Dong Mei, Binlong Chen, Bing He, Haibin Liu, Zhiqiang Lin, Jialiang Lin, Xiaoyan Zhang, Ning Sun, Libo Zhao, Xiaoling Wang, Qiang Zhang
[This corrects the article DOI: 10.1016/j.apsb.2019.03.006.].
June 2020: Acta Pharmaceutica Sinica. B
Qiong Xiao, Minwan Hu, Si Chen, Yifan Tang, Zeyu Shi, Jing Jin, Jinping Hu, Ping Xie, Dali Yin
FTY720 and IMMH002, prodrugs for sphingosine-1-phosphate receptor 1 (S1P1 ) agonists, show inadequate and inconsistent levels of phosphorylation in humans compared to that in rats. In this study, FTY720 or IMMH002 analogues ( 21 - 24 ) were designed and synthesized with modified head pieces to improve the biotransformation of the prodrugs to the active phosphorylated forms. Target compounds were synthesized via a convergent route using the key and optically pure building block 9 , which was first synthesized via asymmetrically catalyzed amination...
June 2020: Acta Pharmaceutica Sinica. B
Ji Li, Yitian Du, Haitao Su, Shixuan Cheng, Yanxia Zhou, Yiguang Jin, Xian-Rong Qi
This study aimed to explore the link between block copolymers' interfacial properties and nanoscale carrier formation and found out the influence of length ratio on these characters to optimize drug delivery system. A library of diblock copolymers of PEG-PCL and triblock copolymers with additional PEI (PEG-PCL-PEI) were synthesized. Subsequently, a systematic isothermal investigation was performed to explore molecular arrangements of copolymers at air/water interface. Then, structural properties and drug encapsulation in self-assembly were investigated with DLS, SLS and TEM...
June 2020: Acta Pharmaceutica Sinica. B
Yan Chen, Chen Chen, Xiaojuan Zhang, Chuanchuan He, Pengxuan Zhao, Minsi Li, Ting Fan, Ruicong Yan, Yao Lu, Robert J Lee, Muhammad Waseem Khan, Muhammad Sarfraz, Xiang Ma, Tan Yang, Guangya Xiang
Platinum-based chemotherapy is used for non-small cell lung cancer (NSCLC). However, it has side effects and minimum efficacy against lung cancer metastasis. In this study, platinum-curcumin complexes were loaded into pH and redox dual-responsive nanoparticles (denoted as Pt-CUR@PSPPN) to facilitate intracellular release and synergistic anti-cancer effects. Pt-CUR@PSPPN was prepared by a nano-precipitation method and had a diameter of ∼100 nm. The nanoparticles showed increased anti-cancer effects both in vivo and in vitro ...
June 2020: Acta Pharmaceutica Sinica. B
Xiaotong Yang, Xianchun Chen, Ting Lei, Lin Qin, Yang Zhou, Chuan Hu, Qingfeng Liu, Huile Gao
In order to better evaluate the transport effect of nanoparticles through the nasal mucosa, an in vitro nasal cavity-mimic model was designed based on M cells. The differentiation of M cells was induced by co-culture of Calu-3 and Raji cells in invert model. The ZO-1 protein staining and the transport of fluorescein sodium and dexamethasone showed that the inverted co-culture model formed a dense monolayer and possessed the transport ability. The differentiation of M cells was observed by up-regulated expression of Sialyl Lewis A antigen (SLAA) and integrin β 1, and down-regulated activity of alkaline phosphatase...
June 2020: Acta Pharmaceutica Sinica. B
Zhonghua Wang, Bingshu He, Yaqi Liu, Meiling Huo, Wenqing Fu, Chunyan Yang, Jinfeng Wei, Zeper Abliz
Understanding of the nephrotoxicity induced by drug candidates is vital to drug discovery and development. Herein, an in situ metabolomics method based on air flow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) was established for direct analysis of metabolites in renal tissue sections. This method was subsequently applied to investigate spatially resolved metabolic profile changes in rat kidney after the administration of aristolochic acid I, a known nephrotoxic drug, aimed to discover metabolites associated with nephrotoxicity...
