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Two phenolic acids (1 and 2) and seven flavonoids (3–9) were isolated from the aerial parts of Alyssum alyssoides (Brassicaceae). All these compounds (1–9) were isolated from this particular species for the first time. Their structures were identified, on the basis of MS and NMR spectra as: p-hydroxy-benzoic acid (1), 3-methoxy-4-hydroxybenzoic acid (vanillic acid) (2), kaempferol 3-O-β-D-glucopyranoside (astragalin) (3), kaempferol 3-O-(6″-α-L-rhamnopyranosyl)-β-D-glucopyranoside (nicotiflorin) (4), quercetin 3-O-β-D-glucopyranoside (isoquercetin) (5), quercetin 3-O-β-D-galactopyranoside (hyperoside) (6), isorhamnetin 3-O-β-D-glucopyranoside (7), isorhamnetin 3-O-β-D-galactopyranoside (8) and isorhamnetin 3-O-(6″-α-L-rhamnopyranosyl)-β-D-glucopyranoside (narcissin) (9). The chemotaxonomic significance of these compounds was summarized.

Ethnopharmacological relevance Actinidia chinensis Planch. (ACP) is a common traditional Chinese medicine, which is mostly used for cancer treatment clinically. Liver cancer is a refractory tumor with a high incidence. Although ACP has been reported in the treatment of liver cancer, its possible mechanism of action is little known. Aim of study The aim of this paper was to investigate the active components of ACP in the treatment of liver cancer and the related mechanisms by a network pharmacology approach. Methods The active components of ACP and the corresponding targets were obtained from multiple databases. Cytoscape software and STRING database were used to build the "herb-component-target (H-C-T)" network and protein–protein interactions (PPI) network. The key components and targets were further predicted by the Cytohubba plug-in in Cytoscape. Then, experiments were carried out on HepG2 cell line and Huh7 cell line to verify the effects and related mechanisms of the key compounds in ACP. Results 28 active components in ACP and 1299 related targets were screened out according to two indicators, oral bioavailability (OB) and drug-likeness (DL). The key compounds predicted include rutinum, astragalin, and L-epicatechin, and the main signaling pathways focus on apoptosis. Astragalin, a key compound in ACP, could inhibit the expression of Bcl-2, up-regulate the expression of Bax, cleaved caspase 3, cleaved caspase 8, and cleaved caspase 9, and regulate the apoptosis signaling pathway to inhibit the proliferation of liver cancer cells to play a therapeutic role in anti-liver cancer. Conclusions These results suggest that ACP can alleviate the progression of liver cancer through the mechanisms predicted by network pharmacology, and provide a basis for the further understanding of the application of ACP in anti-cancer.

Flowers of Prunus persica (L.) Batsch (Rosaceae), known as peach blossoms, have been reported to exert anti-obesity effects by improving hepatic lipid metabolism in obese mice. However, little is known regarding the anti-adipogenic effects of the phenolic compounds isolated from P. persica flowers. This study investigated the inhibitory effects of compounds extracted from P. persica flowers (PPF) on adipogenesis in 3T3-L1 murine preadipocytes using adipogenic differentiation assays. Additionally, we compared the anti-adipogenic effects of the phenolic compounds isolated from PPF, such as prunasin amide (1), amygdalin amide (2), prunasin acid (3), mandelamide (4), methyl caffeate (5), ferulic acid (6), chlorogenic acid (7), benzyl α– l -xylpyranosyl-(1 → 6)-β- d -glucopyranoside (8), prunin (9), naringenin (10), nicotiflorin (11), astragalin (12), afzelin (13), and uridine (14), on adipogenesis in 3T3-L1 murine preadipocytes. PPF and compounds 4–7 and 10 significantly inhibited adipogenesis. Among them, mandelamide (4) exhibited the maximum inhibitory activity with an IC50 of 36.04 ± 1.82 μM. Additionally, mandelamide downregulated the expression of key adipogenic markers, such as extracellular signal-regulated kinase, c-Jun-N-terminal kinase, P38, CCAAT/enhancer-binding protein α, CCAAT/enhancer-binding protein β, peroxisome proliferator activated receptor γ, and glucocorticoid receptor. These results indicate that mandelamide is an active ingredient of PPF possessing anti-obesity properties.

Raspberry, the fruit of Rubus Chingii Hu, has been used as a traditional Chinese medicine (TCM) to nourish kidney and strengthen Yang-qi. In order to determine the quality of raspberry, the quality markers (Q-markers) of raspberry that can improve renal function were investigated using UPLC-ESI-QTOF-MS in this study. The results of serum pharmacochemistry indicated that six components rutin, ellagic acid, kaempferol-3-rutinoside, astragalin, tiliroside, and goshonoside F5 in raspberry were absorbed into rat blood. The HEK293 cells treated with cisplatin were used to evaluate the kidney-protecting activity of these absorbed components. All these components could markedly inhibit cell damage induced by cisplatin and restore the levels of malondialdehyde (MDA) and catalase (CAT) in the cells, suggesting that these components may be the Q-markers of raspberry. More importantly, except for ellagic acid, other five Q-markers in raspberries from Dexing of Jiangxi province were higher than those from most of other areas. It is well known that Dexing raspberry is the Dao-di herbs raspberry used in the clinic of Chinese Medicine, demonstrating that these components could be used as Q-markers of raspberry. This study provides a reliable and valuable method for quality evaluation of raspberry.

