Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.

Abstract: Compounds useful as immunosuppressive, anti-inflammatory and anticancer agents and methods of their preparation and use are described. The compounds are analogs or derivatives of triptolide and related compounds, modified at the 5- and/or 6-position relative to the naturally occurring compounds.

Abstract: The teachings provided herein generally relate to the preparation and uses of compositions comprising extracts of Astragalus membranaceus. The extracts are prepared from Astragalus membranaceus and can comprise, for example, an acid-modified arabinogalactan protein composition having an arabinose:galactose ratio ranging from about 3.5:1 to about 5.0:1, from about 5% to about 10% rhamnose, from about 15% to about 20% galactose, and from about 10% to about 15% glucose. The compositions can be used in the treatment of idiopathic thrombocytopenic purpura and the formulation of medicaments for such treatments.

Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.

Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C?O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C?O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C?O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: The identification of triptolide target molecules is described. Also described are methods of screening triptolide-related compounds for binding to these molecules, including screening for enhanced and/or selective binding, and expression analysis of the target molecules in normal and in diseased tissue.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2?O (oxo); R2?OH, or, R1 and R2 together=O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.

Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2=O (oxo); R2=OH, or, R1 and R2 together=O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.

Abstract: An acid-modified arabinogalactan protein composition, having an arabinose-galactaose ratio of less than 3.5:1, comprising 5–10% Rha, 20–35% Gal, and less than 5% Glc, prepared from Astragalus membranaceus, is useful for treating a number of conditions. For example, an acid-modified arabinogalactan protein composition having features of the invention is useful for stimulating hematopolesis, inducing the proliferation of megakaryocytes, inducing the maturation of megakaryocytes, and stimulating the production of IL-1?, IL-6, TNF-?, IFN-?, GM-CSF, G-CSF, and neutrophils, and stimulating the action of neutrophils; stimulating the immune and/or hematopoietic system of a mammal suffering from neutropenia, anemia, thrombocytopenia, exposure to cytotoxic agents, exposure to radiation, cachexia, emesis, and drug withdrawal symptoms; and is effective to restore the immune response to infection, in immunosuppressive conditions, and to protect hepatic cells in hepatitis B.

Abstract: Combinations of diterpenoid triepoxides and anti-proliferative agents are used in a combination therapy to treat hyperproliferative disorders. Anti-proliferative agents of interest include agents active in killing tumor cells, as well as immunosuppressants, and a variety of other agents that reduce cellular proliferation in targeted tissues. Synergistic combinations provide for comparable or improved therapeutic effects, while lowering adverse side effects.

Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C?O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C?O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C?O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.

Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.

Abstract: Compounds having the structure I: 1

Abstract: Compounds having the structure I: 1

Abstract: An acid-modified arabinogalactan protein composition, having an arabinose-galactose ratio of less than 3.5:1 or less than 80% of the arabinose:galactose ratio of the arabinogalactan protein component of the composition prior to acid modification, prepared from Astragalus membranaceus, especially from the roots of Atragalus membranaceus, is capable of reconstitution into an aqueous intravenously injectable formulation; and is useful for stimulating hematopoiesis, inducing the proliferation or maturation of megakaryocytes, stimulating the production of IL-1&bgr;, Il-6, TNF-&agr;, IFN-&ggr;, GM-CSF, or G-CSF, stimulating the production or action of neutrophils, treating neutropenia, anemia, or thrombocytopenia, accelerating recovery from exposure (e.g.