著者
Shadi Sedghi Masoud Kazuo Nagasawa
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.66, no.12, pp.1091-1103, 2018-12-01 (Released:2018-12-01)
参考文献数
112
被引用文献数
14 41

The i-motif is a high-order DNA structure formed by hemiprotonated cytosine–cytosine base pairs under acidic conditions. It is less well studied than other high-order DNA structures, such as G-quadruplexes. However, increasing numbers of i-motif-binding ligands are being reported, and they are being used as tools to investigate the i-motif’s structure and biological functions. It has become clear that the i-motif has a functional role in the regulation of gene expression. In this review, we provide an overview of i-motif ligands so far reported, and we summarize their effects on the structure and their use as tools to investigate its biological functions.
著者
Wei Peng Yan-Yan Ma Kun Zhang Ai-Yu Zhou Yu Zhang Huaqian Wang Zhiyun Du Deng-Gao Zhao
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.64, no.6, pp.609-615, 2016-06-01 (Released:2016-06-01)
参考文献数
18
被引用文献数
9 13

Long-term use of nonsteroidal antiinflammatory drugs (NSAIDs) may cause serious side effects such as gastric mucosal damage. Resveratrol, a naturally dietary polyphenol, exhibited anti-inflammatory activity and a protective effect against gastric mucosa damage induced by NSAIDs. In this regard, we synthesized a series of resveratrol-based NSAIDs derivatives and evaluated their anti-inflammatory activity against nitric oxide (NO) overproduction in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. We identified mono-substituted resveratrol–ibuprofen combination 21 as the most potent anti-inflammatory agent, which is more active than a physical mixture of ibuprofen and resveratrol, individual ibuprofen, or individual resveratrol. In addition, compound 21 exerted potent inhibitory effects on the LPS-induced expression of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β). Furthermore, compound 21 significantly increased the survival rate in an LPS-induced acute inflammatory model and produced markedly less gastric damage than ibuprofen. It was found that compound 21 may be a potent anti-inflammatory agent for the treatment of inflammation-related diseases.
著者
Hayato Ishimoto Manabu Kano Hirokazu Sugiyama Hirofumi Takeuchi Katsuhide Terada Atsushi Aoyama Takuji Shoda Yosuke Demizu Jinen Shimamura Reiji Yokoyama Yuji Miyamoto Koji Hasegawa Masaru Serizawa Kazuomi Unosawa Kazuo Osaki Naochika Asai Yoshihiro Matsuda
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.69, no.2, pp.211-217, 2021-02-01 (Released:2021-02-01)
参考文献数
27
被引用文献数
3

As a result of the research activities of the Japan Agency for Medical Research and Development (AMED), this document aims to show an approach to establishing control strategy for continuous manufacturing of oral solid dosage forms. The methods of drug development, technology transfer, process control, and quality control used in the current commercial batch manufacturing would be effective also in continuous manufacturing, while there are differences in the process development using continuous manufacturing and batch manufacturing. This document introduces an example of the way of thinking for establishing a control strategy for continuous manufacturing processes.
著者
大場 節哉 今野 昌悦 山中 宏
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.39, no.2, pp.486-488, 1991-02-25 (Released:2008-03-31)
参考文献数
25
被引用文献数
19 33

A cyano group in 1, 2, 4-triaznes, regardless of its position, acted as an effective leaving group in reactions with carbanions. Thus, the reactions gave the corresponding substituted products in place of the compounds formed by addition reaction of carbanions to the cyano group. Grignard reaction of these carbonitriles is also described.
著者
Hayato Ishimoto Manabu Kano Hirokazu Sugiyama Hirofumi Takeuchi Katsuhide Terada Atsushi Aoyama Takuji Shoda Yosuke Demizu Jinen Shimamura Reiji Yokoyama Yuji Miyamoto Koji Hasegawa Masaru Serizawa Kazuomi Unosawa Kazuo Osaki Naochika Asai Yoshihiro Matsuda
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
pp.c20-00824, (Released:2020-12-08)
参考文献数
27
被引用文献数
3

As a result of the research activities of the Japan Agency for Medical Research and Development (AMED), this document aims to show an approach to establishing control strategy for continuous manufacturing of oral solid dosage forms. The methods of drug development, technology transfer, process control, and quality control used in the current commercial batch manufacturing would be effective also in continuous manufacturing, while there are differences in the process development using continuous manufacturing and batch manufacturing. This document introduces an example of the way of thinking for establishing a control strategy for continuous manufacturing processes.
著者
Magie Melanie Kapojos Delfly Booby Abdjul Hiroyuki Yamazaki Akiho Yagi Ryuji Uchida
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.68, no.9, pp.903-906, 2020-09-01 (Released:2020-09-01)
参考文献数
14
被引用文献数
1

