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An Irish strain of the dinoflagellate Amphidinium carterae was previously shown to produce antibacterial amphidinol derivatives of unknown masses. Inspection of the major metabolites present in a bulk culture of this strain led to the isolation and structure elucidation of a new amphidinol derivative named amphidinol C featuring an unprecedented tetrahydropyran ring between the positions C-7 and C-11. The structure was determined using extensive analyses of NMR and MS data and comparison with data of analogues. The new ring was proposed to stem from a nucleophilic substitution of the sulphate present on the side chain of Amphidinol B. The major metabolites isolated were tested for their antibacterial and antifungal activities and Amphidinol C showed moderate fungicidal activity against yeast and filamentous fungi at 8–16 µg mL−1. [Display omitted] • Amphidinol C was isolated from an Irish strain of the dinoflagellate Amphidinium carterae. • Amphidinol C features an unusual tetrahydropyrane ring between the positions C-7 and C-11. • The tetrahydropyrane ring could result from the substitution of the sulphate group of amphidinol B. • Amphidinol C exhibited moderate fungicidal activity. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • 5-Arylbenzofuran neolignan (1) was semi-synthesized from honokiol in a high yield. • Twenty-four 5-arylbenzofuran neolignan derivatives were synthesized. • Several derivatives displayed potent fungicidal and insecticidal activity. • Promising compounds showed low toxicity in the model of human cells. Abstract As shown in a number of previous researches, the extracts of Magnolia officinalis exhibited broad-spectrum fungicidal and insecticidal activity. In our preliminary study, 5-arylbenzofuran neolignans, the secondary metabolite of Magnolia officinalis , was found to inherit the activity of Magnolia officinalis. For developing novel agrochemicals, natural 5-arylbenzofuran neolignan was selected as lead compound. After structural optimization, the fungicidal and insecticidal activity and selectivity were significantly improved. Compounds 5a , 5b , 6c and 6d displayed similar or equivalent activity compared with the positive controls against corresponding fungi or pests. Especially, compounds 6c and 6d exhibited the most promising insecticidal ability against Aphis fabae with the LC 50 values of 3.56 mg/L and 5.96 mg/L, respectively. The preliminary structure-activity relationship was obtained, and the promising derivatives showed low toxicity in the model of human cells. The results of research indicated great potential of 5-arylbenzofuran neolignan derivatives in the field of fungicide and insecticide. [ABSTRACT FROM AUTHOR]

[Display omitted] The phyto nanotechnology strategy was executed for the genesis of zinc oxide nanoparticles by applying bark aqueous extract of Acacia nilotica (AN-ZnO NPs). The AN-ZnO NPs emergence was substantiated through a distinct peak at 350 nm in the ultraviolet–visible spectroscopy. The fourier transform infrared spectroscopy exposed the phyto-organic moieties engaged as reduction and stabilization factors in fabricating nanoparticles. The crystalline trait, elemental proportions, spherical and hexagonal geometry of AN-ZnO NPs was witnessed by X-ray diffraction, energy-dispersive X-ray analysis and scanning electron microscopy. The high-resolution transmission electron microscopic technique provided the average size of 35 nm. AN-ZnO NPs presented larger inhibition zone against Candida albicans (22.7 ± 0.32 mm) at 40 µg/mL as an effectual fungicidal agent. Execution of in vitro antiradical scavenging assay of AN-ZnO NPs applying 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), hydroxyl radical (OH–), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid) displayed radical scavenging trait with the minimum inhibitory concentration (IC 50) of 34.54 µg/mL, 38.0 µg/mL, 41.34 µg/mL, and 35.41 µg/mL, respectively. Cytotoxic feature against MCF-7 cell line was in a dose-manner with IC 50 value of 37.15 µg/mL in addition to apoptotic proteins expressions were displayed by AN-ZnO NPs. An appreciable larvicidal role of AN-ZnO NPs was rendered against Anopheles stephensi with LD 50 (0.31 ppm) and LD 90 (0.59 ppm), besides acetylcholinesterase inhibition. Further, biofilm origination was remarkably ceased by the Staphylococcus aureus and Klebsiella pneumoniae , respectively. All our experimented reports on AN-ZnO NPs attested the credible applicability of ZnO NPs in biomedical care for health troubles. [ABSTRACT FROM AUTHOR]

