovementioned effects can potentially provide positive outcomes in managing inflammatory illnesses, including arthritis, inflammatory bowel disease, and other skin problems. The polysaccharides were isolated from theSpyridaspecies. The water-soluble polysaccharides were extracted and fractionated from several Indian seaweeds (Red) using a simple, cost-effective approach. Anti-inflammatory effects were further evaluated and validated by FTIR and FESEM analyses. FT-IR and FESEM were used to assess the structural features of polysaccharides and the surface morphology. In addition, the red seaweed species of the genusSpyrida, which includes polysaccharides, was shown to significantly inhibit the denaturation of bovine serum albumin (BSA), further proving that the substance has anti-inflammatory qualities. In this work, an assay to suppress protein activity was utilized to investigate the potential anti-inflammatory effects of polysaccharides derived from Spyrida.As predicted, increasing concentrations of the extract, ranging from 25 to 100 µg/ml, led to a rise in the percentage of inhibited protein denaturation. A statistically significant difference was found between these findings and those obtained with aspirin, a commonly used non-steroidal anti-inflammatory medicine (NSAID). The red algae that grow in the shallow waters of the southern Indian Ocean may be used in medicine.

Design, synthesis, biological evaluation, and in silico studies of quinoxaline derivatives as potent p38α MAPK inhibitors.

A new series of quinoxaline derivatives possessing the hydrazone moiety were designed, synthesized, and screened for in-vitro anti-inflammatory activity by the bovine serum albumin (BSA) denaturation technique, and for antioxidant activity, by the (2,2'-diphenyl-1-picrylhydrazyl(DPPH) radical scavenging assay. The synthesized compounds were also tested for p38α mitogen-activated protein (MAP) kinase inhibition. The in-vivo anti-inflammatory activity was assessed by the carrageenan-induced rat paw edema inhibition method. All the compounds (4a-n) exhibited moderate to high in-vitro anti-inflammatory activity. Compound 4a displayed the highest inhibitory activity in the BSA assay (83.42%) in comparison to the standard drug diclofenac sodium (82.90%), while 4d exhibited comparable activity (81.87%). The DPPH assay revealed that compounds 4a and 4d have free radical scavenging potential (74.70% and 74.34%, respectively) comparable to the standard butylated hydroxyanisole (74.09%). Furthermore, the p38α MAP kinase inhibition assay demonstrated that compound 4a is highly selective against p38α MAP kinase (IC50 = 0.042) in comparison to the standard SB203580 (IC50 = 0.044). The five most active compounds (4a-4d and 4f) with good in-vitro profiles were selected for in-vivo anti-inflammatory studies. Compounds 4a and 4d were found to display the highest activity (83.61% and 82.92% inhibition, respectively) in comparison to the standard drug diclofenac sodium (82.65% inhibition). These compounds (4a and 4d) also exhibited better ulcerogenic and lipid peroxidation profiles than diclofenac sodium. The molecular docking and molecular dynamics simulation studies were also performed and found to be in agreement with the p38α MAP kinase inhibitory activity.

Exploring the therapeutic potential of Prinsepia utilis Royle seed oil: A comprehensive study on chemical composition, physicochemical properties, anti-inflammatory, and analgesic activities

