142 research outputs found
Total Synthesis of Zephycarinatines via Photocatalytic Reductive Radical ipso‐Cyclization
We report herein a nonbiomimetic strategy for the total synthesis of the plicamine‐type alkaloids zephycarinatines C and D. The key feature of the synthesis is a stereoselective reductive radical ipso‐cyclization using visible‐light‐mediated photoredox catalysis. This cyclization enabled the construction of a 6, 6‐spirocyclic core structure through the addition of a carbon‐centered radical onto the aromatic ring. Biological evaluation of zephycarinatines and their derivatives revealed that the synthetic derivative with a keto group displays moderate inhibitory activity against LPS‐induced NO production. This approach could offer future opportunities to expand the chemical diversity of plicamine‐type alkaloids as well as providing useful intermediates for their syntheses
Effects of phosphodiesterase inhibitors on secretions of human monokines
ABSTRACTThe purpose of this study was to evaluate the effect of newly developed selective phosphodiesterase (PDE) inhibitors, KF19514 (type l/IV) and cilostazol (type III), and theophylline on the secretions of tumor necrosis factor a (TNFα) and interleukin-1β (IL-1 β) from human peripheral monocytes stimulated by lipopolysaccha- ride (LPS). Human blood monocytes were incubated with LPS in the absence or presence of KF19514, cilostazol or theophylline. TNFα and IL-1in the cell- free supernatants were measured with enzyme-linked immunosorbent assay. KF19514 showed significant inhibition on the release of TNFα (% inhibition ± SEM was 82.8 ± 7.4% at 1 nmol/L) and IL-1 β (34.4 ± 7.5% at 10 (μmol/L). In addition, KF19514 inhibited the expression of TNFa mRNA. Cilostazol inhibited the release of TNFa significantly (60.2 ± 8.9% at 30 μmol/L) but not IL-1 β. Theophylline inhibited slightly but significantly the release of TNFa at a therapeutic concentration (1 7.4 ± 5.1% at 100 μmol/L). These results suggest that theophylline may not only have a bronchodilating action but also an anti-inflammatory property in the treatment of bronchial asthma, and that KF19514 may have an anti-inflammatory action on at least the transcriptional level
StreamDiffusion: A Pipeline-level Solution for Real-time Interactive Generation
We introduce StreamDiffusion, a real-time diffusion pipeline designed for
interactive image generation. Existing diffusion models are adept at creating
images from text or image prompts, yet they often fall short in real-time
interaction. This limitation becomes particularly evident in scenarios
involving continuous input, such as Metaverse, live video streaming, and
broadcasting, where high throughput is imperative. To address this, we present
a novel approach that transforms the original sequential denoising into the
batching denoising process. Stream Batch eliminates the conventional
wait-and-interact approach and enables fluid and high throughput streams. To
handle the frequency disparity between data input and model throughput, we
design a novel input-output queue for parallelizing the streaming process.
Moreover, the existing diffusion pipeline uses classifier-free guidance(CFG),
which requires additional U-Net computation. To mitigate the redundant
computations, we propose a novel residual classifier-free guidance (RCFG)
algorithm that reduces the number of negative conditional denoising steps to
only one or even zero. Besides, we introduce a stochastic similarity
filter(SSF) to optimize power consumption. Our Stream Batch achieves around
1.5x speedup compared to the sequential denoising method at different denoising
levels. The proposed RCFG leads to speeds up to 2.05x higher than the
conventional CFG. Combining the proposed strategies and existing mature
acceleration tools makes the image-to-image generation achieve up-to 91.07fps
on one RTX4090, improving the throughputs of AutoPipline developed by Diffusers
over 59.56x. Furthermore, our proposed StreamDiffusion also significantly
reduces the energy consumption by 2.39x on one RTX3060 and 1.99x on one
RTX4090, respectively.Comment: tech report, the code is available at
https://github.com/cumulo-autumn/StreamDiffusio
Evaluation of the Imaging Process for a Novel Subtraction Method Using Apparent Diffusion Coefficient Values
Diffusion-weighted imaging may be used to obtain the apparent diffusion coefficient (ADC), which aids the diagnosis of cerebral infarction and tumors. An ADC reflects elements of free diffusion. Diffusion kurtosis imaging (DKI) has attracted attention as a restricted diffusion imaging technique. The ADC subtraction method (ASM) was developed to visualize restricted diffusion with high resolution by using two ADC maps taken with different diffusion times. We conducted the present study to provide a bridge between the reported basic ASM research and clinical research. We developed new imaging software for clinical use and evaluated its performance herein. This software performs the imaging process automatically and continuously at the pixel level, using ImageJ software. The new software uses a macro or a plugin which is compatible with various operating systems via a Java Virtual Machine. We tested the new imaging software’s performance by using a Jurkat cell bio-phantom, and the statistical evaluation of the performance clarified that the ASM values of 99.98% of the pixels in the bio-phantom and physiological saline were calculated accurately (p<0.001). The new software may serve as a useful tool for future clinical applications and restricted diffusion imaging research
Beyond 5G Fronthaul based on FSO Using Spread Spectrum Codes and Graphene Modulators.
