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Acta Pharmaceutica Sinica. B

Zhizhen Qin, Shoubao Wang, Yihuang Lin, Ying Zhao, Shengqian Yang, Junke Song, Tao Xie, Jinlong Tian, Song Wu, Guanhua Du
A mangiferin aglycon derivative J99745 has been identified as a potent xanthine oxidase (XOD) inhibitor by previous in vitro study. This study aimed to evaluate the hypouricemic effects of J99745 in experimental hyperuricemia mice, and explore the underlying mechanisms. Mice were orally administered 600 mg/kg xanthine once daily for 7 days and intraperitoneally injected 250 mg/kg oxonic acid on the 7th day to induce hyperuricemia. Meanwhile, J99745 (3, 10, and 30 mg/kg), allopurinol (20 mg/kg) or benzbromarone (20 mg/kg) were orally administered to mice for 7 days...
March 2018: Acta Pharmaceutica Sinica. B
Yu Zhang, Zhichao Xu, Aijia Ji, Hongmei Luo, Jingyuan Song
Tanshinones are a class of bioactive components in the traditional Chinese medicine Salvia miltiorrhiza , and their biosynthesis and regulation have been widely studied. Current studies show that basic leucine zipper (bZIP) proteins regulate plant secondary metabolism, growth and developmental processes. However, the bZIP transcription factors involved in tanshinone biosynthesis are unknown. Here, we conducted the first genome-wide survey of the bZIP gene family and analyzed the phylogeny, gene structure, additional conserved motifs and alternative splicing events in S...
March 2018: Acta Pharmaceutica Sinica. B
Yuanyuan Shi, Zhibo Jiang, Xingxing Li, Lijie Zuo, Xuan Lei, Liyan Yu, Linzhuan Wu, Jiandong Jiang, Bin Hong
Chuangxinmycin is an antibiotic isolated from Actinoplanes tsinanensis CPCC 200056 in the 1970s with a novel indole-dihydrothiopyran heterocyclic skeleton. Chuangxinmycin showed in vitro antibacterial activity and in vivo efficacy in mouse infection models as well as preliminary clinical trials. But the biosynthetic pathway of chuangxinmycin has been obscure since its discovery. Herein, we report the identification of a stretch of DNA from the genome of A. tsinanensis CPCC 200056 that encodes genes for biosynthesis of chuangxinmycin by bioinformatics analysis...
March 2018: Acta Pharmaceutica Sinica. B
Linlin Dong, Jiang Xu, Lianjuan Zhang, Ruiyang Cheng, Guangfei Wei, He Su, Juan Yang, Jun Qian, Ran Xu, Shilin Chen
The cultivation of Panax plants is hindered by replanting problems, which may be caused by plant-driven changes in the soil microbial community. Inoculation with microbial antagonists may efficiently alleviate replanting issues. Through high-throughput sequencing, this study revealed that bacterial diversity decreased, whereas fungal diversity increased, in the rhizosphere soils of adult ginseng plants at the root growth stage under different ages. Few microbial community, such as Luteolibacter , Cytophagaceae, Luteibacter , Sphingomonas , Sphingomonadaceae, and Zygomycota, were observed; the relative abundance of microorganisms, namely, Brevundimonas , Enterobacteriaceae, Pandoraea , Cantharellales, Dendryphion , Fusarium , and Chytridiomycota, increased in the soils of adult ginseng plants compared with those in the soils of 2-year-old seedlings...
March 2018: Acta Pharmaceutica Sinica. B
Tongcheng Dai, Kuan Jiang, Weiyue Lu
The blood-brain barrier (BBB) and the blood-brain tumor barrier (BBTB) prevent drug and nano-drug delivery systems from entering the brain. However, ligand-mediated nano-drug delivery systems have significantly enhanced the therapeutic treatment of glioma. In this study we investigated the mechanism especially the integrity of liposomes and lipid disks while traversing the BBB and BBTB both in vitro and in vivo . Fluorophores (DiO, DiI and DiD) were loaded into liposomes and lipid disks to form Förster resonance energy transfer (FRET) nano-drug delivery systems...
March 2018: Acta Pharmaceutica Sinica. B
Xiaomei Gu, Qing Xiao, Qian Ruan, Yuezhong Shu, Ashok Dongre, Ramaswamy Iyer, W Griffith Humphreys, Yurong Lai
In the present study, total membrane proteins from tumor cell lines including HepG2, Hep3B2, H226, Ovcar3 and N87 were extracted and digested with γ LysC and trypsin. The resulting peptide lysate were pre-fractionated and subjected to untargeted quantitative proteomics analysis using a high resolution mass spectrometer. The mass spectra were processed by the MaxQuant and the protein abundances were estimated using total peak area (TPA) method. A total of 6037 proteins were identified, and the analysis resulted in the identification of 2647 membrane proteins...
