bluuebunny/crossref_metadata_2025 huggingface dataset:
Australian biodiversity via its plants and marine organisms. A high-throughput screening approach to drug discovery
Authors: Quinn Ronald J. , de Almeida Leone Priscila , Guymer Gordon , Hooper John N. A.
Published: October 2007

High-throughput screening (HTS) of extracts of Australian plants and marine organisms commenced in our laboratory in 1994. The biota collections commenced in late 1993. The collection has in excess of 30 000 biota samples including over 16 000 biota samples of vascular plants, algae, and macro fungi from Queensland, and over 4000 marine invertebrates from Australian waters. The plant collection represents ∼9 % of the world species diversity of higher plants, with representation from 73 % of the world's plant families. The marine collection contains ∼10 % of the world diversity of sponges, ∼10 % of the world diversity of ascidians, and ∼5 % of the world diversity of soft corals and gorgonians.

The lecture will highlight some of the advances to knowledge about Australian biodiversity as a result of the HTS project, discuss drug discovery using HTS, and give some examples of the chemistry arising from the screening of the extracts.
Aromatic biodiversity among the flowering plant taxa of Turkey
Authors: Baser K. Hüsnü Can
Published: October 2007

Flora of Turkey is rich and diverse with well over 11 000 flowering taxa recorded in the 9-volume set of Prof. Davis's monumental work and its two supplements. Chemical diversity among the flowering plants of Turkey is well documented in the recently published volume 11 of the Flora of Turkey and the East Aegean Islands.

Among the aromatic taxa, remarkable examples can be found in families such as Labiatae, Compositae, Umbelliferae, etc. The occurrence of volatile chemicals in aromatic plants is not only an indication of chemical diversity but may also help solve taxonomical problems is comprehensively studied genera. Aromatic diversity is illustrated with examples from genera such as Sideritis, Salvia, Thymus, Origanum, Satureja, Thymbra, Mentha, Micromeria, Ziziphora, Calamintha, Cyclotrichium, Acinos, Echinophora, Ferulago, Heracleum, Pimpinella, Tanacetum, and Betula.

The economic implications of aromatic biodiversity and the importance of bioprospecting are highlighted.
Diversity of bulbous monocots in Turkey with special reference. Chromosome numbers
Authors: Özhatay Neriman
Published: October 2007

Turkey is among the richest countries in the world in terms of plant diversity. The aim of this paper is to show diversity of the petaloid and bulbous plants, which belong to monocotyledones. According to Flora of Turkey and its supplements, the number of species of bulbous monocotyledones is around 688, of which 244 are endemic (endemism 35.4 %). According to the statistical data of Turkish flowering plants based on the published records, only 15 % of the flora have information about chromosome counts, although bulbous monocots percentage is higher at 58 %. Fritillaria and Tulipa are stable genera as regards chromosome numbers with 2n = 24 and karyotype; on the other hand, the most variable genera are Crocus (2n = 6, 8, 10, 12, 14, 16, 18, 20, 22, 26, 28, 30, 70) and Ornithogalum (2n = 12, 14, 16, 18, 20, 21, 24, 27, 28, 32, 40, 45, 54, 60, 80).
Biodiversity in the alkaloids of Turkish Papaver species
Authors: Sariyar Günay
Published: October 2007

There are about 35 Papaver species growing in Turkey, which are grouped into eight sections, namely Argemonidium, Carinata, Glauca, Miltantha, Oxytona, Papaver, Pilosa, and Rhoeadium.

As a result of our extensive work on the alkaloids of Turkish Papaver species the presence of several chemotypes has been shown. Among these chemotypes, medicinally important alkaloids such as noscapine (=narcotine), papaverine- and thebaine-containing samples have been found as new sources for the production of them.

The infraspecific variation encountered within the Papaver species has been demonstrated mainly in two sections of the genus, Miltantha and Oxytona. The alkaloids of seven species (Papaver armeniacum, P. curviscapum, P. cylindricum, P. fugax, P. persicum, P. polychaetum, and P. triniifolium) of the section Miltantha have been studied, and the existence of chemical strains has been shown mainly in P. fugax, P. persicum, and P. triniifolium.

Investigations on the species of the section Oxytona indicated that there is a relationship between the major alkaloid content and the chromosome numbers of the samples.

Isolation of new secoberbine-type alkaloids as well as promorphinane- and morphinane-types has revealed the biosynthetic relationship between the alkaloids of Miltantha and Oxytona species. Chemical races are also known for species of Papaver within other sections of the genus.

P. lateritium of Turkish origin from section Pilosa yielded some secoberbine and protoberberine types, whereas P. rhopalothece of the section Rhoeadium contained narcotine as a major alkaloid. Isolation of spirobenzylisoquinoline type from P. argemone (sect. Argemonidium) was the first report of the occurrence of this type in the Papaveraceae.
Sulfate-sensing electrodes. The lead- amalgam/lead-sulfate electrode (IUPAC Technical Report)
Authors: Mussini Patrizia R. , Mussini Torquato
Published: October 2007

