The Classification of VOCs Based on Sensor Images Using a Lightweight Neural Network for Lung Cancer Diagnosis.

The application of artificial intelligence to point-of-care testing (POCT) disease detection has become a hot research field, in which breath detection, which detects the patient's exhaled VOCs, combined with sensor arrays of convolutional neural network (CNN) algorithms as a new lung cancer detection is attracting more researchers' attention. However, the low accuracy, high-complexity computation and large number of parameters make the CNN algorithms difficult to transplant to the embedded system of POCT devices. A lightweight neural network (LTNet) in this work is proposed to deal with this problem, and meanwhile, achieve high-precision classification of acetone and ethanol gases, which are respiratory markers for lung cancer patients. Compared to currently popular lightweight CNN models, such as EfficientNet, LTNet has fewer parameters (32 K) and its training weight size is only 0.155 MB. LTNet achieved an overall classification accuracy of 99.06% and 99.14% in the own mixed gas dataset and the University of California (UCI) dataset, which are both higher than the scores of the six existing models, and it also offers the shortest training (844.38 s and 584.67 s) and inference times (23 s and 14 s) in the same validation sets. Compared to the existing CNN models, LTNet is more suitable for resource-limited POCT devices.

Evaluating the effects of various ethanolic medicinal plant extracts on metastatic breast cancer proliferation, invasion, and expression of a novel potential drug target; CD82 metastatic suppressor protein, and on in vivo angiogenesis using the ex ovo yolk sac membrane (YSM) assay.

PURPOSE: Breast cancer metastasis relies on cellular invasion and angiogenesis facilitated by the downregulation of metastatic suppressor proteins like Cluster of Differentiation 82 (CD82). Currently, no medicines target multiple systems to prevent metastatic progression through CD82 upregulation. This study screened for plant extracts displaying effects on cell proliferation, invasion, and CD82 expression in breast cancer cells, and in vivo angiogenesis, and further correlated between the biological activities and effect on CD82 expression. METHODS: Seventeen ethanolic plant extracts were screened for their effect on cell proliferation (against MDA-MB-231 and MCF-7 breast cancer and Hek293 kidney cells), cell invasion and effect on CD82 expression in metastatic MDA-MB-231 cells. Selected extracts were further evaluated for in vivo anti-angiogenesis. RESULTS: Extracts displayed varying antiproliferative activity against the different cell lines, and those that showed selectivity indexes (SI) > 0.5 against MDA-MB-231 were selected for anti-invasion evaluation. Buddleja saligna Willd. (BS), Combretum apiculatum Sond. (CA), Foeniculum vulgare, Greyia radlkoferi, Gunnera perpensa and Persicaria senegalensis (Meisn.) Soják (PS) displayed 50% inhibitory concentration (IC50) values of 44.46 ± 3.46, 74.00 ± 4.48, 180.43 ± 4.51, 96.97 ± 2.29, 55.29 ± 9.88 and 243.60 ± 2.69 µg/mL, respectively against MDA-MB-231, and compared to Hek293 showed SI of 0.9, 0.7, 1.4, 1.1, 2.2 and 0.5. Significant invasion inhibition was observed at both 20 and 40 µg/mL for BS (94.10 ± 0.74 and 96.73 ± 0.95%) and CA (87.42 ± 6.54 and 98.24 ± 0.63%), whereas GR (14.91 ± 1.62 and 41 ± 1.78%) and PS (36.58 ± 0.54 and 51.51 ± 0.83%), only showed significant inhibition at 40 µg/mL, and FV (< 5% inhibition) and GP (10 ± 1.03 and 22 ± 1.31%) did not show significant inhibition at both concentrations. Due to the significant anti-invasive activity of BS, CA and PS at 40 µg/mL, these extracts were further evaluated for their potential to stimulate CD82. BS showed significant (p < 0.05) reduction in CD82 at 20 and 40 µg/mL (13.2 ± 2.2% and 20.3 ± 1.5% decrease, respectively), whereas both CA and PS at 20 µg/mL increased (p < 0.05) CD82 expression (16.4 ± 0.8% and 5.4 ± 0.6% increase, respectively), and at 40 µg/mL significantly reduced CD82 expression (23.4 ± 3.1% and 11.2 ± 2.9% decrease, respectively). Using the yolk sac membrane assay, BS (59.52 ± 4.12 and 56.72 ± 3.13% newly formed vessels) and CA (83.33 ± 3.17 and 74.00 ± 2.12%) at both 20 and 40 µg/egg showed significant (p < 0.001) angiogenesis inhibition, with BS showing statistical similar activity to the positive control, combretastatin A4 (10 nmol/egg), whereas PS only displayed significant (p < 0.001) angiogenesis stimulation at 40 µg/egg (120.81 ± 3.34% newly formed vessels). CONCLUSION: BS exhibits antiproliferative, anti-invasive, and anti-angiogenic activity despite inhibiting CD82, suggesting an alternative mode of action. CA at 20 µg/mL shows moderate anti-invasive and anti-angiogenic potential by stimulating CD82, while at 40 µg/mL it still displays these properties but inhibits CD82, suggesting an additional mode of action. PS, with the least antiproliferative activity, stimulates CD82 and inhibits angiogenesis at 20 µg/mL but inhibits CD82 and increases angiogenesis at 40 µg/mL, indicating CD82 targeting as a major mode of action. Future studies should explore breast cancer xenograft models to assess the extracts' impact on CD82 expression and angiogenesis in the tumor microenvironment, along with isolating bioactive compounds from the extracts.