Coronavirus Disease-2019 (COVID-19), a viral disease caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) was declared a global pandemic by WHO in 2020. In this scenario, SARS-CoV-2 main protease (COVID-19 Mpro), an enzyme mainly involved in viral replication and transcription is identified as a crucial target for drug discovery. Traditionally used medicinal plants contain a large amount of bioactives and pave a new path to develop drugs and medications for COVID-19. The present study was aimed to examine the potential of Emblica officinalis (amla), Phyllanthus niruri Linn. (bhumi amla) and Tinospora cordifolia (giloy) bioactive compounds to inhibit the enzymatic activity of COVID-19 Mpro. In total, 96 bioactive compounds were selected and docked with COVID-19 Mpro and further validated by molecular dynamics study. From the docking and molecular dynamics study, it was revealed that the bioactives namely amritoside, apigenin-6-C-glucosyl7-O-glucoside, pectolinarin and astragalin showed better binding affinities with COVID-19 Mpro. Drug-likeness, ADEMT and bioactivity score prediction of best drug candidates were evaluated by DruLiTo, pkCSM and Molinspiration servers, respectively. Overall, the in silico results confirmed that the validated bioactives could be exploited as promising COVID-19 Mpro inhibitors.

Aim To assess the potential role of saffron in downregulating inflammation and cytokine storm during COVID-19. Main findings Three main compounds of saffron, i.e., crocetin esters, picrocrocin, and safranal, present strong antioxidant and anti-inflammatory action for several disease states (e.g., Alzheimer's, cancer, and depression) but have also been studied in COVID-19. In particular, based on our comprehensive review of both in vitro and in silico studies, saffron's essential oils and other constituents appear to have both immunomodulatory and anti-asthmatic actions; these actions can be particularly helpful to treat patients with respiratory symptoms due to COVID-19. Moreover, crocin appears to reduce the COVID-19-related cytokine cascade and downregulate angiotensin-converting enzyme 2 (ACE2) gene expression. Last, in silico studies suggest that saffron's astragalin and crocin could have inhibitory actions on SARS-CoV-2 protease and spike protein, respectively. Conclusion Saffron represents a promising substance for toning down cytokine storm during COVID-19, as well as a potential preventive treatment for COVID-19. However, appropriate randomized clinical trials, especially those using biomarkers as surrogates to assess inflammatory status, should be designed in order to assess the clinical efficacy of saffron and allow its use as an adjunct treatment modality, particularly in resource-poor settings where access to drugs may be limited.

Obesity is considered a chronic metabolic disorder that can be associated with multiple medical complications. Currently, there is no or limited curative therapy for obesity. This study focused on the assessment of anti-obesity activity and UPLC standardization of a polyherbal formulation (F2). An anti-obesity activity was investigated using the diet-induced obese (DIO) mice model, where obesity was developed in C57BL/6J mice by providing a high-fat diet (HFD) for five weeks without treating drugs. After the successful development of obesity, the obese mice were treated with F2 for seven weeks with continuing HFD feeding. The major obesity-related parameters such as body weight gain, food efficiency ratio, serum lipid profile, and white adipose tissue (WAT) mass were found to be significantly reduced in F2 treated obese mice. These results were supported by the down-regulation of specific adipogenic transcription factors (PPARγ, SREBP-1c, and ap2) in epididymal WAT. Histological evaluation of liver and WAT also revealed reduced fat deposition in the tissues by F2 compared to the HFD control group. The overall observations indicated that the F2 exhibited pronounced obesity-controlling activity through the inhibition of adipocyte differentiation and triglyceride accumulation in the tissues, and serum lipid depletion. In addition, F2 ameliorated obesity-induced insulin resistance. Furthermore, the UPLC-DAD method for quality control of F2 was validated and standardized using five reference compounds: astragalin, ellagic acid, fisetin, fustin, and sulfuretin.

Opuntia ficus-indica is a cactaceous plant native to America but, nowadays, widely found worldwide, having been the most common domesticated species of cactus grown as a crop plant in semiarid and arid parts of the globe, including several Mediterranean basin countries. Opuntia ficus-indica can be regarded as a medicinal plant, being source of numerous bioactive phytochemicals such as vitamins, polyphenols, and amino acids. The urgent need for therapeutic treatments for the COronaVIrus Disease 19 (COVID-19), caused by the Severe Acute Respiratory Syndrome (SARS)-Coronavirus (CoV)-2, justifies the great attention currently being paid not only to repurposed antiviral drugs, but also to natural products and herbal medications. In this context, the anti-COVID-19 utility of Opuntia ficus-indica as source of potential antiviral drugs was investigated in this work on the basis of the activity of some of its phytochemical constituents. The antiviral potential was evaluated in silico in docking experiments with Mpro, i.e., the main protease of SARS-CoV-2, that is one of the most investigated protein targets of therapeutic strategies for COVID-19. By using two web-based molecular docking programs (1-Click Mcule and COVID-19 Docking Server), we found, for several flavonols and flavonol glucosides isolated from Opuntia ficus-indica, good binding affinities for Mpro, and in particular, binding energies lower than −7.0 kcal/mol were predicted for astragalin, isorhamnetin, isorhamnetin 3-O-glucoside, 3-O-caffeoyl quinic acid, and quercetin 5,4′-dimethyl ether. Among these compounds, the chiral compound astragalin showed in our in silico studies the highest affinity for Mpro (−8.7 kcal/mol) and also a low toxicity profile, emerging, thus, as an interesting protease inhibitor candidate for anti-COVID-19 strategies.

