Description

PROBLEM BEING SOLVED

The invention aims to address the challenge of delivering therapeutic agents to the central nervous system (CNS) by designing transition metal complexes with high barrier permeability. Currently, the blood-brain barrier (BBB) restricts the entry of most drugs, limiting treatment options for CNS diseases like Alzheimer's and brain tumors. The lack of effective transport through the BBB hinders the translation of promising therapeutics from the lab to clinical use, highlighting the need for innovative solutions.

METHOD USED

The unique approach of the invention involves utilizing appropriately designed transition metal complexes to enhance BBB permeability for diagnostic and therapeutic purposes in CNS diseases. By incorporating a cyclopentadienyl tricarbonyl metallic core, these complexes exhibit favorable properties such as low molecular weight, suitable lipophilicity, stability, and easy conjugation to bioactive molecules targeting amyloid plaques. Through chemical affinity tests, binding constant determination, and biodistribution experiments, the complexes show potential for diagnosing Alzheimer's disease and brain tumors with improved brain uptake.

ADVANTAGES

Compared to existing methods, the transition metal complexes developed in this invention offer significant advantages in CNS drug delivery. While traditional drugs struggle to cross the BBB, these complexes show promise in effectively penetrating the barrier and reaching the target sites in the brain. By enhancing brain uptake and providing a platform for specific targeting of amyloid plaques in diseases like Alzheimer's, the complexes represent a novel and potentially transformative approach to diagnosing and treating CNS disorders. Additionally, the use of widely available 99mTc as a radionuclide for imaging further enhances the practicality and accessibility of this innovative solution.

Description

PROBLEM BEING SOLVED

The invention aims to address the ineffectiveness of current infectious disease management approaches caused by widespread resistance of parasites to drugs and insect disease vectors to insecticides used in vector control programs. The lack of effective vaccines and the undesirable properties of existing synthetic mosquito repellents, such as DEET, Icaridine and IR3535, have further complicated disease control efforts. The need for new natural and synthetic compounds with mosquito repellent activity similar to DEET, Icaridine and IR3535 but without their drawbacks has become increasingly urgent.

METHOD USED

The invention discloses novel natural compounds and compositions for repelling arthropods, particularly insects and arachnid disease vectors, by targeting specific chemosensory proteins in the vectors. These repellent compounds were shown to bind to mosquito proteins called odorant binding proteins (OBPs), affect mosquito behavior and reduce interactions with human hosts. Compositions may include carvacrol, cumin, and cinnamate compounds, among others, to achieve mosquito repellence and prevent blood meals. Methods for reducing mosquito bites on individuals or infestations in specific locations involve applying the disclosed repellent compounds or compositions, offering a natural and effective alternative to existing synthetic repellents.

ADVANTAGES

The disclosed compounds and compositions offer a safer and more effective solution for controlling diseases transmitted by mosquitoes and arachnids. By targeting specific chemosensory proteins in mosquitoes, the invention provides a unique approach to repelling insects and arachnids that act as vectors for infectious pathogens. The use of essential oils and natural compounds derived from them as repellents presents advantages over synthetic repellents like DEET, Icaridine and IR3535, which have known health risks and environmental disadvantages. The invention's methods for identifying and screening essential oils and constituent compounds for repellent activity provide a promising avenue for disease prevention and vector control.

Description

PROBLEM BEING SOLVED

The invention aims to address the growing issue of antibiotic resistance, particularly in bacterial infections caused by pathogens producing metallo-beta-lactamases (MBLs). These enzymes hydrolyze the amide bond of antibiotics containing a β-lactam ring, leading to resistance against virtually all β-lactams, which are crucial for treating infections. The emergence of carbapenemase-producing Enterobacterales (CRE) poses a significant threat, as no new classes of antibiotics have been introduced in the last 25 years.

METHOD USED

The invention proposes the use of heptakis- and octakis-cyclodextrins (IDA = iminodiacetic acid) as potent inhibitors of bacterial MBLs. These cyclodextrins form complexes with lanthanide metal cations, allowing them to inhibit the activity of MBLs effectively. By combining these cyclodextrins with β-lactam antibiotics, the invention enables the potentiation and reactivation of antibiotics, making them effective against MBL-producing bacterial pathogens. Unlike other inhibitors, the IDACYDs exhibit no cytotoxicity, acute toxicity, or immune response, making them safe for use in treating severe bacterial infections.

ADVANTAGES

Compared to existing treatments, the invention offers a novel approach to combat antibiotic resistance by targeting MBL-producing pathogens. The IDACYDs provide a safe and effective solution for treating infections that are resistant to current antibiotics, without inducing harmful side effects. By utilizing cyclodextrins in combination with antibiotics, the invention opens up new possibilities for overcoming the limitations of existing treatments and offers a promising strategy for managing life-threatening infections caused by MBL-producing bacteria.