June 2020: Acta Pharmaceutica Sinica. B
Yong Li, Yuxun Zhu, Zhaoxin Zhang, Li Li, Yunbao Liu, Jing Qu, Shuanggang Ma, Shishan Yu
Twelve new grayanoids ( 1 - 12 ) along with five known compounds were isolated from flowers of Rhododendron molle . Their structures were fully characterized using a combination of spectroscopic analyses, computational calculations, and single crystal X-ray diffraction. Rhomollone A ( 1 ) possesses an unprecedented 5/6/6/5 tetra-cyclic ring system (B- nor grayanane) incorporating a cyclopentene-1,3-dione scaffold. Rhodomollein XLIII ( 2 ) is a dimeric grayanoid, containing a novel 14-membered heterocyclic ring with a C 2 symmetry axis...
June 2020: Acta Pharmaceutica Sinica. B
Yishan Ye, Laure Ricard, Lama Siblany, Nicolas Stocker, Frédéric De Vassoigne, Eolia Brissot, Baptiste Lamarthée, Arsène Mekinian, Mohamad Mohty, Béatrice Gaugler, Florent Malard
Arsenic trioxide (As2 O3 ) is recently found to have therapeutic potential in systemic sclerosis (SSc), a life-threatening multi-system fibrosing autoimmune disease with type I interferon (IFN-I) signature. Chronically activated plasmacytoid dendritic cells (pDCs) are responsible for IFN-I secretion and are closely related with fibrosis establishment in SSc. In this study, we showed that high concentrations of As2 O3 induced apoptosis of pDCs via mitochondrial pathway with increased BAX/BCL-2 ratio, while independent of reactive oxygen species generation...
June 2020: Acta Pharmaceutica Sinica. B
Wenjie Zhai, Xiuman Zhou, Hongfei Wang, Wanqiong Li, Guanyu Chen, Xinghua Sui, Guodong Li, Yuanming Qi, Yanfeng Gao
PD-1 and CTLA-4 antibodies offer great hope for cancer immunotherapy. However, many patients are incapable of responding to PD-1 and CTLA-4 blockade and show low response rates due to insufficient immune activation. The combination of checkpoint blockers has been proposed to increase the response rates. Besides, antibody drugs have disadvantages such as inclined to cause immune-related adverse events and infiltration problems. In this study, we developed a cyclic peptide C25 by using Ph.D.-C7C phage display technology targeting LAG-3...
June 2020: Acta Pharmaceutica Sinica. B
Lu Liang, Jijun Fu, Siran Wang, Huiyu Cen, Lingmin Zhang, Safur Rehman Mandukhail, Lingran Du, Qianni Wu, Peiquan Zhang, Xiyong Yu
MiR-142-3p has been reported to act as a tumor suppressor in breast cancer. However, the regulatory effect of miR-142-3p on drug resistance of breast cancer cells and its underlying mechanism remain unknown. Here, we found that miR-142-3p was significantly downregulated in the doxorubicin (DOX)-resistant MCF-7 cell line (MCF-7/DOX). MiR-142-3p overexpression increased DOX sensitivity and enhanced DOX-induced apoptosis in breast cancer cells. High-mobility group box 1 (HMGB1) is a direct functional target of miR-142-3p in breast cancer cells and miR-142-3p negatively regulated HMGB1 expression...
June 2020: Acta Pharmaceutica Sinica. B
Zhihua Wang, Wenbo Wu, Xiangchen Guan, Shuang Guo, Chaowen Li, Ruixue Niu, Jie Gao, Min Jiang, Liping Bai, Elaine Laihan Leung, Yuanyuan Hou, Zhihong Jiang, Gang Bai
Although the tumor suppressor P53 is known to regulate a broad network of signaling pathways, it is still unclear how certain drugs influence these P53 signaling networks. Here, we used a comprehensive single-cell multiomics view of the effects of ginsenosides on cancer cells. Transcriptome and proteome profiling revealed that the antitumor activity of ginsenosides is closely associated with P53 protein. A miRNA-proteome interaction network revealed that P53 controlled the transcription of at least 38 proteins, and proteome-metabolome profiling analysis revealed that P53 regulated proteins involved in nucleotide metabolism, amino acid metabolism and "Warburg effect"...
