A Novel 4H-Chromen-4-One Derivative from Marine Streptomyces ovatisporus S4702T as Potential Antibacterial and Anti-Cancer Agent.

BACKGROUND: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities. OBJECTIVE: Herein, it was aimed to elucidate the bioactive potential of a marine-derived Streptomyces ovatisporus S4702T, isolated previously. METHODS: Streptomyces ovatisporus S4702T was cultured in N-Z Amine broth, and extraction was carried out using different organic solvents. Bioassay-guided purification was followed by chemical characterization using NMR and LC-MS/MS. The compound was then evaluated for its antibacterial, antioxidant and cytotoxic activities. RESULTS: Etyl acetate extracts gave the highest antibacterial activity, and chemical characterization of this extract indicated the formula as C15H29O5N3 and the corresponding possible molecular structure as 4H-chromen-4-one derivative. It was found highly potent against Bacillus subtilis ATCC 6633 (MIC: 0.25 µg ml-1) and Micrococcus luteus ATCC 9341 (MBC: 0.5 µg ml-1). It has no remarkable antioxidant activity, but a higher EC50 value and less cytotoxicity against normal cells. The EC50 values of this chromen derivative were found as 9.68 µg ml-1 for human colon carcinoma, 9.93 µg ml-1 for human prostate adenocarcinoma and 25.5 µg ml-1 for human embryonic kidney cells. CONCLUSION: Overall, the presented 4H-chromen-4-one derivative is a remarkable bioactive compound with potent antibacterial and cytotoxic activity. With its high bioactive potential, it is proposed as a good candidate in medicine.

A soft Pickering emulsifier made from chitosan and peptides endows stimuli-responsiveness, bioactivity and biocompatibility to emulsion.

Polymeric Pickering emulsifiers may bring new insights to emulsion theory and practice due to their soft characters. Herein, a group of soft Pickering emulsifiers, chitosan-casein hydrophobic peptides nanoparticles (CS-CHP NPs) were prepared with a non-covalent anti-solvent procedure. The CS-CHP NPs provided the contact angles of 37.2°-87.4°, stabilizing O/W or W/O emulsions with enhanced thermal stability, endowing the emulsion with pH and CO2/N2 responsiveness. The emulsifying behavior and mechanism presented by CS-CHP NPs were different from that of ordinary hard Pickering emulsifiers, where the appropriate contact angle was 37.2° instead of 87.4° for stabilizing O/W emulsions. Moreover, the nanoparticles possess antioxidant, antibacterial activities and excellent biocompatibility. DPPH and ABTS scavenging activity of the CS-CHP NPs were >220% of that of CS NPs. The last, the emulsion provided high-efficient encapsulation of curcumin, making the soft Pickering emulsifiers a group candidate for drug delivery in food, cosmetics and pharmaceutical industry.

GC-MS Analysis and Biomedical Therapy of Oil from n-Hexane Fraction of Scutellaria edelbergii Rech. f.: In Vitro, In Vivo, and In Silico Approach.

The current study aimed to explore the crude oils obtained from the n-hexane fraction of Scutellaria edelbergii and further analyzed, for the first time, for their chemical composition, in vitro antibacterial, antifungal, antioxidant, antidiabetic, and in vivo anti-inflammatory, and analgesic activities. For the phytochemical composition, the oils proceeded to gas chromatography-mass spectrometry (GC-MS) analysis and from the resultant chromatogram, 42 bioactive constituents were identified. Among them, the major components were linoleic acid ethyl ester (19.67%) followed by ethyl oleate (18.45%), linolenic acid methyl ester (11.67%), and palmitic acid ethyl ester (11.01%). Tetrazolium 96-well plate MTT assay and agar-well diffusion methods were used to evaluate the isolated oil for its minimum inhibitory concentrations (MIC), minimum bactericidal concentration (MBC), half-maximal inhibitory concentrations (IC50), and zone of inhibitions that could determine the potential antimicrobial efficacy's. Substantial antibacterial activities were observed against the clinical isolates comprising of three Gram-negative bacteria, viz., Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and one Gram-positive bacterial strain, Enterococcus faecalis. The oils were also effective against Candida albicans and Fusarium oxysporum when evaluated for their antifungal potential. Moreover, significant antioxidant potential with IC50 values of 136.4 and 161.5 µg/mL for extracted oil was evaluated through DPPH (1,1-Diphenyl-2-picryl-hydrazyl) and ABTS assays compared with standard ascorbic acid where the IC50 values were 44.49 and 67.78 µg/mL, respectively, against the tested free radicals. The oils was also potent, inhibiting the α-glucosidase (IC50 5.45 ± 0.42 µg/mL) enzyme compared to the standard. Anti-glucosidase potential was visualized through molecular docking simulations where ten compounds of the oil were found to be the leading inhibitors of the selected enzyme based on interactions, binding energy, and binding affinity. The oil was found to be an effective anti-inflammatory (61%) agent compared with diclofenac sodium (70.92%) via the carrageenan-induced assay. An appreciable (48.28%) analgesic activity in correlation with the standard aspirin was observed through the acetic acid-induced writhing bioassay. The oil from the n-hexane fraction of S. edelbergii contained valuable bioactive constituents that can act as in vitro biological and in vivo pharmacological agents. However, further studies are needed to uncover individual responsible compounds of the observed biological potentials which would be helpful in devising novel drugs.

