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The bioflavonoid quercetin synergises with PPAR-γ agonist pioglitazone in reducing angiotensin-II contractile effect in fructose-streptozotocin induced diabetic rats

Kunasegaran T, Mustafa MR, Murugan DD, Achike FI

Biochimie, 2016 Jun;125:131-9.
PMID: 27012965 DOI: 10.1016/j.biochi.2016.03.008

This study investigated the effects of combined minimal concentrations of quercetin and pioglitazone on angiotensin II-induced contraction of the aorta from fructose-streptozotocin (F-STZ)-induced type 2 diabetic rats and the possible role of superoxide anions (O2(-)) and nitric oxide (NO) in their potential therapeutic interaction. Contractile responses to Ang II of aortic rings from Sprague-Dawley (SD) and F-STZ rats were tested following pre-incubation of the tissues in the vehicle (DMSO; 0.05%), quercetin (Q, 0.1 μM), pioglitazone (P, 0.1 μM) or their combination (P + Q; 0.1 μM each). The amount of superoxide anion was evaluated by lucigenin-enhanced chemiluminescence and dihydroethidium fluorescence, and NO by assay of total nitrate/nitrite, and 4-Amino-5-Methylamino-2',7'-Difluorofluorescein (DAF-FM) diacetate. The synergistic reduction of Ang II-induced contraction of diabetic but not normal aorta with minimally effective concentrations of P + Q occurs through inhibiting O2(-) and increasing NO bioavailability. This finding opens the possibility of maximal vascular protective/antidiabetic effects with low dose pioglitazone combined with quercetin, thus minimizing the risk of adverse effects.

Matched MeSH terms: Quercetin
Fulltext Mechanism(s) of action underlying the gastroprotective effect of ethyl acetate fraction obtained from the crude methanolic leaves extract of Muntingia calabura

Zakaria ZA, Balan T, Azemi AK, Omar MH, Mohtarrudin N, Ahmad Z, et al.

BMC Complement Altern Med, 2016 Feb 24;16:78.
PMID: 26912079 DOI: 10.1186/s12906-016-1041-0

BACKGROUND: Muntingia calabura L. (family Muntingiaceae), commonly known as Jamaican cherry or kerukup siam in Malaysia, is used traditionally to treat various ailments. The aim of this study is to elucidate the possible underlying gastroprotective mechanisms of ethyl acetate fraction (EAF) of Muntingia calabura methanolic leaves extract (MEMC).
METHODS: MEMC and its fractions were subjected to HPLC analysis to identify and quantify the presence of its phyto-constituents. The mechanism of gastroptotection of EAF was further investigated using pylorus ligation-induced gastric lesion rat model (100, 250, and 500 mg/kg). Macroscopic analysis of the stomach, evaluation of gastric content parameters such as volume, pH, free and total acidity, protein estimation, and quantification of mucus were carried out. The participation of nitric oxide (NO) and sulfhydryl (SH) compounds was evaluated and the superoxide dismutase (SOD), gluthathione (GSH), catalase (CAT), malondialdehyde (MDA), prostaglandin E2 (PGE2) and NO level in the ethanol induced stomach tissue homogenate was determined.
RESULTS: HPLC analysis confirmed the presence of quercetin and gallic acid in EAF. In pylorus-ligation model, EAF significantly (p <0.001) prevent gastric lesion formation. Volume of gastric content and total protein content reduced significantly (p quercetin and gallic acid.

Matched MeSH terms: Quercetin/analysis; Quercetin/pharmacology*; Quercetin/therapeutic use
Fulltext Green tea yogurt: major phenolic compounds and microbial growth

Amirdivani S, Baba AS

J Food Sci Technol, 2015 Jul;52(7):4652-60.
PMID: 26139940 DOI: 10.1007/s13197-014-1670-6

The purpose of this study was to evaluate fermentation of milk in the presence of green tea (Camellia sinensis) with respect to changes in antioxidant activity, phenolic compounds and the growth of lactic acid bacteria. Pasteurized full fat cow's milk and starter culture were incubated at 41 °C in the presence of two different types of green tea extracts. The yogurts formed were refrigerated (4 °C) for further analysis. The total phenolic content was highest (p quercetin-rhamnosylgalactoside and quercetin-3-O-galactosyl-rhamnosyl-glucoside for MGTY and JGTY respectively during first 7 day of storage. Diphenyl picrylhydrazyl and ferric reducing antioxidant power methods showed highest antioxidant capacity in MGTY, JGTY and PY. Streptococcus thermophillus and Lactobacillus spp. were highest in MGTY followed by JGTY and PY. This paper evaluates the implementation of green tea yogurt as a new product with functional properties and valuable component to promote the growth of beneficial yogurt bacteria and prevention of oxidative stress by enhancing the antioxidant activity of yogurt.

