Potential role of Citrus bergamia flower essential oil against oral pathogens.

BACKGROUND: Oral bacterial infections are difficult to treat due to emergence of resistance against antibiotic therapy. Essential oils are considered emerging alternate therapy against bacterial infections and biofilms. We investigated Citrus bergemia flower essential oil against oral pathogens. METHODS: The essential oil was analsyed using Gas Chromatography(GC-MS), in silico investigations, antioxidant, antimicrobial, antibiofilm and antiquorum sensing assays. RESULTS: Gas Chromatography analysis confirmed presence of 17 compounds including 1,6-Octadien-3-ol,3,7-dimethyl, 48.17%), l-limonene (22.03%) and p-menth-1-ol, 8-ol (7.31%) as major components. In silico analysis showed compliance of all tested major components with Lipinski's rule, Bioavailability and antimicrobial activity using PASS (prediction of activity spectrum of substances). Molecular docking with transcriptional regulators 3QP5, 5OE3, 4B2O and 3Q3D revealed strong interaction of all tested compounds except 1,6-Octadien-3-ol,3,7-dimethyl. All tested compounds presented significant inhibition of DPPH (2,2-diphenyl-1-picrylhydrazyl) (IC50 0.65 mg/mL), H2O2 (hydrogen peroxide) (63.5%) and high FRAP (ferrous reducing antioxidant power) value (239.01 µg). In antimicrobial screening a significant activity (MIC 0.125 mg/mL) against Bacillus paramycoides and Bacillus chungangensis was observed. Likewise a strong antibiofilm (52.1 - 69.5%) and anti-QS (quorum sensing) (4-16 mm) activity was recorded in a dose dependent manner. CONCLUSION: It was therefore concluded that C. bergemia essential oil posess strong antioxidant, antimicrobial and antibiofilm activities against tested oral pathogens.

Exploring opportunities of Artificial Intelligence in aquaculture to meet increasing food demand.

The increasing global population drives a rising demand for food, particularly fish as a preferred protein source, straining capture fisheries. Overfishing has depleted wild stocks, emphasizing the need for advanced aquaculture technologies. Unlike agriculture, aquaculture has not seen substantial technological advancements. Artificial Intelligence (AI) tools like Internet of Things (IoT), machine learning, cameras, and algorithms offer solutions to reduce human intervention, enhance productivity, and monitor fish health, feed optimization, and water resource management. However, challenges such as data collection, standardization, model accuracy, interpretability, and integration with existing aquaculture systems persist. This review explores the adoption of AI techniques and tools to advance the aquaculture industry and bridge the gap between food supply and demand.

Multiple integrated computational approach to analyse wound healing potential of Symplocos racemosa bark as Matrix metalloproteinase inhibitors.

The healing of wounds is the flagging concern in chronic wound cases especially when accompanied by pathogenic, diabetic comorbidities. Matrix metalloproteinases are associated with widespread pathological ailments, and the selective inhibitors for metalloproteinases can be of great interest in wound healing strategies. In the present research study, six constituents of Symplocos racemosa Roxb were evaluated for the docking aptitudes on human matrix metalloproteinase MMP 2 (PDB ID: 1QIB) and MMP 9 (PDB ID: 4H1Q) utilising Autodock Vina followed by the visualisation using Discovery studio (DS). The Pymol was used to generate the poses and the best binding pose was chosen for the docking aptitudes. 2D interactions and the 3D poses of the docked complex were accomplished using DS and LigPlot + software respectively. Working on SWISS ADME and OSIRIS software accomplished the physicochemical characteristics, absorption, distribution, metabolism, excretion, molecular properties, bioactivity score, and toxicity predictions. The molecule's physiochemical investigations discovered that all of the ligands comply with Lipinski's rule of five except compound 6, which deviated with two violations. Docking studies against 4H1Q revealed that compounds 1, 3, 5 and 6 exhibited maximum interactions with the target protein, with the free binding energies of -8.3 kJ Mol-1, -9.3 kJ Mol-1, -7.2 kJ Mol-1 and -11.0 kJ Mol-1 respectively. In case of the 1QIB target, compounds 1, 3 and 6 displayed remarkable binding energies of -8.7 kJ mol-1, -9.0 kJ mol-1 and -8.8 kJ mol-1. Bioactivity prediction study revealed that all of the selected Phytoconstituents displayed incredible Bioactivity scores. None of the selected chemical compounds was found to be irritant to the skin as discovered by toxicity studies. The contacts of the ligand-protein complex during the simulation studies revealed that the H-bond interactions of the ligands with LEU188, ALA189, GLN402, ARG420, MET422, PRO421, and ARG424 of 4H1Q were stable for more than 30% of the simulation time. It was thus concluded that the tested compounds predominantly compounds 1, 5 and 6 might rank among the vital supplementary lead drugs in chronic wounds and healing complexities. It is also worth noting the potential aptitude of the compound 3, however, its toxicity concern must be considered.

