bluuebunny/crossref_metadata_2025_split huggingface dataset:
Specific Crystal Chemical Interactions between Carcinogenic Aromatic Compounds and Cholesterol
Authors: Contag Bodo 
Published: August 2018

Abstract
Polycyclic aromatic hydrocarbons and aromatic amines exercise a highly specific influence on the crystallization of cholesterol. The strength of these non-covalent, presumably epitaxial interactions correlates with the carcinogenic activity of these substances. The presented results are in support of the assumption that a specific process of adsorption and crystallization with cholesterol of the plasma membrane takes place during the initial phase of the carcinogenesis by aromatic compounds.
Studies in Enteric Anthelmintics: Activity Profile of Prodrug of a Bisbenzimidazole
Authors: Khan A. M. , Gupta Suman , Katiyar J. C. , Singh Sudhir K. , Sharma V. L. , Sharma Satyavan , Bhaduri A. P. 
Published: August 2018

Abstract
The comparative anthelmintic activity of a possible prodrug, 2,2′-dicarbomethoxyamino-5,5′-dibenzimidazolyl methanol (2) with its parent compound 2,2′-dicarbomethoxyamino-5,5′-dibenzimidazolyl ketone (1) and the reference drug mebendazole (3 a) is reported. At a dose of 25 mg/kg, compound 2 was 100% effective against Ancylostoma ceylanicum in hamsters. Compound 2 also exhibited a similar order of activity against Syphacia obvelata, Hymenolepis nana and H. diminuta at a dose of 100 mg/kg. The drug exhibited lethal effects against metamorphic forms of A. ceylanicum at a dose of 100 mg/kg. However the trichostrongylids, Nippostrongylus brasiliensis remained unaffected up to a dose of 250 mg/kg of 2. Both 1 and 3 a exhibited inferior activity than 2 except against adult A. ceylanicum. The activity of 1 and 2 has been explained on the basis of their ability to resist systemic hydrolysis resulting in higher concentration of the active drug in biophase.
Directed Cell Movement with Steric Exclusion
Authors: Gruler H. 
Published: August 2018

Abstract
The space-dependent density of cells is evaluated for the following situation: (i) The cells are forced to make a directed movement (ii) the space for the cellular migration is restricted. The steady state distribution density is obtained when the drift current density equals the diffusion current density. The analogy to the Boltzmann statistics is shown. In a further step the cellular volume is introduced. For this case the density distribution is described in analogy to the Fermi statistics. The necrotactic response of granulocytes is used to verify the model.
Growth Inhibitions on Human Cancer Cell Cultures with the Indole Sulphur-Containing Phytoalexins and Their Analogues
Authors: Tempête Christiane , Devys Michel , Barbier Michel 
Published: August 2018

Abstract
Cell growth inhibitions on human cancer cell cultures were determined for the indole sulphur-containing phytoalexins cyclobrassinin, brassilexin (previously isolated from vegetables of the Cruciferae family) and their synthetic analogues 5-methoxybrassilexin and homocyclobrassinin. The most biologically active of these products is brassilexin (LD50= 8 μg/ml).
Isoflavone Glycoside Formation in Transformed and Non-Transformed Suspension and Hairy Root Cultures of Lupinus polyphyllus and Lupinus hartwegii
Authors: Berlin J. , Fecker L. , Rügenhagen C. , Sator C. , Strack D. , Witte L. , Wray V. 
Published: August 2018

Abstract
Transformed cell suspension and hairy root cultures were established by infecting seedlings of Lupinus polyphyllus and L. hartwegii with various wild type strains of Agrobacterium tume-faciens and A. rhizogenes. Transformation of the cultures was confirmed either by their phyto­hormone autotrophy, detection of opines or southern analysis. Glueosides of genistein and 2′-hydroxygenistein, were found to be the main secondary metabolites in normal and trans­formed suspension cultures as well as in hairy root cultures. Although some of the isoflavone glycosides of the cultures were apparently new constituents of Lupinus, they were afterwards also found in young seedlings.
Schweres Wasser (D2O) als Protektivum proteinhaltiger Arzneimittel. Beispiel: humane Cholinesterase/Protein Drugs Stabilized by Heavy Water (D2O). For Example: Human Cholinesterase
Authors: Heyde Ch. , Wenzel M. 
Published: August 2018

Abstract
Looking for a possible protective effect of heavy water on proteins, cholinesterase and lac­tate dehydrogenase in combination with D2O and further protective substances were exposed to a temperature of 60 °C (for 10 min) and about 45 °C (for several days). In combination with glycerine there resulted an additive protective effect; with NaCl and/or albumin being added the individual effects raised to a higher level. In the cold D2O protects cholinesterase only against acid denaturation, but in combination with warmth also against basic denaturation.
Bioactive Chemical Bond Systems in Safeners and Prosafeners
Authors: Dutka Ferenc 
Published: August 2018

