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1.
Absorption and Metabolism of γ-Oryzanol, a Characteristic Functional Ingredient in Rice Bran.
Sawada, K, Rahmania, H, Matsuki, M, Hashimoto, H, Ito, J, Miyazawa, T, Nakagawa, K
Journal of nutritional science and vitaminology. 2019;(Supplement):S180-S184
Abstract
γ-Oryzanol (OZ), a functional substance found in rice bran, consists of multiple molecular species. In both in vitro and in vivo studies, the researches exploring the various function of rice bran OZ have been conducted for a long time, and it has become clear that OZ has a lot of pharmaceutical activities. It is assumed that each type of OZ molecular species may have different effects. In contrast, the profile behaviour of OZ inside the body has not been fully understood. This article reviews the previous studies about the digestion, absorption, metabolism, and effects of rice bran OZ and also introduces the new method to evaluate the OZ metabolic fate by using high-performance liquid chromatography (HPLC) combined with tandem mass-spectrometry (MS/MS) which has higher selectivity and sensitivity.
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2.
Genetic factors involved in the bioavailability of tomato carotenoids.
Desmarchelier, C, Landrier, JF, Borel, P
Current opinion in clinical nutrition and metabolic care. 2018;(6):489-497
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Abstract
PURPOSE OF REVIEW To provide an update on the genetic factors recently associated with the interindividual variability of tomato carotenoid bioavailability. RECENT FINDINGS Several clinical studies have demonstrated that the main carotenoids found in tomatoes (lycopene, phytoene, phytofluene, β-carotene, lutein) all display relatively large interindividual variabilities of their bioavailability, with coefficients of variations more than 70%. The bioavailability of the parent molecules, and the blood/tissue appearance of their metabolites, is modulated by numerous proteins, involved in intestinal absorption and metabolism, blood lipoprotein transport or tissue uptake. Several single nucleotide polymorphisms (SNPs) have been associated with the interindividual variability of lycopene, lutein and β-carotene bioavailability, with six genes consistently shared between the three carotenoids, and in particular one SNP in ELOVL fatty acid elongase 2. The effects of the genetic variants taken separately are relatively low, that is each variant is usually associated with only a few percentage of the variability but multivariate analyses suggest that the additive effect of several genetic variants can explain a significant fraction of tomato carotenoid bioavailability. SUMMARY Additional studies are needed to improve our knowledge of the genetic determinants of tomato carotenoid bioavailability but progress in this field could one day allow nutritionists to provide more personalized dietary recommendations.
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Low colonic absorption drugs: risks and opportunities in the development of oral extended release products.
Xu, J, Lin, Y, Boulas, P, Peterson, ML
Expert opinion on drug delivery. 2018;(2):197-211
Abstract
INTRODUCTION Currently numerous drugs have been observed with lower colonic absorption than small intestine absorption, which can significantly impact in vivo performance of their oral extended release (ER) products. AREAS COVERED We reviewed over 300 publications, patents, book chapters, and commercial reports of drug products from regulatory agencies for low colonic absorption (LCA) drugs and critical findings are discussed. The focuses of this article are (1) current findings on the causes of low colonic absorption to support early assessment of LCA candidates, and (2) current knowledge on successful ER strategies and technical platforms used for LCA drugs in commercial drug products to facilitate oral ER product development. EXPERT OPINION Colonic drug absorption is one of the critical considerations in successful development of oral ER products. The root causes of low colonic absorption in many LCA drugs are still unclear. It is recommended to evaluate colonic drug absorption of drug candidate at early stage of oral ER product development. After evaluation, the selection of a formulation platform to develop an oral ER product needs to be carefully considered for LCA drugs. Based on the current commercial oral ER formulation platforms for LCA drugs, compounds are first divided into five types (I-V) and different ER formulation approaches with higher success rate are recommended for each type.
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Glutathione depleting drugs, antioxidants and intestinal calcium absorption.
