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L. 草药提取物、其氨基酸制剂及3D打印剂型:植物化学、技术、分子对接及药理学研究。

L. Herb Extract, Its Amino Acids Preparations and 3D-Printed Dosage Forms: Phytochemical, Technological, Molecular Docking and Pharmacological Research.

作者信息

Koshovyi Oleh, Hrytsyk Yurii, Perekhoda Lina, Suleiman Marharyta, Jakštas Valdas, Žvikas Vaidotas, Grytsyk Lyubov, Yurchyshyn Oksana, Heinämäki Jyrki, Raal Ain

机构信息

Institute of Pharmacy, Faculty of Medicine, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.

Department of Pharmacognosy and Nurtricioligy, National University of Pharmacy, 61002 Kharkiv, Ukraine.

出版信息

Pharmaceutics. 2025 Mar 24;17(4):407. doi: 10.3390/pharmaceutics17040407.

Abstract

: The Canadian goldenrod ( L.) is one of the most widespread species of the genus from the Asteraceae family. It has a rich composition of biologically active compounds and is traditionally used to address kidney, urinary tract, and liver diseases. Previously, it was proven that the extract obtained with a 40% ethanol solution had the most promising anti-inflammatory and hepatoprotective activity. Therefore, this extract was selected for the further formulation of amino acid preparations and 3D-printed dosage forms. The aims of the present study were to investigate the chemical composition, toxicity, and antimicrobial, anti-inflammatory, and hepatoprotective activity of dry extract, its amino acid preparations, and 3D-printed dosage forms. : A total of 18 phenolic compounds and 14 amino acids were determined in the extracts. The herb extracts were verified to be practically non-toxic preparations (toxicity class V, LD₅₀ > 5000 mg/kg). They also showed moderate antimicrobial activity against , and β-hemolytic . The most pronounced hepatoprotective activity was observed with herb extract and its amino acid preparations with phenylalanine, alanine, and lysine at a dose of 25 mg/kg body weight. The most pronounced anti-inflammatory activity was found with herb extract and its preparation with arginine. According to the calculated docking score array and the analysis of binding modes in the active sites of COX-1 and COX-2, the flavonoid fraction and caffeic acid in the extracts presented moderate inhibitory activity. : The development of innovative 3D-printed oral dosage forms represents a promising strategy to formulate dietary supplements or pharmaceutical preparations for these herbal extracts.

摘要

加拿大一枝黄花(L.)是菊科该属中分布最广的物种之一。它含有丰富的生物活性化合物成分,传统上用于治疗肾脏、尿路和肝脏疾病。此前已证明,用40%乙醇溶液获得的提取物具有最有前景的抗炎和保肝活性。因此,选择该提取物用于进一步制备氨基酸制剂和3D打印剂型。本研究的目的是研究加拿大一枝黄花干提取物、其氨基酸制剂和3D打印剂型的化学成分、毒性以及抗菌、抗炎和保肝活性。:提取物中总共测定出18种酚类化合物和14种氨基酸。加拿大一枝黄花提取物被证实为实际无毒制剂(毒性等级V,半数致死量>5000mg/kg)。它们对金黄色葡萄球菌、大肠杆菌和β-溶血链球菌也表现出中等抗菌活性。在体重25mg/kg剂量下,加拿大一枝黄花提取物及其含苯丙氨酸、丙氨酸和赖氨酸的氨基酸制剂表现出最显著的保肝活性。加拿大一枝黄花提取物及其含精氨酸的制剂表现出最显著的抗炎活性。根据计算的对接得分阵列以及对COX-1和COX-2活性位点结合模式的分析,加拿大一枝黄花提取物中的黄酮类成分和咖啡酸呈现出中等抑制活性。:开发创新的3D打印口服剂型是为这些草药提取物配制膳食补充剂或药物制剂的一种有前景的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7da1/12030483/5ab676086ba9/pharmaceutics-17-00407-g001.jpg

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