Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compounds for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.

Abstract: Method and composition for detecting one or more selected polynucleotide regions in a target polynucleotide. In the method, a mixture of sequence-specific probes are reacted with the target polynucleotide under hybridization conditions, and the hybridized probes are treated to selectively modify those probes which are bound to the target polynucleotide in a base-specific manner. The resulting labeled probes include a polymer chain which imparts to each different-sequence probe, a distinctive ratio of charge/translational frictional drag, and a detectable label. The labeled probes are fractionated by electrophoresis in a non-sieving matrix, and the presence of one or more selected sequences in the target polynucleotide are detected according to the observed electrophoretic migration rates of the labeled probes in a non-sieving medium.

Abstract: The invention is directed to methods to assess connective tissue, especially bone, metabolism in disease or to monitor therapy, which method comprises assessing the levels of native free collagen-derived crosslinks in biological fluids, especially urine. The method can be enhanced by concomitantly determining the levels of an indicator of bone formation in biological fluids of the same individual and assessing the differences between the degradation marker and the formation indicator. Antibodies which are specifically immunoreactive with forms of crosslinks which occur free in biological fluids are also disclosed.

Abstract: The invention is directed to methods to assess connective tissue, especially bone, metabolism in disease or to monitor therapy, which method comprises assessing the levels of native free collagen-derived crosslinks in biological fluids, especially urine. The method can be enhanced by concomitantly determining the levels of an indicator of bone formation in biological fluids of the same individual and assessing the differences between the degradation marker and the formation indicator. Antibodies which are specifically immunoreactive with forms of crosslinks which occur free in biological fluids are also disclosed.

Abstract: A new class of oligonucleotide N3'.fwdarw.P5' phosphoramidates having 2' fluoro substituents are provided that have superior acid stability. The invention includes oligo-2'-fluoronucleotide N3'.fwdarw.P5' phosphoramidates, methods of synthesis, and duplexes and triplexes formed with DNA and RNA. Compounds of the invention are useful where the formation of stable and specific duplex and/or triplex structures is desired, including antisense and/or anti-gene pharmaceuticals, branched DNA components, DNA and/or RNA capture agents, components of DNA-based diagnostic assays, and the like.

Abstract: A method of forming a thiohydantoin from an N-protected amino acid is described. The method employs a phosphate compound selected from the group consisting of(R.sub.1 O)(R.sub.2 O)P(.dbd.O)X and(R.sub.1 O)(R.sub.2 O)P(.dbd.O)--O--P(.dbd.O)(OR.sub.3)(OR.sub.4)to form acylphosphate moieties from the carboxyl groups of internal aspartic acid and glutamic acid residues and an acylphosphate moiety at a C-terminal carboxyl. The later acylphosphate, unlike the internal acylphosphates, spontaneously cyclizes to an oxazolone, which is less reactive with nucleophilic reagents. R.sub.1 and R.sub.2 are each alkyl, aryl, or alkaryl groups which are the same or different and which may be covalently linked to each other; R.sub.3 and R.sub.4 are each alkyl, aryl, or alkaryl groups which are the same or different and which may be covalently linked to each other; and X is a leaving group, such as chlorine or bromine, which is substantially unreactive towards thiohydantoins.

Abstract: Compounds and methods for use in immunosuppressive and anti-inflammatory treatment are described. The compounds are triptolide analogs with improved water solubility and low toxicity.

Abstract: Long wavelength, narrow emission bandwidth fluorecein dyes are provided for detecting spacially overlapping target substances. The dyes comprise 4,7-dichlorofluoresceins, and particularly 2',4',5',7'-tetrachloro-4,7-dichloro-5- (and 6-) carboxyfluoresceins. Methods and kits for using the dyes in DNA analysis are provided.

Abstract: Disclosed is a method of inhibiting hepatitis B infection by administering a therapeutically effective amount of a compound having the formula (Formula 1): ##STR1## wherein R1 is selected from the group consisting of H, lower alkanoyl, lower arylalkylacyl, arylacyl, and C-1-linked saccharide, and R2 is separately selected from the group consisting of H, lower alkyl, lower arylalkyl, aryl, and C-1-linked saccharide. The compounds may also be used to treat other conditions, such as inflammatory bowel disease, autoimmune diseases, transplant rejection, septic shock, and for protection against irradiation damage. Novel celastrol derivatives are also disclosed.

