De quelques catéchismes créoles anciens: oublis, pertes, disparitions, réapparitions, découvertes

Il existe, dans le très vaste domaine des études postcoloniales, des territoires contigus ou semblables qui connaissent des phénomènes communs mais aux histoires très différentes, sinon radicalement opposées : tels les catéchismes - en langues romanes - fruit de la colonisation. Plus précisément, à l’histoire des catéchismes issus de la colonisation hispano-américaine, s’oppose l’histoire des catéchismes issus de la colonisation française, de l’Amérique et d’ailleurs. Ces derniers arrivent un siècle et demi environ après les espagnols et se manifestent de tout autre manière ; différents en sont l’époque, la scène et les acteurs : les destinateurs mais surtout les destinataires. Ce travail se propose de retracer l’histoire souvent aventureuse des plus anciens catéchismes des colonies ou ex-colonies françaises de la Caraïbe et de l’Océan Indien ; écrits en créole ou, parfois, en d’autres langues autochtones, ils constituent aussi des témoignages linguistiques absolument précieux. Rédigés généralement sur place, mais non toujours publiés, leur histoire est faite d’oublis, pertes, disparitions, réapparitions et découvertes. - - - In the wide field of postcolonial studies, there exist related or similar areas whose stories are nevertheless very different, if not indeed opposed. This is the case of catechisms in Romance languages (or of Romance origin), outcomes of European colonization. In particular, contradictions between the history of catechisms from Hispanic-American colonization and the catechisms produced by French colonization, in America and elsewhere. The latter appear a century and a half after the Spanish texts, and exhibit completely distinct characteristics: different periods, settings, actors, and especially recipients. I set out to recount the often adventurous history of the oldest catechisms in the French colonies, or ex-colonies, of the Caribbean and the Indian Ocean. Written in Creole or sometimes other indigenous languages, they are precious linguistic records. Compiled in the colonies, but not always published, these texts are often forgotten, lost, misplaced, resurfaced, discovered

Aurantoside K, a New Antifungal Tetramic Acid Glycoside from a Fijian Marine Sponge of the Genus Melophlus

A new tetramic acid glycoside, aurantoside K, was isolated from a marine sponge belonging to the genus Melophlus. The structure of the compound was elucidated on the basis of spectroscopic analysis (1H NMR, 1H–1H COSY, HSQC, and HMBC, as well as high-resolution ESILCMS). Aurantoside K did not show any significant activity in antimalarial, antibacterial, or HCT-116 cytotoxicity assays, but exhibited a wide spectrum of antifungal activity against wild type Candida albicans, amphotericin-resistant C. albicans, Cryptococcus neoformans, Aspergillus niger, Penicillium sp., Rhizopus sporangia and Sordaria sp

Aurantoside K, a New Antifungal Tetramic Acid Glycoside from a Fijian Marine Sponge of the Genus Melophlus

A new tetramic acid glycoside, aurantoside K, was isolated from a marine sponge belonging to the genus Melophlus. The structure of the compound was elucidated on the basis of spectroscopic analysis (1H NMR, 1H–1H COSY, HSQC, and HMBC, as well as high-resolution ESILCMS). Aurantoside K did not show any significant activity in antimalarial, antibacterial, or HCT-116 cytotoxicity assays, but exhibited a wide spectrum of antifungal activity against wild type Candida albicans, amphotericin-resistant C. albicans, Cryptococcus neoformans, Aspergillus niger, Penicillium sp., Rhizopus sporangia and Sordaria sp

