Bis(2-amino­benzothia­zole-κN 1)bis­(thio­cyanato-κN)zinc(II)

The ZnII ion in the title complex, [Zn(NCS)2(C7H6N2S)2], is tetra­hedrally coordinated within an N4 donor set defined by two N atoms of two terminal isothio­cyanate ligands and by two heterocyclic N atoms of two different 2-amino­benzothia­zole ligands. This arrangement is stabilized by intra­molecular N—H⋯N hydrogen bonds. In the crystal structure, mol­ecules are linked through N—H⋯S hydrogen bonds to form a two-dimensional array

Protein Fractions from Korean Mistletoe ( Viscum Album coloratum

Mistletoe (Viscum Album coloratum) has been known as a medicinal plant in European and Asian countries. Recent data show that biological activity of mistletoe alleviates hypertension, heart disease, renal failure, and cancer development. In this study, we report the antidiabetic effect of Korean mistletoe extract (KME). KME treatments enhanced the insulin secretion from the pancreatic β-cell without any effects of cytotoxicity. PDX-1 and beta2/neuroD known as transcription factors that regulate the expression of insulin gene were upregulated by treatment of the KME protein fractions isolated by ion-exchange chromatography after ammonium sulfate precipitation. Furthermore, these KME protein fractions significantly lowered the blood glucose level and the volume of drinking water in alloxan induced hyperglycemic mice. Taken together with the findings, it provides new insight that KME might be served as a useful source for the development of medicinal reagent to reduce blood glucose level of type I diabetic patients

Bis(2-amino-1,3-thia­zole-κN 3)diazido­zinc

In the title complex, [Zn(N3)2(C3H4N2S)2], the ZnII atom is tetra­hedrally coordinated by two terminal azide ligands and by the ring N atoms of two different 2-amino­thia­zole ligands. Intra­molecular N—H⋯N hydrogen bonds between the amino groups of both 2-amino­thia­zole ligands and the N atom of one of the azide ligands ensure that the heterocyclic rings are oriented in the same direction. Inter­molecular N—H⋯N hydrogen bonds link the mol­ecules into zigzag sheets in the ac plane

Protective effects of isoflavones on alcoholic liver diseases: Computational approaches to investigate the inhibition of ALDH2 with isoflavone analogues

Excessive and chronic alcohol intake can lead to the progression of alcoholic liver disease (ALD), which is a major cause of morbidity and mortality worldwide. ALD encompasses a pathophysiological spectrum such as simple steatosis, alcoholic steatohepatitis (ASH), fibrosis, alcoholic cirrhosis, and hepatocellular carcinoma (HCC). Aldehyde dehydrogenase (ALDH2) is the most vital enzyme that produces acetate from acetaldehyde and is expressed at high levels in the liver, kidneys, muscles, and heart. The ALDH2*2 allele is found in up to 40% of East Asian populations, and has a significant impact on alcohol metabolism. Interestingly, several studies have shown that individuals with ALDH2 deficiency are more susceptible to liver inflammation after drinking alcohol. Furthermore, there is growing evidence of an association between ALDH2 deficiency and the development of cancers in the liver, stomach, colon, and lung. Isoflavone analogues are low molecular-weight compounds derived from plants, similar in structure and activity to estrogen in mammals, known as phytoestrogens. Recent studies have reported that isoflavone analogues have beneficial effects on the progression of ALD. This mini-review summarizes the current knowledge about the roles of isoflavone analogues in ALD and discusses the therapeutic potential of isoflavone analogues in liver pathophysiology. In particular, we highlight the significance of computational approaches in this field

Sp1 up-regulates cAMP-response-element-binding protein expression during retinoic acid-induced mucous differentiation of normal human bronchial epithelial cells.

CREB [CRE (cAMP-response element)-binding protein] is an important transcription factor that is differentially regulated in cells of various types. We recently reported that RA (retinoic acid) rapidly activates CREB without using RARs (RA receptors) or RXRs (retinoid X receptors) in NHTBE cells (normal human tracheobronchial epithelial cells). However, little is known about the role of RA in the physiological regulation of CREB expression in the early mucous differentiation of NHTBE cells. In the present study, we report that RA up-regulates CREB gene expression and that, using 5\u27-serial deletion promoter analysis and mutagenesis analyses, two Sp1 (specificity protein 1)-binding sites located at nt -217 and -150, which flank the transcription initiation site, are essential for RA induction of CREB gene transcription. Furthermore, we found that CREs located at nt -119 and -98 contributed to basal promoter activity. Interestingly, RA also up-regulated Sp1 in a time- and dose-dependent manner. Knockdown of endogenous Sp1 using siRNA (small interfering RNA) decreased RA-induced CREB gene expression. However, the converse was not true: knockdown of CREB using CREB siRNA did not affect RA-induced Sp1 gene expression. We conclude that RA up-regulates CREB gene expression during the early stage of NHTBE cell differentiation and that RA-inducible Sp1 plays a major role in up-regulating human CREB gene expression. This result implies that co-operation of these two transcription factors plays a crucial role in mediating early events of normal mucous cell differentiation of bronchial epithelial cells

Amphiphilic [pi]-allyliridium catalyzed nucleophilic and electrophilic allylation

Transition metal-catalyzed allylic substitution has emerged as a powerful method for stereoselective C-N bond formation. Chiral iridium-phosphoramidite complexes have proven especially effective as catalysts for regio- and enantioselective allylic amination, but are limited to aryl-substituted π-allyl electrophiles. With commercially available π-allyliridium C,O-benzoates, which are stable to air, water and SiO₂ chromatography, and are well known to catalyze allylic acetate mediated carbonyl allylation, highly regio- and enantioselective electrophilic allylation of aliphatic amines, primary and secondary aromatic or heteroaromatic amines were demonstrated. Furthermore, indoles and related azoles can also undergo the amination and generate enantiomerically enriched N-allyl indoles with completely N-selective and exclusive branched regioselectivity, which are an unmet challenge in this field. Moreover, indoles and related azoles are prevalent structural motifs in clinical candidates and FDA approved drugs, so these results also show the utility and importance of asymmetric allylic alkylation.Chemistr