In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-administered with Western drugs as a part of integrative medicine practice. Carboxylesterase 1 (CES1) plays a pivotal role in the metabolisms of pro-drugs. Since (S)-2-(2-(6-dimethylamino)-benzothiazole)-4,5-dihydro-thiazole-4-carboxylate (NLMe) has recently been identified by us as a selective CES1 bioluminescent sensor, we developed a rapid method using this substrate for the direct measurement of CES1 activity in rats. This bioluminescence assay was applied to determine CES1 activity in rat tissues after a two-week oral administration of each of the four herbs noted above. The results demonstrated the presence of CES1 enzyme in rat blood and all tested tissues with much higher enzyme activity in the blood, liver, kidney and heart than that in the small intestine, spleen, lung, pancreas, brain and stomach. In addition, the four herbs showed tissue-specific effects on rat CES1 expression. Based on the CES1 biodistribution and its changes after treatment in rats, the possibility that Danshen, Gegen and Danggui might alter CES1 activities in human blood and kidney should be considered. In summary, a selective and sensitive bioluminescence assay was developed to rapidly evaluate CES1 activity and the effects of orally administered TCMs in rats.

在中药中，丹参、葛根、当归、川芎等被广泛用于预防和治疗心血管疾病，也作为中西医结合实践的一部分，通常与西药联合给药。羧酸酯酶 1 (CES1) 在前药代谢中发挥着关键作用。由于 ( S )-2-(2-(6-二甲基氨基)-苯并噻唑)-4,5-二氢-噻唑-4-羧酸酯 (NLMe) 最近被我们确定为选择性 CES1 生物发光传感器，我们开发了一种快速使用该底物直接测量大鼠 CES1 活性的方法。该生物发光测定法用于测定大鼠组织中口服上述四种草药两周后的 CES1 活性。结果表明，大鼠血液和所有测试组织中均存在CES1酶，其中血液、肝脏、肾脏和心脏中的酶活性远高于小肠、脾脏、肺、胰腺、脑和胃中的酶活性。此外，四种草药对大鼠 CES1 表达表现出组织特异性作用。根据CES1在大鼠体内的生物分布及其治疗后的变化，应考虑丹参、葛根和当归可能改变人体血液和肾脏中CES1活性的可能性。总之，开发了一种选择性且灵敏的生物发光测定法来快速评估 CES1 活性和口服中药对大鼠的影响。