Comparison of four techniques to estimate milk production in singleton-rearing non-dairy ewes

Accurate estimates of milk production or milk intake are difficult, as all methods interfere to some degree with the natural behaviour of the dam and her young, and potentially alter milk yield itself. The present study compared milk yield obtained by the “oxytocin” method, udder dimensions (UD), the isotope dilution method, and live weight change of the lamb, in an attempt to select the most accurate and convenient way of measuring milk production in non-dairy sheep. In addition, the study investigated which of the three milk-estimation techniques was an accurate predictor of growth rates of lambs. Thirty-seven singleton-bearing and rearing ewes were milked once a week, for seven consecutive weeks, using the “oxytocin” method. Prior to each afternoon milking, the external dimensions of the ewe's udder were measured. Lambs were weighed weekly for the first seven weeks of life and live weight change was calculated. The deuterium oxide (D₂O) dilution technique was used to estimate milk intake of the lambs and performed at approximately 7 days post-partum and finishing on approximately day 14. Pearson's correlation coefficients and multiple regression coefficients among techniques were calculated. The UD-models at d7 (R² = 0.35), d35 (R² = 0.36) and d42 (R² = 0.34), were the best models explaining variation in milk yield (concordance correlation coefficient (CCC) = 0.49; 0.53; 0.51; for d7, d35 and d42, respectively). The lamb live weight-change model explained the variation in milk yield best at d28 (R² = 0.32; CCC = 0.49), at d35 (R² = 0.22; CCC = 0.36) and at d42 (R² = 0.28; CCC = 0.44). At d14, the intake of milk by lambs as measured by the D₂O technique, did not explain the variation in milk yield. In conclusion, udder dimensions, lamb live weight change and lamb milk intake are relatively poor estimators of the milk yield of singleton-rearing ewes obtained by the “oxytocin” method. Additionally, udder dimensions, milk yield and lamb milk intake do not give an accurate prediction of growth rates of singleton lambs. These results emphasize that there is a difference between ewe milk production potential and lamb milk intake, which need to be considered when estimating milk production in non-dairy animals.     

The relationship between fetal and maternal selenium concentrations in sheep and goats

In this study, biological samples (slaughterhouse material) were collected from 30 sheep and 36 goats and classified according to gestational stage into either early or late gestation. Samples consisted of allantoic fluid, amniotic fluid, fetal liver, fetal kidney, fetal thyroid gland, maternal plasma and liver to determine selenium (Se) concentrations throughout gestation. The Se concentrations in the allantoic fluid, fetal liver and kidney increased significantly (p < 0.01) during late gestation. Concurrently, the Se concentrations in amniotic fluid, maternal plasma and liver decreased significantly (p < 0.01) over time. Significant (p < 0.01) positive relationships were recorded between the age of the fetus and Se concentrations in the allantoic fluid (r = 0.57–0.75), fetal liver (r = 0.43–0.59) and kidney (r = 0.80–0.81) in both sheep and goats. A significant (p < 0.05) positive relationships were also recorded between the Se concentrations in the allantoic fluid and fetal liver (r = 0.35–0.37), the maternal plasma and liver Se concentrations (r = 0.37–0.57) between sheep and goats. A significant (p < 0.05) negative correlation was recorded between the Se concentrations in the allantoic fluid with maternal plasma of sheep (r = −0.41) as well as between the fetal liver and maternal liver Se (r = −0.22 to 0.50) and a negative correlation (r = −0.42 to 0.43) (p < 0.01) between Se concentrations in the fetal liver and amniotic fluid in both sheep and goats, respectively. Se concentration in the fetal liver was significantly (p < 0.01) higher than that of the kidney and thyroid. In the thyroid gland no morphological differences were noted. Strong fetal–maternal relationships in Se concentration were evident throughout the gestational period and dams seem to sacrifice Se levels in order to maintain that in the fetus. Se concentrations in the amniotic and allantoic fluids could be used as a possible indicator of the Se status of the fetus throughout gestation.     

