ABSTRACT
A new polyenyl-α-pyrone polyketide, aspopyrone A (1), was isolated from a culture broth of Okinawan plant-associated Aspergillus sp. TMPU1623 by solvent extraction, ODS column chromatography, and preparative HPLC (ODS). The structure of 1 was assigned based on NMR experiments. Compound 1 exhibited protein tyrosine phosphatase (PTP) 1B and T-cell PTP (TCPTP) inhibitory activities with IC50 values of 6.7 and 6.0 µM, respectively.
Subject(s)
Polyketides/pharmacology , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Pyrones/antagonists & inhibitors , Aspergillus/metabolismSubject(s)
Aspergillus/metabolism , Enzyme Inhibitors/isolation & purification , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Xanthones/isolation & purification , Dimerization , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Fresh Water , Japan , Xanthones/chemistry , Xanthones/pharmacologyABSTRACT
We developed a new technique to quantitatively analyze visual evaluation single photon emission computed tomography (SPECT). Short axis tomograms and color scales were computer scanned. The scales were divided into 25 parts; numbers of each hue pixel were scored 0-100%. Short-axis images were divided into eight equal partitions, numbers of hue pixels distributed in each partition were scored, and total scores were obtained. Each partition's radio-isotope (RI) accumulation index was calculated as partition score/highest score. For method validation, scintigrams from each left ventricular phantom part were divided into eight partitions and filled with (123)I-BMPP (10-100%). The error between theoretical and calculated concentrations was within 20% in the concentration range of ≥50%, suggesting a good correlation and indicating the method's validity.
