An Updated Review Summarizing the Anticancer Potential of Naringenin.

One important phytochemical is naringenin, which belongs to the flavanone class of polyphenols. It is found in citrus fruits, such as grapefruits, but it can also be found in tomatoes, cherries, and other food-grade medicinal plants. Naringenin has a significant chemotherapeutic promise, as several investigations have conclusively shown. Therefore, the goal of this review is to synthesize the literature that has been done on naringenin as a possible anti-cancer agent and clarify the mechanisms of action that have been described in treatment plans for different kinds of cancer. In a variety of cancer cells, naringenin works by affecting several pathways associated with cell cycle arrest, anti-metastasis, apoptosis, anti-angiogenesis, and DNA repair. It has been shown to alter several molecular targets linked to the development of cancer, such as drug transporters, transcription factors, reactive nitrogen species, reactive oxygen species, cellular kinases, and inflammatory cytokines and regulators of the cell cycle. In summary, this research provides significant insights into the potential of naringenin as a strong and prospective candidate for use in medicines, nutraceuticals, functional foods, and dietary supplements to improve the management of carcinoma.

Complete genome sequence of mcr-9 containing Leclercia adecarboxylata.

Here, we provide the genome sequence of a Leclercia adecarboxylata isolated from a screen of an environmental bacterial isolate library for resistance to the plant flavonoid berberine. We detected the colistin resistance gene mcr-9, located on an IncFII(pECLA) plasmid.

Inhibition of azole-resistant Candida albicans ATPase and oxidoreductase activity by a flavonoid from Dalea elegans.

BACKGROUND: The flavonoid 2', 4'-dihydroxy-5'-(1''', 1'''-dimethylallyl)-8-prenylpinocembrin (8PP) obtained from Dalea elegans roots inhibits cell growth and cdr pumps, in addition to reversing fluconazole (FCZ) resistance in Candida albicans. AIMS: To study the effects of 8PP and FCZ on cdr-associated ATPase and cell energy generation in azole-resistant C. albicans planktonic cultures. MATERIALS AND METHODS: ATPase activity was measured as oligomycin-sensitive release of inorganic phosphate in fractions containing plasmatic membranes. Cell oxidoreductase activity was evaluated by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) reduction in C. albicans cells. RESULTS: FCZ, 8PP and their combination at a concentration of 125 µM of each compound inhibit ATPase activity by 61; 58 and 70, respectively. Inhibitory concentration 50 % (IC50) of 8PP was 78.59 ± 1.45 and 104.70 ± 1.25 µM for FCZ. In combination with 125 µM 8PP, FCZ IC50 was reduced by 3 times. Km was 0.96 ± 0.35 mM and Vmax 43.58 ± 5.49 picomoles/mg protein.min. At 125 µM, 8PP shifts the ATP saturation plot to right. A Dixon study using 2 and 5 mM ATP suggests a competitive interaction of 8PP and ATP for the hydrolysis enzymatic site. FCZ, 8PP or their combination at 125 µM does not produce cytotoxicity dependent on oxidoreductase activity. At higher concentrations, toxic effects are observed with both drugs at the MTT assay. IC50 (µM) was 355 ± 6 and 789 ± 11, for 8PP and FCZ, respectively. CONCLUSIONS: The flavonoid 8PP inhibits competitively oligomycin-sensitive ATPase activity associated to cdr transporters and decreases oxidoreductase-dependent cell viability in azole-resistant Candida albicans.

Quercetin: A Potential Candidate for the Treatment of Arthritis.

Diet plays a significant role in ensuring healthy life, and the bioactive compounds present in food and medicinal plants may be developed as drugs that combat various illnesses. A bioactive flavanoid, quercetin which is a dietary component, possesses numerous health-promoting effects. In preclinical models of rheumatoid arthritis, gouty arthritis and osteoarthritis, quercetin has shown significant joint protective effects. Taking into account the significance of this compound, the present review discusses its anti-arthritic properties, demonstrating its mechanism of action for the treatment of arthritis with its therapeutic potential.

The relationship between Hirshfeld potential and cytotoxic activity: a study along a series of flavonoid and chromanone derivatives.

