The Safety and Pharmacokinetics of Cyanidin-3-Glucoside after 2-Week Administration of Black Bean Seed Coat Extract in Healthy Subjects

We analyzed the pharmacokinetics of C3G on data from twelve subjects, after 2-week multiple dosing of black bean (Phaseolus vulgaris, Cheongjakong-3-ho) seed coat extract, using the mixed effect analysis method (NONMEM, Ver. 6.2), as well as the conventional non-compartmental method. We also examined the safety and tolerability. The PK analysis used plasma concentrations of the C3G on day 1 and 14. There was no observed accumulation of C3G after 2-week multiple dosing of black bean seed coat extract. The typical point estimates of PK were CL (clearance)=3,420 l/h, V (volume)=7,280 L, Ka (absorption constant)=9.94 h^-1, ALAG (lag time)=0.217 h. The black bean seed coat extract was well tolerated and there were no serious adverse events. In this study, we confirmed that a significant amount of C3G was absorbed in human after given the black bean seed coat extract.     

Anthocyanins from Vaccinium arctostaphylos Berries

The systematic investigation of the berries of Vaccinium arctostaphylos L. (Ericaceae), a native medicinal plant growing in Iran, permitted the identification of three major anthocyanins. The compounds were isolated from the acidified extract of the berries using the repeated paper chromatography with different mobile phases and were characterized using chromatographic, chemical, and spectroscopic methods as delphinidin 3-O-β-glucoside, petunidin 3-O-β-glucoside, and malvidin 3-O-β-glucoside.     

Effects of blackcurrant anthocyanin intake on peripheral muscle circulation during typing work in humans

This double-blind, placebo-controlled, crossover study investigated the effect of blackcurrant anthocyanin (BCA) intake on peripheral circulation during rest and during typing work by using near-infrared spectroscopy (NIRS), and it also assessed improvement in shoulder stiffness caused by poor local circulation. In a resting circulation study, nine healthy male subjects took capsules of BCA at a dosage of 17 mg kg^–1 or placebo (isoenergetic sugar). NIRS was used to measure left forearm blood flow (FBF) following venous occlusion and muscle oxygen consumption following arterial occlusion prior to and hourly for 4 h after ingestion of BCA. Plasma anthocyanin concentration was measured prior to ingestion and 1, 2, and 4 h later. FBF increased significantly 2 h after BCA ingestion [BCA 1.22 (0.13)-fold increase relative to pre-values vs placebo 0.83 (0.06) of pre-values; P<0.05] and then tended to increase for a further 3 h after ingestion [BCA 1.26 (0.15)-fold increase relative to pre-values vs placebo 0.82 (0.07) of pre-values; P=0.078]. There was, however, no significant difference in muscle oxygen consumption between BCA and placebo intake at any time point. In a typing work study, 11 healthy subjects took capsules of BCA (7.7 mg kg^–1) or placebo (isoenergetic sugar) daily for 2 weeks. The subjects then performed intermittent typing workload for 30 min in order to induce acute shoulder stiffness. During the workload, total hemoglobin and oxygenated hemoglobin (oxy-Hb) were determined using NIRS and myoelectric signals measured in the right trapezius muscle using electromyography (EMG). The viscoelasticity of the trapezius muscle was also evaluated using a muscle stiffness meter before and after the typing workload. BCA intake prevented the decrease in oxy-Hb significantly (P<0.05), and also tended to alleviate the increase in root mean square (RMS) of the EMG during the typing workload, and also muscle stiffness after the workload. There was no improvement in typing performance with BCA intake. The results of this study suggest that intake of BCA may improve shoulder stiffness caused by typing work by increasing peripheral blood flow and reducing muscle fatigue.     

Antioxidant and memory enhancing effects of purple sweet potato anthocyanin and cordyceps mushroom extract

The effects of purple sweet potato anthocyanin (SPA) and Cordyceps mushroom extract (CME) on lipid peroxidation, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and cognitive deficits were examined. Both SPA and CME exhibited DPPH radical scavenging activities with similar potency. In contrast, only SPA was shown to effectively inhibit lipid peroxidation initiated by Fe2+ and ascorbic acid in rat brain homogenates. Furthermore, SPA markedly enhanced cognitive performance, assessed by passive avoidance test in ethanol-treated mice. Combined treatments with SPA and CME did not significantly influence the effects of SPA alone. These results demonstrate that anthocyanin prepared from purple sweet potato exhibits memory enhancing effects, which may be associated with its antioxidant properties.     