The aim of this study was to investigate the protective effect of Diospyros lotus leaf extract (DLE) on UVB-induced skin damage in mice. UVB irradiation of mice skin incurred significant damage to mice skin; increased thiobarbituric acid-reactive substance level; decreased superoxide dismutase; and glutathione levels in mice skin tissues. More so, UVB irradiation led to collagen degradation and infiltration of mast cell and neutrophils into mice skin leading to inflammation. However, topical application of DLE significantly reversed these conditions with the result comparable to l-ascorbic acid. Myricitrin, gallic acid, astragalin, myricetin-3-O-glactosside, and myricetin through high-performance liquid chromatography analysis were further determined to be the primary active compounds in DLE. In conclusion, our study showed that DLE has potentials as local therapeutic materials against skin damage by inhibiting oxidative stress and UVB-induced skin damage.

A new benzofuran derivative, pumiloside (1), together with seven known flavonoid glycosides, afzelin (2), astragalin (3), quercitrin (4), isoquercitrin (5), kaempferol 3-O-rutinoside (6), rutin (7) and kaempferol 3-O-sophoroside (8) were isolated from the leaves of Ficus pumila. Their structures were established by spectroscopic data and comparison with the literature values.

The aim of this study was to establish the influence of harvest time on the contents of flavonoid compounds (rutin, isoquercetin, nicotiflorin, and astragalin) and chlorogenic acid, as well as the antiradical activity in white mulberry (Morus alba L.) leaves grown in Lithuania. Mulberry leaves contain a wide range of bioactive compounds, such as flavonoids and phenolic acids, which are responsible for beneficial effects on human health. Leaves from two mulberry cultivars were collected from July to September in 2015-2016. Quantitative determinations of four flavonoids and chlorogenic acid were conducted by HPLC method and antiradical activity using the 2.2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method. The results showed that the total flavonoid contents of mulberry leaves in the two cultivars ranged from 921.92 to 1512.02 mg 100 g−1 (dry matter). The highest accumulated rutin, nicotiflorin, and chlorogenic acid contents and the greatest antioxidant activity were found in the leaves of ‘Plodovaja 3’. The bioactive compounds in the leaves of the mulberry cultivars varied over a period of time, where ‘Turchanka’ and ‘Plodovaja 3’ accumulated the highest total flavonoid contents in September and August, respectively. In both cultivars, the antiradical activity was highest in September. There were a very strong positive correlations between the antiradical activity as determined using the DPPH method and the chlorogenic acid contents (r = 0.887, p < 0.05) and the isoquercetin contents (r = 0.848, p < 0.05).

Site-specific accumulation of flavonoids in Apocyni Veneti Folium was determined by laser scanning confocal microscope (LSCM) and the localization of catechins also was observed via vanillin-HCl staining under the conventional optical microscope. The contents of five flavonoids in Apocyni Veneti Folium from different harvest times and growth parts were measured using HPLC method. LSCM observation showed that flavonoids are accumulated in cuticle of epidermal cells and vessel walls, especially in protoplasts and nucleolus of the collenchyma cells and the epidermal cells. Catechins are localized in the palisade parenchyma cells and vessel walls, particularly in the laticifers found in the phloem. On the basis of the difference of the maximal emission wavelength between quercetin and kaempferol derivatives which have fluorescence behavior by appropriate treatment, kaempferol and its derivatives are localized exclusively in the cuticle. Results showed that the content of astragalin in Apocyni Veneti Folium from different parts revealed the decreasing trend, while hyperin and isoquercitrin were higher in June and July analyzed by HPLC. In summary, the site-specific accumulation of flavonoids in Apocyni Veneti Folium can be determined by LSCM and vanillin-HCl staining. The contents of flavonoids in Apocyni Veneti Folium are correlated with harvest times and growth parts.

Though Astragalin (kaempferol-3-glucoside) contained in Paeonia lactiflora and other plants was known to have anti-oxidant, antiinflammatory, and anti-tumor activity, the anti-tumor mechanism of Astragalin has never been reported in melanomas until now. Thus, in the present study, the underlying apoptotic mechanism of Astragalin isolated from Aceriphyllum rossii was elucidated in A375P and SK-MEL-2 melanoma cells. Astragalin exerted cytotoxicity in A375P and SK-MEL-2 cells in a concentration-dependent manner. Also, Astragalin significantly increased the number of TdT-mediated dUTP nick end labeling positive cells and sub-G1 population as a feature of apoptosis in A375P and SK-MEL-2 cells compared with untreated control. Consistently, western blotting revealed that Astragalin activated caspase 9/3 and Bax, cleaved poly (ADP-ribose) polymerase, and attenuated the expression of cyclin D1, Mcl-1, and Sry-related HMg-Box gene 10 (SOX10) in A375P and SK-MEL-2 cells. Of note, ectopic expression of SOX10 reduced the apoptotic ability of Astragalin to inhibit proliferation, cleave poly (ADP-ribose) polymerase, and caspase 3 in A375P and SK-MEL-2 melanoma cells. Overall, our findings provide evidence that Astragalin induces apoptosis in A375P and SK-MEL-2 melanoma cells via activation of caspase9/3 and inhibition of SOX10 signaling. Copyright © 2017 John Wiley & Sons, Ltd.

