Ethyl Acetate Extract Research Articles

LC-MS/MS Profiling, Biological Activities and Molecular Docking Studiesof Simmondsia Chinensis Leaves.

This study aimed to assess the biological activities of Tunisian Simmondsia chinensis and characterize their potential bioactive compounds. Different extracts of S. chinensis were tested for their antioxidant, antibacterial, anti α-amylase, and anti-acetylcholinesterase activities through in vitro assays. The methanolic extract exhibited the highest levels of antioxidant activity and total phenolic content (976.03 GAE/g extract) compared to the other extracts. Additionally, it demonstrated a substantial anti-acetylcholinesterase activity (PI= 75%) and potent antibacterial property, particularly against Enterococcus faecalis, Listeria monocytogenes, Bacillus cereus, Bacillus subtilis, and Salmonella enterica. The IC50 values of ethyl acetate and methanolic extracts against α-amylase were 42 μg/mL and 40 μg/mL, respectively, indicating potent anti-diabetic effects. HPLC-ESI-MS/MS analyses identified flavonoids and lignans as the major phenolic compounds in the methanolic extract. To better comprehend the mechanisms behind inhibitory effects on α-amylase and acetylcholinesterase enzymes, a molecular docking study was conducted. Consequently, these findings indicate that S. chinensis is a highly valuable natural resource with potential industrial applications.

GC-MS/HPLC Profiling and Sono-maceration Mediated Extraction of Osbeckia parvifolia Polyphenols: In Silico and In Vitro Analysis on Anti-Proliferative activity in Ovarian Cancer Cell Lines.

Osbeckia parvifolia, an endemic edible plant of Western Ghats, was investigated in the present study for its polyphenolic compounds, including content, constituents, extraction through an ultrasonic-assisted maceration technique and therapeutic potential in biomedical applications. The methanolic extract (OPM) exhibited an IC50 value of 1.25 µg/mL against 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radicals. Furthermore, the ethyl acetate and methanolic extracts also strongly inhibited 5-lipoxygenase, especially OPM (84.93%), which was comparable to standard curcumin. OPM also elicited cytotoxicity in SKOV3 ovarian cancer cells (93.80%), surpassing paclitaxel. Bio-accessibility analysis demonstrated that the release of phenolic compounds and antioxidant potential were very high (above 100%), revealing the possibility of synergistic efficacy of polyphenolic complexes in drug development. Gas Chromatography -Mass Spectrometry (GC-MS) analysis revealed 22 bioactive polyphenolic compounds in OPM, such as epicatechin, quercetin, and psoralidin. This was confirmed by High Performance Liquid Chromatography (HPLC) and High-Pressure Thin Layer Chromatography (HPTLC) analyses, which revealed a high quantity of catechin (37.45 mg/g). Molecular docking revealed the significant binding affinity of these proteins for the ovarian oncoproteins PI3K (-8.52 kcal/mol) and Casp-8 (-8.41 kcal/mol). Adsorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) profiling indicated the favorable pharmacokinetic properties of these compounds, supporting their candidacy in drug formulations against ovarian cancer.

2,4-Di-Tert-Butylphenol of Streptomyces luridiscabiei MMS-10 Inhibits Biofilm Forming Cariogenic Streptococcus mutans ULSP-2.