Hazelnut Shells as Source of Active Ingredients: Extracts Preparation and Characterization.

Hazelnut shells represent a waste material (about 42% of the total biomass) deriving from hazelnut harvest. These are mainly used as a heating source; however, they represent an interesting source of polyphenols useful in health field. The impact on phenolic profile and concentrations of hazelnut shell extracts obtained by three extraction methods (maceration, ultrasonic bath, and high-power ultrasonic), as well as temperature, extraction time, and preventive maceration, was studied. The prepared extracts were characterized in terms of chemical composition, antioxidant and antimicrobial activities. Eighteen different phenolic compounds were identified and quantified by chemical analysis and gallic acid was the most abundant in all the extracts analyzed. Other relevant compounds were chlorogenic acid, protocatechuic acid and catechin. Preventive maceration had a positive effect on the extraction of different types of compounds regardless of the method performed. Application of the high-power ultrasonic method had different effects, either positive or negative, depending on the type of compound and extraction time. All the prepared extracts showed antioxidant activity especially those prepared by maceration, and many of them were able to inhibit the growth of both B. subtilis and B. cereus.

Black Bean (Phaseolus vulgaris L.) Polyphenolic Extract Exerts Antioxidant and Antiaging Potential.

Phenolic compounds present in common beans (Phaseolus vulgaris L.) have been reported to possess antimicrobial, anti-inflammatory and ultraviolet radiation (UVR) protective properties. UVR from sunlight, which consists of UV-B and UV-A radiations, induces reactive oxygen species (ROS) and free radical formation, consequently activating proteinases and enzymes such as elastase and tyrosinase, leading to premature skin aging. The objective of this work was to extract, characterize and evaluate the antioxidant and antiaging potential of polyphenols from a black bean endemic variety. The polyphenolic extract was obtained from black beans by supercritical fluid extraction (SFE) using CO2 with a mixture of water-ethanol as a cosolvent and conventional leaching with a mixture of water-ethanol as solvent. The polyphenolic extracts were purified and characterized, and antioxidant potential, tyrosinase and elastase inhibitory potentials were measured. The extract obtained using the SFE method using CO2 and H2O-Ethanol (50:50 v/v) as a cosolvent showed the highest total phenolic compounds yield, with 66.60 ± 7.41 mg GAE/g coat (p > 0.05) and 7.30 ± 0.64 mg C3GE/g coat (p < 0.05) of anthocyanins compared to conventional leaching. Nineteen tentative phenolic compounds were identified in leaching crude extract using ESI-QTOF. Quercetin-3-D-galactoside was identified in crude and purified extracts. The purified SFC extract showed IC50 0.05 ± 0.002 and IC50 0.21 ± 0.008 mg/mL for DPPH and ABTS, respectively. The lowest IC50 value of tyrosinase inhibition was 0.143 ± 0.02 mg/mL and 0.005 ± 0.003 mg/mL of elastase inhibition for leaching purified extract. Phenolic compounds presented theoretical free energy values ranging from -5.3 to -7.8 kcal/mol for tyrosinase and -2.5 to -6.8 kcal/mol for elastase in molecular docking (in silico) studies. The results suggest that the purified extracts obtained by SFE or conventional leaching extraction could act as antioxidant and antiaging ingredients for cosmeceutical applications.

Phytochemical Screening and Antioxidant Activity of Seven Native Species Growing in the Forests of Southern Chilean Patagonia.

