Read by QxMD icon Read

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 HNMR and HRMS (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...
September 7, 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 iNOS and 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...
August 21, 2018: Chemical & Pharmaceutical Bulletin
Mohammed K Abd Elhameid, Noha Ryad, Al-Shorbagy My, 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...
August 14, 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 compounds 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...
July 25, 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
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
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
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"