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草药阿马拉提取物通过抑制M2毒蕈碱受体诱导胃底松弛。

Herbal Amara extract induces gastric fundus relaxation via inhibition of the M2 muscarinic receptor.

作者信息

Piqué-Borràs Maria-Riera, Röhrl Johann, Künstle Gerald

机构信息

Preclinical Research and Development, Weleda AG, Arlesheim, Switzerland.

出版信息

Neurogastroenterol Motil. 2025 Jan;37(1):e14924. doi: 10.1111/nmo.14924. Epub 2024 Sep 30.

DOI:10.1111/nmo.14924
PMID:39344827
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11650409/
Abstract

BACKGROUND

Impaired gastric accommodation is one of the most frequent symptoms of functional dyspepsia. The safety and efficacy of conventional treatments remain to be proven and alternative herbal therapies have been proposed to alleviate gastrointestinal symptoms. This preclinical study examined the role of herbal Amara extract (containing Artemisia absinthium, Centaurium erythraea, Cichorium intybus, Gentiana lutea, Juniperus communis, Achillea millefolium, Peucedanum ostruthium, Salvia officinalis, and Taraxacum extracts) on gastric (fundus) accommodation and the possible implication of muscarinic receptors in its regulation.

METHODS

The effect of Amara extract on fundus motility was investigated in organ baths of smooth muscle strips isolated from the fundus of guinea pigs, and the role of the muscarinic receptor pathway was evaluated using functional and radioligand binding assays in cell lines expressing the M2 or M3 muscarinic receptor.

KEY RESULTS

Amara extract inhibited carbachol-induced contraction of guinea pig smooth muscle strips in a dose-dependent manner. This relaxant effect was not affected by the M3 antagonist J-104129. Amara extract also inhibited M2, but not M3, receptor activity in CHO-K1 cells (IC 219 μg mL), and specifically bound the M2 receptor (IC 294 μg mL). Of the nine herbal components of Amara extract, Juniperus communis, P. ostruthium, and Salvia officinalis inhibited M2 receptor activity (IC 32.0, 20.8, and 20.1 μg mL, respectively), and P. ostruthium was sufficient to reverse carbachol-induced ex vivo contraction of guinea pig fundic smooth muscles.

CONCLUSION AND INFERENCES

Amara extract relaxes gastric smooth muscles by inhibiting the M2 muscarinic receptor. This study suggests the potential benefit of Amara extract for patients with impaired gastric accommodation.

摘要

背景

胃容受功能受损是功能性消化不良最常见的症状之一。传统治疗方法的安全性和有效性仍有待证实,人们已提出使用替代草药疗法来缓解胃肠道症状。这项临床前研究探讨了草药苦艾提取物(含有苦艾、红百金花、菊苣、黄龙胆、杜松、蓍草、欧前胡、鼠尾草和蒲公英提取物)对胃(胃底)容受功能的作用以及毒蕈碱受体在其调节中的可能作用。

方法

在从豚鼠胃底分离的平滑肌条的器官浴中研究苦艾提取物对胃底运动的影响,并在表达M2或M3毒蕈碱受体细胞系中使用功能和放射性配体结合试验评估毒蕈碱受体途径的作用。

主要结果

苦艾提取物以剂量依赖性方式抑制卡巴胆碱诱导的豚鼠平滑肌条收缩。这种舒张作用不受M3拮抗剂J-104129的影响。苦艾提取物还抑制CHO-K1细胞中的M2受体活性(IC50为219μg/mL),但不影响M3受体活性,并特异性结合M2受体(IC50为294μg/mL)。在苦艾提取物的九种草药成分中,杜松、欧前胡和鼠尾草抑制M2受体活性(IC50分别为32.0、20.8和20.1μg/mL),且欧前胡足以逆转卡巴胆碱诱导的豚鼠胃底平滑肌离体收缩。

结论与推论

苦艾提取物通过抑制M2毒蕈碱受体来舒张胃平滑肌。本研究提示苦艾提取物对胃容受功能受损患者可能有益。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/bc345e488d9f/NMO-37-e14924-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/cf3adc17a790/NMO-37-e14924-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/3625d09c1772/NMO-37-e14924-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/61fd74271c76/NMO-37-e14924-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/5dad91996ed0/NMO-37-e14924-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/e0d9ad010afd/NMO-37-e14924-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/0034ce9750e9/NMO-37-e14924-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/ac69289d83b5/NMO-37-e14924-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/bc345e488d9f/NMO-37-e14924-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/cf3adc17a790/NMO-37-e14924-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/3625d09c1772/NMO-37-e14924-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/61fd74271c76/NMO-37-e14924-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/5dad91996ed0/NMO-37-e14924-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/e0d9ad010afd/NMO-37-e14924-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/0034ce9750e9/NMO-37-e14924-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/ac69289d83b5/NMO-37-e14924-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e34/11650409/bc345e488d9f/NMO-37-e14924-g006.jpg

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