Bioassay-directed fractionation of extracts from the fermentation broth and mycelium of the fungus Edenia sp. led to the isolation of five antileishmanial compounds, preussomerin EG1 (1), palmarumycin CP 2 (2), palmarumycin CP 17 (3), palmarumycin CP 18 (4), and CJ-12,371 (5). Compounds 3 and 4 are new natural products, and this is only the second report of compound 1. The structures of compounds 1−5 were established by spectroscopic analyses (HRMS and NMR). All metabolites caused significant inhibition of the growth of Leishmania donovani in the amastigote form, with IC 50 values of 0.12, 3.93, 1.34, 0.62 and 8.40 μM, respectively. Compounds 1−5 were inactive when tested against Plasmodium falciparum or Trypanasoma cruzi at a concentration of 10 μg/mL, indicating that they have selective activity against Leishmania parasites. Compounds 1−5 showed weak cytotoxicity to Vero cells (IC 50 of 9, 162, 174, 152 and 150 μM, respectively), however, the therapeutic window of these compounds is quite significant with 75, 41, 130, 245 and 18 times (respectively) more anti-leishmanial activity than cytotoxicity.Leishmaniasis is a major tropical disease which largely affects populations those of the developing world. According to the World Health Organization (WHO), leishmaniasis can be classified into four main forms: visceral leishmaniasis (the most dangerous because it can be mortal), cutaneous leishmaniasis (the most common form, which causes a variety of skin lesions), mucocutaneous leishmaniasis (which begins with skin ulcers that can spread, causing tissue destruction, mainly of the nose and mouth), and diffuse cutaneous leishmaniasis (produces chronic skin lesions which are very difficult to cure). 1 Current treatment against leishmaniasis is based on toxic chemotherapeutic compounds, such as sodium stibogluconate and meglumine antimonate, that have several serious side effects which themselves can be fatal to patients. 1,2 Moreover, these agents are expensive and therapies are required for relatively long durations, two characteristics which combine to exclude many patients from having access to any treatment. 1,2 While approximately 600,000 infections are officially reported each year, *Author to whom correspondence should be addressed. (Table 1), interpreted from multiplicity-edited HSQC data as 10 quaternary, two methylene, and eight methine carbons. This spectrum also had resonances for a cyclic ketone (δ C 202.0, C-4) and a naphthalene ring system [δ C 146.3 (C-1'); 110.5 (C-2'); 127.6 (C-3'); 121.9 (C-4'); 134.1 (C-4a'); 121.9 (C-5'); 127.6 (C-6'); 110.5 (C-7'); 146.3 (C-8'); 113.5 (C-8a')]. HMBC correlations supported these assignments as did data comparisons with known compounds 2 and 5. The chemical shift of the two-carbon resonance at δ C 146.3 was consistent with the placement of a dioxin bridge to C-1' and C-8' of the naphthalene core. Finally, the chemical shifts of the signals at δ C 157.2 and 147.6 were consistent with the positioning of phenolic hydroxy groups at C-5 and C-8. HMBC correlati...

Domestication Syndrome in Caimito (Chrysophyllum cainitoL.): Fruit and Seed Characteristics: The process of domestication is understudied and poorly known for many tropical fruit tree crops. The star apple or caimito tree (Chrysophyllum cainito L., Sapotaceae) is cultivated throughout the New World tropics for its edible fruits. We studied this species in central Panama, where it grows wild in tropical moist forests and is also commonly cultivated in backyard gardens. Using fruits collected over two harvest seasons, we tested the hypothesis that cultivated individuals of C. cainito show distinctive fruit and seed characteristics associated with domestication relative to wild types. We found that cultivated fruits were significantly and substantially larger and allocated more to pulp and less to exocarp than wild fruits. The pulp of cultivated fruits was less acidic; also, the pulp had lower concentrations of phenolics and higher concentrations of sugar. The seeds were larger and more numerous and were less defended with phenolics in cultivated than in wild fruits. Discriminant Analysis showed that, among the many significant differences, fruit size and sugar concentration drove the great majority of the variance distinguishing wild from cultivated classes. Variance of pulp phenolics among individuals was significantly higher among wild trees than among cultivated trees, while variance of fruit mass and seed number was significantly higher among cultivated trees. Most traits showed strong correlations between years. Overall, we found a clear signature of a domestication syndrome in the fruits of cultivated caimito in Panama.