Bioassay screening using Indonesian plants, such as traditional foods (vegetables, spices, and tea) and folk medicinal herbs, identified eight protein tyrosine phosphatase (PTP) 1B inhibitory and two antibacterial plants. The leaves of Syzygium polyanthum (Wight) Walp. were examined in more detail to define PTP1B inhibitory components, resulting in the isolation of a new active acylbenzene (1) along with four related congeners of 1 (2–5) and four oleanane triterpenes (6–9). The structure of 1 was elucidated as 12-oxo-12-(2,3,5-trihydroxy-4-methylphenyl)dodecanoic acid based on its spectroscopic data. The acylbenzenes 1 and 3–5 inhibited PTP1B activity with IC50 values ranging between 9.5 and 14 µM, whereas the triterpenes 7–9 also suppressed this activity with IC50 values of 3.3–5.7 µM.
著者
本橋 範子 西川 晴美 森 五彦
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.39, no.1, pp.142-145, 1991-01-25 (Released:2008-03-31)
参考文献数
26
被引用文献数
3 5

The inhibitory effects of sulfur compounds, namely cysteine and α-mercaptopropionylglycine (α-MPG) (thiol type), and N-methyl-3-mercaptoimidazole (MMI), 6-propylthiouracil (PTU) and ergothioneine (ESH) (thione type) on melanin formation reaction by tyrosinase, in the presence of tyrosine as a substrate, were assessed. Tyrosine oxidation was monitored both by radioassay using L-[3, 5-3H]tyrosine, L-[2, 6-3H]tyrosine and L-[carboxyl-14C]tyrosine as substrates, and by spectrometry to quantitate the dopachrome formed from L-tyrosine. The rated compounds, ranked as to inhibitory effect in descending order are : cysteine ≃α-MPG>MMI>PTU>ESH. Cysteine and α-MPG, both noncyclic thiol compounds, formed a 3, 4-dihydroxyphenylalanine (dopa) conjugate to inhibit melanin formation when added at low concentrations. At high concentrations, they inctivated the enzyme by interacting with tyrosinase. In MMI, PTU and ESH of heterocyclic thione structure, dopa conjugate formation was more inhibitory than tyrosinase inactivation on melanin formation.
著者
大村 智 片桐 通子 小倉 治夫 秦 藤樹
出版者
公益社団法人日本薬学会
雑誌
CHEMICAL & PHARMACEUTICAL BULLETIN (ISSN:00092363)
巻号頁・発行日
vol.16, no.7, pp.1181-1186, 1968
被引用文献数
1 11

Leucomycin A<SUB>3</SUB> (I) was oxidized with active manganese dioxide to dehydroleucomycin A<SUB>3</SUB> (II) which was identical with magnamycin B. Acid treatment of I yielded demycarosylleucomycin A<SUB>3</SUB> (VII), which was converted to a triacetate showing mass spectrum M<SUP>+</SUP> (m/e 725), and this observation confirmed the structure of I. The diene system of I was assumed to have a trans-trans configuration on the basis of its NMR spectrum, and a full structure of I was proposed with stereochemistry.
著者
大村 智 中川 彰 山田 陽城 秦 藤樹 古崎 昭雄 渡辺 得之助
出版者
公益社団法人日本薬学会
雑誌
CHEMICAL & PHARMACEUTICAL BULLETIN (ISSN:00092363)
巻号頁・発行日
vol.21, no.5, pp.931-940, 1973
被引用文献数
1 118

