Adenosine: a partially discovered medicinal agent

Background A plethora of chemicals exists in human body which can alter physiology in one way or other. Scientists have always been astounded by such abilities of chemicals but as the technology advances, even the chemical which was once expected to be well known changes its status to not really well known. Adenosine is one of the chemicals which is in consonance with the aforementioned statements, although previous articles have covered vast information on role of adenosine in cardiovascular physiology, bacterial pathophysiology and inflammatory diseases. In this review we have discussed adenosine and its congeners as potential promising agents in the treatment of Huntington’s disease, post-traumatic stress disorder, erectile dysfunction, viral infections (SARS-CoV) and anxiety. Main text Adenosine is a unique metabolite of ATP; which serves in signalling as well. It is made up of adenine (a nitrogenous base) and ribo-furanose (pentose) sugar linked by β-N9-glycosidic bond. Adenosine on two successive phosphorylation forms ATP (Adenosine Triphosphate) which is involved in several active processes of cell. It is also one of the building blocks (nucleotides) involved in DNA (Deoxy-ribonucleic Acid) and RNA (Ribonucleic Acid) synthesis. It is also a component of an enzyme called S-adenosyl-L-methionine (SAM) and cyano-cobalamin (vitamin B-12). Adenosine acts by binding to G protein-coupled receptor (GPCR: A1, A2A, A2B and A3) carries out various responses some of which are anti-platelet function, hyperaemic response, bone remodelling, involvement in penile erection and suppression of inflammation. On the other hand, certain microorganisms belonging to genus Candida, Staphylococcus and Bacillus utilize adenosine in order to escape host immune response (phagocytic clearance). These microbes evade host immune response by synthesizing and releasing adenosine (with the help of an enzyme: adenosine synthase-A), at the site of infection. Conclusion With the recent advancement in attribution of adenosine in physiology and pathological states, adenosine and its congeners are being looked forward to bringing a revolution in treatment of inflammation, viral infections, psychiatric and neurodegenerative disorders.

PENGARUH RADIASI SINAR ULTRAVIOLET TIPE C (UVC) TERHADAP KULTUR TOTAL MIKROBA IKAN ASAP PINEKUHE

Untuk meningkatkan mutu produk olahan khas daerah, khususnya ikan asap pinekuhe, pengembangan teknik atau instrumen baru menjadi sebuah keharusan. Sejauh ini, metode yang umum digunakan untuk mempertahankan mutu produk pangan, khususnya mutu mikrobiologis, adalah mensterilkan produk pangan untuk mengurangi dan menginaktifkan mikroba kontaminan misalnya melalui perebusan, penggaraman atau pengasapan. Tetapi metode steriliasi menggunakan sinar ultraviolet khususnya tipe C (UVC) belum banyak diterapkan pada produk pangan di Indonesia. Sinar ultraviolet adalah gelombang elektromagnetik yang memiliki muatan elektron berfrekuensi tinggi dan panjang gelombang 100-400 nm. Sinar UV dapat memotong rantai basa nitrogen dalam RNA atau DNA sehingga menyebabkan kegagalan pemberian kode genetik untuk sintesa protein dan kematian mikroba. Penelitian ini bertujuan untuk mempelajari pengaruh sinar UVC terhadap isolat kultur mikroba dari ikan asap pinekuhe dengan menggunakan metode observasi dan analisa data secara deskriptif. Koloni bakteri yang diisolasi dari ikan pinekuhe dipaparkan dengan sinar UVC dengan perlakuan (12, 24, 36 dan 48) jam. Hasil penelitian menunjukan bahwa sinar ultra violet tipe c (UVC) dengan daya 8 va dan penyinaran 48 jam mempengaruhi pertumbuhan koloni mikroba ikan asap pinekuhe secara maksimal berupa kekeringan pada koloni bakteri isolat dari ikan asap pinekuhe. To improve quality of pinekuhe smoked fish locally produced in Sangihe Islands, development of new techniques or instruments becomes necessary. Widely used techniques for maintaining food quality mainly include sterilization through boiling, salting or smoking. To date, however, sterilization by ultraviolet type C (UVC) has been poorly practiced for preserving food products in Indonesia. Ultraviolet light is an electromagnetic wave that has a high frequency electron charge with a wavelength of 100-400 nm. It can cut the nitrogenous base chains in RNA or DNA resulting in coding failure in protein synthesis, causing the death of microbes. This research aimed to study the effect of UVC on microbes isolated from pinekuhe. The results showed that UVC radiation with 8 va for 48 hours significantly affected the growth of microbial colonies isolated from the smoked fish, drying up the bacterial colony.

