Ascorbic acid drug class
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Ascorbic Acid Drug Class: Therapeutic Applications and Mechanisms
Introduction to Ascorbic Acid (Vitamin C)
Ascorbic acid, commonly known as Vitamin C, is a water-soluble vitamin renowned for its antioxidant properties. It plays a crucial role in various metabolic functions, including the maintenance of healthy bones, teeth, gums, ligaments, and blood vessels6. Due to its inability to be synthesized by humans, it must be obtained through diet or supplements.
Ascorbic Acid as an Anticancer Agent
Antiproliferative and Cytotoxic Effects
Ascorbic acid has been identified as an antiproliferative agent, particularly in cancer treatment. However, its efficacy requires high concentrations, often necessitating intravenous administration. Recent studies have shown that derivatives of ascorbic acid, such as K873, exhibit potent antiproliferative and cytotoxic effects at much lower concentrations compared to ascorbic acid itself. These derivatives selectively target cancer cells without harming normal cells, making them promising candidates for cancer therapy1.
Pro-Oxidant Activity in Cancer Therapy
At pharmacological concentrations, ascorbic acid exhibits pro-oxidant activity, generating reactive oxygen species (ROS) that induce cytotoxic effects in cancer cells. This pro-oxidant mechanism has been particularly effective in treating oral neoplasms, where it induces apoptosis and DNA fragmentation in cancer cells while sparing normal cells4. Additionally, in cervical cancer cells, ascorbic acid increases ROS levels, induces DNA damage, and enhances the efficacy of chemotherapeutic drugs like cisplatin and doxorubicin5.
Synergistic Effects with Targeted Therapies
In chronic lymphocytic leukemia (CLL), ascorbic acid has shown cytotoxic effects at low doses and can overcome the protective microenvironment of CLL cells. It also synergistically enhances the cytotoxicity of targeted therapies such as Ibrutinib, Idelalisib, and Venetoclax, suggesting its potential as an adjuvant therapy in CLL treatment8.
Epigenetic Regulation in Leukemia
Ascorbic acid acts as a co-factor for 2-oxoglutarate-dependent dioxygenases, which are involved in epigenetic regulation through the control of TET enzymes. This mechanism is crucial in the treatment of acute myeloid leukemia (AML), where ascorbic acid's role in epigenetic regulation and antioxidant response makes it a valuable therapeutic agent9.
Ascorbic Acid in Neurological Drug Delivery
Enhancing Brain Drug Delivery
Ascorbic acid conjugates have been explored to improve the delivery of drugs to the brain via the Vitamin C transporter SVCT2. Conjugation with ascorbic acid increases the affinity and uptake of drugs like nipecotic and kynurenic acids, enhancing their therapeutic effects in neurological conditions2 3.
Ascorbic Acid in Skin Health
Antioxidative and Photoprotective Effects
Topically applied ascorbic acid is widely used in dermatology for its antioxidative properties, which help neutralize free radicals and prevent photoaging. It is also effective in treating hyperpigmentation and other skin conditions. The challenge lies in stabilizing ascorbic acid in formulations to maintain its efficacy6.
Conclusion
Ascorbic acid, beyond its well-known role as a dietary antioxidant, has significant therapeutic potential in various medical fields. Its antiproliferative, pro-oxidant, and epigenetic regulatory properties make it a promising candidate for cancer therapy. Additionally, its ability to enhance drug delivery to the brain and its benefits in skin health further underscore its versatility as a therapeutic agent. Future research and clinical trials will be crucial in fully realizing the potential of ascorbic acid and its derivatives in medical treatments.
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Most relevant research papers on this topic
Ascorbic acid derivatives as a new class of antiproliferative molecules.
Ascorbic acid derivatives, such as K873, show potential as a promising new class of anti-cancer drugs by selectively killing cancer cells without harming normal cells.
In Vitro StudyAscorbic and 6-Br-ascorbic acid conjugates as a tool to increase the therapeutic effects of potentially central active drugs.
Ascorbic acid and 6-Br-ascorbic acid conjugation can improve brain drug delivery by the Vitamin C transporter SVCT2, potentially increasing therapeutic effects of potentially central active drugs.
In Vitro StudyDesign, synthesis and activity of ascorbic acid prodrugs of nipecotic, kynurenic and diclophenamic acids, liable to increase neurotropic activity.
Ascorbic acid conjugates of nipecotic, kynurenic, and diclophenamic acids can improve drug entry into the brain by inhibiting ascorbate transport in human retinal pigment epithelial cells.
In Vitro Study
Highly CitedAscorbic acid and its pro-oxidant activity as a therapy for tumours of oral cavity -- a systematic review.
Ascorbic acid shows potential as an effective cytotoxic agent against oral neoplastic cells without harming normal oral cells, but more clinical trials and in vivo human studies are needed to confirm its effectiveness.
Systematic ReviewHighly CitedMechanisms and Applications of the Anti-cancer Effect of Pharmacological Ascorbic Acid in Cervical Cancer Cells
Pharmacological ascorbic acid increases the susceptibility of cervical cancer cells to cisplatin and doxorubicin, potentially enhancing the efficacy of cancer therapies.
In Vitro StudyAscorbic Acid in Skin Health
Ascorbic acid, a vitamin C, is used topically in dermatology to treat and prevent photoaging and hyperpigmentation, with potential roles in maintaining skin health and overall well-being.
Highly CitedAscorbic acid inhibits human insulin aggregation and protects against amyloid induced cytotoxicity.
Ascorbic acid inhibits human insulin aggregation and protects against amyloid-induced cytotoxicity, offering potential as a drug candidate against aggregation diseases.
In Vitro StudyHighly CitedAscorbic acid (vitamin C) synergistically enhances the therapeutic effect of targeted therapy in chronic lymphocytic leukemia
Ascorbic acid (vitamin C) synergistically enhances the therapeutic effect of targeted therapies in chronic lymphocytic leukemia, potentially improving treatment outcomes.
In Vitro Study
Rigorous JournalThe Anti-Leukemia Effect of Ascorbic Acid: From the Pro-Oxidant Potential to the Epigenetic Role in Acute Myeloid Leukemia
Ascorbic acid shows potential as a novel anti-leukemia therapy due to its role in epigenetic regulation and antioxidant properties, potentially benefiting patients with acute myeloid leukemia.
Literature ReviewMETABOLIC INTERACTIONS BETWEEN L‐ASCORBIC ACID AND DRUGS
Drugs like Chloretone and 3-methylcholanthrene can stimulate ascorbic acid synthesis in rats, with the latter having a more prolonged effect than Chloretone.
Highly Cited