Assessment of novel inhibitors of Helicoverpa aminopeptidases as anti-insect agents

Helicoverpa species present problems worldwide as pests on a variety of agricultural crops. In Australia, the costs of controlling H. armigera (Hübn.) and H. punctigera (Wall.) are a major burden on the cotton industry, and novel mechanisms are continually sought to combat these pests. Potential new targets for insecticides are the digestive proteases of the insect, including the aminopeptidases (APs). A variety of compounds, designed to be similar in structure to known AP inhibitors, were synthesized and screened for activity in inhibiting H. armigera larval growth and AP activity. The most effective compounds in both assays proved to be hydroxamic acids and methylphosphonic acids. Compounds that incorporated both of these groups were also found to have significant potential as control agents. The most inhibitory compounds included valine methylphosphonic acid and a leucine methylphosphonic acid/hydroxamic acid derivative. The valine methylphosphonic acid compound was tested further in vitro, with the aim of producing a new active capable of restricting the viability of Helicoverpa populations on commercial crops.     

Impact of controlled fermentation and steeping of high moisture corn on its nutritional value for pigs

High moisture corn (HMC) can undergo fermentation during storage that may improve its nutritional value for pigs. Stored HMC used in this study contained (n = 4) 75% dry matter (DM), and, on a DM basis, 63.8% starch, 0.5% mono and disaccharides, 9.9% protein, 19 mM acetic acid, 18 mM lactic acid (LA), 1.25 × 10⁷ cfu g^− 1 of LA producing bacteria, 2.88 g kg^− 1 total phosphorus (P), and 1.26 g kg^− 1 soluble P. The soluble P content was higher than in freshly harvested HMC (0.27 g kg^− 1 DM) and indicates P release during storage. Studies were aimed at altering the nutritional value of stored HMC by controlled fermentation or steeping. Changes in LA content were not affected (P > 0.05) by addition of exogenous Lactobacillus and Bacillus bacteria. Steeping of HMC with phytase (Ronozyme) was examined at four inclusion levels (0, 500, 750, 1000 FTU kg^− 1) and at either 21 °C or 37 °C. At 37 °C added phytase released virtually all phytate P within 6 h irrespective of the level (levels increased by 1.44 g P kg^− 1 DM); at 21 °C, the increase was maximized at 1.2 g P kg^− 1 DM after 24 h. The feeding value of HMC for pigs can be altered by steeping with exogenous phytase and does not appear to require microbial inoculants.     

日粮中添加植酸酶和锌对断奶仔猪生产性能及其组织锌浓度的影响

通过三个试验测定日粮中植酸酶、过量的锌及两者共同对哺乳仔猪的影响。在所有的试验中,每个处理组有5～7栏,每栏有6～7头猪,当日粮中添加植酸酶时,则日粮中钙和有效磷的水平降低0.1%,锌是通过氧化锌的形式添加,试验日粮中含锌水平均为127mg/kg,本试验的周期为19～21d。在试验1中,试验采用2×3因子试验设计,两个水平的植酸酶(即0和500植酸酶单位/kg)和三水平过量的锌(即0,1000和2000mg/kg)。仔猪(5.7kg和18日龄)被随机分配采食以上日粮。试验表明,平均日增重(ADG)和平均日采食量(ADFI)随日粮中锌含量的增加而线性增加,第一阶段为(P=0.01～0.06),第二阶段为(P=0.02～0.09),整个试验阶段为(P=0.01～0.02),肉料比(G∶F)也随日粮锌含量的增加而线性增加,但仅限于第一阶段(P=0.01)。当仔猪采食1000或2000mg/kg锌时的同时添加植酸酶可降低第二阶段ADG(锌与植酸酶互作;P=0.10),但对整个试验周期内ADFI没有影响(P=0.27～0.62),并可降低第二阶段G∶F(P=0.01),及整个试验周期内G∶F(P=0.07)。随着日粮锌添加量的增加,血浆中锌含量也随之增加(Zn2,P=0.01),并且不受植酸酶添加的影响(P=0.70)。在试验2中,试验采用2×2因子试验设计,两个水平的植酸酶(即0和500植酸酶单位/kg)和两水平过量的锌(即0和2000mg/kg)。仔猪(5.2kg和18日龄)被随机分配采食以上日粮。试验表明,日粮中锌含量的增加可使第二阶段ADG和肉料比增加(P=0.02～0.09)和整个试验阶段的ADG和G∶F增加(P=0.07～0.08),但对第一阶段ADG和整个试验阶段ADFI的变化没有影响。植酸酶的添加可增加第二阶段ADG(P=0.06)和G∶F(P=0.01)。当仔猪采食2000mg/kgZn和植酸酶时,G∶F值最大(锌与植酸酶互作;P=0.01)。骨(20日龄)中锌和血浆锌(7和20日龄)随着日粮中锌的添加量的增加而增加(P=0.01),但不受植酸酶添加的影响(P=0.51～0.90)。在试验3中,仔猪(5.7kg和19日龄)被随机分配采食添加500植酸酶单位/kg的植酸酶或不添加植酸酶的基础日粮或添加500植酸酶单位/kg的植酸酶或不添加植酸酶且钙和有效磷含量降低0.10%的基础日粮。试验表明,植酸酶的添加对仔猪生产性能没有影响(P=0.21～0.81)。降低钙和有效磷的含量,可降低整个试验周期内ADG,ADFI和G∶F(P=0.02～0.08)。这些试验结果表明,日粮中添加过量的锌可增加ADG及血浆和骨中锌的浓度。日粮中植酸酶对血浆和骨中锌的浓度没有影响。     