Abstract: An immunosuppressant compound is produced having the structure: ##STR1## or a mirror image thereof, wherein X.sub.1 is 2,2-dimethylvinyl and X.sub.2 and X.sub.3 together are .dbd.CH.sub.2 ; or X.sub.1 is 2,2-dimethyloxiranyl, and X.sub.2 and X.sub.3 together are --0--CH.sub.2 --; or X.sub.1 is 1,2-dihydroxy-2-methyl-propyl, X.sub.2 is --CH.sub.2 OH, and X.sub.3 is OH; or X.sub.1 is 2-hydroxy-2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.2 OH; or X.sub.1 is COOR, and X.sub.2 and X.sub.3 together are .dbd.O, where R is a lower alkyl, phenyl, or benzyl group; or X.sub.1 is 2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.3. The compound can be produced by culturing Fusarium subglutinans f. sp. tripterygii ATCC 74358 isolated from the stems of Tripterygium wilfordii. A pharmaceutical composition for immunosuppression therapy is prepared containing the compound and a pharmaceutically acceptable vehicle.

Abstract: A device for determining size variations of tissue particles. The device includes a light source and an illuminating light guide capable of irradiating light into a human tissue to produce back-scattered light, and at least two receiving light guides at different radial distances from the illuminating light guide, for receiving back-scattered light from the tissue. The device can be used for determining size variations of tissue particles such as mitochondria.

Abstract: A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ").sub.2, where R.sub.1 ' and R.sub.1 " are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

Abstract: A method of assaying bone collagen degradation activity in a human subject. In the method, a human urine sample is reacted with an antibody which (i) is capable of reacting immunospecifically with pyridinium crosslinks selected from the group consisting of native free pyridinoline and native free deoxypyridinoline, and (ii) has a ratio of reactivity toward the selected pyridinium crosslinks and urinary pyridinium peptides larger than 1,000 daltons in molecular weight, of greater than about 5:1. An immunocomplex forms between the antibody reagent and the selected pyridinium crosslinks which are present in the sample, and the amount of immunocomplex is measured. Also disclosed are antibody reagents and kits which can be used in the method.

Abstract: A solid support and method for immobilization and sequence analysis of polypeptides. In one aspect, the invention is directed to a method for immobilizing a polypeptide on a solid support. In the method, a solid support having surface-attached carboxylic acid groups is reacted with an isoxazolium salt to form an activated support. After the activated support has been washed to remove residual isoxazolium salt and base, the support is dried. The dried support is then contacted with a polypeptide under conditions effective to bind the polypeptide covalently to the support. The immobilized polypeptide can be conveniently sequenced by N- and C-terminal sequencing methods.

Abstract: A thin-film magnetic recording disc for use with a read/write head in a disc drive is disclosed. To reduce the static and dynamic frictional coefficients of the disc surface, the disc is coated with a lubricant layer composed of a mixture of a polyphenoxycyclotriphosphazene lubricant and a perfluoropolyether oil. Also disclosed is a lubricant composition containing these two components, as well as a method for improving the lubricating properties of a perfluoropolyether oil.

Abstract: Disclosed is a method for increasing the electro-osmotic flow rate available for a silica surface. In the method, there is provided an electrophoretic channel which is defined by one or more silica surfaces. The surface(s) are contacted with an alkaline aqueous solution containing a solubilized silicate-monovalent metal complex in an amount effective to increase the acidity of the silica surface(s), as evidenced by a reduction in the average bulk pKa of the surface(s). The achieved increase in acidity is greater than would be obtained using an otherwise identical solution lacking said silicate. In one preferred embodiment, the monovalent metal used in the solution is Li.sup.+, Na.sup.+, or K.sup.+. Also disclosed is a method for increasing the acidity of a silica surface, by contacting the surface with an alkaline aqueous solution of the type noted above.

Abstract: A method of inhibiting tumor-cell growth in a mammalian subject, by administering a therapeutically effective amount of a selected 2-phenyl-4-quinolone compound. The selected compound shows unexpectely high activity against a variety of solid tumor cells.

Abstract: A method of treating inflammation in a subject by administering a therapeutically effective amount of a compound having the structure: ##STR1## where R.sub.1 to R.sub.4 are the same or different and are each selected from the group consisting of H, an alkylacyl group, an arylacyl group, or a C-1-linked saccharide.

Abstract: Novel acceptor-donor-acceptor and donor-acceptor-donor compound for use in forming a thermally-stable electro-optic waveguide are disclosed. Also disclosed is a thermally stable waveguide material containing thermally stable acceptor-donor-acceptor or donor-acceptor-donor guest dipole compounds in a temperature-resistant polymer matrix. The waveguide has selected regions in which the net dipoles of the guest molecules are oriented, for electro-optic switching when an electric field is placed across these regions.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.