Pulp or Peel? Comparative Analysis of the Phytochemical Content and Selected Cosmetic-Related Properties of Annona cherimola L., Diospyros kaki Thumb., Cydonia oblonga Mill. and Fortunella margarita Swingle Pulp and Peel Extracts.

Fruit peels might be a valuable source of active ingredients for cosmetics, leading to more sustainable usage of plant by-products. The aim of the study was to evaluate the phytochemical content and selected biological properties of hydroglycolic extracts from peels and pulps of Annona cherimola, Diospyros kaki, Cydonia oblonga, and Fortunella margarita as potential cosmetic ingredients. Peel and pulp extracts were compared for their antiradical activity (using DPPH and ABTS radical scavenging assays), skin-lightening potential (tyrosinase inhibitory assay), sun protection factor (SPF), and cytotoxicity toward human fibroblast, keratinocyte, and melanoma cell lines. The total content of polyphenols and/or flavonoids was significantly higher in peel than in pulp extracts, and the composition of particular active compounds was also markedly different. The HPLC-MS fingerprinting revealed the presence of catechin, epicatechin and rutoside in the peel of D. kaki, whereas kaempferol glucoside and procyanidin A were present only in the pulp. In A. cherimola, catechin, epicatechin and rutoside were identified only in the peel of the fruit, whereas procyanidins were traced only in the pulp extracts. Quercetin and luteolinidin were found to be characteristic compounds of F. margarita peel extract. Naringenin and hesperidin were found only in the pulp of F. margarita. The most significant compositional variety between the peel and pulp extracts was observed for C. oblonga: Peel extracts contained a higher number of active components (e.g., vicenin-2, kaempferol rutinoside, or kaempferol galactoside) than pulp extract. The radical scavenging potential of peel extracts was higher than of the pulp extracts. D. kaki and F. margarita peel and pulp extracts inhibited mushroom and murine tyrosinases at comparable levels. The C. oblonga pulp extract was a more potent mushroom tyrosinase inhibitor than the peel extract. Peel extract of A. cherimola inhibited mushroom tyrosinase but activated the murine enzyme. F. margarita pulp and peel extracts showed the highest in vitro SPF. A. cherimola, D. kaki, and F. margarita extracts were not cytotoxic for fibroblasts and keratinocytes up to a concentration of 2% (v/v) and the peel extracts were cytotoxic for A375 melanoma cells. To summarize, peel extracts from all analyzed fruit showed comparable or better cosmetic-related properties than pulp extracts and might be considered multifunctional active ingredients of skin lightening, anti-aging, and protective cosmetics.

An opportunity for acerola pulp (Malpighia emarginata DC) valorization evaluating its performance during the block cryoconcentration by physicochemical, bioactive compounds, HPLC-ESI-MS/MS, and multi-elemental profile analysis.

The present study evaluated the effect of cryoconcentration of pulp blocks of acerola (Malpighia emarginata DC). The study evaluated cryoconcentration in three stages. The cryoconcentrated samples, the ice fractions, and the initial pulp were evaluated for physicochemical composition, bioactive composition, and multielement profile. The cryoconcentrated sample obtained in the third stage of cryoconcentration showed the best results for the concentration factor, process efficiency, total soluble solids content, red color intensity, and increasing of the macro and micronutrients: Cu, Ca, S, Sr, K, Mn, Na, P, Mg, Fe. All stages presented good performance in the total soluble solids content, increase in the titratable acidity of the concentrates, and progressive increase in the intensity of the red color. Generally, higher levels of total phenolic and antioxidant activity were found for the 2nd and 3rd concentrates. The phenolic activity showed an increase of 166.90% in the 3rd stage concentrate compared to fresh pulp, and the antioxidant activity was 112.10% by the ABTS method and 131.60% by the DPPH method, both in the 3rd stage concentrate. The major individual polyphenols were Ferulic acid, Protocatechuic acid, and Taxifolin, with significant increases in the concentration of the compounds in the 2nd and 3rd stage concentrates. In addition, the contents of potentially toxic metals were below detection limits. During the cryoconcentration process, there was a decrease in the values ​​of vitamin C content, moisture content, density, and elements Cu, Sr, and Zn.

