The combined antibacterial and anticancer properties of nano Ce-containing Mg-phosphate ceramic.

AIM: This paper was mainly aimed at synthesis of Ce-containing nano-Mg-phosphate ceramic as a multifunctional material. MATERIALS AND METHODS: Two ceramics based on Mg3(PO4)2 and Ce0.2Mg2.8(PO4)2 formulas (MP and MP-C, respectively) were synthesized. The synthesized powders were characterized by XRD, TEM, Zeta potential, and FTIR. Also, their dissolution behavior was tested in Tris-HCl buffer solution. Moreover, the antimicrobial efficacy was evaluated against gram-positive bacteria (Bacillus sphaericus MTCC 511 &Staphylococcus aureus MTCC 87) and gram-negative bacteria (Enterobacter aerogenes MTCC 111 &Pseudomonas aeruginosa MTCC 1034) using dick diffusion assay and microdilution method. Furthermore, the cell viability test was performed for the ceramics on Vero cells (African green monkey kidney cells), and their antitumor activity was determined by PC3 cell line (prostatic cancer). Also, the cellular uptake was determined by the flow cytometry. KEY FINDINGS: The results showed that the substitution of Mg by Ce decreased the particle size from 40 to 90 nm for MP sample to 2-10 nm for MP-C sample and increased the degradation rate. Both samples showed excellent antimicrobial activities. Moreover, MP demonstrated more cell viability than MP-C on Vero cells at high concentrations, whereas, MP-C showed more antitumor activity on PC3 cells than MP sample. Moreover, MP-C showed a higher cell uptake than MP due to its smaller size and more negative charge. SIGNIFICANCE: Mg-phosphate ceramic can be used in this study successfully as a delivery system for cerium ions and showed a high antitumor activity, which makes it highly recommended as safe and effective cancer treatment materials.

Dual Valorization of Olive Mill Wastewater by Bio-Nanosynthesis of Magnesium Oxide and Yarrowia lipolytica Biomass Production.

This research investigates an efficient dual valorization of olive mill wastewater in the biosynthesis of magnesium oxide nanoparticles and in the depollution of the effluent by Yarrowia lipolytica growth evaluation. After removal of polyphenols, the recovered biophenols were reacted with the magnesium precursor to provide magnesium oxide nanoparticles. In order to confirm the biosynthesized magnesium oxide nanoparticles, several analyses were undertaken. The Fourier transform infrared spectrum gives a broad absorption at 658 cm-1 confirming the presence of the magnesium oxide nanoparticles, while the UV/VIS absorption spectroscopy reveals an intense transition with a maximum absorption at 300 nm. The X-ray diffraction and transmission electron microscopy analyses show that nanoparticles are in pure cubic crystalline with spherical and hexagonal shapes (average size is 19.4 nm). The zeta potential analysis illustrates a negative potential proving a good stability of the biosynthesized nanoparticles. Nanoparticles were assigned for their in vitro antibacterial activity against Escherichia coli, Enterobacter aerogenes, Salmonella typhimurium, Staphylococcus cohnii, and Bacillus niacini. The evaluation of the growth of Yarrowia lipolytica on the recovered olive mill wastewater after removal of polyphenols yielded 3.2 g/L of the Yarrowia biomass in 72 h without nutriment additions, providing an important decrease of chemical oxygen demand (73 %).

Hydromethanolic extract of Rehum emodi exhibits significant antimicrobial activity against acute gastroenteriti bacterial strains.

Rehum emodi is an important medicinal herbal and has been reported to exhibit tremendous pharmacological potential. The present study was designed to evaluate the antibacterial activity of hydromethanolic extract of rhizome of Rehum emodi against the acute gastroenteriti bacterial strains. The antimicrobial activity was determined by micro-dilution method. Antioxidant activity was determined by DPPH assay and cytotoxicity by MTT assay. Phytochemical analysis was carried out by LC/MS analysis. The results of the present study showed that hydromethanolic extract of rhizome of Rehum emodi (REE) exhibited significant antimicrobial activity against the gastroenteriti bacterial strains. The MIC values ranged from 25 µg/ml to 125 µg/ml. Moreover, the cytotoxicity of the REE was evaluated against the human breast cell line FR-2 and it was observed that REE exerted minimal cytotoxic effects on these cells with an IC50 of 250 µg/ml indicating that this extract is non-toxic to human cells. The phytochemical analysis revealed the presence of several secondery metabolites such as anthroquinones (anthrone, emodin, aloe emodin and rhein) flavonoids (quercetin, and naringenin) and phenolics (sinapinic acid and gallic acid) which could potentially be responsible for the activity of the extract. In conclusion REE could potentially prove to be useful in the treatment of acute gastroenteritis.