Astragalin (kaempferol-3-O-β- d -glucopyranoside, Ast) is a kind of flavonoid known to have anti-oxidant, anti-HIV, anti-allergic, and anti-inflammatory effects. It has low solubility in water. In this study, novel astragalin galactosides (Ast-Gals) were synthesized using β-galactosidase from Bacillus circulans and reaction conditions were optimized to increase the conversion yield of astragallin. Purified Ast-Gal1 (11.6% of Ast used, w/w) and Ast-Gal2 (6.7% of Ast used, w/w) were obtained by medium pressure chromatography (MPLC) with silica C18 column and open column packed with Sephadex LH-20. The structures of Ast-Gal1 and Ast-Gal2 were identified by nuclear magnetic resonance (NMR) to be kaempferol-3-O-β- d -glucopyranosyl-(1 → 6)-β- d -galactopyranoside and kaempferol-3-O-β- d -glucopyranosyl-(1 → 6)-β- d -galactopyranosyl-(1 → 4)-β- d -galactopyranoside, respectively. The water solubility of Ast, Ast-Gal1, and Ast-Gal2 were 28.2 ± 1.2 mg/L, 38,300 ± 3.5 mg/L, and 38,800 ± 2.8 mg/L, respectively. The SC50 value (the concentration required to scavenge 50% of the ABTS + ) of Ast, Ast-Gal1, and Ast-Gal2 were 5.1 ± 1.6 μM, 6.5 ± 0.4 μM, and 4.9 ± 1.1 μM, respectively. The IC50 values (the half maximal inhibitory concentration) of Ast, Ast-Gal1, and Ast-Gal2 against angiotensin converting enzyme (ACE) were 171.0 ± 1.2 μM, 186.0 μM, and 139.0 ± 0.2 μM, respectively.

Astragalin (ASG) can be found in a variety of food components. ASG exhibits cytotoxic effects on several different types of malignant cells. However, its effects on hepatocellular carcinoma (HCC) cells and the underlying molecular mechanisms have remained to be fully elucidated. Here, we revealed that ASG remarkably suppressed the proliferation of HCC cells. In HCC cells, ASG inhibited glucose glycolysis and promoted oxidative phosphorylation, resulting in a surge of reactive oxygen species (ROS). Mechanistically, ASG suppressed the expression of hexokinase 2 (HK2). This event was indispensible for ASG-mediated metabolic reprogramming, ROS accumulation, and subsequent growth arrest. Our further investigations unveiled that ASG repressed HK2 expression via increasing miR-125b. In vivo experiments showed that gavage of ASG decreased the proliferation of Huh-7 HCC xenografts in nude mice and inhibited the growth of transplanted H22 HCC cells in Kunming mice. Declined HCC tumor growth in vivo was associated with boosted miR-125b and reduced expression of HK2 in tumor tissues. Collectively, our results demonstrated that ASG is able to suppress the proliferation of HCC cells both in vitro and in vivo. Inhibition of HK2 through upregulating miR-125b and subsequent metabolic reprogramming is implicated in the antiproliferative effects of ASG on HCC cells.

Background Mori Fructus and Mori Ramulus are two traditional Chinese herbal medicines from mulberries. The present work explores their beneficial effects on •OH–treated mesenchymal stem cells (MSCs) and discusses possible mechanisms. Methods Lyophilized aqueous extracts of Mori Fructus (LAMF) and Mori Ramulus (LAMR) were prepared and analyzed using HPLC. LAMF and LAMR (along with morin) were further investigated for their effects on •OH-treated MSCs using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl (MTT) assay. The direct antioxidation mechanisms were studied using 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide (PTIO•)-scavenging, 2,2′-azino-bis (3-ethylbenzo-thiazoline-6-sulfonic acid (ABTS+•)-scavenging and 1,1-diphenyl-2-picryl-hydrazl (DPPH•)-scavenging, as well as Cu2+-reducing and Fe3+-reducing antioxidant power. Finally, the indirect antioxidant mechanism was investigated based on the UV-vis spectra of Fe2+-chelation. Results In each LAMF and LAMR, seven phytophenols were successfully measured by HPLC, including five flavonoids (morin, rutin, astragalin, isoquercitrin and luteolin) and two non-flavonoids (chlorogenic acid and maclurin). MTT assays revealed that LAMF, LAMR and morin could effectively increase the survival of •OH-treated MSCs at 10–100 μg/mL, and could effectively scavenge PTIO• (IC 50 6609.7 ± 756.6, 4286.9 ± 84.9 and 103.4 ± 0.9 μg/mL, respectively), DPPH• (IC 50 208.7 ± 3.0, 97.3 ± 3.1 and 8.2 ± 0.7 μg/mL, respectively) and ABTS+• (IC 50 73.5 ± 5.8, 34.4 ± 0.1 and 4.2 ± 0.2 μg/mL, respectively), and reduce Cu2+ (IC 50 212.5 ± 7.0, 123.2 ± 0.9 and 14.1 ± 0.04 μg/mL, respectively) & Fe3+ (IC 50 277.0 ± 3.1, 191.9 ± 5.2 and 5.0 ± 0.2 μg/mL, respectively). In the Fe2+-chelating assay, the five flavonoids produced much stronger shoulder-peaks than the two non-flavonoids within 420–850 nm. Conclusion Mori Fructus and Mori Ramulus, can protect MSCs from •OH-induced damage. Such beneficial effects can mainly be attributed to the antioxidant action of phytophenols, which occurs via direct (ROS-scavenging) and indirect mechanism (Fe2+-chelating). The ROS-scavenging mechanism, however, include at least a H+-transfer and an electron-transfer (ET), and possibly includes a hydrogen-atom-transfer (HAT). In the Fe2+-chelating, flavonoids are more effective than non-flavonoids. This can be attributed to several adjacent planar chelating-sites between the 3-OH and 4-C = O, between the 4-C = O and 5-OH, or between the 3′-OH and 4′-OH in flavonoids. Such multiple-Fe2+-chelating reactions cause overlap in the UV-vis absorptions to deepen the complex color, enhance the peak strength, and form shoulder-peaks. By comparison, two non-flavonoids with catechol moiety produce only a weak single peak. Electronic supplementary material The online version of this article (doi:10.1186/s12906-017-1730-3) contains supplementary material, which is available to authorized users.

