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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
Haiyun Chen, Guolian Tan, Jie Cao, Gaoxiao Zhang, Peng Yi, Pei Yu, Yewei Sun, Zaijun Zhang, Yuqiang Wang
Oxidative stress plays a crucial role in neurological diseases, resulting in excessive production of reactive oxygen species, mitochondrial dysfunction and cell death. In this work, we designed and synthesized a series of tetramethylpyrazine derivatives and investigated their abilities for scavenging free radicals and preventing against oxidative stress-induced neuronal damage in vitro. Among them, compound 22a, consisted of TMP, caffeic acid and a nitrone group, showed potent radical-scavenging activity. Compound 22a had broad neuroprotective effects, including rescuing iodoacetic acid-induced neuronal loss, preventing from t-BHP-induced neuronal injury...
October 14, 2016: Chemical & Pharmaceutical Bulletin
Katsuhiko Yamamoto, Taro Kojima, Masatoshi Karashima, Yukihiro Ikeda
To judge the developability and analyze functional mechanism of co-amorphouses, we investigated the physicochemical properties of co-amorphouses and compare the properties with the co-crystals having the same drug and counters. Co-amorphous compounds are a novel approach to improve the physicochemical properties of drugs. A co-amorphous is in an amorphous solid state allowing non-ionic interactions between drug molecules and counter molecules. The co-amorphous compounds composed of itraconazole (ITZ) with the organic carboxyl acid, fumaric acid (FA) or L-tartaric acid (TA), were prepared by mechanical grinding...
December 1, 2016: Chemical & Pharmaceutical Bulletin
Zi-Li Ren, Jing Zhang, Hai-Dong Li, Ming-Jie Chu, Li-Song Zhang, Xiao-Kang Yao, Yong Xia, Xian-Hai Lv, Hai-Qun Cao
Acetylcholinesterase (AChE) is a key enzyme which present in the central nervous system of living organisms. Organophosphorus pesticides (OPs) that serve as insecticides are AChE inhibitors which have been used widely in agriculture. A series of novel OPs containing pyrazole moiety have been designed and synthesized. The biological evaluation indicated compound 4e appeared 81% larvicidal activity against Plutella xylostella at the concentration of 0.1 mg/L and the inhibition of AChE by compound 4e was distinctly enhanced with the increasing doses...
December 1, 2016: Chemical & Pharmaceutical Bulletin
Phan Van Kiem, Le Canh Viet Cuong, Bui Huu Tai, Nguyen Xuan Nhiem, Hoang Le Tuan Anh, Tran Hong Quang, Nguyen Thi Thanh Ngan, Hyuncheol Oh, Youn Chul Kim
Two new lignans (7S,7'R,8S,8'R)-3,3'-dimethoxy-7,7'-epoxylignan-4,4',9-triol 4-O-β-D-glucopyranoside (1) and 9-O-formylaviculin (2) together with other thirteen known secondary metabolites were isolated from the leaves of Antidesma hainanensis. Their chemical structures were determined using NMR, electrospray ionization (ESI)-MS, circular dichroism (CD) spectroscopic methods, and as well as by comparison with those reported in the literature. Neuro-inflammatory activity of isolated compounds was evaluated by their inhibition on nitric oxide (NO) production in activated BV2 microglial cells...
December 1, 2016: Chemical & Pharmaceutical Bulletin
Yayoi Kawano, Ayano Imamura, Tomoe Nakamura, Mio Akaishi, Mitsutoshi Satoh, Takehisa Hanawa
The stomatitis caused by anticancer agents and radiation therapy deteriorates patient QOL, potentially causing eating disorders as a result of pain. Although gargling and ointments can be used in the treatment of stomatitis, patients must spit out mouthwash after use, while ointment application requires a finger to be inserted into the oral cavity. In contrast, sprays eliminate these potential compliance problems. Therefore, we developed a stomatitis spray that remains on the oral mucosa. It has been reported that irsogladine maleate (IM) is effective against stomatitis via oral administration...