Ethnopharmacological relevancePrinsepiautilis (PU) Royle, native to the Himalayan region, is a deciduous thorny shrub with numerous traditional uses of its roots, leaves and seeds for treatment of conditions such as rheumatic pain, joint pain, arthritis, and inflammation. Aim of the studyKeeping in mind the growing demand of products of natural origin as alternate medicine, the present study was undertaken to scientifically validate for the first time the traditional claims of healing pain and inflammation by evaluating the fatty oil isolated from the seeds using established in vitro and in vivo models. Materials and methodsPU Seeds were Soxhlet extracted using n-hexane and fatty oil was isolated. Chemical composition of the oil was established with the aid of Gas Chromatography-Flame Ionization Detection (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS). The oil was then subjected to in vitro anti-inflammatory activity by following the established protocols of trypsin inhibitory and bovine serum albumin denaturation assays. The acute toxicity of the oil was also studied using OECD guidelines 423. The anti-inflammatory property of the oil was further evaluated using carrageenan-induced and formalin-induced edema in the rat paw. Moreover, hot plate latency and tail immersion assay were employed to evaluate analgesic activity of the oil. To establish the quality of the oil, various physicochemical properties were also studied. ResultsGC-FID and GC-MS analysis of the oil revealed the presence of linoleic acid (59.06 ± 0.00%), oleic acid (28.11 ± 0.01%), palmitic acid (9.51 ± 0.01%) and stearic acid (3.32 ± 0.01%). In vitro trypsin inhibitory and bovine serum albumin denaturation assay revealed dose-dependent notable activity of the oil with IC50 value of 63.57 μg/mL and 518.14 μg/mL, respectively. The physico-chemical characterization demonstrated that the oil possesses a low acidity and a high oxidative stability index. The oil was found to be non-toxic and displayed effective anti-inflammatory activities with significant inhibition till 4 h in carrageenan-induced and formalin-induced rat paw edema at maximum tested dose of 200 mg/kg b.w. The oil also exhibited significant results in hot plate latency and tail immersion assay with positive effects showing up to 4 h after dose administration. ConclusionThese findings, besides supporting the traditional claims, suggest that P. utilis seed oil has potential therapeutic applications as a natural anti-inflammatory and analgesic agent. Further studies are warranted to explore its mechanisms of action and potential use in pharmaceutical and nutraceutical industries.

Antinociceptive and Anti-inflammatory Properties of Triumfetta cordifolia A. Rich. (Tiliaceae) Root Methanol/Dichloromethane Extract

Objective: Triumfetta cordifolia is a terrestrial plant of the Tiliaceae family used traditionally for the treatment of many diseases. Different parts are traditionally used for the treatment of diseases that cause pain and inflammation. This study aims to evaluate the antinociceptive and anti-inflammatory activities of the methanol/dichloromethane extract of T. cordifolia roots in animal models.
 Methodology: Phytochemical screening and the toxicity study of methanol/dichloromethane extract of Triumfetta cordifolia roots were performed. Antinociceptive activity was evaluated using acetic acid and formalin tests. In vitro anti-inflammatory activity was evaluated using the bovine serum albumin (BSA) denaturation method and In vivo on carrageenan-induced oedema. The extract was given orally at doses of 50, 100 and 150 mg/kg of body weight.
 Results: The phytochemical analysis revealed the presence of alkaloids, saponins, flavonoïds, polyphenols, reducing sugars, tannins, coumarins and steroids. No signs of toxicity were observed after 14 days experiment. Regarding antinociceptive activity, Triumfetta cordifolia (200 mg/kg) has decreased significantly (P ˂ 0.0001) the number of abdominal contortions and also significantly inhibited the formalin-induced neurogenic pain at the dose of 50 mg/kg body weight. In anti-inflammatory tests, the extract inhibited oedema (P˂ 0,001) at 50mg/kg at the fourth hour and also protected the serum albumin bovine denaturation (P <0.05) at a concentration of 50 μg/ml.
 Conclusion: The results obtained indicate that the methanol/dichloromethane extract is without acute toxicity and has peripheral and central analgesic properties, as well as anti-inflammatory properties In vivo and In vitro.

Evaluation of the Anti-inflammatory, Antimicrobial, Antioxidant, and Cytotoxic Effects of Chitosan Thiocolchicoside-Lauric Acid Nanogel.

