Medicinal chemistry from fungi and back: discovery of novel anti-fungal drugs and mycotherapy of cancer and other diseases with fungal metabolites

Fungi are important organisms for human population and could find important applications namely, in many pharmaceutical and food industries. A variety of compounds has been isolated from medicinal and edible mushrooms, and their healthbeneficial effects have been reported. On the other hand, it is important to control microfungi as parasites and contaminants since they can provoke, in some cases, serious issues to human health. The following issue is devoted to recent findings in the fields of novel antifungal drugs, mycotherapy of cancer and other diseases with compounds recently isolated from fungi. It is covered by eight hot topic manuscripts from the mentioned relevant fields. A review on antifungal activity of mushrooms (Basidiomycetes) and their isolated compounds including high (e.g. peptides and proteins) and low (e.g. sesquiterpenes and other terpenes, steroids, organic acids, acylcyclopentenediones and quinolines) molecular weight compounds is presented. Furthermore, antioxidant protective effects of mushroom metabolites is presented covering antioxidant features of numerous compounds isolated from mushrooms, such as phenolic compounds, vitamins, polysaccharides, peptides, proteins, organic acids, carotenoids, alkaloids, and nucleotides. Cyclodextrins are usually used in antifungal formulations as auxiliary substances to improve solubility, stability, or other physicochemical properties of the active compound. Nevertheless, recent research and practical use results indicate that cyclodextrins might also act as active compounds in pharmaceutical formulations. Furthermore, Recent advances in synthesis of compounds and their biological evaluation considering antifungal activity is also presented, covering the broad spectrum of compounds from different chemical classes. Therapeutic properties of mushrooms in managing adverse effects in the metabolic syndrome deeply discusses the use of edible mushrooms, their extracts, polysaccharide fractions and isolated compounds as hypoglycaemic agents, as holders of cholesterol and triglyceride lowering ability, hypotensive agents, as well as weight managing holders. New and highly potent antitumor natural products from marine-derived fungi presents recent finding on cytotoxic activities of fungal compounds. Essential oils for the control of fungi and the production of aflatoxins, especially the most toxic aflatoxins B1 and G1, is essential and decisive, therefore highlighting the possibilities of utilizing essential oils in biological control of aflatoxin contamination. The last paper focuses on recent update of cytotoxic and antitumor activity of mushroom extracts and compounds belonging to the heteropolysaccharides, β-glucans, α-glucans, proteins, complexes of polysaccharides with proteins, fatty acids, nucleoside antagonists, terpenoids, sesquiterpenes, lanostanoids, sterols and phenolic compounds. Molecular mechanisms of cytotoxic and antitumor activities are briefly discussed

Antifungal activity of ethanolic extract of Phlomis fruticosa L.

In the ethanolic extract of Phlomis fruticosa L. two flavonoid aglycones, luteolin and chrysoeriol were identified. Antifungal activity of the total ethanolic extract, extract hydrolyzed with β-glucosidase and that hydro-lyzed with HCI against seven micromycetes: Aspergillus niger, A. ochraceus, Penicillium ochrochloron, Cladosporium cladosporioides, Thchoderma viride, Fusamim tricinctum and Phomopsis helianthi was tested. The ethanolic extract hydrolyzed with HCI possessed the greatest antifungal activity against all fungal species tested.U etanolnom ekstraktu vrste Phlomis fruticosa L. identifikovana su dva aglikona flavonoida, luteolin i hrizoeriol. Antifungaliia aktivnost ukupnog etapolnogekstrakta, etanolpog ekstrakta hidrolizovapog β-glukozidazom i ekstrakta hidrolizovanog hlorovodoničnom kiselinom istraživana je na sedam mikromiceta: Aspergillus niger, A. ochraceus, Penicillium ochrochloron, Cladosporium cladosporioides, Trichoderma viride, Fusarium tricinctum i Phomopsis helianthi. Najosetljivije mikromicete cy P. helianthi i C. cladosporioides. Pomenute vrste pokazale su najmanju rezistentnost na sva tri ispitivana ekstrakta. Mikromicete koje su pokazale najveću rezistentnost na sva tri ispitivana ekstrakta su P. ochrochloron i T. viride. Ukupni etanolni ekstrakt pokazao je najmanji antifungalni potencijal. Etanolni ekstakt hidrolizovan enzimom pokazuje porast antifungalnog potencijala, dok etanolni ekstrakt hidrolizovan hlorovodoničnom kiselinom poseduje najveći antifugalni potencijal.Projekat ministarstva br. 03E08/1, 03E2