Anti-obesity effects of artificial planting blueberry (Vaccinium ashei) anthocyanin in high-fat diet-treated mice

This study aimed to evaluate the anti-obesity effects of artificial planting blueberry (Vaccinium ashei) anthocyanin (BA) in high-fat diet-induced obese male C57BL/6 mice. BA at doses of 50, 100, and 200?mg/kg was supplemented in the daily food of obese C57BL/6 mice during an 8-week experiment. Our findings indicate that consumption of BA at high doses reduced body weight by 19.4%, whereas both low and middle doses did not affect the body weight. Furthermore, BA supplementation at high dose could effectively decrease serum glucose, attenuate epididymal adipocytes, improve lipid profiles, and significantly down-regulate expression levels of TNFα, IL-6 PPARγ, and FAS genes. Therefour, BA might alter bodyweight by suppressing fatty acid synthesis and alleviating inflammation.     

A ROS-Responsive Self-Assembly Driven by Multiple Intermolecular Interaction Enhances Tumor-Targeted Chemotherapy

To develop a drug carrier sensitive to reactive oxygen species (ROS), a nanocomplex (NCs) based on sulfuric hyaluronic acid (sHA)-anthocyanin (ATC) was developed. Doxorubicin (DOX) is loaded into the sHA-ATC NCs (AD@sHA) through intermolecular π-π stacking and hydrophobic interactions. AD@sHA can be prepared in aqueous phase by simple mixing method. In AD@sHA, DOX content and load efficiency are high. Compared with D@sHA (without ATC), the ROS-ATC co-mediated responsive degradation and drug release of AD@sHA was confirmed. In addition, AD@sHA also improved apoptosis of CD44⁺ colon cancer HT29 cells. HT29 tumor-bearing mice model was used to confirm the role of AD@SHA in targeted tumor therapy. The results showed that AD@SHA could optimize the biodistribution of DOX. These data, from tumor volume and TUNEL analysis, observed the delay of tumor growth and apoptosis of cancer cells. Even more exciting is that AD@sHA significantly reduces the myelosuppression of DOX. This study means that AD@sHA has a better effect on chemotherapy for CD44-positive tumors.     

花色苷通过腺苷一磷酸激活蛋白激酶减少肝脏HepG2细胞的脂肪积聚

目的探讨花色苷单体矢车菊素-3-葡萄糖苷(Cy-3-g)对HepG2细胞脂肪含量的影响以及可能机制。方法HepG2细胞分别用1、10、100μmol/LCy-3-g处理1h,设置对照,检测腺苷一磷酸激活蛋白激酶(AMPK)及其磷酸化水平、肉碱脂酰转移酶-I(CPT-I)、乙酰辅酶A羧化酶(ACC)磷酸化水平、AMPK活性、甘油三酯含量以及脂肪酸氧化水平。结果与对照组相比,显著上调CPT-I蛋白的表达水平,显著增强AMPK的活性,显著促进AMPK蛋白磷酸化,但对AMPK蛋白表达水平无影响,显著减少HepG2细胞内的甘油三酯含量,10、100μmol/LCy-3-g能显著促进ACC的磷酸化,100μmol/LCy-3-g能显著促进HepG2细胞脂肪酸氧化。结论花色苷Cy-3-g可以减少HepG2细胞脂肪积聚;其机制可能与调节HepG2细胞AMPK-ACC-CPT-I信号通路,促进脂肪酸氧化有关。     

Dietary supplementation with New Zealand blackcurrant extract enhances fat oxidation during submaximal exercise in the heat