Matched MeSH terms: Quercetin
Hyptis verticillata attenuates dyslipidaemia, oxidative stress and hepato-renal damage in streptozotocin-induced diabetic rats

Ogar I, Egbung GE, Nna VU, Atangwho IJ, Itam EH

Life Sci, 2019 Feb 15;219:283-293.
PMID: 30668955 DOI: 10.1016/j.lfs.2019.01.027

AIMS: Chronic hyperglycaemia in diabetes mellitus (DM) increases the production of free radicals which results in oxidative stress and related disorders such as cardiovascular diseases, compromised hepatic and renal functions. Hyptis verticillata reportedly demonstrated glucose lowering activity in previous studies. The present study therefore evaluated the effect of H. verticillata on hyperglycaemia-induced dyslipidaemia, hepatorenal distortions, oxidative stress, as well as calculated indices of cardiovascular function.
METHODS: Wistar rats employed for this study consisted of normoglycaemic and diabetic rats in nine experimental groups. The normoglycaemic and diabetic rats were either treated with metformin (500 mg/kg b.w.), quercetin (10 mg/kg b.w.), or ethanol extract of H. verticillata leaf (250 mg/kg b.w. and 500 mg/kg b.w.) administered orally for 28 days.
KEY FINDINGS: Results revealed that H. verticillata significantly lowered blood glucose level, attenuated dyslipidaemia, decreased atherogenic coefficient, atherogenic and coronary risk indices, and increased cardioprotective index in diabetic rats. Also, H. verticillata significantly decreased serum urea, creatinine, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and unconjugated bilirubin levels, relative to untreated diabetic rats. Further, H. verticillata increased serum superoxide dismutase, catalase and glutathione peroxidase activities and glutathione level, and decreased malondialdehyde level in diabetic rats in a manner similar to metformin and quercetin. Histopathological investigation of the liver and kidney revealed restored hepatocytes and amelioration of congested interstitial blood vessel of the Bowman's space of the kidneys upon intervention with H. verticillata.
SIGNIFICANCE: H. verticillata in addition to its anti-hyperglycaemic activity ameliorates oxidative stress, dyslipidaemia, atherogenicity and hepatorenal lesions in DM.

Matched MeSH terms: Quercetin
Fulltext Antiamoebic activity of plant-based natural products and their conjugated silver nanoparticles against Acanthamoeba castellanii (ATCC 50492)

Anwar A, Ting ELS, Anwar A, Ain NU, Faizi S, Shah MR, et al.

AMB Express, 2020 Feb 03;10(1):24.
PMID: 32016777 DOI: 10.1186/s13568-020-0960-9

Acanthamoeba spp. are the causative agent of Acanthamoeba keratitis and granulomatous amoebic encephalitis (GAE). The current options to treat Acanthamoeba infections have limited success. Silver nanoparticles show antimicrobial effects and enhance the efficacy of their payload at the specific biological targets. Natural folk plants have been widely used for treating diseases as the phytochemicals from several plants have been shown to exhibit amoebicidal effects. Herein, we used natural products of plant or commercial sources including quercetin (QT), kolavenic acid (PGEA) isolated from plant extracts of Polyalthia longifolia var pendula and crude plant methanolic extract of Caesalpinia pulcherrima (CPFLM) as antiacanthamoebic agents. Furthermore, these plant-based materials were conjugated with silver nanoparticles (AgNPs) to determine the effects of the natural compounds and their nanoconjugates against a clinical isolate of A. castellanii from a keratitis patient (ATCC 50492) belonging to the T4 genotype. The compounds were conjugated with AgNPs and characterized by using ultraviolet visible spectrophotometry and atomic force microscopy. Quercetin coated silver nanoparticles (QT-AgNPs) showed characteristic surface plasmon resonance band at 443 nm and the average size distribution was found to be around 45 nm. The natural compounds alone and their nanoconjugates were tested for the viability of amoebae, encystation and excystation activity against A. castellanii. The natural compounds showed significant growth inhibition of A. castellanii while QT-AgNPs specifically exhibited enhanced antiamoebic effects as well as interrupted the encystation and excystation activity of the amoebae. Interestingly, these compounds and nanoconjugates did not exhibit in vitro cytotoxic effects against human cells. Plant-based compounds and extracts could be an interesting strategy in development of alternative therapeutics against Acanthamoeba infections.

Matched MeSH terms: Quercetin
Extraction of bioactive compounds from Psidium guajava leaves and its utilization in preparation of jellies

Sampath Kumar NS, Sarbon NM, Rana SS, Chintagunta AD, Prathibha S, Ingilala SK, et al.