A biological method for in-situ synthesis of hydroxyapatite-coated magnetite nanoparticles using Enterobacter aerogenes: Characterization and acute toxicity assessments.

Hydroxyapatite (HA)-coated magnetite nanoparticles (MNPs) are being widely investigated for various applications in medical engineering and wastewater treatment. In this work, the MNPs were thoroughly coated by bacterial synthesized HA nanoparticles during biomineralization process using Enterobacter aerogenes. The resulting bacterial-induced precipitate was then calcined at 600°C and investigated with respect to structural characteristics, particle size and magnetic strength by XRD, FT-IR, SEM, EDS, TEM and VSM analyses. The effects of MNPs and HA-coated MNPs (HA-MNPs) on the viability of human MCF-7 cell lines were also investigated via mitochondrial activity test (MTT) and lactate dehydrogenase (LDH) assays. The powder characterization results showed appropriate structural properties for HA-MNPs samples. The particles diameter size of the MNPs and HA-MNPs were in the range of 3-25nm and 20-80nm, respectively. The biologically-synthesized HA-MNPs formed a stable suspension in water while keeping their magnetic property. The saturation magnetization (Ms) of HA-MNPs was measured at ~10emug-1 which was in good agreement with the structural composition of this sample. Finally, the results of the cell lines viability indicated that coating of toxic MNPs via biomineralization was a promising approach in order to synthesize bio-compatible magnetic nanoparticles with suitable physical and chemical structural characteristics. The toxicity level of MNPs was reduced by 10 fold when coated by bacterial-synthesized HA.

Risk factors for mortality in patients with ventilator-associated pneumonia caused by carbapenem-resistant Enterobacteriaceae

Abstract Background: The ideal therapeutic option for ventilator associated pneumonia caused by carbapenem-resistant Enterobacteriaceae is not defined. The aim of this study was to assess mortality-associated risk factors in patients with VAP by CRE and determine the outcome of several treatment options. Methods: This was a retrospective study performed in two tertiary hospitals involving patients with VAP caused by CRE between January 2010 and August 2014. The outcomes were mortality within 30 days of VAP diagnosis and overall mortality during hospital admission. Risk factors for mortality were assessed by comparing variables of survivors and non-survivors. Results: One hundred and twelve patients with CRE-VAP were included, 73 (65%) male, median age 56 years. The 30-day mortality was 57.1% and the overall hospital mortality was 67%. In the binary logistic regression analysis, only age >50 years was independently associated to increased mortality. Polymyxin was the most used drug (47.5%), followed by tigecycline (29.2%) and aminoglycosides (2.4%). Combined therapy with two active drugs was used by 17 patients (20.8%). No therapeutic option was independently associated to survival. However, combined therapy with two active drugs was superior to the therapy with a single active drug when inappropriate therapy was the comparator (p = 0.044). The addition of carbapenem was not associated with increased survival. Conclusion: The best therapeutic option for VAP by CRE is still not completely defined, but the therapy with at least two active drugs was superior in this study.

Facile green fabrication of nanostructure ZnO plates, bullets, flower, prismatic tip, closed pine cone: Their antibacterial, antioxidant, photoluminescent and photocatalytic properties.

Green synthesis of multifunctional Zinc oxide nanoparticles (NPs) with a variety of morphologies were achieved by low temperature solution combustion route employing neem (Azadirachta indica) extract as fuel. The nanoparticles were characterized by PXRD, FTIR, XPS, Raman and UV-Visible spectroscopic studies. The Morphologies were studied by SEM and TEM analysis. The NPs were subjected for photoluminescence, photocatalytic, antibacterial and antioxidant activity studies. PXRD pattern confirmed the hexagonal wurtzite structure of the product. SEM images indicated the transformation of mushroom like hexagonal disks to bullets, buds, cones, bundles and closed pine cone structured NPs with increase in the concentration of neem extract in reaction mixture. The NPs exhibited prominent green emission due to the presence of intrinsic defect centers. The as-formed bullet shaped ZnO with 4ml of neem extract was found to decolorize Methylene blue (MB) under Sunlight and UV light irradiation. The antibacterial studies indicated that ZnO NPs of concentration 500, 750 and 1000µg resulted in significant antibacterial activity on Klebsiella aerogenes and Staphylococcus aureus but not against Escherichia coli and Pseudomonas aeruginosa in agar well diffusion method. Further, ZnO NPs exhibited significant antioxidant activity against scavenging DPPH free radicals. The current investigation demonstrated green engineering method for the synthesis of multifunctional ZnO NPs with interesting morphologies using neem extract.

