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Chemical & Pharmaceutical Bulletin

Jiaxin Li, Yujie Wang, Jian Xue, Pengsi Wang, Shangmei Shi
To investigate the dietary exposure risk of flonicamid application on Lonicerae Japonicae Flos and the effect of flonicamid on constituents of Lonicerae Japonicae Flos, field experiments were conducted in Fengqiu, Henan province, and flonicamid residue in samples collected was detected by gas chromatography equipped with electron capture detector (GC-ECD). And chlorogenic acid and luteoloside were determined by HPLC. Dietary exposure risk assessment was conducted through comparing the estimated daily intake (EDI) which was calculated by using the consumed residual level along with the acceptable daily intake (ADI)...
March 14, 2018: Chemical & Pharmaceutical Bulletin
Ryosuke Koyama, Wataru Hakamata, Takako Hirano, Toshiyuki Nishio
Three Golgi mannosidases (GMs), namely Golgi α-mannosidases IA, IB, and IC, remove mannose residues from N-glycans and regulate the quality control and transportation of nascent proteins. GM inhibitors regulate several biological events such as cell-cell communication, differentiation, and apoptosis in cancer cells. As a result, GM inhibitor-based therapies have gained significant attention for cancer treatment. However, to date, no GM inhibitor has been approved and none is in clinical development for anti-cancer treatment...
March 13, 2018: Chemical & Pharmaceutical Bulletin
Manman Li, Yanping Chen, Pengfei Zhang, Ling Zhang, Ri Zhou, Yan Xu, Hongda Ding, Qiujing Wang, Zhicai Wang
Tweleve pseudo-ginsensides were synthesized under a mild condition, via a simple three-step called acetylation, elimination-addition and saponification. The inhibitory effects of these tweleve pseudo-ginsenosides were screened on the hemolysis of rabbit erythrocytes caused by 2,2' -azobis (2-amidinopropane hydrochloride) (AAPH). It was found that the IC50 values followed the sequence of (20Z) pseudo-protopanaxatriol (pseudo-PPT) < (20Z) pseudo-protopanaxadiol (pseudo-PPD) < (20Z) pseudo-Rh2 < (20E) pseudo-PPT< (20E) pseudo-PPD < (20E) pseudo-Rh2 < (20Z) pseudo-Rg2 < (20E) pseudo-Rg2 < Rb1 < (20Z) pseudo-Rh1 < Rg2 < (20E) pseudo-Rh1...
March 7, 2018: Chemical & Pharmaceutical Bulletin
Jiakun Long, Yang Wang, Chen Xu, Tingting Liu, Gengli Duan, Yingjia Yu
Uncaria rhynchophylla is woody climber plant distributed mainly in China and Japan, the stems and hooks of which can be collected as "Gou-Teng" for the treatment of hyperpyrexia, epilepsy and preeclampsia. Fudan University first manufactured KHR98, the extract of Uncaria rhynchophylla. In order to study the active components and structural information of KHR98, we established a high- performance liquid chromatography (HPLC) coupled with quadrupole time-of-flight mass spectrometry (Q-TOF-MS) method for rapid analysis of alkaloids...
March 2, 2018: Chemical & Pharmaceutical Bulletin
Takuya Izawa, Koji Nakayama, Noritaka Uchida, Kazuhiro Nojima
Dehydroacetic acid (1) was found to induce photoisomerization, converting aldrin (3) and dieldrin (4) into photoaldrin (5) and photodieldrin (6), respectively, not only when irradiated with artificial light at wavelengths longer than 290 nm in air but also when exposed to sunlight in air. By contrast, sodium dehydroacetate (2) induced both photoisomerization, primarily converting 3 to 5 and photoepoxidation, partially forming 6. Thus, because 2 is usually used as a water-soluble antiseptic, photo-erethism might occur due to the isomerization and epoxidation properties of this compound...