Design and Synthesis of Natural Product-Based Screening Libraries

Natural products (NPs) continue to have significant impact in the area of drug discovery and development. More than 50% of the approved drugs between 1981 and 2014 were either unaltered NPs, NP derivatives or synthetic drugs inspired by NP pharmacophores. NPs have also served as lead molecules in drug development programs; noteworthy example include the semi-synthetic antifungal drugs caspofungin, anidulafungin, and micafungin that were based on NP lead compounds isolated from the fermentation products of various fungus. Other notable examples include the sponge metabolite halichondrin B that was developed into the anticancer drug eribulin, and camptothecin, a plant NP that was developed into the oncology drugs, topotecan and irinotecan. Many research groups are now utilizing isolated NPs as scaffolds for the generation of semi-synthetic analogue libraries rather than pursuing the total synthesis of a bioactive NP followed by classic medicinal chemistry. This approaches main advantage is the reduction in timelines and resource allocation, which is typically associated with de novo multi-step syntheses of a bioactive NP. Furthermore, once the NP scaffold has been isolated from the source biota rapid analogue generation and subsequent SAR data can be acquired. Thus the evaluation of a scaffold chemotype for potential lead optimization studies is quickly assessed.Thesis (PhD Doctorate)Doctor of Philosophy (PhD)School of Natural SciencesScience, Environment, Engineering and TechnologyFull Tex

Design and synthesis of a screening library using the natural product scaffold 3-chloro-4-hydroxyphenylacetic acid

The fungal metabolite 3-chloro-4-hydroxyphenylacetic acid (1) was utilized in the generation of a unique drug-like screening library using parallel solution-phase synthesis. A 20-membered amide library (3–22) was generated by first converting 1 to methyl (3-chloro-4-hydroxyphenyl)acetate (2), then reacting this scaffold with a diverse series of primary amines via a solvent-free aminolysis procedure. The structures of the synthetic analogues (3–22) were elucidated by spectroscopic data analysis. The structures of compounds 8, 12, and 22 were confirmed by single X-ray crystallographic analysis. All compounds were evaluated for cytotoxicity against a human prostate cancer cell line (LNCaP) and for antiparasitic activity toward Trypanosoma brucei brucei and Plasmodium falciparum and showed no significant activity at 10 μM. The library was also tested for effects on the lipid content of LNCaP and PC-3 prostate cancer cells, and it was demonstrated that the fluorobenzyl analogues (12–14) significantly reduced cellular phospholipid and neutral lipid levels

The Structure of Orthomorphism Graph Z2 × Z4

Abstract In this paper, we gave a theoretical proof of the fact that Orthomorphism graph of group Z2 × Z4 has maximal clique 2, by determining the structure of the graph. 2020 Mathematical Subject Classification: 05B15</jats:p

The use of isolated natural products as scaffolds for the generation of chemically diverse screening libraries for drug discovery

A diverse range of strategies leading to natural product derived or inspired screening libraries aims to increase the number of new chemical entities emerging per year. However, the use of isolated natural products as scaffolds for the semi-synthesis of larger biological screening libraries remains rare. This particular method avoids the time-consuming and resource intensive de novo synthetic strategy for scaffold production, and has become more feasible through improvements to synthetic and isolation methodologies. This Highlight examines the increasing popularity of small- to large-sized screening libraries generated directly from isolated natural products. Several of the examples detailed herein show how this strategy can lead to improvements in not only potency but also other important (and often forgotten) drug discovery parameters such as toxicity, selectivity, lipophilicity and bioavailability. However, there are still improvements to be made to this method, particularly in the choice of the natural product scaffold and the derivatising reagents used. Avoidance of known nuisance compounds or structural alert motifs (e.g. PAINS) that interfere with bioactivity screens, and impact downstream drug development will play a significant role in the future success of this methodology. Incorporation of rational design strategies that take into account the physicochemical parameters (e.g. log P, MW, HBA, HBD) of the final semi-synthetic library analogues will also facilitate the discovery and development of leads and drugs. A multi-pronged approach to drug discovery that incorporates the use of isolated natural product scaffolds for library generation will surely be beneficial.Griffith Sciences, School of Natural SciencesFull Tex

Three bioactive sesquiterpene quinones from the Fijian marine sponge of the genus Hippospongia

