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Acta Pharmaceutica Sinica. B

Gregory Jensen, Christian Morrill, Yu Huang
Tissue engineering and the tissue engineering model have shown promise in improving methods of drug delivery, drug action, and drug discovery in pharmaceutical research for the attenuation of the central nervous system inflammatory response. Such inflammation contributes to the lack of regenerative ability of neural cells, as well as the temporary and permanent loss of function associated with neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and traumatic brain injury. This review is focused specifically on the recent advances in the tissue engineering model made by altering scaffold biophysical and biochemical properties for use in the treatment of neurodegenerative diseases...
September 2018: Acta Pharmaceutica Sinica. B
Ruifeng Wang, Qing Shen, Xue Li, Cao Xie, Weiyue Lu, Songli Wang, Jing Wang, Dongli Wang, Min Liu
The dense extracellular matrix and high interstitial fluid pressure of tumor tissues prevent the ability of anti-tumor agents to penetrate deep into the tumor parenchyma for treatment effects. C-end rule (CendR) peptides can enhance the permeability of tumor blood vessels and tumor tissues via binding to neuropilin-1 (NRP-1), thus aiding in drug delivery. In this study, we selected one of the CendR peptides (sequence RGERPPR) as the parent l-peptide and substituted d-amino acids for the l-amino acids to synthesize its inverso peptide D (RGERPPR)...
September 2018: Acta Pharmaceutica Sinica. B
Xu Zhang, Bing Han, Ziming Feng, Jianshuang Jiang, Yanan Yang, Peicheng Zhang
Three new thionic compounds, ( S )-2-(2-carboxyl-2-hydroxyethylthio)-ferulic acid ( 1 ), ( E )-2-methoxy-4-(3-(methylsulfonyl)prop-1-en-1-yl)phenol ( 2 ), and thiosenkyunolide C ( 3 ), together with two new aromatic glycosides ( 4 and 5 ) were isolated from the rhizome of Ligusticum chuanxiong Hort. Two known compounds ( 6 and 7 ) were also obtained. Their structures were elucidated based on extensive spectroscopic data (UV, IR, 1D and 2D NMR, and HR-ESI-MS). Furthermore the absolute configurations were established by comparison of their calculated and experimental circular dichroism spectra and by a dimolybdenum tetraacetate [Mo2 (AcO)4 ]-induced circular dichroism procedure...
September 2018: Acta Pharmaceutica Sinica. B
Zhenpeng Mai, Gang Ni, Yanfei Liu, Zhao Zhang, Li Li, Naihong Chen, Dequan Yu
The EtOH extracts of the whole plants of Euphorbia helioscopia afforded 17 new jatrophane diterpenoid esters, helioscopianoids A-Q ( 1 - 17 ), along with eight known compounds ( 18 - 25 ). Their structures were elucidated by extensive spectroscopic methods and Mo2 (OAc)4 -induced ECD analysis, and the structures of compounds 1 , 2 , and 7 were confirmed by X-ray crystallography. Compounds 1 - 17 were evaluated for inhibitory effects on P-glycoprotein (P-gp) in an adriamycin (ADM)-resistant human breast adenocarcinoma cell line (MCF-7/ADR) and neuroprotective effects against serum deprivation-induced and rotenone-induced PC12 cell damage...
September 2018: Acta Pharmaceutica Sinica. B
Keke Wang, Ranran Ding, Yanping Ha, Yanan Jia, Xiaomin Liao, Sisi Wang, Rujia Li, Zhihua Shen, Hui Xiong, Junli Guo, Wei Jie
Hypoxia is beneficial for the differentiation of stem cells transplanted for myocardial injury, but mechanisms underlying this benefit remain unsolved. Here, we report the impact of hypoxia-induced Jagged1 expression in cardiomyocytes (CMs) for driving the differentiation of cardiac stem cells (CSCs). Forced hypoxia-inducible factor 1 α (HIF-1 α ) expression and physical hypoxia (5% O2 ) treatment could induce Jagged1 expression in neonatal rat CMs. Pharmacological inhibition of HIF-1 α by YC-1 attenuated hypoxia-promoted Jagged1 expression in CMs...
September 2018: Acta Pharmaceutica Sinica. B
Xiangge Tian, Chao Wang, Peipei Dong, Yue An, Xinyu Zhao, Weiru Jiang, Gang Wang, Jie Hou, Lei Feng, Yan Wang, Guangbo Ge, Xiaokui Huo, Jing Ning, Xiaochi Ma
Human cytosolic sulfotransferase 2A1 (SULT2A1) is an important phase II metabolic enzyme. The detection of SULT2A1 is helpful for the functional characterization of SULT2A1 and diagnosis of its related diseases. However, due to the overlapping substrate specificity among members of the sulfotransferase family, it is difficult to develop a probe substrate for selective detection of SULT2A1. In the present study, through characterization of the sulfation of series of bufadienolides, arenobufagin (AB) was proved as a potential probe substrate for SULT2A1 with high sensitivity and specificity...