Modification of hordein by gallic acid in ethanol-free environments: Impact of covalent and non-covalent interactions on structure, physicochemical properties and self-assembly.

The objectives of this study were to modify hordein with gallic acid (GA) in alcohol-free media and to compare the impact of covalent and non-covalent binding on the properties of hordein. Covalent hordein-GA complexes (H-GA) and non-covalent hordein/GA complexes (H/GA) were distinguished by molecular weight, free sulfhydryl groups and free amino groups. Isothermal titration calorimetry (ITC) demonstrated that physical mixing induced non-covalent binding of GA to hordein via hydrogen bonding and hydrophobic interactions, with a lower binding efficiency than covalent ones. Both complexation types led to a structural shift of hordein toward disorder, while grafting of oligomeric GA and alkaline treatment resulted in lower surface hydrophobicity and higher antioxidant activity of H-GA compared to H/GA. The nanoparticles assembled from H-GA had smaller particle sizes and higher physical stability than those formed from H/GA. The results of this study may provide new insights into the modification of hordein by polyphenols.

In vitro Antibacterial Activity of Ethanolic Tanao Si Kan Dang RD1 (Cannabis sativa L.) Extracts Against Human Antibiotic-Resistant Bacteria.

<b>Background and Objective:</b> A new strain of cannabis, <i>Cannabis sativa</i> L. Tanao Si Kan Dang RD1, has been approved and registered by the Rajamangala University of Technology Isan, Thailand. The <i>C. sativa</i> is acknowledged for its medicinal properties which demonstrated various therapeutic properties, such as anti-cancer and antibacterial activities. This study aimed to investigate the antibacterial activity of ethanolic extracts from the stems and leaves of the Tanao Si Kan Dang RD1 strain against seven antibiotic-resistant bacteria. <b>Materials and Methods:</b> The primary antibacterial activity of ethanolic Tanao Si Kan Dang RD1 extracts were determined using the disc diffusion method, while the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined using the broth microdilution method. <b>Results:</b> The largest inhibition zone, measuring 12 mm, was observed in leaf extracts against <i>Pseudomonas aeruginosa</i> 101. The lowest MIC, at 0.78 mg/mL, was obtained from stem extracts against <i>Stenotrophomonas maltophilia</i>. The lowest MBCs, at 12.5 mg/mL, were observed in leaf extracts against <i>Enterococcus faecalis</i>, <i>Acinetobacter baumannii</i>, multidrug-resistant <i>Klebsiella</i> <i>pneumoniae</i>, <i>Stenotrophomonas maltophilia</i> and <i>Pseudomonas aeruginosa</i> 101 and stem extracts against <i>Acinetobacter baumannii</i>, multidrug-resistant <i>Klebsiella pneumoniae</i>, <i>Stenotrophomonas maltophilia</i> and <i>Pseudomonas aeruginosa</i> 101. <b>Conclusion:</b> This study presents a novel finding regarding the antibacterial activity of ethanolic extracts from the leaves and stems of Tanao Si Kan Dang RD1 against antibiotic-resistant bacteria. The potential application of these cannabis plant extracts in the development of antibiotics capable of combating antibiotic-resistant pathogenic bacteria represents a promising strategy to address a significant global health concern.

Vasorelaxant and Blood Pressure-Lowering Effects of Cnidium monnieri Fruit Ethanol Extract in Sprague Dawley and Spontaneously Hypertensive Rats.