Bioactive agents from Parkia biglobosa (Jacq.) R.Br. ex G. Don bark extracts for health promotion and nutraceutical uses.

BACKGROUND: Parkia biglobosa stem bark extracts were prepared using methanol, methanol 80%, water and ethyl acetate to investigate their phytochemical contents, as well as antioxidant and enzyme inhibitory properties. RESULTS: Liquid chromatography (LC) quadrupole time-of-flight mass spectrometry (MS) and LC-MSn revealed the presence of flavonoids, hydroxycinnamic acid derivatives and gallotannins. Particularly, the water extract contained rutin (480 µg per 100 mg) and 3-caffeoylquinic acid (1109 µg per 100 mg) in higher amounts, whereas the 80% methanol extract contains methoxyluteolin-7-O-rutinoside and catechin derivatives as major compounds. Total phenolic and flavonoid contents of the extracts were yielded in the range of 32.26-119.88 mg gallic acid equivalents g-1 and 0.60-2.39 mg rutin equivalents g-1 , respectively. Total antioxidant capacity was also displayed in the range of 0.53-6.34 mmol Trolox equivalents (TE) g-1 . Both the methanolic extracts showed higher total antioxidant capacity that could be related to the total phenolic contents. Radical scavenging capacity in DPPH (2,2-diphenyl-2-picryl-hydrazyl) (37.21-508.30 mg TE g-1 ) and ABTS [2,2-azinobis(3-ethylbenzothiazoline- 6-sulfonic acid)] (60.95-1068.06 mg TE g-1 ) assays, reducing power in cupric ion reducing antioxidant capacity (54.23-1002.78 mg TE g-1 ) and ferric ion reducing antioxidant power (33.18-558.68 mg TE g-1 ) assays, as well as metal chelating activity (2.45-11.28 mg EDTA equivalents g-1 ), were exhibited by all extracts. All extracts were found to inhibit acetylcholinesterase [0.23-2.47 mg galanthamine equivalents (GALAE) g-1 ], tyrosinase [27.20-83.33 mg kojic acid equivalents g-1 ], amylase [mmol acarbose equivalents (ACAE) g-1 ]. On the other hand, all extracts, except the water extract, inhibited butyrylcholinesterase (5.38-6.56 mg GALAE g-1 ), whereas only the water and ethyl acetate extract showed glucosidase inhibitory potential (1.96 and 1.82 mmol ACAE g-1 ). In general, the water extract was found to be a weaker enzyme inhibitor suggesting that water is not the preferrable extraction solvent to obtain active products. CONCLUSION: The present study demonstrated that the stem bark extracts of P. biglobosa contains good amount of phytochemical and extracts present significant antioxidant, as well as reasonable enzyme inhibitory effects. Hence, these findings suggest that further studies can be performed on more specific biological targets and models of bioactivity to determine their safe usage as a nutraceutical or for the preparation functional foods. © 2023 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Comparative Analysis of Polyphenols in Lycium barbarum Fruits Using UPLC-IM-QTOF-MS.

Variety, geographical origin, and harvest season are important factors affecting the accumulation of polyphenols in Lycium barbarum. In this study, the effects of these factors on the polyphenolic components of this species were analyzed using ultra-performance liquid chromatography ion mobility quadrupole time-of-flight mass spectrometry. Moreover, the in vitro antioxidant activities of fruit extracts from this species were evaluated. The total polyphenolic contents of L. barbarum fruits from Jinghe County in Xinjiang and Zhongning County in Ningxia were 5.52-11.72 and 7.06-9.37 mg (gallic acid equivalent)/g dry weight, while the total flavonoid contents of L. barbarum fruits from these regions were 12.52-30.29 and 12.67-20.77 mg (rutin equivalent)/g dry weight, respectively. Overall, 39 types of polyphenols were identified in the fruit extracts, including 26 flavonoids, 10 phenolic acids, and three tannins. Of these, 11 polyphenols were quantitatively analyzed, which revealed rutin to be the most dominant polyphenolic component in fruits from Jinghe and Zhongning. There were significant differences (p < 0.05) in the polyphenolic contents and antioxidant activities of L. barbarum fruit extracts, depending on the geographical origin, variety, and harvest season. The antioxidant activity of this species was found to be significantly positively correlated with the polyphenolic contents. This study provided scientific guidance for comprehensive applications of polyphenols from different varieties of L. barbarum from separate geographical origins.

