Chemical & pharmaceutical bulletin最新文献

Concise Synthesis of 4'-Modified Thymidines via 1,5-Hydrogen Atom Transfer/Intermolecular 1,4-Addition Process. 1,5-氢原子转移/分子间1,4加成简明合成4'-修饰胸腺嘧啶

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-00021

Yuta Ito, Kang Juri, Yasufumi Fuchi, Yoshiyuki Hari

引用次数: 0

Synthesis and Anti-hypoxic Activity Research of Daidzein Derivatives. 大豆苷元衍生物的合成及抗缺氧活性研究。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-00014

Xiaohan Liu, Xinru Liu, Wenteng Zheng, Jing Xu, Tingting Chen, Tao Peng, Ruixin Liu, Shuchen Liu, Lin Wang, Shouguo Zhang

{"title":"Synthesis and Anti-hypoxic Activity Research of Daidzein Derivatives.","authors":"Xiaohan Liu, Xinru Liu, Wenteng Zheng, Jing Xu, Tingting Chen, Tao Peng, Ruixin Liu, Shuchen Liu, Lin Wang, Shouguo Zhang","doi":"10.1248/cpb.c25-00014","DOIUrl":"https://doi.org/10.1248/cpb.c25-00014","url":null,"abstract":"To search for safe and efficient anti-hypoxia active molecules, 27 derivatives were synthesized by introducing aminoalkyl groups at daidzein's position-7 and position-8. The structures of these derivatives were confirmed by 1H-NMR, 13C-NMR, and mass spectrometry. The anti-hypoxia activity was evaluated in vitro using a cell hypoxia model established with the AnaeroPack-anaero. The results showed that 9 compounds significantly enhanced cell viability under hypoxic conditions, with compounds 2a, 2b, 4d, 5a, and 5d exhibiting in vitro anti-hypoxia activity significantly superior to daidzein. And the drug-like properties prediction results of the target compounds indicated that compounds 2a, 2b, 4d, 5a, and 5d may also demonstrate favorable pharmacokinetic properties. Further, the anti-hypoxia activity in vivo of these 5 derivatives were evaluated via normobaric hypoxia and hypobaric hypoxia models. The results indicated that all of the 5 compounds extended the survival time of mice under normobaric hypoxia to varying degrees, and they also alleviated oxidative stress damage to the brain and heart of mice under hypobaric hypoxia. Among these, compound 2a demonstrated superior anti-hypoxia activity both in vitro and in vivo compared to daidzein, making it worthy of further study as a potential candidate for an anti-hypoxia drug.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"73 5","pages":"434-444"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143969524","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

Brominated 3-Acetyl-11-keto-β-boswellic Acid Derivative from Boswellia serrata Extract Characterized by Single-Crystal X-Ray Structure Analysis and Mass Spectroscopy. 单晶x射线结构分析和质谱分析表征了锯齿状乳香提取物中溴化3-乙酰基-11-酮-β-乳香酸衍生物的性质。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c24-00819

Masataka Ito, Keisuke Misao, Hironori Suzuki, Shuji Noguchi

引用次数: 0

Foreword. 前言。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-ctf7304

Yasuko Obata

引用次数: 0

Foreword. 前言。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-ctf7303

Tetsuro Ito, Wei Li

引用次数: 0

Experimental and DFT Studies of Intermolecular Interaction-Assisted Oxindole Cyclization Reaction of Di-t-butyl 2-Aminophenyl-2-methyl Malonate. 二叔丁基-2-氨基苯基-2-甲基丙二酸酯分子间相互作用辅助的氧吲哚环化反应的实验和DFT研究。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c24-00663

Ryo Kakehi, Yu-Suke Yamai, Akio Tanaka, Kyoji Ishida, Shinichi Uesato, Yasuo Nagaoka, Takaaki Sumiyoshi

引用次数: 0

Resin Glycosides from the Leaves and Stems of Ipomoea lacunosa. 木榄叶和茎中的树脂苷。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-00244

Masateru Ono, Kazumasa Furuike, Yusuke Sato, Yuko Hieda, Keigo Saruwatari, Rikiya Kaino, Madoka Mikazuki, Hirotaka Nishikawa, Nodoka Misuda, Shin Yasuda, Hiroyuki Miyashita, Hitoshi Yoshimitsu, Ryota Tsuchihashi, Masafumi Okawa, Junei Kinjo