A series of new antibiotics, Kinamycin A, B, C, and D which are mainly effective against gram-positive bacteria, were extracted with chloroform from the broth filtrate of Streptomyces murayamaensis sp. nov. HATA et OHTANI. Kinamycin C (I), C<SUB>24</SUB>H<SUB>20</SUB>O<SUB>10</SUB>N<SUB>2</SUB>, m/e 496 (M<SUP>+</SUP>), was determined to have an 8-hydroxynaphthoquinone skeleton, nitrile, acetoxyl, and tertiary methyl groups from its ultraviolet (UV), infrared (IR), and nuclear magnetic resonance (NMR) spectra, and was further found to have a unique structure of N-C-N from some chemical reactions and X-ray diffraction. Structure relationship among I and other components A, B, and D was assumed to be due to the difference in the number and position of the acetoxyl group from analyses of IR, NMR, and mass spectra of their acetylated compounds. The antimicrobial activity of the four kinamycins increases with the decreasing number of acetoxy group, in the order of kinamycin C, A, D, and B. In addition, some derivatives obtained during structural studies on I were found to have nearly equal or increased antimicrobia1 activity compared with I and kinamycin D (XI).
著者
Yasuhiro Abe Eiichi Yamamoto Hiroyuki Yoshida Akiko Usui Naomi Tomita Hitomi Kanno Sayaka Masada Hidetomo Yokoo Genichiro Tsuji Nahoko Uchiyama Takashi Hakamatsuka Yosuke Demizu Ken-ichi Izutsu Yukihiro Goda Haruhiro Okuda
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
pp.c20-00431, (Released:2020-08-08)
参考文献数
28
被引用文献数
18

The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations were stored under various conditions, and subjected to LC-MS/MS analysis. When ranitidine tablets from two different brands (designated as tablet A and tablet B) were stored under accelerated condition (40°C with 75% relative humidity), following the drug stability guidelines issued by the International Conference on Harmonisation (ICH-Q1A), for up to 8 weeks, the amount of NDMA in them substantially increased from 0.19 to 116 ppm and from 2.89 to 18 ppm, respectively. The formation of NDMA that exceeded the acceptable daily intake limit (0.32 ppm) at the temperature used under accelerated storage conditions clearly highlights the risk of NDMA formation in ranitidine formulations when extrapolated to storage under ambient conditions. A forced-degradation study under the stress condition (60°C for 1 week) strongly suggested that environmental factors such as moisture and oxygen are involved in the formation of NDMA in ranitidine formulations. Storage of ranitidine tablets and reagent powders at the high temperatures also increased the amount of nitrite, which is considered one of the factors influencing NDMA formation. These data indicate the necessity of controlling/monitoring stability-related factors, in addition to controlling impurities during the manufacturing process, in order to mitigate nitrosamine-related health risks of certain pharmaceuticals.
著者
木村 善行 奥田 拓道 有地 滋
出版者
公益社団法人日本薬学会
雑誌
Chem. Pham. Bull. (ISSN:00092363)
巻号頁・発行日
vol.30, pp.4444-4447, 1982
被引用文献数
1

The effects of geniposide isolated from Gardeniae Fructus ("San-shi-shi"in Japanese) on metabolic alterations in high sugar diet-fed rats were investigated. It was found that the oral administration of the high sugar diet caused hyperlipemia, liver injury with elevation of glutamic pyruvic transaminase (GPT) in the serum, and the accumulation of lipid peroxide in the liver. Geniposide reduced the serum triglyceride, lipid peroxide, phospholipid, glucose, insulin and GPT in the high sugar diet-fed rats. It was found that the administration of geniposide reduced the sucrase activity in the small intestine and the deposition of lipid peroxide in the liver.
著者
木村 善行 奥田 拓道 奥田 拓男 吉田 隆志 波多野 力 有地 滋
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.31, no.7, pp.2501-2506, 1983-07-25

The effects of various tannins and related compounds on the actions of adrenocorticotropic hormone (ACTH) and insulin in fat cells isolated from rats were investigated. Hydrolyzable tannins such as geraniin, mallotusinic acid, chebulinic acid and chebulagic acid enhanced the ACTH-induced lipolysis at the concentration of 20 μg/ml or 5 μg/ml. On the other hand, these hydrolyzable tannins had no effect on the insulin-stimulated lipogenesis from glucose. Condensed tannins such as Ss-tannin 1 and RSF-tannin H showed weak inhibitory effects on the ACTH-induced lipolysis, while they enhanced the insulin-stimulated lipogenesis from glucose. Based on these results, the relationship between the structures and physiological actions of these tannins is discussed.
著者
木村 善行 久保 道徳 草加 君代 谿 忠人 東野 正行 有地 滋 奥田 拓道
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.30, no.1, pp.219-222, 1982-01-25

