Polyphenol-rich Fraction Research Articles

Cocoa and Polyphenol-Rich Cocoa Fractions Fail to Improve Acute Colonic Inflammation in Dextran Sulfate Sodium-Treated Mice.

A study is conducted to determine the anti-inflammatory effects of cocoa and polyphenol-rich cocoa fractions in the dextran sulfate sodium (DSS)-induced mouse model of acute colonic inflammation. Male C57BL/6J mice are treated with dietary cocoa powder, an extractable cocoa polyphenol fraction, or a non-extractable cocoa polyphenol fraction for 2 weeks prior to treatment with 2.5% DSS in the drinking water for 7 days to induce colonic inflammation. Cocoa treatment continues during the DSS period. Cocoa and/or cocoa fractions exacerbate DSS-induced weight loss and fail to mitigate DSS-induced colon shortening but do improve splenomegaly. Cocoa/cocoa fraction treatment fails to mitigate DSS-induced mRNA and protein markers of inflammation. Principal component analysis shows overlap between cocoa or cocoa fraction-treated mice and DSS-induced controls, but separation from mice not treated with DSS. The results suggest cocoa and cocoa polyphenols may not be useful in mitigating acute colonic inflammation.

Grape Pomace Polyphenols Reduce Acute Inflammatory Response Induced by Carrageenan in a Murine Model.

Grape pomace (GP), a by-product of wine production, contains bioactive polyphenols with potential health benefits. This study investigates the anti-inflammatory properties of a polyphenolic fraction derived from GP, obtained by ultrasound-microwave hybrid extraction and purified using ion-exchange chromatography. In the inflammation model, mice were divided into six groups: intact, carrageenan, indomethacin, and three GP polyphenols treatment groups. Paw edema was induced by subplantar injection of carrageenan, and the GP polyphenols were administered intraperitoneally at doses of 10, 20, and 40 mg/kg. The anti-inflammatory effect was evaluated by measuring paw volume, and expression of inflammatory markers: cyclooxygenase-2 (COX-2), myeloperoxidase (MPO), and cytokines (IL-1β and IL-6), along with lipid peroxidation levels. The GP polyphenols significantly reduced paw edema and expression levels of COX-2, MPO, and cytokines in a dose-dependent manner effect, with the highest dose showing the greatest reduction. Additionally, lipid peroxidation levels were also decreased by GP polyphenols treatment at doses of 10 and 20 mg/kg. These findings suggest that ultrasound-microwave extraction combined with amberlite purification proved to be effective in obtaining a polyphenolic-rich fraction from GP. Thus, GP polyphenols may serve as a natural anti-inflammatory and antioxidant agent for treating inflammation and oxidative stress-related diseases.

The protective effect of bergamot polyphenolic fraction on reno-cardiac damage induced by DOCA-salt and unilateral renal artery ligation in rats

Abstract Funding Acknowledgements None. The complex pathological interactions between renal and cardiovascular systems represent a real global epidemic and renovascular hypertension remains among the most prevalent, but also potentially reversible, risk factor for numerous reno-cardiac diseases in humans and pets. Here, we investigated the anti-inflammatory and reno-cardiac protective effects of a polyphenol-rich fraction of citrus bergamot (BPF) in an experimental model of hypertension induced by unilateral renal artery ligation (RAL). Adult male Wistar rats underwent unilateral renal artery ligation and treatment with 20 mg/kg deoxycorticosterone acetate (DOCA), twice a week for a period of 4 weeks, and 1% sodium chloride water. A subgroup of hypertensive rats received 100 mg/kg/day of BPF for 28 days, by gavage. Another group of animals was treated with a sub-cutaneous injection of vehicle (CTRL). RAL DOCA-Salt rats showed a significant increase in mean arterial blood pressure (MAP; p<0.05 vs CTRL) which strongly increased the resistive index (RI; p<0.05 vs CTRL) of contralateral renal artery flow and kidney volume after 4 weeks (p<0.001 vs CTRL). Renal dysfunction also led to a dysfunction of cardiac tissue strain associated with overt dyssynchrony in cardiac wall motion, as shown by the increased time-to-peak (T2P; p<0.05) and the decreased whole peak capacity (Pk; p<0.01) in displacement and strain rate (p<0.05) in longitudinal motion. The hearts of RAL DOCA-Salt rats showed a larger time delay between the fastest and the lowest region (Maximum Opposite Wall Delay-MOWD) (p<0.05 in displacement and p<0.01 in strain rate vs CTRL). A significant increase in the levels of the circulating pro-inflammatory cytokines and chemokines (p<0.05 for IL-12(40), p<0.01 for GM-CSF, KC, IL-13, and TNF- α) and in the NGAL expression of the ligated kidney (p<0.001) was observed.This pathological condition was prevented by BPF treatment, by reducing the increase of blood pressure in RAL DOCA-Salt rats (p<0.05) and exerting a protective effect on the volume of the contralateral kidney (p<0.01). BPF ameliorates cardiac tissue strain dysfunction by increasing Pk in displacement (p<0.01) and reducing the T2P in strain rate motion (p<0.05). These effects significantly improve MOWD (p<0.05) preventing the overt dyssynchrony in cardiac wall motion. The reno-cardiac protective effect of BPF was associated with a significant reduction in serum level of the pro-inflammatory cytokines and chemokines (p<0.05 for KC and IL-12(40), p<0.01 for GM-CSF, IL-13, and TNF- α)restoring physiological levels of NGAL (p<0.05) protein of the tethered kidney. In conclusion, the present results show that BPF promotes an efficient renovascular protection preventing the progression of inflammation and reno-cardiac damage, suggesting the potential clinical and veterinary role of dietary supplementation with the polyphenol-rich fraction of citrus bergamot in counteracting hypertension-induced reno-cardiac syndrome.

