Efficacy of 3% diquafosol long-acting eye drops in dry eye patients treated for three months.

Purpose: To investigate changes in the ocular surface and subjective symptoms during a three months administration of 3% diquafosol long-acting (DQL) eye drops.

Study Design: Prospective observational study.

Methods: DQL eye drops were administered as the sole treatment for all patients, including those in the group where DQL eye drops were newly prescribed (New DQL) and the group who switched from 3% diquafosol (DQS) eye drops (Switched DQL) in this prospective study.

Gualamycin, a novel acaricide produced by Streptomyces sp. NK11687. II. Structural elucidation.

A novel acaricide, gualamycin was isolated from the culture broth of Streptomyces sp. NK11687. The structure of gualamycin was determined to be (2R,3S,4S)-2-O-[4-O-(2-amino-2-deoxy-beta-D-gulopyranosyl)-alpha-D - galactopyranosyl]-2,3,4-trihydroxy-4-[(2S,3S,4S,5S)-3,4-dihydroxy-5-hydr oxy - methylpyrrolidin-2-yl] butanoic acid by FAB-MS, 1H and 13C NMR, COSY, HMQC, HMBC, IR, X-ray crystallographic analyses and synthetic studies.

Pironetin, a novel plant growth regulator produced by Streptomyces sp. NK10958. II. Structural elucidation.

A novel plant growth regulator, pironetin was isolated from the culture broth of Streptomyces sp. NK10958. The structure of pironetin was determined to be (5R,6R)-5-ethyl- 5,6-dihydro-6-[(E)-(2R,3S,4R,5S)-2-hydroxy-4-methoxy-3,5-dimethyl-7- nonenyl]-2H-pyran-2-one by FAB-MS, 1H and 13C NMR, COSY, COLOC, DEPT, IR, X-ray crystallographic analyses and adapted Mosher's method.

Structures and solid state tautomeric forms of two novel antileukemic tropoloisoquinoline alkaloids, pareirubrines A and B, from Cissampelos pareira.

Two novel tropoloisoquinoline alkaloids, Pareirubrines A and B, have been isolated as antileukemic substances from Cissampelos pareira (Menispermaceae), together with the same skeleton alkaloids, grandirubrine and isoimerubrine. Their structures were elucidated by nuclear magnetic resonance (NMR) studies, and their solid state tautomeric forms were examined by X-ray crystallographic analysis.

Reactions of vitamin E and its model compound 2,2,5,7,8-pentamethylchroman-6-ol with ozone.

Reaction of vitamin E [(R,R,R)-alpha-tocopherol] with ozone in acetonitrile yielded alpha-tocopheryl quinone and its precursor 8a-hydroxytocopherone, which accounted for approximately 30% of the products at < 50% alpha-tocopherol oxidation. In addition, two novel products were identified as epimers of 10-acetyl-7-(4',8',12'-trimethyltridecyl)-3,4,7-trimethyl-2-oxo- 1,6-dioxaspiro[4.5]-deca-3,9-diene.

Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. II. Structure determination of benastatins A and B.

Benastatins A and B, new inhibitors of glutathione S-transferase, have been isolated from the culture broth of Streptomyces sp. MI384-DF12. By X-ray crystallography, benastatin A was determined to be 8,13-dihydro-1,7,9,11-tetrahydroxy-13-dimethyl-8-oxo-3-pentyl- benzo[a]naphthacene-2-carboxylic acid.

Biologically active constituents of Magnolia salicifolia: inhibitors of induced histamine release from rat mast cells.

The extracts of the flower buds of Magnolia salicifolia showed remarkable anti-allergy effects in passive cutaneous anaphylaxis (PCA) test. The bioactive constituents of this medicinal drug were isolated by monitoring their activities with an in vitro bioassay system measuring inhibitory effects on induced histamine release from rat mast cells. Of the ten isolated compounds magnosalicin is a new compound of neolignan structure.

Biologically active constituents of Arnebia euchroma: structures of new monoterpenylbenzoquinones: arnebinone and arnebifuranone.

Two quinonic compounds, arnebinone and arnebifuranone, were isolated from the roots of Arnebia euchroma and their structures were elucidated on the basis of spectral evidence. Arnebionone is a monoterpenyl-benzoquinone in which the monoterpene moiety forms a fused ring to the benzoquinone. Arnebifuranone is another monoterpenylbenzoquinone with a furan ring containing side chain which is bonded to the benzoquinone at the head carbon of C10 moiety originating from the geranyl moiety of geranylhydroquinone.

