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Acta Pharmaceutica Sinica. B

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https://www.readbyqxmd.com/read/28388695/regulation-of-drug-metabolism-and-toxicity-by-multiple-factors-of-genetics-epigenetics-lncrnas-gut-microbiota-and-diseases-a-meeting-report-of-the-21-st-international-symposium-on-microsomes-and-drug-oxidations-mdo
#1
Ai-Ming Yu, Magnus Ingelman-Sundberg, Nathan J Cherrington, Lauren M Aleksunes, Ulrich M Zanger, Wen Xie, Hyunyoung Jeong, Edward M Morgan, Peter J Turnbaugh, Curtis D Klaassen, Aadra P Bhatt, Matthew R Redinbo, Pengying Hao, David J Waxman, Li Wang, Xiao-Bo Zhong
Variations in drug metabolism may alter drug efficacy and cause toxicity; better understanding of the mechanisms and risks shall help to practice precision medicine. At the 21(st) International Symposium on Microsomes and Drug Oxidations held in Davis, California, USA, in October 2-6, 2016, a number of speakers reported some new findings and ongoing studies on the regulation mechanisms behind variable drug metabolism and toxicity, and discussed potential implications to personalized medications. A considerably insightful overview was provided on genetic and epigenetic regulation of gene expression involved in drug absorption, distribution, metabolism, and excretion (ADME) and drug response...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303231/synthesis-characterization-and-pharmacological-evaluation-of-pyrazolyl-urea-derivatives-as-potential-anti-inflammatory-agents
#2
Kanagasabai Somakala, Mohammad Amir
p38α mitogen activated protein kinase (MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders. A series of fifteen pyrazolyl urea derivatives (3a-o) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant potential. Compounds 3a-e, 3g and 3h showed low micromolar range potency (IC50 values ranging from 0.037 ± 1.56 to 0.069 ± 0.07 µmol/L) compared to the standard inhibitor SB 203580 (IC50 = 0.043 ± 3.62 µmol/L) when evaluated for p38α MAPK inhibition by an immunosorbent-based assay...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303230/a-novel-class-of-apical-sodium-dependent-bile-salt-transporter-inhibitors-1-2-4-bifluorophenyl-7-dialkylamino-1-8-naphthyridine-3-carboxamides
#3
Hongtao Liu, Guoxun Pang, Jinfeng Ren, Yue Zhao, Juxian Wang
The apical sodium--dependent bile acid transporter (ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation. Inhibition of ASBT could increase the excretion of bile acids, thus increasing bile acid synthesis and consequently cholesterol consumption. Therefore, ASBT is an attractive target for developing new cholesterol-lowering drugs. In this report, a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303229/cloning-and-characterization-of-squalene-synthase-and-cycloartenol-synthase-from-siraitia-grosvenorii
#4
Huan Zhao, Qi Tang, Changming Mo, Longhua Bai, Dongping Tu, Xiaojun Ma
Mogrosides and steroid saponins are tetracyclic triterpenoids found in Siraitia grosvenorii. Squalene synthase (SQS) and cycloartenol synthase (CAS) are key enzymes in triterpenoid and steroid biosynthesis. In this study, full-length cDNAs of SgSQS and SgCAS were cloned by a rapid amplification of cDNA-ends with polymerase chain reaction (RACE-PCR) approach. The SgSQS cDNA has a 1254 bp open reading frame (ORF) encoding 417 amino acids, and the SgCAS cDNA contains a 2298 bp ORF encoding 765 amino acids. Bioinformatic analysis showed that the deduced SgSQS protein has two transmembrane regions in the C-terminal...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303228/molecular-cloning-and-functional-identification-of-a-cdna-encoding-4-hydroxy-3-methylbut-2-enyl-diphosphate-reductase-from-tripterygium-wilfordii
#5
Qiqing Cheng, Yuru Tong, Zihao Wang, Ping Su, Wei Gao, Luqi Huang
The 4-hydroxy-3-methylbut-2-enyl diphosphate reductase (HDR) is the last step key enzyme of the methylerythritol phosphate (MEP) pathway, synthesizing isopentenyl diphosphate and its allyl isomer dimethylallyl diphosphate, which is important for regulation of isoprenoid biosynthesis. Here the full-length cDNA of HDR, designated TwHDR (GenBank Accession No. KJ933412.1), was isolated from Tripterygium wilfordii for the first time. TwHDR has an open reading frame (ORF) of 1386 bp encoding 461 amino acids. TwHDR exhibits high homology with HDRs of other plants, with an N-terminal conserved domain and three conserved cysteine residues...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303227/analysis-of-cordyceps-by-multi-column-liquid-chromatography
#6
Zhengming Qian, Shaoping Li
Cordyceps is a famous traditional Chinese medicine (TCM) that has been used in China for hundreds of years. In the present study a multi-column liquid chromatography (MC-LC) system was developed for the qualitative analysis of macromolecules and micromolecules in Cordyceps. The MC-LC system includes a size exclusion pre-column, a size exclusion column (SEC) and a reversed phase column (RP) which were controlled by column-switching valves. The sample was separated by the size exclusion pre-column into two fractions (macromolecules and micromolecules)...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303226/simultaneous-determination-of-14-active-constituents-of-shengjiang-xiexin-decoction-using-ultrafast-liquid-chromatography-coupled-with-electrospray-ionization-tandem-mass-spectrometry
