Chemical & pharmaceutical bulletin最新文献_第9页

Nucleophilic Deprotection of p-Methoxybenzyl Ethers Using Heterogeneous Oxovanadium Catalyst. 使用异质氧化钒催化剂对甲氧基苄基醚进行亲核脱保护。

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c23-00897

Rei Ikeda, Tomoya Nishio, Kyohei Kanomata, Shuji Akai

引用次数: 0

Controlled Release of Lysozyme Using Polyvinyl Alcohol-Based Polymeric Nanofibers Generated by Electrospinning. 利用电纺丝生成的聚乙烯醇基聚合物纳米纤维控制溶菌酶的释放。

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00024

Riho Ogawa, Kouji Hara, Ayaka Kobayashi, Nobuyoshi Yoshimura, Yutaka Taniguchi, Eriko Yamazoe, Takaaki Ito, Kohei Tahara

{"title":"Controlled Release of Lysozyme Using Polyvinyl Alcohol-Based Polymeric Nanofibers Generated by Electrospinning.","authors":"Riho Ogawa, Kouji Hara, Ayaka Kobayashi, Nobuyoshi Yoshimura, Yutaka Taniguchi, Eriko Yamazoe, Takaaki Ito, Kohei Tahara","doi":"10.1248/cpb.c24-00024","DOIUrl":"10.1248/cpb.c24-00024","url":null,"abstract":"Polymeric nanofibers generated via electrospinning offer a promising platform for drug delivery systems. This study examines the application of electrospun polyvinyl alcohol (PVA) nanofibers for controlled lysozyme (LZM) delivery. By using various PVA grades, such as the degree of polymerization/hydrolysis, this study investigates their influence on nanofiber morphology and drug-release characteristics. LZM-loaded PVA monolithic nanofibers having 50% drug content exhibit efficient entrapment, wherein rapid dissolution is achieved within 30 min. The initial burst of LZM from the nanofiber was reduced as the LZM content was lowered. The initial dissolution is greatly influenced by the choice of PVA grade used; fully hydrolyzed PVA nanofibers demonstrate controlled release due to the reduced water solubility of PVA. Furthermore, coaxial electrospinning, which creates core-shell nanofibers with polycaprolactone as a controlled release layer, enables sustained LZM release over an extended period. This study confirms a correlation between PVA characteristics and controlled drug release and provides valuable insights into tailoring nanofiber properties for pharmaceutical applications.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140173893","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Eperisone Hydrochloride, a Muscle Relaxant, Is a Potent P2X7 Receptor Antagonist. 肌肉松弛剂盐酸依哌立松是一种强效的 P2X7 受体拮抗剂

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00032

Makoto Okada, Takashi Nose

引用次数: 0

Visualization of the Plasmid DNA Delivery System by Complementary Fluorescence Labeling of Arginine-Rich Peptides. 通过对富精氨酸肽进行互补荧光标记实现质粒 DNA 运送系统的可视化。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00479

Ayumi Imayoshi, Hidetomo Yokoo, Masashi Kawaguchi, Kazunori Tsubaki, Makoto Oba

{"title":"Visualization of the Plasmid DNA Delivery System by Complementary Fluorescence Labeling of Arginine-Rich Peptides.","authors":"Ayumi Imayoshi, Hidetomo Yokoo, Masashi Kawaguchi, Kazunori Tsubaki, Makoto Oba","doi":"10.1248/cpb.c24-00479","DOIUrl":"https://doi.org/10.1248/cpb.c24-00479","url":null,"abstract":"Cell-penetrating peptides, such as arginine-rich peptides, encapsulate nucleic acid drugs and deliver them to intracellular compartments. Comprehensive tracking of drug delivery systems (DDSs) provides information about the behavior of the drug as well as the fate of the drug carrier after drug release, which is crucial for minimizing side effects. In this study, we labeled peptides designed to carry plasmid DNA with two types of dyes, traditional dye fluorescein and aggregation-induced emission (AIE) dye tetraphenylethylene, and subsequently tracked the DDS through the complementary ON and OFF fluorescence behaviors of the dyes. Traditional fluorescent dyes are susceptible to aggregation-caused quenching during bioimaging, a problem that is mitigated by using AIE dyes. However, by using both of these contrasting fluorescent labels, we were able to clearly visualize the DDS at different stages of its deployment, from drug transport and delivery to carrier dissociation and migration, demonstrating the feasibility of accurate DDS visualization by complementary fluorescence labeling.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142380120","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Foreword. 前言

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-ctf7207

Ken-Ichi Kusakabe

引用次数: 0

Anti-amyloid-β Antibodies and Anti-tau Therapies for Alzheimer's Disease: Recent Advances and Perspectives. 治疗阿尔茨海默病的抗淀粉样蛋白-β抗体和抗tau疗法：最新进展与展望》。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-00069

Naoyuki Suzuki, Takuya Hatta, Mana Ito, Ken-Ichi Kusakabe

{"title":"Anti-amyloid-β Antibodies and Anti-tau Therapies for Alzheimer's Disease: Recent Advances and Perspectives.","authors":"Naoyuki Suzuki, Takuya Hatta, Mana Ito, Ken-Ichi Kusakabe","doi":"10.1248/cpb.c24-00069","DOIUrl":"https://doi.org/10.1248/cpb.c24-00069","url":null,"abstract":"Amyloid-β (Aβ) plaques and neurofibrillary tangles containing phosphorylated tau protein are major hallmarks of Alzheimer's disease (AD). Drug discovery efforts to target Aβ and tau have been the primary focus for several decades. Recently, substantial breakthroughs have been achieved in the clinical development of Aβ antibodies; aducanumab was approved under conditional accelerated pathway by Food and Drug Administration (FDA) in the U.S. as the first disease-modifying agent for treating AD, and lecanemab has been granted traditional full approved in the U.S. and Japan. In addition, donanemab met the primary endpoint in a phase 3 study. On the other hand, tau-targeting therapies have failed to show clinical benefit although that increased tau levels show a strong correlation with cognitive impairment relative to Aβ depositions. Currently, tau immunotherapies, such as anti-tau antibodies and tau vaccines, have shown functional benefits in clinical trials. Also, clinical trials for combination therapy of Aβ and tau antibodies to see their potential are being investigated. In this review, we provide updates on the results of clinical trials of anti-Aβ antibodies and anti-tau therapeutics and suggest future directions for these therapeutics.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141466471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor. 评估作为竞争性抑制剂的 HTLV-1 蛋白酶逆转录抑制剂。

