Diclofenac Research Articles

Formulation of Neem and Echinacea Gel for Oral Health Along With the Evaluation of Antimicrobial, Cytotoxic, Anti-inflammatory, and Free Radical Scavenging Activity: An In Vitro Study.

Background Herbs have been used in medical practice for centuries and continue to play a significant role in modern complementary and alternative medicine.Phytochemicals in these herbs possess strong antioxidant and anti-inflammatory properties, which are beneficial in targetingoral health issues, such as dental plaque, gingivitis, and oral microbial infections.As research progresses, the challenge remains to translate these natural compounds into safe, effective, and accessible treatments for a wide range of diseases. Aim The aim of this research was to formulate the neem and echinacea gel along with the evaluation of antimicrobial, anti-inflammatory, free-radical scavenging activity, and cytotoxic potential. Materials and methods The neem and echinacea gel was prepared using a concentrated powdered mixture of neem and echinacea (5 grams each) to which 100 ml of distilled water was added, and the mixture was boiled for 30 minutes at 60°C. The 10 ml concentrate was mixed with 20 ml of a carbopol and carboxymethyl cellulose (CMC) mixture and mixed thoroughly, which resulted in neem and echinacea gel. Then, theantimicrobial, anti-inflammatory, cytotoxic potential, and free-radical scavenging activity of the gel were evaluated. The data obtained were statistically analyzed with the help of a paired t-test, where a p-value of less than 0.05 was considered statistically significant. Results The antimicrobial assay showed that neem and echinacea gel at the concentration of 100 micrograms showed a greater zone of inhibition against Staphylococcus aureus(3.15 ± 0.26), Streptococcus mutans (2.48 ± 0.45), Enterococcus faecalis (2.89 ± 0.15), and Candida albicans (4.28 ± 0.87). The cytotoxic test revealed that even at an 80 µg concentration of the extract,more than 70% of the nauplii were vital, which indicated that the gel was not cytotoxic.The highest anti-inflammatory activity (78.39 ± 1.82) of the gel was seen at 50 micrograms when compared with diclofenac sodium (73.16 ± 1.80). The free radical scavenging activity showed that the 2,2-diphenyl-1-picrylhydrazyl (DPPH) absorbance of the neem and echinacea extract was highest at 50 micrograms. Conclusion The combination of neem and echinacea extract-based gel possessed high antimicrobial and anti-inflammatory activity when compared with standard drugs, such as amoxicillin and diclofenac sodium. The antioxidant activity of the gel was equal to butylated hydroxytoluene (BHT), and also the gel has a low cytotoxic potential even at its higher concentrations. Hence, the gel can be used as a natural remedy with minimal side effects, making it a valuable alternative to chemical agents.

An In Vitro Study of Antioxidant, Anti-inflammatory, and Cytotoxic Effects of Echinacea-Mediated Zinc Oxide Nanoparticles.

Background Plant extracts, such asEchinacea, are preferred in the pharmaceutical industry for their natural availability and minimal adverse effects.Echinacea is known for its anti-inflammatory and other biological properties. Zinc oxide nanoparticles (ZnONPs) are cost-effective, safe, and easily synthesized, making them prominent in nanoparticle research. This study aims to determine theanti-inflammatory, cytotoxic, and antioxidant properties of ZnONPs synthesized using Echinacea. Methodology In this study, 5 mg of powdered Echinacea was mixed with 100 mL of distilled water, heated at 44°C until vaporization, cooled, and filtered twice. The extract was mixed with 0.1 g of zinc oxide and exposed to sunlight for two weeks for nanoparticle synthesis. After centrifugation at 3,500 rpm for eight minutes, nanoparticles were collected. Scanning electron microscope analysis was done to determine nanoparticle formation. Cytotoxicity analysis was conducted using the brine shrimp method, with surviving nauplii counted after exposure to different nanoparticle concentrations. Antioxidant activity was assessed via 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and ferric-reducing antioxidant power (FRAP) assay. Anti-inflammatory activity was assessed using membrane stabilization assay andbovine serum albumin (BSA) assay. Using SPSS Statistics Version 23 (IBM Corp., Armonk, NY, USA), the mean and standard deviation between the prepared extract and the standard were compared for all assays. Results In the cytotoxicity assessment, at 5 µL, the mortality of nauplii remained unchanged from the control. However, at 10 and 20 µL, a 10% increase in mortality was observed, which then stabilized at 40 and 80 µL with 20%. Regarding antioxidant activity, as nanoparticle concentration increased from 10 to 50 µL in the DPPH and FRAP assays, their effectiveness also increased accordingly. According to the anti-inflammatory assay, the membrane stabilization and BSA assay showed an increase in activity with increasing concentrations of 10 to 50 μL extract against similar concentrations of standard diclofenac sodium. Conclusions Echinacea-based ZnONPs demonstratedeffective antioxidant and anti-inflammatory properties with low cytotoxicity, suggesting their potential use in future pharmaceutical or therapeutic applications.

