Polyphenol-rich Fraction Research Articles

Polyphenolic rich fraction of Physalis peruviana calyces and its nano emulsion induce apoptosis by caspase 3 up-regulation and G2/M arrest in hepatocellular carcinoma

Phytocompounds found in fruit wastes serve as nature's precious gift to humans in cancer treatment. In this context, the present work aimed to use of Physalis peruviana calyces (PPC) and its nano-emulsion as a novel method in hepatocellular carcinoma treatment. PPC butanolic fraction (PPCBF) was prepared and tested for its total phenol, total flavonoids, and HPLC analysis for phenolics, as well as the in vitro anticancer activity for both normal and nano-emulsion was evaluated. Twenty-four male Sprague-Dawley rats were used; 18 rats were administered intraperitoneally diethylnitrosamine (DEN) once (200 mg/kg body weight) in a saline solution. All nutritional parameters, biochemical parameters, and histopathological examinations were assessed. Results revealed that PPCBF and its nano-emulsion showed high anti-HepG2 activity and induced Pre-G1 apoptosis and cell cycle arrest (G2/M phase). Moreover, PPCBF and its nano-emulsion caused up-regulation of caspase-3 mRNA in HepG2, which could indicate that the intrinsic mitochondrial route triggered apoptosis. All the nutritional and biochemical changes were confirmed by histopathological examination. In conclusion, PPC and its nano-emulsion could be serving as a successful and effective drug from waste with a bright future in the treatment of hepatocellular carcinoma (HCC).

Melaleuca rugulosa (Link) Craven Tannins: Appraisal of anti-inflammatory, radical scavenging activities, and molecular modeling studies

Ethnopharmacological relevanceGenus Melaleuca or tea tree species are well known to be an important source of biological active oils and extracts. The biological significance appears in their usage for treatment of several clinical disorder owing to their traditional uses as anti-inflammatory, antibacterial, antifungal, and cytotoxic activities.Aim of the study: Our study aimed to investigate the metabolic profile of the M. rugulosa polyphenol-rich fraction along with determination of its anti-inflammatory potential, free radical scavenging and antiaging activities supported with virtual understanding of the mode of action using molecular modeling strategy. Materials and methodsThe anti-inflammatory activity of the phenolic rich fraction was investigated through measuring its inhibitory activity against inflammatory mediators viz tumor necrosing factor receptor-2 (TNF-α) and cyclooxygenases 1/2 (COX-1/2) in a cell free and cell-based assays. Moreover, the radical scavenging activity was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), oxygen radical absorbance capacity (ORAC) and β-carotene assays, while the antiaging activity in anti-elastase, anti-collagenase, and anti-tyrosinase inhibitory assays. Finally, the biological findings were supported with molecular docking study using MOE software. ResultsThe chromatographic purification of the polyphenol-rich fraction of Melaleuca rugulosa (Link) Craven afforded fourteen phytoconstituents (1–14). The anti-inflammatory gauging experiments demonstrated inhibition of inflammatory-linked enzymes COX-1/2 and the TNF-α at low μg/mL levels in the enzyme-based assays. Further investigation of the underlying mechanism was inferred from the quantification of protein levels and gene expression in the lipopolysaccharide (LPS)-activated murine macrophages (RAW264.7) in vitro model. The results revealed the reduction of protein synthesis of COX-1/2 and TNF-α with the down regulation of gene expression. The cell free in vitro radical scavenging assessment of the polyphenol-rich fraction revealed a significant DPPH reduction, peroxyl radicals scavenging, and β-carotene peroxidation inhibition. Besides, the polyphenol-rich fraction showed a considerable inhibition of the skin aging-related enzymes as elastase, collagenase, and tyrosinase. Ultimately, the computational molecular modelling studies uncovered the potential binding poses and relevant molecular interactions of the identified polyphenols with their targeted enzymes. Particularly, terflavin C (8) which showed a favorable binding pose at the elastase binding pocket, while rosmarinic acid (14) demonstrated the best binding pose at the COX-2 catalytic domain. In short, natural polyphenols are potential candidates for the management of free radicals, inflammation, and skin aging related conditions. ConclusionNatural polyphenols are potential candidates for the management of free radicals, inflammation, and skin aging related conditions.