Phenolic enriched fraction of Clerodendrum glandulosum Lindl. leaf extract ameliorates hyperglycemia and oxidative stress in streptozotocin-nicotinamide induced diabetic rats

BackgroundClerodendrum glandulosum Lindl. is an important ethnomedicinal shrub of Northeast India, used by traditional healers to control various ailments like diabetes, hypertension, arthritis, etc. ObjectivesThe present study was conducted to explore the anti-hyperglycemic and antioxidative effects of the polyphenol-rich fraction (PRF) of C. glandulosum leaf extract and identification of its major bioactive compounds. Further, an in-silico molecular docking study was also performed to understand the molecular interactions of the identified major compounds with some target proteins associated with diabetic complications. Materials and methodsPRF was purified from the hydromethanolic (80% MeOH) extract of leaves and subjected to assessment of in-vitro antioxidant and anti-diabetic properties. It was also subjected to evaluate the ameliorative effect during streptozotocin-nicotinamide-induced hyperglycemia in Wistar albino rats. An in-silico molecular docking study was also performed to complement the in-vitro/in-vivo studies. ResultsChemical analysis of PRF showed the presence of phenolics like caffeic acid, verbascoside, isoverbascoside, and apigenin, of which verbascoside (598.14 ± 1.24 mg/g) was found to be the principal compound. In-vitro studies showed potent antioxidant (IC50 of DPPH:32.45 ± 2.16 μg/mL; ABTS:39.08 ± 0.53 μg/mL) properties and excellent aldose reductase inhibition potential (IC50 2.18 ± 0.10 μg/mL). Treatment with PRF showed reduced blood glucose levels and increased plasma insulin levels. The results also indicate an improvement of endogenous antioxidants and suppression of inflammatory cytokines (IL-6 and TNF-α) comparable to the standard. Molecular docking studies predicted promising interactions between the identified molecules and the crucial amino acid residues of the enzymes involved in the development of hyperglycemia. ConclusionThis study revealed the antihyperglycemic and antioxidant potential of partially purified fraction PRF of C. glandulosum leaves.

Anticancer Activity of Encapsulated Pearl Millet Polyphenol-Rich Extract against Proliferating and Non-Proliferating Breast Cancer Cells In Vitro.

Plant-derived polyphenols are bioactive compounds with potential health-promoting properties including antioxidant, anti-inflammatory, and anticancer activity. However, their beneficial effects and biomedical applications may be limited due to their low bioavailability. In the present study, we have considered a microencapsulation-based drug delivery system to investigate the anticancer effects of polyphenol-rich (apigenin, caffeic acid, and luteolin) fractions, extracted from a cereal crop pearl millet (Pennisetum glaucum), using three phenotypically different cellular models of breast cancer in vitro, namely triple negative HCC1806, ER-positive HCC1428, and HER2-positive AU565 cells. Encapsulated polyphenolic extract induced apoptotic cell death in breast cancer cells with different receptor status, whereas it was ineffective against non-tumorigenic MCF10F cells. Encapsulated polyphenolic extract was also found to be cytotoxic against drug-resistant doxorubicin-induced senescent breast cancer cells that were accompanied by increased levels of apoptotic and necrotic markers, cell cycle inhibitor p21 and proinflammatory cytokine IL8. Furthermore, diverse responses to the stimulation with encapsulated polyphenolic extract in senescent breast cancer cells were observed, as in the encapsulated polyphenolic extract-treated non-proliferating AU565 cells, the autophagic pathway, here cytotoxic autophagy, was also induced, as judged by elevated levels of beclin-1 and LC3b. We show for the first time the anti-breast cancer activity of encapsulated polyphenolic extract of pearl millet and postulate that microencapsulation may be a useful approach for potentiating the anticancer effects of phytochemicals with limited bioavailability.