Electromyographic and mechanomyographic responses across repeated maximal isometric and concentric muscle actions of the leg extensors

The purpose of the present study was to examine the patterns of responses for torque, electromyographic (EMG) amplitude, EMG mean power frequency (MPF), mechanomyographic (MMG) amplitude, and MMG MPF across 30 repeated maximal isometric (ISO) and concentric (CON) muscle actions of the leg extensors. Twelve female subjects (21.1 ± 1.4 yrs; 63.3 ± 7.4 kg) performed ISO and CON fatigue protocols with EMG and MMG signals recorded from the vastus lateralis. The relationships for torque, EMG amplitude, EMG MPF, MMG amplitude, and MMG MPF versus repetition number were examined using polynomial regression. The results indicated there were decreases (p < 0.05) across the ISO muscle actions for torque (r² = 0.95), EMG amplitude (R² = 0.44), EMG MPF (r² = 0.62), and MMG MPF (r² = 0.48), but no change in MMG amplitude (r² = 0.07). In addition, there were decreases across the CON muscle actions for torque (R² = 0.97), EMG amplitude (R² = 0.46), EMG MPF (R² = 0.86), MMG amplitude (R² = 0.44), and MMG MPF (R² = 0.80). Thus, the current findings suggested that the mechanisms of fatigue and motor control strategies used to modulate torque production were similar between maximal ISO and CON muscle actions.     

The relationship between the volatile fatty acids supply and the nitrogen retention in growing sheep nourished by total intragastric infusions

Twelve four-month old Suffolk × Small-tail-Han male sheep (live weight 21–26 kg), fitted with rumen and abomasum fistulas and nourished by total intragastric infusions, were used to study the relationship between the volatile fatty acids (VFA) supply and the nitrogen (N) retention in sheep. The animals were randomly divided into four groups and four levels of mixed VFA energy (the molar proportion of acetic acid, propionic acid and butyric acid was 65:25:10), i.e. 333, 378, 423 and 468 kJ kg^?1 W^0.75 d^?1, were infused into the rumen, as treatments I, II, III and IV, respectively. The results showed that the N retention was significantly increased (P < 0.05) with the VFA infusion level. Significant regression relationship was found between the VFA supply (x, g d^?1) and the N retention (y, mg d^?1): y = 2.75x ? 403, r² = 0.86, n = 12, P < 0.01. It was concluded that to get efficient utilization of dietary N and high N retention in sheep, it is necessary to supply enough dietary energy.     

Forest biomass and volume estimation using airborne LiDAR in a cool-temperate forest of northern Hokkaido,Japan

Trees are recognized as a carbon reservoir, and precise and convenient methods for forest biomass estimation are required for adequate carbon management. Airborne light detection and ranging (LiDAR) is considered to be one of the solutions for large-scale forest biomass evaluation. To clarify the relationship between mean canopy height determined by airborne LiDAR and forest timber volume and biomass of cool-temperate forests in northern Hokkaido, Japan, we conducted LiDAR observations covering the total area of the Teshio Experimental Forest (225 km²) of Hokkaido University and compared the results with ground surveys and previous studies. Timber volume and aboveground tree carbon content of the studied forest stands ranged from 101.43 to 480.40 m³ ha^–1 and from 30.78 to 180.54 MgC ha^–1, respectively. The LiDAR mean canopy height explained the variation among stands well (volume: r² = 0.80, RMSE = 55.04 m³ ha^–1; aboveground tree carbon content: r² = 0.78, RMSE = 19.10 MgC ha^–1) when one simple linear regression equation was used for all types (hardwood, coniferous, and mixed) of forest stands. The determination of a regression equation for each forest type did not improve the prediction power for hardwood (volume: r² = 0.84, RMSE = 62.66 m³ ha^–1; aboveground tree carbon content: r² = 0.76, RMSE = 27.05 MgC ha^–1) or coniferous forests (volume: r² = 0.75, RMSE = 51.07 m³ ha^–1; aboveground tree carbon content: r² = 0.58, RMSE = 19.00 MgC ha^–1). Thus, the combined regression equation that includes three forest types appears to be adequate for practical application to large-scale forest biomass estimation.     