A new, simplified design and a convenient preparation procedure for the Pb(Hg)|PbSO4|SO4
2- electrode are proposed. This procedure ensures preparation of stable amalgams and reproducible electrode potentials, which make this electrode useful and attractive for both thermodynamic investigations and electroanalytical applications. For these purposes, the electrode prepared according to the proposed procedure has been exhaustively characterized both thermodynamically and as a sulfate-sensing electrode, in different sulfate solutions, including H2SO4. Also, a practical standardization procedure has been proposed. The Pb(Hg)|PbSO4|SO4
2- electrode can be structured with a built-in concentrated Li2SO4 salt bridge for use as a sulfate-based reference electrode. This electrode can be operated as a reference electrode alternative to the conventional calomel or Ag|AgCl reference electrodes in electroanalytical practice.
Molecular basis of biodiversity, conservation, and sustained innovative utilization (IUPAC Technical Report)
Authors: Fischli Albert E. , Pandit U. K. , Black David StC.
Published: October 2007

In this Technical Report, recommendations are presented for international cooperation between academia and industry on molecular biodiversity. The recommendations are based on discussions in workshops/meetings held in Amsterdam (The Netherlands), Belo Horizonte (Brazil), Bangkok (Thailand), Kunming (China), and Antalya (Turkey) involving national and international representatives of relevant organizations.
Medicinal chemistry in the new millennium. A glance into the future
Authors: Erhardt Paul W.
Published: October 2007

The future of medicinal chemistry as both a pure and an applied science has been considered relative to trends that are already having a significant impact upon drug discovery and development. After quickly reviewing how medicinal chemistry has been practiced to date, topics considered into the future include: pursuing therapeutic efficacy, addressing 3D structure within database settings, assuring absorption, directing distribution, controlling metabolism, optimizing elimination, and avoiding toxicity. It is suggested that as the exploration of these topics proceeds into the new millennium by deploying combinatorial chemistry coupled to high-throughput screening, medicinal chemistry will play a key role as a central interpreter of the underlying structure­activity relationships such that the overall process of drug discovery and development will be knowledge-generating. As fundamental knowledge accumulates across all of these areas, virtual approaches will eventually become firmly anchored to experimental and theoretical databases having validated clinical predictability. The potential impact of some of the recent trends in process chemistry, and in analytical chemistry using X-ray diffraction as an exemplary method, are additionally highlighted before reiterating the article's major points in a summary section. From this purview, the summary also considers the education of future medicinal chemists, notes potential issues related to the future of pharmaceutical-related intellectual property, and concludes by alluding to a brewing paradox between enhanced knowledge and enhanced molecular diversity relative to the future discovery of new drugs.
Naming of new elements(IUPAC Recommendations 2002)
Authors: Koppenol W. H.
Published: October 2007

A procedure is proposed to name new elements. After the discovery of a new element is established by a joint IUPAC­IUPAP Working Group, the discoverers are invited to propose a name and a symbol to the IUPAC Inorganic Chemistry Division. Elements can be named after a mythological concept, a mineral, a place or country, a property, or a scientist. After examination and acceptance by the Inorganic Chemistry Division, the proposal follows the accepted IUPAC procedure and is then submitted to the IUPAC Council for approval.
"Heavy metals" a meaningless term? (IUPAC Technical Report)
Authors: Duffus John H.
Published: October 2007

Over the past two decades, the term "heavy metals" has been widely used. It is often used as a group name for metals and semimetals (metalloids) that have been associated with contamination and potential toxicity or ecotoxicity. At the same time, legal regulations often specify a list of "heavy metals" to which they apply. Such lists differ from one set of regulations to another and the term is sometimes used without even specifying which "heavy metals" are covered. However, there is no authoritative definition to be found in the relevant literature. There is a tendency, unsupported by the facts, to assume that all so-called "heavy metals" and their compounds have highly toxic or ecotoxic properties. This has no basis in chemical or toxicological data. Thus, the term "heavy metals" is both meaningless and misleading. Even the term "metal" is commonly misused in both toxicological literature and in legislation to mean the pure metal and all the chemical species in which it may exist. This usage implies that the pure metal and all its compounds have the same physicochemical, biological, and toxicological properties, which is untrue. In order to avoid the use of the term "heavy metal", a new classification based on the periodic table is needed. Such a classification should reflect our understanding of the chemical basis of toxicity and allow toxic effects to be predicted.
Phane nomenclature. Part II. Modification of the degree of hydrogenation and substitution derivatives of phane parent hydrides (IUPAC Recommendations 2002)
Authors: Favre H. A. , Hellwinkel D. , Powell W. H. , Smith H. A. , Tsay S. S.-C.
Published: October 2007

Cyclophane and linear phane systems are considered as parent hydrides. Their derivatives are named in conformity with the principles, rules, and conventions prescribed for naming organic compounds. The following nomenclatural features are described: indicated and added hydrogen, order of seniority for numbering, substituents expressed as suffixes, substituents cited as prefixes, phane parent hydrides modified by addition or subtraction of hydrogen atoms, and polyfunctional derivatives.
Polyaniline. Preparation of a conducting polymer(IUPAC Technical Report)
Authors: Stejskal J. , Gilbert R. G.
Published: October 2007

