Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways

Background. Testosterone deficiency is reportedly correlated with an elevation of cholesterol in plasma, but the mechanism remains unclear. Our objective was to investigate the effects of testosterone deficiency on cholesterol metabolism and the corresponding molecular changes in vivo and in vitro....

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Main Authors: Yu Yuefeng, Lin Zhiqi, Chen Yi, Zhu Keyu, Wan Heng, Wang Yuying, Wang Ningjian, Yu Yuetian, Gu Xinjie, Zhang Yihao, Lu Yingli, Xia Fangzhen
Format: Article
Language:English
Published: Wiley 2022-01-01
Series:International Journal of Endocrinology
Online Access:http://dx.doi.org/10.1155/2022/7989751
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author Yu Yuefeng
Lin Zhiqi
Chen Yi
Zhu Keyu
Wan Heng
Wang Yuying
Wang Ningjian
Yu Yuetian
Gu Xinjie
Zhang Yihao
Lu Yingli
Xia Fangzhen
author_facet Yu Yuefeng
Lin Zhiqi
Chen Yi
Zhu Keyu
Wan Heng
Wang Yuying
Wang Ningjian
Yu Yuetian
Gu Xinjie
Zhang Yihao
Lu Yingli
Xia Fangzhen
author_sort Yu Yuefeng
collection DOAJ
description Background. Testosterone deficiency is reportedly correlated with an elevation of cholesterol in plasma, but the mechanism remains unclear. Our objective was to investigate the effects of testosterone deficiency on cholesterol metabolism and the corresponding molecular changes in vivo and in vitro. Methods. SD rats were randomized into three groups: sham-operated (SHAM), subtotal orchiectomized (SO), and orchiectomized (ORX) and fed for 8 weeks. HepG2 cells were cultured with medium containing testosterone with the final concentrations of 0, 10, 30, and 300 nM. Method of isotope tracing and fluorescence labelling was adopted to investigate cholesterol metabolism. Several key molecules of cholesterol metabolism were also analyzed. Results. SO and ORX rats displayed dysfunctional liver uptake of cholesterol. HepG2 cells incubated with testosterone of lower and excessive level exhibited reduced capacity of cholesterol uptake. Further investigation revealed that lack of testosterone induced increased proprotein convertase subtilisin/kexin type 9 (PCSK9) and decreased low-density lipoprotein receptor (LDLR) both in vivo and in vitro. Moreover, the androgen receptor (AR) antagonist flutamide mimicked the effects of testosterone deficiency on PCSK9 and LDLR indicating the role of AR as a mediator in triggering attenuating liver cholesterol uptake in which testosterone instead of dihydrotestosterone (DHT) is the major functional form of androgen. Conclusion. Testosterone deficiency attenuated cholesterol liver uptake mediated by the PCSK9-LDLR pathway, in which AR and testosterone without transforming to DHT play important roles.
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publishDate 2022-01-01
publisher Wiley
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spelling doaj-art-1444cefb3b1f48c2a7db957d64081f4f2025-08-20T02:04:52ZengWileyInternational Journal of Endocrinology1687-83452022-01-01202210.1155/2022/7989751Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR PathwaysYu Yuefeng0Lin Zhiqi1Chen Yi2Zhu Keyu3Wan Heng4Wang Yuying5Wang Ningjian6Yu Yuetian7Gu Xinjie8Zhang Yihao9Lu Yingli10Xia Fangzhen11Institute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismInstitute and Department of Endocrinology and MetabolismBackground. Testosterone deficiency is reportedly correlated with an elevation of cholesterol in plasma, but the mechanism remains unclear. Our objective was to investigate the effects of testosterone deficiency on cholesterol metabolism and the corresponding molecular changes in vivo and in vitro. Methods. SD rats were randomized into three groups: sham-operated (SHAM), subtotal orchiectomized (SO), and orchiectomized (ORX) and fed for 8 weeks. HepG2 cells were cultured with medium containing testosterone with the final concentrations of 0, 10, 30, and 300 nM. Method of isotope tracing and fluorescence labelling was adopted to investigate cholesterol metabolism. Several key molecules of cholesterol metabolism were also analyzed. Results. SO and ORX rats displayed dysfunctional liver uptake of cholesterol. HepG2 cells incubated with testosterone of lower and excessive level exhibited reduced capacity of cholesterol uptake. Further investigation revealed that lack of testosterone induced increased proprotein convertase subtilisin/kexin type 9 (PCSK9) and decreased low-density lipoprotein receptor (LDLR) both in vivo and in vitro. Moreover, the androgen receptor (AR) antagonist flutamide mimicked the effects of testosterone deficiency on PCSK9 and LDLR indicating the role of AR as a mediator in triggering attenuating liver cholesterol uptake in which testosterone instead of dihydrotestosterone (DHT) is the major functional form of androgen. Conclusion. Testosterone deficiency attenuated cholesterol liver uptake mediated by the PCSK9-LDLR pathway, in which AR and testosterone without transforming to DHT play important roles.http://dx.doi.org/10.1155/2022/7989751
spellingShingle Yu Yuefeng
Lin Zhiqi
Chen Yi
Zhu Keyu
Wan Heng
Wang Yuying
Wang Ningjian
Yu Yuetian
Gu Xinjie
Zhang Yihao
Lu Yingli
Xia Fangzhen
Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
International Journal of Endocrinology
title Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
title_full Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
title_fullStr Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
title_full_unstemmed Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
title_short Testosterone Deficiency Promotes Hypercholesteremia and Attenuates Cholesterol Liver Uptake via AR/PCSK9/LDLR Pathways
title_sort testosterone deficiency promotes hypercholesteremia and attenuates cholesterol liver uptake via ar pcsk9 ldlr pathways
url http://dx.doi.org/10.1155/2022/7989751
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