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Flavonoid Nobiletin Exhibits Differential Effects on Cell Viability in Keratinocytes Exposed to UVA versus UVB Radiation.

The polymethoxylated flavonoid nobiletin has been shown to suppress inflammatory responses to UVB radiation and to enhance circadian rhythms. Because expression of the core nucleotide excision repair (NER) factor XPA and the rate of removal of UV photoproducts from DNA are regulated by the circadian clock, we investigated whether the beneficial effects of nobiletin in UVB-exposed cells could be due in part to enhanced NER. Although nobiletin limited UVB-irradiated human keratinocytes from undergoing cell death, we found that this enhanced survival was not associated with increased NER or XPA e

Improved production of the antidiabetic metabolite montbretin A in Nicotiana benthamiana: discovery, characterization, and use of Crocosmia shikimate shunt genes.

The plant-specialized metabolite montbretin A (MbA) is being developed as a new treatment option for type-2 diabetes, which is among the ten leading causes of premature death and disability worldwide. MbA is a complex acylated flavonoid glycoside produced in small amounts in below-ground organs of the perennial plant Montbretia (Crocosmia × crocosmiiflora). The lack of a scalable production system limits the development and potential application of MbA as a pharmaceutical or nutraceutical. Previous efforts to reconstruct montbretin biosynthesis in Nicotiana benthamiana (Nb) resulted in low yie

Synthesis of Cr(III)-morin complex: characterization and antioxidant study.

The complex formation between Cr(III) and morin was carried out in methanol and confirmed by analytical characterization using UV-Vis, IR, (1)H NMR, and TG-DTA. UV-Vis shows significant bathochromic shift in benzoyl upon coordination as well as IR well illustrates the peak shift of C=O group and formation of a O-Cr(III) bond. Likewise, (1)H NMR studies clarify that Cr(III) metal ion replaces the 5OH proton hence; 5-hydroxy-4-keto site is employed by morin in chelation to form six-membered stable ring system out of three available chelating sites. In addition, TG-DTA denotes the presence of coo

Widely targeted metabolomic profiling combined with transcriptome analysis sheds light on flavonoid biosynthesis in sweet orange 'Newhall' (C. sinensis) under magnesium stress.

Sweet orange 'Newhall' peels (SOPs) are abundant in flavonoids, making them increasingly popular in the realms of nutrition, food, and medic … condary metabolites in SOPs. Among them, 740 flavonoids were classified into eight categories, with flavones identified as the dominant flavonoid component. The influence of magnesium stress on flavonoid composition was evaluated using a combination of heat map and volcanic map, which indicated significant variations between MS and MD varieties at differen …

The 8-bromobaicalein inhibited the replication of dengue, and Zika viruses and targeted the dengue polymerase.

Dengue and Zika viruses are mosquito-borne flaviviruses burdening millions every year with hemorrhagic fever and neurological symptoms. Baicalein was previously reported as a potential anti-flaviviral candidate and halogenation of flavones and flavanones potentiated their antiviral efficacies. Here, we reported that a chemically modified 8-bromobaicalein effectively inhibited all dengue serotypes and Zika viruses at 0.66-0.88 micromolar in cell-based system. The compound bound to dengue serotype 2 conserved pocket and inhibited the dengue RdRp activity with 6.93 fold more than the original bai…

Phytochemical Investigation and Biological Activities of Lantana rhodesiensis.

Lantana rhodesiensis Moldenke is a plant widely used to treat diseases, such as rheumatism, diabetes, and malaria in traditional medicine. T … and tannins; and total flavonoids) and the antioxidant activity of all extracts. Furthermore, four flavones were isolated from leaf dichloromethane and ethyl acetate fractions: a new flavone named rhodescine (5,6,3',5'-tetrahydroxy-7,4'-dimethoxyflavone) (1), 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2), 5-hydroxy-6,7,3',4'-tetramethoxyflavone (3), and …

Ovicidal, pupicidal, adulticidal, and repellent activity of Helicteres velutina K. Schum against Aedes aegypti L. (Diptera: Culicidae).