Dirlotapide: a review of its properties and role in the management of obesity in dogs

Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor developed specifically for canine weight reduction. MTP catalyzes the assembly of triglyceride-rich apolipoprotein-B containing lipoproteins to form chylomicrons in the intestinal mucosa and very low-density lipoproteins in the liver. Following oral administration, dirlotapide has in vivo selectivity for intestinal MTP compared with hepatic MTP. In addition to reducing intestinal fat absorption, dirlotapide also reduces food intake in a dose-dependent manner, probably via increased release of peptide YY into the circulation. The decrease in food intake is responsible for the majority of the weight reduction effect. In clinical use, it is recommended to adjust the dose according to the observed weight loss of each individual. The initial dose of 0.05 mg/kg is doubled after 14 days and then adjusted monthly, the maximum permitted daily dose is 1.0 mg/kg, although doses as high as 10 mg/kg have been administered to dogs without severe adverse experience in safety studies. Dirlotapide can be used without necessitating changes to the current feeding or exercise regimens, but it is desirable to monitor the food intake during weight-stabilization to establish revised feeding and exercise routines that will minimize the risk of weight regain post-treatment. The drug offers a novel approach that is applicable in cases where dietary management alone has proved to be unsuccessful.     

Evaluation of turnip-rooted parsley (Petroselinum crispum ssp. tuberosum) for root and foliage production under a warm,Mediterranean climate

Two experiments were undertaken in southern Greece during 2000–2002 in which turnip-rooted parsley was tested for its suitability for cultivation in comparison with locally grown curly-leafed and plain-leafed forms. Plants were harvested when the foliage was acceptable for marketing, rather than on completion of the vegetative cycle, hence root size was relatively small. In year 1, the foliage development of plain-leafed parsley was significantly higher than that of the other two forms, irrespective of sowing date. In year 2, both plain-leafed and curly-leafed parsley produced more foliage than turnip-rooted parsley in the early sowing (November), but not in subsequent sowings (December and February). During both years, root development was higher in turnip-rooted parsley than in curly-leafed parsley, although in the November and February sowings of year 1 the root weight of both plain-leafed and turnip-rooted forms were similar. In all three types of parsley, foliage yield fell off significantly in the spring sowing (February), and in year 1 there was a considerable decrease in root production as well. In most cultivars, foliage weight was higher when plants were grown from transplanted seedlings rather than by direct sowing, whereas the effect of sowing method on root weight was sowing date dependent. Cultivar differences in the foliage weight of direct sown and transplanted plants were reflected by differences in plant height and, in some cases, by leaf number. It is concluded that although overall turnip-rooted parsley produced rather less foliage than that plain-leafed parsley, this was compensated for by the satisfactory production of roots and therefore turnip-rooted cultivars may constitute a suitable crop for introduction to the Mediterranean region.     

The subchondral split line patterns of the medial coronoid process in canine ulnae

The subchondral split line patterns of the canine medial coronoid process (MCP) were compared with fragmentation line patterns of the MCP in case of elbow dysplasia. Split line patterns were determined in paired ulnae from the killed 26 large-breed dogs ranging in age between 0.8 and 15 years and in two ulnae affected by fragmentation of the MCP. The macerated ulnae were degreased with methylene chloride and decalcified in 5% nitric acid. The subchondral bony layer was pierced at right angles in regular intervals using a round needle that was dipped in black liquid acrylic colour. Three main types of split line patterns could be differentiated (i.e. a sagittal type, a transverse type and an intermediate type). In the sagittal type, split lines were aligned in parallel to the lateral border and at right angles to the rim of the tip and medial border of the MCP. In the transverse type, split lines were orientated in a transverse line to both collateral borders. The intermediate type was characterized as a transition type between sagittal and transverse type as the split lines were aligned obliquely to the longitudinal axis of the MCP. These three types corresponded well with the fissure and fragmentation line patterns of the MCP. The present findings strongly suggest an association between split line pattern and type of fragmentation of the MCP.     

A morphometric investigation on breed-specific features affecting sagittal rotational and lateral bending mobility in the canine cervical spine (c3-c7)

Vertebral and inter-vertebral parameters obtained in large breeds (n = 74), small breeds (n = 35), and Dachshunds (n = 30) were compared to reveal potential differences in the range of motion of the cervical spine between these three groups of breeds. Body size normalized dimensions of vertebral and inter-vertebral parameters and correlations between these indicate large canine breeds to have a tendency towards higher range of motion in sagittal rotation and lateral bending compared with Dachshunds and small breeds. Higher mobility in large breeds is based on significantly (P < 0.05) lower vertebral endplate heights and widths, shorter vertebral bodies and longer inter-vertebral discs, wider but shorter cranial and caudal articular surfaces, larger differences in width between caudal and cranial joining facets (compared with Dachshunds from C3/4 to C6/7, compared with small breeds from C4/5 to C5/6), and larger differences in length between caudal and cranial joining facets. Large differences in width between caudal and cranial joining facets were associated with small distances between the most medial (C3/4 to C6/7) and lateral (C3/4 to C5/6) aspects of the articular surfaces as well as with small differences in length between caudal and cranial joining facets (C3/4 to C5/6). This suggests that from C3/4 to C5/6 a higher range of motion in lateral bending is coupled to a lower range of motion in sagittal rotation. The present findings contribute also to explain the higher incidence of degenerative lesions of the cervical spine in large dogs.