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At least 739 records · Page 41Linked to original sources
PubMed2002

Chemical ecology of marine microbial defense.

Because marine animals and plants are continuously exposed to a large diversity of potentially harmful microorganisms, it seems reasonable to hypothesize that potential hosts might produce bioactive compounds to deter microbial attack. However, little is known about how host metabolites may defend against harmful microbes or facilitate the growth or colonization of helpful symbionts. While there is a large body of literature describing the antimicrobial activities of marine secondary metabolites, we are only now beginning to understand how these compounds function in an ecological context. For example, there is mounting evidence that nontoxic concentrations of secondary metabolites can have significant effects on microbial behavior, suggesting that certain host-microbe interactions are chemically mediated. Herein, we discuss the importance of employing ecologically relevant assays to elucidate microbiological effects and the need to develop a better understanding of host-microbe associations within an ecologically realistic context. Continued research in this field along with improved techniques will certainly provide further insight into how microbes have influenced the evolution of secondary metabolite production in marine organisms.

Animal Population Groups↗
PubMed2002

Chemoprevention of carcinoma prostate: a review.

PURPOSE: Chemoprevention of prostate cancer is the administration of agents to prevent, inhibit, or delay progression of prostate cancer. Opportunities exist for testing various types of chemopreventive interventsion. MATERIAL AND METHODS: The authors reviewed the relevant articles published in the last twenty years and studied the biology of the prostate cancer. An attempt is made to identify intermediate markers and surrogate endpoint markers. The various interventions and initial clinical trial results are described. End points for evaluation are mainly based on changes in PSA, changes of histological precursors, or time of onset of clinical disease. RESULTS: Nutritional factors such as reduced fat intake, vitamin A, vitamin E, vitamin C, vitamin D, Lycopene and selenium may have a protective effect against prostate cancer. CONCLUSION: Numerous studies implicate dietary and nutritional factors in the onset and progression of prostate cancer. Hence, it is possible that bioactive compounds (anti-oxidants) like vits. A, C, D, E, minerals like selenium and carotenoids like lycopene can be a part of chemopreventive strategies for prostate cancer. Ongoing studies on nutrition and prostate cancer may bring the required evidence to support what is still only a hypothesis at present. However, absolute recommendation will have to await the results of long term prospective clinical trials.

Animals↗
PubMed2003

Isolation and structural characterization of a water-soluble germination inhibitor from Scotch thistle (Onopordum acanthium) cypselas.

Cypsela dormancy in Scotch thistle (Onopordum acanthium) may be affected by the presence of chemical inhibitors. To investigate this phenomenon, a leachate from O. acanthium cypselas was tested for its ability to inhibit germination of the cypselas from which it was derived (i.e., autoinhibition). Leachates varied in their degree of autoinhibition, depending on the cypsela population from which they were prepared. Overall, removal of leachate from a group of O. acanthium cypselas increased their germinability. Using lettuce (Lactuca sativa) cypselas as an indicator species, bioactivity-guided fractionation was used to isolate a water-soluble, para-substituted benzamide from O. acanthium cypselas, which caused germination inhibition. Various chromatographic, spectroscopic, and spectrometric techniques were applied to the characterization of the bioactive compound.

Biological Assay↗
PubMed2000

Screening of basidiomycetes for antimicrobial activities.

As a part of a screening programme developed to evaluate the antimicrobial activity of basidiomycetes, 317 isolates representing 204 species collected in Spain were screened against a range of human clinical pathogens and laboratory controls. Extracts from 45% of the isolates, representing 109 species, showed antimicrobial activity. Antibacterial activity was more pronounced than antifungal activity. The proportion of extracts from basidiomycetes showing antimicrobial activity was similar to or above that obtained for representative orders of Ascomycetes, such as Pezizales and Xylariales, but lower than that produced by members of the orders Diaporthales, Eurotiales, Hypocreales, Leotiales and Sordariales. Suprageneric taxa (orders and families) did not show pronounced differences in their antimicrobial activities though such differences were observed at the genus level, suggesting that the ability to produce these bioactive compounds is not homogenously distributed amongst the basidiomycetes. Isolates from some species showed large differences in their ability to produce metabolites with antimicrobial activity, possibly reflecting genetic differences at the infraspecific level.

