Current Pharmaceutical Biotechnology - Volume 16, Issue 3, 2015

Inflammatory bowel disease (IBD) is an idiopathic chronic, relapsing inflammation of the bowel which is caused by dysregulation of the mucosal immune system. Polyphenols as the secondary plant metabolites universally present in vegetables and fruits and are the most abundant antioxidants in the human diet. There is evidence demonstrating the beneficial health effects of dietary polyphenols. This review criticizes the potential of commonly used polyphenols including apple polyphenol, bilberry anthocyanin, curcumin, epigallocatechin-3-gallate (EGCG) and green tea polyphenols, naringenin, olive oil polyphenols, pomegranate polyphenols and ellagic acid, quercetin, as well as resveratrol specifically in IBD with an emphasis on cellular mechanisms and pharmaceutical aspects. Scientific research confirmed that dietary polyphenols possess both protective and therapeutic effects in the management of IBD mediated via down-regulation of inflammatory cytokines and enzymes, enhancing antioxidant defense, and suppressing inflammatory pathways and their cellular signaling mechanisms. Further preclinical and clinical studies are needed in order to understand safety, bioavailability and bioefficacy of dietary polyphenols in IBD patients.

Amyotrophic lateral sclerosis (ALS) is a neuromuscular disease that occurs throughout the world with no racial, ethnic or socioeconomic boundaries. Despite its high morbidity and mortality, there are limited medications available for ALS that may increase survival in patients with amyotrophic lateral sclerosis by approximately 2-3 months. Inasmuch as negative effects of riluzole on muscle atrophy and wasting, weakness, muscle spasticity, dysarthria, dysphagia, and overall patient quality of life and its different adverse effects, much attention has been paid to natural products and herbal medicines. Overall scientific reports indicate that natural products have beneficial effects on patients with ALS low side effects and multiple targets. In the present paper, we review the scientific reports on beneficial role of natural polyphenolic compounds in treatment of ALS.

Lots of epidemiological studies have put forward the beneficial effects of dietary polyphenols consumption in the prevention of diseases related to aging i.e vascular pathologies, neurodegeneration, cancers and associated inflammatory processes. Among polyphenols, resveratrol (trans-3,4’,5- trihydroxystilbene, RSV), a naturally occurring stilbene widely distributed in foodstuffs such as grapes and wine, has been the most studied. Researches performed since the last decades in vitro, in animal models and in (pre)clinical studies have pointed out its pleiotropic health benefits by acting on multiple signaling pathways which go beyond its originally described direct antioxidant activity. However, its low bioavailability upon oral ingestion and lack of specificity may hamper the translation of the encouraging experimental data into human health benefits. Herein we provide an overview on the capacity of RSV to regulate oxidative stress-induced signaling and to modulate key components of signal transduction pathways which are commonly altered in cardiovascular, neurodegenerative and cancer pathologies. We also have attempted to provide a comprehensive outlook on RSV metabolism and biological activity of its main metabolites and discussed about the new strategies developed to circumvent its poor bioavailability and to improve its therapeutic efficacy, including synthesis of new derivatives and new formulations for its cell delivery.

Atherosclerosis is a multifactorial disease mainly caused by deposition of low-density lipoprotein (LD) cholesterol in macrophages of arterial walls. Atherosclerosis leads to heart attacks as well as stroke. Epidemiological studies showed that there is an inverse correlation between fruit and vegetable consumption and the risk of atherosclerosis. The promising effect of high vegetable and fruit containing diet on atherosclerosis is approved by several experimental studies on isolated phytochemicals such as flavonoids. Flavonoids are known to up-regulate endogenous antioxidant system, suppress oxidative and nitrosative stress, decrease macrophage oxidative stress through cellular oxygenase inhibition as well as interaction with several signal transduction pathways and from these ways, have therapeutic effects against atherosclerosis. Naringenin is a well known flavonoid belonging to the chemical class of flavanones. It is especially abundant in citrus fruits, especially grapefruits. A plethora of evidences ascribes to naringenin antiatherosclerotic effects. Naringenin abilities to decrease LDL and triglycerides as well as inhibit glucose uptake; increase high-density lipoprotein (HDL); co-oxidation of NADH; suppress protein oxidation; protect against intercellular adhesion molecule-1(ICAM-1); suppress macrophage inflammation; inhibit leukotriene B4, monocyte adhesion and foam cell formation; induce of HO-1 and G 0/G 1 cell cycle arrest in vascular smooth muscle cells (VSMC) and down regulate atherosclerosis related genes are believed to have crucial role in the promising role against atherosclerosis. In the present review, we have summarized the available literature data on the anti-atherosclerotic effects of naringenin and its possible mechanisms of action.

