Lipase-catalyzed hydrazine insertion for the synthesis of N'-alkyl benzohydrazides.

N'-alkyl benzohydrazides are classic organic compounds that have been widely utilized in organic chemistry. In this study, an efficient method was developed for the synthesis of N'-alkyl benzohydrazides by hydrazine insertion catalyzed by lipase. Under the optimal conditions (Morita-Baylis-Hillman ketone [1 mmol], phenylhydrazine [1.3 mmol], N,N-dimethylformamide [2 ml], lipase [20 mg], room temperature, 12 h), satisfactory yields (71-97%) and substrate tolerance were obtained when porcine pancreatic lipase was used as biocatalyst. These findings imply the great potential for the lipase-catalyzed synthesis of N'-alkyl benzohydrazides and extend the utilization of lipase in organic chemistry.

LncRNA HOTAIR targets miR-126-5p to promote the progression of Parkinson's disease through RAB3IP.

Parkinson's disease (PD) is a common neurological disorder characterized by dopaminergic (DA) neuron degeneration and death in the midbrain, and the long noncoding RNA HOTAIR has been shown to affect disease progression in PD. In this study, we aimed to further illustrate the molecular mechanism of HOTAIR in PD. Bioinformatics analysis was utilized to determine the potential downstream targets of HOTAIR in PD. Luciferase assay and the RNA Binding Protein Immunoprecipitation (RIP) assay were used to validate the existence of binding sites between competing endogenous RNAs (ceRNAs). Real-time quantitative polymerase chain reaction (qRT-PCR) and Western blotting indicated that HOTAIR and RAB3IP increased while miR-126-5p decreased in PD cells and PD mice. Additionally, the CCK-8 assay and flow cytometric analysis indicated that the knockdown of HOTAIR and RAB3IP and the overexpression of miR-126-5p significantly increased cell proliferation and reduced apoptosis in PD cells. Furthermore, the results of in vivo experiments suggested that knockdown of HOTAIR expression increased the number of TH-positive cells and the number of α-synuclein-positive cells decreased while reducing the apoptosis rate among DA neurons. Our study confirmed that HOTAIR promotes PD progression by regulating miR-126-5p and RAB3IP in a ceRNA-dependent manner and further clarified how HOTAIR works in PD.

Radiation-induced FAP + fibroblasts are involved in keloid recurrence after radiotherapy.

Background: Keloid scars (KSs), which are composed of abnormal hyperplastic scar tissue, form during skin wound healing due to excessive fibroblast activation and collagen secretion. Although surgical resection and radiation therapy are used to prevent recurrence, KS recurrence rates range from 15 to 23%, and the underlying mechanism is unclear. Methods: To elucidate the mechanism of keloid recurrence, we established a PDX model and the grafts remained for over 20 weeks after transplantation on the bilateral backs of the NCG mice. Results: RNA-seq revealed that KS tissue gene expression was highly consistent before and after transplantation. Then, one side of the KS graft was irradiated with electron beam therapy (10 Gy), significant increases in vimentin and fibroblast activation protein alpha (FAP) expression were observed after irradiation and were accompanied by severe microvascular destruction. Surprisingly, 4 weeks after irradiation, significantly increased recurrence was observed with increased FAP + tissue and cell cycle regulator expression, resulting in a remarkable altered graft volume. Moreover, irradiation-induced FAP upregulation markedly facilitated radiation resistance and increased cell cycle progression, decreased senescence, and increased energy production. Conclusion: Our findings revealed that irradiation causes increased abundance of FAP + cells, which was associated with cell proliferation and delayed cellular senescence, accompanied by ATP production.

A Purification Method of 18F-FP-(+)-DTBZ via Solid-Phase Extraction With Combined Cartridges.

