O gênero Croton abriga aproximadamente 1300 espécies, muitas delas reconhecidas pela sua utilização terapêutica, que se deve a presença de grande diversidade de metabólitos secundários. Tais propriedades foram ponto de partida para investigações sobre as propriedades fitoquímicas do gênero. C. vulnerarius e C. echinocarpus são espécies endêmicas do Brasil pertencentes à seção Cyclostigma e até então pouco estudadas. Neste projeto foram extraídos, identificados e isolados componentes químicos destas espécies e analisadas as suas propriedades bioativas (antioxidante, antimicrobiana e anti-HIV). Foi verificado que, diferentemente de outras espécies da mesma seção, C. echinocarpus e C. vulnerarius não apresentam diterpenos em sua composição. No entanto, C. echinocarpus possui entre seus principais componentes um alcaloide, identificado por espectrometria de massas como coridina. Em relação às substâncias fenólicas, observamos que as espécies possuem perfis semelhantes, com alguns flavonoides em comum, sendo que o principal componente de C. echinocarpus é a apigenina vitexina e de C. vulnerarius , o derivado de campferol tilirosídeo. Em relação às atividades biológicas, foi verificado que ambas as espécies possuem potencial antioxidante e antimicrobiano contra espécies de bactérias Gram negativas, especialmente nos extratos mais ricos em compostos fenólicos. Quanto à ação anti-HIV, foi observado que a fração contendo o alcaloide coridina isolado apresentou um grande potencial de atividade anti transcriptase reversa, atingindo valores acima de 90% de atividade, mesmo para a menor concentração testada / Croton comprises approximately 1,300 species, many of them known for their therapeutic uses, which is due to the presence of a large diversity of secondary metabolites. Those properties were the starting point for research on the phytochemical characteristics of the genus. C. vulnerarius e C. echinocarpus are Brazilian endemic species belonging to section Cyclostigma. This project aimed the extraction, identification and isolation of chemical constituents from both species and the analyze of the bioactive properties of such constituents (antioxidant, antimicrobial and anti-HIV). It was found that, unlike other species of the same section, C. echinocarpus and C. vulnerarius does not present diterpenes in their composition. However, C. echinocarpus showed alkaloids among its main constituents, one of them identified by mass spectrometry as coridine. Regarding the phenolic substances, we observed that the two species have similar profiles, with some flavonoids in common. C. echinocarpus presents the flavone C-glycosylated vitexin as its main flavonoid constituent, while C. vulnerarius has the acylated derivative of kaempferol, tiliroside. Regarding the biological activities, both species showed antioxidant potential; antimicrobial effects against Gram-negative bacteria, especially the extracts richer in vitexin; and anti-HIV activity, where the fraction containing the alkaloid coridine showed great potential, reaching values above 90% of the anti-HIV activity, even when the lowest concentration was tested (100 mg.mL-1)

Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Student: Jiří Olšar Supervisor: doc. PharmDr. Tomáš Siatka, CSc. Title of diploma thesis: Podophyllotoxin in eastern red cedar (Juniperus virginiana) This thesis describes the optimisation of the extraction process for quantity determination of podophyllotoxin in the leaves of Juniperus virginiana L. This determination was conducted through three different methods: the extraction in ultrasound bath, the extraction in the orbital shaker and the maceration in cold environment of 4 řC. Extractions were affected by various factors which were monitored, for instance time of extraction, temperature, and extraction solvents. The most efficient method appears to be the extraction in ultrasound bath with the use of methanol or a combination of phosphate buffer with ethyl-acetate.

