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Chemical & Pharmaceutical Bulletin

Cuiyun Li, Jing Xu, Yan Zheng, Guiling Chen, Jianmeng Wang, Liying Ma, Yan Qiao, Junqi Niu, Min Wu, Hong Zhang, Xiaojiiao Li, Hong Chen, Xiaoxue Zhu, Chengjiao Liu, Yanhua Ding
The present study was designed to assess the bioequivalence of two agomelatine formulations (25-mg tablets) in healthy Chinese male subjects. This single-dose, open-label, randomized, four-way replicate study with a 1-week washout period was conducted in 60 healthy Chinese male volunteers under fasting conditions. Blood samples were collected over a 12-h period after a single dose of the 25-mg agomelatine test (T) formulation or a reference (R) formulation, and the drug concentrations were assayed by liquid chromatography tandem mass spectrometry (LC-MS/MS)...
April 8, 2017: Chemical & Pharmaceutical Bulletin
Tingting Pan, Chunguang Xia, Huijuan Jiang, Zhongtang Zhang, Xueyan Zhu, Yulei Yang
An efficient synthesis of ODM-201's diastereomers has been developed from (R)-methyl 3-hydroxybutanoate or (S)-methyl 3-hydroxybutanoate, respectively, with high overall yield and excellent diastereomeric purity. The key step in this synthesis is the preparation of the key intermediate (R)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid or (S)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid through intramolecular 1,3-dipolar cycloaddition of the vinyl diazo carbonyl compounds...
April 5, 2017: Chemical & Pharmaceutical Bulletin
Le Thi Huyen, Dan Thi Thuy Hang, Nguyen Xuan Nhiem, Pham Hai Yen, Hoang Le Tuan Anh, Tran Hong Quang, Bui Huu Tai, Nguyen Van Dau, Phan Van Kiem
Two new naphtoquinones (smenocerones A and B, 1 and 2) and four known sesquiterpene cyclopentenones (dactylospongenones A-D, 3-6) were isolated from sponge Smenospongia cerebriformis living in the Eastern Sea of Vietnam. Their chemical structures were determined by high resolution electrospray ionization mass spectrometry (HR-ESI-MS), nuclear magnetic resonance (NMR) spectroscopic analysis, and in comparison with the reported data. The chiroptical properties of compounds 3-6 were examined by experiment and theoretical calculation of circular dichroism (CD) spectra to prove their absolute configurations...
March 31, 2017: Chemical & Pharmaceutical Bulletin
Ninh Thi Ngoc, Tran Thi Hong Hanh, Nguyen Van Thanh, Do Thi Thao, Nguyen Xuan Cuong, Nguyen Hoai Nam, Do Cong Thung, Phan Van Kiem, Chau Van Minh
Fifteen steroids, including two new compounds, leptosteroid (1) and 5,6β-epoxygorgosterol (2), were isolated and structurally elucidated from the Vietnamese soft coral Sinularia leptoclados. Their cytotoxic effect against a panel of eight human cancer cell lines was evaluated using sulforhodamine B (SRB) method. Significant cytotoxicity against hepatoma cancer (HepG2, IC50 = 21.13±0.70 µM) and colon adenocarcinoma (SW480, IC50 = 28.65±1.53 µM) cell lines were observed for 1 and against acute leukemia (HL-60, IC50 = 20...
March 18, 2017: Chemical & Pharmaceutical Bulletin
Yujie Wang, Jian Xue, Hongyu Jin, Shuangcheng Ma
The dissipation of flonicamid in Honeysuckle and transfer pattern from Honeysuckle to its tea infusion were investigated. Flonicamid was applied on Honeysuckle crop at two dosages, 60 g of active gradient per hectare (g a.i. hm(-2)) and 180 g a.i. hm(-2) (recommended and triple the recommended) in Fenqiu, Henan Province in 2015 and 2016. Gas chromatography-Electron Capture Detector (GC-ECD) detection methods were developed for the analysis of flonicamid residues in honeysuckles and its infusion. The recoveries in both honeysuckles and its infusion ranged from 81...
March 18, 2017: Chemical & Pharmaceutical Bulletin
Tian Jin, Jing Zhai, Xiao Liu, Yan Yue, Maolin Huang, Zonghe Li, Caixia Ni, Qishan Deng, Yankui Sang, Zhongwei Yao, Hong Zhang, Xiaopeng Hu, Zhe-Bin Zheng
Several glutathione derivatives bearing the S-(N-aryl-N-hydroxycarbamoyl) or S-(C-aryl-N-hydroxycarbamoyl) moieties [10, 10' and 13-15] were synthesized, characterized, and their human glyoxalase I (hGLO1) inhibitory activity was evaluated. Compound 10 was proved to be the effective hGLO1 inhibitor with a Ki value of 1 nM and the inhibition effect of compound 10 on hGLO1 was nearly ten-fold higher than that of the strongest inhibitor 2 (Ki = 10 nM) which has been reported in the field of glutathione-type hGLO1 inhibitors...