Anti-Bacterial Agents↗
PubMed2003

Allelochemical potential of Callicarpa acuminata.

The allelochemical potential of Callicarpa acuminata (Verbenaceae) was investigated by using a biodirected fractionation study as part of a long-term project to search for bioactive compounds among the rich biodiversity of plant communities in the Ecological Reserve El Eden, Quintana Roo, Mexico. Aqueous leachate, chloroform-methanol extract, and chromatographic fractions of the leaves of C. acuminata inhibited the root growth of test plants (23-70%). Some of these treatments caused a moderate inhibition of the radial growth of two phytopathogenic fungi, Helminthosporium longirostratum and Alternaria solani (18-31%). The chloroform-methanol (1:1) extract prepared from the leaves rendered five compounds: isopimaric acid (1), a mixture of two diterpenols [sandaracopimaradien-19-ol (3) and akhdarenol (4)], alpha-amyrin (5), and the flavone salvigenin (6)]. The phytotoxicity exhibited by several fractions and the full extract almost disappeared when pure compounds were evaluated on the test plants, suggesting a synergistic or additive effect. Compounds (4), (5), and the semisynthetic derivative isopimaric acid methyl ether (2) had antifeedant effects on Leptinotarsa decemlineata. Compound 5 was most toxic to this insect, followed by (2), (4), and (6) with moderate to low toxicity. No correlation was found between antifeedant and toxic effects on this insect, suggesting that different modes of action were involved. All the test compounds were cytotoxic to insect Sf9 cells while (6), (4), and (1) also affected mammalian Chinese Hamster Ovary (CHO) cells. Compound 5 showed the strongest selectivity against insect cells. This study contributes to the knowledge of the defensive chemistry and added value of C. acuminata.

Animals↗
PubMed2003

Potential risks and benefits of phytoestrogen-rich diets.

Interest in the physiological role of bioactive compounds present in plants has increased dramatically over the last decade. Of particular interest in relation to human health are the class of compounds known as the phytoestrogens, which embody several groups of non-steroidal oestrogens including isoflavones & lignans that are widely distributed within the plant kingdom. Data from animal and in vitro studies provide plausible mechanisms to explain how phytoestrogens may influence hormone dependent states, but although the clinical application of diets rich in these oestrogen mimics is in its infancy, data from preliminary studies suggest potential beneficial effects of importance to health. Phytoestrogens are strikingly similar in chemical structure to the mammalian oestrogen, oestradiol, and bind to oestrogen receptors (ER) with a preference for the more recently described ER beta. This suggests that these compounds may exert tissue specific effects. Numerous other biological effects independent of the ER (e.g. antioxidant capacity, antiproliferative and antiangiogenic effects) have been ascribed to these compounds. Whether phytoestrogens have any biological activity in humans, either hormonal or non hormonal is a contentious issue and there is currently a paucity of data on human exposure. Much of the available data on the absorption and metabolism of dietary phytoestrogens is of a qualitative nature; it is known that dietary phytoestrogens are metabolised by intestinal bacteria, absorbed, conjugated in the liver, circulated in plasma and excreted in urine. Recent studies have addressed quantitatively what happens to isoflavones following ingestion--with pure compound and stable isotope data to compliment recent pharmacokinetic data for soy foods. The limited studies conducted so far in humans clearly confirm that soya isoflavones can exert hormonal effects. These effects may be of benefit in the prevention of many of the common diseases observed in Western populations (such as breast cancer, prostate cancer, menopausal symptoms, osteoporosis) where the diet is typically devoid of these biologically active naturally occurring compounds. However since biological effects are dependent on many factors including dose, duration of use, protein binding affinity, individual metabolism and intrinsic oestrogenic state, further clinical studies are necessary to determine the potential health effects of these compounds in specific population groups. However we currently know little about age related differences in exposure to these compounds and there are few guidelines on optimal dose for specific health outcomes.

Animals↗
PubMed2005

Cytotoxic activities of new jadomycin derivatives.

Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.

Antibiotics, Antineoplastic↗
PubMed2005

Chemogenomic profiling on a genome-wide scale using reverse-engineered gene networks.