Cnidium monnieri (L.) Cusson, a member of the Apiaceae family, is rich in coumarins, such as imperatorin and osthole. Cnidium monnieri fruit (CM) has a broad range of therapeutic potential that can be used in anti-bacterial, anti-cancer, and sexual dysfunction treatments. However, its efficacy in lowering blood pressure through vasodilation remains unknown. This study aimed to assess the potential therapeutic effect of CM 50% ethanol extract (CME) on hypertension and the mechanism of its vasorelaxant effect. CME (1-30 µg/mL) showed a concentration-dependent vasorelaxation on constricted aortic rings in Sprague Dawley rats induced by phenylephrine via an endothelium-independent mechanism. The vasorelaxant effect of CME was inhibited by blockers of voltage-dependent and Ca2+-activated K+ channels. Additionally, CME inhibited the vascular contraction induced by angiotensin II and CaCl2. The main active compounds of CM, i.e., imperatorin (3-300 µM) and osthole (1-100 µM), showed a concentration-dependent vasorelaxation effect, with half-maximal effective concentration values of 9.14 ± 0.06 and 5.98 ± 0.06 µM, respectively. Orally administered CME significantly reduced the blood pressure of spontaneously hypertensive rats. Our research shows that CME is a promising treatment option for hypertension. However, further studies are required to fully elucidate its therapeutic potential.

A 70% Ethanol Neorhodomela munita Extract Attenuates RANKL-Induced Osteoclast Activation and H2O2-Induced Osteoblast Apoptosis In Vitro.

The rapid aging of the population worldwide presents a significant social and economic challenge, particularly due to osteoporotic fractures, primarily resulting from an imbalance between osteoclast-mediated bone resorption and osteoblast-mediated bone formation. While conventional therapies offer benefits, they also present limitations and a range of adverse effects. This study explores the protective impact of Neorhodomela munita ethanol extract (EN) on osteoporosis by modulating critical pathways in osteoclastogenesis and apoptosis. Raw264.7 cells and Saos-2 cells were used for in vitro osteoclast and osteoblast models, respectively. By utilizing various in vitro methods to detect osteoclast differentiation/activation and osteoblast death, it was demonstrated that the EN's potential to inhibit RANKL induced osteoclast formation and activation by targeting the MAPKs-NFATc1/c-Fos pathway and reducing H2O2-induced cell death through the downregulation of apoptotic signals. This study highlights the potential benefits of EN for osteoporosis and suggests that EN is a promising natural alternative to traditional treatments.

Separation, enrichment and cytoprotection of antioxidant peptides from Xuanwei ham using aqueous two-phase extraction.

An ethanol/(NH4)2SO4 biphasic (aqueous two-phase) system was designed to effectively separate antioxidant peptides from Xuanwei ham, and its potential to prevent ultraviolet A-induced damage to skin cells was explored. Optimization via single factor experiments and response surface methodology revealed that under 20 % ethanol aqueous solution (w/w), 25.5 % (NH4)2SO4 aqueous solution (w/w), and pH 8.80 conditions, the optimal extraction ratio was 59.0 ± 1.73 %. In vitro antioxidant activity and cellular assays showed that the peptide purified in the upper phase exhibited strong antioxidant activity, increasing the viability of HaCat cells damaged by UVA irradiation from 56.14 ± 1.05 % to 66.3 ± 1.76 %. We used an in silico peptide screening strategy and identified 10 with potential antioxidant activity, emphasizing the important role of amino acids Pro, Gly, and Ala in antioxidant activity.

Origanum Grosii Extracts as Novel Eco-Friendly Corrosion Inhibitors for Mild Steel In HCl Medium.

Two green inhibitors extracted from an endemic species (Origanum grosii (Og)) using two solvents of different polarity (water and ethanol), OgW (aqueous extract) and OgE (ethanolic extract), were used for the anticorrosion of mild steel (M steel) in a 1 M HCl medium. Anticorrosive performance of OgW and OgE was assessed using standard electrochemical techniques, EIS/PDP measurements, weight loss method and SEM/EDX surface analysis. The results show that OgW achieves a maximum inhibition efficiency of 92 % and that the extract in aqueous medium (more polar) is more efficient than the extract in ethanolic medium (less polar). Both extracts act as mixed inhibitors and their corrosion process is predominantly governed by a charge transfer. Concentration and temperature effect was studied and shown that they are two antagonistic parameters for the evolution of inhibitory effectiveness of both OgW and OgE. The adsorption isotherms of the two inhibitors OgE and OgW obey to the Langmuir adsorption model. Moreover, the examination of SEM images and EDX spectra support a deposit of both extracts on the metal surface by an adsorption phenomenon. Besides, theoretical approach of the molecular structures of the major compounds M-OgW and M-OgE and inhibition efficiency was examined via DFT calculations and molecular dynamics simulations and it was consistent with the experimental findings.