The present study examines a series of six biologically-active flavonoid and chromanone derivatives by X-ray crystal structure analysis: (E)-3-benzylidene-2-phenylchroman-4-one, C22H16O2, I, (E)-3-(4-methylbenzylidene)-2-phenylchroman-4-one, C23H18O2, II, (E)-3-(3-methylbenzylidene)-2-phenylchroman-4-one, C23H18O2, III, (E)-3-(4-methoxybenzylidene)-2-phenylchroman-4-one, C23H18O3, IV, (E)-3-benzylidenechroman-4-one, C16H12O2, V, and (E)-3-(4-methoxybenzylidene)chroman-4-one, C17H14O3, VI. The cytotoxic activities of the presented crystal structures have been determined, together with their intermolecular interaction preferences and Hirshfeld surface characteristics. An inverse relationship was found between the contribution of C...C close contacts to the Hirshfeld surface and cytotoxic activity against the WM-115 cancer line. Dependence was also observed between the logP value and the percentage contribution of C...H contacts to the Hirshfeld surface.

Flavonoid glucosides from the flowers of Trollius chinensis Bunge.

Four new flavonoid glucosides, 2″-O-(6‴-O-caffeoyl)-galactopyranosylvitexin (1), 2″-O-(6‴-O-veratroyl)-galactopyranosylvitexin (2), 2″-O-(6‴-O-feruloyl)-galactopyranosylorientin (3), 2″-O-(2‴-O-methylbutyryl)-glucopyranosylisoswertisin (4), along with three known compounds were isolated from the flowers of Trollius chinensis Bunge. Their structures were determined by extensive spectroscopic analyses.

Effect of pregelatination on rheology, cooking and antioxidant activity of pasta.

The present study explores the possibility of using twin screw extruder for preparation of pregelatinized pasta. The effects of extrusion parameters feed moisture (28 and 32%), barrel temperature (60-105 °C) and screw speed (100-200 rpm) on pregelatinized pasta were investigated. Prepared pasta was analysed for quality characteristics in terms of cooking quality, degree of gelatinization, color, texture, pasting properties, bioactive composition. Results indicated that higher screw speed improved the cooking quality of pasta and decreased gruel solid loss. Degree of gelatinization revealed positive relation with temperature and feed moisture. Extrusion conditions, altered the color of pasta, a decrease in L*, increase in a* and b* values was observed. Higher peak viscosity was observed at lower barrel temperature and feed moisture. A significant retention in total phenolic content and flavonoid content was observed with higher feed moisture. Extrusion leads to increase in antioxidant activity and firmness upon increasing screw speed and feed moisture.

Interactions of a prenylated flavonoid from Dalea elegans with fluconazole against azole- resistant Candida albicans.

BACKGROUND: The prenylated flavonoid 2', 4'-dihydroxy-5'-(1'″, 1'″-dimethylallyl)-8-prenylpinocembrin (8PP, formerly 6PP) shows antifungal activity, inhibits rhodamine 6G efflux and reverses fluconazole (FCZ) resistance in azole-resistant Candida albicans overexpressing cdr1, cdr2 and mdr1 transporters. PURPOSE AND DESIGN: In this paper, we tried to characterize 8PP in vitro interactions on the cell growth and lethality of C. albicans. We also initiated preliminary in vivo toxicological studies on mice. METHODS: The effects of 8PP and FCZ on cell growth and viability of C. albicans were evaluated by CLSI guidelines. The checkerboard assay was used to search for interactions on cell growth. The time-kill assay was used to study fungicidal effects. Acute toxicity was evaluated at a single dose schedules. RESULTS: From the checkerboard design, and using a starting inoculum of 103CFU/ml, the fractional inhibitory concentration (FIC) of FCZ and 8PP could be determined as 0.11 and 0.50, respectively, with a FIC index value (FICI) of 0.61. This FICI and the isobologram showing a concave shape suggests an additive interaction between them. At a higher starting inoculum (105CFU/ml), C. albicans growth and viability were decreased by FCZ, 8PP and their combination in a concentration-dependent way. For FCZ, minimum fungicidal concentration (MFC) and FC50 (the concentration that kills 50% of the fungal cells) were 4-fold reduced (280-70µM) in combination with 125µM 8PP. A decrease of 3 log units in viable counts with respect to control was reached (3.65 ± 1.05 ‰, p< 0.0001). Thus, both fungistatic compounds when combined achieved an almost complete fungicidal effect at lower concentrations respecting of each of them alone. In preliminary toxicological assessment, lethal dose 50% (LD50) for 8PP by the i.p. route was 357 and 245mg/kg, for female and male adult albino mice, respectively. FCZ LD50 was 785 and 650mg/kg for female and male animals, respectively CONCLUSIONS: In vitro results suggest additive interactions between 8PP and FCZ with respect to C. albicans cell growth. Besides killing per se, 8PP helps FCZ to achieve an almost complete fungicidal effect, which would be crucial to eradicate fungal infections.