Eight persons from five institutions in different countries carried out polymerizations of aniline following the same preparation protocol. In a "standard" procedure, aniline hydrochloride was oxidized with ammonium peroxydisulfate in aqueous medium at ambient temperature. The yield of polyaniline was higher than 90 % in all cases. The electrical conductivity of polyaniline hydrochloride thus prepared was 4.4 ± 1.7 S cm-1 (average of 59 samples), measured at room temperature. A product with defined electrical properties could be obtained in various laboratories by following the same synthetic procedure. The influence of reduced reaction temperature and increased acidity of the polymerization medium on polyaniline conductivity were also addressed. The conductivity changes occurring during the storage of polyaniline were monitored. The density of polyaniline hydrochloride was 1.329 g cm-3. The average conductivity of corresponding polyaniline bases was 1.4 x10­8 S cm-1, the density being 1.245 g cm-1. Additional changes in the conductivity take place during storage. Aging is more pronounced in powders than in compressed samples. As far as aging effects are concerned, their assessment is relative. The observed reduction in the conductivity by ~10 % after more than one-year storage is large but, compared with the low conductivity of corresponding polyaniline (PANI) base, such a change is negligible. For most applications, an acceptable level of conductivity may be maintained throughout the expected lifetime.
Grid computing and bioinformatics development. A case study on the Oryza sativa (rice) genome
Authors: Rungsarityotin Wasinee , Khiripet Noppadon , Tanpraset Chularat , Chitradon Royol
Published: October 2007

The bioinformatics research area is now faced with a mountain of ever-increasing and distributed information. For example, finding a single gene of the Oryza sativa (rice) genome one must spend weeks, if not months, wandering through approximately 40 million base pairs. These data are scattered in many data repositories. Thus, not only do we need an efficient tool to visualize and analyze DNA data, but the integration and exchange of information on a particular gene or coding regions from different international collaborative databases needs to be done in a careful, but robust manner as well. This research suggests a feasible means to overcome these problems by employing two main technologies. To support the exchange and communication between several sources of data, the grid database technology will be employed on the fast Internet2 backbone. Then, XML-based DNA data will be transported between collaborative sources for further analysis and representation. A preliminary version of our Web-based viewer for the XML data of the Oryza sativa genome is presented to illustrate the idea.
Definitions relating to stereochemically asymmetric polymerizations (IUPAC Recommendations 2001)
Authors: Hatada K. , Kahovec J. , Barón Máximo , Horie K. , Kitayama T. , Kubisa P. , Moss G. P. , Stepto R. F. T. , Wilks E. S.
Published: October 2007

Asymmetric polymerization has been of interest to many academic and industrial polymer scientists, but no reference has been made by IUPAC explicitly to classification and definitions of reactions involving the asymmetric synthesis of polymers. This document presents definitions concerned with asymmetric and related polymerizations, with examples included to clarify the meaning of the definitions. Asymmetric polymerizations embrace two main categories, "asymmetric chirogenic polymerizations" and "asymmetric enantiomer-differentiating polymerizations".
Potentiometric selectivity coefficients of ion-selective electrodes. Part II. Inorganic anions (IUPAC Technical Report)
Authors: Umezawa Yoshio , Umezawa Kayoko , Bühlmann Philippe , Hamada Naoko , Aoki Hiroshi , Nakanishi Jun , Sato Moritoshi , Xiao Kang Ping , Nishimura Yukiko
Published: October 2007

Potentiometric selectivity coefficients, K
A,B
pot have been collected for ionophore-based ion-selective electrodes (ISEs) for inorganic anions reported during 1988-1998. In addition to the actual numerical values of K
A,B
pot together with the methods and conditions for their determination, response slopes, linear concentration (activity) ranges, chemical compositions, and ionophore structures for the ISE membranes are tabulated.
Potentiometric coefficients of ion-selective electrodes. Part III. Organic ions (IUPAC Technical Report)
Authors: Umezawa Yoshio , Buhlmann Phillipe , Umezawa Kayoko , Hamada Naoko
Published: October 2007

Potentiometric selectivity coefficients, K
A,B
pot, have been collected for ionophore-based ion-selective electrodes (ISEs) for organic ions reported during 1988-1998. In addition to the actual numerical values of K
A,B
pot together with the methods and conditions for their determination, response slopes, linear ranges, chemical compositions, and ionophore structures for the ISE membranes are tabulated.
Role of water in sweet taste chemoreception
Authors: Birch Gordon G.
Published: October 2007

The mechanistic understanding of sweet taste chemoreception has been advanced by the microscopic and macroscopic studies of sweetener­water interactions. This approach has led to the concept of water mobility as a key to interpreting sweetness. The apparent specific volume of a solution is a determinant of its taste quality, as sweetness is known to be confined to the range 0.51­0.71 cm3 g-1. Thus, the "ideal" quality of the sugars is presumed to be due to their occupancy of the center of this range (i.e., 0.618 cm3 g-1). Most sweeteners elicit off-tastes and flavors and exhibit different apparent specific volumes. This leads to the conclusion that taste quality is broadly determined by the packing characteristics of sweet molecules among water molecules and the compactness of their hydration shells, expressed as their apparent specific isentropic compressibilities. The role of water can, therefore, be applied in modern attempts to optimize sweet taste quality, and different food salts can be explored as useful taste modifiers. Salts interact more strongly with water structure than do any other taste solutes, and it emerges that the ionic charge density is an important criterion. Such studies show how sweetener formulations are likely to improve within the next decade.
Homology-based model of the extracellular domain of the taste receptor T1R3
Authors: Walters D. Eric
Published: October 2007

