Diosmin is a flavonoid found in citrus fruits. Flavonoids are anti-inflammatory plant compounds that protect your body from free radicals and other unstable molecules. The most prevalent uses for Diosmin include hemorrhoids and leg sores caused by poor blood flow. It is also claimed to heal a variety of diseases, albeit there is no hard evidence to back up these claims. Hesperidin is frequently used with Diosmin which is another plant chemical. Diosmin may work by reducing swelling and restoring normal vein function. It also appears to have antioxidative effects. Diosmin was first found in 1925 in the wort plant and has since been used as a natural treatment for hemorrhoids, varicose veins, venous insufficiency, leg ulcers, and other circulatory issues. It may help people with venous insufficiency, a condition in which blood flow is restricted, reduce inflammation, and restore normal blood flow.[1]

Due to its beneficial effects in a number of major human organ systems, such as the cardiovascular system, Diosmin is now one of the most sought-after natural compounds in the treatment of a variety of human diseases, including chronic venous insufficiency (CVI), a progressive disorder affecting an increasing number of people. Diosmin’s effects in combination with other flavonoids, as well as its delivery routes, have also been investigated in details. Diosmin was shown to have anti-oxidant characteristics, allowing it to successfully modulate the activities of a range of variables (including enzymes and biomarkers) connected to oxidative imbalance in a variety of illnesses. Induced apoptosis has been shown to have anti-cancer characteristics and activity in a variety of cell types. In MCF-7, MDA-MB-231, and SKBR-3 breast cancer cells, as well as DU145 prostate cancer cells, A431 skin cancer cells, and colon, oral, urinary bladder, and esophageal carcinogenesis, Diosmin has been found to trigger apoptosis. Diosmin has also been found to have anti-diabetic properties. Diosmin has therapeutic effects in the event of diabetes and associated complications, such as neuropathy and dyslipidemia. Some evidence of a weak antimicrobial action was also found. A combination of Diosmin and hesperidin has been shown to be particularly effective in the treatment of chronic venous insufficiency and hemorrhoids. Diosmin is a great medical medication that can be used alone or in conjunction with other flavonoids.

Pharmacology of Diosmin

Flavonoids are phytochemicals that have been proven to have medicinal properties. Diosmin, a flavone glycoside, is also found in hesperidin. Daflon is an oral phlebotonic flavonoid combination based on Diosmin and Hesperidin that is widely used to treat and protect against 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. Diosmin’s pharmacological properties have been investigated in a number of in vitro and in vivo studies, and it has been found to have anti-inflammatory, antioxidant, antidiabetic, antibacterial, antihyperlipidemic, and antifibrotic properties in a variety of disease models. In a number of clinical studies, Diosmin has also been proven to have a number of positive properties. According to toxicological investigations, Diosmin has a favorable safety profile. As a result, Diosmin has the potential to be an effective and safe treatment for a wide range of conditions. However, Diosmin inhibits a variety of metabolic enzymes, encouraging clinical trials to look into its potential therapeutic efficacy and safety in a variety of illnesses while taking into consideration potential interactions.[2]

Diosmin is a venoactive drug that works on blood vessels in a variety of ways to improve circulation. It improves lymphatic drainage and microcirculation, as well as venous tone and suppleness. For these reasons, Diosmin is often used to improve vascular health in people with chronic venous disease, and it has been demonstrated to improve quality of life. Diosmin also has antioxidant characteristics and scavenges oxygen free radicals, lowering oxidative stress levels that can be detected by biomarkers such as prostaglandin isoprostane precursors.

Anti-Oxidant Property

Oxidative stress has been linked to the development of various diseases, including myocardial ischemia, cerebral ischemia–reperfusion injury, diabetes, neuronal cell injury, hypoxia, and cancer. In rat models, Diosmin was found to exhibit anti-oxidant effects and to stimulate human neutrophils. Because of its anti-oxidant properties, Diosmin has been shown to offer a variety of therapeutic effects for illnesses characterized by oxidative stress.In diabetic rats fed streptozotocin nicotinamide (STZ-NA), Diosmin was found to have significant anti-diabetic effects. When compared to normal control rats, diabetic control rats exhibited lower activities of anti-oxidant enzymes such as glutathione-S-transferase (GST), glutathione peroxidase (GPx), superoxide dismutase (SOD), and catalase (CAT), as well as lower levels of low molecular weight antioxidants like vitamin C, vitamin E, and reduced glutathione (GSH). Lipid peroxidation was increased, and hyperglycemia with a significant drop in plasma insulin levels was observed.

