ABSTRACT
CR1642D, an endophytic isolate of Penicillium sp. collected from a Costa Rican rainforest, was identified through a high-throughput approach to identify natural products with enhanced antitumor activity in the context of tumor-stromal interactions. Bioassay-guided separation led to the identification of five xanthones (1-5) from CR1642D. The structures of the xanthone dimer penexanthone A (1) and monomer penexanthone B (2) were elucidated on the basis of spectroscopic analyses, including 2D NMR experiments. All of the compounds were tested against a panel of tumor cell lines in the presence and absence of bone marrow stromal cells. Compound 3 was the most active, with IC(50) values of 1-17 µM, and its activity was enhanced 2-fold against tumor cell line RPMI8226 in the presence of stromal cells (IC(50) 1.2 µM, but 2.4 µM without stromal cells).
Subject(s)
Penicillium/chemistry , Xanthones/isolation & purification , Xanthones/pharmacology , Costa Rica , Humans , Molecular Sequence Data , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Stromal Cells/drug effects , Xanthones/chemistryABSTRACT
CONTEXT: Subcutaneous mycoses are chronic infections caused by slow growing environmental fungi. Latin American plants are used in folk medicine to treat these afflictions. Moreover, the potential of the rich Latin American biodiversity for this purpose has not been fully explored. OBJECTIVES: The aim of the study was to screen Latin American plant extracts against two species of subcutaneous fungi: Sporothrix schenckii and Fonsecaea pedrosoi. MATERIALS AND METHODS: One hundred ninety-five organic extracts from 151 Latin American plants were screened against two subcutaneous fungi by the agar dilution method at a concentration of 100 µg/mL, and minimum inhibitory concentrations (MICs) of active extracts were determined. Positive (amphothericin B) and negative (50% ethanol) controls were used. RESULTS AND DISCUSSION: Twenty eight extracts showed activity at ≤100 µg/mL. Of these, four extracts from Gnaphalium gaudichaudianum DC (Asteraceae), Plumeria rubra L (Apocynaceae), Tecoma stans (L.) Juss. ex Kunth. (Bignoniaceae), and Trichostigma octandum (L.), H. Walter showed activity against F. pedrosoi at MIC 12.5 µg/mL; and, four extracts from Bourreria huanita (Lex.) Hemsl. (Boraginaceae), Phytolacca bogotensis Kunth (Phytolaccaceae), Monnina xalapensis Kunth (Polygalaceae) and Crataegus pubescens (C. Presl) C. Presl (Rosaceae) against S. schenckii. This is the first report on antifungal activity of the Latin American plants against these two subcutaneous fungi. CONCLUSION: S. schenkii and F. pedrosoi were inhibited by B. huanita (MIC: 12.5 and 25 µg/mL), G. gaudichaudianum (MIC: 50 and 12.5 µg/mL) and T. triflora (MIC: 25 µg/mL).
Subject(s)
Antifungal Agents/pharmacology , Ascomycota/drug effects , Drug Evaluation, Preclinical , Mycoses/drug therapy , Phytotherapy , Plant Extracts/pharmacology , Sporothrix/drug effects , Amphotericin B/pharmacology , Antifungal Agents/analysis , Antifungal Agents/therapeutic use , Ethanol/pharmacology , Fungi/drug effects , Humans , Latin America , Medicine, Traditional , Microbial Sensitivity Tests , Mitosporic Fungi/drug effects , Plant Extracts/analysis , Plant Extracts/therapeutic use , Terminalia/chemistry , Terminalia/metabolismABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: This study reports the antifungal evaluation of 327 plant species (92 families and 251 genera) from seven Latin American countries which were selected on the basis of their reported ethnomedical uses and compared them with plants selected at random. AIM OF THE STUDY: (a) The main aim of this study was to investigate whether the probability of detecting antifungal plants is higher when plants have reports of ethnopharmacological uses related to fungal infections (PAU group) than when they are selected at random (PNAU group). (b) The second objective was to determine, within the PAU group, whether the probability of obtaining a positive result will be higher when the plants are tested against dermatophytes, than against yeasts or Aspergillus spp. (c) The third goal was to investigate, within all MICs
Subject(s)
Antifungal Agents , Drug Discovery/methods , Ethnopharmacology/methods , Fungi/drug effects , Health Knowledge, Attitudes, Practice , Plants, Medicinal , Antifungal Agents/pharmacology , Arthrodermataceae/drug effects , Aspergillus/drug effects , Data Collection , Drug Evaluation, Preclinical/methods , Latin America , Medicine, Traditional , Microbial Sensitivity Tests/statistics & numerical data , Phytotherapy , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Species Specificity , Statistics as Topic , Terminology as Topic , Yeasts/drug effectsABSTRACT
Rhytidhysteron rufulum is a poorly known, common, pantropical species, capable of utilizing different substrata and occupying diverse habitats, and is the only species of its genus in Costa Rica. We have employed molecular, morphological, and chemical data to assess the variability and differentiation of R. rufulum in Costa Rica, including sites from the Pacific and Atlantic coast. Phylogenetic analyses of nuclear ITS rDNA sequences revealed the presence of four distinct lineages in the R. rufulum complex. Re-examination of the morphology and anatomy showed differences between these lineages in ascomatal, ascal, and ascospore size that have previously been regarded as intraspecific variations. In addition, there was a correlation between molecular phylogenies and chemical components as determined by hplc and nuclear magnetic resonance (NMR). Two lineages (clades I and II) produced the palmarumycins MK-3018, CJ-12372, and CR(1), whereas clade III produced dehydrocurvularin, and clade IV unidentified compounds. Our results based on a polyphasic approach contradict previous taxonomic interpretations of one morphologically variable species.