Opuntia monacantha: Validation of the anti-inflammatory and anti-arthritic activity of its polyphenolic rich extract in silico and in vivo via assessment of pro- and anti-inflammatory cytokines.

ETHNOPHARMACOLOGICAL RELEVANCE: Opuntia monacantha belongs to the cactus family Cactaceae and is also known by cochineal prickly pear, Barbary fig or drooping prickly pear. It was traditionally used to treat pain and inflammation. O. monacantha cladodes showed pharmacological effects such as antioxidant potential owing to the presence of certain polysaccharides, flavonoids, and phenols. AIM OF THE STUDY: This research aimed to evaluate the anti-inflammatory as well as the anti-arthritic potential of ethanol extract of Opuntia monacantha (E-OM). MATERIALS AND METHODS: In vivo edema in rat paw was triggered by carrageenan and used to evaluate anti-inflammatory activity, while induction of arthritis by Complete Freund's Adjuvant (CFA) rat model was done to measure anti-arthritic potential. In silico studies of the previously High performance liquid chromatography (HPLC) characterized metabolites of ethanol extract was performed by using Discovery Studio 4.5 (Accelrys Inc., San Diego, CA, USA) within active pocket of glutaminase 1 (GLS1) (PDB code: 3VP1; 2.30 Å). RESULTS: EOM, particularly at 750 mg/kg, caused a reduction in the paw edema significantly and decreased arthritic score by 80.58% compared to the diseased group. It revealed significant results when histopathology of ankle joint was examined at 28th day as it reduced inflammation by 18.06%, bone erosion by 15.50%, and pannus formation by 24.65% with respect to the diseased group. It restored the altered blood parameters by 7.56%, 18.47%, and 3.37% for hemoglobin (Hb), white blood count (WBC), and platelets, respectively. It also reduced rheumatoid factor RF by 13.70% with concomitant amelioration in catalase (CAT) and superoxide dismutase (SOD) levels by 19%, and 34.16%, respectively, in comparison to the diseased group. It notably decreased mRNA expression levels of COX-2, IL-6, TNF-α, IL-1, NF-κß and augmented the levels of IL-4 and IL-10 in real time PCR with respect to the diseased group and piroxicam. HPLC analysis previously performed showed that phenolic acids and flavonoids are present in E-OM. Molecular docking studies displayed pronounced inhibitory potential of these compounds towards glutaminase 1 (GLS1), approaching and even exceeding piroxicam. CONCLUSIONS: Thus, Opuntia monacantha could be a promising agent to manage inflammation and arthritis and could be incorporated into pharmaceuticals.

Leaf extracts of eight selected southern African medicinal plants modulate pro-inflammatory cytokine secretion in LPS-stimulated RAW 264.7 macrophages.

This study investigates the anti-inflammatory properties of extracts prepared from the leaves of eight southern African medicinal plants used traditionally to treat inflammation and pain. The inhibitory effect of aqueous and ethanol extracts on the release of pro-inflammatory cytokines was determined in lipopolysaccharide (LPS) stimulated and unstimulated RAW 264.7 murine macrophage cells. The levels of interleukin (IL)-1ß, IL-6, tumour necrosis factor-α (TNF-α), interferon-gamma (IFN-γ), monocyte chemoattractant protein 1 (MCP-1) and macrophage inflammatory protein (MIP)-2 release were determined using cytokine multiplex-bead assays. The ethanol extracts of Melianthus comosus Vahl (commonly known as honey flower), Tetradenia riparia (Hochst.) Codd (misty plume bush) and Warburgia salutaris (G. Bertol.) Chiov. (pepper-bark tree), demonstrated the most significant inhibitory activity, with over 50-fold inhibition of IL-1ß, IL-6 and TNF-α levels in LPS-stimulated RAW 264.7 macrophages. The aqueous extract of M. comosus also significantly inhibited the secretion of all the tested cytokines and chemokines. Phytochemical investigation of M. comosus ethanol leaf extract using ultra-high-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-HRMS) led to the detection of crassolide, deoxylimonoic acid D-ring-lactone, 2-hydroxynonanoic acid and 5-noniloxytryptamine. To the best of our knowledge, the cytokine inhibition properties of most of the medicinal plants screened in this study are reported for the first time. Our results support the use of southern African medicinal plants as anti-inflammatory remedies and provide an insight into the immunomodulatory mechanisms of action.