Integrated pharmacokinetic-pharmacodynamic modeling and metabolomic research on polyphenol-rich fraction of Thymus quinquecostatus Celak. Alleviating cerebral ischemia-reperfusion injury

Ethnopharmacological relevanceThymus quinquecostatus Celak., a member of thymus genus in Lamiaceae family, has been used as a folk medicine for relieving exterior syndrome and alleviating pain in China. The polyphenol-rich fraction (PRF) derived from Thymus quinquecostatus Celak. had been validated that it can protect cerebral ischemia-reperfusion injury (CIRI) by activating Keap1/Nrf2/HO-1 signaling pathway.Aim of this study: To explore effective components and their pharmacokinetic and pharmacodynamic characteristics as well as possible mechanisms of PRF in treating CIRI. Materials and methodsNormal treated group (NTG) and tMCAO model treated group (MTG) rats were administrated PRF intragastrically. The prototype components and metabolites of PRF in plasma and brain were analyzed by the UPLC-Q-Exactive Orbitrap MSn method. Subsequently, the pharmacokinetics properties of indicative components were performed based on HPLC-QQQ-MS/MS. SOD and LDH activities were determined to study the pharmacodynamic (PD) properties of PRF. The PK-PD relationship of PRF was constructed. In addition, the effect of PRF on endogenous metabolites in plasma and brain was investigated using metabolomic method. ResultsSalvianic acid A, caffeic acid, rosmarinic acid, scutellarin, and apigenin-7-O-glucuronide were selected as indicative components based on metabolic analysis. The non-compartmental parameters were calculated for indicative components in plasma and brain of NTG and MTG rats. Furthermore, single-component and multi-component PK-PD modeling involved Emax, Imax PD models for effect indexes were fitted as well as ANN models were established, which indicated that these components can work together to regulate SOD and LDH activities in plasma and SOD activity in brain tissue to improve CIRI. Additionally, PRF may ameliorate CIRI by regulating the disorder of endogenous metabolites in lipid metabolism, amino acid metabolism, and purine metabolism pathways in vivo, among which lipid metabolism and purine metabolism are closely related to oxidative stress. ConclusionThe PK-PD properties of effect substances and mechanisms of PRF anti-CIRI were further elaborated. The findings provide a convincing foundation for the application of T. quinquecostatus Celak. in the maintenance of human health disorders.

Recovery of antioxidants and oils from blackcurrant and redcurrant wastes by ultrasound-assisted extraction

An investigation of the ultrasound-assisted extraction (UAE) of polyphenols and oils from blackcurrant and redcurrant pomaces was carried out. The aim of the study was to select optimal conditions for the UAE process in order to obtain polyphenol-rich extracts with highest total polyphenol content and highest antioxidant capacity. In case of oils, the optimization was focused on choosing the UAE parameters to achieve the highest oil yield and the longest oxidation induction times. The most effective conditions of UAE were provided by the results of response surface methodology procedure, which involved variables of time (2–10 min) and ultrasound amplitude (30%–80%). Solvents used for extractions were distilled water and n-hexane for bioactive compounds and oils extractions, respectively. In terms of polyphenol-rich fractions the most effective conditions were: amplitude of around 51% and 3 min time for blackcurrant pomace and amplitude of around 91% and 11 min time for redcurrant pomace. In case of oils, the amplitude of 99% and 11.5 min time were chosen for blackcurrant. For redcurrant seed oil it was the amplitude of 96% and extraction time equal to 12 min. The actual results obtained in optimized conditions were comparable to the results predicted by models. It was proved that response surface methodology could be useful tool in optimization of UAE process for blackcurrant and redcurrant polyphenol-rich extracts and seed oils.

