Flometoquin, 2-ethyl-3,7-dimethyl-6-4-(trifluoromethoxy)phenoxyquinolin-4-yl methyl carbonate, is a novel insecticide with a structurally unique phenoxy-quinoline. It was discovered in 2004 by the ...collaborative research of Nippon Kayaku and Meiji Seika Kaisha, Ltd. (currently, Mitsui Chemicals Crop & Life Solutions, Inc.). The compound demonstrates strong and quick insecticidal action against a variety of thrips species at the nymphal and adult stages through contact and feeding activity, which could minimize crop damage and economic loss by insect pest species. In addition, flometoquin is safe for tested non-target arthropods, which makes it suitable for controlling the insect pests mentioned above under Integrated Pest Management (IPM) programs. Here, we describe a structure–activity relationship study from lead generation to the discovery of flometoquin and its insecticidal properties, including knockdown activity and effects against non-targeted arthropods.
The indication for surgical intervention in spontaneous intracerebral hemorrhage remains controversial. Although many clinical trials have failed to demonstrate its efficacy over medical treatment, ...less invasive endoscopic treatment is expected to demonstrate its superiority. A novel endoscopic system for hematoma removal consisting of a 3.1-mm-diameter 4K high-resolution rigid endoscope was used.The system was used in eight cases of spontaneous intracerebral hemorrhage. It provided improved maneuverability of the surgical instrument while maintaining satisfactory image quality. The surgical goal was achieved in all cases without any complications, including perioperative rebleeding.Endoscopic hematoma removal using the 3.1 mm high-resolution endoscope is an alternative minimally invasive approach to spontaneous intracerebral hemorrhage with improved reliability.
Objectives
As mindfulness practices become mainstream, it is increasingly common for participants in mindfulness-based interventions (MBI) to have previous meditation experience. The primary aim of ...this study was to assess whether the impacts of a mindfulness-based stress reduction (MBSR) program on a variety of self-report measures differed for novice meditators (NM) and regular meditators (RM).
Methods
A total of 158 Japanese participants in 10 cohorts completed questionnaires before and after an 8-week community-based MBSR program. The questionnaire consisted of Five Facet Mindfulness Questionnaire (FFMQ), Self-Compassion Scale (SCS), Total Mood Disturbance (TMD) from Profile of Mood States 2, Mental Component Summary (MCS) and Physical Component Summary (PCS) of the 12-Item Short Form Health Survey (2nd version), and Perceived Stress Scale (PSS). Baseline scores and pre-post change scores were compared for RM (participants who had reported meditating ≥ 45 min/week prior to MBSR) and NM (< 45 min/week).
Results
At baseline, RM (38.0% of the sample) had significantly higher scores than NM on FFMQ, SCS, and MCS, and lower scores on TMD and PSS (i.e., less mood disturbance and less stress). Post-program, both groups showed significant improvements in all measures except PCS, with NM’s post-MBSR scores comparable to RM’s baseline scores. A significant Group (NM vs. RM) × Time (pre- vs. post-) interaction was observed only for FFMQ.
Conclusions
Regular meditators, who show greater self-compassion and better mental health than novice meditators at baseline, can benefit from MBSR to a similar extent in measures of self-compassion and other aspects of well-being.
Numerous large-scale clinical studies have revealed that the low-density lipoprotein cholesterol (LDL-C)-lowering effect of 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase inhibitors (statins) ...prevents coronary heart disease (CHD). Statins have not only LDL-C-lowering effects but also high-density lipoprotein cholesterol (HDL-C)-elevating effects, which differ among statins. In this article, we discuss the molecular mechanisms of HDL-C elevation by statins and its effect on HDL functions. We summarize the reports to date on the effects of statins on various proteins, enzymes and receptors involved in reverse cholesterol transport (RCT), which is one of the protective systems against atherosclerosis. Since statins increase the synthesis of apolipoprotein A-I (ApoA-I) and HDL neogenesis in the liver, the HDL-C-increasing effect of statins may reflect RCT activation. Moreover, HDL has pleiotropic effects, including anti-inflammatory and anti-oxidative effects, as well as RCT. In the future, it may be necessary to assess the functions of HDL elevated by statins, and select statins based on differences in their effects in clinical practice.
Objective: Intracranial atherosclerosis disease (ICAD) is one of the most common causes of acute ischemic stroke. In endovascular treatment (EVT) for acute large vessel occlusion stroke-related ICAD, ...reocclusion of the recanalized artery due to in situ thrombosis is problematic. In this study, the safety and efficacy of prasugrel administration to avoid reocclusion of emergent EVT for ICAD was investigated.Methods: All consecutive emergent EVTs for ICAD between September 2019 and December 2022 were included in this study. The procedures were divided into two groups as receiving periprocedural prasugrel (PSG group) or not (non-PSG group). Target vessel patency on follow-up, postprocedural intracranial hemorrhage (ICH), and clinical outcome were compared between PSG and non-PSG groups.Results: A total of 27 procedures were included in this analysis. Nineteen target vessels were patent on follow-up and eight were non-patent. Fifteen patients received prasugrel (18.75 mg: 11 cases, 11.25 mg: 4 cases), and twelve patients did not receive prasugrel. The target vessel patency rate was better in the PSG group vs. non-PSG group (100% vs. 33.3%, respectively; p = 0.0002). The postprocedural ICH rate was not different between the groups (PSG: 40.0% vs. non-PSG: 25.0%; p = 0.68), and all ICHs were asymptomatic. Good clinical outcome (modified Rankin Scale score of 0 to 3 at discharge) was more frequent in the PSG group than that in the non-PSG group (66.7% vs. 16.7%, respectively; p = 0.019).Conclusion: Prasugrel administration was significantly associated with target vessel patency and good clinical outcome after emergent EVT for ICAD without increasing the symptomatic ICH rate. Prasugrel administration might be safe and effective to avoid reocclusion during and after emergent EVT for ICAD.
