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Plant α-amylase inhibitors and their effect on the utilization of polysaccharides contained in the diet.
Kurhajec, S, Franc, A
Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti. 2019;(4):148-156
Abstract
Development of civilization diseases such as diabetes mellitus, metabolic syndrome or obesity, enforces the increasing effort to find new drugs, especially from natural sources. These include α-amylase inhibitors, which break down polysacharides into simple sugars in the body of a healthy person. As this cleavage affects the level of blood sugar, which is sought to be therapeutically influenced, there is a growing interest in these substances. This review maps the types of amylase inhibitors, including their natural resources.
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2.
[Importance of annexin V in kidney diseases].
Jakubowska, A, Kiliś-Pstrusińska, K
Postepy higieny i medycyny doswiadczalnej (Online). 2015;:153-7
Abstract
Annexin V (AnV) belongs to a cytoplasmic calcium binding protein family found in many body tissues, including distal tubule cells and glomerular epithelial cells. The biological role of this protein discovered so far is connected with apoptosis. AnV is considered as an early marker of that process and is used in one of the most frequently applied apoptosis detection methods, consisting in the detection of biochemical and morphological changes in cells. Measuring the AnV level may help understand many renal processes. Elevated AnV levels have been found in both acute and chronic renal conditions. Applying AnV to identify cells in the early phase of apoptosis in acute pyelonephritis caused by Escherichia coli showed that hemolysins of pathogenic bacteria stimulate the death of tubular cells and that the intensification of the process depends on the level of the toxin and its activity time. Studies on the mechanisms of reperfusion injury in acute renal injury have revealed protective activity of a synthetic AnV homodimer with regard to tubular cells. AnV was also used in diabetic nephropathy to study the influence of metabolic disorders on the intensification of apoptosis in renal tubular cells. Additionally, the suitability of AnV measurement as a biochemical marker of atherosclerosis in patients with a chronic renal condition was evaluated. It was also used to study the causes of immunodeficiency in patients diagnosed with the above-mentioned condition. There have been few papers published so far on the significance of AnV in children with renal conditions. The prognostic value of AnV and T cell apoptosis was evaluated in children with nephrotic syndrome.
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3.
A proprietary alpha-amylase inhibitor from white bean (Phaseolus vulgaris): a review of clinical studies on weight loss and glycemic control.
Barrett, ML, Udani, JK
Nutrition journal. 2011;:24
Abstract
Obesity, and resultant health hazards which include diabetes, cardiovascular disease and metabolic syndrome, are worldwide medical problems. Control of diet and exercise are cornerstones of the management of excess weight. Foods with a low glycemic index may reduce the risk of diabetes and heart disease as well as their complications. As an alternative to a low glycemic index diet, there is a growing body of research into products that slow the absorption of carbohydrates through the inhibition of enzymes responsible for their digestion. These products include alpha-amylase and glucosidase inhibitors. The common white bean (Phaseolus vulgaris) produces an alpha-amylase inhibitor, which has been characterized and tested in numerous clinical studies. A specific and proprietary product named Phase 2® Carb Controller (Pharmachem Laboratories, Kearny, NJ) has demonstrated the ability to cause weight loss with doses of 500 to 3000 mg per day, in either a single dose or in divided doses. Clinical studies also show that Phase 2 has the ability to reduce the post-prandial spike in blood glucose levels. Experiments conducted incorporating Phase 2 into food and beverage products have found that it can be integrated into various products without losing activity or altering the appearance, texture or taste of the food. There have been no serious side effects reported following consumption of Phase 2. Gastro-intestinal side effects are rare and diminish upon extended use of the product. In summary, Phase 2 has the potential to induce weight loss and reduce spikes in blood sugar caused by carbohydrates through its alpha-amylase inhibiting activity.
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4.
Inhibitors of aldo-keto reductases AKR1C1-AKR1C4.
Brožič, P, Turk, S, Rižner, TL, Gobec, S
Current medicinal chemistry. 2011;(17):2554-65
Abstract
The AKR1C aldo-keto reductases (AKR1C1-AKR1C4) are enzymes that interconvert steroidal hormones between their active and inactive forms. In this manner, they can regulate the occupancy and trans-activation of the androgen, estrogen and progesterone receptors. The AKR1C isoforms also have important roles in the production and inactivation of neurosteroids and prostaglandins, and in the metabolism of xenobiotics. They thus represent important emerging drug targets for the development of agents for the treatment of hormone-dependent forms of cancer, like breast, prostate and endometrial cancers, and other diseases, like premenstrual syndrome, endometriosis, catamenial epilepsy and depressive disorders. We present here the physiological roles of these enzymes, along with their structural properties and an overview of the recent developments regarding their inhibitors. The most important strategies of inhibitor design are described, which include the screening of banks of natural compounds (like cinnamic acids, flavonoids, jasmonates, and related compounds), the screening of and structural modifications to non-steroidal anti-inflammatory drugs, the substrate-inspired design of steroidal and nonsteroidal inhibitors, and computer-assisted structure-based inhibitor design.
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5.
Allopurinol, an inhibitor of uric acid synthesis--can it be used for the treatment of metabolic syndrome and related disorders?
Suzuki, I, Yamauchi, T, Onuma, M, Nozaki, S
Drugs of today (Barcelona, Spain : 1998). 2009;(5):363-78
Abstract
Allopurinol is an inhibitor of xanthine oxidoreductase (XOR) and inhibits the generation of uric acid (UA) as the final product of purine catabolism, as well as the resulting generation of superoxide (O2(-)), in humans. Elevation of the serum UA (SUA) level, referred to as hyperuricemia (HU), eventually leads to gout and allopurinol has been used for the treatment of HU and gout. Studies have revealed the role of elevated SUA levels and the associated oxidative stress (OS) in a broad spectrum of pathological conditions and it is anticipated that these findings would also expand the use of allopurinol as a therapeutic drug. This article presents a review of reports, mainly of recent studies, on the efficacy of allopurinol in various diseases and explores novel potential uses of the drug. Important novel and potential uses of great interest include metabolic syndrome (MetS) and related disorders, chronic kidney disease (CKD), nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH). Ischemia-reperfusion injury and mucositis, encountered as adverse effects of cancer treatment, have also been under investigation as potential targets for allopurinol.
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6.
The prominent role of the liver in the elimination of asymmetric dimethylarginine (ADMA) and the consequences of impaired hepatic function.
Richir, MC, Bouwman, RH, Teerlink, T, Siroen, MP, de Vries, TP, van Leeuwen, PA
JPEN. Journal of parenteral and enteral nutrition. 2008;(6):613-21
Abstract
Asymmetric dimethylarginine (ADMA) is an endogenous inhibitor of nitric oxide synthase (NOS), the enzyme which converts the amino acid arginine into nitric oxide (NO). ADMA has been identified as an important risk factor for cardiovascular diseases. Besides the role of ADMA in cardiovascular diseases, it also seems to be an important determinant in the development of critical illness, (multiple) organ failure, and the hepatorenal syndrome. ADMA is eliminated from the body by urinary excretion, but it is mainly metabolized by the dimethylarginine dimethylaminohydrolase (DDAH) enzymes that convert ADMA into citrulline and dimethylamine. DDAH is highly expressed in the liver, which makes the liver a key organ in the regulation of the plasma ADMA concentration. The prominent role of the liver in the elimination of ADMA and the consequences of impaired hepatic function on ADMA levels will be discussed in this article.