Oral administration of Diosmin enhanced the glycemic and anti-oxidant status of diabetic rats. Diosmin treatment was also found to reduce lipid peroxidation. Due to its anti-oxidant properties, Diosmin functions as an anti-hypertensive drug in deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats. Hypertension is characterized by excessive production of reactive oxygen species. In DOCA-salt-treated rats, non-enzymatic and enzymatic antioxidants were found to be lower, while lipid peroxidation products (thiobarbituric acid reactive substances, lipid hydroperoxides, and conjugated dienes) were significantly higher in blood plasma and tissues such as the liver, kidney, heart, and aorta. Diosmin treatment restored antioxidant levels to near-normal and reduced lipid peroxidation products. These findings were confirmed by histopathological examinations of the kidney and heart. Diosmin was found to have a hepatoprotective effect against ferrous sulfate-induced liver damage in adult male albino rats. Excess iron causes oxidative stress, reactive oxygen species (ROS), lipid peroxidation, inflammation, and tissue necrosis. Elevated levels of ALT, AST, ALP, GGT, LDH activity, and bilirubin indicate hepatocyte membrane damage. After Diosmin treatment, these values were significantly normalized. Diosmin maintains membrane integrity, reduces oxidative stress, and helps correct dyslipidemia, making it an effective hepatoprotective drug. The antioxidant and anti-inflammatory properties of Diosmin are primarily responsible for its hepatoprotective effects. According to research, pre-treatment with Diosmin reduces oxidative stress in the rat heart after ischemia/reperfusion.

Anti-Inflammatory Property

Many diseases, including arthritis, allergies, asthma, autoimmune diseases, atherosclerosis, diabetes, and cancer, are caused by inflammation. Inflammation can be detected by measuring levels of certain biomarkers known as inflammatory markers. These markers include immune cells (such as neutrophils, basophils, eosinophils, platelets, and macrophages), cell surface receptors and adhesion molecules (such as selectins), and soluble mediators (such as cytokines, chemokines, and NF-κB).[3]

Diosmin has been shown to reduce these inflammatory markers due to its anti-inflammatory effects. For example, in a study on lung damage induced by lipopolysaccharide (LPS) therapy, pro-inflammatory cytokines (IL-2, IL-6, IL-17, and TNF-α) and NF-κB were found to be elevated. However, pre-treatment with Diosmin significantly lowered the levels of these markers. In another study, Diosmin was found to decrease the production of LTB4 (an eicosanoid) and colonic MDA in rats with trinitrobenzenesulfonic acid-induced colitis. LTB4 promotes neutrophil chemotaxis, adhesion, and degranulation, while MDA is a product of lipid peroxidation. Diosmin also reduces COX-2 and iNOS levels in chemically induced hepatocarcinogenesis in rats. In a long-term study, Diosmin was administered orally at doses of 10 and 20 mg/kg body weight for 9 weeks, and it was found to lower levels of tumor necrosis factor (TNF-α) and cyclooxygenase-2 (COX-II) in a dose-dependent manner in rats with acetic acid-induced ulcerative colitis . These findings suggest that Diosmin can effectively modulate inflammatory pathways and protect against tissue damage in various inflammatory conditions.

References

[1] Bogucka-Kocka, A.; Wo?niak, M.; Feldo, M.; Kockic, J.; Szewczyk, K. Diosmin—Isolation techniques, determination in plant material and pharmaceutical formulations, and clinical use. Nat. Prod. Commun. 2013, 8, 545–550.

[2] Gerges, S.H.; Wahdan, S.A.; Elsherbiny, D.A.; El-Demerdash, E. Pharmacology of Diosmin, a Citrus Flavone Glycoside: An Updated Review. Eur. J. Drug Metab. Pharmacokinet. 2021, 47, 1–18.

[3] Liu, W.Y.; Liou, S.-S.; Hong, T.-Y.; Liu, I.-M. The Benefits of the Citrus Flavonoid Diosmin on Human Retinal Pigment Epithelial Cells under High-Glucose Conditions. Molecules 2017, 22, 2251.