Sitosterolemia is a rare, autosomal recessive inherited sterol storage disease associated with high tissue and serum plant sterol concentrations, caused by mutations in the adenosine ...triphosphate-bind-ing cassette (ABC) transporter ABCG5 or ABCG8 genes. Markedly increased serum concentration of plant sterols. such as sitosterol and campesterol, cause premature atherosclerosis and massive xanthomas. Hitherto known treatments for sitosterolemia, including a low-sterol diet, bile-salt binding resins, ileal bypass surgery and low density lipoprotein (LDL) apheresis have not yielded sufficient reduction of serum plant sterol levels and many patients show a sustained elevation of plant sterol levels, subsequently developing premature atherosclerotic cardiovascular diseases. Ezetimibe, an inhibitor of intestinal cholesterol absorption through its binding to Niemann-Pick C1-like 1 (NPC1L1), has been widely used for decreasing serum LDL-cholesterol levels in patients with hypercholesterolemia. Ezetimibe also reduces the gastrointestinal absorption of plant sterols, thereby also lowering the serum concentrations of plant sterols. This pharmacological property of ezetimibe shows its potential as a novel effective therapy for sitosterolemia. In the current review, we discuss the current therapy for patients with sitosterolemia and present two Japanese adolescent patients with this disease, one of whom underwent percutaneous coronary intervention for accelerated coronary atherosclerosis. Ezetimibe administration in addition to conventional drug therapy successfully reduced serum sitosterol levels by 51.3% and 48.9%, respectively, in the two patients, demonstrating ezetimibe as a novel and potent treatment agent for sitosterolemia that could work additively with conventional drug therapy.
Eur J Clin Invest 2012; 42 (9): 992–999
Background Postprandial hyperlipidemia partially refers to the postprandial accumulation of chylomicrons and chylomicron remnants (CM‐R). Many in vitro ...studies have shown that CM‐R has highly atherogenic properties, but consensus is lacking on whether CM‐R accumulation correlates with the development of atherosclerotic cardiovascular diseases. We investigated the correlation between CM‐R accumulation and the prevalence of coronary artery disease (CAD).
Design Subjects who received a coronary angiography and did not take any lipid‐lowering drugs (n = 189) were enrolled. Subjects with coronary artery stenosis (≥ 75%) were diagnosed as CAD. Biochemical markers for glucose and lipid metabolism including fasting apolipoprotein (apo) B‐48 concentration were compared between CAD patients (n = 96) and age‐, sex‐, and body mass index (BMI)‐matched non‐CAD subjects without overt coronary stenosis (< 75%) (n = 67). We tried to determine which metabolic parameters were correlated with the prevalence of CAD by multiple logistic regression analysis, and whether or not the combination of high apo B‐48 and other coronary risk factors (high triglyceride, low HDL‐C, high HbA1c or low adiponectin levels) increased the prevalence of CAD.
Results Fasting serum apo B‐48 levels were significantly higher in CAD patients than in non‐CAD subjects (3·9 ± 2·4 vs. 6·9 ± 2·6 μg/mL, P < 0·0001) and had the most significant correlation with the existence of CAD. The clustering of high fasting apo B‐48 levels (> 4·34 μg/mL, the cut‐off value) and other coronary risk factors were found to be associated with a stronger risk of CAD compared with single high fasting apo B‐48 levels.
Conclusion Fasting serum apo B‐48 levels significantly correlated with the prevalence of CAD.
Progranulin (PGRN) is a multifunctional protein known to be involved in inflammation. However, the relation between PGRN and atherosclerosis remains elusive. The aim of this study was to define the ...role of PGRN in the development of atherosclerosis.
First, we checked the expression levels of PGRN in human atherosclerotic plaques. Immunohistochemical analysis showed that PGRN is strongly expressed in foam cells of atherosclerotic plaques. We also found that PGRN is expressed more abundantly in macrophages than in the smooth muscle cells of atherosclerotic lesions in ApoE(-/-) mice fed a high-fat diet for 12 weeks. Next, PGRN(-/-)ApoE(-/-) mice were generated to investigate the effect of PGRN on the development of atherosclerosis. PGRN(-/-)ApoE(-/-) mice exhibited severe atherosclerotic lesions compared with PGRN(+/+)ApoE(-/-) mice, despite their anti-atherogenic lipid profile. These results are partly due to enhanced expression of inflammatory cytokines, adhesion molecules, and decreased expression of endothelial nitric oxide synthase. In addition, lack of PGRN leads to accumulate excessive cholesterol in the macrophages and alter HDL-associated proteins.
PGRN seems to be involved in the pathogenesis of atherosclerosis, possibly by various anti-atherogenic effects, including modulation of local and/or systemic inflammation.