March 2018: Acta Pharmaceutica Sinica. B
Xiaoxv Gao, Chengpeng Sun, Zhenglong Yu, Jian Cang, Xiangge Tian, Xiaokui Huo, Lei Feng, Xinguang Liu, Chao Wang, Baojing Zhang, Xiaochi Ma
In order to clarify regions of production and to discriminate processing methods, quantitative and qualitative analyses for saccharides and terpenes in 35 batches of Alismatis Rhizoma were performed. Methodologies included HPLC-PDA, HPLC-VWD and UHPLC-MS n , combined with principal component analysis (PCA) and partial least squares regression techniques (PLSR). The inhibitory effects of triterpenes and Alismatis Rhizoma extracts on lipase activity were evaluated in vitro . PLSR analysis revealed significant positive correlations ( R 2 = 0...
March 2018: Acta Pharmaceutica Sinica. B
Qingce Zang, Yang Gao, Luojiao Huang, Jiuming He, Sheng Lin, Hongtao Jin, Ruiping Zhang, Zeper Abliz
With the rapid development and wide application of traditional Chinese medicine injection (TCMI), a number of adverse events of some TCMIs have incessantly been reported and have drawn broad attention in recent years. Establishing effective and practical analytical methods for safety evaluation and quality control of TCMI can help to improve the safety of TCMIs in clinical applications. In this study, a sensitive and rapid high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method has been developed and validated for the quantitative determination of potentially harmful substance 5,5'-oxydimethylenebis (2-furfural, OMBF) in TCMI samples...
March 2018: Acta Pharmaceutica Sinica. B
Chunsu Liang, Hui Sun, Xiangjun Meng, Lei Yin, J Paul Fawcett, Huaidong Yu, Ting Liu, Jingkai Gu
Because many therapeutic agents are contaminated by epimeric impurities or form epimers as a result of metabolism, analytical tools capable of determining epimers are increasingly in demand. This article is a proof-of-principle report of a novel DMS-MS/MS method to separate and simultaneously quantify epimers, taking PGF2 α and its 8-epimer, 8- iso -PGF2 α , as an example. Good accuracy and precision were achieved in the range of 10-500 ng/mL with a run time of only 1.5 min. Isopropanol as organic modifier facilitated a good combination of sensitivity and separation...
March 2018: Acta Pharmaceutica Sinica. B
Yan Lu, Yun Jiang, Lijun Ling, Yunyi Zhang, Hong Li, Daofeng Chen
Houttuynia cordata Thunb. is a traditional herb used for clearing heat and eliminating toxins, and has also been used for the treatment of severe acute respiratory syndrome (SARS). In vitro, the crude H. cordata polysaccharides (CHCP) exhibited potent anti-complementary activity through both the classical and alternative pathways by acting on components C3 and C4 of the complement system without interfering with the coagulation system. This study was to investigate the preventive effects of CHCP on acute lung injury (ALI) induced by hemorrhagic shock plus lipopolysaccharide (LPS) instillation (two-hit) and LPS-induced fever in rats...
March 2018: Acta Pharmaceutica Sinica. B
Xue Han, Hong Jiang, Li Han, Xi Xiong, Yanan He, Chaomei Fu, Runchun Xu, Dingkun Zhang, Junzhi Lin, Ming Yang
Traditional Chinese herbs (TCH) are currently gaining attention in disease prevention and health care plans. However, their general bitter taste hinders their use. Despite the development of a variety of taste evaluation methods, it is still a major challenge to establish a quantitative detection technique that is objective, authentic and sensitive. Based on the two-bottle preference test (TBP), we proposed a novel quantitative strategy using a standardized animal test and a unified quantitative benchmark. To reduce the difference of results, the methodology of TBP was optimized...
March 2018: Acta Pharmaceutica Sinica. B
Qing Chen, Ke Tang, Xiaoyu Zhang, Panpan Chen, Ying Guo
Filoviruses cause severe and fatal viral hemorrhagic fever in humans. Filovirus research has been extensive since the 2014 Ebola outbreak. Due to their high pathogenicity and mortality, live filoviruses require Biosafety Level-4 (BSL-4) facilities, which have restricted the development of anti-filovirus vaccines and drugs. An HIV-based pseudovirus cell infection assay is widely used for viral entry studies in BSL-2 conditions. Here, we successfully constructed nine in vitro pseudo-filovirus models covering all filovirus genera and three in vivo pseudo-filovirus-infection mouse models using Ebola virus, Marburg virus, and Lloviu virus as representative viruses...
March 2018: Acta Pharmaceutica Sinica. B
Eneida Turiján-Espinoza, Rául Alejandro Salazar-González, Edith Elena Uresti-Rivera, Gloria Estela Hernández-Hernández, Montserrat Ortega-Juárez, Rosa Milán, Diana Portales-Pérez
Arylamine N -acetyltransferase (NAT; E.C. enzymes are responsible for the biotransformation of several arylamine and hydrazine drugs by acetylation. In this process, the acetyl group transferred to the acceptor substrate produces NAT deacetylation and, in consequence, it is susceptible of degradation. Sirtuins are protein deacetylases, dependent on nicotine adenine dinucleotide, which perform post-translational modifications on cytosolic proteins. To explore possible sirtuin participation in the enzymatic activity of arylamine NATs, the expression levels of NAT1, NAT2, SIRT1 and SIRT6 in peripheral blood mononuclear cells (PBMC) from healthy subjects were examined by flow cytometry and Western blot...
