MicroPET imaging with 2-[18F] fluoropropionic acid in Lewis lung carcinoma-bearing mice / 中华核医学与分子影像杂志

Objective To prepare 2-[18F]fiuoropropionic acid (18F-FPA) and evaluate its biodistribution and imaging capacity in Lewis lung carcinoma-bearing mice.Methods 18F-FPA was prepared by nucleophilic substitution reaction,and its hydrophilicity was analyzed.18F-FPA (7.4-11.1 MBq) was injected into Lewis lung carcinoma-bearing mice via tail vein.MicroPET imaging was performed at 20,80 min after the injection.The biodistribution of 18F-FPA in organs was analyzed.The blocking effects of sodium propionate and dichloroacetate to 18F-FPA were tested in vivo.Data were analyzed by two-sample t test using GraphPad Prism software.Results The synthesis of 18F-FPA took 40 min.18F-FPA had high radiochemical purity (＞99％) and hydrophilicity.18F-FPA was mainly distributed in the carcinoma,the urinary bladder and the caecum.The radioactive uptakes in muscles,brown fat and bones were relatively low.Quantitative analysis showed that the uptake of 18F-FPA in Lewis lung carcinoma from 20 min to 80 min was slightly increased ((17.03±2.87) ％ID/g vs (19.33±2.45) ％ID/g) without significant difference (t=1.100,P＞0.05).Neither sodium propionate nor dichloroacetate could block the uptake of 18F-FPA in Lewis lung carcinoma (t=1.544,0.894;both P＞0.05).Conclusions 18F-FPA can be quickly synthesized and has good physicochemical properties.It can be used as a tracer to visualize Lewis lung carcinoma in mice,and its tumor uptaking can not be blocked by propionate and dichloacetate.18 F-FPA PET has the potential to detect lung cancer noninvasively in clinic.

In vitro colonic catabolism of orange juice (poly)phenols.

SCOPE: The role of colonic microbiota in the breakdown of hesperetin, naringenin, and ferulic acid, compounds found as glycosides in orange juice, was investigated using an in vitro fermentation model. METHODS AND RESULTS: Test compounds were incubated with human fecal slurries cultured under anaerobic conditions, and the production of phenolic acid catabolites were monitored by GC-MS and HPLC-MS(2) . Hesperetin was converted to 3-(3'-hydroxy-4'-methoxyphenyl)propionic acid, 3-(3',4'-dihydroxyphenyl)propionic acid, and 3-(3'-hydroxyphenyl)propionic acid while 3-(phenyl)propionic acid was the major end product derived from naringenin. The data obtained are compared to our previously published data on urinary excretion of phenolic and aromatic acids after acute orange juice consumption (Pereira-Caro et al. Am. J. Clin. Nutr. 2014, 100, 1385-1391). Catabolism pathways are proposed for events occurring in the colon and those taking place postabsorption into the circulatory system with particular reference to the excretion of 3-(3'-hydroxy-4'-methoxyphenyl)hydracrylic acid, which is not formed in fecal incubations. Ferulic acid was also degraded by the colonic microflora being converted principally to 3-(3'-methoxy-4'-hydroxyphenyl)propionic acid, a phenolic acid that appears in urine after orange juice consumption. CONCLUSION: The study provides novel information on the potential involvement of the colonic microbiota in the overall bioavailability of orange juice (poly)phenols through the production of phenylpropionic acids and subsequent hepatic conversions that lead to hippuric acid and its hydroxylated analogues.

Study on inhibition of lymphangiogenesis in gastric cancer by NM-3 / 中华消化杂志

Objective To evaluate the inhibitory effect of 2-(8-hydroxy-6-methoxy-1-oxo-1-H-2-benzopyran-3-Y1) propionic acid (NM-3) on lymphangiogenesis in gastric cancer using orthotopic implantated tumor models of BALB/C nude mice. Methods A BALB/C nude mouse model of transplanted in situ human gastric cancer was established. Twenty-eight nude mice were divided into four groups with 7 each: control group, NM-3 treated group, carboplatin (10 mg/kg) treated group,and NM-3 combiantion group injected with normal saline, 5 mg/kg of NM-3, 10 mg/kg of carboplatin or 5 mg/kg of NM-3, + 10 mg/kg carboplatin, respectively, twice a week for 8 weeks. At the end of the 8th week, all mice were sacrificed for detection of lymphatic microvessel density (LMVD),lymphatic vessel endothelial hyaluranic acid receptor 1 (LYVE-1), podoplanin and Prox-1 byimmunohistochemistry with staining. Results In comparison with control group, the LYVE-1 level in other three groups was decreased with no significant difference (P＞ 0.05). The concentrations of podoplanin and Prox-1 in NM-3 group and combination group decreased significantly than those in control group and carboplatin group (P ＜ 0.05). The number of LMVD in NM-3 group and combination group was 4.72±0.50 and 4.78± 0.38, respectively, which was significantly lower than that in control group (7.35±0.55)and carboplatin group (6.98i0.35, P＜0.05). Conclusion The NM-3 can inhibit the growth of gastric cancer by interfering lymphangiogenesis of gastric cancer.

Chemical preconditioning with 3-nitropropionic acid reduces myocardial ischemia-reperfusion injury in rats / 中华麻醉学杂志

Objective To investigate the cardioprotective effects of 3-nitropropionic acid (3-NPA) pretreatment against ischemia-reperfusion (I/R) injury. Methods Sixteen male Wistar rats weighing 200-250 g were randomly divided into 2 groups ( n = 8 each):(1) 3-NPA group received intraperitoneal 3-NPA 4 mg?kg-1 24 h before the animals were sacrificed and (2) control group received normal saline instead of 3-NPA. The animals were sacrificed and the hearts were immediately removed and mounted on Langendorff apparatus and perfused with K-H solution saturated with 95% O2 and 5% CO2 at 37℃ . After being perfused for 30 min the hearts were subjected to 30 min global ischemia by suspension of perfusion followed by 60 min reperfusion. The HR, left ventricular developed pressure (LVDP) and ? dp/dtmaxd were recorded before ischemia and at 30 and 60 min of reperfusion. Coronary effluent was collected at 15 min of reperfusion for determination of CK and LDH activity. At the end of 60 min reperfusion the hearts were removed for determination of myocardial MDA content and SOD activity.Results LVDP and ? dp/dtmax recovered significantly better in 3-NPA group than in control group. The myocardial MDA content, CK and LDH release were significantly lower in 3-NPA group than in control group. The myocardial SOD activity was significantly higher in 3-NPA group than in control group. Conclusion Chemical preconditioning with 3-NPA protects the heart from I/R injury.