Pharmacological activity and structural analysis of a benzamide (TKS159) and its optical isomers in an in vitro study and in an in vivo study in mice

Author(s):  
J.I. Mizoguchi ◽  
T. Yanagi ◽  
K. Anzai ◽  
K. Kodama ◽  
O. Kamoda ◽  
...  
2020 ◽  
Vol 4 (Supplement_2) ◽  
pp. 449-449
Author(s):  
Patricia Perez ◽  
Desiree Wanders ◽  
Hannah Land ◽  
Kathryn Chiang ◽  
Rami Najjar ◽  
...  

Abstract Objectives Studies suggest that inflammation mediates the link between obesity and its comorbidities including type 2 diabetes and cardiovascular disease. Hence, there is a demand for effective alternative or complementary approaches to treat obesity-associated inflammation. The objective of this study was to determine whether consumption of blackberries (BL) and raspberries (RB) alone or in combination reduce obesity-induced inflammation. Methods In Vitro Study: RAW 264.7 macrophages were pretreated with either BL, RB, or BL + RB, each at a final concentration of 200 µg/mL for 2 h. LPS (1 ng/mL) was then added to the media for 16 h. mRNA expression of inflammatory cytokines was measured. In Vivo Study: Five-week-old mice were acclimated to a low-fat low-sucrose (LFLS) diet for one week after which mice were randomized 10 per group to one of five groups: 1) LFLS, 2) high-fat high-sucrose (HFHS), 3) HFHS + 10% BL, 4) HFHS + 10% RB, or 5) HFHS + 5% BL + 5% RB. Expression of inflammatory markers was measured in the liver as well as epididymal and inguinal white adipose tissue. Results In Vitro Study: Each berry alone and in combination suppressed the LPS-induced increase in inflammatory markers, with the combination (BL + RB) having the greatest effect. The combination suppressed LPS-induced expression of Ccl2, Tnfa, F4/80, and Il6 by 3.7−, 5.3−, 5.3−, and 4.4-fold, respectively. In Vivo Study: Gene expression analysis indicated that berry consumption had no significant effect on proinflammatory (Ccl2, Il1b, Tnfa, Il6, Itgam) or anti-inflammatory (Adipoq, Arg1, Mgl1) markers in adipose tissue depots or liver. However, relatively low gene expression of inflammatory markers in the tissues indicates that the mice fed the HFHS diet failed to develop a robust inflammatory state. Conclusions BL and RB have direct anti-inflammatory effects on immune cells. Initial analysis indicates that consumption of BL and RB has no significant effects on markers of inflammation in a diet-induced mouse model of obesity. However, it is possible that the relatively low levels of inflammation in these mice masked the anti-inflammatory potential of BL and RB. Ongoing analysis will provide additional insights into the effects of BL and RB on inflammation in these tissues. Funding Sources Lewis Foundation Award.


2008 ◽  
Vol 32 (3) ◽  
pp. 226-229 ◽  
Author(s):  
Kiyotaka Fukamachi ◽  
Yoshio Ootaki ◽  
Chiyo Ootaki ◽  
Masatoshi Akiyama ◽  
Keiji Kamohara ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4527
Author(s):  
Mohammad Gharaibeh ◽  
Mohammad Khalifeh ◽  
Adi Nawasreh ◽  
Wael Hananeh ◽  
Mofleh Awawdeh

Necrotic enteritis (NE) caused by Clostridium perfringens is one of the most important enteric diseases in poultry. The antibacterial activity of two different essential oil (EO) blends against C. perfringens was investigated both in vitro and in vivo. Additionally, the immunological response to EO treatment was assessed. In the in vitro study, the antibacterial activity of EO formulas and commonly used antibiotics was evaluated against C. perfringens using disk diffusion assay, minimum inhibitory concentration (MIC) assay, and minimum bactericidal concentration (MBC) assay. In the in vivo study, NE experimental infection was performed on 440 Ross broiler chicks at 19 days of age for 4 continuous days. The chicks were treated with either EOs or amoxicillin at 22 days of age for 5 continuous days. One day after the end of treatment, the birds’ performance was evaluated by calculating the feed conversion ratio. Serum samples from 120 birds were collected to measure the levels of IL-1β, IFN-γ, IL-8, IL-10, and IL-17. After that, all birds were slaughtered, and their small intestines were subjected to gross and histopathological evaluation. In addition, bacterial counts in the small intestines were evaluated. In the in vitro study, EOs showed higher antimicrobial activities in comparison with antibiotics against C. perfringens. In the in vivo study, birds treated with EOs showed a significant decrease in bacterial counts, a significant decrease in intestinal lesions, and a significant improvement in performance compared with untreated birds (p < 0.05). Moreover, treating birds with EOs directed the immune system toward an anti-inflammatory pathway. None of the treated birds died due to NE compared with the 10% mortality rate in untreated birds. In conclusion, EOs might be an effective and safe alternative to antibiotics in the treatment of chicken NE.


2018 ◽  
Vol 60 (6) ◽  
pp. 687-693 ◽  
Author(s):  
Shu Min Tao ◽  
Fan Zhou ◽  
U Joseph Schoepf ◽  
Addison A Johnson ◽  
Zhu Xiao Lin ◽  
...  

Background As abdominal computed tomography (CT) radiation dose can be higher compared with other organ systems, monitoring the radiation exposure from this exam type is especially important. Purpose To evaluate the effect of abdominal contrast-enhanced CT (CE-CT) on levels of DNA double-strand breaks (DSBs) in peripheral blood lymphocytes. Material and Methods This study was performed in two parts: (i) an in vitro study: venous blood samples from 12 volunteers were divided into four groups. Samples in group A did not undergo radiation exposure, while groups B, C, and D received one CT scan with 1–3 times the radiation dose equivalent to abdominal CE-CT scan, respectively; and (ii) an in vivo study: blood was taken before CT and 5 min after CT in 30 patients. Lymphocytes were isolated and stained by immunofluorescence of γ-H2AX protein. DSB levels were compared by variance analysis or paired t-test. The relationship between radiation dose and γ-H2AX focus increase was analyzed using Pearson correlation analysis. Results In the in vitro study, DSBs levels in groups B, C, and D were 49.4%, 96.6%, and 149.4% higher than those in Group A, respectively (all P < 0.001). Radiation dose in the four subgroups had a linear correlation to DSB levels ( P < 0.001). In the in vivo study, the DSB level was 43.5% higher after CT ( P < 0.001). Conclusion Abdominal CE-CT significantly increased DSB levels in both in vitro and in vivo experiments. A positive linear correlation of CT radiation dose with intracellular DSBs levels was observed in the in vitro study.


2014 ◽  
Author(s):  
Ivo Dumic-Cule ◽  
Dunja Rogic ◽  
Damir Jezek ◽  
Lovorka Grgurevic ◽  
Slobodan Vukicevic

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