Avocado Paste Phenolics Mitigate a High-Fat Diet-Induced Plasma HDL Decrease in Male Wistar Rats, by Altering the mRNA Expression of Hepatic SCARB1.

Avocado paste (AP) is the main industrial byproduct of its processing, and retains various phenolic compounds (PCs). PCs are known to normalize the plasma lipid profile, but those from avocado byproducts have been minimally studied. We report the normalizing effects of an AP-derived phenolic extract (PE) on the plasma lipid profile of male Wistar rats. A standard (SD) and high-fat diet (HFD) were formulated, and the same diets were supplemented with 1 g/kg of diet of PE (SD + PE and HFD + PE). Rats were fed these diets during an 8-week period. The HFD induced signs of dyslipidemia, but PE treatment countered the decrease in HDL. Relative mRNA expression (real-time PCR) of the hepatic HDL receptor (SCARB1) increased in both groups (SD + PE and HFD + PE), while the LDR receptor (LDLR) increased in SD + PE group. The mRNA expression of apolipoproteins APOA1 and APOB was unaffected. We conclude that PCs from AP can counter a diet-induced decrease in plasma HDL by acting on the mRNA expression of its hepatic receptor.

Caesalpinia palmeri: First Report on the Phenolic Compounds Profile, Antioxidant and Cytotoxicity Effect.

This study aimed to determine the phenolic compounds profile, antioxidant potential and cytotoxicity of extracts and fractions of Caesalpinia palmeri. Methanolic extracts were generated from C. palmeri berries, stems and flowers. The latter was subjected to liquid-liquid partition, obtaining hexane, ethyl acetate and residues fractions. Results showed that the flower extract and ethyl acetate fraction had a larger concentration of phenolic compounds (148.9 and 307.9 mg GAE/g, respectively), being ellagic acid (6233.57 and 19550.08 µg/g, respectively), quercetin-3-ß-glycoside (3023.85 and 8952.55 µg/g, respectively) and gallic acid (2212.98 and 8422.34 µg/g, respectively) the most abundant compounds. Flower extract and ethyl acetate fraction also presented the highest antioxidant capacity on all tested methods (DPPH, ABTS, ORAC and FRAP) and low cytotoxicity against ARPE-19 cells (IC50 >170 µg/mL). C. palmeri possessed high antioxidant potential, associated with the presence of phenolic compounds and low cytotoxicity, suggesting that they could represent an option to counter oxidative stress.

Lesser-Consumed Tropical Fruits and Their by-Products: Phytochemical Content and Their Antioxidant and Anti-Inflammatory Potential.

Açaí, lychee, mamey, passion fruit and jackfruit are some lesser-consumed tropical fruits due to their low commercial production. In 2018, approximately 6.8 million tons of these fruits were harvested, representing about 6.35% of the total world production of tropical fruits. The present work reviews the nutritional content, profile of bioactive compounds, antioxidant and anti-inflammatory capacity of these fruits and their by-products, and their ability to modulate oxidative stress due to the content of phenolic compounds, carotenoids and dietary fiber. Açaí pulp is an excellent source of anthocyanins (587 mg cyanidin-3-glucoside equivalents/100 g dry weight, dw), mamey pulp is rich in carotenoids (36.12 mg ß-carotene/100 g fresh weight, fw), passion fruit peel is rich in dietary fiber (61.16 g/100 dw). At the same time, jackfruit contains unique compounds such as moracin C, artocarpesin, norartocarpetin and oxyresveratrol. These molecules play an important role in the regulation of inflammation via activation of mitogen-activated protein kinases (including p38, ERK and JNK) and nuclear factor κB pathways. The properties of the bioactive compounds found in these fruits make them a good source for use as food ingredients for nutritional purposes or alternative therapies. Research is needed to confirm their health benefits that can increase their marketability, which can benefit the primary producers, processing industries (particularly smaller ones) and the final consumer, while an integral use of their by-products will allow their incorporation into the circular bioeconomy.

Phenolic compounds can induce systemic and central immunomodulation, which result in a neuroprotective effect.