The Effect of Carica pubescens Seeds Ethanol Extract on Lymphocyte Count and Paw Edema in Male White Swiss Webster Mice

Inflammation is a natural tissue response to infection in the body. The potential anti-inflammatory effect of secondary metabolites in carica seeds has been overlooked. This study aimed to investigate and develop the anti-inflammatory activity of the ethanolic extract of carica seeds (Carica pubescens) against foot edema and lymphocyte count in male white mice. Bioactive carica seeds were extracted using the maceration method with 70 % ethanol solvent. The identification of secondary metabolites was conducted using the thin-layer chromatography method. Treatments were administered to six groups: the negative control group (sick), solvent control, positive control with Diclofenac Sodium, and three doses of the ethanol extract of carica seeds (cS) at 100, 200, and 400 mg/kg body weight (BW). Edema was induced using intraplantar 1 % carrageenan on the soles of mice, and lymphocyte count was determined by blood sampling from the lateral tail vein using a hematology analyzer. Carica seeds doses of 200 mg/kg BW and 400 mg/kg BW demonstrated anti-inflammatory activity comparable to the positive control Diclofenac Sodium (p 0.05). Variations in CS doses influenced the lymphocyte count at the 3rd and 6th hours. In conclusion, the ethanolic extract of carica seeds exhibits anti-inflammatory effects in male white mice induced by 1 % carrageenan, reducing edema thickness and affecting leukocyte count.

Synthesis and characterization of Cu and Tb substituted NiFe2O4@MXene nanocomposite as a new photocatalyst for removal of organic dyes and drugs from industrial wastewater

The study aimed to establish a correlation between the photocatalytic degradation of Congo red (CR), Crystal violet (CV) dyes and Diclofenac sodium (DS) drug by copper, terbium substituted nickel ferrite (CuxNi1-xTbyFe2-yO4) and MXene (CTNF/MXene) composite where (x, y = 0.1). Terbium and copper doping reduced crystallite size, band gap energy, improve visible light absorption and impede electron-hole pair recombination. Superior complexation ability of terbium forces more pollutants to adsorb on the surface of photocatalyst and hence more degradation. Results indicated that MXene, acting as a co-catalyst, effectively lowered the charge recombination rates by electron trapping and enhanced the visible light absorption, improving the photocatalytic activity. CTNF/MXene composite exhibited greater rate constant and photocatalytic degradation of CR (91 %), CV (77 %) and DS (81 %) as compared to NF, CNF, TNF, CTNF. The increased surface area of CuxNi1-xTbyFe2-yO4 with MXene and reduced electron-hole pair recombination are possible factors for its successful use as photocatalyst.

