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diosmin + hesperidine (Daflon / Capiven / Detralex)

✓ Approved

Servier · 治疗药物

什么是 diosmin + hesperidine？

diosmin + hesperidine 是一种治疗药物，由Servier研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Daflon, Capiven, Detralex
公司Servier
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Servier

治疗适应症

diosmin + hesperidine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Vascular disordersPeripheral venous disease✓ Approved

相关研究文献

PubMedJournal of ethnopharmacology2026-10-16

Ziziphora clinopodioides Flavonoids exerts neuroprotective effects through PI3K/Akt pathway to improve ischemic stroke.

Zhuo Xingjie X, Li Siyi S, Zhang Wencong W, Deng Mingcong M et al.

Ziziphora clinopodioides Lam. is a traditional Uyghur medicinal herb used for centuries in Xinjiang, China, to treat cardiovascular and cerebrovascular disorders. According to local ethnopharmacological records, it is traditionally employed to promote blood circulation, remove blood stasis, calm the heart, and relieve chest tightness and palpitations. Modern studies have shown that its total flavonoids (ZCF) possess anti-inflammatory and antioxidant activities. Ischemic stroke (IS) is a leading cause of death and disability, involving neuroinflammation, oxidative stress, and blood-brain barrier (BBB) disruption. However, the neuroprotective mechanism of ZCF against IS and its active constituents remain unclear. This study aimed to elucidate the neuroprotective mechanism of ZCF against IS and to identify its potential active flavonoids. Network pharmacology and transcriptomics were used to predict core pathways, followed by in vitro and in vivo experiments. Neurological deficits, infarct volume, BBB integrity, and PI3K/Akt-related inflammatory/oxidative markers were assessed. The PI3K inhibitor LY294002 was used, and active flavonoids were screened by molecular docking, molecular dynamics simulations, and ELISA. Integrated transcriptomics and network pharmacology identified that ZCF modulates the PI3K/Akt pathway. In MCAO/R-treated rats, ZCF reduced cerebral infarction, and preserved neuronal morphology. ZCF protected BBB integrity by restoring ZO-1, Occludin, Claudin-5, reducing MMP-9 and MMP-2 levels, rebalancing the Ang-1/Ang-2 ratio, decreasing NaF permeability, and increasing TEER. ZCF activated PI3K/Akt signaling in both bEnd.3 cells and MCAO/R-treated rat brain tissues, and the PI3K inhibitor LY294002 reversed ZCF-mediated regulation of tight junction proteins, matrix metalloproteinases, and Ang-1/Ang-2, suggesting that ZCF preserves BBB integrity at least partly through a PI3K/Akt-dependent mechanism. ZCF inhibited the TLR4/NF-κB/NLRP3 axis, reduced IL-1β, IL-6, TNF-α and MDA, and up-regulated Nrf2 and SOD, and these effects were reversed by LY294002. Molecular docking and MD simulations suggested that Diosmin, Glycitin, and Tilianin may form stable binding with PI3K. Diosmin, Glycitin and Tilianin could significantly restore the activity of PI3K in PC12 cells treated with OGD/R, reduce the levels of IL-1β, IL-6, TNF-α and MDA, and enhance the activity of SOD. Under preconditioning conditions, ZCF maintains BBB and inhibits neuroinflammation and oxidative stress through integrity and PI3K/Akt dependence, thereby exerting anti-IS protection. Diosmin, Glycitin, and Tilianin are potential active flavonoids that may contribute to PI3K/Akt activation.

PMID 42887834
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PubMedMedical oncology (Northwood, London, England)2026-10-08

Nano-Diosmin mitigates EAC-induced renal injury through Nrf2-mediated antioxidant activation and NF-κB-dependent apoptotic suppression.

Alshammari Ahmad Najem AN, Alfawaz Mohammed Saleh MS, Oraby Fatma F, Mohamed Ahmed M AM et al.

The present study provides the first evidence of the anticancer-associated renoprotective efficacy of diosmin (DI) delivered via chitosan nanoparticles (DI-CHNPs) in mice bearing Ehrlich ascites carcinoma (EAC). Sixty female Swiss albino mice were divided into six groups: controls, DI, DI-CHNPs, EAC, EAC+DI, and EAC+DI-CHNPs. Treatments involved DI or DI-CHNPs (100 mg/kg/day) for 20 days with or without tumor induction. DI-CHNPs significantly reduced tumor burden, as evidenced by lower body weight gain, abdominal circumference, tumor volume, and viable tumor cell count, and these effects were superior to free DI. DI-CHNPs also prolonged survival and improved renal function markers (urea, creatinine, electrolytes), indicating that attenuation of tumor progression was accompanied by reduced secondary renal injury. Antioxidant defenses in kidney tissues were strengthened through increased superoxide dismutase, catalase, glutathione peroxidase activities, and reduced glutathione levels, alongside reduced malondialdehyde. DI-CHNPs activated the Nrf2/HO-1/NQO1 pathway while down-regulated the inflammatory pathways controlling genes (Tgfb 1, Nfkb 1, Il6) and pro-apoptotic markers (Bax, Caspase-3), with increased Bcl-2 expression. Histopathological and ultrastructural analyses confirmed superior renal protection compared with DI. Molecular docking provided in silico supportive evidence for DI interaction with Nrf2, NF-κB, caspase-3, and TGF-β-related molecular targets involved in oxidative stress, inflammation, and apoptosis. Overall, the findings suggest that nanoparticle formulation enhanced the therapeutic performance of DI, likely through improved stability and sustained-release properties, resulting in superior antitumor efficacy and attenuation of tumor-associated renal injury.