AMB Express, 2021 Mar 01;11(1):36.
PMID: 33646462 DOI: 10.1186/s13568-021-01194-9

Psidium guajava L. (guava) is predominantly grown throughout the world and known for its medicinal properties in treating various diseases and disorders. The present work focuses on aqueous extraction of bioactive compounds from the guava leaf and its utilization in the formulation of jelly to improve the public health. The guava leaf extract has been used in the preparation of jelly with pectin (1.5 g), sugar (28 g) and lemon juice (2 mL). The prepared guava leaf extract jelly (GJ) and the control jelly (CJ, without extract) were subjected to proximate, nutritional and textural analyses besides determination of antioxidant and antimicrobial activities. GJ was found to contain carbohydrate (45.78 g/100 g), protein (3.0 g/100 g), vitamin C (6.15 mg/100 g), vitamin B3 (2.90 mg/100 g) and energy (120.6 kcal). Further, the texture analysis of CJ and GJ indicated that both the jellies showed similar properties emphasizing that the addition of guava leaf extract does not bring any change in the texture properties of jelly. GJ exhibited antimicrobial activity against various bacteria ranging from 11.4 to 13.6 mm. Similarly, GJ showed antioxidant activity of 42.38% against DPPH radical and 33.45% against hydroxyl radical. Mass spectroscopic analysis of aqueous extract confirmed the presence of esculin, quercetin, gallocatechin, 3-sinapoylquinic acid, gallic acid, citric acid and ellagic acid which are responsible for antioxidant and antimicrobial properties.

Matched MeSH terms: Quercetin
Fulltext Efficacy of the Aqueous Extract of Azadirachta indica Against the Marine Parasitic Leech and Its Phytochemical Profiling

Venmathi Maran BA, Josmeh D, Tan JK, Yong YS, Shah MD

Molecules, 2021 Mar 29;26(7).
PMID: 33805254 DOI: 10.3390/molecules26071908

Zeylanicobdella arugamensis (Hirudinea), a marine parasitic leech, not only resulted in the mortality of the host fish (Groupers) but also caused economic losses. The current study aimed to elucidate the antiparasitic efficacy of the aqueous extract of the Azadirachta indica leaves against Z. arugamensis and to profile the composition via LC-Q Exactive HF Orbitrap mass spectrometry. Different concentrations (25, 50 and 100 mg/mL) of A. indica extract were prepared and tested on the parasitic leeches. The total mortality of leeches was noticed with an exposure to the A. indica aqueous extract. The average times required for the aqueous extract at concentrations of 25, 50 and 100 mg/mL to kill the leeches were 42.65 ± 9.20, 11.69 ± 1.11 and 6.45 ± 0.45 min, respectively, in a dose-dependent manner. The Orbitrap mass spectrometry analysis indicated the presence of five flavonoids (myricetin 3-O-galactoside, trifolin, isorhamnetin, quercetin and kaempferol), four aromatics (4-methoxy benzaldehyde, scopoletin, indole-3-acrylic acid and 2,4-quinolinediol), three phenolics (p-coumaric acid, ferulic acid and phloretin) and two terpenoids (pulegone and caryophyllene oxide). Thus, our study indicates that A. indica aqueous extract is a good source of metabolites with the potential to act as a biocontrol agent against the marine parasitic leech in aquaculture.

Matched MeSH terms: Quercetin
Garlic flavonoids alleviate H2 O2 induced oxidative damage in L02 cells and induced apoptosis in HepG2 cells by Bcl-2/Caspase pathway

Gao X, Yanan J, Santhanam RK, Wang Y, Lu Y, Zhang M, et al.

J Food Sci, 2021 Feb;86(2):366-375.
PMID: 33448034 DOI: 10.1111/1750-3841.15599

Liver damage is a common liver disorder, which could induce liver cancer. Oral antioxidant is one of the effective treatments to prevent and alleviate liver damage. In this study, three flavonoids namely myricetin, isoquercitrin, and isorhamnetin were isolated and identified from Laba garlic. The isolated compounds were investigated on the protective effects against H2 O2 -induced oxidative damages in hepatic L02 cells and apoptosis inducing mechanism in hepatic cancer cells HepG2 by using MTT assay, flow cytometry and western blotting analysis. Myricetin, isoquercitrin, and isorhamnetin showed proliferation inhibition on HepG2 cells with IC50 value of 44.32 ± 0.213 µM, 49.68 ± 0.192 µM, and 54.32 ± 0.176 µM, respectively. While they showed low toxicity on normal cell lines L02. They could significantly alleviate the oxidative damage towards L02 cells (P < 0.05), via inhibiting the morphological changes in mitochondria and upholding the integrity of mitochondrial structure and function. The fluorescence intensity of L02 cells pre-treated with myricetin, isoquercitrin, and isorhamnetin (100 µM) was 89.23 ± 1.26%, 89.35 ± 1.43% and 88.97 ± 0.79%, respectively. Moreover, the flavonoids could induce apoptosis in HepG2 cells via Bcl-2/Caspase pathways, where it could up-regulate the expression of Bax and down-regulate the expression of Bcl-2, Bcl-xL, pro-Caspase-3, and pro-Caspase-9 proteins in a dose dependent manner. Overall, the results suggested that the flavonoids from Laba garlic might be a promising candidate for the treatment of various liver disorders. PRACTICAL APPLICATION: Flavonoids from Laba garlic showed selective toxicity towards HepG2 cells in comparison to L02 cells via regulating Bcl-2/caspase pathway. Additionally, the isolated flavonoids expressively barred the oxidative damage induced by H2 O2 in L02 cells. These results suggested that the flavonoids from laba garlic could be a promising agent towards the development of functional foods.

