Think yellow and keep green—Role of sulfanes from garlic in agriculture

Reactive sulfur species from garlic have long been renowned for their health benefits and antimicrobial properties. In agriculture the subject matter is now gathering momentum in the search for new bio-pesticides to addressing emerging environmental concerns and tighter restrictions on the use of many conventional chemical pesticides. Although the precise modes of action of these garlic-derived bioactives is complex, recent research has provided a number of new insights that deepen our understanding of garlic-derived products, such as garlic extracts and oils. Herein, their activity against various crop-damaging pests is reviewed. In many cases, there seems to be a broad range of activity associated with the sulfur-containing compounds derived from Allium species, which manifests itself in diverse insecticidal, antifungal, and nematicidal activities. These activities open a new understanding to develop this natural chemistry as a “green pesticide”

Importance-performance analysis of UK and US bank customer perceptions of service delivery technologies

Importance-performance analysis is utilised to compare the perceptions held by bank customers regarding selected service delivery technologies (SDTs) such as automated teller machines (ATMs), telephone banking and internet banking. Bank patrons in the United Kingdom and the United States are surveyed to examine which service delivery factors they consider to be most important toward assessing the performance of SDTs offered by banking institutions. Customer views are plotted onto importance-performance grids which offer banking strategists a straightforward, graphic illustration of service factors that patrons consider to be salient and well-addressed by current installations of bank SDTs in each respective nation. The grids also offer heuristic decision guides for translating customer perceptions into strategic allocations of organisational investments toward SDT

Unusual Nucleophilic Addition of Grignard Reagents in the Synthesis of 4-Amino-pyrimidines

Pyrimidines have always received considerable attention because of their importance in synthesis and elucidation of biochemical roles, in particular that of vitamin B1. Herein, we describe a reaction pathway in a Grignard reagent-based synthesis of substituted pyrimidines. A general synthesis of α-keto-2-methyl-4-amino pyrimidines and their C6-substituted analogues from 4-amino-5-cyano-2-methylpyrimidine is reported. The presence of the nitrile substituent in the starting material also results in an unusual reaction pathway leading to C6-substituted 1,2-dihydropyrimidines. Grignard reagents that give normal pyrimidine products under standard reaction conditions can be 14 switched to give dihydropyrimidines by holding the reaction at 0 °C before quenching

Physiological Studies of Chlorobiaceae Suggest that Bacillithiol Derivatives Are the Most Widespread Thiols in Bacteria

Low-molecular-weight (LMW) thiols mediate redox homeostasis and the detoxification of chemical stressors. Despite their essential functions, the distribution of LMW thiols across cellular life has not yet been defined. LMW thiols are also thought to play a central role in sulfur oxidation pathways in phototrophic bacteria, including the Chlorobiaceae. Here we show that Chlorobaculum tepidum synthesizes a novel LMW thiol with a mass of 412 ± 1 Da corresponding to a molecular formula of C14H24N2O10S, which suggests that the new LMW thiol is closely related to bacillithiol (BSH), the major LMW thiol of low-G+C Gram-positive bacteria. The Cba. tepidum LMW thiol structure was N-methyl-bacillithiol (N-Me-BSH), methylated on the cysteine nitrogen, the fourth instance of this modification in metabolism. Orthologs of bacillithiol biosynthetic genes in the Cba. tepidum genome and the CT1040 gene product, N-Me-BSH synthase, were required for N-Me-BSH synthesis. N-Me-BSH was found in all Chlorobiaceae examined as well as Polaribacter sp. strain MED152, a member of the Bacteroidetes. A comparative genomic analysis indicated that BSH/N-Me-BSH is synthesized not only by members of the Chlorobiaceae, Bacteroidetes, Deinococcus-Thermus, and Firmicutes but also by Acidobacteria, Chlamydiae, Gemmatimonadetes, and Proteobacteria. Thus, BSH and derivatives appear to be the most broadly distributed LMW thiols in biology

Prednisolone improves the response to primary endocrine treatment for advanced breast cancer.