Dual action of galanthamine as potent cholinesterase inhibitor and nicotinic modulator has attracted a great attention to be used in the treatment of AD. Consequently, galanthamine, a natural alkaloid isolated from a Galanthus species (snowdrop, Amaryllidaceae), has become an attractive model compound for synthesis of its novel derivatives to discover new drug candidates. Numerous studies have been done to elucidate interactions between galanthamine and its different derivatives and the enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using in vitro and in silico experimental models. The in vitro studies revealed that galanthamine inhibits AChE in strong, competitive, long-acting, and reversible manner as well as BChE, although its selectivity towards AChE is much higher than BChE. The in silico studies carried out by employing molecular docking experiments as well as molecular dynamics simulations pointed out to existence of strong interactions of galanthamine with the active gorge of AChE, mostly of Torpedo californica (the Pasific electric ray) origin. In this review, we evaluate the mainstays of cholinesterase inhibitory action of galanthamine and its various derivatives from the point of view of chemical and molecular aspects.

Polyphenols are an extensive group of substances present in plants. Animals and humans achieve them through the diet. Polyphenols have been related to several processes, such as oxidative stress and signaling pathways modulating gene expression that promote an anti-inflammatory environment. Moreover, polyphenols also have a possible role in the protection of several diseases, including major depression. Depression is an important public-health problem with a multifactorial etiology and lots of pathways that can be altered in affected subjects. Moreover, this disease can be affected by exercise, sleep and diet. There are animal works studying polyphenols and depression, but human studies are scarce. This review summarizes recent evidences in relation to the effects of polyphenols as antidepressant agents in the depression.

Black, green, and white teas are the main commercial teas obtained from buds and leaves of Camellia sinensis (L.). The postharvest processing treatments, together with genotype and growing techniques, may strongly affect the chemical composition of the tea infusion and, thereby, its potential effects on health. Catechins constituted up to 30% of tea leaves dry weight. During fermentation, polyphenols undergo enzymatic oxidation, leading to the formation of condensed polymeric compounds regarded as responsible for the typical organoleptic properties of black tea leaves and related infusions. Scientific studies has been recently focusing on the possibility that tea polyphenols, particularly those of black and green tea, may lead to healthy properties in individuals affected by diseases correlated to metabolic syndrome. In vivo experiments reveal that green and black tea polyphenols may be able to reduce hyperglycemia and insulin resistance. Other works suggest that black tea polymeric products may be effective in decreasing blood cholesterol levels and hypertriacylglycerolemia. To this regard, very few data about white tea, being the rarest and the least handled tea, are available so far. It has been reported that white tea could show higher antioxidative capacity than green tea and to exert in vitro lipolytic activity. Considering the increasing interest towards healthy potential through diet and natural medicaments, the aim of the present review was to overview the nutraceutical potential of polyphenols from tea after various degrees of fermentation.

Biological effects of natural polyphenols from mango and their potential impact on human health have become of increasing interest. The occurrence of glycosilated molecules, such as mangiferin (C2-β-Dglucopyranosyl- 1,3,6,7-tetrahydroxyxanthone), main component of the mango polyphenolic fraction, and benzophenones, flavonoids (catechin and epicatechin), phenolic acids (benzoic and gallic), and a wide range of derivatives, provide a high chemical complexity. In this review, the potential impact of mango polyphenols and its protective effects on diseases associated to oxidative stress is discussed.

Premature ejaculation (PE) is an important and common sexual issue in male adults, since its etiology is still unknown. There are many suggested treatments such as paroxetine, clomipramine, dapoxetine, tramadol and topical agents; all of them have stigma or considerable side effects. Therefore, present study aimed to examine the effect of on-demand caffeine consumption on treating patients with PE. In this double blind RCT, 40 otherwise healthy individuals with PE were allocated into 2 groups of caffeine and placebo group. The caffeine group received 100 mg encapsulated caffeine for 3 weeks, 2 hours prior to each intercourse. Intravaginal ejaculation latency time (IELT) and index of sexual satisfaction (ISS) were measured before and after treatment in both groups. Suitable statistical analysis was performed. (Registration code: IRCT2013091614677N1). Mean age of the participants was 39.88±8.72 years. No significant difference was found between pre-treatment and post-treatment values of both IELT and ISS in the placebo group, but significant difference was seen in post treatment values between our two groups and pre-treatment and post-treatment values of the caffeine group (IELT: 144s vs 312s, p<0.001 and ISS: 77 vs 97, p<0.001; respectively). Furthermore, high significant correlation was found in post-treatment values (r>0.07, p<0.05). There are negligible scientific evidences regarding the beneficial effects of caffeine on several aspects of sexual life, which makes comparison impossible. Considering the fact that caffeine is a well-known and widely used drug in common disease, using this compound will not result in any stigma. Our study demonstrates that 100mg on-demand caffeine can significantly increase both IELT and ISS. Furthermore, the slope of these increasings is correlated with each other. More studies are needed to make stronger conclusions.