Editorial: Antioxidants and prooxidants: effects on health and aging

Reactive species are compounds related to two types of molecules, the reactive oxygen species and the reactive nitrogen species. These compounds are produced in the normal metabolism of cells and may take part in the pathological process named oxidative stress, which is promoted when the balance between free radicals and antioxidants tends to favour the former. As a result, the excess of free radicals within the human body leads to oxidative stress, resulting in the development or potentiation of many types of diseases, namely, chronic disorders, cardiovascular problems, diabetes, cancer, and rheumatoid arthritis [1].info:eu-repo/semantics/publishedVersio

Antibacterial and antifungal activity of the liverwort (Ptilidium pulcherrimum) methanol extract

The antimicrobial activity of the methanol extract from the liverwort, Ptilidium pulcherrimum was evaluated against five bacterial and six fungal species. In vitro antibacterial activity was assessed by disc diffusion and microdilution methods. The extract showed a stronger effect against tested Gram (+) than Gram (-) bacteria. The antifungal activity of the methanol extract was tested using a microdilution method. The methanol extract showed strong antifungal activity. The best antifungal activity was achieved against Trichoderma viride compared to the synthetic fungicide bifonazol

Hibiscus sabdariffa L. como uma fonte de nutrientes, compostos bioativos e agentes corantes

As plantas são uma fonte de pigmentos naturais que podem ser utilizados como corantes alimentares com baixo risco de toxicidade e com benefícios nutricionais e bioativos. Esta temática despertou o interesse da comunidade científica e desencadeou estudos com o objetivo de explorar matrizes naturais como fonte de compostos bioativos e corantes. Neste trabalho, a composição química de Hibiscus sabdariffa L. em compostos hidrofílicos (açúcares e ácidos orgânicos) e lipofílicos (ácidos gordos e tocoferóis) foi determinada por técnicas cromatográficas. Além disso, foram avaliadas as propriedades bioativas (antioxidante e antimicrobiana) e o perfil fenólico dos seus extratos aquoso e hidroetanólico. A frutose e a glucose foram os açúcares livres detetados, estando este último presente em maior quantidade (6,5±0,6 g/100 g massa seca). Foram identificados quatro ácidos orgânicos, ácido oxálico, málico, shiquímico e fumárico, destacando o ácido málico que foi encontrado em maior concentração (9,10±0,09 g/100 g). Quanto aos tocoferóis foram identificados os vitâmeros α e β-tocoferóis, sendo o α-tocoferol o mais abundante (39,19±0,06 mg/100 g). Na determinação do perfil de ácidos gordos, foram identificados 18 compostos, evidenciando-se o ácido linoleico com uma contribuição de 32,65±0,07%. Na avaliação do potencial antioxidante e antimicrobiano, ambos os extratos apresentaram atividade. Analisando o perfil fenólico, foram identificados 12 compostos, sendo o 5- (hidroximetil)furfural e a delfinidina-3-O-sambobiósido as moléculas não-antociânica e antociânica mais abundante, respetivamente. Tendo em conta os resultados obtidos, esta espécie revelou ser uma fonte promissora de compostos bioativos e corantes, que poderá ser explorada pelas indústrias alimentar, cosmética e farmacêutica.info:eu-repo/semantics/publishedVersio

Effects of a 26-weeks shallow water head-out aquatic exercise program in the anthropometrics, body composition and physiological response of healthy middle-age women

The aim of this study was to assess the chronic adaptations (anthropometrics, body composition, physiologic) of the middle-aged women participating in a head-out aquatic exercise program during 26 weeks. Twenty-three healthy middle-age female subjects participated in a head-out aquatic exercise program (26 weeks, two sessions per week, and 40 minutes per session). Data was collected before starting the program (pre-test), at the 13th week (post-test 1) and at the 26th week (post-test 2). Anthropometrical data included body mass, body mass index and several anatomical perimeters. Body composition was assessed measuring several body skinfolds. Physiological measures included the resting heart rate, systolic, diastolic and mean blood pressures. The body mass and the body mass index presented non-significant improvements throughout the program. On the other hand, subjects improved their body composition, decreasing the fat mass. Main improvements happened in the first 13 weeks, since most variables did not presented significant improvements between the post-test 1 and post-test 2. As a conclusion, a head-out aquatic exercise program with 26 weeks promotes a significant improvement in the anthropometrics, body composition and physiological response of healthy middle-age women

Chemical, nutritive composition and a wide range of bioactive properties of honey mushroom: Armillaria mellea (Vahl: Fr.) Kummer