Apoptosis-inducing anti-proliferative and quantitative phytochemical profiling with in silico study of antioxidant-rich Leea aequata L. leaves

Natural products have been important parts of traditional medicine since ancient times, with various promising health effects. Leea aequata (L. aequata), a natural product, has been widely used for treating several diseases due to its promising pharmacological activities. Therefore, the present study aimed to explore the phytochemical profiling and molecular docking of the antioxidant-rich part of L. aequata leaves and its antiproliferative activity. L. aequata leaves were extracted with methanol, followed by fractionation with the respective solvents to obtain the petroleum ether, chloroform, ethyl acetate, and aqueous fractions. The antioxidant activity was evaluated by spectrophotometric methods. The cytotoxic and antiproliferative activities were detected using MTT colorimetric and confocal microscopy methods, respectively. Phytochemical compositions were analyzed using gas chromatography‒mass spectrometry analysis. Computer aided (molecular docking SwissADME, AdmetSAR and pass prediction) analyses were undertaken to sort out the best-fit phytochemicals present in the plant responsible for antioxidant and anticancer effects. Among the fractions, the ethyl acetate fraction was the most abundant polyphenol-rich fraction and showed the highest antioxidant, reducing power, and free radical scavenging activities. Compared to untreated MCF-7 cells, ethyl acetate fraction-treated MCF-7 cells showed an increase in apoptotic characteristics, such as membrane blebbing, chromatin condensation, and nuclear fragmentation, causing apoptosis and decreased proliferation of HeLa and MCF-7 cells. Furthermore, gas chromatography mass spectrometry data revealed that the ethyl acetate fraction contained 16 compounds, including methyl esters of long-chain fatty acids, which are the major chemical constituents. Moreover, hexadecanoic acid, methyl ester; 9-octadecenoic acid (Z)-, methyl ester; 9,12-octadecadienoic acid, methyl ester (Z, Z) and phenol, 2,4-bis(1,1-dimethylethyl) are known to have antioxidant and cytotoxic activity, as confirmed by computer-aided models. A strong correlation was observed between the antioxidant and polyphenolic contents and the anticancer activity. In conclusion, we explored the possibility that L. aequata could be a promising source of antioxidants and anticancer agents with a high phytochemical profile.

Potential benefits of Malva sylvestris in dry-eye disease pathology in vitro based on antioxidant, wound-healing and anti-inflammatory properties

Dry eye disease (DED) is a common chronic ocular surface disease. Available therapies are effective but often associated with side effects. This study investigates the potential of a Malva sylvestris L. flower extract and two defined preparations, a mucilage and a polyphenol rich fraction, on cells that are essential for the DED pathology. Furthermore, single compounds were isolated and characterised out of the polyphenol fraction. The M. sylvestris extract and its two fractions reduced reactive oxygen species (ROS) in an ultraviolet-induced model and promoted wound healing capacity of HCE-T cells, but only the polyphenol fraction and the flower extract exhibited significant radical scavenging activity. The flower extract and the polyphenol fraction inhibited cytokine secretion (IL-6, TNF-α, IL-8) from HCE-T cells and THP-1 cells. In contrast, the mucilage fraction led to an increase in mediator secretion. The NF-κB activity and calcium influx in THP-1 and Jurkat cells, respectively was decreased by treatment with the flower extract and the polyphenol fraction, whereas the mucilage fraction had no influence on these parameters. Moreover, the flower extract and the mucilage fraction at low concentration could stimulate meibomian gland cells’ lipid accumulation. The isolated single compounds showed no effect on analysed parameters, except a coumarin derivative and malvin which showed ROS inhibition effects.

Glycemic and Biochemical Effects of Polyphenol-Rich Fraction of Parkia biglobosa Leaves in Wistar rats Experimentally Induced with Diabetes

Glycemic and Biochemical Effects of Polyphenol-Rich Fraction of Parkia biglobosa Leaves in Wistar rats Experimentally Induced with Diabetes

Bioactivity-Guided Isolation and Antihypertensive Activity of Citrullus colocynthis Polyphenols in Rats with Genetic Model of Hypertension.