Phytochemical profile analysis by LC-ESI-MSn and LC-HR-ESI-MS and validated HPLC method for quantification of rutin in herbal drug and products from leaves of Croton blanchetianus.

Phytochemical analysis of Croton blanchetianus leaves was performed by. After that, a high performance liquid chromatography method was developed and validated for the determination of rutin in herbal drug and products of C. blanchetianus. The separation was achieved on a C18 column, and the mobile phase was composed of ultrapure water and methanol (acidified with trifluoroacetic acid) with a gradient of 0.8 ml/min. The method was validated following international guidelines. The chemical analysis revealed the presence of flavonoids. Among them rutin was used as the standard for validation. In the HPLC the presence of rutin was observed at 24.7 min. The method was robust, with no significant variations, and linear in the range evaluated with R2 > 0.99. Regarding the matrix effect, it was possible to prove the absence of interference of the constituents in the herbal drug. The precision was determined with a relative standard deviation of <1.34%. The recovery results were achieved between 89.29 and 101.21%. Furthermore, with partial validation, the method was proved to be suitable for the liquid extract, dry extract and effervescent granules. Therefore, this study demonstrated that the method is effective for the quality control analysis of C. blanchetianus leaves and products.

Bioactive Compounds, Antioxidant Activities, and HPLC Analysis of Nine Edible Sprouts in Cambodia.

The non-nutritional health benefits of sprouts are unconfirmed. Thus, nine sprout methanolic extracts were tested for phytoconstituents and antioxidant activity. The TPC, TCC, TFC, TAC, and TALC were measured. ABTS and DPPH radical scavenging and ferric-reducing antioxidant power assays were used to assess the antioxidant activity. HPLC detected gallic acid, vanillin, syringic acid, chlorogenic acid, caffeic acid, and rutin in the extracts. The sprout extracts contained six compounds, with caffeic acid being the most abundant. Gallic acid, syringic acid, chlorogenic acid, caffeic acid, vanillin, and rutin were highest in soybean, black sesame, mustard, sunflower, white radish, and black sesame sprouts, respectively. Sunflower sprouts had the highest level of TCC while soybean sprouts had the highest level of TFC, Taiwanese morning glory had the highest level of TPC, mustard sprouts had the highest level of TALC, and black sesame sprouts had the highest level of TAC. Taiwanese morning glories scavenged the most DPPH and ABTS radicals. Colored and white radish sprouts had similar ferric-reducing antioxidant power. Antioxidation mechanisms varied by compound. Our findings demonstrated that sprouts have biological effects, and their short time for mass production offers an alternative food source for health benefits, and that they are useful for future research development of natural products and dietary supplements.

Haskap Berry Leaves (Lonicera caerulea L.)-The Favorable Potential of Medical Use.

The presented research evaluates the medical use potential of Lonicera caerulea leaves, which are waste plants in cultivating berries. The study's screening activity included the leaves of five varieties of Lonicera caerulea: Atut, Duet, Wojtek, Zojka, and Jugana. The microbiological analysis confirmed the safety of using Lonicera caerulea leaves without significant stabilization. Lonicera caerulea leaves standardization was carried out based on the results of the chromatographic analysis, and it showed differences in the contents of active compounds (loganic, chlorogenic and caffeic acids, and rutin), which are attributed to biological activity. For the Lonicera caerulea leaves varieties tested, the differences in the content of total polyphenol content, chlorophylls, and carotenoids were also confirmed. The screening of biological activity of five Lonicera caerulea leaf varieties was carried out concerning the possibility of inhibiting the activity of α-glucosidase, lipase, and hyaluronidase as well, and the antioxidant potential was determined. The defined profile of the biological activity of Lonicera caerulea leaves makes it possible to indicate this raw material as an essential material supporting the prevention and treatment of type II diabetes. However, this research showed that tested enzymes were strongly inhibited by the variety Jugana. The health-promoting potential of Lonicera caerulea leaves was correlated with the highest chlorogenic acid and rutin content in the variety Jugana.

