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A novel PSMA targeting molecule ［177Lu］Lu-DOTA-CPN-PSMA with high uptake and long retention in prostate cancer was developed, in which DOTA was used as the bifunctional chelator, glutamic acid-urea-lysine(Glu-Urea-Lys) was used as the targeting group, and 4-(p-tolyl)butyric acid(CP) group together with quinoline ring were introduced at the linker of this molecule. The precursor DOTA-CPN-PSMA was synthesized using solid-phase peptide synthesis method. DOTA-CPN-PSMA was labeled with carrier-free 177Lu. The influences of pH, reaction time, temperature, and ratio of 177Lu/PSMA on the radiolabeling were investigated respectively, and the optimal labeling condition was determined accordingly. The lipid water partition coefficient and in vitro stability of ［177Lu］Lu-DOTA-CPN-PSMA were also measured. Preliminary SPECT/CT imaging study of ［177Lu］Lu-DOTA-CPN-PSMA was performed in nude mice bearing 22RV1 tumor and compared with ［177Lu］Lu-PSMA-I&T. The optimization of the labeling condition shows that the addition of gentisic acid is essential, and the reaction pH is at the range of 3.5-5.5, the reaction temperature and time is 60.94 ℃ and 5.15 min respectively, the ratio of 177Lu/PSMA(mCi/μg, 1 Ci=3.7×1010 Bq) is controlled at 1∶1-2∶1. The radiochemical purity reaches over 95%, and even up to 99%. The results of in vitro stability study show that the radiochemical purity is remained ≥95% after being incubated in saline and bovine serum at 37 ℃ for 24 h. So that the solution of ［177Lu］Lu-DOTA-CPN-PSMA is used for imaging study directly without further purification. The lipid-water partition coefficient of ［177Lu］Lu-DOTA-CPN-PSMA is -2.02, indicate that it is more lipophilic than ［177Lu］Lu-PSMA-I&T. Preliminary SPECT/CT studies reveal that ［177Lu］Lu-DOTA-CPN-PSMA is mainly metabolized through kidneys. Compared with images of ［177Lu］Lu-PSMA-I&T, higher uptake in prostate tumors and lower uptake in the kidneys are displayed. After 72 h, ［177Lu］Lu-DOTA-CPN-PSMA demonstrates longer retension in tumor than ［177Lu］-PSMA-I&T, but also displays longer retention in the body. These results demonstrate the potential of ［177Lu］Lu-DOTA-CPN-PSMA as a candidate for the treatment of prostate cancer and it is worth further study.

The purpose of this experiment was to investigate the effects of different proportions of soft acid in drinking water on the production performance, egg quality, and serum biochemical indexes of Jingfen No.2 laying hens at the late of laying peak. A total of 270 Jingfen No.2 laying hens with normal body condition and similar weight at 556 days old were randomly divided into three groups with six replicates in each group and 15 laying hens in each replicate. The control group (CON group) drank tap water. 500 mg/kg and 800 mg/kg of soft acid were added to tap water in the soft acid 500 group and 800 group, respectively. The pre-test period was seven days, and the formal test period was 42 days. The results showed that compared with the control group, the unqualified egg rate of the soft acid 500 group and the soft acid 800 group decreased significantly (P<0.05), the average egg weight increased significantly (P<0.05), and the feed to egg ratio of the soft acid 800 group decreased significantly (P<0.05). Compared with the control group, the eggshell scores of soft acid 500 group and soft acid 800 group increased significantly (P<0.05), and the egg weight, yolk weight, eggshell strength, yolk ratio and yolk score all showed an increasing trend (P>0.05). Compared with the control group, the total protein content in serum of the soft acid 800 group increased significantly (P<0.05). Compared with the control group, the levels of serum IgA and IgG in the soft acid 500 group and 800 group increased significantly (P<0.05). The study indicates that adding 500 mg/kg and 800 mg/kg soft acid in drinking water has positive effects on improving production performance, egg quality, serum biochemical indexes, and immune function of Jingfen No.2 laying hens, and the effect of adding 800 mg/kg soft acid is better than that of 500 mg/kg soft acid. [ABSTRACT FROM AUTHOR]

