Pituitary adenylate cyclase-activating polypeptide

Pituitary adenylate cyclase-activating polypeptide (PACAP) which belongs to the secretin/glucagon/ VIP family has been originally isolated from the sheep hypothalamus on the basis of its ability to stimulate cAMP formation in culture rat anterior pituitary cells. Post-translational processing of the PACAP precursor generates two biologically active molecular forms, PACAP-38 and PACAP-27. The primary structure of PACAP has been remarkably conserved during evolution. The sequence of PACAP-27 exhibits substantial similarities with those of vasoactive intestinal polypeptide (VIP), glucagon and secretin. The gene encoding the PACAP precursor is widely expressed in brain and various peripheral organs, notably in endocrine glands, gastro-intestinal, urogenital tracts and respiratory system. In vivo, and in vitro studies have shown that PACAP exhibits multiple activities especially a trophic activity during ontogenesis, notably in the adrenal medulla and the central nervous system. The biological effects of PACAP are mediated through three distinct receptor subtypes which exhibit differential affinities for PACAP and VIP. The PAC1 receptor, which shows high selectivity for PACAP, is coupled to several transduction systems. In contrast, VPAC1 and VPAC2, which bind with the same affinity for PACAP and VIP, are mainly coupled to the adenylyl cyclase pathway. In conclusion, PACAP is neuropeptide, and it functions as a hypothalamic hormone, neurohormone, neuromodulator, vasodilator, neurotransmitter or trophic factor in the brain and the various organs.

A taxonomic study of Oconnorella (Enchytraeidae, Oligochaeta) from Changbaishan Mountain, China

We describe three enchytraeid species, including two new species, from Mt. Changbaishan, Jilin Province, northeastern China. Oconnorella cheni sp. nov. is characterized by a simple spermatheca; absence of the oesophageal appendages and seminal vesicle; and nephridia from 6/7, with a distinct funnel and the efferent duct arising from the anterior part of the postseptale. Oconnorella globula sp. nov. is distinguished by a spermatheca with two diverticula; lack of oesophageal appendages and seminal vesicle; and nephridia from 6/7, with distinct funnel and the efferent duct arising from the mid-ventral or posteroventral part of the postseptale. We redescribe Oconnorella changbaishanensis (Xie et al., 2000) from type and live specimens, and amend some characters that cannot be investigated clearly from mounted specimens. We revise the generic diagnosis of Oconnorella.

Four new terrestrial species of Marionina (Clitellata, Enchytraeidae) from China and re-examination of M. hoVbaueri Moller

Enchytraeid surveys were made in China, mainly along the Changjiang (Yangtze) River Basin, during the period 1991-1999. Among the findings, four terrestrial species of Marionina are new to science and well illustrate the taxonomic complexity of the genus as currently defined. Marionina sinica sp. n. is characterized by a specific chaetal distribution, the marionine pattern of the dorsal blood vessel, and elongate, fusiform, spermathecal ectal ducts. Marionina sacculata sp. n. is distinguished by the possession of a pair of pouch-like oesophageal appendages in IV, the lack of lateral chaetae in VII-XI, a marionine pattern of the dorsal blood vessel, and short spermathecal ectal ducts gradually expanding into spherical ampullae. Both M. sinica and M. sacculata have minute bodies (2-3 mm long in vivo) and lack spermathecal accessory glands. The former species shows its closest aYnities with the European M. brendae Rota, 1995, whereas the latter is closest to the German M. hoVbaueri Moller, 1971, for which an amended diagnosis is provided. Marionina seminuda sp. n. has only ventral chaetal bundles, distributed from III onwards and bisetose. It is similar to the Holarctic M. subterranea (Knollner, 1935) in lacking entirely the lateral chaetae and in having the brain incised posteriorly, the dorsal vessel bifurcating behind the pharynx, and coelomocytes containing opaque granules, but diVers from it in having the longest chaetae in preclitellar segments and gland cells distributed all over the spermathecal ectal ducts. Marionina righiana sp. n. is diagnosed by the location of the head pore on the prostomium, the absence of lateral chaetae from VIII ( VII or IX) onwards, the possession of free spermathecae extending backwards through one to four segments, the brain deeply incised posteriorly, the lumbricilline pattern of the dorsal blood vessel, and the opacity of coelomocytes in vivo. Prior to this study, members of the genus so atypical as M. righiana with respect to the position of the head pore and the structure of the spermathecae were known only from South American soils. Until the taxonomy of Marionina has been more thoroughly assessed and revised, the assignment of the four species to this large assemblage should be regarded as tentative.