Biologically active constituents of Arnebia euchroma: structure of arnebinol, an ansa-type monoterpenylbenzenoid with inhibitory activity on prostaglandin biosynthesis.

Three phenolic compounds were isolated from the roots of Arnebia euchroma as inhibitors of in vitro prostaglandin biosynthesis. Two known compounds were identified as shikonofurans and des-O-methyllasiodiplodin. The other new compound was named arnebinol and its structure was elucidated as a novel ansa-type monoterpenylbenzenoid derivative.

New antitumor principles, casearins A-F, for Casearia sylvestris Sw. (Flacourtiaceae).

New antitumor clerodane diterpenes, named casearins A-F, have been isolated from the leaves of Casearia sylvestris Sw. (Flacourtiaceae). These structures have been completely elucidated by two dimensional nuclear magnetic resonance, circular dichroism spectroscopy, X-ray analysis, and chemical evidences.

Production, isolation and structure determination of a novel beta-glucosidase inhibitor, cyclophellitol, from Phellinus sp.

In the course of our screening of beta-glucosidase inhibitor, a culture filtrate of a mushroom, Phellinus sp. strongly inhibited the enzyme activity. The active substance was isolated through charcoal separation, column chromatography and crystallization.

Structure of strychnine hydrochloride sesquihydrate.

C21H23N2O2+.Cl-.1.

Altemicidin, a new acaricidal and antitumor substance. II. Structure determination.

The structure of altemicidin, a new acaricidal and antitumor agent, was determined to be (1R,2S,3aR,7aS)-4-carbamoyl-2-hydroxy-6-methyl-1-(sulfamo ylacetamido)-2,3,3a,6, 7,7a-hexahydro-6-azaindene-1-carboxylic acid by a combination of spectroscopic and X-ray crystallographic analysis of its derivatives. Altemicidin is a monoterpene alkaloid.

Structure of thiolactomycin.

[4R,(2E,5E)]-3-Hydroxy-2,4,6-trimethyl-2,5,7-octatriene-4-thiol ide, C11H14O2S, Mr = 210.30, hexagonal, P6(5), a = b = 9.8514 (6), c = 19.

Thrazarine, a new antitumor antibiotic. II. Physico-chemical properties and structure determination.

A new antitumor antibiotic thrazarine was soluble in water and positive to anisaldehyde-sulfuric acid and ninhydrin color reactions. The absolute structure of thrazarine was determined to be O-[3R)-2-diazo-3-hydroxybutyryl)-L-serine by acid hydrolysis, spectroscopic analysis and X-ray crystallographic analysis. Structurally, thrazarine was a new member of azaserine group antibiotics.

Structure of a modified cytosine: an antiviral nucleoside analog, homo-Ara-C.

Homo-Ara-C [5'-(hydroxymethyl)-5'-deoxy-1-beta-D-arabinofuranosyl-3H- cytosine], C10H16N3O5, Mr = 258.25, P2,2,2, a = 8.261 (2), b = 19.

A receptor model for tumor promoters: rational superposition of teleocidins and phorbol esters.

Four 12-O-tetradecanoyl-13-O-acetylphorbol-type tumor promoters--teleocidin, phorbol ester, aplysiatoxin, and ingenol ester--are superposed in an attempt to understand their common biological activity on the assumption that they may bind to the same receptor site. A method using three-dimensional computer graphics was applied for superposing molecules and receptor mapping. The main feature of the method is that molecules are superposed in terms of spatial arrangement of physical and chemical properties but not in terms of the atomic positions as in conventional methods.

Bisucaberin, a new siderophore, sensitizing tumor cells to macrophage-mediated cytolysis. II. Physico-chemical properties and structure determination.

The structure of bisucaberin, a new siderophore, was determined to be 1,12-dihydroxy-1,6,12,17-tetraazacyclodocosane-2,5,13,16-tetron e by spectroscopic analysis and X-ray crystallographic analysis. The molecule of bisucaberin consists of a cyclic dimer of 1-hydroxy-1,6-diazaundecane-2,5-dione moiety and is closely related to nocardamine, the trimer of the same moiety.

A method for fast energy estimation and visualization of protein-ligand interaction.

A new computational and graphical method for facilitating ligand-protein docking studies is developed on a three-dimensional computer graphics display. Various physical and chemical properties inside the ligand binding pocket of a receptor protein, whose structure is elucidated by X-ray crystal analysis, are calculated on three-dimensional grid points and are stored in advance. By utilizing those tabulated data, it is possible to estimate the non-bonded and electrostatic interaction energy and the number of possible hydrogen bonds between protein and ligand molecules in real time during an interactive docking operation.