In vitro fermentation characteristics of blueberry anthocyanins and their impacts on gut microbiota from obese human.

It has been demonstrated that the gut microbiota may play an important intermediary role in anthocyanins' beneficial impacts on obesity. However, the microbe-related anti-obesity mechanism of blueberry anthocyanins remains unclear. In this study, the interactions between blueberry anthocyanin extracts (BAE) and gut microbiota from obese humans were explored using an in vitro fermentation model. Due to hydrolysis and metabolism by the microbiota, the contents of blueberry anthocyanins are reduced during fermentation. It was demonstrated that both aglycones and glycosides affected the degradation rate. The microbial composition evaluation revealed that BAE could alleviate obesity by promoting the colonization of probiotics such as Lachnospiraceae_UCG-004 and Bacteroides, as well as inhibiting the proliferation of harmful bacteria including Escherichia-Shigella, Clostridium_sensu_stricto_1, and Klebsiella. Blueberry anthocyanin extracts facilitate the production of short-chain fatty acids (SCFAs), which is beneficial for obesity control. The relationship between blueberry anthocyanins, gut microbiota, and SCFAs was further investigated. Overall, this data provides new insights into the positive interaction between blueberry anthocyanins and gut microbiota in obese humans.

In vitro digestion under simulated saliva, gastric and small intestinal conditions and fermentation of nicotinamide mononucleotide, and its effects on the gut microbiota.

Nicotinamide Mononucleotide (NMN) is a derivative of vitamin B3, which plays a significant role in a plethora of metabolic reactions in the human body and is intricately associated with both immunity and metabolism. Nonetheless, in the intestine metabolic pathway of NMN and the relationship between NMN, gut microbiota, and SCFAs remain hitherto obscure. This study examined the digestion of NMN in simulated saliva, gastric, and small intestine environments, as well as exploring the interaction between NMN and human gut microbiota utilizing an in vitro fermentation model. NMN was progressively degraded into nicotinamide ribose (NR), nicotinamide (NAM), and ribose, with niacinate (NA) constituting the ultimate degradation product due to hydrolysis and metabolism by microbiota. NMN was ingested by human intestinal microbiota with a slower fermentation rate. As a result of NMN ingestion by human gut bacteria，the concentrations of propionate and butyrate increased by 88% and 23%, respectively, compared to the blank control group, the proliferation of beneficial gut bacteria (Bifidobacterium, Phascolarctobacterium, Faecalibacteriun, and Alistipes) significantly increased, while the proliferation of some harmful bacteria (Sutterella, Desulfovibrio and Pseudomonas) drastically declined. These findings illustrated the metabolic processes of NMN in the intestine, elaborating the relationship between NMN, SCFAs and gut microbiota. NMN might be a potential prebiotic to improve intestinal health.

Simulated Digestion and Fermentation In Vitro by Obese Human Gut Microbiota of Sulforaphane from Broccoli Seeds.

BACKGROUND: sulforaphane is a kind of isothiocyanate, which is obtained by hydrolysis of glucosinolate by the unique myrosinase in plants. It has been proved to prevent the occurrence of many chronic diseases, such as obesity, diabetes and cancer. OBJECTIVE: The impact of SFN on obese human gut flora, however, has not been established. METHODS: In this research, SFN was isolated from broccoli seeds and then refined to achieve 95% purity. Next, an investigation was conducted into the digestion and fermentation processes of SFN. RESULTS: The stability of the SFN in simulated saliva, gastric fluid, and intestinal juice provides evidence that it can reach the gut and be available for utilization by gut microflora. In vitro fermentation of SFN by gut microbes in obese patients results in alteration in constitution of microbiota and production of short chain fatty acids. As the result of SFN ingestion by human gut bacteria, the content of butyric and valeric acids increased 1.21- and 1.46-fold, respectively. In obese human guts, the relative abundances of the beneficial genera including Lactobacillus, Weissella, Leuconosto, Algiphilus and Faecalibacterium significantly increased, whilst the detrimental genera, such as Escherichia-Shigella, Klebsiella, Clostridium_sensu_stricto_1, Sutterella, Megamonas and Proteus drastically declined. CONCLUSION: Taken together, these findings demonstrate that SFN can be used as a nutraceutical ingredient for obese patients and for improving human health.

Heat-Moisture Treatment Further Reduces In Vitro Digestibility and Enhances Resistant Starch Content of a High-Resistant Starch and Low-Glutelin Rice.

