Comparison of Three 18F-Labeled Butyrophenone Neuroleptic Drugs in the Baboon Using Positron Emission Tomography

The butyrophenone neuroleptics spiroperidol, benperidol, and haloperidol were radiolabeled with fluorine-18 and studied in baboon brain using positron emission transaxial tomography (PETT). Pretreatment of the baboon with a high pharmacological dose of (+)-butaclamol reduced the specifically bound component of radioactivity distribution in the striatum to approximately the radioactivity distribution found in the cerebellum. Comparative studies of brain distribution kinetics over a 4-h period indicated that either [18F]spiroperidol or [18F]benperidol may be suitable for specific labeling of neuroleptic receptors. In an 8-h study with [18F]spiroperidol, striatal radioactivity did not decline, suggesting that spiroperidol either has a very slow dissociation rate or that it binds irreversibly to these receptors in vivo. [18F]Haloperidol may not be suitable for in vivo PETT studies, because of a relatively high component of nonspecific distribution and a faster dissociation from the receptor. Analysis of 18F in plasma after injection of [18F]spiroperidol indicated rapid metabolism to polar and acidic metabolites, with only 40% of the total radioactivity being present as unchanged drug after 30 min. Analysis of the metabolic stability of the radioactively labeled compound in rat striatum indicated that greater than 95% of [18F]spiroperidol remains unchanged after 4 h.     

Catalytic properties of the resolved flavoprotein and cytochrome B components of the NADPH dependent O2−• generating oxidase from human neutrophils

The resolved flavoprotein and cytochrome b₅₅₉ components of the NADPH dependent $\text{O}{}_2{}^{\mathrm{?}}{}_{\mathrm{?}}$ generating oxidase from human neutrophils were the subject of further study. The resolved flavoprotein, depleted of cytochrome b₅₅₉, was reduced by NADPH under anaerobic conditions and reoxidized by oxygen. NADPH dependent $\text{O}{}_2{}^{\mathrm{?}}{}_{\mathrm{?}}$ generation by the resolved flavoprotein fraction was not detectable, however it was competent in the transfer of electrons from NADPH to artificial electron acceptors. The resolved cytochrome b₅₅₉, depleted of flavoprotein, demonstrated no measureable NADPH dependent $\text{O}{}_2{}^{\mathrm{?}}{}_{\mathrm{?}}$ generating activity and was not reduced by NADPH under anaerobic conditions. The dithionite reduced form of the resolved cytochrome b₅₅₉ was rapidly oxidized by oxygen, as was the cytochrome b₅₅₉ in the intact oxidase.     

Differential subcellular localization of ACTH and α-MSH in corticotropes of the rat anterior pituitary

Summary Specific antisera to -melanotropin (-MSH) and corticotropin (ACTH 1-39) were used to obtain immunocytochemical evidence for the differential localization of -MSH and ACTH in the secretory granules of corticotropes of rat anterior pituitary. The specificity of the antisera was established by binding ¹³¹I-labeled -MSH and ACTH 1-39 to their respective antisera. Double-labeling immunocytochemistry (for -MSH, ferritin; for ACTH, colloidal gold) was performed. Some secretory granules were labeled with ferritin particles (-MSH), whereas others contained gold particles (ACTH). Only a few granules showed both ACTH and -MSH. In typical corticotropes (stellate in form with a small number of secretory granules aligned along the cell periphery) only some of the secretory granules that were labeled with anti-ACTH serum were also immunoreactive to anti--MSH. In atypical corticotropes (polygonal in shape and containing a large number of secretory granules) almost all of the immunoreactive ACTH secretory granules were also positive to anti--MSH serum. An intermediate type of corticotrope was observed containing a small number of secretory granules, almost all of which were labeled with anti--MSH. Thus, rat anterior pituitary corticotropes may be classified into three types according to the distribution and content of -MSH. The light-microscopic immuncytochemistry provided similar results.     

Levonorgestrel as a new radioligand for determination of sex hormone binding globulin in human plasma

Levonorgestrel which binds with high affinity to SHBG, is suggested as a new radioligand for estimation of SHBG in human plasma. Using 3H-levonorgestrel as a ligand, a number of samples from men, women pregnant and non-pregnant were analysed. The SHBG content was lowest in men, low in women and rose to higher level during pregnancy. The results of the present study suggest that levonorgestrel appears to be a better ligand than dihydrotestosterone for measuring SHBG.     