Background and Objectives: Citrullus colocynthis belongs to the Cucurbitaceae family and is a wild medicinal plant used in folk literature to treat various diseases. The purpose of the current study was to explore the antihypertensive and antioxidant potentials of Citrullus colocynthis (CC) polyphenol-rich fractions using a spontaneous hypertensive rat (SHR) model. Materials and Methods: The concentrated aqueous ethanol extract of CC fruit was successively fractioned using solvents of increasing polarity, i.e., hexane, chloroform, ethyl acetate and n-butanol. The obtained extracts were analyzed for total phenolic content (TPC), total flavonoid content (TFC) and total flavonol content (TOF). Moreover, the CC extracts were further evaluated for radical scavenging capacity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays and antioxidant activity using inhibition of linoleic acid peroxidation and determination of reducing potential protocols. The phytochemical components were characterized by HPLC-MWD-ESI-MS in positive ionization mode. Results: The results showed that ethyl acetate fraction (EAF) exhibited a higher content of phenolic compounds in term of TPC (289 mg/g), TFC (7.6 mg/g) and TOF (35.7 mg/g). EAF showed higher antioxidant and DPPH and ABTS scavenging activities with SC50 values of 6.2 and 79.5 µg/mL, respectively. LCMS analysis revealed that twenty polyphenol compounds were identified in the EAF, including phenolic acids and flavonoids, mainly myricetin and quercetin derivatives. The in vivo antihypertensive activity of EAF of CC on SHR revealed that it significantly decreased the mean arterial pressure (MAP), systolic blood pressure (SBP), diastolic blood pressures (DBP) and pulse pressure (PP) as compared to normal and hypertensive control groups. Moreover, EAF of CC significantly reduced the oxidative stress in the animals in a dose-dependent manner by normalizing the levels of superoxide dismutase (SOD), malondialdehyde (MDA), reduced glutathione (GSH), nitric oxide (NOx) and total antioxidant capacity (TAC). Furthermore, the treatment groups, especially the 500 mg of EAF per kg body weight (EA-500) group, significantly (p ≤ 0.05) improved the electrocardiogram (ECG) pattern and pulse wave velocity (PWV). Conclusion: It was concluded that the EAF of CC is a rich source of polyphenols and showed the best antioxidant activity and antihypertensive potential in SHR.

Identification of polyphenols using UPLC-QTOF MS/MS, in-vitro photoprotective and antiaging activities of brown macroalga Padina tetrastromatica

Brown algae produce several bioactive compounds including unique secondary metabolites like polyphenols, which are known for various pharmacological activities. The present study focused on the cosmeceutical properties of polyphenol-rich fraction from brown macroalga (Padina tetrastromatica). Two fractions (ethyl acetate and aqueous) were obtained by liquid-liquid purification. Total phenolic and phlorotannin contents were assessed by in-vitro methods (Folin-Ciocalteu test and 2,4-dimethoxybenzaldehyde assay). Antioxidant properties were assessed through 2,2-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, nitric oxide radical scavenging activity, and ferric-reducing antioxidant power assay. Ethyl acetate fraction showed high radical scavenging activity and was used for in-vitro photoprotective assays, cell viability tests, and anti-aging related enzyme inhibition tests (anti-tyrosinase, anti-elastase, anti-collagenase). Ethyl acetate fraction showed potential ultraviolet A absorption and a strong sun protection factor (SPF) value and was not toxic to the human skin cell line up to a concentration of 100 μg mL−1. Interestingly, this fraction also showed a strong tyrosinase inhibition and a significant inhibition of elastase and collagenase enzymes. Major polyphenols including phlorotannins present in the fraction were identified using Fourier transform infrared (FTIR) spectroscopy, Ultra pressure liquid chromatography (UPLC)-quadrupole-time of flight (QTOF) mass spectrometry (MS) and NMR spectroscopy. The findings suggest the ethyl acetate fraction of P. tetrastromatica as a promising source for cosmetic use with photoprotection and anti-aging properties.

Phytochemical Profiling, Antioxidant Activity, and Protective Effect against H2O2-Induced Oxidative Stress of Carlina vulgaris Extract.

Carlina vulgaris is a little-understood plant with unexplored biological potential, and the papers regarding its chemical composition are scarce. In our study, for the first time, the phytochemical profile of the plant, focusing on polar metabolites, was established using modern chromatographic techniques including LC-HRMS-QTOF-CAD, UHPLC-PDA-MS. Phytochemical analysis revealed that the species is a rich source of polyphenolic components, with the most abundant being chlorogenic acid and C-glycosides of luteolin, including carlinoside, orientin, isoorientin, and C-glycosides of apigenin, schaftoside, isoschaftoside, and vitexin. Furthermore, we assessed the impact of the polyphenolic-rich fraction of C. vulgaris extracts on human skin fibroblasts using the MTT and NR assays. It was found that the extract was non-toxic and exhibited potent antioxidant activity in the cells subjected to induced oxidative stress. Additionally, it effectively protected the cells against H2O2-induced cytotoxicity. Our study contributes to the general trend of searching for new phytotherapeutics with potential applications in pharmacy and medicine. The results indicate that further exploration of C. vulgaris species is worthwhile, as they can serve as valuable plant material for cosmetic use.

