Chemical and Pharmaceutical Bulletin
The Pharmaceutical Society of Japan, established in 1880, is one of Japan’s oldest and most distinguished academic societies. The Society currently has around 18,000 members. It publishes three monthly scientific journals. Chemical and Pharmaceutical Bulletin (Chem. Pharm. Bull.) began publication in 1953 as Pharmaceutical Bulletin. It covers chemistry fields in the pharmaceutical and health sciences. Biological and Pharmaceutical Bulletin (Biol. Pharm. Bull.) began publication in 1978 as the Journal of Pharmacobio-Dynamics. It covers various biological topics in the pharmaceutical and health sciences. A fourth Society journal, the Journal of Health Science, was merged with Biol. Pharm. Bull. in 2012. Yakugaku Zasshi (Japanese for “Pharmaceutical Science Journal”) has the longest history, with publication beginning in 1881. Yakugaku Zasshi is published mostly in Japanese, except for some articles related to clinical pharmacy and pharmaceutical education, which are published in English.
The main aim of the Society’s journals is to advance the pharmaceutical sciences with research reports, information exchange, and high-quality discussion. The average review time for articles submitted to the journals is around one month for first decision. The complete texts of all of the Society’s journals can be freely accessed through J-STAGE. The Society’s editorial committee hopes that the content of its journals will be useful to your research, and also invites you to submit your own work to the journals.

Chairman of Committee
Ken-ichi Hosoya
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama

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26,996 registered articles
(updated on July 28, 2017)
Online ISSN : 1347-5223
Print ISSN : 0009-2363
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Volume 65 (2017) Issue 7 Pages 605-610
Potential of Enzymomics Methodologies to Characterize Disease-Related Protein Functions

Enzymatic functions are often altered during disease onset and progression, and therefore chemical–biological studies, which utilize chemical knowledge to discover novel protein functions, are often employed to find proteins with functions closely related to disease phenotypes. Such studies are known as forward chemical–biological approaches and form part of the emerging field of enzymomics (omics of enzymes). This review provides an overview of methodologies available for discovering and characterizing disease-related alterations of enzymatic functions and prospects for the future.

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Editor’s picks

Cellular functions are mediated by a great variety of enzymes, and altered enzymatic functions are often observed during disease onset and progression. Therefore, discovering the novel connection between the functions of enzymes and specified diseases is the key to developing novel diagnostic methods, as well as therapeutic drugs.  In this review, we describe the recently advancing field of chemical biology that aims to discover and characterize disease-related alternation of enzymatic functions, which can be termed as “enzym-omics (omics of enzymes)”.  The review covers several key technologies that can be considered as the representative experimental systems used for this purpose.  

Volume 65 (2017) Issue 6 Pages 511-523
Creation of Novel Cyclization Methods Using sp-Hybridized Carbon Units and Syntheses of Bioactive Compounds

Some recent results on the development of new and reliable procedures for the construction of diverse ring systems based on the chemistry of sp-hybridized species, especially allene functionality, are described. This review includes: (i) synthesis of the multi-cyclic skeletons by combination of the π-component of allene with suitable other π-components such as alkyne, alkene, or additional allene under Rh-catalyzed conditions; (ii) synthesis of heterocycles as well as carbocycles by reaction of the sp-hybridized center of allene with some nucleophiles in an endo-mode manner; and (iii) total syntheses of natural products and related compounds from the sp-hybridized starting materials.

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In this review, new and reliable procedures for the construction of diverse ring systems based on the chemistry of sp-hybridized species are described. The synthetic application includes (i) multi-cyclic skeletons by the Rh-catalyzed reaction of allenes with other π-components such as alkyne, alkene, and allene, (ii) hetero- and carbocycles from appropriate allenes and nucleophiles, and (iii) natural products and related compounds.

