Development and application of diosmin, an extract of Citrus aurantium sp.

Citrus Aurantium Extract Diosmin is a venotonicity enhancing drug and vasoprotective agent that improves the function of the venous, lymphatic and microcirculatory systems. Its chemical formula is C28H32O15 and molecular weight is 608.54. It is soluble in dimethyl sulfoxide and strong alkaline solution, insoluble in water, methanol or ethanol, and very slightly soluble in 0.1 mol/L sodium hydroxide. Its mechanism of action is mainly as follows

For the venous system, it can prolong the time when adrenaline acts on the venous wall to cause contraction, thus enhancing venous tone.
For the microcirculatory system, it can reduce the permeability of capillaries and enhance their resistance, preventing the exudation of water and protein.
For the lymphatic system, it can increase the lymphatic drainage rate and lymphatic vasoconstriction, improve lymphatic reflux and reduce edema.
In addition, it can inhibit the release of inflammatory mediators, reduce the adhesion and aggregation of leukocytes and platelets, and prevent thrombosis.
Diosmin has a variety of pharmacological effects, which are mainly manifested:

Enhancing venous wall tone and elasticity, reducing venous distensibility and venous stasis.
Reducing the viscosity of the blood and increasing the flow rate reducing stagnation.
Normalizes capillary wall permeability and increases its resistance.
Enhances lymphatic constriction and lymphatic drainage rate, accelerates reflux reduces edema.
Inhibits leukocyte adhesion and migration to endothelial cells to reduce inflammatory response.
Inhibit the production and damage of free radicals, with antioxidant effect.
Diosmin is mainly used for the treatment of various symptoms related to venous and lymphatic insufficiency (such as venous edema, soft tissue swelling, heaviness, numbness, pain in the limbs, morning sickness, thrombophlebitis and deep vein thrombosis syndrome, etc.), and for the treatment of symptoms related to acute hemorrhoidal attacks (such as anus moisture, itching, blood in stool, pain and other symptoms of acute attacks of internal and external hemorrhoids caused by hemorrhoidal varicose vein ). It is usually taken orally as a tablet or capsule, usually one or two capsules twice daily.


Prospects for the use of Diosmin

Its application prospect is relatively broad, as it can effectively improve various clinical problems caused by venous dysfunction, and has a good safety and tolerability. At present, Diosmin has been widely used in the treatment of varicose veins of the lower limbs, acute or chronic hemorrhoids, lymphatic reflux disorders, lymphedema, peripheral skin ulcers and other diseases. In addition, Diosmin has the potential to be used in the treatment of other diseases related to abnormal vascular function, such as hypertension, coronary heart disease, stroke, diabetes mellitus, etc., which are all directions worthy of further exploration and research.

It is currently mainly derived from the semi-synthesis of Hesperidin extracted from natural plants. Although this method can ensure the naturalness and biological activity of Diosmin, it also has some drawbacks, such as restricted raw material sources, higher cost, and the purity is not easy to control. Therefore, finding a method to synthesize Diosmin is an important topic. Currently, some methods for synthesizing deosmin have been proposed and implemented, but they still need to be improved and optimized. In the future, if an efficient, low-cost and high-purity synthesis of diosmet can be realized, it will bring more convenience and advantages for its clinical application.