The extracellular ligand binding domain of the sweet receptor T1R3 has been homology-modeled on the basis of the crystal structure of the metabotropic glutamate receptor (mGluR1). The region of the model that corresponds to the ligand binding site of mGluR1 has numerous polar and charged side-chains, consistent with expectations for a site that would respond to poly hydroxy compounds such as mono- and disaccharides. Docking studies show that proposed active conformations of the high-potency sweeteners neotame, superaspartame, and SC-45647 could interact favorably in this binding site, forming ion pairs or ionic hydrogen bonds with His-163, Glu-318, and His-407, in addition to hydrophobic interactions with numerous nonpolar side-chains.
Molecular mechanisms of taste transduction
Authors: Margolskee Robert F.
Published: October 2007

Taste transduction is a specialized form of signal transduction by which taste receptor cells (TRCs) encode at the cellular level information about chemical substances encountered in the oral environment (so-called tastants). Bitter and sweet taste transduction pathways convert chemical information into a cellular second messenger code utilizing cyclic nucleotides, inositol trisphosphate, and/or diacyl glycerol. These messengers are components of signaling cascades that lead to TRC depolarization and Ca++ release. Bitter and sweet taste transduction pathways typically utilize taste-specific or taste-selective seven transmembrane-helix receptors, G proteins, effector enzymes, second messengers, and ion channels. The structural and chemical diversity of tastants has led to the need for multiple transduction mechanisms. Through molecular cloning and data mining, many of the receptors, G proteins, and effector enzymes involved in transducing responses to bitter and sweet compounds are now known. New insights into taste transduction and taste coding underlying sweet and bitter taste qualities have been gained from molecular cloning of the transduction elements, biochemical elucidation of the transduction pathways, electrophysiological analysis of the function of taste cell ion channels, and behavioral analysis of transgenic and knockout models.
Ion channels and second messengers involved in transduction and modulation of sweet taste in mouse taste cells
Authors: Sugimoto Kumiko , Shigemura Noriatsu , Yasumatsu Keiko , Ohta Rie , Nakashima Kiyohito , Kawai Kirio , Ninomiya Yuzo
Published: October 2007

Leptin, a hormone released from the adipose tissue, inhibits food intake and increases energy expenditure. We have found a novel function of leptin as a modulator of sweet taste sensitivity in mice. In lean normal mice, the gustatory nerve responses to sweet stimuli were selectively suppressed depending on plasma leptin level after an intraperitoneal injection of recombinant leptin. Patch-clamp studies using isolated taste cells of lean mice showed that extracellular leptin enhanced K+ currents of sweet-responsive taste cells, which led to membrane hyperpolarization and a reduction of sweetener-induced depolarization. Reverse transcription-polymerase chain reaction (RT-PCR) and in situ hybridization analyses demonstrated specific expression of mRNA of the long-form functional leptin receptor (Ob-Rb) in taste tissue and cells of lean mice. The genetically diabetic db/db mice, which have defects in Ob-Rb, demonstrated neither a suppression of gustatory neural responses to sweeteners nor an increment of whole-cell K+ conductance of taste cells even with high doses of leptin. These results suggest that Ob-Rb is specifically expressed in sweet-responsive taste cells of lean mice and that leptin suppresses sweetener-induced depolarization via activation of K+ channels, leading to a decrease in impulses of sweet-best fibers. The enhanced sweet responses of db/db mice may result from the lack of inhibitory modulation by leptin.
Specialization and phyletic trends of sweetness reception in animals
Authors: Glaser Dieter
Published: October 2007

During the last decades, the comparison in various animal species of their gustatory responses to compounds eliciting a sweet taste in humans has extended our knowledge of the great biodiversity of the taste responses and evidenced some specialization and/or phyletic trends within species. Our interest was focused on responses to natural sugars, polyols, and naturally occurring sweeteners, but also on various artificial sweetening compounds, including the very powerful guanidine sweeteners. New results obtained with kangarooswhich originated about 130 MYAhave shown that their sweetness receptor is not designed to taste any of the artificial sweeteners tested. Therefore, the ability to taste complicated artificial sweeteners must have evolved later in higher developed mammals, about 100 million years ago.
Drosophila sweet taste receptor
Authors: Isono Kunio , Ueno Kohei , Ohta Masayuki , Morita Hiromi
Published: October 2007

Like the Sac locus controlling sugar sensitivity in mice, the taste gene Tre of the fruitfly Drosophila was discovered in wild populations as a genetic dimorphism controlling gustatory sensitivity to a sugar trehalose. By activating a P-element transposon near the gene locus we obtained induced Tre mutations and analyzed the associated changes in gene organizations and the mRNA expressions. The analysis showed that Tre is identical to Gr5a, a gene that belongs to a novel seven-transmembrane receptor family expressed in chemosensory neurons and predicted to encode chemosensory receptors. Thus, Gr5a is a candidate sweet taste receptor in the fly. An amino acid substitution in the second intracellular loop domain was identified to be functionally correlated with the genetic dimorphism of Tre. Since Tre controls sweet taste sensitivity to a limited subset of sugars, other Gr genes phylogenetically related to Tre may also encode sweet taste receptors. Those candidate sweet taste receptors, however, are phylogenetically distinct from vertebrate sweet taste receptors, suggesting that the sweet taste receptors in animals do not share a common origin.
Isovanillyl sweeteners. From molecules to receptors
Authors: Bassoli Angela , Merlini Lucio , Morini Gabriella
Published: October 2007