La-CeO2/ZnO nanocomposites for photocatalytic mineralization of diclofenac under solar irradiation

Sodium diclofenac is an emerging pharmaceutical pollutant detected in many wastewater treatment plant effluents. Heterogeneous photocatalysis is one of the most sustainable and cheap technologies of water remediation. In the present work, several La-CeO2/ZnO nanocomposites have been synthesized with 10 to 40 % ZnO, for photocatalysing the mineralization of Diclofenac under solar irradiation. They have been characterized by XRD, XPS, UV-DRS, SEM and BET analyses. XRD patterns of La-CeO2/ZnO nanocomposites have shown the presence of only two distinct phases: fluorite and wurtzite, corresponding to CeO2 and ZnO, respectively. The band gap energy of La-CeO2/ZnO calculated using the Tauc plot, varied between 2.46 and 2.78 eV. XPS spectra of the nanocomposites revealed the presence of Zn, Ce, O, and La elements, where Zn, La and Ce showed 2+, 3+ and 4+ oxidation states, respectively. After confirming the stability of Diclofenac under solar irradiation without composite, photomineralization with La-CeO2/ZnO nanocomposites achieved 85 to 95 % diclofenac degradation, except for CeO2/ZnO nanocomposite without Lanthanum. The most effective composite CeLaZn0.1 (synthesized with 10 % ZnO (w/w)) allowed 80 % diclofenac mineralization after only 2 h irradiation which is remarkable. Reusability of CeLaZn0.1 was effective for five photocatalytic cycles under solar irradiation. The addition of radical quenchers during photomineralization experiments showed the significant role of superoxide radicals in tandem with photogenerated holes in diclofenac degradation by CeLaZn0.1 nanocomposite under solar irradiation.

Transcriptional and biochemical changes in mouse liver following exposure to a metal/drug cocktail. Attenuating effect of a selenium-enriched diet

Real-life pollution usually involves simultaneous co-exposure to different chemicals. Metals and drugs are frequently and abundantly released into the environment, where they interact and bioaccumulate. Few studies analyze potential interactions between metals and pharmaceuticals in these mixtures, although their joint effects cannot be inferred from their individual properties. We have previously demonstrated that the mixture (PC) of the metals Cd and Hg, the metalloid As and the pharmaceuticals diclofenac (DCF) and flumequine (FLQ) impairs hepatic proteostasis. To gain a deeper vision of how PC affects mouse liver homeostasis, we evaluated here the effects of PC exposure upon some biochemical and morphometric parameters, and on the transcriptional profiles of selected group of genes. We found that exposure to PC caused oxidative damage that exceeded the antioxidant capacity of cells. The excessive oxidative stress response resulted in an overabundance of reducing equivalents, which hindered the metabolism and transport of metabolites, including cholesterol and bile acids, between organs. These processes have been linked to metabolic and inflammatory disorders, cancer, and neurodegenerative diseases. Therefore, our findings suggest that unintended exposure to mixtures of environmental pollutants may underlie the etiology of many human diseases. Fortunately, we also found that a diet enriched with selenium mitigated the harmful effects of this combination of toxicants.

Persulfate photolysis and limited irrigation of recycled wastewater for turfgrass growth: Accumulation of pharmaceutical and personal care products and physiological responses

Recycled wastewater effluent irrigation and implementing limited irrigation rates are two promising strategies for water conservation in agriculture. However, one major challenge is the accumulation and translocation of Pharmaceutical and Personal Care Products (PPCPs) from recycled water to crops. This study investigated the effects of UV persulfate (UV/PS) treatment of recycled water and limited irrigation rate on PPCPs accumulation and physiological responses of St. Augustine turfgrass via a 14-week field trial. Carbamazepine (CBZ), sulfamethoxazole (SMX), triclosan (TCS), fluoxetine (FLX) and diclofenac (DCF) were spiked at 0.1–1.5 µg/L into recycled water and two limited irrigation rates corresponding to 60 % and 80 % of reference Evapotranspiration (ETo) were applied. Results showed that UV/PS removed 60 % of CBZ and > 99 % of other PPCPs from recycled water. Irrigation with UV/PS treated recycled water resulted in approximately a 60 % reduction in CBZ accumulation and complete removal of SMX, DCF, FLX and TCS in both turfgrass leaves and roots. A more limited irrigation rate at 60 % ETo resulted in a higher accumulation of CBZ accumulation compared to 80 % ETo. Similarly, the canopy temperature increased under 60 % ETo irrigation rate compared to 80 % ETo, suggesting that turfgrass under 60 % ETo was more prone to water stress. Applying a 60 % ETo irrigation rate was not sufficient to maintain the turfgrass quality in the acceptable range. A negative correlation between the visual quality and cumulative mass of PPCPs in turfgrass leaves at different irrigation rates was observed, yet irrigation rate was the major driver of turfgrass overall quality and health. Insights from this study will help to integrate recycled water with treatment and limited irrigation, thereby enhancing agricultural water reuse practices.

