Initial Studies of a Potent Antiheparin Agent (Ubiquin®)

1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura
Keyword(s):  
Side Effects ◽  
Acute Toxicity ◽  
Propylene Oxide ◽  
Toluidine Blue ◽  
Water Soluble ◽  
Per Se

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.

CLINICAL INVESTIGATIONS OF A LONG-ACTING OESTRIOL (POLYOESTRIOL PHOSPHATE)

1961 ◽  
Vol 38 (1) ◽  
pp. 73-87 ◽  
Author(s):  
Christian Lauritzen ◽  
Semih Velibese
Keyword(s):  
Side Effects ◽  
Phosphoric Acid ◽  
Quantitative Data ◽  
Water Soluble ◽  
Cholesterol Concentration ◽  
Experimental Investigations ◽  
Clinical Investigations ◽  
Prolonged Duration ◽  
High Doses ◽  
Long Acting

ABSTRACT A description is given of experimental investigations and preliminary clinical experience with the long-acting oestriol compound polyoestriol phosphate – a water-soluble polymere of oestriol and phosphoric acid. The compound seems to exert all the physiologically important effects of oestriol. Even with high doses the hormone causes no proliferation of the endometrium and no withdrawal bleeding. It has no untoward effect on metabolism. It decreases slightly the cholesterol concentration (to the extent of ⅓–⅕ of the effect produced by long-acting oestradiol esters). The compound has a wide therapeutic range. No side-effects have been observed. Doses of 10 mg or more have a prolonged duration. Additional prolongation of the effect is largely dependent on dosage. To ensure an effect lasting for 4 weeks 40 mg polyoestriol phosphate (corresponding with 30 mg oestriol) is required – an amount which roughly corresponds with physiological quantitative data. The compound, which involves an interesting new principle of prolongation, was most effectively used in the treatment of menopausal symptoms and genital organic disorders. For these indications it can be recommended without reservation.

Effects Attributed to Maleic Hydrazide when used for Chemical Sucker Control on Bright Tobacco

1980 ◽  
Vol 10 (2) ◽  
Author(s):  
Heinz Seltmann
Keyword(s):  
Statistical Difference ◽  
Reducing Sugars ◽  
Maleic Hydrazide ◽  
Water Soluble ◽  
Total Volatile ◽  
Total Alkaloids ◽  
Group I ◽  
Excellent Control ◽  
Per Se ◽  
Group Ii

AbstractThe effect of maleic hydrazide (MH) per se on bright tobacco was determined by comparing plants treated with MH to those without MH under conditions of good chemical sucker control. Sequential applications of each of five contact-type agents with MH one week later (Group I) were compared to dual applications of each of the same contact agents (Group II). In Group II suckers missed during applications were individually wetted to ensure excellent control. Sucker control was measured as 95 % for Group I and assumed to be 99 % for Group II. There were no agronomic differences between Groups I and II. In the visual warehouse appraisal, there was only a statistical difference for thin-bodied tobaccos between the two groups and a trend for slightly more heavy-bodied tobaccos in Group I. The chemical and physical analyses showed that filling value at 13 % moisture and equilibrium moisture content (EMC) measured at 60 % relative humidity were significantly lower in Group I than Group II. The result for EMC was questioned. Actual values for total alkaloids, total volatile bases minus nicotine, total ash, and alkalinity number of water-soluble ash were lower and reducing sugars were higher where MH was used. Except for EMC, the findings in this study reflected those established in studies where MH-treated and normally hand-suckered tobaccos were compared, but the differences here were generally not as great.

Chemosensitizing Activity of Histone Deacetylases Inhibitory Cyclic Hydroxamic Acids for Combination Chemotherapy of Lymphatic Leukemia

2018 ◽  
Vol 18 (4) ◽  
pp. 365-371 ◽  
Author(s):  
Denis V. Mishchenko ◽  
Margarita E. Neganova ◽  
Elena N. Klimanova ◽  
Tatyana E. Sashenkova ◽  
Sergey G. Klochkov ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Acute Toxicity ◽  
Histone Deacetylases ◽  
Hydroxamic Acids ◽  
Water Soluble ◽  
Male Rat ◽  
Hybrid Male ◽  
Cyclic Hydroxamic Acids

Background: Anti-tumor effect of hydroxamic acid derivatives is largely connected with its properties as efficient inhibitors of histone deacetylases, and other metalloenzymes involved in carcinogenesis. Objective: The work was aimed to (i) determine the anti-tumor and chemosensitizing activity of the novel racemic spirocyclic hydroxamic acids using experimental drug sensitive leukemia P388 of mice, and (ii) determine the structure-activity relationships as metal chelating and HDAC inhibitory agents. Method: Outbreed male rat of 200-220 g weights were used in biochemical experiments. In vivo experiments were performed using the BDF1 hybrid male mice of 22-24 g weight. Lipid peroxidation, Fe (II) -chelating activity, HDAC fluorescent activity, anti-tumor and anti-metastatic activity, acute toxicity techniques were used in this study. Results: Chemosensitizing properties of water soluble cyclic hydroxamic acids (CHA) are evaluated using in vitro activities and in vivo methods and found significant results. These compounds possess iron (II) chelating properties, and slightly inhibit lipid peroxidation. CHA prepared from triacetonamine (1a-e) are more effective Fe (II) ions cheaters, as compared to CHA prepared from 1- methylpiperidone (2a-e). The histone deacetylase (HDAC) inhibitory activity, lipophilicity and acute toxicity were influenced by the length amino acids (size) (Glycine < Alanine < Valine < Leucine < Phenylalanine). All compounds bearing spiro-N-methylpiperidine ring (2a-e) are non-toxic up to 1250 mg/kg dose, while compounds bearing spiro-tetramethylpiperidine ring (1a-e) exhibit moderate toxicity which increases with increasing lipophility, but not excite at 400 mg/kg. Conclusion: It was shown that the use of combination of non-toxic doses of cisplatin (cPt) or cyclophosphamide with CHA in most cases result in the appearance of a considerable anti-tumor effect of cytostatics. The highest chemosensitizing activity with respect to leukemia Р388 is demonstrated by the CHA derivatives of Valine 1c or 2c.