Inflammation may negatively impact health, particularly that of the central nervous system. Phenolic compounds are bioactive molecules present in fruits and vegetables with potential anti-inflammatory effects. The purpose of the present work is to review the immunomodulatory bioactivities of phenolic compounds in the periphery and in the central nervous system. Results show that various types of phenolics are able to counter diet- or pathogen-induced systemic inflammation (among others) in various models. In vitro data show significant effects of flavonoids and phenolic acids in particular; similar bioactivities were reported in vivo, when administering them as pure compounds or from fruit and vegetable extracts that contain them. In the central nervous system, phenolics counter chronic inflammation and aggressive acute inflammatory processes, such as ischemic events, when administered preemptively and even therapeutically. We therefore conclude that the immunomodulatory potential of phenolic compounds can maintain an adequate immune response; their regular consumption should therefore be prioritized in order to maintain health. PRACTICAL APPLICATIONS: The immune response must be carefully regulated in order to avoid its deleterious effects. The present work highlights how phenolic compounds, dietary components ubiquitous in everyday diet, are able to maintain it within an adequate range. As humans are exposed to more proinflammatory stimuli (inadequate dietary pattern, mental stress, environmental pollution, chronic diseases, etc.), it becomes necessary to counter them, and consuming adequate amounts of foods that contain compounds with this ability is a rather simple strategy. Thus, the present work highlights how fruits and vegetables can help to maintain an adequate immune response that can preserve systemic health and that of the central nervous system. Furthermore, specific compounds contained in them can also be ideal candidates for additional in-depth studies, which can potentially lead to the development of potent, targeted, and safe anti-inflammatory molecules.

Use of nanosystems to improve the anticancer effects of curcumin.

Curcumin (CUR) is a phenolic compound that is safe for human consumption. It exhibits chemopreventive, antiproliferative, antiangiogenic, and antimetastatic effects. However, these benefits can be hampered due to the lipophilic nature, rapid metabolism, low bioavailability, and fast elimination of the molecule. Considering this, the present work reviews the use of CUR-based nanosystems as anticancer agents, including conventional nanosystems (i.e., liposomes, nanoemulsions, nanocrystals, nanosuspensions, polymeric nanoparticles) and nanosystems that respond to external stimuli (i.e., magnetic nanoparticles and photodynamic therapy). Previous studies showed that the effects of CUR were improved when loaded into nanosystems as compared to the free compound, as well as synergist effects when it is co-administrated alongside with other molecules. In order to maximize the beneficial health effects of CUR, critical factors need to be strictly controlled, such as particle size, morphology, and interaction between the encapsulating material and CUR. In addition, there is an area of study to be explored in the development of CUR-based smart materials for nanomedical applications. Imaging-guided drug delivery of CUR-based nanosystems may also directly target specific cells, thereby increasing the therapeutic and chemopreventive efficacy of this versatile compound.

Sub-chronic consumption of a phenolic-rich avocado paste extract induces GLP-1-, leptin-, and adiponectin-mediated satiety in Wistar rats.

Avocado paste (AP) is a phenolic-rich byproduct of avocado oil extraction. The effects of sub-chronic consumption of diets supplemented with an AP phenolic extract (PE) were analyzed. A standard diet (SD), high-fat diet (HFD), and these supplemented with PE (SD + PE and HFD + PE) were used. Significantly increased satiety was observed in PE-supplemented groups, according to less food consumption (-15% in SD + PE vs. SD, and -11% in HFD + PE vs. HFD), without changes in weight gain or percentage of adipose tissue. PE-supplemented groups had an increased plasma concentration ( + 16% in SD + PE vs. SD, and +26% in HFD + PE vs. HFD) and relative mRNA expression (+74% in SD + PE vs. SD, and +46% in HFD + PE vs. HFD) of GLP-1; an increase in plasma leptin and adiponectin was independent of their mRNA expression. Our results suggest that AP-derived PE exerts a satiety effect in vivo, possibly mediated by GLP-1, leptin, and adiponectin. PRACTICAL APPLICATIONS: Minimizing food waste is a top priority in most of the world, thus, researchers seek methods to reintroduce industrial fruit and vegetable byproducts into the food processing chain. The present work highlights the potential of avocado byproducts as sources of bioactive phenolic compounds, whose sub-chronic consumption (8 weeks) exerts a satiety action in vivo. Avocado farming is resource-intensive, making it of relevance to producers and processing industries to avoid discarding its byproducts as much as possible.