Dental caries is a common chronic infectious disease of the oral cavity that affects the overall oral health of the individual. Cariogenic bacteria have long been recognized for their role in developing chronic dental infections. Drug-resistant bacteria represent a global challenge to effective pathogen control in caries. The present study aimed to isolate and identify soil actinomycetes for their antibacterial and anti-biofilm activities against antibiotic-resistant and biofilm-forming cariogenic bacteria. Thirteen caries bacteria isolated from infected tooth samples were evaluated for antibiotic resistance and biofilm formation. The isolate ULSP-2 showed the highest antibiotic resistance score (0.714) and was found to be a strong biofilm producer when tested by congo red agar and microtiter plate assays. The bacterium was identified as Streptococcus mutans based on morphological, biochemical, and molecular characterization. The effect of ethyl acetate extracts from 20 soil actinomycetes on the growth and biofilm formation ability of S. mutans was evaluated. The MMS-10 extract strongly inhibited growth (18.5 ± 0.5mm) and biofilm formation (56.46 ± 0.32%) of S. mutans at 100µg/mL. The isolate MMS-10 was identified at the molecular level as Streptomyces luridiscabiei. Based on FTIR, NMR, and GC-MS analysis, the purified MMS-10 extract was characterized and identified as 2,4-Di-tert-butylphenol. The metabolite's physiological, physicochemical, and pharmacokinetic properties were analyzed using the Swiss ADME web server and found to satisfy the criteria of drug-likenessof a molecule. The study revealed the significance of soil actinomycetes in controlling growth and biofilm formation in cariogenic S. mutans.

Antifungal Potential of Struchium sparganophora (Antsbush): A Promising Candidate for Treating Candidiasis and Cryptococcosis

Aims: The incidence of Candidiasis and Cryptococcosis, and the emergence of acquired antifungal resistance have increased rapidly. This study aimed to evaluate the effectiveness of S. sparganophora leaf extracts against C. albicans and C. neoformans; and to determine whether there was any difference between the antifungal effects of S. sparganophora leaf extracts and two conventional antifungal agents (AFAs). Study Design: Experiment-based study. Place and Duration of Study: S. sparganophora leaves was obtained from a site in Kimbia, Berbice River, Guyana; identified by the Biodiversity Centre and tested at the Main Laboratory at the College of Medical Sciences, University of Guyana during January- August 2023. Methodology: Dried pulverised leaves were macerated using different solvents and concentrated using a rotary evaporator. Sterile filter paper discs were soaked in different concentrations of the various extracts. Antifungal discs were placed on Sabouraud’s Dextrose Agar plates seeded with fungi. All plates were incubated and zones of inhibitions (ZOIs) were measured and expressed as mean ± SD. Results: S. sparganophora leaf extracts showed large ZOI especially at the 100 mg/ml concentrations against all organisms tested. The largest ZOI was seen for the hexane extract against C. neoformans (35.5±5 mm) and C. Albicans In-House B (18.5±3.5 mm) at 100 mg/ml concentrations. No ZOI was observed against the AFA fluconazole by C. albicans In-House B, while large ZOI were observed with the hexane and ethyl acetate extracts at 100 mg/ml concentrations. Statistical analysis showed correlation between the ZOI and concentrations, ZOI and solvent extract, and ZOI and type of fungi. Conclusion: In conclusion, S. sparganophora leaf extracts have great antifungal activity and in some cases showed greater activity when compared to conventional AFAs.

Centaurea dimorpha Viv. (Asteraceae) growing in Algeria extracts as a promising natural cosmetic active ingredient: Broad-spectrum photoprotection and antioxidant efficacy

Recently, plants have been considered as a valuable natural source of cosmetic active ingredientsowing to their sustainability and weak toxicity. Thus, this study was conducted to investigate the cosmetic efficacy of Centaurea dimorpha Viv (Asteraceae), an endemic species of North Africa, as a promising natural cosmetic active ingredient. In the present study, Ethyl acetate and Butanolic extracts obtained from powdered Centaurea dimorpha aerial parts were investigated for their phenolic and flavonoid contents, which were evaluatedvia Folin-ciocalteu reagent and aluminium chloride methods, the in vitro antioxidant potential was evaluated by DPPH radical scavenging,phosphomolybdenum and phenanthroline assays, the UVB and broad spectrum protective efficacy was spectrophotometrically assessed by measuring SPF, UVA/UVB ratio and critical wavelength (CW) indices. The highest levels of TPC and TFCwere recorded by the ethyl-acetate extract (119.20 ± 0.32 µg GAE mg-1, 50.65 ± 0.43 µg QEmg-1, respectively). Similarly, this extract displayed a significant antioxidant effect, particularly in the phenanthroline assay (152.63 ± 0.49 µg AAEmg-1). Ethyl acetate extract also showed UVB and broad-spectrum (UVB-UVA) protective efficacy (SPF=12.30 ± 0.001, UVA/UVB ratio=0.63 ± 0.001, λc= 371). The results obtained show the possibility to use Ethyl acetate extract as a promising active ingredient for sunscreen formulations.