A. mellea fruiting bodies collected from nature were chemically characterized and shown to be rich in carbohydrates (81.25 g per 100 g dw), ash, fat and proteins (8.84 g per 100 g dw, 1.97 g per 100 g dw and 1.81 g per 100 g dw, respectively). Mannitol was the main free sugar while malic acid was the most abundant organic acid. d-Tocopherol was the dominant form of tocopherols with 42.41 µg per 100 g dw. Polyunsaturated fatty acids were predominant, followed by saturated and monounsaturated fatty acids. A methanolic extract prepared from these samples was tested for antioxidant, quorum sensing and antimicrobial assays, as well as for its cytotoxicity effects. The extract showed antimicrobial activity against all tested microorganisms, including Candida albicans. Furthermore, when tested at sub-MIC concentration, it showed reduction of virulence factors and biofilm formation against Pseudomonas aeruginosa. The extract also exhibited antioxidant activity and did not show toxicity against tumor and non-tumor cells. Due to the observed bioactive properties and compounds of the honey mushroom and its well-balanced nutrients, this mushroom emerges as an interesting functional food and a source of nutraceuticals with applications in different diseases based on antioxidant and antimicrobial effects.The authors are grateful to the Serbian Ministry of Education, Science and Technological Development, grant number 173032 for financial support. The authors are also grateful to the Foundation for Science and Technology (FCT, Portugal) and FEDER under Programme PT2020 for financial support to CIMO (UID/AGR/00690/2013) and L. Barros contract.info:eu-repo/semantics/publishedVersio

Antibacterial and antifungal activity of the liverwort (Ptilidium pulcherrimum) methanol extract

The antimicrobial activity of the methanol extract from the liverwort, Ptilidium pulcherrimum was evaluated against five bacterial and six fungal species. In vitro antibacterial activity was assessed by disc diffusion and microdilution methods. The extract showed a stronger effect against tested Gram (+) than Gram (-) bacteria. The antifungal activity of the methanol extract was tested using a microdilution method. The methanol extract showed strong antifungal activity. The best antifungal activity was achieved against Trichoderma viride compared to the synthetic fungicide bifonazol.Antibakterijsko i antifungalno dejsto metanolnog ekstrakta jetrenjače Ptilidium pulcherrimum ispitivano je na 5 vrsta bakterija i 6 mikromiceta. Za ispitivanje in vitro antimikrobnog dejstva ekstrakta korišćena je metoda mikrodilucije na mikrotitracionim pločama i metoda difuzije sa filter diskova. Ekstrakt je pokazao jači efekat na testirane Gram (+), nego na Gram (-) bakterije. Antifungalna aktivnost metanolnog ekstrakta ispitana je mikrodilucionom metodom. Testirani ekstrakt pokazao je jak antifungalni potencijal na Trichoderma viride, Bifonazol je pokazao skoro identičnu fungistatičku aktivnost, dok je njegova fungicidna aktivnost bila nešto viša u poređenju sa metanolnim ekstraktom analizirane jetrenjače.Projekat ministarstva br. 143049 i 14304

Antimicrobial activity of secondary metabolites isolated from Centaurea spruneri Boiss. & Heldr.

Two coumarins, scopoletin (1) and isoscopoletin (2), two simple phenolic acids, protocatechuic acid (3) and isovanillic acid (4) and one flavonoid, eriodictyol (5) were isolated from the aerial parts of Centaurea spruneri. The structure of the compounds was established by spectroscopic methods. The in vitro antimicrobial activity of the isolated compounds was tested against eight bacteria and eight fungal species, using a microdilution method. All compounds tested showed moderate antibacterial and antifungal activities. Their minimum inhibitory concentrations were in the range 0.655-2.38 µmol ml-1 and their minimal bactericidal concentrations ranged from 0.694 to 4.15 µmol ml-1 against the tested bacterial species. All compounds showed fungistatic activity at 0.259-2.38 µmol ml-1 and fungicidal at 0.69-2.6 µmol ml-1 against all fungi tested.Iz nadzemnog dela Centaurea spruneri izolovana su dva kumarina skopoletin (1) i izoskopoletin (2), dve proste fenolske kiseline protokatehuinska kiselina (3) i izovanilinska kiselina (4) i flavonoid eriodiktiol. Hemijske strukture poznatih jedinjenja su utvrđene korišćenjem 1D i 2D NMR, MS i UV spektroskopskih analiza. U in vitro testu za određivanje antimikrobne aktivnosti izolovanih jedinjenja korišćena je mikrodiluciona metoda. Dobijena jedinjenja testirana su na po osam bakterijskih i gljivičnih vrsta. Sva jedinjenja su imala umerenu antibakterijsku i antifungalnu aktivnost. Minimalna inhibitorna koncentracija testiranih jedinjenja se kretala od 0,655 do 2,38 µmol ml-1, a minimalna baktericidna koncentracija 0,694-4,15 µmol ml-1. Testirana jedinjenja su pokazala fungicidnu aktivnost od 0,259-2,38 µmol ml-1 i fungistatičku 0,694-2,60 µmol ml-1, na sve testirane gljive.Projekat ministarstva br. 14304