Recent Progress of Benzimidazole Hybrids for Anticancer Potential

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

Improving data quality and expanding BioSAXS experiments to low-molecular-weight and low-concentration protein samples

The addition of compounds to scavenge the radical species produced during biological small-angle X-ray scattering (BioSAXS) experiments is a common strategy to reduce the effects of radiation damage and produce better quality data. As almost half of the experiments leading to structures deposited in the SASBDB database used scavengers, finding potent scavengers would be advantageous for many experiments. Here, four compounds, three nucleosides and one nitrogenous base, are presented which can act as very effective radical-scavenging additives and increase the critical dose by up to 20 times without altering the stability or reducing the contrast of the tested protein solutions. The efficacy of these scavengers is higher than those commonly used in the field to date, as verified for lysozyme solutions at various concentrations from 7.0 to 0.5 mg ml−1. The compounds are also very efficient at mitigating radiation damage to four proteins with molecular weights ranging from 7 to 240 kDa and pH values from 3 to 8, with the extreme case being catalase at 6.7 mg ml−1, with a scavenging factor exceeding 100. These scavengers can therefore be instrumental in expanding BioSAXS to low-molecular-weight and low-concentration protein samples that were previously inaccessible owing to poor data quality. It is also demonstrated that an increase in the critical dose in standard BioSAXS experiments leads to an increment in the retrieved information, in particular at higher angles, and thus to higher resolution of the model.

Inequality in the Frequency of the Open States Occurrence Depends on Single 2H/1H Replacement in DNA

In the present study, the effect of 2H/1H isotopic exchange in hydrogen bonds between nitrogenous base pairs on occurrence and open states zones dynamics is investigated. These processes are studied using mathematical modeling, taking into account the number of open states between base pairs. The calculations of the probability of occurrence of open states in different parts of the gene were done depending on the localization of the deuterium atom. The mathematical modeling study demonstrated significant inequality (dependent on single 2H/1H replacement in DNA) among three parts of the gene similar in length of the frequency of occurrence of the open states. In this paper, the new convenient approach of the analysis of the abnormal frequency of open states in different parts of the gene encoding interferon alpha 17 was presented, which took into account both rising and decreasing of them that allowed to make a prediction of the functional instability of the specific DNA regions. One advantage of the new algorithm is diminishing the number of both false positive and false negative results in data filtered by this approach compared to the pure fractile methods, such as deciles or quartiles.

Syntheses and crystal structures of new aurate salts of adenine or guanine nucleobases

Two new gold(III) complexes with adenine or guanine nitrogenous bases as counter-cations were synthesized. These are 6-amino-7H-purine-1,9-diium tetrachloridogold(III) chloride monohydrate, (C5H7N5)[AuCl4]Cl·H2O, 1, and 2-amino-6-oxo-6,7-dihydro-1H-purin-9-ium tetrachloridogold(III) hemihydrate, (C5H6N5O)[AuCl4]·0.5H2O, 2. Their crystal structures were studied using single-crystal X-ray diffraction and FT–IR spectroscopic techniques. The arrangement of species in the studied crystal structures implies π-stacking interactions, as well as concomitant C—H...π interactions, hydrogen bonds and other types of noncovalent interactions, which were studied qualitatively and quantitatively using the method of molecular Voronoi–Dirichlet polyhedra. The variation of the nitrogenous base from adenine to guanine results in evident differences in the packing of the species in the crystals of 1 and 2. The splitting and shifting of bands in the FT–IR spectra of the title compounds reveals several features representative of noncovalent interactions in their crystal structures.

PARTICIPATION OF ENT3 TRANSPORTER IN CYTOKININ DISTRIBUTION BETWEEN THE ROOT AND THE SHOOT AND IN REGULATION OF GROWTH RESPONSE OF ARABIDOPSIS PLANTS TO INCREASED LEVEL OF MINERAL NUTRITION

The nitrogenous base riboside transporter ENT3 is known for its ability to transport ribosylated cytokinins across the membrane. However, its role in the distribution of cytokinins between plant organs has not yet been studied. For this purpose, we compared the content and distribution of either endogenous cytokinins or the exogenous trans-zeatin riboside introduced into the nutrient solution in mutant ent3-1 plants and the parent genotype Columbia. In the mutant, the accumulation of endogenous cytokinins in the roots was suppressed, and the ability to deliver exogenous trans-zeatin riboside to shoots increased. The roots of ent3-1 were about 15% longer and had a lower cytokinin concentration. A thirtyfold increase in the concentration of macronutrients led to inhibition of root elongation in the original Columbia line, but not in ent3-1 plants. This growth response occured in accordance with the content of cytokinins in the roots: in Columbia plants, cytokinins accumulated in these organs. The increase in the level of hormones in the roots of ent3-1 was to a lesser extent and was not significant. It was concluded that the ENT3 transporter is involved in the distribution of endogenous cytokinins between the apoplast and symplast, facilitating their uptake by root cells, thereby limiting the export of cytokinins to shoots through the xylem, and can play an important adaptive role in changing the level of mineral nutrition.