luteolin-7-O-glucoside Research Articles

Cloning and Direct Evolution of a Novel 7-O-Glycosyltransferase from Cucurbita moschata and Its Application in the Efficient Biocatalytic Synthesis of Luteolin-7-O-glucoside.

Luteolin-7-O-glucoside(L7G), a glycosylation product of luteolin, is present in a variety of foods, vegetables, and medicinal herbs and is commonly used in dietary supplements due to its health benefits. Meanwhile, luteolin-7-O-glucoside is an indicator component for the quality control of honeysuckle in the pharmacopoeia. However, its low content in plants has hindered its use in animal pharmacological studies and clinical practice. In this study, a novel 7-O-glycosyltransferase CmGT from Cucurbita moschata was cloned, which could efficiently convert luteolin into luteolin-7-O-glucoside under optimal conditions (40 °C and pH 8.5). To further improve the catalytic efficiency of CmGT, a 3D structure of CmGT was constructed, and directed evolution was performed. The mutant CmGT-S16A-T80W was obtained by using alanine scanning and iterative saturation mutagenesis. This mutant exhibited a kcat/Km value of 772 s-1·M-1, which was 3.16-fold of the wild-type enzyme CmGT. Finally, by introducing a soluble tag and UDPG synthesis pathway, the strain BXC was able to convert 1.25 g/L of luteolin into 1.91 g/L of luteolin-7-O-glucoside under optimal conditions, achieving a molar conversion rate of 96% and a space-time yield of 27.08 mg/L/h. This study provides an efficient method for the biosynthesis of luteolin-7-O-glucoside, which holds broad application prospects in the food and pharmaceutical industry.

Multiplex Approach of Metabolomic and Transcriptomic Reveals the Biosynthetic Mechanism of Light-induced Flavonoids and CGA in Chrysanthemum

Light, as an important environmental signal for plant growth and development, has been reported to be involved in the metabolism of phenylpropane. However, the light-induced phenylpropane biosynthesis mechanism in Chrysanthemum morifolium Ramat., especially flavonoid and chlorogenic acid (CGA) metabolism, is not clear. In this study, we found the flower phenotype of chrysanthemum 'HangBaiJu' became lighter after bagging. Besides, the content of main active ingredients, such as Luteolin-7-O-glucoside (Lu-7-O-G), Diosmetin-7-O-glucoside (Di-7-O-G), Apigenin-7-O-glucoside, Apigenin and CGA, was significantly decreased. Comparative transcriptome analysis (pairwise comparison, WGCNA, and k-means clustering) revealed that the expression of structural genes, such as CmPAL, CmCHS1/2, CmF3’H, CmFNS and CmHQT, was notably declined under dark conditions. Meanwhile, ‘bridge proteins’ CmMYB3/6/16 and signal transduction factors CmBBX20/22.2/22.3 were identified as key regulatory factors in the light-mediated synthesis of flavonoids and CGA in chrysanthemum. Among that, CmBBX20 could promote the accumulation of flavonoids and CGA by directly binding to the G-box core sequences of downstream target genes based on transient overexpression and Y1H assays. Overall, the preliminary molecular mechanism of BBXs and MYBs coordinately regulating the accumulation of flavonoids and CGA in chrysanthemum under different light inductions has been clarified, which provided a theoretical basis for the molecular breeding and quality improvement of chrysanthemum.

Optimization of β-cyclodextrin based ultrasound-assisted extraction: A green strategy to enhance the extraction of bioactive compounds from taro leaf byproduct

The present study aims to develop a green and sustainable process for the effective extraction of phytochemicals bearing antioxidant potency from Colocasia esculenta L. leaves, the by-product of taro cultivation, using β-cyclodextrin (β-CD) as a green booster for polyphenol isolation, along with ultrasound irradiation. Process optimization based on response surface methodology demonstrated that the maximum total phenolic content (11.90 mg gallic acid equivalents g−1 sample), total flavonoid content (4.66 mg catechin equivalents g−1 sample), and antioxidant activity in terms of 2,2-diphenyl-1-picrylhydrazyl radical inhibition (80.70%) and ferric-reducing antioxidant power (85.39 μmol trolox equivalents g−1 sample) could be obtained by ultrasonication of leaves at 59.6 °C for 55.4 min using an ethanolic solution (50% v/v) of β-CD (15 mM) and a solvent-solid ratio of 25.4 mL g−1. The extract obtained with β-CD was significantly enriched in flavonoids and, in particular, flavone derivatives (mainly apigenin and luteolin glucosides). The outcomes of the present study suggest that the proposed extraction procedure can serve as a highly effective and green strategy for the recovery of taro leaf polyphenols opening new horizons in the valorization of underutilized by-products from food and pharmaceutical sector.