Volume 65 (2017) Issue 5 Pages 409-425
Palladium(0)-Catalyzed Benzylic C(sp3)–H Functionalization for the Concise Synthesis of Heterocycles and Its Applications

C–H functionalization reactions involve the activation of otherwise unreactive C–H bonds, and represent atom economical methods for the direct transformation of simple substrates to complex molecules. While transition metal-catalyzed C(sp2)–H functionalization reactions are regularly used in synthesis, C(sp3)–H functionalization is rarely applied to the synthesis of complex natural products because of the difficulties associated with controlling selectivity. With this in mind, we focused on the development of new palladium (Pd)(0)-catalyzed C(sp3)–H functionalization reactions for the synthesis of complex molecules, resulting in several new methods capable of solving these problems. We initially developed a concise synthetic method for the facile construction of oxindoles and spirooxindoles via a Pd-catalyzed benzylic C(sp3)–H functionalization reaction. This method was subsequently extended to the synthesis of various heterocycles, including 2-arylindoles, benzocarbazole, indolocarbazole, indoloquinazolinone, and indoloquinazolinedione, as well as the total synthesis of several pyrrolophenanthridine alkaloids without the need for any protecting groups. This method was also successfully applied to the synthesis of the right-hand fragment of benzohopane from tetrahydro-2H-fluorene, which was constructed by a Pd-catalyzed benzylic C(sp3)–H functionalization. In this review, we provide a detailed discussion of our most recent investigations pertaining to Pd(0)-catalyzed benzylic C(sp3)–H functionalization.

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Editor’s picks

This review summarizes author’s recent reports on Pd(0)-catalyzed benzylic C(sp3)-H functionalization for the synthesis of various heterocycles including oxindoles, spirooxindoles, 2-arylindoles, benzocarbazoles, indolocarbazoles, and indoloquinazolinones. The key feature would be a chemoselective C(sp3)-H activation in the oxindole synthesis. The developed method was successfully applied to the total synthesis of several pyrrolophenanthridine alkaloids as well as a synthesis of the right-hand fragment of benzohopane.

Volume 65 (2017) Issue 4 Pages 356-358
Alternative Formation of Red-Shifted Channelrhodopsins: Noncovalent Incorporation with Retinal-Based Enamine-Type Schiff Bases and Mutated Channelopsin

Red-shifted channelrhodopsins (ChRs) are attractive for optogenetic tools. We developed a new type of red-shifted ChRs that utilized noncovalent incorporation of retinal and 3,4-dehydroretinal-based enamine-type Schiff bases and mutated channelopsin, C1C2-K296G. These ChRs exhibited absorption maxima that were shifted 10–30 nm toward longer wavelengths than that of C1C2-ChR regenerated with all-trans-retinal.

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In this communication, development of a new type of red-shifted channelrhodopsins (ChRs) is described. Optogenetics is a powerful new technique which allows control of neuronal activity by light, and ChRs are now widely used in optogenetics due to their function of a light-gated cation channel. In neuroscience, ChRs responding to a long-wavelength light are eagerly required, because ChRs now used are maximally sensitive to green and blue light, and does not penetrate tissues. Here developed new type of ChRs model consisted of red-shifted chromophores (retinal-based enamine-type Schiff bases) and mutated channelopsin (C1C2-K296G), in which chromophores were incorporated noncovalently. Thus prepared new ChRs exhibited absorption maxima that were 10-30 nm red-shifted compared with the original C1C2.

Volume 65 (2017) Issue 3 Pages 268-275
Adsorption Capability of Cationic Dyes (Methylene Blue and Crystal Violet) onto Poly-γ-glutamic Acid

In this study, the adsorption capability of cationic dyes, which were methylene blue and crystal violet, by poly-γ-glutamic acid (PGA) in a single or binary solution system was investigated. The effect of the molecular weight of PGA, initial dye concentration, solution pH, and temperature on the adsorption of dyes was evaluated. The adsorption mechanism of dyes onto PGA was the interaction between –COOH group on the PGA surface and the polarity groups of dyes. These results indicated that PGA is useful for removal of dyes and cationic organic compounds from a single or binary solution system.

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Editor’s picks

In this paper, the adsorption capacity of methylene blue (MB) and crystal violet (CV) to poly-γ-glutamic acid (PGA) is described. PGA contained in natto (Japanese traditional fermented food) is a homopolyamide having bonds between α-amino and γ-carboxy groups of D- and L-glutamic acid monomers. The removal rate of MB or CV by PGA was 94.6 to 100% after 120 min. In addition, PGA has a dye adsorption capacity in a binary solution system. The results of this study indicate that PGA is useful for removing dyes from aqueous solutions.

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