Polyphenolic Characterization, Antioxidant, Antihyaluronidase and Antimicrobial Activity of Young Leaves and Stem Extracts from Rubus caesius L.

Fruits are the main food part of the European dewberry (Rubus caesius L.), known as a source of polyphenols and antioxidants, while very little attention is paid to leaves and stems, especially young first-year stems. The purpose of this work was to analyze for the first time water and ethanol extracts obtained from young, freshly developed, leaves and stems of the European dewberry to determine their antioxidant and biological activity, whereas most of the papers describe biological properties of leaves collected during summer or autumn. As the phytochemical profile changes during the growing season, the quantitative and qualitative content of flavonoid glycosides and flavonoid aglycones was analyzed using reversed phase liquid chromatography/electrospray ionization triple quadrupole mass spectrometry (LC-ESI-MS/MS) with multiple reaction monitoring (MRM). The ability to inhibit hyaluronidase as well as antioxidant activity (2,2 diphenyl-1-picrylhydrazyl: DPPH and ferric antioxidant power: FRAP) were estimated. Extracts were also analyzed against Gram-positive and Gram-negative bacteria. The results of the qualitative phytochemical analysis indicated the presence of flavonoid aglycones and flavonoid glycosides, with the highest amount of tiliroside, hyperoside, isoquercetin, astragalin, rutin and catechin in ethanol extracts. DPPH and FRAP tests proved the high antioxidant activity of the extracts from leaves or stems and the antihyaluronidase assay revealed for the first time that water and ethanol extracts obtained from the stems exhibited the ability to inhibit hyaluronidase activity resulting in an IC50 of 55.24 ± 3.21 and 68.7 ± 1.61 µg/mL, respectively. The antimicrobial activity has never been analyzed for European dewberry and was the highest for Clostridium bifermentans and Clostridium sporogenes-anaerobic sporulation rods as well as Enterococcus faecalis for both water and ethanol extracts.

An Examination of the Effect of Rutin against Neurotoxicity Induced by Ciprofloxacin Antibiotic in Wistar Rats.

Rutin is a citrus flavonoid that exists in different types of food, such as fruits, tea, as well as vegetables, and is considered a natural antioxidant. This study aimed to investigate the therapeutic role of Rutin in oxidative stress-induced in Wistar rats exposed to Ciprofloxacin (CPX). The study included 36 healthy adult Wistar rats, which were randomly divided into six groups (n=6). The control group (C) received normal drinking water for 20 days. The first treatment group (T1) received Rutin at a dose of 50 mg/kg of b.w for 20 days. The second treatment group (T2) received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days. The third treatment group (T3) received Rutin at a dose of 50 mg/kg of b.w for 20 days, and afterward, they received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days. The fourth treatment group (T4) received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days, and then, they received Rutin at a dose of 50 mg/kg of b.w for 20 days. The fifth treatment group (T5) received CPX antibiotic at a dose of 14 mg/ kg of b.w and Rutin at a dose of 50 mg/ kg of b.w together for 20 days. All the treatments were administrated by oral gavage. Analysis of the recorded data showed a significant increase (P<0.05) in the concentration of Methylenedioxyamphetamine (MDA) in the T2 group, compared to the other groups. The MDA level significantly (P<0.05) increased in the T3 group (2.29±0.04), compared to the C (1.71±0.01), T1 (1.54±0.04), T4 (1.18±0.02), and T5 (1.29±0.03) groups. However, there were no significant differences (P<0.05) between the C (1.71±0.01) and T1 (1.54±0.04) groups, as well as the T4 (1.18±0.02) and T5 (1.29±0.03) groups with regards to the MDA. The results clarified a significant increase (P<0.05) in the antioxidant activity, Glutathione (GSH), Superoxide dismutase (SOD), and Catalase (CAT) contents in the T1 group, determined at 5.91±0.26, 5.78±0.02, and 1.98±0.05, respectively, compared to the other groups. The lowest antioxidant activity, GSH, SOD, and CAT contents were recorded in the T2 group, in comparison with the other groups (P<0.05). The findings revealed that the level of SOD, GSH, and CAT in the T4 and T5 groups significantly (P<0.05) increased, compared to the T2 and T3 groups. Histological examination of the slides obtained from the brain demonstrated that in the T2 group, some histopathological changes were observed, compared to the C, T1, T4, and T5 groups. These changes were as follows: 1) damaged and clear blood vessel congestion with the deposition of fibrous networks, 2) brain edema, 3) multiple necrotic foci, 4) accumulation of neutrophils, and 5) simple histopathological changes in the brain of animals in the T2 group, compared to the other groups. It is, therefore, concluded that Rutin supplementation at a dose of 50 mg/kg b.w can be the most appropriate dose in protecting brain tissue against tissue damages caused by CPX.