The Extract of Humulus japonicus Inhibits Lipogenesis and Promotes Lipolysis via PKA/p38 Signaling

Introduction: Previous research has shown that an aqueous extract of Humulus japonicus (EH) can ameliorate hypertension, nonalcoholic fatty liver disease, and oxidative stress in adipocytes by activating the thermogenic pathway. However, the effects of an ethanol (30%) extract of EH on obesity are unknown. Methods: Various protein expression levels in fully differentiated 3T3-L1 adipocytes were assessed by Western blotting. Lipid deposition in 3T3-L1 adipocytes was examined by oil red O staining. The MTT assay was used to evaluate adipocyte viability. Caspase 3 activity and glycerol release were determined using commercial assay kits. Results: In this study, we discovered that EH treatment inhibited lipogenesis and promoted lipolysis in both differentiated 3T3-L1 adipocytes and adipose tissue of mice fed a high-fat diet. EH treatment also increased phosphorylated protein kinase A (PKA) levels while reducing p38 phosphorylation. When H89, a PKA inhibitor, was used, the effects of EH on lipogenic lipid accumulation and lipolysis in 3T3-L1 adipocytes were eliminated. Treatment with luteolin 7-O-β-d-glucoside (LU), the major active compound in EH, also suppressed lipid deposition and p38 phosphorylation but enhanced lipolysis in 3T3-L1 adipocytes. These changes were abrogated by H89. Conclusion: These findings indicate that EH containing LU reduces lipogenesis and stimulates lipolysis via the PKA/p38 signaling pathway, leading to an improvement in obesity in mice. Therefore, our study suggested that EH could be a promising therapeutic agent for treating obesity.

Influence of Aspergillus parasiticus on aflatoxins production and quality change in Chrysanthemum morifolium at various storage conditions

SummaryIn this study, a full factorial design with three temperature levels (20, 30 and 40 °C), three moisture content (MC) levels (8%, 15% and 22%), and four storage times (7, 14, 21 and 28 days) was used to investigate the changes of aflatoxins (AFs), active constituents, and antioxidant activities in Hangbaiju (HBJ, Chrysanthemum morifolium) after simulated inoculation with Aspergillus parasiticus. The results showed that AFs could be produced in the range of 20~30 °C and 8~22% MC after mould infection, but both mould growth and AFs production were inhibited under the tested MC condition at 40 °C. The analysis of variance (anova) indicated that the temperature, time, interaction between the temperature and time, and interaction between MC and time had significant effects on the total aflatoxins (AFTOT) accumulation. Under 20 and 30 °C, AFTOT in inoculated HBJ usually increased with the increase of MC and storage time, while its active constituents and antioxidant activities decreased with the increase of AFTOT under corresponding storage conditions. Pearson correlation analysis suggested that relatively stronger negative correlations were observed between luteolin‐7‐O‐glucoside (LUT7G), total phenolic content (TPC), total flavonoid content (TFC), and AFTOT. Grey correlation analysis (GCA) showed that antioxidant activity was highly linked to the content of active constituents, and the characteristic flavonoid LUT7G exhibited the highest grey correlation degrees (GCDs) in the three antioxidant activities. The AFTOT reached the highest level (31.15 μg kg−1) after 28 days of storage at 30 °C and 22% MC; meanwhile, LUT7G, TPC and TFC decreased by 93.66%, 20.77% and 55.50%, respectively, and all the three antioxidant activities indicated more than 25% reduction. This is the first study about the changes and relationships of AFTOT, active constituents and bioactivities in the medicinal food influenced by A. parasiticus under different storage conditions. These results provide important references to prevent AFs production and quality control for HBJ and other medicinal foods influenced by A. parasiticus in storage strategy.