High data rate coverage, security, and energy efficiency will play a key role in the continued performance scaling of next-generation mobile systems. Dense, small mobile cells based on a novel network architecture are part of the answer. Motivated by the recent mounting interest in free-space optical (FSO) technologies, this paper addresses a novel mobile fronthaul network architecture based on FSO, spread spectrum codes, and graphene modulators for the creation of dense small cells. The network uses an energy-efficient graphene modulator to send data bits to be coded with spread codes for achieving higher security before their transmission to remote units via high-speed FSO transmitters. Analytical results show the new fronthaul mobile network can accommodate up to 32 remote antennas under error-free transmissions with forward error correction. Furthermore, the modulator is optimized to provide maximum efficiency in terms of energy consumption per bit. The optimization procedure is carried out by optimizing both the amount of graphene used on the ring resonator and the modulator’s design. The optimized graphene modulator is used in the new fronthaul network and requires as low as 4.6 fJ/bit while enabling high-speed performance up to 42.6 GHz and remarkably using one-quarter of graphene only
Evaluation of Fast Diffusion Kurtosis Imaging Using New Software Designed for Widespread Clinical Use
Clinical research using restricted diffusion-weighted imaging, especially diffusion kurtosis (DK) imaging, has been progressing, with reports on its effectiveness in the diagnostic imaging of cerebral infarctions, neurodegenerative diseases, and tumors, among others. However, the application of DK imaging in daily clinical practice has not spread because of the long imaging time required and the use of specific software for image creation. Herein, with the aim of promoting clinical research using DK imaging at any medical facility, we evaluated fast DK imaging using a new software program. We developed a new macro program that produces DK images using general-purpose, inexpensive software (Microsoft Excel and ImageJ), and we evaluated fast DK imaging using bio-phantoms and a healthy volunteer in clinical trials. The DK images created by the new software with diffusion-weighted images captured with short-time imaging sequences were similar to the original DK images captured with long-time imaging sequences. The DK images using three b-values, which can reduce the imaging time by 43%, were equivalent to the DK images using five b-values. The DK imaging technique developed herein might allow any medical facility to increase its daily clinical use of DK imaging and easily conduct clinical research
Long-term Survival of a Case of Rectal Neuroendocrine Carcinoma with Liver Metastasis
Colorectal neuroendocrine carcinoma(NEC)is extremely rare and has a dismal prognosis. However, no standardized treatment strategy has been established for this lesion. For patients with NEC and distant metastasis, disease stabilization is difficult even after treatment with multidisciplinary strategies including chemotherapy. Here we describe a case of rectal NEC that presented as multiple liver metastases; a favorable prognosis was obtained after treatment with a multidisciplinary strategy that included surgery, irradiation, and chemotherapy. A 66-year-old male presented with diarrhea and constipation. Colonoscopy and a computed tomography(CT)scan revealed a rectal mass involving all of the luminal circumference, after which a diagnosis of NEC was confirmed by pathological examination. A CT scan also revealed several liver metastases in S5, S6, and S8. Abdominoperineal resection with total mesenteric excision and lymphadenectomy, including the lateral area, was performed. After resection, we administered radiation for local disease control in the lateral area. We also administered chemotherapy consisting of cisplatin and irinotecan for the liver metastases because only the endocrine cell component constituted this tumor. After chemotherapy, a CT scan was performed to confirm that the liver metastasis in S5 and S6 had disappeared, and it was shown that the other lesion in S8 had shrunk substantially(it eventually disappeared). Then, 48 months after resection, all metastatic liver tumors were under good control, and no other recurrent lesion was recognized. In conclusion, a multidisciplinary strategy including optimal chemotherapy seems to be important to achieve a favorable prognosis of NEC of the colorectum with distant metastasis
Unified Total Synthesis, Stereostructural Elucidation, and Biological Evaluation of Sarcophytonolides
Sarcophytonolides are cembranolide diterpenes isolated from the soft corals of genus Sarcophyton. Unified total synthesis of sarcophytonolides C, E, F, G, H, and J and isosarcophytonolide D was achieved. The synthetic routes feature NaHMDS- or SmI2-mediated fragment coupling, alkoxycarbonylallylation, macrolactonization, and transannular ring-closing metathesis. These total syntheses led to the absolute configurational confirmation of sarcophytonolide H, elucidation of sarcophytonolides C, E, F, and G, and revision of sarcophytonolide J and isosarcophytonolide D. We also evaluated the antifouling activity and toxicity of the synthetic sarcophytonolides H and J and their analogues as well as the cytotoxicity of the synthetic sarcophytonolides and the key synthetic intermediates
- …