Gold nanoparticles inhibited the receptor activator of nuclear factor-κb ligand (RANKL)-induced osteoclast formation by acting as an antioxidant

Gold nanoparticles inhibited osteoclast (OC) formation induced by the receptor activator of nuclear factor-κB ligand (RANKL) in bone marrow-derived macrophages (BMMs). This was accompanied by a decreased level of tartrate-resistant alkaline phosphatase (TRAP) and less activation of nuclear factor (NF)-κB. The nanoparticles also reduced the production of reactive oxygen species (ROS) in response to RANKL and upregulated RANKL-induced glutathione peroxidase-1 (Gpx-1), suggesting a role as an antioxidant in the BMM. The inhibitory effects on OC formation might have been due to elevated defense against oxidative stress.     

Predicting protein subcellular location: exploiting amino acid based sequence of feature spaces and fusion of diverse classifiers

A novel approach CE-Ploc is proposed for predicting protein subcellular locations by exploiting diversity both in feature and decision spaces. The diversity in a sequence of feature spaces is exploited using hydrophobicity and hydrophilicity of amphiphilic pseudo amino acid composition and a specific learning mechanism. Diversity in learning mechanisms is exploited by fusion of classifiers that are based on different learning mechanisms. Significant improvement in prediction performance is observed using jackknife and independent dataset tests.     

Seasonal changes of functional groups in coleopteran communities in pine forests

Fauna assemblages reflect their habitat relating to ecological function in an ecosystem. The functional groups are concerned with how a resource is processed by different species to provide a specific ecosystem service or function. We elucidated seasonal changes of coleopteran functional groups in forests, and evaluated their ecological roles related to available food resources. Coleopteran communities were collected weekly or biweekly using Malaise traps at nine study sites in Japanese red pine forests in Korea from late June to September 2005. Compositions of the functional groups were compared at the different sites and at sampling times with respect to taxa richness and abundance. Cluster analysis and non-metric multidimensional scaling were used to characterize spatial and temporal changes of functional groups. Herbivores and dead/live wood feeders regulating primary production in the pine forests were the dominant coleopteran groups in July, followed by detritivores and predators that dominated from July to August, resulting from the accumulation of detritus. Then, fungivores became dominant due to increased fungal biomass in the forest. Seasonal changes of coleopteran functional groups shifted from regulators of primary production to regulators of decomposition, reflecting their available food resources. In addition, abundance of detritivores and predators were dependent on total abundance of coleopterans, suggesting that these two groups reflect their habitat condition.     

Novel pyrimidines as acid pump antagonists (APAs)

A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H⁺/K⁺ ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a potent APA with H⁺/K⁺ ATPase, IC₅₀ = 52 nM.     

2,6-Dithienyl-4-furyl pyridines: Synthesis,topoisomerase I and II inhibition,cytotoxicity, structure–activity relationship,and docking study

For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against several human cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong topoisomerase I inhibitory activity. In addition, a docking study with topoisomerase I and compound 24 was performed.     

A newly synthesized,potent tyrosinase inhibitor: 5-(6-Hydroxy-2-naphthyl)-1,2,3-benzenetriol

In searching for new agents with a depigmenting effect, we synthesized a derivative of resveratrol, 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol (5HNB) with a potent tyrosinase inhibitory activity. 5HNB inhibited mushroom tyrosinase with an IC₅₀ value of 2.95 μM, which is more potent than the well-known anti-tyrosinase activity of kojic acid (IC₅₀ = 38.24). The results of the enzymatic inhibition kinetics by Lineweaver–Burk analysis indicated 5HNB inhibits tyrosinase non-competitively when l-tyrosine was used as the substrate. Based on the strong inhibitory action of 5HNB, it is expected that 5HNB can suppress melanin production in which tyrosinase plays the essential role. Our expectation was confirmed by the experimentations with B16 melanoma cells in which 5HNB inhibited melanin production. We propose that 5HNB might have skin-whitening effects as well as therapeutic potential for treating skin pigmentation disorders.     

Synthesis and antiproliferative activity of pyrrolo[3,2-b]pyridine derivatives against melanoma

Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij–k and Iv–w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375.     

Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: A novel series of atypical antipsychotic agents

(Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT_2C and 5-HT₆ receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin-1-yl)-phenyl]-amide (6b) exhibits the highest affinity towards both 5-HT_2C (IC₅₀ = 4 nM) and 5-HT₆ receptors (IC₅₀ = 3 nM) with good selectivity over other serotonin (5-HT_1A, 5-HT_2A, and 5-HT₇) and dopamine (D₂–D₄) receptor subtypes. In 5-HT_2C and 5-HT₆ receptor functional assays, this compound showed considerable antagonistic activity for both receptors.