Synthesis, antioxidant, and cytotoxic activities of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl Acetamides

A new class of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl acetamides was prepared from the respective (oxazolyl/thiazolyl/imidazolyl)carbamoyl-methylthio acetic acid and studied their antioxidant activity and cytotoxic activitity against A549 lung adenocarcinoma cells. The methyl-substituted sulfonyl bisoxazoles exhibited excellent radical scavenging activity. On the other hand, the chloro-substituted sulfonyl bisthiazoles (IC50 = 49 A mu M) and sulfonyl bisimidazoles (IC50 = 24 A mu M) showed noticeable cytotoxic activity on A549 cells.

A Review of the Aquatic Environmental Fate of Triclopyr and its Major Metabolites

The purpose of this paper is to provide an overview of the aquatic environmental fate of triclopyr and its major metabolites, TCP and TMP. This review is primarily based on results of laboratory and field studies conducted by various Federal Agencies and the registrant to support the US aquatic registration for triclopyr TEA.

Resveratrol Metabolites Modify Adipokine Expression and Secretion in 3T3-L1 Pre-Adipocytes and Mature Adipocytes

Objective: Due to the low bioavailability of resveratrol, determining whether its metabolites exert any beneficial effect is an interesting issue. Methods: 3T3-L1 maturing pre-adipocytes were treated during differentiation with 25 mu M of resveratrol or with its metabolites and 3T3-L1 mature adipocytes were treated for 24 hours with 10 mM resveratrol or its metabolites. The gene expression of adiponectin, leptin, visfatin and apelin was assessed by Real Time RT-PCR and their concentration in the incubation medium was quantified by ELISA. Results: Resveratrol reduced mRNA levels of leptin and increased those of adiponectin. It induced the same changes in leptin secretion. Trans-resveratrol-3-O-glucuronide and trans-resveratrol-4'-O-glucuronide increased apelin and visfatin mRNA levels. Trans-resveratrol-3-O-sulfate reduced leptin mRNA levels and increased those of apelin and visfatin. Conclusions: The present study shows for the first time that resveratrol metabolites have a regulatory effect on adipokine expression and secretion. Since resveratrol has been reported to reduce body-fat accumulation and to improve insulin sensitivity, and considering that these effects are mediated in part by changes in the analyzed adipokines, it may be proposed that resveratrol metabolites play a part in these beneficial effects of resveratrol.

Estudo toxicológico de extratos do coral alcionáceo Chromonephthea braziliensis (Alcyonacea, Nephtheidae)

Os recifes de corais são ecossistemas diversos com alta densidade de biodiversidade, o que leva a intensa competição entre as espécies. Estas espécies podem produzir substâncias desconhecidas, muitas com valor farmacológico. Chromonephthea braziliensis é um coral mole invasor, originário do Oceano Indo-Pacífico, que foi possivelmente transportado por plataformas de petróleo e cuja presença é uma ameaça para a biodiversidade da região de Arraial do Cabo (RJ). Esta espécie produz metabólitos secundários que são responsáveis pela indução de danos para o ecossistema local. A finalidade deste estudo é a busca de novas substâncias para quimioterapia geral com base na estrutura de compostos bioativos. Extratos desse coral foram preparados a partir de colônias liofilizadas (solventes: hexano, diclorometano, acetato de etila e metanol). Realizaram-se análises químicas para a caracterização dos extratos e avaliaram-se as atividades: mutagênicas e citotóxicas, usando o ensaio de mutação reversa bacteriana (Salmonella/microssoma) com as linhagens TA97, TA98, TA100 e TA102; genotóxicas, utilizando análise da quebra do DNA e formação de micronúcleos na linhagem RAW 264,7 de macrófagos e; tóxicas para náuplios de microcrustáceos Artemia salina. Observou-se citotoxicidade, na presença de S9 mix, dos extratos diclorometano para a linhagem TA102 na concentração de 20 g/100 L/placa e metanol para a TA97 com 5 e 20 g/100 L/placa. Os extratos diclorometano, acetato de etila e metanol apresentaram genotoxicidade no DNA plasmidial em concentrações elevadas (250 g/mL), mas nenhum dano ao DNA foi observado no ensaio de micronúcleo. Todos os extratos foram tóxicos para os náuplios de microcrustáceos em pelo menos uma das concentrações usadas (0,01 1000 g/mL), e a LC50 pode ser determinada apenas para os extratos hexano, diclorometano e acetato de etila.