Characteristics of Central Serous Chorioretinopathy Patients at Padang Eye Center Hospital in 2019-2023

Background: Central Serous Chorioretinopathy (CSCR) is a condition where serous fluid collects in the retinal pigment epithelium (RPE) which results in detachment of the neurosensory layer of the retina. Several risk factors that cause CSCR are gender, age, use of corticosteroids, 3rd trimester pregnancy, stress, type A personality, and use of anti-psychotic drugs. Objective: The purpose of this study was to describe the characteristics of Central Serous Chorioretinopathy (CSCR) patients at RSKM Padang Eye Center in 2019-2023. Method: The scope of this research is the field of eye disease. This research was conducted from December 2023 the study was conducted using categorical descriptive study. The population of this study were all Central Serous Chorioretinopathy (CSCR) patients recorded in the medical records at RSKM Padang Eye Center with a total of 34 samples using a total sampling technique. Data analysis uses univariate analysis, the data obtained will be processed with SPSS Statistics 26.0 and presented in table form. Results: From 34 patients with Central Serous Chorioretinopathy (CSCR) at RSKM Padang Eye Center, the majority were in the late adult age category ranged from 36-45 years old (52.9%). The most common gender is male by 73.5%. The initial visual acuity of the patients was good (6/6-6/18) were 35.3%, moderate visual acuity (<6/18-6/60) were 41.2%, and poor visual acuity (<6/60) were 23.5%. The most common treatment was diclofenac sodium as much as 73,5%. The patient's final visual acuity was good (6/6-6/18) were 82.4%, moderate visual acuity (<6/18-6/60) were 14.7%, and poor visual acuity (<6/60) were 2.9%. A total of 82.4% experienced improved visual acuity. Conclusion: Central Serous Chorioretinopathy (CSCR) were mostly 36-45 years old, male, with moderate initial visual acuity, received diclofenac sodium management, and good final visual acuity, most of the patient’s experienced improvement in visual acuity.

Enhanced Selective Degradation of Pharmaceutical and Personal Care Products by β-Cyclodextrin-Decorated ZIF-67 Nanocomposites in Reclaimed Water.

A peroxymonosulfate oxidation system was developed via modification of β-cyclodextrin (β-CD) on the surface of Fe2+-doped ZIF-67 (CD/Fe@ZIF-67) as an activator. The 99.7% carbamazepine, 91.3% bisphenol A (BPA), and 95.4% diclofenac (DCF) degradation efficiency were achieved within 10 min, 60, and 1 min, respectively. The hydrophobicity of these three pollutants is positively correlated with their adsorption kinetic constants by CD/Fe@ZIF-67 due to the introduction of β-CD. Scavenger experiments and electron spin resonance spectra confirmed that carbamazepine was preferentially oxidized by SO4•- [λ(SO4•-)(70.5%) > λ(•OH)(28.2%) > λ(O2•-)(1.3%)], where SO4•- and O2•- played dominant roles in the degradation of BPA [λ(SO4•-)(71.7%) > λ(O2•-)(22.8%) > λ(•OH)(5.5%)], and O2•- was responsible for DCF removal [λ(O2•-) = 93.2%]. Additionally, the particulate catalyst was immobilized in the shell side of a ceramic membrane in a membrane reactor for catalyst recovery. This reactor achieved nearly 100% removal efficiency under optimal conditions: 0.036 wt % catalyst loading, 0.5 mM peroxymonosulfate concentration, 1 L inflow, 10 mg/L initial carbamazepine concentration, and 0.012 L/min hydraulic retention time. In summary, this study elucidates the active role of β-CD in a polymetallic/peroxymonosulfate system and provides valuable insights into the development of effective oxidation methods for pharmaceutical and personal care products in wastewater.

