Bis Picolinato Oxo Vanadium
Also known as: Bis(picolinato)oxovanadium(IV) complex, Bis Picolinato Oxo Vanadium, bis(picolinato)oxovanadium(IV), VPA, VO(pic)2
Overview
Bis(picolinato)oxovanadium(IV) is a synthetic vanadium coordination complex, where vanadium is chelated by two picolinic acid ligands and an oxo group. It is primarily investigated for its potent insulin-mimetic properties and potential antidiabetic effects, particularly in the context of insulin-dependent diabetes mellitus. Unlike natural extracts, it is a laboratory-synthesized compound. Its main proposed application is to mimic insulin action to help lower blood glucose levels. Research on this compound is in a moderately mature stage, with numerous in vitro and animal studies demonstrating its efficacy. However, high-quality human clinical trials are limited, and there are no large-scale meta-analyses or systematic reviews specifically focusing on this compound. The current evidence base is predominantly preclinical and early-phase clinical, indicating promising but not yet clinically validated potential.
Benefits
Bis(picolinato)oxovanadium(IV) has demonstrated strong insulin-mimetic activity, primarily in preclinical models. In vitro studies show it effectively inhibits free fatty acid release from rat adipocytes, mimicking insulin's action. Animal studies, specifically in streptozotocin (STZ)-induced diabetic rats, have shown that oral or intraperitoneal administration can normalize blood glucose levels. These effects were observed to be long-lasting, with glucose normalization sustained for approximately 30 days after a 14-day treatment period. Additionally, treated diabetic rats experienced improved metabolic status, indicated by promoted body weight gain. The primary population benefiting from these effects in research has been animal models of insulin-dependent diabetes mellitus (IDDM), as robust human data are currently unavailable. While quantitative effect sizes are not detailed in available abstracts, the glucose-normalizing effect in animal models is described as strong and sustained, bringing levels close to the normal range. The evidence for these benefits is primarily from well-controlled animal studies and in vitro research, indicating a promising but not yet clinically proven therapeutic potential.
How it works
Bis(picolinato)oxovanadium(IV) functions as an insulin mimetic by enhancing glucose uptake and inhibiting lipolysis (free fatty acid release) in adipocytes. Its mechanism involves the inhibition of protein tyrosine phosphatases, such as PTP-1B, which in turn enhances the signaling pathways of the insulin receptor. This complex is orally bioavailable and sufficiently stable to exert systemic effects. It acts as a 'prodrug,' meaning the complex dissociates within cells to release active vanadium species that then exert the insulin-like effects. The chelation with picolinic acid ligands significantly improves its absorption and bioavailability compared to inorganic vanadium salts, allowing for more effective systemic delivery and action.
Side effects
The overall safety profile of Bis(picolinato)oxovanadium(IV) in humans is not well-established due to a lack of comprehensive clinical trials. While animal studies suggest tolerability at effective doses, detailed documentation of common side effects in these studies is limited. Generally, vanadium compounds are known to have a narrow therapeutic index and can cause gastrointestinal discomfort and potential toxicity, particularly at higher doses. Specific human safety data, including reports of adverse events or drug interactions, are not available from the reviewed literature. Therefore, extreme caution is advised when considering this compound, as its potential for toxicity and interactions with other medications remains largely unexplored in human subjects. It is not approved for clinical use, and its safety in various populations, including pregnant or breastfeeding individuals, children, or those with pre-existing medical conditions, is unknown.
Dosage
There are no established human dosing guidelines for Bis(picolinato)oxovanadium(IV) due to the absence of clinical trials. Effective doses have only been determined in animal studies; for instance, oral administration for 14 days normalized glucose levels in diabetic rats. However, these animal doses cannot be directly extrapolated to humans without further research. The exact human equivalent doses remain undetermined. The timing of administration in animal studies involved oral dosing, which demonstrated efficacy and led to long-term effects even after treatment cessation. It is known that the chelation with picolinic acid significantly enhances the absorption and bioavailability of vanadium compared to inorganic vanadium salts, which is a key factor in its observed efficacy in preclinical models. Without human clinical data, any discussion of specific dosage ranges, timing considerations, or upper safety limits for human use is purely speculative and not recommended.
FAQs
Is Bis(picolinato)oxovanadium(IV) safe for human use?
Human safety data are largely lacking. While animal studies suggest potential, caution is warranted due to the absence of robust clinical trials and the known narrow therapeutic index of vanadium compounds.
Does it work better than vanadyl sulfate?
Preclinical research indicates that organically chelated vanadium complexes like Bis(picolinato)oxovanadium(IV) exhibit higher potency and better bioavailability compared to inorganic salts such as vanadyl sulfate.
How quickly does it act?
In animal models, effects on glucose metabolism have been observed within days of administration, with notable long-lasting effects persisting for about a month after treatment cessation.
Is Bis(picolinato)oxovanadium(IV) approved for diabetes treatment?
No, it is currently an experimental compound and is not approved for clinical use in treating diabetes or any other condition.
Research Sources
- https://pubmed.ncbi.nlm.nih.gov/7575515/ – This animal study demonstrated that oral administration of bis(picolinato)oxovanadium(IV) normalized blood glucose levels and inhibited free fatty acid release in streptozotocin-induced diabetic rats, mimicking insulin's action. The effects were sustained for approximately 30 days after a 14-day treatment, indicating a strong and long-lasting insulin-mimetic activity in an animal model of diabetes.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC5068500/ – This review discusses the pharmacokinetics and improved potency of chelated vanadium complexes, including dipicolinato-oxidovanadium, in the context of their potential as insulin mimetics. It explains the 'prodrug' concept, where the complex dissociates to release active vanadium species, highlighting how chelation enhances bioavailability and therapeutic efficacy compared to inorganic vanadium salts.
- https://pubs.rsc.org/en/content/articlelanding/2018/nj/c7nj04189f – This in vitro study investigated the insulin-mimetic activity of bis(picolinato) vanadium complexes using rat adipocytes. It found that these complexes effectively inhibited free fatty acid release, demonstrating an insulin-mimetic effect that was comparable to or even superior to that of vanadyl sulfate, providing mechanistic support for their potential antidiabetic properties.