Cynaroside improved depressive-like behavior in CUMS mice by suppressing microglial inflammation and ferroptosis

Depression is a common mental health disorder, and in recent years, the incidence of various forms of depression has been on the rise. Most medications for depression are highly dependency-inducing and can lead to relapse upon discontinuation. Therefore, novel treatment modalities and therapeutic targets are urgently required. Traditional Chinese medicine (TCM) offers advantages in the treatment of depression owing to its multi-target, multi-dimensional approach that addresses the root cause of depression by regulating organ functions and balancing Yin and Yang, with minimal side effects. Cynaroside (CNS), an extract from the traditional Chinese herb honeysuckle, is a flavonoid compound with antioxidant properties. In this study, network pharmacology identified 44 potential targets of CNS associated with depression and several highly correlated inflammatory signaling pathways. CNS alleviated LPS-induced M1 polarization and the release of inflammatory factors in BV-2 cells. Transcriptomic analysis and validation revealed that CNS reduced inflammatory polarization, lipid peroxidation, and ferroptosis via the IRF1/SLC7A11/GPX4 signaling pathway. In vivo experiments showed that CNS treatment had effects similar to those of fluoxetine (FLX). It effectively ameliorated anxiety-, despair-, and anhedonia-like states in chronic unpredictable mild stress (CUMS)-induced mice and reduced microglial activation in the hippocampus. Thus, we conclude that CNS exerts its therapeutic effect on depression by inhibiting microglial cells from polarizing into the M1 phenotype and reducing inflammation and ferroptosis levels. This study provides further evidence that CNS is a potential antidepressant, offering new avenues for the treatment of depression.

Antiobesity and antidiabetes effects of Cyperus rotundus rhizomes presenting protein tyrosine phosphatase, dipeptidyl peptidase 4, metabolic enzymes, stress oxidant and inflammation inhibitory potential

Diabetes is a significant global health concern that increases the vulnerability to various chronic illnesses. In view of this issue, the current research aimed to examine the effects of administering an extract derived from the tubers of Cyperus rotundus L (CrE) on obesity, type 1 diabetes, and liver-kidney toxicity. Through the utilization of HPLC-DAD analysis, it was discovered that the extract contained several components, including quercetin (47.8%), luteolin glucoside (17%), luteolin (7.56%), apigenin-7-glucoside (6.29%), naringinin (4.52%), and seven others. In vitro experiments they have demonstrated that CrE effectively inhibited key digestive enzymes associated with obesity and type 2 diabetes, such as DPP-4, PTP1B, lipase, and α-amylase, as evidenced by their respective IC50 values are about 23, 51,83, and 67 μg/ml respectively. Furthermore, when diabetic rats were administered CrE, the activity of pancreatic enzymes linked to inflammation, namely 5-lipoxygenase (5-LO), hyaluronidase (HAase), and myeloperoxidase (MPO), was significantly suppressed by 48, 41, 75, and 47%, respectively. Moreover, CrE exhibited protective effects on pancreatic β-cells by inhibiting the formation of thiobarbituric acid reactive substances (TBARS) by 65% and the induction of superoxide Dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) activities by 62, 108, and 112% respectively as compared to diabetic untreated rat. Additionally, CrE significantly inhibited the activities of intestinal, pancreatic, and serum lipase and α-amylase activities. In diabetic rats, CrE administration suppressed glycogen phosphorylase (GP) stimulated glycogen synthase (GS) activities by 45 and 30%; and this increased liver glycogen content by 45%. Furthermore, CrE modulated key hepatic enzymes involved in carbohydrate metabolism, including hexokinase (HK), glucose-6-phosphate dehydrogenase (G6PD), glucose-6-phosphatase (G6P), and fructose-1,6-bisphosphatase (FBP). Notably, the average food and water intake (AFI and AWI) of diabetic rats treated with CrE was reduced by 15 and 16% respectively as compared to those without any treatment. Therefore, this study demonstrated the effectiveness of Cyperus rotundus tubers in preventing and treating obesity and diabetes.