Epicatechin Isolated from Litchi chinensis Sonn. (Litchi) Fruit Peel Ethyl Acetate Extract Modulated Glucose Uptake in Chang Cells and Suppressed ROS Production in RAW 264.7 Macrophages.

Bioactive flavonoid epicatechin has been reported in the peel of litchi fruit but isolated from its hydroalcoholic extracts. This study isolated epicatechin with cellular glucose uptake modulatory and ROS production inhibitory properties from the ethyl acetate (EtOAc) extract using a bioassay-guided approach. The fruit peel was defatted with hexane and sequentially extracted using dichloromethane (DCM), EtOAc, methanol (MeOH) and water. In vitro phytochemical models, namely antioxidant (Fe3+ reducing, radical scavenging and anti-linoleic acid peroxidative) and glycaemic control (α-glucosidase and α-amylase inhibitory and glucose uptake modulatory), were employed for the bioassay-guided isolation, while the isolated compound was characterised using NMR and mass spectrometry and assessed for dose-dependent inhibition of α-glucosidase and lipopolysaccharide (LPS)-induced cellular ROS production, as well as modulation of cellular glucose uptake. Relative to the other extracts, the EtOAc extract had appreciable phenol and flavonoid contents, which perhaps influenced its potent anti-lipid peroxidative (65.0%) and α-glucosidase inhibitory (52.4%) effects. The α-glucosidase inhibitory potency of the fractions (1-8) from the EtOAc extracts correlated with their flavonoid contents, with fraction 5 outperforming other fractions. The fraction comprised a pool of fractions obtained from the DCM:MeOH:water (7:3:0.281 v/v/v) solvent system. LC-MS revealed the predominant presence of epicatechin in fraction 5, which was later isolated from one of the sub-fractions (sub-fraction 4) of fraction 5. This sub-fraction had stronger anti-lipid peroxidative (65.5%), α-glucosidase inhibitory (65.8%) and glucose uptake modulatory (38.2%) effects than the other sub-fractions from fraction 5, which could have been influenced by the isolated epicatechin. Moreover, the isolated epicatechin inhibited α-glucosidase (IC50 = 35.3 µM), modulated cellular glucose uptake (EC50 = 78.5 µM) and inhibited LPS-induced ROS production in RAW 264.7 macrophages in a dose-dependent fashion [IC50 = 18.9 µM; statistically comparable (p > 0.05) to ascorbic acid, IC50 = 9.57 µM]. Epicatechin from litchi peel EtOAc extract could potentiate glucose uptake modulatory, α-glucosidase inhibitory and ROS suppressive capacities, which could be influential in the use of litchi fruit peel for managing diabetes and associated oxidative damage.

Enhanced Biological Potential and Phytochemical Profiling of Phoenix Dactylifera Leaves (Deglet Nour and Alig) by Kombucha Fermentation: Focus on Polyphenols, Antioxidant, Antidiabetic, and Cytotoxic Activities.