Fractionation of oil palm fronds using ethanol-assisted deep eutectic solvent: Influence of ethanol concentration on enhancing enzymatic saccharification and lignin ß-O-4 content.

Numerous fractionation methods have been developed in recent years for separating components such as cellulose, hemicellulose, and lignin from lignocellulosic biomass wastes. Deep eutectic solvents (DES) have recently been widely investigated as captivating green solvents for biomass fractionation. However, most acidic-based deep eutectic solvent fractionation produces condensed lignin with low ß-O-4 content. Besides, most DESs exhibit high viscosity, which results in poor mass transfer properties. This study aimed to address the challenges above by incorporating ethanol into the deep eutectic solvent at various concentrations (10-50 wt%) to fractionate oil palm fronds at a mild condition, i.e., 80 °C, 1 atm. Cellulose residues fractionated with ethanol-assisted deep eutectic solvent showed a maximum glucose yield of 85.8% when 20 wt% of ethanol was incorporated in the deep eutectic solvent, significantly higher than that achieved by pure DES (44.8%). Lignin extracted with ethanol-assisted deep eutectic solvent is lighter in color and higher in ß-O-4 contents (up to 44 ß-O-4 per 100 aromatic units) than pure DES-extracted lignin. Overall, this study has demonstrated that incorporating ethanol into deep eutectic solvents could enhance the applicability of deep eutectic solvents in the complete valorization of lignocellulosic biomass. Highly enzymatic digestible cellulose-rich solid and ß-O-4-rich lignin attained from the fractionation could serve as sustainable precursors for the production of biofuels.

Ipomoea carnea mitigates ethanol-induced ulcers in irradiated rats via Nrf2/HO-1 pathway: an in vivo and in silico study.

The aim of this study was to investigate the potential of Ipomoea carnea flower methanolic extract (ICME) as a natural gastroprotective therapy against ethanol-induced gastric ulcers, particularly in individuals exposed to ionizing radiation (IR). The study focused on the Nrf2/HO-1 signaling pathway, which plays a crucial role in protecting the gastrointestinal mucosa from oxidative stress and inflammation. Male Wistar rats were divided into nine groups, the control group received distilled water orally for one week, while other groups were treated with ethanol to induce stomach ulcers, IR exposure, omeprazole, and different doses of ICME in combination with ethanol and/or IR. The study conducted comprehensive analyses, including LC-HRESI-MS/MS, to characterize the phenolic contents of ICME. Additionally, the Nrf2/HO-1 pathway, oxidative stress parameters, gastric pH, and histopathological changes were examined. The results showed that rats treated with IR and/or ethanol exhibited histopathological alterations, increased lipid peroxidation, decreased antioxidant enzyme activity, and reduced expression levels of Nrf2 and HO-1. However, pretreatment with ICME significantly improved these parameters. Phytochemical analysis identified 39 compounds in ICME, with flavonoids, hydroxybenzoic acids, and fatty acids as the predominant compounds. Virtual screening and molecular dynamics simulations suggested that ICME may protect against gastric ulceration by inhibiting oxidative stress and inflammatory mediators. In conclusion, this study demonstrates the potential of ICME as a natural gastroprotective therapy for preventing gastric ulcers. These findings contribute to the development of novel interventions for gastrointestinal disorders using natural plant extracts particularly in individuals with a history of radiation exposure.

Organosolv Treatment of Red Grape Pomace for Effective Recovery of Antioxidant Polyphenols and Pigments Using a Ternary Glycerol/Ethanol/Water System under Mild Acidic Conditions.