An Innovative, Green Cascade Protocol for Grape Stalk Valorization with Process Intensification Technologies

Valorization of agri-food residues to produce bio-based platform chemicals will enhance the transition to the bio-economy era. To this end, a sustainable process has been developed for the overall valorization of grape stalks (GS) according to a circular approach, starting from the lignin fraction to further deal with the cellulose-rich residue. This non-conventional protocol fully adheres to green chemistry principles, exploiting the so-called enabling technologies—mainly ultrasound and microwaves—for energy-saving innovative processes. Firstly, ultrasound-assisted extraction (UAE, 40 kHz, 200 W) demonstrated to be an excellent technique for GS delignification combined with natural deep eutectic solvents (NaDESs). Delignification enables isolation of the pertinent lignin framework and the potential to obtain a polyphenol-rich liquid fraction, focusing on the valorization of GS as source of bioactive compounds (BACs). Among the NaDESs employed, the combination of choline chloride (ChCl) and levulinic acid (LevA) (ChLevA) presented noteworthy results, enabling a delignification higher than 70%. LevA is one of the top-value biobased platform chemicals. In this work, a flash microwave (MW)-assisted process was subsequently applied to the cellulose-rich fraction remained after delignification, yielding 85% LevA. The regeneration of this starting compound to produce ChLevA can lead to a further biomass delignification cycle, thus developing a new cascade protocol for a full valorization of GS.

In vitro Evaluation of Polyphenol Rich Fraction of Ipomea batatas (Mother delight) Leaf Extract as Anti-inflammatory Agents and its LCMS Profile

High intake of plant foods is associated with lower risk of chronic diseases as suggested by epidemiological evidence. This study aimed to investigate the anti-inflammatory potential of polyphenol rich fraction of Ipomoea batatas leaf extract and the compounds possibly responsible for the activity using LCMS. The anti-inflammatory studies were carried out in vitro by protein denaturation technique. The result shows significant different (p<0.05) percentage inhibition of denaturation 90.59% at 1000 μg/ml of the extract compared to the standard drug (declofenac) 95.12% at 1000 μg/ml. The LCMS profiling of the extract revealed the presence of many metabolites (polyphenols) such as chrogenic acid, myricetin, furocoumarinic acid, aromadendrin, naringenin, 4,5-dicaffeolquinic acid and abietinol among others. The presence of these metabolites could be the reason for the anti-inflammatory effect of the extract observed. This implies that the plant can be exploited for its medicinal, therapeutic properties and possibly used to reduce the risk of many chronic diseases. Keyword: Anti-inflammatory activity, Protein denaturation technique, Mother delight, LCMS, Phytochemicals.

Therapeutic Efficacy of Polyphenol-Rich Fraction of Boesenbergia rotunda in Diabetic Rats: A Focus on Hypoglycemic, Antihyperlipidemic, Carbohydrate Metabolism, Antioxidant, Anti-Inflammatory and Pancreato-Protective Activities.

Boesenbergia rotunda is a famous culinary/medicinal herb native to Southeast Asia region and it is traditionally used in the treatment of several diseases. This study investigated the anti-diabetic properties of Boesenbergia rotunda polyphenol extract (BRE) in high fructose/streptozotocin-induced diabetic rats. The in vitro antioxidant activity was evaluated using DPPH and ABST colorimetric assays, while the Folin-Ciocalteu method was used for the total phenolic content of BRE. For diabetes induction, a combination of high fructose solution and streptozotocin was administered to the rats and diabetic rats were orally administrated with BRE (100 and 400 mg/kg) for 5 weeks. The fasting blood glucose, body weight gain, food and water consumption were determined during the treatment period. BRE showed excellent in vitro DPPH and ABTS scavenging activity with high phenolic content. BRE significantly lowered fasting blood glucose level, HbA1c, lipid profile, hepatorenal biochemical parameters and ameliorated the IPGTT in diabetic rats. Additionally, BRE reversed body weight loss, attenuated food and water intake, serum insulin level, pancreatic β-cell function and pancreatic cell morphology. Furthermore, fructose 1,6 biphosphatase, glucose-6-phosphatase, malondialdehyde (MDA) and proinflammatory cytokines levels were also ameliorated in the BRE-treated diabetic rats, while pancreatic antioxidant enzymes activities (GSH, SOD and CAT) were significantly increased in the treated rats. In conclusion, the results showed that BRE effectively displayed antidiabetic effects and has possible value for antidiabetic oral medication.

