Morphological Features and Hatching Patterns of Eggs in Acartia Steueri (Crustacea, Copepoda) from Sagami Bay, Japan

Morphology, production rate and hatching success of the eggs spawned by Acartia steueri from Sagami Bay, Japan were examined from November 2000 to December 2001. A. steueri produced two morphological types of egg. One with a smooth surface (smooth egg) and the other with branched spines on the envelope (spiny egg). Abundance of adult A. steueri increased from April to June 2001, and then decreased from July 2001. Adult A. steueri were low in abundance between August and October 2001, then increased in November 2001. Smooth eggs were produced through out the study period, while spiny eggs were produced during restricted periods from March to July 2001. Six of thirteen females produced both smooth and spiny eggs within 24 h. All the smooth eggs hatched within 48 h, like the so-called subitaneous eggs. Spiny eggs that did not hatch within the time determined by the Bělehrádek's temperature function of egg development time plus 24 h were categorized as diapausing eggs. In the present study, A. steueri seems to survive by utilizing egg dormancy during the period of environmental adversity, and produced two physiologically different types of eggs. This may be why A. steueri dominants in temperate coastal waters where environmental conditions vary drastically.     

Discovery of sympatric cryptic species within Gekko hokouensis (Gekkonidae: Squamata) from the Okinawa Islands, Japan, by use of allozyme data

An electrophoretic survey of samples of the gekkonid lizard, Gekko hokouensis , from the East Asian islands demonstrated that two genetically divergent, but morphologically almost identical, entities occur on five islands of the Okinawa Group, Ryukyu Archipelago, Japan. These entities, while sharing all of the external character states diagnostic of G. hokouensis , exhibited fixed allele differences at six to eight out of 30 loci examined and great overall genetic distances [ Nei's (1978) D  = 0.489–0.654]. On Kumejima and Tonakijima Islands of the Okinawa Group, the two entities were collected together from identical microhabitats. These results indicate that the two entities represent separate biological species. Genetic comparisons of these two cryptic species from the Okinawa Group with ' G. hokouensis ' from other island groups revealed that one occurs broadly in the insular region of East Asia, whereas the other is restricted to the Okinawa Group. Implications of the present findings for the morphological evolution of ' G. hokouensis ' are also discussed.     

Effects of clear-cutting and burning on characteristics of nitrogen mineralization and microbes in the forest soil of a Pinus massoniana plantation in Southern China

The aim of this study was to clarify the effects of clear-cutting and burning (CCB) on soil fertility in a Pinus massoniana (Masson pine) plantation after CCB in Fujian Province, China. We investigated changes in nitrogen (N) mineralization potential (N₀), N mineralization rate constant (k) and the apparent activation energy (Ea) of the soil, with a mathematical analysis using a kinetics model based on the results of in vitro incubation. Changes in the amount of microbial biomass nitrogen (MBN), as well as the number of heterotrophic and nitrite-oxidizing bacteria, were also investigated. The N₀, MBN and the number of fungi and actinomycetes in forest soil was reduced for at least 18 months after CCB. The number of heterotrophic and nitrite-oxidizing bacteria increased, and k, Ea and N mineralization became greater after 6 months of CCB, compared with the control plots. Because there were few young trees planted, which would have taken up mineralized N in the post-CCB site, it is probable that a high proportion of the mineralized N that accumulated in the soil may have been lost during the summer rainy season. Therefore, it is suggested that CCB led to a deficiency in available N during short rotations, which resulted in soil degradation.     

Structures and inclusion properties of racemic and enantiopure dimethyl and diphenyl 9,9'-bianthryl-2,2'-dicarboxylates

The authors prepared the dimethyl and diphenyl esters of 9,9'-bianthryl-2,2'-dicarboxylic acid in racemic and enantiopure (M) forms. The enantiopure dimethyl ester forms inclusion compounds with various organic compounds such as benzene, methanol, phenol, and aniline whereas the racemic form does this only with benzene. No guest molecules are included by the racemic and enantiopure diphenyl esters. These effects of substituents and homochirality on the inclusion properties are discussed on the basis of X-ray structures of some inclusion and guest-free compounds.     

Structural requirements for the stability of novel cephalosporins to AmpC beta-lactamase based on 3D-structure

