Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan最新文献_第6页

[Effect of Epilobium angustifolium Extract Containing Oenothein B on Autophagy]. [含酒皂苷B的枇杷提取物对自噬的影响]。

IF 0.2 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 Epub Date: 2025-10-06 DOI: 10.1248/yakushi.25-00091

Yuki Mukai, Ryota Yoshimura, Yuriko Naka, Junichi Tsuruoka, Koichiro Ohnuki

{"title":"[Effect of Epilobium angustifolium Extract Containing Oenothein B on Autophagy].","authors":"Yuki Mukai, Ryota Yoshimura, Yuriko Naka, Junichi Tsuruoka, Koichiro Ohnuki","doi":"10.1248/yakushi.25-00091","DOIUrl":"10.1248/yakushi.25-00091","url":null,"abstract":"Benign prostatic hyperplasia (BPH) and overactive bladder (OAB) are common conditions in adult men and women. The use of Epilobium angustifolium extract has garnered attention, especially in Europe. Clinical trials have revealed that E. angustifolium extract may improve symptoms of BPH and OAB. Additionally, this extract contains Oenothein B, an ellagitannin, and has been reported to have anti-inflammatory, antioxidant and anti-ageing effects. The mechanism of Oenothein B's anti-inflammatory and antioxidant effects is unclear. Therefore, this study evaluated the autophagy activity of Oenothein B to determine if E. angustifolium extract containing Oenothein B activates autophagy. To evaluate the autophagy activity of E. angustifolium extract containing Oenothein B, we used the tfLC3 assay, which evaluates the formation of autolysosomes. E. angustifolium extract containing Oenothein B activates autophagy starting at 0.01 mg/mL. The results suggest that E. angustifolium extract containing Oenothein B activates autophagy, potentially exerting anti-inflammatory and antioxidant effects through this activation.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":" ","pages":"79-83"},"PeriodicalIF":0.2,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145233708","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

[Evaluation of Drug Cost-Saving Effects of Drug Vial Optimization Using an Anticancer Drug Compounding Robot: A Single-center Study]. [基于抗癌药物复合机器人的药瓶优化药物成本节约效果评价：单中心研究]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.26-00021

Hikaru Sato, Ayami Kato, Yasuaki Mino, Tatsuya Yagi, Hironao Aono, Chiaki Uchida, Sayaka Kato, Kazuki Yamamoto, Junichi Kawakami

引用次数: 0

[The Effects Centella asiatica Extract and Its Component Araliadiol on Dementia Prevention]. 积雪草提取物及其成分芳二醇对痴呆的预防作用

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.26-00002

Honoka Fujimori, Yoshiki Kuse, Masamitsu Shimazawa, Hideaki Hara

引用次数: 0

[Life Science Research Using Small Membered Cyclic Unsaturated Compounds]. [利用小环不饱和化合物的生命科学研究]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.26-00121

Kenji Mishiro

{"title":"[Life Science Research Using Small Membered Cyclic Unsaturated Compounds].","authors":"Kenji Mishiro","doi":"10.1248/yakushi.26-00121","DOIUrl":"https://doi.org/10.1248/yakushi.26-00121","url":null,"abstract":"Small-membered unsaturated molecules possess unique molecular strain, electronic structures, and photochemical properties, making them attractive platforms for the development of functional molecules in life science research. This review summarizes our efforts to exploit cyclopropenones, cyclobutenediones, and deltic guanidines as photoreactive molecules and bioactive molecular scaffolds. Cyclopropenones can generate highly reactive alkynes upon photoirradiation, enabling light-controlled reactions such as carboxy group modification through photogenerated ynamines and amino group modification through ketene intermediates. Photocatalytic activation further allows these transformations to proceed under longer-wavelength light irradiation and may provide a basis for proximity-dependent labeling strategies. Aminocyclobutenediones were also developed as photoreactive molecules that generate bisketene intermediates and enable selective modification of acidic functional groups in aqueous media. These reactions allowed the introduction of carboxylate, phosphate, and sulfate groups under light-controlled conditions. In addition to their utility as photoreactive molecules, small-membered unsaturated scaffolds were explored as bioactive molecular frameworks. Deltic guanidines were synthesized as highly basic guanidine bioisosteres and shown to exhibit guanidine-like properties in cell permeability and integrin-targeting ligands. Aminocyclopropenones were also identified as a new class of anticancer molecules that suppress cancer cell growth by inhibiting BRD4 function. These studies demonstrate the broad potential of small-membered unsaturated molecules in chemical biology, molecular imaging, and drug discovery.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":"146 10","pages":"821-827"},"PeriodicalIF":0.4,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149115588","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 Protein and RNA Degraders for Drug Discovery]. [用于药物发现的蛋白质和RNA降解物的发展]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.25-00183-1