The purpose of this investigation was (i) the development of a novel, green tertiary solvent system, composed of water, ethanol and glycerol, and (ii) the implementation of an organosolv treatment of red grape pomace (RGP) for the efficient production of polyphenol-containing extracts with enhanced antioxidant properties. The treatment developed was performed under mild acidic conditions, imparted by the addition of citric acid, and it was first evaluated on the basis of severity, establishing linear models that described the correlation between treatment performance and combined severity factors. To solicit treatment optimization, response surface methodology was implemented, considering solvent acidity and residence time as the treatment variables. The optimized treatment afforded maximum total polyphenol (166 ± 6 mg GAE g-1 DM), total pigment (4.4 ± 0.2 mg MvE g-1 DM) and total flavanol (31.5 mg CtE g-1 DM) yields and extracts with particularly enhanced antioxidant activity. This might be attributed to specific constituents with high antioxidant potency, such as catechin, determined in the extract using high-performance liquid chromatography. Thus, the treatment developed is proposed as a highly efficient process to generate RGP extracts enriched in polyphenolic compounds, with enhanced antioxidant activity. Such extracts might then be valorized as food additives, to provide antioxidant protection and/or pigmentation.

Characterization and Anti-Ultraviolet Radiation Activity of Proanthocyanidin-Rich Extracts from Cinnamomum camphora by Ultrasonic-Assisted Method.

The ultrasonic-assisted extraction (UAE) method was employed to separate Cinnamomum camphora proanthocyanidin-rich extracts (PCEs). This extraction process was optimized by the Box-Behnken design, and the optimal conditions, on a laboratory scale, were as follows: an ethanol concentration of 75%, a liquid-to-solid ratio of 24 mL/g, an ultrasonic time of 39 min, and an ultrasonic power of 540 W. Under the obtained conditions, the PCE yield extracted by UAE was higher than that from heat reflux extraction and soaking extraction. An ultra-performance liquid chromatography-tandem mass spectrometry analysis was employed to characterize the phloroglucinolysis products of the C. camphora PCEs, by which epigallocatechin, catechin, epicatechin, and (-)-epigallocatechin-3-O-gallate were identified as the terminal units; epigallocatechin, epicatechin, and (-)-epigallocatechin-3-O-gallate were recognized as extension units. The C. camphora PCEs possessed higher anti-ultraviolet activity in vitro compared with the commercially available sunscreen additive of benzophenone with respect to their ethanol solutions (sun protection factor of 27.01 ± 0.68 versus 1.96 ± 0.07 at a concentration of 0.09 mg/mL) and sunscreens (sun protection factor of 17.36 ± 0.62 versus 14.55 ± 0.47 at a concentration of 20%). These results demonstrate that C. camphora PCEs possess an excellent ultraviolet-protection ability and are promising green sunscreen additives that can replace commercial additives.

Bioactivity, phytochemistry studies and subacute in vivo toxicity of ethanolic leaf extract of white mulberry (Morus alba linn.) in female mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional uses of Morus alba L. leaf extracts (MLE) have been reported for treating hyperglycaemia and diabetes. Phytochemical compounds in the leaves demonstrated the ability to enhance insulin sensitivity and ß-cell secretory function, suggesting their potential value in reducing blood glucose and treating diabetes. However, the phytochemical constituents and safety of the herbal medicines need to be verified in each experimental field from different growing areas. Studies on the phytochemistry and toxicity of Morus alba leaves in Southeast Asia, especially in Brunei, have never been investigated. AIM OF THE STUDY: This study aimed to investigate the bioactivity and phytochemistry of Morus alba ethanolic leaf extract from Brunei Darussalam and its subacute toxic effects in the Institute of Cancer Research (ICR) female mice. MATERIALS AND METHODS: The phenolic yield and antioxidant of the extract were analysed. Meanwhile, liquid chromatography-mass spectrometry and high-performance liquid chromatography were utilised to determine the phenolic compound of the MLE. In the subacute toxicity study, twenty-five female mice were randomly divided into five groups: the control group, which received oral gavage of 5% dimethyl sulfoxide solvent (DMSO), and the MLE treatment group, which received the extract at a dose of 125, 250, 500 and 1000 mg/kg. Physiology, haematology, biochemistry, and histology were evaluated during the study. RESULTS: Morus alba leaf depicted total phenolic 10.93 mg gallic acid equivalents (GAE)/g dry weight (DW), flavonoid 256.67 mg quercetin equivalents (QE)/g DW, and antioxidant bioactivity content of 602.03 IC50 µg/mL and 13.21 mg Fe2+/g DW. Twenty compounds in the Morus alba ethanolic leaf extract were identified, with chlorogenic acid (305.60 mg/100 g DW) as the primary compound. As for subacute toxicity in this study, neither mortality nor haematological changes were observed. On the other hand, administration of 500 and 1000 mg/kg MLE resulted in mild hepatocellular injury, as indicated by a significant (p < 0.05) increase in liver enzyme activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). The histopathological score showed mild hepatocellular necrosis in administering 250, 500, and 1000 mg/kg of MLE. The parameters of renal injury were within normal limits, with the increase in eosinophilic cytoplasm observed in the histological scoring at 1000 mg/kg of MLE. CONCLUSIONS: Morus alba leaf extract showed abundant polyphenols. In a study on subacute toxicity, MLE caused mild hepatotoxicity in mice. The toxic effect of the extract may be due to kaempferol and chlorogenic acid compounds. The 125 mg/kg MLE dose was safe with no adverse effects.