Tumor Necrosis Factor-α, Interleukins-12(p40), 6, and 10 levels in cerebrospinal fluid and outcome prediction in Ossimi sheep with encephalitic listeriosis

Encephalitic listeriosis in sheep is a life-threatening disease. However, little is known about the cytokine response and their predictive value in this disease. The aim of present study was to assess the prognostic significance of Tumor Necrosis Factor-α (TNF-α), Interleukin-12(p40) (IL-12 p40), Interleukin-6 (IL-6), and Interleukin 10 (IL-10) levels in cerebrospinal fluid (CSF) in sheep with encephalitic listeriosis. Fifty-nine ewes in 14 flocks were diagnosed clinically as having listeriosis. CSF was collected and subjected to bacteriological examination and estimation of selected cytokines. Twenty-eight ewes were confirmed to be infected with Listeria monocytogenes. Based on antimicrobial sensitivity test, sheep were treated and the outcome was recorded as survivors (n = 10) and non-survivors (n = 18). Cutoff points for CSF cytokines were determined by Receiver operating characteristic analysis (ROC). Association between levels of CSF cytokines and outcome of listeriosis was assessed by logistic regression. TNF-α, IL-6 and IL-12(p40) levels as well as TNF-α/IL-10 ratio were significantly higher in non-survivors than survivors (p = 0.002, 0.0021, 0.0033, and 0.001, respectively). However, IL-10 level was significantly lower in non-survivors than survivors (p = 0.0058). ROC analysis revealed that IL-6 and TNF-α/IL-10 ratio had the highest AUC values (0.98, 0.984, respectively). Final multivariate logistic regression model showed that TNF-α/IL-10 ratio was the only variable that has predictive value for mortality in diseased sheep (p: 0.001; OR: 7.2; 95% CI: 5.7–9.8). TNF-α showed a positive correlation with IL-12β (r = 0.917) and IL-6 (r = 0.965). IL-12 (p40) showed also a positive correlation with IL-6 (r = 0.906). However, IL-10 showed a negative correlation with TNF-α (r = −0.915), IL-12(p40) (r = −0.790), and IL-6 (r = −0.902). In conclusion, TNF-α/IL-10 ratio may provide predictive information about outcome of encephalitic listeriosis in sheep.     

Fecal nitrogen to estimate intake and digestibility in grazing ruminants

This study aimed at evaluating forage intake and digestibility in ruminants using fecal nitrogen content, as well as validating a non-linear model to estimate digestibility in ruminants. A total of 58 conventional metabolism trials, carried out with sheep fed 27 forages (offered pure or in mixture) used in Rio Grande do Sul (RS) during the period 1969–1989 was analyzed. OM intake and OM digestibility (OMD) results were regressed linearly against fecal N, and OMD was also estimated from fecal crude protein (N × 6.25) content by a non-linear regression model. Fecal nitrogen excretion estimated forage intake in sheep with an R² = 0.73, whereas a low R² value of 0.36 was observed for OMD estimates. The equation obtained using the non-linear model was OMD = 0.7326 ? 0.3598 exp [(?0.9052 CP (g/kg OM))/100]. The parameters a (0.7326) and b (0.3598) estimated by the equation for all forages were significant (P<0.00001) and there was no effect of type of forage (P=0.38). The mean prediction error (MSPE), was 0.2379, indicating that the equation fit well to the data. The difference between estimated and observed organic matter digestibility was mainly caused by random variation (0.9765). The results indicated that the equation using the non-linear model developed with all forages can be used with enough precision to estimate the OM digestibility of forage consumed by sheep in Rio Grande do Sul.     