September 2018: Acta Pharmaceutica Sinica. B
Weiwei Wang, Chao Liu, Ningyu Zhu, Yuan Lin, Jiandong Jiang, Yanchang Wang, Yan Li, Shuyi Si
Gram-negative bacteria have become the main pathogens and cause serious clinical problems with increased morbidity and mortality. However, the slow discovery of new antimicrobial agents is unable to meet the need for the treatment of bacterial infections caused by drug-resistant strains. The interaction of L12 and L10 is essential for ribosomal function and protein synthesis. In this study, a yeast two-hybrid system was established to successfully detect the interaction between L12 and L10 proteins from gram-negative bacteria Escherichia coli , which allows us to screen compounds that specifically disrupt this interaction...
September 2018: Acta Pharmaceutica Sinica. B
Rajesh Basnet, Grace Qun Gong, Chenyao Li, Ming-Wei Wang
The serum and glucocorticoid inducible protein kinase (SGK) family members share similar structure, substrate specificity and function with AKT and signal downstream of the phosphatidylinositol 3-kinase (PI3K) signalling pathway. They regulate a range of fundamental cellular processes such as cell proliferation and survival, thereby playing an important role in cancer development. This perspective intends to give an overview on the involvement of SGKs (particularly SGK3) in cancer progression, and compares the actions of SGK3 and AKT in cell cycle regulation, oncogenic signalling, and the potential as a therapeutic target for cancer...
September 2018: Acta Pharmaceutica Sinica. B
Eknath Ahire, Shreya Thakkar, Mahesh Darshanwad, Manju Misra
Advancements in in silico techniques of lead molecule selection have resulted in the failure of around 70% of new chemical entities (NCEs). Some of these molecules are getting rejected at final developmental stage resulting in wastage of money and resources. Unfavourable physicochemical properties affect ADME profile of any efficacious and potent molecule, which may ultimately lead to killing of NCE at final stage. Numerous techniques are being explored including nanocrystals for solubility enhancement purposes...
September 2018: Acta Pharmaceutica Sinica. B
Zhoupeng Zhang, Wei Tang
Drug metabolism as a discipline plays an important role in drug discovery and development and the effects of drug metabolism on pharmacokinetics (PK), pharmacodynamics (PD), and safety should be carefully considered. This communication provides an overview of common strategies in the area of drug metabolism for improving PK/PD and safety profiles of drug candidates; these include, but are not limited to, collaboration with medicinal chemists on structure-activity relationships (SAR) to overcome high clearance, using deuterium replacement to further optimize a lead, prodrug approaches to circumvent formulation and delivery difficulties, and addressing issues such as species differences in metabolism, drug-drug interactions (DDI) and formation of reactive metabolites...
September 2018: Acta Pharmaceutica Sinica. B
Jinyi Liu, Xiangjin Zheng, Xiaocong Pang, Li Li, Jinhua Wang, Cui Yang, Guanhua Du
Gangliosides are a class of important glycosphingolipids containing sialic acid that are widely distributed on the outer surface of cells and are abundantly distributed in brain tissue. Disialoganglioside with three glycosyl groups (GD3) and disialoganglioside with two glycosyl groups (GD2) are markedly increased in pathological conditions such as cancers and neurodegenerative diseases. GD3 and GD2 were found to play important roles in cancers by mediating cell proliferation, migration, invasion, adhesion, angiogenesis and in preventing immunosuppression of tumors...
September 2018: Acta Pharmaceutica Sinica. B
Dandan Wang, Liwei Zou, Qiang Jin, Jie Hou, Guangbo Ge, Ling Yang
Mammalian carboxylesterases (CEs) are key enzymes from the serine hydrolase superfamily. In the human body, two predominant carboxylesterases (CES1 and CES2) have been identified and extensively studied over the past decade. These two enzymes play crucial roles in the metabolism of a wide variety of endogenous esters, ester-containing drugs and environmental toxicants. The key roles of CES in both human health and xenobiotic metabolism arouse great interest in the discovery of potent CES modulators to regulate endobiotic metabolism or to improve the efficacy of ester drugs...
September 2018: Acta Pharmaceutica Sinica. B
Jian Bai, Rong Mu, Man Dou, Daojiang Yan, Bingyu Liu, Qian Wei, Jun Wan, Yi Tang, Youcai Hu
Epigenetic modifications have been proved to be a powerful way to activate silent gene clusters and lead to diverse secondary metabolites in fungi. Previously, inactivation of a histone H3 deacetylase in Calcarisporium arbuscula had led to pleiotropic activation and overexpression of more than 75% of the biosynthetic genes and isolation of ten compounds. Further investigation of the crude extract of C. arbuscula ΔhdaA strain resulted in the isolation of twelve new diterpenoids including three cassanes ( 1 - 3 ), one cleistanthane ( 4 ), six pimaranes ( 5 - 10 ), and two isopimaranes ( 11 and 12 ) along with two know cleistanthane analogues...
