A series of 4(3H)-quinazolinone derivatives bearing dithiocarbamate side chains have been synthesized through the reaction of 6-bromomethyl-2-methyl-4(3H)-quinazolinone with CS2 and various amines in the presence of anhydrous K3PO4, and their structures were confirmed with ESI-MS, H NMR, elemental analysis or HRMS. The target compounds 8a -8q were tested for their in vitro antitumor activity against human myelogenous leukaemia K562 and human Hela cell lines by means of colorimetric MTT assay. Among the tested compounds, 8q exhibited in vitro inhibitory activity against K562 and Hela cells with IC50 values of 0.5 and 12.0 micromol x L(-01), respectively. Therefore, compound 8q is worthy to be a lead compound for the design and synthesis of new antitumor agents.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Ethylenebis(dithiocarbamates) ; chemical synthesis ; chemistry ; pharmacology ; HeLa Cells ; Humans ; Inhibitory Concentration 50 ; K562 Cells ; Molecular Structure ; Quinazolinones ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

This study was conducted to identify the Colletotrichum species causing anthracnose disease of strawberry in Balgladesh and to evaluate in vitro activity of commercial fungicides it. Based on morphological and cultural characteristics, all 22 isolates were identified as Colletotrichum gloeosporioides. They developed white or glittery colonies with grey to dark grey reverse colony colors and they produced cylindrical conidia. The efficacy of five commercial fungicides, Bavistin DF, Dithane M-45, Sulcox 50 WP, Corzim 50 WP and Rovral 50 WP, were tested against the fungus. Bavistin inhibited radial growth completely and was followed in efficacy by Dithane M-45. In Bavistin DF treated media, the fungus did not produce conidia. The percent inhibition of radial growth of the fungus was increased with the increasing concentrations of fungicide.
Aminoimidazole Carboxamide ; Bangladesh ; Benzimidazoles ; Carbamates ; Colletotrichum ; Cultural Characteristics ; Fragaria ; Fungi ; Humans ; Hydantoins ; Maneb ; Spores, Fungal ; Zineb

The present study was undertaken to explore the inhibitory effect of cyanobacterial extracts of Nostoc commune FA-103 against the tomato-wilt pathogen, Fusarium oxysporum f. sp. lycopersici. In an optimal medium, cell growth, antifungal activity, and antifungal compound production could be increased 2.7-fold, 4.1-fold, and 13.4-fold, respectively. A crude algal extract had a similar effect as mancozeb at the recommended dose, both in laboratory and pot tests. In vitro and in vivo fungal growth, spore sporulation and fungal infection of wilt pathogen in tomato seeds were significantly inhibited by cyanobacterial extracts. Nostoc commune FA-103 extracts have potential for the suppression of Fusarium oxysporum f. sp. lycopersici.
Azepines ; Cyanobacteria ; Fluoroquinolones ; Fusarium ; Lycopersicon esculentum ; Maneb ; Nostoc commune ; Seeds ; Spores ; Zineb

OBJECTIVETo study the dominant seed-borne fungi of Glycyrrihiza seeds which were from different producing area and compare the disinfection effect of several fungicides on seed-borne fungi of Glycyrrihiza seed.

METHODPetri-dish testing was used to determine the external and internal seed-borne fungi and the disinfection effect of fungicides.

RESULT AND CONCLUSIONThe result showed that the amount of spore on the surface of one Glycyrrihiza seed varied from 0.3% to 37.0% among samples. Penicillium spp. and Aspergillus spp. were the two major dominant fungi and there was few differences in the type of the fungi among producing areas but differences in the isolation frequency of the furgi; Penicillium spp. , Rhizopus spp. , Aspergillus spp. and Alternaria spp. were the internally dominant seed-borne fungi, including seed capsule and the internal tissue of seed and their fungi-carrying percentage was 8.0%-48.3% and 3.5%-42.0% respectively. There were differences in fungi percentage and dominant seed borne fungi among different producing areas. The disinfection effect of both mancozeb and thriam was up to 89.0%, so it is suggested to use them to disinfect Glycyrrihiza seed.

Aspergillus ; drug effects ; isolation & purification ; Fungicides, Industrial ; pharmacology ; Glycyrrhiza uralensis ; microbiology ; Maneb ; pharmacology ; Penicillium ; drug effects ; isolation & purification ; Plants, Medicinal ; microbiology ; Rhizopus ; drug effects ; isolation & purification ; Seeds ; microbiology ; Zineb ; pharmacology

OBJECTIVETo investigate the effects of exposure of paraquat and maneb on the behavior, the morphology and electrical activity of the Substantia nigra and striatum, and to discuss the relationship between this two pesticides and Parkinson's disease.

METHODS37 rats were divided randomly into 3 groups: control group (n = 11), paraquat (10 mg/kg) group (n = 13) and combinative group of paraquat (10 mg/kg) and maneb (30 mg/kg) (n = 13), and were exposed twice a week for 6 weeks by intraperitoneal injection. The behavior of animals in the declined-plane, the vertical-grid and the open-field test were observed. The morphology of substantia nigral neurons were investigated by HE pathology. The spontaneous discharge of striatum neurons were recorded after exposure.

RESULTSCompared to the control group and the pre-exposure group, both the numbers of animals sliding down from the declined-plane and the latency of rats' moving on the vertical-grid significantly increased, and the animals' autonomic movement decreased significantly (P < 0.05, P < 0.001). After the combinative exposure, the neurons of the Substantial nigra pars compacta (SNPc) were progressively impaired, the cell density of the paraquat group [(82.17 ± 12.91) n/mm(2)] and the combined group [(41.15 ± 6.44) n/mm(2)] were lower than that in control group (143.10 ± 20.85 n/mm(2)] (P < 0.01). In the paraquat group (5.97 ± 7.30 Hz) and the combined group [(6.95 ± 9.87) Hz], the average discharge rates of the striatum neurons were increased significantly compared to the control group [(1.78 ± 5.05) Hz] (P < 0.01). The bursting discharge was increased significantly in the combined group (22.3%) compared to the control group (9.8%) and the paraquat group (5.6%) (P < 0.05, P < 0.01).

CONCLUSIONThe co-exposure of paraquat and maneb could induce similar symptoms to Parkinsonism syndrome of rats such as rigidity, moving reduction and etc, and the combined exposure had a certain enhanced effect compared to alone paraquat exposure. The combinative exposure of paraquat and maneb could cause neural loss in SNPc and it is involved with the enhanced electrophysiological activity in striatum. The synergy toxicity of paraquat and maneb in nigrostriatal system is related to Parkinson's disease.

Animals ; Corpus Striatum ; drug effects ; Male ; Maneb ; toxicity ; Paraquat ; toxicity ; Parkinsonian Disorders ; chemically induced ; Pesticides ; toxicity ; Rats ; Rats, Sprague-Dawley ; Substantia Nigra ; drug effects