Matched MeSH terms: Quercetin/analogs & derivatives; Quercetin/analysis; Quercetin/pharmacology
Fulltext Optimized aqueous extraction conditions for maximal phenolics, flavonoids and antioxidant capacity from Artocarpus heterophyllus (Jackfruit) leaves by response surface methodology (RSM)

Nor Hafiza Sayuti, ‘Ammar Akram Kamarudin, Nor Asma Ab. Razak, Norazalina Saad, Mohd Sabri Pak Dek, Norhaizan Mohd Esa

Malaysian Journal of Medicine and Health Sciences, 2020;16(2):135-144.
MyJurnal

Introduction: There are numerous studies on the therapeutic properties of Artocarpus heterophyllus. However, stud- ies on the aqueous extraction of A. heterophyllus leaves are limited. This present study was conducted to optimize the extraction conditions of A. heterophyllus leaves to yield the highest phenolic, flavonoids and antioxidant contents. Methods: Response surface methodology (RSM) was employed to obtain a higher phenolic extraction parameter(s) of A. heterophyllus leaves using Central Composite Design (CCD). The antioxidant activity was then determined via ABTS (2,29-azinobis (3 ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay and analysis of the individual phenolics was performed by high performance liquid chromatography (HPLC). Results: The optimum extraction conditions with higher phenolics content and antioxidant activity was achieved at 81°C, 100 min and 40 mL/g sample with a good desirability value of 0.87. Under these optimized parameters, total phenolics and flavonoids were 174.48 ± 4.05 mg GAE/g sample and 21.44 ± 0.05 mg RE/g sample, respectively. Meanwhile, antioxidant activity via ABTS and DPPH assays were 90.88% ± 0.09 and 87.22% ± 0.62, respectively. Finally, under optimal extraction conditions revealed 4 compounds identified as chlorogenic acid, quercetin, rutin and kaempferol. Conclusion: The optimisation are promising to improve phenolic yield and antioxidant activity in A. heterophyllus leaves. It also proved that A. heterophyllus leaves can be used as an alternative natural antioxidant especially in medicinal applications since all identified compound possess significant biological activities for human health.

Matched MeSH terms: Quercetin
Fulltext CORRELATION BETWEEN TPC AND TFC WITH ANTIOXIDANT ACTIVITY OF Piper sarmentosum EXTRACT AND ITS FORMULATION FOR COSMETIC PURPOSES

WAN ASIAH WAN SUKAIRI, LAILI CHE ROSE, ASNUZILAWATI ASARI, RAZIFAH MOHD RAZALI

UMT Journal of Undergraduate Research, 2021;3(2):51-60.
MyJurnal

This study investigates the characteristics of an antioxidant cream made from the methanol extract of Piper sarmentosum leaves, which is locally known as the wild betel or pokok kadok in Malay. The secondary metabolites of the leaves were subjected to phytochemical tests to detect the presence of natural compounds. Antioxidant activity was described by its total phenolic content (TPC) and total flavonoid content (TFC), which was assessed by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay. A phase diagram was constructed to find a possible region to formulate an antioxidant cream. In phytochemical screening, the methanolic extract showed positive presence of alkaloids, flavonoids, steroids, terpenoids and tannins. In quantitative analysis of antioxidative components, besides having significantly higher TFC content compared with quercetin (P

Matched MeSH terms: Quercetin
Fulltext Optimum Extraction Condition of Clitorea ternatea Flower on Antioxidant Activities, Total Phenolic, Total Flavonoid and Total Anthocyanin Contents

Jaafar NF, Ramli ME, Mohd Salleh R

Trop Life Sci Res, 2020 Jul;31(2):1-17.
PMID: 32922666 DOI: 10.21315/tlsr2020.31.2.1

Clitoria ternatea is a herbaceous plant with many health benefits. Extraction is crucial to obtain its bioactive components which contribute to its antioxidant properties. Therefore, this study was conducted to find an optimum extraction condition of C. ternatea flower on total phenolic content (TPC) and antioxidant activity (2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical-scavenging activity) as well as to determine its total flavonoid content (TFC) and anthocyanin content based on the optimum extraction condition generated by Response Surface Methodology (RSM)-Design Expert 7.1.5. TPC, TFC and total anthocyanin of C. ternatea were conducted by Folin Ciocalteu (FC), calorimetric assay and pH differential method, respectively. The ranges of selected independent variables were ethanol concentration (30°C-90% v/v), time (60-120 min) and temperature (30°C-70°C). The optimum extraction condition was obtained at 39.62% v/v ethanol concentration, 90 min and 44.24°C. However, these values were slightly adjusted according to the convenience of equipment to operate in which ethanol concentration was adjusted to 37% v/v, time remain at 90 min and temperature at 45°C. The predicted values of TPC and DPPH radical scavenging activity were 41.60 mg GAE/g dry samples and 68.12% inhibition and were experimentally verified to be 41.17 ± 0.5 mg GAE/g dry samples and 63.53 ± 0.95% inhibition of TPC and DPPH radical scavenging activity respectively. This result has showed RSM can optimise TPC and radical scavenging activity of C. ternatea. Upon the optimum condition, the TFC determined was 187.05 ± 3.18 mg quercetin/g dried sample which was higher than TPC and the total anthocyanin content was 28.60 ± 0.04 mg/L. Hence, the extractable phenolic, flavonoid and anthocyanin compounds indicated that C. ternatea is a good source of natural antioxidant.