Climatic dependency of soil organic carbon isotopic composition along the S–N Transect from 34°N to 52°N in central-east Asia

We explored the relationships between surface-soil (1–20 cm) organic carbon isotopic signatures and associated climatic factors in central-east Asia in an attempt to develop transfer functions that can be used to retrieve the paleoclimatic information stored in the thick eolian–paleosol sequences within the area. Our analysis shows that the negative correlation between the surface-soil organic δ¹³C values and the mean annual precipitation is robust (R² = 0.453; n = 196; p < 0.05) and the negative correlation with the growing-season (April–September) precipitation is more significant (R² = 0.4966; n = 196; p < 0.05). Our study further shows that the positive correlation between the surface-soil organic δ¹³C values and mean growing-season aridity is most significant (R² = 0.5805; n = 196; p < 0.05). We have smoothed both the organic δ¹³C values and the mean growing-season aridity values using a 3-point moving-window average-filter method in an attempt to remove some of random errors and found that the positive correlation between the two is further increased (R² =  0.7784; n =  192; p < 0.05). These robust linear relationships demonstrate their value in reconstructing paleoclimate changes in the study area. The documented climatic dependency of the surface-soil carbon isotopic composition in the study area might have resulted both from the humidity-related isotopic enrichment processes of the dominant C₃ plants (stomatal conductance and photosynthetic discrimination) and from the aridity-related abundance of C₄ plants (mainly Chenopodiaceae species) along the S–N bioclimatic gradient.     

Testing the effectiveness of surrogates for assessing biological diversity of arthropods in cereal agricultural landscapes

Agricultural intensification is altering biodiversity patterns worldwide. Rapid and effective methods are needed to monitor these changes in farmland biodiversity, but it becomes both a cost- and time-prohibitive task, particularly for hyper-diverse groups such as arthropods. We evaluated the effectiveness of surrogates in irrigated and rainfed wheat fields in a Mediterranean farmland in NW Spain in order to get a rapid tool to assess arthropod biodiversity. We studied six groups with different ecological needs (i.e. Aphididae, Aphidiinae, Coccinellidae, Formicidae, Heteroptera and Syrphidae) at species level (147 species), genus (105), family (10, only Heteroptera) and order (19) level. Higher taxa, cross-taxa and subset-taxa or total richness approaches were tested as well as the correlation in composition between levels for the selected groups, and the influence of farming regime. Genus richness was a good surrogate of species richness in all six groups studied (R² = 0.38–0.60), like family and order were for Heteroptera (R² = 0.37 and 0.29, respectively). Cross-taxa analyses showed that Aphididae and Aphidiinae genera (R² = 0.19 and 0.30, respectively) and species (R² = 0.20 and 0.28, respectively) were good surrogates for Aphidiinae and Aphididae species respectively. Coccinellidae genera (R² = 0.26) and species (R² = 0.25) were good surrogates for Heteroptera species. Finally, Aphididae and Coccinellidae both at genera (R² = 0.14 and 0.20, respectively) and at species levels (R² = 0.12–0.22, respectively) were good surrogates for total species richness of all groups. Genera composition was the best surrogate for the species composition within each group. Farming regime had no influence on the relationships between surrogates and species patterns in most cases. Our results suggest that genera level is a useful surrogate for all the studied groups and family is appropriate for Heteroptera. Genus level provided a saving of 15% of identification time in Aphididae and 80% for Coccinellidae. This proves its usefulness to asses and monitor biodiversity in wheat croplands and the possibility to reduce costs.     

Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists

The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R¹ = –Me and R² = –ⁱPr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22.     

Whole crop rice silage: Predictions of yield and content of metabolizable energy,metabolizable protein and other nutrients for dairy cows from crop maturity and botanical fractions at harvest