The ethanol extracts of Chimonanthus nitens Oliv. leaves were prepared sequentially by ethanol gradient elution and tested for their α-glucosidase inhibitory. The fraction of 50% ethanol eluate (EE) exhibited the notable inhibition with IC50 of 0.376mg/mL. Also, 50% EE was chemically characterized by liquid chromatography-mass spectrometry (LC-MS) analysis. Eight compounds including rutin (1), hyperin (2), isoquercitrin (3), luteoloside (4), astragalin (6), quercetin (13), naringenin (14), kaempferol (15) were identified by compared with standard substances as well as proper luteolin-5-O-glucoside (5), kaempferol-7-O-rhamnoside (9), 5,7,8-trihydroxy-2-methoxyl-flavone-7-O-glucoside (10), kaempferol-7-O-acetyl-galactoside (11). The experiments of ultra-filtration combined with liquid chromatography-mass spectrometry (UF-LC-MS) guided quercetin and kaempferol as the key factors for 50% EE showing highly inhibitory activity on α-glucosidase. Quercetin and kaempferol inhibited yeast α-glucosidase in a mixed-type manner with IC50 of 66.8 and 109μg/mL, respectively. These results would provide theoretical underpinning for the C. nitens Oliv. leaves ethanol extracts used as nutraceutical health supplement in the management of type 2 diabetes.

Daily changes in the composition and content of phenolic compounds in the aerial parts Potentilla fruticosa L., growing in culture of the Novosibirsk Region, using the method of high performance liquid chromatography (HPLC) was investigated. Six glycosides of flavonol (hyperoside, isoquercitrin, rutin, avicularin, quercitrin and astragalin), two aglycones (quercetin and kaempferol) and tannins (ellagic acid and its glycoside) were identified. Established that phenolic composition of P. fruticosa is the time of day remains constant. The highest total content of phenolic compounds in the leaves (28–29 mg/g of absolutely dry solid matter) and stems (4–4,5 mg/g) of P. fruticosa found in the evening and at night. In the flowers, in contrast, the maximum content of phenolic compounds was observed in the middle of the day (42 mg/g). The level of variability of the total content of phenolic compounds was evaluated as the lowest for leaves and flowers (СV = 10–11%). It was found a threefold increase in free aglycones - quercetin and kaempferol in the leaves with 3 to 6 o'clock in the morning on the background of reduction of the relevant glycosides in 1,5–2,5 times. Maximum accumulation of glycosides of quercetin and minimum content of free quercetin in flowers was observed at 12 o'clock. It is shown predominant accumulation of ellagic compounds quercitrin, component 10, hyperoside, isoquercitrin and rutin in the leaves in the evening and at night, in the flowers – in the middle of the day. The level of variability content of most of the individual components in the above-ground organs of P. fruticosa during the day was estimated as high (СV ≥ 21%)., Исследованы суточные изменения состава и содержания фенольных соединений в надземных органах Potentilla fruticosa при интродукции с использованием метода высокоэффективной жидкостной хроматографии (ВЭЖХ). Идентифицированы шесть флавонолгликозидов – гиперозид, изокверцитрин, рутин, авикулярин, кверцитрин и астрагалин, два агликона – кверцетин и кемпферол, а также эллаговые соединения – эллаговая кислота и ее гликозид. Состав фенольных соединений надземных органов P. fruticosa в течение суток не изменяется. Наибольшее суммарное содержание фенольных соединений в листьях (28–29 мг/г от абсолютно-сухой массы) и стеблях (4–4,5 мг/г) P. fruticosa обнаружено в вечернее и ночное время. В цветках, напротив, максимальное содержание фенольных соединений наблюдалось в середине дня (42 мг/г). Уровень вариабельности суммарного содержания фенольных соединений оценивался как низкий (СV = 10–11%). Установлено трехкратное повышение содержания свободных агликонов – кверцетина и кемпферола в листьях с 3 до 6 ч утра на фоне снижения содержания соответствующих флавонолгликозидов в 1,5–2,5 раза. В цветках максимальное накопление гликозидов кверцетина на фоне минимального содержания свободного кверцетина наблюдалось в 12 ч дня. Отмечено преимущественное накопление эллаговых соединений, кверцитрина, компонента 10, гиперозида, изокверцитрина и рутина в листьях в вечернее и ночное время, в цветках – в середине дня. Уровень вариабельности содержания большинства отдельных компонентов во всех органах P. fruticosa в течение суток оценивался как высокий (СV≥ 21%). Отмечен факт несовпадения динамики флавонолгликозидов и их агликонов.

