A prodrug approach towards the development of tricyclic-based FBPase inhibitors

For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug 4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug 20, which strongly inhibited glucose production in monkey hepatocytes and also showed weak CYP3A4 inhibitory potency.     

Structure and diversity of remnant natural evergreen broad-leaved forests at three sites affected by urbanization in Chongqing metropolis,Southwest China

Evergreen broad-leaved forests (EBLFs, lucidophyllous forests) are vegetation types characteristic of East Asia. The extent of EBLFs has decreased significantly due to long-term anthropogenic disturbance, and remnant EBLFs in urban area are rare and important landscape types contributing to biodiversity and sustainable development. This study focuses on remnant EBLFs on Mt. Gele (GL), Mt. Tieshanping (TSP), and Mt. Jinyun (JY), located from the inner city to outskirts of Chongqing metropolis, Southwest China. Species of Theaceae, Lauraceae, Symplocaceae, and other families, which are essential floristic components of primary EBLFs, were still the main components at the three sites. GL and JY showed higher biodiversity, with richer heliophytes and shade-tolerant species, respectively. Castanopsis carlesii var. spinulosa was the sole dominant species at all three sites in woody layer, with codomination by Pinus massoniana and Cinnamomum camphora at GL and by Machilus pingii and Castanopsis fargesii at JY; these evergreen broad-leaved trees all showed inverse-J or sporadic-shaped size distribution with large numbers of small stems, but the conifer tree Pinus massoniana showed unimodal distribution with small stems at GL. The height growth of tree species, especially Castanopsis carlesii var. spinulosa, was increasingly restricted from JY to TSP to GL. Sprouting is an important life history strategy at community and population level, and differences were exhibited from GL to TSP to JY. A rural–urban gradient from JY to TSP to GL was indicated in this study. Species composition, biodiversity, and stand structure of these remnant EBLFs showed obvious differences along this gradient, and conservation responses to address the effects of urbanization need to be carefully considered.     

Cloning and characterization of a novel gene cry9Ec1 encoding lepidopteran-specific parasporal inclusion protein from a Bacillus thuringiensis serovar galleriae strain

A novel delta-endotoxin gene from a lepidopteran-specific Bacillus thuringiensis serovar galleriae strain was cloned, and the full sequence of the cry gene was determined. The cloned 6.5-kb DNA fragment included the full sequence of the cry gene and three open reading frames located upstream of the cry gene. The gene, designated cry9Ec1, encodes a polypeptide of 1154 amino acid residues with a predicted molecular weight of 130 237. The deduced amino acid sequence of the Cry9Ec1 protein had the highest homology (77.7%) with the Cry9Ea1 protein when compared with existing Cry proteins. The expression, in an acrystalliferous B. thuringiensis strain, of the cry9Ec1 gene was high when controlled by the cyt1A2 promoter, leading to the formation of large spherical inclusions. The purified crystals from the recombinant strain were toxic when tested against two lepidopteran species, Bombyx mori and Plutella xylostella. However, the Cry9Ec1 protein gave no toxicity against Spodoptera litura, Spodoptera exigua, Plodia interpunctella, Helicoverpa zea, and Culex pipiens molestus.     

Sterol utilization in honey bees fed a synthetic diet: Effects on brood rearing

The dietary sterols, cholesterol, campesterol, sitosterol, stigmasterol and 24-methylenecholesterol, were tested for their ability to support brood rearing in the honey bee, Apis mellifera L., by adding them singly to a chemically-defined worker bee diet. Diet supplemented with 24-methylenecholesterol supported the greatest survival of worker bees, but diet supplemented with either 24-methylenecholesterol or cholesterol supported the production of nearly equivalent amounts of sealed brood and more than any of the other three sterols tested. Diets containing stigmasterol, sitosterol, campesterol, or no supplement produced less sealed brood, in decreasing order.     

Seroepidemiological survey for antibody to Borrelia burgdorferi in cows.

Antibody to Borrelia burgdorferi was examined in 380 healthy and 38 clinical cases of cows from Hokkaido and Shizuoka in Japan. In healthy animals, IgG and IgM antibody to B. burgdorferi HO14 strain were found in 44 cows (14.6%) and 24 cows (8.0%) from Hokkaido. In contrast, antibody-positive case was not observed except for only 1 case which was IgM positive (1/79: 1.3%) in cows from Shizuoka. Mean antibody levels of healthy animals in Hokkaido and Shizuoka were 0.651 and 0.263 (IgG antibody to HO14 strain), 0.642 and 0.169 (IgG to HP3 strain), 0.613 and 0.367 (IgM to HO14 strain) and 0.582 and 0.286 (IgM to HP3 strain). The differences of the antibody levels between cows from Hokkaido and Shizuoka were significant. Seasonal difference was found in seropositive cows from Hokkaido. The rate of seropositive cows was high in summer (23.4% in June and 11.8% in July) but low in winter (0% in January and February). The pattern was discussed to be associated with activation of ticks. One of 4 cows with arthritis showed significantly higher IgG antibody level than that of healthy cows and cows with some disease, although the serum was collected from Shizuoka where antibody-positive animals for B. burgdorferi were rare among healthy cows. This high IgG antibody may suggest that the arthritis of such cows was caused by infection with B. burgdorferi. Two of 7 cows with unclassified abortion showed positive antibody reaction in Hokkaido. These cases, however, may not be related to the B. burgdorferi infection because the positive rate was similar to those of healthy cows in the same season.     

Redescription of Dendrochirus zebra (Scorpaenidae: Pteroinae) with a new species of Dendrochirus from the Ogasawara Islands,Japan

Ichthyological Research - Dendrochirus zebra (Cuvier in Cuvier and Valenciennes 1829) (Scorpaenidae: Pteroinae) is redescribed on the basis of 405 specimens from the Indo-West Pacific region. The...