Aedes aegypti is a vector of emerging and neglected diseases, such as dengue, chikungunya, and Zika. Helicteres velutina, known as "pitó" in Brazil, is traditionally used as an insect repellent, and several studies have demonstrated its larvicidal activity. The aim of this study was to investigate this species and evaluate its potential ovicidal, pupicidal, adulticidal, and repellent activity. The viability of the eggs was evaluated using different concentrations of the test substances for 25 days. The hexane fraction killed 72.7% of the eggs, while dichloromethane killed 67.7%. The survival o

Identification of Dipeptidyl Peptidase-4 and α-Amylase Inhibitors from Melicope glabra (Blume) T. G. Hartley (Rutaceae) Using Liquid Chromatography Tandem Mass Spectrometry, In Vitro and In Silico Methods.

The present study investigated the antidiabetic properties of the extracts and fractions from leaves and stem bark of M. glabra based on dipeptidyl peptidase-4 (DPP-4) and α-Amylase inhibitory activity assays. The chloroform extract of the leaves was found to be most active towards inhibition of DPP-4 and α-Amylase with IC50 of 169.40 μg/mL and 303.64 μg/mL, respectively. Bioassay-guided fractionation of the leaves' chloroform extract revealed fraction 4 (CF4) as the most active fraction (DPP-4 IC50: 128.35 μg/mL; α-Amylase IC50: 170.19 μg/mL). LC-MS/MS investigation of CF4 led to the identifi

Protective effects of Arctium lappa L. root extracts (AREs) on high fat diet induced quail atherosclerosis.

BACKGROUND: This study was designed to evaluate the protective effects of Arctium lappa L. root extracts (AREs) from different extraction me … cantly alleviated the atherosclerotic changes similar to simvastatin. Among the different extracts, flavones fraction exerted best protective effects. CONCLUSIONS: Our data suggest that the protective effects of AREs were medicated via hypolipidemic and anti-oxidant effects. Underlying molecular mechanisms are under investigation.

Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression.

Accumulation of bilirubin, primarily because of its insolubility, has been found to be associated with liver diseases including jaundice. Free bilirubin is insoluble; its glucuronidation by bilirubin-UGT enzyme (UGT1A1) makes it soluble and eliminates it through urine and faeces. Taking CCl(4) induced rat liver dysfunction model, we demonstrated that suppression of UGT1A1 activity in rat liver increased serum bilirubin level which could be reversed by carlinoside (Cln), a flavone glycoside. Although Cln is a flavone compound, it escaped self-glucuronidation in the intestine and readily absorbe

Analytical Quality by Design-Driven RP-HPLC Method Conditions to Concomitantly Determine Cinnarizine and Morin Hydrate in Combined Drug Solution and Dual Drug-Loaded Formulations.

BACKGROUND: The replacement of traditional oils with a camphor and menthol-based eutectic mixture is done to prepare oil-less emulsion-like dispersions for co-delivery of cinnarizine (CNZ) and morin hydrate (MH) for managing Meniére's disease (MD). Since two drugs are loaded into the dispersions, the development of a suitable reverse phase-high performance liquid chromatography (RP-HPLC) method for their simultaneous analysis becomes inevitable. OBJECTIVE: By applying the analytical quality by design (AQbD) approach, the RP-HPLC method conditions were optimized for the concomitant determinati

Tangeretin as an adjuvant and chemotherapeutic sensitizer against various types of cancers: a comparative overview.

OBJECTIVES: Cancer is a leading cause of disabling morbidities and death worldwide. Although there are various strategies for the management of cancer, the severe adverse effects negatively impact the patient's quality of life. In addition, the development of resistance limits the efficacy of many chemotherapeutics. Many natural agents are capable of reducing the adverse effects associated with chemotherapy and improving the therapeutic outcome. Tangeretin, a polymethoxy flavone, is one of the promising natural anticancer agents. KEY FINDINGS: Tangeretin not only targets various malignancies

Tissue-Specific Bioactive Metabolites and Antioxidant Activity in Minicitrus (Fortunella hindsii) and Responses to a Fruit-Associated Weissella Strain.