Candida infections vary in severity and manifestation. Common infections include invasive bloodstream infections among hospitalized/immunocompromised patients and vulvovaginal candidiasis among women. Echinocandins and azoles are commonly utilized to treat Candida infections, although echinocandin use has been restricted to indications amenable to once-daily IV administration. CD101, a novel echinocandin with a long plasma half-life and enhanced stability, is in development for once-weekly IV administration for the treatment of candidemia and invasive candidiasis. In this study, the MIC of CD101 and comparators against 500 recent clinical Candida isolates was determined per Clinical and Laboratory Standards Institute guidelines. For select isolates, the minimum fungicidal concentration (MFC; n = 49) and time-kill ( n = 9) of CD101 and comparators was evaluated. The MIC 50/90 s (μg/mL; n = 100/species) for CD101, anidulafungin, fluconazole, and amphotericin B, respectively, were: C. albicans (0.008/0.03, 0.004/0.008, 0.25/4, 0.25/0.5), C. tropicalis (0.008/0.03, 0.004/0.015, 0.5/2, 0.5/1), C. parapsilosis (1/1, 0.5/2, 0.5/1, 0.5/1), C. glabrata (0.03/0.03, 0.03/0.03, 8/>32, 0.5/0.5), and C. krusei (0.03/0.03, 0.03/0.03, 32/>32, 1/1). CD101 MICs were comparable to anidulafungin and both maintained potency against fluconazole-resistant isolates. Against rare anidulafungin-resistant isolates, the MICs of CD101 and anidulafungin were elevated vs. anidulafungin-susceptible isolates. Similar to anidulafungin, CD101 was fungicidal with an MFC:MIC ratio ≤4 for 95% of evaluable isolates and resulted in 3-log killing by 24–48 h for all isolates evaluated by time-kill. The potent fungicidal activity of CD101 highlights the potential clinical utility of CD101 IV for the treatment of invasive candidiasis and candidemia. [ABSTRACT FROM AUTHOR]

Multifunctional redox-active pyocyanin (PYC) produced by Pseudomonas aeruginosa has diverse biotechnological applications, but no efforts have been made to improve its yield. The yield obtained in initial study using Pseudomonas spp. MCC 3145 was 24.21 mg L −1 PYC in pigment production medium D; hence, optimization of the media components using statistical tools for more production of PYC was undertaken. Of the 11 medium constituents screened for PYC production using Plackett–Burman design (PBD), glycerol, peptone, and CuSO 4 were recognized as the most significant variables. The optimal concentration of the variables for maximum PYC production was evaluated using a five-level three-factor central composite design (CCD). Optimal concentration of the three variables, glycerol, peptone and CuSO 4 showed 313.94 ± 10.09 mg L −1 the PYC production, with an 18-fold increase. Fine structural details of PYC were verified by chromatographic and various spectroscopic analyses. In vitro bioactivity studies demonstrated significant antifungal activity of PYC against fungal phytopathogens and substantial cytostatic activity against four major cancer cell lines. Furthermore, PYC displayed nonspecific DNA intercalation, which may be the reason for proliferation arrest in cancer cells. Thus, the study rigorously improved PYC production through medium optimization and further demonstrated its agricultural and therapeutic applications. [ABSTRACT FROM AUTHOR]

The plant growth promoting bacterial strain 213B was isolated from rice rhizosphere and identified with phenetic, fatty acid profiling, 16 S ribotyping (NCBI accession no. KF291253) and phylogenetic tree as Pseudomonas spp. The strain demonstrated multiple plant growth promoting traits including phosphate solubilization production of indole-3-acetic acid (IAA), hydrogen cyanide (HCN), ammonia and secreted different bioactive metabolites including phenazine, biosurfactant and siderophore. Mung bean ( Vigna radiata ) seed coated with the strain had shown enhanced seed germination and plant root length. Besides, the strain exhibited significant tolerance against common agricultural contaminants like salt, metals, herbicide and pesticides. Of the bioactives, strain was able to produce yellow colored phenazine derivatives in Pigment Production Medium D (PPMD) after 96 h at 28 ℃ and 120 rpm. The yellow compound was extracted and purified to obtain needle crystals and further characterized by HPLC, FTIR, LCMS, 1 H and 13 C NMR, EDAX and XRD analysis as phenazine-1-carboxylic acid (PCA). The purified PCA showed profound fungicidal activity against major phytopathogens including Colletotrichum circinans , Colletotrichum dematium , Fusarium oxysporum , Rhizoctonia solani and Sclerotinia sclerotiorum , while, substantial cytostatic activity (<10 μg ml -1 ) against breast (MCF-7), lung (A549), cervical (HeLa) and liver (Hep-G2) cancer cell lines in dose dependent manner. Thus, the present study unraveled the innate plant growth promoting Pseudomonas spp. MCC 3145 with biotic and abiotic stress tolerant attributes. Besides, the organism was able to produce PCA having fungicidal and cytostatic competency for therapeutic use and for sustainable crop production. [ABSTRACT FROM AUTHOR]

