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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 computer-aided molecular design2026-07-25

Immunomodulatory activity of Inula viscosa (L.) compounds identified via LC-ESI-MS and their COX-2-targeted anti-inflammatory potential: in vitro, in vivo and in silico analysis.

Ouari Sara S, Benzidane Nadia N, Yahiaoui Sonia S, Merakeb Mohamed Sofiane MS et al.

Inula viscosa is a medicinal plant widely recognized in the Mediterranean area. Endemically, it has been used to manage various inflammatory conditions and alleviate rheumatic discomfort. However, its immunomodulatory mechanisms remain insufficiently characterized. In this study, we investigated the immunosuppressive activity of I. viscosa leaves and flowers methanol extracts, through a combined in vitro, in vivo, phytochemical identification, and in silico approach, using the SRBC-induced humoral immune response model, both extracts at 50 mg/kg significantly (***p < 0.001) reduced hemagglutination titers and (****p < 0.0001) decreased splenic CD138⁺ plasma cell recruitment, restoring white/red pulp architecture, confirming their ability to downregulate antibody-mediated immunity. LC-ESI-MS analysis identified 20 phenolic compounds, including flavonoids and phenolic acids known for antioxidative and immunosuppressive effects. Molecular docking against COX-2 revealed that several phytochemicals, particularly diosmin, silymarin, and quercetin exhibited stronger binding affinities (- 9.7, - 9.1 and - 9.0 kcal/mol, respectively) than diclofenac (- 7.3 kcal/mol), with quercetin showing the most favorable pharmacokinetic profile as ADME evaluations through Lipinski's "rule of five" confirmed that it fulfills the pharmaceutical requirement. These findings align with our previous formaldehyde-induced arthritis study, reinforcing the anti-inflammatory potential of I. viscosa at low doses, through combined antioxidant action, suppression of humoral immune responses, and COX-2 inhibition.

PMID 42501144
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PubMedInternational journal of nanomedicine2026-06-30

Diosmin-Capped Silver Nanoparticles Promote Osteogenic Differentiation of Human Periodontal Ligament Stem Cells: Box-Behnken Optimization and in vitro Evaluation.

Abdel Gawad Roxane R, Hatem Shymaa S, I Rizk Nehal N, N Raafat Shereen S et al.

Diosmin is a bioactive flavonoid with anti-inflammatory, anti-oxidant, and osteogenic properties; however, its poor water solubility limits its therapeutic use. To overcome this, the study developed Diosmin-loaded silver nanoparticles (AgNPs), leveraging the bone-regenerative potential of silver, as a unique strategy to improve the osteogenic differentiation of periodontal ligament stem cells (PDLSCs). The nanoparticles loaded with the extracted Diosmin were prepared using a scalable green reduction method and optimized using the Box-Behnken design (BBD) and response surface methodology. Key factors (silver nitrate concentration, Diosmin concentration, and reaction temperature) were assessed for their effects on the particle size, zeta potential, and polydispersity index. This study also evaluated the effects of Diosmin-loaded AgNPs on the viability and osteogenic differentiation of human PDLSCs. Alizarin Red staining and alkaline phosphatase activity were used to assess osteogenic differentiation. Moreover, real-time quantitative polymerase chain reaction (RT-qPCR) was used to track the expression of osteogenic-associated markers, osteoprotegerin (OPG) and runt-related transcription factor 2 (RUNX2), as well as proinflammatory markers, TNF-α and IL-1β. The optimized Diosmin-loaded AgNPs identified by the BBD showed high desirability, with particle size of 181.0±8.45 nm using dynamic light scattering technique (DLS) and a negative surface charge of -21.45±1.27 mV, confirmed by transmission electron microscopy (TEM) photomicrographs. Moreover, energy-dispersive X-ray (EDX) analysis showed the preparation of AgNPs through showing their elemental peaks. Stability studies demonstrated that formulations remained stable at 4.0±2.0°C for up to 3 months. The results showed that, in contrast to silver nitrate (AgNO3), Diosmin-loaded AgNPs promoted osteogenic differentiation and modulated the expression of inflammatory markers, indicating a potential role in the regulation of the local inflammatory microenvironment associated with osteogenesis. Green AgNPs have proven their efficacy as a potential approach for osteogenic differentiation.

