Search results for: quercetin

Authors: Khusboo Agrawal, S. Saraf

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Quercetin, a flavonol provides a cellular protection against UV induced oxidative damages due to its excellent free radical scavenging activity and direct pro-apoptopic effect on tumor cells. However, its topical use is limited due to its unfavorable physicochemical properties. The present study was aimed to evaluate the potential of mesoporous silica nanoparticles as topical carrier system for quercetin delivery. Complexes of quercetin with mesoporous silica was prepared with different weight ratios and characterized by thermo gravimetric analysis, X-ray diffraction, high resolution TEM, FT-IR spectroscopy, zeta potential measurements and differential scanning calorimetry The protective effect of this vehicle on UV-induced degradation of the quercetin was investigated revealing a certain positive influence of the inclusion on the photostability over time. Epidermal accumulation and transdermal permeation of this molecule were ex vivo evaluated by using Franz diffusion cells. The immobilization of Quercetin in mesoporous silica nanoparticles (MSNs) increased the stability without undermining the antioxidant efficacy.

Keywords: cancer, MSNs, quercetin, topical delivery

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Authors: Samira Ghizellaoui, Manel Boumagoura

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Calcium carbonate precipitation is a widespread problem, especially in hard water systems. The main water supply that supplies the city of Constantine with drinking water is underground water called Hamma water. This water has a very high hardness of around 590 mg/L CaCO₃. This leads to the formation of scale, consisting mainly of calcium carbonate, which can be responsible for the clogging of valves and the deterioration of equipment (water heaters, washing machines and encrustations in the pipes). Plant extracts used as scale inhibitors have attracted the attention of several researchers. In recent years, green inhibitors have attracted great interest because they are biodegradable, non-toxic and do not affect the environment. The aim of our work is to evaluate the effectiveness of a chemical antiscale treatment in the presence of three green inhibitors: gallicacid; quercetin; alginate, and three mixtures: (gallic acid-quercetin); (quercetin-alginate); (gallic acid-alginate). The results show that the inhibitory effect is manifested from an addition of 1mg/L of gallic acid, 10 mg/L of quercetin, 0.2 mg/L of alginate, 0.4mg/L of (gallic acid-quercetin), 2mg/L of (quercetin-alginate) and 0.4 mg/L of (gallic acid-alginate). On the other hand, 100 mg/L (Drinking water standard) of Ca2+is reached for partial softening at 4 mg/L of gallic acid, 40 mg/L of quercetin, 0.6mg/L of alginate, 4mg/L of (gallic acid-quercetin), 10mg/L of (quercetin-alginate) and 1.6 mg/L of (gallic acid-alginate).

Keywords: water, scaling, calcium carbonate, green inhibitor

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Authors: Fernando G. Torres, Omar P. Troncoso

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Quercetin is a naturally occurring polyphenol found in many vegetables, such as onion, with antioxidant properties. It is a dietary component with a documented role in reducing different human cancers. However, its low bioavailability, poor water solubility, and chemical instability limit its applications. Different nano-delivery systems such as nanoparticles, micelles, and nanohydrogels have been studied in order to improve the bioavailability of quercetin. Nanoparticles based on natural polymers such as starch have the advantage of being biocompatible, biodegradable, and non-toxic. In this study, quercetin was loaded into starch nanoparticles using a nanoprecipitation method. Different routes, using sodium tripolyphosphate and Tween® 80 as tensioactive agents, were tested in order to obtain an optimized starch-based nano-delivery system. The characterization of the nanoparticles loaded with quercetin was assessed by Fourier Transform Infrared Spectroscopy, Dynamic Light Scattering, Zeta potential, and Differential scanning calorimetry. UV-vis spectrophotometry was used to evaluate the loading efficiency and capacity of the samples. The results showed that starch-based systems could be successfully used for the nano-delivery of quercetin.

Keywords: starch nanoparticles, nanoprecipitation, quercetin, biomedical applications

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Authors: S. B. Bhandare, K. S. Laddha

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Podphyllum hexandrum belonging to family berberidaceae has gained attention in phytochemical and pharmacological research as it shows excellent anticancer activity and has been used in treatment of skin diseases, sunburns and radioprotection. Chemically it contains lignans and flavonoids such as kaempferol, quercetin and their glycosides. Objective: To isolate and identify Kaempferol and Quercetin from Podophyllum rhizome. Method: The powdered rhizome of Podophyllum hexandrum was subjected to soxhlet extraction with methanol. This methanolic extract is used to obtain podophyllin. Podohyllin was extracted with ethyl acetate and this extract was then concentrated and subjected to column chromatography to obtain purified kaempferol and quercetin. Result: Isolated kaempferol, quercetin were light yellow and dark yellow in colour respectively. TLC of the isolated compounds was performed using chloroform: methanol (9:1) which showed single band on silica plate at Rf 0.6 and 0.4 for kaempferol and quercetin. UV spectrometric studies showed UV maxima (methanol) at 259, 360 nm and 260, 370 nm which are identical with standard kaempferol and quercetin respectively. Both IR spectra exhibited prominent absorption bands for free phenolic OH at 3277 and 3296.2 cm-1 and for conjugated C=O at 1597 and 1659.7 cm-1 respectively. The mass spectrum of kaempferol and quercetin showed (M+1) peak at m/z 287 and 303.09 respectively. 1H NMR analysis of both isolated compounds exhibited typical four-peak pattern of two doublets at δ 6.86 and δ 8.01 which was assigned to H-3’,5’ and H-2’,6’ respectively. Absence of signals less than δ 6.81 in the 1H NMR spectrum supported the aromatic nature of compound. Kaempferol and Quercetin showed 98.1% and 97% purity by HPLC at UV 370 nm. Conclusion: Easy and simple method for isolation of Kaempferol and Quercetin was developed and their structures were confirmed by UV, IR, NMR and mass studies. Method has shown good reproducibility, yield and purity.