The present study explored the anti-inflammatory, antimicrobial, antioxidant, and cytotoxic effects of a combination of chitosan thiocolchicoside and lauric acid (CTLA) nanogel. Materials and methods: A nanogel formulation of thiocolchicoside and lauric acid was developed and tested for potential applications. The antimicrobial activity was assessed using the well diffusion method, while the antioxidant activity was evaluated using the 2,2-diphenyl-1-picryl hydrazyl (DPPH) free radical scavenging assay and hydrogen peroxide (H2O2) antioxidant assay methods. The anti-inflammatory activity was determined through the egg albumin denaturation method, the bovine serum albumin denaturation method, and the membrane stabilization assay. A brine shrimp lethality assay was used to study the cytotoxic effect of the nanogel. We identified significant positive outcomes for the CTLAnanogel. The results showed a percentage of inhibition of 81% at 50μg/mL, which showed the nanogel's significant anti-inflammatory activity by inhibiting bovine serum albumin denaturation. The anti-inflammatory properties of the nanogel were comparable to the standard diclofenac sodium at all tested concentrations. The egg albumin denaturation assay results revealed a percentage inhibition of 76% at 50 μg/mL. In the membrane stabilization assay, a percentage inhibition of86%was obtained at a concentration of 50 μg/mL against 89% for the standard drug. The nanogel exhibited a zone of inhibition of 20 mm against Streptococcus mutans and 22 mm with a dilution of 100 µg/mL of CTLA nanogel against Staphylococcus aureus. The antioxidant activity was studied by using the DPPH method, 50 μg/ml has an 89% inhibition, which was similar to the standard. The inhibitory activity of CTLAnanogel at 50 μg/ml was81.6%in the hydroxyl free radical scavenging assay, which was comparable to the standard drug. At 5 μg/mL concentration of CTLA nanogel, approximately 90% of the nauplii remained alive after 48 hours. The CTLAnanogel showed excellent anti-inflammatory and antioxidant properties suggesting its potential for managing inflammatory conditions and oxidative stress-related disorders.

Unveiling the Chemical Profiling Antioxidant and Anti-Inflammatory Activities of Algerian Myrtus communis L. Essential Oils, and Exploring Molecular Docking to Predict the Inhibitory Compounds against Cyclooxygenase-2.

Considering the large spectrum of side effects caused by synthetic drugs and the development of natural alternatives utilizing Algerian flora, this study aimed to place a spotlight on the chemical profile and antioxidant and anti-inflammatory activities of Myrtus communis L. essential oils (MCEOs). In this study, essential oils (EOs) were collected via hydro-distillation of the plant's leaves, and a chemical constituent analysis was performed using gas chromatography-mass spectrophotometry (GC-MS). The in vitro antioxidant activity was evaluated using DPPH, ABTS, and hydroxyl radical scavenging tests. The in vitro anti-inflammatory capacity was estimated by studying the antidenaturation effect using bovine serum albumin (BSA) as a protein model. The in vivo anti-inflammatory activity was carried out by utilizing the classical model of carrageenan-induced paw edema in rats, using diclofenac (DCF) as the reference drug. Moreover, the molecular interaction of the compounds obtained from the GC-MS analysis was studied within the binding site of cyclooxygenase-2 (COX-2) using an in silico approach as the confirmatory tool of the in vitro and in vivo experiments. The GC-MS analysis revealed that MCEOs were mainly composed of oxygenated monoterpenes (70.56%), oxygenated sesquiterpenes (3.1%), sesquiterpenes (4.17%), and monoterpenes (8.75%). Furthermore, 1,8-cineole was the major compound (19.05%), followed by cis-geranyl acetate (11.74%), methyl eugenol (5.58%), α-terpineol (4.62%), and β-myrcene (4.40%). MCEOs exhibited remarkable concentration-dependent free radical scavenging activity, with an IC50 of 15.317 ± 0.340 µg/mL, 18.890 ± 2.190 µg/mL, and 31.877 ± 0.742 µg/mL for DPPH, ABTS, and hydroxyl radical, respectively. The significant in vitro anti-inflammatory activity due to the inhibition of BSA denaturation was proportional to the EO concentration, where the highest value was recorded at 100 μg/mL with an approximately 63.35% percentage inhibition and an IC50 of 60.351 ± 5.832 μg/mL. MCEOs showed a good in vivo anti-inflammatory effect by limiting the development of carrageenan-induced paw thickness. The in silico study indicated that, among the 60 compounds identified by the GC-MS analysis, 9 compounds were observed to have a high binding energy to cyclooxygenase-2 as compared to diclofenac. Our study revealed that EOs from Algerian Myrtus communis L. can be considered to be a promising candidate for alleviating many debilitating health problems and may provide new insights in the fields of drug design, agriculture, and the food industry.

