F1 F5 Research Articles

Tornado Occurrence in the United States as Modulated by Multidecadal Oceanic Oscillations Using Empirical Model Decomposition

Studies have analyzed U.S. tornado variability and correlated F1–F5 tornado occurrence with various natural climate oscillations and anthropogenic factors. Using a relatively new empirical mode decommission (EMD) method that extracts time-frequency modes adaptively without priori assumptions like traditional time-series analysis methods, this study decomposes U.S. tornado variability during 1954–2022 into intrinsic modes on specific temporal scales. Correlating the intrinsic mode functions (IMFs) of EMD with climate indices found that 1. the U.S. overall tornado count is negatively (positively) correlated with the Atlantic Multidecadal Oscillation (AMO) index (the Southern Oscillation Index (SOI)); 2. the negative (positive) correlation tends to be more prevalent in the western (eastern) U.S.; 3. the increase in weak (F1–F2) and decrease in strong (F3–F5) tornadoes after around 2000, when both the AMO and the Pacific Decadal Oscillation (PDO) shifted phases, are likely related to their secular trends and low-frequency IMFs; and 4. the emerging Dixie Tornado Alley coincides with an amplifying intrinsic mode of the SOI that correlates positively with the eastern U.S. and Dixie Alley tornadoes. The long-term persistence of these climate indices can offer potential guidance for future planning for tornado hazards.

Transdermal drug delivery of rizatriptan using microneedles array patch: preparation, characterization and ex-vivo/in-vivo study

Given the extensive first pass metabolism of rizatriptan in oral administration and its delayed absorption during a migraine attack as a result of gastric stasis, focus has been on transdermal delivery. The main purpose of this study is to prepare and assess transdermal formulation of rizatriptan, loaded on hydrogel microneedles delivery system, to avoid first pass metabolism and also improve its percutaneous permeation rate. Rizatriptan hydrogel microneedles were prepared using micromolding method and evaluated in terms of mechanical strength, encapsulation efficiency, permeation and in-vivo skin absorption. Different formulations of rizatriptan microneedles (F1–F5) were successfully prepared using different concentrations of carboxymethyl cellulose and gelatin type A. Rizatriptan hydrogel microneedles demonstrated favorable mechanical properties, including withstanding insertion forces, thereby enhancing its skin insertion ability. In permeation study, the percent cumulative drug released after 24 h ranged between 93.1–100% which means that microneedles were able to deliver the drug effectively. For in-vivo study, F3 formulation was selected due to its superior characteristics over other formulations as it exhibited the highest swelling capacity, and demonstrated favorable mechanical properties. Furthermore, F3 showcased the most controlled drug release over a 24-hour period. Relative bioavailability of F3 microneedles was 179.59% compared to oral administration based on the AUC0-24. The observed AUC0-24 in F3 microneedles was statistically significant and 1.80 times greater than that in oral administration. The higher rizatriptan level in the microneedle demonstrated adequate drug permeability through the rat skin, suggesting the potential of microneedles for enhanced therapeutic effectiveness.

Deep fault sliding rates for Ka-Ping block of Xinjiang based on repeating earthquakes

Abstract The seismically active Ka-Ping Block within Xinjiang, China, represents a zone of potential earthquake hazards, and existing surface measurements cannot fully reflect the area’s sub-surface slip rates. To determine these slip rates and characterize the level of hazard that the study area may face in future years, using a cross-correlation of waveforms, we identified 432 repeat sequences along large faults (F1–F5) in the Ka-Ping Block between September 2009 and April 2022 and computed the annual slip rate for every sequence with the empirical relationship of the moment and the seismic magnitude. Spatial distribution images and temporal evolution characteristics of deep deformation in fault zones were constructed. We obtained five asperities in the Ka-Ping Block, the western portion of the PiQiang fault (F4) had a larger yearly slide rate than its eastern portion, and the southwest and eastern areas of the KEP station show an elevated risk of seismic activity within the next two years.

