Four new polyketides: nectriacids A-C (1-3) and 12-epicitreoisocoumarinol (4), together with three known compounds: citreoisocoumarinol (5), citreoisocoumarin (6), and macrocarpon C (7) were isolated from the culture of the endophytic fungus Nectria sp. HN001, which was isolated from a fresh branch of the mangrove plant Sonneratia ovata collected from the South China Sea. Their structures were ...

A series of new ceritinib analogs by extensive functionalization of the tail piperidine ring with various phosphamides and carbamates have been synthesized. All the ceritinib derivatives were evaluated for their cytotoxic activities against H2228 cell line. From the activity profile obtained, three of the tested compounds (compounds 4, 7 and 9) showed significant cytotoxic effects. Among these ...

PARP-1 inhibition has been studied over the last decades for the treatment of various diseases. Despite the fact that several molecules act as PARP-1 inhibitors, a reduced number of compounds are used in clinical practice. To identify new compounds with a discriminatory PARP-1 inhibitory function, explicit-solvent molecular dynamics simulations using different inhibitors bound to the PARP-1 cat...

A new compound (1), named diaporthelactone, together with two known compounds (2 and 3) were isolated from the culture of Diaporthe sp., a marine fungus growing in the submerged rotten leaves of Kandelia candel in the mangrove nature conservation areas of Fugong, Fujian Province of China. The new compound was elucidated to be 1,3-dihydro-4-methoxy-7-methyl-3-oxo-5-isobenzofuran-carboxyaldehyde ...

Organic wastewater contaminants, including pharmaceuticals, caffeine, and nicotine, have received increased scrutiny because of their detection in water bodies receiving wastewater discharge. Despite recent measurement in United States streams, caffeine's effect on freshwater organisms is not well documented. The present study measured caffeine's lethal and sublethal effects on the freshwater s...

objective the standard of hygiene in daily life and hospitals can be increased by the use of new antimicrobial fibers, which diminish the danger of pathogenic bacteria. in this study, the antimicrobial effect of special fibers on some staphylococcus isolates was investigated. materials and methods the antimicrobial effect of special type of fibers produced in isfahan poly acryl plant on three s...

conclusions the kin gingival chlorhexidine mouthwash has a greater effect than behsa and boht mouthwashes on oral microorganisms and is recommended to be used for plaque chemical inhibition. results the mics for kin gingival, behsa and boht mouthwashes were 0.14, 0.48 and 1000 micrograms/ml using the tube method for s. mutans, respectively. the mbcs for the mentioned mouthwashes were 0.23, 1.9 ...

The petroleum ether and chloroform fractions of ethanol extract of leaf and stem from the plant Passiflora edulis (Fam: Passifloraceae) was subjected to antioxidant, antibacterial and cytotoxic activity. All the fractions showed potent antioxidant activity, of which the chloroform and petroleum ether fraction of stem demonstrated the strongest antioxidant activity with the IC50 value of 51.28 μ...

The effect of tetrahydro-9-aminoacridine (THA) and related compounds on ligand binding to the dissociative anesthetic (phencyclidine, PCP) receptor site was assessed using a rat brain homogenate assay. THA displaced the dissociative anesthetic ligand [3H]N-(1-[2-thienyl]cyclohexyl)3-4-piperidine [( 3H]TCP) binding with an IC50 of 26 microM. Other acridine derivatives displayed similar potency a...

Treatment of cytomegalovirus (CMV) retinitis with oral ganciclovir results in relatively low plasma concentrations of drug, which theoretically could cause more frequent viral resistance compared with intravenous (iv) ganciclovir. By use of a plaque-reduction assay to quantify phenotypic sensitivity to ganciclovir, virus isolates were studied from patients with CMV retinitis participating in fo...