Antioxidant and antimicrobial properties of polyphenolics fromWithania adpressa(Coss.) Batt. against selected drug-resistant bacterial strains

AbstractWithania adpressa(Coss.) Batt. (W. adpressa) is a wild medicinal plant in the family Solanaceae, which is used as an alternative medicine. The present study aims to investigate the chemical composition, antioxidant, and antibacterial potentials of polyphenol-rich fraction from the leaves ofW. adpressa. Polyphenol-rich fraction was characterized by use of high-performance liquid chromatography (HPLC). Antioxidant potency was determined by use of 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), and total antioxidant capacity (TAC) assays. Antibacterial activity was assessed against gram-positive and gram-negative bacteria by use of disc diffusion and microdilution assays. Chromatographic analysis by HPLC showed four compounds in the polyphenol-rich fraction including 1-O-Caffeoyl glucose, Luteolin-7-diglucuronide, Apigenin-O-pentoside, and Quercetin-3-O-glucuronide. Polyphenol-rich fraction exhibited important antioxidant activity as assessed by DPPH and FRAP assays, with IC50and EC50values of 14.27 ± 0.43 and 39.48 ± 0.81 µg/mL, respectively, while butylated hydroxytoluene (BHT) and Quercetin exhibited IC50values of 28.92 ± 0.24 and 22.48 ± 0.54 µg/mL. Results of TAC showed that the polyphenol-rich fraction scored 781.74 ± 2.83 µg AAE/mg. Polyphenol-rich fraction showed an important antibacterial effect vs gram-positive and gram-negative strains recording inhibition zone diameters varying from 19.5 to 29.2 mm, while antibiotics were almost ineffective toward all strains except forE. coli. It can be concluded thatW. adpressapolyphenol-rich fraction possesses promising phenols with strong antioxidant and antibacterial properties, which may help fight pathogenic bacteria and free radicals.

Polyphenol-rich Fraction of Terminalia catappa Prevents Chronic Lead Acetate Induced Oxidative Stress and Cardiorenal Toxicities in Rats

Lead (Pb), a naturally occurring environmental contaminant, has been implicated in several pathological conditions of the cardiovascular and renal systems. The study was designed to evaluate the modulatory roles of the polyphenol-rich fraction of Terminalia catappa on chronic lead acetate-induced cardiovascular and renal toxicities in rats. Thirty-six rats were randomly selected and divided into six groups of six rats each. Pb toxicity was induced by the administration of 100 mg/L Pb in drinking water for 12 weeks in groups B-F. Groups A and B were left untreated; groups C and D were treated with polyphenol-rich fraction of Terminalia catappa [PRFTC (100 and 200 mg/kg b.w.)]; vitamin E (50 mg/kg b.w.) and lisinopril (10 mg/kg b.w.) were administered to groups E and F, respectively. Exposure of rats to Pb induced significantly elevated ( P < 0.05) primary haemodynamic parameters, severe disseminated congestion of blood vessels and haemorrhages in the cardiac and renal tissues, significantly elevated ( P < 0.05) markers of oxidative stress markers of inflammation and myocardial infarction, but significantly decreased serum nitric oxide and the systemic antioxidants. Furthermore, rats exposed to Pb showed heightened immune-positive reactions to Caspase-3, a marker of apoptosis, in both renal and cardiac tissues. All manifestations of Pb-associated toxicities in the cardiovascular and renal systems were alleviated by the PRFTC treatment in rats. The polyphenol-rich fraction of T. catappa proved effective in the reduction of oxidative stress-mediated derangements of the physiological homeostasis and decreased apoptosis in the cardiovascular and renal systems of rats chronically exposed to lead acetate toxicities and may therefore have therapeutic potential as a supplement that can be applied in chronic lead poisoning.