Matched MeSH terms: Quercetin
Fulltext Effect of different drying methods on the degradation of selected flavonoids in Centella asiatica

Mohd Zainol, M.K., Abdul-Hamid A., Abu Bakar, F., Pak Dek, S.

International Food Research Journal, 2009;16(4):531-537.
MyJurnal

The effect of different drying methods on the degradation of flavonoids in Centella asiatica was evaluated. C. asiatica leaf, root and petiole were dried using air-oven, vacuum oven and freeze drier. Flavonoid was determined utilizing reverse-phase high performance liquid chromatography (RP-HPLC). Results of the study revealed the presence of high concentration of flavonoids in C. asiatica leaf, root and petiole, which include, naringin (4688.8 ± 69 μg/100 g, 3561.3 ± 205 μg/ 100 g, and 978.3 ± 96 μg/ 100 g), rutin (905.6 ± 123 μg/ 100 g, 756.07 ± 95 μg/ 100 g, and 557.25 ± 58 μg/ 100 g), quercetin (3501.1 ± 107 μg/ 100 g, 1086.31 ± 90 μg/ 100 g, and 947.63 ± 83 μg/ 100 g) and catechin (915.87 ± 6.01 μg/ 100 g, 400.6 ± 67 μg/ 100 g, and 250.56 ± 18 μg/ 100g). Luteolin, kaempferol and apigenin on the other hand, were inconsistently present in some parts of C. asiatica. Air-oven treatment resulted in the highest total flavonoids degradation followed by vacuum oven and freeze dried with percent degradation of 97%, 87.6% and 73%, respectively. Catechin and rutin were found to be the most stable flavonoids with percent degradation up to 35%, 66% and 76% for freeze dried, vacuum oven and air oven, respectively.

Matched MeSH terms: Quercetin
Quercetin and pioglitazone synergistically reverse endothelial dysfunction in isolated aorta from fructose-streptozotocin (F-STZ)-induced diabetic rats

Kunasegaran T, Mustafa MR, Achike FI, Murugan DD

Eur J Pharmacol, 2017 Mar 15;799:160-170.
PMID: 28213289 DOI: 10.1016/j.ejphar.2017.02.022

Pioglitazone is an anti-diabetic drug with potential to cause adverse effects following prolonged use. This study, therefore, investigated the effects of combination treatment of a subliminal concentration of pioglitazone and quercetin, a potent antioxidant, on vascular reactivity of aorta isolated from fructose-streptozotocin (F-STZ)-induced diabetic rats. Relaxation to acetylcholine and sodium nitroprusside, and contraction to phenylephrine were tested in organ bath chambers following pre-incubation with vehicle (DMSO; 0.05%), quercetin (10-7 M), pioglitazone (10-7 M), or their combination (P+Q; 10-7 M each drug). Subliminal concentration of quercetin or pioglitazone did not alter the acetylcholine- induced relaxation nor the phenylephrine-induced contraction in both normal rat and diabetic F-STZ induced tissues. However, P+Q combination synergistically improved the impaired acetylcholine-induced relaxation and decreased the elevated phenylephrine-induced contraction in aortic rings from diabetic, but not in the normal rats. Neither mono nor combination treatment altered sodium nitroprusside-induced relaxation. The combination also synergistically decreased superoxide anion and increased nitric oxide production compared to the individual treatments in aorta from diabetic rats. Overall, these data demonstrated a synergistic effect, in which, a combination (P+Q; 10-7 M each drug) caused a significantly greater effect than 10-6 M of either agent in improving endothelial function of isolated diabetic aorta. In conclusion, a combination of subliminal concentrations of pioglitazone and quercetin is able to decrease oxidative stress and provide synergistic vascular protection in type 2 diabetes mellitus and thus the possibility of using quercetin as a supplement to pioglitazone in the treatment of diabetes with the goal of reducing pioglitazone toxicity.

Matched MeSH terms: Quercetin
Fulltext Antimicrobial activity and chemical composition of Pistacia chinensis Bunge leaves

Rashed, K., Said, A., Abdo, A., Selim, S.

