Synthesis of gingerdione derivatives as potent antiplatelet agents

Ya Yun Lai; Li Jiau Huang; Hsien Cheng Lin; Tian-Shung Wu; Che Ming Teng; Sheng Chu Kuo

Synthesis of gingerdione derivatives as potent antiplatelet agents

Ya Yun Lai, Li Jiau Huang, Hsien Cheng Lin, Tian-Shung Wu, Che Ming Teng, Sheng Chu Kuo

School of Pharmacy

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

Abstract

In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead compounds. A series of their derivatives were synthesized and screened for antiplatelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, [4]-gingerdione (18) and [5]-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-1 and COX-2 inhibition. The exact mechanism of action of these new compounds should be further investigated.

Original language	English
Pages (from-to)	259-269
Number of pages	11
Journal	Chinese Pharmaceutical Journal
Volume	54
Issue number	4
Publication status	Published - 2002 Aug 1

All Science Journal Classification (ASJC) codes

Pharmacology
Pharmaceutical Science

Cite this

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title = "Synthesis of gingerdione derivatives as potent antiplatelet agents",

abstract = "In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead compounds. A series of their derivatives were synthesized and screened for antiplatelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, [4]-gingerdione (18) and [5]-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-1 and COX-2 inhibition. The exact mechanism of action of these new compounds should be further investigated.",

author = "Lai, {Ya Yun} and Huang, {Li Jiau} and Lin, {Hsien Cheng} and Tian-Shung Wu and Teng, {Che Ming} and Kuo, {Sheng Chu}",

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T1 - Synthesis of gingerdione derivatives as potent antiplatelet agents

AU - Lai, Ya Yun

AU - Huang, Li Jiau

AU - Lin, Hsien Cheng

AU - Wu, Tian-Shung

AU - Teng, Che Ming

AU - Kuo, Sheng Chu

PY - 2002/8/1

Y1 - 2002/8/1

N2 - In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead compounds. A series of their derivatives were synthesized and screened for antiplatelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, [4]-gingerdione (18) and [5]-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-1 and COX-2 inhibition. The exact mechanism of action of these new compounds should be further investigated.

AB - In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead compounds. A series of their derivatives were synthesized and screened for antiplatelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, [4]-gingerdione (18) and [5]-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-1 and COX-2 inhibition. The exact mechanism of action of these new compounds should be further investigated.

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Synthesis of gingerdione derivatives as potent antiplatelet agents

Abstract

All Science Journal Classification (ASJC) codes

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