March 2018: Acta Pharmaceutica Sinica. B
Wen Jin, Bing Cui, Pingping Li, Fang Hua, Xiaoxi Lv, Jichao Zhou, Zhuowei Hu, Xiaowei Zhang
Vitamin D3 has been found to produce therapeutic effects on obesity-associated insulin resistance and dyslipidemia through its potent anti-inflammatory activity, but the precise immunomodulatory mechanism remains poorly understood. In the present study we found that 1,25-dihydroxyvitamin D3 [1,25(OH)2 D3 ], the biologically active form of vitamin D3 , significantly attenuated monosodium glutamate (MSG)-induced obesity and insulin resistance as indicated by body weight reduction, oral glucose tolerance improvement, and a glucose infusion rate increase as detected with hyperinsulinemic-euglycemic clamp...
March 2018: Acta Pharmaceutica Sinica. B
Yixian Zhou, Guilan Quan, Qiaoli Wu, Xiaoxu Zhang, Boyi Niu, Biyuan Wu, Ying Huang, Xin Pan, Chuanbin Wu
Mesoporous silica nanoparticles (MSNs) are attracting increasing interest for potential biomedical applications. With tailored mesoporous structure, huge surface area and pore volume, selective surface functionality, as well as morphology control, MSNs exhibit high loading capacity for therapeutic agents and controlled release properties if modified with stimuli-responsive groups, polymers or proteins. In this review article, the applications of MSNs in pharmaceutics to improve drug bioavailability, reduce drug toxicity, and deliver with cellular targetability are summarized...
March 2018: Acta Pharmaceutica Sinica. B
Angela M Wagner, Margaret P Gran, Nicholas A Peppas
Therapeutic proteins and peptides have revolutionized treatment for a number of diseases, and the expected increase in macromolecule-based therapies brings a new set of challenges for the pharmaceutics field. Due to their poor stability, large molecular weight, and poor transport properties, therapeutic proteins and peptides are predominantly limited to parenteral administration. The short serum half-lives typically require frequent injections to maintain an effective dose, and patient compliance is a growing issue as therapeutic protein treatments become more widely available...
March 2018: Acta Pharmaceutica Sinica. B
Juan Zhang, Chengshi Jiang, João Paulo Figueiró Longo, Ricardo Bentes Azevedo, Hua Zhang, Luis Alexandre Muehlmann
Photodynamic therapy (PDT), based on the photoactivation of photosensitizers (PSs), has become a well-studied therapy for cancer. Photofrin® , belonging to the first generation of PS, is still widely used for the treatment of different kinds of cancers; however, it has several drawbacks that significantly limit its general clinical use. Consequently, there has been extensive research on the design of PS molecules with optimized pharmaceutical properties, with aiming of overcoming the disadvantages of traditional PS, such as poor chemical purity, long half-life, excessive accumulation into the skin, and low attenuation coefficients...
March 2018: Acta Pharmaceutica Sinica. B
Xingquan Zhang
The pace of discovery of new antiretroviral (ARV) drugs has slowed, although the efficacy and safety of once-daily fixed dose combinations have been extensively investigated. Several traditional ARV drugs remain in phase III clinical trials. This review summarizes current information on ARV drugs in phase III clinical trials and focuses on the development of ARV drugs in the next decade.
March 2018: Acta Pharmaceutica Sinica. B
Limei Wang, Kewei Wang
To foster communication and interactions amongst international scholars and scientists in the field of ion channel research, the 6th International Ion Channel Conference (IICC-2017) was held between June 23-27, 2017 in the eastern coastal city of Qingdao, China. The meeting consisted of 450 attendees and 130 speakers and poster presenters. The program consisted of research progress, new findings and ongoing studies that were focused on (1) Ion channel structure and function; (2) Ion channel physiology and human diseases; (3) Ion channels as targets for drug discovery; (4) Technological advances in ion channel research...
November 2017: Acta Pharmaceutica Sinica. B
Xuewei Cheng, Xia Lv, Hengyan Qu, Dandan Li, Mengmeng Hu, Wenzhi Guo, Guangbo Ge, Ruihua Dong
UDP-glucuronosyltransferase 1A1 (UGT1A1) plays a key role in detoxification of many potentially harmful compounds and drugs. UGT1A1 inhibition may bring risks of drug-drug interactions (DDIs), hyperbilirubinemia and drug-induced liver injury. This study aimed to investigate and compare the inhibitory effects of icotinib and erlotinib against UGT1A1, as well as to evaluate their potential DDI risks via UGT1A1 inhibition. The results demonstrated that both icotinib and erlotinib are UGT1A1 inhibitors, but the inhibitory effect of icotinib on UGT1A1 is weaker than that of erlotinib...
November 2017: Acta Pharmaceutica Sinica. B
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