Miconia albicans (Melastomataceae) to treat Chikungunya viral infection: An effectual symptom-driven ethnomedicinal repurposing of an anti-inflammatory species?

Ethnopharmacological relevanceMiconia albicans (MA) is consumed all over the Brazilian territory as a remedy to treat rheumatoid arthritis and has been increasingly used to alleviate the deleterious symptoms caused by Chikungunya virus (CHIKV). Aim of the studyTo investigate the effect of MA leaf and stem hydroethanolic extracts (LE and SE, respectively), their fractions enriched in triterpene acids or polyphenols as well isolated constituents, on CHIKV hosted in Vero cells. Materials and methodsPolyphenol profiles of LE and SE were dereplicated by HPLC-DAD-ESI-MS/MS, aided by standards. Polyphenol-rich (LEx and SEx) and triterpenic acid-rich (LOH and SOH) fractions were obtained in Amberlite XAD-4 and alkalinized 95% ethanol (EtOH) extraction, respectively. TPC and TFC were assessed by colorimetric methods. Three representative flavonoids and two triterpenic acids were quantified by HPLC. CHIKV load suppression was evaluated in Vero cells by real-time qRT‒PCR at noncytotoxic concentrations. ResultsFifteen flavonoids were characterized in LE and SE. LEx presented isoquercitrin, quercitrin, rutin (0.49–1.51%) and quercetin. The TPC was 48 and 62 mg QE/g extract, and the TFC was 11.93 and 0.76 mg QE/g extract for LEx and SEx, respectively. LOH presented ursolic (15.3%) and oleanolic (8.0%) acids. A reduction (91–97%) in the CHIKV load was produced by the triterpene fraction, quercitrin and quercetin; the latter maintained the activity down to one twentieth of the tolerated concentration. ConclusionM. albicans contains flavonoids and triterpenic acids that are effective against CHIKV, which might justify its use to alleviate sequelae of CHIKV infection. However, further investigations on the species and its active constituents are needed.

Annona crassiflora Mart. Fruit Peel Polyphenols Preserve Cardiac Antioxidant Defense and Reduce Oxidative Damage in Hyperlipidemic Mice.

Dyslipidemia and oxidative stress are directly related to the pathogenesis of cardiovascular diseases. Annona crassiflora Mart. (ACM) has been traditionally used in folk medicine to alleviate inflammation and pain. This plant is rich in polyphenols, which exhibit high antioxidant capacity. The present study aimed to elucidate the antioxidant properties of ACM in the heart of hyperlipidemic mice. The animals were orally administered either a crude ethanol extract (CEAc) or a polyphenols-rich fraction (PFAc) obtained from ACM fruit peel. There were correlations between blood and fecal biochemical data with cardiac oxidative stress biomarkers. Here, the pre-treatment with CEAc for 12 d led to an increase in glutathione content (GSH) and a reduction in the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase. Moreover, PFAc was found to enhance the total antioxidant capacity as well as GSH, SOD and CAT activities, which were reduced by Triton WR-1339-induced hyperlipidemia. Moreover, the administration of PFAc before the treatment resulted in a decrease in protein carbonylation and lipid peroxidation levels, as well as a reduction in the activities of glutathione reductase and glucose-6-phosphate dehydrogenase. ACM fruit peel showed improvement in the glutathione system, mainly its polyphenols-rich fraction, indicating a potential cardioprotective antioxidant usage of this plant extract.

In Vitro Modulation of Genotoxicity and Oxidative Stress by Polyphenol-Rich Fraction of Chinese Ladder Brake (Pteris vittata L.).

