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Four compounds, including two novel macrolides, were isolated from an endophyte Streptomyces sp. Is9131 of Maytenus hookeri. Spectral data indicated that these compounds were dimeric dinactin (1), dimeric nonactin (2), cyclo-homononactic acid (3), and cyclo-nonactic acid (4). Bioassay results...
KR-33028 ( N -(4-cyano-benzo(b)thiophene-2-carbonyl)guanidine) is a new cardioprotective agent for preventing ischemia-reperfusion injury. This study was performed to identify the metabolic pathway of KR-33028 in human liver microsomes and to compare its metabolism with that of cryopreserved...
2-Thiouracil-5-sulphonic acid N -(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the...
The vascular endothelial growth factor (VEGF) plays a key role in angiogenesis, which is a process where new blood vessels develop from the endothelium of a pre-existing vasculature. VEGF exerts its activity by binding to its receptor tyrosine kinase, KDR/Flk-1, which is expressed on the surface...
Recently, it was reported that reduction in serum adiponectin levels is correlated with the incidence of breast cancer. As an effort to explain this, we screened various human breast cancer cell lines to identify those in which proliferation is directly controlled by adiponectin. Among the five...
The G q/11 protein-coupled receptors, such as muscarinic (M1 & M3) receptors, have been shown to regulate the release of a soluble amyloid precursor protein (sAPPα) produced from α-secretase processing. However, there is no direct evidence for the precise characteristics of G proteins, and the...
N,N -Dialkylditihiocarbamate derivatives have been well known as broad-range fungicides. In this study, the triazole derivatives of ten new N,N - disubstituted dithiocarbamates ( 3a-j ) were synthesized and their structures were identified by spectral and elemental analysis. Results of the...
A new phenolic glycoside, ophiopojaponin D ( 1 ), together with two known compounds, was isolated from the tubers of a famous traditional Chinese herb -Ophiopogon japonicus Ker-Gawl. The spectroscopic and chemical data revealed their structures to be...
The in vivo immunomodulatory function of the activity of murine natural killer (NK) cells induced by high mannuronic acid-containing alginate (HMA) was examined. HMA was injected i.p at doses of 25 and 100 mg/kg. The NK activity was 3 times higher with 100 mg/kg HMA than the baseline. In...
6-(2-(Benzoxazol-2-ylmethylamino)ethoxy)-1-alkyl-1H-indole-2-carboxylic acids were designed and synthesized as β-amyloid (Aβ) fibril assembly inhibitors. Their inhibitory activity on Aβ, aggregation was evaluated by thioflavin T assay although their activities were insignificant.
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