The genus Nothofagus is one of the most abundant in the subantarctic Patagonian forests. Five species inhabit these ecosystems, three evergreen (Nothofagus betuloides, Nothofagus dombeyi, and Nothofagus nitida) and two deciduous (Nothofagus pumilio and Nothofagus antarctica). This is the first report on the levels of secondary metabolites and the antioxidant capacity of Patagonian tree species growing in natural environments. The aim of this work was to carry out a phytochemical screening, to determine the antioxidant capacity, the sun protection factor, and the α-glucosidase and tyrosinase inhibitory activity of foliar extracts of the five previous species. Besides, Aristotelia chilensis and Berberis microphylla, two species of Patagonian shrubs growing in the same forests, were used as reference. N. dombeyi was the Nothofagus with the best antioxidant capacity. B. microphylla differed from all studied species. Moreover, the Nothofagus was split into two groups. N. betuloides and N. dombeyi are the most similar species to A. chilensis. The α-glucosidase was completely inhibited by all studied extracts. Furthermore, N. antarctica, N.pumilio, and N. nitida inhibited about 70% of the tyrosinase activity. All the results found in this study for the species of the genus Nothofagus support further research on their potential beneficial properties for human health.

Evaluation of Pomelo Seed Extracts as Natural Antioxidant, Antibacterial, Herbicidal Agents, and Their Functional Components.

Pomelo seeds (PS) are important by-product of pomelo fruits (Citrus grandis Osbeck). The value-added utilization of PS remains highly challenged. This study aimed to investigate the utilization potential of PS as natural antioxidant, antibacterial, herbicidal agents, and their functional components. The ethanolic extract (EE) of PS and its four fractions as PEE (petroleum ether extract), AcOEtE (ethyl acetate extract), BTE (butanol extract), and WE (water extract), were prepared and biologically evaluated. BTE exhibited the best antioxidant activity among all these extracts, in both ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and FRAP (ferric reducing antioxidant power) assays. AcOEtE was superior to other extracts in herbicidal assay against both Festuca elata Keng (IC50 of 0.48 mg mL-1 ) and Amaranthus retroflexus L. (IC50 of 0.94 mg mL-1 ). Meanwhile, both AcOEtE and BTE demonstrated inhibitory effects against Bacillus subtilis, Escherichia coli, and Xanthomonas citri subsp. citri, with MIC ranging 2.5-5.0 mg mL-1 . Furthermore, the primary chemical components involving naringin, deacetylnomilin, limonin, nomilin, and obacunone, were quantified in all these extracts. PCA (principal component analysis) suggested that naringin might highly contribute to the antioxidant activity of PS, and the herbicidal activity should be ascribed to limonoids. This study successfully identified AcOEtE and BTE as naturally occurring antioxidant, antibacterial, and herbicidal agents, showing application potential in food and cosmetics industries, and organic farming agriculture.

Polyphenolic composition and antioxidant potential of underutilized Himalayan wild edible berries by high-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry.

The Himalayan wild berries Myrica esculenta, Duchesnea indica, Prunus cerasoides, and Berberis lycium were studied for the first time for polyphenolic compositions using high-performance liquid chromatography/electrospray ionization tandem mass spectrometry. The chemical analysis of extracts resulted in the identification of 69 polyphenols, including 11 anthocyanins, 28 phenolic acids, 19 flavanoids, 10 ellagitannins, and 1 dihydrochalcone. The caffeoylquinic acids, quercetin, kaempferol, and cyanidin are the common moieties in studied wild berries. In addition, seven phenolic compounds, that is, gallic acid, vanillic acid, caffeic acid, rutin, ferulic acid, quercetin, and myricetin were quantified. Among anthocyanins, cyanidin-3-O-glucoside was the majorly quantified anthocyanin that ranged from 2.52 to 6.18% followed by delphinidin-3-O-glucoside (0.6%-5.53%). The samples were assessed for total phenolics, total anthocyanin content, and antioxidant potential. The results showed that M. esculenta and B. lycium had the highest total phenolic and anthocyanin content and exhibited promising antioxidant activity with IC50 of 32.100 ± 0.42 and 48.44 ± 0.46 µg/mL, respectively. Principal component analysis was able to clearly differentiate between four underutilized Himalayan wild edible berries. The wide variability of polyphenolic constituents supports the consumption of these berries not only to achieve the nutrient requirements among local people but also as promising sources of antioxidants for the food industry.