The freeliving nematode genus Parodontophora Timm 1963 (Nematoda : Axonolaimidae) is not exclusively marine: Parodontophora limnophila sp nov from freshwater in China

Parodontophora limnophila sp. nov. is described from Poyang Lake, the largest freshwater lake of China. It is characterized by having an amphid with its posterior end close to the base of the stoma, relatively short cephalic setae, opisthocephalic setae arranged as two subdorsal groups of three longitudinally arranged setae and two single subventral setae, excretory pore at the level of the anterior part of the stoma and renette gland 34-47% of the oesophageal length. To date, the new species is the only Parodontophora species found in freshwater habitats.

The development of long - Term ambulatory pH monitoring system and its clinical application

This paper introduced a long-term ambulatory intragastric pH monitoring system, which is designed for prolonged ambulatory studies of Gastroesophageal Reflux Diseases. The whole system is composed of the gastric catheter with two pH sensors, a small data logger (Microdatalog), and a notebook PC. In this paper, the design of monitoring system hardware and software are described in detail. Clinical applications reveal good results.

5-氟尿嘧啶-β-环糊精结肠靶向前体药物的研究

5-氟尿嘧啶(5-Fluorouracil， 5-FU)是一种抗代谢药物，广泛用于临床治疗结直肠癌、胃癌、乳腺癌等多种癌症，但其首过代谢显著、亲脂性较低，选择性差、毒副作用大。为克服这些缺点人们对5-FU进行了大量的修饰工作，包括小分子修饰以及与各种载体形成微球、微囊、纳米粒、共价前药等。 环糊精(Cyclodextrin，简称CD)，可被结肠中的糖苷酶特异性地降解成小分子糖，而胃和小肠中由于缺乏相应的酶而使环糊精不被降解，这一特性在结肠药物的靶向输送及释放中有重要应用价值。环糊精中含有丰富的羟基，易进行化学修饰，将药物与环糊精通过共价键结合制成前药，使其在胃和小肠中不降解，而在盲结肠中被特异性的酶降解释出药物，达到结肠靶向释药的目的。研究表明，环糊精作为一种前药载体为结肠靶向释药和缓释、控释系统提供了一种有效的手段。 本工作选择5-氟尿嘧啶为模型药物、β-环糊精作为载体，通过中间体5-FU羧酸衍生物的制备及其与β-环糊精的偶联，合成了系列5-FU-β-CD前体药物，并利用紫外、红外、质谱、核磁、元素分析、热分析等手段对其进行结构表征。同时，还研究了前体药物的体外释药性质。具体内容包括： 1. 含有羧基的5-FU衍生物中间体的合成：(5-氟尿嘧啶-1-基)-乙酸(FUAC)、3-(5-氟尿嘧啶-1-基)-丙酸(FUPC)、5-(5-氟尿嘧啶-1-基)-戊酸(FUVC)的合成。 2. 中间体5-FU的羧酸衍生物与β-CD的偶联：分别通过以6-OTs-β-CD为中间体的取代法和活化酯法，合成了第一面取代和第二面取代的5-FU-β-CD大分子前体药物。在二面取代的前体药物制备中，通过改变原料的比例，合成了系列不同取代度(DS)的2-[(5-氟尿嘧啶-1-基)-乙酰基] -β-环糊精结合物。 3. 对上述前体药物进行体外释放研究：分别考察了前体药物在不同pH缓冲溶液中的水解行为及其在小鼠胃肠道人工体液中的酶解行为，并通过UV-Vis及HPLC对前体药物释放情况进行检测分析。 5-Fluorouracil(5-Fu), commonly known as a broad-spectrum antineoplastic drug, has been widely used in the treatment of various kinds of cancer including colon cancer for 40 years. However, this antitumor agent exhibits serious adverse effects, such as their marrow toxicity, gastrointestinal reaction and low selectivity in their clinical use. In order to improve its antitumor activity and reduce its toxicity, the compound was modified in various ways, including the formation of conjugated prodrugs with kinds of carrier, microsphere and nanoparticles etc. Cyclodextrins(CDs) are known to be barely capable of being hydrolyzed and only slightly absorbed in passing through the stomach and small intestine; however they are fermented into small saccharides by colonic microflora and thus absorbed as small saccharides in the large intestine. This biodegradation property of CDs may be useful as a colon-targeting carrier, and thus CD prodrugs may serve as a source of site-specific delivery of drugs to colon. It was demonstrated that prodrugs of CDs can provide a versatile means for construction of not only colon targeted delivery systems, but also delayed release systems. 5-Fluorouracil was taken as a model drug and β-CD as the carrier in this study. Series prodrugs of 5-FU was prepared through the preparation of reactive 5-FU derivatives containing carboxyl group and coupling to hydroxyl groups of CD. The structures of the conjugates were charactered by using IR, UV–vis, ESI-MS, 1H, 13C-NMR spectra, elemental analyses, and thermal analysis. In vitro hydrolysis behavior in aqueous solution and in rat gastrointestinal tract contents of the conjugates were also investigated. The main content of this dissertation includes following aspects: 1. The preparation of 5-FU derivatives containing carboxyl group: 5-Fluorouracil- acetic acid(FUAC)、3-(5-FU-1)-propionic acid (FUPC)、and 5-(5-FU-1)-valeric acid(FUVC). 2. The coupling of 5-FU derivatives to β-CD: 5-FU was selectively conjugated onto the primary or secondary hydroxyl groups of β-CD through an ester linkage, by the substitution of 6-OTs-β-CD and the activated ester method respectively. For the secondary face conjugation, the degree of substitution(DS) can be controlled by changing the mole ratio of the starting materials(FUAC and β-CD). 3. In vitro release behavior of the conjugates in aqueous solution and in rat gastro- intestinal tract contents of the conjugates were investigated, and the reaction was monitored and analyzed by using UV-Vis and HPLC methods.

