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Effects of DK-002, a synthesized (6aS,cis)-9,10-Dimethoxy-7,11b-dihydro- indeno[2,1-c]chromene-3,6a-diol, on platelet activity
- Title
- Effects of DK-002, a synthesized (6aS,cis)-9,10-Dimethoxy-7,11b-dihydro- indeno[2,1-c]chromene-3,6a-diol, on platelet activity
- Authors
- Lee K.-S.; Khil L.-Y.; Chae S.-H.; Kim D.; Lee B.-H.; Hwang G.-S.; Moon C.-H.; Chang T.-S.; Moon C.-K.
- Ewha Authors
- 창동신
- SCOPUS Author ID
- 창동신
- Issue Date
- 2006
- Journal Title
- Life Sciences
- ISSN
- 0024-3205
- Citation
- Life Sciences vol. 78, no. 10, pp. 1091 - 1097
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- In the present study, the mechanism of antiplatelet activity of DK-002, a synthesized (6aS,cis)-9,10-Dimethoxy-7,11b-dihydro-indeno[2,1-c]chromene-3,6a- diol, was investigated. DK-002 inhibited the thrombin, collagen, and ADP-induced rat platelet aggregation in a concentration-dependent manner, with IC 50 values of 120, 27, and 47 μM, respectively. DK-002 also inhibited thrombin-induced dense granule secretion, thromboxane A2 synthesis, and [Ca2+]i elevation in platelets. DK-002 did not show any significant effect on ADP-induced inhibition of cyclic AMP elevation by prostaglandin E1, but DK-002 was confirmed to inhibit ADP-induced [Ca2+]i elevation and shape change. DK-002 inhibited 4-bromo-A23187-induced [Ca2+]i elevation in the presence of creatine phosphate/creatine phosphokinase (CP/CPK, a ADP scavenging system) and indomethacin (a specific inhibitor of cyclooxygenase). DK-002 also inhibited Ca2+ mobilization in thrombin- or 4-bromo-A23187-stimulated platelets through its inhibitory effects on both Ca2+ release from intracellular stores and Ca2+ influx, in the presence of CP/CPK and indomethacin. Taken together, the present study shows that DK-002 has inhibitory effects on stimulation of platelets, and suggests that its antiplatelet activity might be related to the inhibitory mechanism on Ca2+ mobilization in stimulated platelets. © 2005 Elsevier Inc. All rights reserved.
- DOI
- 10.1016/j.lfs.2005.06.017
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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