#7
Gang Peng, Huanyu Guan, Xiaoming Wang, Yue Shi
An effective herbal medicinal prescription of Shengjiang Xiexin decoction (SXD) was used in treating the inflammatory bowel disease in clinic. In this study, an ultrafast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) method was developed to separate and to simultaneously determine 14 major active ingredients in SXD. Chromatographic separation was successfully accomplished on an Acquity BEH C18 (100 mm×2.1 mm, 1.7 μm) column using gradient elution with 0.1% (v/v) formic acid water (A) and 0...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303225/identification-and-differentiation-of-major-components-in-three-different-sheng-ma-crude-drug-species-by-uplc-q-tof-ms
#8
Mengxue Fan, Kunming Qin, Fei Ding, Yuting Huang, Xiaoli Wang, Baochang Cai
Cimicifugae Rhizoma (Sheng ma) is a Ranunculaceae herb belonging to a composite family and well known in China. has been widely used in traditional Chinese medicine. The Pharmacopoeia of the People׳s Republic of China contains three varieties (Cimicifuga dahurica (Turcz.), Cimicifuga foetida L. and Cimicifuga heracleifolia Kom.) which have been used clinically as "Sheng-ma". However, the chemical constituents of three components of "Sheng-ma" have never been documented. In this study, a rapid method for the analysis of the main components of "Sheng-ma" was developed using ultra-high performance liquid chromatography with quadrupole-time-of-flight mass spectrometry (UPLC/Q-TOF-MS)...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303224/aromatic-compounds-from-an-aqueous-extract-of-ban-lan-gen-and-their-antiviral-activities
#9
Yufeng Liu, Minghua Chen, Qinglan Guo, Yuhuan Li, Jiandong Jiang, Jiangong Shi
A pair of new diphenyl glycerol ether enantiomers (-)-1 and (+)-1 and two new methyl benzamidobenzoates 2 and 3, named (-)-(R)- and (+)-(S)-isatindigotrioic acid [(-)-1 and (+)-1] and isatindigoticamides A (2) and B (3), respectively, were isolated from an aqueous decoction of the roots of Isatis indigotica (ban lan gen). Their structures were elucidated by spectroscopic data analysis including 2D NMR experiments. The absolute configurations of (-)-1 and (+)-1 were assigned based on the CD exciton chirality method...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303223/four-new-phenolic-glycosides-from-baoyuan-decoction
#10
Xiaoli Ma, Xiaoyu Guo, Mingbo Zhao, Pengfei Tu, Yong Jiang
Four new phenolic glycosides, including two flavonoid glycosides (1 and 2) and two lignan glycosides (3 and 4), were isolated from the traditional Chinese medicine formula, Baoyuan decoction. Their structures were established by detailed analysis of the NMR and HR-ESI-MS spectroscopic data and their absolute configurations were determined by the experimental electronic circular dichroism data as well as chemical methods. Furthermore, the sources of the four new compounds were determined by the UPLC-Qtrap-MS method, which proved that 1 and 2 are originated from Glycyrrhiza uralensis, and 3 and 4 are from Cinnamomum cassia...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303222/a-set-of-interesting-sequoiatones-stereoisomers-from-a-wetland-soil-derived-fungus-talaromyces-flavus
#11
Tianyu Sun, Jian Zou, Guodong Chen, Dan Hu, Bin Wu, Xingzhong Liu, Xinsheng Yao, Hao Gao
Four interesting sequoiatones stereoisomers (1-4) were isolated from a wetland soil-derived fungus Talaromyces flavus by chiral HPLC. On the basis of comprehensive NMR and mass analyses, their planar structures were elucidated as the same as that of sequoiatone B. Among them, 1 and 3 (or 2 and 4) were a pair of enantiomers, and 1 and 2 (or 3 and 4) were a pair of stereoisomers with epimerization at C-12, which indicated that sequoiatione-type metabolites exist as enantiomers rather than as optically pure compounds in some strains...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303221/salvianolic-acid-a-alleviates-renal-injury-in-systemic-lupus-erythematosus-induced-by-pristane-in-balb-c-mice
#12
Yihuang Lin, Yu Yan, Huifang Zhang, Yucai Chen, Yangyang He, Shoubao Wang, Lianhua Fang, Yang Lv, Guanhua Du
The purpose of this study was to investigate the effects of salvianolic acid A (SAA) in systemic lupus erythematosus (SLE) induced by pristane in BALB/c mice. Lupus mice were established by confirming elevated levels of autoantibodies and IL-6 after intraperitoneal injection of pristane. Mice were then treated with daily oral doses of SAA for 5 months in parallel with mice treated with prednisone and aspirin as positive controls. The levels of autoantibodies were monitored at monthly intervals and nephritic symptoms observed by hematoxylin and eosin (H&E) and periodic acid-Schiff (PAS) staining...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303220/anemone-medicinal-plants-ethnopharmacology-phytochemistry-and-biology