Abstract
Acetals and ketals involving a dichloromethyl group on their central carbon atom were found to be active or highly active as safeners of corn against thiocarbamate and chloroacet-anilide herbicide injury. A mechanism for the biotransformation of these compounds as pro­safeners to the actual dichloroacetic ester safeners is proposed.
Similarly, S-and N-analogues of the cyclic acetals (ketals) which show safener activity can also be considered as prosafeners because they can be converted in the biophase by the same mechanism into actual safeners such as dichloroacetic thiolesters or dichloroacetamides sup­porting the bioactivation hypothesis.
Characteristic bioactive chemical bond systems in safeners and prosafeners are suggested.
Chemical Reactivity and Safener Activity of Acetal Compounds
Authors: Ekler Zsigmond , Dutka Ferenc 
Published: August 2018

Abstract
Although detailed examinations have been published on structure-activity relationships of herbicide safeners, only a few data are available on chemical reactivity-safener activity relationships. Chemical reactivity of acetamide type compounds as well as their safener activity against thiocarbamate herbicides change with the number of chlorine substituents in the order: non-chlorinated < monochloro < dichloro. Several compounds of another chemical group, acetals (e.g. MG-191, 2-dichloromethyl-2-methyl-1,3-dioxolane), are also effective safeners for thiocarbamate herbicides. According to our growth room studies, the safener activity of acetals also increases with increasing chlorine content up to two chlorine atoms on the same carbon. A number of differently chlorinated acetals have been synthesized and their acid-catalyzed hydrolysis rate determined in order to establish a relationship between their bioactivity and chemical reactivity. The hydrolysis rate order of acetals containing no, one or two chlorine atoms: non-chlorinated > monochloro > dichloro, is just the opposite than what has been found for acetamides. Thus, safener activity of acetals increases with decreasing chemical reactivity. The opposite reactivity order of acetamides and acetals can be explained by the different mechanisms of their hydrolysis. Dichloroacetals may not be effective safeners in their original structure. In plants, however, they can be biologically activated to active safeners by a transformation other than hydrolysis.
An Overview of the Mechanisms of Action of Herbicide Safeners
Authors: Hatzios Kriton K. 
Published: August 2018

Abstract
Herbicide safeners are chemicals used for manipulating the tolerance of large-seeded grass crops to selected soil-applied herbicides. The physiological interactions of herbicides and their respective safeners are characterized by the following facts: a) safeners are most effective when applied prior to or simultaneously with the herbicides whose injury they prevent; b) safeners exhibit a high degree of botanical and chemical specificity protecting only certain grasses against injury caused from specific classes of herbicides; and c) protected grass crops are moderately tolerant to the antagonized herbicides. At the biochemical level, safeners may act either as “bioregulators” regulating the amount of a given herbicide that reaches its target site in an active form or as “antagonists” of herbicidal effects at a similar site of action. A safener-induced enhancement of herbicide detoxication in protected plants is currently viewed as the most apparent mechanism for the action of the currently available safeners. Safeners enhance the conjugation of carbamothioate and chloroacetanilide herbicides with glutathione either by elevating the levels of reduced glutathione (GSH) or by inducing the activity of specific glutathione S̱-transferases (GSTs). A safener-induced enhancement of the activity of other degradative enzymes such as the cytochrome P450-dependent mixed function oxidases or UDP-glucosyl transferases seems to be important for the protective action of safeners against injury from aryloxyphenoxypropionate, imidazolinone, and sulfonylurea herbicides. Metabolic processes related to acetyl-CoA metabolism have been implicated as likely target sites for a competitive antagonism between safeners and chloroacetanilide or carbamothioate herbicides. At the molecular level, the “gene activation” and “gene amplification” theories offer a likely explanation for the action of safeners.
Comparative Effectiveness and Mode of Action of Safeners for Chloroacetamide Herbicides in Maize Seedlings
Authors: Ekler Zsigmond , Stephenson Gerald R. 
Published: August 2018