Hypoglycemic, anti-inflammatory, and anti-aging potential of Canthium coromandelicum (Burm.f.) Alston leaf extracts: In vitro and in silico ADMET studies

The present study focused on the hypoglycemic, anti-inflammatory and anti-aging effects of Canthium coromandelicum (Burm.f.) Alston leaf extract by in vitro and in silico analyses. In vitro antidiabetic activities were studied by α-amylase and α-glucosidase enzyme inhibition assays. The anti-inflammatory activity was analysed by bovine serum albumin denaturation assay and anti-aging activity by the inhibition of tyrosinase enzyme. The molecular docking study was undertaken to examine the binding mode and interactions of reported compounds of the hydroalcoholic extract of C. coromandelicum leaf with 7TAA, 3WY1, 2Y9X, and 4COX proteins. The plant exhibited promising antidiabetic effects with an inhibition of 86.09% against α-amylase and 83.53% against α-glucosidase enzymes. The extract had a notable anti-inflammatory activity with an inhibition range of 50.23 to 73.17%. The anti-aging activity showed 50.31 to 76.78% of inhibition in anti-tyrosinase assay with a potential effect in hyperpigmentation. In molecular docking analysis, the compounds like linoleic acid, phytol, methyl linoleate, palmitic acid and ethyl octa-decanoate had potent inhibitory activities against 7TAA, 3WY1, 2Y9X and 4COX proteins (6.90 to -4.42 kcal/mol) especially linoleic acid was found to be highly effective (-6.11 kcal/mol) antidiabetic effect with notable binding scores. The obtained results suggest that phytoconstituents identified from the plant have the potential in controlling diabetes by inhibiting α-amylase and α-glucosidase enzymes with promising anti-inflammatory and anti-aging properties. However, further research is required to ascertain its potential effect in experimental animals and isolation of bioactive compounds.

ANTI-INFLAMMATORY STUDY (IN-VITRO AND IN-VIVO) AND HPTLC DENSITOMERIC DETERMINATION OF QUERCETIN FROM METHANOLIC LEAF EXTRACT OF HOTTUYNIA CORDATA THUNB. FROM MIZORAM, INDIA

Objective: This study aimed to investigate the anti-inflammatory activity of the methanolic leaf extract of Houttuynia cordata Thunb. from Mizoram, India, using in-vitro and in-vivo models. In addition, the study also aimed to determine the quercetin content of the methanolic leaf extract using high-performance thin-layer chromatography (HPTLC) densitometry. Methods: The methanolic leaf extract of H. cordata was prepared using successive Soxhlet extraction, and its anti-inflammatory activity was evaluated using in-vitro models such as inhibition of protein denaturation and inhibition of proteinase activity. The in-vivo anti-inflammatory activity of the extract was evaluated using carrageenan-induced paw edema in rats. The quercetin content of the extract was determined using HPTLC densitometry. Results: The methanolic leaf extract of H. cordata showed significant anti-inflammatory activity in both in-vitro and in-vivo models. The extract exhibited a dose-dependent inhibition of protein denaturation and proteinase activity and also significantly reduced paw edema in the rat model. The IC50 values of egg albumin and bovine serum albumin denaturation studies were 317.365 μg/mL and 198.918 μg/mL, respectively. The results showed that the methanolic leaf extract of the plant was 200 mg/kg b.w. and 400 mg/kg b.w., which considerably reduced carrageenan-induced paw edema, and their effects were comparable to those of the standard diclofenac sodium. The HPTLC densitometry analysis revealed the presence of quercetin in the extract, with a quercetin content of 21.8 ng/μL. Conclusion: The methanolic leaf extract of H. cordata Thunb. from Mizoram, India demonstrated significant anti-inflammatory activity in both in-vitro and in-vivo models. The presence of quercetin in the extract may contribute to its anti-inflammatory properties. These findings provide scientific evidence for the traditional use of H. cordata as an anti-inflammatory agent.