HPLC-DAD profile of phenolic compounds and In vitro antioxidant activity of Ficus carica L. fruits from two Algerian varieties.

Ficus carica L., commonly known as the fig tree, is a plant belonging to the Moraceae family whose fruits are traditionally used for edible and therapeutic purposes. The study aimed to investigate the lyophilized aqueous extracts of two native Algerian fig varieties, azendjar (Az) and taamriouth (Ta), as a potential source of antioxidant compounds for possible use as ingredients in pharmaceuticals or nutraceuticals. The HPLC-DAD analysis revealed the presence of two phenolic acids (3,4-dihydroxybenzoic acid and vanillic acid) and two flavonoids (rutin and quercetin) at levels 3.67, 4.80, 84.16, and 6.87 µg/g respectively for Az variety extract, and 6.90, traces, 7.46 and 3.37 µg/g respectively for Ta variety extract. Total phenolic content was determined using the Folin-Ciocalteu method at levels 951.06 ± 61.08 and 730.88 ± 45.25 GAE mg/100 g of the dry extract. In contrast, the total flavonoid content was determined using Christ-Müller's method at levels 428.34 ± 15.42 and 307.63 ± 7.94 QE mg/100 g of dry extract in the Az and Ta varieties, respectively. The total polyphenolic content of the extract may be responsible for its antioxidant action. The gathered results indicate that the extracts from the dark peel fig variety - azendjar, are characterized by a higher content of phenolic and flavonoid compounds and antioxidant activity than the extract from the light peel variety - taamriouth. In conclusion, the conducted studies and in vitro assays indicate that the studied extracts are a source of natural antioxidants and can be considered functional raw materials for producing food supplements and pharmaceuticals.

Phenolics from Defatted Black Cumin Seeds (Nigella sativa L.): Ultrasound-Assisted Extraction Optimization, Comparison, and Antioxidant Activity.

An ultrasound-assisted method was used for the extraction of phenolics from defatted black cumin seeds (Nigella sativa L.), and the effects of several extraction factors on the total phenolic content and DPPH radical scavenging activity were investigated. To improve the extraction efficiency of phenolics from black cumin seed by ultrasonic-assisted extraction, the optimal extraction conditions were determined as follows: ethanol concentration of 59.1%, extraction temperature of 44.6 °C and extraction time of 32.5 min. Under these conditions, the total phenolic content and DPPH radical scavenging activity increased by about 70% and 38%, respectively, compared with conventional extraction. Furthermore, a complementary quantitative analysis of individual phenolic compounds was carried out using the HPLC-UV technique. The phenolic composition revealed high amounts of epicatechin (1.88-2.37 mg/g) and rutin (0.96-1.21 mg/g) in the black cumin seed extracts. Ultrasonic-assisted extraction can be a useful extraction method for the recovery of polyphenols from defatted black cumin seeds.

Exploring the Palynological, Chemical, and Bioactive Properties of Non-Studied Bee Pollen and Honey from Morocco.