Pteris vittata L. is a terrestrial genus growing in moist, shady forests and on hillsides. The plant has considerable ethnomedicinal importance. Investigations have been carried out on chemical profiling and antioxidant compounds from some genera of pteridophytes but studies on the biological properties of P. vittata are lacking. Therefore, the present study investigates antioxidant, antigenotoxic, and antiproliferative potential of the aqueous fraction of P. vittata (PWE). A battery of assays were carried out to assess the antioxidant potential of the PWE. SOS chromotest and DNA nicking assay were used to evaluate the antigenotoxicity of the fraction. The cytotoxic effect of PWE was analyzed using MTT and Neutral Single Cell Gel Electrophoresis comet assay. EC50 of 90.188µg/ml, 80.13µg/ml, 142.836µg/ml, and 12.274µg/ml was obtained in DPPH, superoxide anion scavenging, reducing power and lipid peroxidation assays, respectively. PWE was potent in inhibiting Fenton's reagent-induced nicking of pBR322 plasmid. The fraction significantly inhibited hydrogen peroxide (H2O2) and 4-nitroquinoline-N-oxide (4NQO) induced mutagenicity and a reduction in induction factor was found with increased PWE concentration. GI50 of 147.16µg/ml was obtained in MTT assay in human MCF-7 breast cancer cell line. PWE induced apoptosis as confirmed from confocal microscopy studies. The protective effects can be attributed to the presence of the phytochemicals in PWE. These results will be helpful in the development of functional food characteristics, as well as unravel the benefits of pteridophytes as promoters of health.

Chemical characterization of the polyphenolic rich fraction of Thunbergia erecta and its therapeutic potential against doxorubicin and cyclophosphamide-induced cognitive impairment in rats.

Thunbergia erecta (Benth.) was traditionally used as anxiolytic, sedative and antidepressant. The study aimed to characterize T. erecta leaf ethyl acetate fraction of alcohol extract (TEAF) and evaluate its neuroprotective effect on doxorubicin and cyclophosphamide-induced chemobrain. Chemical profiling of TEAF was done using (Liquid chromatography coupled with mass (LC-ESI-MS/MS). In vivo chemobrain model was performed by cognitive impairment induced by doxorubicin and cyclophosphamide. Behavioral assessments included moris water maze, y maze, novel object recognition task and passive avoidance tests. Histological examination and oxidative stress markers were investigated. Protein expression of HMDGB1/RAGE/pNF-κB pathway markers was done using western blotting. All results were applied to hippocampus and prefrontal cortex of rats. Molecular docking was done within the active sites of Human Receptor for Advanced Glycation Endproducts (RAGE) using Discovery studio software. Twenty-one phytoconstituents, mostly polyphenolics, were characterized in TEAF of which eleven compounds were tentatively identified for the first time from T. erecta leaves where rosmarinic acid (11) represents the most prevailing compound. TEAF resulted in a marked dose-dependent amelioration of the histopathological changes evidenced by normal histological structure demonstrated in the hypocampal gesture of rats. TEAF demonstrated an enhanced memory and learning functioning in the different behavioral tests assessed especially at 200mg/kg. It showed significant long-term spatial memory enhancement manifested by 50.32% increase in probe trial relative to chemobrain-induced group. It showed pronounced antioxidant activity evidenced by the significant elevation of prefrontal cortical and hippocampal reduced glutathione levels by 2.45 and 2.65 folds, respectively relative to the chemobrain-induced group. The pronounced reduction in hydrogen peroxide (1.24-1.93 folds) and malondialdehyde levels (1.42-2.60 folds) with significant elevation of catalase activity (12.65-31.47%) induced by TEAF supported its potent antioxidant activity. TEAF reversed the inflammatory cytokines release induced by chemotherapy via its interference with HMGB1/RAGE pathway suppressing the expression of HMBG1, RAGE, p65 (NF-kB), and IL-1β. In silico studies showed that rosmarinic acid displayed the best fitting at the active site of RAGE (ΔG=-40.39kcal/mol). Thunbergia erecta can act as a promising remedy for chemobrain that further consolidates its traditional importance.

Protective Effects of the Polyphenolic-Rich Fraction of Cornsilk against Oxidative Stress in Streptozotocin-Induced Diabetic Rats