Interaction mechanism between luteoloside and corn silk glycans and the synergistic role in hypoglycemic activity

As the two most principal active substances in the corn silk, polysaccharides and flavonoids, the mechanism of interaction between them has been a topic of intense research. This study provides an in-depth investigation of the interaction mechanism between corn silk glycans and luteoloside (LUT) and the synergistic role that result from this interaction. The interaction mechanism was evaluated by isothermal titration calorimetry (ITC) and circular dichroism (CD), and the synergistic role was evaluated by the expression of glucose transporters (GLUT-1), insulin secretion and surface plasmon resonance (SPR). CD and ITC results indicated that the interaction between CSGs and LUT mainly driven by the Cotton effects, enthalpy and entropy-driven. This interaction precipitated the formation of complexes (CSGs/LUT complexes) between corn silk glycans (CSGs) with four different molecular weights and luteoloside (LUT). Furthermore, the CSGs and LUT play a synergistic role in glucose regulation through GLUT-1 expression and insulin secretion experiments, compared to single luteoloside group.Graphical

Integrated Metabolomics Approach Reveals the Dynamic Variations of Metabolites and Bioactivities in Paeonia ostii 'Feng Dan' Leaves during Development.

Paeonia ostii 'Feng Dan' is widely cultivated in China for its ornamental, medicinal, and edible properties. The whole plant of tree peony is rich in bioactive substances, while the comprehensive understanding of metabolites in the leaves is limited. In this study, an untargeted metabolomics strategy based on UPLC-ESI-TOF-MS was conducted to analyze the dynamic variations of bioactive metabolites in P. ostii 'Feng Dan' leaves during development. A total of 321 metabolites were rapidly annotated based on the GNPS platform, in-house database, and publications. To accurately quantify the selected metabolites, a targeted method of HPLC-ESI-QQQ-MS was used. Albiflorin, paeoniflorin, pentagalloylglucose, luteolin 7-glucoside, and benzoylpaeoniflorin were recognized as the dominant bioactive compounds with significant content variations during leaf development. Metabolite variations during the development of P. ostii 'Feng Dan' leaves are greatly attributed to the variations in antioxidant activities. Among all tested bacteria, the leaf extract exhibited exceptional inhibitory effects against Streptococcus hemolytis-β. This research firstly provides new insights into tree peony leaves during development. The stages of S1-S2 may be the most promising harvesting time for potential use in food or pharmaceutical purposes.

Luteolin-7-O-glucoside promotes macrophage release of IFN-β by maintaining mitochondrial function and corrects the disorder of glucose metabolism during RSV infection

Respiratory syncytial virus (RSV) pneumonia is the main cause of acute bronchiolitis in infants. Luteolin-7-O-glucoside (LUT-7G) is a natural flavonoid, which exists in a variety of plants and has the potential to treat viral pneumonia. We established RSV pneumonia mouse models and RSV-infected cell models. Clodronate liposomes were used to deplete macrophages. We used HE staining and immunohistochemistry to determine inflammatory damage and virus replication. We detected the expression levels of inflammatory factors and IFN-β through qPCR and ELISA. JC-1 kit was used for detecting the cell mitochondrial Membrane potential (MMP). ROS, SOD, and MDA kits were used for detecting intracellular oxidative stress damage. Metabolites of TCA in lung tissue and serum of mice were detected by GC-MS. Pharmacodynamic studies have shown that intervention with LUT-7G can alleviate lung tissue damage caused by RSV infection, inhibit RSV replication, and downregulate TNF-α, IL-1β, and IL-6 mRNA expression. LUT-7G upregulated the IFN-β content and the expression of IFN-β, ISG15, and OAS1 mRNA. In vitro, LUT-7G inhibited RSV-induced cell death, reversed the RSV-induced decrease of MMP and decreased intracellular oxidative stress. Target metabonomics showed that RSV infection upregulated the levels of glycolysis and TCA metabolites in lung tissue and serum, while LUT-7G could improve the disorder of glucose metabolism. The results indicate that LUT-7G can promote the release of IFN-β in the lung, alleviate inflammatory damage, and inhibit RSV replication during RSV infection. These effects may be achieved by protecting the mitochondrial function of alveolar macrophages and correcting the disorder of glucose metabolism.