Apples are susceptible to various fungal infections following harvest, resulting in significant losses. This study aimed to develop an essential oil based gel formulation to control the postharvest rot of apples caused by Aspergillus foetidus CBS121.28 and increase their shelf life during storage. In vitro, minimal fungistatic and fungicidal doses of MEO and constituents acting in the vapour-phase were established. MFC (Minimum Fungicidal Concentration) for MEO was 1153.85 µL L−1 air, hexanal 384.62 µL L−1 air, and carvacrol 96.15 µL L−1 air. The combinatorial treatment of MEO and constituents indicated synergy (FICI 0.375) between MEO (144.23 µL L−1 air) and hexanal (96.15 µL L−1 air). In contrast, the combination of MEO and carvacrol was antagonistic. In vivo treatment of MEO and hexanal combination on apple fruit by direct fumigation resulted in phytotoxicity. However, the phytotoxicity was remediated using the gel formulations incorporating various concentrations of MEO and hexanal combinations (Carrageenan guar gum gel and soft gel), which showed a synergistic effect (FICI 0.25 and 0.375, respectively). The gel formulations reduced the weight loss, suppressed the degradation of ascorbic acid, and prevented the change of pH and total soluble solids of the stored apples. The antioxidant activity and total phenolic content also increased in the stored apples. These findings suggest that using MEO and hexanal in a gel formulation is a more effective and organic way to protect apples from Aspergillus rot for an extended storage period. • MEO and hexanal showed protection in synergy • Direct fumigation of MEO and hexanal resulted phytotoxicity on apples • Gel formulations not only remediate the phytotoxicity but also provide protection to apples from A. foetidus. • Physicochemical studies suggest that there was no adverse effect on the quality of apples stored with gel formulations. [ABSTRACT FROM AUTHOR]

A series of new thiophene-based guanylhydrazones (iminoguanidines) were synthesized in high yields using a straightforward two-step procedure. The antifungal activity of compounds was evaluated against a wide range of medicaly important fungal strains including yeasts, molds, and dermatophytes in comparison to clinically used drug voriconazole. Cytotoxic properties of compounds were also determined using human lung fibroblast cell line and hemolysis assay. All guanylhydrazones showed significant activity against broad spectrum of clinically important species of Candida spp., Aspergillus fumigatus , Fusarium oxysporum , Microsporum canis and Trichophyton mentagrophytes , which was in some cases comparable or better than activity of voriconazole. More importantly, compounds 10 , 11 , 13 , 14 , 18 and 21 exhibited excellent activity against voriconazole-resistant Candida albicans CA5 with very low minimal inhibitory concentration (MIC) values <2 μg mL −1 . Derivative 14 , bearing bromine on the phenyl ring, was the most effective compound with MICs ranging from 0.25 to 6.25 μg mL −1 . However, bis-guanylhydrazone 18 showed better selectivity in terms of therapeutic index values. In vivo embryotoxicity on zebrafish ( Danio rerio ) showed improved toxicity profile of 11 , 14 and 18 in comparison to that of voriconazole. Most guanylhydrazones also inhibited C. albicans yeast to hyphal transition, essential for its biofilm formation, while 11 and 18 were able to disperse preformed Candida biofilms. All guanylhydrazones showed the equal potential to interact with genomic DNA of C. albicans in vitro, thus indicating a possible mechanism of their action, as well as possible mechanism of observed cytotoxic effects. Tested compounds did not have significant hemolytic effect and caused low liposome leakage, which excluded the cell membrane as a primary target. On the basis of computational docking experiments using both human and cytochrome P450 from Candida it was concluded that the most active guanylhydrazones had minimal structural prerequisites to interact with the cytochrome P450 14α-demethylase (CYP51). Promising guanylhydrazone derivatives also showed satisfactory pharmacokinetic profile based on molecular calculations. [ABSTRACT FROM AUTHOR]