A novel rice germplasm sbeIIb/Lgc1 producing grains rich in resistant starch (RS) but low in glutelin has been developed through CRISPR/Cas9-mediated targeted mutagenesis for its potential benefits to patients with diabetes and kidney diseases. In this study, a hydrothermal approach known as heat-moisture treatment (HMT) was identified as a simple and effective method in reinforcing the nutritional benefits of sbeIIb/Lgc1 rice. As a result of HMT treatment at 120 °C for 2 h, significant reductions in in vitro digestibility and enhancements in RS content were observed in sbeIIb/Lgc1 rice flour when the rice flour mass fraction was 80% and 90%. The low-glutelin feature of sbeIIb/Lgc1 rice was not compromised by HMT. The potential impacts of HMT on a range of physicochemical properties of sbeIIb/Lgc1 rice flour have also been analyzed. HMT resulted in a darker color of rice flour, alteration in the semi-crystalline structure, an increase in gelatinization temperatures, and reductions in the pasting viscosities as the moisture content increased. This study provides vital data for the food industry to facilitate the application of this dual-functional rice flour as a health food ingredient.

Perylenequinonoid-catalyzed photoredox activation for the direct arylation of (het)arenes with sunlight.

Naturally occurring perylenequinonoid pigments (PQPs) have attracted considerable attention owing to their excellent properties of photosensitization. They have been widely investigated as an aspect of photophysics and photobiology. However, their applications in photocatalysis are yet to be explored. We report here that sunlight along with 1 mol% cercosporin, which is one of the perylenequinonoid pigments, catalyzes the direct C-H bond arylation of (het)arenes by a photoredox process with good regioselectivity and broad functional group compatibility. Furthermore, a gram-scale reaction with great conversions of substrates was achieved even by a cercosporin-containing supernatant without organic solvent extraction and purification after liquid fermentation. Thus we set up a bridge between microbial fermentation and organic photocatalysis for chemical reactions in a sustainable, environmentally friendly manner.

Brain distribution and efficacy as chemosensitizer of an oral formulation of PARP-1 inhibitor GPI 15427 in experimental models of CNS tumors.

We previously demonstrated that intravenous or intra-cerebral administration of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors increases the antitumor activity of temozolomide (TMZ), an oral anticancer drug used for the treatment of malignant melanoma and primary or secondary brain tumors. Since the oral route has a number of advantages in terms of safety and convenience with respect to intravenous injection, in this study we tested whether administration per os of the novel PARP-1 inhibitor GPI 15427 allows sufficient absorption of the compound and achievement of brain concentrations capable of enhancing the efficacy of TMZ against tumors growing at the CNS. Pharmacokinetics analysis of GPI 15427 levels in plasma and brain was assessed in Sprague-Dawley rats after oral dosing, by liquid chromatography and tandem mass spectrometry. Antitumor activity of oral GPI 15427 in association with TMZ was evaluated in BD2F1 mice injected intracranially with B16 melanoma or L5178Y lymphoma. Pharmacokinetics studies revealed that GPI 15427 possesses a substantial oral bioavailability (plasma Cmax after a single dose of 40 mg/kg: 1041+/-516 ng/ml). Moreover, the brain levels and brain/plasma ratios of GPI 15427 (3.37 at 0.5 h and 3.19 at 1 h) indicated that the compound readily penetrates the blood-brain barrier. GPI 15427 (10 or 40 mg/kg/per os) was then administered for five days, 1 h before TMZ (100 mg/kg/i.p.), to tumor-bearing mice. The results indicated that GPI 15427+TMZ was well tolerated and significantly increased life-span of the animals with respect to TMZ. In conclusion, PARP-1 inhibitor GPI 15427 is efficacious as chemosensitizer for the treatment of tumors located at the CNS site when it is administered by oral route.

Effect of middle cerebral artery occlusion on mRNA expression for the sodium-coupled vitamin C transporter SVCT2 in rat brain.

The sodium-vitamin C co-transporter SVCT2 is primarily responsible for the accumulation of the important antioxidant ascorbate into brain cells. In vitro studies have demonstrated strong expression of this transporter in cultured astrocytes, whereas in situ hybridization analysis has so far detected SVCT2 only in neurons. In the present study, we examined the response of SVCT2 mRNA expression in the brain to focal ischemia induced for 2 h by unilateral middle cerebral artery occlusion. The mRNA expression patterns of SVCT2 and the glutamate-activated immediate early gene Arc were investigated at 2 and 22 h after ischemia. SVCT2 and Arc mRNA expression was lost in the ischemic core at both time points. In areas outside the core, Arc was strongly up-regulated, primarily at 2 h, whereas SVCT2 showed an increase at 2 and 22 h. SVCT2 expression was increased in neurons as well as in astrocytes, providing the first evidence for SVCT2 expression in astrocytes in situ. These findings underscore the importance of ascorbate as a neuroprotective agent and may have implications for therapeutic strategies. In addition, the increase of SVCT2 in astrocytes after ischemia suggests that cultured astrocytes are exposed to chronic oxidative stress.