Abstract: An extract of Graptopetalum paraguayense prepared by a method that includes: extracting a Graptopetalum paraguayense (GP) starting material with an alcoholic solvent to produce an alcoholic extract and a residue; separating the residue from the alcoholic extract; extracting the residue with an aqueous dimethyl sulfoxide (DMSO) solvent to produce a DMSO extract; subjecting the DMSO extract to ultrafiltration using a filter having a selected molecular weight cutoff; drying a fraction retained by the filter to obtain the extract of Graptopetalum paraguayense. Uses of an extract of Graptopetalum paraguayense for the treatment or prevention of liver fibrosis, hepatic cirrhosis, liver cancer, recurrence of liver fibrosis after surgery, or recurrence of liver cancer after surgery.

Abstract: The present invention discloses an anti-human alpha-enolase (ENO1) antibody, which can bind the peptides, comprising amino-acid sequence 296FD Q D D W G A W Q K F TA309 (SEQ ID: #9) and/or 326K R I A K A V N EK S336 (SEQ ID: #10) of human ENO1 protein (GenBank: AAH50642.1), has a favorable binding activity (the binding affinity is around 2.19×10-10 mol/L) and a remarkable capability to inhibit the cell invasion and tumor metastasis of a varied of tumors. The recognized peptides and antibody of the invention are useful for diagnosis, prognosis, and treatment of cancers that have been reported to express cell-surface ENO1 such as including lung, breast, pancreas, liver, colorectal, prostate cancers and solid tumors.

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein G is a heteroaryl, heterocyclic or alkyne; X is N or CH; L1 is —N(R7)—, —O—, —C(S)—, —C(O)—, or —S—; L2 is —N(R8)— or —O—; R1 and R2 are independently hydrogen, halogen, hydroxyl, amino, cyano, nitro, carboxy, C1-C4 alkoxy, C1-C4 alkoxy C1-C4 alkoxy, N,N—(C1-C4 dialkyl)amino C1-C4 alkoxy, N—(C1-C4 alkyl)amino C1-C4 alkoxy, C1-C4 alkanoyl, C1-C4 alkanoyloxy, N—(C1-C4 alkyl)amino, N,N—(C1-C4 dialkyl)amino, C1-C4 alkanoyl amino, or heterocyclyl, wherein C1-C4 alkyl is optionally substituted with one or more substituents selected from fluorine and chlorine; R3, R4 and R5 are independently hydrogen, fluorine or chlorine; R6 is C1-C4 alkyl or aryl, which is optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, cyano, nitro; or R6 and R8 form a 5-6 membered cyclyl or heterocyclyl.

Abstract: The present invention relates to a plant extract for treating diabetes and a process for making same. The plant extract of the invention is prepared from an overground part of Hedychium coronarium Koenig, which has the efficacies of lowering blood glucose, increasing insulin levels, reducing insulin resistance and treating and/or preventing diabetes without overly reducing blood glucose in a subject, i.e., not reducing blood glucose in a fasting subject. Also provided herein is a method for treating diabetes in a subject in need thereof comprising administering an effective amount of the plant extract to the subject.

Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.

Abstract: This invention relates to bispecific antibodies having combinations of linker and hinge sequences to create linker-hinge interface domains with biological significance. Such linker-hinge interface domains covalently join two molecules, maintain the biological activities of linked molecules (target binding), stabilize the biological characteristics of new molecule (solubility and 4° C. stability), maintain the chemical, biochemical and physical properties (cytotoxicity) of the linked molecules, and modulate the biological characteristics of the linked molecules (activating T-lymphocytes without significant sign of proliferations). Both linker (GGGGS) and hinge (CPPCP) sequences are required to establish functional linker-hinge interface domains as deletion of any of the component resulted in significant lost of T-lymphocyte mediated activity.

