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Morphology and histochemistry of the thalamus in the course of intoxication by ethyl-mercury-p-toluenesulphanilide (EMTS).

Organic Mercury compounds are known for their neurotoxicity. From our previous studies it appeared that a variable degree of damage is brought about in the individual structures of the CNS by ingestion of organic mercurials. A detailed study was undertaken on the histotopography of pathological changes occurring in the thalamus - the major integrator of various cerebral functions - following intragastric administration of EMTS, a fungicide widely applied in agriculture. Rats served as the experimental animals. They were treated intragastrically with a daily dose of 15 mg of EMTS over a period of 10 days ( the per os DL50 for rats is 100 mg/kg of body weight). The results of our study have revealed that chronic ingestion of large doses of EMTS brings about a considerable inhibition of the activities of AChE, BuTJ, acP and ATPase in many thalamic nuclei with a concomitant elevation of TPPase and NsE activities. There was considerable variation as to the degree of histoenzymatic changes in the individual thalamic nuclei. The accompanying glial reaction was evaluated aw well. An interpretation of the findings made in this study has been undertaken.

Acetylcholinesterase↗

Properties and application of a partially purified alkaline xylanase from an alkalophilic fungus Aspergillus nidulans KK-99.

An alkalophilic Aspergillus nidulans KK-99 produced an alkaline, thermostable xylanase (40 IU/ml) in a basal medium supplemented with wheat bran (2% w/v) and KNO3 (at 0.15% N) pH 10.0 and 37 degrees C. The partially purified xylanase was optimally active at pH 8.0 and 55 degrees C. The xylanase was stable in a broad pH range of 4.0-9.5 for 1 h at 55 degrees C, retaining more than 80% of its activity. The enzyme exhibited greater binding affinity for xylan from hardwood than from softwood. The xylanase activity was stimulated (+25%) by Na+ and Fe2+ and was strongly inhibited (maximum by 70%) by Tween-20, 40, 60, SDS, acetic anhydride, phenylmethane sulphonyl fluoride, Triton-X-100. The xylanase dose of 1.0 IU/g dry weight pulp gave optimum bleach boosting of Kraft pulp at pH 8.0 and temperature 55 degrees C for 3 h reaction time.

Acetic Anhydrides↗

Synthesis of some new steroidal [16alpha,17alpha-d]-isoxazolines.

Regioselective synthesis of novel steroidal anti-inflammatory ante drug analogues, viz., [16alpha,17alpha-d]-isoxazolines 1(a-h) and 2(a-h) prepared in a single step in good yield by the reaction of 16-dehydropregnenolone acetate (16-DPA) 1 or related 21-chloro-20-oxopregnane 2 with various aldoximes (a-h) in presence of chloramine-T in refluxing ethanol.

Anti-Inflammatory Agents↗

The effect of ethylmercury-p-toluenesulphanilide on the neurosecretory hypothalamic-hypophyseal system.

The effect of Ethylmercury-p-toluenesulphanilide on the neurosecretory function of the hypothalamic-hypophyseal system has been studied. The p-toluenesulphanilide of ethylmercury is a pesticide with fungicidal properties. The poison has been administered intragastrically for 10 days at a daily dose of 4 mg. The results of experiments presented herewith have shown that ingestion of EMTSA lead to an accumulation of neurosecretory material in the nerve cells of the supraoptic and paraventricular nuclei as well as in those of the neurohypophysis. In spite of the increased content of neurosecretory substances in the hypothalamic-hypophyseal system, the secretory cells of the supraoptic and paraventricular nuclei did not show any features of enhanced secretory activity. Basing on the observations made in this study an assumption was raised that the intragastric poisoning by EMTSA exerted an inhibitory effect on the release of ADH from the neurosecretory system. Intoxication by EMTSA induced only negligible degenerative changes in neurocytes of the hypothalamic nuclei.

Animals↗

[Synthesis of N-alpha-(tosylglycylprolyl)-4-amidinophenylalanine amides as thrombin inhibitors].

N alpha-(Tosylprolylglycyl)-4-cyanphenylalanine was synthesized by the reaction of an activated ester and a mixed anhydride, respectively, of Tos-Pro-Gly-OH with 4-cyanophenylalanine. N alpha-(Tosylglycylprolyl)-4-cyanophenylalanine was prepared by reaction of Tos-Gly-Cl with N alpha-prolyl-4-cyanophenylalanine. These acids were transferred into the amides. The cyano compounds were converted into the desired amidines via the thioamides and the thioimidic esters.

Amidines↗