Abstract: The present invention relates to anti-cancer agents comprising 1,2,4-trioxane compounds and anti-cancer agents comprising combinations comprising 1,2,4-trioxane compounds and chlorogenic acids. The invention further provides pharmaceutical compositions comprising such anti-cancer agents, kits comprising the same as well as methods and treatment regimens of using the aforementioned anti-cancer agents, pharmaceutical compositions and kits in the treatment and prevention of cancer and for prolonging survival of subjects having cancer, in particular ovarian cancer or lung cancer.

Abstract: The present invention relates to conjugates of amphotericin B and gold nanoparticles stabilized with thiohexoses or thiopentoses, and a method to produce said nanoparticles. As the conjugates of amphotericin B to the stabilized gold nanoparticles show several advantages over amphotericin B alone, the present invention is also directed to pharmaceutical compositions comprising said nanoparticles, and to their use for treat fungal and leishmanial infection. These amphotericin B stabilized gold nanoparticles are dispersible in water and are not toxic for mammalian cells differently from free amphotericin B and other currently used amphotericin B preparations. Importantly, the conjugates of amphotericin B and stabilized gold nanoparticles are more efficacious in treating all forms of Cryptococcal infections (planktonic, intracellular and biofilms) than amphotericin B. Additionally, the conjugates are more effective against extracellular and intracellular forms of Leishmania mexicana and Leishmania major.

Abstract: The present invention relates to antiviral 1,2,4-trioxane compounds and compositions comprising the same that are effective inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication, and are thus useful to treat the coronavirus disease 2019 (COVID-19). The invention further provides pharmaceutical compositions containing such antiviral compounds and antiviral compositions, and methods of using these antiviral compounds, antiviral compositions and pharmaceutical compositions in the treatment and prevention of COVID-19.

Abstract: The present disclosure discloses the chemical synthesis method of the Plesiomonas shigelloides serotype O51 O-antigen oligosaccharide, belonging to the field of chemistry. Source-abundant D-glucose, L-fucose, D-glucosamine and the like are used as raw materials to prepare three glycosylation building blocks, the synthetic route composed of 11 reaction modules is designed, and through the optimization of protecting group and the optimization of the time of introducing functional group, the preparation of the target oligosaccharide chain is successfully achieved. The oligosaccharide chain prepared in the present disclosure has the advantages of cheap and easy-to-get raw materials, and simple and easy-to-repeat preparation method. The present disclosure will have good application prospects in the aspects of development of new drugs and vaccines of Plesiomonas shigelloides, and the like.

Abstract: The disclosure discloses a preparation method of outer core octasaccharide of Helicobacter pylori lipopolysaccharide, and belongs to the field of carbohydrate chemistry. The structure of the outer core octasaccharide of Helicobacter pylori is (?-D-Glc-(1-3)-?-D-Glc-(1-4)-?-D-Gal-(1-7)-D-?-D-Hep[?-D-Glc-(1-6)-?-D-Glc-(1-6)-?-D-Glc-(1-2)-D-?-D-Hep]-Linker. The structure consists of three monosaccharides: glucose, galactose and heptose. It contains five ?-glycosidic bonds of glucose, one ?-glycosidic bond of galactose and two ?-glycosidic bonds of heptose. The disclosure prepares the octasaccharide by the synergistic action of remote neighboring group participation effect, solvent effect, temperature effect, additives and leaving groups. The reducing end of the octasaccharide may also be linked with a linker for future attachment to the protein to form a glycoconjugate for immunological studies.

Abstract: The present disclosure discloses an integrated nano system for liver-targeting co-delivery of genes/drugs and a preparation method, belonging to the field of biomedicines. In the disclosure, a plurality of functions are integrated in a carrier having good biocompatibility and safety, a nucleic acid/drug-loading copolymer portion having a pH-stimulating response function is formed by poly(N,N-dimethylaminoethyl methacrylate) (PDMAEMA) grafted with poly(3-azido-2-hydroxypropylmethacrylate) (PGMA-N3), and a fluorescence-based imaging component Rhodamine B (RhB) and galactose are used as targeting ligands. The drug delivery system provided by the present disclosure is safe, is capable of taking a synergistic effect of gene/drug therapy, and is expected to play a great role in clinical application.