Moine, L, Rivoira, M, Díaz de Barboza, G, Pérez, A, Tolosa de Talamoni, N
World journal of gastroenterology. 2018;(44):4979-4988
Abstract
Glutathione (GSH) is a tripeptide that constitutes one of the main intracellular reducing compounds. The normal content of GSH in the intestine is essential to optimize the intestinal Ca2+ absorption. The use of GSH depleting drugs such as DL-buthionine-S,R-sulfoximine, menadione or vitamin K3, sodium deoxycholate or diets enriched in fructose, which induce several features of the metabolic syndrome, produce inhibition of the intestinal Ca2+ absorption. The GSH depleting drugs switch the redox state towards an oxidant condition provoking oxidative/nitrosative stress and inflammation, which lead to apoptosis and/or autophagy of the enterocytes. Either the transcellular Ca2+ transport or the paracellular Ca2+ route are altered by GSH depleting drugs. The gene and/or protein expression of transporters involved in the transcellular Ca2+ pathway are decreased. The flavonoids quercetin and naringin highly abrogate the inhibition of intestinal Ca2+ absorption, not only by restoration of the GSH levels in the intestine but also by their anti-apoptotic properties. Ursodeoxycholic acid, melatonin and glutamine also block the inhibition of Ca2+ transport caused by GSH depleting drugs. The use of any of these antioxidants to ameliorate the intestinal Ca2+ absorption under oxidant conditions associated with different pathologies in humans requires more investigation with regards to the safety, pharmacokinetics and pharmacodynamics of them.
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The role of mucoprotectants in the management of gastrointestinal disorders.
Eutamene, H, Beaufrand, C, Harkat, C, Theodorou, V
Expert review of gastroenterology & hepatology. 2018;(1):83-90
Abstract
The intestinal barrier controls the absorption of nutrients and water whilst helping to prevent the entry of toxins and pathogenic micro-organisms from the lumen into the tissues. Deficiencies in the barrier are associated with various gastrointestinal and extra digestive disorders. Areas covered: This review provides an overview of the relationship between increased intestinal permeability and disease, and considers the role of mucosal protectants (mucoprotectants) in restoring normal intestinal barrier function, with a particular focus on diarrheal disorders. Expert commentary: Impairment of the intestinal barrier characterizes a variety of diseases, and there is ongoing interest in the development of pharmacological approaches targeting the reduction of intestinal permeability. These include corticosteroids, aminosalicylates and anti-tumor necrosis factor-α (TNF-α), which act by reducing inflammation; probiotics, which modulate the production of mucin and epithelial tight junction proteins; and mucoprotectants, which form a protective film over the epithelium. Recently, preclinical and clinical data highlight, the ability of new mucoprotectants, such as gelatin tannate and xyloglucan, to protect the intestinal mucosa and to exert anti-diarrheal effects. In the future the ability of these substances to enhance the intestinal barrier may extend their use in the management of a variety of gastro-intestinal diseases associated with 'leaky gut'.
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Association Between Exercise-Induced Hyperthermia and Intestinal Permeability: A Systematic Review.
Pires, W, Veneroso, CE, Wanner, SP, Pacheco, DAS, Vaz, GC, Amorim, FT, Tonoli, C, Soares, DD, Coimbra, CC
Sports medicine (Auckland, N.Z.). 2017;(7):1389-1403
Abstract
BACKGROUND Prolonged and strenuous physical exercise increases intestinal permeability, allowing luminal endotoxins to translocate through the intestinal barrier and reach the bloodstream. When recognized by the immune system, these endotoxins trigger a systemic inflammatory response that may affect physical performance and, in severe cases, induce heat stroke. However, it remains to be elucidated whether there is a relationship between the magnitude of exercise-induced hyperthermia and changes in intestinal permeability. OBJECTIVE In this systematic review, we evaluated whether an exercise-induced increase in core body temperature (T Core) is associated with an exercise-induced increase in intestinal permeability. METHODS The present systematic review screened the MEDLINE/PubMed and Web of Science databases in September 2016, without any date restrictions. Sixteen studies that were performed in healthy participants, presented original data, and measured both the exercise-induced changes in T Core and intestinal permeability were selected. These studies assessed intestinal permeability through the measurement of sugar levels in the urine and measurement of intestinal fatty acid binding protein or lipopolysaccharide levels in the blood. RESULTS Exercise increased both T Core and intestinal permeability in most of the 16 studies. In addition, a positive and strong correlation was observed between the two parameters (r = 0.793; p < 0.001), and a T Core exceeding 39 °C was always associated with augmented permeability. CONCLUSION The magnitude of exercise-induced hyperthermia is directly associated with the increase in intestinal permeability.
