Chemical & Pharmaceutical Bulletin 

About: Chemical & Pharmaceutical Bulletin is an academic journal published by Pharmaceutical Society of Japan. The journal publishes majorly in the area(s): Bicyclic molecule & Ring (chemistry). It has an ISSN identifier of 0009-2363. It is also open access. Over the lifetime, 26438 publications have been published receiving 428262 citations.

Two new flavonoids and other constituents in licorice root: their relative astringency and radical scavenging effects.

Abstract: Four compounds, including two new flavonoids, were isolated from Si-pei licorice (licorice from the north-western region of China). The structures of the two new flavonoids, named glycyrrhisoflavanone and glycyrrhisoflavone, were (S)-7, 8'-dihydroxy-2', 2'-dimethyl-5-methoxy-[3, 6'-bi-2H-1-benzopyran]-4(3H)-one (6) and 3-[3, 4-dihydroxy-5-(3-methyl-2-butenyl)phenyl]-5, 7-dihydroxy-4H-1-benzopyran-4-one (9). Glycyrrhisoflavone was found to be one of the tannic substances by the measurement of the binding activity to hemoglobin (relative astringency). Licochalcone B (1) was isolated from the fraction which showed the highest binding activity to hemoglobin among the fractions obtained by centrifugal partition chromatography of the extract of Sinkiang licorice (licorice from Sinkiang in China). Licochalcone B also showed the highest activity as a radical scavenger in the experiment using 1, 1-diphenyl-2-picrylhydrazyl radical, among ten tested compounds obtained from several licorices. The order of the radical scavenging effects was the same as the order of the inhibitory effects on the 5-lipoxygenase-dependent peroxidation in arachidonate metabolism [licochalcone B (1)>licochalcone A (3)>>isoliquiritigenin (14)>liquiritigenin (13)].

Studies on Absorption of Eutectic Mixture. I. A Comparison of the Behavior of Eutectic Mixture of Sulfathiazole and that of Ordinary Sulfathiazole in Man.

Abstract: 1) Sulfathiazole forms eutectic mixtures with urea, l-ascorbic acid, acetamide, nicotinic acid, nicotinamide, or succinimide. It was observed that a eutectic mixture of sulfathiazole and urea produces a microcrystalline suspension of sulfathiazole in water. 2) Sulfathiazole in a eutectic mixture with urea shows higher absorption and excretion after oral administration than ordinary sulfathiazole. 3) Since urea does not possess solubilizing action on sulfathiazole and also it does not enhance absorption of the drug physiologically, the accelerated absorption or excretion must be attributed to the physical state of sulfathiazole in its eutectic mixture with easily soluble compound, such as urea. 4) It is assumed that this new form of preparation will give a means of adjusting therapeutic effect of medical compounds.

Effects of the Interaction of Tannins with Co-existing Substances. VI. : Effects of Tannins and Related Polyphenols on Superoxide Anion Radical, and on 1, 1-Diphenyl-2-picrylhydrazyl Radical

Abstract: The scavenging effects of twenty-five tannins including low-molecular polyphenols on the superoxide anion radical (O2-) generated in the hypoxanthine-xanthine oxidase system were estimated by electron spin resonance (ESR) measurements of the adducts formed by 5, 5-dimethyl-1-pyrroline-N-oxide (DMPO) and the radical. The scavenging effects of tannins and related polyphenols having ortho-trihydroxyl (pyrogallol) structure [galloyl, hexahydroxydiphenoyl (HHDP) groups in hydrolyzable tannins, galloyl group in acylated proanthocyanidins, and the B-ring of some flavan-3-ols] were stronger than the effects of unacylated proanthocyanidins. The effects of tannins and related polyphenols on the superoxide anion radical were also compared with those on the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical. Each tannin in an ethanol solution of DPPH radical reduced the intensity of the signal of the DPPH radical, and gave a weak signal assignable to a radical derived from that tannin, in a similar way to the appearance of the signal of dl-α-tocopherol radical, accompanied with reduction of the signal of DPPH radical, in a mixture of dl-α-tocopherol and the DPPH radical. In contrast to the case of the superoxide anion radical, the effects of unacylated proanthocyanidins on DPPH radical were comparable with those of the other types of tannins. The scavenging effects of all of the tannins and related polyphenols tested in the experiments on DPPH radical were stronger than that of dl-α-tocopherol.

Facile Discrimination of Aldose Enantiomers by Reversed-Phase HPLC

Abstract: One-pot reactions of aldoses with L-cysteine methyl ester and o-tolyl isothiocyanate yielded methyl 2-(polyhydroxyalkyl)-3-(o-tolylthiocarbamoyl)-thiazolidine-4(R)-carboxylates. Direct HPLC analysis of the reaction mixture and UV detection at 250 nm discriminated D- and L-enantiomers of aldoses. The reaction was applied to the determination of absolute configuration the sugar residues of an aroma precursor.

A New Technique to Efficiently Entrap Leuprolide Acetate into Microcapsules of Polylactic Acid or Copoly(Lactic/Glycolic) Acid

Abstract: The aim of this work was to develop injectable microcapsules containing leuprolide acetate, that would deliver that drug at a zero-order rate over a period of about one month. A large amount of leuprolide acetate, a hydrophilic drug, was entrapped into polylactic aicd (PLA) and copoly-(lactic/glycolic) acid (PLGA) microcapsules prepared by an in-water dring method using a (w/o)/w emulsion. The basic techniques were designed to increase the viwcosities of the inner water phase and w/o emulsion. Under the conditions used, it was possible for the drug to be completely entrapped by the microcapsules in the range of 10 to 20% on the basis of the polymer. However, the release profiles of the drug in vitro were inadequate for controlled release for one month.