Antimicrobial, antitumor and brine shrimp lethality assay of Ranunculus arvensis L. extracts.

To investigate the antitumor activity, brine shrimp lethality assay, antibacterial and antifungal activity of Methanol Extract (ME), Water Extract (WE), Acetone Extract (AE), Chloroform Extract (CE), Methanol-Water Extract (MWE), Methanol-Acetone Extract (MAE), Methanol-Chloroform Extract (MCE) of Ranunculus arvensis (L.). Antitumor activity was evaluated with Agrobacterium tumefaciens (At10) induced potato disc assay. Cytotoxicity was evaluated with brine shrimp lethality assay. Antibacterial activity was evaluated with six bacterial strains including Escherichia coli, Enterobacter aerogenes, Bordetella bronchiseptica, Klebsiella pneumoniae, Micrococcus luteus and Streptococcus anginosus and antifungal screening was done against five fungal strains including Aspergillus niger, A. flavus, A. fumigates, Fusarium solani and Mucor species by using disc diffusion method. Best antitumor activity was obtained with ME and WE, having highest IC50 values 20.27 ± 1.62 and 93.01 ± 1.33µg/disc. Brine shrimp lethality assay showed LC50 values of AE, MAE and ME were obtained as 384.66 ± 9.42µg/ml, 724.11 ± 8.01µg/ml and 978.7 ±8.01 µg/ml respectively. WE of R. arvensis revealed weak antimicrobial result against the tested microorganisms. On the other hand, the antifungal activity of the plant extracts was found to be insignificant. These findings demonstrate that extracts of R. arvensis possesses significant antitumor activity. Further extensive study is necessary to assess the therapeutic potential of the plant.

Analysis of bioactivities and chemical composition of Ziziphus joazeiro Mart. using HPLC-DAD.

The aim of this study was to evaluate the chemical profile and antioxidant, antimicrobial and antiparasitic activities of the hydroalcoholic extract of the leaves of Ziziphus joazeiro Mart. (HELZJ). The antioxidant DPPH and FRAP assays and chemical profile were determined by colorimetric methods and HPLC/DAD. The antiparasitic, antibiotic and antibiotic-modifying activity were evaluated by microdilution assays. The HPLC-DAD assay showed the presence of mostly tannins and flavonoids, such as caffeic acid and quercetin. The levels of polyphenols and flavonoids were 183.136 mg/g extract and 7.37 mg/g extract, respectively. DPPH and FRAP showed low antioxidant activity for the extract. The antibacterial and antifungal activities were not of clinical relevance, showing MIC>1024 µg/mL. However, synergism was observed between HELZJ and the antibiotics amikacin and gentamicin, which resulted in decreased bacterial drug resistance. EHFZJ showed low toxicity in fibroblasts in vitro, while antiparasitic results against Trypnosoma cruzi, Leishmania braziliensis and Leishmania infantum were not clinically relevant. Thus, our results indicate that Z. joazeiro Mart. (HELZJ) could be a source of plant-derived natural products that could lead to the development of promising new antibiotic compounds for infectious diseases.

Purpurides B and C, two new sesquiterpene esters from the aciduric fungus Penicillium purpurogenum JS03-21.

Purpurides B and C (1 and 2, resp.), two new sesquiterpene alcohol esters generated from a drimane-type sesquiterpenoid lactone and an amino acid, together with two known analogs, berkedrimane B (3) and purpuride (4), were isolated from the aciduric fungus Penicillium purpurogenum JS03-21. Their structures were elucidated by spectroscopic analysis, X-ray single-crystal diffraction, and application of Marfey's method. Compounds 1-4 showed modest antifungal activities against Candida albicans with MIC values in the range of 1.2-3.3 µM. Compounds 1 and 2 showed moderate antimicrobial activities against Enterobacter aerogenes and Pseudomonas aeruginosa with MIC values in the range of 1.2-2.6 µM.

Efficacy of knife disinfection techniques in meat processing.