Butanol Fraction of &lt;i&gt;Rivea ornata&lt;/i&gt; Attenuate Endothelial Dysfunction in Rats via Modulation of Cardiovascular Risk Factors

Atherosclerosis is caused by vascular inflammation and oxidative stress. Pro-atherogenic effect of hypercholesterolemia caused by impairment of nitric oxide generation due to activated arginase. The study takes up to find the atheroprotective role of polyphenolic fraction of &lt;em&gt;Rivea ornata&lt;/em&gt; leaves by using lipid emulsion induced atherosclerosis in rat model. The study carried out by studying atherogenic markers in the serum (lipid profiles, C-reactive protein), vascular tissue (myeloperoxidase, arginase, hydroxyproline, lipid peroxidation) and atheroprotective factors in the serum (paraoxonase, nitric oxide), and in the vascular tissue (thiol levels, endogenous antioxidants) after feeding the rats with lipid emulsion for 12 weeks. Treatment of polyphenolic rich butanol fraction is able to correct the imbalance of atherogenic and antiatherogenic factors induced by lipid emulsion feeding. Butanol fraction at the dose of 400 mg/kg significantly increases high density lipoprotein, paraoxonase, nitric oxide, tissue thiol levels, endogenous antioxidants and decreases total triglycerides, total cholesterol, very low-density lipoprotein, low density lipoprotein, myeloperoxidase, arginase, hydroxyproline, lipid peroxidation. The atheroprotection reflected in histopathology studies also. Lipid emulsion associated foam cells formation is inhibited by butanol fraction. These all are due to the presence of gallic acid in polyphenol rich butanol fraction is responsible for the underlying mechanism of atheroprotection.

Polyphenol Extract from "Greco" Grape Canes: Characterization, Antioxidant Capacity, and Antitumor Effects on Cal-33 and JHU-SCC-011 Head and Neck Squamous Cell Carcinoma.

In the current study, we determined the antioxidant properties of “Greco” grape cane extracts, a typical cultivar of southern Italy. We also explored the anticancer activity of the polyphenol-rich fraction of the extract on head and neck squamous carcinoma cells (HNSCC) and investigated the underlying mechanism. Aqueous extracts were prepared at different pHs and extraction times and the total phenolic and reducing sugar contents were estimated. Radical Scavenging Activity (RSA), Ferric Reducing Antioxidant Power (FRAP), and Total Antioxidant Capacity (TAC) of the extracts were measured. A polyphenol-rich fraction, accounting for 6.7% by weight and characterized mainly by procyanidins and stilbenoids, was prepared from the extract obtained at pH 7 for 60 min. We demonstrated that the extract exerted a cytotoxic effect on HNSCC cell lines by inducing cell cycle arrest via cyclin downregulation and p21 upregulation, and by triggering apoptosis through caspase cascade activation, PARP-1 cleavage, and an increase in the Bax/Bcl-2 ratio. We furnished evidence that the polyphenol-rich fraction played the major role in the anticancer activity of the extract. These outcomes highlighted grape canes from the “Greco” cultivar as a valuable source of polyphenols that may represent good candidates for the design of innovative adjuvant therapies in the treatment of HNSCC.

Fractionation of Extracts from Black Chokeberry, Cranberry, and Pomegranate to Identify Compounds That Influence Lipid Metabolism.