Solanum cernuum is a medicinal plant widely distributed in south-east regions of Brazil and popularly used to treat several disorders. Despite their utilisation as a medicine, few studies on its chemical composition are reported. An efficient separation method for the ethyl acetate fraction was developed by high-performance countercurrent chromatography using n-butanol/chloroform/methanol/water (3:7:3:4, v/v/v/v) as the solvent system, affording five compounds (1–5) in one-step separation. A new cyclic guanidine alkaloid named cernidine (5) was obtained, besides four glycosylated flavonoids: afzelin (1), astragalin (2), kaempferol 3-O-α[apiofuranosyl-(1 → 2)]-α-rhamnopyranoside (3) and kaempferol 3-O-α[apiofuranosyl-(1→2)]-β-galactopyranoside (4). A further purification step afforded a mixture of trans- and cis-tiliroside (6–7). Countercurrent chromatography proved itself as a powerful tool for the isolation of similar compounds since compounds 1–2 and 3–4 possess little structural differences.

During aging, cells secrete molecules called senescence-associated secretory phenotype (SASP). They constitute chronic low-grade inflammation environment to adjacent cells and tissues. In order to find inhibiting agents of SASP formation, 113 plant constituents were incubated with BJ fibroblasts for 6 days after treatment with bleomycin. Several plant constituents showed considerable inhibition of IL-6 production, a representative SASP marker. These plant constituents included anthraquinones such as aurantio-obtusin, flavonoids including astragalin, iristectorigenin A, iristectorigenin B, linarin, lignans including lariciresinol 9-O-glucoside and eleutheroside E, phenylpropanoids such as caffeic acid and methyl caffeate, steroid (ophiopogonin), and others like centauroside, rhoifolin and scoparone. In particular, methyl caffeate down-regulated SASP factors such as IL-1α, IL-1β, IL-6, IL-8, GM-CSF, CXCL1, MCP-2, and MMP-3. Inhibition of these SASP mRNA expression levels also coincided with the reduction of IκBζ expression and NF-κB p65 activation without affecting the expression levels of senescence markers, p21 or pRb. Taken together, the present study demonstrated that methyl caffeate might be a specific and strong inhibitor of SASP production without affecting the aging process. Its action mechanisms involve the reduction of IκBζ expression and NF-κB p65 activation. Therefore, this compound might be effective in alleviating chronic low-grade inflammation linked to age-related degenerative disorders.

Lung inflammation and oxidative stress are the major contributors to the development of obstructive pulmonary diseases. Macrophages are involved in pulmonary inflammation and alveolar damage in emphysema. Astragalin is an anti-inflammatory flavonoid present in persimmon leaves and green tea seeds. This study elucidated that astragalin inhibited inflammatory cell infiltration induced by 20 μM H2O2 and blocked airway thickening and alveolar emphysema induced by 20 μg of ovalbumin (OVA) in mice. OVA induced mouse pulmonary MCP-1, and H2O2 enhanced the expression of MCP-1/ICAM-1/αv integrin in bronchial airway epithelial BEAS-2B cells. Such induction was inhibited by supplying 10–20 mg/kg of astragalin to OVA-challenged mice and 1–20 μM astragalin to oxidant-stimulated cells. Oral administration of 20 mg/kg of astragalin reduced the induction of F4/80/CD68/CD11b in airways of mice challenged with OVA. Additionally, emphysema tissue damage was observed in OVA-exposed alveoli. Mast cell recruitment in the airwa...

Prunella vulgaris is known to contain pentacyclic triterpenoids, flavonoids, phenolic compounds, and steroids. Among the triterpenoids, the oleanane-type, ursane-type, and lupane-type triterpenoids have been known to be predominant. Our phytochemical study led to the isolation of a new neolignan, 9′-O-butyl dehydrodiconiferyl alcohol 4-O-β-D-glucopyranoside (1), together with four known compounds, astragalin (2), benzyl-O-β-D-glucopyranoside (3), paeonoside (4), and 4-hydroxybenzoic acid (5). It is noteworthy that all the isolated compounds are reported for the first time from the genus Prunella.