Magnetic fabric of Ocean Plate Stratigraphy mélanges: a tool for unravelling protracted histories of oceanic plates from seafloor spreading to tectonic emplacement into accretionary wedges

Multiple magnetic fabrics, referred to as F1–F5, were revealed through the anisotropy of magnetic susceptibility in an Ocean Plate Stratigraphy (OPS) mélange of the Neoproterozoic–Cambrian Blovice accretionary complex, Bohemian Massif. The fabrics post-date the formation of the mélange and the rotation of basalt blocks within the matrix and are interpreted in terms of a complex structural history of the mélange. Excluding local fabrics, the F1 fabric formed earlier along the mélange belt, recording shortening of the accretionary wedge front, whereas the higher grade F4 fabric pervasively overprinted both blocks and matrix in the SW part of the belt, recording shearing and vertical shortening at deeper structural levels closer to a megathrust surface. The preservation of angular relationships between the F1 and F4 fabrics across different parts of the mélange suggests that the blocks were only strained and not rotated during deformation, exemplifying the notion that the OPS mélanges may be a product of deformation at very shallow levels. The F1–F5 fabrics may be viewed as snapshots in a protracted evolution of OPS, where the earlier fabrics in basalt blocks may record the travel path of an oceanic plate from mid-ocean ridge towards the trench, before being overprinted in the accretionary wedge. Thematic collection: This article is part of the Ophiolites, melanges and blueschists collection available at: https://www.lyellcollection.org/topic/collections/ophiolites-melanges-and-blueschists Supplementary material: Thin-section photomicrographs, anisotropy of magnetic susceptibility data and summary diagrams for magnetic fabric types are available at https://doi.org/10.6084/m9.figshare.c.7008173

Wildfire risk weighting and behaviour prediction using open geospatial data and ontologies

This article presents a novel approach to wildfire risk assessment and behaviour prediction by leveraging open geospatial data and ontologies. The proposed methodology includes a spatially weighted index model and multicriteria analysis to represent the risk of forest fires in the affected area. It bridges gaps in theory and practice, offering a comprehensive solution for evaluating potential forest fire risk in near real time, predicting fire behaviour and elucidating the semantics of fire management. During dry and hot conditions, forest fires tend to escalate. Hence, we propose an algorithm that combines experts’ empirical criteria and open-source data to identify dangerous fires in near real time, aiding authorities in directing attention to the riskiest areas. The objective is to predict forest fire behaviour, a complex and nonlinear system influenced by dynamic factors such as weather conditions, topography and land use. Our methodology enables real-time assessment of potential forest fire risks, complemented by predictive fire behaviour scenarios and a descriptive ontology of fire management semantics. We examine existing fire-related ontologies and propose a comprehensive one encompassing incident descriptions, firefighting resources, actor interrelations and knowledge for effective action. By classifying fire sources, our algorithm enables strategic decision-making to prevent uncontrolled fires. This solution significantly enhances data using semantic and spatial relationships among wildfire resources. Furthermore, we demonstrate how ontologies improve data integration and interoperability among diverse systems and organisations involved in forest fire risk management, fostering better coordination and faster responses to critical situations. To facilitate decision-making, we create decision-making scenarios linked to analysed hot spots, drawing from open hot spot data such as National Aeronautics and Space Administration (NASA) Fire Information for Resource Management System (FIRMS), OpenStreetMap (OSM), OpenWeatherMap (OWM) and OpenTopoData (OTD). We propose an ordinal and linguistic classification system (F1–F5) denoting risk levels as low, moderate, high, very high and extreme. These values are obtained through factor aggregation and fuzzy logic. A publicly accessible, interactive web map displays the results derived from this model. Overall, our contributions to wildfire risk management provide authorities with a valuable tool to make informed decisions and mitigate the damaging effects of wildfires.