>Magister Scientiae - MSc / Marine invertebrate associated (MIA) bacteria are an important source of bioactive secondary metabolites with the potential to address the current anti-microbial resistance crisis experienced globally. Secondary metabolites (SM) have historically yielded several compounds with pharmaceutical applications such as anti-viral, anti-microbial, anti-cancer, anti-inflammatory and anti-parasitic. This study aimed to use bioassay and genomic approaches in the identification of MIA bacteria isolated from South African marine invertebrates as a source of bioactive compounds and the characterisation of the produced SMs using analytical techniques. A total of 23 MIA bacteria were cultured under different conditions (one strain many compounds approach (OSMAC)) to evaluate their ability to produce anti-microbial compounds against a panel of indicator strains namely Escherichia coli 1699, Bacillus cereus ATCC10702, Pseudomonas putida ATCC12633, Mycobacterium aurum A+, Staphylococcus epidermidis ATCC14990, Aspergillus fumigatus MRC and Candida albicans NIOH.

Ministry of Higher Education; Sultanate of Oman / Digital full-text is unavailable. Submitted disc unusable.

This thesis describes the isolation and structure elucidation of secondary metabolites formed in static culture from a number of endophytic Xylariaceous fungi. Four Xylaria endophytes isolated from a palm tree in Thailand were surface cultured on an aqueous malt extract-glucose medium. They all produced cytochalasin D, coriloxin, (S)-mellein and (3R,4R)-4-hydroxymellein as the main secondary metabolites suggesting that the four endophytes could be the same species. The endophytic fungus A116 produced cytochalasin D as the main secondary metabolite. Another non-endophytic fungus B315, produced cytochalasin D, (R)-mellein, a mixture of two isomers of 4-hydroxymellein and phloroglucinol. X.62, an endophytic fungus, produced 19,20-epoxycytochalasin C from the mycelium as the main secondary metabolite. The fungus Engleromyces sinensis produced engleromycin acetate as the main secondary metabolite. Fungus X. polymorpha produced (3E)-4-(3¿-acetyl-2¿,6¿-dihydroxy-5¿-methylphenyl)-2-methoxybut-3-enoic acid. / Ministry of Higher Education; Kingdom of Saudi Arabia.

<p>Over the last two decades, mycoflorostic studies undertaken in Guyanese forests have uncovered hundreds of new fungal species and genera. One of the recovered fungal families was the Xylariaceae, although most were not identified to species. Members of this family play ecological roles as decomposers, endophytes, and pathogens of vascular plants and grass species. In addition, this group is increasingly recognized as a significant source of novel metabolic products with potential for applications in medicine, agriculture, and industrial biofuel. Given its potential, we took a more targeted approach to the documentation of this group. Our sampling efforts drawing on more than two decades of field collections yielded ca. 90 species in 12 genera, including a putative pathogen, <em>Xylaria karyophthora</em> of the seeds of <em>Chlorocardium</em> spp (Greenheart). Despite the significance of Greenheart to the Guyanese economy, little is known about the biology and ecology of this fungus. Due to the lack of available resources to study this fungus, our objectives were two-fold: first, to sequence and annotate the genome of <em>X. karyophthora</em> to provide a resource for genome-centric explorations, and to use this genome to infer the biology and ecology of this fungus. We focused on identifying and characterizing secretomes, viz. carbohydrate-active enzymes (CAZymes) and secondary metabolites biosynthetic gene clusters (SMBGCs) to infer the nutritional strategy of this fungus. Our results suggest that <em>X. karyophthora</em> has the capacity to act as both an endophyte and a pathogen. To make further inferences about the population, we used SSR markers to elucidate the genetic diversity and population structure of <em>X. karyophthora</em>. <em>X. karyophthora</em> populations have high genetic diversity, potentially exploiting both outcrossing and inbreeding reproductive strategies, and demonstrate a pattern consistent with human-mediated spread. This work will contribute information on new species and records of Xylariaceous fungi and their allies from Guyana with particular emphasis on unraveling the epidemiology, genetic diversity, and population structure of <em>X. karyophthora.</em></p>