Systematic modification of the structure of the sweet natural compound phyllodulcin, containing the isovanillyl glucophoric group, led to the synthesis of about 120 compounds. Features of the heterocyclic ring conferring high sweetness potency were identified. A strong increase in sweetness was obtained by the introduction of sulfur atoms in the ring and by separation of the enantiomers. Results of the quantitative structure­activity relationship (QSAR) studies on this series are reported. Application of the pseudoreceptor modeling approach afforded a three-dimensional binding site model for isovanillyl sweeteners. Extension of this methodology to a large group of structurally diverse compounds, including the commonly used sweeteners, gave a general pseudoreceptor for the sweet compounds, consisting of 16 amino acids. This pseudoreceptor, which has the peculiarity of giving a semiquantitative evaluation of the sweetness intensity, could be used as a valid tool to model the ligand­receptor interactions and to suggest some clues about the identification of a possible binding site once the receptor protein(s) are obtained.
Computational studies of sweet-tasting molecules
Authors: Barker Jodie S. , Hattotuwagama Channa K. , Drew Michael G. B.
Published: October 2007

Quantitative structure­activity relationships (QSARs) are developed for two separate families of sweet-tasting molecules for which sweetness values relative to sucrose (RS) have been measured. For these two families of sucrose and guanidine derivatives, the molecules were divided into training and test sets. Linear multiple regression equations have been generated to relate separately log(RS) to two types of parameters, namely molecular descriptors and energies derived via molecular field analysis (MFA). The parameters used in the development of linear multiple regression equations were selected by the genetic algorithm. The equations obtained show high predictive quality, which is confirmed by statistical parameters obtained with the test sets.

The data for these two families were then combined with data from two other families previously studied, namely the sulfamates and isovanillates, to make a set of 149 compounds. These molecules were also studied by QSAR methods. The generated equations show remarkable predictive power, and the quality of the results suggest that the mechanism of sweet taste receptor is similar and, therefore, that there could well be only one receptor site for sweet taste, particularly for the four sweet taste families considered in this work.
Search for new sulfonyl-containing glucophores
Authors: Polanski Jaroslaw , Jarzembek Krystyna
Published: October 2007

A number of sweeteners contain the sulfur atom and a sulfonyl group. In our current search for new glucophores, several new compounds containing a sulfonyl group were obtained. Synthetic targets have been found both by intuitive modifications of the structural motifs of the known sweet compounds and by the use of molecular modeling techniques. We developed the efficient synthetic routes yielding these compounds and obtained a number of these analogs. We have evaluated the taste quality of the amides and sulfonylated amino acids, finding out that almost all of them are bitter actives. We are now performing basic toxicological tests preceding the systematic taste study within the tetrazoles obtained.
Structure­taste relationships of the sweet protein monellin
Authors: Kohmura Masanori , Mizukoshi Toshimi , Nio Noriki , Suzuki Ei-ichiro , Ariyoshi Yasuo
Published: October 2007

Structure­taste relationship studies were carried out by chemically synthesizing monellin and its analogs. Replacement of the AspB7 by l-2-aminobutyric acid, Gly and d-Asp resulted in complete loss of sweetness. Replacement of IleB6 and IleB8 by different amino acids resulted in a significant decrease of sweetness, or complete loss of sweetness. Comparison of short- and long-range nuclear Overhauser effects (NOEs) and chemical shifts between monellin and [AbuB7]monellin showed no marked differences except for the region of the AspB7. Thus, the complete loss of sweetness in [AbuB7]monellin is caused by the lack of free β-carboxyl group in the AspB7 and not by a result of major disruption in the overall 3-dimensional structure. These results suggested that the free β-carboxyl group of the AspB7 would possibly bind to the receptor site through ionic bonding and trigger the sensation of intense sweet taste, and IleB6 and/or IleB8 would be involved in the hydrophobic interaction with the receptor site. Selectively labeled monellin was synthesized by the solid-phase method by incorporating 15N-labeled amino acids into 10 key residues including AspB7. Relaxation analysis shows that AspB7 is the most flexible of these 10 residues. The flexibility of the active site may be important for receptor binding.
Present status and future of functional oligosaccharide development in Japan
Authors: Nakakuki Teruo
Published: October 2007

Several oligosaccharides such as glycosylsucrose, fructo-oligosaccharides, malto-oligosaccharides, isomalto-oligosaccharides (branched-oligosaccharides), galacto-oligosaccharides, xylo-oligosaccharides, isomaltulose (palatinose), and lactosucrose have been produced on an industrial scale. Recent developments in industrial enzymology have made possible a series of new starch oligosaccharides such as β-1,6 linked gentio-oligosaccharides, α,α-1,1 linked trehalose, α-1,3 linked nigero-oligosaccharides, and branched-cyclodextrins. Some new sweeteners, including trehalose and nigero-oligosaccharides, are being developed as food ingredients with physiologically unique functions such as superoxide dismutase-like activity and immunological activity. Also, soybean oligosaccharides containing raffinose, stachyose, and other oligosaccharides mentioned above are now used in beverages, confectionery, bakery products, yogurts, daily products, and infant milk. In 1991, the Japanese government legislated for Foods for Specified Health Use (FOSHU). FOSHU increased the total to 223 items of which more than 50 % incorporate oligosaccharides as the functional components. Furthermore, the Ministry of Health, Labor, and Welfare published the proposal for a new system named Foods with Health Claims (FHC), which was carried out in April 2002.
Digestion, absorption, fermentation, and metabolism of functional sugar substitutes and their available energy
Authors: Oku Tsuneyuki , Nakamura Sadako
Published: October 2007

Many kinds of oligosaccharides and sugar alcohols have been newly developed as bulking sugar substitutes that have beneficial health effects. A sugar substitute that is not digested and absorbed in the small intestine reaches the large intestine, where it is completely fermented by intestinal bacteria and produces short-chain fatty acids, which are converted to energy. The available energy of a nondigestible sugar substitute, which is completely fermented by intestinal microbes, is estimated as approximately 2 kcal/g.