Keywords: flavonoids, kaempferol, podophyllum rhizome, quercetin

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Authors: S. Lekhavat, U. Srimongkoluk, P. Ratanachamnong, G. Laungsopapun

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Quercetin was encapsulated with whey protein and high methoxyl pectin by spray drying technique. Feed solution, consisting of 0.1875 0.125 and 0.0625 % w/w quercetin, respectively, was prepared and then sprays at outlet temperature of 70, 80 and 90 °C. Quercetin contents either in feed solution or in spray dried powder were determined by HPLC technique. Physicochemical properties such as viscosity and total soluble solid of feed solution as well as moisture content and water activity of spray dried powder were examined. Particle morphology was imaged using scanning electron microscope. The results showed that feed solution has total soluble solid and viscosity in range of 1.73-5.60 ºBrix and 2.58-8.15 cP, in that order. After spray drying, the moisture content and water activity value of powder are in range of 0.58-2.72 % and 0.18-0.31, respectively. Quercetin content in dried sample increased along with outlet drying temperature but decreased when total soluble solid increased. It was shown that particles are likely to shrivel when spray drying at high temperature. The suggested conditions for encapsulation of quercetin are feed solution with 0.0625 % (w/w) quercetin and spray drying at drying outlet temperature of 90°C.

Keywords: drying temperature, particle morphology, spray drying, quercetin

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Authors: Mariam Khomasuridze, Nino Chkhartishvili, Irma Chanturia

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The influence of preharvest and postharvest factors on resveratrol, myricetin and quercetin content of wine was studied during the experiment. The content of cis and trans resveratrol, myricetin and quercetin were analyzed by HPLC. In frame of experiment, the various factors affecting on wine composition were researched: variety, climate, viticulture practices, grape maturity, harvesting methods and wine making techniques. The results have shown that varietal potential and amount of yield play the most important role in formation of antioxidant compounds. Based on achieved results, the usage of medium roast oak chips protects resveratrol, myricetin, and quercetin from coagulation and precipitation. Compared to the control samples, the wines, produced by addition of oak chips were approximately four times richer with these antioxidant compounds. The retention of resveratrol was lowered with 45 % in wines, producing in Qvevri by Georgian traditional technology without controlling temperature during fermentation. The opposite effects in case of myricetin, quercetin and total phenolics content were determined. Their concentrations were higher with 56-78%, then in the fermented tank at 22 -25 °C. As the result of the experiment, the optimal technology scheme of wine was worked out, reached by biologically active compounds: resveratrol, myricetin, and quercetin.

Keywords: resveratrol, miricetin, quercetin, wine

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Authors: Dilek Zorlu Kaya, Sena Çenesiz, Utku Duran

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Infectious pancreatic necrosis virus is a disease of great concern in aquaculture, causing mortality of 80 - 90% of the stocks in salmonid production. We aimed to investigate the efficacy of quercetin on oxidant and antioxidant parameters of infectious pancreatic necrosis virus, which is important for fish farming and economy in vitro. Quercetin experimental model was used in the cell culture of Oncorhynchus mykiss infected with infectious pancreatic necrosis virus. Malondialdehyde, ceruloplasmin, total oxidant capacity, total antioxidant levels, and glutathione-peroxidase were measured in the samples. As a result of the study, it was observed that quercetin can minimize the damage caused by scavenging free radicals in cells infected with infectious pancreatic necrosis virus. Thus, we think that an important development can be achieved for fish farming and the economy.

Keywords: IPNV, oncorhynchus mykiss, TAS, TOS, quercetin

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Authors: D. Pradhan, G. Tripathy, S. Pradhan

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Objectives: Imperviousness gainst estrogen treatments is a noteworthy reason for infection backslide and mortality in estrogen receptor alpha (ERα)- positive breast diseases. Tamoxifen or estrogen withdrawal builds the reliance of breast malignancy cells on INT3 flagging. Here, we researched the commitment of Quercetin and INT3 motioning in endocrine-safe breast tumor cells. Methods: We utilized two models of endocrine treatments safe (ETR) breast tumor: Tamoxifen-safe (TamR) and long haul estrogen-denied (LTED) MCF7 cells. We assessed the transitory and intrusive limit of these cells by Transwell cells. Articulation of epithelial to mesenchymal move (EMT) controllers and in addition INT3 receptors and targets were assessed by constant PCR and western smudge investigation. Besides, we tried in-vitro hostile to Quercetin monoclonal Antibodies (mAbs) and Gamma Secretase Inhibitors (GSIs) as potential EMT inversion remedial specialists. At last, we created stable Quercetin overexpressing MCF7 cells and assessed their EMT components and reaction to Tamoxifen. Results: We found that ETR cells procured an Epithelial to Mesenchymal move (EMT) phenotype and showed expanded levels of Quercetin and INT3 targets. Interestingly, we distinguished more elevated amount of INT3 however lower levels of INT1 and INT3 proposing a change to motioning through distinctive INT3 receptors after obtaining of resistance. Against Quercetin monoclonal antibodies and the GSI PF03084014 were powerful in obstructing the Quercetin/INT3 pivot and in part repressing the EMT process. As a consequence of this, cell relocation and attack were weakened and the immature microorganism like populace was essentially decreased. Hereditary hushing of Quercetin and INT3 prompted proportionate impacts. At long last, stable overexpression of Quercetin was adequate to make MCF7 lethargic to Tamoxifen by INT3 initiation. Conclusions: ETR cells express abnormal amounts of Quercetin and INT3, whose actuation eventually drives intrusive conduct. Hostile to Quercetin mAbs and GSI PF03084014 lessen articulation of EMT particles decreasing cell obtrusiveness. Quercetin overexpression instigates Tamoxifen resistance connected to obtaining of EMT phenotype. Our discovering propose that focusing on Quercetin and INT3 warrants further clinical Correlation as substantial restorative methodologies in endocrine-safe breast.