Kei-apple-mediated NiO nanoparticles and biological studies: anti-inflammatory and cytotoxicity study against HeLa and HEK 293 cell lines

Nickel oxide (NiO) nanoparticles are gaining popularity in multiple fields owing to their useful properties. The application in biomedicine has been further enhanced by combining them with plant extracts that possess unique biological properties. In this report, NiO nanoparticles were synthesized by mediating the reaction process with the leaf extracts of Kei-apple (Dovyallis Caffra), a local fruit tree found in South Africa. Various characterization techniques such as x-ray diffraction (XRD), V–Vis spectroscopy (UV–Vis), transmission electron microscope (TEM), Scanning electron microscope (SEM), and Energy dispersive x-ray analysis (EDX) were employed to establish the different physicochemical properties of the prepared NiO material. The XRD report obtained confirmed the formation of NiO nanoparticles with an average crystallite size of 9 mm. Furthermore, the microscopic techniques showed that the material possessed a spherical-shaped structure, with diameter sizes smaller than 27.18 nm (average size of about 11 nm). The purity of the material was shown in the EDX analysis, in which the primary composition was only the elemental constituents of the NiO nanoparticles. The nanoparticles exhibited good cytotoxicity comparable to the 5-Fluorouracil in both the Human embryo kidney (HEK 293) and Human cervical cancer (HeLa) cell lines, with a half maximal inhibitory concentration (IC50) value of 0.00015 and 13.8 μg ml−1, respectively. The anti-inflammatory study, on the other hand, exhibited a weak anti-inflammatory effect in the used Bovine serum albumin denaturation assay. The finding here thus suggests that the Kei-apple mediated NiO nanoparticles can be safely used in different fields without causing any appreciable harm to the human body due to the specificity to the cancerous cell line and the observed weak viability in the used non-cancerous embryonic kidney cells.

Green Synthesised TiO2 Nanoparticles-Mediated Terenna asiatica: Evaluation of Their Role in Reducing Oxidative Stress, Inflammation and Human Breast Cancer Proliferation.

Oxidative stress and chronic inflammation interplay with the pathogenesis of cancer. Breast cancer in women is the burning issue of this century, despite chemotherapy and magnetic therapy. The management of secondary complications triggered by post-chemotherapy poses a great challenge. Thus, identifying target-specific drugs with anticancer potential without secondary complications is a challenging task for the scientific community. It is possible that green technology has been employed in a greater way in order to fabricate nanoparticles by amalgamating plants with medicinal potential with metal oxide nanoparticles that impart high therapeutic properties with the least toxicity. Thus, the present study describes the synthesis of Titanium dioxide nanoparticles (TiO2 NPs) using aqueous Terenna asiatica fruit extract, with its antioxidant, anti-inflammatory and anticancer properties. The characterisation of TiO2 NPs was carried out using a powdered X-ray diffractometer (XRD), Fourier transform infrared (FTIR), scanning electron microscopy (SEM), energy-dispersive X-ray diffraction (EDX), high-resolution transmission electron microscopy (HR-TEM), dynamic light scattering (DLS), and zeta-potential. TiO2 NPs showed their antioxidant property by scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals in a dose-dependent manner with an IC50 value of 80.21 µg/µL. To ascertain the observed antioxidant potential of TiO2 NPs, red blood cells (RBC) were used as an in vitro model system. Interestingly, TiO2 NPs significantly ameliorated all the stress parameters, such as lipid peroxidation (LPO), protein carbonyl content (PCC), total thiol (TT), superoxide dismutase (SOD), and catalase (CAT) in sodium nitrite (NaNO2)-induced oxidative stress, in RBC. Furthermore, TiO2 NPs inhibited RBC membrane lysis and the denaturation of both egg and bovine serum albumin, significantly in a dose-dependent manner, suggesting its anti-inflammatory property. Interestingly, TiO2 NPs were found to kill the MCF-7 cells as a significant decrease in cell viability of the MCF-7 cell lines was observed. The percentage of growth inhibition of the MCF-7 cells was compared to that of untreated cells at various doses (12.5, 25, 50, 100, and 200 µg/mL). The IC50 value of TiO2 NPs was found to be (120 µg/mL). Furthermore, the Annexin V/PI staining test was carried out to confirm apoptosis. The assay indicated apoptosis in cancer cells after 24 h of exposure to TiO2 NPs (120 µg/mL). The untreated cells showed no significant apoptosis in comparison with the standard drug doxorubicin. In conclusion, TiO2 NPs potentially ameliorate NaNO2-induced oxidative stress in RBC, inflammation and MCF-7 cells proliferation.