PMID 42848291
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PubMedNatural product research2026-10-07

Phytochemical profiling and biological evaluation of Duranta serratifolia (Griseb.) Kuntze cultivated in Egypt: HPLC and lC-mS characterization, antimicrobial and anticancer activities, and in silico validation.

Mahmoud Asmaa A AA, Eid Mona M MM, Mahrous Fatma S FS, Afifi Tarek H TH et al.

The present study provides a phytochemical and biological evaluation of Duranta serratifolia (Griseb.) Kuntze cultivated in Egypt. Preliminary screening revealed the predominance of flavonoids and phenolic compounds, which was supported by high total phenolic (101.6 mg ± 2.1 GAE/g) and flavonoid (166.3 ± 1.1 mg QuE/g) contents. HPLC and LC-MS analyses identified diverse phenolic acids and flavonoid glycosides, with cinnamic acid, naringenin, kaempferol, quercetin derivatives, and diosmin as major constituents. The extract exhibited potent antimicrobial activity, particularly against Bacillus subtilis and Candida albicans, with low MIC values, alongside antioxidant capacity (DPPH IC50 = 12.77 ± 0.4 µg/mL). Cytotoxic effects were observed against MCF-7 and PC-3 cancer cell lines. TEM analysis confirmed microbial ultrastructural damage. Molecular docking demonstrated strong binding affinities of major flavonoids towards β-lactamase and DHFR, supporting the in vitro findings. These results highlight D. serratifolia (Griseb.) Kuntze as a source of bioactive natural products with therapeutic potential.

PMID 42839256
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PubMedRSC advances2026-10-02

The improvement of diosmin dissolution by PLGA complexes for oral delivery: physicochemical characterization and anti-inflammatory evaluation.

Ton Anh-Khoa AK, Phan Truc Thi-Anh TT, Tran Mi Thi-Tra MT, Huynh Thi-Kim-Chi TK et al.

Diosmin (DSN) is a potent flavonoid used for chronic venous insufficiency, but its therapeutic potential is constrained by poor aqueous solubility and low oral bioavailability (BCS Class IV). To overcome these challenges, a hybrid polymeric nanocarrier system comprising poly(lactic-co-glycolic acid) (PLGA) and (2-hydroxypropyl)-β-cyclodextrin (HPCD), surface-stabilized by chitosan, was successfully engineered via single-emulsion solvent evaporation. Systematic optimization identified a 95 : 5 (w/w) PLGA : HPCD formulation (95P5H-DSN), achieving an encapsulation efficiency of 71.47 ± 1.38% and a drug loading of 12.81 ± 0.25%. The nanoparticles exhibited a uniform spherical morphology with a hydrodynamic diameter of 223 ± 15.72 nm, a polydispersity index of 0.329, and a high positive zeta potential (+70.00 ± 7.35 mV), indicating good colloidal stability. Solid-state analyses (XRD, DSC, and FTIR) verified drug amorphization and successful entrapment within the matrix. In vitro release studies demonstrated pH-dependent behavior that fits the Higuchi diffusion model; the nanocarrier suppressed gastric release at pH 2.0 while providing a controlled and improved dissolution profile at intestinal pH 7.8 (17.73% at 24 h). Furthermore, in LPS-stimulated RAW264.7 macrophages, 95P5H-DSN partially attenuated the intrinsic cytotoxicity of raw DSN and exerted concentration-dependent anti-inflammatory efficacy via nitric oxide suppression. The anti-inflammatory IC50 was 58.95 µg mL-1. These findings establish the PLGA-HPCD nanocomplex as a promising oral drug-delivery platform for enhancing the dissolution and therapeutic efficacy of diosmin.

PMID 42825141
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PubMedMolecules (Basel, Switzerland)2026-09-26

Ex Vivo Study of the Vasomotor and Anti-Inflammatory Activity of Class 2 Elastic Venous Compression Devices Combined with Diosmetin-3-O-β-D-Glucuronide.

Belabed Yasmine Y, Boisnic Sylvie S, Stroumza Nathaniel N, Talbot Charlotte P J CPJ et al.

Diosmin, a flavonoid, is widely used to alleviate the symptoms of chronic venous disease (CVD), while compression stockings remain a key component of its conservative management. This study used an ex vivo model of human skin explants to evaluate the vasomotor and anti-inflammatory effects of a class II elastic venous compression model (EVC2), applied alone or in combination with diosmetin-3-O-β-D-glucuronide (DT), the major circulating metabolite of diosmin. The explants were exposed to substance P to induce neurogenic inflammation, after which they were treated with EVC2, DT at a concentration of 2700 pg/mL, or both. Compared with substance P alone, all treatments led to a significant reduction in capillary dilation and IL-8 secretion, as well as a change in endothelial CD34 expression. While the combination improved all parameters, only significant additional effects were observed for reducing low CD34 expression versus DT alone (77% for score 0, no CD34 expression, p = 0.043; 62.1% for score 1, low CD34 expression, p = 0.013), and for decreasing IL-8 versus EVC2 alone (41.2%, p = 0.033). These findings suggest vasomotor and anti-inflammatory effects of DT and mechanical compression, and highlight their combined effects on inflammatory parameters in CVD.

PMID 42796431
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PubMedInternational immunopharmacology2026-09-18

Retraction notice to "Combined diosmin and bisoprolol attenuate cobalt chloride-induced cardiotoxicity and endothelial dysfunction through modulating miR-143-3P/MAPK/MCP-1, ERK5/CXCR4, Orai-1/STIM-1 signaling pathways" [Int. Immunopharmacol. 140 (2024) 112777].

El-Shoura Ehab A M EAM, Mohamed Ahmed A N AAN, Atwa Ahmed M AM, Salem Esraa A EA et al.

PMID 42760158
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