Morus albaL. (MAL) extract has been used in traditional medicine for its cardioprotective and antiplatelet effects, while another herbal remedy,Schisandra chinensis(SCC), has been reported to have anti-inflammatory and antioxidant properties. We evaluated underlying cellular changes exerted by extracts of these plants on platelet function and effects of SCC + MAL on in vivo thrombus formation using AV shunt and tail thrombosis-length models in rats. In vitro platelet aggregation, granule secretion, andCa2+irelease assays were carried out. The activation of integrinαIIbβ3and phosphorylation of downstream signaling molecules, including MAPK and Akt, were investigated using cytometry and immunoblotting, respectively. Scanning electron microscopy (SEM) was used to evaluate changes in platelet shape and HPLC analysis was carried out to identify the marker compounds in SCC + MAL mixture. In vivo thrombus weight and average length of tail thrombosis were significantly decreased by SCC + MAL. In vitro platelet aggregation, granule secretion,Ca2+irelease, and integrinαIIbβ3activation were notably inhibited. SCC + MAL markedly reduced the phosphorylation of MAPK pathway factors along with Akt. HPLC analysis identified four marker compounds: isoquercitrin, astragalin, schizandrol A, and gomisin A. The extracts exerted remarkable synergistic effects as natural antithrombotic and antiplatelet agent and a potent drug candidate for treating cardiovascular diseases.

This study aimed the phytochemical investigation of four different species of the genus Waltheria ( W. douradinha , W. ferruginea , W. indica and W. cinerencens) , collected in the Northeast of Brazil. Different species of the genus previously studied showed the presence of flavonoids and alkaloids as major constituents, being compatible with this study, that led to the isolation of eight substances, two lupan-type triterpenes: betulonic ( 3 ) and betulinic acid ( 4 ), five flavonoids: 5-hydroxy-3, 3′, 4′, 7-tetra-methoxy-flavone (retusine, 1 ), 5-hydroxy-3, 4′, 7-tetramethoxy-flavone ( 2 ), kaempferol-3-O-β- (6 ″-coumaroyl)-glucopyranoside (tiriloside, 5 ), 3-O-β-glucopyranoside (astragalin, 6 ), quercetin-3-O-α-glucopyranoside ( 7 ) and quercetin-3-O-β-glucopyranoside ( 7′ ), and a dibenzamide derivative asperphenamate ( 8 ), also known as auranamide. There are previous reports of the occurrence of amide structures and lupan-type triterpenes from Malvaceae. In addition to, the compound 5 (tiliroside), isolated for the first time from the studied species, is the predominant substance in several Malvaceae species. The obtained results contributed to consolidate the chemotaxonomic knowledge of Waltheria and Malvaceae family.

In this study, we aimed to exploit natural extracts from the spicy vegetables, which are rich in phenolic compounds as an initial treatment step in the cold storage process for shrimp. Firstly, 40 extracts from 10 types of spicy vegetables in Vietnam were prepared and tested for their bioactivities. Among samples, the extract from Persicaria Odorata leaves (E-4) exhibited the highest potential of scavenging DPPH free radical (IC50 of 7.54 µg.mL-1) and decreasing tyrosinase activity with the inhibition percentage of 54.2 % at the concentration of 100 mg/mL. Twenty-two out of a total of 36 chemical compounds in the E-4 extract identified using HPLC-MS technique were phenolic compounds, in which four compounds (morin, quercetin, fisetin, astragalin) are flavonoids. Shrimp (Litopenaus vannamei) samples were treated with the E-4 extract having lower gray values, lipid peroxidation values, and microbiological counts than those of the control samples after 7 days of storage at 2 oC. These results show the potential of using the natural extract as a safe and effective alternative for commercial chemical-derived preservatives in the shrimp storage process.

Sambucus formosana is most commonly used as a traditional herb medicine in Taiwan. In this study, high performance liquid chromatography equipped with photodiode array detection-mass (HPLC&ndash, DAD-ESI-MS) method was developed for the identification and quantification of bioactive phenolics. The developed method was also validated for accuracy, precision, limit of detection, and quantification. In this method, chlorogenic acid, rutin, isoquercetrin, nictoflorin, astragalin, and quercetin were quantified in linearity range of 10&ndash, 100 (&mu, g/mL) with a correlation coefficient of greater than 0.996. High recovery (86.5&ndash, 93.1%) and good reproducibility were obtained for six phenolics with the relative standard deviation ranging from 1.7&ndash, 3.1%. Therefore, the proposed method for simultaneous quantification of six bioactive phenolics in the extract and fractions of S. formosana using HPLC&ndash, DAD-ESI-MS detection under the optimized conditions is accurate and validated. Among the results, methanol extract showed the greatest values of total phenolic content (93.1 mg gallic acid equivalent/g). Additionally, the methanol extract revealed best antioxidant capacity based on the DPPH scavenging activity and anti-glycation activity (IC50 was observed at 97.1 and 77.9 &mu, g/mL, respectively).