The effects of oral administration of flavonoid components of Scutellariae Radix on serum and liver lipid levels of rats treated with ethanol were investigated. It was found that wogonin reduced serum triglyceride level, and that baicalein and baicalin, the major components of the drug, decreased total cholesterol, free cholesterol and triglyceride contents in the liver. Baicalein increased high density lipoprotein-cholesterol (HDL-ch) in the serum of the ethanol-treated rats. In addition to these in vivo experiments, the actions of wogonin, baicalein and baicalin on catecholamine-induced lipolysis in isolated fat cells were investigated. It was found that the three flavones inhibited noradrenaline-induced lipolysis in isolated fat cells. The relationship between these in vivo and in vitro experiments is discussed.
著者
Kensuke Yagi Keiichi Goto Fumio Nanjo
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.57, no.11, pp.1284-1288, 2009-11-01 (Released:2009-11-01)
参考文献数
21
被引用文献数
17 25

The polyphenolic composition of Camellia irrawadiensis, which is a closely related species of Camellia sinensis (cultivated tea), was investigated. The most predominant polyphenol, a kind of ellagitannin, was isolated from leaves of C. irrawadiensis. Its structure was established as 1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-β-D-glucose (2) on the basis of spectral and chemical evidence. Moreover, the polyphenols [catechins, strictinin (1), compound 2, theogallin, and gallic acid] and two methylxanthines (theobromine and caffeine) in leaves of C. irrawadiensis were determined by HPLC-Photodiode array detector analysis, and were compared to those in C. sinensis and Camellia taliensis. Total catechin content in C. irrawadiensis was lower than that in C. sinensis and C. taliensis. Theobromine content in C. irrawadiensis was higher than that in C. sinensis and C. taliensis. The content of 2 in C. irrawadiensis was 8.4% of dry leaf weight and comprised approximately 60% of the total polyphenols detected, while the compound was not detected in C. sinensis and was reported to be 2.4% in C. taliensis.
著者
Ryosuke Mitani Shuji Ohsaki Hideya Nakamura Satoru Watano
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.68, no.8, pp.726-736, 2020-08-01 (Released:2020-08-01)
参考文献数
40
被引用文献数
9

This study investigated the particle adhesion mechanism in a capsule of dry powder inhaler (DPI) based on a combined computational fluid dynamics and discrete element method (CFD–DEM) approach. In this study, the Johnson–Kendall–Roberts (JKR) theory was selected as the adhesion force model. The simulation results corroborated the experimental results—numerous particles remained on the outlet side of the capsule, while a few particles remained on the inlet side. In the computer simulation, the modeled particles were placed in a capsule. They were quickly dispersed to both sides of the capsule, by air fed from one side of the capsule, and delivered from the air inlet side to the outlet side of the capsule. It was confirmed that vortex flows were seen at the outlet side of the capsule, which, however, were not seen at the inlet side. Numerous collisions were observed at the outlet side, while very few collisions were observed at the inlet side. These results suggested that the vortex flows were crucial to reduce the amount of residual particles in the capsule. The original capsule was then modified to enhance the vortex flow in the area, where many particles were found remaining. The modified capsule reduced the number of residual particles compared to the original capsule. This investigation suggests that the CFD–DEM approach can be a great tool for understanding the particle adhesion mechanism and improving the delivery efficiency of DPIs.
著者
染井 正徳 加藤 恵子 井上 里美
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.28, no.8, pp.2515-2518, 1980-08-25 (Released:2008-03-31)
参考文献数
14
被引用文献数
18 29

An improved procedure which avoids prolonged reaction at high temperature and handling under reduced pressure was found for the reduction of heteroaromatic and aromatic nitro compounds with aqueous titanium (III) chloride.
著者
Sirada Boonyaketgoson Yongle Du Ana L. Valenciano Murillo Maria B. Cassera David G. I. Kingston Kongkiat Trisuwan
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.68, no.7, pp.671-674, 2020-07-01 (Released:2020-07-01)
参考文献数
17
被引用文献数
4

Chromatographic separation of the acetone extracts from the twigs and barks of Artocarpus lakoocha led to the isolation of the one new flavanone, lakoochanone (1), together with eleven known compounds (2–12). Lakoochanone (1) and moracin C (4) exhibited weak antiplasmodial activity against Plasmodium falciparum Dd2 with IC50 values of 36.7 and 33.9 µM, respectively. Moreover, moracin C (4) and sanggenofuran B (5) showed cytotoxic activity against A2780 cell line with the respective IC50 values of 15.0 and 57.1 µM. In addition, cyclocommunin (7) displayed strong antimycobacterial activity against Mycobacterium tuberculosis H37Ra with the minimum inhibitory concentration (MIC) value of 12.3 µM.