Biogenic silver nanoparticles: Synthesis, applications and challenges in food sector with special emphasis on aquaculture.

Aquaculture, a rapidly expanding global food sector faces challenges like pathogenic infections, water quality management and sustainability. Silver nanoparticles (AgNPs) have emerged as promising tools in aquaculture due to their antimicrobial, antiviral and antifungal properties. AgNPs offer alternatives to traditional antimicrobial agents. Their small size and unique physicochemical properties enhance antimicrobial activity, effectively inhibiting pathogen growth and reducing disease incidence in aquatic organisms. Additionally, AgNPs can improve water quality by catalyzing the removal of pollutants, heavy metals and nutrients, reducing environmental impacts. Despite their potential benefits, several challenges and knowledge gaps exist in the utilization of AgNPs in aquaculture. Addressing challenges related to regulation, sustainability and environmental impact will be crucial for realizing their full potential in the industry. Therefore, the present review aims to provide insight into the role of AgNPs, its challenges in aquaculture and also highlights key areas for future research.

Assesment of polyphenolic compounds against biofilms produced by clinical Acinetobacter baumannii strains using in silico and in vitro models.

Several types of microbial infections are caused by Acinetobacter baumanii that has developed resistance to antimicrobial agents. We therefore investigated the role of plant polyphenols against A. baumannii using in silico and in vitro models. The clinical strains of A. baumannii were investigated for determination of resistance pattern and resistance mechanisms including efflux pump, extended spectrum beta lactamase, phenotype detection of AmpC production, and Metallo-ß-lactamase. The polyphenolic compounds were docked against transcription regulator BfmR (PDB ID 6BR7) and antimicrobial, antibiofilm, and anti-quorum sensing activities were performed. The antibiogram studies showed that all isolated strains were resistant. Strain A77 was positive in Metallo-ß-lactamase production. Similarly, none of strains were producers of AmpC, however, A77, A76, A75 had active efflux pumps. Molecular docking studies confirmed a strong binding affinity of Rutin and Catechin towards transcription regulator 6BR7. A significant antimicrobial activity was recorded in case of quercetin and syringic acid (MIC 3.1 µg/mL) followed by vanillic acid and caffeic acid (MIC 12.5 µg/mL). All tested compounds presented a strong antibiofilm activity against A. baumanii strain A77 (65 to 90%). It was concluded that all tested polyphenols samples posess antimicrobial and antibiofilm activities, and hence they may be utilized to treat multidrug resistance A. baumannii infections.

In vitro evaluation of herbal based Lesh Nat B cream against Leishmania tropica.