Diabetes Mellitus (DM) has become a significant public health problem worldwide and primarily correlated to hyperglycaemia and abnormal lipid and antioxidant levels. Fruit and vegetable wastes are rich in phenolic compounds thus suitable for antioxidant sources. Cornsilk (CS), a maize cultivar waste, also contains phenolic compounds. The current study investigated the anti-hyperglycemic and antioxidative properties of the Phenolic-Rich Fraction of Cornsilk (PRF-CS) in Streptozotocin (STZ)-induced diabetic rats. Five groups of 30 male Sprague Dawley rats were employed in this study. A sample size of six rats each is placed in five groups: Normal-Control (NC), Diabetic-Control (DC), Diabetic-PRF-CS treated 100 mg/kg (DPRF100) and 200 mg/kg (DPRF200), and Diabetic-Metformin Treated (Dmet) groups. The PRF-CS was administered at 100 and 200 mg/kg doses for 28 consecutive days to the diabetic rats. Treatment with both doses of PRF-CS (DPRF100 and DPRF200) significantly decreased the blood glucose levels of the rats (p<0.05). Additionally, the PRF-treated rats demonstrated significantly decreased (p<0.05) lipid peroxidation (3.60±0.23 and 3.31±0.56 µmol/g, respectively). The hepatic antioxidant enzyme activities of Superoxide Dismutase (SOD) (169.35±4.75 and 175.30±3.69 U/mg, respectively), Catalase (CAT) (1457.51±152.74 and 2011.99±396.96 U/mg), and Glutathione Peroxidase (GSH-Px) (63.43±2.99 and 78.47±4.51 U/mg) were also elevated in contrast to the DC group. Furthermore, the PRF-CS administration improved the histological alterations in the liver tissues of the DPRF100 and DPRF200 rats. In conclusion, PRF-CS treatment exhibited protective effects in the diabetic rat model by decreasing oxidative stress and preserving liver integrity.

Antioxidant, Anti-Inflammatory, and Analgesic Properties of Chemically Characterized Polyphenol-Rich Extract from Withania adpressa Coss. ex Batt.

The current work was undertaken to investigate the chemical composition, antioxidant, anti-inflammatory, and analgesic properties of a polyphenol-rich fraction from Withania adpressa Coss. ex Batt. After being extracted, the polyphenol-rich fraction was chemically characterized through use of high-performance liquid chromatography (HPLC). Antioxidant potency was assessed through the use of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and total antioxidant capacity (TAC). Inflammatory and analgesic properties were assessed in vivo through the use of carrageenan and heat stimulus assays, respectively. Chromatographic analysis of polyphenol-rich fraction revealed the presence of potentially bioactive phenols including epicatechin, apigenin, luteolin, quercetin, caffeic acid, p-coumaric acid, and rosmarinic acid. The polyphenol-rich fraction showed interesting anti-free-radical potency with a calculated IC50 value of 27.84 ± 1.48 µg/mL. At the highest dose used (1000 µg/mL), the polyphenol-rich fraction scored good total antioxidant capacity with a calculated value of 924.0 ± 28.29 µg EAA/mg. The polyphenol-rich fraction strongly alleviated the inflammatory effect of carrageenan injected into the plantar fascia of rats resulting in inhibition up to 89.0 ± 2.08% at the highest tested dose (500 mg/kg). The polyphenol-rich fraction showed a good analgesic effect wherein the delay in reaction time to a thermal stimulus caused by 500 mg/kg had a highly similar effect to that induced by Tramadol used as a positive control. The findings of the current work highlight the importance of polyphenol-rich fractions from W. adpressa Coss. ex Batt. as an alternative source of natural antioxidant, inflammatory, and analgesic drugs to control relative diseases.

IN VITRO ANTIPLATELET ACTIVITY OF AN ISOFLAVANONE ISOLATED FROM METHANOLIC EXTRACT OF EMBLICA OFFICINALIS FRUITS

Objective: In this study, we aimed to isolate a polyphenolic compound from a polyphenolic-rich fraction from Emblica officinalis fruits and also study its effect on adenosine diphosphate (ADP) and collagen-induced in vitro platelet aggregation. Methods: The polyphenolic-rich fraction was prepared by 80% methanolic extraction. The residue was extracted successively with hexane, benzene, ethyl acetate and n-butanol. Ethyl acetate residue was selected for column chromatography because of its high polyphenolic content. It was subjected to repeated column chromatography of series with different eluents of increasing polarity. A brown amorphous powder was obtained from ethyl acetate: methanol (7:3) fraction. This sample was subjected to UV-visible spectrum, IR spectrum, 1H NMR, 13C NMR and electrospray mass spectrum (ES-MS) studies for its structural elucidation. Results: A compound, 5, 7, 4'-trihydroxy 3'-methoxy isoflavanone was identified from polyphenolic rich ethyl acetate: methanol (7:3) fraction separated from the 80% methanolic extract of Embica officinalis fruits by repeated column chromatography. Yield of the compound was 421.05 mg/kg. This compound exhibited antiplatelet activity well comparable with that of quercetin. Conclusion: The present study proved that the isolated compound 5, 7, 4'-trihydroxy 3'-methoxy isoflavanone exerts a significant inhibitory activity on ADP and collagen-induced in vitro platelet aggregation, which can be considered as an effective remedy for alleviating complications of cardiovascular diseases.