The study investigated the suitability of stage of maturity and botanical fractions of whole crop rice (WCR) to predict yield and nutritive value of ensiled WCR for dairy cows. Eight varieties of WCR (i.e., Akichikara, Fukuhibiki, Habataki, Hamasari, Hokuriku 168, Kusanami, Tamakei 96, Yumetoiro) were harvested at four stages of maturity (i.e., 10, 22, 34, 45 days after flowering [DAF]) and ensiled. Dry matter (DM) yield at each harvest was determined. Silage samples were fractionated into four botanical fractions being: leaf blade, leaf sheath, stem and head. Silage samples were also analyzed for chemical composition, fermentation characteristics, in situ DM and N disappearance. Metabolizable energy (ME) and metabolizable protein (MP) content of samples were estimated according to Terada et al. (1988) and AFRC (1993), respectively. Relationships between maturity or proportions of botanical fractions and contents of WCR silage in terms of DM, ME and MP, and their yields, were estimated by correlation and regression analysis. Stage of maturity was positively related (P<0.001) to ME content (R² = 0.46; y = 4.53 + 0.08X) and MP content (R² = 0.56; y = 22.26 + 0.76X), and DM yield (R² = 0.63; y = 9.21 + 0.12X), ME yield (R² = 0.68, y = 36931 + 1708X) and MP yield (R² = 0.72, y = 161.0 + 14.15X) of WCR. Proportion of leaf was negatively related to yields and nutritive value of ensiled WCR, whilst proportion of head was positively related (P<0.05 to <0.001). Proportion of head was best related to the ME content (R² = 0.72; y = 3.26 + 0.009X), MP content (R² = 0.72; y = 12.31 + 0.079X), and DM yield (R² = 0.41; y = 9.02 + 0.009X), ME yield (R² = 0.76, y = 19494 + 165.5X), and MP yield (R² = 0.75, y = 34.37 + 1.32X) of WCR. Results suggest that to optimize yield and nutritive value, WCR should be ensiled within 40 DAF and the proportion of head should be equal to or more than 500 g per kg DM of WCR silage. Stage of maturity and proportion of head of WCR predict yields of DM, ME and MP of WCR, and their contents, in WCR silage with acceptable accuracy. However, these relationships need to be validated using large data sets and in vivo studies.     

Effect of ligand congeniality on energy transfer reaction between photo-excited tris(bipyridine)ruthenium(II) and chromate(III) complexes in aqueous solutions

Energy-transfer rate-constants from photo-excited [Ru(N–N)₃]²⁺ (N–N = 2,2′-bipyridine (bpy), 4,4′-dimethyl-2,2′-bipyridine (4dmb), 5,5′-dimethyl-2,2′-bipyridine (5dmb)) to [Cr(O–O)₃]³⁻ (O–O²⁻ = ox²⁻ ((COO⁻)₂), mal²⁻ (CH₂(COO⁻)₂)) and [Cr(CN)₆]³⁻ in encounter complexes were evaluated in aqueous solutions containing alkali metal ion. The rate constant depends on the molecular size of the ruthenium(II) complex: 1.8 × 10⁸ s⁻¹ for [Ru(bpy)₃]²⁺ (molecular radius, r = 5.8 Å), 1.4 × 10⁸ s⁻¹ for [Ru(5dmb)₃]²⁺ (r = 6.1 Å) and 0.96 × 10⁸ s⁻¹ for [Ru(4dmb)₃]²⁺ (r = 6.7 Å) in the system of [Ru(N–N)₃]²⁺–[Cr(ox)₃]³⁻ in aqueous solution. However, the rate constant is much more sensitive to the chromate(III) complex than to ruthenium(II) complex; 1.8 × 10⁸ s⁻¹ and 0.43 × 10⁸ s⁻¹ for [Cr(ox)₃]³⁻ (r = 4.0 Å) and [Cr(mal)₃]³⁻ (r = 4.2 Å) in the [Ru(bpy)₃]²⁺–[Cr(O–O)₃]³⁻ systems, respectively. We conclude that the congeniality between the donor’s and acceptor’s ligands in encounter complex plays an important role in energy transfer in aqueous solution.     

