Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation

Abstract Background The dried root of Inula helenium L., known as Inulae Radix in Mongolian medicine, is a widely used heat-clearing plant drug within the Asteraceae family. Alantolactone (ATL), a compound derived from Inulae Radix, is a sesquiterpene lactone with a range of biological activities. H...

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Main Authors: Ruqiang Yuan, Mingjing Gao, Hu Xu, Qing Liang, Lei Qian, Yali Wang, Houli Zhang, Erjiao Qiang, Weijing Yun
Format: Article
Language:English
Published: BMC 2025-01-01
Series:BMC Cardiovascular Disorders
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Online Access:https://doi.org/10.1186/s12872-024-04461-2
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author Ruqiang Yuan
Mingjing Gao
Hu Xu
Qing Liang
Lei Qian
Yali Wang
Houli Zhang
Erjiao Qiang
Weijing Yun
author_facet Ruqiang Yuan
Mingjing Gao
Hu Xu
Qing Liang
Lei Qian
Yali Wang
Houli Zhang
Erjiao Qiang
Weijing Yun
author_sort Ruqiang Yuan
collection DOAJ
description Abstract Background The dried root of Inula helenium L., known as Inulae Radix in Mongolian medicine, is a widely used heat-clearing plant drug within the Asteraceae family. Alantolactone (ATL), a compound derived from Inulae Radix, is a sesquiterpene lactone with a range of biological activities. However, there is a lack of studies investigating its effectiveness in the treatment of hypertension. The aim of this study is to explore the regulatory effect of alantolactone on blood pressure and its underlying mechanism. Methods and results Network pharmacology analysis suggested that ATL had a potential therapeutic effect on hypertension induced by angiotensin II (Ang II). Subsequently, the results of animal experiments demonstrated that ATL could suppress the increase in blood pressure caused by Ang II. Vascular ring experiments indicated that ATL could inhibit the vascular contractions induced by Ang II, Phenylephrine, and Ca2⁺. Further experiments demonstrated that ATL could inhibit the calcium influx induced by Ang II and increase the expression of pMLC2. Molecular docking experiments showed that ATL had a high binding affinity with L-type Voltage-gated Calcium Channels (VGCC), and vascular ring experiments indicated that ATL could significantly inhibit the vascular contractions caused by the agonists of L-type VGCC. In addition, we also observed that ATL had an ameliorative effect on the vascular remodeling induced by Ang II. Conclusions ATL exerted an antihypertensive effect by inhibiting the activation of L-type VGCC and reducing calcium influx.
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spelling doaj-art-0b9b180dc0e8409ca0a54a7309a85c8c2025-01-12T12:07:14ZengBMCBMC Cardiovascular Disorders1471-22612025-01-0125111310.1186/s12872-024-04461-2Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activationRuqiang Yuan0Mingjing Gao1Hu Xu2Qing Liang3Lei Qian4Yali Wang5Houli Zhang6Erjiao Qiang7Weijing Yun8Advanced Institute for Medical Sciences, Dalian Medical UniversityDepartment of Pharmacy, Dalian Port HospitalWuhu Hospital and Health Science Center, East China Normal UniversityAdvanced Institute for Medical Sciences, Dalian Medical UniversityAdvanced Institute for Medical Sciences, Dalian Medical UniversityAdvanced Institute for Medical Sciences, Dalian Medical UniversityCollege of Pharmacy, Dalian Medical UniversityDepartment of Pathology, Shanghai General Hospital, Shanghai Jiaotong University School of MedicineAdvanced Institute for Medical Sciences, Dalian Medical UniversityAbstract Background The dried root of Inula helenium L., known as Inulae Radix in Mongolian medicine, is a widely used heat-clearing plant drug within the Asteraceae family. Alantolactone (ATL), a compound derived from Inulae Radix, is a sesquiterpene lactone with a range of biological activities. However, there is a lack of studies investigating its effectiveness in the treatment of hypertension. The aim of this study is to explore the regulatory effect of alantolactone on blood pressure and its underlying mechanism. Methods and results Network pharmacology analysis suggested that ATL had a potential therapeutic effect on hypertension induced by angiotensin II (Ang II). Subsequently, the results of animal experiments demonstrated that ATL could suppress the increase in blood pressure caused by Ang II. Vascular ring experiments indicated that ATL could inhibit the vascular contractions induced by Ang II, Phenylephrine, and Ca2⁺. Further experiments demonstrated that ATL could inhibit the calcium influx induced by Ang II and increase the expression of pMLC2. Molecular docking experiments showed that ATL had a high binding affinity with L-type Voltage-gated Calcium Channels (VGCC), and vascular ring experiments indicated that ATL could significantly inhibit the vascular contractions caused by the agonists of L-type VGCC. In addition, we also observed that ATL had an ameliorative effect on the vascular remodeling induced by Ang II. Conclusions ATL exerted an antihypertensive effect by inhibiting the activation of L-type VGCC and reducing calcium influx.https://doi.org/10.1186/s12872-024-04461-2AlantolactoneHypertensionVoltage-gated Calcium ChannelsCalcium influx
spellingShingle Ruqiang Yuan
Mingjing Gao
Hu Xu
Qing Liang
Lei Qian
Yali Wang
Houli Zhang
Erjiao Qiang
Weijing Yun
Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
BMC Cardiovascular Disorders
Alantolactone
Hypertension
Voltage-gated Calcium Channels
Calcium influx
title Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
title_full Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
title_fullStr Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
title_full_unstemmed Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
title_short Alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin II by inhibiting calcium channel activation
title_sort alantolactone mitigates the elevation of blood pressure in mice induced by angiotensin ii by inhibiting calcium channel activation
topic Alantolactone
Hypertension
Voltage-gated Calcium Channels
Calcium influx
url https://doi.org/10.1186/s12872-024-04461-2
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