Two hundred and twenty patients with progressive advanced breast cancer were given primary endocrine treatment (PET) according to menstrual status. Pre-menopausal patients received ovarian irradiation (O) and post-menopausal tamoxifen 10 mg bd (T). Patients were randomised to receive either no additional treatment or prednisolone 5 mg bd (P). Similar results were observed in each menstrual subgroup. In 194 evaluable patients, the response to PET + P was 49% and to PET alone 30% (P less than 0.01). P increased the median duration of response from 9 to 14 months (P less than 0.002) and the median time to disease progression from 5 to 9 months (P less than 0.001). Response to P after O or T alone occurred in only 2/62 (3%). Median survival in patients randomised to receive P at the outset of PET was prolonged by 4 months (P less than 0.05). The addition of P significantly improves the response to O or T in the treatment of advanced breast cancer

Suramin: Effectiveness of analogues reveals structural features that are important for the potent trypanocidal activity of the drug

Suramin was the first effective drug for the treatment of human African sleeping sickness. Structural analogues of the trypanocide have previously been shown to be potent inhibitors of several enzymes. Therefore, four suramin analogues lacking the methyl group on the intermediate rings and with different regiochemistry of the naphthalenetrisulphonic acid groups and the phenyl rings were tested to establish whether they exhibited improved antiproliferative activity against bloodstream forms of Trypanosomes brucei compared to the parent compound. The four analogues exhibited low trypanocidal activity and weak inhibition of the antitrypanosomal activity of suramin in competition experiments. This indicates that the strong trypanocidal activity of suramin is most likely due to the presence of methyl groups on its intermediate rings and to the specific regiochemistry of naphthalenetrisulphonic acid groups. These two structural features are also likely to be important for the inhibition mechanism of suramin because DNA distribution and nucleus/kinetoplast configuration analyses suggest that the analogues inhibit mitosis while suramin inhibits cytokinesis

Suramin analogues protect cartilage against osteoarthritic breakdown by increasing levels of tissue inhibitor of metalloproteinases 3 (TIMP-3) in the tissue

Osteoarthritis is a chronic degenerative joint disease affecting millions of people worldwide, with no disease-modifying drugs currently available to treat the disease. Tissue inhibitor of metalloproteinases 3 (TIMP-3) is a potential therapeutic target in osteoarthritis because of its ability to inhibit the catabolic metalloproteinases that drive joint damage by degrading the cartilage extracellular matrix. We previously found that suramin inhibits cartilage degradation through its ability to block endocytosis and intracellular degradation of TIMP-3 by low-density lipoprotein receptor-related protein 1 (LRP1), and analysis of commercially available suramin analogues indicated the importance of the 1,3,5-trisulfonic acid substitutions on the terminal naphthalene rings for this activity. Here we describe synthesis and structure-activity relationship analysis of additional suramin analogues using ex vivo models of TIMP-3 trafficking and cartilage degradation. This showed that 1,3,6-trisulfonic acid substitution of the terminal naphthalene rings was also effective, and that the protective activity of suramin analogues depended on the presence of a rigid phenyl-containing central region, with para/para substitution of these phenyl rings being most favourable. Truncated analogues lost protective activity. The physicochemical characteristics of suramin and its analogues indicate that approaches such as intra-articular injection would be required to develop them for therapeutic use

Performing the high-school prom in the UK: Locating authenticity through practice

The purpose of this study was threefold: to develop an understanding of the appropriation of the US High School Prom in the UK and more importantly to generate an insight into the producers and consumers of such an event; to establish if the performance of the prom is hyper-real or if there is an awareness of the authentic or inauthentic elements of this ritual and finally to ascertain local interpretation of authenticity and glocal practice. The method used here was a qualitative approach employing 24 in-depth interviews with young adults (18-20 years) who had attended a prom in the UK in the last three years. The findings illustrated that the role and the social network of the individual was key to engagement with the High School Prom and also indicated a possible symbiosis of the strands of theory associated with authenticity. Diverse localised meanings of the prom performance were also identified. As the school prom is a growth market in the UK businesses should be aware of adolescents’ desire for ownership of this event and should tailor their marketing accordingly

Exploring Appropriation of Global Cultural Rituals

Adolescents, as a consequence of identification with popular culture, have been described as having homogenous consumption patterns. More recently, however, it has been recognised that ‘glocalisation’ (global practices reworked to fit local contexts) affords an opportunity for differentiation. This paper considers a recent UK phenomenon, namely that of the US high school prom, and seeks to explore the ways in which this ritual has been adopted or adapted as part of youth culture. The method employed here was mixed methods and included in-depth interviews with those who attended a prom in the last three years as well as a questionnaire distributed amongst high school pupils who were anticipating a high school prom. The findings illustrate that the high school prom in the UK is becoming increasingly integrated into the fabric of youth culture although, depending on the agentic abilities employed by the emerging adults in the sample, there is differing appropriation of this ritual event particularly in relation to attitudes towards and motivations for attending the prom. A typology of prom attendees is posited. This paper contributes to our understanding of this practice in a local context