Bis Piccolinato Oxo Vanadium
Also known as: Bis Piccolinato Oxo Vanadium, vanadyl bis(picolinate), [VO(pic)₂], Bis(picolinato)oxovanadium(IV)
Overview
Bis(picolinato)oxovanadium(IV), often abbreviated as BMOV, is a synthetic coordination complex of vanadium(IV) designed to enhance the bioavailability and insulin-mimetic activity of vanadium. Vanadium is a trace mineral found naturally in various foods, but its inorganic forms typically exhibit low bioavailability. BMOV aims to overcome this limitation through its organic chelation with two picolinato ligands and an oxo group. This complex is primarily investigated for its potential antidiabetic effects, specifically its ability to mimic insulin action and improve glucose metabolism. Research, predominantly in preclinical animal models and in vitro studies, suggests that BMOV can normalize blood glucose levels and exert antilipolytic effects, similar to insulin. It is considered an orally active and potentially long-acting compound, representing a significant advancement over inorganic vanadium salts in terms of absorption and efficacy in animal studies. However, it remains in the early stages of research, with no large-scale human clinical trials available to confirm its safety or efficacy in humans.
Benefits
Bis(picolinato)oxovanadium(IV) has demonstrated significant insulin-mimetic activity in preclinical studies. Its primary benefit observed in streptozotocin (STZ)-induced diabetic rats is the normalization of blood glucose levels. Oral administration of BMOV for 14 days has been shown to sustain normoglycemia for approximately 30 days post-treatment, indicating a long-lasting effect. This also led to improved metabolic status, evidenced by body weight gain in these diabetic models. A secondary, but crucial, benefit is its antilipolytic effect, where it inhibits the release of free fatty acids from adipocytes, mimicking insulin's action. This has been observed in both in vitro studies using isolated rat adipocytes and in vivo. While these findings are promising, it is critical to note that all evidence is derived from animal studies and in vitro experiments. There are no human data, large-scale human randomized controlled trials, or meta-analyses to support these benefits in humans. Therefore, while the effect sizes in rats appear significant, their clinical relevance to humans is currently unknown.
How it works
Bis(picolinato)oxovanadium(IV) acts as an insulin-mimetic by influencing key metabolic pathways. Its primary mechanism involves inhibiting lipolysis, which is the breakdown of fats and release of free fatty acids from adipocytes, thereby mimicking insulin's antilipolytic effect. It also enhances glucose uptake in cells, contributing to improved glucose metabolism. The enhanced bioavailability of BMOV, attributed to its organic chelation with picolinato ligands, allows for better membrane passage and absorption compared to inorganic vanadium salts. At a molecular level, BMOV is thought to interact with insulin signaling pathways. Crystallographic studies with related vanadium complexes suggest potential binding to protein tyrosine phosphatase 1B (PTP-1B), a negative regulator of insulin signaling. By inhibiting PTP-1B, BMOV could potentially enhance insulin sensitivity and signaling, leading to its observed glucose-lowering and antilipolytic effects. This interaction primarily targets adipocytes and potentially muscle cells to regulate glucose and lipid metabolism.
Side effects
The safety profile of Bis(picolinato)oxovanadium(IV) is largely uncharacterized in humans due to the limited scope of research, which is primarily confined to preclinical animal studies and in vitro experiments. In animal studies, no acute toxicity has been reported at the effective doses used to demonstrate its insulin-mimetic effects. However, common, uncommon, or rare side effects in humans are unknown. There is no established data regarding drug interactions, contraindications, or specific safety considerations for special populations such as pregnant women, children, or individuals with pre-existing medical conditions. Given the lack of human clinical trials, the overall safety assessment for human use remains undetermined. It is crucial to emphasize that any use of this compound in humans would be experimental and carries unknown risks, as comprehensive toxicity profiles and long-term safety data are entirely absent.
Dosage
Dosage guidelines for Bis(picolinato)oxovanadium(IV) are not established for human use, as research is limited to preclinical animal studies. In rat models, oral administration for 14 days was found to be effective in normalizing blood glucose levels, with effects lasting approximately 30 days post-treatment. While the exact dose was not specified in the provided summary, effective doses in preclinical vanadium studies typically range from 1-10 mg/kg of body weight. The optimal dosage ranges and maximum safe dose for humans are unknown. The compound is administered orally, and its organic chelation with picolinato ligands is noted to enhance its absorption and bioavailability compared to inorganic vanadium salts. There are no specific timing considerations for human use, nor are there any known required cofactors. Due to the lack of human data, any attempt to determine a human dosage would be speculative and potentially unsafe.
FAQs
Is bis(picolinato)oxovanadium(IV) effective for diabetes?
In animal models, specifically diabetic rats, it has shown effectiveness in normalizing blood glucose levels and mimicking insulin's effects. However, there is no human data to confirm its efficacy for diabetes in people.
Is it safe for human use?
Human safety data for bis(picolinato)oxovanadium(IV) are currently lacking. All available research is preclinical, meaning its safety profile in humans is unknown and not established.
How does it compare to other vanadium compounds?
It demonstrates superior bioavailability and potency compared to inorganic vanadium salts like vanadyl sulfate in animal and in vitro studies, largely due to its organic chelation.
How long do effects last?
In rat studies, a 14-day oral treatment with bis(picolinato)oxovanadium(IV) produced effects that lasted for approximately 30 days post-treatment, indicating a long-acting nature in animals.
Research Sources
- https://pmc.ncbi.nlm.nih.gov/articles/PMC5068500/ – This review discusses various antidiabetic vanadium complexes, highlighting how organic chelation, including dipicolinato-oxidovanadium, improves bioavailability and potency. It explains the prodrug concept for these complexes and summarizes findings from in vitro and in vivo studies, emphasizing the potential of these compounds as insulin mimetics.
- https://pubmed.ncbi.nlm.nih.gov/7575515/ – This animal study investigated the effects of orally administered bis(picolinato)oxovanadium(IV) in STZ-induced diabetic rats. It found that the compound normalized blood glucose levels and sustained this effect for about 30 days post-treatment, demonstrating its long-term insulin-mimetic activity and potential as an antidiabetic agent in preclinical models.
- https://pubs.rsc.org/en/content/articlelanding/2018/nj/c7nj04189f – This in vitro study explored the insulin-mimetic activity of bis(picolinato) vanadium complexes using isolated rat adipocytes. It concluded that these complexes effectively inhibit free fatty acid release, thereby mimicking insulin's antilipolytic action, providing mechanistic insight into their potential therapeutic effects.