AmpC beta-lactamase is one of the leading causes of Pseudomonas aeruginosa (P. aeruginosa) resistance to cephalosporins. FR259647 is a cephalosporin having a novel pyrazolium substituent at the 3-position and exhibits excellent activity (MIC=1 microg/mL) against the AmpC beta-lactamase overproducing P. aeruginosa FP1380 strain in comparison with the third-generation cephalosporins FK518 [Abstracts of Papers, 30th Interscience Conference on Antimicrobial Agents and Chemotherapy, Atlanta, GA, October 21-24, 1990, Abs. 454; Abstracts of Papers, 30th Interscience Conference on Antimicrobial Agents and Chemotherapy, Atlanta, GA, October 21-24, 1990, Abs. 455; Abstracts of Papers, 30th Interscience Conference on Antimicrobial Agents and Chemotherapy, Atlanta, GA, October 21-24, 1990, Abs. 456; Abstracts of Papers, 30th Interscience Conference on Antimicrobial Agents and Chemotherapy, Atlanta, GA, October 21-24, 1990, Abs. 457] (MIC=16 microg/mL) and ceftazidime (CAZ) (MIC=128 microg/mL). The stability of FR259647 and FK518 to AmpC beta-lactamase was evaluated using MIC assays against both the P. aeruginosa PAO1 strain and a PAO1 mutant strain overproducing AmpC beta-lactamase as a differential assay, which indicates that the main difference derives from their stability to AmpC beta-lactamase. A structural analysis using computer simulations indicated that the difference in stability may be due to steric hindrance of the 3-position substituents causing differential affinity. This steric hindrance may disturb entry of the cephalosporins into the binding pocket. We predicted the possibility of inhibition of entry as a potential means of enhancing stability by conformational analysis. In order to validate this speculation, novel FR259647 derivatives 4-9 were designed, calculated, synthesized, and evaluated. As a result, we demonstrated that their probability of entry correlated with the MIC ratio of the mutant strain to the parent strain and supports the validity of our model.     

Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action

In this study, a novel series of CB(2) receptor agonist imine derivatives, 1-6, was synthesized and evaluated for activity against the CB(2) receptor. In a previous paper we reported the synthesis and SARs of thiazole derivative 1, a potent CB(2) receptor agonist, but we had not assessed chemical modifications of the 5-membered heteroring of 1. In the present study, we therefore tried chemically modifying the 5-membered heteroring of 1 in an attempt to further improve binding affinity for the CB(2) receptor. In the course of making the structural modifications, we discovered that a novel pyrazole derivative 6b (CBS0550) had high affinity for the CB(2) receptor (IC(50)=2.9 nM, EC(50)=1.8 nM, E(max)=85%), high selectivity for CB(2) (CB(1) IC(50)/CB(2) IC(50)=1400), and good physicochemical properties (solubility in water: 5.9 mg/100mL at 25 degrees C). Oral administration of 6b to rats at a dose of 10mg/kg resulted in significant plasma concentrations, and orally administered compound 6b significantly reversed mechanical hyperalgesia in the Randall-Selitto model of inflammatory pain in rats.     

Kinetic parameters and recognition of thymidine analogues with varying functional groups by thymidine phosphorylase

Thymidine phosphorylase (TP, EC 2.4.2.4) recognized the structure of the substrate with high specificity, via both the base and the ribosyl moieties. The replacement of 3'-OH of thymidine markedly influenced its catalytic activity with TP. The conversion of pyrimidine nucleosides with modified base moieties to the corresponding 1-phosphate form was poor. The leaving group activity decreased with an increase in aromaticity of the pyrimidine base moiety, because of increased difficulty in polarizing the base by the amino acids local to the active site. The replacement of 3' and 5' functional groups tended to decrease the reaction rate and the percentage conversion with TP. In particular the ribosyl 3' hydroxyl group was structurally important for the binding of the substrate by the enzyme. The kinetic assay clearly showed high K(m) and low V(max) values on replacing the 3' hydroxyl group with hydrogen.     

6-Shogaol and 6-gingerol, the pungent of ginger, inhibit TNF-alpha mediated downregulation of adiponectin expression via different mechanisms in 3T3-L1 adipocytes

In this study, we demonstrated that the two ginger-derived components have a potent and unique pharmacological function in 3T3-L1 adipocytes via different mechanisms. Both pretreatment of 6-shogaol (6S) and 6-gingerol (6G) significantly inhibited the tumor necrosis factor-α (TNF-α) mediated downregulation of the adiponectin expression in 3T3-L1 adipocytes. Our study demonstrate that (1) 6S functions as a PPARγ agonist with its inhibitory mechanism due to the PPARγ transactivation, and (2) 6G is not a PPARγ agonist, but it is an effective inhibitor of TNF-α induced c-Jun-NH₂-terminal kinase signaling activation and thus, its inhibitory mechanism is due to this inhibitory effect.     

The evolutionary history and taxonomic reevaluation of the Japanese coral snake,Sinomicrurus japonicus (Serpentes,Elapidae), endemic to the Ryukyu Archipelago,Japan, by use of molecular and morphological analyses

Sinomicrurus japonicus has a conspicuous colour pattern of longitudinal black stripes and transverse sets of black and white bands with an orange‐reddish background colour. The pattern varies markedly among island populations, and thus, three subspecies have been recognized. We conducted molecular phylogenetic analyses on the island populations to clarify the evolutionary trajectory of such colour patterns and reevaluate the current classification accordingly. The results indicated relatively deep allopatric divergences within S. j. boettgeri, paraphyly of S. j. boettgeri against other two subspecies, and two independent derivations of S. j. takarai from boettgeri‐like ancestors. Detailed morphological analyses revealed that variations in the boettgeri and takarai forms were more or less continuous and that differences between the two takarai populations were very small. From these results, we propose synonymizing S. j. takarai with S. j. boettgeri. Morphological differences between the genetically most distant populations of S. j. boettgeri were also small, whereas the japonicus form was distinct from the remainder. Considering the possible evolution of S. j. japonicus through peripheral isolation, we propose retention of these two subspecies. This study provides a basis for future work on the adaptive significance of geographic variation in the colour pattern of S. japonicus.