March 17, 2017: Chemical & Pharmaceutical Bulletin
Takuro Yasuyama, Hirofumi Matsunaga, Shin Ando, Tadao Ishizuka
A novel type of molecularly imprinted polymer (MIP), N-benzoyl-(S)-valine anilide-imprinted polymer (IP-2), was prepared using hydrogen-bonding interactions as a main force in the pre-polymerization step. The performance of the IP-2 was evaluated via batch procedure and compared with a (S)-valine anilide-imprinted polymer (IP-1) that was prepared using an ionic interaction that is stronger than hydrogen bonding. Although both polymers showed a preferential adsorbability for (S)-amino acid derivatives, different performances were observed in terms of adsorbability and enantioselectivity...
April 1, 2017: Chemical & Pharmaceutical Bulletin
Heejoo Park, Yeongji Yu, Hyejin Kim, Eun Lee, Hani Lee, Raok Jeon, Woo-Young Kim
Many aminodihydroquinoline compounds have been studied to determine their cytotoxicity to cancer cells. However, anti-cancer stem cells (CSCs) activity of aminodihydroquinoline has not been tested in spite that CSC is believed to do an important roles in chemotherapy resistance and recurrence. The CSC selective targeting activities of 10 recently synthesized 2-aminodihydroquinoline analogs were examined on CSCs and bulk culture of a glioblastoma cell line. A diethylaminopropyl substituted aminodihydroquinoline, 5h, showed a strong anti-CSC effect and general cytotoxicity...
April 1, 2017: Chemical & Pharmaceutical Bulletin
Chunhui Zhao, Peizhe Zhao, Bin Feng, Xiyan Hou, Longxuan Zhao
A series of deoxycholic acid (DCA) derivatives bearing amino acid moiety has been synthesized and investigated for their potential antiproliferative activities. DCA derivative compounds were synthesized by a two or three step synthetic approach. Their bioactivities were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and Western blotting analysis on three tumor cell lines A549 (human lung cancer cell line), MCF-7 (human breast cancer cell line) and HeLa (human cervical carcinoma cell)...
March 1, 2017: Chemical & Pharmaceutical Bulletin
Ninh Thi Ngoc, Pham Thi Mai Huong, Nguyen Van Thanh, Nguyen Thi Phuong Chi, Nguyen Hai Dang, Nguyen Xuan Cuong, Nguyen Hoai Nam, Do Cong Thung, Phan Van Kiem, Chau Van Minh
Twelve steroids, including five new compounds 1-5, were isolated and structurally elucidated from a methanol extract of the Vietnamese soft coral Sinularia conferta. Their cytotoxic effects against three human cancer cell lines, lung carcinoma (A-549), cervical adenocarcinoma (HeLa), and pancreatic epithelioid carcinoma (PANC-1), were evaluated using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assays. Among isolated compounds, 10 exhibited potent cytotoxic effects on all three tested cell lines with IC50 values of 3...
March 1, 2017: Chemical & Pharmaceutical Bulletin
Pakorn Kraisit, Sontaya Limmatvapirat, Jurairat Nunthanid, Pornsak Sriamornsak, Manee Luangtana-Anan
The objectives of this study were to prepare the hydroxypropyl methylcellulose (HPMC)/polycarbophil (PC) mucoadhesive blend film and to investigate the main and interaction effect of HPMC and PC mixtures on the physicochemical and mechanical properties of blend films using a simplex lattice mixture design approach. The cubic and quadratic models were selected to analyze mucoadhesive properties in terms of work of adhesion and maximum detachment force, respectively. It was shown that HPMC/PC blend film had higher mucoadhesive properties than pure HPMC film...
March 1, 2017: Chemical & Pharmaceutical Bulletin
Masafumi Dohi, Wataru Momose, Kazunari Yamashita, Tadashi Hakomori, Shusaku Sato, Shuji Noguchi, Katsuhide Terada
Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we used terahertz attenuated total reflection (THz-ATR) spectroscopy to detect differences in the physical characteristics of the lubricated powder. We applied a simple formulation prepared by blending granulated lactose as filler with magnesium stearate as lubricant...
February 1, 2017: Chemical & Pharmaceutical Bulletin
Nguyen Hai Dang, Nguyen Dinh Chung, Ha Manh Tuan, Nguyen Tuan Hiep, Nguyen Tien Dat
A phytochemical fractionation of a methanol extract of Ophiopogon japonicus tubers led to the isolation of a new homoisoflavanone, homoisopogon A (1), and three new homoisoflavanes, homoisopogon B-D (2-4). Their chemical structures were elucidated by mass, NMR, and circular dichroism (CD) spectroscopic methods. Homoisopogon A (1) exhibited potent cytotoxicity against human lung adenocarcinoma LU-1, human epidermoid carcinoma KB, and human melanoma SK-Mel-2 cancer cells with IC50 values ranging from 0.51 to 0...