Registration of ‘GemCraft’ spring malting barley cultivar

Abstract‘GemCraft’ (Reg. no CV‐379, PI 701910), is a two‐rowed spring malt barley (Hordeum vulgare L.) developed by the USDA‐ARS, Aberdeen, ID, in cooperation with the University of Idaho Agricultural Experiment Station, in 2023. The release is derived from the cross of 2B98‐5312/98Ab11993 and was advanced through the bulk pedigree method F1–F5. GemCraft has been tested at the USDA‐ARS, and all other cooperative trials, as line 2Ab08‐X05M010‐65. This cultivar has been tested across 32 location years under irrigated conditions and 13 location years in dryland conditions. GemCraft has shown similar yield to the current malting barley cultivar checks Voyager, Merit 57, M69, Conrad, and AC Metcalfe but has higher yield potential than ‘CDC Copeland’, M69, and ‘Harrington’ under irrigated conditions. In dryland trials, GemCraft has similar yield to the checks of Voyager and Conrad but higher yield than other checks. Malting quality evaluation results showed GemCraft has high extract, low protein, and competent values in other traits. All the evaluations suggested that GemCraft would be a good choice as a malting cultivar for craft brewers.

Formulation, Development and Evaluation of Sildenafil Citrate Oral Jelly

Background: The site of drug administration, such as oral or intravenous, frequently categorizes the route of administration. Drug delivery through oral jelly reduces product costs and enhances product stability and appearance. Oral jelly is used as a drug carrier for different diseases like erectile dysfunction, arthritis, hypertension, and sore throats. Medicated jelly is easy to administer at any time and place without water. Aim: To formulate, develop, and evaluate sildenafil citrate oral jelly. Methods: Oral jelly formulations (F1–F5) with different amounts of excipients and sildenafil citrate were made and tested for things like pH, appearance, viscosity, and drug release in a test tube. The data were analyzed by SPSS version 25 software. Results: The pre-formulation FTIR study revealed that there was no significant interaction between the drug and the excipients used. The pH of all of the formulations was within the desirable range (6.3-6.8), indicating their suitability for product stability and patient acceptability. The stability study indicated that during one-month storage at 25⁰ C and at 40⁰ C/ 75% RH, no significant changes in the properties of the product were found. The viscosity of the formulations increased with increasing sodium CMC concentrations. The HPLC-based in vitro drug release study indicated that the best drug release was achieved in the F5 formulation. Conclusion: It was concluded that F5 is the formulation of choice, satisfying the ideal characteristics of an oral jelly formulation with an improvement in the drug bioavailability over the existing marketed oral formulations of Sildenafil.

Study of biological characteristics of an improved Japanese white crucian carp lineage derived from Carassius cuvieri (♀) × Megalobrama amblycephala (♂)

Based on the formation of fertile allotetraploid fish (4nJB, 4n = 148) derived from female Carassius cuvieri (JCC, 2n = 100) × male Megalobrama amblycephala (BSB, 2n = 48), an improved Japanese white crucian carp (IJCC) was obtained by mating female 4nJB and male 4nJB, and thus far, the population of IJCC has reached the fifth generations (F1–F5). The purpose of the present study was to comparatively investigate the biological characteristics of the IJCC lineage (F1–F5) and their original female parent JCC. The results of DNA content and chromosome numbers showed that the IJCC lineage was diploid with 100 chromosomes. For morphological characteristics, it appears that IJCC-F1 has smaller head and a higher body width than that of JCC, and some countable traits as well as the ratio of measurable traits were significantly different (P < 0.05) between these two fish. With the passing of generations, the appearance of the IJCC lineage has been stable. Regarding reproductive characteristics, the fecundity, sperm volume, sperm density, fertilization rate and hatching rate were not significantly different (P > 0.05) between the JCC and IJCC lineages, indicating that the reproductive capacity of the IJCC lineage was similar to that of the JCC. Furthermore, the growth performance showed that the average weight of IJCC-F1 and IJCC-F5 was significantly greater (P < 0.05) than that of JCC both at 6 months and 1 year of age. The good fertility of the IJCC lineage ensures the multigeneration utilization of its advantage, and the IJCC lineage has significant value in aquatic applications.

