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Chemical & Pharmaceutical Bulletin

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https://www.readbyqxmd.com/read/28824027/boron-catalyzed-carboxylic-acid-selective-aldol-reaction-with-trifluoromethyl-ketones
#1
Kouhei Ishizawa, Hideoki Nagai, Yohei Shimizu, Motomu Kanai
A catalytic carboxylic acid-selective aldol reaction with trifluoromethyl ketones was developed. Reversible and selective covalent bond formation between a boron catalyst and a carboxylic acid is key to realizing the unprecedented catalytic aldol reaction of simple carboxylic acids. The reaction proceeded chemoselectively at the α-position of carboxylic acid even in the presence of ketone, ester, or amide functional groups in the donor substrates. The chemoselectivity is beneficial for late-stage derivatizations of biologically relevant compounds, as demonstrated by the conversion of indomethacin and triacetylcholic acid...
August 19, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28674282/spiroketalcarminic-acid-a-novel-minor-anthraquinone-pigment-in-cochineal-extract-used-in-food-additives
#2
Yusai Ito, Naoki Harikai, Kyoko Ishizuki, Kazufusa Shinomiya, Naoki Sugimoto, Hiroshi Akiyama
Cochineal extract prepared from the scale insect Dactylopus coccus (American cochineal) has been used as a natural red dye for food, cosmetics, and pharmaceuticals. The major pigment in cochineal extract is carminic acid (CA), an anthraquinone glucoside, and several minor pigments have been previously reported. Our investigation aimed at establishing the safety of cochineal dye products using UPLC-PDA-ESI-TOF/MS found an unknown minor pigment, spiroketalcarminic acid (1), in three commercial cochineal extract samples; cochineal extract used in food additives, carmine that is an aluminum salt of cochineal extract used as natural dye, and a research reagent of CA...
July 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28566563/isolation-of-dihydroartemisinic-acid-from-artemisia-annua-l-by-product-by-combining-ultrasound-assisted-extraction-with-response-surface-methodology
#3
Shuoqian Liu, Jorge Freire da Silva Ferreira, Liping Liu, Yuwei Tang, Dongming Tian, Zhonghua Liu, Na Tian
Malaria is the most devastating parasitic disease worldwide. Artemisinin is the only drug that can cure malaria that is resistant to quinine-derived drugs. After the commercial extraction of artemisinin from Artemisia annua, the recovery of dihydroartemisinic acid (DHAA) from artemisinin extraction by-product has the potential to increase artemisinin commercial yield. Here we describe the development and optimization of an ultrasound-assisted alkaline procedure for the extraction of DHAA from artemisinin production waste using response surface methodology...
August 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28539531/synergistic-activity-of-an-antimetabolite-drug-and-tyrosine-kinase-inhibitors-against-breast-cancer-cells
#4
Yushan Wu, Dongxing Zhang, Baofan Wu, Yuan Quan, Dongwu Liu, Yanyan Li, Xiuzhen Zhang
Antimetabolite drugs, including the adenosine deaminase inhibitor cladribine, have been shown to induce apoptosis in a variety of cancer cells, and have been widely used in clinical trials of various cancers in conjunction with tyrosine kinase inhibitors (TKIs). Combination treatment with cladribine and gefitinib or dasatinib is expected to have a synergistic inhibitory effect on breast cancer cell growth. Our results demonstrated that the combination treatment had synergistic activity against human breast cancer (MCF-7) cells, enhanced G2/M cell arrest and reactive oxygen species (ROS) generation, and increased the loss of mitochondrial membrane potential and cell apoptosis...
August 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28529239/formulation-optimization-of-gastro-retention-tablets-of-paeonol-and-efficacy-in-treatment-of-experimental-gastric-ulcer
#5
Xitong Zhang, Yue Zhang, Han Han, Jun Yang, Benliang Xu, Bing Wang, Tong Zhang
This study aims to develop a gastroretentive sustained-release drug delivery system of paeonol using floating properties and to investigate its therapeutic effects in rat models. The gastric retention tablets of paeonol (GRT-Ps) were prepared by a direct compression method, and the Box-Behnken design was used to optimize its formulation. The optimized formulation containing 15% NaHCO3 and a 2 : 1 ratio of paeonol and HPMC-K4M floated within 1 min and remained afloat for more than 8 h in the simulated gastric fluid (200 mL, pH=1...