Anti-Proliferative Potential of Cynaroside and Orientin—In Silico (DYRK2) and In Vitro (U87 and Caco-2) Studies

Luteolin derivates are plant compounds with multiple benefits for human health. Stability to heat and acid hydrolysis and high resistance to (auto)oxidation are other arguments for the laden interest in luteolin derivates today. The present study was designed to compare the in silico and in vitro anti-proliferative potential of two luteolin derivates, luteolin-7-O-glucoside/cynaroside (7-Lut) and luteolin-8-C-glucoside/orientin (8-Lut). In silico investigations were carried out on the molecular target, namely, the human dual specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) in association with its natural ligand, curcumin (PDB ID: 5ZTN), by CLC Drug Discovery Workbench v. 1.5.1. software and Molegro Virtual Docker (MVD) v. MVD 2019.7.0. software. In vitro studies were performed on two human tumor cell lines, glioblastoma (U87) and colon carcinoma (Caco-2), respectively. Altogether, docking studies have revealed 7-Lut and 8-Lut as effective inhibitors of DYRK2, even stronger than the native ligand curcumin; in vitro studies indicated the ability of both luteolin glucosides to inhibit the viability of both human tumor cell lines, up to 85% at 50 and 100 µg/mL, respectively; the most augmented cytotoxic and anti-proliferative effects were obtained for U87 exposed to 7-Lut (IC50 = 26.34 µg/mL). The results support further studies on cynaroside and orientin to create drug formulas targeting glioblastoma and colon carcinoma in humans.

Chemical Characterization and Antifungal Activity of Blue Tansy (Tanacetum annuum) Essential Oil and Crude Extracts against Fusarium oxysporum f. sp. albedinis, an Agent Causing Bayoud Disease of Date Palm.

Tanacetum annuum L. is a Mediterranean plant, commonly known as Blue Tansy due to its blue colour as an essential oil, which is widely used for medicinal purposes. However, there are no studies on the bioactive compounds (especially, phenolic compounds) and the biological properties of their organic extracts. Herein, the purpose of the present work was to investigate the chemical composition of the essential oil and crude extracts of the T. annuum aerial parts collected from northern Morocco and to evaluate their antioxidant and antifungal activity against Fusarium oxysporum f. sp. albedinis, an agent causing Bayoud disease of the date palm, an important food source and commercial perennial crop in the Sahara and North Africa. Chemically, Folin-Ciocalteu and aluminium chloride colourimetric methods were used to determine the total phenolic (TPC) and total flavonoid (TFC) contents, respectively; polyphenols were characterized using HPLC-MS, while GC-MS was used to analyse the essential oil composition. Moreover, the evaluation of antioxidant and antifungal activities was carried out using the DPPH test and microdilution method, respectively. The results showed that the three T. annuum parts (stems, leaves and flowers) extracts contained important TPC and TFC with values varied between 51.32 and 116.32 mg/g of dry crude extract (DCE). HPLC-MS analysis revealed the identification and quantification of 19 phenolic acids and flavonoids with an emphasis on apigenin 7-glucoside (4540 µg/g of dry weight (DW)), luteolin 7-glucoside (2804 µg/g DW) and salicylic acid (1878 µg/g DW). Additionally, 39 biomolecules were identified in the essential oil using GC-MS, which were predominated by camphor (16.69%), α-pinene (12.37%), bornyl acetate (11.97%) and limonene (11.10%). The methanolic and hydro-methanolic extracts of T. annuum parts demonstrated a strong antioxidant property with IC50 values ranging between 0.22 and 0.65 mg/mL. Concerning antifungal activity, the essential oil and crude extracts of the Moroccan Blue Tansy exhibited a potent capacity against F. oxysporum f. sp. albedinis at low concentrations, with MIC and MFC values of 3.33 and 4.58 µL/mL for the essential oil and values of 3.33 and 9.17 mg/mL for crude extracts, respectively. Overall, these results demonstrated T. annuum as an important source of bioactive compounds and contribute significantly to the potential of using essential oils and extracts for controlling the Bayoud disease of date palms. Moreover, the finding suggests that T. annuum can be highly useful for phytosanitary and pharmaceutical industries.