In vitro and in silico studies on novel N-substituted-3,5-diaryl-pyrazoline derivatives as COX-2 inhibitors and anti-inflammatory agents

The presence of a reactive α,β-unsaturated keto group along with substituted aryl ring improves biological profile of pyrazoline nucleus. Considering this fact a study was planned to synthesize novel pyrazoline derivatives incorporated with chalcone backbone and their evaluation as COX-2 inhibitors and anti-inflammatory agents. Bovine serum albumin denaturation assay was used to measure in vitro anti-inflammatory activity. Molecular docking study was performed using Schrödinger-Maestro 9.0 molecular docking software and cyclooxygenase-2 (COX-II) receptor PDB ID: 4-COX. Some of the synthesized compounds showed remarkable anti-inflammatory potential. The compound (E)-3-(4-hydroxyphenyl)-1-(3-(4-hydroxyphenyl)-5-phenyl-4,5-dihydropyrazol-1-yl)prop-2-en-1-one 6d was found to be the most potent anti-inflammatory agents with 69.88% inhibition of protein denaturation. The outcome of docking study also supported results of in vitro anti-inflammatory activity and docking score for compound 6d was found to be –6.70379 which was comparable to the co-crystallized ligand. The results reveal that the synthesized compound can serve as potential lead for the development of novel anti-inflammatory agents.

Therapeutic Potential of Alstonia scholaris Latex in the Management of Inflammatory Diseases: An in vitro Approach

Pharmacognosy Research,2023,15,3,478-483.DOI:10.5530/pres.15.3.049Published:June 2023Type:Original Article Authors:Bapan Banik, and Malay Kumar Das Author(s) affiliations:Bapan Banik, Malay Kumar Das* Department of Pharmaceutical Sciences, Drug Delivery Research Laboratory, Dibrugarh University, Dibrugarh, Assam, INDIA. Abstract:Background: The different parts of Alstonia scholaris (AS) viz. leaf, bark root, and latex are used traditionally to treat pain, swelling, stiffness, immune deficiency, malaria, ulcer, and arthritis. The traditional healers in Dhemaji district of Assam prescribe raw AS latex for topical treatment of inflammatory diseases. The unique feature of this study is that the AS latex has been evaluated scientifically for the first time for its anti-inflammatory properties. Objectives: The present investigation evaluates the anti-inflammatory potential of the AS latex in arthritis using in vitro assays. Materials and Methods: Anti-arthritic potential of AS latex was evaluated using in vitro assays of bovine serum albumin (BSA) denaturation, egg albumin denaturation, and human red blood cell (HRBC) membrane stabilization. Results: It was observed that the standard diclofenac sodium and the AS latex showed good anti-arthritic potential. In BSA denaturation method, the latex, and diclofenac sodium showed 71.59% and 85.23% inhibition of proteinase enzyme at 250 μg/mL, respectively. In the egg albumin denaturation method, the latex, and standard showed the maximum percentage of inhibition of protein denaturation of 70.42% and 81.32%, respectively, at 250 μg/mL. In the HRBC membrane stabilization model, the latex produced considerable anti-arthritic potential in a concentration–dependent manner. At 250 μg/ mL in hypotonic solution, latex, and diclofenac sodium showed 68.77% and 72.12% membrane stabilization, respectively. Conclusion: The present investigation proved the antiarthritic activity of AS latex. It may also be used in the management of other inflammatory diseases. Keywords:Alstonia scholaris, Anti-arthritic, Anti-inflammatory, in vitro., LatexView:PDF (226.19 KB)

Curative potential of Populus ciliata Wall ex. Royle extract against adjuvant-induced arthritis and peripheral neuropathy in Wistar rats.