Background: To optimize [18F] 9-fluoropropyl-(+)-dihydrotetrabenazine (18F-FP-(+)-DTBZ) purification via solid-phase extraction (SPE) with combined cartridges to facilitate its widespread clinical application. Methods: A modified SPE purification method, employing Sep-Pak PS-2 and Sep-Pak C18 cartridges, was used for the preparation of 18F-FP-(+)-DTBZ. This method was compared to the purification method of high-pressure liquid chromatography (HPLC) and SPE with one cartridge, following quality control test and positron emission tomography (PET) imaging in healthy volunteers and patients with parkinsn's disease (PD). Results: A SPE purification method integrating Sep-Pak PS-2 and Sep-Pak C18 cartridges was implemented successfully. The retention time of 18F-FP-(+)-DTBZ purified by HPLC, SPE with Sep-Pak PS-2, SPE with Sep-Pak C18, and SPE with combined use of Sep-Pak PS-2 and Sep-Pak C18 cartridges was 8.7, 8.8, 8.7, and 8.9 min, respectively. Fewest impurity peak was detected in 18F-FP-(+)-DTBZ purified by the SPE with combined use of Sep-Pak PS-2 and Sep-Pak C18 cartridges. This modified SPE purification method provided a satisfactory radiochemical yield of 29 ± 1.8% with radiochemical purity >99% and shortened synthesis time to 27 min. The brain uptake of 18F-FP-(+)-DTBZ purified by the modified SPE was comparable to that purified by HPLC in both healthy volunteers and PD patients. Conclusions: A SPE method integrating Sep-Pak PS-2 and Sep-Pak C18 cartridges for purification of 18F-FP-(+)-DTBZ may be highly suited to automatic synthesis for routine clinical applications, as it provides excellent radiochemical purity, high yield as well as operational simplicity.

Femoral epithelioid hemangioendothelioma detected with magnetic resonance imaging and positron emission tomography/computed tomography: A case report.

BACKGROUND: Epithelioid hemangioendothelioma (EHE) is an uncommon low-grade aggressive vascular tumor. It can occur in almost all locations, but is rarely encountered in bone. CASE SUMMARY: We report a 23-year-old man who presented with left hip pain with no obvious cause. X-ray revealed bone destruction in the left femoral neck with sclerosis at the edges of the lesions. Magnetic resonance imaging (MRI) showed bone destruction in the medullary cavity of the left femoral head and neck. 18F-deoxyglucose-positron emission tomography/computed tomography (PET/CT) imaging showed bone destruction in the left ischium, acetabulum, and left femoral head neck, accompanied by increased radioactive uptake; the maximum standard uptake value was 4.2. Histopathologic examination revealed spindle-shaped mesenchymal tissue hyperplasia with scattered epithelioid cells. The patient underwent left femoral head replacement surgery. No signs of recurrence were observed as of the 18-mo follow-up. CONCLUSION: The definitive diagnosis of femoral EHE can be established aided by the MRI and PET/CT findings.

The DLG1-AS1/miR-497/YAP1 axis regulates papillary thyroid cancer progression.

The long non-coding RNA (lncRNA), DLG1-AS1, is upregulated in papillary thyroid cancer (PTC) tissues and cell lines. Here, we found that increased expression of DLG1-AS1 caused lymph node metastasis and advanced tumor-node-metastasis (TNM) stage. DLG1-AS1 knockdown inhibited proliferation, invasion, and migration of PTC cells, and impaired tumorigenesis in vivo in mouse xenografts. DLG1-AS1 functions as a competing endogenous RNA (ceRNA) for miR-497. Further investigation revealed that DLG1-AS1 regulated yes-associated protein 1 (YAP1; a known target of miR-497) by competitively binding to miR-497. Moreover, inhibition of miR-497 abrogated the inhibitory effects of DLG1-AS1 depletion on PTC cells. These findings demonstrate that the DLG1-AS1-miR-497-YAP1 axis promotes the growth and metastasis of PTC by forming a ceRNA network.

Monascin exhibits neuroprotective effects in rotenone model of Parkinson's disease via antioxidation and anti-neuroinflammation.

Increasing evidence verified that oxidative stress and neuroinflammatory response exacerbates motor deficits and increases neuronal loss in several rodent models of Parkinson's disease. In the present study, we explore the neuroprotective effects of monascin in a rotenone-induced Parkinson's disease model as well as the underlying mechanisms. Our results showed that monascin remarkedly attenuated behavioral impairments and the depletion of dopaminergic neurons induced by rotenone in the rats. Besides, monascin decreased the levels of pro-inflammatory factors such as interleukin-1ß, interleukin-6, tumor necrosis factor-α and oxidative stress marker malondialdehyde while promoted the expression of superoxide dismutase, glutathione peroxidase and other antioxidant factors. Further detection of the expression of related proteins showed that monascin significantly promoted the expression of proliferator-activated receptor-gamma, F-E2-related factor 2 and heme oxygenase-1, but inhibited the expression of NF-κB. What's more, levels of growth factors that are essential for neuronal and synaptic function were increased under the effects of monascin. All in all, our results revealed that monascin exerted neuroprotective effects in rotenone model of Parkinson's disease via antioxidation and anti-neuroinflammation.