The composition and content of phenolic compounds in the leaves of Spiraea aemiliana Schneid. from 2 natural populations growing on the Island of Kunashir were studied by HPLC. The chromatographic profiles of S. aemiliana and closely related species S. betulifolia Pall and S. beauverdiana Schneid. were compared. Nineteen compounds were detected in 40 % water-ethanol extracts from the leaves of S. aemiliana. Of these, сhlorogenic, p-сoumaric and cinnamic acids, quercetin, kaempferol, hyperoside, isoquercitrin rutin, avicularin, astragalin and dihydroquercetin (taxifolin) were identified. A specific compound in the leaves of S. aemiliana is isoquercitrin, not identified in other closely related species. The chromatographic profiles of S. aemiliana and S. betulifolia are generally very similar. This is additional evidence of the opinion of scientists about the taxonomic rank of S. aemiliana as a subspecies, variation, or form of S. betulifolia. S. aemiliana (the sum of phenolic compounds varies from 16.4 to 23.,88 mg/g) is more similar to S. beauverdiana in the quantitative content of phenolic compounds. Leaves of S. aemiliana contain a lot of hyperoside (up to 9.50 mg/g), which is almost twice as much as that of S. beauverdiana (up to 4.3 mg/g) and 6 times that of S. betulifolia (up to 1.55 mg/g). The revealed difference in the hyperoside content between the three Spiraea taxa is statistically significant. &nbsp, Методом ВЭЖХ изучены состав и содержание фенольных соединений в листьях Spiraea aemiliana Schneid. из 2 природных популяций, произрастающих на острове Кунашир. Проведено сравнение хроматографических профилей S. aemiliana и близкородственных видов S. betulifolia Pall. и S. beauverdiana Schneid. В 40 % водно-этанольных экстрактах из листьев S. aemiliana выявлено 19 соединений. Из них идентифицированы хлорогеновая, n-кумаровая и коричная кислоты, кверцетин, кемпферол, гиперозид, изокверцитрин, рутин, авикулярин, астрагалин и дигидрокверцетин. Специфичным соединением в листьях S. aemiliana является изокверцитрин, не идентифицированный у других близких видов. Хроматографические профили S. aemiliana и S. betulifolia в целом очень сходны. Это является дополнительным доказательством мнения учёных о таксономическом ранге S. aemiliana как подвида, вариации или формы S. betulifolia. По количественному содержанию фенольных соединений S. aemiliana (сумма фенольных соединений варьирует от 16,4 до 23,88 мг/г) более сходна с S. beauverdiana. Листья S. aemiliana содержат много гиперозида (до 9,50 мг/г), что практически в два раза больше, чем у S. beauverdiana (до 4,3 мг/г) и в 6 раз у S. betulifolia (до 1,55 мг/г). Выявленная разница в содержании гиперозида между тремя таксонами Spiraea статистически достоверна.

The changes of phenolic compounds from the freeze-dried, hot-air dried, roasted and steamed mulberry (Morus alba L.) leaves during the in vitro digestion were investigated. Caffeoylquinic acids, quercitrin glycosides and kaempferol glycosides were the main compounds. After simulated gastrointestinal digestion, the bioaccessibility of phenolics was much higher in roasted samples than those in hot-air, dried and steamed samples. Approximately 50%–80% of the bioaccessible phenolics were dialyzable depending on the different processing methods. The freeze-dried samples contributed to the highest amount of bioaccessible phenolics, followed by hot-air dried and roasted ones. All the initial phenolics degraded rapidly and were not detected after 24 h of faecal fermentation, except that at 0.5 h the amount of isoquercitrin and astragalin were increased by 156.48% and 177.44%, respectively. Consequently, quercetin, kaempferol, dihydrocaffeic acid, 3-(4-hydroxyphenyl) propionic acid and 3-methoxyphenyl-acetic acid were formed at different time. Transformation pathways for phenolics in the faecal fermentation were proposed.

The active components of Malus pumila flowers on antioxidant and tyrosinase activity were investigated with the method of spectrum-effect relationship and knock-out. Some compounds were identified by UPLC-MS/MS method. The chemical fingerprints were established by HPLC and the activity of antioxidant and tyrosinase were assayed in vitro. Chromatographic peaks P34, P35, P39, P44, P45 and P49 were identified as phloridzin, hyperoside, astragalin, afzelin, quercetin and kaempferol by UPLC-MS/MS method. Hyperoside and kaempferol were identified in M. pumila flowers for the first time. When the concentration was 1 g/mL of sample (equivalent to raw material), the scavenging capacity of P35 (hyperoside) on DPPH free radicals were consistent with the spectrum-effect relationship. The scavenging capacity of P34 (phloridzin) and P45 (quercetin) on ABTS free radicals were consistent with the spectrum-effect relationship. The activation effect of P45 (quercetin) on tyrosinase was consistent with the spectrum-effect relationship. The inhibitory effect of P34 (phloridzin), P35 (hyperoside) on tyrosinase were consistent with the spectrum-effect relationship.

The present study aimed to determine the chemical composition, antioxidant effects and antitumor properties of a methanol extract of Anchusa azurea Mill. (Boraginaceae) aerial parts against four tumour cell lines (MCF-7, MDA-MB-231, RKO, and R2C). The antioxidant effects were assessed by using β-carotene bleaching, 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing ability power (FRAP) tests. HPLC analyses revealed chlorogenic acid, catechin, caffeic acid, and astragalin as the most abundant compounds. Interesting results were obtained in the β-carotene bleaching test with IC50 values of 7.6 and 27.5 μg mL−1 after 30 and 60 min of incubation, respectively. Furthermore, the A. azurea extract protects 3T3-L1 mouse cells from oxidative stress induced by menadione and exhibits good antitumor activity, with very low toxicity. Our data indicate that the antitumor properties are due to the ability to induce programmed cancer cell death through caspase 3/7 and 9 activation and interference with the cytoskeleton dynamics.