Investigation on the Phytochemical Composition, Antioxidant and Enzyme Inhibition Potential of Polygonum Plebeium R.Br: A Comprehensive Approach to Disclose New Nutraceutical and Functional Food Ingredients.

The present work describes medicinal potential and secondary metabolic picture of the methanol extract (PP-M) of Polygonum plebeium R.Br. and its fractions; hexane (PP-H), ethyl acetate (PP-E) and water (PP-W). In total bioactive component estimation, highest contents of phenolic (89.38±0.27 mgGAE/g extract) and flavonoid (51.21±0.43 mgQE/g extract) were observed in PP-E, and the same fraction exhibited the highest antioxidant potential in DPPH (324.80±4.09 mgTE/g extract), ABTS (563.18±11.39 mgTE/g extract), CUPRAC (411.33±15.49 mgTE/g extract) and FRAC (369.54±1.70 mgTE/g extract) assays. In Phosphomolybdenum activity assay, PP-H and PP-E showed nearly similar potential, however, PP-H was the most active (13.54±0.24 mgEDTAE/g extract) in metal chelating activity assay. PP-W was the stronger inhibitor (4.03±0.05 mgGALAE/g extract) of the enzyme AChE, while PP-H was potent inhibitor of BChE (5.62±0.27 mg GALAE/g extract). Interestingly, PP-E was inactive against BChE. Against tyrosinase activity, PP-E was again the most active fraction with inhibitory value of 71.89±1.44 mg KAE/g extract, followed by the activity of PP-M and PP-W. Antidiabetic potential was almost equally distributed among PP-M, PP-H and PP-E. For mapping the chemodiversity of P. plebeium, PP-M was analyzed through UHPLC/MS, which led to the identification of more than 50 compounds. Flavonoids were the main components derived from isovitexin, kaempferol and luteolin however, gallic acid, protocatechuic acid, gingerols and lyoniresinol 9'-sulfate were among important bioactive phenols. These findings prompted to conclude that Polygonum plebeium can be a significant source to offer new ingredient for nutraceuticals and functional foods.

Mushroom Species Stereum hirsutum as Natural Source of Phenolics and Fatty Acids as Antioxidants and Acetylcholinesterase Inhibitors.

Many lignicolous mushroom species are used as a food supplement and may represent an alternative treatment of Alzheimer's disease (AD). This study aimed to evaluate acetylcholinesterase inhibition (AChEI) of Stereum hirsutum together with antioxidant activity (AO) and cytotoxic activity against HepG2 cells. Different extracts (water, ethanol, methanol, polysaccharide) were analyzed, with respect to their mineral composition and chemical content. Ethanol extract was the most potent in AChEI (98.44 %) and demonstrated cytotoxic activity (91.96 % at 900.00 µg/mL), while the highest AO was demonstrated for polar extracts (methanol and water) as well. These activities may be attributed to determined phenolics (hydroxybenzoic and quinic acid) and fatty acids (FA), while biflavonoid amentoflavone may be responsible for cytotoxic activity. The most prevalent FA was linoleic (40.00 %) and the domination of unsaturated FA (UFA) (71.91 %) over saturated (26.96 %) was observed. This is the first report of AChEI of S. hirsutum extracts and first detection of amentoflavone. Due to high amount of UFA and well-expressed AChEI, this species can be considered as a potent food supplement in the palliative therapy of AD.

Determination of Phenolic Compounds in Various Propolis Samples Collected from an African and an Asian Region and Their Impact on Antioxidant and Antibacterial Activities.

The biological activities of propolis samples are the result of many bioactive compounds present in the propolis. The aim of the present study was to determine the various chemical compounds of some selected propolis samples collected from Palestine and Morocco by the High-Performance Liquid Chromatography-Photodiode Array Detection (HPLC-PDA) method, as well as the antioxidant and antibacterial activities of this bee product. The chemical analysis of propolis samples by HPLC-PDA shows the cinnamic acid content in the Palestinian sample is higher compared to that in Moroccan propolis. The results of antioxidant activity demonstrated an important free radical scavenging activity (2,2-Diphenyl-1-picrylhydrazyl (DPPH); 2,2'-azino-bis 3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and reducing power assays) with EC50 values ranging between 0.02 ± 0.001 and 0.14 ± 0.01 mg/mL. Additionally, all tested propolis samples possessed a moderate antibacterial activity against bacterial strains. Notably, Minimum Inhibitory Concentrations (MICs) values ranged from 0.31 to 2.50 mg/mL for Gram-negative bacterial strains and from 0.09 to 0.125 mg/mL for Gram-positive bacterial strains. The S2 sample from Morocco and the S4 sample from Palestine had the highest content of polyphenol level. Thus, the strong antioxidant and antibacterial properties were apparently due to the high total phenolic and flavone/flavonol contents in the samples. As a conclusion, the activities of propolis samples collected from both countries are similar, while the cinnamic acid in the Palestinian samples was more than that of the Moroccan samples.

