Cancer Cell Cytotoxicities of 1-(4-Substitutedbenzoyl)-4-(4-chlorobenzhydryl) piperazine Derivatives

Cataloged from PDF version of article.A series of novel 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives 5a-g was designed by a nucleophilic substitution reaction of 1-(4-chlorobenzhydryl) piperazine with various benzoyl chlorides and characterized by elemental analyses, IR and H-1 nuclear magnetic resonance spectra. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7, FOCUS, MAHLAVU, HEPG2, HEP3B), breast (MCF7, BT20, T47D, CAMA-1), colon (HCT-116), gastric (KATO-3) and endometrial (MFE-296) cancer cell lines. Time-dependent cytotoxicity analysis of compound 5a indicated the long-term in situ stability of this compound. All compounds showed significant cell growth inhibitory activity on the selected cancer cell lines

Cancer cell Cytotoxicities of 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives

A series of novel 1-(4-substitutedbenzoyl)-4-(4-chlorobenzhydryl)piperazine derivatives 5a-g was designed by a nucleophilic substitution reaction of 1-(4-chlorobenzhydryl)piperazine with various benzoyl chlorides and characterized by elemental analyses, IR and 1H nuclear magnetic resonance spectra. Cytotoxicity of the compounds was demonstrated on cancer cell lines from liver (HUH7, FOCUS, MAHLAVU, HEPG2, HEP3B), breast (MCF7, BT20, T47D, CAMA-1), colon (HCT-116), gastric (KATO-3) and endometrial (MFE-296) cancer cell lines. Time-dependent cytotoxicity analysis of compound 5a indicated the long-term in situ stability of this compound. All compounds showed significant cell growth inhibitory activity on the selected cancer cell lines. © 2012 by the authors; licensee MDPI, Basel, Switzerland

Synthesis and cytotoxic activity of novel 3-methyl-1-[(4- substitutedpiperazin-1-yl)methyl]-1H-indole derivatives

A series of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1H- indoles (3a-l) were synthesized and their cytotoxicities were analyzed against 3 different human cell lines, including liver (HUH7), breast (MCF7) and colon (HCT116). The Mannich reaction of 3-methylindole (1) with 4- substitutedpiperazines (2) and formaldehyde resulted to the 3-methyl-1-[(4- substitutedpiperazin-1-yl)methyl]-1H-indoles (3a-l) in 38-69% yields. The investigation of anticancer screening revealed that the tested compounds showed comparable activity to the reference drug 5-fluorouracil and compounds 3g, 3h, 3i and 3k, had lower 50% inhibition (IC 50) concentration than reference drug. Moreover, the cytotoxic effect of the most potent compound 3h on HUH7 and MCF7 cells through apoptosis was visualized by Hoechst staining and compared with paclitaxel, which is a mitotic inhibitor acting on microtubules. The morphological features of apoptosis were observed as condensed and fragmented nuclei that are similar to paclitaxel. © Georg Thieme Verlag KG Stuttgart.New York

Cytotoxic activities of some benzothiazole-piperazine derivatives

Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Compound 1d is highly cytotoxic against all tested cancer cell lines. Further investigation of compound 1d by Hoechst Staining and Fluorescence-Activated Cell Sorting Analysis (FACS) revealed that this compound causes apoptosis by cell cycle arrest at subG1 phase. © 2014 Informa UK Ltd. All rights reserved

Synthesis and cytotoxicity studies of novel benzhydrylpiperazine carboxamide and thioamide derivatives

Synthesis and cytotoxic activities of 32 benzhydrylpiperazine derivatives with carboxamide and thioamide moieties were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. In general, 4-chlorobenzhydrylpiperazine derivatives were more cytotoxic than other compounds. In addition, thioamide derivatives (6a-g) have higher growth inhibition than their carboxamide analogs. © 2014 Informa UK Ltd. All rights reserved

Mammary fibroadenoma in a lamb

A fibroadenoma was diagnosed in the left udder of a 3-month-old female Chios lamb. No recurrence was observed after surgery. Grossly, the tumor had a whitish-gray lobular appearance, and the lobules were interlaced with thin septa. Microscopically, the tumor was composed of proliferating fibroepithelial tissue, including differentiated ducts lined by whorls and interlacing bundles of abundant loose fibrovascular stroma. Immunohistochemistry revealed the ductal epithelium to be positive for pancytokeratin (AE1/AE3) and loose fibrovascular stroma was positive for vimentin and basal cells covering the ductal epithelium of alpha-smooth-muscle actin. Immunostaining for the estrogen and progesterone receptors was negative. A diagnosis of mammary fibroadenoma was made based on the histological and immunohistochemical findings

Choroid epithelial cells: Source cerebrospinal fluid progesterone in sheep?