On the other hand, a sufficiently high ingestion of nondigestible sugar substitutes regularly causes overt diarrhea in human and animals. However, the diarrhea disappears within a few days because intestinal microbes, which readily utilize these saccharides, increase during ingestion. The maximum permissible dose, by which transitory diarrhea is not caused by the ingestion of nondigestible sugar substitutes, is estimated as approximately 0.3 g per kg body weight in single ingestion for Japanese adults. The value is varied by some factors, such as separate ingestion, repeat ingestion, test substance, and body condition, etc.
Novel physiological functions of oligosaccharides
Authors: Hirayama Masao
Published: October 2007

This paper reviews the evidence for novel physiological functions of oligosaccharides. A history of the research and development and the types of health benefits are discussed. A key property of the physiological functions lies in the indigestibility of oligosaccharides, which gives rise to fermentation in the large intestine, followed by an increase of Bifidobacteria and short-chain fatty acid (SCFA) production. This property leads to several kinds of physiological functions, classified into three types of health benefits. The first is the improvement of gastrointestinal conditions, including a normal stool frequency, less constipation, and healthy intestinal microflora. The second is the promotion of mineral absorption, including an increase of bone density and relief of anemia. The third is an immunomodulation effect, such as allergy and cancer prevention.
Role of sweeteners in the etiology and prevention of dental caries
Authors: Hamada Shigeyuki
Published: October 2007

Dental caries is a multifactorial disease that is caused by an interplay of three major factors, i.e., teeth, cariogenic bacteria, and fermentable sugars. Streptococcus mutans and S. sobrinus, collectively termed mutans streptococci (MS), are principal causative agents of dental caries. Initial MS-tooth surface attachment is followed by firm and irreversible adhesion of MS to the tooth surface, accompanied by the synthesis of water-insoluble glucan from sucrose via enzymatic action of glucosyltransferases (GTases). MS induce severe dental caries in rats fed on a high-sucrose diet. Epidemiological surveys indicate that frequent sucrose intakes are associated with high prevalence of dental caries in humans. In contrast, dietary sucrose restrictions and/or use of nonfermentable sucrose substitutes clearly influence the GTase activities of MS, resulting in decreased caries development. Structural isomers of sucrose (i.e., disaccharides composed of glucose and fructose with different linkages) will not function as substrates for GTases of MS, nor be utilized as energy sources by MS. Palatinose and trehalulose are included in this category, and are produced in commercial scales in Japan. Glucose oligomers containing α-1, 6 and/or α-1, 4 linkages are found to inhibit glucan synthesis by MS from sucrose, although these oligomers are hydrolyzed by MS to release acids. Lastly, sugar alcohols, including maltitol and palatinit, are useful as noncaries-inducing sweeteners.
Antidiabetogenic constituents from several natural medicines
Authors: Matsuda Hisashi , Morikawa Toshio , Yoshikawa Masayuki
Published: October 2007

In the course of our studies on antidiabetogenic and antidiabetic principles of natural medicines and medicinal foodstuffs, we have isolated salacinol and kotalanol with unique thiosugar sulfonium sulfate inner salt structures from the antidiabetic Ayurvedic traditional medicines, Salacia reticulata and S. oblonga. Salacinol and kotalanol showed potent inhibitory activities against intestinal α-glucosidase, and also inhibitory effects of salacinol on the increase in serum glucose levels in maltose- and sucrose-loaded rats were found to be more potent than those of acarbose. In addition, various flavonoids with potent inhibitory activities against rat lens aldose reductase such as quercitrin desmanthin-1 and guaijaverin were isolated from Myrcia multiflora and several natural medicines, and some structural requirements of flavonoids for aldose reductase inhibitory activity were clarified.
Cancer-chemopreventive effects of natural sweeteners and related compounds
Authors: Konoshima Takao , Takasaki Midori
Published: October 2007

To search for possible cancer-chemopreventive agents from natural resources, several natural sweeteners were screened by the in vitro assay indicated by the inhibitory effects of Epstein-Barr virus early antigen (EBV-EA) induction. Of active compounds that showed the remarkable inhibitory effects on the EBV-EA induction, stevioside, from the leaves of Stevia rebaudiana, and mogroside V, from the fruits of Momordica grosvenori, exhibited significant inhibitory effects on the two-stage mouse skin carcinogenesis in vivo induced by 7,12-dimethylbenz[a]anthracene (DMBA) and 12-O-tetradecanoylphorbol-13-acetate (TPA). The inhibitory effect of stevioside is stronger than that of glycyrrhizin, which had been known as an antitumor-promoter in chemical carcinogenesis. Furthermore, stevioside also inhibited mouse skin carcinogenesis initiated by peroxynitrite. These results suggest that stevioside and mogroside V might be valuable as chemopreventive agents for chemical carcinogenesis.
Transition metal-catalyzed reactions in heterocyclic chemistry
Authors: Beletskaya Irina P.
Published: October 2007