Abstract: A method for treating cancer includes administering to a subject in need thereof an antibody against a transmembrane and coiled-coil domains protein 3 (TMCC3), wherein the antibody binds to an epitope in an extracellular domain of TMCC3. The antibody binds to an epitope in an intercoil domain of TMCC3. A method of diagnosing or assessing a cancer condition includes assessing a level of expression or activity of a transmembrane and coiled-coil domains protein 3 (TMCC3) in a sample, wherein an increase in the level of expression of activity of TMCC3 as compared to a standard indicates the presence of cancer stem cells in the sample.

Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.

Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.

Abstract: The main goals of the invention are to develop the long-term release of Granisetron injection implant composition with biodegradable polymer and to develop relative processing. Granisetron is mixed with different biodegradable polymers, and then hot melt extrusion technique with different diameter, temperature, rate of extrusion and holding time is applied to make implant. In vitro dissolution of the Granisetron injection implant composition shows the component continued release of the drug for over 7 days.

Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRaRb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.

Abstract: An anti-granulysin antibody, or an scFv or Fab fragment thereof, capable of binding to an epitope region from R64 to R113 of granulysin and capable of neutralizing an activity of granulysin. The antibody may contain a sequence selected from the sequences of SEQ ID NO:82 to SEQ ID NO:195, or the antibody may contain a sequence selected from the sequences of SEQ ID NO:39 to SEQ ID NO:76. The antibody may be a monoclonal antibody. A method for treating or preventing an unwanted immune response disorder includes administering to a subject in need thereof an effective amount of an anti-granulysin antibody capable of neutralizing the activity of granulysin. The unwanted immune response disorder may be SJS, TEN, or GVHD.

Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.

Abstract: A compound for controlling blood glucose level has a structure shown in Formula I: wherein R5-R8 are as defined herein. A method for controlling blood glucose level includes administering to a subject in need thereof a compound of Formula I. The method further includes administering to the subject a GLP-1 receptor ligand. The compound and the GLP-1 receptor ligand may be administered together. The compound may be Galanal A or Galanal B. The GLP-1 receptor ligand may be GLP-1 or exendin-4.

Abstract: The present invention provides a process for the preparation of Plectranthus amboinicus extracts using a stirring separation method. The present invention also relates to a pharmaceutical composition comprising the Plectranthus amboinicus crude extract and/or extract for treating skin disorders, including enhancing the healing of wounds, especially in diabetic patients.

Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.

Abstract: This invention describes a novel format of monomeric bispecific fusion protein with immune activating property for clinical therapies. A bispecific fusion protein includes a first targeting domain with a specificity for a first target of interest; a bridging domain derived from a constant region of a light chain or heavy chain of an immunoglobulin, which may be a human immunoglobulin; and a second targeting domain with a specificity for a second target of interest. The bispecific fusion protein may further include a linker fused to the N-terminus or the C-terminus of the bridging domain. The first targeting domain is fused to the bridging domain and the second targeting domain is fused to the bridging domain or the linker. The linker may include a GGGGS sequence. The first target of interest may be CD20, Her2/neu, or EpCAM, and the second targeting domain is a T-lymphocyte activating domain.

Abstract: This invention relates to bispecific antibodies having combinations of linker and hinge sequences to create linker-hinge interface domains with biological significance. Such linker-hinge interface domains covalently join two molecules, maintain the biological activities of linked molecules (target binding), stabilize the biological characteristics of new molecule (solubility and 4° C. stability), maintain the chemical, biochemical and physical properties (cytotoxicity) of the linked molecules, and modulate the biological characteristics of the linked molecules (activating T-lymphocytes without significant sign of proliferations). Both linker (GGGGS) and hinge (CPPCP) sequences are required to establish functional linker-hinge interface domains as deletion of any of the component resulted in significant lost of T-lymphocyte mediated activity.

Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRa Rb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.

Abstract: The present invention provides a process for the preparation of Plectranthus amboinicus extracts using a stirring separation method. The present invention also relates to a pharmaceutical composition comprising the Plectranthus amboinicus crude extract and/or extract for treating skin disorders, including enhancing the healing of wounds, especially in diabetic patients.