Chemical Constituents of the Essential Oil from Ecuadorian Endemic Species Croton ferrugineus and Its Antimicrobial, Antioxidant and α-Glucosidase Inhibitory Activity.

Croton ferrugineus Kunth is an endemic species of Ecuador used in traditional medicine both for wound healing and as an antiseptic. In this study, fresh Croton ferrugineus leaves were collected and subjected to hydrodistillation for extraction of the essential oil. The chemical composition of the essential oil was determined by gas chromatography equipped with a flame ionization detector and gas chromatography coupled to a mass spectrometer using a non-polar and a polar chromatographic column. The antibacterial activity was assayed against three Gram-positive bacteria, one Gram-negative bacterium and one dermatophyte fungus. The radical scavenging properties of the essential oil was evaluated by means of DPPH and ABTS assays. The chemical analysis allowed us to identify thirty-five compounds representing more than 99.95% of the total composition. Aliphatic sesquiterpene hydrocarbon trans-caryophyllene was the main constituent with 20.47 ± 1.25%. Other main compounds were myrcene (11.47 ± 1.56%), ß-phellandrene (10.55 ± 0.02%), germacrene D (7.60 ± 0.60%), and α-humulene (5.49 ± 0.38%). The essential oil from Croton ferrugineus presented moderate activity against Candida albicans (ATCC 10231) with an MIC of 1000 µg/mL, a scavenging capacity SC50 of 901 ± 20 µg/mL with the ABTS method, and very strong antiglucosidase activity with an IC50 of 146 ± 20 µg/mL.

Proteome Analysis and In Vitro Antiviral, Anticancer and Antioxidant Capacities of the Aqueous Extracts of Lentinula edodes and Pleurotus ostreatus Edible Mushrooms.

In this study, we examined aqueous extracts of the edible mushrooms Pleurotus ostreatus (oyster mushroom) and Lentinula edodes (shiitake mushroom). Proteome analysis was conducted using LC-Triple TOF-MS and showed the expression of 753 proteins by Pleurotus ostreatus, and 432 proteins by Lentinula edodes. Bioactive peptides: Rab GDP dissociation inhibitor, superoxide dismutase, thioredoxin reductase, serine proteinase and lectin, were identified in both mushrooms. The extracts also included promising bioactive compounds including phenolics, flavonoids, vitamins and amino acids. The extracts showed promising antiviral activities, with a selectivity index (SI) of 4.5 for Pleurotus ostreatus against adenovirus (Ad7), and a slight activity for Lentinula edodes against herpes simplex-II (HSV-2). The extracts were not cytotoxic to normal human peripheral blood mononuclear cells (PBMCs). On the contrary, they showed moderate cytotoxicity against various cancer cell lines. Additionally, antioxidant activity was assessed using DPPH radical scavenging, ABTS radical cation scavenging and ORAC assays. The two extracts showed potential antioxidant activities, with the maximum activity seen for Pleurotus ostreatus (IC50 µg/mL) = 39.46 ± 1.27 for DPPH; 11.22 ± 1.81 for ABTS; and 21.40 ± 2.20 for ORAC assays. This study encourages the use of these mushrooms in medicine in the light of their low cytotoxicity on normal PBMCs vis à vis their antiviral, antitumor and antioxidant capabilities.

Versatile Fluorescent Carbon Dots from Citric Acid and Cysteine with Antimicrobial, Anti-biofilm, Antioxidant, and AChE Enzyme Inhibition Capabilities.

