2022
DOI: 10.1016/j.apsb.2021.09.013
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Atractylenolide-I covalently binds to CYP11B2, selectively inhibits aldosterone synthesis, and improves hyperaldosteronism

Abstract: Hyperaldosteronism is a common disease that is closely related to endocrine hypertension and other cardiovascular diseases. Cytochrome P450 11B2 (CYP11B2), an important enzyme in aldosterone (ALD) synthesis, is a promising target for the treatment of hyperaldosteronism. However, selective inhibitors targeting CYP11B2 are still lacking due to the high similarity with CYP11B1. In this study, atractylenolide-I (AT-I) was found to significantly reduce the production of ALD but had no effect on cortisol synthesis, … Show more

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Cited by 14 publications
(7 citation statements)
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“…In addition, other studies have used 60 or 120 mg/kg ATL I to ameliorate acetaminophen-induced acute liver injury [33]. Another study used 10 to 40 mg/kg ATL I to inhibit aldosterone synthesis and improve hyperaldosteronism [52]. Taking these together, we believe that the dose of ATL I we used in the present study was safe.…”
Section: Discussionmentioning
confidence: 66%
See 1 more Smart Citation
“…In addition, other studies have used 60 or 120 mg/kg ATL I to ameliorate acetaminophen-induced acute liver injury [33]. Another study used 10 to 40 mg/kg ATL I to inhibit aldosterone synthesis and improve hyperaldosteronism [52]. Taking these together, we believe that the dose of ATL I we used in the present study was safe.…”
Section: Discussionmentioning
confidence: 66%
“…To establish diet-induced obesity models, mice were fed a high-fat diet (D12492, Research Diets, New Brunswick, NJ, USA) for 8 weeks before ATL I (CSN16457, CSNpharm, Shanghai, China) (high dose (h): 4 mg/kg, ATL I medium dose (m): 2 mg/kg, and ATL I low dose (l): 1 mg/kg) treatment for another four weeks. Dimethyl sulfoxide (DMSO) (ST2335, Beyotime, Shanghai, China) was set as vehicle, and saline was set as negative control [52]. All animal care and experimental studies were approved by and in accordance with the guidelines of the Animal Ethics Committee of Guangdong Medical University.…”
Section: Animal Treatmentmentioning
confidence: 99%
“…For example, TCM includes multiple types of antidiarrheal drugs, each exerting different effects on symptoms and the intestinal bacterial community despite all being used to treat diarrhea [ 16 ]. The beneficial efficacies of TCM are summarized in terms of various treatment outcomes, such as qi-tonifying and drying dampness , which have facilitated clinical applications [ 17 , 18 ]. These concise descriptions were closely related to the organic functions of the human body.…”
Section: The Modernization Of Traditional Chinese Medicinementioning
confidence: 99%
“…ATL I and III are hypotensive and useful in the treatment of aldosteronism [ 109 ] and pre-eclampsia. Pre-eclampsia is a common hypertension disease that increases the risk of maternal and fetal morbidity and mortality during pregnancy [ 110 ].…”
Section: Pharmacological Effects Of Atractylenolidesmentioning
confidence: 99%