August 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28442642/vaginal-delivery-of-benzydamine-hydrochloride-through-liposomes-dispersed-in-mucoadhesive-gels
#6
Fatmanur Tuğcu-Demiröz
Liposomal vaginal drug delivery systems are important strategy in the treatment of both topical and systemic diseases. The aim of this study was to develop a vaginal delivery system for benzydamine hydrochloride (BNZ) loaded liposomes dispersed into mucoadhesive gels. The delivery system was also designed for a once a day dosage and to obtain controlled release of the BNZ. For this purpose BNZ containing gel formulations using hydroxypropyl methylcellulose (HPMC) K100M and Carbopol(®) 974P, which are composed of polymers that show promising potential as mucoadhesive vaginal delivery systems, were developed...
July 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28652548/spongian-diterpenes-from-the-sponge-hyattella-aff-intestinalis
#7
Peni Ahmadi, Takahiro Haruyama, Nobuyuki Kobayashi, Nicole J de Voogd, Junichi Tanaka
Extracts of the sponge Hyattella aff. intestinalis showed moderate inhibition against adenovirus. Chromatographic separation of the extracts followed by analysis of spectroscopic data allowed us to elucidate the structures of three new metabolites as 2α-hydroxyspongia-13(16),14-diene-3-one (4), 3β-hydroxyspongia-13(16),14-diene-2-one (7), and 2α,3α-diacetoxy-17,19-dihydroxyspongia-13(16),14-diene (8) and to identify six known ones 1-3, 5-6 and 9. Among the molecules, compounds 1 and 3 showed antiviral activity at IC50 17...
June 23, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28392509/bioequivalence-and-pharmacokinetic-profiles-of-agomelatine-25-mg-tablets-in-healthy-chinese-subjects-a-four-way-replicate-crossover-study-demonstrating-high-intra-and-inter-individual-variations
#8
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)...
June 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28381698/chemical-synthesis-of-the-odm-201-s-diastereomers-through-an-efficient-intramolecular-1-3-dipolar-cycloaddition
#9
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...
June 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28367873/naphtoquinones-and-sesquiterpene-cyclopentenones-from-the-sponge-smenospongia-cerebriformis-with-their-cytotoxic-activity
#10
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 (HR-ESI)-MS, 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...
June 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28320975/cytotoxic-steroids-from-the-vietnamese-soft-coral-sinularia-leptoclados
#11
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...
June 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28320998/design-synthesis-and-biological-evaluation-of-potent-human-glyoxalase-i-inhibitors
#12
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', 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 1.0 nM and the inhibition effect of compound 10 on hGLO1 was nearly ten-fold higher than that of the strongest inhibitor 2 (Ki=10.0 nM) which has been reported in the field of glutathione-type hGLO1 inhibitors...
May 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28320974/dissipation-of-flonicamid-in-honeysuckle-and-its-transfer-during-brewing-process
#13
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...
May 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28163272/a-study-of-the-strength-of-a-template-molecule-a-functional-monomer-interaction-that-affects-the-performance-of-molecularly-imprinted-polymers-and-its-application-to-chiral-amplification
#14
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
https://www.readbyqxmd.com/read/28132960/selective-targeting-of-cancer-stem-cells-by-2-aminodihydroquinoline-analogs
#15
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
https://www.readbyqxmd.com/read/28090067/discovery-and-synthesis-of-amino-acids-modified-deoxycholic-acid-derivatives-and-in-vitro-antiproliferative-evaluation
#16
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
https://www.readbyqxmd.com/read/28077809/cytotoxic-steroids-from-the-vietnamese-soft-coral-sinularia-conferta
#17
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
https://www.readbyqxmd.com/read/27980251/preparation-and-characterization-of-hydroxypropyl-methylcellulose-polycarbophil-mucoadhesive-blend-films-using-a-mixture-design-approach
#18
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
https://www.readbyqxmd.com/read/27928130/application-of-terahertz-attenuated-total-reflection-spectroscopy-to-detect-changes-in-the-physical-properties-of-lactose-during-the-lubrication-process-required-for-drug-formulation
#19
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
https://www.readbyqxmd.com/read/27916782/cytotoxic-homoisoflavonoids-from-ophiopogon-japonicus-tubers
#20
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
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