Herein, we describe the antifungal evaluation of 43 bisamidine compounds, of which 26 are new, having the scaffold [Am]–[HetAr]–[linker]–[HetAr]–[Am], in which [Am] is a cyclic or acyclic amidine group, [linker] is a benzene, pyridine, pyrimidine, pyrazine ring, or an aliphatic chain of two to four carbon, and [HetAr] is a 5,6-bicyclic heterocycle such as indole, benzimidazole, imidazopyridine, benzofuran, or benzothiophene. In the head-to-head series the two [HetAr] units are oriented such that the 5-membered rings are connected through the linker, and in the head-to-tail series, one of the [HetAr] systems is connected through the 6-membered ring; additionally, in some of the head-to-tail compounds, the [linker] is omitted. Many of these compounds exhibited significant antifungal activity against Candida albicans , Candida krusei , Candida glabrata , Candida parapsilosis , and Cryptococcus neoformans (MIC ⩽ 4 μg/ml). The most potent compounds, for example, P10 , P19 and P34 , are comparable in antifungal activities to amphotericin B (MIC 0.125 μg/ml). They exhibited rapid fungicidal activity (>3 log 10 decrease in cfu/ml in 4 h) at concentrations equivalent to 4× the MIC in time kill experiments. The bisamidines strongly inhibited DNA, RNA and cell wall biosynthesis in C. albicans in macromolecular synthesis assays. However, the half-maximal inhibitory concentration for DNA synthesis was approximately 30-fold lower than those for RNA and cell wall biosynthesis. Fluorescence microscopy of intact cells of C. albicans treated with a bisamidine exhibited enhanced fluorescence in the presence of DNA, demonstrating that the bisamidine was localized to the nucleus. The results of this study show that bisamidines are potent antifungal agents with rapid fungicidal activity, which is likely to be the result of their DNA-binding activity. Although it was difficult to obtain a broad-spectrum antifungal compound with low cytotoxicity, some of the compounds (e.g., P9 , P14 and P43 ) exhibited favorable CC 50 values against HeLa cells and maintained considerable antifungal activity. [ABSTRACT FROM AUTHOR]

Complexes of nickel(II), and copper(II) were synthesized with pantadentate ligand i.e. 3,3′-thiodipropionicacid-bis(5-amino-1,3,4-thiadiazole-2-thiol) (L). The ligand was synthesized by the condensation of thiodipropionic acid and 5-amino-1,3,4-thiadiazole-2-thiol in 1:2 ratio, respectively. Synthesized ligand was characterized by elemental analysis, mass, 1 H NMR, IR, and molecular modeling. All the complexes were characterized by elemental analysis, molar conductance, magnetic moment, IR, electronic spectra, ESR, and molecular modeling. The newly synthesized complexes possessed general composition [M(L)X 2 ] where M = Ni(II), Cu(II), L = pantadentate ligand and X = Cl − , CH 3 COO − . The IR spectral data indicated that the ligand behaved as a pantadentate ligand and coordinated to the metal ion through N 2 S 3 donor atoms. The molar conductance value of Ni(II), and Cu(II) complexes in DMSO corresponded to their electrolytic behavior. On the basis of spectral study, octahedral and tetragonal geometry was assigned for Ni(II) and Cu(II) complexes, respectively. In vitro fungicidal study of ligand and its complexes was investigated against fungi Candida albicans , Candida parapsilosis , Candidia krusei , and Candida tropicalis by means of well diffusion method. [ABSTRACT FROM AUTHOR]

Highlights: [•] Thermotolerant bacteria and Cyanobacteria were evaluated in coriander, cumin and fennel. [•] Microbial inoculation stimulated peroxidase and endoglucanase activity. [•] Significant enhancement in growth and vigour of plants by microbial fortification. [•] Bacillus pumilus and Calothriix elenkinii proved most promising. [•] Microbial inoculation can be eco-friendly plant growth promoting options for spice crops. [ABSTRACT FROM AUTHOR]

Abstract: A new naphthoquinone derivative was isolated from the heartwood of the teak stem. The chemical structure of this new compound, 4′,5′-dihydroxy-epiisocatalponol, was determined using 1-D and 2-D nuclear magnetic resonance experiments, vibrational circular dichroism, HRMS, and optical rotation. We showed that this new naphthoquinone derivative plays a key role in the variability of decay resistance in teak wood. A high negative correlation was found between its concentration and the mass losses of the wood samples after exposure to the brown rot Antrodia sp., the fungus that is the most virulent against teak (R = −0.9; ρ < 0.0001). In-vitro bioassays allowed us to demonstrate that 4′,5′-dihydroxy-epiisocatalponol acted as a fungicide against Trametes versicolor (white rot) at 58 mg ml-1 (0.22 mM). Overall, our results demonstrated that the concentration of 4′,5′-dihydroxy-epiisocatalponol could be used as a new tool to evaluate teak wood durability. [Copyright &y& Elsevier]