Growth performance and carcass traits of forage-fed hair sheep wethers

The objective of the present study was to compare live animal performance and carcass characteristics of 3/4 or 7/8 Dorper (DO; n = 30), purebred Katahdin (KA; n = 20), purebred St. Croix (SC; n = 17) and purebred Suffolk (SU; n = 10) lambs born in the spring and fall of 2001. After weaning, lambs were supplemented with up to 680 g of a corn-soybean meal supplement while grazing bermudagrass pastures overseeded with ryegrass. Lambs were slaughtered at approximately 210 d of age. From birth to weaning, DO lambs gained faster (P < 0.001) than KA or SC lambs, whereas KA lambs had higher (P < 0.001) ADG than SC lambs. Additionally, DO and SU wethers had greater (P < 0.02) ADG from weaning to slaughter than SC or KA wethers. Suffolk lambs were heavier (P < 0.001) at slaughter and produced heavier (P < 0.001) carcasses than lambs from hair-sheep breeds. Carcasses of KA lambs were fatter (actual fat thickness; P < 0.02) resulting in higher yield grades (P < 0.03) than carcasses of DO, SC, or SU lambs. Carcasses of DO and SU had larger (P < 0.001) longissimus muscle (LM) areas than those of KA or SC carcasses, whereas kidney fat weight and percentage were greater (P < 0.001) in carcasses from KA and SC than DO and SU lambs. Lean maturity was similar (P = 0.32) among breed-types. However, skeletal maturity was greater (P < 0.001) in SU than hair-sheep carcasses. Flank-streaking scores were similar (P = 0.19) among the breed-types, but conformation scores were higher (P < 0.001) for DO and SU carcasses and resulted in higher (P < 0.001) quality grades than SC carcasses. The LM of SU lambs was lighter (higher L^* values; P < 0.05) than that of KA and SC lambs, whereas the LM from DO lambs was redder (higher a^* values; P < 0.001) than SC and SU and more (P < 0.001) yellow than that of the other breed-types. Chops from SU lambs were tougher (higher shear force values; P < 0.007) than chops from the hair-sheep breeds. Results of this study indicate that ADG, carcass muscularity and meat quality were similar between DO and SU lambs, and, although fatter, carcass muscularity of KA was similar to that of DO lambs.     

Trispyrazolylmethane piano stool complexes of iron(II) and cobalt(II)

A series of cationic trispyrazolylmethane complexes of the general form [Tm^RM(CH₃CN)₃]²⁺ (Tm = tris(pyrazolyl)methane, 1, R = 3,5-Me₂, M = Fe(II); 2, R = 3-Ph, M = Fe(II); 3, R = 3,5-Me₂, M = Co(II); 4, R = 3-Ph, M = Co(II)) with ‘piano-stool’ structures was prepared by the reaction of the N₃tripodal ligands (Tm^R)with [(CH₃CN)₆M](BF₄)₂ in a 1:1 stoichiometric ratio. Magnetic susceptibility measurements indicate that all four complexes with BF₄⁻ counter anions are paramagnetic, high-spin systems in the solid state with μ_eff at high temperatures of 5.2 (1, S = 2), 5.4 (2, S = 2), 4.9 (3, S = 3/2) and 4.6 (4, S = 3/2) BM, respectively. Comparisons of bond lengths from the metal centre to the Tm^R nitrogen donors, and from the metal centre to the acetonitrile nitrogen donors indicate that the neutral tripodal ligands appear to be more weakly coordinated to the metal centre than are the acetonitrile ligands. Reactions of these tripodal complexes with bidentate phosphine ligands, such as 1,2-diphosphinoethane or 1,2-bis(diallylphosphino)ethane leads to displacement of the tripodal ligand, or to the formation of more thermally stable bis-ligand complexes M(Tm^R)₂ (R = 3,5-dimethyl).     

Betacarotene supplementation increases ovulation rate without an increment in LH secretion in cyclic goats