A major challenge in drug discovery is to distinguish the molecular targets of a bioactive compound from the hundreds to thousands of additional gene products that respond indirectly to changes in the activity of the targets. Here, we present an integrated computational-experimental approach for computing the likelihood that gene products and associated pathways are targets of a compound. This is achieved by filtering the mRNA expression profile of compound-exposed cells using a reverse-engineered model of the cell's gene regulatory network. We apply the method to a set of 515 whole-genome yeast expression profiles resulting from a variety of treatments (compounds, knockouts and induced expression), and correctly enrich for the known targets and associated pathways in the majority of compounds examined. We demonstrate our approach with PTSB, a growth inhibitory compound with a previously unknown mode of action, by predicting and validating thioredoxin and thioredoxin reductase as its target.

Algorithms↗
PubMed2025

Chromosome-level genome assembly of Elaeocarpus petiolatus (Elaeocarpaceae).

Elaeocarpus petiolatus is an ecologically and economically important species in tropical and subtropical forests. Despite its significance, the lack of genomic resources has hindered research on the genetic diversity and adaptive traits of E. petiolatus. To address this gap, we present a comprehensive chromosome-level genome assembly of E. petiolatus generated using advanced PacBio high-fidelity (HiFi) long-read sequencing and Hi-C technology. The assembly spans 322.45 Mb, with a scaffold N50 of 20.58 Mb, indicating that 37.11% of the genome is composed of repetitive elements. We identified 25,295 protein-coding genes, of which 96.74% were functionally annotated. This high-quality genome provides a critical resource for understanding the genetic mechanisms underlying environmental adaptability and biosynthesis of bioactive compounds in E. petiolatus, thereby supporting conservation efforts and sustainable forest management. The assembled genome and associated sequencing data are publicly available, facilitating further evolutionary and functional studies on the Elaeocarpaceae family.

Chromosomes, Plant↗
PubMed2002

The need to review the Spanish recommended dietary energy and nutrient intakes.

BACKGROUND: In the last decade, research in the field of nutrition has grown both in width and depth, and has incorporated the advances of other scientific fields, like artificial intelligence theories. Specifically in the case of recommended nutrient intakes, the fuzzy theory is an interesting contribution to the development of a new concept for the recommendations. The recommended intakes have passed from avoiding deficiency status to preventing several pathological aspects and reducing risk factors. OBJECTIVE: To establish whether the recommended dietary intakes for Spain (IREs) must be reviewed, taking into account the current scientific state of the art. METHODS: We have compared IREs, published in 1994, with the recently published 'Dietary Reference Intakes' (DRIs) for the American and Canadian population, the 'Referenzwerte für die Nährstoffzufuhr' (DACH) for the German, Swiss and Austrian population. In addition, the main guidelines of the EURODIET criteria (Nutrition and Diet for Healthy Lifestyles), which was developed for the population of the European Union Member States, were taken into account. As an example, comparisons were made for the elderly population group, establishing differences and similarities between the different scientific communities and the adequacy of Spanish recommended intakes for energy and nutrients. RESULTS: Recommended intakes for folate, calcium and vitamins C, D and E are lower in the IREs and probably should be increased. Recommended intakes for nutrients which have not previously been included in the IREs, such as vitamin K, selenium, copper, chromium, molybdenum, manganese, phosphorus, sodium, potassium, and water need to be developed. CONCLUSIONS: The current recommended intakes for the Spanish population need to be reviewed in order to encompass current scientific knowledge. Moreover, the opportunity to include non-nutrients (bioactive compounds) should be considered.

Adult↗
PubMed2002

Photoremovable protecting groups: reaction mechanisms and applications.

Photolabile protecting groups enable biochemists to control the release of bioactive compounds in living tissue. 'Caged compounds' (photoactivatable bioagents) have become an important tool to study the events that follow chemical signalling in, e.g., cell biology and the neurosciences. The possibilities are by no means exhausted. Progress will depend on the development of photoremovable protecting groups that satisfy the diverse requirements of new applications--a challenging task for photochemists.

Journal Article↗
PubMed2006

Dissecting non-ribosomal and polyketide biosynthetic machineries using electrospray ionization Fourier-Transform mass spectrometry.

