Nutraceuticals, Volume 2, Issue 2 (June 2022) – 6 articles

Obesity is a prevalent public health concern in several countries, and is closely associated with several pathological disorders, including diabetes, hypertension, cardiovascular diseases, and increased dyslipidemia. Dyslipidemia is an asymptomatic condition characterized by high levels of low-density lipoproteins (LDL) and low levels of high-density lipoproteins (HDL), leading to the increased risk of ischemic heart disease. As lipid disorders are strongly associated with lifestyle and diet, in this work we have evaluated the effect of associating chitosan and exercise on the improvement of the lipid profile of high-fat diet-fed rats. Animals were submitted orally to hypercaloric diets based on liquid butter at 1 mL/100 g to induce a hyperlipidemic state for 8 weeks (as shown by body weight and measures of the Lee obesity index). After 8 weeks, the 40 rats were separated into five groups (n = 8) and adapted to different treatment strategies: physical exercise and/or treatment with chitosan (at a concentration of 2%). The hyperlipidemic group exhibited altered levels of glucose and hepatic enzymes, i.e., aspartate aminotransferase (AST) and alanine aminotransferase (ALT). The treatment with chitosan over 8 weeks significantly reduced the bodyweight of the animals, reaching values lower than the control group. Exercise reduced the Lee obesity index values of all the treated groups compared to non-treated rats. The concentration of total cholesterol, triglycerides, LDL, and VLDL was significantly reduced at the end of the study to healthy thresholds. The hepatic parenchyma of hyperlipidemic animals was recovered to show normal morphology when treated with chitosan; improved histological features (ca. 20–30% of parenchymal cells) could be achieved with physical exercise. In conclusion, oral administration of chitosan associated with physical exercise had a hypolipidemic effect in a model of dyslipidemia in rodents, showing decreased levels of total cholesterol, triglycerides, LDL-c, VLDL-c, glucose, and liver enzymes (AST and ALT). Our results are attributed to the synergism between the administration of chitosan and physical exercise that helps to reduce oxidative stress. Full article

Pterostilbene (Pt) is a natural phenol found in blueberries and grapes; it shows remarkable biomedical activities similar to those of resveratrol, but its higher bioavailability is a major advantage for possible biomedical applications. Our group has recently demonstrated that long-term (30 weeks) administration of Pt to mice maintained on a high-fat diet counters weight gain and promotes browning of subcutaneous white adipose tissue (sWAT). By Real-time quantitative PCR and Western Blot analysis of the sWAT and visceral white adipose tissue (vWAT) from the same mice used in the previous study, we show here that Pt induced a long-term increase of Adiponectin, Interleukin 10 and of M2 macrophage marker Cd206. The effects were observed in sWAT, while no significant changes were detected in vWAT. The process taking place seems to mimic that occurring in sWAT during cold-induced browning. Analysis of a few pro-inflammatory cytokines (Interleukin 6, Tumor necrosis factor α) and of the NFkB pathway did not reveal marked effects of Pt supplementation. In summary, the mechanisms and processes through which Pt acts in adipose tissue appear to closely mimic those set in motion by cold-induced browning, and point to a possible impact of experimental conditions in the final output of a nutraceutical intervention. Full article

We previously reported that the dried peel powder of Citrus kawachiensis, a citrus product of Japan, exerted anti-inflammatory and neuroprotective effects in the brains of transient global cerebral ischemia model mice. It also ameliorated the hyperphosphorylation of Tau protein and the suppression of neurogenesis in the brains of the senescence-accelerated mouse-prone 8 aging model. Chronic unpredictable mild stress (CUMS) induces anxiety-like behavior, changes the composition of the gut microbiota and suppresses neurogenesis in the hippocampus. Therefore, we herein examined the effects of the dried peel powder of C. kawachiensis in a CUMS mouse model: CUMS enhanced locomotor activity, shown as the distance travelled in the open field test at the beginning of the test, while the C. kawachiensis treatment suppressed this increase. The C. kawachiensis treatment also prevented CUMS-induced decreases in hippocampal neurogenesis. The CUMS treatment changed the composition of the gut microbiota by reducing the abundance of Lactobacillus and increasing that of Bacteroides, whereas the C. kawachiensis treatment attenuated these changes. Collectively, the present results suggest that the dried peel powder of C. kawachiensis exerts neuroprotective effects in the brain and maintains the condition of the microbiome under mild stress. Full article

Over the past few years, nutraceuticals have gained substantial attention due to the health-promoting and disease-preventing functions behind their nutritional value. The global prevalence of nutraceuticals is reflected in the increasing number of commercially available nutraceuticals and their wide range of applications. Therefore, a unique opportunity emerges for their further exploration using innovative, reliable, accurate, low cost, and high hit rate methods to design and develop next generation nutraceuticals. Towards this direction, computational techniques constitute an influential trend for academic and industrial research, providing not only the chemical tools necessary for further mechanism characterization but also the starting point for the development of novel nutraceuticals. In the present review, an overview of nutraceuticals is discussed, underscoring the crucial role of chemoinformatic platforms, chemolibraries, and in silico techniques, as well as their perspectives in the development of novel nutraceuticals. This review also aims to record the latest advances and challenges in the area of nanonutraceuticals, an innovative field that capitalizes on the assets of nanotechnology for the encapsulation of bioactive components in order to improve their release profile and therapeutic efficacy. Full article

The tobacco cembranoid (1S,2E,4R,6R,7E,11E)-2,7,11-cembratriene-4,6-diol (4R) interacts with nicotinic acetylcholine receptors, which results in neuroprotection against organophosphate toxicity, brain ischemia, and Parkinson’s disease. The present study is a continuation of our previous research in which we applied a single dose of 4R 1 h before or 24 h after exposure to diisopropylfluorophosphate (DFP) (analog of the nerve agent sarin). The 4R dose robustly decreased neuroinflammation and neuronal death at both timepoints. Here, we investigated the toxicity of a single dose of 4R in male and female Sprague Dawley (SD) rats after a subcutaneous (s.c.) injection of 6, 24, or 98 mg/kg. Body weight was not affected by 4R during the 7-day observation period. No histopathologic changes in the organs were attributed to 4R. Minor hematological and blood composition variations were detected on Day 3 in the mid- and the high-dose males, but these were resolved by Day 8. At the area of the s.c. injection site, alopecia and dry skin were detected in both the 4R-treated males and females and in the female controls. Full article

Numerous native Australian plants are widely used as traditional medicines by the Australian Aboriginal and Torres Strait Islander peoples. Among the native plants, Pittosporum angustifolium Lodd. (Gumby Gumby) is claimed to be a promising medicinal plant in the treatment of a wide range of diseases that includes viral symptoms (colds and coughs), eczema, cancer, muscle aches, varicose veins, and many more. Various extraction techniques are used to extract the bioactive compounds of P. angustifolium, which are formulated into nutraceuticals. The present paper will provide an overview of the recent development in the extraction of bioactive ingredients from P. angustifolium, as well as the findings on the phytochemicals and antimicrobial activity of P. angustifolium extracts. Full article