Abstract

US 2012/0065273 A1 Patent application Published 15 March 2012
TTO-Based Wide Spectrum Therapeutics, Disinfectants, and Anesthetics for Use in Aquaculture
Applicant/Inventor
Abstract
The invention discloses a novel wide-spectrum aquaculture pharmaceutical with therapeutic, disinfective, and/or anesthetic effects. The preparation is comprised of TTO (tea tree oil) in a stable water-in-oil emulsion of alkali or ammonium salts of organic fatty acid. The emulsion is also stable when converted into an oil-in-water emulsion, wherein this preparation is for the treatment of aquatic animals suffering from bacterial, parasitic, viral, or mycotic diseases. The invention also discloses a method for treating diseases selected from bacterial, parasitic, viral, and mycotic origin, in an aquatic animal suffering therefrom, whose method comprises administering a therapeutic active amount of a preparation comprising TTO in a stable water-in-oil emulsion of alkali or ammonium salts of organic fatty acid; said emulsion is also stable when converted into an oil-in-water emulsion to said aquatic animal.
http://www.patentlens.net/patentlens/patent/US_2012_0065273_A1/en/
Summary
This work pertains to the search for nontoxic, environmentally friendly substances that are effective broad-spectrum aquaculture pharmaceuticals. Though presented in the context of large-scale commercial aquaculture, both for ornamental and nonornamental animals, such compounds could also be useful for smaller aquaculture ventures such as research laboratories. Fish and other aquaculture organisms are subject to a wide variety of bacterial, fungal, and viral diseases, as well as parasites and environmental stresses. With many currently available treatments, there are concerns about developing pathogen resistance and environmental impact. However, the inventor states that a wide spectrum of biocidal activity has been documented for tea tree oil (TTO) and its bioactive constituents, while pathogen resistance to the same has not yet been documented. Disclosed and claimed here are formulations of TTO emulsions designed for aquaculture purposes, including use with zebrafish.
WO 2012/026748 A2 Patent application Published 1 March 2012
Pharmaceutical Composition Containing Melastoma sanguineum Extracts or Fractions Thereof as Active Ingredients for Preventing and Treating Diabetic Complications
Applicants/Inventors
The present invention relates to a composition containing Melastoma sanguineum extracts or fractions thereof as active ingredients for preventing or treating diabetic complications. More particularly, Melastoma sanguineum extracts, or ethyl acetate fractions and n-butanol fractions that are systematic fractions thereof, inhibit the formation of advanced glycation end-products, as well as the activity of aldose reductases, which may serve as an index of the onset of diabetic complications. The Melastoma sanguineum extracts or ethyl acetate fractions and n-butanol fractions have the effects of potently inhibiting vasodilatation caused by hyperglycemia in zebrafish, which are vertebrates, and inhibiting diabetic complications when administered to animal models for diabetic disease. Therefore, the Melastoma sanguineum extracts or ethyl acetate fractions and n-butanol fractions, which are systematic fractions thereof, according to the present invention may be used as active ingredients for a pharmaceutical composition for preventing and treating diabetic complications.
http://www.patentlens.net/patentlens/patent/WO_2012_026748_A2/en/
WO 2012/021390 A1 Patent application Published 16 February 2012
Ligands and Methods for Labeling Biomolecules in Vivo
Applicants/Inventors
Abstract
Disclosed are tris(triazolylmethyl)amine ligands, and kits and methods for labeling and/or imaging a biomolecule of interest in a subject or living system.
http://www.patentlens.net/patentlens/patent/WO_2012_021390_A1/en/
Summary
Bio-orthogonal click chemistry involves selective covalent labeling of biomolecules in cells and living organisms, enabling imaging of labeled biomolecules “live” in their native milieu. Here, the inventors describe a new Cu(I) ligand for use in live cell labeling that promotes rapid reaction progress with little associated copper cytotoxicity. The inventors used zebrafish embryos as an in vivo system for determining ligand effectiveness and toxicity, as well as for evaluating its suitability for conducting time-lapse imaging. The claimed invention includes the structure, synthesis, and use of the ligand for in vivo detection of biomolecules or other detectable markers.
WO 2012/017004 A1 Patent application Published 9 February 2012
Novel Artemisinin-Like Derivatives with Cytotoxic and Anti-angiogenic Properties
Applicant/Inventor
Abstract
The present invention relates to novel artemisinin-like derivates, and especially dihydroartemisinin derivates and pharmaceutical compositions comprising the present compounds. The present invention further relates to the use of the present compounds for the treatment of cancer, especially by oral administration. The present invention especially relates to dihydroartemisinin compounds (DHA) substituted by, through an ester linkage by a linear or branched C 1 to C 6 alkyl optionally substituted by one or more halogens. Especially preferred substituents are acetate, propionate, isopropionate, butyrate, and isobutyrate.
http://www.patentlens.net/patentlens/patent/WO_2012_017004_A1/en/
Summary
This work evaluates novel derivatives of known biologically active compounds for new therapeutic possibilities. Zebrafish are used for in vivo testing of anti-cancer therapeutics. Artemisinins, known as highly active anti-malarials, exhibit a range of biological activities; relevant here are their anti-angiogenic and anti-tumorigenic activities, making them potential anti-cancer therapeutics. The inventors used the zebrafish as an in vivo model for evaluating the anti-angiogenic properties of the claimed compounds, a range of novel artemisinin-like derivatives. They report that certain of the novel derivatives blocked ISV sprouting, as assayed in Tg(fli1:EGFP) embryos. The derivative compounds with the highest anti-angiogenic activity in zebrafish embryos also showed anti-proliferative activity in cellular assays. The inventors claim a range of formulas for artemisinin and dihydroartemisinin derivatives, as well as the therapeutic administration of the claimed compounds, including oral formulations, generally and specifically for cancer treatment.
US 2012/0029055 A1 Patent application Published 2 February 2012
Modulators of Apoptosis and the Uses Thereof
Applicants/Inventors
Abstract
Here we demonstrate that miR-125b, a brain-enriched microRNA, is a negative regulator of p53 in animals. miR-125b-mediated downregulation of p53 is dependent on the binding of miR-125b to a microRNA response element in the 39 untranslated region of p53 mRNA. Overexpression of miR-125b represses the endogenous level of p53 protein and suppresses apoptosis in cells. In contrast, knockdown of miR-125b elevates the level of p53 protein and induces apoptosis in cells. This phenotype can be rescued significantly by either an ablation of endogenous p53 function or ectopic expression of miR-125b in zebrafish. Ectopic expression of miR-125b suppresses the increase of p53 and stress-induced apoptosis. Together, our study demonstrates that miR-125b is an important negative regulator of p53 and p53-induced apoptosis during development and during the stress response.
http://www.patentlens.net/patentlens/patent/US_2012_0029055_A1/en/
Summary
The microRNA miR-125b, a conserved lin-4 homolog, is involved in regulating p53 activity and has been found to display mis-regulated expression levels in some cancers. Here, the inventors used the zebrafish model to characterize miR-125b. They found that the 3'UTRs of both human and zebrafish p53 mRNAs contain miR-125b microRNA response elements (MREs). Morpholino targeting of pre-miR-125b in zebrafish embryos resulted, as expected, in a severe neural death phenotype indicative of increased apoptosis. Moreover, they state that both the miR-125b knockdown phenotype and stress-induced apoptosis could be rescued by co-expression of synthetic miR-125b. With an eye to miR-125b as a potential anti-cancer therapeutic target, the inventors claim various methods of regulating apoptosis via modulation of miR-125b.