A sesquiterpenoid quinone, epi-ilimaquinone (1), and two sesquiterpene amino quinones, smenospongine (2) and glycinylilimaquinone (3), were isolated from the Fijian marine spongeHippospongia sp. The structures of these compounds were determined by spectroscopic analysis. Compounds 1 and 3 were reported for the first time in this study from the sponge of the genusHippospongia. Compound 1 displayed potent cytotoxic activity and showed antibacterial activity against methicillin-resistant Staphylococcus aureus, wild type S. aureus and vancomycin-resistantEnterococcus faecium and displayed antifungal activity against amphotericin-resistant Candida albicans while compounds 2 and 3 showed moderate cytotoxic activity. However, compound 1 did not show appreciable antifungal activity against wild type C. albicans, Cryptococcus neoformans,Aspergillus niger, Penicillium sp., Rhizopus sporangia or Sordaria sp

Temperature-Responsive Pyraclostrobin-Loaded Octadecane Submicrocapsules with Lowered Toxicity

Pyraclostrobin (Pyr) is one of the most effective fungicides. However, it can degrade via photolysis in water, it is toxic to aquatic life and if inhaled, it has a low solubility in water, that leads to difficulties when applying to plants by spraying. Additionally, the necessity of repeated (weekly) sprays of fungicides when the pathogen growth risk is the highest, such as at the temperature range of 24 to 36 °C and increased humidity of about 95%, leads to loss of efficiency of the fungicide and overdose of chemicals. In the present study, pyraclostrobin was microencapsulated to solve the abovementioned issues. As a core of capsules octadecane (OD) with a melting point of 28 °C was used, thus, the release of pyraclostrobin was controlled via temperature change. Pyraclostrobin-loaded submicrocapsules (PyrSMCs) were characterized using SEM, DLS, TGA/DSC, HPLC, FTIR methods; stimuli-responsivity was tested employing in vitro tests with pathogenic culture (Fungal strain of Pyrenophora teres - CPPF-453) grown in Petri dishes. Toxicity of PyrSMCs to Artemia salina was studied as well. Size of capsules was 200–600 nm along with the presence of bigger capsules with a diameter of 1–4 µm. PyrSMCs showed excellent antifungal effects above the melting point of octadecane. PyrSMCs demonstrated 29 times less toxicity than pyraclostrobin of technical grade. Overall, results show the potential of such capsules to be applied in the agricultural industry for precise agriculture strategies.</jats:p

Cytotoxic and antibacterial substances against multi - drug resistant pathogens from marine sponge symbiont: Citrinin, a secondary metabolite of Penicillium sp.

Objective: To Isolate, purify, characterize, and evaluate the bioactive compounds from the sponge-derived fungus Penicillium sp. FF001 and to elucidate its structure. Methods: The fungal strain FF001 with an interesting bioactivity profile was isolated from a marine Fijian sponge Melophlus sp. Based on conidiophores aggregation, conidia development and mycelia morphological characteristics, the isolate FF001 was classically identified as a Penicillium sp. The bioactive compound was identified using various spectral analysis of UV, high resolution electrospray ionization mass spectra, 1H and 13C NMR spectral data. Further minimum inhibitory concentrations (MICs) assay and brine shrimp cytotoxicity assay were also carried out to evaluate the biological properties of the purified compound. Results: Bioassay guided fractionation of the EtOAc extract of a static culture of this Penicillium sp. by different chromatographic methods led the isolation of an antibacterial, anticryptococcal and cytotoxic active compound, which was identified as citrinin (1). Further, citrinin (1) is reported for its potent antibacterial activity against methicillin-resistant Staphylococcus aureus (S. aureus), rifampicin-resistant S. aureus, wild type S. aureus and vancomycin-resistant Enterococcus faecium showed MICs of 3.90, 0.97, 1.95 and 7.81 μg/mL, respectively. Further citrinin (1) displayed significant activity against the pathogenic yeast Cryptococcus neoformans (MIC 3.90 μg/mL), and exhibited cytotoxicity against brine shrimp larvae LD50 of 96 μg/mL. Conclusion: Citrinin (1) is reported from sponge associated Penicillium sp. from this study and for its strong antibacterial activity against multi-drug resistant human pathogens including cytotoxicity against brine shrimp larvae, which indicated that sponge associated Penicillium spp. are promising sources of natural bioactive metabolites