#13
REVIEW
Da-Cheng Hao, Xiaojie Gu, Peigen Xiao
The Ranunculaceae genus Anemone (order Ranunculales), comprising more than 150 species, mostly herbs, has long been used in folk medicine and worldwide ethnomedicine. Various medicinal compounds have been found in Anemone plants, especially triterpenoid saponins, some of which have shown anti-cancer activities. Some Anemone compounds and extracts display immunomodulatory, anti-inflammatory, antioxidant, and antimicrobial activities. More than 50 species have ethnopharmacological uses, which provide clues for modern drug discovery...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303219/new-sensor-technologies-in-quality-evaluation-of-chinese-materia-medica-2010-2015
#14
REVIEW
Xiaosu Miao, Qingyu Cui, Honghui Wu, Yanjiang Qiao, Yanfei Zheng, Zhisheng Wu
New sensor technologies play an important role in quality evaluation of Chinese materia medica (CMM) and include near-infrared spectroscopy, chemical imaging, electronic nose and electronic tongue. This review on quality evaluation of CMM and the application of the new sensors in this assessment is based on studies from 2010 to 2015, with prospects and opportunities for future research.
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303218/the-modification-of-natural-products-for-medical-use
#15
REVIEW
Zongru Guo
Drug innovation is characterized by painstaking molecular-level syntheses and modifications as the basic components of research and development. Similarly, natural products are chemically tailored and modified based upon their structural and biological properties. To some extent, the modification of natural products is quite different from de novo structure-based drug discovery. This review describes the general strategies and principles for the modification of natural products to drugs, as illustrated by several successful medicines that originated from natural products...
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303217/editorial
#16
EDITORIAL
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28303216/editor-profile-luqi-huang-and-wei-gao
#17
EDITORIAL
(no author information available yet)
No abstract text is available yet for this article.
March 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119815/synthesis-of-hydroxycinnamic-acid-derivatives-as-mitochondria-targeted-antioxidants-and-cytotoxic-agents
#18
Jiyu Li, Dian He, Baitao Wang, Ling Zhang, Kun Li, Qinjian Xie, Lifang Zheng
In order to develop agents with superior chemopreventive and chemotherapeutic properties against hepatocellular carcinomas, mitochondria-targeted hydroxycinnamic acids (MitoHCAs) were synthesized by conjugation with a triphenylphosphonium cation. These synthetic compounds were evaluated for their antioxidant activities in hepatic mitochondria, including against OH(∙-) and ROO(∙-) induced lipid peroxidation. H2O2 production was decreased significantly by increasing glutathione peroxidase and catalase activities...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119814/structure-of-the-40s-ribosomal-subunit-of-plasmodium-falciparum-by-homology-and-de-novo-modeling
#19
Harrison Ndung'u Mwangi, Peter Wagacha, Peterson Mathenge, Fredrick Sijenyi, Francis Mulaa
Generation of three dimensional structures of macromolecules using in silico structural modeling technologies such as homology and de novo modeling has improved dramatically and increased the speed by which tertiary structures of organisms can be generated. This is especially the case if a homologous crystal structure is already available. High-resolution structures can be rapidly created using only their sequence information as input, a process that has the potential to increase the speed of scientific discovery...
January 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28119813/c0818-a-novel-curcumin-derivative-interacts-with-hsp90-and-inhibits-hsp90-atpase-activity
#20
Yingjuan Fan, Yang Liu, Lianru Zhang, Fang Cai, Liping Zhu, Jianhua Xu
The aims of the present study were to estimate the affinity between 3,5-(E)-bis(3-methoxy-4-hydroxybenzal)-4-piperidinone hydrochloride (C0818) and heat shock protein 90 (Hsp90) and to investigate the inhibitory effects of this compound on Hsp90 ATPase activity. Fluorescence spectroscopy was used to examine the affinity between varying concentrations of C0818 and Hsp90, N-Hsp90, M-Hsp90 and C-Hsp90. Fluorescence intensities were recorded in the range of 290-510 nm at 293, 303 and 310 K, respectively. A colorimetric assay for inorganic phosphate (based on the formation of a phosphomolybdate complex and the subsequent reaction with malachite green) were used to examine the inhibitory effects of C0818 on Hsp90 ATPase activity...
January 2017: Acta Pharmaceutica Sinica. B
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