Shrimp disease management using bioactive marine secondary metabolites: an eco-friendly approach

Vibriosis caused by opportunistic and secondary bacterial pathogens is still a serious disease problem in aquaculture of the black tiger shrimp Penaeus monodon. Attempts were made for controlling shrimp bacterial disease using Marine Secondary Metabolites (MSMs). Findings indicated that the MSMs of seaweed Ulva fasciata and Dendrilla nigra are effective for controlling shrimp bacterial pathogens.

Immnunomodulatory and cytotoxic effects of aqueous leaf extracts of certain plants on common carp, Cyprinus carpio

Effect of aqueous leaf extracts of Catheranthus roseus, Calotropis gigantium and Datura stromoneum on common carp, Cyprinus carpio were investigated. C. carpio were separately fed with 1 and 2% aqueous extracts of these three plant leaves for a period of seven days. In 1% Catheranthus roseus of leaf extract fed group no significant tissue level changes were recorded. One and 2% of other two species fed treated group showed mild to severe necrotic and cellular changes in liver, kidney and spleen. Immunologically, significant rise in antibody titre and respiratory burst activity was recorded for 1% Catheranthus roseusfed group.

Indole and carbazole alkaloids from Glycosmis montana with weak anti-HIV and cytotoxic activities

A diprenylated indole, (E)-3-(3-hydroxymethyl-2-butenyl)-7-(3-methyl-2-butenyl)-1H-indole (1), and six known carbazole alkaloids were isolated from the twigs and leaves of Glycosmis montana Pierre (Rutaceae). Their structures were determined on the basis of analysis of spectral evidence including 1D and 2D NMR and MS. The alkaloids (1-3) exhibited weak to moderate take in vitro inhibitory activity against HIV replication in C8166 cells, and they (as well as carbalexine A and B) had cytotoxic activity against the human leukaemia cell line CCRF-CEM. (c) 2005 Elsevier Ltd. All rights reserved.

Impact of phosphamidon and its metabolites on histopathology of the liver, gill and intestine of Labeo rohita

Impact of phosphamidon, an organophosphorus pesticide and its metabolites viz. dimethyl phosphoric acid and 2-chloro 2-diethyl carbamoylmethyl vinyl acid on histopathology of a common teleost, Labeo rohita was studied by exposing the fish to sub-lethal concentrations which were taken as 1/3rd of LC50 and were equal to 0.0123 ppm for phosphamidon, 0.0160 ppm for dimethyl phosphoric acid and 0.0167 ppm for 2-chloro 2-diethyl carbamoylmethyl vinyl acid respectively. The results revealed that hepatocytes in the liver were markedly swollen and exhibited hydropic degeneration. Fusion of primary lamellae and moderate congestion of blood vessels were evident in the gill. Intestine showed degeneration of mucosa and cellular infiltration in sub-mucosa. LC50 values and histopathological photomicrographs suggest that phosphamidon is more toxic as compared to dimethyl phosphoric and 2-chloro 2-diethyl carbamoylmethyl vinyl acid.