Pentavalent antimonials continue to be the standard treatment for cutaneous leishmaniasis. But their use is retarded owing to highly-priced, prolonged hospitalization, noxious and poor solubility. Therefore, there is a dire need to characterize new potential compounds possessing anti-leishmanial activity. Topical therapies that are more successful are an essential alternative therapeutic option for the localized self-limiting form of this disease. We tested the herbal-based topical cream Lesh Nat B against Leishmania tropica KWH23 promastigotes and axenic amastigotes in vitro. The anti-leishmanial activity of Lesh Nat B cream was evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay against promastigotes and axenic amastigotes. The results of Lesh Nat B cream were concentration and incubation time-dependent. After 72 h of incubation, Lesh Nat B cream efficiently suppresses the promastigote form of the parasite, followed by 48 h and 24 h. At 72 h, the lowest and highest levels of activity were 37% and 90%. Amastigotes had a minimum activity of 34% and a maximum activity of 78.5%, respectively. This formulation was more cytotoxic against promastigote form than amastigotes form at 72 h incubation periods. All the experiments were carried out in triplicates. Half-maximal inhibitory concentration (IC50) values were determined to be (66 ug/ml) and (70 ug/ml) against promastigote and amastigote forms, respectively. Moreover, 1.63% hemolytic activity was observed in Lesh Nat B cream at (10 µg/ml) while 3% hemolytic activity was observed at (37 µg/ml). It can be concluded that Lesh Nat B cream demonstrated effective Leishmanicidal and less hemolytic activity and can be used as an alternative therapeutic option for the treatment of cutaneous leishmaniasis; however, more studies are expected to justify its effectiveness in treating cutaneous leishmaniasis in both humans and animals.

Fabrication of Novel Omeprazole-Based Chitosan Coated Nanoemulgel Formulation for Potential Anti-Microbia; In Vitro and Ex Vivo Characterizations.

Infectious diseases remain inevitable factors for high mortality and morbidity rate in the modern world to date. Repurposing is a novel approach to drug development has become an intriguing research topic in the literature. Omeprazole is one of the top ten proton pump inhibitors prescribed in the USA. The literature suggests that no reports based on omeprazole anti-microbial actions have been discovered to date. This study entails the potential of omeprazole to treat skin and soft tissue infections based on the literature's evident anti-microbial effects. To get a skin-friendly formulation, a chitosan-coated omeprazole-loaded nanoemulgel formulation was fabricated using olive oil, carbopol 940, Tween 80, Span 80, and triethanolamine by high-speed homogenization technique. The optimized formulation was physicochemically characterized for zeta potential, size distribution, pH, drug content, entrapment efficiency, viscosity, spreadability, extrudability, in-vitro drug release, ex-vivo permeation analysis, and minimum inhibitory concentration determination. The FTIR analysis indicated that there was no incompatibility between the drug and formulation excipients. The optimized formulation exhibited particle size, PDI, zeta potential, drug content, and entrapment efficiency of 369.7 ± 8.77 nm, 0.316, -15.3 ± 6.7 mV, 90.92 ± 1.37% and 78.23 ± 3.76%, respectively. In-vitro release and ex-vivo permeation data of optimized formulation showed 82.16% and 72.21 ± 1.71 µg/cm2, respectively. The results of minimum inhibitory concentration (1.25 mg/mL) against selected bacterial strains were satisfactory, suggesting a successful treatment approach for the topical application of omeprazole to treat microbial infections. Furthermore, chitosan coating synergistically increases the antibacterial activity of the drug.

Development and Evaluation of Essential Oil-Based Nanoemulgel Formulation for the Treatment of Oral Bacterial Infections.

Prevalence of oral infections in diabetic patients is a health challenge due to persistent hyperglycemia. However, despite great concerns, limited treatment options are available. We therefore aimed to develop nanoemulsion gel (NEG) for oral bacterial infections based on essential oils. Clove and cinnamon essential oils based nanoemulgel were prepared and characterized. Various physicochemical parameters of optimized formulation including viscosity (65311 mPa·S), spreadability (36 g·cm/s), and mucoadhesive strength 42.87 N/cm2) were within prescribed limits. The drug contents of the NEG were 94.38 ± 1.12% (cinnamaldehyde) and 92.96 ± 2.08% (clove oil). A significant concentration of clove (73.9%) and cinnamon essential oil (71.2 %) was released from a polymer matrix of the NEG till 24 h. The ex vivo goat buccal mucosa permeation profile revealed a significant (52.7-54.2%) permeation of major constituents which occurred after 24 h. When subjected to antimicrobial testing, significant inhibition was observed for several clinical strains, namely Staphylococcus aureus (19 mm), Staphylococcus epidermidis (19 mm), and Pseudomonas aeruginosa (4 mm), as well as against Bacillus chungangensis (2 mm), whereas no inhibition was detected for Bacillus paramycoides and Paenibacillus dendritiformis when NEG was utilized. Likewise promising antifungal (Candida albicans) and antiquorum sensing activities were observed. It was therefore concluded that cinnamon and clove oil-based NEG formulation presented significant antibacterial-, antifungal, and antiquorum sensing activities.