December 1, 2016: Chemical & Pharmaceutical Bulletin
Yan Sun, Jiao Fan, Dong Chai, Minghua Zhang
The hypothesis that oxidative stress contributes to renal dysfunction in sinoaortically denervated (SAD) rats was investigated. Rats were sinoaortically denervated and received treatment with tempol (0.5 mmol/L in drinking water) for 8 weeks. Although the tempol treatment of the SAD rats had no significant effect on blood pressure or blood pressure viability, it significantly ameliorated the renal dysfunction as indicated by increases in renal blood flow (RBF) and the glomerular filtration rate (GFR) and reductions in plasma creatinine, blood urea nitrogen (BUN), the urine albumin excretion rate (UAE), and the glomerular sclerosis score (GSS)...
October 1, 2016: Chemical & Pharmaceutical Bulletin
Hideyuki Konishi, Fumika Hoshino, Kei Manabe
We have developed a safe and practical synthetic method for preparing axially chiral diphenyl dicarboxylates using Pd-catalyzed external-CO-free carbonylation with phenyl formate as a CO surrogate. Optimized conditions consisted of axially chiral [1,1'-binaphthalene]-2,2'-diyl ditriflate and its congeners, each easily prepared from commercially available enantiomerically pure diols, Pd(OAc)2, 1,3-bis(diphenylphosphino)propane, ethyldiisopropylamine, and no solvent. To demonstrate the potential utility of these products, this method was conducted on gram-scale and the phenyl ester products were converted to other useful compounds, and both processes were carried out without difficulty...
October 1, 2016: Chemical & Pharmaceutical Bulletin
Tsung-Chang Tsai, Yu-Ting Huang, Shih-Kai Chou, Ming-Cheng Shih, Ching-Ying Chiang, Jui-Hsin Su
A new 10-demethylated steroid, nephtheasteroid A (1), a new 19-oxygenated steroid, nephtheasteroid B (2) as well as five known steroids 3-7 were isolated from the organic extract of a Taiwanese soft coral Nephthea erecta. The structure was determined by means of IR, MS, and NMR techniques. Among these metabolites, 1 is rarely found in steroids possessing a 19-norergostane skeleton. In vitro cytotoxicity study using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay revealed that compounds 3 and 4 exhibited cytotoxicity against human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (Molt-4), human T lymphoblastoid (Sup-T1), and human leukemic monocyte lymphoma (U937), with IC50 of 6...
October 1, 2016: Chemical & Pharmaceutical Bulletin
Shinji Harada, Kexin Li, Ryuto Kino, Takuya Takeda, Chia-Hsien Wu, Shiharu Hiraoka, Atsushi Nishida
We have developed a new method for synthesizing chiral isotwistane and homoisotwistane skeletons as well as aminocyclitols in a highly stereoselective manner. These results were achieved through the use of a common intermediate, which was derived from the ytterbium-catalyzed asymmetric Diels-Alder reaction of Danishefsky diene.
October 1, 2016: Chemical & Pharmaceutical Bulletin
Le Thi Vien, Tran Thi Hong Hanh, Phan Thi Thanh Huong, Nguyen Hai Dang, Nguyen Van Thanh, Ekaterina Lyakhova, Nguyen Xuan Cuong, Nguyen Hoai Nam, Phan Van Kiem, Alla Kicha, Chau Van Minh
Two new pyrrole oligoglycosides, plancipyrrosides A and B (1 and 2), were isolated from methanol extract of the Vietnamese starfish Acanthaster planci using various chromatographic procedures. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR and Fourier transform ion cyclotron resonance (FT-ICR)-MS. The finding of 1 and 2 represents the third case of pyrrole oligoglycosides obtaining reported to date. Moreover, plancipyrroside B (2) exhibits a potent inhibitory effect on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264...
