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羟基红花黄色素A在天然低共熔溶剂中的口服生物利用度增强及抗肥胖作用

Oral Bioavailability-Enhancing and Anti-obesity Effects of Hydroxysafflor Yellow A in Natural Deep Eutectic Solvent.

作者信息

Gao Huan, Zhou Hao-Ming, Yue Shi-Jun, Feng Li-Mei, Guo Dong-Yan, Li Jia-Jia, Zhao Qi, Huang Lu, Tang Yu-Ping

机构信息

Key Laboratory of Shaanxi Administration of Traditional Chinese Medicine for TCM Compatibility, Shaanxi University of Chinese Medicine, Xi'an 712046, China.

State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), and Shaanxi Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Shaanxi University of Chinese Medicine, Xi'an 712046, China.

出版信息

ACS Omega. 2022 Jun 3;7(23):19225-19234. doi: 10.1021/acsomega.2c00457. eCollection 2022 Jun 14.

DOI:10.1021/acsomega.2c00457
PMID:35721932
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9202288/
Abstract

Hydroxysafflor yellow A (HSYA), a primary active component in Carthami Flos, has been extensively applied in the treatment of cardiometabolic diseases. In this study, a natural deep eutectic solvent composed of glucose and choline chloride with 10% (v/v) of water (90% GCH) was evaluated to enhance the oral absorption of HSYA. Compared with HSYA in water, the relative oral bioavailability of HSYA in 90% GCH was increased to 326.08%. Furthermore, 90% GCH was demonstrated to decrease the mucus viscosity and increase the absorption rate constant of HSYA in the jejunum by 2.95 times. A pharmacodynamic study revealed that HSYA in 90% GCH was more effective in reducing body weight and correcting steatohepatitis and dyslipidemia in high-fat diet-induced obese rats. Serum metabolomics results showed that the correction of serum aromatic amino acid disorder may contribute to the anti-obesity effect of HSYA in 90% GCH. In conclusion, 90% GCH could be a delivery carrier for HSYA against obesity.

摘要

羟基红花黄色素A(HSYA)是红花的主要活性成分,已广泛应用于心脏代谢疾病的治疗。在本研究中,评估了一种由葡萄糖和氯化胆碱组成并含有10%(v/v)水的天然深共熔溶剂(90% GCH)对提高HSYA口服吸收的作用。与HSYA水溶液相比,HSYA在90% GCH中的相对口服生物利用度提高到了326.08%。此外,90% GCH可降低黏液黏度,并使HSYA在空肠中的吸收速率常数提高2.95倍。药效学研究表明,90% GCH中的HSYA在减轻高脂饮食诱导的肥胖大鼠体重、纠正脂肪性肝炎和血脂异常方面更有效。血清代谢组学结果显示,纠正血清芳香族氨基酸紊乱可能有助于90% GCH中的HSYA发挥抗肥胖作用。总之,90% GCH可能是HSYA抗肥胖的递送载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/c5638cd0fa2b/ao2c00457_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/e1290bfd1d7c/ao2c00457_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/3c988b9fd424/ao2c00457_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/c5638cd0fa2b/ao2c00457_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/e1290bfd1d7c/ao2c00457_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/3c988b9fd424/ao2c00457_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20e1/9202288/c5638cd0fa2b/ao2c00457_0004.jpg

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Food Chem. 2021 Aug 15;353:129337. doi: 10.1016/j.foodchem.2021.129337. Epub 2021 Feb 27.
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Hydroxysafflor Yellow A: A Systematical Review on Botanical Resources, Physicochemical Properties, Drug Delivery System, Pharmacokinetics, and Pharmacological Effects.
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Food Chem. 2021 Jun 30;348:129090. doi: 10.1016/j.foodchem.2021.129090. Epub 2021 Jan 18.
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