{"title":"Resin Glycosides from the Leaves and Stems of Ipomoea lacunosa.","authors":"Masateru Ono, Kazumasa Furuike, Yusuke Sato, Yuko Hieda, Keigo Saruwatari, Rikiya Kaino, Madoka Mikazuki, Hirotaka Nishikawa, Nodoka Misuda, Shin Yasuda, Hiroyuki Miyashita, Hitoshi Yoshimitsu, Ryota Tsuchihashi, Masafumi Okawa, Junei Kinjo","doi":"10.1248/cpb.c25-00244","DOIUrl":"https://doi.org/10.1248/cpb.c25-00244","url":null,"abstract":"Alkaline hydrolysis of the crude resin glycoside fraction from the leaves and stems of Ipomoea lacunosa L. (Convolvulaceae) yielded organic acid and glycosidic acid fractions. The organic acid fraction included n-decanoic and n-dodecanoic acids. Acidic hydrolysis of the glycosidic acid fraction yielded 3 monosaccharides (d-glucose, d-fucose, and l-rhamnose) and 2 known hydroxyl fatty acids (11S-hydroxytetradecanoic and 11S-hydroxyhexadecanoic acids). Treatment of the glycosidic acid fraction with trimethylsilyldiazomethane (in hexane) afforded 1 new glycosidic acid methyl ester (lacunosinic acid J methyl ester) and 6 known glycosidic acid methyl esters. Eight new resin glycosides (lacunosins V-XII) were isolated from the leaves and stems, along with 2 known resin glycosides. Their structures were determined using spectroscopic and chemical analyses. Three types of resin glycosides were identified: those with 18-membered macrolactone, those with 19-membered macrolactone, and those with non-macrolactone structures. All these compounds contained n-decanoic and n-dodecanoic acids as the organic acid components. Nine of the isolated resin glycosides were tested for cytotoxic activity against HL-60 human promyelocytic leukemia cells. One compound exhibited activity with an IC50 value of 44.5 μM, while 3 compounds demonstrated moderate activity, with inhibition rates ranging from 53.5 to 68.7% at a concentration of 200 μM. In contrast, the remaining 5 compounds showed negligible effects even at 200 μM.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"73 6","pages":"547-558"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144504949","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 Cell-Penetrating Peptides and Their Application to DDS. 细胞穿透肽的研究进展及其在DDS中的应用。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c25-00272

Makoto Oba

引用次数: 0

Comparative Analysis of Needleless and Needle-Based Electrospinning Methods for Polyamide 6: A Technical Note. 聚酰胺 6 的无针和有针电纺方法比较分析：技术说明。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c24-00611

Arash Yavari, Takaaki Ito, Kouji Hara, Kohei Tahara

{"title":"Comparative Analysis of Needleless and Needle-Based Electrospinning Methods for Polyamide 6: A Technical Note.","authors":"Arash Yavari, Takaaki Ito, Kouji Hara, Kohei Tahara","doi":"10.1248/cpb.c24-00611","DOIUrl":"10.1248/cpb.c24-00611","url":null,"abstract":"This study investigates the influence of needleless versus needle-based electrospinning methods on the fiber diameter of polyamide 6 (PA6) nanofibers under comparable conditions, with an emphasis on potential pharmaceutical applications. Additionally, it examines how varying solvent systems impact fiber diameter specifically in needleless electrospinning. In this study, it was found that fibers produced by the needleless method were thicker compared to those produced by the needle-based method, a trend attributable to the specific solution characteristics and parameter settings unique to this study. Notably, a 2 : 1 acetic acid : formic acid solvent mixture yielded the largest fiber diameters among the solvent systems assessed for needleless electrospinning. These results underscore the potential of PA6 nanofibers in pharmaceutical applications, suggesting that further optimization of electrospinning conditions could enhance their suitability. The study also discusses the implications of scale-up production using needleless technology, highlighting its viability for industrial applications over single-needle electrospinning.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"73 1","pages":"18-24"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142977785","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

Permeation of Model Chemicals through Medical Gowns Used in Anticancer Drug Preparation. 模型化学物质在抗癌药物制备医用服中的渗透。

IF 1.5 4区医学

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI: 10.1248/cpb.c24-00838

Takuya Sotome, Takeshi Oshizaka, Tomoaki Toyama, Keiko Shinozaki, Satoru Usui, Kenji Mori, Kenji Sugibayashi

{"title":"Permeation of Model Chemicals through Medical Gowns Used in Anticancer Drug Preparation.","authors":"Takuya Sotome, Takeshi Oshizaka, Tomoaki Toyama, Keiko Shinozaki, Satoru Usui, Kenji Mori, Kenji Sugibayashi","doi":"10.1248/cpb.c24-00838","DOIUrl":"https://doi.org/10.1248/cpb.c24-00838","url":null,"abstract":"The wearing of medical gowns during anticancer drug preparation is recommended for the prevention of drug exposure. Non-breathable and breathable gowns (gown- and gown+, respectively) are both available. However, anticancer drugs may permeate \"gown+.\" In the present study, water, hydrophilic and lipophilic dyes, and aqueous solutions of several model chemicals with different physical properties (pyridoxine, antipyrine, ethyl p-hydroxybenzoate, and butyl p-hydroxybenzoate) were applied to four types of gowns and their chemical permeabilities were measured. The permeability of gowns to vaporized ethanol was also investigated because several volatile anticancer drugs are currently used in the treatment of cancer. The results obtained showed that the hydrophilic chemical, pyridoxine, did not permeate any of the gowns tested. Furthermore, gowns became more permeable as the lipophilicity of chemicals increased. No significant changes were observed in the chemical permeability between \"gown-\" and \"gown+,\" suggesting that the protective efficacy of the gowns against permeation by anticancer drugs was similar regardless of breathability. On the contrary, \"gown + \" was permeable to vaporized ethanol, whereas \"gown-\" was not. The present study demonstrates the need for safety measures in lipophilic or volatile anticancer drug handling and the importance of developing medical gowns that are highly resistant to chemical permeation.","PeriodicalId":9773,"journal":{"name":"Chemical & pharmaceutical bulletin","volume":"73 3","pages":"227-233"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143699689","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