This thesis describes the isolation and structure elucidation of secondary metabolites from a number of endophytic Xylaria fungi. Six Xylaria endophytes were surface cultured on an aqueous malt extract-glucose medium. The fungus A311R, from a palm tree in Thailand, produced nonane-1,2,3-tricarboxylic acid, which was isolated for the first time as a natural product. Also isolated from the same fungus was spiculisporic acid; the first instance of isolation from a Xylaria fungus. The fungus 6RD12 produced cycloepoxydon, which was isolated for the first time from a Xylaria fungus, and 4,5,6-trihydroxy-3-propyl-3,4,6,7-tetrahydro-l//-isochromen- 8(5//)-one, which is a novel compound. The fungi A217R and A517R produced cytochalasin D, (S)-mellein and (3S,4S)-4-hydroxymellein as main secondary metabolites suggesting that the two fungi are the same species. The fungus X04 (Xylaria cf. juruensis) produced 2-Hydroxy-5-ethoxy-3-methylcyclohexa-2,5-dien- 1,4-dione as a novel compound, coriloxin as the main secondary metabolite in addition to (R)-mellein and a mixture of two stereoisomers of the 4-Hydroxymellein. The fungus 6RD8 produced (S)-Omethylmellein as the main secondary metabolite. l

Expanding global populations, unequal food distribution and disease pressure suggest food poverty is increasing. Consequently, much attention is focussed on alternative natural methods in which to increase agricultural yield. Previously, it was observed that Trichoderma hamatum strain GD12 and its respective N-acetyl-β-D-Glucosamine mutant ∆Thnag:hph promoted plant biomass and fitness that, as a result, may provide a credible natural alternative to synthetic fertilisers. However, on a molecular level, the manner in which this is achieved has not been fully elucidated. In this thesis, I report the biofertiliser effect of GD12 and mutant ∆Thnag::hph once applied to autoclaved peat microcosms as sole applications. Furthermore, I demonstrate the biocontrol ability of GD12 when co-inoculated with Sclerotinia sclerotiorum or Rhizoctonia solani and reveal, that once mycelium co-inoculation has occurred, GD12 increase plant biomass and provide protection; whilst ∆Thnag::hph does not. Consequently, I challenged the biocontrol effects of Trichoderma metabolite extract where I validate that both Trichoderma wild type GD12 and mutant ∆Thnag::hph are incapable of suppressing pathogen growth. Subsequently, I characterised the up-regulated signatures associated with GD12 and ∆Thnag::hph using LC-MS techniques where unique compounds were discovered from each strain of Trichoderma. In conclusion, I provide evidence that N-acetyl-β-D-Glucosamine mutation bring about metabolomic changes that affect the fungal secretome which, in turn, alters plant phenotype, fitness and germination. Furthermore, I have shown that these effects are species specific and depend upon pathogen, plant and fungal properties. However, further investigations are needed to fully elucidate the compound(s) responsible for biocontrol and biofertilisation; especially plant-specific effects that take place as a consequence of fungal activity.

No description available.

This thesis describes the isolation and structure elucidation of secondary metabolites formed in static culture from a number of endophytic Xylariaceous fungi. Four Xylaria endophytes isolated from a palm tree in Thailand were surface cultured on an aqueous malt extract-glucose medium. They all produced cytochalasin D, coriloxin, (S)-mellein and (3R,4R)-4-hydroxymellein as the main secondary metabolites suggesting that the four endophytes could be the same species. The endophytic fungus A116 produced cytochalasin D as the main secondary metabolite. Another non-endophytic fungus B315, produced cytochalasin D, (R)-mellein, a mixture of two isomers of 4-hydroxymellein and phloroglucinol. X.62, an endophytic fungus, produced 19,20-epoxycytochalasin C from the mycelium as the main secondary metabolite. The fungus Engleromyces sinensis produced engleromycin acetate as the main secondary metabolite. Fungus X. polymorpha produced (3E)-4-(3'-acetyl-2',6'-dihydroxy-5'-methylphenyl)-2-methoxybut-3-enoic acid.