Three novel meroterpenoids, insuetolides A–C (1–3) and four drimane sesquiterpenes, the new (E)-6-(4′-hydroxy-2′-butenoyl)-strobilactone A (4) and the known 2α, 9α, 11-trihydroxy-6-oxodrim-7-ene (5), ...strobilactone A (6) and (E,E)-6-(6′,7′-dihydroxy-2′,4′-octadienoyl)-strobilactone A (7), were isolated from the EtOAc extract of the culture medium of the marine-derived fungus Aspergillus insuetus (OY-207), which was isolated from the Mediterranean sponge Psammocinia sp. The structures of the compounds were determined by spectroscopic methods. Insuetolides A-C reveal a new carbon skeleton derived from the cyclization of farnesyl and 3, 5-dimethylorsellinic acid. Compounds 1, 6, and 7 exhibited anti-fungal activity towards Neurospora crassa with MIC values of 140, 242, and 162μM, respectively; and compounds 3, 4, and 7 exhibited mild cytotoxicity towards MOLT-4 human leukemia cells.
Nepenthes spp. are carnivorous plants that have developed insect capturing traps, evolved by specific modification of the leaf tips, and are able to utilize insect degradation products as nutritional ...precursors. A chitin-induced antifungal ability, based on the production and secretion to the trap liquid of droserone and 5-O-methyldroserone, is described here. Such specific secretion uniquely occurred when chitin injection was used as the eliciting agent and probably reflects a certain kind of defence mechanism that has been evolved for protecting the carnivory-based provision of nutritional precursors. The pitcher liquid containing droserone and 5-O-methyldroserone at 3:1 or 4:1 molar ratio, as well as the purified naphthoquinones, exerted an antifungal effect on a wide range of plant and human fungal pathogens. When tested against Candida and Aspergillus spp., the concentrations required for achieving inhibitory and fungicidal effects were significantly lower than those causing cytotoxicity in cells of the human embryonic kidney cell line, 293T. These naturally secreted 1,4-naphthoquinone derivatives, that are assumed to act via semiquinone enhancement of free radical production, may offer a new lead to develop alternative antifungal drugs with reduced selectable pressure for potentially evolved resistance.
Corneal Staining and Hot Black Tea Compresses Achiron, Asaf; Birger, Yael; Karmona, Lily ...
The Israel Medical Association journal,
03/2017, Letnik:
19, Številka:
3
Journal Article
Recenzirano
Warm compresses are widely touted as an effective treatment for ocular surface disorders. Black tea compresses are a common household remedy, although there is no evidence in the medical literature ...proving their effect and their use may lead to harmful side effects.
To describe a case in which the application of black tea to an eye with a corneal epithelial defect led to anterior stromal discoloration; evaluate the prevalence of hot tea compress use; and analyze, in vitro, the discoloring effect of tea compresses on a model of a porcine eye.
We assessed the prevalence of hot tea compresses in our community and explored the effect of warm tea compresses on the cornea when the corneal epithelium's integrity is disrupted. An in vitro experiment in which warm compresses were applied to 18 fresh porcine eyes was performed. In half the eyes a corneal epithelial defect was created and in the other half the epithelium was intact. Both groups were divided into subgroups of three eyes each and treated experimentally with warm black tea compresses, pure water, or chamomile tea compresses. We also performed a study in patients with a history of tea compress use.
Brown discoloration of the anterior stroma appeared only in the porcine corneas that had an epithelial defect and were treated with black tea compresses. No other eyes from any group showed discoloration. Of the patients included in our survey, approximately 50% had applied some sort of tea ingredient as a solid compressor or as the hot liquid.
An intact corneal epithelium serves as an effective barrier against tea-stain discoloration. Only when this layer is disrupted does the damage occur. Therefore, direct application of black tea (Camellia sinensis) to a cornea with an epithelial defect should be avoided.
Pahutoxin (PHN) is a long chain detergent—like quaternary ammonium cationic substance derived from defensive skin secretions of trunkfish. A recent study has revealed that PHN's ichthyotoxicity and ...its phospholipid membrane disruption effect are produced by two separate mechanisms, which presumably represent two separate physicochemical domains in the PHN molecule
Kalmanzon, E., Rahamim, Y., Barenholz, Y., Carmeli, S., Zlotkin, E., 2003. Receptor-mediated toxicity of pahutoxin, a marine trunkish surfactant. Toxicon 42, 63–71.
Here we report on the occurrence of a natural endogenous mechanism, which regulates the above PHN's functional duality. The regulation is performed by the aid of two separates constituents of the trunkfish secretion, which either selectively amplify PHN's ichthyotoxicity (factor I) or suppress its phospholipids permeabilization effect (factor II).
The ecological significance of such endogenous regulation is discussed.
Pahutoxin (PHN, choline chloride ester of 3-acetoxypalmitic acid) is a natural fish-killing (ichthyotoxic) agent derived from the defensive secretions of trunkfish. In spite of its obvious structural ...resemblance to synthetic cationic long-chain quaternary ammonium detergents, we show that PHN's action does not rely on its surfactant properties and is in fact, receptor-mediated. The above conclusion is supported by the following data:
1.
Ichthyotoxicity is not related to its detergency or surfactivity, as indicated by the fact that the lethal concentration is about 1.5 orders of magnitude below its critical micelle concentration value (69 μM) and its liposomal/seawater partition coefficient is low (62–85);
2.
The trunkfish is tolerant to its own pahutoxin;
3.
Ichthyotoxicity occurs only upon application to the surrounding water, suggesting the existence of externally located receptors;
4.
The receptor hypothesis was supported by the aid of equilibrium saturation binding assays revealing the presence of specific binding sites to PHN on the fish gill membranes;
5.
The PHN tolerant trunkfish was shown to be devoid of PHN-binding sites.
Some chemo-ecological, and environmental implications are discussed.
Pahutoxin a quaternary ammonium salt surfactant serves as an active ingredient in the defensive skin secretion of various marine trunkfish (Ostracociidae). In the defensive skin secretion of the Red ...Sea trunkfish, Ostracion cubicus the effect of PHN is amplified due to the existence of non toxic polypeptides which act as (a) PHN - chelators and (b) potentiators. The secretion of the Red Sea trunkfish includes an additional category of pharmacologically active polypeptides represented by boxin 7 which similarly to PHN they independently kill fish exclusively through medium application. By the aid of radiolabeled PHN and a fish gill membrane preparation a series of equilibrium saturation binding assays were carry out which demonstrate that PHN performs its biological defensive function via receptors and not due to its surface activity. The gill membranes of the trunkfish were shown to be devoid of PHNreceptors. The pharmacological, ecological and environmental implications of the above data are discussed.
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