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A theoretical physiologically based pharmacokinetic approach for modeling the fate of anthocyanins in vivo.
Celli, GB, Ghanem, A, Brooks, MS
Critical reviews in food science and nutrition. 2017;(15):3197-3207
Abstract
Recent studies on the pharmacokinetics of anthocyanins (ACNs) and their metabolites have uncovered evidence for hitherto unknown physiological effects affecting the fate of these compounds in vivo. In particular, it has been shown that the stomach, in addition to the small intestine, has an important role in absorption. Most studies still use a noncompartmental or one-compartmental approach to determine the pharmacokinetic parameters of ACNs, which does not represent the anatomical and physiological conditions that a compound is subject to in the organism. Thus, the objective of this study was to review the current knowledge of the different processes involved in the metabolism of ACNs once ingested and, based on this information, propose a theoretical physiologically based, multicompartmental pharmacokinetic (PBMK) model to describe their fate in vivo. This is the first study that reports a PBMK model for ACNs; the model provides a more physiologically representative approach for ANC metabolism, which could be used as a basis for experimental designs and interspecies scale-up.
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[DRUG THERAPY FOLLOWING BARIATRIC SURGERY: EXAMINATION OF POTENTIAL IMPACT AND CLINICAL RECOMMENDATIONS].
Azran, C, Dahan, A
Harefuah. 2017;(1):31-37
Abstract
Bariatric surgery is the most effective solution for morbid obesity, and the number of patients undergoing bariatric surgery is rapidly and constantly growing. The modified gastrointestinal (GI) anatomy of the patient may lead to significant pharmacokinetic alterations in the oral absorption of drugs after surgery. However, due to insufficient available literature and inadequate awareness of the medical team, bariatric surgery patients may be discharged from the hospital with insufficient instructions regarding their medication therapy. In this article, we aim to present the various mechanisms by which bariatric surgery may influence oral drug absorption, to provide an overview of the currently available literature on the subject, and to present guidelines on instruction recommendations that bariatric surgery patients should receive before leaving the hospital. To date, and until more robust data is published, it is essential to follow and monitor patients closely to enhance the safety and efficacy of their medication therapies, both in the immediate and long term periods post-surgery.
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9.
Absorption of Carotenoids and Mechanisms Involved in Their Health-Related Properties.
Cervantes-Paz, B, Victoria-Campos, CI, Ornelas-Paz, Jde J
Sub-cellular biochemistry. 2016;:415-54
Abstract
Carotenoids participate in the normal metabolism and function of the human body. They are involved in the prevention of several diseases, especially those related to the inflammation syndrome. Their main mechanisms of action are associated to their potent antioxidant activity and capacity to regulate the expression of specific genes and proteins. Recent findings suggest that carotenoid metabolites may explain several processes where the participation of their parent carotenoids was unclear. The health benefits of carotenoids strongly depend on their absorption and transformation during gastrointestinal digestion. The estimation of the 'bioaccessibility' of carotenoids through in vitro models have made possible the evaluation of the effect of a large number of factors on key stages of carotenoid digestion and intestinal absorption. The bioaccessibility of these compounds allows us to have a clear idea of their potential bioavailability, a term that implicitly involves the biological activity of these compounds.
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10.
Physiology of Intestinal Absorption and Secretion.
Kiela, PR, Ghishan, FK
Best practice & research. Clinical gastroenterology. 2016;(2):145-59
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Abstract
Virtually all nutrients from the diet are absorbed into blood across the highly polarized epithelial cell layer forming the small and large intestinal mucosa. Anatomical, histological, and functional specializations along the gastrointestinal tract are responsible for the effective and regulated nutrient transport via both passive and active mechanisms. In this chapter, we summarize the current state of knowledge regarding the mechanism of intestinal absorption of key nutrients such as sodium, anions (chloride, sulfate, oxalate), carbohydrates, amino acids and peptides, lipids, lipid- and water-soluble vitamins, as well as the major minerals and micronutrients. This outline, including the molecular identity, specificity, and coordinated activities of key transport proteins and genes involved, serves as the background for the following chapters focused on the pathophysiology of acquired and congenital intestinal malabsorption, as well as clinical tools to test and treat malabsorptive symptoms.