Populus ciliata (PCCR) is traditionally used to treat muscular swelling, inflammation, pain, and fever. The current study was designed to validate the potential of aqueous ethanolic extract of the plant against inflammation, peripheral neuropathy, and pain in arthritic rats. The PCCR was chemically characterized by gas chromatography-mass spectroscopy and high-performance liquid chromatography. In vitro antioxidant, and in vitro anti-inflammatory assays were carried out on PCCR. For anti-arthritic potential, Wistar rats' rear paws were injected with 0.1ml Complete Freund's Adjuvant using methotrexate (3mg/kg/week) as standard control. PCCR at 100, 200, and 400mg/kg was given orally to arthritic rats for 21days. The PCCR exhibited significant inhibition of bovine serum albumin denaturation (IC-50: 202.1µg/ml), egg albumin denaturation (IC-50:553.5mg/ml) and RBC membrane stabilization (IC-50: 122.5µg/ml) and antioxidant (IC-50 = 49.43µg/ml) activities. The PCCR notably decreased the paw diameter and increased body weight of treated arthritic animals as equated to diseased control. The treatment notably (p < 0.05-0.0001) decreased malondialdehyde, and increased superoxide dismutase, reduced glutathione, and catalase in the liver and sciatic nerve homogenate in compared to diseased rats. The PCCR treatment remarkably (p < 0.05-0.0001) regulated the levels of nor-adrenaline and serotonin in sciatic nerve in contrast to diseased rats. Treatment with PCCR improved the motor activity, pain, ligament degeneration, and synovial hyperplasia in arthritic rats. Moreover, PCCR significantly (p < 0.01-0.0001) decreased the IL-6 and TNF-α. It is evident from the current study that PCCR had ameliorated polyarthritis and peripheral neuropathy through reduction of inflammatory markers, and improvement of oxidative stress might be due to presence of phenolic acids, flavonoids, phytosterols, and other fatty acids.

Synthesis of (E)-N'-(Pyridine-2-ylmethylene) Picolino Hydrazide with Promising Antimicrobial and Anti-inflammatory Activities Along with their In-silico Studies

In recent years, there has been a significant amount of interest in hydrazide-hydrazone compounds as a result of their extensive use in the pharmaceutical industry. In this study, the new compound (E)-N'-(pyridin-2-ylmethylene) picolino hydrazide, with the formula C20H19N3O2, was synthesised and confirmed using different spectroscopic techniques. The newly synthesised compound was tested for anti-inflammatory and antibacterial properties in vitro. The results of an in vitro anti-inflammatory activity test using the denaturation of bovine serum albumin as the measurement kit revealed a highly effective inhibitory effect. In addition, the results of the antimicrobial test showed that the compound demonstrated a maximum zone of inhibition (18.2 mm) against the Staphylococcus aureus strain at a higher concentration (32 μg/ml) of the tested sample (32 g/ml), which is greater than the standard drug (ciprofloxacin: 17.5 mm). The antifungal activity of (E)-N'-(pyridin-2-ylmethylene) picolinohydrazide indicated a maximum inhibition zone of 9.2 mm at a higher concentration (32 μg/ml) of the tested sample, which is comparable to that of the standard drug (ketoconazole: 9.0 mm). The anti-inflammatory activity performed by the carrageenan-induced paw edema method also gave a promising result. Molecular docking analysis revealed that the active compounds had a higher docking score and interacted effectively with the target protein. In silico molecular docking, results revealed the COX-5 and LL-37 (residues 17–29) proteins mainly depends on H-bonds between the pyridine groups of the synthesized ligand and the catalytic residues of the binding site, π-cation/anion interactions, (iii) π-alkyl interactions, and formation of carbon-hydrogen bond, π- π bond that stabilizes the interaction with the active site. Among the analogs of the hydrazine hydride class, the newly synthesized compound: (E)-N'-(pyridin-2-ylmethylene) picolino hydrazide proved to be a vital bioactive molecule.

Antiarthritic potential of the butanol fraction of Sesuvium sesuvioides: An in vitro, in vivo, and in silico evaluation.