Polyphenols show a spectrum of bioactive effects, including an influence on lipid metabolism. In this study, we performed activity-guided fractionations of black chokeberry (aronia), cranberry, and pomegranate extracts to identify the biologically active compounds. The extracts were prepared from fruit juice concentrates with the adsorbent resin Amberlite XAD-7 and were separated into a copigment and an anthocyanin fraction, followed by fractionation into a polymer and monomeric fraction by means of hexane precipitation. For further fractionation of the cranberry and pomegranate copigment fractions, high-performance countercurrent chromatography (HPCCC) was used. The compounds in each fraction were identified by high-performance liquid chromatography/electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS), and the quantification was performed by ultra high-performance liquid chromatography-diode array detector (UHPLC-DAD) analyses. Each of the (sub-)fractions was tested in three in vitro assays: phosphodiesterase 3B (PDE) activity, lipid accumulation, and lipolysis in 3T3-L1 cells. The results showed that various fractions and subfractions can inhibit lipid accumulation and PDE activity as well as increase lipolysis, particularly copigments. Overall, our results indicate an influence of polyphenol-rich (sub-)fractions on the lipid metabolism.

UPLC-PDA-MS/MS Profiling and Healing Activity of Polyphenol-Rich Fraction of Alhagi maurorum against Oral Ulcer in Rats.

Camelthorn, Alhagi maurorum Boiss, family Fabaceae has long been used in African folk medicine owing to its richness in pharmacologically active metabolites. The crude extract (CEAM), ethyl acetate fraction (EFAM) and n-butanol (BFAM) fraction of A. maurorum aerial parts were investigated for their total polyphenols and oral antiulcer activity using in-vitro and in-vivo models. The major phenolic compound was isolated from the polyphenol-rich EFAM fraction and identified by conventional and spectroscopic methods of analysis as isorhamnetin-3-O-rutinoside. Furthermore, standardization of EAFM using UPLC-PDA-UV quantified isorhamnetin-3-O-rutinoside as 262.91 0.57 g/mg of the fraction. Analysis of EFAM using UPLC-PDA-MS/MS revealed tentative identification of 25 polyphenolic compounds. EFAM exhibited the most potent free radical scavenging activity against DPPH, with an IC50 (27.73 ± 1.85 µg/mL) and an FRAP value of (176.60 ± 5.21 μM Trolox equivalent (TE)/mg fraction) in comparison with CEAM and BFAM. Acetic acid-induced oral ulcers in a rat model were used to evaluate the healing properties of A. maurorum aerial parts. EFAM significantly decreased tumor necrosis factor-alpha (TNF-α) and interleukin-2 (IL-2) by 36.4% and 50.8%, respectively, in the ulcer tissues while, CEAM and BFAM exhibited lower activity at the same dose. In addition, EFAM led to a significant (p < 0.0001) rise in the expression of proliferating cell nuclear antigen (PCNA), a cell proliferation marker. A. maurorum exhibited a potent healing effect in acetic acid-induced oral ulcers in rats by mitigating the release of pro-inflammatory cytokines and improving PCNA expression.

Chemical profile and cytotoxic activity of a polyphenolic-rich fraction from Euphorbia dendroides aerial parts

Taking into account the great interest of Euphorbia plants as potential sources of active phytochemicals, this study aims to investigate the polyphenols of Euphorbia dendroides aerial parts in relation to its cytotoxic activity. the total phenolic and flavonoid contents of E. dendroides aerial parts were determined as 152.2 ± 10.16 mg GAE/g DW and 66.68 ± 4.46 mg RE/g DW, respectively. Polyphenolic-rich fraction (EdPh-B) was chromatographically fractionated from the hydro-ethanolic extract of this plant. LC-ESI-MS/MS analysis of EdPh-B showed the presence of three phenolic acids and five flavonoids. Additionally, the extensive chromatographic purification of EdPh-B resulted in identified of seven known compounds; vanillin (1), luteolin (2), quercetin-3-O-β-d-glucuronopyranoside (3), kaempferol-3-O-β-d-glucuronopyranoside (4), gallic acid (5), trans-caffeic acid (6) and protocatechuic acid (7), which are first reported from the plant. Moreover, in vitro cytotoxic activity of two fractions (EdPh and EdPh-B) as well as the two isolated flavonoids (3 and 4) against two cancer (OVK-18 and MCF-7) and a normal (NHDF) cell lines was evaluated. EdPh, EdPh-B and compound 3 showed remarkable inhibitory activities against OVK-18 with IC50 values 3.21, 5.10 μg/mL and 10.35 µM, and MCF-7 with IC50 of 25.29, 6.09 μg/mL and 15.17 µM, respectively compared to vinblastine as a positive control.