ObjectivesThis study investigated the effect of 7 days’ supplementation with New Zealand blackcurrant extract on thermoregulation and substrate metabolism during running in the heat.DesignRandomized, double-blind, cross-over study.MethodsTwelve men and six women (mean ± SD: Age 27 ± 6 years, height 1.76 ± 0.10 m, mass 74 ± 12 kg, V̇O_2max 53.4 ± 7.0 mL kg⁻¹ min⁻¹) completed one assessment of maximal aerobic capacity and one familiarisation trial (18 °C, 40% relative humidity, RH), before ingesting 2 × 300 mg day⁻¹ capsules of CurraNZ™ (each containing 105 mg anthocyanin) or a visually matched placebo (2 × 300 mg microcrystalline cellulose M102) for 7 days (washout 14 days). On day 7 of each supplementation period, participants completed 60 min of fasted running at 65% V̇O_2max in hot ambient conditions (34 °C and 40% relative humidity).ResultsCarbohydrate oxidation was decreased in the NZBC trial [by 0.24 g min⁻¹ (95% CI: 0.21–0.27 g min^-1)] compared to placebo (p =  0.014, d = 0.46), and fat oxidation was increased in the NZBC trial [by 0.12 g min⁻¹ (95% CI: 0.10 to 0.15 g min⁻¹)], compared to placebo (p = 0.008, d = 0.57). NZBC did not influence heart rate (p = 0.963), rectal temperature (p = 0.380), skin temperature (p = 0.955), body temperature (p = 0.214) or physiological strain index (p = 0.705) during exercise.ConclusionsSeven-days intake of 600 mg NZBC extract increased fat oxidation without influencing cardiorespiratory or thermoregulatory variables during prolonged moderate intensity running in hot conditions.     

Cold storage of blueberry (Vaccinium spp.) fruits and juice: Anthocyanin stability and antioxidant activity

Blueberries (Vaccinium spp.) may be considered one of the best potential sources of antioxidants in the diet. This characteristic results from the presence of flavonoids (especially anthocyanins), tannins and phenolic acids in the fruits. The objective of this work was to analyze the anthocyanin stability and antioxidant activity of refrigerated whole blueberry juice stored at 4 °C for 10 d, and of fruits stored frozen (−18 °C) for 6 months, in order to determine the changes occurring during storage. The frozen fruits showed a significant increase (p < 0.05) in antioxidant activity during the 3rd month of frozen storage, followed by a decrease up to the end of the 6-month period. The juice was analyzed every other day, and the antioxidant activity changed on the 8th d of refrigerated storage, remaining stable up to the 10th d. There were significant losses of anthocyanins both in the frozen fruits (59%) and refrigerated juice (83%). The antioxidant capacity was shown to be stable during cold storage both in the case of the fruits and whole juice, whereas the anthocyanins were degraded, possibly due to oxidations and/or condensation reactions with other phenolic compounds. More studies are required to optimize the storage time and temperature of these products with respect to nutrient stability.     

蓝莓对大鼠肝纤维化模型中转录因子KLF11表达的影响

目的:观察蓝莓对肝纤维化模型中抗纤维化转录因子Krüppel样因子11(KLF11)的影响,探讨其可能的机制。方法:40只健康同周龄SD大鼠被随机分为正常对照组、蓝莓对照组、模型组和蓝莓预防组,每组10只,使用四氯化碳制作肝纤维化模型。测定各组大鼠血清丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)、Ⅳ型胶原、Ⅲ型前胶原(PCⅢ)、透明质酸(HA)和层粘连蛋白水平;Masson和HE染色对肝组织进行病理学检查;Western blot和免疫组织化学染色检测肝组织中KLF11的蛋白表达,Western blot检测肝组织中α-平滑肌肌动蛋白(α-SMA)的蛋白表达;real-time PCR检测肝组织中KLF11和Ⅰ型胶原(ColⅠ)的mRNA表达情况。结果:与正常对照组比较,模型组KLF11蛋白表达显著降低(P<0.01),而α-SMA蛋白表达显著升高(P<0.01);与模型组比较,蓝莓预防组KLF11的mRNA表达显著升高(P<0.01)而ColⅠ的mRNA表达显著降低(P<0.01);与模型组比较,其它各组大鼠血清ALT、AST、HA和PCⅢ水平均显著降低(P<0.01),蓝莓预防组大鼠肝纤维化分级显著降低(P<0.01)。结论:蓝莓对四氯化碳所致大鼠肝纤维化有一定的预防作用,其机制可能与其影响KLF11表达有关。