• YAKHAK HOEJI
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• v.39 no.5
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• pp.565-568
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• 1995

A new antiplatelett agent, aspalatone ([3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) was demonstrated to inhibit MDA generation from arachidonic acid catalyzed by partially purified bovine seminal vesicle cyclooxygenase. This inhibition was also observed with acetylsalicylic acid. The results suggest that the mechanism for the antiplatelet effect of aspalatone is, like acetylsalicylic acid, due to its inhibition of cyclooxygenase.

• The Korean Journal of Pharmacology
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• v.5 no.1
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• pp.57-64
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• 1969

Acetylsalicylic acid, administered intravenously in a dose of 120 mg+250 mg/h, markedly decreased the urinary excretion of sodium and chloride, and slightly depressed potassium excretion, so that the ratio of urinary concentrations of potassium to sodium increased after ASA. Osmolar and free water clearances also diminished during water diuresis, and free water reabsorption $(T^cH_2O)$ decreased after ASA during mannitol diuresis. Glomerular filtration rate and urine flow rate changed little. When infused directly into a renal artery, ASA exhibited identical action on both kidneys, indicating that the renotropic action is mediated by some endogenous humoral agents or by some metabolites of ASA. A dose of 100 mg i.v. of spironolactone, a aldosterone antagonist, slightly reversed the renal reflect when given during maximum action of ASA. Ethacrynic acid could display its full diuretic action unhindered during maximum ASA action. Above observations lead to the suggestion that acetylsalicylic acid might release aldosterone and the action on electrolyte excretion may be mediated by the mineralocorticoid.

• YAKHAK HOEJI
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• v.13 no.2_3
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• pp.80-83
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• 1969

Acetylsalicylic acid gives a water-insoluble violet complex with $<\alpha>$-Picolin-Cu(II) reagent. The Complex is extractable well with a mixture of $<\alpha>$-Picolin-tetrachloromethane solution. The Complex salt dissolved in the mixed solution shows a maximum absorption at 620 m$<\mu>$. It has a melting point at $171^{\circ}C-$173^{\circ}C and molar ratio of Acetylsalicylic acid: Cu(II): $<\alpha>$-Picolin was estimated as 2:1:2 by continuous variation method and chelate titration method.

• Biomolecules & Therapeutics
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• v.4 no.2
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• pp.122-126
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• 1996

In vitro inhibitory effect of aspalatone ((3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) on collagen-, ADP-, and epinephrine-induced platelet aggregation in human platelet rich plasma (PRP) was compared with the effects of reference drugs (acetylsalicylic acid, cilostazol and ticlopidine). Aspalatone inhibited time and dose dependently human platelet aggregation induced by collagen; relative potency was in the order of cilostazol>acetylsalicylic acid>aspalatone>ticlopidine. Aspalatone, like acetylsalicylic acid, potently inhibited only the secondary phase of ADP-and epinephrine-induced aggregation. Thromboxane $B^2$ production evoked by collagen in human PRP was inhibited significantly and concentration-dependently by aspalatone and acetylsalicylic acid. These results were in agreement with the earlier studies in which the antiplatelet action of aspalatone was indicated to be due to the inhibition of platelet cyclooxygenase activity (Han et al., Arzneim. Forsch./Drug Res. 44(II), 1122, 1994; Suh and Han, Yakhak Hoeji 39, 565, 1995). In addition, the inhibitory activity of aspalatone on the platelet aggregation appears to be inversely related to the rate of nonspecific deacetylation of the drug in plasma.

• YAKHAK HOEJI
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• v.25 no.1
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• pp.9-14
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• 1981

Anti-infammatory, analgesic and ulcerogenic activities of fentiazac were investigated in comparison with those of acetylsalicylic acid, fenbufen, naproxen and phenylbutazone. On the anti-inflammatory activity in carrageenin-induced rat paw edema and the analgesic activity on writhing syndrome induced with acetic acid in mice, fentiazac displayed more potent effect than acetylsalicylic acid, fenbufen and pbenylbutazone. But the ulcerogenic action of fentiazac on gastrointestinal tract in fasting rats was less than that of reference drugs. From these investigation, fentiazac seemed to indicate a poor correlation between the extent of anti-inflammatory activity and ulcerogenic action.