International Food Research Journal, 2016;23(1):316-321.
MyJurnal

This work was carried out for determining antimicrobial activity of Pistacia chinensis leaves
methanol extract and identifying the chemical composition of the plant extract. Methanol extract
was tested for antimicrobial activity using disc-diffusion assay and the extract was fractionated
on silica gel column chromatography for the isolation of the bio-active constituents. The leaves
extract of P. chinensis showed a significant antimicrobial effect, it strongly inhibited the growth
of the test bacteria and yeast studied. Chromatograpic separation of the methanol extract of
P. chinensis leaves has led to the isolation and characterization of β-sitosterol, luepol, and
six flavonoids, quercetin, myricetin, quercetin 3-O-α-rhamnoside, quercetin 3-O-β-glucoside,
myricetin 3-O-α-rhamnoside and myricetin 3-O-β-glucuronide using various chromatographic
procedures and the interpretation of spectral data in comparison with already existing data
reported in the literature. The results presented here may suggest that the leaves extract of P.
chinensis possess antimicrobial properties, and therefore, can be used as natural preservative
ingredients in food and/or pharmaceuticals.

Matched MeSH terms: Quercetin
In-depth hepatoprotective mechanistic study of Phyllanthus niruri: In vitro and in vivo studies and its chemical characterization

Ezzat MI, Okba MM, Ahmed SH, El-Banna HA, Prince A, Mohamed SO, et al.

PLoS One, 2020;15(1):e0226185.
PMID: 31940365 DOI: 10.1371/journal.pone.0226185

Phyllanthus niruri L. is a widespread tropical plant which is used in Ayurvedic system for liver and kidney ailments. The present study aims at specifying the most active hepatoprotective extract of P. niruri and applying a bio-guided protocol to identify the active compounds responsible for this effect. P. niruri aerial parts were extracted separately with water, 50%, 70% and 80% ethanol. The cytoprotective activity of the extracts was evaluated against CCl4-induced hepatotoxicity in clone-9 and Hepg2 cells. Bioassay-guided fractionation of the aqueous extract (AE) was accomplished for the isolation of the active compounds. Antioxidant activity was assessed using DPPH (1, 1-diphenyl-2-picrylhydrazyl) radical scavenging method and ferric reducing antioxidant power (FRAP). The in vivo hepatoprotective activity of AE was evaluated in CCl4-induced hepatotoxicity in rats at different doses after determination of its LD50. Pretreatment of clone-9 and Hepg2 with different concentrations of AE (1, 0.1, 0.01 mg/ml) had significantly reduced the levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) against CCl4 injures, and restored the activity of the natural antioxidants; glutathione (GSH) and superoxide dismutase (SOD) towards normalization. Fractionation of AE gave four fractions (I-IV). Fractions I, II, and IV showed a significant in vitro hepatoprotective activity. Purification of I, II and IV yielded seven compounds; corilagin C1, isocorilagin C2, brevifolin C3, quercetin C4, kaempferol rhamnoside C5, gallic acid C6, and brevifolin carboxylic acid C7. Compounds C1, C2, C5, and C7 showed the highest (p< 0.001) hepatoprotective potency, while C3, C4, and C6 exhibited a moderate (p< 0.001) activity. The AE exhibited strong antioxidant DPPH (IC50 11.6 ± 2 μg/ml) and FRAP (79.352 ± 2.88 mM Ferrous equivalents) activity. In vivo administration of AE in rats (25, 50, 100 and 200 mg/kg) caused normalization of AST, ALT, alkaline phosphatase (ALP), lactate dehydrogenase (LDH), total cholesterol (TC), triglycyrides (TG), total bilirubin (TB), glucose, total proteins (TP), urea and creatinine levels which were elevated by CCl4. AE also decreased TNF-α, NF-KB, IL-6, IL-8, IL10 and COX-2 expression, and significantly antagonizes the effect of CCl4 on the antioxidant enzymes SOD, catalase (CAT), glutathione reductase (GR), and glutathione peroxidase (GSP). The histopathological study also supported the hepatoprotective effect of AE. P. niruri isolates exhibited a potent hepatoprotective activity against CCl4-induced hepatotoxicity in clone-9 and Hepg2 cell lines through reduction of lipid peroxidation and maintaining glutathione in its reduced form. This is attributable to their phenolic nature and hence antioxidative potential.

