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地奥司明的药理学:一个柑橘黄酮糖苷:更新综述。

Pharmacology of Diosmin, a Citrus Flavone Glycoside: An Updated Review.

机构信息

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Organization of African Unity Street, Abbassia, Cairo, 11566, Egypt.

出版信息

Eur J Drug Metab Pharmacokinet. 2022 Jan;47(1):1-18. doi: 10.1007/s13318-021-00731-y. Epub 2021 Oct 23.

DOI:10.1007/s13318-021-00731-y
PMID:34687440
Abstract

Flavonoids are phytochemicals that are well known for their beneficial pharmacological properties. Diosmin is a flavone glycoside derived from hesperidin, a flavanone abundantly found in citrus fruits. Daflon is an oral phlebotonic flavonoid combination containing diosmin and hesperidin (9:1) that is commonly used for the management of blood vessel disorders. After oral administration, diosmin is converted to diosmetin, which is subsequently absorbed and esterified into glucuronide conjugates that are excreted in the urine. Pharmacological effects of diosmin have been investigated in several in vitro and in vivo studies, and it was found to possess anti-inflammatory, antioxidant, antidiabetic, antihyperlipidemic, and antifibrotic effects in different disease models. Diosmin also demonstrated multiple desirable properties in several clinical studies. Moreover, toxicological studies showed that diosmin has a favorable safety profile. Accordingly, diosmin is a potential effective and safe treatment for many diseases. However, diosmin exhibits inhibitory effects on different metabolic enzymes. This encourages the investigation of its potential therapeutic effect and safety in different diseases in clinical trials, while taking potential interactions into consideration.

摘要

类黄酮是一种植物化学物质,以其有益的药理特性而闻名。地奥司明是一种源自橙皮苷的黄酮糖苷,橙皮苷是一种在柑橘类水果中大量存在的黄烷酮。达肝素是一种含有地奥司明和橙皮苷(9:1)的口服血管舒缓黄酮类化合物混合物,常用于治疗血管疾病。口服后,地奥司明转化为地奥汀,然后被吸收并酯化形成葡萄糖醛酸缀合物,从尿液中排出。地奥司明的药理作用已在多项体外和体内研究中进行了研究,结果发现它在不同的疾病模型中具有抗炎、抗氧化、抗糖尿病、抗高血脂和抗纤维化作用。地奥司明在多项临床研究中也表现出多种理想特性。此外,毒理学研究表明地奥司明具有良好的安全性。因此,地奥司明是治疗许多疾病的一种有潜力的有效且安全的药物。然而,地奥司明对不同的代谢酶具有抑制作用。这鼓励在临床试验中研究其在不同疾病中的潜在治疗效果和安全性,同时考虑到潜在的相互作用。

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Therapeutic potential of diosmin, a citrus flavonoid against arsenic-induced neurotoxicity via suppression of NOX 4 and its subunits.地奥司明,一种柑橘类黄酮,通过抑制 NOX4 及其亚基发挥其对抗砷诱导的神经毒性的治疗潜力。
Indian J Pharmacol. 2021 Mar-Apr;53(2):132-142. doi: 10.4103/ijp.IJP_837_19.
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Diosmin Mitigates Cyclophosphamide Induced Premature Ovarian Insufficiency in Rat Model.
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Drug Des Devel Ther. 2025 Jul 1;19:5553-5596. doi: 10.2147/DDDT.S535517. eCollection 2025.
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Diosmin Administration Slightly Counteracted the Changes in Bone Mechanical Properties Induced by Experimental Type 1 Diabetes in Rats.地奥司明给药略微抵消了实验性1型糖尿病诱导的大鼠骨力学性能变化。
Pharmaceuticals (Basel). 2025 May 13;18(5):715. doi: 10.3390/ph18050715.
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Zein-sodium caseinate-diosmin nanoparticles as a promising anti-cancer agent with targeted efficacy against A2780 cell line.玉米醇溶蛋白-酪蛋白酸钠-地奥司明纳米粒作为一种有前景的抗癌剂,对A2780细胞系具有靶向疗效。
Sci Rep. 2025 Mar 13;15(1):8762. doi: 10.1038/s41598-025-93772-1.
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Cell Biochem Biophys. 2025 Feb 19. doi: 10.1007/s12013-025-01696-4.
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Post-ischemic reperfusion with diosmin attenuates myocardial injury through a nitric oxidase synthase-dependent mechanism.地奥司明进行缺血后再灌注通过一氧化氮合酶依赖性机制减轻心肌损伤。
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Aescin and diosmin each alone or in low dose- combination ameliorate liver damage induced by carbon tetrachloride in rats.七叶皂苷和地奥司明单独或低剂量联合使用均可改善四氯化碳诱导的大鼠肝损伤。
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Effects of diosmin and crocin on metabolic syndrome-associated cardio-vascular complications in rats.橙皮苷和西红花苷对大鼠代谢综合征相关心血管并发症的影响。
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Diosmin suppresses the proinflammatory mediators in lipopolysaccharide-induced RAW264.7 macrophages via NF-κB and MAPKs signal pathways.地奥司明通过NF-κB和丝裂原活化蛋白激酶(MAPKs)信号通路抑制脂多糖诱导的RAW264.7巨噬细胞中的促炎介质。
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