Aronia juice improves working memory and suppresses δ-secretase activity in 5XFAD mice

Asparagine endopeptidase (AEP) cleaves amyloid precursor protein to facilitate amyloid β (Aβ) production in the brain. Aronia berry (Aronia melanocarpa) has various beneficial effects on health through inhibition of enzymes such as dipeptidyl peptidase IV. In this study, to examine neuroprotective effects of aronia juice (AJ), AJ was given to male 5XFAD Alzheimer's disease model mice via drinking bottles over a period from 2 weeks to 12 weeks of age. AJ intake improved the performance of Y-maze test in 5XFAD mice, and suppressed the δ-secretase activity in the mouse brains. AJ intake reduced significantly Aβ deposition in the brain. AJ reduced δ-secretase activity in human neuroblastoma SH-SY5Y cells. Out of five fractions (F1–F5) obtained from AJ, only F5 reduced δ-secretase activity in SH-SY5Y cells in a dose-dependent manner. LC-MS/MS analysis suggested that F5 contains three quercetin glycosides. AJ has neuroprotective function through inhibition of δ-secretase activity of AEP.

Seed yield improvement in navy bean: Registration of ‘ND Polar’

Abstract‘ND Polar’ (Reg. no. CV‐349, PI 700767) is a new navy bean (Phaseolus vulgaris L.) cultivar developed by the Dry Edible Bean Breeding Program at North Dakota State University and released by the North Dakota Agricultural Experiment Station. ND Polar was developed using a modified pedigree method (F1–F5), followed by pure line selection based on agronomic performance, disease resistance, and seed quality characteristics. With ∼16% of the total dry bean production in the United States, navy bean is the third most important market class after pinto and black. Accounting for 35% of the total production, North Dakota is the largest producer of dry bean in the United States. Between 2015 and 2021, ND Polar was tested across 23 environments in North Dakota, where seed yield was significantly higher than ‘HMS Medalist’, ‘Blizzard’, and ‘Ensign’ and similar to ‘T9905’. ND Polar is resistant to Bean common mosaic virus and has intermediate resistance to common bacterial blight. ND Polar has desirable upright architecture to facilitate direct harvest. Under North Dakota environments, ND Polar shows an average plant height of 52 cm, has a 100‐seed weight of 18.3 g, and matures in 102 days. Canning quality was rated as acceptable. Similar to the commercial checks, ND Polar is susceptible to local races/strains of the bean rust pathogen, anthracnose, and white mold. Other traits of agronomic and economic importance are within acceptable ranges.

Production of Taxol by Endophytic Fungi Isolated from Roots of Himalayan Yew (Taxus wallichiana Zucc.)

Taxol® (generic name – Paclitaxel), the most promising chemotherapeuticagent was isolated from bark of different Taxus sp. As Taxus species arethreatened with extinction (endangered in Himalaya), thus it is imperativeto develop alternate and sustainable method for commercialization and scaleup production of paclitaxel. In this respect, physical and chemical parametersare effective and important key points for active compound production par-ticularly by using endophytic microbes. In the present study, five endophyticfungi isolated from the roots of Taxus wallichiana, are tested for paclitaxelproduction using biochemical and molecular methods. Subsequently, effectof physico-chemical parameters like temperature, pH, incubation time, andmedium constituents i.e., salt concentration, carbon and nitrogen sources onpaclitaxel production were also analyzed. Among isolates, two of the fungiviz. GBPI TWR F1 (Penicillium sp.) and GBPI TWR F5 (Aspergillus sp.)were found to be paclitaxel producing. The genomic DNA samples were sequenced to confirm the presence of two genes viz. 10-deacetylbaccatinIII-10-O-acetyl transferase (DBAT) and C-13 phenylpropanoid side chain-CoA acyltransferase (BAPT), implicated in paclitaxel biosynthesis. Boththe endophytes showed the amplicons of DBAT and BAPT genes. Resultsrevealed that after optimization of medium components and physical condi-tion, paclitaxel production was increased in both the endophytes, maximumpaclitaxel production i.e., 5.45 ± 0.98 mg/L was obtained by GBPI TWR F5(Aspergillus sp.) following 10 days of incubation at 15◦C in optimized S7liquid medium composition