Nanostructured fluorescent particles derived from natural molecules were prepared by a green synthesis technique employing a microwave method. The precursors citric acid (CA) and cysteine (Cys) were used in the preparation of S- and N-doped Cys carbon dots (Cys CDs). Synthesis was completed in 3 min. The graphitic structure revealed by XRD analysis of Cys CDs dots had good water dispersity, with diameters in the range of 2-20 nm determined by TEM analysis. The isoelectric point of the S, N-doped CDs was pH value for 5.2. The prepared Cys CDs displayed excellent fluorescence intensity with a high quantum yield of 75.6 ± 2.1%. Strong antimicrobial capability of Cys CDs was observed with 12.5 mg/mL minimum bactericidal concentration (MBC) against gram-positive and gram-negative bacteria with the highest antimicrobial activity obtained against Staphylococcus aureus. Furthermore, Cys CDs provided total biofilm eradication and inhibition abilities against Pseudomonas aeruginosa at 25 mg/mL concentration. Cys CDs are promising antioxidant materials with 1.3 ± 0.1 µmol Trolox equivalent/g antioxidant capacity. Finally, Cys CDs were also shown to inhibit the acetylcholinesterase (AChE) enzyme, which is used in the treatment of Alzheimer's disease, even at the low concentration of 100 µg/mL.

Chemical Composition and Antioxidant, Antiparasitic, Cytotoxicity and Antimicrobial Potential of the Algerian Limonium Oleifolium Mill. Essential Oil and Organic Extracts.

This work aimed to investigate, for the first time, the chemical composition, antioxidant, antiparasitic, cytotoxicity, and antimicrobial activities of the aromatic plant Limonium oleifolium Mill. essential oil (EO) and organic extracts. L. oleifolium aerial parts essential oil was analyzed by GC-FID and GC-MS, and 46 constituents representing 98.25±1.12 % of the oil were identified. γ-Muurolene (10.81±0.07 %), cis-caryophyllene (7.71±0.06 %), o-cymene (7.07±0.01 %) and α-copaene (5.02±0.05 %) were the essential oil main compounds. The antioxidant activity of L. oleifolium EO and organic extracts (MeOH, CHCl3 , AcOEt, BuOH) was explored using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS, ß-carotene/linoleic acid, cupric reducing antioxidant capacity (CUPRAC), and ferric reducing power assays. The results showed that L. oleifolium EO exhibit antioxidant capacity (IC50 =17.40±1.32 µg/mL for DPPH assay, IC50 =29.82±1.08 µg/mL for ß-carotene assay, IC50 =25.23±1.01 µg/mL for ABTS assay, IC50 =9.11±0.08 µg/mL for CUPRAC assay and IC50 =19.41±2.06 mg/mL for reducing power assay). Additionally, the EO showed significant activity against trophozoite form of Acanthamoeba castellanii (IC50 =7.48±0.41 µg/mL) and promastigote form of Leishmania amazonensis (IC50 =19.36±1.06 µg/mL) and low cytotoxicity on murine macrophages (LC50  90.23±1.09 µg/mL), as well as good antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella oxytoca, and Pseudomonas aeruginosa. These results suggest that L. oleifolium essential oil is a valuable source of bioactive compounds presenting antioxidant, antiparasitic, and antimicrobial activities. Furthermore, it is considered nontoxic.

Recent Advance on Chemistry and Bioactivities of Secondary Metabolites from Viburnum Plants: An Update.

Viburnum species are a group of small trees or shrubs that are of great ornamental and medicinal values. Some of them have been used for a long time both as conventional and ethnic medicine. Viburnum fruits, eaten in fresh and processed forms, have been revealed to contain various health-promoting nutrients. With the increasing research on Viburnum plants, they are considered to be an abundant resource of bioactive natural products possessing diverse pharmacological properties and unique chemical structures, that is powerfully proved by the existence of structurally novel vibsane-type diterpenoids which only occur in Viburnum species, newly discovered lignan constituents with unusual side chains and other noteworthy natural components. This review describes 185 new and 228 known secondary metabolites from Viburnum genus between 2008 and 2020, including their chemical structures, sources and bioactivities, and highlights the corresponding structure-activity relationships.

Protective Effect of Lemon Peel Extract on Oxidative Stress in H9c2 Rat Heart Cell Injury.