Profile Phenolic Compounds in Spanish-Style and Traditional Brine Black Olives (‘Gemlik’ Cv.) Provided from Different Regions of Türkiye

The aim of this study was to evaluate the effect of growing regions and processing methods on the composition and the quantity of phenolic compounds in ‘Gemlik’ variety table olives. Two different processing methods, Spanish-style and traditional brine (naturally processed) olives, were used in the processing of ‘Gemlik’ table olives. According to the data obtained in this study, the highest concentrations of phenolic compounds were observed for 3-hydroxytyrosol (4.58–168.21 mg/kg), followed by 4-hydroxyphenyl (0.76–97.58 mg/kg), luteolin 7-glucoside (0.32–58.64 mg/kg), tyrosol (1.57–47.24 mg/kg), and luteolin (0.17–53.56 mg/kg) in overall samples. The highest quantity of phenolic compounds was determined in raw olives, and the lowest phenolic compound content was determined in Spanish-style processed olives. Table olives which are produced by the natural process were observed to contain higher concentrations of phenolic compounds compared with the olives, which are produced in the Spanish style. In this sense, statistical results showed that region and processing methods have significant impacts on the phenolic compounds of table olives.

Genome-Wide Association Study (GWAS) of the Agronomic Traits and Phenolic Content in Sorghum (Sorghum bicolor L.) Genotypes

Sorghum (Sorghum bicolor L.) is a promising biomass crop with high yields of cellulose, hemicellulose, and lignin. Sorghum biomass has emerged as an eco-friendly industrial material useful for producing biofuels and bioplastics. This study conducted genotyping-by-sequencing (GBS)-based genome-wide association studies (GWAS) to establish the genetic basis of traits associated with biomass. Specifically, the researchers evaluated agronomic traits and phenolic compounds using 96 sorghum genotypes. Six phenolic compounds, luteolinidin diglucoside, luteolin glucoside, apigeninidin glucoside, luteolinidin, apigeninidin, and 5-O-Me luteolinidin, were found to be the major phenolic compounds in all genotypes. Out of our six detected phenolic compounds (luteolinidin diglucoside, luteolin glucoside, apigeninidin glucoside, luteolinidin, apigeninidin, and 5-O-Me luteolinidin), luteolinidin was the major phenolic compound in all genotypes. Next, a GWAS analysis was performed to confirm significant associations between 192,040 filtered single-nucleotide polymorphisms (SNPs) and biomass-related traits. The study identified 40 SNPs on 10 chromosomes that were significantly associated with heading date (4 SNPs), plant height (3 SNPs), dry yield (2 SNPs), and phenolic compounds (31 SNPs). The GWAS analysis showed that SbRio.10G099600 (FUT1) was associated with heading date, SbRio.09G149200 with plant height, SbRio.06G211400 (MAFB) with dry yield, SbRio.04G259800 (PDHA1) with total phenolic content and luteolinidin diglucoside, and SbRio.02G343600 (LeETR4) with total phenolic content and luteolinidin, suggesting that these genes could play key roles in sorghum. These findings demonstrate the potential value of sorghum as a biomass resource and the potential for selecting sorghum genotypes with reduced phenolic contents for use in the bioindustry.

Hydroxypropyl-β-Cyclodextrin-Glycerol-Assisted Extraction of Phenolics from Satureja montana L.: Optimization, Anti-Elastase and Anti-Hyaluronidase Properties of the Extracts

