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Chemical & Pharmaceutical Bulletin

Zhenjiang Xia, Lixin Wei, Yuzhi Du, Lulu Wang, Jichun Han, Qiangqiang He, Haijuan Chen, Xiaoyan Zou, Huali Wu, Jing Shang
Zuotai is a drug containing mercury considered to be the king of Tibetan medicine. The biosafety of Zuotai led people's attention and so far little is known about the toxicity of Zuotai to mast cells. RBL-2H3 cells which used as an alternative model of mast cells were treated with Zuotai, β-HgS and positive drug Compound 48/80 respectively. MTT assay was used to determine the toxicity of drugs to RBL-2H3 cells. The degranulation of RBL-2H3 cells was studied from β-hexosaminidase, histamine, IL-4 and TNF-α...
May 31, 2018: Chemical & Pharmaceutical Bulletin
Hiroaki Todo, Kazuki Sato, Kozo Takayama, Kenji Sugibayashi
Direct compression is a popular choice as it provides the simplest way to prepare the tablet. It can be easily adopted when the active pharmaceutical ingredient (API) is unstable in water or to thermal drying. An optimal formulation of preliminary mixed powders (premix powders) is beneficial if prepared in advance for tableting use. The aim of this study was to find the optimal formulation of the premix powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC) by using statistical techniques...
May 8, 2018: Chemical & Pharmaceutical Bulletin
Keiji Nishiwaki, Kanae Ohigashi, Takahiro Deguchi, Kazuya Murata, Shinya Nakamura, Hideaki Matsuda, Isao Nakanishi
Hydroxychavicol (HC), which is obtained from the leaves of Piper betle Linn. (Piperaceae), inhibits xanthine oxidase (XO) with an IC50 value of 16.7 μM, making it more potent than the clinically used allopurinol (IC50 = 30.7 μM). Herein, a structure-activity relationship analysis of the polar part analogs of HC was conducted and an inhibitor was discovered with a potency 13 times that of HC. Kinetic studies have revealed that HC and its active analog inhibit XO in an uncompetitive manner. The binding structure prediction of these inhibitor molecules to the XO complex with xanthine suggested that both compounds (HC and its analog) could simultaneously form hydrogen bonds with xanthine and XO...
April 26, 2018: Chemical & Pharmaceutical Bulletin
Tomoko Takamiya, Saki Kitamura, Shunichiro Suzuki, Nao Shioda, Yoshifumi Matsuo, Kento Murase, Yuka Kaiho, Yurika Tsurumaki, Yukiko Fujiwara, Mayumi Sone, Tomomi Machida, Ryohei Matsumoto, Aoi Miyamoto, Dai Hirose, Megumi Furukawa, Mitsuko Makino, Keiichi Matsuzaki, Susumu Kitanaka, Tomohisa Yukawa, Hiroshi Iijima
Genus Dendrobium (Orchidaceae) contains numerous species. Phylogenetic analyses based on morphological characteristics and DNA sequences indicated that this genus is divided into two major groups: Asian and Australasian clades. On the other hand, little is known about the phytochemical differences and similarities among the species in each clade. In this study, we selected 18 Dendrobium species (11 from the Asian clade and 7 from the Australasian clade) and constructed HPLC profiles, arrays composed of relative intensity of the chromatographic peaks...
June 1, 2018: Chemical & Pharmaceutical Bulletin
Yoshio Nakano, Yoshimitsu Katakuse, Yasutaka Azechi
An attempt to apply X-Ray Fluorescence (XRF) analysis to evaluate small particle coating process as a Process Analytical Technologies (PAT) was made. The XRF analysis was used to monitor coating level in small particle coating process with at-line manner. The small particle coating process usually consists of multiple coating processes. This study was conducted by a simple coating particles prepared by first coating of a model compound (DL-methionine) and second coating by talc on spherical microcrystalline cellulose cores...
June 1, 2018: Chemical & Pharmaceutical Bulletin
Jia-Xi Wang, Qian Wang, Yong-Qi Zhen, Shuang-Mei Zhao, Feng Gao, Xian-Li Zhou
We isolated two new lathyrane-type diterpenes L27 (1) and L28 (2) along with seven known compounds (3-9) from the seeds of Euphorbia lathyris. These compounds were identified by NMR, high-resolution electrospray ionisation (HR-ESI)-MS as well as IR spectroscopy. Compounds 1 and 2 were assigned NMR spectrums with 1 H-NMR, 13 C-NMR, distortionless enhancement by polarization (DEPT), correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple bond connectivity (HMBC) and nuclear Overhauser effect spectroscopy (NOESY)...
June 1, 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...
June 1, 2018: 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)...
June 1, 2018: Chemical & Pharmaceutical Bulletin
Manman Li, Yanping Chen, Pengfei Zhang, Ling Zhang, Ri Zhou, Yan Xu, Hongda Ding, Qiujing Wang, Zhicai Wang
Twelve pseudo-ginsenosides were synthesized under a mild condition, via a simple three-step called acetylation, elimination-addition and saponification. The inhibitory effects of these twelve 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...
May 1, 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 HPLC coupled with quadrupole time-of-flight (Q-TOF)-MS method for rapid analysis of alkaloids. In qualitative analysis, a total of eight compounds, including four known alkaloids and four unknown components, were detected and identified...
May 1, 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...
May 1, 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.
May 1, 2018: Chemical & Pharmaceutical Bulletin
Yanyan Zhang, Jichen Wang, Chijing Zuo, Weidong Chen, Qian Zhu, Dongdong Guo, Huanru Wu, Huizhuo Wang, Daiyin Peng, Lan Han
Abnormal uterine bleeding (AUB) induced by incomplete abortion is a common gynecological disease. Taohong Siwu decoction (TSD) is a traditional Chinese medicine (TCM) formula, which has been developed to treat AUB for hundreds of years. In this study, rats had incomplete abortion induced in early pregnancy using mifepristone and misoprostol. The duration and quantity of uterine bleeding were recorded and measured. The pathologic histologic grade was evaluated by hematoxylin-eosin staining (HE). Estradiol (E2 ) and progesterone (P) levels were measured by enzyme linked immunosorbent assays (ELISA)...
April 14, 2018: Chemical & Pharmaceutical Bulletin
Xuwen Zhang, Zhaodi Wu, Yongji Lai, Dongyan Li, Jianping Wang, Zengwei Luo, Yongbo Xue, Hucheng Zhu, Chunmei Chen, Yonghui Zhang
Terreinlactone A (1a/1b), a pair of 3-substituted δ-lactone enantiomers, and terreinlactone B (2), a new biosynthetic intermediate of 1a/1b, were isolated from Aspergillus terreus, along with their biosynthetic precursor (+)-terrein (3) and (+)-isoterrein (4). Compounds 1a and 1b were separated by using a Daicel chiral-pak ASH column eluting with n-hexane-EtOH (80:20). The structures of 1a/1b with absolute configurations were determined by comprehensive spectroscopic analyses and electronic circular dichroic (ECD) calculations...
April 13, 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...
April 1, 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...
April 1, 2018: Chemical & Pharmaceutical Bulletin
Davor Jovan Korčok, Nada Aleksandar Tršić-Milanović, Nevena Djuro Ivanović, Brižita Ivan 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...
April 1, 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...
March 1, 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...
March 1, 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...
March 1, 2018: Chemical & Pharmaceutical Bulletin
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