Epicuticular waxes from Agropyron dasystachyum,agropyron riparium and Agropyron elongatum

Epicuticular waxes from whole plants of Agropyron dasystachyum var. psammophylum, A. riparium and A. elongatum contain hydrocarbons (5–8 %), long chain esters (12–15%) and free acids (2–5%). The major esters are C₃₄C₅₆ esters derived from C₁₆C₃₀ acids and alcohols (1-hexacosanol is the major alcohol) but C₃₁, C₃₃ and C₃₅ esters (3–11%) are also present. The latter esters are C₁₈ and C₂₀ acid esters of C₁₃ and C₁₅ 2-alkanols. A. dasystachyum wax contains 2% free alcohols, that of A. riparium contains 17% and that of A. elongatum 11% (1-hexacosanol is the major alcohol in each). Diesters (2%), C₈C₁₂ diols esterified by (E)-2-alkenoic acids, are present in A. riparium wax. Hentriacontane-14,16-dione is present: 29% in A. dasystachyum wax and 32% in A. riparium wax, but only 5% in A. elongatum wax. 25-Oxohentriacontane-14,16-dione forms 14% of A. dasystachyum wax and 27% of A. elongatum wax but the oxo β-diketones of A. riparium wax (5%) consist of both 10-oxo- and 25-oxohentriacontane-14,16-diones in the ratio 4:1. Hydroxy β-diketones of the waxes are 25- and 26-hydroxyhentriacontane-14,16-diones; in A. dasystachyum (20%) the ratio is 3:1, in A. elongatum (20%) the ratio is 9:1 but in A. riparium (5%) it is ca 1:2. The configuration of the hydroxyl group in the 26-hydroxy β-diketone is opposite to that in the 25-hydroxy derivative. The unusual composition of the oxygenated β-diketones of A. riparium confirms that this species should be regarded as separate from A. dasystachyum. Wax from A. elongatum also contains 4-hydroxy-25-oxohentriacontane-14,16-dione (4%) and an unusual oxo-β-ketol, 18-hydroxy-7,16-hentriacontanedione (2%), both these components are probably derived biosynthetically from the 25-oxo β-diketone which is the major component of this wax. Syntheses of racemic 18-hydroxy-7,16-hentriacontanedione and of a model β-ketol, 12-hydroxy-10-pentacosanone, are described.     

Molecular evolution of pteridophytes and their relationship to seed plants: Evidence from complete 18S rRNA gene sequences

Complete 18S ribosomal RNA sequence data from representatives of all extant pteridophyte lineages together with RNA sequences from different seed plants were used to infer a molecular phylogeny of vascular plants that included all major land plant lineages. The molecular data indicate that lycopsids are monophyletic and are the earliest diverging group within the vascular land plants, whereasPsilotum nudum is more closely related to the seed plants than to other pteridophyte lineages. The phylogenetic trees based on maximum likelihood, parsimony and distance analyses show substantial agreement with the evolutionary relationships of land plants as interpreted from the fossil record.     

Archiascomycetes: detection of a major new lineage within the Ascomycota

For phylogenetic analysis of the higher fungi, we sequenced the nuclear small subunit rRNA (18S rRNA) gene fromTaphrina populina, the type species of the genusTaphrina, andProtomyces lactucae-debilis. The molecular phylogeny inferred from these 2 sequences and 75 sequences from the DNA data bank divided the Ascomycota into three major lineages: the hemiascomycetes, the euascomycetes, and the archiascomycetes, newly described herein. The former two lineages are monophyletic, whereas the archiascomycetes, which originated first and are comprised ofTaphrina, Protomyces, Saitoella, Schizosaccharomyces, andPneumocystis, may not be monophyletic. Among the archiascomycetes, theTaphrina/Protomyces branch is monophyletic. Confirmation of the archiascomycetes as a monophyletic taxonomic class will require comparison of additional genetically defined characters.This work was supported in part by grants 05454030 from the Ministry of Education, Science, and Culture of Japan (to J. S.) and 4369 from the Japan Society for the Promotion of Science Fellowship Programs (to H. N.).     

PCR检测HPV－18DNA

采用聚合酶链式反应（ＰＣＲ）技术,对ＨＰＶ－１８序列中引物ＨＰ＿１、ＨＰ＿２之间的片段（Ｆ）进行扩增,通过两组阴、阳性对照实验证明扩增片段的特异性。用不同Ｍｇ浓度的缓冲系统进行ＰＣＲ反应发现,缓冲系统中Ｍｇ浓度高低是影响ＨＰＶ－１８／ＨＰ＿１、ＨＰ＿２特异扩增的重要因素,高浓度Ｍｇ导致扩增特异性降低。对１７例宫颈癌组织ＤＮＡ进行ＰＣＲ检测,有９例检出Ｆ片段,其检出率是５３％,为ＨＰＶ－１８与宫颈癌的相关性提供证据。