Polyphenol-rich fraction from Thymus quinquecostatus Celak attenuates the myocardial ischemia injury in mice induced by isoproterenol through inhibiting apoptosis, antioxidation and activating PI3K/AKT pathway

Polyphenol-rich fraction from Thymus quinquelostatus Celak (TCPRF) reduced myocardial apoptosis of ISO-induced MI mice by inhibiting oxidative stress and activating PI3K/AKT signaling pathway. These effects are related with the improvement of TCPRF on ST segment change in ECG, serum CK level, and the pathological damage in myocardial tissue. • TCPRF has protective effect against myocardial ischemia. • TCPRF attenuates oxidative stress in myocardium of myocardial ischemia mice. • TCPRF relieves myocardial ischemia injury by inhibiting apoptosis. • PI3K/AKT signal pathway plays a key role in the cardioprotection of TCPRF. Thymus quinquelostatus Celak, a kind of food additive and folk medicine, has obvious antioxidative and anti-inflammatory effects. However, there have been no reports about the cardioprotective effects of polyphenol-rich fraction from Thymus quinquelostatus Celak (TCPRF). Here, we predicted the targets and pathways of TCPRF related to myocardial ischemia (MI) using network pharmacology, and examined the effects as well as the mechanisms of TCPRF in ISO-induced MI mice. The results verified that TCPRF could decrease the serum CK level, improve ECG and the pathological alterations of myocardium. TCPRF also increased SOD activity, decreased MDA content, reduced the positive apoptotic cells, decreased the expression of Bax, and increase the expression of Bcl-2, PI3K and p-AKT in the myocardium. These results demonstrated that TCPRF was able to alleviate ISO-induced MI injury, which is partly related to inhibiting myocardium apoptosis, antioxidation and activating PI3K/AKT pathway.

Strawberry Polyphenol-Rich Fractions Can Mitigate Disorders in Gastrointestinal Tract and Liver Functions Caused by a High-Fructose Diet in Experimental Rats

Strawberry Polyphenol-Rich Fractions Can Mitigate Disorders in Gastrointestinal Tract and Liver Functions Caused by a High-Fructose Diet in Experimental Rats

Mechanistic studies on polyphenol rich fractions of Kangra tea by HPTLC and NMR for their antioxidant activities.

The antioxidant activity in tea is largely driven by its polyphenolic content, however, the antioxidant reaction mechanism and the compounds involved are not well characterized. Therefore, in this study, we performed in-depth profiling ofthe antioxidant reaction mechanism of Green Tea (GT), Black Tea (BT), and their polyphenolic fractions with free radical using state-of-the-art analytical techniques. The polyphenol enriched fractions from GT and BT were isolated using column chromatography. Catechins were isolated and characterized by diverse spectroscopic techniques. Samples were screened for their antioxidant activity by HPTLC and further evaluated using a spectrophotometer. The free radical reactions with GT, BT, enriched fractions viz, GT Polyphenols (GTP), BT Polyphenols (BTP), and isolated catechins were studied using the13C NMR technique. The highest polyphenol content was found in GTP (795.4 ± 0.012mg/g) whereas GT (321.0 ± 0.028mg/g) showed maximum flavonoids content. Individual catechins isolated from GTP were EGCG, ECG, EGC, EC and C. Antioxidant activity followed the order EGCG > ECG > EGC > EC > GTP > C > BTP > GT > BT. In GT, the antioxidant reaction mechanism showed single electron and H-transfer in all catechins, which involved the transformation of the hydroxyl group to the carbonyl group. Whereas in BT theaflavins, conversion of the benzotropolone ring to the six-membered ring was observed. The online version contains supplementary material available at 10.1007/s13197-021-05297-w.