Matched MeSH terms: Quercetin
Fulltext Endogenous Antioxidant and LOX-Mediated Systems Contribute to the Hepatoprotective Activity of Aqueous Partition of Methanol Extract ofMuntingia calaburaL. Leaves against Paracetamol Intoxication

Zakaria ZA, Mahmood ND, Mamat SS, Nasir N, Omar MH

Front Pharmacol, 2017;8:982.
PMID: 29497375 DOI: 10.3389/fphar.2017.00982

Methanol extract ofMuntingia calaburaL. (family Muntingiaceae) leaf has been reported to exert various pharmacological activities including hepatoprotection. The present study was carried out to identify the most effective hepatoprotective partition derived from the extract and to determine the mechanisms of action involved. The extract was partitioned using solvents with different polarity to yield petroleum ether (PEMC), ethyl acetate (EAMC), and aqueous (AQMC) extracts. Each extract, at 250 mg/kg, was subjected to the paracetamol (PCM)-induced hepatotoxic assay and several parameters such as liver weight, liver/body weight ratio, serum liver enzymes' level, and histopathological examinations were determined. Each partition was also tested for their antioxidant and anti-inflammatory potentials. The most effective extract (AQMC) was prepared in additional dose of 50 and 500 mg/kg, and then subjected to the same liver toxicity test in addition to the endogenous antioxidant enzymes assay. Moreover, AQMC was also subjected to the phytochemical screening and HPLC analysis. Overall, from the results obtained: AQMC exerted significant (p< 0.05): (i) antioxidant activity when assessed using the DPPH, SOD and ORAC assays with high TPC detected; (ii) anti-inflammatory activity via LOX, but not XO pathway; (iii) hepatoprotective activity indicated by its ability to reverse the effect of PCM on the liver weight and liver/body weight ratio, the level of serum liver enzymes (ALT, AST, and ALP), and activity of several endogenous antioxidant enzymes (SOD and CAT). Phytochemicals analyses demonstrated the presence of several flavonoid-based bioactive compounds such as gallic acid and quercetin, which were reported to possess hepatoprotective activity. In conclusion, AQMC exerts hepatoprotective activity against the PCM-induced toxicity possibly by having a remarkable antioxidant potential and ability to activate the endogenous antioxidant system possibly via the synergistic action of its phytoconstituents.

Matched MeSH terms: Quercetin
Fulltext Safety Assessment of Methanol Extract of Melastoma malabathricum L. Leaves following the Subacute and Subchronic Oral Consumptions in Rats and Its Cytotoxic Effect against the HT29 Cancer Cell Line

Kamsani NE, Zakaria ZA, Md Nasir NL, Mohtarrudin N, Mohamad Alitheen NB

Evid Based Complement Alternat Med, 2019;2019:5207958.
PMID: 31885651 DOI: 10.1155/2019/5207958

Methanol extract of Melastoma malabathricum (MEMM) has been traditionally used by the Malay to treat various ailments. In an attempt to develop the plant as an herbal product, MEMM was subjected to the subacute and subchronic toxicity and cytotoxicity studies. On the one hand, the subacute study was performed on three groups of male and three groups of female rats (n = 6), which were orally administered with 8% Tween 80 (vehicle control group) or MEMM (500 and 1000 mg/kg) daily for 28 days, respectively. On the other hand, the subchronic study was performed on four groups of rats (n = 6), which were orally administered with 8% Tween 80 (vehicle control group) or MEMM (50, 250, and 500 mg/kg) daily for 90 days, respectively. In the in vitro study, the cytotoxic effect of MEMM against the HT29 colon cancer cell line was assessed using the MTT assay. MEMM was also subjected to the UHPLC-ESI-HRMS analysis. The results demonstrated that MEMM administration did not cause any mortality, irregularity of behaviour, modification in body weight, as well as food and water intake following the subacute and subchronic oral treatment. There were no significant differences observed in haematological parameters between treatment and control groups in both studies, respectively. The in vitro study demonstrated that MEMM exerts a cytotoxic effect against the HT29 colon cancer cell line when observed under the inverted and phase-contrast microscope and confirmed by the acridine orange/propidium iodide (AOPI) staining. The UHPLC-ESI-HRMS analysis of MEMM demonstrated the occurrence of several compounds including quercetin, p-coumaric acid, procyanidin A, and epigallocatechin. In conclusion, M. malabathricum leaves are safe for oral consumption either at the subacute or subchronic levels and possess cytotoxic action against the HT29 colon cancer cells possibly due to the synergistic action of several flavonoid-based compounds.

Matched MeSH terms: Quercetin
Fulltext Optimization of Extraction Conditions of Phytochemical Compounds and Anti-Gout Activity of Euphorbia hirta L. (Ara Tanah) Using Response Surface Methodology and Liquid Chromatography-Mass Spectrometry (LC-MS) Analysis

Abu Bakar FI, Abu Bakar MF, Abdullah N, Endrini S, Fatmawati S

Evid Based Complement Alternat Med, 2020;2020:4501261.
PMID: 32047524 DOI: 10.1155/2020/4501261