EU Regulation 853/2004 requires that knives used in meat processing be disinfected by submerging them in hot water (+82°C). Alternative procedures are permitted if the efficacy is proved to be equivalent. In the present study, various time-temperature combinations together with pure water, water with lactic acid (2 %), and the use of ultrasound with and without lactic acid (2%) were investigated. Steel plates were covered with fat and protein and then inoculated with a standardized bacterial contamination assembled according to the composition of bacterial contamination found in a previous field trial conducted with regard to the slaughter of pigs. Several combinations with diverse temperatures and time intervals were tested until no microbial load was detectable by using a wet-dry-swab technique that had previously been tested to ensure maximum bacterial recovery. The following were effective in bringing the tested bacterial flora below the detection limit: • 70 °C water bath for 10 s • 60 °C water bath + ultrasound for 5 s • 40 °C water bath + lactic acid (2%) for 10 s • 40 °C water bath + ultrasound + lactic acid (2%) for 5 s In particular, the use of lactic acid permitted a relevant reduction of the temperature, while providing effective sterilization. The use of such non-hazardous food-safe additives is particularly suitable for successful disinfection at lower temperatures.

A possible role of partially pyrolysed essential oils in Australian Aboriginal traditional ceremonial and medicinal smoking applications of Eremophila longifolia (R. Br.) F. Muell (Scrophulariaceae).

ETHNOPHARMACOLOGICAL SIGNIFICANCE: Eremophila longifolia is one of the most respected of the traditional medicines used by Australian Aboriginal people. Customary use involves smoldering the leaves over hot embers of a fire to produce an acrid smoke, believed to have therapeutic effects broadly consistent with antimicrobial, antifungal and anti-inflammatory capacity. AIM OF THE STUDY: The current study aims to examine the contribution of partially pyrolysed and non-pyrolysed essential oils in traditional usage of Eremophila longifolia. MATERIALS AND METHODS: Non-pyrolysed and partially pyrolysed essential oils were produced by hydrodistillation and part-wet/part-dry distillation, respectively. All samples were tested for antimicrobial activity by broth dilution. Some of these samples were further treated to an incrementally stepped temperature profile in a novel procedure employing a commercial thermocycler in an attempt to mimic the effect of temperature gradients produced during smoking ceremonies. Components from the pyrodistilled oils were compared with the non-pyrodistilled oils, using GC-MS, GC-FID and HPLC-PAD. The 2,2-diphenyl-1-picrylhydrazyl method, was used to compare free radical scavenging ability. RESULTS: Partially pyrolysed oils had approximately three or more times greater antimicrobial activity, enhanced in cultures warmed incrementally to 60°C and held for 30s and further enhanced if held for 2 min. Partially pyrolysed oils showed a radical scavenging capacity 30-700 times greater than the corresponding non-pyrolysed oils. HPLC-PAD revealed the presence of additional constituents not present in the fresh essential oil. CONCLUSION: These results, by showing enhanced antimicrobial and antioxidant activities, provide the first known Western scientific justification for the smoking ceremonies involving leaves of Eremophila longifolia. During customary use, both partially pyrolysed as well as non-pyrolysed essential oils may contribute significantly to the overall intended medicinal effect.

Antimicrobial aflatoxins from the marine-derived fungus Aspergillus flavus 092008.

A new aflatoxin, aflatoxin B(2b) (1), together with six known compounds, were isolated from the marine-derived fungus Aspergillus flavus 092008 endogenous with the mangrove plant Hibiscus tiliaceus (Malvaceae). The structure of 1 was determined by the spectroscopic and chemical methods. Compound 1 exhibited a moderate antimicrobial activity against Escherichia coli, Bacillus subtilis and Enterobacter aerogenes, with MIC values of 22.5, 1.7 and 1.1 M, respectively. Compound 1 also showed a weak cytotoxicity against A549, K562 and L-02 cell lines, with IC(50) values of 8.1, 2.0 and 4.2 M, respectively. The results showed that hydration and hydrogenation of (8)-double bond significantly reduces the cytotoxicity of aflatoxins, while the esterification at C-8 increases the cytotoxicity.

Thymus maroccanus essential oil, a membranotropic compound active on Gram-negative bacteria and resistant isolates.