This study aimed to evaluate the effects of betacarotene (BC) supplementation on ovulation rate (OR) and luteinizing hormone (LH) secretion in adult goats during the breeding season. Additionally, total ovarian activity (TOA) comprising the total number of ultrasonographically detectable antral follicles (AF) and corpora lutea (OR) was also assessed. In early October, adult goats [n = 22, 3.5 years of age, 7/8 Sannen-Alpine; 26°N, 103°W at 1117 m.a.s.l.] were randomly assigned to: (i) BC group (BCG), orally supplemented with 50 mg of BC/goat/day [n = 10; live weight (LW) = 45.9 ± 2.0 kg, body condition score (BCS; range: 0-emaciated to 5-obese) = 3.0 ± 0.1], and (ii) control group (CONT) [n = 12; LW = 46.2 ± 2.0 kg, BCS = 3.0 ± 0.1]. All animals received a basal diet of alfalfa hay, corn silage and corn grain, with free access to water and mineral salts. The whole experimental period spanned 34 days before and 17 days after ovulation. On day 23 of the experiment, estrus was synchronized with progestin-releasing intravaginal sponges; 36 h prior to estrus, an intensive blood sampling (every 15 min for 6 h) was performed to determine mean LH concentrations, pulsatility (LH-PULSE) and area under the curve (LH-AUC) for serial LH concentrations. Afterwards, by the end of the luteal phase (i.e., 17 days after the onset of estrus), an ultrasonographic scanning was performed to evaluate OR and TOA [AF + OR]. The average LW and BCS did not differ (p > 0.05) during the experimental period. BC-supplemented goats showed an increase in OR (3.4 ± 0.2 versus 2.8 ± 0.2; p < 0.05) and exhibited lower (p < 0.05) serum LH concentrations, LH-AUC and LH-PULSE compared to CONT. A positive correlation was recorded between OR and LW (r² = 0.42, p < 0.05) and BCS (r² = 0.47, p < 0.05). In addition, AF (5.0 ± 0.6 versus 3.4 ± 0.6) and TOA (8.4 ± 0.6 versus 6.2 ± 0.6) were greater (p < 0.05) in the BC-supplemented group than CONT. Supplementation with BC enhanced ovarian follicular development and ovulation rate in adult female goats under decreased photoperiods through LHRH-independant pathways or direct effects of BC on ovarian function.     

Antimycobacterial activity evaluation,time-kill kinetic and 3D-QSAR study of C-(3-aminomethyl-cyclohexyl)-methylamine derivatives

A series of C-(3-aminomethyl-cyclohexyl)-methylamine derivatives were synthesized and evaluated for their antitubercular activity. Some of the compounds exhibited potent activity against Mycobacterium tuberculosis H37Rv. One of the compound having t-butyl at para position of the benzene ring showed excellent activity even better than the standard drug ethambutol with MIC value 1.1 ± 0.2 μM. The time-kill kinetics study of two most active compounds showed rapid killing of the M. tuberculosis within 4 days. Additionally atom-based quantitative structure–activity relationship (QSAR) model was developed that gave a statistically satisfying result (R²) = 0.92, Q² = 0.75, Pearson-R = 0.96 and effectively predicts the anti-tuberculosis activity of training and test set compounds.     

Cathepsin G activity lowers plasma LDL and reduces atherosclerosis

Cathepsin G (CatG), a serine protease present in mast cells and neutrophils, can produce angiotensin-II (Ang-II) and degrade elastin. Here we demonstrate increased CatG expression in smooth muscle cells (SMCs), endothelial cells (ECs), macrophages, and T cells from human atherosclerotic lesions. In low-density lipoprotein (LDL) receptor-deficient (Ldlr^–/–) mice, the absence of CatG reduces arterial wall elastin degradation and attenuates early atherosclerosis when mice consume a Western diet for 3 months. When mice consume this diet for 6 months, however, CatG deficiency exacerbates atherosclerosis in aortic arch without affecting lesion inflammatory cell content or extracellular matrix accumulation, but raises plasma total cholesterol and LDL levels without affecting high-density lipoprotein (HDL) or triglyceride levels. Patients with atherosclerosis also have significantly reduced plasma CatG levels that correlate inversely with total cholesterol (r = –0.535, P < 0.0001) and LDL cholesterol (r = –0.559, P < 0.0001), but not with HDL cholesterol (P = 0.901) or triglycerides (P = 0.186). Such inverse correlations with total cholesterol (r = –0.504, P < 0.0001) and LDL cholesterol (r = –0.502, P < 0.0001) remain significant after adjusting for lipid lowering treatments among this patient population. Human CatG degrades purified human LDL, but not HDL. This study suggests that CatG promotes early atherogenesis through its elastinolytic activity, but suppresses late progression of atherosclerosis by degrading LDL without affecting HDL or triglycerides.     