Sesuvium sesuvioides (Fenzl) Verdc (Aizoaceae) has been traditionally used in the treatment of inflammation, arthritis, and gout. However, its antiarthritic potential has not been evaluated scientifically. The current study was designed to assess the antiarthritic properties of the n-butanol fraction of S. sesuvioides (SsBu) by phytochemical analysis, in vitro and in vivo pharmacological activities, and in silico studies. Phytochemical analysis showed total phenolic contents (90.7 ± 3.02mg GAE/g) and total flavonoid contents (23.7 ± 0.69mg RE/g), and further analysis by GC-MS identified possible bioactive phytocompounds belonging to phenols, flavonoids, steroids, and fatty acids. The in vitro antioxidant potential of SsBu was assessed by DPPH (175.5 ± 7.35mgTE/g), ABTS (391.6 ± 17.1mgTE/g), FRAP (418.2 ± 10.8mgTE/g), CUPRAC (884.8 ± 7.97mgTE/g), phosphomolybdenum (5.7 ± 0.33mmolTE/g), and metal chelating activity (9.04 ± 0.58mg EDTAE/g). Moreover, in the in vitro studies, inhibition (%) of egg albumin and bovine serum albumin denaturation assays showed that the anti-inflammatory effect of SsBu at the dose of 800μg/ml was comparable to that of diclofenac sodium used as a standard drug. The in vivo antiarthritic activity was assessed to determine the curative impact of SsBu against formalin-induced (dose-dependent significant (p < 0.05) effect 72.2% inhibition at 750mg/kg compared to standard; 69.1% inhibition) and complete Freund's adjuvant-induced arthritis (40.8%; inhibition compared to standard, 42.3%). SsBu significantly controlled PGE-2 level compared to the control group (p < 0.001) and restored the hematological parameters in rheumatoid arthritis. Treatment with SsBu significantly reduced oxidative stress by reinstating superoxide dismutase, GSH, and malondialdehyde along with pro-inflammatory markers (IL-6 and TNF-α) in arthritic rats. Molecular docking revealed the antiarthritic role of major identified compounds. Kaempferol-3-rutinoside was found to be more potent for COX-1 (-9.2kcal/mol) and COX-2 inhibition (-9.9kcal/mol) than diclofenac sodium (COX-1, -8.0 and COX-2, -6.5kcal/mol). Out of the 12 docked compounds, two for COX-1 and seven for COX-2 inhibition showed more potent binding than the standard drug. The results from the in vitro, in vivo, and in silico approaches finally concluded that the n-butanol fraction of S. sesuvioides had antioxidant and antiarthritic potential, which may be due to the presence of potential bioactive compounds.

Phytochemical analysis and synergistic antimicrobial potential of extracts from Carica papaya and Betavulgaris

Antibiotics are losing their efficacies at an alarming rate due to antibiotic resistance. The current study aimed to explore the phytochemical composition of Carica papaya and Betavulgaris and to assess their antibiotic potential individually and in synergy. The antimicrobial potential of C. papaya and Beta vulgaris crude methanolic leaves extracts and their combinations with commercially available antibiotics against multidrug resistant bacterial strains was evaluated. The extracts were more active against Staphylococcus aureus with the ZOI of 26 and 24 ​mm. In synergy with ampicillin, ciprofloxacin, erythromycin and tetracycline, the methanolic extracts were more active against Acinetobacter baumannii followed by Klebsiella pneumoniae with the ZOI ranging between 16 and 25 ​mm. The In-vitro anti-inflammatory potential of C. papaya and B. vulgaris was assessed by bovine serum albumin denaturation assay. The methanolic extracts of C. papaya and B. vulgaris prevent the denaturation of albumin protein in a dose-dependent manner with the IC50 of 982 and 1597 ​μg/ml respectively. Gas chromatography-Mass spectrometric analysis revealed the presence of bioactive phyto-constituents with the major peaks. The current study affirmed that the efficacy of antibiotics was enhanced when screened in combination with methanolic extracts of C. papaya and B. vulgaris and they can serve as a natural source of obtaining therapeutically valued metabolites against irresistible microbial infections and inflammation related diseases.