Although aspalatone (acetylsalicylic acid maltol ester) is recognized as an antithrombotic agent with antioxidative and antiplatelet potential; its efficacy in preventing endothelial dysfunction is not known. In this study, we examined the antiangiogenic, antioxidative, and anti‐inflammatory effect of aspalatone in human aortic endothelial cells (HAECs). Specifically, the effect of aspalatone on VEGF‐induced HAECs growth, migration, tube formation, and levels of lipid peroxidation‐derived malondialdehyde (MDA) was examined. Our results indicate that the treatment of HAECs with aspalatone decreased VEGF‐induced cell migration, tube formation, and levels of MDA. Aspalatone also inhibited VEGF‐induced decrease in the expression of eNOS and increase in the expression of iNOS, ICAM‐1, and VCAM‐1. Aspalatone also prevented the VEGF‐induced adhesion of monocytes to endothelial cells. Furthermore, aspalatone also prevented VEGF‐induced release of inflammatory markers such as Angiopoietin‐2, Leptin, EGF, G‐CSF, HB‐EGF, and HGF in HAECs. Thus, our results suggest that aspalatone could be used to prevent endothelial dysfunction, an important process in the pathophysiology of cardiovascular diseases.

01 Dec 2001·Archives of Pharmacal ResearchQ3 · MEDICINE

Effect of vehicles and enhancers on thein vitro skin penetration of aspalatone and its enzymatic degradation across rat skins

Q3 · MEDICINE

Article

Author: Hye Sun Gwak ; In Koo Chun

The feasibility of skin penetration was studied for aspalatone (AM, acetylsalicylic acid maltol ester), a novel antithrombotic agent. In this study, hairless mouse dorsal skins were used as a model to select composition of vehicle and AM. Based on measurements of solubility and partition coefficient, the concentration of PG that showed the highest flux for AM across the hairless mouse skin was found to be 40%. The cumulative amount permeated at 48 h, however, appear inadequate, even when the PG concentration was employed. To identify a suitable absorption enhancer and its optimal concentration for AM, a number of absorption enhancers and a variety of concentration were screened for the increase in transdermal flux of AM. Amongst these, linoleic acid (LOA) at the concentration of 5% was found to have the largest enhancement factor (i.e., 132). However, a further increase in AM flux was not found in the fatty acid concentration greater than 5%, indicating the enhancement effect is in a bell-shaped curve. In a study of the effect of AM concentration on the permeation, there was no difference in the permeation rate between 0.5 and 1% for AM, below its saturated concentration. At the donor concentration of 2%, over the saturated condition, the flux of AM was markedly increased. A considerable degradation of AM was found during permeation studies, and the extent was correlated with protein concentrations in the epidermal and serosal extracts, and skin homogenates. In rat dorsal skins, the protein concentration decreased in the rank order of skin homogenate > serosal extract > epidermal extract. Estimated first order degradation rate constants were 6.1 5 +/- 0.14, 0.57 +/- 0.02 and 0.011 +/- 0.004 h(-1) for skin homogenate, serosal extract and epidermal extract, respectively. Therefore, it appeared that AM was hydrolyzed to some extent into salicylmaltol by esterases in the dermal and subcutaneous tissues of skin. Taken together, our data indicated that transdermal delivery of AM is feasible when the combination of PG and LOA is used as a vehicle. However, since AM is not metabolically stable, acceptable degradation inhibitors may be necessary to fully realize the transdermal delivery of the drug.

01 Nov 1997·Life SciencesQ3 · MEDICINE

Aspalatone, a new antiplatelet agent, attenuates the neurotoxicity induced by kainic acid in the rat

Q3 · MEDICINE

Article

Author: Kim, Chin ; Lee, Dong-Wook ; Koo, Chang-Hui ; Jhoo, Wang-Kee ; Kim, Hyoung-Chun ; Choi, Dong-Young

The antioxidant efficacy of aspalatone (APT; acetyl salicylic acid maltol ester), a new antiplatelet agent, has been characterized in vivo as well as in vitro, and several observations indicated that the antioxidant could prevent the neuroexcitation caused by oxidative stress. In this report, the effect of APT was evaluated on kainic acid (KA)-induced neurotoxicity, since the neurotoxicity induced by KA is, at least in part, mediated via the formation of free radicals. The results showed that pretreatments with APT or maltol (MAL) significantly attenuated seizure activity, oxidative stress (lipid peroxidation and protein oxidation) and the loss of hippocampal neurons induced by KA. On the other hand, the pretreatments with aspirin (ASP), ASP together with MAL or vitamin E failed to protect against the toxicity produced by KA suggesting that the mechanism of action for APT on the KA-induced neurotoxicity is different from that of ASP. These finding raise the possibility that salicylmaltol, a metabolite of APT, plays a role in preventing the neurotoxicity evoked by KA. Therefore, our results suggest that an APT-related antioxidant mechanism, which is linked to the MAL moiety, is involved in the neuroprotective effect against KA.

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Indication	Highest Phase	Country/Location	Organization	Date
Atherosclerosis	Phase 2	-	Bukwang Pharmaceutical Co., Ltd.	-
Thrombosis	Phase 2	-	Bukwang Pharmaceutical Co., Ltd.	-

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