PMID 42376637
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PubMedFrontiers in molecular biosciences2026-06-30

Interaction of diosmetin, diosmin and diosmetin-7-O-glucoside with human erythrocytes, their model membrane, hemoglobin and redox-active metal ions.

Kaźmierczak Teresa T, Lomozová Zuzana Z, Mladěnka Přemysl P, Gąsior-Głogowska Marlena M et al.

Diosmin, a flavonoid with documented vascular-protective properties, together with the closely related compounds diosmetin and diosmetin-7-O-glucoside, has not previously been subjected to a systematic comparative biophysical characterization. In this study, we performed an integrated biophysical comparison of these three structurally related flavonoids to delineate how structural differences translate into distinct patterns of metal-ion coordination, membrane interaction and hemoglobin engagement, thereby providing a mechanistic context for their behavior in complex erythrocyte- and simplified hemoglobin-based redox systems. All three compounds exhibited low direct radical-scavenging activity in the DPPH• assay and showed differences in predicted lipophilicity and metal-ion interactions. Diosmetin, the most lipophilic derivative, selectively chelated Cu2+/Cu+, while diosmin showed the strongest chelation of both Fe2+ and Fe3+; none of the tested flavonoids reduced iron ions. Diosmetin inhibited rat intestinal α-glucosidase, and both diosmetin and diosmin inhibited lipoxygenase with comparable potency. In intact human erythrocytes, all flavonoids did not cause hemolysis and did not alter osmotic resistance within the concentration range tested, but they differentially affected cell morphology and response to Fe3+-induced oxidative stress. Diosmin and diosmetin-7-O-glucoside predominantly induced echinocyte formation, whereas diosmetin favored stomatocytes and, at the highest concentration, partially reduced Fe3+-induced hemolysis. Measurements in erythrocyte-mimetic liposomes showed no effect of any compound on acyl chain order, while diosmetin induced a pronounced decrease in membrane dipole potential, in contrast to the modest changes observed for diosmin, indicating different modes of interaction with the lipid headgroup region. All three flavonoids quenched the hemoglobin tryptophan fluorescence via a static mechanism, with a similar quenching efficiency but differing binding constants. ATR-FTIR spectroscopy did not reveal detectable alterations in the overall secondary-structure content of hemoglobin. Collectively, the results demonstrate systematic differences among diosmetin, diosmetin-7-O-glucoside and diosmin in metal-ion coordination, membrane-related effects and hemoglobin interactions, providing a comparative biophysical basis for distinguishing their activities. Based on these results, diosmetin appears to be a particularly interesting candidate for further biophysical and functional investigation.

PMID 42376190
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PubMedMolecules (Basel, Switzerland)2026-06-26

Diosmetin Modulates EMT-Associated Plasticity and Fibroblast-Activation Markers in Parallel Breast Cancer In Vitro Models.

Michalczyk Monika M, Kubik Joanna J, Józefczyk Aleksandra A, Iwan Magdalena M et al.

Metastasis remains the leading cause of mortality in breast cancer and is closely linked to epithelial-mesenchymal transition (EMT) and tumor microenvironment (TME)-associated processes. Diosmetin (DT), the active metabolite of diosmin, a widely used venoactive drug, has emerged as a potential anticancer agent. Building on our previous findings demonstrating that DT enhances doxorubicin efficacy, this study investigated its effects on tumor cell plasticity and stromal activation-associated responses. EMT was induced in MCF-7 cells, while a stromal model was established by TGF-β-mediated activation of BJ fibroblasts toward a cancer-associated fibroblast (CAF)-like phenotype. Additionally, doxorubicin-induced senescence was generated in fibroblasts. Migration assays and quantitative real-time PCR were used to assess functional and transcriptional changes. EMT induction resulted in decreased CDH1 expression and increased levels of VIM, MMP2, MMP9, IL-6, and HIF-1A, accompanied by enhanced migratory activity. DT attenuated TGF-β-induced CAF-like activation, as reflected by reduced expression of ACTA2, HGF, MMP2, MMP9, and IL6, and modulated hyaluronan turnover-related genes. Moreover, DT partially alleviated selected senescence-associated features in doxorubicin-treated fibroblasts. Collectively, these findings indicate that DT modulates EMT-associated plasticity and stromal activation-related responses in parallel in vitro models. Given its origin as a metabolite of a clinically used compound and its previously demonstrated chemosensitizing properties, DT may warrant further investigation as a potential adjunctive agent to modulate tumor- and stromal-associated processes in breast cancer.