Yukihiro Itoh

{"title":"[Development of Protein and RNA Degraders for Drug Discovery].","authors":"Yukihiro Itoh","doi":"10.1248/yakushi.25-00183-1","DOIUrl":"https://doi.org/10.1248/yakushi.25-00183-1","url":null,"abstract":"Targeted protein degradation (TPD) is an emerging approach that selectively eliminates specific proteins using synthetic molecules, such as proteolysis-targeting chimeras (PROTACs). It has attracted increasing attention in medicinal chemistry and chemical biology, with several PROTACs being tested in clinical settings. Unlike traditional small molecules, such as enzyme inhibitors and receptor antagonists, PROTACs exhibit a fundamentally different mechanism. Conventional drugs block enzymatic activities or receptor interactions, whereas PROTACs induce the degradation of target proteins, decreasing their cellular levels and abolishing all associated functions. PROTACs targeting enzymes in protein complexes disrupt both their catalytic activity and involvement in complex formation. In some cases, they also degrade other proteins in complexes, facilitating the elimination of entire assemblies. Our study leverages these unique features of TPD. We are currently developing various PROTACs targeting the enzymes responsible for lysine acetylation or methylation in proteins. Recently, the TPD concept has been extended beyond proteins to include nucleic acids, and ribonuclease-targeting chimeras (RIBOTACs) that selectively degrade RNA have been developed. We are also actively exploring new RNA-targeted degradation strategies. Herein, we highlight our recent work on TPD-inducing small molecules and provide an overview of RIBOTACs, which represent an area of growing research interest.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":"146 7","pages":"617-624"},"PeriodicalIF":0.4,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148370098","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

[Potent Tissue Protection by Lipid-modified Extracellular Vesicles SPLEVs]. 脂质修饰的细胞外囊泡SPLEVs的有效组织保护作用。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.25-00171-2

Shunya Nakayama, Ai Kotani

引用次数: 0

[Synthesis of Functional Molecules for the Control of Biomolecular Functions]. [控制生物分子功能的功能分子合成]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.26-00003

Takayuki Iwata

{"title":"[Synthesis of Functional Molecules for the Control of Biomolecular Functions].","authors":"Takayuki Iwata","doi":"10.1248/yakushi.26-00003","DOIUrl":"10.1248/yakushi.26-00003","url":null,"abstract":"This study focuses on developing functional \"molecules\" and \"reactions\" aimed at controlling biomolecular functions. In the aspect of molecules, the asymmetric total syntheses of (-)-stemonamine and (-)-isostemonamine, which are stemona alkaloids isolated from Stemona japonica, were achieved. The strategy featured an intramolecular acylation to construct a seven-membered lactam and a tandem [2+2] cycloaddition/Dieckmann condensation to build the cyclopentenone ring, yielding the stemona alkaloids with high optical purity. Detailed kinetic analyses experimentally revealed, for the first time, the details of racemization and epimerization of/between stemonamine and isostemonamine. Biological assays demonstrated that (-)-isostemonamine exhibited potent antiproliferative activity against ERα-negative breast cancer cells. This synthetic methodology paves the way for the supply of stemona alkaloids whose biological activities are unknown and which have not yet been synthesized, and it is expected to greatly contribute to elucidating the biological functions hidden within their unique structures. In the aspect of reaction, a highly acid-sensitive Nazarov reaction proceeding under weakly acidic or even neutral conditions was developed. Key to this unprecedented reaction was the synergistic combination of (i) enhanced Lewis basicity of the carbonyl group, (ii) promotion of cyclization, and (iii) irreversible phenol elimination that shifts the reversible cyclization equilibrium toward the product. This system was further extended to a \"molecular release reaction,\" enabling fluorescent dye liberation in aqueous media. While further development is still required, the methodology offers a basis for future exploration of biocompatible acid-responsive reactions and the establishment of new biochemical tools that releases molecules targeting the acidic environment within living systems.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":"146 6","pages":"547-556"},"PeriodicalIF":0.4,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148138945","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