Green extraction of polyphenols from citrus peel by-products and their antifungal activity against Aspergillus flavus

Aspergillus flavus is a pathogenic fungus associated with food safety issues worldwide. This study investigated the antifungal activity of citrus peel extracts prepared using food-grade solvents (hot water or ethanol). Mandarin (Citrus reticulata) peel ethanol extracts inhibited the mycelial growth of A. flavus (39.60%) more effectively than those of orange (32.31%) and lemon (13.51%) after 7 days of incubation. The growth of A. flavus could be completely inhibited by mandarin extracts at 300–400 mg mL−1, depending on the extraction solvent. Solid-phase extraction (SPE) separated the polyphenol-rich fractions, which showed up to 40% higher antifungal activity than crude extracts. Twelve polyphenols (2 phenolic acids and 10 flavonoids) were identified by HPLC-DAD, narirutin and hesperidin were the most abundant. In conclusion, citrus peels are promising bioresources of antifungal agents with potential applications in food and other industries.

Polyphenol-Rich Purified Bioactive Fraction Isolated from Terminalia catappa L.: UHPLC-MS/MS-Based Metabolite Identification and Evaluation of Their Antimicrobial Potential

Background: Antimicrobial resistance is a major threat to humankind and the advancement of resistance due to genetic modifications and other defense mechanisms that make the current antibiotics ineffective or less efficacious. Objective: This investigation aims to isolate bioactive compounds from the leaf acetone extract of Terminalia catappa and to evaluate their antimicrobial potential against human pathogenic organisms. Materials and Methods: The bioactive extract was subjected to column chromatography. The fractions were assessed for their minimum inhibitory concentration, minimum fungicidal concentration, and time kill assays. UHPLC-MS/MS analysis was used to identify the bioactive molecules in the fraction. Results: The isolated fraction exhibited antimicrobial activity, with the most sensitive being Staphylococcus aureus (clinical isolate) and Methicillin Resistant Staphylococcus aureus 1503 (0.097 mg/mL), and the fungi Trichophyton rubrum and Candida albicans were inhibited at 0.097 mg/mL. The time kill assay exhibited bactericidal properties towards S. aureus (clinical isolate) and Salmonella typhi (MTCC 733). Additionally, MRSA 1503 and Proteus vulgaris exhibited bacteriostatic activities. The UHPLC-MS/MS analysis revealed that the fraction was rich in polyphenols. Alkaloids and some ellagitannins were identified for the first time. Conclusion: The results highlight the significant inhibition of multidrug-resistant MRSA strains and fungi by the polyphenol-rich fraction. The investigation reveals the potential use of the identified compounds for antimicrobial use, which could lower the implication of multidrug resistance.

Antioxidant compounds from Annona crassiflora fruit peel reduce lipid levels and oxidative damage and maintain the glutathione defense in hepatic tissue of Triton WR-1339-induced hyperlipidemic mice

Dyslipidemia is a risk factor for the pathogenesis of several diseases, such as obesity, hypertension, atherosclerosis and cardiovascular diseases. In addition to interfering with serum concentrations of cholesterol and triglycerides, hyperlipidemia is involved in oxidative stress increase and reduction of the endogenous antioxidant defenses. The fruit peel of Annona crassiflora crude extract (CEAc) and its polyphenols-rich fraction (PFAc) were investigated against hypertriglyceridemia, hypercholesterolemia and hepatic oxidative stress in Triton WR-1339-induced hyperlipidemic mice. Lipid parameters in serum, feces and liver, as well as hepatic oxidative status, and enzymatic and non-enzymatic antioxidant defense systems were analyzed. Pre-treatment with CEAc for 12 days decreased hepatic triglycerides and total cholesterol, and similar to PFAc, increased the high-density lipoprotein level. There were reductions in lipid peroxidation and protein carbonylation, as well as restoration of the glutathione defense system and total thiol content in the liver of the hyperlipidemic mice treated with PFAc. The fruit peel of A. crassiflora, a promising natural source of bioactive molecules, showed a potential lipid-lowering action and hepatoprotective activities triggered by reduction of oxidative damage and maintenance of the enzymatic and non-enzymatic antioxidant systems impaired by the hyperlipidemic state.