Many virulence factors and bioactive compounds with antifungal, antimicrobial, and antitumor properties are produced via the non-ribosomal peptide synthetase (NRPS) or polyketide synthase(PKS) paradigm. During the biosynthesis of these natural products, substrates, intermediates and side products are covalently tethered to the NRPS or PKS catalyst, introducing mass changes, making these biosynthetic systems ideal candidates for interrogation by large molecule mass spectrometry. This review serves as an introduction into the application of electrospray ionization Fourier-Transform massspectrometry (ESI-FTMS) to investigate NRPS and PKS systems. ESI-FTMS can be used to understand substrate tolerance, timing of covalent linkages, timing of tailoring reactions and the transfer of substrates and biosynthetic intermediates from domain to domain. Therefore we not only highlight key mechanistic insights for thiotemplate systems as found on the enterobactin,yersiniabactin, epothilone, clorobiocin, coumermycin, pyoluteorin, gramicidin, mycosubtilin, C-1027,6-deoxyerythronolide B and FK520 biosynthetic pathways, but we also explain the approaches taken to identify active sites from complex digests and compare the FTMS based assay to traditional assays and other mass spectrometric techniques. Although mass spectrometry was introduced over two decades ago to investigate NRPS and PKS biosynthetic systems, this is the first review devoted to this methodology.

Molecular Structure↗
PubMed1992

Biochemical studies on the activity of delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine synthetase from Streptomyces clavuligerus.

The enzyme activity of purified delta-(L-alpha-aminoadipyl)-L-cysteinyl-D-valine (ACV) synthetase from Streptomyces clavuligerus was studied biochemically. The dependence of ACV synthetase activity on reaction parameters, including substrates, cofactors, temperature and pH, were determined, resulting in a substantially increased enzyme activity. The activity is very labile to high temperature and is also unstable at acidic pH. The enzyme specificity is strict towards L-alpha-aminoadipate, but rather loose with respect to L-valine; certain modifications of L-cysteine can also be tolerated. Some unnatural tripeptides synthesized by ACV synthetase can be converted into bioactive compounds by isopenicillin N synthase. The only nutrient found to negatively affect ACV synthetase activity is phosphate, but various compounds such as thiol-blocking reagents and ATP-utilization products (AMP and pyrophosphate) are inhibitory to the enzyme.

2-Aminoadipic Acid↗
PubMed2026

Proteomic profiling reveals that DPP4 overexpression increases cell adhesion, inhibits cell migration, and restores androgen sensitivity in prostate cancer.

Dipeptidyl peptidase-4 (DPP4), a serine protease with both enzymatic and non-enzymatic roles, has emerged as a context-dependent modulator of tumor progression. In the present study, we investigated the expression and function of DPP4 in androgen-sensitive and castration-resistant prostate cancer (CRPC) models. Proteomic analysis of androgen-resistant prostate cells overexpressing DPP4 identified the involvement of the cellular adhesion molecules pathway. In prostate cells, lentiviral-mediated DPP4 overexpression restored androgen receptor signaling, inhibited epithelial-to-mesenchymal transition, and reduced cell migration, whereas DPP4 silencing produced the opposite effects. We demonstrate that DPP4 expression is down-regulated in CRPC cells and that treatment with capsaicin (CAP), a bioactive compound derived from red peppers, restores DPP4 expression. Moreover, DPP4 restoration by CAP suppresses prostate tumorigenesis in the TRAMP mice in vivo model of prostate cancer. Our results suggest that DPP4 could be a new target for CRPC.

Male↗
PubMed2006

Mechanisms controlling the expression of the components of the exocytotic apparatus under physiological and pathological conditions.

The last decade has witnessed spectacular progress in the identification of the protein apparatus required for exocytosis of neurotransmitters, peptide hormones and other bioactive products. In striking contrast, our knowledge of the mechanisms determining the expression of the components of the secretory machinery has remained rudimentary. Since modifications in secretory functions are associated with several physiological processes and contribute to the development of human pathologies, a better knowledge of the control of the expression of the genes involved in exocytosis is urgently needed. Recent studies have led to the identification of transcription factors and other regulatory molecules such as microRNAs that modulate the cellular level of key controllers of the exocytotic process. These findings furnish a new perspective for understanding how secretory functions can adapt to normal physiological conditions and shed light on the mechanisms involved in the development of important human diseases such as diabetes mellitus characterized by defective release of bioactive compounds.