Identification of RdRp inhibitors against SARS-CoV-2 through E-pharmacophore-based virtual screening, molecular docking and MD simulations approaches.

The outbreak of novel Coronavirus, an enduring pandemic declared by WHO, has consequences to an alarming ongoing public health menace which has already claimed several million human lives. In addition to numerous vaccinations and medications for mild to moderate COVID-19 infection, lack of promising medication or therapeutic pharmaceuticals remains a serious concern to counter the ongoing coronavirus infections and to hinder its dreadful spread. Global health emergencies have called for urgency for potential drug discovery and time is the biggest constraint apart from the financial and human resources required for the high throughput drug screening. However, computational screening or in-silico approaches appeared to be an effective and faster approach to discover potential molecules without sacrificing the model animals. Accumulated shreds of evidence on computational studies against viral diseases have revealed significance of in-silico drug discovery approaches especially in the time of urgency. The central role of RdRp in SARS-CoV-2 replication makes it promising drug target to curtain on going infection and its spread. The present study aimed to employ E-pharmacophore-based virtual screening to reveal potent inhibitors of RdRp as potential leads to block the viral replication. An energy-optimised pharmacophore model was generated to screen the Enamine REAL DataBase (RDB). Then, ADME/T profiles were determined to validate the pharmacokinetics and pharmacodynamics properties of the hit compounds. Moreover, High Throughput Virtual Screening (HTVS) and molecular docking (SP & XP) were employed to screen the top hits from pharmacophore-based virtual screening and ADME/T screen. The binding free energies of the top hits were calculated by conducting MM-GBSA analysis followed by MD simulations to determine the stability of molecular interactions between top hits and RdRp protein. These virtual investigations revealed six compounds having binding free energies of -57.498, -45.776, -46.248, -35.67, -25.15 and -24.90 kcal/mol respectively as calculated by the MM-GBSA method. The MD simulation studies confirmed the stability of protein ligand complexes, hence, indicating as potent RdRp inhibitors and are promising candidate drugs to be further validated and translated into clinics in future.

Bioinformatics approaches and big data analytics opportunities in improving fisheries and aquaculture.

Aquaculture has witnessed an excellent growth rate during the last two decades and offers huge potential to provide nutritional as well as livelihood security. Genomic research has contributed significantly toward the development of beneficial technologies for aquaculture. The existing high throughput technologies like next-generation technologies generate oceanic data which requires extensive analysis using appropriate tools. Bioinformatics is a rapidly evolving science that involves integrating gene based information and computational technology to produce new knowledge for the benefit of aquaculture. Bioinformatics provides new opportunities as well as challenges for information and data processing in new generation aquaculture. Rapid technical advancements have opened up a world of possibilities for using current genomics to improve aquaculture performance. Understanding the genes that govern economically relevant characteristics, necessitates a significant amount of additional research. The various dimensions of data sources includes next-generation DNA sequencing, protein sequencing, RNA sequencing gene expression profiles, metabolic pathways, molecular markers, and so on. Appropriate bioinformatics tools are developed to mine the biologically relevant and commercially useful results. The purpose of this scoping review is to present various arms of diverse bioinformatics tools with special emphasis on practical translation to the aquaculture industry.

Evaluation of Major Constituents of Medicinally Important Plants for Anti-Inflammatory, Antidiabetic and AGEs Inhibiting Properties: In Vitro and Simulatory Evidence.