Abstract: The present disclosure discloses the chemical synthesis method of the Plesiomonas shigelloides serotype O51 O-antigen oligosaccharide, belonging to the field of chemistry. Source-abundant D-glucose, L-fucose, D-glucosamine and the like are used as raw materials to prepare three glycosylation building blocks, the synthetic route composed of 11 reaction modules is designed, and through the optimization of protecting group and the optimization of the time of introducing functional group, the preparation of the target oligosaccharide chain is successfully achieved. The oligosaccharide chain prepared in the present disclosure has the advantages of cheap and easy-to-get raw materials, and simple and easy-to-repeat preparation method. The present disclosure will have good application prospects in the aspects of development of new drugs and vaccines of Plesiomonas shigelloides, and the like.

Abstract: The present invention relates to a method for determining in an expedient manner and with minimal sample consumption the structure of an unknown carbohydrate by using ion mobility-mass spectrometry (IM-MS) in negative ionization mode and fragmentation and a database containing structures of carbohydrates and/or of the fragments of the negative ions of carbohydrates, and for each of the structures of the target carbohydrates the collision cross section value and the mass-to-charge ratio value of the negative ion thereof, and for each of the structures of the fragments of the negative ions of the target carbohydrates the collision cross section value and the mass-to-charge ratio value of the fragment of the negative ion of the target carbohydrate.

Abstract: The disclosure discloses a preparation method of outer core octasaccharide of Helicobacter pylori lipopolysaccharide, and belongs to the field of carbohydrate chemistry. The structure of the outer core octasaccharide of Helicobacter pylori is (?-D-Glc-(1-3)-?-D-Glc-(1-4)-?-D-Gal-(1-7)-D-?-D-Hep[?-D-Glc-(1-6)-?-D-Glc-(1-6)-?-D-Glc-(1-2)-D-?-D-Hep]-Linker. The structure consists of three monosaccharides: glucose, galactose and heptose. It contains five ?-glycosidic bonds of glucose, one ?-glycosidic bond of galactose and two ?-glycosidic bonds of heptose. The disclosure prepares the octasaccharide by the synergistic action of remote neighboring group participation effect, solvent effect, temperature effect, additives and leaving groups. The reducing end of the octasaccharide may also be linked with a linker for future attachment to the protein to form a glycoconjugate for immunological studies.

Abstract: The present disclosure discloses an integrated nano system for liver-targeting co-delivery of genes/drugs and a preparation method, belonging to the field of biomedicines. In the disclosure, a plurality of functions are integrated in a carrier having good biocompatibility and safety, a nucleic acid/drug-loading copolymer portion having a pH-stimulating response function is formed by poly(N,N-dimethylaminoethyl methacrylate) (PDMAEMA) grafted with poly(3-azido-2-hydroxypropylmethacrylate) (PGMA-N3), and a fluorescence-based imaging component Rhodamine B (RhB) and galactose are used as targeting ligands. The drug delivery system provided by the present disclosure is safe, is capable of taking a synergistic effect of gene/drug therapy, and is expected to play a great role in clinical application.

Abstract: The present invention relates to a method for determining in an expedient manner and with minimal sample consumption the structure of an unknown carbohydrate by using ion mobility-mass spectrometry (IM-MS) in negative ionization mode and fragmentation and a database containing structures of carbohydrates and/or of the fragments of the negative ions of carbohydrates, and for each of the structures of the target carbohydrates the collision cross section value and the mass-to-charge ratio value of the negative ion thereof, and for each of the structures of the fragments of the negative ions of the target carbohydrates the collision cross section value and the mass-to-charge ratio value of the fragment of the negative ion of the target carbohydrate.

