Readily Accessible and Brightly Fluorogenic BODIPY/NBD-Tetrazines via SNAr Reactions.

We describe SNAr reactions of some commercial amino-tetrazines and halo-dyes, which give efficiently quenched BODIPY/NBD-tetrazines (ΦFl < 0.01) in high yields and, importantly, with high purities affordable via simple silica gel chromatography only. The dyes exhibit large Stokes shifts, moderate environmental sensitivity, and emission enhancements (up to 193-fold) upon Tz ligation with BCN─a strained dienophile. They successfully serve as labels for HSA protein premodified with BCN, resulting in bright blue-green emission upon ligation.

Effects of black cumin (Nigella sativa L.) seed on growth performance, blood parameters, liver oxidant/anti-oxidant levels and fatty liver syndrome in quails.

This research aimed to evaluate the effect of different doses of black cumin (Nigella sativa L.) seed (BCS) on growth performance, blood parameters, liver oxidant/anti-oxidant levels and fatty liver syndrome in quails. Four hundred and thirty-two unsexed (male and female) three-day-old Japanese quail (Coturnix coturnix japonica) chicks were divided into four treatment groups (108 chicks per group) with six replicates (18 chicks per replicate). Control and experimental groups were fed for 35 days with basal quail feed including 0.00, 0.50, 1.00 and 2.00% BCS supplement, respectively. At the end, a total of 96 quails, 24 from each group (12 females and 12 males) were slaughtered. The BCS-addition did not affect the growth performance in the experimental groups compared to the control group. Addition of BCS to the diet significantly decreased serum aspartate aminotransferase, lactate dehydrogenase and urea amounts compared to the controls. Whereas, cholesterol decreased significantly with the addition of only 1.00% and low-density lipoprotein with the addition of 0.50 and 1.00% BCS compared to the controls. Liver glutathione levels significantly elevated in 0.50 and 1.00% BCS fed groups; while, glutathione peroxidase levels significantly decreased in 1.00 and 2.00% BCS fed groups. Adding 1.00 and 2.00% BCS to the feed reduced fatty liver incidence in male quails. It is concluded that adding 0.50 and 1.00% BCS positively affects the blood and liver parameters; therefore, BCS may be suggested as an anti-oxidant source to help protect hepatocytes against tissue damage as it has a significant effect on maintaining oxidant and anti-oxidant balance.

The evaluation of early stage oxidative status in streptozotocin induced diabetes in rats.

Early-stage diabetes can be defined as the stages before absolute insulin deficiency in patients. In this study, the early stage oxidative effect of streptozotocin(STZ) induced diabetes mellitus was evaluated. 28 male adult Sprague-Dawley rats were divided into four groups; control group and 7th, 14th, 21st days diabetic groups. Diabetic groups received single 65 mg/kg STZ injection intraperitoneally. Rats were decapitated at 7th, 14th and 21st days, liver tissues were taken. Nitric oxide(NO), malondialdehyde(MDA) levels and catalase, arginase activities were measured. MDA and NO levels were increased (respectively p < .001 and p < .01), mainly 14 and 21 days after STZ administration; moreover, while liver catalase activity was progressively decreased (p < .001), oppositely arginase was increased in the same time period (p < .01). Results show that MDA and nitric oxide together with catalase and arginase switch at an early stage of diabetes and they may contribute to subsequent complications related to diabetes via increased oxidative damage.

Calcium Fructoborate Prevents Skin Cancer Development in Balb-c Mice: Next Part, Reverse Inflammation, and Metabolic Alteration.

Metabolic alterations and inflammation are regarded as hallmarks of cancer. Glycolytic flux and intermediate accumulation lead to the production of building blocks and NADPH which is important in protecting the cell from oxidative damage. Inflammation causes the release of mediators responsible for regulating molecular mechanism affecting metabolic pathways. CaFB due to its cis-diol-rich feature may have the potential to interact with molecules taking part in cancer development. This study was aimed to investigate the effects of CaFB on metabolic alterations and inflammation in 7,12-dimethylbenz(a)anthracene (DMBA)/12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin cancer. For this purpose, 92 Balb-c mice were distributed into 6 groups as control, CaFB, DMBA/TPA (D-T), treatment 1 (T1), 2 (T2), and 3(T3). Apart from control and CaFB in other groups, tumors initiated with 97.5-nmol DMBA and 6.5-nmol TPA. Treatment groups received 3 mg/kg/day CaFB with DMBA (T1), with TPA (T2), and after tumor formation (T3). In the D-T group, glyceraldehyde-3-phosphate dehydrogenase (GAPDH) activity, 6-phosphogluconate dehydrogenase (PGD), glutathione (GSH), interleukin 6 (IL-6), (IL-1ß), tumor necrosis factor-α (TNF-α) levels increased (p < 0.001) while malondialdehyde (MDA) levels decreased (p < 0.001) compared with that in control. CaFB application ameliorated DMBA-TPA effect according to the distribution time. It is noteworthy to consider CaFB as a potential preventive agent in skin cancer development.

Calcium Fructoborate Prevents Skin Cancer Development in Balb-c Mice.

Tumor microenvironment, genetic, and non-genetic factors are responsible for the atypical metabolic feature of cancer cells. Aberrant activity of PI3K/Akt pathway, increased glycolytic flux, and decreased intracellular pH gradient are the leading causes of this feature. Calcium Fructoborate (CaFB), a sugar-borate ester, has major benefits for human health. The aim of this study was to explore the implication of CaFB on experimentally induced skin cancer in vivo. According to the treatment, 92 female Balb-c mice are divided into six groups: control, CaFB (3 mg/kg/day), 7,12-Dimethylbenz(a)anthracene (DMBA)+12-O-tetradecanoylphorbol-13-acetate (TPA) (97.5 nmol DMBA, 6.5 nmol TPA), T1: CaFB+DMBA+TPA (3 mg/kg/day CaFB together with DMBA), T2: DMBA+CaFB+TPA (3 mg/kg/day CaFB together with TPA), T3: DMBA+TPA+CaFB (3 mg/kg/day CaFB after tumor formation). Topical DMBA and TPA application resulted in a significant increase in the protein levels, immunoreactivity, and mRNA expression of HRAS, HIF1α, Akt, and PTEN (p < 0.05). Moreover, an increase in the number of TUNEL-positive cells was observed in DMBA-TPA group compared with the control group (p < 0.05). CaFB application reduced the protein levels, immunoreactivity, and mRNA expressions of HRAS, HIF1α, Akt, and PTEN and also decreased the number of TUNEL-positive cells. Recent evidence obtained from our study validated that CaFB treatment may have skin cancer-preventing effect.