The date palm, scientifically known as Phoenix dactylifera, is an important cultural and economic source of wealth in southern Tunisia. It produces considerable agricultural waste, including palm leaves, the disposal of which is often a challenge. Our study addresses the sustainable conversion of date palm leaves into a valuable product through kombucha fermentation, focusing on two widely used varieties in Tunisia: Deglet Nour and Alig. HPLC-RI analysis showed a significant difference in the fermentation process between the treated samples, which is reflected in the highest sugar consumption and metabolite production in Alig palm. Unfermented and fermented date palm leaves were sequentially extracted with solvents of increasing polarity to evaluate their chemical composition and bioactivity. The results showed that kombucha fermentation significantly increased the total phenolic content, with the highest amounts in the ethyl acetate fraction. In terms of antioxidant activity, the ethyl acetate extracts showed a high percentage inhibitory activity (82.76%) against the DPPH radical found in fermented Palm Alig, which also exhibited the most important antidiabetic capacity (resulting in an IC50 value of 20 µg/mL). The chemical analyses resulted in the detection of 19 compounds by HPLC-DAD and 50 volatiles by GC-MS, which are mainly found in kombucha extracts.

HPLC analysis and antimicrobial activity of Vitex altissima leaves extracts

The exploration of ethnomedicinal plants for phytochemical and pharmacological properties is crucial for developing novel therapeutics for chronic diseases. Vitex altissima, known as the Peacock chaste tree, is a significant member of the Verbenaceae family, is widely utilized in traditional medicine. This study investigates the phytochemical composition and antibacterial properties of V. altissima, a plant recognized for its medicinal use by various indigenous communities, including the Malayali tribes of Servarayan hills. The study involved extracting phytochemicals from the leaves of V. altissima using hexane, ethyl acetate and methanol through soxhlet extraction. The extracts were analyzed for secondary metabolites, including carbohydrates, proteins, amino acids, steroids, glycosides, alkaloids, tannins, phenolics, flavonoids, terpenoids, saponins, anthraquinones, oils and resins, diterpenes, phlobatannins and coumarins. Quantitative assessments of phenolic compounds, flavonoids and alkaloids were performed. Column chromatography was employed to fractionate the methanolic extract, resulting in 12 distinct fractions. These fractions were screened for antibacterial activity against E. coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Streptococcus mutans and Staphylococcus aureus using the agar well diffusion method. The minimal inhibitory concentration (MIC) was determined through a 2-fold serial dilution technique. High-performance liquid chromatography (HPLC) was utilized to identify the polyphenolic compounds responsible for antibacterial activity. Phytochemical screening revealed a diverse array of bioactive compounds in the extracts, with methanol extracts showing the highest total phenolic content (218 ± 7.21 mg GAE/g of extract) and significant antibacterial activity. The ethyl acetate extract exhibited the highest total flavonoid content (40.67 ± 6.65 mg QE/g of extract). Among the fractions, the column fraction from the chloroform-methanol gradient (VACF) demonstrated superior antimicrobial activity, particularly against S. mutans and P. aureginosa. The MIC values for VACF were 427 µg/mL for P. aeruginosa and 400 µg/mL for S. aureus, indicating potent antibacterial properties. HPLC analysis identified key polyphenolic compounds, including p-coumaric acid, ferulic acid and elagic acid, as the primary contributors to the antibacterial activity. The presence of these compounds aligns with the observed antimicrobial efficacy and highlights the potential of V. altissima extracts as a source of natural antibacterial agents.

A combined in vitro , in silico and Polyphenolic Profile of stem extracts of Juncus maritimus (Juncaceae) harvested from eastern Algeria as potential anti-inflammatory and antioxidant agents.

The extremophilic species Juncus maritimus known for its medicinal virtues was collected in the Biskra region with the aim of its valorization. The volume size of polyphenols, flavonoids and condensed tannins was carried out by Folin-Ciocalteu methods, aluminum trichloride and vanillin respectively. Polyphenols volume is 127.73±0.20 μg EAG/mg ES, flavonoids 16.42±0.42 μg EQ/mg ES and condensed tannins 10.10±0.35 μg EC/mg ES. The result of antioxidant activity tested by employing DPPH and ABTS methods reveal that the ethyl acetate extract had the highest activity in both tests. The result of in vitro anti-inflammatory activity, by the BSA protein denaturation test, showed that the percentage inhibition of denaturation is proportional to the concentration of the extract. At a concentration of 5 mg/mL, the percentage inhibition of the extract was close to that an anti-inflammatory drug Diclofenac with 82.03 and 80.23% respectively. Furthermore, molecular docking simulations revealed that Berberine was shown high binding affinity with the COX-2 and PLA-2 targets. Indeed, bioisosteric replacement is applied to discover novel analogs of Berberine. Finally, ADME-Tox prediction demonstrated that this compound and its analogs are without Hepatotoxicity. The results might be selecting that Berberine and its analogs as active compound with anti-inflammatory and antioxidant activities.