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Plant endophytic fungi spend all or part of their lives inside host tissues without causing disease symptoms. They can colonize the plant to protect against predators, pathogens and abiotic stresses generated by drought, salinity, high concentrations of heavy metals, UV radiation and temperature fluctuations. They can also promote plant growth through the biosynthesis of phytohormones and nutrient acquisition. In recent years, the study of endophytic fungi for biological control of plant diseases and pests has been intensified to try to reduce the ecological and public health impacts due the use of chemicals and the emergence of fungicide resistance. In this review, we examine 185 patents related to endophytic fungi (from January 1988 to December 2019) and discuss their applicability for abiotic stress tolerance and growth promotion of plants, as agents for biocontrol of herbivores and plant pathogens and bio- and phytoremediation applications.

With the combined goal of finding the best anti-parasitic and anti-cancer activities as well as isolating the bioactive agents and studying their structures and biological properties, we proceeded to perform a small-scale cultivation of Aspergillus sp. strain F1544 using Potato Dextrose, Malt Extract, Czapek Dox and Eight Vegetables media. From the more promising extracts (obtaining using potato dextrose and czapek dox media in large scale) of this fungus, we isolated the five compounds: pseurotin A (1), 14-norpseurotin A (2), FD-838 (3), and pseurotin D (4), and fumoquinone B (5). All compounds showed good antileishmanial and moderate anticancer activities.

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Endophytic fungi are an important group of microorganisms and one of the least studied. They enhance their host’s resistance against abiotic stress, disease, insects, pathogens and mammalian herbivores by producing secondary metabolites with a wide spectrum of biological activity. Therefore, they could be an alternative source of secondary metabolites for applications in medicine, pharmacy and agriculture. In this review, we analyzed patents related to the production of secondary metabolites and biotransformation processes through endophytic fungi and their fields of application. We examined 245 patents (224 related to secondary metabolite production and 21 for biotransformation). The most patented fungi in the development of these applications belong to the Aspergillus, Fusarium, Trichoderma, Penicillium, and Phomopsis genera and cover uses in the biomedicine, agriculture, food, and biotechnology industries.

Chemical investigation of a new endophytic fungus, Mycosphaerella sp. nov. strain F2140 associated with the foliage of the plant Psychotria horizontalis (Rubiaceae) in Panama, resulted in the isolation of cercosporin (1) and a new cercosporin analogue (3) as the major components. The structures of minor compounds in the extract were elucidated by detailed spectroscopic analysis as 2-(2-butyl)-3-hydroxy-6-ethyl-6-methylcyclohex-2-ene-1,5-dione (4), 3-(2-butyl)-6-ethyl-6-methyl-5-hydroxy-2-methoxy-cyclohex-2-eneone (5), and an isomer of 5 (6). To study the influence of the hydroxy groups on the anti-parasitic activity of cercosporin, compound 1 was acetylated to obtain derivative 2. The isolated compounds 1–6 were tested in vitro to determine their anti-parasitic activity against the causal agents of malaria (Plasmodium falciparum), leishmaniasis (Leishmania donovani), and Chagas disease (Trypanosoma cruzi). Also, the cytotoxicity and potential anticancer activity of these compounds were evaluated using mammalian Vero cells and MCF7 cancer cell lines, respectively. Compounds 1 and 2 displayed high potency against L. donovani (IC50 0.46 and 0.64 μM), T. cruzi (IC50 1.08 and 0.78 μM), P. falciparum (IC50 1.03 and 2.99 μM), and MCF7 cancer cell lines (IC50 4.68 and 3.56 μM). Compounds 3–6 were not active in these assays at a concentration of 10 μg/mL.