Antioxidant, Anti-inflammatory and Anthelminthic Activities of Traditionally used Ocimum basilicum L., and Ocimum tenuiflorum L. Extract Loaded Emulsion

The demand for cosmeceuticals is rapidly expanding. Various phytoconstituents are identified from Ocimum basilicum and O. tenuiflorum and have several pharmacological properties. The present study aimed to formulate a novel alternative herbal formulation for topical administration with natural antioxidant properties for the treatment of inflammatory conditions with the destructive capacity of parasitic worms. The egg albumin denaturation technique was used to evaluate the test formulations’ and the standard’s in-vitro anti-inflammatory properties, and the hydrogen peroxide assay was used to measure the extracts’ antioxidant properties. Eudrilus eugeniae was the target of the investigation into in-vitro anthelmintic action. The pH of the cream was 6.8 (average), it was easily spreadable and washable, no gritty particles were found and the dye test confirmed that it was an o/w type of cream. The egg albumin denaturation technique was utilized to evaluate the anti-inflammatory properties. The results cleared those herbal formulations (F1 and F2) and protein denaturation was decreased by diclofenac sodium (Standard) in a dose-dependent manner. Test samples exhibited higher anti-inflammatory activities than the standard with their percentage inhibitions being 41.5 ± 0.5 (F2), 39.1 ± 0.4 mg/mL (F1), and 37.3 ± 0.3 mg/mL (F-Standard), respectively. Antioxidants are compounds that either completely stop or significantly reduce the harm that free unstable radicals. F2 showed a higher concentration-dependent anthelmintic activity than F1 and standard albendazole. Increasing the concentration decreases the paralysis and death time of earthworms. Finally concluded that F2 indicates higher anti-inflammatory and anthelmintic activities than others with high natural antioxidant power.

Isolation, Chemical Modification and In vivo Pharmacological Screening of Piperine and its Derivatives

Piperine (1) extracted from black pepper was transformed into its derivatives piperic acid (2) and piperonal (3) with good yields (69-76%). Animal models were used to examine the compounds' in vivo peripheral as well as central analgesic and anti-inflammatory effects. In the peripheral analgesic experiment, compound 2 displayed remarkable action having writhing inhibition by 78% at 50 mg/kg dose, superior to that of 1 (74% writhing inhibition) when administered at the same dose and compared with standard diclofenac sodium (85%). Concerning central analgesic efficacy, piperonal outperformed compounds 1 and 2 at 25 mg/kg dose, with % tail-flick elongation times of 194%, 178%, and 178% at 30, 60, and 90 min, respectively. Conversely, at 50 mg/kg dose, piperic acid exhibited the highest activity, demonstrating % tail-flick elongation times of 231%, 213%, and 206% at 30, 60, and 90 min, respectively, as compared to the standard morphine (278%, 247%, and 160%) in the same duration. In anti-inflammatory property evaluation, piperonal portrayed outstanding effects with paw edema inhibitions of 57%, 66%, 76%, and 81%, respectively from 1st hour onwards, compared to standard aceclofenac (61%, 72%, 78%, and 89%) and parent compound piperine (20%, 34%, 51%, and 60%). This study suggests that piperine derivatives could act as promising leads for future drug development. Dhaka Univ. J. Pharm. Sci. 23(1): 13-22, 2024 (June)

Hydroxypropyl methylcellulose phthalate films reinforced with nanocrystalline cassava starch and intended its applications for colonic drug delivery

Controlled-release drug delivery systems are crucial for improving therapeutic efficacy and patient compliance. Hydroxypropyl methylcellulose phthalate (HPMCP) films are promising candidates due to their film-forming properties and tunable release profiles. However, their mechanical properties can limit their applicability. This study aimed to assess the effect of addition of nanocrystalline cassava (NCS) starches to HPMCP films on the physicochemical and mechanical properties and the ability of films to control drug release rate. Reinforced HPMCP films with 2, 4 and 6 % w/w of NCS were characterized as a function of the microstructure, X-ray diffraction pattern, mechanical properties, and dissolution property. It was found that increasing starch amount induced an increase in heterogeneity of the film microstructure and crystallinity. The tensile strength of HPMCP films increased with addition of starches, while the elongation at break decreased. The lowest dissolution in pH 6.8 phosphate buffer solution was found for films containing NCS at 2 and 4 % w/w. For the application purposes, HPMCP containing different amounts of NCS was used to coat over diclofenac sodium tablets. The tablets coated with HPMCP containing 4 % w/w NCS showed the lowest drug release of 73.5 % in pH 6.8 phosphate buffer solution at 240 min. According to our results, the addition of NCS at adequate amount allowed to improve the mechanical properties of HPMCP films and to decrease the drug release rate which is important for the site-specific drug delivery process.