N,N,N ',N '-Tetramethylchloroformamidinium Chloride-Mediated Cyclizations of beta-Oxo Amides: Facile and Divergent One-Pot Synthesis of Substituted 2H-Pyrans, 4H-Pyrans and Pyridin-2(1H)-ones

An efficient and divergent one-pot synthesis of substituted 2H-pyrans, 4H-pyrans and pyridin-2(1H)-ones from beta-oxo amides based on the selection of the reaction conditions is reported. Mediated by N,N,N',N'-tetramethylchloroformamidinium chloride, beta-oxo amides underwent intermolecular cyclizations in the presence of triethylamine at room temperature to give substituted 2H-pyrans in high yields, which could be converted into substituted 4H-pyrans in the presence of sodium hydroxide in ethanol at room temperature, or into substituted pyridin-2(1H)-ones under reflux.

A Facile and Practical One-Pot Synthesis of beta-Oxo Thioamides from beta-Oxo Amides and Isothiocyanates

A facile and practical one-pot synthesis of beta-oxo thioamides from beta-oxo amides has been developed. By treatment with isothiocyanates in ethanol in the presence of potassium carbonate, a series of beta-oxo amides was converted, under reflux, in high yields into the corresponding beta-oxo thioamides.

Effects of ultrahigh pressure extraction conditions on yields and antioxidant activity of ginsenoside from ginseng

Ultrahigh pressure technique was employed to extract ginsenosides from roots of ginseng (Panax ginseng C.A. Meyer). The optimal conditions for ultrahigh pressure extraction (UPE) of total ginsenosides were quantified by UV-vis spectrophotometry with the ginsenoside Re as standard, the signal ginsenosides were quantified by HPLC and ELSD with ginsenosides Re, Rg(1), Rb-1, Rc and Rb-2 as standards. Orthogonal design was applied to evaluate the effects of four independent factors (extraction pressure, extraction temperature, extraction time and ethanol concentration) on the yield and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity of ginsenoside, which are based on microwave extraction (ME), ultrasound extraction (UE), soxhlet extraction (SE) and heat reflux extraction (HRE) method. The results showed that UPE method can produce ginsenoside with the highest yield and the best radical scavenging activity compared to other used ones. Scanning electron microscopic (SEM) images of the plant cells after ultrahigh pressure treatment was obtained to provide visual evidence of the disruption effect.