Abstract: A series of substituted benzylsulfanyl-phenylamines was synthesized, of which four substituted benzylsulfanyl-phenylguanidines (665, 666, 667 and 684) showed potent fungicidal activity (minimal fungicidal concentration, MFC⩽10μM for Candida albicans and Candida glabrata). A benzylsulfanyl-phenyl scaffold with an unsubstituted guanidine resulted in less active compounds (MFC=50–100μM), whereas substitution with an unsubstituted amine group resulted in compounds without fungicidal activity. Compounds 665, 666, 667 and 684 also showed activity against single C. albicans biofilms and biofilms consisting of C. albicans and Staphylococcus epidermidis (minimal concentration resulting in 50% eradication of the biofilm, BEC50⩽121μM for both biofilm setups). Compounds 665 and 666 combined potent fungicidal (MFC=5μM) and bactericidal activity (minimal bactericidal concentration, MBC for S. epidermidis ⩽4μM). In an in vivo Caenorhabditis elegans model, compounds 665 and 667 exhibited less toxicity than 666 and 684. Moreover, addition of those compounds to Candida-infected C. elegans cultures resulted in increased survival of Candida-infected worms, demonstrating their in vivo efficacy in a mini-host model. [Copyright &y& Elsevier]

Abstract: Aqueous solutions from table olives constitute a major environmental problem because of their high mineral and organic contamination but they also contain compounds with antimicrobial properties. In this study, the bactericidal and fungicidal activities of salt-free table olive solutions against several phytopathogenic micro-organisms were examined. The storage solutions of black ripe olives showed noticeable bactericidal activity against species of Erwinia, Clavibacter, Agrobacterium and Pseudomonas, although the washing waters from Spanish-style green olives were less effective. In fact, black olive storage solutions diluted to 20–30% were able to reduce the inoculated population of Erwinia amylovora and Pseudomonas syringae up to 6–7log. This bactericidal activity was correlated with the presence of olive glutaraldehyde-like compounds such as the dialdehydic form of decarboxymethyl elenolic acid in these solutions, either free or linked to hydroxytyrosol. Experiments in vitro demonstrated that the bactericidal activity of these substances could explain most of the activity of the black olive storage solutions. Moreover, these salt-free table olive solutions also showed fungicidal activity against species of Phytophthora, Colletotrichum, Alternaria, Botrytis and Pestalotiopsis. The black olive storage solutions were more fungicidal than the washing solutions from Spanish-style green olives, with mycelial growth inhibition of up to 100% being attained, in some instances. These findings open the possibility of using table olive wastewaters in agriculture for pest management. [ABSTRACT FROM AUTHOR]

Abstract: The antifungal activity of the silver nanoparticles (NPs) prepared by the modified Tollens process was evaluated for pathogenic Candida spp. by means of the determination of the minimum inhibitory concentration (MIC), minimum fungicidal concentration (MFC), and the time-dependency of yeasts growth inhibition. Simultaneously the cytotoxicity of the silver NPs to human fibroblasts was determined. The silver NPs exhibited inhibitory effect against the tested yeasts at the concentration as low as 0.21mg/L of Ag. The inhibitory effect of silver NPs was enhanced through their stabilization and the lowest MIC equal to 0.05mg/L was determined for silver NPs stabilized by sodium dodecyl sulfate against Candida albicans II. The obtained MICs of the silver NPs and especially of the stabilized silver NPs were comparable and in some cases even better than MICs of the conventional antifungal agents determined by E-test. The silver NPs effectively inhibited the growth of the tested yeasts at the concentrations below their cytotoxic limit against the tested human fibroblasts determined at a concentration equal to 30mg/L of Ag. In contrast, ionic silver inhibited the growth of the tested yeasts at the concentrations comparable to the cytotoxic level (approx. 1mg/L) of ionic silver against the tested human fibroblasts. [Copyright &y& Elsevier]

Abstract: A series of arylhydrazino-substituted cyanoacrylates 3 and N-aryl pyrazolecarboxylates 6 were synthesized and their bioactivities were evaluated. Though compounds 3 were designed as herbicide, some of them showed fungicidal activity and anti-tumor activity. Some of the compounds 6 exhibited plant growth regulatory activity. [Copyright &y& Elsevier]