February 1, 2017: Chemical & Pharmaceutical Bulletin
Yeongbin Lee, Prakash Thapa, Seong Hoon Jeong, Mi Hee Woo, Du Hyung Choi
Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses...
February 1, 2017: Chemical & Pharmaceutical Bulletin
Aoi Miyamoto, Takahiko Aoyama, Yoshiaki Matsumoto
A high-performance liquid chromatography-ultraviolet spectrophotometry (HPLC-UV) method for the determination of meloxicam (MEL) and meloxicam metabolites (5'-hydroxy meloxicam (5-HMEL) and 5'-carboxy meloxicam (5-CMEL)) has been developed. After extraction of MEL, 5-HMEL, and 5-CMEL from rat plasma using Oasis HLB cartridges, the extracts were separated with a Luna C18 (2) 100 A column (5 µm, 4.6×150 mm, Phenomenex) using a mobile phase of 50 mM phosphate buffer (pH 2.15, solvent A) and acetonitrile (solvent B) at a flow rate of 0...
February 1, 2017: Chemical & Pharmaceutical Bulletin
Jairo Quiroga, Yazmín Villarreal, Jaime Gálvez, Alejandro Ortíz, Braulio Insuasty, Rodrigo Abonia, Marcela Raimondi, Susana Zacchino
A series of pyrazolo[3,4-b]pyridines were prepared by a microwave-assisted aza-Diels-Alder reaction between pyrazolylformimidamides 1 and β-nitrostyrenes 2 in toluene as the solvent. This procedure provides a simple one-step and environmentally friendly methodology with good yields for the synthesis of these compounds. All compounds were tested for antifungal activity against two clinically important fungi Candida albicans and Cryptococcus neoformans. Within the compounds of the series bearing a -CH3 group on the carbon C-3 of the azole ring (3a-e), the compound without a substituent on the p'-phenyl ring (3a), showed the best activity against both fungi, followed by the p'-Br-phenyl (3c)...
February 1, 2017: Chemical & Pharmaceutical Bulletin
Hong-Mei Li, Min Fan, Yong Xue, Li-Yan Peng, Xing-De Wu, Dan Liu, Rong-Tao Li, Qin-Shi Zhao
Twelve guaiane-type sesquiterpenoids, including four new ones, 10-O-methyl-orientalol A (1), 10-O-ethyl-alismoxide (2), 3β,4β-expoxy-chrysothol (3), orientalol G (4), and a new norsesquiterpenoid, orientalol H (5), were isolated from Chinese Alismatis Rhizoma, the dried rhizome of Alisma orientale. The structures of new compounds were elucidated on the basis of spectroscopic data. Moreover, the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells of all compounds was tested...
2017: Chemical & Pharmaceutical Bulletin
Hitomi Uchimoto, Miki Ikeda, Saori Tanida, Kayo Ohhashi, Yoshiko Chihara, Takashi Shigeta, Kenji Arimitsu, Masayuki Yamashita, Kiyoharu Nishide, Ikuo Kawasaki
We synthesize optically active (R)-terbutaline 2, which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of acyl substituted substrates 4c yields chiral secondary alcohols 5c in good yield and enantioselectivity. Furthermore, (R)-terbutaline 2 can be synthesized in one step from the resulting secondary alcohol 5 without racemization...
2017: Chemical & Pharmaceutical Bulletin
Yingfei Wang, Xiaojing Zhang, Changjiang Xu, Gaoxiao Zhang, Zaijun Zhang, Pei Yu, Luchen Shan, Yewei Sun, Yuqiang Wang
Myocardial ischemia is a primary cause of sudden death worldwide. Numerous active ingredients of traditional Chinese medicines including danshensu (DSS) and tetramethylpyrazine (TMP) have been widely used for the treatment of myocardial ischemia. To enhance their therapeutic efficacy and improve their drugability, in this work, we designed new DSS and TMP conjugates. Their water solubility and protective effects were studied in vitro and in experimental animal models. The new compounds demonstrated higher activities than the positive control agents acetylated danshensu and tetramethylpyrazine conjugate (ADTM) and salvianolic acid B (SAB) in preventing cells from oxidative insult...
2017: Chemical & Pharmaceutical Bulletin
Shinji Katsura, Nobuo Yamada, Atsushi Nakashima, Sumihiro Shiraishi, Mihoko Gunji, Takayuki Furuishi, Tomohiro Endo, Haruhisa Ueda, Etsuo Yonemochi
We observed that uncoated furosemide tablets turned yellow in a light-shielded automatic packaging machine and discoloration of the furosemide tablets was heterogeneity and occurred on the surface of the tablets only. The machine was equipped with an internal blower to maintain a constant temperature. Therefore, we investigated the effect of air flow on the discoloration of the furosemide tablets using a blower in a dark environment. The color difference (ΔE) of the furosemide tablets increased linearly as the blowing time increased...
2017: Chemical & Pharmaceutical Bulletin
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