Four new prenylated phloroglucinol derivatives (+)-erectumol I (1a), (−)-erectumol I (1b), (−)-erectumol II (2a), and (+)-erectumol II (2b) were isolated from the methanol extracts of the whole ...plants of Hypericum erectum. These new compounds were isolated as a pair of enantiomers, respectively. The planar chemical structures and relative configurations of the new compounds were suggested by Cu-Kα X-ray diffraction analysis and been confirmed by high-resolution mass and 1D and 2D NMR spectroscopic data. The absolute configuration of the four new compounds were established by comparing the experimental and predicted electronic circular dichroism data. Isolated compounds 1b and 2b induced death of Adriamycin-treated HeLa cells. Their enantiomers 1a and 2a did not. In addition, the apparent mechanism of cell death of 1b was the inhibited expression of heat shock protein 105.
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A 67-year-old woman with obstructive rectal cancer underwent laparoscopic low anterior resection 2 years prior and total hysterectomy and bilateral adnexectomy for uterine cancer at another hospital ...20 years earlier, which led to the diagnosis of Lynch syndrome. During the postoperative follow-up, chronic anemia was noted. Upper and lower gastrointestinal endoscopy and contrast-enhanced abdominal computed tomography were performed to evaluate the etiology of the anemia; however, the findings were unremarkable. Small bowel endoscopy was performed and a full circumferential type 2 lesion was found in the jejunum. Biopsy confirmed a moderately differentiated adenocarcinoma. Thus, laparoscopic partial resection of the small bowel was performed, and the patient was discharged on the 11th hospital day with an uneventful postoperative course. Although a preoperative diagnosis of small bowel cancer is difficult to establish, this was considered due to Lynch syndrome, and the preoperative diagnosis was confirmed via small bowel endoscopy.
While rapid advancements in regenerative medicine strategies for spinal cord injury (SCI) have been made, most research in this field has focused on the early stages of incomplete injury. However, ...the majority of patients experience chronic severe injury; therefore, treatments for these situations are fundamentally important. Here, we hypothesized that environmental modulation via a clinically relevant hepatocyte growth factor (HGF)-releasing scaffold and human iPS cell-derived neural stem/progenitor cells (hNS/PCs) transplantation contributes to functional recovery after chronic complete transection SCI. Effective release of HGF from a collagen scaffold induced progressive axonal elongation and increased grafted cell viability by activating microglia/macrophages and meningeal cells, inhibiting inflammation, reducing scar formation, and enhancing vascularization. Furthermore, hNS/PCs transplantation enhanced endogenous neuronal regrowth, the extension of graft axons, and the formation of circuits around the lesion and lumbar enlargement between host and graft neurons, resulting in the restoration of locomotor and urinary function. This study presents an effective therapeutic strategy for severe chronic SCI and provides evidence for the feasibility of regenerative medicine strategies using clinically relevant materials.
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Linderapyrone, a Wnt signal inhibitor was isolated from the methanolic extract of the stems and twigs of Lindera umbellata together with epi-(-)-linderol A. Linderapyrone inhibited ...TCF/β-catenin transcriptional activity that was evaluated using cell-based TOPFlash luciferase assay system. To evaluate the structure-activity relationship and mechanism, we synthesized linderapyrone and its derivatives from piperitone. As the results of further bioassay for synthesized compounds, we found both of pyrone and monoterpene moieties were necessary for inhibitory effect. cDNA microarray analysis in a linderapyrone derivative treated human colorectal cancer cells showed that this compound downregulates Wnt signaling pathway. Moreover, we successes to synthesize the derivative of linderapyrone that has stronger inhibitory effect than linderapyrone and ICG-001 (positive control).
A versatile reducing agent, diimide, can be generated efficiently by the aerobic oxidation of hydrazine with neutral and cationic synthetic flavin catalysts 1 and 2. This technique provides a ...convenient and safe method for the aerobic reduction of olefins, which proceeds with 1 equiv of hydrazine under an atmosphere of O2 or air. The synthetic advantage over the conventional gas‐based method has been illustrated through high hydrazine efficiency, easy and safe handling, and characteristic chemoselectivity. Vitamin B2 derivative 6 acts as a highly practical, robust catalyst for this purpose because of its high availability and recyclability. Association complexes of 1 b with dendritic 2,5‐bis(acylamino)pyridine 15 exhibit unprecedented catalytic activities, with the reduction of aromatic and hydroxy olefins proceeding significantly faster when a higher‐generation dendrimer is used as a host pair for the association catalysts. Contrasting retardation is observed upon similar treatment of non‐aromatic or non‐hydroxy olefins with the dendrimer catalysts. Control experiments and kinetic studies revealed that these catalytic reactions include two independent, anaerobic and aerobic, processes for the generation of diimide from hydrazine. Positive and negative dendrimer effects on the catalytic reactions have been ascribed to the specific inclusion of hydrazine and olefinic substrates into the enzyme‐like reaction cavities of the association complex catalysts.
The versatile reducing agent diimide can be generated efficiently by the aerobic oxidation of hydrazine with a variety of flavin catalysts, such as cationic and neutral flavins and flavin–dendrimer association complexes. This technique provides a convenient and safe method for the aerobic reduction of olefins, which proceeds with one equivalent of hydrazine under an atmosphere of O2 or air (see scheme).