Diabetes mellitus (DM) is a global health concern that is associated with several micro- and macrovascular complications. We evaluated several important medicinal plant constituents, including polyphenols and flavonoids, for α-glucosidase inhibition, AGEs' inhibitory activities using oxidative and no-oxidative assays, the inhibition of protein cross link formation, 15-lipoxydenase inhibition and molecular docking. The molecular docking studies showed high binding energies of flavonoids for transcriptional regulars 1IK3, 3TOP and 4F5S. In the α-glucosidase inhibition assay, a significant inhibition was noted for quercitrin (IC50 7.6 µg/mL) and gallic acid (IC50 8.2 µg/mL). In the AGEs inhibition assays, quercetin showed significant results in both non-oxidative and (IC50 0.04 mg/mL) and oxidative assays (IC50 0.051 mg/mL). Furthermore, quercitrin showed inhibitory activity in the non-oxidative (IC50 0.05 mg/mL) and oxidative assays (IC50 0.34 mg/mL). A significant inhibition of protein cross link formation was observed by SDS-PAGE analysis. Quercitrin (65%) and quercetin (62%) showed significant inhibition of 15-lipoxygenase. It was thus concluded that flavonoids and other polyphenols present in plant extracts can be effective in management of diabetes and allied co-morbidities.

Novel Curcumin-Encapsulated α-Tocopherol Nanoemulsion System and Its Potential Application for Wound Healing in Diabetic Animals.

Objective: This project was aimed at formulating a novel nanoemulsion system and evaluating it for open incision wound healing in diabetic animals. Methods: The nanoemulsions were characterized for droplet size and surface charge, drug content, antioxidant and antimicrobial profiling, and wound healing potential in diabetic animals. The skin samples excised were also analyzed for histology, mechanical strength, and vibrational and thermal analysis. Results: The optimized nanoemulsion (CR-NE-II) exhibited droplet size of26.76 ± 0.9 nm with negative surface charge (-10.86 ± 1.06 mV), was homogenously dispersed with drug content of68.05 ± 1.2%, released almost82.95 ± 2.2%of the drug within first 2 h of experiment with synergistic antioxidant (95 ± 2.1%) and synergistic antimicrobial activity against selected bacterial strains in comparison to blank nanoemulsion, and promoted significantly fast percent reepithelization (96.47%). The histological, vibrational, thermal, and strength analysis of selected skin samples depicted a uniform and even distribution of collagen fibers which translated into significant increase in strength of skin samples in comparison to the control group. Conclusions: The optimized nanoemulsion system significantly downregulated the oxidative stress, enhanced collagen deposition, and precluded bacterial contamination of wound, thus accelerating the skin tissue regeneration process.

Fabrication and Optimization of Essential-Oil-Loaded Nanoemulsion Using Box-Behnken Design against Staphylococos aureus and Staphylococos epidermidis Isolated from Oral Cavity.

Oral bacterial infections are fairly common in patients with diabetes mellitus; however, due to limited treatment options, herbal medicines are considered an alternate solution. This study aimed to formulate a stable essential-oil-loaded nanoemulsion for the treatment of oral bacterial infections. Essential oils from edible sources including coriander, clove, cinnamon and cardamom were extracted by hydrodistillation. The response surface methodology was used to optimize the nanoemulsion formulation by applying the Box-Behnken design. The oil concentration, surfactant concentration and stirring speed were three independent factors, and particle size and polydispersity index were two responses. The particle size, polydispersity index and zeta potential of the optimized formulation were 130 mm, 0.222 and -22.9, respectively. The ATR-FTIR analysis revealed that there was no incompatibility between the active ingredients and the excipients. A significant release profile in active ingredients of nanoemulsion, i.e., 88.75% of the cinnamaldehyde and 89.33% of eugenol, was recorded after 24 h. In the ex vivo goat mucosal permeation study, 71.67% of the cinnamaldehyde permeated and that of the eugenol 70.75% from the nanoemulsion. The optimized formulation of the essential-oil-loaded nanoemulsion showed a 9 mm zone of inhibition against Staphylococcus aureus and Staphylococcus epidermidis, whereas in anti-quorum sensing analysis, the optimized nanoemulsion formulation showed an 18 mm zone of inhibition. It was concluded that formulated essential-oil-loaded nanoemulsion can be used against S. epidermidis and S. aureus infections in oral cavity.

Determination of antioxidant and bimolecular protective effect of Berberis calliobotrys Aitch. ex Koehne extracts and essential oil against H2O2 induced oxidative damage to pBR 322 DNA and RBCs.