Characterization and Evaluation of Anti-inflammatory Melinjo Seed Extract Nanoparticles

Melinjo seed extract is rich in various active compounds, including trans-resveratrol, commonly known as “melinjo resveratrol,” with antioxidant and antimicrobial pharmacological functions. However, a comprehensive exploration of the anti-inflammatory potential of melinjo seed extract has not been conducted. Converting melinjo seed extract into nanoparticles offers distinct advantages, including the ability to permeate intercellular spaces and higher cell walls through diffusion or opsonification. This flexibility allows for synergies with various technologies, presenting extensive potential for diverse applications and targets. Therefore, this experimental research aimed to obtain an extract from melinjo seed through an extraction process and apply it in nanoparticle dosage forms. Characterization was performed by evaluating the particle size, zeta potential, surface morphology, and anti-inflammatory activity. The results showed that the nanoparticles were successfully prepared using the ionic gelation method, yielding a particle size of 267.5 nm, a stable potential zeta, and well-defined spherical morphology. Additionally, the nanoparticles produced the highest anti-inflammatory activity compared to treatments with conventional melinjo seed extract and sodium diclofenac.

Development of Unique Pyrazoline Analogues for Screening Anticancer and Anti-inflammatory Studies

Cancer is a major threat to human society in the world, which results in a maximum probability of death. In the present scenario, chemotherapy is the main cancer treatment, but still, it has its limitations. Hence, cytotoxic and chemotherapy medicines are the main focus of research for medicinal chemists. So, it is the need of the hour to explore the possibility of effective and safe anticancer drugs. The current research involves the synthesis of pyrazoline derivatives (PYR1-PYR8), which are novel cytotoxic agents developed from recently formulated chalcones (CHL1-CHL8). Title compounds were prepared by subjecting the chalcones with by hydrazine hydrate in ethanolic acetic acid. The purified synthesized compounds were characterized by IR, 1H-NMR, and mass spectroscopic evaluation. Using in-vitro models, cytotoxicity evaluations were conducted on cell lines associated with lung cancer by MTT and SRB methods using doxorubicin as standard, which revealed differing levels of cytotoxic effects among the compounds. The egg albumin denaturation and protein denaturation methods were used to access in-vitro anti-inflammatory activity. Compound PYR4 and PYR6 showed significant anti-inflammatory efficacy in relation to diclofenac sodium as the reference drug. Compound PYR3, PYR4, and PYR6 displayed noteworthy anticancer activity matched to doxorubicin, which is a reference drug. The current research asserts that the newly developed pyrazoline derivatives exhibit high levels of cytotoxicity and anti-inflammatory effects. However, their preclinical and clinical significance needs a thorough evaluation.

Effectiveness of Mesotherapy in Post-COVID Pain Syndrome: Retrospective Cohort Study of 96 Patients