A green method for hydroxypropyl-β-cyclodextrin-glycerol-assisted extraction (HCGAE) of bioactive phenolics from S. montana, Lamiaceae was optimized using Box-Behnken design and response surface methodology and compared conventional water/ethanol-based extraction. The procedure was aimed at obtaining extracts with the maximum content of total phenols (TP), flavonoids (TF), dihydroxycinnamic acids (TDCA), rosmarinic acid (RA), and luteolin 7-O-glucoside (LG). The impact of glycerol content (0–70%), 2-hydroxypropyl-β-cyclodextrin content (0–0.4 mmol), temperature (20–70 °C), herbal material weight (0.3–0.8 g), extraction duration (5–25 min), and ultrasound power (144–720 W) on the extraction efficiency was analyzed. Four extracts with maximum amounts of target phenols, OPT-TP (5.93 mg/mL), OPT-TDCA-RA (4.17 mg/mL and 1.16 mg/mL, respectively), OPT-TF (0.99 mg/mL), and OPT-LG (0.28 mg/mL) were prepared. Comparison of the content of TDCA, TF, RA, and LG with those obtained in water/ethanol-based extraction demonstrated the superiority of the HCGAE approach for the extraction of phenols from S. montana. The extracts displayed good anti-elastase and excellent anti-hyaluronidase activity. IC50 values of the anti-hyaluronidase activity (1.67 ± 0.06 μL extract/mL, 1.16 ± 0.08 μL extract/mL, 0.85 ± 0.03 μL extract/mL, and 0.79 ± 0.05 μL extract/mL for OPT-TP, OPT-TDCA-RA, OPT-TF, and OPT-LG, respectively) surpassed that of the applied positive control, tannic acid. The observed bioactivity of the optimized extracts makes them promising active ingredients for natural cosmetics. The results of this research indicate that HCGAE is an excellent alternative to conventional water/ethanol-based extraction of phenolics from Satureja montana L.-yielding extracts with potent anti-elastase and anti-hyaluronidase properties suitable for direct use in cosmetic products.

Humulus japonicus Extract Ameliorates Hepatic Steatosis Through the PPARα-Mediated Suppression of Alcohol-Induced Oxidative Stress.

Humulus japonicus has been used to treat obesity, hypertension, and nonalcoholic fatty liver and to alleviate inflammation and oxidative stress. In the present study, we aimed to investigate the effects of H. japonicus ethanol extracts (HE) and luteolin 7-O-β-d-glucoside (LU), which is identified as a major active component of H. japonicus, on ethanol-induced oxidative stress and lipid accumulation in primary hepatocytes. Mouse primary hepatocytes were treated with HE and stimulated with ethanol. The MTT test was used to determine cell viability. By using Western blotting, the effects of HE on the expression of different proteins were investigated. Experimental mice were given a 5% alcohol liquid Lieber-DeCarli diet to induce alcoholic fatty liver. We found that both HE and LU individually attenuated ethanol-induced lipid accumulation, lipogenic protein expression, and cellular oxidative stress in hepatocytes. Treatment with HE or LU increased PPARα and SOD1 expression and catalase activity in a dose-dependent manner. Small interfering RNA of PPARα reduced the effects of HE on oxidative stress, lipid metabolism, and levels of antioxidants. We also observed that orally administered HE treatment alleviated hepatic steatosis in a diet containing ethanol-fed mice. This study suggests HE as a functional food that can improve hepatic steatosis, thereby preventing hepatic injury caused by alcohol consumption.

Antioxidant and Antibacterial Properties of a Functional Sports Beverage Formulation.

Athletes often consume functional beverages in order to improve performance and reduce oxidative stress caused by high-intensity exercise. The present study aimed to evaluate the antioxidant and antibacterial properties of a functional sports beverage formulation. The beverage's antioxidant effects were assessed on human mesenchymal stem cells (MSCs) by determining thiobarbituric acid reactive substances (TBARS; TBARS levels decreased significantly by 52.67% at 2.0 mg/mL), total antioxidant capacity (TAC; TAC levels increased significantly by 80.82% at 2.0 mg/mL) and reduced glutathione (GSH; GSH levels increased significantly by 24.13% at 2.0 mg/mL) levels. Furthermore, the beverage underwent simulated digestion following the INFOGEST protocol to assess its oxidative stability. The analysis of the total phenolic content (TPC) using the Folin-Ciocalteu assay revealed that the beverage contained a TPC of 7.58 ± 0.066 mg GAE/mL, while the phenolics identified by HPLC were catechin (2.149 mg/mL), epicatechin (0.024 mg/mL), protocatechuic acid (0.012 mg/mL), luteolin 7-glucoside (0.001 mg/mL), and kaempferol-3-O-β-rutinoside (0.001 mg/mL). The beverage's TPC was strongly correlated with TAC (R2 = 896). Moreover, the beverage showcased inhibitory and bacteriostatic effects against Staphylococcus aureus and Pseudomonas aeruginosa. Lastly, the sensory acceptance test demonstrated that the functional sports beverage was well accepted by the assessors.

