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Chemical & Pharmaceutical Bulletin

Qin-Qin Zhao, Xiang Li, Li-Ping Luo, Yi Qian, Yi-Lin Liu, Hang-Ting Wu
Stroke is one of the leading causes of death and disability globally, while intravenous thrombolysis with recombinant tissue plasminogen activator remains the only FDA-approved therapy for ischemic stroke. The attempts to develop new treatments for acute ischemic stroke meet costly and spectacularly disappointing results, which requires both long time and high costs, whereas repurposing of safe existing drugs to new indications provides a cost-effective and not time-consuming alternative. Vascular protection is a promising strategy for improving stroke outcome, as vascular function is critical to both cardiovascular diseases (CVD) and ischemic cerebrovascular disease (ICD)...
November 8, 2018: Chemical & Pharmaceutical Bulletin
Noriyuki Hayashi, Yusuke Miura, Satoshi Yokoshima, Tohru Fukuyama
An alternative synthetic route toward a key intermediate in the total synthesis of isoschizogamine is described. The Claisen-Johnson rearrangement stereoselectively constructed a quaternary carbon. Trifluoroperacetic acid mediated the Baeyer-Villiger oxidation to form a bicyclic lactone. The Mukaiyama-Matsuo protocol converted the lactone into an α,β-unsaturated lactone, that was used as the substrate for the rhodium-mediated 1,4-addition of an arylboronic acid.
October 31, 2018: Chemical & Pharmaceutical Bulletin
Nobumichi Ohoka, Osamu Ujikawa, Kenichiro Shimokawa, Tomoya Sameshima, Norihito Shibata, Takayuki Hattori, Hiroshi Nara, Nobuo Cho, Mikihiko Naito
Targeted protein degradation by small molecules is an emerging modality with significant potential for drug discovery. We previously developed chimeric molecules, termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which induce the ubiquitylation and proteasomal degradation of target proteins. This degradation is mediated by the IAPs; the target proteins include bromodomain-containing protein 4 (BRD4), an epigenetic regulator protein. The SNIPER that degrades this particular protein, SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a bromodomain and extra-terminal (BET) inhibitor, (+)-JQ-1...
October 26, 2018: Chemical & Pharmaceutical Bulletin
Yosuke Ota, Arisa Nakamura, Elghareeb E Elboray, Yukihiro Itoh, Takayoshi Suzuki
Prodrug approaches are useful for enhancing the efficacies and reducing the side effects of anticancer drugs. Previously, we proposed a prodrug strategy for targeting cancers overexpressing lysine-specific demethylase 1 (LSD1), namely, conjugates of trans-2-phenylcyclopropylamine (PCPA, an LSD1 inhibitor) and anticancer drugs. In this study, we applied this prodrug strategy to the anticancer agent 5-fluorouracil (5-FU). In vitro assays showed that the PCPA-5-FU conjugate (1) released 5-FU upon the inhibition of LSD1...
October 24, 2018: Chemical & Pharmaceutical Bulletin
Hirofumi Ochiai, Kenta Yoshida, Hiroshi Shibutani, Akio Kanatani, Yuji Nishiuchi
Reversibly glycosylated conjugates were developed by adding complex-type N-linked oligosaccharides to peptides through self-cleavable linkers with the aim of increasing the solubility and stability of the peptides in plasma. The amino or carboxyl group of the peptide was connected to a glycosylated Ascendis or ester/thioester-type linker, respectively. Use of the linkers enabled extended release of the peptides depending on the pH and temperature of the buffer according to a first order reaction, and their cleavage rate was also affected by the structure of the peptide-linker coupling...
October 10, 2018: Chemical & Pharmaceutical Bulletin
Mohammed K Abd El Hameid
The work reported the design and cytotoxic screening of synthetic small molecules: carbonitriles 3a-c, carboximidamides 4a-c, and oxadiazoles 5-19 as antitumor molecules. Molecules 4c, 9, 12, and 14 show promising cytotoxicity profiles against two cell lines higher than prodigiosin (PG). The results of topoisomerase enzyme inhibition assay show that carboximidamide 4c and oxadiazole 14 display potent inhibitory activity in nano-molar concentration higher than PG. In addition, carboximidamide 4c and oxadiazoles 9, 12, and 14 exhibit antiproliferative activities over MCF-7 cells by cell cycle arrest at G1  phase and apoptosis inducing activity by increasing cell population percentages at pre G1  and G2 /M phases as shown by DNA-flow cytometry assay and annexin V analysis...