[Clinical Application of Targeted Alpha Therapy Using Astatine]. [阿司丁靶向α治疗的临床应用]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.25-00146-4

Tadashi Watabe

{"title":"[Clinical Application of Targeted Alpha Therapy Using Astatine].","authors":"Tadashi Watabe","doi":"10.1248/yakushi.25-00146-4","DOIUrl":"10.1248/yakushi.25-00146-4","url":null,"abstract":"Targeted alpha therapy is gaining prominence owing to its superior therapeutic efficacy compared with conventional radionuclide therapies using beta emitters. Astatine (211At, half-life: 7.2 h) has recently emerged as a promising alpha emitter, along with actinium (225Ac) and lead (212Pb). It can be produced domestically by irradiating natural bismuth targets with alpha particles using a 30 MeV cyclotron. Chemically analogous to iodine, astatine accumulates in differentiated thyroid cancer cells via the sodium/iodide symporter and demonstrated significant antitumor effects in a xenograft model. At The University of Osaka, we completed the first-in-human investigator-initiated clinical trial using [211At]sodium astatide (NaAt) in patients with metastatic thyroid cancer refractory to radioiodine (131I) therapy. The disappearance of iodine-avid lesions and a marked reduction in serum thyroglobulin levels (a tumor marker) were observed, suggesting clinical efficacy. In addition, we developed 211At-labeled compounds targeting the prostate-specific membrane antigen (PSMA), and a clinical trial is currently underway to confirm their efficacy and safety in preclinical studies. Furthermore, pan-tumor-targeting probes, including amino acid derivatives specific for L-type amino acid transporter 1 (LAT1) and antibodies targeting ephrin type-A receptor 2 (EphA2), are under active development and optimization for clinical applications. Targeted alpha therapy using astatine has great potential to significantly alter the future landscape of cancer therapy.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":"146 3","pages":"211-216"},"PeriodicalIF":0.4,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147327230","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

[Paradigm Shift by Utilization of Linear Transport Technology in Pharmaceutical Manufacturing]. [利用线性运输技术在制药生产中的范式转变]。

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.24-00210-1

Masahiko Kikuchi

引用次数: 0

[Metal-Assisted N-Terminal Modification of Polypeptides via Amino Acid-Metal Ion Interactions]. 金属辅助n端修饰多肽的氨基酸-金属离子相互作用研究

IF 0.4 4区医学

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan Pub Date : 2026-01-01 DOI: 10.1248/yakushi.26-00120

Kengo Hanaya

{"title":"[Metal-Assisted N-Terminal Modification of Polypeptides via Amino Acid-Metal Ion Interactions].","authors":"Kengo Hanaya","doi":"10.1248/yakushi.26-00120","DOIUrl":"https://doi.org/10.1248/yakushi.26-00120","url":null,"abstract":"Selective chemical modification of proteins under mild aqueous conditions is an important technique in chemical biology and biopharmaceutical research. Among the various targets for protein modification, the N-terminus is particularly attractive because it is uniquely present in each polypeptide and is often exposed on the protein surface. However, because the N-terminal amino group exhibits reactivity similar to that of lysine side chains, selective N-terminal modification based solely on the intrinsic amino-group reactivity remains a challenge. Our approach utilizes metal coordination involving the N-terminus and neighboring functional groups to selectively activate N-terminal intermediates. Using this approach, we developed several N-terminal modification reactions, including nickel(II)-mediated C-N coupling of pyroglutamic acid-histidine (pGlu-His) sequences, copper(II)-mediated aldol reactions, sequential multifunctionalization via nickel(II)-mediated aldol and Pictet-Spengler reactions, and one-step dual-functionalization via copper(II)-mediated [3+2] cycloaddition. Unlike conventional bioconjugation methods that rely on side-chain-specific reactions, our approach is based on metal-complex formation involving the peptide backbone, allowing broad applicability of our approach to diverse peptides and proteins without depending on specific side-chain functionalities. Furthermore, these reactions have been successfully applied to protein assembly and antibody-drug conjugate (ADC) construction. We believe that these methods will serve as useful tools in a wide range of studies in protein chemistry and chemical biology.","PeriodicalId":23810,"journal":{"name":"Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan","volume":"146 10","pages":"811-819"},"PeriodicalIF":0.4,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149115577","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