AIM: Lemon peel, a traditional Chinese medicine, was tested in this study for its novel application in inhibiting cellular oxidative stress, and the effect of lemon peel extract (LPE) on protecting H9c2 rat heart cells from oxidative stress was investigated. METHODS: The scavenging effects of LPE on 1,1-diphenyl-2-picryhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) free radicals were measured in extracellular experiments. The 3-(4,5-dimethyl-2-thiazolinyl)-2,5-diphenyl-2-h-tetrazolylammonium bromide (MTT) assay was used to detect the cell survival rate. The cell supernatant and intracellular oxidation-related indicators were detected by a kit, and the mRNA expression in H9c2 cells was detected by quantitative polymerase chain reaction (qPCR). The chemical substances of LPE were analyzed by high-performance liquid chromatography (HPLC). RESULTS: The results showed that LPE exhibited better DPPH and ABTS free radical scavenging abilities than vitamin C. Compared with the cells in the normal state (control group), the cell survival rate in the model group decreased, and the level of lactate dehydrogenase (LDH) increased, the levels of superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) decreased, and the content of malondialdehyde (MDA) increased. Compared with the control group, the expression of Bcl-2-related X protein (Bax), caspase-3, nuclear factor erythroid 2-related factor 2 (Nrf2), and heme oxygenase-1 (HO-1) in the model group was increased, and the expression of B-cell lymphoma-2 (Bcl-2) was reduced. Compared with the model group, LPE treatment improved the cell survival rate, reduced the levels of LDH and MDA, increased the levels of SOD, CAT, and GSH, downregulated the expression of Bax, caspase-3, Nrf2 and HO-1, and upregulated the expression of Bcl-2. The composition analysis showed that LPE contained catechin, rutin, naringin, quercetin, and hesperidin. CONCLUSION: The results indicated that LPE could protect H9c2 cells from oxidative stress through five active components. LPE has the potential to be developed into natural medicine or health food for the inhibition of cell oxidative damage.

Prevalence of Diterpenes in Essential Oil of Euphorbia mauritanica L.: Detailed Chemical Profile, Antioxidant, Cytotoxic and Phytotoxic Activities.

Plants belonging to Euphorbia L. genus are considered very interesting from a medicinal point of view due to their diverse metabolites and bioactivities. The essential oil (EO) of Euphorbia mauritanica L. is not studied up to date. Therefore, the present study aimed to explore the chemical profile of this EO and evaluate its antioxidant, cytotoxic, and allelopathic potentialities. The EO was extracted from the whole plant via hydrodistillation and then, analyzed by gas chromatography/mass spectrometry (GC/MS). The correlation of E. mauritanica with the other Euphorbia plants was established using chemometric analysis. The antioxidant activity was determined based on scavenging of the free radical, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). The anti-proliferation of the EO on the Hep G2 and MCF-7 cells was evaluated. Finally the allelopathic activity of the EO was assessed against the two noxious weeds, Dactyloctenium aegyptium and Urospermum picroides. Forty-one compounds were identified using GC/MS analysis, with an abundance of terpenoids (91.54 %) that were categorized into mono- (30.75 %), sesqui- (15.23 %), and diterpenes (45.56 %). Interestingly, the results revealed the preponderance of diterpenoid constituents although they are rarely found in the EOs of the plant kingdom. The major compounds were (3E)-cembrene A (18.66 %), verticiol (17.05 %), limonene (7.91 %), eucalyptol (7.26 %), α-pinene (5.61 %), neo-cembrene A (3.52 %), kaur-16-ene (3.24 %), and cembrene (3.09 %). The EO showed moderate antioxidant activity where it attained IC50 values of 83.34 and 64.21 µg mL-1 for DPPH and ABTS compared to 23.01 and 19.23 µg mL-1 for ascorbic acid as standard, respectively. The EO exhibited very weak cytotoxic effect on MCF-7 and Hep G2 cells. The EO showed significant allelopathic activities against the weeds D. aegyptium and U. picroides in a concentration-dependent manner. EO was found more effective against U. picroides than D. aegyptium with IC50 values of 0.79, 0.45, and 0.67 mg mL-1 and 1.17, 0.55, and 1.08 mg mL-1 for germination, root, and shoot growth, respectively. Due to the high content of diterpenes in E. mauritanica, further study is recommended for more characterization of pure forms of the identified diterpenes as well as evaluating their bioactivity either solely or synergistically.

White Tip Silver Needle (Slightly Fermented White Tea) Flavonoids Help Prevent Aging via Antioxidative and Anti-Inflammatory Effects.

