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Parasitic plants in the Orobanchaceae family include devastating weed species, such as

The present work aimed to compare the betalain profiles and contents in the red inflorescence of Celosia argentea extract obtained using different ethanol-water ratios. The impact of betalain content on the health-promoting properties was also evaluated. Freeze-dried inflorescence powder was extracted three times with aqueous-ethanol (0, 20, 40, 60, and 80% (v/v) ethanol). The highest total betacyanin content was found in the 40 and 60% aqueous-ethanolic extracts. Total phenolic content and antioxidant activities of the extracts increased with increasing ethanol concentration. The antioxidant activities measured by oxygen radical absorbance capacity (ORAC) assay of the 60 and 80% aqueous-ethanolic extracts were significantly higher than that of ascorbic acid. The IC50 of α-glucosidase inhibitory activities of all extracts were comparable to that of acarbose. Phenolics were the major responsible compounds for antioxidant (r = 0.975, p < 0.01 by ORAC assay), α-amylase (r = -0.725, p < 0.01), and lipase (r = 0.607, p < 0.05) inhibitory activities, whilst betacyanins corresponded to α-glucosidase inhibitory activities (r = 0.627, p < 0.05). The 60% aqueous-ethanolic extract was superior to the others in terms of colour, phytochemical contents, and health-promoting activities. These extracts can be utilised as natural food colorant, functional ingredients, and nutraceuticals.

The alpha-amylase inhibitory effect of daucosterol purified from the peel of Chinese water chestnut (CWC), a common Chinese vegetable, was assessed. The alpha-amylase inhibitory properties were elucidated by enzyme inhibition, fluorescence quenching and molecular docking experiments. It was found that three saponins from CWC peel exhibited potent inhibitory activity on alpha-amylase and daucosterol was found to be the main inhibitory factor against alpha-amylase with a mixed-type mode. Strong fluorescence quenching of alpha-amylase was observed under static fluorescence quenching with hydrophobic interactions with daucosterol. Molecular docking revealed that the conformation of daucosterol in the high-affinity sites I and II of alpha-amylase was optimum, and hydrophobic interactions were produced by daucosterol aglycone, and hydrogen bonding by the β-D-glucopyranosyl residue. Ingested daucosterol suppressed the elevation of blood glucose levels through inhibition of alpha-amylase in the small intestine in starch-loaded mice. This study provides data supporting the potential benefit of daucosterol from CWC peel in the treatment of diabetes.

The inhibitory properties towards α-glucosidase in vitro and elevation of postprandial glycemia in mice by the saponin constituent from Eleocharis dulcis peel were evaluated for the first time. Three saponins were isolated by silica gel and HPLC, identified as stigmasterol glucoside, campesterol glucoside and daucosterol by NMR spectroscopy. Daucosterol presented the highest content and showed the strongest α-glucosidase inhibitory activity with competitive inhibition. Static fluorescence quenching of α-glucosidase was caused by the formation of the daucosterol–α-glucosidase complex, which was mainly derived from hydrogen bonds and van der Waals forces. Daucosterol formed 7 hydrogen bonds with 4 residues of the active site and produced hydrophobic interactions with 3 residues located at the exterior part of the binding pocket. The maltose-loading test results showed that daucosterol inhibited elevation of postprandial glycemia in ddY mice. This suggests that daucosterol from Eleocharis dulcis peel can potentially be used as a food supplement for anti-hyperglycemia.

(2S)-3-(2-sulfanylidene-1,3-dihydroimidazol-4-yl)-2-(trimethylazaniumyl)propanoate (ergothioneine, ET) is hy-drophilic antioxidant produced only by certain low-level organisms, but has been reported in the organs of some animals upon dietary intake, facilitated by the ergothioneine transporter (ETT). In this study, it was hypothesised that ETT is involved in the uptake of ET from diet in salmonids. The mechanism of ET uptake was evaluated through knockdown of candidate gene encoding ETT in a cell line (RTG-2) from rainbow trout (Oncorhynchus mykiss). ETT gene expression in blood cells and certain tissues from rainbow trout was also investigated as ET from the diet is expected to be carried over to the muscle. Knockdown of an ETT candidate (E1) in RTG-2 cells resulted in a remarkable decrease in E1 mRNA expression; uptake of ET was lower in the knocked group than in the control group suggesting that E1 functions as an ETT for rainbow trout. Furthermore, the expression of ETT gene in different tissues including the muscle points to ET uptake from the diet to the muscle of salmonids. In conclusion, this study partly reveals the possible pathway underlying ET uptake from the diet and its deposition in the muscle of edible fish species., 公開予定日：2022-06-05