Gout is a common disease affected most of the people due to the elevation of uric acid in the blood. Flavonoid and phenolic compounds are reported to exert the anti-gout activity of medicinal plants. Hence, this study aimed at optimizing the extraction conditions of phenolic and flavonoid compounds as well as the anti-gout (xanthine oxidase inhibitory activity) in vitro of Euphorbia hirta using response surface methodology (RSM). The plant part used was the whole plant excluding roots. The effects of three independent variables (extraction time, X1; extraction temperature, X2; and solid-to-liquid ratio, X3) on three response variables (total flavonoid content, Y1; total phenolic content, Y2; and xanthine oxidase inhibitory activity, Y3) were determined using central composite design (CCD) while phytochemical profiling of the extracts was determined by liquid chromatography-mass spectrometry (LC-MS). Quadratic models produced a satisfactory fitting of the experimental data with regard to total flavonoid content (r2 = 0.9407, p < 0.0001), total phenolic content (r2 = 0.9383, p < 0.0001), and xanthine oxidase inhibitory activity (r2 = 0.9794, p < 0.0001). The best extraction conditions observed for total flavonoid content, total phenolic content, and xanthine oxidase inhibitory activity were at a temperature of 79.07°C for 17.42 min with solid-to-liquid ratio of 1 : 20 g/ml. The optimum values for total flavonoid, total phenolic, and xanthine oxidase inhibitory activity were 67.56 mg RE/g, 155.21 mg GAE/g, and 91.42%, respectively. The main phytochemical compounds in the optimized E. hirta extract are neochlorogenic acid, quercetin-3β-D-glucoside, syringic acid, caffeic acid, ellagic acid, astragalin, afzelin, and quercetin. As conclusion, this study clearly demonstrated the best conditions to obtain higher xanthine oxidase inhibitory activity and phytochemical compounds which can be further used for the development of anti-gout agents.

Matched MeSH terms: Quercetin
Fulltext Evaluation of Bioactive Compounds, Pharmaceutical Quality, and Anticancer Activity of Curry Leaf (Murraya koenigii L.)

Ghasemzadeh A, Jaafar HZ, Rahmat A, Devarajan T

Evid Based Complement Alternat Med, 2014;2014:873803.
PMID: 24693327 DOI: 10.1155/2014/873803

In this study, we investigated some bioactive compounds and pharmaceutical qualities of curry leaf (Murraya koenigii L.) extracts from three different locations in Malaysia. The highest TF and total phenolic (TP) contents were observed in the extracts from Kelantan (3.771 and 14.371 mg/g DW), followed by Selangor (3.146 and 12.272 mg/g DW) and Johor (2.801 and 12.02 mg/g DW), respectively. High quercetin (0.350 mg/g DW), catechin (0.325 mg/g DW), epicatechin (0.678 mg/g DW), naringin (0.203 mg/g DW), and myricetin (0.703 mg/g DW) levels were observed in the extracts from Kelantan, while the highest rutin content (0.082 mg/g DW) was detected in the leaves from Selangor. The curry leaf extract from Kelantan exhibited higher concentration of gallic acid (0.933 mg/g DW) than that from Selangor (0.904 mg/g DW) and Johor (0.813 mg/g DW). Among the studied samples, the ones from Kelantan exhibited the highest radical scavenging activity (DPPH, 66.41%) and ferric reduction activity potential (FRAP, 644.25 μ m of Fe(II)/g) followed by those from Selangor (60.237% and 598.37 μ m of Fe(II)/g) and Johor (50.76% and 563.42 μ m of Fe(II)/g), respectively. A preliminary screening showed that the curry leaf extracts from all the locations exhibited significant anticarcinogenic effects inhibiting the growth of breast cancer cell line (MDA-MB-231) and maximum inhibition of MDA-MB-231 cell was observed with the curry leaf extract from Kelantan. Based on these results, it is concluded that Malaysian curry leaf collected from the North (Kelantan) might be potential source of potent natural antioxidant and beneficial chemopreventive agents.

Matched MeSH terms: Quercetin
Antinociceptive and antineuropathic effects of Trifolium resupinatum L. on formalin-induced nociception and cervical spinal cord hemi-contusion: Underlying Mechanisms

Jabbari S, Zakaria ZA, Mohammadi S

J Ethnopharmacol, 2025 Jan 30;337(Pt 2):118913.
PMID: 39369921 DOI: 10.1016/j.jep.2024.118913

ETHNOPHARMACOLOGICAL RELEVANCE: Trifolium resupinatum L. (Fabaceae), known as Persian clover, ethnomedicinally used in Persian folk medicine to treat peritoneal inflammation, rheumatism, and back pain.
AIM OF THE STUDY: To investigate the antineuropathic and antinociceptive activities of Trifolium resupinatum leaves essential oil (TREO) in male Wistar rats, as well as to explore the potential mechanisms of action.
MATERIALS AND METHODS: The antinociceptive activity of TREO and its main constituents, quercetin (Qc) was assessed using the formalin-induced paw licking test. Moreover, the potential mechanisms of antinociception were evaluated through various competitive and non-competitive antagonisms. Additionally, the antineuropathic potential was investigated using the cervical spinal cord hemi-contusion (CCS) model, and the role of phosphorylated Stat-3 was analyzed using Western blotting.
RESULTS: TREO exerted significant antinociceptive activity (P

Matched MeSH terms: Quercetin/analogs & derivatives; Quercetin/isolation & purification; Quercetin/pharmacology

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