Isolatin [sic] the bacteria produced biactive [sic] metabolits [sic] cytotoxic compound in order to prduction [sic] anticancer substance in the coral regin [sic] the Persian Gulf (Larak Island)

In the present investigation the marine bacteria isolated from corals, sponges sea water and sediments of coral regions in the larak Island located in the Persian Gulf and were examined for ability to produce cytotoxic metabolits in order to use as an anticancer compounds. Cytotoxic effect were isolated bacteria from different samples and were examined by Artemia Cytotoxic Bioassay test, in which 4.5 percent of sea waters, 12 percent of sediments and 28 percent of marine invertebrat showed cytotoxic activity, using Brine Shrimp Bioassay test. Streptomyces S-2004 isolated from soft coral specified as Sinularia erecta had LC50=0.5mg/m1 in Brine Shrimp Bioaassay test. The streptomyces S-2004 produced cytotoxic metabolits in low nutrient condition and sea water medium after 7 days on 250 rpm shaken in vitro condition. The extract partially were semipurified. Then ethyl acetate extraction from aceton extracted of bacterial plate had cytotoxic effect (LC50=4.19ktg/m1) in Human epidermoid carcinoma of mouth cells (KB) by using neutral red assay. Morphological effects of this extract on KB cells showed turgescence, cellular blebs and apoptosis which was a proof for anticancer compounds of the extract. It is seems that streptomyces S-2004 is a new strain and could be introduced as a talented bacteria, which produced cytotoxic metabolits.

Short-term cytotoxic and inflammatory responses of human monocytes to stainless steel fibre networks

The aim of the current work was to examine the human monocyte response to 444 ferritic stainless steel fibre networks. 316L austenitic fibre networks, of the same fibre volume fraction, were used as control surfaces. Fluorescence and scanning electron microscopies suggest that the cells exhibited a good degree of attachment and penetration throughout both networks. Lactate Dehydrogenase (LDH) and TNF-α releases were used as indicators of cytotoxicity and inflammatory responses respectively. LDH release indicated similar levels of monocyte viability when in contact with the 444 and 316L fibre networks. Both networks elicited a low level secretion of TNF-α, which was significantly lower than that of the positive control wells containing zymosan. Collectively, the results suggest that 444 ferritic and 316L austenitic networks induced similar cytotoxic and inflammatory responses from human monocytes. © 2012 Materials Research Society.

Determination of microcystin-LR and its metabolites in snail (Bellamya aeruginosa), shrimp (Macrobrachium nipponensis) and silver carp (Hypophthalmichthys molitrix) from Lake Taihu, China

This paper describes seasonal changes of microcystin-LR (MC-LR) and its glutathione (MC-LR-GSH) and cysteine conjugates (MC-LR-Cys) in three aquatic animals - snail (Bellamya aeruginosa), shrimp (fMacrobrachium nipponensis) and silver carp (Hypophthalmichthys molitrix) collected from Lake Taihu, China. MC-LR, MC-LR-GSH, and MC-LR-Cys were determined by liquid chromatography electrospray ionization mass spectrum (LC-ESI-MS). The mean MC-LR concentrations in the hepatopancreas of snail and shrimp and liver of silver carp were 6.61, 0.24, and 0.027 mu g g(-1) dry weight (DW), respectively: while the average MC-LR-Cys concentrations were 0.50, 0.97, and 5.72 mu g g(-1) DW, respectively. MC-LR-GSH was usually not detectable in these samples. The above results suggest that: (1) in aquatic animals, especially fish, the main excretion form of MC-LR could be MC-LR-Cys, but not MC-LR-GSH, whereas MC-LR-Cys might play an important role in detoxication of MC-LR and (2) that efficiency of MC-LR-Cys formation differs among species. The main detoxication pathway of MC-LR in aquatic animals is suggested as follows: when MC-LR enters into liver/hepatopancreas, it firstly conjugates with polypeptide or protein (including GSH, PP-1 and 2A) containing Cys residues, perhaps also some free cysteine; subsequently, MC-LR-Cys is degraded from these polypeptide or protein; and finally is excreted from animals by the compound of MC-LR-Cys. (C) 2009 Elsevier Ltd. All rights reserved.