PurposeMusculoskeletal pain may occur after becoming infected with SARS-Cov2. This study was designed to evaluate the efficacy of mesotherapy in treating chronic pain following COVID-19 infection. MethodsA retrospective review was conducted of the records of 96 patients with post-COVID pain syndrome. Those who were eligible for oral therapy or mesotherapy, included in the study. Patients receiving oral treatment with diclofenac potassium, thiocolchicoside and cyanocobalamin were included in one group (n = 46), and patients receiving intradermal mesotherapy with 2% lidocaine + cyanocobalamin were included in another group (n = 50). The results of the Visual Analogue Scale (VAS) and the Leeds Assessment of Neuropathic Symptoms and Signs (LANSS) were individually assessed before and one week after the treatment. FindingsThe participants were 40.2 ± 11.1 years old on average. Of the participants, 35.4% (n = 34) were male and 64.6% (n = 62) were female. Before treatment, there was no statistically significant difference between the patients in terms of VAS and LANSS scores. Following the treatment, a notable positive response was observed in both groups. Nevertheless, when compared to the oral treatment group, the mesotherapy group exhibited a more pronounced enhancement in VAS and LANSS scores (P < 0.001, P < 0.001, respectively). ImplicationsWhile both mesotherapy and oral therapy offer benefits in reducing pain and alleviating neuropathic symptoms in post-COVID pain syndrome, mesotherapy stands out as an especially effective and well-tolerated treatment method, surpassing the efficacy of the oral alternative.

Fabrication of hierarchically porous CuO nanostructures using Brij 52 and silica nanoparticles as reinforcing agents for the reduction of 3-nitroaniline to 3-phenylenediamine and sensing against diclofenac sodium

Fabrication of hierarchically porous CuO nanostructures using Brij 52 and silica nanoparticles as reinforcing agents for the reduction of 3-nitroaniline to 3-phenylenediamine and sensing against diclofenac sodium

In vitro anti-inflammatory and anticoagulant activities of alkaloïds extracted from nopals of inermis Algerian Opuntia ficus indica (L).

The dearth of information surrounding the utilization of Opuntia cladode alkaloids underscores a critical gap in understanding their pharmacological properties and therapeutic potential, emphasizing the need for further comprehensive investigations. The present study aims to investigate the in vitro anti-inflammatory, anticoagulant, and antimicrobial activities of alkaloïds belonging to young cladodes (nopals) of inermis Algerian Opuntia ficus indica. The assessed alkaloïds showed a moderate anti-inflammatory effect regarding the BSA protein protection with a maximum of 51.04±1.84 % compared to 84.22±2.38 % for Diclofenac sodium as a positive standard. However, their stabilization of red blood cells membrane against induced hemolysis was greater than Diclofenac (52.38±2.01 % vs 48.97±2.73 %). The two assays had a significant correlation (&lt; 0.05) of 0,968. Nopal alkaloïds extended the coagulation time (1.24 fold) by significantly affecting the exogenous pathway PT only, whilst they were ineffective against the endogenous pathway APTT. Conversely, Algerian nopal alkaloïds had neither bacteriostatic nor bactericide influence at 2 mg ml-1 on Candida albicans yeast or the six tested pathogenic bacterial strains. In perspective, the purification of these Opuntia nopal alkaloïds and understanding their accurate mechanism of action are clearly the strategic steps to illustrate their overall curative potential.

In vitro evaluation of ethyl cellulose and polyvinyl pyrrolidone composite nanofibers for transdermal delivery of diclofenac diethylamine

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prominent painkiller and anti-inflammatory drugs with gastrointestinal (GI) adverse effects. Transdermal drug delivery systems (TDDS) could overcome GI adverse effects associated with oral ingestion of NSAIDs as well as maintaining a prolonged release of the drug. The main aim of this study was to prepare and investigate diclofenac diethylamine (DDA) loaded nanofibers made of ethyl cellulose (EC) and polyvinyl pyrrolidone K90 (PVP) using electrospinning. The impact of penetration enhancers such as nerolidol and farnesol on release profiles through cellophane membranes and other characteristics of nanofibers were also investigated. Based on release studies, some formulations were selected for release examination through rate skin using Franz diffusion cells. To gain insight about potential interactions between drug and polymers FTIR, DSC, and XRD analyses were performed. Morphology examination was also conducted using scanning electron microscopy (SEM). Morphology studies showed that nanofibers made of EC only are greater in the mean diameter than other nanofibers while other formulations were not significantly different from each other regardless of the presence of penetration enhancers. EC nanofibers had the lowest elastic modulus and tensile strength and most elongation at break which makes them the least tough and most flexible nanofibers among all the formulations. The addition of PVP increased the toughness and decreased the flexibility of nanofibers. The addition of nerolidol did not alter the mechanical properties of nanofibers significantly, while the addition of farnesol increased elastic modulus, tensile strength, and elongation at break significantly in a concentration-dependent manner. EC nanofibers had the lowest release rate and lowest total cumulative release content while the addition of PVP significantly improved both of these features. In release studies through cellophane membrane, the addition of 5 % of penetration enhancer slightly increased the release rate while did not significantly alter cumulative release while the addition of 10 % farnesol notably increased the release rate and total cumulative released content. Release studies through rat skin were in accordance with cellophane membrane studies and the formulation with 10 % farnesol had the most release rate and total cumulative release and these findings confirm the positive effect of penetration enhancers. DSC thermogram showed an amorphous state of the drug in fibres and this was supported by XRD results. The FTIR results confirmed that no chemical interaction between the drug and other formulation components has occurred and no new compounds have been formed. Based on these results, the utilization of DDA-loaded PVP and EC nanofibers in conjunction with a penetration enhancer showed significant potential for application in transdermal patches.