Minicitrus (Fortunella hindsii) is a wild kumquat with potential nutritional and medicinal value, but its tissue-specific bioactive metabolites, antioxidant activity, and endophytes remain poorly characterized. Here, we integrated LC-MS profiling, HPLC quantification, chemical and cellular antioxidant assays, 16S rRNA gene sequencing, bacterial isolation, and treatment experiments across five tissues. Among all the metabolites determined by HPLC, 13 were quantified using authentic standards and 24 were semi-quantified as linarin equivalents. Leaves, stems, and fruits accumulated abundant flavo

Обнаружение азалита как потенциального аллостерического ингибитора денге NS2B-NS3 протеза с использованием in vitro и в исследованиях силико.

Рост числа случаев заболевания денге в тропических и субтропических районах стал серьезной проблемой в области здравоохранения. В настоящее время не существует окончательного средства для лечения лихорадки денге, что подчеркивает важность выявления мощных ингибиторов. Денге NS2B-NS3 протеза является главной целью наркотика, поскольку она имеет жизненно важное значение для воспроизведения. Кверцетин, флавон, обладает антиденгическими вирусными свойствами, но ограничен низкой биодоступностью. Предыдущие исследования показали, что замена метокси в флавонах повышает биодоступность и метаболическую

Совпадение в аннотации оригинала
The rise in dengue cases in tropical and sub-tropical areas has become a significant health concern. At present, there is no definitive cure … ies but is limited by low bioavailability. Previous studies have shown that methoxy substitution in flavones improves bioavailability and metabolic stability. Azaleatin is a derivative of quercetin with a methoxy substitution at the C5 position, however its ability to inhibit dengue is unknown. In this study, azaleatin was investigated for its inhibition a …

Non-alkaloidal constituents of Sophora flavescens:structure, activity and biosynthesis.

Sophora flavescens Aiton (Kushen) is a widely used medicinal herb known for its rich phytochemical composition. The plant contains alkaloids … their NMR spectroscopic features and the biosynthesis of the side-chain cyclization in isopentenyl flavones. Pharmacological studies have shown that non-alkaloid compounds have many biological activities, including anti-inflammation, antioxidant, antitumor and anti-Alzheimer disease. This review provides a comprehensive reference for the structural elucid …

Amylin Amyloid Inhibition by Flavonoid Baicalein: Key Roles of Its Vicinal Dihydroxyl Groups of the Catechol Moiety.

Amyloid formation of the 37-residue amylin is involved in the pathogenesis of type 2 diabetes and, potentially, diabetes-induced neurological deficits. Numerous flavonoids exhibit inhibitory effects against amylin amyloidosis, but the mechanisms of inhibition remain unclear. Screening a library of natural compounds uncovered a potent lead compound, the flavone baicalein. Baicalein inhibits amylin amyloid formation and reduces amylin-induced cytotoxicity. Analogue analyses demonstrated, for the first time, key roles of the vicinal hydroxyl groups on the A-ring. We provided mass spectrometric ev

Analysis of the differential components of five processed products of Cuscuta chinensis based on HPLC-Q Exactive Orbitrap/MS and chemometrics.

Cuscuta chinensis Lam., a common TCM herb, nourishes liver-kidney and treats lumbago, tinnitus and vitiligo. Processing alters its constitue … rocessing and toasting induced the most prominent compositional variations mainly from heat action. Flavones/isoflavones dominated distinctive metabolites of salt-processed and toasted samples, whereas carboxylic acids prevailed in raw, cake-prepared and wine-processed groups. Cleavage rules of hyperoside and chlorogenic acid were speculated to clarify pro …

Selective cytotoxic effects on human breast carcinoma of new methoxylated flavonoids from Euryops arabicus grown in Saudi Arabia.

The chloroform-methanol extract of Euryops arabicus, collected from Saudi provenance, yielded a new kaurane diterpene (1) and seven methoxylated flavones (2-8), two of which are new (2 and 3). Structures of the compounds were elucidated through interpretation of spectral data of NMR, MS and comparison with literature values. All compounds were evaluated for their anti-tumor activities, employing four different cancer cell lines (WI-38, VERO, HepG2 and MCF-7), ABTS free radical scavenging and immunemodulatory effects. All metabolites had considerable antioxidant and immunestimulatory effects. A…