塔里木盆地塔北、塔中地区早古生代白云岩形成机理

In Tarim Basin, extensive carbonates of Lower Paleozoic occur, in which thick Cambrian and Lower Ordovician dolostones are widespread and show a potential perspective in hydrocarbon exploration. So they are viewed as an important target for exploration. Tarim Basin is a poly phase composite basin, which underwent multiphase tectonic modification and volcanic activities; these exerted significant influences on the basin-fills and basin fluid evolution, thereby the diagenetic history, particularly on the deep-buried Lower Paleozoic dolostones. Referring to the classification of dolomite texture proposed by Gregg & Sibley (1984) and Sibley & Gregg (1987). In view of crystal size, crystal shape, crystal surface and contact relation, eight genetic textures of dolomite crystals are identified, based on careful petrographic examinatoins. These textures include: 1) micritic dolomite; 2) relict mimetic dolomite; 3)finely crystalline, planar-e(s), floating dolomite; 4)finely crystalline, planar-e(s) dolomite; 5) finely-coarse crystalline, nonplanar-a dolomite; 6)coarse crystalline, nonplanar saddle dolomite; 7) finely-medium crystalline, planar-e(s) dolomite cement; 8) coarse crystalline, nonplanar saddle dolomite cement, in which the former six textures occurs as in matrix, the latter two in the cements. Detailed geochemistry analysis is carried out on the basis of genetic textures of dolomite and related minerals such as quartz and calcite. The result showed that the calcite has the highest average content in Sr, which can be sorted into two groups; micritic dolomite has the highest average content in Sr among all kinds of dolomites; the REE patterns of all kinds of dolomites is similar to those of marine limestone samples. Saddle dolomite cement has δ13C values from -2.44‰ to 1.27‰ PDB, and δ18O values from -13.01‰ to -5.12‰ PDB, which partially overlap with those of matrix dolomite (δ13C values from -2.83‰ to 2.01‰ PDB, δ18O values from -10.63‰ to -0.85‰ PDB). Saddle dolomite cement has 87Sr/86Sr ratios from 0.7086 to 0.7104, which totally overlap with those of matrix dolomite (0.7084 ~ 0.7116). Compared with saddle dolomite derived from other basins all over the world, the saddle dolomites of Tarim Basin have similar δ13C, δ18O and 87Sr/86Sr ratios values with those of matrix dolomite. This scenario reflects the unusual geological setting and special dolomitizing liquid of Tarim Basin. The values of δ18O, δ13C and 87Sr/86Sr ratios of calcite also can be sorted out two groups, which may been resulted from the one stage of extensive uplift of Tarim Basin from Mesozoic to Cenozoic. Fluid inclusion microthermometry data of the diagenetic mineral indicates that matrix dolomite has relatively low homogenization temperatures (Th) of 80～105oC and salinities of 12.3％ (wt% NaCl equivalent); saddle dolomite has highest Th values, which concentrate in 120～160oC and salinities of 13.5～23.7％ (wt% NaCl equivalent); quartz has relatively low Th of 135～155oC and salinities of 17.8～22.5％ (wt% NaCl equivalent); calcite has relatively low Th of 121～159.5oC and salinities of 1.4～17.5％ (wt% NaCl equivalent). These data suggest that the saddle dolomites could have formed in thermal brine fluids. Based on comprehensive petrographical study, detailed geochemistry and fluid inclusion microthermometry analysis on Lower Paleozoic dolomite of Tarim Basin, three types of dolomitisation mechanism are proposed: Penecontemporaneous dolomitisation (Sabkha dolomitisation & Reflux dolomitisation); Burial dolomitisation (shallow-intermediate burial dolomitisation & Deep burial dolomitisation ); Hydrothermal cannibalized dolomitisation. In view of host-specified occurrences of hydrothermal dolomite, the low abundance of saddle dolomite and high geochemical similarities between saddle dolomite and host dolomite, as well as highest Th and high salinities , the hydrothermal dolomite in Tarim Basin is thus unique, which could have been precipitated in modified fluid in the host dolomite through intraformational thermal fluid cannibalization of Mg ions from the host. This scenario is different from the cases that large scale dolomitizing fluid migration took place along the fluid pathways where abundant saddle dolomite precipitated. Detailed observations on 180 petrographic and 60 casting thin sections show original pores in Lower Paleozoic dolomite were almost died out by complicated diagenetic process after a long time geologic evolution. On the other hand, deep-buried dolomite reservoirs is formed by tectonic and hydrothermal reforming on initial dolomites. Therefore, the distribution of structure-controlled hydrothermal dolomite reservoirs is predicted in Tabei and Tazhong Area of Tarim Basin based on the geophysical data.