February 22, 2018: Chemical & Pharmaceutical Bulletin
Hideyuki Konishi, Tomoyuki Sekino, Kei Manabe
A practical Pd-catalyzed carbonylation of (hetero)aryl bromides using a crystalline carbon monoxide (CO) surrogate, 2,4,6-trichlorophenyl formate (TCPF), was developed. This reaction proceeds without the slow addition technique that was previously required and with a low catalyst loading (1 mol%). The utility of this Pd-catalyzed external-CO-free carbonylation using TCPF was demonstrated in the synthesis of a histone deacetylase inhibitor.
February 14, 2018: Chemical & Pharmaceutical Bulletin
Wen-Yi Mei, Ming-Jun Yu, Sen Yao, Kui-Ling Wang, Ri-Sheng Yao
The anti-inflammatory effects of (R)-2-(1H-imidazol-1-yl) ethyl-3-(1H-indol-3- yl)-2-(2-p-tolylacetamido)propanamide (RH-1402), a previous designed small molecule Gastrin releasing peptide (GRP) antagonist were evaluated in adjuvant-induced arthritic model of rats, and the inhibitory effect on neutrophil migration induced by GRP was determined by a transwell system experiment in vitro. The arthritis was induced by injection of Complete Freund's Adjuvant (CFA) containing 10 mg/mL of heat killed mycobacterium into the left hind footpad...
February 8, 2018: Chemical & Pharmaceutical Bulletin
Si-Li Zheng, Zhi-Yong Li, Zheng Zhang, Dong-Sheng Wang, Jian Xu, Chao-Yu Miao
Metrnl is a newly discovered secreted protein with neurotrophic activity and metabolic effect, while in earlier studies its circulating level in human was not explored. We evaluated two commercial enzyme-linked immunosorbent assay kits (DY7867-05, R&D Systems and SK00478-02, Aviscera Bioscience) for the detection of human circulating Metrnl. The DY7867-05 kit showed superiority over the SK00478-02 kit since it generated better curve fitting degree, smaller variation among tests, higher inter-assay reproducibility and better specificity, and could effectively detect human Metrnl in six types of blood samples...
February 2, 2018: Chemical & Pharmaceutical Bulletin
Davor J Korčok, Nada Tršić-Milanoviće, Nevena Ivanović, Brižita Đorđević
Probiotics are increasingly more present both as functional foods, and in pharmaceutical preparations with multiple levels of action that contribute to human health. Probiotics realize their positive effects with a proper dose, and by maintaining a declared number of probiotics cells by the expiration date. Important precondition for developing a probiotic product is the right choice of clinically proven probiotic strain, the choice of other active components, as well as, the optimization of the quantity of active component of probiotic per product dose...
January 19, 2018: Chemical & Pharmaceutical Bulletin
Tatsuya Hirano, Tomohiko Kinoshita, Daichi Kazamori, Satoshi Inoue, Kouji Nishimura, Asuka Sakurai, Kensuke Ohishi, Yasuhiro Kuramoto, Hirotaka Amano, Akira Yazaki
WFQ-101 with a unique N-1 substituent, 5-amino-4-fluoro-2-(hydroxymethyl)phenyl group, was selected as a lead compound through combination screening based on antimicrobial activity and the efflux index against quinolone-resistant (QR) Pseudomonas aeruginosa (P. aeruginosa). Through structural optimization, we identified WFQ-228 as a novel fluoroquinolone antibiotic candidate. WFQ-228 had potent and superior activity in comparison to levofloxacin (LVX) and ciprofloxacin (CIP) against clinical isolates of P. aeruginosa, Escherichia coli and Acinetobacter baumannii, including QR strains...
