Mini Reviews in Medicinal Chemistry - Volume 18, Issue 15, 2018

The ellagitannins are a group of phenolic compounds with biological activities. Ellagic acid is the product obtained from hydrolysis of ellagitannins. Information related to the biosynthesis of ellagitannins still been scarce and confused. The ellagitannins are obtained from plants and their purification process implies mainly the use of chromatographic techniques. The ellagitannin acyl hydrolase (EAH) also known as ellagitannase is an enzyme capable of hydrolyzing the ester bonds of ellagitannins and the consequent releasing of ellagic acid. Information about the EAH is not clear because the enzyme had showed different activities due to the low purity or complexity of substrates and there is no available information about the biochemical, physicochemical and molecular characteristics of EAH. The present review describes information related to the sources, biosynthesis and the purification of ellagitannins and a current assessment on the production of ellagitannase.

Objective: Polyphenols are widespread constituents of different food commodities. These are regarded as essential micronutrients because of their well-documented health benefits. These health benefits depend on the amount of polyphenols consumed and their bioavailability in the gut. The microbial transformation of polyphenols in gut is poorly characterized, where, these polyphenols may act as promoting factors for proliferation of beneficial gut inhabitants and inhibiting the pathogenic species. Conclusion: The aim of this review is to present a holistic view on occurrence of polyphenols, their health benefits and influence of dietary polyphenols on gut microbiota.

Still now, for many forms of the disseminated cancers there is no curative therapy available. The discovery of novel active chemotherapeutic agents is largely essential to overcome this problem. Natural compounds polyphenols are mainly characterized by a huge structural variance; they can render them intrinsic dietary components due to their common occurrence in plants. Now-a-days, polyphenols (secondary metabolites) are characterized by a vast spectrum of physiological significance. From the past twenty years in the world of scientific research, polyphenols play an important role in a wide range of physiological processess. This review focuses on the development of polyphenols as antitumor agent in recent research studies.

Inflammation plays an important role in maintaining the body's homeostasis. It repairs the damaged tissues of the body resulting from injury or infection. In addition, a diverse array of diseases like hepatitis, arthritis and colitis has been reported and described to be associated with inflammatory processes. Some autoimmune diseases like inflammatory bowel disease (IBD) emerge by the influence of numerous genes in complex environmental situations belong to inflammation. The currently available processes for curing inflammation and related disorders facilitate the use of non steroidal antiinflammatory drugs (NSAIDs). Moreover, intolerable side effects are also associated with the consumption of these medications. It is well known that phenolic compounds, largely present in vegetables and fruits, serve as an integral part of normal human diet besides having great medicinal value. These are considered to reflect a variety of anti-inflammatory properties, and can be used as an alternate natural source for the prevention of chronic inflammatory disorders. This mini-review summarized the antiinflammatory benefits of plants derived very prominent dietary polyphenolic compounds particularly, Oleocanthal, Curcumin, Resveratrol and Quercetin.

Gallic acid and its derivatives not only exhibit excellent antioxidant, anticarcinogenic, antimutagenic, antimicrobial properties but also provide protection to the cells against oxidative stress. Gallic acid (3, 4, 5-trihydroxybenzoic acid), a low molecular triphenolic compound emerged as an efficient apoptosis inducing agent. The antimicrobial and other biological properties of gallic acid and its derivatives seemed to be linked with the hydrolysis of ester linkage between gallic acid and polyols like tannins hydrolyzed after ripening of many edible fruits. Gallic acid serves a natural defense mechanism against microbial infections and modulation of immune responses. The current review updates us with the diverse roles played by gallic acid, its antioxidant potential, action mechanism and more importantly the diverse array of applications in therapeutic and pharmaceutical areas.

Background & Objective: The inhibitory effects of four series of aryl butene derivatives, active against breast cancer, on the monophenolase activity of tyrosinase, in melanin-free ink from Sepia officinalis, have been studied. Hydroxytamoxifen 1, ferrociphenol 17 and several aryl butene analogs have shown strong antiproliferative activity on hormone-dependent and hormone-independent breast cancer cells and were evaluated in leukemia K562 cell proliferation. Their potential to induce skin depigmentation by evaluating their anti-tyrosinase activity was also estimated. In order to better rationalize the tyrosinase inhibitory action and the binding mode of the compounds, docking studies were carried out. Conclusion: Hydroxytamoxifen and some aryl butenes showed strong antiproliferative effects against K562 cells at 1 μM without showing tyrosinase inhibition. If phenolic compounds 16 and 17 showed the best antiproliferative activity on K562, Hydroxytamoxifen and compounds 5, 10, 20 and 21 have been identified as candidates for further development against chronic myeloid leukemia (CML), and are predicted to not induce depigmentation of the skin, a side effect encountered with imatinib, conventionally used for the treatment of CML.

1,3,5-Triazine-based compounds form a privileged class of compounds in the medicinal chemistry field as they are versatile synthetic scaffolds possessing wide spectra of biological effects including potential anticancer activity. 1,3,5-Triazine compounds explored for anticancer activities have been reported to act by various mechanisms on several molecular targets in human cells such as methyltransferase (DNMT), heat shock protein 90 (Hsp90) and phosphoinositide 3-kinase (PI3K). This review focuses on the synthetic strategies for current developments of 1,3,5-triazine-based anticancer agents and discuses the docking studies that confirm their unique binding modes in the targeted receptors active sites. This article also aims to highlight the future directions for the easy access to these frameworks of more potent and specific anticancer activity.

Indandione is a hydrocarbon classified as bicyclic aromatic β-diketone. It can be applied in many fields of science and industry. It is successfully used as a substrate in organic synthesis, pharmaceutical sciences and as a substrate for the production of dyes. Indandione derivatives and analogs are useful in medicine, chemistry and the judiciary. Among the indandione derivatives can find compounds that have interesting properties and many of them have biological activity (incl. anticancer, anticoagulation, anti-inflamatory, antimicrobial activities). Based on the indan-1,3-dione structure created acetylcholinesterase inhibitors. Indan-1,3-dione derivatives are also used as a derivating agent for the analysis of fatty aldehydes and a substance that is an element of dye-sensitized solar cells. This work presents a brief overview of construction, properties and activities of indandione and its derivatives. This work describes selected indandione derivatives that have properties useful in medicine and industry with particular regard to the anticoagulants and neuroprotective activities in AD.