In vitro and In vivo Effects of Ethanolic Extract of Fumaria parviflora Lam. Embedded in Chitosan Nanoparticles Against Leishmania major.

INTRODUCTION: Fumaria has been traditionally used to treat skin damages due to anti-inflammatory properties. In the present study, we evaluated the effect of the ethanolic extract of Fumaria parviflora Lam. (F. parviflora) against Leishmania major (L. major) using chitosan biopolymer drug delivery system both In vitro and In vivo models. MATERIALS AND METHODS: The ethanolic extract of F. parviflora was analyzed by HPLC to determine its active ingredients content. The extract was then loaded on chitosan nanoparticles (CNPs). The parasite was treated with various concentrations of the ethanolic extract, CNPs and CNPs loaded with F. parviflora extract (CNPs@ F. parviflora). The size of lesions of treated mice were measured on a weekly basis. The parasite burden was evaluated 8 weeks after treatment. RESULTS: The HPLC analysis showed the presence of Fumaric acid at a high concentration. The percentage of the drug released from CNPs@ F. parviflora within 24 and 72 h were 65% and 90% respectively. The results showed that F. parviflora extract and CNPs@ F. parviflora caused 84% and 96% growth inhibition of L. major promastigotes as revealed by Neubauer chamber counting and MTT test respectively. The IC50 values of F. parviflora extract and CNPs@ F. parviflora were 450 and 68.4 µg/ml respectively. In amastigote assay, the best results showed in CNPs@ F. parviflora that only 2% of macrophages were infected with amastigotes. In vivo experiments for mice treated with F. parviflora and CNPs @ F. parviflora in comparison to control group showed a significant reduction (P < 0.05) in the mean diameter of the lesions (2.3 and 1.72 mm and 9.91 mm respectively). CONCLUSION: The ethanolic extract of F. parviflora both as standalone and loaded in CNPs showed promising inhibitory effects against L. major both upon In vitro and In vivo experimentation as well as therapeutic effects for wound healing in infected mice.

Regiospecificity of Immobilized Candida antarctica Lipase B (CAL-B) towards 2,3-Diacyl-1-O-alkyl Glyceryl Ether in Ethanol.

Highly pure 2,3-dioleoyl-1-O-alkyl glyceryl ether (DOGE), whose 1-position is a lipase-tolerant ether bond, was chemically synthesized and its detailed regioselectivity and acyl transfer were confirmed. During ethanolysis using immobilized Candida antarctica lipase B (CAL-B) with DOGE as the substrate, monooleoyl-1-O-alkyl glyceryl ethers (MOGEs) and a few 1-alkyl glyceryl ethers were formed upon consumption of the substrate. The structure of MOGE was confirmed using nuclear magnetic resonance spectroscopy and only the isomer of 2-MOGE was formed, indicating that CAL-B has complete α- regiospecificity. During ethanolysis, 3-MOGE was formed via acyl migration. These results indicate that the formation of 1-alkyl glyceryl ethers is not due to the imperfect regiospecificity of CAL-B, but rather due to ethanolysis of the formed 3-MOGE. The ethanolysis rate at the 3-α-position of DOGE was faster and the rate of acyl transfer was slightly slower for chain lengths greater than 14. These results show for the first time that both deacylation at the 3-position and acyl migration from the 2- to 3-position are affected by the structure of 1-position.

A comprehensive review on transethosomes as a novel vesicular approach for drug delivery through transdermal route.