Incidental detection of primary hepatocellular carcinoma on 18F-prostate-specific membrane antigen-1007 positron emission tomography/computed tomography imaging in a patient with prostate cancer: A case report.

RATIONALE: Prostate-specific membrane antigen positron emission tomography-computed tomography (F-PSMA-1007 PET/CT) imaging is an emerging method for the diagnosis of prostate cancer (PC), but its efficiency in detecting other accompanying diseases has rarely been investigated. PATIENT CONCERNS: A 77-year-old man presented with a complaint of bone pain throughout his entire body lasting for 2 weeks. Routine preoperative whole-body bone scanning revealed multiple osteogenic metastases. His alpha-fetoprotein and prostate-specific antigen levels were 108.2 ng/mL and 53.32 ng/mL, respectively. F-PSMA-1007 PET/CT imaging revealed high tracer uptake in the primary lesion in the liver and the peripheral zone of the prostate. DIAGNOSES: Due to the results from imaging and pathological examinations, a diagnosis of PC with multiple bone metastases accompanied by primary hepatocellular carcinoma was made. INTERVENTIONS: Taking into consideration the patient's age, interventional therapy was performed for the liver lesion, whereas the prostate and bone lesions were treated with endocrine therapy. OUTCOMES: The patient recovered well and was discharged uneventfully postoperatively. The patient was also doing well at the 6-month follow-up. LESSONS: PSMA-PET/CT imaging results must be interpreted cautiously when the uptake of PSMA increases in a single lesion instead of the most common sites of PC metastasis. Pathological examination of the suspected lesions is also recommended.

The role of dual time point PET/CT for distinguishing malignant from benign focal 18F-FDG uptake duodenal lesions.

The aim of this study was to evaluate the diagnostic criteria of dual time point Fluorine-18 fluorodeoxyglucose (F-FDG) positron emission tomography/computed tomography (PET/CT) in differentiating malignant from benign focal hypermetabolic lesions of duodenum.A total of 50 patients underwent F-FDG PET/CT at 2 points: 60 ±â€Š13.7 minutes (early imaging) and 120 ±â€Š26.4 minutes (delayed imaging) after tracer injection. Early maximum standardized uptake value (SUVE), delayed maximum standardized uptake value (SUVD), difference between early and delayed maximum standardized uptake value (D-SUVmax), and retention index (RI) were calculated for each duodenal lesion. Receiver operating characteristic analysis (ROC) was performed to evaluate the discriminating validity of the parameters.There were 32 malignant and 18 benign focal F-FDG uptake duodenal lesions. The values of SUVE, SUVD, and D-SUVmax were significantly different between malignant and benign lesions (12.5 ±â€Š6.3 vs 5.8 ±â€Š1.2, 13.5 ±â€Š6.5 vs 5.5 ±â€Š1.1 and 0.3 ±â€Š0.8 vs 1.0 ±â€Š1.0, respectively). The areas under the curves (AUCs) of SUVE, SUVD, D-SUVmax were 0.932, 0.964 and 0.707, respectively. There was no significantly difference between SUVE and SUVD based on AUC. In detecting malignant lesions, SUVE=6.9 yielded a sensitivity of 88.9% and specificity of 84.4%, SUVD=7.2 yielded a sensitivity of 94.6% and specificity of 90.6%, D-SUVmax=0.5 yielded a sensitivity of 72.2% and specificity of 68.8%. SUVD was the best diagnostic indicator, regarding specificity and specificity.SUVE and SUVD had good sensitivity, specificity for differentiating duodenal lesions. But there was no significantly difference between diagnostic value of SUVE and SUVD. F-FDG uptake patterns are helpful for differentiating benign and malignant duodenal lesions.