DNA methylation 6 mA and histone methylation involved in multi-/trans-generational reproductive effects in Caenorhabditis elegans induced by Atrazine

Atrazine (ATR), a widely used triazine herbicide, is an environmental endocrine disruptor that can cause health problems. However, whether there are multi/trans-generational reproductive impacts of ATR have not been studied. Therefore, in this study, Caenorhabditis elegans was used as a preferable model organism to identify the multi/trans-generational reproductive toxicity of ATR. Only parental C.elegans (P0) were exposed to different concentrations (0.0004–40 mg/L) for 48 h and the subsequent offspring (F1–F5) were grown under ATR-free conditions and ATR conditions.The results showed that ATR exposure during P0 decreased fecundity, including a reduction in fertilized eggs, oocytes, and ovulation rate, delayed gonadal development, and decreased the relative area of gonad arm and germ cell number. Furthermore, continuous ATR exposure (P0–F5) causes a significant increase in reproductive toxicity in subsequent generations, although no significant toxicity occurred in the P0 generation after exposure to environmental-related concentrations, suggesting that ATR exposure might have cumulative effects. Likewise, parental exposure to ATR caused transgenerational toxicity impairments. Interestingly, only reproductive toxicity, not development toxicity, was transmitted to several generations (F1–F4), and the F2 generation showed the most notable changes. QRT-PCR results showed that genes expression related to DNA methylation 6 mA (damt-1, nmad-1) and histone H3 methylation (mes-4, met-2, set-25, set-2, and utx-1) can also be passed on to offspring. The function of H3K4 and H3K9 methylation were explored by using loss-of-function mutants for set-2, set-25, and met-2. Transmissible reproductive toxicity was absent in met-2(n4256), set-2(ok952), and set-25(n5021) mutants, which suggests that the histone methyltransferases H3K4 and H3K9 activity are indispensable for the transgenerational effect of ATR. Finally, the downstream genes of DNA methylation and histone H3 methylation were determined. ATR upregulated the expression of ZC317.7, hsp-6, and hsp-60. Mitochondrial stress in parental generation dependent transcription 6 mA modifiers may establish these epigenetic marks in progeny.

Bioassay Guided Fractionation Protocol for Determining Novel Active Compounds in Selected Australian Flora.

A large variety of unique and distinct flora of Australia have developed exceptional survival methods and phytochemicals and hence may provide a significant avenue for new drug discovery. This study proposes a bioassay guided fractionation protocol that maybe robust and efficient in screening plants with potential bioactive properties and isolating lead novel compounds. Hence, five native Australian plants were selected for this screening process, namely Pittosporum angustifolium (Gumbi gumbi), Terminalia ferdinandiana (Kakadu plum, seeds (KPS), and flesh (KPF)), Cupaniopsis anacardioides (Tuckeroo, seeds (TKS) and flesh (TKF)), Podocarpus elatus (Illawarra plum, seeds (IPS) and flesh (IPF)) and Pleiogynium timoriense (Burdekin plum, seeds (BPS) and flesh (BPF)). The methanolic extracts of the plants samples were analysed for Total phenolic content (TPC) and antioxidant capacity measure by FRAP. The highest values were found in the KPF which were 12,442 ± 1355 mg GAE/ 100 g TPC and 16,670 ± 2275 mg TXE/100 g antioxidant capacity. Extracts of GGL was deemed to be most potent with complete cell inhibition in HeLa and HT29, and about 95% inhibition in HuH7 cells. Comparative activity was also seen for KPS extract, where more than 80% cell inhibition occurred in all tested cell lines. Dose-dependent studies showed higher SI values (0.72-1.02) in KPS extracts than GGL (0.5-0.73). Microbial assays of the crude extracts were also performed against five bacterial strains commonly associated with causing food poisoning diseases were selected (Gram positive-Staphylococcus aureus and Gram negative-Escherichia coli, Salmonella typhi and Pseudomonas aeruginosa bacteria). KPF extracts were effective in suppressing microbial growth of all tested bacterial strains except for P. aeruginosa, while TKS and TKF were only slightly effective against S. aureus. Due to the potential of the GGL crude extract to completely inhibit the cells compared to KPS, it was further fractionated and tested against the cell lines. HPLC phenolic profiling of the crude extracts were performed, and numerous peak overlaps were evident in the fruit extracts. The KPF extracts demonstrated the strongest peaks which was coherent with the fact that it had the highest TPC and antioxidant capacity values. A high occurrence of t-ferulic acid in the GGL extracts was found which may explain the cytotoxic activity of GGL extracts. Peaks in KPS and KPF extracts were tentatively identified as gallic acid, protocatechuic acid, 4-hydroxybenzoic acid and syringic acid and possibly ellagic acid. HPLC time-based fractionation of the GGL extract (F1-F5) was performed and Dose dependent cytotoxic effects were determined. It was construed that F1, having the highest SI value for HeLa, HT29 and HuH7 (1.60, 1.41 and 1.67, respectively) would be promising for further fractionation and isolation process.

