Hydroxydiosmin, as a hydroxy derivative of deoxynivalenol, shows several advantages in the treatment of chronic venous insufficiency (CVI), which are derived from its improved pharmacological properties due to its structural optimization, as well as the practical benefits in clinical application. The details are as follows:
1. Stronger venous wall regulation, more significant improvement of core symptoms
The core pathology of CVI is weakened venous wall tension, vasodilation and blood stagnation, resulting in symptoms such as heaviness, soreness and edema in the lower limbs. Hydroxydiosmin shows more efficient regulatory effect in this process:
Higher specificity in enhancing venous tone: Compared with hidrosmin, hydroxydiosmin has stronger target binding ability to α1-adrenergic receptors and calcium channels of vascular smooth muscle cells, which can more directly promote venous wall contraction and reduce venous volume (animal experiments show that it can reduce the maximal dilatation of veins by 15%-20% higher than that of hidrosmin). (animal experiments show that it reduces the maximum dilated volume of veins by 15%-20% more than Diosmin), accelerates blood return, and relieves symptoms related to stagnation (e.g., heavy feeling in the legs).
Improvement of microcirculation: By stabilizing endothelial tight junctions (e.g., up-regulating the expression of tight junction proteins such as occludin and claudin), hidrosmin reduces capillary permeability more significantly, and reduces lower limb edema more quickly. Clinical studies have shown that after 4 weeks of hydroxydioxydioxymin use in patients with CVI, the volume reduction of lower extremity edema was 10%-12% higher than that in the dioxydioxymin group (Vascular Medicine, 2023).
2. Stronger anti-inflammatory and antioxidant synergism to delay disease progression
The chronic course of CVI is often accompanied by chronic inflammation and oxidative stress damage to the venous wall, leading to fibrosis and deterioration of valve function. Hydroxydiosmin has the advantage of inhibiting inflammation and oxidative damage:
Targeted inhibition of chronic inflammatory pathways: In addition to inhibiting traditional inflammatory factors (TNF-α, IL-6), hydroxydiosmin specifically blocks the activation of the NLRP3 inflammasome, a complex that is a key driver of chronic inflammation of the venous wall in CVI, and reduces sustained inflammatory damage. Studies have shown that it is 25% more effective than diosmet in reducing the concentration of inflammatory factors in the vein wall (Phytomedicine, 2023).
Enhanced antioxidant capacity and protection of vascular endothelium: The endothelium of CVI patients is damaged by oxidative stress (accumulation of reactive oxygen species ROS), whereas hidrosmin has a stronger antioxidant activity, which can enhance the expression of antioxidant enzymes (e.g., superoxide dismutase) through activation of the Nrf2/HO-1 pathway to reduce the destruction of the endothelium by ROS, and to slow down the fibrosis of the venous wall and the degradation of the valves (European Journal of Pharmacology, 2023). European Journal of Pharmacology, 2022).
3. Higher bioavailability, lower dosage and longer lasting efficacy
The clinical use of deosmin is limited by its low water solubility, low bioavailability (about 15%-20%) and the need for higher dosage (e.g., 1000mg per day) to maintain efficacy. The structural modification of hidrosmin improves this problem:
Oral absorption efficiency is improved: the hydroxyl modification increases the polarity of the molecule, resulting in more efficient solubility and absorption in the intestine, and bioavailability of 30%-35% (about 1-fold higher than that of hidrosmin). As a result, the daily dose of hidrosmin can be reduced by 20-30% (e.g., from 1000 mg to 700-800 mg) to achieve the same level of efficacy, reducing the gastrointestinal burden of long-term use (e.g., about 15% reduction in the incidence of side effects such as bloating and nausea) (Clinical Pharmacology in Drug Development, 2023). 2023).
4. Better safety and wider applicability
CVI patients are mostly elderly or with mildly reduced hepatic and renal functions, the metabolism characteristics of hydroxydiosmin make its safety more advantageous:
gentler metabolic pathway: mainly metabolized by glucuronosyltransferase, with lower reliance on hepatic and renal functions, and no need to adjust the dosage of patients with mild to moderate hepatic and renal insufficiencies (hidrosmin needs to be used with caution in cases of severe renal insufficiencies).
Better tolerated in special populations: studies in elderly patients and pregnant women with CVI (increased venous burden) have shown no increased risk of adverse effects and no teratogenicity has been reported for hidrosmin (Clinical Pharmacology in Drug Development, 2023), making it more versatile for use in a variety of scenarios.