The palladium-catalyzed substitution reactions forming carbon­carbon and carbon­element bonds, as well as nickel-catalyzed addition of E­H and E­E' bonds across multiple bonds, are considered in their application to the chemistry of heterocyclic compounds.
Alkaloid synthesis via [3+2] cycloadditions
Authors: Pearson William H.
Published: October 2007

Tin-lithium exchange on (2-azaallyl)stannanes affords nonstabilized 2-azaallyllithiums (2-azaallyl anions) that undergo [π4s+π2s] cycloadditions with alkenes to afford pyrrolidines. The scope of this method has been expanded to include 2-azapentadienyllithiums and heteroatom-substituted 2-azaallyllithiums. Alternatively, the (2-azaallyl)stannanes may also be used to generate nonstabilized azomethine ylides via N-alkylation/destannylation or N-protonation/destannylation, and these ylides were also found to be useful for the synthesis of pyrrolidines by [π4s+π2s] cycloadditions with alkenes. Applications of both methods to the total synthesis of alkaloids such as (+)-coccinine, lepadiformine stereoisomers, lapidilectine B, and indolizidine 239CD have been accomplished.
Recent advances in industrial carotenoid synthesis
Authors: Ernst Hansgeorg
Published: October 2007

Symmetrical C40-carotenoids are efficiently produced by double Wittig olefination of the corrresponding C15-phosphonium salts with C10-dialdehyde. Industrial syntheses of lycopene-, astaxanthin-, and (3R,3'R)-zeaxanthin-C15-phosphonium salts are discussed. An efficient route to a monoprotected C10-dialdehyde for the synthesis of unsymmetrical

C40-carotenoids is presented. Primary polyene allyl alcohols can be converted to the corresponding aldehydes by "TEMPO" oxidation. A high-yield synthesis of meso-zeaxanthin as an example for syntheses of unsymmetrical carotenoids is presented.
Oxidative cleavage of carotenoids catalyzed by enzyme models and beta-carotene 15,15´-monooxygenase
Authors: Woggon Wolf-D.
Published: October 2007

The enzyme that catalyzes the central cleavage of β-carotene is an iron monooxygenase. The protein was isolated from chicken intestinal mucosa and overexpressed in two different cell lines. Inductively coupled plasma (ICP) emission analysis revealed that the hydrophobic 60.3-kDa enzyme contains one iron/mole protein. The substrate specificity was investigated, and the reaction mechanism elucidated incubating α-carotene in the presence of highly enriched 17O2 and H2
18O. A supramolecular enzyme model was synthesized, binding carotenoids Ka > 106 mol-1, which mimics the regiospecific enzymatic cleavage of carotenoids.
Regulation of carotenoid synthesis and accumulation in plants
Authors: Cunningham Francis X.
Published: October 2007

Although genes that encode most enzymes of the carotenoid pathway in higher plants have been identified, the regulatory mechanisms that govern the synthesis and accumulation of carotenoid pigments are still obscure. Recent findings relevant to two aspects of carotenoid pathway control are reviewed: availability of substrate and pathway branching. Experimental approaches that are likely to enhance our understanding of carotenoid pathway regulation are also described.
Lycopene, tomato products, and prostate cancer prevention. Have we established causality?
Authors: Miller Elizabeth C. , Hadley Craig W. , Schwartz Steven J. , Erdman John W. , Boileau Thomas W.-M. , Clinton Steven K.
Published: October 2007

The relationship between tomato products and prostate cancer prevention has been the subject of increasingly intense research activity over the past decade. The hypothesis that tomato products contain phytochemicals, perhaps lycopene and others, that modify prostate carcinogenesis warrants investigation. However, scientists, regulatory agencies, marketers of products, and those defining public health policy have differing opinions regarding the strength of the data when applied to criteria for inference and causality. It is useful to briefly review these criteria and discuss the relative strengths and weaknesses of the published data in order to better define future directions for research. Accepted categories of criteria include: consistency, strength of association, biological gradient, temporality, specificity, biological mechanisms and coherence, and experimental evidence. We believe that continued support for research regarding tomato products, lycopene and other phytochemicals, and prostate cancer risk is warranted and may ultimately serve as the basis for more consistent public health recommendations for the consumer. But, what do we say to the public when the data is still inconclusive? The authors support the recommendation that a minimum of five servings of fruit and vegetables should be consumed daily from a variety of sources. We believe that the hypothesized benefits of tomato products for prostate cancer prevention may be achieved with approximately five servings of tomato products per week. The consumption of lycopene supplements is not currently recommended for prostate cancer prevention or therapy. Future research will allow us to provide more definitive guidelines.
Lycopene in the treatment of prostate cancer
Authors: Kucuk Omer , Sarkar Fazlul H. , Sakr Wael , Khachik Fred , Djuric Zora , Banerjee Mousumi , Pollak Michael N. , Bertram John S. , Wood David P.
Published: October 2007