Bee products are known for their beneficial properties widely used in complementary medicine. This study aims to unveil the physicochemical, nutritional value, and phenolic profile of bee pollen and honey collected from Boulemane-Morocco, and to evaluate their antioxidant and antihyperglycemic activity. The results indicate that Citrus aurantium pollen grains were the majority pollen in both samples. Bee pollen was richer in proteins than honey while the inverse was observed for carbohydrate content. Potassium and calcium were the predominant minerals in the studied samples. Seven similar phenolic compounds were found in honey and bee pollen. Three phenolic compounds were identified only in honey (catechin, caffeic acid, vanillic acid) and six phenolic compounds were identified only in bee pollen (hesperidin, cinnamic acid, apigenin, rutin, chlorogenic acid, kaempferol). Naringin is the predominant phenolic in honey while hesperidin is predominant in bee pollen. The results of bioactivities revealed that bee pollen exhibited stronger antioxidant activity and effective α-amylase and α-glycosidase inhibitory action. These bee products show interesting nutritional and bioactive capabilities due to their chemical constituents. These features may allow these bee products to be used in food formulation, as functional and bioactive ingredients, as well as the potential for the nutraceutical sector.

Integration of Metabolomics and Transcriptomics Reveal the Mechanism Underlying Accumulation of Flavonols in Albino Tea Leaves.

Albino tea plants (Camellia sinensis) have been reported to possess highly inhibited metabolism of flavonoids compared to regular green tea leaves, which improves the quality of the tea made from these leaves. However, the mechanisms underlying the metabolism of catechins and flavonols in albino tea leaves have not been well elucidated. In this study, we analyzed a time series of leaf samples in the greening process from albino to green in a thermosensitive leaf-color tea mutant using metabolomics and transcriptomics. The total content of polyphenols dramatically decreased, while flavonols (such as rutin) were highly accumulated in albino leaves compared to in green leaves. After treatment with increasing environment temperature, total polyphenols and catechins were increased in albino mutant tea leaves; however, flavonols (especially ortho-dihydroxylated B-rings such as rutin) were decreased. Meanwhile, weighted gene co-expression network analysis of RNA-seq data suggested that the accumulation of flavonols was highly correlated with genes related to reactive oxygen species scavenging. Histochemical localization further demonstrated that this specific accumulation of flavonols might be related to their biological functions in stress tolerance. These findings suggest that the temperature-stimulated accumulation of total polyphenols and catechins in albino mutant tea leaves was highly induced by enhanced photosynthesis and accumulation of its products, while the initial accumulation and temperature inhibition of flavonols in albino mutant tea leaves were associated with metabolism related to oxidative stress. In conclusion, our results indicate that the biosynthesis of flavonoids could be driven by many different factors, including antioxidation and carbon skeleton storage, under favorable and unfavorable circumstances, respectively. This work provides new insights into the drivers of flavonoid biosynthesis in albino tea leaves, which will further help to increase tea quality by improving cultivation measures.

Analysis of Citrus Bioflavonoid Content and Dipeptidyl Peptidase-4 Inhibitory Potential of Commercially Available Supplements.

Citrus bioflavonoids are polyphenolic plant-derived pigments found in high levels in oranges, lemons, grapefruits and other citrus fruits. The three most abundant types of citrus bioflavonoids are hesperidin, naringenin and eriocitrin. Citrus bioflavonoids have long been known to possess powerful free radical-scavenging properties and cardioprotective effects. The study involved the analysis of 10 commercially available citrus bioflavonoid supplements from three different countries: Australia, the United States and Canada. The supplements were tested for their citrus bioflavonoid content which varied from 0.8 to 33.3% w/w. The daily bioflavonoid dose varied from 19 mg to 560 mg. Hesperidin was the major citrus bioflavonoid in nine out of ten supplements. One supplement was found to contain less than 10% of the quantity of rutin claimed to have been added. The DPP-4 inhibitory potential, compared through an estimation of rutin equivalence, ranged from 1.9 mg to 400 mg per day. This data highlights the variability between the supplements in their potential to inhibit DPP-4 for subsequent health benefits.

Ultrasensitive electrochemical sensor for detection of rutin antioxidant by layered Ti3Al0.5Cu0.5C2 MAX phase.