Biodiversity and Bioprospecting of Fungal Endophytes from Houttuynia cordata Thunb. as a Potential Antibacterial and Anticancer Agent.

Endophytic fungi are considered a new source of bioactive compounds that have important applications in agriculture and medicine. This study aims to investigate the biodiversity and potential of endophytic fungi isolated from Houttuynia cordata Thunb. as antimicrobials and anticancer agents. Out of ten isolated endophytes, four species have never been reported to be associated with H. cordata: Ceratobasidium sp., Cladosporium sp., Phomopsis sp., and Fusarium sp. The antibacterial activity assay revealed that the ethyl acetate extract of Ceratobasidium sp. HCS-3 possessed most potent antibacterial activity against Escherichia coli and Staphylococcus aureus. In addition, its cytotoxic activity test showed the promising anticancer activity on lung cancer A549, osteosarcoma MG-63, and cervical cancer HeLa cells with IC50 of 4.55 ±1.16, 32.14 ±2.78, and 1.54 ±0.66 ppm, respectively. Furthermore, metabolite profiling identified 66 compounds suggesting that benzoic acid, farnesol, and cyclopeptides may contribute to the antibacterial activity, while 4-methoxycinnamic acid may have anticancer potential.

Antibacterial and anticancer potential of bioactive compounds and secondary metabolites of endophytic fungi isolated from Anethum graveolens.

Fungal endophytes are known to produce bioactive chemicals and secondary metabolites that are often identical to those produced by their host plants. The main objective of the current study was to isolate and identify endophytic fungi associated with the medicinal plant Anethum graveolens, and to investigate their potential antibacterial and anticancer properties. The ethyl acetate extracts from the isolated endophytic fungi, as well as the host plant A. graveolens, were subjected to bioactivity assays to evaluate their antibacterial and anticancer potential against multi-drug resistant bacterial strains and the human hepatocellular carcinoma cell line HepG2. The endophytic fungi isolated and identified from the A. graveolens samples included Diaporthe, Auxarthron, Arthrinium, Aspergillus, Microsporum, Dothiorella, Trichophyton, Lophiostoma, Penicillium, and Trichoderma species. The minimum inhibitory concentration (MIC) assay revealed that the A. graveolens extract exhibited the strongest antibacterial activity, with an MIC value of 4 μg/ml, followed by the Trichoderma sp. (5 μg/ml) and Penicillium sp. (6 μg/ml) extracts. Additionally, the crude extracts of Trichoderma sp., Penicillium sp., and Fusarium sp. demonstrated high anticancer activity against HepG2 cells, with inhibition rates ranging from 89 to 92% at a concentration of 50 μg/ml. Interestingly, the A. graveolens extract showed the most potent anticancer activity, with a 95% inhibition rate against HepG2 cells at the same concentration. These findings highlight the significant potential of endophytic fungi associated with A. graveolens, as a source of bioactive compounds with promising antibacterial and anticancer properties. The results reinforce the hypothesis that medicinal plants and their endophytic fungi can serve as an attractive alternative for the development of novel therapeutic agents, potentially offering a more sustainable and less harmful approach to disease management compared to traditional chemical-based methods.