Dietary intake of lycopene is associated with reduced risk of prostate cancer (PCa). We conducted a clinical trial in men with prostate cancer to investigate the biological and clinical effects of lycopene supplementation. Twenty-six men with prostate cancer were randomly assigned to receive a lycopene supplement or no supplement for three weeks before radical prostatectomy. Subjects in the intervention group (n = 15) were instructed to take a tomato oleoresin extract soft gel capsule (Lyc-O-Mato®, LycoRed Company, Beer Sheva, Israel) containing 15 mg lycopene, 1.5 mg phytoene, 1.5 mg phytofluene, and 5 mg tocopherol twice daily with meals. Prostatectomy specimens were evaluated for pathologic stage, Gleason score, volume of cancer, and extent of high-grade prostatic intraepithelial neoplasia (HGPIN). Biomarkers of cell proliferation and apoptosis were assessed by Western blot analysis in benign and cancerous tissue samples obtained from the prostatectomy specimens. Oxidative stress was assessed by measuring the peripheral blood lymphocyte DNA oxidation product 5-hydroxymethyl-deoxyuridine (5-OH-mdU). Plasma levels of lycopene, insulin-like growth factor-1 (IGF-1), insulin-like growth factor binding protein-3 (IGFBP-3), and prostate-specific antigen (PSA) were measured at baseline and after three weeks of study period. After the intervention, more men in the intervention group had smaller (<4 cc) tumors, organ-confined disease without involvement of surgical margins or extra-prostatic tissues, and focal involvement of the prostate with HGPIN compared to the control group. Mean plasma PSA levels were lower in the intervention group compared to the control group. This pilot study suggests that a tomato extract containing lycopene and other tomato carotenoids and phytochemicals may have a potential role in the treatment of prostate cancer. Larger clinical trials are necessary to definitively address potential uses of lycopene or tomato extract in the prevention or treatment of prostate cancer.
Role of gene regulation in the anticancer activity of carotenoids
Authors: Sharoni Yoav , Danilenko Michael , Walfisch Shlomo , Amir Hadar , Nahum Amit , Ben-Dor Anat , Hirsch Keren , Khanin Marina , Steiner Michael , Agemy Lilach , Zango Gabriel , Levy Joseph
Published: October 2007

There is extensive evidence that high intake of fruits and vegetables is associated with decreased risk of many types of cancers. Thus, it is widely accepted that diet changes are a powerful means to prevent cancer. Although there is a growing interest in the role of the tomato carotenoid lycopene in cancer prevention and treatment, we hypothesize that a single micronutrient cannot replace the power of the concerted action of multiple agents derived from a diet rich in fruits and vegetables. Indeed, we found that lycopene can synergize with other phytonutrients in the inhibition of cancer cell growth. The mechanism underlying the inhibitory effects of lycopene and other carotenoids involves interference in several pathways related to cancer cell proliferation and includes changes in the expression of many proteins participating in these processes, such as connexins, cyclins, cyclin-dependent kinases, and their inhibitors. These changes in protein expression suggest that the initial effect involves modulation of transcription by ligand-activated nuclear receptors or by other transcription factors. It is feasible to suggest that carotenoids and their oxidized derivatives interact with a network of transcription systems that are activated by different ligands at low affinity and specificity and that this activation leads to the synergistic inhibition of cell growth.
Concepts and applications of the term "dimensionality" in analytical chemistry (IUPAC Technical Report)
Authors: Danzer Klaus , van Staden Jacobus F. , Burns Duncan Thorburn
Published: October 2007

The term "dimensionality" has been used by the analytical chemistry community with several meanings. On different occasions, analysts speak about "two-dimensional" analytical methods, for example, 2D nuclear magnetic resonance spectroscopy, 2D thin-layer chromatography, "two-dimensional" or "three-dimensional" analytical information [1], "two-dimensional" or "three-dimensional" images in surface analytical chemistry, and of "m-dimensional" analytical data [2] obtained, for example, as a result of multicomponent analyses. These examples show that the use of the term "dimensionality" is at times contradictory. This confused position does not promote the unequivocal application of the term "dimensionality" in analytical chemistry. The aim of this document is to provide a concept for the use of the term "dimensionality" as it is related to analytical information.
Sonochemistry as a tool for preparation of porous metal oxides
Authors: Srivastava D. N. , Perkas N. , Zaban A. , Gedanken A.
Published: October 2007

The porous metal oxides are an important class of materials, because the surface area/volume ratio of a material is increased by many fold, making them very useful in surface-related applications. The mesoporous materials were discovered in the 1990s, and since then they have been excellent candidates for materials science research. These mesoporous materials are prepared by hydrolyzing the inorganic precursor (usually metal alkoxide) in an acid, basic, or neutral medium in the presence of an organic structure-directing agent, the surfactant, in a conventional method. Recently, we have demonstrated that the sonochemical technique can be employed for the synthesis of mesoporous metal oxides. The sonochemical method reduced the time period required for such synthesis by many fold, and also produced more stable structures. We got excellent results with silica, titania, yittria-stabilized zirconia (YSZ), and Fe2O3. We also used an inorganic precursor other than an alkoxide for the preparation of mesoporous metal oxides. In this article, we present some of the recent results on this topic.
Structural variations in nanocrystalline nickel films
Authors: Gai Pratibha L. , Mitra Rahul , Weertman Julia R.
Published: October 2007

Nanocrystalline nickel films of technological importance have been grown on various liquid nitrogen-cooled substrates by magnetron sputtering with and without a substrate bias. The atomic structural and chemical studies have unveiled variations in inter- and intragranular structures under the different process conditions. The origin and the development of the crystallization process with and without the substrate bias voltage have been inferred from the results.