Abstract: Petroleum ether, dichloromethane, ethanol (70%) and water extracts of 12 South African plants were screened using microdilution assays against Gram-positive (Bacillus subtilis, Staphylococcus aureus), Gram-negative (Escherichia coli) bacteria, and the fungus Candida albicans. No antimicrobial activity was observed in water extracts. The ethanol extracts of Becium obovatum leaves showed the best antibacterial activity with a minimum inhibitory concentration value of 0.074 mg/ml against B. subtilis. The petroleum ether extract of leaves of Cucumis hirsutus, Haworthia limifolia and Protea simplex showed good antibacterial activity with MIC values ranging between 0.098 and 0.780 mg/ml against all the test bacteria. The petroleum ether extract of P. simplex leaves showed the best anti-candidal activity with a minimum fungicidal concentration value of 0.014 mg/ml. The ethanol extracts of Agapanthus campanulatus (leaves and root), Dissotis princeps and Gladiolus dalenii as well as the dichloromethane extract of P. simplex leaves showed good anti-candidal activity with minimum fungicidal concentration values ranging between 0.037 and 0.39 mg/ml. Mutagenicity tests conducted on extracts that showed good antimicrobial activity suggest the plants are probably safe for consumption. The results obtained in this study show that some of the traditional plants may indeed be effective for the treatment of ailments related to gastro-intestinal disorders that may be due to the test pathogens. [Copyright &y& Elsevier]

Abstract: Zygomycoses is a rapidly progressive infection associated with high mortality. Although amphotericin B (AMB) has been the only treatment option for years, recent studies have demonstrated that posaconazole (PCZ) has good activity against Zygomycetes. Because rapid onset of antifungal activity is crucial in the management and never studied before, we compared the time for maximum fungicidal activity of AMB versus PCZ using time–kill curves. The MIC of AMB and PCZ against clinical isolates of Mucor spp. and Rhizopus spp. was determined by the Clinical and Laboratory Standards Institute M38-A2 method, and the fungicidal activity was examined by time–kill studies. AMB was rapidly fungicidal, with 95% killing noted as early as 6 h and 99.9% killing at 24 h; PCZ showed <70% killing at 6 h and 99.9% killing at 48 h. In vivo animal studies using AMB in the early phase, followed by a switch to high-dose PCZ later, could provide data that may have clinical implications because there are only a few drugs currently available for the management of zygomycoses. [Copyright &y& Elsevier]

Abstract: Statins (anticholesterol drugs) inhibit HMG-CoA reductase, which is a key rate-limiting enzyme in the synthesis of sterols in fungi. We therefore investigated the in vitro inhibitory activity of various statins against Aspergillus fumigatus alone and in combination with antifungal drugs. Fresh conidial suspensions from 10 clinical isolates of A. fumigatus were obtained. The MIC and minimum fungicidal concentration (MFC) were determined by the Clinical and Laboratory Standards Institute M-38A protocol and the fungicidal activity by time–kill study. Fluvastatin (FST) showed good activity (MIC, 2 mg/L; MFC, 4 mg/L) against A. fumigatus; other statins had no activity (MIC ≥256 mg/L). FST enhanced the activity of caspofungin (CFG) against A. fumigatus; subinhibitory concentrations of FST in combination with CFG showed >99.9% killing of A. fumigatus conidia, whereas either drug alone showed poor activity at subinhibitory concentrations. FST potentiated the antifungal activity of CFG but displayed no specific interaction with voriconazole or amphotericin B. [Copyright &y& Elsevier]

Abstract: The evaluation of susceptibility patterns of clinical and laboratory isolates of dermatophytes and Candida to sertaconazole nitrate has been determined using macrodilution and microdilution test methods in laboratories worldwide. Antimycotics that have been compared to sertaconazole nitrate include itraconazole, clotrimazole, miconazole, and terbinafine. A comparison of the minimum inhibitory concentrations clearly shows differences in potency and spectrum among the various agents. This article reviews the antifungal activity of sertaconazole nitrate against major fungal pathogens that cause and complicate tinea pedis. In light of the new topical formulation of sertaconazole nitrate, this compilation of data from the literature is helpful for relating in vitro data to the tissue concentrations required for effective eradication of cutaneous fungal infections. [Copyright &y& Elsevier]

Summary: The bactericidal and fungicidal activity of Akacid plus, a novel polymeric compound of the cationic family of disinfectants, was compared with chlorhexidine digluconate using quality control strains of Staphylococcus aureus, Enterococcus hirae, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. In vitro activity was determined using the quantitative suspension tests described by the European Committee for Standardization. These use concentrations of 0.01–0.5% against bacterial strains/C. albicans, with 0.5–4% against A. niger, and exposure times of 5, 15 and 60min in the presence and absence of 0.3% bovine albumin and with dilution in distilled and hard water. In the basic quantitative suspension test, Akacid plus destroyed all bacterial pathogens at a concentration of 0.1% in ≤5min. Chlorhexidine was also highly active against S. aureus, E. coli and P. aeruginosa, but failed to eliminate E. hirae within 5min. A high organic load reduced the bactericidal activity of both disinfectants slightly. Akacid plus showed fungicidal activity against C. albicans within 15–60min and eliminated A. niger at a concentration of 1% in 5min of contact. Chlorhexidine was fungicidal against C. albicans, but not against A. niger. [Copyright &y& Elsevier]