Phenolic compounds that cross the blood-brain barrier exert positive health effects as central nervous system antioxidants.

The blood-brain barrier (BBB) is a physical structure whose main function is to strictly regulate access to circulating compounds into the central nervous system (CNS). Vegetable-derived phenolic compounds have been widely studied, with numerous epidemiologic and interventional studies confirming their health-related bioactivities across multiple cells, organs and models. Phenolics are non-essential xenobiotics, and should theoretically be unable to cross the BBB. The present work summarizes current experimental evidence that reveals that not only are phenolic compounds able to cross the BBB and bioaccumulate in the brain, but there is some stereoselectivity, which suggests the presence of specific transporters that allow them to reach the brain. Some molecules cross the BBB intact, while others do so only after being biotransformed or metabolized elsewhere. Once inside the CNS, they prevent or counter oxidative stress, which maintains the molecular, cellular, structural and functional integrity of the brain, and subsequently, overall human health.

Curcumin Loaded and Co-loaded Nanosystems: A Review from a Biological Activity Enhancement Perspective.

BACKGROUND: Curcumin is a natural phenolic compound exhibiting multiple bioactivities that have been evaluated in vitro, in vivo as well as through clinical studies in humans. Some of them include antimicrobial, antioxidant, anti-inflammatory, and central nervous system protective effects. Further, curcumin is generally recognized as a safe substance because of its low toxicity. However, its molecular structure is susceptible to changes in pH, oxidation, photodegradation, low aqueous solubility, and biotransformation compromising its bioavailability; these drawbacks are successfully addressed through nanotechnology. OBJECTIVE: The present review systematizes findings on the enhancement of curcumin's beneficial effects when it is loaded and co-loaded into different types of nanosystems covering liposomes, polymeric and solid-lipid nanoparticles, nanostructured lipid carrier, lipid-polymeric hybrids, self- -assembled and protein-based core-shell systems in relation to its antimicrobial, antioxidant, anti-inflammatory and central nervous system protective bioactivities. CONCLUSION: Curcumin is a versatile molecule capable of exerting antimicrobial, antioxidant, anti- inflammatory, and central nervous system protective effects in an enhanced manner using the possibilities offered by the nanotechnology-based approach. Its enhanced bioactivities are associated with increments in solubility, stability, bioavailability, as well as in improved intracellular uptake and cell internalization. These advantages, in addition to curcumin's low toxicity, indicate the potential of curcumin to be loaded and co-loaded into nanosystems capable of providing a controlled release and targeted administration.

Annonas: Underutilized species as a potential source of bioactive compounds.

The genus Annona belongs to the family Annonaceae and includes several species of tropical and subtropical crops characterized by their edible and exotic fruits. Twenty species of Annona have been reported in Mexico, localized mainly in the tropical southeastern regions of the country. Most species, however, are not marketable and remain underutilized, and are often referred to as wild Annona species, but they are a valuable source of bioactive compounds. According to ethnobotanical evidence, extracts obtained from different Annona species and different parts of the plant (stem bark, leaves, roots, seeds, and peel) have been used in traditional medicine to treat various ailments. Most of their reported health benefits are attributed to the presence of bioactive compounds with various in vitro and in vivo biological activities, such as antidepressant, antidiabetic, neuroprotective, anticonvulsant, anti-inflammatory, antiproliferative, vasorelaxant, antipyretic, anti-ulcer, analgesic, and healing activities. Therefore, further extensive knowledge of these species especially information on their health benefits is essential to increase their cultivation and commercial use. The present review focuses on traditional uses of underutilized Annona species, their bioactive compounds content, and biological activities.