September 7, 2016: Chemical & Pharmaceutical Bulletin
Liang Lu, Shao Sha, Kai Wang, Yuan-Heng Zhang, Yan-Dong Liu, Guo-Dong Ju, Baozhong Wang, Hai-Liang Zhu
A series of novel chromeno[4,3-c]pyrazol-4(2H)-one containing carbonyl or oxime derivatives (4a-4n, 5a-5n) have been synthesized and evaluated their biological activities as PI3K inhibitors. Out of them, compound 5l showed the most potent antiproliferative activities against HCT-116 with IC50 of 0.10 μM in vitro, and exhibited the most potent activity for PI3Kα with the value of 0.012 μM. Docking simulation of 5l into PI3Kα active site were performed to determine the probable binding model, and it indicated that compound 5l could be optimized as a potential inhibitor of PI3Kα in the further study...
September 1, 2016: Chemical & Pharmaceutical Bulletin
Jung-Sub Shin, Hee-Won Park, Gyo In, Hyun Kyu Seo, Tae Hyung Won, Kyoung Hwa Jang, Byung-Goo Cho, Chang Kyun Han, Jongheon Shin
Panax ginseng C.A. MEYER is one of the most popular medicinal herbs in Asia and the chemical constituents are changed by processing methods such as steaming or sun drying. Metabolomic analysis was performed to distinguish age discrimination of four- and six-year-old red ginseng using ultra-performance liquid chromatography quadruple time of flight mass spectrometry (UPLC-QToF-MS) with multivariate statistical analysis. Principal component analysis (PCA) showed clear discrimination between extracts of red ginseng of different ages and suggest totally six discrimination markers (two for four-year-old and four for six-year-old red ginseng)...
September 1, 2016: Chemical & Pharmaceutical Bulletin
Xiao-Yan Han, Yi-Fan Zhong, Sheng-Bin Li, Guo-Chao Liang, Guan Zhou, Xiao-Ke Wang, Bao-Hua Chen, Ya-Li Song
Invasive fungal disease constitutes a growing health problem and development of novel antifungal drugs with high potency and selectivity against new fungal molecular targets are urgently needed. In order to develop potent antifungal agents, a novel series of 6-alkyl-indolo[3,2-c]-2H-thiochroman derivatives were synthesized. Microdilution broth method was used to investigate antifungal activity of these compounds. Most of them showed good antifungal activity in vitro. Compound 4o showed the best antifungal activity, which (inhibition of Candida albicans and Cryptococcus neoformans) can be achieved at the concentration of 4 µg/mL...
September 1, 2016: Chemical & Pharmaceutical Bulletin
Sayaka Masada, Yutaka Takahashi, Yukihiro Goda, Takashi Hakamatsuka
Red vine leaf extracts (RVLEs) have traditionally been used for leg wellness and are now standardized to be used as OTC drugs in Europe. In Japan, one brand of RVLE products was recently approved as a direct OTC drug, and RVLEs are still used as ingredients in health food products. Since there is no mandated criterion for the quality of health food products in Japan, the consistent quality and composition of these products are not assured. Here we analyzed OTC drug and health food products containing RVLEs with different lot numbers by LC/MS...
September 1, 2016: Chemical & Pharmaceutical Bulletin
Ninh Thi Ngoc, Pham Thi Mai Huong, Nguyen Van Thanh, Nguyen Xuan Cuong, Nguyen Hoai Nam, Do Cong Thung, Phan Van Kiem, Chau Van Minh
Six steroids (1-6), including the two new compounds 3β,4α-dihydroxyergosta-5,24(28)-diene (1) and 24(S),28-epoxyergost-5-ene-3β,4α-diol (2), were isolated from the methanol extract of the Vietnamese soft coral Sinularia nanolobata. Their structures were elucidated by spectroscopic methods including one and two dimensional (1D- and 2D)-NMR, Fourier transform ion cyclotron resonance (FT-ICR)-MS, and circular dichroism (CD). Compound 2 exhibited moderate cytotoxicity against the acute leukemia (HL-60) cell line with IC50 value of 33...
September 1, 2016: Chemical & Pharmaceutical Bulletin
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