Potential anticonvulsants: Substituted N-benzylidene derivatives of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins

1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Acute Toxicity ◽  
Water Soluble ◽  
Hypotensive Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Soluble Salts ◽  
Sleeping Time ◽  
Central Depression ◽  
Derivatives Of ◽  
Electroshock Seizures

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.

scholarly journals Enzymatic identification of the load-bearing boundary lubricant in the joint.

Rheumatology ◽  
1998 ◽  
Vol 37 (2) ◽  
pp. 137-142 ◽  
Author(s):  
B A Hills ◽  
M K Monds
Keyword(s):  
Water Soluble ◽  
Surprising Result ◽  
Lubrication System ◽  
Load Bearing ◽  
Bovine Articular Cartilage ◽  
Boundary Lubricant ◽  
Surface Active ◽  
Per Se ◽  
Dose Dependent ◽  
Wear Tests

Abstract Bovine articular cartilage and synovial fluid (SF) were co-incubated with one of three enzymes selected to destroy each of the three major contenders for the active ingredient imparting such remarkable load-bearing lubrication to the normal joint. Destroying hyaluronic acid (HA), alias hyaluronan, with hyaluronidase, both frictional and wear tests displayed no significant change in accordance with most previous studies of SF alone. Destroying surface-active phospholipid (SAPL) with phospholipase A2, there was a highly significant dose-dependent compromise of lubrication as recorded on both tests. Trypsin produced a somewhat surprising result in that lubrication of the cartilage actually improved. This result can be interpreted as indicating that lubricin is not the lubricant per se, but, as a water-soluble, macromolecular, proteinaceous carrier for phospholipid, its destruction caused more SAPL to be deposited as the true load-bearing lubricant. These results are discussed in the context that SAPL, lubricin and HA each have specific roles in a comprehensive lubrication system.

Highly Effective, Water-Soluble, Hemocompatible 1,3-Propylene Oxide-Based Antimicrobials: Poly[(3,3-quaternary/PEG)-copolyoxetanes]

2011 ◽  
Vol 12 (3) ◽  
pp. 757-769 ◽  
Author(s):  
Souvik Chakrabarty ◽  
Allison King ◽  
Pinar Kurt ◽  
Wei Zhang ◽  
Dennis E. Ohman ◽  
...  
Keyword(s):  
Propylene Oxide ◽  
Water Soluble ◽  
Highly Effective ◽  
Effective Water

scholarly journals A novel zinc complex with antibacterial and antioxidant activity

BMC Chemistry ◽  
2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Yun Zhang ◽  
Xiaojing Li ◽  
Jia Li ◽  
Md. Zaved Hossain Khan ◽  
Fanyi Ma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Acute Toxicity ◽  
Intestinal Absorption ◽  
Antioxidant Activities ◽  
Zinc Ion ◽  
Water Soluble ◽  
Zinc Supplement ◽  
Citrate Complex ◽  
Morphology Characterization

Abstract Background In order to enhance the antibacterial activity and reduce the toxicity of Zn2+, novel complexes of Zn(II) were synthesized. Results A water-soluble zinc-glucose-citrate complex (ZnGC) with antibacterial activity was synthesized at pH 6.5. The structure, morphology, characterization, acute toxicity, antibacterial and antioxidant activities, and in situ intestinal absorption were investigated. The results showed that zinc ion was linked with citrate by coordinate bond while the glucose was linked with it through intermolecular hydrogen bonding. The higher the molecular weight of sugar is, the more favorable it is to inhibit the formation of zinc citrate precipitation. Compared with ZnCl2, ZnGC complex presented better antibacterial activity against Staphylococcus aureus (S. aureus, Gram-positive) and Escherichia coli (E. coli, Gram-negative). Conclusions The results of acute toxicity showed no obvious toxicity in this test and in situ intestinal absorption study, suggesting that ZnGC complex could be used as a potential zinc supplement for zinc deficiency.

Endodontic Materials: Reactor Response

1988 ◽  
Vol 2 (1) ◽  
pp. 25-28 ◽  
Author(s):  
I.A. Mjör
Keyword(s):  
Side Effects ◽  
Review Paper ◽  
Defense Mechanism ◽  
The Body ◽  
Endodontic Treatment ◽  
Bridge Formation ◽  
Per Se ◽  
Apical Area

This discussion of a review paper on endodontic materials focuses on the need for standardization of this group of materials, including clinical and biological investigations. It was concluded that the search for endodontic materials that are both adhesive to dentin and insoluble must continue. When such materials become available, the defense mechanism of the body would take care of the healing per se. This approach as well as techniques and materials which induce dentin bridge formation in the apical area were considered feasible for improving endodontic treatment. The need to report side-effects of endodontic materials was stressed, and it was suggested that such reports should be mandatory for clinicians and for manufacturers of endodontic materials.

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