Abstract
In growth room bioassays, four herbicide safeners {BAS-145138: 1-dichloroacetyl-hexa-hydro-3,3,8a-trimethyl-pyrrolo(1,2a)pyrimidin-6(2H)-one, dichlormid: N,N-diallyl-2,2-dichloroacetamide, flurazole: phenylmethyl 2-chloro-4-(trifluoromethyl)-5-thiazole-carboxylate and MG-191: 2-dichloromethyl-2-methyl-1,3-dioxolane} were compared for their effective­ ness in reducing metazachlor {N-(2,6-dimethylphenyl)-N-(1-pyrazolylmethyl)-chloroacet-amide} injury to maize seedlings. Three of these compounds (BAS-145138, dichlormid and MG-191) and two different compounds (AD-67: N-dichloroacetyl-1-oxa-4-azaspiro-4,5-de-cane and DKA-24: N ,N2-diallyl-N2-dichloroacetylglycineamide) were also evaluated as safe­ners for acetochlor {N-(2-ethyl-6-methylphenyl)-N-(ethoxymethyl)chloroacetamide} in maize seedlings. Both BAS-145138 and dichlormid were highly effective as safeners for metazachlor and BAS-145138 and DKA-24 were equally good safeners for acetochlor.
Metazachlor and acetochlor uptake and metabolism by maize seedlings were enhanced sig­nificantly in response to treatment with every safener examined. Rates of metazachlor and acetochlor uptake and metabolism were greatest in seedlings treated with BAS-145138 -the most effective safener.
In the absence of any safener treatment, the non-enzymatic conjugation of the herbicides with glutathione either exceeded (metazachlor) or was similar (acetochlor) to enzymatic conjugation. However, the rate of enzymatic conjugation was generally increased by safener treat­ ment. This was particularly true when the herbicide (14C-labeled) was employed as a conjuga­tion substrate instead of the less specific substrate, CDNB (1-chloro-2,4-dinitrobenzene).
A significant linear correlation was observed between safener effectiveness and rates of metazachlor metabolism or glutathione S-transferase activity in maize seedlings. However, a similar correlation could not be established for the five compounds evaluated as safeners for acetochlor.
Influence of the Safener Benoxacor on the Metabolism of Metolachlor in Corn
Authors: Cottingham C. K. , Hatzios K. K. 
Published: August 2018

Abstract
The herbicide safener benoxacor (CGA -154281) is effective in protecting corn from meto­lachlor injury. Glutathione-S-transferase (GST) activity of corn seedlings was stimulated by low concentrations of benoxacor as was the formation of a polar metabolite identified as the glutathione (GSH) conjugate of metolachlor. A similar degree of enhancement of metolachlor metabolism was observed in both a metolachlor-tolerant (’Cargill 7567’) and a metolachlor-susceptible (’Northrup-King 9283’) corn line. The total GSH content of shoots of the metolachlor-susceptible corn hybrid was not affected by benoxacor treatment, but an increase was noted for shoots of the tolerant corn hybrid. The two corn hybrids with differential tolerance to metolachlor also differ in their dose response to benoxacor with higher safener concentra­tions failing to induce or inhibit GST activity of the tolerant ’Cargill 7567’ corn line. Stimula­tion of GST activity and a corresponding enhanced rate of metolachlor metabolism can ac­count for the safening effect of benoxacor. These mechanism of action of dichloroacetamide safeners.
Effects of the Herbicide Pretilachlor and the Safener Fenclorim on Glutathione Content and Glutathione-Dependent Enzyme Activity of Rice
Authors: Han Seong , Hatzios Kriton K. 
Published: August 2018

Abstract
The influence of individual or combined treatments of the chloroacetanilide herbicide preti­lachlor and the safener fenclorim on glutathione content and the activity of glutathione reduc­tase (GR, EC 1.6.4.2) and glutathione-S-transferase (GST, EC 2.5.1.18) of rice (Oryza sativa L., var. Lamont) was investigated in a time-course study including 0, 12, 24, 48, and 72 h peri­ods after treatment. Pretilachlor applied alone at 2 μM did not influence the levels of total or reduced glutathione of germinating rice seedlings. Fenclorim applied alone at 20 μM increased significantly the levels of total and reduced glutathione of rice seedlings at 12, 24, and 72 h after treatment. The combination of pretilachlor and fenclorim increased the levels of total and reduced glutathione of rice at all time periods. GR activity extracted from pretilachlor-treated rice seedlings was significantly lower than that extracted from untreated rice seedlings. Pretreatment of rice seedlings with the safener fenclorim increased GR activity at 12 and 24 h, but not at 48 and 72 h after treatment. GR activity extracted from rice seedlings treated with the combination of pretilachlor and fenclorim was significantly higher than that of untreated controls at 12, 24, and 48 h after treatment. Pretreatment of rice seedlings with pretilachlor reduced the activity of GST which catalyzes the conjugation of this herbicide with reduced glutathione at time intervals greater than 24 h. Pretreatment with fenclorim did not have any effect on GST activity of rice seedlings. Pretreatment with the combination of pretilachlor and fenclorim increased GST activity of rice seedlings at the 48 and 72 h periods. These results suggest that a simultaneous application of pretilachlor and fenclorim is critical for the enhance­ment of glutathione and glutathione-related enzyme activity and the protection of rice from pretilachlor injury.
Effect of a Safener Towards Thiocarbamates on Plant Lipid Metabolism
Authors: Abulnaja Khalid O. , Harwood John L. 
Published: August 2018