Design and development of some thiazole-based flavanoids as novel antibacterial against pathogens causing surgical site infection for possible benefit in bone trauma via inhibition of DNA gyrase.

In this study, a novel class of hybrid thiazole-based flavanoid derivatives were synthesized and characterized by FT-IR, 1 H-NMR, 13 C-NMR, mass and elemental analysis. These derivatives were evaluated for antibacterial activity for possible benefit in bone trauma via inhibition of DNA gyrase enzyme. Results suggested that compounds 9n, 9o, and 9p showed considerable inhibition of DNA gyrase with considerable activity against tested forty strains of Staphylococcus aureus clinical isolates. Moreover, compound 9n showed hydrogen bonding with LYS460 along with low binding free energy of -4.36 kcal/mol against DNA gyrase enzyme. The hemolytic activity of the potent compounds showed mild to no activity together with excellent pharmacokinetics, suggesting to have a potential for the development of designed compounds as novel antibacterial agents.

Variation in Phenolics, Flavanoids, Antioxidant and Tyrosinase Inhibitory Activity of Peach Blossoms at Different Developmental Stages.

Peach blossoms were harvested and classified into six developmental stages: (I) bud emerging stage; (II) middle bud stage; (III) large bud stage; (IV) initial-flowering stage; (V) full-flowering stage; and (VI) end-flowering stage. The contents of total phenolics, flavanoids, individual phenolic compounds as well as antioxidant and tyrosinase inhibitory activity of peach blossoms at different developmental stages were investigated. The total phenolic contents varied from 149.80 to 74.80 mg chlorogenic acid equivalents/g dry weight (DW), and the total flavanoid contents ranged from 93.03 to 44.06 mg rutin equivalents/g DW. Both the contents of total phenolics and flavanoids decreased during blossom development. Chlorogenic acid was the predominant component, accounting for 62.08%-71.09% of the total amount of identified phenolic compounds in peach blossom. The antioxidant capacities determined by different assays and tyrosinase inhibitory activity also showed descending patterns during blossom development. Significant correlations were observed between antioxidant capacities with contents of total phenolics and total flavanoids as well as chlorogenic acid, cinnamic acid and kaempferol-3-O-galactoside, while the tyrosinase inhibitory activity had lower correlations with total phenolics and total flavanoids as well as chlorogenic acid, quercetin-3-O-rhamnoside, kaempferol-3-O-galactoside and cinnamic acid. The antioxidant activities of peach blossom seemed to be more dependent on the phenolic compounds than tyrosinase inhibitory activity.

Phytochemical screening and analysis of antioxidant properties of aqueous extract of wheatgrass.

OBJECTIVE: To screen the phytochemical constituents and study antioxidant properties of the aqueous extract of the wheatgrass. METHODS: The current study was focused on broad parameters namely, phytochemical analysis, gas chromatography-mass spectrometry analysis and antioxidant properties in order to characterize the aqueous extract of wheatgrass as a potential free radical quencher. RESULTS: The phytochemical screening of the aqueous extract of wheatgrass showed the presence of various secondary metabolites but the absence of sterols and quinone in general. Wheatgrass was proved to be an effective radical scavenger in all antioxidant assays. The gas chromatography-mass spectrometry analysis confirmed the presence of diverse category of bioactive compounds such as squalene, caryophyllene and amyrins in varying percentage. CONCLUSIONS: From the results obtained, we conclude that wheatgrass aqueous extract contains various effective compounds. It is a potential source of natural antioxidants. Further analysis of this herb will help in finding new effective compounds which can be of potent use in pharmacological field.