Saccorhiza polyschides-A Source of Natural Active Ingredients for Greener Skincare Formulations.

The growing knowledge about the harmful effects caused by some synthetic ingredients present in skincare products has led to an extensive search for natural bioactives. Thus, this study aimed to investigate the dermatological potential of five fractions (F1–F5), obtained by a sequential extraction procedure, from the brown seaweed Saccorhiza polyschides. The antioxidant (DPPH, FRAP, ORAC and TPC), anti-enzymatic (collagenase, elastase, hyaluronidase and tyrosinase), antimicrobial (Staphylococcus epidermidis, Cutibacterium acnes and Malassezia furfur), anti-inflammatory (nitric oxide, tumor necrosis factor-α, interleukin-6 and interleukin-10) and photoprotective (reactive oxygen species) properties of all fractions were evaluated. The ethyl acetate fraction (F3) displayed the highest antioxidant and photoprotective capacity, reducing ROS levels in UVA/B-exposed 3T3 fibroblasts, and the highest anti-enzymatic capacity against tyrosinase (IC50 value: 89.1 µg/mL). The solid water-insoluble fraction (F5) revealed the greatest antimicrobial activity against C. acnes growth (IC50 value: 12.4 µg/mL). Furthermore, all fractions demonstrated anti-inflammatory potential, reducing TNF-α and IL-6 levels in RAW 264.7 macrophages induced with lipopolysaccharides. Chemical analysis of the S. polyschides fractions by NMR revealed the presence of different classes of compounds, including lipids, polyphenols and sugars. The results highlight the potential of S. polyschides to be incorporated into new nature-based skincare products.

Scope of solid lipid nanoparticles per se as all-purpose moisturising sunscreens

Sun blocking effect is defined as the ability to protect the skin against ultraviolet-induced damage, indicated in terms of sun protection factor (SPF). This protection can be physical or chemical. Chemical sun protecting agents can permeate the skin leading to toxic side effects. Solid lipid nanoparticles (SLNs), also known as lipid carriers have been widely investigated across the world and have evolved as promising nano-sized drug carriers. In this study, different placebo SLN formulations demonstrate sun protection. Five different SLN formulations (F1–F5) with varying lipid content were developed using three industry amenable techniques viz. high speed stirring (HSH), high pressure homogenisation (HPH) and microemulsification method (MEM). A correlation between morphology (HR TEM), particle size-polydispersity index (DLS), sun protection factor (SPF) and occlusive effect (OE) were established. Results indicated promising SPF (6.0–24.0) and hydrating effects (OE 6.0–71.0) of spherical, mono disperse lipidic nanoparticles with lipid content of ≥4%. SLNs were found to offer hydration effects comparable to Vaseline® petroleum jelly (OE 71.0 and 82.0, respectively). Hence, SLNs per se can be regarded as: (i) safe alternative to current toxic chemical sunscreen agents, or (ii) carriers for latter, employed at low concentration to provide similar effects, and (iii) as suitable moisturisers.