1,10-Phenanthroline (phen) and metal–phen complexes display fungicidal and fungiststic activity, disrupt mitochondrial function and induce oxidative stress. We have examined the effect of these drugs on the structure of yeast and mammalian cell organelles and the integrity of cellular DNA. Exposure of Candida albicans to [Mn(phen)2(mal)].2H2O or [Ag2(phen)3(mal)].2H2O (mal H2=malonic acid) resulted in DNA degradation whereas exposure to phen or [Cu(phen)2(mal)].2H2O did not. All drugs induced extensive changes to the internal structure of yeast cells including retraction of the cytoplasm, nuclear fragmentation and disruption of the mitochondrion. In the case of cultured mammalian cells [Cu(phen)2(mal)].2H2O induced apoptosis as evidenced by the ladder pattern of DNA fragments following gel electrophoresis and also the blebbing of the cell membrane. The other drugs produced non-specific DNA degradation in mammalian cells. In conclusion, phen and metal–phen complexes have the potential to induce apoptosis in fungal and mammalian cells. Given their distinct mode of action compared to conventional anti-fungal drugs, phen and metal–phen complexes may represent a novel group of anti-fungal agents for use either in combination with existing drugs or in cases where resistance to conventional drugs has emerged. [Copyright &y& Elsevier]

Hexaethylamino- and hexabenzylamino- derivatives of cyclotriphosphazene were prepared by substituting the chlorine atoms of hexachlorocyclotriphosphazene. A number of addition complexes of copper(II) acetate were then prepared with these cyclophosphazene ligands in different stoichiometric ratios. The complexes have been characterized on the basis of analytical and physico — chemical studies. The molar conductance measurements suggest the complexes are non - electrolytes. Infrared spectra indicate the coordination of phosphazene ring nitrogen to the copper but copper(II) acetate dimer was found intact after the complex formation. Electronic spectra suggest a distorted octahedral geometry around copper(II) ion. Room temperature magnetic moment values are lower than the spin — only values for d9 system with one unpaired electron which suggests the possibility of weak antiferromagnetic coupling between two unpaired electrons present on the two Cu2+ ions in the dimer. The plausible structures of the complexes have been suggested on the basis of molecular weight determinations. The fungicidal activities of the cyclophosphazene ligands and their Cu(II) derivatives were obtained against the fungi Aspergillus flavus and Aspergillus niger. It was found that the fungicidal activities of Cu(II) derivatives of cyclophosphazene ligands have been considerably enhanced compared to the ligands. [Copyright &y& Elsevier]

This study determined the favourable fermentation conditions for the production of antifungal peptides from kenaf seeds and their effectiveness in extending the shelf-life of tomato puree. The optimum fermentation conditions for the maximum activity of the antifungal peptides were 8.4% (w/v), 7 days and 3.7% for substrate/water ratio, fermentation time and glucose concentration, respectively. Eight cationic peptides of low molecular weight ranging from 840 to 1876 Da were identified in kenaf seed peptides mixture (KSPM). The minimum inhibitory concentration and minimum fungicidal concentration of KSPM against Fusarium sp. were 0.18 mg/mL and 0.70 mg/mL, respectively, while those for Aspergillus niger were 1.41 mg/mL and 2.81 mg/mL respectively. KSPM exhibited a fungicidal effect and a prolonged lag phase, with increased fungal membrane permeability as the concentration of KSPM increased, as evidenced by the release of intracellular constituents. The treatment of tomato puree with 1000 mg/kg KSPM delayed fungal growth for up to 14 and 23 days at 25 °C and 4 °C respectively, significantly reducing Aspergillus niger and Fusarium sp. counts. In conclusion, kenaf seed peptides prepared by lacto-fermentation possess antifungal activity, hence can be applied as natural bio preservatives to extend the shelf-life of food products such as tomato puree. [Display omitted] • Kenaf seed protein was bio-transformed into a peptide mixture by L. pentosus RK3. • The peptide mixture displayed fungicidal effects towards A. niger and Fusarium sp. • The peptide mixture extended tomato puree shelf-life for up to 23 days at 4 °C. • Kenaf seed peptides constitute a natural alternative to synthetic preservatives. [ABSTRACT FROM AUTHOR]