New acid anhydride from Phalaris canariensis with antimicrobial activity assessed through in vitro and in silico approaches

In this study, a novel fatty acid anhydride, named phalarisin 1, was successfully isolated from the ethyl acetate extract of Phalaris canariensis growing in Tunisia. The structural characterisation of the compound was achieved through various spectroscopic techniques including FT-IR, 1D and 2D-NMR spectroscopy, as well as acidic hydrolysis analyses. Remarkably, phalarisin exhibited potent antimicrobial properties against a range of pathogens including Micrococcus luteus, Bacillus subtilis, Fusarium oxysporum, and Fusarium phylophylum, with minimum inhibitory concentrations (MICs) ranging from 31.25 to 62.5 μg/mL. To grasp the antimicrobial potential of compound 1, molecular docking studies were performed and they furnished evidence indicating its ability to bind to proteins in bacteria and fungi that are pivotal for drug resistance.

Qualitative and GC-MS analysis of medicinally potent aquatic herb Pistia stratiotes L. Assam, India

Pistia stratiotes L. belongs to Araceae family, is a free-floating aquatic plant found in rivers, lakes, and ponds It is commonly known as water cabbage or water lettuce. P. stratiotes stands out as a prominent Ayurvedic remedy, extensively utilized over time for treating a multitude of ailments, The present study was aimed to carry out the detailed preliminary phytochemical and GC-MS analysis of the leaves and root of P. stratiotes. The preliminary phytochemical analysis of P. stratiotes indicated the presence of alkaloids, carbohydrades, reducing sugars, glycosides, flavonoids, phenolic, tannins, triterpinoids, saponins, proteins and amino acids. GC-MS analysis was also carried out to detect the phytoconstituents present in the methanolic, hexane and ethylacetate extract of leaves and root of P. stratiotes.

Integrated lipidomic and transcriptomics to explore the effects of ethyl acetate extract of Herpetospermum pedunculosum on nonalcoholic fatty liver disease in mice

Ethnopharmacological relevanceHerpetospermum pedunculosum (Ser.) C.B. Clarke (HP), a traditional Tibetan medicine used to treat hepatobiliary diseases, was confirmed that lignans-enriched ethyl acetate extract of HP (EAHP) could alleviate the hepatic injury by modern pharmacological evidence. However, the effects and potential mechanisms of EAHP against nonalcoholic fatty liver disease (NAFLD) are still unknown. Aim of the studyTo reveal the effects of EAHP on NAFLD and explore the potential mechanisms from the perspective of lipidomics and transcriptomics. Materials and methodsUPLC‒Q–TOF‒MS analysis was carried out to investigate the chemical components of EAHP. A Choline-deficient, L-amino acid defined, high fat diet (CDAHFD) was used to establish a NAFLD mouse model. The anti-NAFLD effects of various dosages of EAHP were evaluated by biochemical indexes and histological analysis. Hepatic lipidomic and transcriptomic analysis and multiple bioinformatics methods were used to screen biomarkers and signaling pathways. The levels of the corresponding genes were verified by qPCR. Results36 kinds of compounds were identified by UPLC‒Q–TOF‒MS analysis. Oral treatment with EAHP significantly decrease the liver index and the levels of ALT and AST in the serum. The measurements lipid content and Oil Red O staining results suggested that EAHP ameliorated lipid metabolism disorders by reducing the content of TG and LDL-C, increasing HDL-C in the liver. H&E staining and ELISA revealed that EAHP restored hepatic inflammatory infiltration and decrease the levels of IL-1β, IL-6, TNF-α, and increase IL-10 in the serum. Lipidomic analysis showed that EAHP could regulate CDAHFD-induced lipid metabolic disorder. The different lipid metabolites included TG, phosphatidyl choline (PC), diacylglycerol (DG), phosphatidylethanolamine (PE), phosphatidylinositol (PI), ceramide (Cer). Transcriptomic analysis revealed that Bmp8b, Nbl1, Rgma, Sphk1, Thbs1, and Ugt8a were important regulators, which were associated with TGF-β signaling pathway and sphingolipid metabolism. The expressions of above genes detected by were qPCR consistent with transcriptomic data. ConclusionsThe ameliorative effects of EAHP on NAFLD are potentially attributable to the regulation of sphingolipid metabolism and TGF-β signaling pathway, etc., which results in abnormal hepatic lipid metabolism and inflammatory response.