PMID 42357508
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PubMedThe Canadian journal of infectious diseases & medical microbiology = Journal canadien des maladies infectieuses et de la microbiologie medicale2026-06-25

Bioactive Profiling of Achillea millefolium L. Growing in Kashmir: A Study on Its Phytochemical and LC-MS Analysis, Antioxidant Properties, and Antimicrobial and Molecular Docking Analysis.

Paul Zahid Ahmad ZA, Mir Reyaz Hassan RH, Malla Aamir Tariq AT, Adnan Mohd M et al.

Achillea millefolium L. (yarrow) is one of the oldest known medicinal plants recognized for properties, such as wound healing, fever, common cold, liver problems, nosebleeding, toothache, and headache. Yarrow, being native to Europe, grows wild in the whole of Asia, Northern Europe, and North America and also occurs wild in Kashmir. This study aimed to investigate the antioxidant and antimicrobial properties of Achillea millefolium L. (AM), focusing on its ethanolic extract and its fractions (hexane and ethyl acetate). The antioxidant activity of the extracts was assessed using reducing power and DPPH radical scavenging assays. The extract and its fractions (hexane and ethyl acetate) were evaluated for antimicrobial activity by the agar well diffusion method. Additionally, LC-MS was employed to analyze the chemical composition of the ethyl acetate fraction, and molecular docking studies were conducted to understand its mechanisms of action. The ethyl acetate fraction showed the highest antioxidant activity with an IC50 value of 199.12 (μg/mL), antibacterial activity against B. subtilis, ZOI = 14.74 ± 0.16, and antifungal activity against C. neoformans 34.70 ± 0.58. LC-MS identified key compounds, including diosmin, pelargonin, and epicatechin. From the docking analysis, the highest binding affinity was monitored in the cases of diosmin with -10.7 kcal, followed by pelargonin (-9.3 kcal) and epicatechin (-8.6 kcal) with the EF-TU complex protein. In summary, this study highlights the antioxidant and antimicrobial capabilities of Achillea millefolium L. These findings will establish the groundwork for bioassay-guided separation of bioactive components that could serve as leads for future research to combat diseases caused by microbes that are resistant to drugs.

PMID 42344762
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PubMedFood & function2026-05-27

Integrated RNA-seq and network pharmacology analyses suggest PI3K-Akt and NF-κB pathway modulation in the protective effects of diosmin against experimental colitis.

Wang Shuo S, Tan Cheng C, He Haodong H, Li Xiangyun X et al.

Ulcerative colitis (UC), a chronic inflammatory bowel disease, remains difficult to treat due to incomplete understanding of its mechanisms and limited therapeutic options. Diosmin, a natural citrus-derived flavonoid, has shown promising anti-inflammatory effects, but its molecular mechanisms in UC are unclear. In this study, we investigated the protective role of diosmin using dextran sulfate sodium (DSS)-induced colitis in mice and LPS-stimulated HT-29 cells, integrating transcriptomic and network pharmacology analyses. Diosmin treatment significantly alleviated colitis symptoms, reduced inflammation, preserved colon length, and enhanced intestinal barrier integrity, with efficacy comparable to 5-aminosalicylic acid. RNA-seq and network pharmacology identified PI3K-Akt and NF-κB as key pathways associated with diosmin-mediated protection, while molecular docking was used as a supportive computational analysis to explore potential interactions with selected hub-associated proteins. Experimental validation confirmed that diosmin inhibited activation of PI3K-Akt-mTOR and NF-κB signaling, decreased pro-inflammatory cytokines (TNF-α, IL-1β and IL-6), increased IL-10, promoted intestinal barrier repair via upregulation of ZO-1, occludin, and E-cadherin, and suppressed apoptosis of colonic epithelial cells. Together, these findings suggest that diosmin exerts multi-target protective effects against experimental colitis by modulating inflammation, supporting barrier integrity, and regulating key signaling pathways, providing mechanistic insight into the actions of this citrus-derived bioactive compound in colitis.

PMID 42191164
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