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c23-00879

Chiyuki Awahara, Daiki Oku, Kazuya Kobayashi, Yasunao Hattori

引用次数: 0

Errata for Chemical and Pharmaceutical Bulletin. 化学与制药公报》勘误表。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c24-e7204

引用次数: 0

Dual Engineering of Olivetolic Acid Cyclase and Tetraketide Synthase for the Formation of Longer Alkyl-Chain Olivetolic Acid Analogs and Their Antibacterial Activities 橄榄醇酸环化酶和四酮酸合成酶的双重工程技术用于形成更长烷基链的橄榄醇酸类似物及其抗菌活性

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c23-00692

Hiroyuki Morita

{"title":"Dual Engineering of Olivetolic Acid Cyclase and Tetraketide Synthase for the Formation of Longer Alkyl-Chain Olivetolic Acid Analogs and Their Antibacterial Activities","authors":"Hiroyuki Morita","doi":"10.1248/cpb.c23-00692","DOIUrl":"https://doi.org/10.1248/cpb.c23-00692","url":null,"abstract":"Among presently used pharmaceuticals, about 60% were developed from natural products with unique chemical diversity and biological activities. Hence, the discovery of new bioactive compounds from natural products is still important for further drug development. In addition, breakthroughs in synthetic biology have also begun to produce many useful compounds through manipulations of the biosynthetic genes for secondary metabolites. Theoretically, this approach can also be exploited to generate new unnatural compounds by intermixing the genes from different biosynthetic pathways and/or engineering the secondary metabolite enzyme(s) with expanded substrate and product specificities. Δ9-Tetrahydrocannabinol (Δ9-THC), the heat-decarboxylated tetrahydrocannabinolic acid (Δ9-THCA) produced by Cannabis sativa, is the most important therapeutic cannabinoid due to its useful pharmacological features, such as analgesic, anti-emetic, anti-inflammatory, and anti-epileptic activities. In the structures of cannabinoids, the resorcinyl alkyl chain is a critical pharmacophore, and the therapeutic effects of Δ9-THC can be enhanced by converting the pentyl (C5) moiety at C-3 to other acyl moieties. Thus, the expansion of unnatural cannabinoids with different C-3 alkyl moiety analogs might establish an excellent platform for the further development of therapeutically beneficial cannabinoids. This article reviews the structure-based dual engineering of both enzymes responsible for the formation of the resorcinyl core of Δ9-THC and describes the effect of C-6 alkyl-length extension of olivetolic acid, along with related analogs, on the antibacterial activities against Bacillus subtilis and Staphylococcus aureus.\u0000\u0000<img alt=\"\" src=\"https://www.jstage.jst.go.jp/pub/cpb/72/1/72_c23-00692/figure/72_c23-00692.png\"/>\u0000Fullsize Image","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139063653","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins 开发针对 HIV-1 帽状蛋白的小分子抗 HIV-1 药物

IF 1.7 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI: 10.1248/cpb.c23-00618

Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Sayaka Boku, Masaki Kurakami, Masayuki Fujino, Takahiro Ishii, Yutaro Miura, Soshi Nishimura, Kouki Shinohara, Kenichi Yamamoto, Peter Bolah, Osamu Kotani, Tsutomu Murakami, Hironori Sato, Hirokazu Tamamura

{"title":"Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins","authors":"Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Sayaka Boku, Masaki Kurakami, Masayuki Fujino, Takahiro Ishii, Yutaro Miura, Soshi Nishimura, Kouki Shinohara, Kenichi Yamamoto, Peter Bolah, Osamu Kotani, Tsutomu Murakami, Hironori Sato, Hirokazu Tamamura","doi":"10.1248/cpb.c23-00618","DOIUrl":"https://doi.org/10.1248/cpb.c23-00618","url":null,"abstract":"The capsid of human immunodeficiency virus type 1 (HIV-1) forms a conical structure by assembling oligomers of capsid (CA) proteins and is a virion shell that encapsulates viral RNA. The inhibition of the CA function could be an appropriate target for suppression of HIV-1 replication because the CA proteins are highly conserved among many strains of HIV-1, and the drug targeting CA, lenacapavir, has been clinically developed by Gilead Sciences, Inc. Interface hydrophobic interactions between two CA molecules via the Trp184 and Met185 residues in the CA sequence are indispensable for conformational stabilization of the CA multimer. Our continuous studies found two types of small molecules with different scaffolds, MKN-1 and MKN-3, designed by in silico screening as a dipeptide mimic of Trp184 and Met185 have significant anti-HIV-1 activity. In the present study, MKN-1 derivatives have been designed and synthesized. Their structure–activity relationship studies found some compounds having potent anti-HIV activity. The present results should be useful in the design of novel CA-targeting molecules with anti-HIV activity.\u0000\u0000<img alt=\"\" src=\"https://www.jstage.jst.go.jp/pub/cpb/72/1/72_c23-00618/figure/72_c23-00618.png\"/>\u0000Fullsize Image","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139082138","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0