Keywords: endocrine, epithelial, mesenchymal, INT3, quercetin, MCF7

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Authors: S. Pradhan, D. Pradhan, G. Tripathy

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Anti-estrogen treatment resistant is a noteworthy reason for disease relapse and mortality in estrogen receptor alpha (ERα)- positive breast cancers. Tamoxifen or estrogen withdrawal increases the dependance of breast malignancy cells on INT3 signaling. Here, we researched the contribution of Quercetin and INT3 signaling in endocrine resistant breast cancer cells. Methods: We utilized two models of endocrine therapies resistant (ETR-) breast cancer: tamoxifen-resistant (TamR) and long term estrogen-deprived (LTED) MCF7 cells. We assessed the migratory and invasive limit of these cells by Transwell assay. Expression of epithelial to mesenchymal transition (EMT) controllers and in addition INT3 receptors and targets were assessed by real-time PCR and western blot analysis. Besides, we tried in vitro anti-Quercetin monoclonal antibodies (mAbs) and gamma secretase inhibitors (GSIs) as potential EMT reversal therapeutic agents. At last, we created stable Quercetin over expessing MCF7 cells and assessed their EMT features and response to tamoxifen. Results:We found that ETR cells acquired an epithelial to mesenchymal transition (EMT) phenotype and showed expanded levels of Quercetin and INT3 targets. Interestingly, we detected higher level of INT3 however lower levels of INT31 and INT32 proposing a switch to targeting through distinctive INT3 receptors after obtaining of resistance. Anti-Quercetin monoclonal antibodies and the GSI PF03084014 were effective in obstructing the Quercetin/INT3 axis and in part inhibiting the EMT process. As a consequence of this, cell migration and invasion were weakened and the stem cell like population was considerably decreased. Genetic hushing of Quercetin and INT3 prompted proportionate impacts. Finally, stable overexpression of Quercetin was adequate to make MCF7 lethargic to tamoxifen by INT3 activation. Conclusions: ETR cells express abnormal amounts of Quercetin and INT3, whose actuation eventually drives invasive conduct. Anti-Quercetin mAbs and GSI PF03084014 lessen expression of EMT molecules decreasing cellular invasiveness. Quercetin overexpression instigates tamoxifen resistance connected to obtaining of EMT phenotype. Our discovering propose that focusing on Quercetin and/or INT3 warrants further clinical assessment as substantial therapeutic methodologies in endocrine-resistant breast cancer.

Keywords: quercetin, INT3, mesenchymal transition, MCF7 breast cancer cells

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Authors: Jehad Dumireih, Malak Dmirieh, Michael Wink

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The present work is aimed to use plant cell suspension cultures of Crataegus monogyna for biosynthesis of valuable natural products by using quercetin as an inexpensive precursor. Suspension cell cultures of C. monogyna were established by using Murashige and Skoog medium (MS) supplemented with 1 mg/L 2,4-dichlorophenoxyacetic acid and 1 mg/L kinetin. Cells were harvested from the cultures and extracted by using methanol and ethyl acetate; then the extracts were used for the identification of isoquercetin by HPLC and by mass spectrometry. The incubation of the cells with 0.24 mM quercetin for one week resulted in an 16 fold increase of isoquercetin biosynthesis; the growth rate of the cells increased by 20%. Moreover, the biosynthesis of isoquercetin was enhanced by 40% when we divided the added quercetin into three portions each one with concentration 0.12 mM supplied at 3 days intervals. In addition, we didn’t find any positive effects of adding different concentrations the precursors phenylalanine (0.2 mM) and galactose to the cell cultures. In conclusion, the efficiency of the biotransformation of quercetin into isoquercetin depended on the concentration quercetin, its incubation time and the way of its administration. The results of the present work suggest that the biotechnological methods such as cell suspension cultures could be successfully used to obtain highly valuable natural product starting from inexpensive compound.

Keywords: biosynthesis, biotransformation, Crataegus, isoquercetin

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Authors: Lubna Azmi, Ila Shukla, Shyam Sundar Gupta, Padam Kant, C. V. Rao

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Elvitegravir is the mainstay of anti-HIV combination therapy in most endemic countries presently. However, it cannot be used alone owing to its long onset time of action. 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxychromen-4-one (Quercetin: QU) is a polyphenolic compound obtained from Argeria speciosa Linn (Family: Convolvulaceae), an anti-HIV candidate. In the present study, a sensitive, simple and rapid high-performance liquid chromatography coupled with positive ion electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method was developed for the simultaneous determination elvitegravir and Quercetin, in rat plasma. The method was linear over a range of 0.2–500 ng/ml. All validation parameters met the acceptance criteria according to regulatory guidelines. LC–MS/MS method for determination of Elvitegravir and Quercetin was developed and validated. Results show the potential of drug–drug interaction upon co-administration this marketed drugs and plant derived secondary metabolite.

Keywords: anti-HIV resistance, extraction, HPLC-ESI-MS-MS, validation

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Authors: D. Baranova, E. Neborak

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Polyphenols, particularly flavonoids like quercetin, fisetin, and kaempferol, have gained significant attention in nutrition due to their antioxidant, senolytic, and anti-inflammatory properties. These compounds are commonly found in various plant-based foods and are represented by diverse subclasses, each with unique health benefits. Understanding their absorption, metabolism, and bioactivity within the human body is crucial for unlocking their full potential. Quercetin, for instance, exists in multiple forms, impacting its solubility and absorption in the intestine. Its intake, often derived from sources like apples, is affected by cooking methods, with medium heat retaining its potency. Fisetin, also present in fruits and vegetables, demonstrates neuroprotective qualities and stability under varied conditions compared to quercetin. Similarly, kaempferol, found in fruits and vegetables, displays antioxidative effects but is influenced by cooking techniques, with specific methods preserving its polyphenolic content better. Overall, these polyphenols offer promising health benefits, yet their optimal dosage and specific dietary recommendations warrant further research to harness their full nutritional potential.

