Activity

Agmatine is a neurotransmitter with anticonvulsant, anti-neurotoxic and antidepressant-like effects, in addition it has hypoglycemic actions. Agmatine is converted to putrescine and urea by agmatinase (AGM) and by an agmatinase-like protein (ALP), a new type of enzyme which is present in human and rodent brain tissues. Recombinant rat brain ALP is the only mammalian protein that exhibits significant agmatinase activity in vitro and generates putrescine under in vivo conditions. ALP, despite differing in amino acid sequence from all members of the ureohydrolase family, is strictly dependent on Mn2+ for catalytic activity. However, the Mn2+ ligands have not yet been identified due to the lack of structural information coupled with the low sequence identity that ALPs display with known ureohydrolases. In this work, we generated a structural model of the Mn2+ binding site of the ALP and we propose new putative Mn2+ ligands. Then, we cloned and expressed a sequence of 210 amino acids, here called the “central-ALP”, which include the putative ligands of Mn2+. The results suggest that the central-ALP is catalytically active, as agmatinase, with an unaltered Km for agmatine and a decreased kcat. Similar to wild-type ALP, central-ALP is activated by Mn2+ with a similar affinity. Besides, a simple mutant D217A, a double mutant E288A/K290A, and a triple mutant N213A/Q215A/D217A of these putative Mn2+ ligands result on the loss of ALP agmatinase activity. Our results indicate that the central-ALP contains the active site for agmatine hydrolysis, as well as that the residues identified are relevant for the ALP catalysis.Amphiphilic Polymer Co-networks Synthesis, Properties, Modelling and Applications is a new and very interesting book published by the Royal Society of Chemistry and edited by Prof. Costas S. Patrickios (University of Cyprus). Herein, a brief review of the most important features of the book and its contents is provided from a personal perspective.Long-distance transport of information molecules in the vascular tissues could play an important role in regulating plant growth and enabling plants to cope with adverse environments. Various molecules, including hormones, proteins, small peptides and small RNAs have been detected in the vascular system and proved to have systemic signaling functions. Sporadic studies have shown that a number of mRNAs produced in the mature leaves leave their origin cells and move to distal tissues to exert important physiological functions. In the last 3-5 years, multiple heterograft systems have been developed to demonstrate that a large quantity of mRNAs are mobile in plants. BTK inhibitor in vivo Further comparison of the mobile mRNAs identified from these systems showed that the identities of these mRNAs are very diverse. Although species-specific mRNAs may regulate the unique physiological characteristic of the plant, mRNAs with conserved functions across multiple species are worth more effort in identifying universal physiological mechanisms existing in the plant kingdom.Hot flushes are best-known for affecting menopausal women, but men who undergo life-saving castration due to androgen-sensitive prostate cancer also suffer from these vasomotor symptoms. Estrogen deficiency in these patients is a direct consequence of androgen deprivation, because estrogens (notably 17β-estradiol, E2) are produced from testosterone. Although estrogens alleviate hot flushes in these patients, they also cause adverse systemic side effects. Because only estrogens can provide mitigation of hot flushes on the basis of current clinical practices, there is an unmet need for an effective and safe pharmacotherapeutic intervention that would also greatly enhance patient adherence. To this end, we evaluated treatment of orchidectomized (ORDX) rats with 10β, 17β-dihydroxyestra-1,4-dien-3-one (DHED), a brain-selective bioprecursor prodrug of E2. A pilot pharmacokinetic study using oral administration of DHED to these animals revealed the formation of E2 in the brain without the appearance of the hormone in the circulation. Therefore, DHED treatment alleviated androgen deprivation-associated hot flushes without peripheral impact in the ORDX rat model. Concomitantly, we showed that DHED-derived E2 induced progesterone receptor gene expression in the hypothalamus without stimulating galanin expression in the anterior pituitary, further indicating the lack of systemic estrogen exposure upon oral treatment with DHED.Vitrimers are a new class of cross-linked materials that are capable of network topology alternation through the associative dynamic bond-exchange mechanism, which has recently been invented to solve the problem of conventional cross-linked materials, such as poor recyclability and healability. Thus far, the concept of vitrimers has been applied to various commercial polymers, e.g., polyesters, polylactides, polycarbonates, polydimethylsiloxanes, polydienes, polyurethanes, polyolefins, poly(meth)acrylates, and polystyrenes, by utilizing different compatible bond-exchange reactions. In this review article, the concept of vitrimers is described by clarifying the difference from thermoplastics and supramolecular systems; in addition, the term “associative bond-exchange” in vitrimers is explained by comparison with the “dissociative” term. Several useful functions attained by the vitrimer concept (including recyclability and healability) are demonstrated, and recent molecular designs of vitrimers are classified into groups depending on the types of molecular frameworks. This review specifically focuses on the vitrimer molecular designs with commercial polymer-based frameworks, which provide useful hints for the practical application of the vitrimer concept.The addition of functional ingredients to breads could have effects on preventing cardiovascular diseases, cancers and inflammation. The incorporation of 0-5-10-15% of three populations of dried purslane flour on the rheological, sensorial and nutritional quality of fortified durum wheat breads were evaluated. The increase in dried purslane (up to 15%) caused an increase in the resistance to the mixture and a consequent reduction in its extensibility. The “panel test” gave a largely positive evaluation in 10% of enrichment. The fatty acids in breads resulted higher with the 5% substitution. Contrary to what has been imagined, the increase in percentage of substitution to 10 and 15% did not lead to an increase in linoleic (omega-3) and α-linolenic (omega-6) acid and probably the cause is in the cooking. The total phenols content and the antioxidant potential, evaluated by ferric reducing antioxidant potential (FRAP) and 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays of the enriched breads increased with the percentage of the dry purslane substitution.