We investigated the protective effect of fractions and essential oil from Berberis calliobotrys on H2O2 induced oxidative damage on pBR322 DNA. The crude plant material was extracted using 90% methanolic and liquid-liquid fractionation was accomplished. The essential oil analysis was performed using GC/MS. The FRAP and DPPH assays were performed to determine antioxidant activity. The DNA protection assay was performed using plasmid pBR 322 DNA. The essential oil analysis indicated presence of germacrene D (9.26%), stearic acid (7.50%), methyl tetradecanoate (6.36%) α-thujene (5.71%) and α-muurolol (5.30%) methyl eugenol (5.17%). In vitro analysis showed significant antioxidant activity of all tested extracts and essential oil. The extract showed significant effects at (1000 µg/mL) on pBR322 DNA. Finally it was concluded that Berberis calliobotrys possesses signifgant protective on effects pBR322 DNA and RBC cellular membrane.

Formulation and Characterization of Chitosan-Decorated Multiple Nanoemulsion for Topical Delivery In Vitro and Ex Vivo.

In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was evaluated physiochemically for its size and zeta potential, surface morphology, creaming and cracking, viscosity and pH. A Franz diffusion cell apparatus was used to carry out in vitro drug-release and permeation studies. The formulated nanoemulsion showed uniform droplet size and zeta potential. The pH and viscosity of the formulated emulsion were in the range of and suitable for topical delivery. The drug contents of the simple nanoemulsion (SNE), the chitosan-decorated nanoemulsion (CNE) and the MNE were 71 ± 2%, 82 ± 2% and 90 ± 2%, respectively. The formulated MNE showed controlled release of itraconazole as compared with that of the SNE and CNE. This was attributed to the chitosan decoration as well as to formulating multiple emulsions. The significant permeation and skin drug retention profile of the MNE were attributed to using the surfactants tween 80 and span 20 and the co-surfactant PEG 400. ATR-FTIR analysis confirmed that the MNE mainly affects the lipids and proteins of the skin, particularly the stratum corneum, which results in significantly higher permeation and retention of the drug. It was concluded that the proposed MNE formulation delivers drug to the target site of the skin and can be therapeutically used for various cutaneous fungal infections.

Assessment of in vitro and in vivo effect of Quercetin 3-Glucoside, Oxyresveratrol and Quercetin O-Hexoside against Leishmania tropica

Abstract The aim was to scrutinize the in vivo and in vitro activities against Leishmania tropica with compounds of Oxyresveratrol, Quercetin O-Hexoside, and Quercetin 3-Glucoside. The in vitro outcomes against Leishmania were analyzed for 24-48 hours on L. tropica KWH23 promastigotes with compounds materials having 50 - 200 µg/mL concentration with negative control and standard drug Amphotericin B. The compounds were analyzed in L. tropica infected BALB/c mice against Leishmania tropica. The Quercetin 3-Glucoside shows mean inhibition of extracellular promastigotes after 48 hours at 50, 100, 150, 200 µg/mL were 91.02 ± 0.12, 94.50 ± 0.07, 96.15 ± 0.17 and 97.01 ± 0.08 % respectively. In BALB/c mice, the intracellular amastigotes were 91% cured at 200 µg/mL and mean lesion size decreased to 0.41 ± 0.21 mm (p < 0.01). The result shows that Quercetin 3-Glucoside possesses significant anti-leishmanial activity.

Computational analysis and in vitro investigation on Citrus flavonoids for inflammatory, diabetic and AGEs targets

Abstract Flavonoids are a diverse class of polyphenolic substances largely found in plants including citrus peels and are reported to posess a variety of biological activities. We investigated important flavonoids apigenin, hesperidin, narigin, quercetin and tangeritine against diabetes and associated conditions. In current project drug likeness, ADMET analysis, molecular docking and in vitro assays were performed. The apigenin, quercetin and tanagretin exhibited compliance with Lipinski's rule of five. The molecular docking analysis showed best fit in transcriptional regulator 3TOP and 1IK3 in all tested compounds. During antioxidant assays, all flavonoids presented excellent activities. In the α-glucosidase assay, quercetin showed highest inhibition (76% at final concentration of 52 µg/ml) followed by tangeritin (73% at final concentration of 52 µg/ml). In case of 15-Lox assay, highest inhibition was seen in case of quercetin (75%) followed by apigenin (53%). In the AGEs assay, the quercetin showed 47% inhbition of protein cross link formation preceeded by the tenegretin exhited 37% inhibition. It was therefore concluded that tested flavonoids have significant activities in both in silico and in vitro models that is mainly due to differences in structural features and polar surface area.