Keywords: polyphenols, flavonoids, absorption, quercetin, kaempferol, fisetin, senolytics, absorption, cooking method

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Authors: Ayu S. Muhamad, Michael Gleeson

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Immunomodulators are substances that alter immune system via dynamic regulation of messenger molecules. It can be divided into immunostimulant and immunosuppressant. It can help to increase immunity of people with a low immune system, and also can help to normalize an overactive immune system. Aim of this study is to investigate the effects of in vitro exposure to low and high doses of several immunomodulators which include caffeine, kaloba and quercetin on antigen-stimulated whole blood culture cytokine production. Whole blood samples were taken from 5 healthy males (age: 32 ± 12 years; weight: 75.7 ± 6.1 kg; BMI: 24.3 ± 1.5 kg/m2) following an overnight fast with no vigorous activity during the preceding 24 h. The whole blood was then stimulated with 50 µl of 100 x diluted Pediacel vaccine and low or high dose of immunomodulators in the culture plate. After 20 h incubation (5% CO2, 37°C), it was analysed using the Evidence Investigator to determine the production of cytokines including IL-2, IL-4, IL-10, IFN-γ, and IL-1α. Caffeine and quercetin showed a tendency towards decrease cytokine production as the doses were increased. On the other hand, an upward trend was evident with kaloba, where a high dose of kaloba seemed to increase the cytokine production. In conclusion, we found that caffeine and quercetin have potential as immunosuppressant and kaloba as immunostimulant.

Keywords: caffeine, cytokine, immunomodulators, kaloba, quercetin

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Authors: Dipali Nagaonkar, Mahendra Rai

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Chitosan, a carbohydrate polymer at nanoscale level has gained considerable momentum in drug delivery applications due to its inherent biocompatibility and non-toxicity. However, conventional synthetic strategies for chitosan nanoparticles mainly rely upon physicochemical techniques, which often yield chitosan microparticles. Hence, there is an emergent need for development of controlled synthetic protocols for chitosan nanoparticles within the nanometer range. In this context, we report the green synthesis of size controlled chitosan nanoparticles by using Pongamia pinnata (L.) leaf extract. Nanoparticle tracking analysis confirmed formation of nanoparticles with mean particle size of 85 nm. The stability of chitosan nanoparticles was investigated by zetasizer analysis, which revealed positive surface charged nanoparticles with zeta potential 20.1 mV. The green synthesized chitosan nanoparticles were further explored for encapsulation and controlled release of antioxidant biomolecule, quercetin. The resulting drug loaded chitosan nanoparticles showed drug entrapment efficiency of 93.50% with drug-loading capacity of 42.44%. The cumulative in vitro drug release up to 15 hrs was achieved suggesting towards efficacy of green synthesized chitosan nanoparticles for drug delivery applications.

Keywords: Chitosan nanoparticles, green synthesis, Pongamia pinnata, quercetin

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Authors: Samira Ghizellaoui, Manel Boumagoura

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The municipality of Constantine in eastern Algeria draws water from the Hamma groundwater source. The high fouling capacity is due to the high content of bicarbonate (442 mg/L) and calcium (136 mg/L). This work focuses on the use of three new green inhibitors for reducing calcium carbonate scale formation: gallic acid, quercetin and alginate, and on the comparison between them. These inhibitors have proven to be green antiscalants because they have no impact on the environment. Electrochemical methods (chronoamperometry and impedancemetry) were used to evaluate their performance. According to the study, these inhibitors are excellent green chemical inhibitors of scaling, and the best inhibitor is quercetin because it gave a good result with a lower concentration (2mg/L) compared to others inhibitors.

Keywords: scaling, green inhibitor, chronoamperometry, impedancemetry

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Authors: Iliyasu Musa Omoyine, Musa Sunday Abraham, Oladele Sunday Blessing, Iliya Ibrahim Abdullahi, Ibegbu Augustine Oseloka, Nuhu Nana-Hawau, Animoku Abdulrazaq Amoto, Yusuf Abdullateef Onoruoiza, Sambo Sohnap James, Akpulu Steven Peter, Ajayi Abayomi

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The neuroprotective role of inflammation from detrimental intrinsic and extrinsic factors has been reported. However, the overactivation of astrocytes and microglia due to lead toxicity produce excessive pro-inflammatory cytokines, mediating neurodegenerative diseases. The present study investigated the mitigatory effects of quercetin on neuroinflammation, correlating with memory function in lead-exposed rats. In this study, Wistar rats were administered orally with Quercetin (Q: 60 mg/kg) and Succimer as a standard drug (S: 10 mg/kg) for 21 days after lead exposure (Pb: 125 mg/kg) of 21 days or in combination with Pb, once daily for 42 days. Working and reference memory was assessed using an Eight-arm radial water maze (8-ARWM). The changes in brain lead level, the neuronal nitric oxide synthase (nNOS) activity, and the level of neuroinflammatory markers such as tumour necrosis factor-alpha (TNF-α) and Interleukin 1 Beta (IL-1β) were determined. Immunohistochemically, astrocyte expression was evaluated. The results showed that the brain level of lead was increased significantly in lead-exposed rats. The expression of astrocytes increased in the CA3 and CA1 regions of the hippocampus, and the levels of brain TNF-α and IL-1β increased in lead-exposed rats. Lead impaired reference and working memory by increasing reference memory errors and working memory incorrect errors in lead-exposed rats. However, quercetin treatment effectively improved memory and inhibited neuroinflammation by reducing astrocytes’ expression and the levels of TNF-α and IL-1β. The expression of astrocytes and the levels of TNF-α and IL-1β correlated with memory function. The possible explanation for quercetin’s anti-neuroinflammatory effect is that it modulates the activity of cellular proteins involved in the inflammatory response; inhibits the transcription factor of nuclear factor-kappa B (NF-κB), which regulates the expression of proinflammatory molecules; inhibits kinases required for the synthesis of Glial fibrillary acidic protein (GFAP) and modifies the phosphorylation of some proteins, which affect the structure and function of intermediate filament proteins; and, lastly, induces Cyclic-AMP Response Element Binding (CREB) activation and neurogenesis as a compensatory mechanism for memory deficits and neuronal cell death. In conclusion, the levels of neuroinflammatory markers negatively correlated with memory function. Thus, quercetin may be a promising therapy in neuroinflammation and memory dysfunction in populations prone to lead exposure.