Bile acid toxicity structure–activity relationships: Correlations between cell viability and lipophilicity in a panel of new and known bile acids using an oesophageal cell line (HET-1A)

The molecular mechanisms and interactions underlying bile acid cytotoxicity are important to understand for intestinal and hepatic disease treatment and prevention and the design of bile acid-based therapeutics.Bile acid lipophilicity is believed to be an important cytotoxicity determinant but the relationship is not well characterized. In this study we prepared new azido and other lipophilic BAs and altogether assembled a panel of 37 BAs with good dispersion in lipophilicity as reflected in RPTLC R_Mw. The MTT cell viability assay was used to assess cytotoxicity over 24 h in the HET-1A cell line (oesophageal). R_Mw values inversely correlated with cell viability for the whole set (r² = 0.6) but this became more significant when non-acid compounds were excluded (r² = 0.82, n = 29). The association in more homologous subgroups was stronger still (r² >0.96). None of the polar compounds were cytotoxic at 500 μM, however, not all lipophilic BAs were cytotoxic. Notably, apart from the UDCA primary amide, lipophilic neutral derivatives of UDCA were not cytotoxic. Finally, CDCA, DCA and LagoDCA were prominent outliers being more toxic than predicted by R_Mw. In a hepatic carcinoma line, lipophilicity did not correlate with toxicity except for the common naturally occurring bile acids and their conjugates. There were other significant differences in toxicity between the two cell lines that suggest a possible basis for selective cytotoxicity. The study shows: (i) azido substitution in BAs imparts lipophilicity and toxicity depending on orientation and ionizability; (ii) there is an inverse correlation between R_Mw and toxicity that has good predictive value in homologous sets; (iii) lipophilicity is a necessary but apparently not sufficient characteristic for BA cytocidal activity to which it appears to be indirectly related.     

Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel,high affinity ligands for CB1 and CB2 cannabinoid receptors

A small library of N-benzyl indolequinuclidinone (IQD) analogs has been identified as a novel class of cannabinoid ligands. The affinity and selectivity of these IQDs for the two established cannabinoid receptor subtypes, CB1 and CB2, was evaluated. Compounds 8 (R = R² = H, R¹ = F) and 13 (R = COOCH₃, R¹ = R² = H) exhibited high affinity for CB2 receptors with K_i values of 1.33 and 2.50 nM, respectively, and had lower affinities for the CB1 receptor (K_i values of 9.23 and 85.7 nM, respectively). Compound 13 had the highest selectivity of all the compounds examined, and represents a potent cannabinoid ligand with 34-times greater selectivity for CB2R over CB1R. These findings are significant for future drug development, given recent reports demonstrating beneficial use of cannabinoid ligands in a wide variety of human disease states including drug abuse, depression, schizophrenia, inflammation, chronic pain, obesity, osteoporosis and cancer.     

Sexual performance of Awassi ram lambs reared in different sex composition groups

The objective of this study was to evaluate the effect of sex composition of the group of lambs before puberty on later sexual performance in Awassi ram lambs. Thirteen Awassi ram lambs of the same age were raised in either all-male group (n = 7) or in a group mixed with females (n = 6) from weaning to puberty. Blood samples, body weights (BW) and scrotal circumferences (SC) of ram lambs were recorded between eight and 10 months of age. Sexual performance testing was performed at 9 months of age by individually exposing ram lambs to oestrous females on five occasions. Body weight and SC were greater (P < 0.01) in the all-male compared with the mixed group. Plasma testosterone concentrations were not influenced (P > 0.05) by treatment. Plasma testosterone concentrations were significantly correlated (P ≤ 0.05) with BW (r = 0.3) and SC (r = 0.4). No treatment effects were detected regarding bouts of leg-kicking. Bouts of anogenital sniffing, the frequency of mount attempts and mounting frequency were greater (P < 0.05) in the all-male group. Even though the frequency of raising the fat tail of females was similar between the two treatments, the mixed group tended to be (P = 0.08) more efficient in doing so than the all-male group (higher tail raising/mount). Results of the current study indicate that mixing groups of ram and ewe lambs before puberty may be insufficient to improve later sexual performance of ram lambs.