Analysis of Plant Origin Antibiotics against Oral Bacterial Infections Using In Vitro and In Silico Techniques and Characterization of Active Constituents.

The pervasiveness of oral bacterial infections in diabetic patients is a serious health concern that may produce severe complications. We investigated 26 Ayurvedic medicinal plants traditionally used for treatment of the oral bacterial infections with the aim to look for new promising drug leads that can be further employed for herbal formulation design. The plants were grouped into three categories based on traditional usage. All plant extracts were examined for antibacterial, antibiofilm and antiquorum-sensing properties. The plants with significant activities including Juglans regia, Syzygium aromaticum, Eruca sativa, Myristica fragrans, Punica granatum and Azadirachta indica were further analyzed using HPLC-DAD-QToF and GC-MS. In silico and in vitro activity was evaluated for selected constituents. Finally, it could be concluded that eugenol and 2-phenylethylisothiocyanate are major contributors towards inhibition of bacterial biofilms and quorum sensing.

Development, characterization and optimization of methotrexate-olive oil nano-emulsion for topical application.

The chronic inflammatory conditions like psoriasis has an increased prevalence and is linked with various associated life threatening disease conditions. The main objective of this project was to developed a methotrexate-olive loaded nano emulsion. The formulation was assessed for various parameters including Thermodynamic Stability, physico-chemically characterization, drug release kinetics and entrapment efficiency and in vitro/ in vivo skin permeation analysis. Final optimized formulation had a particle size 18.27±5.78 nm with a PDI of 0.25±0.01, whereas the average entrapment efficiency of formulation was 74.68±2.1%. The release kinetics suggested 97.72% drug release at pH 5 after 20 hrs. The FTIR data confirmed that the chemical structure of drug is retained with efficient loading into the formulation. Permeation data showed that an average of 79.23±3.6µg/cm2 of methotrexate was permeated from the nano emulsion with an average flux of 2.326±0.45µg/cm2/h after 24 hrs. Finally in vivo studies on rabbit skin confirmed that the structural changes of intercellular lipid layers in the stratum corneum are not responsible for enhanced skin permeation of methotrexate loaded nano emulsion. It was concluded that olive oil based MTX-NE is suitable for topical application and can be used for management of psoriasis.

Inhibitive efficacy of Nymphoides indica rhizome extract on α-glucosidase, and cross-link formation of advanced glycation end product.

OBJECTIVE: To investigate the inhibitive efficacy of Nymphoides Indica (L.) Kuntze rhizome extract on α-glucosidase and on cross-link formation of advanced glycation end products (AGEs). METHODS: The plant extracts were prepared by cold maceration and fractionated in solvents of diverse polarity. The in vitro α-glucosidase inhibition assay, fluorescence spectrometry and SDS-PAGE analysis was performed for antiglycation assays. RESULTS: During α-glucosidase inhibition assay significant inhibition by chloroform (0.43 mg/mL) and methanol fractions (0.66 mg/mL) was noticed. During the AGEs inhibition assay, both oxidative (BSA-MGO) and non-oxidative (BSA-glucose) modes were employed. The inhibition of AGEs by total extract was considered moderate (IC50 0.10 mg/mL) as a result of non-oxidative mode, whereas in case of oxidative mode (BASA-MGO) no activity was recorded. Among fractions the methanolic fraction presented significant results both in oxidative (IC50 0.01 mg/mL) and non-oxidative modes (IC50 0.3 mg/mL). Likewise the ethyl acetate fraction was more active in non-oxidative mode (IC50 0.04 mg/mL) compared to oxidative mode (IC50 0.32 mg/mL). During assay for inhibition of cross-link formation, the chloroform fraction significantly inhibited cross-link formation in a dose dependent mode. CONCLUSION: It was finally concluded that N. Indica rhizome extract possesses significant properties that inhibit α-glucosidase, and AGEs cross-link formation.