Keywords: lead, quercetin, neuroinflammation, memory

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Authors: P. S. Seboletswe, Z. Mkhize, L. M. Katata-Seru

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Protorhus longifolia is known as a medicinal plant that has been used traditionally to treat various ailments such as hemiplegic paralysis, blood clotting related diseases, diarrhoea, heartburn, etc. The study reports a High-Performance Thin Layer Chromatography (HPTLC) fingerprint profile of Protorhus longifolia methanolic extract and its qualitative analysis of gallic acid, rutin, and quercetin. HPTLC analysis was achieved using CAMAG HPTLC system equipped with CAMAG automatic TLC sampler 4, CAMAG Automatic Developing Chamber 2 (ADC2), CAMAG visualizer 2, CAMAG Thin Layer Chromatography (TLC) scanner and visionCATS CAMAG HPTLC software. Mobile phase comprising toluene, ethyl acetate, formic acid (21:15:3) was used for qualitative analysis of gallic acid and revealed eight peaks while the mobile phase containing ethyl acetate, water, glacial acetic acid, formic acid (100:26:11:11) for qualitative analysis of rutin and quercetin revealed six peaks. HPTLC sillica gel 60 F254 glass plates (10 × 10) were used as the stationary phase. Gallic acid was detected at the R_f = 0.35; while rutin and quercetin were not evident in the extract. Further studies will be performed to quantify gallic acid in Protorhus longifolia leaves and also identify other biomarkers.

Keywords: biomarkers, fingerprint profiling, gallic acid, HPTLC, Protorhus longifolia

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Authors: Asif Husain, Shah Alam Khan

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Coumarins and flavones are oxygen containing heterocyclic compounds which are present in various biologically active compounds. Both the heterocyclic rings are associated with diverse biological actions, therefore considered as an important scaffold for the design of molecules of pharmaceutical interest. Aim: To synthesize and evaluate the in vivo anti-inflammatory activity of few coumrain and flavone derivatives containing 1,4 dioxane ring system. Materials and methods: Coumarin derivatives (3a-d) were synthesized by reacting 7,8 dihydroxy coumarin (2a) and its 4-methyl derivative (2b) with epichlorohydrin/ethylene dibromide. The flavone derivatives (10a-d) were prepared by using quercetin and 3,4 dihydroxy flavones. Compounds of both the series were also evaluated for their anti-inflammatory, analgesic activity and ulcerogenicity in animal models by reported methods. Results and Discussion: The structures of all newly synthesized compounds were confirmed with the help of IR, 1H NMR, 13C NMR and Mass spectral studies. Elemental analyses data for each element analyzed (C, H, N) was found to be within acceptable range of ±0.4 %. Flavone derivatives, but in particular quercetin containing 1,4 dioxane ring system (10d) showed better anti-inflammatory and analgesic activity along with reduced gastrointestinal toxicity as compared to other synthesized compounds. The results of anti-inflammatory and analgesic activities of both the series are comparable with the positive control, diclofenac. Conclusion: Compound 10d, a quercetin derivative, emerged as a lead molecule which exhibited potent anti-inflammatory and analgesic activity with significant reduced gastric toxicity.

Keywords: analgesic, anti-inflammatory, 1, 4 dioxane, coumarin, flavone

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Authors: Sumira Jan, Javid Iqbal Mir, Desh Beer Singh, Anil Sharma, Shafia Zaffar Faktoo

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Background and Aims: Climatic and edaphic factors immensely influence crop quality and proper development. Regardless of economic potential, Himalayan Oregano has not subjected to phytonutrient and chemometric evaluation and its relationship with environmental conditions are scarce. The central objective of this research was to investigate microclimatic variation among wild and cultivated populations located in a microclimatic gradient in north-western Himalaya, Kashmir and analyse if such disparity was related with diverse climatic and edaphic conditions. Methods: Micrometeorological, Atomic absorption spectroscopy for micro elemental analysis was carried for soil. HPLC was carried out to estimate variation in phytonutrients and phytochemicals. Results: Geographic variation in phytonutrient was observed among cultivated and wild populations and among populations diverse within regions. Cultivated populations exhibited comparatively lesser phytonutrient value than wild populations. Moreover, our results observed higher vegetative growth of O. vulgare L. with higher pH (6-7), elevated organic carbon (2.42%), high nitrogen (97.41Kg/ha) and manganese (10-12ppm) and zinc contents (0.39-0.50) produce higher phytonutrients. HPLC data of phytonutrients like quercetin, betacarotene, ascorbic acid, arbutin and catechin revealed direct relationship with UV-B flux (r2=0.82), potassium (r2=0.97) displaying parallel relationship with phytonutrient value. Conclusions: Catechin was found as predominant phytonutrient among all populations with maximum accumulation of 163.8 ppm while as quercetin exhibited lesser value. Maximum arbutin (53.42ppm) and quercetin (2.87ppm) accumulated in plants thriving under intense and high UV-B flux. Minimum variation was demonstrated by beta carotene and ascorbic acid.

