Abstract | BACKGROUND: The hyperfunction and activation of platelets have been strongly implicated in the development and recurrence of arterial occlusive disease, and various antiplatelet drugs are used to treat and prevent such diseases. New antiplatelet drugs and many other drugs have been developed, but some drugs may have adverse effects on platelet functions. OBJECTIVE: The aim of this study was to establish an evaluation method for evaluating the effect and adverse effect of various drugs on platelet functions. MATERIALS AND METHODS: Human erythroid leukemia (HEL) cells were used after megakaryocytic differentiation with phorbol 12-myristate 13-acetate as an alternative to platelets. Drugs were evaluated by changes in intracellular Ca2+ concentration ([Ca2+]i) mobilization in Fura2-loaded phorbol 12-myristate 13-acetate-induced HEL cells. Aspirin and cilostazol were selected as antiplatelet drugs and ibuprofen and sodium valproate as other drugs. RESULTS: CONCLUSION: It is possible to induce HEL cells to differentiate into megakaryocytes, which are a useful model for the study of platelet functions, and the quantification of the inhibition of thrombin-induced increases in [Ca2+]i is applicable to the evaluation of the effects of various drugs on platelets.
|
Authors | Tomoki Tada, Kensaku Aki, Wataru Oboshi, Kazuyoshi Kawazoe, Toshiyuki Yasui, Eiji Hosoi |
Journal | Drug design, development and therapy
(Drug Des Devel Ther)
Vol. 10
Pg. 3099-3107
( 2016)
ISSN: 1177-8881 [Electronic] New Zealand |
PMID | 27713620
(Publication Type: Journal Article)
|
Chemical References |
- Phorbol Esters
- Platelet Aggregation Inhibitors
- Tetrazoles
- phorbol-12-myristate
- Cilostazol
- Tetradecanoylphorbol Acetate
- Aspirin
|
Topics |
- Aspirin
(pharmacology)
- Blood Platelets
(drug effects)
- Cilostazol
- Humans
- Megakaryocytes
(drug effects)
- Phorbol Esters
(pharmacology)
- Platelet Activation
(drug effects)
- Platelet Aggregation
(drug effects)
- Platelet Aggregation Inhibitors
(pharmacology)
- Platelet Function Tests
- Tetradecanoylphorbol Acetate
(pharmacology)
- Tetrazoles
(pharmacology)
|