January 11, 2018: Chemical & Pharmaceutical Bulletin
Yo Muraki, Midori Yamasaki, Hirohisa Takeuchi, Kimio Tohyama, Noriyasu Sano, Takanori Matsuo
Pulmonary hypertension (PH) is a life-threatening lung disease. Despite the availability of several approved drugs, the development of a new treatment method is needed because of poor prognosis. Tissue selective drug delivery systems can avoid the adverse effects of current therapy and enhance efficacy. We evaluated the possibility of delivering drugs to the lungs of a PH rat model using fluorescence dye-labeled nanosized liposomes. To evaluate the tissue distribution following systemic exposure, fluorescent dye-labeled, 40-180 nm liposomes with and without polyethylene glycol (PEG) were intravenously administered to a monocrotaline-induced PH (MCT) rat model and tissue fluorescence was measured...
January 6, 2018: Chemical & Pharmaceutical Bulletin
Shuoqian Liu, Jorge Freire da Silva Ferreira, Dongming Tian, Yuwei Tang, Liping Liu, Wei Yang, Zhonghua Liu, Na Tian
In order to make full use of artemisinin production waste and thus to reduce the production cost of artemisinin, we developed an efficient and scalable method to isolate high-purity dihydroartemisinic acid from artemisinin production waste by combining anion-exchange resin with silica-gel column chromatography. The adsorption and desorption characteristics of dihydroartemisinic acid on 10 types of anion-exchange resin were investigated, and the results showed that the 717 anion-exchange resin exhibited the highest capacity of adsorption and desorption to dihydroartemisinic acid...
December 28, 2017: Chemical & Pharmaceutical Bulletin
Khaled M Elamin, Yuki Yamashita, Taishi Higashi, Keiichi Motoyama, Hidetoshi Arima
Methyl-β-cyclodextrin (M-β-CyD) exhibits cytotoxic activity, and has the potentials as an antitumor agent. However, a tumor-selectivity of M-β-CyD is low, leading to low antitumor activity and the adverse effects. Meanwhile, hyaluronic acid (HA) is known as a promising tumor targeting ligand, because various cancer cells overexpress CD44, a HA-binding glycoprotein. In the present study, to develop a tumor-selective delivery system for M-β-CyD, we designed a supramolecular complex of M-β-CyD with adamantane-grafted HA (Ad-HA/M-β-CyD) and evaluated it as a tumor-selective antitumor agent...
December 22, 2017: Chemical & Pharmaceutical Bulletin
Toshiya Nagai, Kengo Hanaya, Shuhei Higashibayashi, Mitsuru Shoji, Takeshi Sugai
3β-tert-Butyldimethylsiloxy-22-phenylthio-23,24-bisnorchola-5,9(11)-diene, which has a double bond between C-9 and C-11 and a phenylsulfenyl group on the terminus of the side chain, is a potential synthetic intermediate for steroids with 9,11-unsaturation or 9,11-seco skeletons. We describe here the synthesis of the title compound from 17-ethylenedioxy-3-acetoxyandrosta-3,5-dien-11-one. The introduction of an ethylene unit to 3β-tert-butyldimethylsiloxyandrosta-5,9(11)-dien-17-one by the action of ethyltriphenylphosphonium bromide under basic conditions resulted in an inseparable mixture of two stereoisomeric products (5 : 1)...
2018: Chemical & Pharmaceutical Bulletin
Sabrina Dahlizar, Mika Futaki, Akie Okada, Wesam Radhi Kadhum, Hiroaki Todo, Kenji Sugibayashi
Palmitoyl-glycine-histidine (Pal-GH) is a new low molecular weight gelling agent. It exhibits thixotropic behavior, low viscosity, and high dissolving properties for a wide range of hydrophilic to lipophilic drugs. Orally administered ivermectin (IVM) is used to treat scabies. However, this treatment is associated with well-known side effects, thus a study is awaited to search for alternative routes of administration. Although a topical formulation of IVM could be a candidate, it requires whole body application except the head and face for several hours on a daily basis...