MAX phases have attracted great attention due to unique features such as thermal and electrical conductivity, easy fabrication, heat resistant, and lightweight. In this study, an easy and green method was employed to successfully develop a Ti3Al0.5Cu0.5C2 MAX phase structure, and a Ti3Al0.5Cu0.5C2 based glassy carbon electrode (GCE) was applied for the electrochemical determination of rutin antioxidants in mandarin and kiwi samples. The developed Ti3Al0.5Cu0.5C2 MAX phase was characterized by different techniques such as X-ray photoelectron spectroscopy (XPS), thermogravimetry and differential scanning calorimetry (TG-DSC), X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET), diffuse reflectance spectroscopy (DRS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM) to obtain information on the structural and morphological properties. Electrochemical methods such as cyclic voltammetry (CV) and differential pulse voltammetry (DPV) were employed for the determination of rutin using Ti3Al0.5Cu0.5C2/GCE. The GCE modified with Ti3Al0.5Cu0.5C2 demonstrated amplified electrochemical response (ca. 4.25 times) in comparison to the bare GCE towards rutin, and exhibited ultra-sensitivity and selectivity in the presence of other interfering antioxidants. Under the optimum conditions, good linearity in the range of 0.02-50.00 µmol L-1 was obtained for rutin analysis by the Ti3Al0.5Cu0.5C2-based sensor with a limit of detection (LOD, 3σ/K) as low as 0.015 µmol L-1. The fabricated Ti3Al0.5Cu0.5C2 MAX phase was applied to determine trace levels of rutin in mandarin and kiwi samples with validation by high-performance liquid chromatography (HPLC), thus highlighting its potential for the electrochemical determination of small molecules in the agricultural field.

Preclinical safety assessment of the crude extract from Sida rhombifolia L. aerial parts in experimental models of acute and repeated-dose 28 days toxicity in rats.

Sida rhombifolia (Malvaceae) is popularly used as a treatment for several pathological conditions; however, there is a lack of studies that identify its compounds and that evaluate comprehensively the safety of its consumption. Therefore, the aim of this study was to determinate the phytochemical constitution of the crude extract of Sida rhombifolia (CESR), and its safety in models of acute and repeated doses (28 days) toxicity. The tested dose for the model of acute toxicity was 2000 mg/kg doses for the repeated dose model were 150, 300 e 600 mg/kg. Hematological, biochemical, histopathological and oxidative markers were investigated. HPLC-DAD-MS analysis evidenced the presence of caffeic acid, coumarin, and rutin. In the acute toxicity model the only altered parameters were tissue ROS, and AST and BUN in serum. As for the repeated dose experiment both hematological and biochemical markers remained within the values of reference for the species. Obtained results demonstrate that the CESR did not present significant toxic effects when administrated orally to male and female rats in acute and repeated doses.

Novel insights on the multi-functional properties of flavonol glucosides from red onion (Allium cepa L) solid waste - In vitro and in silico approach.

Flavonol glucosides was extracted from red onion solid waste (ROSW) and multi-functional properties were determined to develop alternative strategy for therapeutic beneficiation and utilisation as functional food. The major flavonol glucosides extracted from ROSW were confirmed as quercetin-3, 4'-O-diglucoside (QDG), quercetin-3-O-glucoside (isoquercetin), quercetin-4'-O-glucoside (spiraeoside), isorhamnetin- 4'-glucoside (IMG), quercetin glycoside (QG), and quercetin (Q) using a combination of chromatographic, spectroscopic and scientific literature data. The ROSW solvent fractions and extracted flavonol glucosides showed significant antioxidant effect with DPPH, ABTS, FRAP, and ORAC radical scavenging assays. The in vitro and in silico study revealed that the QG, QDG, isoquercetin, and spiraeoside from ROSW exhibited potent α-glucosidase, tyrosinase and xanthine oxidase enzyme inhibitory activity. In addition, QG, QDG, isoquercetin, and spiraeoside showed potent anticancer effect on HeLa cancer lines. Considering these results, the utilization of ROSW and their flavonol glucosides might be helpful for developing potential antioxidant, anticancer and enzyme inhibitory agents.

Network pharmacology for the identification of phytochemicals in traditional Chinese medicine for COVID-19 that may regulate interleukin-6.