The inhibitory properties towards α-glucosidase

Steroidal gylcosides are the predominant metabolites of starfish and are responsible for various biological activities. Some of these activities are recognized as a part of self-defense mechanism of starfish. Cholesterol-binding ability was evaluated with seven starfish crude extracts, where significantly (p

In this paper, class-C fly ash (FA) and ground granulated blast-furnace slag (GGBS)-based geopolymer activated in NaOH and NaOH + Na2SiO3 was studied regarding setting time, compressive strength, porosity, microstructure, and formation of crystalline phases. When comparing the effects of alkali type on the FA and GGBS geopolymer composites, results revealed that NaOH has a lesser effect in developing strength and denser microstructure than does NaOH + Na2SiO3, since the addition of Na2SiO3 provides the silica source to develop more compact structure. Incorporation of Na2SiO3 reduced the crystallinity and the paste was more amorphous compared to NaOH activated pastes. The class-C FA and GGBS blends resulted in prolonged setting time, reduced strength, and loose matrix with the increase in fly ash content. The un-reactivity of calcium in blends was observed with increasing fly ash content, leading to strength loss. It is evident from XRD patterns that calcium in fly ash did not contribute in forming C-S-H bond, but formation of crystalline calcite was observed. Furthermore, XRD analyses revealed that the reduction in fly ash leads to the reduction in crystallinity, and SEM micrographs showed the unreactive fly ash particles, which hinder the formation of a denser matrix.

The effects of supplementing ergothioneine-rich mushroom extracts (ME) on discoloration and lipid oxidation in astaxanthin-pigmented salmon muscles were evaluated. ME (Flammulina velutipes) were added (in vitro) to minced Oncorhynchus mykiss muscles and stored at -10°C. During several weeks of storage, the ME-treated group showed lower lipid hydroperoxide (HPO) accumulation and higher retained astaxanthin levels than in the control group. The effects of adding concentrated ME (Pleurotus cornucopiae) to Oncorhynchus kisutch diets were also tested over a 2-month feeding trial. No adverse effects on fish growth or pigmentation were observed. Muscle samples were collected, stored (-2 or -18°C), and evaluated. At the end of the storage period, the ME-treated group had lower HPO and higher retained astaxanthin levels in the muscle samples than the levels in the control group. Thus, the addition of ergothioneine from MEs successfully controlled lipid oxidation and stabilized astaxanthin during post-harvest storage at low temperatures.

Nonalcoholic fatty liver disease (NAFLD) is one of the most common liver diseases with no approved treatment. Zonarol, an extract from brown algae, has been proven to have anti-inflammatory and antioxidant effects. In this study, we investigated the role of zonarol in the progression of methionine- and choline-deficiency (MCD) diet-induced NAFLD in mice. After oral treatment with zonarol, a lighter body weight was observed in zonarol group (ZG) mice in comparison to control group (CG) mice. The NAFLD scores of ZG mice were lower than those of CG mice. Hepatic and serum lipid levels were also lower in ZG mice with the reduced expression of lipid metabolism-related factors. Furthermore, ZG mice showed less lipid deposition, less inflammatory cell infiltration and lower inflammatory cytokine levels in comparison to CG mice. Moreover, the numbers of 8-hydroxy-20-deoxyguanosine (8-OHdG)-positive hepatocytes and levels of hepatic and serum thiobarbituric acid reactive substances (TBARS) were significantly lower in comparison to CG mice. The expression levels of nuclear factor erythroid 2 related factor 2 (Nrf2), as well as its upstream and downstream molecules, changed in ZG mice. Zonarol could prevent the progression of NAFLD by decreasing inflammatory responses, oxidative stress and improving lipid metabolism. Meanwhile the Nrf2 pathway may play an important role in these effects.

The enantioselective total syntheses of lepadiformine marine alkaloids, azatricyclic natural products isolated from marine tunicates, were completed. These alkaloids have a unique chemical structure characterized by the trans-1-azadecalin (AB ring system) fused with the spirocyclic ring (AC ring system). Here we found that a cycloisomerization reaction from functionalized linear substrates to a 1-azaspiro[4.5]decane framework corresponding to the AC ring in lepadiformines is promoted by a catalytic amount of mercury(II) triflate (Hg(OTf)2). The total syntheses of (−)-lepadiformines A and B were achieved in 28 % and 21 % overall yields, respectively, through the novel cycloisomerization reaction. The syntheses of (+)- and (−)-lepadiformine C hydrochloride salts also enabled us to determine the absolute configuration of natural lepadiformine C. It has been found that a phenomenon of enantiodivergence occurs in lepadiformine alkaloids from a single species of marine tunicate, Clavelina moluccensis. The cytotoxic activities of synthesized lepadiformine hydrochloride salts and their synthetic intermediates were evaluated.