AIMS: The effects of Thymus maroccanus essential oil (EO) on the integrity of the cell membranes and the permeability of the outer membrane (OM) and inner membrane (IM) of Escherichia coli, Enterobacter aerogenes and Salmonella enterica Typhimurium were investigated. METHODS AND RESULTS: The bacterial release of intracellular proteins, cytoplasmic ß-galactosidase and periplasmic ß-lactamase induced by T. maroccanus EO was compared to the membranotropic activity of polymyxin B (PB) known as an effective permeabilizer of the membrane of Gram-negative bacteria. Results showed that T. maroccanus EO increased the permeability of the OM and IM of studied bacteria and induced the release of intracellular proteins into the external medium. CONCLUSIONS: The effect of T. maroccanus EO on the outer membrane was comparable to that of PB, and both T. maroccanus EO and PB induce similar levels of ß-lactamase release. In addition, it also promoted the release of the cytoplasmic ß-galactosidase. Moreover, the lipopolysaccharide molecules and the overexpression of efflux pumps seem to play a crucial role in the level of susceptibility of studied bacteria to the permeabilizing effect of T. maroccanus EO. SIGNIFICANCE AND IMPACT OF STUDY: These results demonstrate that T. maroccanus EO can restore antibiotic activity by targeting the two bacterial membranes and would be attractive candidates for developing new adjuvants for combating resistant Gram-negative bacteria.

Isolation and identification of chromium-resistant bacteria: Test application for prevention of chromium toxicity in plant.

The purpose of this study was to isolate chromium resistant bacteria and characterize in depth before being applied for bioremediation or construction of chromium biosesnors. One of the major objectives was to identify the most useful strains with respect to chromium removal efficiency. Chromium resistant bacteria were isolated from tannery waste samples. These were characterized through biochemical tests and antibiotic assays. Cross metal reactivity, plasmid curing and cysteine quantifications were also performed. Gene sequencing was done for all the isolates and accession numbers received after submission to National Center for Biotechnology Information (NCBI). The removal capacity was also studied in broth cultures. The results were very encouraging since six new bacteria were recognised to withstand high concentrations of chromium. Out of these six bacteria, three i.e. Enterobacter aerogenes, Aeromonas sp., Acinetobacter sp. PD 12 performed very well by removing about 99% (average) from initial 19.8 ppm of Cr(VI) from a synthetic culture media. Enterobacter aerogenes, being the most efficient strain, was used to remediate hexavalent chromium from soil of potted plants- very encouraging results were obtained. These bacteria may be exploited for bioremediation of Cr (VI) and construction of microbial sensor in future.

Susceptibility of the multi-drug resistant strain of Enterobacter aerogenes EA289 to the terpene alcohols from Cistus ladaniferus essential oil.

The essential oil (EO) of Cistus ladaniferus was separated into non polar, moderately polar and polar fractions by column chromatography. The EO and its fractions were analysed by gas chromatography in combination with retention indices [GC-(RI)] and 13C nuclear magnetic resonance (13C NMR) spectroscopy. A minimum inhibitory concentration (MIC) assay was used to evaluate their antibacterial activity against Gram-positive and Gram-negative pathogens of clinical relevance, including a multi-drug resistant (MDR) strain. The most polar fraction, constituted by mono- and sesquiterpene alcohols, strongly inhibited the growth of all tested bacteria with MIC values ranging from 0.05 to 0.8 mg/mL. More importantly, this fraction displayed high activity against the MDR strain of Enterobacter aerogenes EA289. Transmission electron microscopy (TEM) observations of the MDR bacteria treated with the terpene alcohol-rich fraction revealed cell wall distortion with an outer cytoplasmic membrane detachment. The susceptibility of the MDR strain of E. aerogenes EA289 to the polar fraction of C. ladaniferus oil suggests the possible use of these natural products to treat infections caused by highly resistant bacteria.

Three new compounds from Aspergillus terreus PT06-2 grown in a high salt medium.

To investigate the structurally novel and bioactive natural compounds from marine-derived microorganisms under high salinity, the fungus Aspergillus terreus PT06-2 was isolated from the sediment of the Putian Sea Saltern, Fujian, China. Three new compounds, terremides A (1) and B (2) and terrelactone A (3), along with twelve known compounds (4-15) were isolated and identified from the fermentation broth of A. terreus PT06-2 at 10% salinity. Among these metabolites, compounds 4 and 15 only produced in the 10% salinity culture, were identified as methyl 3,4,5-trimethoxy-2-(2-(nicotinamido) benzamido) benzoate, and (+)-terrein, respectively. The new compounds 1 and 2 exhibited antibacterial activity against Pseudomonas aeruginosa and Enterobacter aerogenes with MIC values of 63.9 and 33.5 µM, respectively. Compounds 5 showed moderate anti-H1N1 activity and lower cytotoxicity with IC50 and CC50 values of and 143.1 and 976.4 µM, respectively.