October 5, 2018: Chemical & Pharmaceutical Bulletin
Takaya Togo, Youhei Sohma, Yoichiro Kuninobu, Motomu Kanai
We developed a palladium-catalyzed C-H N-heteroarylation of N-protected-2,5-disubstituted imidazoles at the C4-position using N-heteroaryl halides as a coupling partner. Intensive reaction condition screening led us to identify fluorinated bathophenanthroline 7 as the optimum ligand for the palladium catalyst. This reaction will enhance lead optimization of drug candidates by facilitating the synthesis of heterobiaryl compounds containing an imidazole ring.
October 4, 2018: Chemical & Pharmaceutical Bulletin
Hanan M El-Laithy, Alia Badawi, Nevine Shawky Abdelmalak, Nihal El-Sayyad
Clopidogrel bisulphate (CB) is a first line antiplatelet drug for treatment of myocardial infarction and stoke. Yet, its efficacy is limited by its poor solubility in intestinal pH, its main site of absorption. The main aim of this study is to enhance the intestinal release of CB by loading in cubosome nanoparticles. Glyceryl monooleate (GMO) based CB loaded cubosomes were prepared using a 33 factorial design to study the effect of polyvinyl alcohol (PVA), poloxamer 407 (PL407) concentrations and ratio of CB to the disperse phase on the average particle size, entrapment efficiency (%EE), in vitro release at 15 minutes (%Q15 ), and their morphology using TEM...
September 19, 2018: Chemical & Pharmaceutical Bulletin
Jiajia Feng, Hui Qi, Xiaoyang Sun, Siran Feng, Zhenming Liu, Yali Song, Xiaoqiang Qiao
Molecules bearing pyrazole nucleus present diverse biological properties such as antitumor and anti-inflammatory activities that can be associated with DNA interactions. This study aimed to the synthesis of new pyrazol derivatives and evaluated their ability to interact with the DNA and antitumor and topoisomerase inhibition activities. All derivatives were successfully synthesized, and their structures were elucidated by 1 H-NMR and high resolution (HR)-MS (electrospray ionization positive mode (ESI+ )). Antiproliferative inhibition assays, UV titration assays, fluorescence titration assays, circular dichroism (CD) assays, KI quenching studies, topoisomerase inhibitory activity assays and molecular docking were evaluated for these compounds...
November 1, 2018: Chemical & Pharmaceutical Bulletin
Le Thi Vien, Tran Thi Hong Hanh, Phan Thi Thanh Huong, Nguyen Hai Dang, Nguyen Van Thanh, Nguyen Xuan Cuong, Nguyen Hoai Nam, Do Cong Thung, Phan Van Kiem, Chau Van Minh
Seven anthraquinones including two new compounds namely capillasterquinones A and B (1 and 2) and one new butenolide namely capillasterolide (8) were isolated and structurally elucidated from the crinoid Capillaster multiradiatus. The inhibitory effect of compounds 1-8 on lipopolysaccharide (LPS)-induced nitric oxide (NO) production as well as inhibition of 1 on expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) proteins in RAW264.7 cells were also evaluated. As the obtained results, capillasterquinone A (1) showed strong NO production inhibitory activity with an IC50 of 5...
November 1, 2018: Chemical & Pharmaceutical Bulletin
Mohammed K Abd Elhameid, Noha Ryad, M Y Al-Shorbagy, Manal R Mohammed, Mohammed M Ismail, Salwa El Meligie
A new series of pyridine and pyrimidine derivatives is designed and synthesized as potential antitumor molecules. The tested compounds show promising in vitro cytotoxic activity against HL-60 cell line as eight compounds: 4, 6, 11, 13, 14, 15, 18 and 21 exhibit potent cytotoxic activity in sub-micromolar concentration higher than the combretastatin A4 (CA-4). Compound 21 shows a cytotoxic activity 5-fold more potent than CA-4 on HL-60 cells. DNA-Flow cytometry cell cycle analysis and annexin-V assay on HL-60 cells show that compounds 4, 18 and 21 exhibit potent cell growth inhibition, cell cycle arrest at G2 /M phase and pro-apoptotic inducing activities...
October 1, 2018: Chemical & Pharmaceutical Bulletin
Abdelsattar M Omar, Tamer M Abdelghany, Mohamed S Abdel-Bakky, Abdulrahman M Alahdal, Mohamed F Radwan, Moustafa E El-Araby
The 2-styryl-3,5-dihydro-4H-imidazol-4-one might be considered as a system with isosteric properties similar to trans-cinnamaldehyde (styrylaldehyde), a safe natural compound that exhibited interesting activities against various cancers. We synthesized a series of compounds that differ structurally in having different alkyl, aryl and heterocyclic substituents at the N3 position of the 2-styryl-4-imidaolone pharmacophore. The compounds were assayed for their cytotoxicity against both cancer and normal cell lines...
October 1, 2018: 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. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (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, interleukin (IL)-4 and tumor necrosis factor-α (TNF-α)...
August 1, 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...
July 1, 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...
July 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)...
July 1, 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...
July 1, 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
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