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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 MTT method and Western blotting analysis on three tumor cell lines A549, MCF-7 and HeLa. The novel derivatives DCA3d, DCA5a, DCA5b, DCA5c, and DCA5d were found to be promising antiproliferative agents. Furthermore, DCA5b showed the greatest cytotoxic activity by induction of apoptosis...
January 13, 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...
January 12, 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...
December 16, 2016: 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...
December 6, 2016: 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 CD spectroscopic methods. Homoisopogon A (1) exhibited potent cytotoxicity against LU-1, KB, and SK-Mel-2 cancer cells with IC50 values ranging from 0.51 to 0.66 μM.
December 3, 2016: 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...
December 1, 2016: 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...
November 30, 2016: Chemical & Pharmaceutical Bulletin
Jairo Quiroga, Yazmín Villareal, Jaime Gálvez, Alejandro Ortíz, Braulio Insuasty, Rodrigo Abonia, Marcela Raimondi, Susana Zacchino
A series of pyrazolo[3,4-b]pyridines were prepared by a microwawe-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-3e), 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)...
November 25, 2016: Chemical & Pharmaceutical Bulletin
Haruka Katsui, Sachiko Sugimoto, Katsuyoshi Matsunami, Hideaki Otsuka, Sorasak Lhieochaiphant
From the leaves of Cananga odorata var. odorata, three relatively large molecules, namely two aryl naphthalene lignan diesters of canangafruticoside A and one cyclobutane lignan diester of canangafruticoside A, were isolated along with four known compounds. The structures of the new compounds were elucidated based on spectroscopic evidence.
2017: Chemical & Pharmaceutical Bulletin
Maher Abd El-Aziz El-Hashash, Sobhi Mohamed Gomha, Elham Ezz El-Arab
A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolyl-benzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolyl-chalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, (1)H- and (13)C-NMR, Mass)...
2017: Chemical & Pharmaceutical Bulletin
Guoqing Sui, Wen Zhang, Kun Zhou, Yulin Li, Bingyu Zhang, Dan Xu, Yong Zou, Wenming Zhou
As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of (1)H-NMR, (13)C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL...
2017: Chemical & Pharmaceutical Bulletin
Meropi Sklepari, Nikolaos Lougiakis, Athanasios Papastathopoulos, Nicole Pouli, Panagiotis Marakos, Vassilios Myrianthopoulos, Thomas Robert, Stéphane Bach, Emmanuel Mikros, Sandrine Ruchaud
A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against glycogen synthase kinase 3 (GSK3)α/β as well as against cdc2-like kinases 1 (CLK1) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with good selectivity and remarkable structure-activity relationships (SARs), without being cytotoxic. Molecular simulations in correlation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent...
2017: Chemical & Pharmaceutical Bulletin
Takatoshi Terada, Toshiro Ohtsubo, Yasunori Iwao, Shuji Noguchi, Shigeru Itai
The purpose of this study was to develop a deeper understanding of the key physicochemical parameters involved in the release profiles of microsphere-encapsulated agrochemicals at different temperatures. Microspheres consisting of different polyurethanes (PUs) were prepared using our previously reported solventless microencapsulation technique. Notably, these microspheres exhibited considerable differences in their thermodynamic characteristics, including their glass transition temperature (Tg), extrapolated onset temperature (To) and extrapolated end temperature (Te)...
2017: Chemical & Pharmaceutical Bulletin
Md Ashraf Ali, Noriko Kataoka, Abdul-Hackam Ranneh, Yasunori Iwao, Shuji Noguchi, Toshihiko Oka, Shigeru Itai
Monoolein cubosomes containing either spironolactone (SPI) or nifedipine (NI) were prepared using a high-pressure homogenization technique and characterized in terms of their solubility and oral bioavailability. The mean particle size, polydispersity index (PDI), zeta potential, solubility and encapsulation efficiency (EE) values of the SPI- and NI-loaded cubosomes were determined to be 90.4 nm, 0.187, -13.4 mV, 163 µg/mL and 90.2%, and 91.3 nm, 0.168, -12.8 mV, 189 µg/mL and 93.0%, respectively, which were almost identical to those of the blank cubosome...
2017: Chemical & Pharmaceutical Bulletin
Mio Tange, Akino Matsumoto, Miyako Yoshida, Honami Kojima, Tamami Haraguchi, Takahiro Uchida
The purpose of the study was to evaluate the adsorption of filgrastim on infusion sets (comprising infusion bag, line and filter) and to compare the adsorption of the original filgrastim preparation with biosimilar preparations using HPLC. The inhibitory effect of polysorbate 80 on this adsorption was also evaluated. Filgrastim was mixed with isotonic sodium chloride solution or 5% (w/v) glucose solution in the infusion fluid. Filgrastim adsorption on infusion sets was observed with all preparations and with both types of infusion solution...
2017: Chemical & Pharmaceutical Bulletin
Eito Yoshioka, Shigeru Kohtani, Takurou Hashimoto, Tomoko Takebe, Hideto Miyabe
In the presence of charge-transfer complexes between iodine and tertiary amines, the aqueous-medium atom-transfer radical reactions proceeded under visible light irradiation without the typical photocatalysts.
2017: Chemical & Pharmaceutical Bulletin
Hironori Takeuchi, Yoshihiro Ueda, Takumi Furuta, Takeo Kawabata
A short-step total synthesis of the natural glycosides pterocarinin C and tellimagrandin II (eugeniin) has been performed by sequential and site-selective functionalization of free hydroxy groups of unprotected D-glucose. The key reactions are β-selective glycosidation of a gallic acid derivative using unprotected D-glucose as a glycosyl donor and catalyst-controlled site-selective introduction of a galloyl group into the inherently less reactive hydroxy group of the glucoside.
2017: Chemical & Pharmaceutical Bulletin
Shun-Ichiro Uesugi, Yusuke Sasano, Shogo Matsui, Naoki Kanoh, Yoshiharu Iwabuchi
A concise, protecting-group-free synthesis of the antipsychotic agent (+)-nemonapride has been achieved featuring a europium(III) trifluoromethanesulfonate (Eu(OTf)3)-catalyzed C4 selective aminolysis of a 3,4-epoxy alcohol by benzylamine and an expedient use of the resulting 4-benzylamino-1,3-diol product for constructing the pyrrolidine skeleton.
2017: Chemical & Pharmaceutical Bulletin
Yasunari Monguchi, Tomohiro Ichikawa, Hironao Sajiki
This paper describes practical and selective hydrogenation methodologies using heterogeneous palladium catalysts. Chemoselectivity develops dependent on the catalyst activity based on the characteristic of the supports, derived from structural components, functional groups, and/or morphologies. We especially focus on our recent development of heterogeneous palladium catalysts supported on chelate resin, ceramic, and spherically shaped activated carbon. In addition, the application of flow technology for chemoselective hydrogenation using the palladium catalysts immobilized on molecular sieves 3A and boron nitride is outlined...
2017: Chemical & Pharmaceutical Bulletin
Zhao Li, Masamichi Tamura, Ryo Yazaki, Takashi Ohshima
A highly chemoselective conjugate addition of amino alcohols to α,β-unsaturated ester using a soft Lewis acid/hard Brønsted base cooperative catalyst was developed. This catalysis achieved chemoselective addition of a hydroxy group over an amino group. Moreover, soft metal alkoxide generation enabled chemoselective soft conjugate addition over hard transesterification. Various amino alcohols, including unprecedented cyclic β-amino alcohol, were applicable to the present catalysis.
2017: Chemical & Pharmaceutical Bulletin
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