Animals↗
PubMed2001

Review article: herbal treatment in gastrointestinal and liver disease--benefits and dangers.

Herbal medicines are now used by up to 50% of the Western population, in a substantial minority of instances for the treatment or prevention of digestive disorders. Although most indications for the use of such remedies are anecdotally or traditionally derived, controlled trials suggest some benefits for ginger in nausea and vomiting, liquorice extracts in peptic ulceration, Chinese herbal medicine in irritable bowel syndrome, opium derivatives in diarrhoea and senna, ispaghula and sterculia in constipation. Herbal preparations contain many bioactive compounds with potentially deleterious as well as beneficial effects. There is clearly a need for greater education of patients and doctors about herbal therapy, for legislation to control the quality of herbal preparations, and in particular for further randomized controlled trials to establish the value and safety of such preparations in digestive and other disorders.

Complementary Therapies↗
PubMed1999

Interspecies complementation in Saccharopolyspora erythraea : elucidation of the function of oleP1, oleG1 and oleG2 from the oleandomycin biosynthetic gene cluster of Streptomyces antibioticus and generation of new erythromycin derivatives.

Two glycosyltransferase genes, oleG1 and oleG2, and a putative isomerase gene, oleP1, have previously been identified in the oleandomycin biosynthetic gene cluster of Streptomyces antibioticus. In order to identify which of these two glycosyltransferases encodes the desosaminyltransferase and which the oleandrosyltransferase, interspecies complementation has been carried out, using two mutant strains of Saccharopolyspora erythraea, one strain carrying an internal deletion in the eryCIII (desosaminyltransferase) gene and the other an internal deletion in the eryBV (mycarosyltransferase) gene. Expression of the oleG1 gene in the eryCIII deletion mutant restored the production of erythromycin A (although at a low level), demonstrating that oleG1 encodes the desosaminyltransferase required for the biosynthesis of oleandomycin and indicating that, as in erythromycin biosynthesis, the neutral sugar is transferred before the aminosugar onto the macrocyclic ring. Significantly, when an intact oleG2 gene (presumed to encode the oleandrosyltransferase) was expressed in the eryBV deletion mutant, antibiotic activity was also restored and, in addition to erythromycin A, new bioactive compounds were produced with a good yield. The neutral sugar residue present in these compounds was identified as L-rhamnose attached at position C-3 of an erythronolide B or a 6-deoxyerythronolide B lactone ring, thus indicating a relaxed specificity of the oleandrosyltransferase, OleG2, for both the activated sugar and the macrolactone substrate. The oleP1 gene located immediately upstream of oleG1 was likewise introduced into an eryCII deletion mutant of Sac. erythraea, and production of erythromycin A was again restored, demonstrating that the function of OleP1 is identical to that of EryCII in the biosynthesis of dTDP-D-desosamine, which we have previously proposed to be a dTDP-4-keto-6-deoxy-D-glucose 3, 4-isomerase.

Chromatography, High Pressure Liquid↗
PubMed2001

Indigenous mucuna tempe as functional food.

The aim of the present study was to obtain the nutritive and bioactive compounds of mucuna tempe and the consumer preference of its formulated snack. The tempe was made traditionally from mucuna prurience seeds using 'ragi tempe' as inoculants. Proximate, vitamin, mineral and dietary fibre analysis was done using the methods of the Association of Official Analytical Chemists, isoflavone was analysed using high performance liquid chromatography (HPLC) with an RP-18 column and a UV detector. The preference test was done using scoring methods by trained panelists. The study demonstrates that compared with soybean tempe, mucuna tempe had a higher dietary fibre level, but lower vitamin E content. The mucuna tempe contains 31.5% protein, 7.3% fat, 3.0% ash, 58.1% carbohydrate and 9.1% fibre. It contains 0.551 mg/L isoflavone aglucone; daidzin is the highest, followed by Factor II (6,7,4 trihydroxy isoflavone) that is much higher than that of soybeans tempe. These are much higher isoflavone aglucone contents than found in soybeans tempe. The preference score for a 20% mucuna tempe-based snack was not significantly different compared with control or with the preference score for a 10% soybean tempe-based snack. This preliminary study needs to be followed by both in vitro and in vivo studies.

Biological Availability↗