2018: Chemical & Pharmaceutical Bulletin
Rafat Milad Mohareb, Amira Elsayed Mahmoud Abdallah, Abeer Abdelazeem Mohamed
The reactivity of compounds 2-(1-(2-chloroacetyl)-1H-benzo[d]imidazol-2-yl)acetonitrile 2 and 3-(1-(2-chloroacetyl)-1H-benzo[d]imidazol-2-yl)-2H-chromen-2-one 8 towards different chemical reagents were studied and a series of novel benzimidazole derivatives were obtained (2-6a-d and 8-12a-d). Moreover, in vitro growth inhibitory effect of the newly synthesized compounds were evaluated in term of [IC50  µM] against the six cancer cell lines, human lung carcinoma (A549), lung cancer (H460), human colorectal (HT29), gasteric cancer cell (MKN-45), glioma cell line (U87MG) and cellosaurus cell line (SMMC-7721) where foretinib was used as standard reference...
2018: Chemical & Pharmaceutical Bulletin
Yukiko Karuo, Kohei Yamada, Munetaka Kunishima
Benzylating reagents, 4-(4,6-di-t-butyl-1,3,5-triazin-2-yl)-4-benzylmorpholinium triflate, and related derivatives have been developed. The reagents release benzyl triflate as a benzyl cation equivalent upon heating the solution to 40°C under neutral conditions. The O-benzylation of alcohols using a stoichiometric amount of these reagents afforded corresponding benzyl ethers in good to high yields. This was due to the presence of a bulky t-butyl group on the triazine ring of these reagents that prevents the consumption of benzyl triflate via a side reaction with a morpholinotriazine derivative...
2018: Chemical & Pharmaceutical Bulletin
Fumihiko Ogata, Noriaki Nagai, Erimi Ueta, Takehiro Nakamura, Naohito Kawasaki
In this study, we prepared novel adsorbents containing virgin and calcined tapioca products for removing strontium (Sr(II)) and cesium (Cs(I)) from aqueous solutions. The characteristics of tapioca, along with its capacity to adsorb Sr(II) and Cs(I), were evaluated. Multiple tapioca products were prepared and tested. The adsorbent prepared by boiling the tapioca followed by calcination at 300°C (BTP300) was the most effective. In addition, adsorption was affected by the adsorbent's surface properties. The Sr(II) and Cs(I) adsorbed onto BTP300 could be recovered through desorption by hydrochloric acid at different concentrations, which indicates that BTP300 can be used several times for adsorption/desorption...
2018: Chemical & Pharmaceutical Bulletin
Ayaka Chino, Ryushi Seo, Yasushi Amano, Ichiji Namatame, Wataru Hamaguchi, Kazuya Honbou, Takuma Mihara, Mayako Yamazaki, Masaki Tomishima, Naoyuki Masuda
In this study, we report the identification of potent pyrimidoindazoles as phosphodiesterase10A (PDE10A) inhibitors by using the method of fragment-based drug discovery (FBDD). The pyrazolopyridine derivative 2 was found to be a fragment hit compound which could occupy a part of the binding site of PDE10A enzyme by using the method of the X-ray co-crystal structure analysis. On the basis of the crystal structure of compound 2 and PDE10A protein, a number of compounds were synthesized and evaluated, by means of structure-activity relationship (SAR) studies, which culminated in the discovery of a novel pyrimidoindazole derivative 13 having good physicochemical properties...
2018: Chemical & Pharmaceutical Bulletin
Taichiro Togo, Toshiya Taniguchi, Yoshitaka Nakata
Aripiprazole (APZ) is used to treat schizophrenia and is administered as a tablet containing the anhydrous form of APZ. In this study, the effect of compaction force on the crystal form transition was investigated. The crystalline state was observed by X-ray diffraction (XRD). APZ Anhydrous Form II was compacted into tablets. The XRD intensity of anhydrous APZ became lower with higher compressive force. The degree of crystallinity decreased with the compaction force. The powder and the compacted tablets of anhydrous APZ were stored for one week under 60°C and 75% relative humidity...
2018: Chemical & Pharmaceutical Bulletin
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