Active Antialopecia Chemical Identification of Merremia peltata Leaves and Computational Study toward Androgen Receptor Using Molecular Docking and Molecular Dynamic Simulation

Alopecia is a health condition in which the hair loses its function in some or all of the body. Alopecia occurs due to various genetic, environmental, and nutritional factors. One of the methods developed to treat alopecia is through inhibition of the enzyme 5-α-reductase, which converts testosterone into its more potent metabolite, dihydrotestosterone (DHT). In ethnomedicine, the leaves of Merremia peltata are used by the people of Sulawesi as a remedy for baldness. Therefore, in this study, an in vivo study was conducted on rabbits to investigate the antialopecia activity of the ethanolic extract of M. peltata leaves. The purified M. peltata leaf extract was fractionated using vacuum liquid chromatography with several solvents to produce fractions F1–F5. Each fraction was then retested in vivo in rabbits, and its content was then analyzed by LC-MS. An in silico study was then carried out using minoxidil as a comparison ligand; 17 compounds derived from M. peltata leaves were identified as antialopecia compounds through prediction of molecular interactions and molecular dynamics simulation and prediction of absorption, distribution, metabolism, excretion, and toxicology (ADME-Tox). The assay results showed that fractions F2 and F3 had a better effect on hair growth compared to the positive control, and the test compound obtained from the LC-MS analysis, bufotalinin, had a strong binding energy to the receptor in the molecular docking interaction study: −5.99 kcal/mol compared to −4.8 kcal/mol for minoxidil. Molecular dynamics simulation analysis with complex stability parameters based on solvent-accessible surface area (SASA), principal component analysis (PCA), root mean square deviation (RMSD), and root mean square fluctuation (RMSF) showed that bufotalinin has good affinity for androgen receptors. ADME-Tox prediction for bufotalinin showed good results for the parameters of skin permeability, absorption, and distribution. Therefore, bufotalinin, a steroid compound, is a potential androgen receptor antagonist and could be useful in the treatment of alopecia.

Flavonoid Derivatives as Potential Cholinesterase Inhibitors in Scopolamine-Induced Amnesic Mice: An In Vitro, In Vivo and Integrated Computational Approach.

Flavonoids are one of the most exciting types of phenolic compounds with a wide range of bioactive benefits. A series of flavone derivatives (F1–F5) were previously synthesized from substituted O-hydroxy acetophenone and substituted chloro-benzaldehydes. The titled compounds F1–F5 in the present study were evaluated for their anticholinesterase potential (against AChE and BuChE). The obtained results were then validated through a molecular docking approach. Compound F5 was found to be the most potent inhibitor of AChE (IC50 = 98.42 ± 0.97 µg/mL) followed by compound F4, whereas compound F2 was found to be the most promising inhibitor of BuChE (IC50 = 105.20 ± 1.43 µg/mL) among the tested compounds. The molecular docking analysis revealed a similar trend in the binding affinity of compounds with the targeted enzymes and found them to be capable of forming highly stable complexes with both receptors. The selected compounds were further subjected to in vivo assessment of cognitive function in a scopolamine-induced amnesic animal model, in which almost all compounds F1–F5 significantly attenuated the amnesic effects as evaluated through Y-Maze Paradigm and novel object discrimination (NOD) tasks, findings that were further supported by ex vivo experimental results. Among (F1–F5), F5 showed significant anti-amnesic effects in scopolamine-induced amnesic models and ameliorated the memory loss in behavioral model studies as compared to counterparts. In ex vivo study, noteworthy protection from oxidative stress in the brains of scopolamine-induced amnesic mice was also recorded for F5. These findings also confirmed that there were no significant differences among the in vivo and ex vivo results after administration of F1–F5 (7.5 or 15 mg/kg) or donepezil (2 mg/kg). These synthesized flavonoids could serve as potential candidates for new neuroprotective and nootropic drugs. However, further studies are needed to validate their observed potential in other animal models as well.