AIM: White tip silver needle, a slightly fermented white tea, is abundant in flavonoids, and it has great significance in terms of D-galactose/lipopolysaccharide-induced aging in mice. METHODS: We analyzed the antioxidant capacity of white tip silver needle flavonoids (WTSNF) in vitro, assessed the effects of WTSNF on organ indexes, pathological changes, liver function indexes, biochemical indicators, molecular biological indicators, and genes related to oxidation and inflammation. RESULTS: Ultra-high performance liquid chromatography-tandem mass spectrometry results showed that WTSNF contained baicalin, kaempferol, kaempferide, quercetin, isorhamnetin, lespenephryl, and rutin. WTSNF showed strong scavenging ability for both 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) free radicals. Pathological analysis results showed that WTSNF reduced liver, kidney, and lung damage in mice with induced aging. In the serum and liver tissue, WTSNF effectively increased the antioxidant-related levels of superoxide dismutase, catalase, glutathione peroxidase, glutathione, and total antioxidant capacity and reduced the levels of aspartate aminotransferase, alanine aminotransferase, malondialdehyde and nitric oxide. WTSNF also reduced the inflammation-related levels of interleukin-6, interleukin-1 beta, tumor necrosis factor alpha (TNFα), and interferon gamma (IFN-γ) and increased the levels of interleukin-10 and interleukin-12. Furthermore, WTSNF upregulated the mRNA expression levels of cupro-zinc superoxide dismutase, manganese superoxide dismutase, catalase, glutathione peroxidase, interleukin-10, neuronal nitric oxide synthase, endothelial nitric oxide synthase, nuclear factor erythroid 2-related factor, heme oxygenase 1, NAD(P)H dehydrogenase [quinone] 1, nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha (IκB-α), and thioredoxin, while it downregulated the mRNA expression levels of interleukin-6, interleukin-18, interleukin-1 beta, TNFα, IFN-γ, inducible nitric oxide synthase, cyclooxygenase-2, and nuclear factor kappa-light chain-enhancer of activated B cells (NF-κB). CONCLUSION: WTSNF is a high-quality natural product with antioxidative and anti-inflammatory properties that can inhibits D-galactose/lipopolysaccharide-induced aging in mice.

Comparison of the Phytochemical Properties, Antioxidant Activity and Cytotoxic Effect on HepG2 Cells in Mongolian and Taiwanese Rhubarb Species.

The Mongolian rhubarb-Rheum undulatum L. (RU)-and Rumex crispus L. (RC)-a Taiwanese local rhubarb belonging to the family of Polygonaceae-are principal therapeutic materials in integrative medicine due to their rich quantities of bioactive compounds; however, their phytochemical and antioxidant properties, and anti-cancer activity is poorly investigated. Furthermore, the phytochemical characteristics of both species may be affected by their different geographical distribution and climatic variance. The current study aimed to compare RU with RC extracts in different polarity solvents (n-hexane, ethyl acetate, acetone, ethanol, and water) for their phytochemical contents including the total phenolic content (TPC), total anthraquinone content (TAC), total flavonoid content (TFC), antioxidant and free radical scavenging capacities, and anticancer ability on the HepG2 cell. Except for the n-hexane extract, all of the RU extracts had considerably higher TPCs than RC extracts, ranging from 8.39 to 11.16 mg gallic acid equivalent (GAE) per gram of dry weight, and the TPCs of each extract were also significantly correlated with their antioxidant capacities by ABTS, DPPH, and FRAP assays (p < 0.05). Moreover, there was no remarkable association between the antioxidant capacities and either TACs or TFCs in both the RU and RC extracts. Besides, high-performance liquid chromatography (HPLC) analysis revealed that both the RU and RC extracts contained chrysophanol, emodin, and physcion, and those bioactive compounds were relatively higher in the n-hexane solvent extracts. Additionally, we observed different levels of dose-dependent cytotoxic effects in all the extracts by cell viability assay. Notably, the ethanol extract of RU had a compelling cytotoxic effect with the lowest half-maximum inhibition concentration (IC50-171.94 ± 6.56 µg/mL at 48 h) among the RU extracts than the ethanol extract of RC. Interestingly, the ethanol extract of RU but not RC significantly induced apoptosis in the human liver cancer cell line, HepG2, with a distinct pattern in caspase-3 activation, resulting in increased PARP cleavage and DNA damage. In summary, Mongolian Rhubarb, RU, showed more phytochemical contents, as well as a higher antioxidant capacity and apoptotic effect to HepG2 than RC; thus, it can be exploited for the proper source of natural antioxidants and liver cancer treatment in further investigation.