Keywords: phytonutrient, ascorbic acid, beta carotene, quercetin, catechin

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Authors: Palaniyandi Karuppaiya, Hsin Sheng Tsay, Fang Chen

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Medicinal herbs do represent a huge and noteworthy reservoir for novel anticancer drugs discovery. Dysosma pleiantha (Hance) Woodson (Berberidaceae), one of the oldest traditional Chinese medicinal herb, highly prized by the mountain tribes of Taiwan and China for its medicinal properties contained pharmaceutically important antitumor compounds podophyllotoxin, quercetin and kaempferol. Among lignans, podophyllotoxin is an active antitumor compound and has now been modified to produce clinically useful drugs etoposide and teniposide. In recent years, natural populations of D. peliantha have declined considerably due to anthropogenic activities such as habitat destruction and commercial exploitation for medicinal applications. As to its overall conservation status, D. pleiantha has been ranked as threatened on the China Species Red List. In the present study, an efficient in vitro callus culture system of D. pleiantha was established on Gamborg’s medium with various combinations and concentrations of different auxins and cytokinins under dark condition. Best callus induction was recorded in 2 mg/L 2, 4 - Dichlorophenoxyacetic acid (2,4-D) along with 0.2 mg/L kinetin and the maximum callus proliferation was achieved at 1 mg/L 2,4-D. Among the explants tested, maximum callus induction (86 %) was achieved from tender leaves. Hence, in subsequent experiments, leaf callus was further investigated for suitable callus biomass and production level of anticancer compounds under the influence of different additives. A maximum fresh callus biomass (8.765 g) was recorded in callus proliferation medium contained 500 mg/L casein hydrolysate. High performance liquid chromatography results revealed that the addition of different concentrations of peptone (1, 2 and 4 g/L) in callus proliferation medium enhanced podophyllotoxin (16 fold), quercetin (12 fold) and kaempferol (5 fold) accumulation than control. Thus, the established in vitro callus culture under the influence of different additives may offer an alternative source of enhanced production of podophyllotoxin, kaempferol and quecertin without harming natural plant population.

Keywords: dysosma pleiantha, kaempferol, podophyllotoxin, quercetin

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Authors: Sunil Kumar

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Background: The present study was performed to investigate the antidiabetic effect of the constituents isolated from Sarca asoca by enzyme inhibitory activity. Methods: The dried leaves of Sarca asoca were defatted with petroleum ether and further the same amount plant materials were extracted with methanol. The dried methanol extract was subjected to fractionation and chromatographic separation, which led to the isolation of kaemferol, β-sitosterol and quercetin stigmasterol. Their structures were elucidated on the basis of spectroscopic studies as well as by comparison with the data available in the literature. The compounds were evaluated for in vitro enzyme inhibition effect. Results: The isolated compounds kaemferol, β-sitosterol and stigmasterol showed 45.32, 40.5 and 41.23% α-amylase inhibition respectively and 43.45, 39.29 and 32.43% α-glucosidase inhibition respectively at the conc. of 50 µg/kg. Conclusion: The compounds isolated from Sarca asoca showed in vitro and in vivo antidiabetic activity. So, Euphorbia hirta is a beneficial plant for management of diabetic disorders.

Keywords: diabetes, quercetin, sitosterol, stigmasterol

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Authors: Rajendra Jangde, Deependra Singh

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Present work was based with objective to release of the antimicrobial and debriding agent in sustained manner at the wound surface. In order to provide a long-lasting antimicrobial action and moist environment on wound space, Biocompatible moist system was developed for complete healing. In the present study, a biocompatible moist system of PVA-gelatin hydrogel was developed capable of carrying multiple drugs- Quercetin and Cabopol in controlled manner for effective and complete wound healing. Carbopol and Quercetin were prepared by thin film hydration techniques and optimized system was incorporated in PVA-Gelatin slurry. PVA-Gelatin hydrogels were prepared by freeze thaw method. The prepared dispersion was casted into films to prepare multiphase hydrogel system and characterized by in vitro and in vivo studies. Results revealed the uniform dispersion of microspheres in a three-dimensional matrix of the PVA-Gelatin hydrogel observed at different magnifications. The in vitro release data showed typical biphasic release pattern, i.e., a burst release followed by a slower sustained release for 5 days. Prepared system was found to be stable under both normal and accelerated conditions. Histopathological study showed significant (p<0.05) increase in fibroblast cells, collagen fibres and blood vessels formation. All parameters such as wound contraction, tensile strength, histopathological and biochemical parameters- hydroxyproline content, protein level, etc. were observed significant (p<0.05) in comparison to control group. Present results suggest an accelerated re-epithelialization under moist wound environment with delivery of multiple drugs effective at different stages of wound healing cascade with minimum disturbance of wound bed.

Keywords: multiphase hydrogel, optimization quercetin, wound healing

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Authors: Al-Braa Kashegari, Ali M. El-Halawany, Akram A. Shalabi, Sabrin R. M. Ibrahim, Hossam M. Abdallah

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Chemical investigation of Chrozophora oblongifolia resulted in the isolation of five major compounds that were identified as apeginin-7-O-glucoside (1), quercetin-3-O-glucuronic acid (2), quercetin-3-O-glacturonic acid (3), rutin (4), and 1,3,6-trigalloyl glucose (5). The identity of isolated compounds was assessed by different spectroscopic methods, including one- and two-dimensional NMR. The isolated compounds were tested for their antioxidant activity using different assays viz., DPPH, FRAP, ABTS, ORAC, and metal chelation effects. In addition, the inhibition of target enzymes involved in the metabolic syndrome, such as alpha-glucosidase and pancreatic lipase, were carried out. Moreover, the effect of the compounds on the advanced glycation end-products (AGEs) as one of the major complications of oxidative stress and hyperglycemia in metabolic syndromes were carried out using BSA‐fructose (bovine serum albumin), BSA-methylglyoxal, and arginine methylglyoxal models. The pure isolates showed a protective effect in metabolic syndromes as well as promising antioxidant activity. The results showed potent activity of compound 5 in all measured parameters meanwhile, none of the tested compounds showed activity against pancreatic lipase.