The experiment aimed to explore the effects of compound organic acidifiers on the production performance, egg quality, serum biochemical indexes, and economic benefits of laying hens in the late laying period. Five hundred and forty 72-week-old Jingfen No.2 laying hens with similar body condition were selected and randomly divided into three groups (CON group, L-COA group, and H-COA group), with six replicates in each group and 30 hens in each replicate. Each group was fed the same diet. The CON group drank tap water throughout the whole process. The L-COA group and H-COA group added 0.10% and 0.15% compound organic acidifiers to the drinking water, respectively. The test period was 42 days. The results showed that compared to the CON group, the egg production rate and egg qualified rate of the L-COA group were significantly increased (P<0.05), the egg production rate, average egg weight, and egg qualified rate of the H-COA group were significantly increased (P<0.05). The eggshell strength and egg yolk score of the L-COA group were significantly improved (P<0.05). The serum low-density lipoprotein content and alanine aminotransferase activity in the L-COA group and H-COA group were significantly reduced (P<0.05). The breeding profits of the L-COA group and H-COA group increased by 1.08% and 13.64%, respectively. The study indicates that adding compound organic acidifiers to the drinking water of laying hens during the late laying period has a positive effect on egg production efficiency, egg quality, serum biochemical indexes, and economic benefits, and the better effect is achieved when the added amount of compound organic acidifiers is 0.15%. [ABSTRACT FROM AUTHOR]

The purpose of this experiment was to explore the effects of crude extract of Codonopsis pilosula and Astragalus membranaceus (CAE) on growth performance, serum biochemical index, immune organ index, and intestinal morphology of Sanhuang chickens. A total of 360 one-day-old Guangxi Sanhuang chicks weighing (27.0±0.5) g and in good physiological condition were randomly divided into three groups with six replicates in each group and 20 chickens in each replicate. CON group was fed a basal diet, CAE group was fed basal diet with 2.5 g/kg crude extract of Codonopsis pilosula and Astragalus membranaceus, and ANT group was fed basal diet with 0.05 g/kg chlortetracycline. The trial period was 42 days. The results showed that compared with CON group, the final weight and average daily gain of CAE group and ANT group increased significantly (P<0.05), the feed-to-weight ratio decreased significantly (P<0.05), and the mortality rate decreased by 3.33% (P>0.05). Compared with CON group, the activity of aspartate aminotransferase and the content of triglyceride and cholesterol in serum of CAE group and ANT group decreased significantly (P<0.05). Compared with CON group, CAE group and ANT group had significantly higher French capsule index (P<0.05). Compared with CON group, the villus height and villus-saphenous ratio of twelve intestines in CAE group and ANT group were significantly higher (P<0.05). The study indicates that the crude extract of Codonopsis pilosula and Astragalus membranaceus has positive effects on the growth performance, serum biochemical index, immune organ index and intestinal morphology of Sanhuang chickens, which was equivalent to the application effect of antibiotics. [ABSTRACT FROM AUTHOR]

Two series of 1,4-naphthoquinone-chromone hybrids 4a (4aa–4ao) and 4b (4ba–4bq) were designed, synthesized and evaluated as antitumor agents. Most of the compounds exhibited moderate to excellent cytotoxicity to tumor cells (K562 and A549), especially the 4a series compounds that showed equal or stronger antiproliferative activity compared to positive control cisplatin on two different types of cells (except for 4al and 4an). Among them, compound 4ac showed significant inhibitory activity on A549 cells with an IC50 value of 2.93 μM, and was 5.2 times more active than cisplatin (IC50 = 15.32 ± 2.64 μM). Meanwhile, AO/EB staining, flow cytometry, cell morphology, and ultrastructural analysis revealed that compound 4ac could induce A549 cell apoptosis and arrest at the G1 phase. Further mechanism studies speculated that compound 4ac may regulate the p53-MDM2 pathway, alter the Bax/Bcl-2 ratio to release Cyt c, activate the mitochondrial apoptosis pathway to induce cell apoptosis, and inhibit A549 cell proliferation through cycle arrest. Collectively, compound 4ac could be used as a potential candidate compound for anti-lung cancer drugs. [ABSTRACT FROM AUTHOR]