This study focused on the quick initial setting time and the expansion strain that occurs during the early aging of &alpha, calcium sulfate hemihydrate (&alpha, HH) and examined the setting, compressive strength, and shrinkage strain of &alpha, HH-replaced cement mortar. The results show that the initial setting time significantly decreased with an increase in the &alpha, HH replacement ratio. Drastic occurrence of ettringite was observed early in the aging of cement mortar when &alpha, HH was substituted into the cement, however, the ettringite was not converted to monosulfate with increasing age and thus was not favorable for the development of the compressive strength. When &alpha, HH was substituted into cement, using Portland blast-furnace slag cement (PSC) was more advantageous than using ordinary Portland cement (OPC) for the development of the compressive strength. Meanwhile, the expansion of early age &alpha, HH can decrease the shrinkage strain of cement mortar. The generation of ettringite is more effective when &alpha, HH is substituted into PSC than into OPC and is thus more effective in suppressing the shrinkage strain.

Correction for ‘Inhibition and interactions of alpha-amylase by daucosterol from the peel of Chinese water chestnut (Eleocharis dulcis)’ by Yipeng Gu et al., Food Funct., 2021, DOI: 10.1039/D1FO00887K.

Marine cyanobacteria are known as important creators of novel natural products. From this valuable source, various bioactive compounds have been found and characterized in terms of their pharmacological and toxicological activities.1 In the previous work, we have reported on the isolation and structure determination of potent cytotoxic compounds, lyngbyacyclamide A and B;2 an inhibitor of osteoclastogenesis, biselyngbyaside;3 and a protein kinase inhibitor, bisebromoamide.4 In the recent work, we have reported the new marine γ-pyrones yoshinone A, B1 and B2 from Leptolyngbya sp., and determined their planar structures using NMR spectral analysis.5 Yoshinone A, as the major compound among them, showed inhibitory activity against the adipogenic differentiation of 3T3-L1 cells with an half maximal inhibitory concentration (IC50) value of 420 nm without cytotoxicity (IC50>50 μm). On the other hand, the yoshinone B1 and B2 showed only limited activity against 3T3-L1 cells, with higher concentrations compared with yoshinone A. Further studies of the structure–activity relationship lead us to conclude that the position of a pyrone ring and an olefin in the side chain will be important for the inhibition of adipogenic differentiation. These γ-pyrones have olefins in their side chain at positions 7 and 6 in the cases of yoshinones A and B1/B2, respectively. To express the effects on adipocyte, the olefin should not be conjugated with γ-pyrone moiety, such as yoshinone A (Figure 1). In the previous studies, kalkipyrone6 isolated from cyanobacteria, aureothin,7 and actinopyrones A and B8 isolated from streptomyces fell into the same 7-en γ-pyrones. Then, we confirmed that kalkipyrone and aureothin showed this activity, with IC50 values of 67.5 and 54.2 nm, respectively. On the basis of these data, we are focusing on the 7-en γ-pyrone (unconjugated type) compounds. These pyrones are expected to be candidates for novel lead compounds for the treatment of obesity and related diseases.9 Studies on useful tools that regulate adipocytes will contribute to the prevention and treatment of these diseases. At the present stage of our research, we have evaluated the anti-obesity activities of the 7-en γ-pyrones using in vitro and in vivo experiments. In this study, we report on the interesting properties of these pyrones.

In this paper, class-C fly ash (FA) and ground granulated blast-furnace slag (GGBS)-based geopolymer activated in NaOH and NaOH + Na2SiO3 was studied regarding setting time, compressive strength, porosity, microstructure, and formation of crystalline phases. When comparing the effects of alkali type on the FA and GGBS geopolymer composites, results revealed that NaOH has a lesser effect in developing strength and denser microstructure than does NaOH + Na2SiO3, since the addition of Na2SiO3 provides the silica source to develop more compact structure. Incorporation of Na2SiO3 reduced the crystallinity and the paste was more amorphous compared to NaOH activated pastes. The class-C FA and GGBS blends resulted in prolonged setting time, reduced strength, and loose matrix with the increase in fly ash content. The un-reactivity of calcium in blends was observed with increasing fly ash content, leading to strength loss. It is evident from XRD patterns that calcium in fly ash did not contribute in forming C-S-H bond, but formation of crystalline calcite was observed. Furthermore, XRD analyses revealed that the reduction in fly ash leads to the reduction in crystallinity, and SEM micrographs showed the unreactive fly ash particles, which hinder the formation of a denser matrix.