July 2018: Acta Pharmaceutica Sinica. B
Jianhua Li, Ridao Chen, Ruishan Wang, Xiao Liu, Kebo Xie, Dawei Chen, Jungui Dai
Prenylflavonoids are valuable natural products that have diverse biological properties, and are usually generated biologically by multiple metabolic enzymes in nature. In this study, structurally diverse prenylflavonoids were conveniently synthesized by enzymatic catalysis by combining GuILDT, a regiospecific chalcone prenyltransferase, and GuCHI, a stereospecific chalcone isomerase that has promiscuous activity for both chalcones and prenylchalcones as substrates. Our findings provided a new approach for the synthesis of natural/unnatural bioactive prenylflavonoids, including prenylchalcones and optical prenylflavanones with chalcone origins...
July 2018: Acta Pharmaceutica Sinica. B
Yang Chu, Shuiming Xiao, He Su, Baosheng Liao, Jingjing Zhang, Jiang Xu, Shilin Chen
Ginseng ( Panax ginseng C.A. Meyer) is one of the best-selling herbal medicines, with ginsenosides as its main pharmacologically active constituents. Although extensive chemical and pharmaceutical studies of these compounds have been performed, genome-wide studies of the basic helix-loop-helix (bHLH) transcription factors of ginseng are still limited. The bHLH transcription factor family is one of the largest transcription factor families found in eukaryotic organisms, and these proteins are involved in a myriad of regulatory processes...
July 2018: Acta Pharmaceutica Sinica. B
Xia Lv, Shuguang Zhang, Huipeng Ma, Peipei Dong, Xiaodong Ma, Ming Xu, Yan Tian, Zeyao Tang, Jinyong Peng, Haibo Chen, Jianbin Zhang
Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus...
July 2018: Acta Pharmaceutica Sinica. B
Yao Liu, Qingqing Song, Wenjing Liu, Peng Li, Jun Li, Yunfang Zhao, Liang Zhang, Pengfei Tu, Yitao Wang, Yuelin Song
Herein, a strategy is proposed for the simultaneous determination of primary coumarins in Peucedani Radix (Chinese name: Qianhu). The methodology consists of three consecutive steps: 1) Semi-preparative LC in combination with a home-made automated fraction collection module to fragment the universal metabolome standard into ten fractions (Frs. I-X); 2) LC-accurate MS/MS and quantitative 1 H NMR spectroscopy conducted in parallel to acquire the qualitative and quantitative data of each fraction; 3) Robust identification and quantification of components by use of LC coupled to multiple reaction monitoring...
July 2018: Acta Pharmaceutica Sinica. B
Jian Chen, Xiaona Fan, Jianhua Zhu, Liyan Song, Zhiwei Li, Fei Lin, Rongmin Yu, Hanhong Xu, Jiachen Zi
Four new limonoid-type nortriterpenoids, 1-detigloyl-1- O -methacryloylsalannin ( 1 ), 28-deoxo-2,3-dihydronimbolide ( 2 ), 12-acetoxy-3- O -acetyl-7- O -tigloylvilasinin ( 3 ) and 12-acetoxy-3- O -acetyl-7- O -methacryloylvilasinin ( 4 ), along with five known ones, were isolated from seeds of Azadirachta indica A. Juss. Their structures were elucidated by various spectroscopic methods, including UV, IR, MS, NMR, X-ray crystallography, quantum chemical calculation, as well as by comparison of their spectroscopic data with those reported...
July 2018: Acta Pharmaceutica Sinica. B
Xin Zhang, Qiang Liu, Qianqian Li, Yinghong Li, Zhandong Liu, Hongbin Deng, Sheng Tang, Yanxiang Wang, Youchun Wang, Danqing Song
Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus (EBOV) activities. Structure-activity relationship analysis indicated: (i) 12 N -dichlorobenzyl motif was beneficial for the activity; (ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound 7d exhibited the most potent potency against EBOV with an IC50 value of 5.29 μmol/L and an SI value of over 37...
July 2018: Acta Pharmaceutica Sinica. B
Xu-Nian Wu, Ya-Dan Huang, Jin-Xuan Li, Yan-Fa Yu, Zhou Qian, Chen Zhang, Yinuo Wu, Hai-Bin Luo
The pathological processes of Alzheimer's disease and type 2 diabetes mellitus have been demonstrated to be linked together. Both PDE9 inhibitors and PPAR γ agonists such as rosiglitazone exhibited remarkable preclinical and clinical treatment effects for these two diseases. In this study, a series of PDE9 inhibitors combining the pharmacophore of rosiglitazone were discovered. All the compounds possessed remarkable affinities towards PDE9 and four of them have the IC50 values <5 nmol/L. In addition, these four compounds showed low cell toxicity in human SH-SY5Y neuroblastoma cells...
July 2018: Acta Pharmaceutica Sinica. B
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