Evaluation of bioactive compounds of plants used in Mexico, to predict potential SARS-CoV-2 inhibitors: Analysis between two molecular docking servers

Plants traditionally used for their antiviral activity could be an alternative against SARS-CoV-2. In this study, the efficacy of 10 bioactive plant compounds commonly used in Mexico against COVID-19 was evaluated by molecular docking with two online servers: COVID-19 Docking Server and DockThor. Remdesivir was used as a control. The results showed that Cypellocarpin B, Cypellocarpin C, Luteolin 7-glucoside and Syringetin glucopyranoside showed the highest affinity towards viral proteins Mpro and RdRp respect to Remdesivir. Comparison of molecular docking servers showed differences in the docking motors and proteins available on each server. The use of bioactive compounds represents an alternative for the treatment of patients with COVID-19.

Pimpinella pruatjan Molk: LC-MS/MS-QTFT Analysis of Bioactive Compounds from Decoction and Ethanol Extract of Aerial Parts.

Pimpinella pruatjan Molk is native to Java and well known as aphrodisiac in traditional medicine. A water-boiled extract of the plant has been used in the treatment of erectile dysfunction (ED). No study has been found on the phytochemical constituents and identification of corresponding biological activities in water and polar extract. This study is aimed to identify phytoconstituents of a decoction and ethanol extract from the aerial parts of P. pruatjan Molk. Liquid chromatography-tandem mass spectroscopy (LC-MS/MS) was used to analyze and predict the bioactive compounds in both extracts. LC-MS/MS revealed both extracts contained two important compounds: Luteolin-7-O-β-D glucopyranoside and Undulatoside A. Luteolin and Luteolin glucoside are also found in P.anisum L. Lutein 7-O glucoside was found in water extract, while more bioactive compounds, including populnin, 3,5-O-dicaffeoylquinic acid, quercetin-3'- O glucoside, methylophiopogononeone-A, kaempferol-7-O-α-L-arabinofuranoside, and 7-hydroxy-3,5,6,3',4'- pentamethoxyflavone, were found in ethanol extract. Accumulation of flavonoids, phenols, phenylpropanoids, alkaloids, and furanochromone in low quantities was observed in both extracts. This is the first report providing evidence justifying its use as a traditional medicine. Further investigation into the pharmacology mechanism of action is required.

INVESTIGATION ON THE INTERACTION OF β-SITOSTEROL AND LUTEOLIN-7-GLUCOSIDE BINDING TO BOVINE SERUM ALBUMIN

Objective: The study ondrug–protein interactions is an important field of interest because of the prospective of unraveling of drug action mechanisms and the possibility of designing novel medicines. Bovine serum albumin (BSA) has been studied extensively because of its structural homology with human serum albumin (HSA). The objective of the work was to study the interaction between β-sitosterol and Luteolin–7-glucoside with bovine serum albumin (BSA) investigated by molecular docking. Methods: Docking studies were carried out using a crystal structure of bovine serum albumin complexed with naproxen (pdb code-4OR0). Auto dock 4.2 was used to perform molecular docking. Ligands were found flexible during the docking process, and protein was kept rigid. Results: Molecular docking studies revealed that the β-sitosterol can bind in the large hydrophobic cavity of BSA, mainly by the hydrophobic interaction but also by hydrogen bond interactions between the hydroxyl (OH) group of β-sitosterol to SER 488 with hydrogen bond distance of 2.1Å. Luteolin-7-glucoside molecule interact by hydrophobic interaction with LYS 431, ARG 427, ALA 193 amino acids of Bovine Serum Albumin. The amino acids ARG 458, ARG 435, ARG 185 are involved in forming a hydrogen bond with hydroxyl oxygens, carbonyl carbon of Luteolin-7-glucoside with hydrogen bond distance of 2.4, 2.3 and 1.9 Å, respectively. Conclusion: Study indicated that hydrophobic and hydrogen bonding interactions were mostly responsible for albumin interaction. Further research of the pharmaceutical potential of plant molecules will be valuable for monitoring their biological functions.