OBJECTIVE: ´Three formulas and three medicines,' namely, Jinhua Qinggan Granule, Lianhua Qingwen Capsule, Xuebijing Injection, Qingfei Paidu Decoction, HuaShi BaiDu Formula, and XuanFei BaiDu Granule, were proven to be effective for coronavirus disease 2019 (COVID-19) treatment. The present study aimed to identify the active chemical constituents of this traditional Chinese medicine (TCM) and investigate their mechanisms through interleukin-6 (IL-6) integrating network pharmacological approaches. METHODS: We collected the compounds from all herbal ingredients of the previously mentioned TCM, but those that could down-regulate IL-6 were screened through the network pharmacology approach. Then, we modeled molecular docking to evaluate the binding affinity between compounds and IL-6. Furthermore, we analyzed the biological processes and pathways of compounds. Finally, we screened out the core genes of compounds through the construction of the protein-protein interaction network and the excavation of gene clusters of compounds. RESULTS: The network pharmacology research showed that TCM could decrease IL-6 using several compounds, such as quercetin, ursolic acid, luteolin, and rutin. Molecular docking results showed that the molecular binding affinity with IL-6 of all compounds except γ-aminobutyric acid was < -5.0 kJ/mol, indicating the potential of numerous active compounds in TCM to directly interact with IL-6, leading to an anti-inflammation effect. Finally, Cytoscape 3.7.2 was used to topologize the biological processes and pathways of compounds, revealing potential mechanisms for COVID-19 treatment. CONCLUSION: These results indicated the positive effect of TCM on the prevention and rehabilitation of COVID-19 in at-risk people. Quercetin, ursolic acid, luteolin, and rutin could inhibit COVID-19 by down-regulating IL-6.

Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography.

Yanghe decoction is a traditional Chinese medicine prescription and has been used for breast cancer treatment for many years. However, the effective ingredients in the decoction have not been identified. The expression of poly(ADP-ribose) polymerase-1 is highly related to breast cancer. Using poly(ADP-ribose) polymerase-1 as a probe, we expressed the haloalkane dehalogenase-tagged protein in BL21(DE3) E. coli, immobilized it on hexachlorocaproic acid-modified macroporous silica gel, and established a poly(ADP-ribose) polymerase-1 chromatographic model. The feasibility of the model was verified by testing the retention behaviors of five drugs on the protein column. We applied the model in screening the bioactive components in yanghe decoction. Rutin, liquiritin, and a compound ([M-H]- 681.7) were identified to be the potential bioactive ingredients. We studied the binding property between rutin and poly(ADP-ribose) polymerase-1 by injection amount dependent method, competitive studies, and molecular docking. We found that rutin can bind to the protein through the typical inhibitor binding site of the protein. Therefore, the chromatographic model is a useful tool to screen bioactive compounds from traditional Chinese medicine. The method is fast, reliable, and applicable to other functional proteins that can screen the potential lead compounds for the treatment of the related diseases.

Phenolic compounds from Nerium oleander leaves: microwave assisted extraction, characterization, antiproliferative and cytotoxic activities.

A microwave-assisted extraction (MAE) method was used for the extraction of phenolic compounds from Nerium oleander leaves. The influence of variables such as ethanol concentration, microwave power, irradiation time and liquid/solid ratio on polyphenol extraction was modelled using a second-order regression equation based on response surface methodology (RSM). The optimal conditions for MAE were: extraction solvent 35% ethanol concentration, 500 W microwave power, 60 s irradiation time and a solvent/material ratio of 20 mL g-1. Under optimal MAE conditions, the recovery of TPC was 25.752 mg GAE per g dw. 19 compounds have been identified by HPLC-ESI-MS/MS analysis; the main compounds identified were chlorogenic acid, rutin and quinic acid esters, such as caffeoylquinic acids and dicaffeoylquinic acids. Additionally, the optimized extract demonstrated potential to inhibit HT29 colorectal cancer cell growth (EC50 = 2.432 µg mL-1) without presenting cytotoxicity in confluent Caco-2 cells, a model of human intestinal epithelium. These results supply new information about the phenolic composition of Nerium oleander leaves and their antiproliferative effect.