Abstract
The effect of tenidap [(±)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide], a new anti-inflammatory agent, was investigated on DNA synthesis by means of [3H]thymidine incorporation, collagen synthesis by means of [3H]proline incorporation, cell proliferation, and intracellular pH in nicardipine-reactive human gingival fibroblasts. Tenidap significantly inhibited [3H]thymidine incorporation at concentrations greater than 20 μM on the 4th and 8th day of treatment. Tenidap also significantly inhibited [3H]proline incorporation at a concentration greater than 50 μM on the 4th day and at more than 20 μM on the 8th day of treatment. The presence of 1 μM nifedipine or 1 μM nicardipine did not alter the depressing effect of tenidap. Tenidap (20 μM) also lowered intracellular pH. These results suggest that tenidap might be effective for the prevention of gingival overgrowth caused by calcium channel blockers.
Footnotes
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This work was supported in part by Grants-in-Aid for Scientific Research Fund 09671908, 1997–1998 (A.F.) and 10557173, 1998–1999 (A.F.), and for Encouragement of Young Scientists 07771715, 1995 (H.M.), from the Ministry of Education, Science and Culture, Japan.
- Abbreviations:
- BK
- bradykinin
- [Ca2+]i
- intracellular free Ca2+concentration
- DMEM-10
- Dulbecco's modified Eagle's medium
- FCS
- fetal calf serum
- DPBS
- Dulbecco's phosphate-buffered saline
- pHi
- intracellular pH
- BCECF-AM
- 3′-O-acetyl-2′,7′-bis(carboxyethyl)-4- or 5-carboxyfluorescein, diacetoxymethyl ester
- BCECF
- 2′,7′-Bis(carboxyethyl)-4- or 5-carboxyfluorescein, diacetoxymethyl ester
- Received June 14, 2001.
- Accepted October 19, 2001.
- The American Society for Pharmacology and Experimental Therapeutics
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