Evaluation of nanoherbal gel for anti-warts activity

In the present experimental investigation a novel nanoherbal gel containing iron nanoparticles and extract from Cuscuta reflexa was used as a drug. Synthesized nanoherbal increased the drug solubility and penetration in the skin and is useful as a novel delivery system for better anti-warts activity. The experimental work includes preformulation studies of drug (Cuscuta reflexa) which include organoleptic properties, identification and solubility studies. Spectroscopy characterization was performed for identification of drug. The iron nanoparticles were evaluated for their characteristic such as appearance, viscosity and odor. Various formulations F1–F5 was prepared using different formulation variables based on experiment design. The result showed that the formulation F-5 provide the better release using 5.5 pH acetate buffer and at 37 °C temperature for anti-warts activity. The maximum drug release through synthesized nanoherbal gel was found to be 91.3%. Nanoherbal formulation was evaluated for physical appearance, pH, consistency, spreadibility and drug content. Stability study of formulation F5 was carried out for a period of 3 months to determine the percentage release and the results revealed that the formulation is stable under varied humidity and temperature condition and there was no major change in the amount of drug release during the storage condition, which reflected the stability of F5 formulation.

Gelidiales Are Not Just Agar-Revealing the Antimicrobial Potential of Gelidium corneum for Skin Disorders.

In recent decades, seaweeds have proven to be an excellent source of bioactive molecules. Presently, the seaweed Gelidium corneum is harvested in a small area of the Portuguese coast exclusively for agar extraction. The aim of this work was to fully disclosure Gelidium corneum as a sustainable source of antimicrobial ingredients for new dermatological formulations, highlighting its potential to be explored in a circular economy context. For this purpose, after a green sequential extraction, these seaweed fractions (F1–F5) were chemically characterized (1H NMR) and evaluated for their antimicrobial potential against Staphylococcus aureus, Staphylococcus epidermidis and Cutibacterium acnes. The most active fractions were also evaluated for their effects on membrane potential, membrane integrity and DNA damage. Fractions F2 and F3 displayed the best results, with IC50 values of 16.1 (7.27–23.02) μg/mL and 51.04 (43.36–59.74) μg/mL against C. acnes, respectively, and 53.29 (48.75–57.91) μg/mL and 102.80 (87.15–122.30) μg/mL against S. epidermidis, respectively. The antimicrobial effects of both fractions seem to be related to membrane hyperpolarization and DNA damage. This dual mechanism of action may provide therapeutic advantages for the treatment of skin dysbiosis-related diseases.

Tacrolimus-Loaded Solid Lipid Nanoparticle Gel: Formulation Development and In Vitro Assessment for Topical Applications.

The currently available topical formulations of tacrolimus have minimal and variable absorption, elevated mean disposition half-life, and skin irritation effects resulting in patient noncompliance. In our study, we fabricated tacrolimus-loaded solid lipid nanoparticles (SLNs) that were converted into a gel for improved topical applications. The SLNs were prepared using a solvent evaporation method and characterized for their physicochemical properties. The particle size of the SLNs was in the range of 439 nm to 669 nm with a PDI of ≤0.4, indicating a monodispersed system. The Zeta potential of uncoated SLNs (F1–F5) ranged from −25.80 to −15.40 mV. Those values reverted to positive values for chitosan-decorated formulation (F6). The drug content and entrapment efficiency ranged between 0.86 ± 0.03 and 0.91 ± 0.03 mg/mL and 68.95 ± 0.03 and 83.68 ± 0.04%, respectively. The pH values of 5.45 to 5.53 depict their compatibility for skin application. The surface tension of the SLNs decreased with increasing surfactant concentration that could increase the adherence of the SLNs to the skin. The release of drug from gel formulations was significantly retarded in comparison to their corresponding SLN counterparts (p ≤ 0.05). Both SLNs and their corresponding gel achieved the same level of drug permeation, but the retention of the drug was significantly improved with the conversion of SLNs into their corresponding gel formulation (p ≤ 0.05) due to its higher bioadhesive properties.