Synthesis and biological evaluation of baicalein derivatives as potent antitumor agents.

Baicalein (5,6,7-trihydroxy-2-phenyl-4H-chromen-4-one), a major flavonoid extracted from the root of Scutellaria baicalensis Georgi (Chinese name: Huangqin), showed potent anti-proliferative activity against a broad panel of human cancer cell lines both in vitro and in vivo. A novel series of baicalein derivatives were synthesized by introducing a group to C6-OH and a nitrogen-containing hydrophilic heterocyclic ring to C7-OH via a length of 3 or 4-carbon chain in this study. The in vitro antiproliferative activities of the 30 derivatives against HepG2, A549, BCG-823 cancer cell lines were evaluated. Among them, 10 compounds exhibit more potent cytotoxicity than baicalein against the three cancer cell lines. The most potent compound 9b possesses highest anti-proliferative potency against HepG2, A549, and BCG-823 with an IC50 value of 2.0 µM, 0.8 µM and 3.2 µM, respectively. Preliminary mechanism studies with compound 9b using Annexin V/PI double-staining assay and DAPI staining assay indicated that 9b inhibits tumor cell proliferation potentially through inducing apoptosis.

Phytochemical screening and analysis of antioxidant properties of aqueous extract of wheatgrass

Objective: To screen the phytochemical constituents and study antioxidant properties of the aqueous extract of the wheatgrass. Methods: The current study was focused on broad parameters namely, phytochemical analysis, gas chromatography-mass spectrometry analysis and antioxidant properties in order to characterize the aqueous extract of wheatgrass as a potential free radical quencher. Results: The phytochemical screening of the aqueous extract of wheatgrass showed the presence of various secondary metabolites but the absence of sterols and quinone in general. Wheatgrass was proved to be an effective radical scavenger in all antioxidant assays. The gas chromatography-mass spectrometry analysis confirmed the presence of diverse category of bioactive compounds such as squalene, caryophyllene and amyrins in varying percentage. Conclusions: From the results obtained, we conclude that wheatgrass aqueous extract contains various effective compounds. It is a potential source of natural antioxidants. Further analysis of this herb will help in finding new effective compounds which can be of potent use in pharmacological field.

Phytochemical screening and analysis of antioxidant properties of aqueous extract of wheatgrass

OBJECTIVE@#To screen the phytochemical constituents and study antioxidant properties of the aqueous extract of the wheatgrass.@*METHODS@#The current study was focused on broad parameters namely, phytochemical analysis, gas chromatography-mass spectrometry analysis and antioxidant properties in order to characterize the aqueous extract of wheatgrass as a potential free radical quencher.@*RESULTS@#The phytochemical screening of the aqueous extract of wheatgrass showed the presence of various secondary metabolites but the absence of sterols and quinone in general. Wheatgrass was proved to be an effective radical scavenger in all antioxidant assays. The gas chromatography-mass spectrometry analysis confirmed the presence of diverse category of bioactive compounds such as squalene, caryophyllene and amyrins in varying percentage.@*CONCLUSIONS@#From the results obtained, we conclude that wheatgrass aqueous extract contains various effective compounds. It is a potential source of natural antioxidants. Further analysis of this herb will help in finding new effective compounds which can be of potent use in pharmacological field.

The effects of flavanoid on the treatment of hepatopulmonary syndrome.

PURPOSE: Hepatopulmonary syndrome is an arterial oxygenation disorder brought about by advanced liver failure and pulmonary vascular dilatations. The reason why hypoxia develops in hepatopulmonary syndrome depends on the broadening of perialveolar capillary veins. Our study aims to investigate the effects of Flavanoid on hepatopulmonary syndrome through its inhibition of nitric oxide. METHODS: Three groups, each having 8 rats, were formed within the scope of our study. Group I (the control group) only received laparatomy, group II received choledoch ligation, and group III was administered Flavanoid (90% flavonoid diosmin, 10% flavonoid hesperidin) following choledoch ligation. The rats were administered Flavanoid at week two following choledoch ligation. The rats' livers and lungs were examined histopathologically following a five-week follow-up and the perialveolar vein diameters were measured. Arterial blood gases and biochemical parameters were evaluated. RESULTS: It was seen that fibrosis and oxidative damage in the liver with obstructive jaundice as well as hypoxia with pulmonary perialveolar vein sizes were significantly lower than the other group with cirrhosis formed through the administration of Flavanoid. CONCLUSION: We have concluded that Flavanoid administration might be useful in the treatment of hypoxia in hepatopulmonary syndrome and the delay of cirrhosis contraction.