Keywords: Chrozophora oblongifolia, antioxidant, pancreatic lipase, metabolic syndromes

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Authors: Pakakrong Thongdeeying, Srisopa Ruangnoo, Arunporn Itharat

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The rhizomes of Smilax corbularia Kunth have long been used as common ingredients in anticancer preparations. Thus, the objective of this study is to investigate cytotoxicity of S. corbularia and its ingredients against cholangiocarcinoma cell line (KKU-M156) by SRB assay. Ethanolic and water extracts of S. corbularia rhizomes were obtained using the procedures followed by Thai traditional doctors. Bioassay guided isolation was used to isolate cytotoxic compounds. The results revealed that the ethanolic extract of S. corbularia exhibited activity against KKU-M156 cell line with an IC50 value of 84.53±1.62 µg/ml, but the water extract showed no cytotoxic activity. Three flavonoid compounds [astilbin (1), engeletin (2), and quercetin (3)] were isolated from the ethanolic extract. Compound 3 exhibited the strongest activity against KKU-M156 cell line (IC50 = 8.14 ± 1.15 µg/ml), but 1 and 2 showed no cytotoxic activity (IC50 > 100 µg/ml). In conclusion, quercetin showed the highest efficacy against cholangiocarcinoma. These results support the traditional use of this plant by Thai traditional doctors for cancer treatment.

Keywords: cholangiocarcinoma, cytotoxicity, flavonoid, Smilax corbularia

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Authors: Iman A. A. Kassem, Ayman A. Farghaly, Zeinab M. Hassan, Farouk R. Melek, Neveen S. Ghaly

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Lipidium sativum L, an annual herb that grows to 50 cm, is known as an important member of family Brassicaceae. Besides its nutritional value, the seeds were widely used in folk medicine for treatment of cough, asthma, and headache. It was also reported to possess hypocholesterolemic, anti-inflammatory, antidiarrheal, antimicrobial and anticancer activities. In this study, the genoprotective properties of L. sativum seed methanolic extract (LSME) were evaluated in vivo. Three groups of mice were given LSME for five consecutive days at the three dose levels 25, 50 and 100 mg/kg b.wt. The three groups were then injected intraperitoneally with cyclophosphamide at a dose of 20 mg/kg b.wt. to induce DNA damage. A group received only cyclophosphamide (20 mg/kg b.wt.) served as control. LSME significantly inhibited the DNA aberrations in mice caused by cyclophosphamide in a dose-dependent manner in the two groups that received LSME at 50 and 100 mg/kg b.wt. dose levels. The chromosomal aberrations' inhibitory indices were calculated as 18 and 31 in mice bone marrow cells and 27 and 48 in mice spermatocytes, respectively. Phytochemical examination carried out by us revealed that flavonoids were the main chemical constituents of LSME. The major flavonoids kaempferol, kaempferol-3-O-rhamnoside, kaempferol-3-O-glucoside, quercetin, and quercetin-3-O-glucoside were isolated and characterized. It was concluded that the genoprotective effect of LSME might be attributed to the presence of flavonoids which are well-known for their antioxidant properties.

Keywords: cyclophosphamide, flavonoids, genoprotective effect, Lepidium sativum

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Authors: Sara Torabi, Sadegh Khazalpour, Mahdi Jamshidi

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Nitro aromatic compounds are valuable materials because of their applications in the preparation of chemical intermediates for the synthesis of dyes, plastics, perfumes, energetic materials, and pharmaceuticals. Chemical and electrochemical procedures are reported for nitration of aromatic compounds. Flavonoid derivatives are present in many vegetables and fruits and are constituent of many common pharmaceuticals and dietary supplements. Electrochemistry provides very versatile means for the electrosynthesis, mechanistic and kinetic studies. To the best of our knowledge, and despite the importance of these compounds in numerous scientific fields, there are no reports on the electrochemical nitration of Quercetin derivatives. Herein, we describe a green electrochemical synthesis of a nitro compound. In this work, electrochemical oxidation of Quercetin has been studied in the presence of nitrite ion as a nucleophile in acetate buffer solution (c = 0.2 M, pH = 6.0), by means of cyclic voltammetry and controlled-potential coulometry. The results indicate the participation of produced o-benzoquinones in Michael reaction with nitrite ion (in the divided cell) to form the corresponding nitro diol (EC mechanism). The purity of product and characterization was done using ¹H NMR, ¹³C NMR, FTIR spectroscopic techniques. The presented strategies use a water/ethanol mixture as solvent. Ethanol as cosolvent was also used in the previous studies because of its low cost, safety, easy availability, recyclability, bioproductability, and biodegradability. These strategies represent a one-pot and facile process for the synthesis of nitro compound in high yield and purity under green conditions.

Keywords: electrochemical synthesis, green chemistry, cyclic voltammetry, molecular docking

Procedia PDF Downloads 113

Authors: E. Kayitesi, S. Moyo, V. Mavumengwana

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Cleome gynandra (spider plant) is an African green leafy vegetable categorized as an indigenous, underutilized and has been reported to contain essential phenolic compounds. Phenolic compounds play a significant role in human diets due to their proposed health benefits. These compounds however may be affected by different processing methods such as cooking and drying. Cleome gynandra was subjected to boiling, steam blanching, and drying processes and analysed for Total Phenolic Content (TPC), Total Flavonoid Content (TFC), antioxidant activity and flavonoid composition. Cooking and drying significantly (p < 0.05) increased the levels of phenolic compounds and antioxidant activity of the vegetable. The boiled sample filtrate exhibited the lowest TPC followed by the raw sample while the steamed sample depicted the highest TPC levels. Antioxidant activity results showed that steamed sample showed the highest DPPH, FRAP and ABTS with mean values of 499.38 ± 2.44, 578.68 ± 5.19, and 214.39 ± 12.33 μM Trolox Equivalent/g respectively. An increase in quercetin-3-rutinoside, quercetin-rhamnoside and kaempferol-3-rutinoside occurred after all the cooking and drying methods employed. Cooking and drying exerted positive effects on the vegetable’s phenolic content, antioxidant activity as a whole, but with varied effects on the individual flavonoid molecules. The results obtained help in defining the importance of African green leafy vegetable and resultant processed products as functional foods and their potential to exert health promoting properties.