• Korean Journal Plant Pathology
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• v.14 no.5
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• pp.386-392
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• 1998

Reproduction of the soybean cyst nematode (SCN), Heterodera glycines Ichinohe on the susceptible soybean cultivar, Lee 74, was significantly reduced by pre-, post- and simultaneous treatments of acetylsalicylic acid (ASA, aspirin). The control efficiencies were 60%, 64% and 87% for pre-, post- and simultaneous treatments, respectively. ASA had no significant effect on the survival of 2nd stage juveniles and their penetration into the soybean root tissues, but significantly inhibited the early stage nematode growth in the roots. Syncytia were formed 2∼3 days after inoculation in the susceptible soybean without ASA treatment, characterized by dense cytoplasm and increased cellular organelles such as mitochondria and endoplasmic reticulum. The nematode stylet was penetrated into the syncytial cell, and feeding tube was formed at the nematode stylet was penetrated into the syncytial cell, and feeding tube was formed at the nematode stylet entry. However, in the ASA treatments, syncytium was not formed or degenerated, depending on the root tissues. In the pre-treatments of ASA, nematode stylets did not penetrate into cells, showing callose-like cell wall thickening formed at the nematode probing sites, or retracted from the infected cells. The stylet penetration sites of syncytial cells appeared to be sealed off with fibrillar materials. With post-treatment of ASA, syncytia formed by the nematode were degenerated, characterized by degradation of syncytial cytoplasm.

• Journal of Radiation Industry
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• v.5 no.3
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• pp.253-258
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• 2011

Acetylsalicylic acid (ASA) has been issued recently in contaminated water environments because of potential impacts on ecosystem and public health. This study was aimed at investigating the possibility of ASA degradation using gamma ray irradiation. In addition, the use of sodium persulfate, hydrogen peroxide, ferrous sulfate were tested in order to examine a synergistic effect with gamma ray. The absorbed dose was ranged from 0.2 to 10 kGy and the concentration of oxidants were from 0.1 to 10 mM in this study. The concentration of ASA was gradually decreased corresponding to the increase of the absorbed dose. When soudium persulfate was simultaneously applied, most of the parent compound was completely degraded even at a low dose of 0.8 kGy. The removal efficiency of total organic carbon was 90% even at the highest dose of 10 kGy without sodium persulfate. However, the efficiency was dramatically enhanced up to 98% at the same dose by adding 10 mM of oxidants. It was suggested that hydroxyl radical ($OH{\cdot}$) and sulfate radical ($SO{_4}^-{\cdot}$) were formed in the system and made roles in degrading ASA at the same time.

• Archives of Pharmacal Research
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• v.18 no.2
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• pp.69-74
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• 1995

In order to improve physico-chemical properties and to enhance stability of drugs, amino acid salt has been widely adoptd in pharmaceutical synthesis. Acetylsalicylic acid lysinate is one of the widely used analgesics and it is a good example of t5his synthesis. In the case of bacetylsalicylic acid lysinate synthesis, racemization of natrually occurred lysine is esential because the racemic lysine salt of the drug shows better yield, crystallinity and dryness than that of the L-lysine salt. To esatablish a simple, practical and economical process for L-lysine racemization, L-lysine treatments with phosphoric acid and with acetic acid were compared and the optimum conditions for its process and derivatization were investigated by chiral separation methods using GC_MS spectroscopy.

• Biomolecules & Therapeutics
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• v.13 no.4
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• pp.246-250
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• 2005

In this study, we tried to investigate whether diclofenac, acetaminophen, nimesulide, acetylsalicylic acid and tumor necrosis factor-alpha (TNF-alpha) significantly affect mucin release from cultured airway goblet cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hr and chased for 30 min or 24 hr in the presence of each agent to assess the effects on $^3H$-mucin release. The results were as follows: (1) TNF-alpha significantly increased mucin release from cultured HTSE cells during 24 hr of treatment period; (2) However, diclofenac, acetaminophen, nimesulide and acetylsalicylic acid did not affect mucin release, during 30 min of treatment period. Basically, this finding suggests that non-steroidal antiinflammatory drugs (NSAIDs) might not function as a mucoregulator in various inflammatory respiratory diseases showing mucus hypersecretion, although further studies are needed.

• Journal of Pharmaceutical Investigation
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• v.25 no.4
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• pp.365-369
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• 1995

The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of $IC_{50}$ values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The $IC_{50}$ of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.