The present study was conducted to immunolocalize 3?-hydroxysteroid dehydrogenase (3?-HSD), an enzyme metabolizing pregnenolone to progesterone in the choroid plexus of the lateral ventricle in sheep, as well as to measure progesterone concentration in cerebrospinal fluid (CSF) and plasma using radioimmunoassay (RIA). Akkaraman breed rams (n = 16) and ewes (n = 16) were utilized in the study. 3?-HSD was immunolocalized in choroid epithelial cells of the choroid plexus with an apparent cytoplasmic immunoreactivity. Progesterone was detected in CSF with no significant differences between the ewes (0.76 ± 0.14 ng/mL) and rams (0.74 ± 0.13 ng/mL) (p > 0.05). However, the plasma progesterone concentration in the ewes (0.27 ± 0.04 ng/mL) was significantly higher than that of the rams (0.11 ± 0.02 ng/mL) (p < 0.001). Consequently, CSF in sheep contains progesterone in significant levels. As evidenced by 3?-HSD immunoreactivity, choroid epithelial cells may be a site of progesterone synthesis in sheep

Effects of oregano or red pepper essential oil supplementation to diets for broiler chicks with delayed feeding after hatching. 1. Performance and microbial population

WOS: 000330523300009This study was conducted to investigate the effects of dietary supplementation of oregano or red pepper essential oil on the performance, digestive organs, serum biochemistry parameters, and microbial population of the small intestine of broilers with immediate, or 24- or 48-h posthatching delayed access to diet and water. The dietary treatments included (1) a non-supplemented corn-soybean meal diet (CONT), (2) CONT + 250 mg/kg of oregano essential oil (OO250), and (3) CONT + 250 mg/kg of red pepper essential oil (RPO250). Irrespective of dietary treatment, especially delayed access to diet and water for 48 h posthatch significantly decreased daily BW gain from 0 to 21 d and daily feed intake from 4 to 21 d and increased the relative weight of the yolk sac at 3 d of broilers. The relative weight of the liver or gizzard of chickens at 21 d was significantly decreased by delayed access to diet and water for 24 h posthatch. The diet containing RPO250 significantly increased the relative weight of the pancreas at 21 d. Delayed access to diet and water for 24 or 48 h posthatch significantly reduced serum glucose levels at 21 d. The serum aspartate aminotransferase level in broilers given immediate access to feed and water was significantly decreased by the diet containing RPO250. Generally, the coliform bacteria and total yeast contents of the small intestine of chickens were significantly increased by extending the time to access to feed and water for broilers. Total aerobic bacteria contents of the small intestine of broilers with immediate, or 24- or 48-h posthatching delayed access to diet and water was significantly decreased by CONT, OO250, and RPO250 diets

Experimental listeriosis in rabbits : Biochemical changes in serum and cerebrospinal fluid

/0000-0002-0636-4214WOS: 000223398200003This study was focused on serum and cerebrospinal fluid (CSF) biochemical changes in experimental Listeria monocytogenes infection in rabbits. Total of 20 New Zealand White rabbits were used. 14 New Zealand White rabbits were inoculated with Listeria monocytogenes 1/2a (L.m. 1/2a) by intracerebral way and 6 rabbits served as controls. Ten hours after the inoculation of the bacteria the rabbits developed symptoms of meningitis, with stiffness of the neck and fever. The existence and the severity of the inflammatory reaction were controlled by microscopic observation. The presence of bacteria into the cytoplasm of neutrophils and macrophages localised in inflammatory areas was confirmed by immunohistochemical analysis using rabbit polyclonal antibodies. We have analysed in serum and cerebrospinal fluid (CSF) the concentrations of glucose, total protein, and the enzymatic activities of aspartate aminotransferase (ASAT), alanine aminotransferase (ALAT) and lactate dehydrogenase (LDH). After intracerebral inoculation of bacteria the glucose concentrations in the serum and CSF decreased to 428.69 +/- 5.50 mg/l and 309.56 +/- 3.93 mg/l (mean +/- SE) respectively compared to control values of 975.33 +/- 84.34 mg/l and 689.22 +/- 65.13 mg/l (p less than or equal to 0.001). Total protein contents, the activities ofASAT, ALAT and LDH in the serum of infected animals increased to 98.92 +/- 1.97 g/l, 327.87 +/- 22.18 U/l, 292.39 +/- 4.66 U/l, 153.28 +/- 3.04 U/l respectively compared to 64.42 +/- 1.14 g/l, 67.91 +/- 7.79 U/l, 74.25 +/- 1.79 U/l, 49.35 +/- 1.20 U/l in control rabbits. In CSF, increases in total protein concentrations and in enzyme activities were also evidenced in inoculated rabbits. Moreover, serum and CSF LDH activities were correlated with brain injury (p < 0.05)

Neurosteroidogenesis in oligodendrocytes and Purkinje neurones of cerebellar cortex of dogs

/0000-0002-0636-4214WOS: 000221913400006PubMed: 15144282The cerebellum is a steroidogenic organ that expresses steroidogenic enzymes and produces neurosteroids. Purkinje neurones appear to be the most active steroidogenic cells in the cerebellar cortex. These neurones express 3beta-hydroxysteroid dehydrogenase (3beta-HSD), P450 side-chain cleavage (P450scc), 17alpha-hydroxylase/c17, 201yase (P450c17), P450 aromatase (P450arom) and produce pregnenolone, progesterone, dehydroepiandrosterone, androstenedion, oestradion and oestrone. Oligodendrocytes are predominantly the producer of myeline protein. The oligodendrocytes were identified by immunohistochemistry using a monoclonal antibody against myeline 2', 3'-cyclic nucleotide 3'-phosphodiesterase (CNPase), a myeline specific enzyme. In this study we have examined the distribution of 3beta-HSD and CNPase by immunohistochemistry using monoclonal antibody in canine cerebellar cortex. The localization of oligodendrocytes within the cerebellar cortex was determined to be close to Purkinje neurones. This result suggests that endogenous progesterone synthesized de novo in the Purkinje neurone can promote myeline protein synthesis in oligodentrocytes