Determination of Phenolic and Flavonoid Total Levels and Antioxidant Activity of Ethanol, Ethyl Acetate, and n-Hexane Extracts of Citrus reticulata Blanco Fruit Peel by DPPH and ABTS Methods

Determination of Phenolic and Flavonoid Total Levels and Antioxidant Activity of Ethanol, Ethyl Acetate, and n-Hexane Extracts of Citrus reticulata Blanco Fruit Peel by DPPH and ABTS Methods

Investigation of bioactive metabolites produced by the endophytic fungus Aspergillus iranicus from Houttuynia cordata Thunb

The endophytic fungus Aspergillus iranicus, capable of producing bioactive substances, was isolated from the roots of Houttuynia cordata Thunb. Through chromatographic methods, five compounds were isolated in this study for the first time from the fermentation broth and mycelia of the endophytic fungus Aspergillus iranicus obtained from Houttuynia cordata Thunb. using ethyl acetate extracts. These compounds were identified as palmitic acid (1), protocatechuic acid (2), 4-hydroxybenzophenone (3), stigmasterol (4), and β-sitosterol (5). The IC50 values for compound 2 was 1.32 mg/mL, which indicate strong DPPH radical scavenging activity. Compounds 2, 3, and 5 significantly inhibited the growth of Escherichia coli, demonstrating MIC values of 6.25, 3.13, and 3.13 mg/mL, respectively. Additionally, displaying a MIC value of 0.78 mg/mL, compound 3 demonstrated remarkable inhibition against Candida albicans growth. These findings suggest the presence of endophytic fungi in H. cordata, producing several valuable medicinal secondary metabolites.

The Impact of Amphimedon chloros Ethyl Acetate Extract on MDA-MB-231 Cell Lines' Expression of Bax, Cyclin D, Caspase 3, P21, C-myc, and Bcl2: Mechanism of inhibition of the Growth of Cancer Cells

The Impact of Amphimedon chloros Ethyl Acetate Extract on MDA-MB-231 Cell Lines' Expression of Bax, Cyclin D, Caspase 3, P21, C-myc, and Bcl2: Mechanism of inhibition of the Growth of Cancer Cells

From agricultural waste to value: Integrated chemo and biocatalytic biorefinery processes to produce 2-furoic acid

The integration of biocatalysis in biorefineries can lead to synergies for raw material valorization. Enzymes must perform efficient and selective reactions when using crude effluents (to avoid costly downstream units). Herein, this is showcased with the synthesis of 2-furoic acid, starting from rice husk (agricultural waste), via a sequential organic-acid catalyzed pretreatment – to afford xylose and cellulose and lignin –, followed by the microwave-assisted acidic xylose dehydration to furfural, in situ extraction in ethyl acetate, and the final biocatalytic selective oxidation of furfural to 2-furoic acid (2-FA). To validate the concept, a xylose-rich hydrolysate (∼ 15 g xylose L−1) obtained from rice husk (RH) was used, achieving a furfural yield of 70 % in a biphasic system (water – ethyl acetate). The obtained furfural extracted in the ethyl acetate was subsequently oxidized to 2-furoic acid via an organic peroxide reaction mediated by Candida antarctica lipase B (CALB), with an overall yield of 90 %, and, with a yield of 41.72 % based on the initial xylose in biomass. Notably, 20 mg/mL CALB could tolerate up to 400 mM of furfural under optimum conditions of 40 °C, 48 h. The recyclability of the biocatalyst was investigated, enabling an efficient reuse of four consecutive cycles.

Aqueous Extract of Rhubarb Promotes Hepatotoxicity via Facilitating PKM2-Mediated Aerobic Glycolysis in a Rat Model of Diethylnitrosamine-Induced Liver Cancer.