Anti-inflammatory amino acid derivatives from the ascidian Herdmania momus.

Four new amino acid derivatives, herdmanines A-D (1-4), were isolated from the marine ascidian Herdmania momus. Herdmanines A-C contain the unusual D-form of arginine. Compounds 3 and 4 had a moderate suppressive effect on the production of NO, with IC50 values of 96 and 9 µM, respectively. These compounds were found to inhibit the mRNA expression of iNOS. The inhibitory activities on the production and mRNA expression of pro-inflammatory cytokines such as TNF-α, IL-1ß, and IL-6 were evaluated.

Identification and characterization of a phospholipase A2 from the venom of the Saw-scaled viper: Novel bactericidal and membrane damaging activities.

Phospholipase A(2) (PLA(2)), a common toxic component of snake venom, has been implicated in various pharmacological effects. In this study, a basic myotoxic PLA(2), named EcTx-I was isolated from Echis carinatus snake venom by using gel filtration on Superdex G-75, and reverse phase HPLC on C18 and C8 Sepharose columns. PLA(2), EcTx-I was 13,861.72 molecular weight as estimated by MALDI-TOF (15 kD by SDS-PAGE), and consisted of 121 amino acid residues cross-linked by seven disulfide bonds. The N-terminal sequences revealed significant homology with basic myotoxic PLA(2)s from other snake venoms. The purified PLA(2) EcTx-I was evaluated (250 µg/ml) for bactericidal activity of a wide variety of human pathogens against Burkholderia pseudomallei (KHW&TES), Enterobacter aerogenes, Escherichia coli, Proteus vulgaris, Proteus mirabilis, Pseudomonas aeruginosa and Staphylococcus aureus. EcTx-I showed strong antibacterial activity against B. pseudomallei (KHW) and E. aerogenes among the tested bacteria. Other Gram-negative and Gram-positive bacteria showed only a moderate effect. However, the Gram-positive bacterium E. aerogenes failed to show any effect on EcTx-I protein at tested doses. The most significant bacteriostatic and bactericidal effect of EcTx-I was observed at MICs of >15 µg/ml against (B. pseudomallei, KHW) and MICs >30 µg/ml against E. aerogenes. Mechanisms of bactericidal and membrane damaging effects were proved by ultra-structural analysis. EcTx-I was able to induce cytotoxicity on THP-1 cells in vitro as well as lethality in BALB/c mice. EcTx-I also induced mild myotoxic effects on mouse skin, but was devoid of hemolytic effects on human erythrocytes up to 500 µg/ml. It is shown that the toxic effect induced by E. carinatus venom is due to the presence of myotoxic PLA(2) (EcTx-I). The result also corroborates the hypothesis of an association between toxic and enzymatic domains. In conclusion, EcTx-I displays a heparin binding C-terminal region, which is probably responsible for the cytotoxic and bactericidal effects.

Antiviral and anti-inflammatory diterpenoids from the soft coral Sinularia gyrosa.

Chemical investigation of the soft coral Sinularia gyrosa led to the purification of three new diterpenoids, designated as gyrosanols A-C (1-3). The structures of 1-3 were elucidated through extensive spectroscopic analyses. Compounds 1 and 2 exhibited antiviral activity against HCMV with IC(50)'s of 2.6 and 3.7 microM, respectively. In addition, compounds 1 and 2 showed significant anti-inflammatory activity by reducing the levels of the COX-2 protein (19.6 + or - 3.9% and 29.1 + or - 9.6%, respectively) in RAW 264.7 macrophages.

Novel cyclic hexapeptides from marine-derived fungus, Aspergillus sclerotiorum PT06-1.

Two novel cyclic hexapeptides containing both anthranilic acid and dehydroamino acid units, sclerotides A (1) and B (2), were isolated from the marine-derived halotolerant Aspergillus sclerotiorum PT06-1 in a nutrient-limited hypersaline medium. Both 1 and 2 are photointerconvertible and could be interconverted via a radical reaction initiated by direct photoisomerization. Both compounds showed moderate antifungal activity. Compound 2 also showed weak cytotoxicity and antibacterial activity.