Abstract
It has been found that various thiocarbamate herbicides, known to alter surface wax and cutin synthesis, inhibit the elongation of fatty acids. We have proposed this as a mode of ac­tion of such compounds. Because it is believed that the sulphoxide metabolites of thiocarba­mates are the active intermediates, we have examined the action of 1-aminobenzotriazole (an inhibitor of sulphoxide formation) on the inhibition of very long-chain fatty acid biosynthesis. In all tissues tested, aminobenzotriazole was able to block the specific inhibitory effect of thio­carbamates on fatty acid elongation. These results add further support to our proposal that fatty acid elongation is a sensitive target site for thiocarbamate herbicides in plants.
Safeners as Corn Seedling Protectants against Acetolactate Synthase Inhibitors
Authors: Milhomme Henri , Roux Christophe , Bastide Jean 
Published: August 2018

Abstract
Zea mays L., cv. Potro, shoots had a higher level of resistance to imazaquin (IQ) and metsul­furon methyl (MSM) than roots. Shoot lengths were increased by pretreating the seeds with commercial 1,8-naphthalic anhydride (NA) at 1% (w/w) or oxabetrinil at 0.2% (w/w). The growth of shoots of safened seeds was unaffected by 400 nᴍ IQ and by 40 nᴍ MSM.
The in vivo activity of acetolactate synthase (ALS) extracted from corn shoots and roots was not affected by treatments with IQ or MSM , but pretreatment of seeds with NA or oxabetrinil, prior to germination, caused an increase in the level of extractable ALS from shoots. ALS activity from roots and shoots of NA-pretreated seedlings was increased to a large degree (> 40 %) when the seedlings were germinated on 40 nᴍ MSM , whereas ALS acti­vities from oxabetrinil-pretreated seedlings were enhanced to a lesser degree (≈20%). ALS from unsafened seedlings was inhibited 21% by 400 nᴍ IQ and 70% by 40 nᴍ MSM in vitro, but ALS from roots of seedlings germinated on 400 nᴍ IQ was not inhibited by 400 nᴍ IQ in vitro.
Chlorophyll Proteins and Lipids in Paraquat Treated Sensitive and Resistant Conyza Canadensis Leaves
Authors: Szigeti Zoltán , Sárvári Éva , Lehoczki Endre 
Published: August 2018

Photosynthetic activity and molecular composition of thylakoid membranes of sensitive and atrazine/paraquat coresistant biotypes of Conyza canadensis (L.) Cronq was compared before and after 5 × 10-4 molar paraquat spraying. In contrast to the irreversibly damaged sensitive plants the Rfd values (vitality indices) calculated from parameters of fluorescence induction curves, and the in vivo CO2 fixation in resistant plants showed - after a transitory inhibition - a recovery.
Resistant thylakoids contained higher amount of PS II and LHC II, (i.e. lower relative amount of CP I) which can be the result of an adaptation process. Fatty acid composition of total leaf extract was almost the same in both biotype even after spraying. The amount of the oligomeric form of LHCP II decreased in paraquat treated sensitive thylakoids, which was in correlation with the reduction of Δ3-transhexadecanoic acid content. Decrease in oligomeric LHCP II and/or special lipids (PG) in sensitive thylakoids may change the association of LHCP II and photosystem II core as it is evidenced from lowering of the Mg2+ induced changes of the short wavelength fluorescence intensity and increase in the relative quantum requirement values. The results are discussed in connection with a possible effect of paraquat on PS II.
Non-Essential Activation of Rat Liver Porphobilinogen-Deaminase by Folic Acid
Authors: Noriega Guillermo O. , Juknat Adela A. , Batlle Alcira M. del C. 
Published: August 2018

