| API_（0134）对钙调素及其依赖性环核苷酸磷酸二酯酶的作用 |
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| 引用本文： | 聂磊,傅良武,张婷,赵华月,周世豪,马宝瑕,熊一力.API_（0134）对钙调素及其依赖性环核苷酸磷酸二酯酶的作用[J].中国药理学通报,1994(5). |
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| 作者姓名： | 聂磊 傅良武 张婷 赵华月 周世豪 马宝瑕 熊一力 |
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| 作者单位： | 中山医科大学生化教研室，同济医科大学同济医院内科 |
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| 摘 要： | 应用钙调素（ＣａＭ）靶酶环核苷酸磷酸二酯酶（ＰＤＥ－Ｉ）活性测定方法观察穿心莲有效成分（ＡＰＩ０１３４）拮抗ＣａＭ的作用。当ＡＰＩ０１３４浓度大于７．８ｍｇ·Ｌ－１时能明显抑制ＣａＭ激活ＰＤＥ－Ｉ的活性，其半抑制浓度（ＩＣ５０）为２６·９ｍｇ·Ｌ－１，在浓度为７．８～１２５ｍｇ·Ｌ－１范围内，ＡＰＩ０１３４对ＰＤＥ－Ｉ的基础活性没有影响。
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| 关 键 词： | 穿心莲有效成分，API_（0134），钙调素钙调素拮抗剂，环核苷酸磷酸二酯酶 |
The effects of API_(0134) extracted from andrographis paniculata on the activities of calmodulin/calmodulin dependent cyclic nucleotide phosphodiesterase |
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| NIE Lei,FU Liang-Wu, ZHANG Ting et al.The effects of API_(0134) extracted from andrographis paniculata on the activities of calmodulin/calmodulin dependent cyclic nucleotide phosphodiesterase[J].Chinese Pharmacological Bulletin,1994(5). |
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| Authors: | NIE Lei FU Liang-Wu ZHANG Ting |
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| Abstract: | Using the assay of Ca2+/calmodulin (CaM)-dependent cyclic uncleotide phosphodiesterase (PDE), We observed the antagonistic effect of API0134 extracted from Andrographis Paniculata on CaM. The activity of PDE-I stimulated by CaM was apparently inhibited by API0134 at a concentration of more than 7.8 mg·L-1and the IC50 was 26·9 mg·L-1. The basal activity of PDE-I was not effected by API0134 in concentration range of 7.8～125 mg·L-1. The results suggest that API0134 may be a specific antagonist of CaM. This experiment gives us a new clue to study the mechanism of antiplatelet drugs and chinese medicinal herbs. |
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| Keywords: | andrographis Paniculata API_(0134) calmodulin cyclic nucleotide phosphodiesterase calmodulin antagonist |
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