LCMS/MS analysis and evaluation of anti-inflammatory and antioxidant activities of the polyphenol fraction of Litsea quinqueflora (Dennst.) Suresh

The main aim of the work was to scientifically prove the anti-inflammatory property of the polyphenol-rich fraction of hydro-alcoholic leaf extract of Litsea quinqueflora (Dennst.) Suresh by protein denaturation and free radical scavenging activity. The polyphenol-rich fraction of hydro-alcoholic leaf extract was obtained via acid-alkali hydrolysis, followed by fractionation with chloroform and ethyl acetate. HPTLC profiling of the finally obtained ethyl acetate fraction and consequent derivatisation with aluminium chloride revealed the presence of flavonoids in a more purified form. LCMS/MS analysis tentatively identified the presence of bioactive polyphenolic compounds such as gallocatechin, sinapic acid, pinocembrin, paeonol and umbelliferone in the separated fraction. The polyphenol-rich fraction of hydro-alcoholic extract of leaves showed anti-denaturing activity in heat-induced bovine serum albumin denaturation with an IC50 value of 23.59 µg/ml and was statistically significant at 0.1% level. The antioxidant property of the polyphenol-rich fraction determined by its free radical scavenging ability against DPPH and ABTS showed IC50 values 122.98 and 135.44 µg/ml respectively and was also statistically significant at 0.1% level. Hence, the traditional use of Litsea quinqueflora as an anti-inflammatory agent can be attributed to the presence of polyphenols.

Thymus quinquecostatus Celak. ameliorates cerebral ischemia-reperfusion injury via dual antioxidant actions: Activating Keap1/Nrf2/HO-1 signaling pathway and directly scavenging ROS

BackgroundThymus quinquecostatus Celak. has been widely used as a spice and a folk medicine for relieving exterior syndrome and alleviating pain in China. PurposeTo explore the protective effects and the underlying mechanism against cerebral ischemia-reperfusion injury (CIRI) of the T. quinquecostatus combining with its chemical composition. Study design and methodsHigh-polar extract (HPE) was extracted from T. quinquecostatus and polyphenols in HPE were enriched to obtain polyphenol-rich fraction (PRF) using Macroporous resin. The free radicals and zebrafish embryos were used to compare the antioxidant activities of HPE and PRF in vitro and in vivo. Then, the transient middle cerebral artery occlusion (tMCAO) model was established in rats. Neurological deficit score, infarction rate, morphology and apoptosis of neurons were examined to investigate the protective effects of PRF on CIRI. The mRNA and protein levels of nuclear factor erythroid 2-related factor 2 (Nrf2) and hemeoxygenase-1 (HO-1) and the activities of downstream antioxidant enzymes in ischemia tissues were determined to clarify the underlying mechanisms. Also, reactive oxygen species (ROS) level in zebrafish embryos were detected after incubation with PRF for a short time (2 h) to investigate whether PRF could directly eliminate free radicals. Finally, chemical composition of PRF were analyzed to investigate the material basis for antioxidant activity and anti-CIRI effect. ResultsCompared with HPE, PRF showed stronger antioxidant activities. PRF exhibited obvious protective effects including ameliorating neurological deficit, lowering infarction rate, and improving the cellular morphology in hippocampus CA1 and cortex after tMCAO. TUNEL staining suggested PRF dose-dependently improved the apoptosis of the neurons in ischemic cortex. RT-qPCR and Western Blot results suggested that PRF regulated oxidative stress (OS) via activating the Keap1/Nrf2/HO-1 signaling pathway. Also, PRF could directly scavenge excessive ROS in zebrafish embryos after a short-time PRF incubation. The anti-CIRI effect might be primarily attributed to the abundant polyphenols in PRF, including flavonoids, polymethoxylated flavonoids, flavonoid glycosides, and phenolic acids. ConclusionT. quinquecostatus contains abundant polyphenols and exhibited a good protective effect against CIRI via dual antioxidant mechanisms, providing a reference for further research and application for this plant.