Visual Eosin Y-Based Photosensitization Sensing Systems for Ultrasensitive Detection of Diclofenac with Single-Atom Co─N2O2 Site-Immobilized g-C3N4 Nanosheets.

It is highly desired to develop a visual sensing system for ultrasensitive detection of colorless diclofenac (DCF), yet with a significant challenge. Herein, a novel dye-based photosensitization sensing system has been successfully developed for detecting DCF for the first time, in which the used dye eosin Y (DeY) can strongly absorb visible light and then be decolorized obviously by transferring photogenerated electrons to g-C3N4 nanosheets (CN), while the built single-atomic Co─N2O2 sites on CN by boron-oxygen connection can competitively adsorb DCF to impede the photosensitization decoloration of DeY. This system exhibits a broad detection range from 8ngL-1 to 2 mgL-1 with 535nm light, an exceptionally low detection limit (3.5ngL-1), and remarkable selectivity. Through the time-resolved, in situ technologies, and theoretical calculations, the decolorization of DeY is attributed to the disruption of DeY's conjugated structure caused by the triplet excited state electron transfer from DeY to CN, meanwhile, the adsorbed oxygen facilitates the charge transfer process. The preferential adsorption of DCF mainly depends on the strong interactions between the as-constructed single-atom Co and Cl in DCF. This study opens an innovative light-driven sensing system by combining dye and single-atom metal/nanomaterial for visually intuitive detection of environmental pollutants.

Synthesis, crystal structure, spectroscopic characterization, in vitro, molecular docking and DFT studies of 1- (Tert-Butyl) 2-methyl (2S, 4R)-4-hydroxy pyrrolidine-1,2-dicarboxylate

A chiral pyrrolidine-based compound, namely 1-(Tert-Butyl) 2-Methyl (2S, 4R)-4-Hydroxy Pyrrolidine-1,2-Dicarboxylate (NHP), was synthesized and crystallized by the slow evaporation technique. NMR, FT-IR, ESI-MS, UV–visible spectroscopy, and elemental analysis designate the molecule. The molecule crystallized in the orthorhombic space group P212121, identified by X-ray diffraction (XRD). Quantum chemical calculations were performed using DFT at the B3LYP/6–311++G (d,p) level. The DFT-calculated optimal structural parameters and the XRD-derived parameters showed a good correlation. The frequency of NHP is calculated using the DFT method and compared with observed results. The synthesized compound's molecular reactivity was further investigated using Mulliken atomic charges, HOMO-LUMO, and molecular electrostatic potential (MEP). The molecule was tested for molecular docking with bio-enzymes such as α-amylase (1HNY) and cyclooxygenases (1PGG & 4COX). The compound showed 7 hydrogen bonding interactions with 1HNY and 8 hydrogen bonding interactions with 4COX. The DFT investigations strongly support the molecular docking results. The molecule's in-vitro anti-inflammatory and anti-diabetic activity was compared with conventional medication. The NHP showed superior anti-inflammatory activity with protein denaturation technique than the standard diclofenac sodium. The results showed that the molecule outperformed the conventional medication in tests for inflammation.