The enantioselective total syntheses of lepadiformine marine alkaloids, azatricyclic natural products isolated from marine tunicates, were completed. These alkaloids have a unique chemical structure characterized by the trans-1-azadecalin (AB ring system) fused with the spirocyclic ring (AC ring system). Here we found that a cycloisomerization reaction from functionalized linear substrates to a 1-azaspiro[4.5]decane framework corresponding to the AC ring in lepadiformines is promoted by a catalytic amount of mercury(II) triflate (Hg(OTf)

Krebs cycle intermediates (KCIs) are reported to function as energy substrates in mitochondria and to exert antioxidants effects on the brain. The present study was designed to identify which KCIs are effective neuroprotective compounds against oxidative stress in neuronal cells. Here we found that pyruvate, oxaloacetate, and α-ketoglutarate, but not lactate, citrate, iso-citrate, succinate, fumarate, or malate, protected HT22 cells against hydrogen peroxide-mediated toxicity. These three intermediates reduced the production of hydrogen peroxide-activated reactive oxygen species, measured in terms of 2′,7′-dichlorofluorescein diacetate fluorescence. In contrast, none of the KCIs—used at 1 mM—protected against cell death induced by high concentrations of glutamate—another type of oxidative stress-induced neuronal cell death. Because these protective KCIs did not have any toxic effects (at least up to 10 mM), they have potential use for therapeutic intervention against chronic neurodegenerative diseases.

It is known that the compressive strength of concrete will increase as the powder is mixed into the concrete at constant cement content, even in the case of non-hydraulic powder. Despite this, the understanding of the mechanisms is very limited, and this has prevented the establishment of methods for estimating the compressive strength from the mix proportion. In this paper, the authors focus on the phenomenon of the pore size becoming small even if the total pore volume is constant by mixing in various types of powder, and the volume of pores of 50 nm or larger, which have a negative effect on the compressive strength, decreasing. A method for estimating compressive strength, applicable to concrete mixed with various types of powder at constant cement content, was evolved.無機粉体をコンクリートに外割混合することで，その粉体に水硬性がなくとも，圧縮強度が増加することが知られている。しかし，このときのメカニズムについては不明な点が多く，副産物として発生する粉体を外割混合したコンクリートの圧縮強度を調合設計の段階で推定する手法は必ずしも確立されていない。本論文では，コンクリートに粉体を外割混合することで硬化体の総細孔量が変化せずとも個々の細孔が微細になり，その結果，圧縮強度に悪影響を与える50nm以上の細孔量が減少することに着目した。そして，コンクリートの調合から50nm以上の細孔量を一義的に予測する手法，および50nm以上の細孔量と圧縮強度の関係を示すことで，各種粉体を外割混合するコンクリートに適用可能な圧縮強度の推定式を導いた。

Oral administration of Terminalia catappa extract (TCE; 1,000 mg/kg) for 5 wk suppressed bone weight loss and trabecular bone loss in ovariectomized mice. An in vitro experiment showed that TCE (1.3-20 µg/mL) did not increase alkaline phosphatase activity, which would indicate osteoclast formation, in osteoblast-like 3T3-L1 cells. On the other hand, TCE (12.5 µg/mL) markedly decreased the number of tartrate resistant acid phosphatase (TRAP)-positive multinucleated cells, which would indicate osteoclast formation, in a co-culture system (bone marrow cells/osteoblastic UAMS-32 cells). A detailed analysis of the stages of osteoclast differentiation revealed that TCE mainly suppressed the differentiation of bone marrow mononuclear cells into osteoclast progenitor cells in the presence of M-CSF and TGF-β. An additional experiment using fractionated TCE revealed that the water-soluble fraction suppressed the bone weight loss in OVX-mice and osteoclast differentiation in vitro. Therefore, the suppressive effects of TCE on bone weight loss in mice might be due to the suppressive effects of highly polar components on the early stage of osteoclast differentiation.

Peach leaf extract has anti-hyperglycemic effects on the postprandial blood glucose level in glucose-loaded mice. In our previous study, the mechanism of action was considered to be the inhibition of glucose absorption in the small intestine. To elucidate the active principle in peach leaf, purification of the active compound and a structure determination were performed. With the use of bioassay-guided fractionation using glucose-loaded mice, the acetylated kaempferol glycoside multiflorin A (MFA), a potent inhibitor of glucose absorption from the intestine, was isolated from the MeOH extract of leaf of the edible peach Prunus persica. The structure was identified by HPLC using thiazolizine derivatives and by an analysis of its spectral data. The inhibitory effect of MFA against glucose absorption was demonstrated in the dose dependent manner in mice. However, as the deacetylated analog of MFA, multiflorin B did not show the activity at the in vivo, the activity of MFA was suggested to depend on the acetyl group on the sugar moiety. This is the first report of anti-hyperglycemic activity of MFA in peach leaf extract. MFA may be useful in functional foods or medicines for preventing the postprandial absorption of glucose in hyperglycemia.