Subject(s)
Ascomycota/chemistry , Ascomycota/genetics , Phylogeny , Soil Microbiology , Ascomycota/classification , Ascomycota/cytology , Costa Rica , DNA, Fungal/genetics , DNA, Ribosomal Spacer/genetics , Molecular Sequence Data , Mycological Typing TechniquesABSTRACT
From the standpoints of both basic research and biotechnology, there is considerable interest in reaching a clearer understanding of the diversity of biological mechanisms employed during lignocellulose degradation. Globally, termites are an extremely successful group of wood-degrading organisms and are therefore important both for their roles in carbon turnover in the environment and as potential sources of biochemical catalysts for efforts aimed at converting wood into biofuels. Only recently have data supported any direct role for the symbiotic bacteria in the gut of the termite in cellulose and xylan hydrolysis. Here we use a metagenomic analysis of the bacterial community resident in the hindgut paunch of a wood-feeding 'higher' Nasutitermes species (which do not contain cellulose-fermenting protozoa) to show the presence of a large, diverse set of bacterial genes for cellulose and xylan hydrolysis. Many of these genes were expressed in vivo or had cellulase activity in vitro, and further analyses implicate spirochete and fibrobacter species in gut lignocellulose degradation. New insights into other important symbiotic functions including H2 metabolism, CO2-reductive acetogenesis and N2 fixation are also provided by this first system-wide gene analysis of a microbial community specialized towards plant lignocellulose degradation. Our results underscore how complex even a 1-microl environment can be.
Subject(s)
Bacteria/metabolism , Genome, Bacterial/genetics , Genomics , Intestines/microbiology , Isoptera/metabolism , Isoptera/microbiology , Wood/metabolism , Animals , Bacteria/enzymology , Bacteria/genetics , Bacteria/isolation & purification , Bioelectric Energy Sources , Carbon/metabolism , Catalytic Domain , Cellulose/metabolism , Costa Rica , Genes, Bacterial/genetics , Glycoside Hydrolases/chemistry , Glycoside Hydrolases/genetics , Glycoside Hydrolases/metabolism , Hydrolysis , Lignin/metabolism , Models, Biological , Molecular Sequence Data , Polymerase Chain Reaction , Symbiosis , Wood/chemistry , Xylans/metabolismABSTRACT
This study describes the results and collection practices for obtaining arthropod samples to be studied as potential sources of new medicines in a bioprospecting effort. From 1994 to 1998, 1800 arthropod samples of 6-10 g were collected in 21 sites of the Area de Conservaci6n Guancaste (A.C.G) in Northwestern Costa Rica. The samples corresponded to 642 species distributed in 21 orders and 95 families. Most of the collections were obtained in the rainy season and in the tropical rainforest and dry forest of the ACG. Samples were obtained from a diversity of arthropod orders: 49.72% of the samples collected corresponded to Lepidoptera, 15.75% to Coleoptera, 13.33% to Hymenoptera, 11.43% to Orthoptera, 6.75% to Hemiptera, 3.20% to Homoptera and 7.89% to other groups. Different life stages per arthropod species were obtained in most samples, 54.26% of them were adults, 19.90% corresponded to larvae, 6.46% to pupae, 6.12% to pre-pupae, 2.07% to nymphs and 3.74% to other stages. Other materials associated to insects like frass represented 11.20% of the samples collected. Several collecting methods were explored, based on the possibility of accessing the necessary amount of material causing the less impact. Most of the samples were obtained by manual collection (44.38%),. followed by insects breeding (25.73%), light traps (18.80%), different types of nets (10.52%) and other methods (0.16%). In general, collecting methods and practices excluded the use of solvents, mixing different species or life stages in the same bag, which might have introduced undesirable effects in the screening systems for new compounds. Based on the possibility of finding new chemicals in similar samples associated to one arthropod species, the collecting strategy included the generation of several samples from same species, separated according to differences in life stages, collecting sites, ecosystems. seasons, feeding materials or behavioral aspects. This strategy allowed the generation a larger number of samples submitted to bioassays in different areas of pharmaceutical research.