To identify the polar parts in Rhubarb that cause hepatotoxicity and explore the underlying mechanisms. The rat model of liver cancer was established by gavage of diethylnitrosamine (DEN; 0.002 g/rat) for 14weeks. Starting from the 11th week, Rhubarb granule (4 g/kg), aqueous, ethyl acetate and n-butanol extract of Rhubarb or Rhein equivalent to a dose of 4 g/kg Rhubarb granule were administered intragastrically for 4 consecutive weeks. Liver tissues from rats treated with DEN and Rhubarb granules were used for non-targeted metabolomics analysis. The correlation between pyruvate kinase isozyme type M2 (PKM2) expression level and the progress and prognosis of hepatocellular carcinoma (HCC) was evaluated through bioinformatics analysis based on TCGA database. Liver tissues and blood samples from rats treated with DEN and aqueous, ethyl acetate and n-butanol extract of Rhubarb were used for the screening of hepatotoxic polar parts of Rhubarb. The liver injuries were evaluated by the changes in pathology, liver function, and the expression levels of proliferating cell nuclear antigen (PCNA) and transforming growth factor beta1 (TGF-β1). The mechanism studies focus on PKM2 expression, and the metabolic reprogramming via detecting the activities of lactate dehydrogenase A (LDHA) and isocitrate dehydrogenase (ICDH). Furthermore, molecular docking analysis was performed to validate the target interaction between Rhein and PKM2, and the hepatotoxicity of Rhein was evaluated by testing liver function in the DEN-induced liver cancer model. The non-targeted metabolomics analysis revealed that Rhubarb promoted aerobic glycolysis in the rat model of DEN-induced liver cancer. And bioinformatics analysis revealed that high PKM2 expression was closely related to the progression and poor prognosis of HCC. In vivo studies indicated that the aqueous extract of Rhubarb, but not ethyl acetate and n-butanol extract, promoted the liver injuries induced by DEN. The mechanism study showed that the aqueous extract of Rhubarb increased the expression of PKM2 and promoted aerobic glycolysis. Moreover, Rhein had a strong binding affinity for PKM2 and aggravated liver injury in the DEN-induced liver cancer model. Aqueous extract of Rhubarb promoted hepatotoxicity via facilitating PKM2-mediated aerobic glycolysis in the rat model of DEN-induced liver cancer.

Formulation and evaluation of physical stability and antidiabetic activity from nanoliposomes containing an ethyl acetate extract of Solanum xanthocarpum Schrader & Wendland fruit in rats

Introduction: The extract of Solanum xanthocarpum fruit has antidiabetic activity. This research aims to formulate nanoliposomes containing ethyl acetate extracts of S. xanthocarpum selected from multilevel extraction, evaluate their physical stability and antidiabetic activity, and compare them with the extract. Methods: The extracts were prepared using n-hexane, ethyl acetate, ethanol, and water as solvents, and their antidiabetic activities were evaluated to select the extract most effective in lowering blood sugar levels in rats. That extract was formulated into three nanoliposomes using varying amounts of phospholipid, cholesterol, and Span 60, i.e., F1 (40 mmol), F2 (50 mmol), and F3 (60 mmol). Various sonication times ranging from 10 to 30 minutes were evaluated for particle size, entrapment efficiency, and physical stability. The selected formulations were evaluated for antidiabetic activity. Results: The ethyl acetate extract showed the highest decrease in glucose in rats and was selected for nanoliposome formulation. The nanoliposomes obtained were physically stable at low temperatures for 12 weeks. F2 had the smallest particle size (143.97 nm) and the greatest entrapment efficiency (92.981% ± 0.35%) with a sonication time of 30 minutes and was significantly different from F1 and F3 (P<0.05). The highest percentage reduction in blood sugar levels was with F2 at 74.57% and significantly differed (P<0.05) from the ethyl acetate extract of S. xanthocarpum at 73.98% and the positive control rat group. Conclusion: The results show the potential uses of the prepared nanoparticles, especially the F2 formulation, as an antidiabetic formula.