Abstract: A process for the preparation of polymer lattices comprising polymer nanoparticles by a photo-initiated heterophase polymerization includes preparing a heterophase medium comprising a dispersed phase and a continuous phase and at least one of at least one surfactant, at least one photoinitiator, and at least one polymerizable monomer. The at least one polymerizable monomer is polymerized by irradiating the heterophase medium with electromagnetic radiation so as to induce a generation of radicals. The at least one photoinitiator is selected from compounds comprising at least one phosphorous oxide group (P?O) or at least one phosphorous sulfide (P?S) group. The irradiating of the heterophase medium is effected so that a ratio of an irradiated surface of the heterophase medium to a volume of the heterophase medium is at least 200 m?1.

Abstract: A process for the preparation of modified polymers by a photo-initiated polymerization includes preparing a polymerization medium comprising at least one photoinitiator comprising at least one phosphorous oxide (P?O) group or at least one phosphorous sulfide (P?S) group, and at least one polymerizable monomer. The at least one polymerizable monomer is polymerized by irradiating the polymerization medium with electromagnetic radiation so as to induce a generation of radicals so as to obtain a polymer. The polymer is modified by irradiating the polymer with electromagnetic radiation so as to induce a generation of radicals from the polymer in a presence of at least one modifying agent.

Abstract: A process for the preparation of polymer lattices comprising polymer nanoparticles by a photo-initiated heterophase polymerization includes preparing a heterophase medium comprising a dispersed phase and a continuous phase and at least one of at least one surfactant, at least one photoinitiator, and at least one polymerizable monomer. The at least one polymerizable monomer is polymerized by irradiating the heterophase medium with electromagnetic radiation so as to induce a generation of radicals. The at least one photoinitiator is selected from compounds comprising at least one phosphorous oxide group (P?O) or at least one phosphorous sulfide (P?S) group. The irradiating of the heterophase medium is effected so that a ratio of an irradiated surface of the heterophase medium to a volume of the heterophase medium is at least 200 m?1.

Abstract: A process for the preparation of modified polymers by a photo-initiated polymerization includes preparing a polymerization medium comprising at least one photoinitiator comprising at least one phosphorous oxide (P?O) group or at least one phosphorous sulfide (P?S) group, and at least one polymerizable monomer. The at least one polymerizable monomer is polymerized by irradiating the polymerization medium with electromagnetic radiation so as to induce a generation of radicals so as to obtain a polymer. The polymer is modified by irradiating the polymer with electromagnetic radiation so as to induce a generation of radicals from the polymer in a presence of at least one modifying agent.

Abstract: The present invention generally relates to compositions comprising antigen-carbohydrate conjugates and methods of immune modulation featuring these reagents.

Abstract: The present invention generally relates to compositions comprising antigen-carbohydrate conjugates and methods of immune modulation featuring these reagents.

Abstract: One aspect of the present invention relates to an apparatus for the efficient synthesis of oligosaccharides on a solid support, e.g., formed by subunit addition to terminal subunits immobilized on solid-phase particles. In certain embodiments, the apparatus of the present invention is used in combinatorial methods, e.g., as described herein, of synthesizing oligosaccharides.

Abstract: The present invention generally relates to organic polymers able to participate in an analyte-recognition process, where an analyte facilitates an energy transfer between an energy donor and an energy acceptor. Certain embodiments of the invention make use of fluorescent conjugated polymers, such as poly(phenylene ethynylene)s and other polymers comprising pi-conjugated backbones. For example, one aspect of the invention provides a fluorescent conjugated polymer and an indicator that can interact with each other in the presence of an analyte to produce an emissive signal. In some cases, the interaction may include energy exchange mechanisms, such as Dexter energy transfer or the strong coupling effect. The interaction of the conjugated polymer and the indicator, in some instances, may be facilitated through specific interactions, such as a protein/carbohydrate interaction, a ligand/receptor interaction, etc.

Abstract: One aspect of the present invention relates to solution-phase approaches to GPI synthesis. Another aspect of the present invention relates to key building blocks, and syntheses thereof, useful for GPI assembly. Yet another aspect of the invention relates to an automated method for the synthesis of GPIs and fragments thereof.