Keywords: Cleome gynandra, phenolic compounds, cooking, drying, health promoting properties

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Authors: Niharul Alam

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The development of energy efficient, economic and eco-friendly synthetic protocols for metal nanoparticles (NPs) with tailor-made structural properties and biocompatibility is a highly cherished goal for researchers working in the field of nanoscience and nanotechnology. In this context, green chemistry is highly relevant and the 12 principles of Green Chemistry can be explored to develop such synthetic protocols which are practically implementable. One of the most promising green chemical synthetic methods which can serve the purpose is biogenic synthetic protocol, which utilizes non-toxic multifunctional reactants derived from natural, biological sources ranging from unicellular organisms to higher plants that are often characterized as “medicinal plants”. Over the past few years, a plethora of medicinal plants have been explored as the source of this kind of multifunctional green chemical agents. In this presentation, we focus on the syntheses of stable monometallic Au and Ag NPs and also bimetallic Au/Ag alloy NPs with highly efficient catalytic property using aqueous extract of leaves of Indian Curry leaf plat (Murraya koenigii Spreng.; Fam. Rutaceae) as green multifunctional agents which is extensively used in Indian traditional medicine and cuisine. We have also studied the interaction between the synthesized metal NPs and surface-adsorbed fluorescent moieties, quercetin and quercetin glycoside which are its chemical constituents. This helped us to understand the surface property of the metal NPs synthesized by this plant based biogenic route and to predict a plausible mechanistic pathway which may help in fine-tuning green chemical methods for the controlled synthesis of various metal NPs in future. We observed that simple experimental parameters e.g. pH and temperature of the reaction medium, concentration of multifunctional agent and precursor metal ions play important role in the biogenic synthesis of Au NPs with finely tuned structures.

Keywords: green multifunctional agent, metal nanoparticles, biogenic synthesis

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Authors: Richa Shri, Varinder Singh, Kundan Singh Bora, Abhishek Bhanot, Rahul Kumar, Amit Kumar, Ravinder Kaur

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The term ‘neuroprotection’ means preserving/salvaging function and structure of neurons. Neuroprotection is an adjunctive treatment option for neurodegenerative disorders. Oxidative stress is considered a major culprit in neurodegenerative disorders; hence, management strategies include use of antioxidants. Our search for a neuroprotective agent began with Allium cepa L. or onions, (family Amaryllidaceae) - a potent antioxidant. We have investigated the neuroprotective potential of onions in experimental models of ischemic stroke, diabetic neuropathy, neuropathic pain, and dementia. In pre and post-ischemic stroke model, the methanol extract of outer scales of onion bulbs (MEOS) prevented memory loss and motor in-coordination; reduced oxidative stress and cerebral infarct size. This also prevented and ameliorated diabetic neuropathy in mice. The MEOS was fractionated to yield a flavonoid rich fraction (FRF) that successfully reversed ischemia-reperfusion induced neuronal damage, thereby demonstrating that the flavonoids are responsible for the activity. The FRF effectively ameliorated chronic constriction induced neuropathic pain in rats. The FRF was subjected to bioactivity-guided fractionated. It was seen that FRF is more effective as compared to the isolated components probably due to synergism among the constituents (i.e., quercetin and quercetin glucosides) in the FRF. The outer scales of onion bulbs have great potential for prevention as well as for treatment of neuronal disorders. Red onions, with higher amounts of flavonoids as compared to the white onions, produced more significant neuroprotection. Thus, the standardized FRF from the waste material of a commonly used vegetable, especially the red variety, may be developed as a valuable neuroprotective agent.

Keywords: Allium cepa, antioxidant activity, flavonoid rich fraction, neuroprotection

Procedia PDF Downloads 119

Authors: R. Raudonis, L. Raudonė, V. Janulis, P. Viškelis

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Pharmacological and clinical studies demonstrated that phenolic compounds particularly flavonoids and phenolic acids are responsible for a wide spectrum of therapeutic activities. Flavonoids and phenolic acids are regarded as natural antioxidants that play an important role in protecting cells from oxidative stress. Qualitatively prepared dry extracts possess high stability and concentration of bio active compounds, facility of standardization and quality control. The aim of this work was to determine the phenolic and antioxidant profiles of Hippophaë rhamnoides L., Betula pendula Roth., Tilia cordata Mill., Sorbus aucuparia L. leaves dry extracts and to identify markers of antioxidant activity. Extracts were analyzed using high-performance liquid chromatography (HPLC) with FRAP post-column assay. Dry extracts are versatile forms possessing wide area of applications, final product ensure consistent phytochemical and functional properties. Seven flavonoids: rutin, hyperoside, isorhamnetin 3-O-rutinoside, isorhamnetin 3-O-glucoside, quercetin, kaempferol, isorhamnetin were identified in dry extract of Hippophaë rhamnoides L. leaves. Predominant compounds were flavonol glycosides which were chosen as markers for quantitative control of dry extracts. Chlorogenic acid, hyperoside, rutin, quercetin, isorhamnetin were prevailing compounds in Betula pendula Roth. leaves extract, whereas strongest ferric reducing activity was determined for chlorogenic acid and hyperoside. Notable amounts of protocatechuic acid and flavonol glycosides, rutin, hyperoside, quercitrin, isoquercitrin were identified in the chromatographic profile of Tilia cordata Mill. Neochlorogenic and chlorogenic acids were significantly dominant compounds in antioxidant profile in dry extract of Sorbus aucuparia L. leaves. Predominant compounds of antioxidant profiles could be proposed as functional markers of quality of phenolic rich raw materials. Dry extracts could be further used for manufacturing of pharmaceutical and nutraceuticals.

Keywords: dry extract, FRAP, antioxidant activity, phenolic

Procedia PDF Downloads 470