The effects of flavanoid on the treatment of hepatopulmonary syndrome / 대한외과학회지

PURPOSE: Hepatopulmonary syndrome is an arterial oxygenation disorder brought about by advanced liver failure and pulmonary vascular dilatations. The reason why hypoxia develops in hepatopulmonary syndrome depends on the broadening of perialveolar capillary veins. Our study aims to investigate the effects of Flavanoid on hepatopulmonary syndrome through its inhibition of nitric oxide. METHODS: Three groups, each having 8 rats, were formed within the scope of our study. Group I (the control group) only received laparatomy, group II received choledoch ligation, and group III was administered Flavanoid (90% flavonoid diosmin, 10% flavonoid hesperidin) following choledoch ligation. The rats were administered Flavanoid at week two following choledoch ligation. The rats' livers and lungs were examined histopathologically following a five-week follow-up and the perialveolar vein diameters were measured. Arterial blood gases and biochemical parameters were evaluated. RESULTS: It was seen that fibrosis and oxidative damage in the liver with obstructive jaundice as well as hypoxia with pulmonary perialveolar vein sizes were significantly lower than the other group with cirrhosis formed through the administration of Flavanoid. CONCLUSION: We have concluded that Flavanoid administration might be useful in the treatment of hypoxia in hepatopulmonary syndrome and the delay of cirrhosis contraction.

Antiviral actions of flavanoid-derived compounds on dengue virus type-2.

Dengue viruses, mosquito-borne members of the Flaviviridae family, are the causative agents of dengue fever and its associated complications, dengue haemorrhagic fever and dengue shock syndrome. To date, more than 2.5 billion people in over 100 countries are at risk of infection, and approximately 20 million infections were reported annually. There is currently no treatment or vaccine available for dengue infection. This study employed a whole-cell organism model or in vitro methods to study the inhibitory property of the flavanoid-derived compounds against DENV2 activity. Results showed that at concentration not exceeding the maximum non-toxic dose (MNTD), these compounds completely prevented DENV2 infection in HepG2 cells as indicated by the absence of cytophatic effects. The in vitro antiviral activity assessed in HepG2 cells employing virus inhibition assay showed high inhibitory activity in a dose dependent manner. At concentration below MNTD, compounds exhibited inhibitory activity against DENV2 with a range of potency strengths of 72% to 100%. The plaque forming unit per ml (pfu/ml) was reduced prominently with a maximum reduction of 98% when the infected HepG2 cells were treated with the highest non-toxic dose of compounds. The highly potent activity of the compounds against DENV2 infection strongly suggests their potential as a lead antiviral agent for dengue.

Chemical components of Rumex gmelini (Ⅳ) / 中草药

Objective To study the chemical constituents from the root of Rumex gmelini.MethodsThe compounds were isolated and purified by chromatography,polyamide column chromatography,and preparation HPLC etc.Their structures were elucidated by physicochemical and spectroscopic evidences.Results Ten compounds were identified as:nepodin (Ⅰ),emodin (Ⅱ),citreorosein (Ⅲ),chrysophanol 8-O-?-(6'-acetyl) glucopyranoside (Ⅳ),chrysophanol 8-O-?-D-glucopyranoside (Ⅴ),resveratrol (Ⅵ),9,9'-dianthranone-2,2'-dimethyl-5,5'-bis (?-D-glucopyranose)-9,9',10,10'-tetrahydro-4,4'-dihydroxy-10,10'-dioxo (trivial name:rumoside A) (Ⅶ),emodin-8-O-?-D-glucopyranoside (Ⅷ),resveratrol-3-O-?-D-glucoside (Ⅸ),and rutin (Ⅹ).Conclusion Compound Ⅶ is a new compound,named rumoside A.Compounds Ⅴ,Ⅷ,and Ⅹ are separated from R.gmelini for the first time.Compounds Ⅲ and Ⅳ are the compounds which have been found in the plants of Rumex L.for the first time.