Over the years, post-harvest management strategies of fungal pathogens have depended on the aggressive usage of synthetic chemicals (fungicides). This conduct has been reported to have a negative environmental impact, cause potential harm to humans due to exposure to residues, and increase the risk of spoilage and pathogenic microorganisms resistant. These emphasises the need for safe and effective alternative treatments capable of preventing fruit infections and maintaining quality in order to minimize post-harvest losses. Ethno-pharmacological assessments of various plant extracts and other natural compounds such as active metabolites and enzymes produced by microorganisms have shown potential as fungi-static and/or -cidal agents against fruit pathogens. This review provides an overview on: the mechanisms and action of fruit pathogens and the existing synthetic fungicides and biological controls strategies. The potentials of plant extracts as alternative control was discussed with emphasises on the phyto-chemistry of selected plant extracts with high efficacy against fruit pathogens in order to gain insight into their bioactive compounds. In addition, the implication of extensive spatial scale application of synthetic fungicides leading to fungal resistance was discussed and the importance of synergistic use of natural compound were addressed. Challenges associated with upscaling plant extracts and other natural compounds from lab scale and commercialization were highlighted. • Synthetic fungicides as a broad strategy for post-harvest fungal pathogen management is increasingly challenged. • Ethno-pharmacological study of plant extracts and other natural compounds have shown potential antifungal activity. • Biological control using antagonistic microorganisms is an emerging method for fungal pathogens management. • Market access for biocontrols requires a trilateral co-operation amongst researchers, industries and policy makers. [ABSTRACT FROM AUTHOR]

Abstract: Synthesis and antiAIDS, anticancer, antitubercular, fungicidal and antibacterial activities of 2-methyl-4-N-2′-cyanoethyl-N-methane/benzenesulphonylaminobenzaldehyde and their hydrazones are reported. [Copyright &y& Elsevier]

Abstract: The minimal fungicidal concentration (MFC) of dihydrosphingosine (DHS), phytosphingosine (PHS), and five short-chain DHS derivatives was determined for Candida albicans and Candida glabrata. In this respect, a C15- and a C17-homologue of DHS showed a 2- to 10-fold decreased MFC as compared to native DHS (i.e. C18-DHS). DHS derivatives that were active, that is, comprising 12, 15, 17, or 18 carbon atoms, induced accumulation of reactive oxygen species (ROS) in C. albicans. [Copyright &y& Elsevier]

• Pyrimido[4,5- d pyridazinone- N -acylhydrazones were synthesized by simple methodologies. • Antifungal activity of compounds was evaluated against P. brasiliensis and Candida spp. • Six compounds showed inhibition against Pb18 with MIC of 0.125 to 64 µg.mL−1. • N -acylhydrazone 5a showed potent fungicidal profile with MFC of 0.5 µg mL−1. • Compound 5a showed good synergic effect with amphotericin B and not showed toxicity. Paracoccidioidomycosis is an endemic mycosis in Latin America for which there is a high mortality rate and limited treatment options. There are no specific drugs to treat the systemic disease. Thus, there is a need for further studies focused on the development of specific drugs. In this work we synthesized new hybrids pyrimido[4,5- d pyridazinone- N -acylhydrazone (5a-p) by simple methodologies with good yields. The antifungal activity of compounds was evaluated against P. brasiliensis (Pb18) and Candida spp. Compounds 5a , 5f , 5i , 5 k , 5 m and 5n showed significant inhibition against Pb18 with MIC of 0.125 to 64 µg mL−1. Compound 5a is the most promising, showing potent fungicidal profile with MFC of 0.5 µg mL−1, synergic effect with amphotericin B, besides showing no toxicity against HeLa and Vero cells. [ABSTRACT FROM AUTHOR]

A naturally occurring phenylpropanoid, trans-anethole (anethole), was assayed for its fungicidal activity in Saccharomyces cerevisiae grown under hypoxic and aerobic conditions. Anethole killed the growing cells in malt extract broth only under hypoxic conditions. Anethole did not exhibit fungicidal effects against non-growing cells. The cells of a mitochondrial-DNA-lacking rho0 mutant, which grew fermentatively even in the presence of O2, were killed by anethole regardless of aeration. The fungicidal potency of anethole against a strain capable of respiration under aerobic conditions was enhanced by the addition of a respiratory inhibitor antimycin A3. Therefore, anethole possibly expresses fungicidal activities only against fermentatively growing cells of S. cerevisiae. [Copyright &y& Elsevier]