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α-Silylalkylamines and α-borylalkylamines are versatile synthetic intermediates and attractive scaffolds found in pharmaceutical drugs and agrochemicals. Despite great progress on synthetic methods for preparation of α-silylalkylamines or α-borylalkylamines, there are no general strategies for preparation of α-boryl-α-silylalkylamines and the reactivity has not been explored. Here we report deoxygenative geminal silylboration of amides using silylboronates in the presence of alkoxide base catalyst, producing α-boryl-α-silylalkylamines. The silicon and boron groups in α-boryl-α-silylalkylamines are found to be utilized to chemoselective transformations, such as protonation and alkylation. This protocol serves various α-silylalkylamines and α-borylalkylamines from readily available amides.
RESUMO
[Purpose] The objective of this study was to provide cerebral stroke patients with virtual reality videos of gait occurring at a faster speed than their actual measured gait speed and ascertain the effect on generating errors of gait. [Participants and Methods] The participants were 12 stroke patients. They were given a 2-minute virtual reality presentation of gait occurring at a speed faster than their actual measured comfortable walking speed. Immediately following the presentation, their 10-m walking speed was measured again to observe the immediate effect of the intervention, after which the time required to walk at maximum gait speed was measured. Stride length, cadence, and walking speed before and after the intervention were compared. In addition, heard an immersive feeling. [Results] At a comfortable walking speed, the cadence improved significantly post-intervention. Walking speed and stride length also tended to increase. At the maximum walking speed, there were no significant differences in any parameter. There was no problem with the immersive feeling. [Conclusion] After watching virtual reality videos of gait at a speed faster than the patients' actual gait speed, their walking speed tended to increase in comfortable walking. It was speculated that this technique could be applied to walking training, depending on the device.
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Crithidia mellificae (C. mellificae) and Lotmaria passim (L. passim) are trypanosomatids that infect Apis mellifera. We analyzed the prevalence of C. mellificae and L. passim in six regions of Japan from 2018 to 2019. The detection rate of C. mellificae was 0.0% in all regions, whereas L. passim was detected in 16.7%-66.7% of the honeybees. L. passim was detected at a significantly lower rate in the Cyugoku-Shikoku region than in other regions. Furthermore, phylogenetic analysis of the internal transcribed spacer 1 (ITS1) locus of related species was performed. All the samples in this study could be assigned to the L. passim clade. This study reveals that L. passim infection is predominantly prevalent in Japan. Further epidemiological surveys are needed to clarify the prevalence of C. mellificae infection in honeybees in Japan.
Assuntos
Trypanosomatina , Abelhas , Animais , Japão/epidemiologia , Filogenia , CrithidiaRESUMO
Cancer chemotherapy targeted to angiogenic vessels is expected to cause indirect tumor regression through the damage of the neovasculature without the induction of drug resistance. To develop a tool for neovasculature-specific drug delivery, we isolated novel peptides homing to angiogenic vessels formed by a dorsal air sac method from a phage-displayed peptide library. Three distinct phage clones that markedly accumulated in murine tumor xenografts presented PRPGAPLAGSWPGTS-, DRWRPALPVVLFPLH- or ASSSYPLIHWRPWAR-peptide respectively. After the determination of the epitope sequences of these peptides, we modified liposomes with epitope penta-peptides. Liposome modified with APRPG-peptide showed high accumulation in murine tumor xenografts, and APRPG-modified liposome encapsulating adriamycin effectively suppressed experimental tumor growth. Finally, specific binding of APRPG-modified liposome to human umbilical endothelial cells, and that of PRP-containing peptide to angiogenic vessels in human tumors, i.e., islet cell tumor and glioblastoma, were demonstrated. The present study indicates the usefulness of APRPG-peptide as a tool for anti-neovascular therapy, a novel modality of cancer treatment.
Assuntos
Inibidores da Angiogênese/uso terapêutico , Melanoma Experimental/irrigação sanguínea , Neovascularização Patológica/tratamento farmacológico , Peptídeos/uso terapêutico , Sarcoma Experimental/irrigação sanguínea , Sequência de Aminoácidos , Animais , Antibióticos Antineoplásicos/farmacologia , Divisão Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Doxorrubicina/farmacologia , Endotélio Vascular/efeitos dos fármacos , Humanos , Injeções Subcutâneas , Lipossomos/metabolismo , Linfocinas/farmacologia , Masculino , Melanoma Experimental/patologia , Camundongos , Camundongos Endogâmicos BALB C , Microscopia Confocal , Dados de Sequência Molecular , Neovascularização Patológica/patologia , Biblioteca de Peptídeos , Sarcoma Experimental/patologia , Tomografia Computadorizada de EmissãoRESUMO
This report describes a rare case of an arterial anomaly in the celiaco-mesenteric region, encountered in a Japanese female cadaver for dissection at the gross anatomy laboratory of Kurume University School of Medicine in 2003. The usual celiac trunk was not identified, and the left gastric artery, the splenic artery and the hepato-mesenteric trunk independently arose from the abdominal aorta. Moreover, the hepatic artery arising from the hepato-mesenteric trunk ran behind the portal vein. The classification for this type of arterial anomaly is a Type II' of Morita's classification and Type II of Higashi and Hirai's classification, not belong to the Adachi's.
Assuntos
Aorta Abdominal/anormalidades , Artéria Hepática/anormalidades , Artéria Esplênica/anormalidades , Estômago/irrigação sanguínea , Idoso , Feminino , HumanosRESUMO
We previously reported that liposomalized 5'-O-dipalmitoylphosphatidyl 2'-C-cyano-2'-deoxy-1-beta-D-arabino-pentofuranosylcytosine (DPP-CNDAC), a hydrophobized derivative of the novel antitumor nucleoside CNDAC, is quite useful for cancer therapy. On the other hand, for anti-neovascular therapy, we recently isolated peptides homing to angiogenic vessels from a phage-displayed random peptide library, and observed that peptide-modified liposomal adriamycin strongly suppressed tumor growth, perhaps through damaging angiogenic endothelial cells. In the present study, we modified DPP-CNDAC-liposomes with one of the angiogenic homing peptides, APRPG, and examined their antitumor activity. Three doses of APRPG-modified DPP-CNDAC-liposomes (15 mg/kg as CNDAC) strongly inhibited tumor growth compared with the same number of doses of unmodified DPP-CNDAC-liposomes. The life span was increased 31.8%, with one completely cured mouse out of the six mice treated. Since the accumulation of liposomes in the tumor tissue was not so much different between APRPG-liposomes and non-modified liposomes, the enhanced therapeutic efficacy may be explained as the alteration of targets, i.e. APRPG-modified DPP-CNDAC-liposomes caused tumor growth suppression through damage of angiogenic endothelial cells. Anti-neovascular therapy promises no drug resistance, and should be effective against essentially any kind of solid tumor; and thus the present results demonstrate another benefit of the therapy, namely, high efficacy of cancer treatment.