Drug delivery through transdermal route is one of the effective methods for the application of drugs. It overcomes many drawbacks which are encountered with the oral route. Moreover, many drugs are not able to pass through the stratum corneum, which is the main barrier for the transdermal drug delivery. Formation of ultra-deformable vesicles (UDVs) is a novel technique for the transdermal applications of the drugs. Transethosomes (TEs), ethosomes, and transferosomes are all part of the UDV. Because of the presence of increased concentrations of ethanol, phospholipids, and edge activators, TEs provide improved drug permeation through the stratum corneum. Because of the elasticity of TEs, drug penetration into the deeper layer of skin also increases. TEs can be prepared using a variety of techniques, including the cold method, hot method, thin film hydration method, and the ethanol injection method. It increases patient adherence and compliance because it is a non-invasive procedure of administering drugs. Characterization of the TEs includes pH determination, size and shape, zeta potential, particle size determination, transition temperature, drug content, vesicle stability, and skin permeation studies. These vesicular systems can be utilized to deliver a variety of medications transdermally, including analgesics, antibiotics, antivirals, and anticancer and arthritis medications. This review aims to describe vesicular approaches that had been used to overcome the barrier for the transdermal delivery of drug and also describes brief composition, method of preparation, characterization tests, mechanism of penetration of TEs, as well as highlighted various applications of TEs in medicine.

Phytochemical compounds with promising biological activities from Ascophyllum nodosum extracts using microwave-assisted extraction.

Phytochemical-rich antioxidant extracts were obtained from Ascophyllum nodosum (AN) using microwave-assisted extraction (MAE). Critical extraction factors such as time, pressure, and ethanol concentration were optimized by response surface methodology with a circumscribed central composite design. Under the optimal MAE conditions (3 min, 10.4 bar, 46.8 % ethanol), the maximum recovery of phytochemical compounds (polyphenols and fucoxanthin) with improved antioxidant activity from AN was obtained. In addition, the optimized AN extract showed significant biological activities as it was able to scavenge reactive oxygen and nitrogen species, inhibit central nervous system-related enzymes, and exhibit cytotoxic activity against different cancer cell lines. In addition, the optimized AN extract showed antimicrobial, and anti-quorum sensing activities, indicating that this extract could offer direct and indirect protection against infection by pathogenic microorganisms. This work demonstrated that the sustainably obtained AN extract could be an emerging, non-toxic, and natural ingredient with potential to be included in different applications.

Anti-oxidative, anti-apoptotic, and anti-inflammatory activities of Connarus semidecandrus Jack ethanol extract in UVB-irradiated human keratinocytes.

ETHNOPHARMACOLOGICAL RELEVANCE: Connarus semidecandrus Jack (Family: connaraceae) is a medicinal plant known for its wide distribution throughout Southeast Asia. Renowned for its diverse therapeutic properties, it has been traditionally used for treating fever, skin irritation, and colic. AIM OF THE STUDY: Numerous individuals suffer from skin issues, including wrinkles, hyperpigmentation, and inflammation, due to environmental factors. Although many drugs are available to treat skin problems, chemical drugs have many shortcomings and side effects. Therefore, natural products are attractive potential medicines for alleviating skin troubles. We recently showed that Connarus semidecandrus Jack ethanol extract (Cs-EE) has anti-alopecia potential. This paper aims to explore the potential skin-protective effects and underlying molecular mechanisms of Connarus semidecandrus Jack in UVB-induced human keratinocytes (HaCaT). MATERIALS AND METHODS: Before utilization, Cs-EE was dissolved in dimethyl sulfoxide (DMSO) and was preserved at a temperature of -20 °C. The phytochemical constituents of Cs-EE were detected by gas chromatography-mass spectrometry analysis (GC-MS). Sequentially, HaCaT cells were exposed to varying concentrations of Cs-EE prior to ultraviolet B (UVB) irradiation. Evaluations of cellular responses in HaCaT cells, including assessments of cell viability, deoxyribonucleic acid (DNA) damage, and gene and protein expressions, were carried out. To explore the specific signaling pathway involved, we conducted a luciferase assay in addition to validating these pathways using Western blot analysis. RESULTS: Nitric oxide (NO) and intracellular reactive oxygen species were decreased. Melanin production through the activation of melanocytes by α-melanocyte-stimulating hormone (MSH) was also inhibited by Cs-EE. Furthermore, the mRNA expression levels of key factors such as cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), interleukin 6 (IL-6), MMP-1, MMP-3, and MMP-9 exhibited a remarkable decrease. In addition, the phosphorylation of TAK1 within the signaling cascade exhibited a decline, and the activities of the transcription factor AP-1 were decreased according to a luciferase reporter assay. CONCLUSIONS: Taken together, these findings suggest that the anti-inflammatory, anti-aging, and anti-apoptotic effects of Cs-EE indicate the compound's potential usefulness as a natural component in pharmaceutical and cosmetic products.