This report demonstrates the ability of folic acid to activate rat liver porphobilinogen-deaminase (PBG -D). Lineweaver-Burk analysis revealed an increase in Vmax (38%) without affecting the Km. In the concentration range assayed, secondary replots of 1/Δslope and 1/Δintersect versus 1/[folic acid] yielded straight lines, indicating the binding of a single molecule of activator to the enzyme PBG-D , with a KA = 1.66 mᴍ. Results presented here show that folic acid acts as a non-essential activator (α = 1; β = 1.6).
The activating effect of folic acid has been observed employing the 35-70% ammonium sulphate precipitated fraction, desalted by dialysis or gel filtration, whereas no action was detected when other partially purified PBG -D preparations were utilized as the enzyme source, suggesting either the presence of sites saturated for the activator, or the existence of a different structural protein conformation, or both.
Effects of Chloroquine on the Photosensory Membrane Turnover and the Ultrastructure of Lysosome-Related Bodies of the Crayfish Photoreceptor
Authors: Schraermeyer Ulrich 
Published: August 2018

The effect of chloroquine in combination with bright light on the ultrastructure of crayfish (Orconectes limosus R.) photoreceptors was investigated in vivo. Chloroquine had several effects upon the crayfish retina. Multivesicular bodies (MVB) that are involved in lysosomal degradation of photosensory membrane were altered in ultrastructure. MVB frequently contained smaller MVB in a state of more advanced membrane degradation. Additionally screening pigment-like granules appeared in MVB. MVB accumulated in and filled the retinular cell cytoplasm just proximal or distal to the basement membrane which indicated inhibition of photosensory membrane degradation. Under chloroquine treatment rhabdom degradation appeared to be inhibited, as rhabdom diameter was less reduced under these conditions.
Also chloroquine caused accumulation of screening pigment granules in glial cells within the lamina ganglionaris.
Labeling and Isolation of Hemes from Scenedesmus
Authors: Drechsler-Thielmann Beate , Dörnemann Dieter , Senger Horst 
Published: August 2018

Abstract
Protoheme and small quantities of heme a were isolated and purified from the wild type and the developmental mutant, C-2 A′, of Scenedesmus obliquus. In fast growing synchronized WT cells and greening cells of the mutant protoheme could be labeled with [1- 14C]glutamate and [2-14C]glycine. The labeling of heme a was ambiguous and of minor quantity. During rapid chlorophyll biosynthesis the turnover of protoheme was determined by a pulse-chase experiment to have a half-life of 2 h. At the current stage of investigations the question, whether [2-14C]glycine is incorporated into protoheme via the Shemin pathway or via photorespiration or refixation of 14CO2 during general metabolism remains open.
Cereal Grain Alk(en)ylresorcinols Protect Lipids against Ferrous Ions-Induced Peroxidation
Authors: Struski Dariusz G . J. , Kozubek Arkadiusz 
Published: August 2018

Abstract
Resorcinolic lipids, significant constituents of cereal grains are long chain (C 13 -C 27) derivatives of 1,3-dihydroxy-5-alk(en)ylbenzene. It was shown that due to their phenolic nature resorcinolic lipids are effective in protection against fatty acids peroxidation. The phospholipid bilayers appeared to be also protected in the presence of these compounds. The maximal inhibition of peroxidation was 50-90% with IE50 values in the range of 0.8 5-3.6 mol% of resorcinolic lipids.
Embryotoxische Wechselwirkungen zwischen einem Hydrolysenprodukt des Thalidomids und dem Tensid Tween 20 bei der Maus / Embryotoxic Interactions between a Hydrolysis Product of Thalidomide and the Surfactant Tween 20 in Mice
Authors: Kocher-Becker Ursula , Kocher Walter , Ockenfels Heinrich 
Published: August 2018

Abstract
N,N-phtaloyl-ʟ-glumatic acid (NPLG), a hydrolysis product of thalidomide, and the surfactant Tween 20 were co-administred intraperitoneally to pregnant NMRI mice on days 9a and 8⅔ p.c. at doses where the hydrolysis product as well as the surfactant alone induce minimal embryotoxicity. The combined substances (350 mg/kg NPLG + 1.0 ml/kg Tween 20) caused a potentiative teratogenic and an additive embryolethal response. Enhancement of the amount of Tween 20 in the combinations to 2.5 ml/kg led to the same potentiative teratogenic and, in addition, potentiative embryolethal response. Distribution studies using 14C-NPLG showed a strongly increased NPLG content in the maternal plasma under the influence of 2.5 ml/kg Tween 20 but not after co-administration with 1.0 ml/kg Tween 20.
The malformations obtained were of the same type in all groups and mostly located in the vertebrae and ribs. These axial and paraxial defects were frequently more severe and included more affected elements after application of the combined than of the single substances. Extension of our experiments with the combined substances to treatment days 8½ and 9½ p.c. revealed that the first affected segment shifts in caudal direction depending on an increasing embryonal age at treatment. Limb malformations occurred at a low frequency; most of them were of the same type as described in cases of human thalidomide embryopathy.