June 2020: Acta Pharmaceutica Sinica. B
Zhaoming Lu, Xiaojing Shi, Fanghua Gong, Shenglei Li, Yang Wang, Yandan Ren, Mengyin Zhang, Bin Yu, Yan Li, Wen Zhao, Jianying Zhang, Guiqin Hou
Dysregulation of mTORC1/mTORC2 pathway is observed in many cancers and mTORC1 inhibitors have been used clinically in many tumor types; however, the mechanism of mTORC2 in tumorigenesis is still obscure. Here, we mainly explored the potential role of mTORC2 in esophageal squamous cell carcinoma (ESCC) and its effects on the sensitivity of cells to mTOR inhibitors. We demonstrated that RICTOR, the key factor of mTORC2, and p-AKT (Ser473) were excessively activated in ESCC and their overexpression is related to lymph node metastasis and the tumor-node-metastasis (TNM) phase of ESCC patients...
June 2020: Acta Pharmaceutica Sinica. B
Jingshu Tang, Yuying Kang, Longjian Huang, Lei Wu, Ying Peng
Blood-brain barrier (BBB) breakdown and the associated microvascular hyperpermeability are hallmark features of several neurological disorders, including traumatic brain injury (TBI). However, there is no viable therapeutic strategy to rescue BBB function. Tissue inhibitor of metalloproteinase-1 (TIMP1) has been considered to be beneficial for vascular integrity, but the molecular mechanisms underlying the functions of TIMP1 remain elusive. Here, we report that TIMP1 executes a protective role on neuroprotective function via ameliorating BBB disruption in mice with experimental TBI...
June 2020: Acta Pharmaceutica Sinica. B
Qin Guo, Chen Jiang
With the development of biotherapy, biomacromolecular drugs have gained tremendous attention recently, especially in drug development field due to the sophisticated functions in vivo . Over the past few years, a motley variety of drug delivery strategies have been developed for biomacromolecular drugs to overcome the difficulties in the druggability, e.g ., the instability and easily restricted by physiologic barriers. The application of novel delivery systems to deliver biomacromolecular drugs can usually prolong the half-life, increase the bioavailability, or improve patient compliance, which greatly improves the efficacy and potentiality for clinical use of biomacromolecular drugs...
June 2020: Acta Pharmaceutica Sinica. B
Chunlin Zhuang, Christophe Pannecouque, Erik De Clercq, Fener Chen
Human immunodeficiency virus (HIV) is the primary infectious agent of acquired immunodeficiency syndrome (AIDS), and non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the cornerstone of HIV treatment. In the last 20 years, our medicinal chemistry group has made great strides in developing several distinct novel NNRTIs, including 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT), thio-dihydro-alkoxy-benzyl-oxopyrimidine ( S -DABO), diaryltriazine (DATA), diarylpyrimidine (DAPY) analogues, and their hybrid derivatives...
June 2020: Acta Pharmaceutica Sinica. B
Chenxi Zhao, Chenming Zeng, Song Ye, Xiaoyang Dai, Qiaojun He, Bo Yang, Hong Zhu
Hypoxia is a common feature of solid tumors. As transcription factors, hypoxia-inducible factors (HIFs) are the master regulators of the hypoxic microenvironment; their target genes function in tumorigenesis and tumor development. Intriguingly, both yes-associated protein (YAP) and its paralog transcriptional coactivator with a PDZ-binding motif (TAZ) play fundamental roles in the malignant progression of hypoxic tumors. As downstream effectors of the mammalian Hippo pathway, YAP and/or TAZ (YAP/TAZ) are phosphorylated and sequestered in the cytoplasm by the large tumor suppressor kinase 1/2 (LATS1/2)-MOB kinase activator 1 (MOB1) complex, which restricts the transcriptional activity of YAP/TAZ...
June 2020: Acta Pharmaceutica Sinica. B
Zheng Luo, Chao Liu, Peng Quan, Degong Yang, Hanqing Zhao, Xiaocao Wan, Liang Fang
Background: Hydrogen bonding interaction was considered to play a critical role in controlling drug release from transdermal patch. However, the quantitative evaluation of hydrogen bonding strength between drug and polar functional group was rarely reported, and the relationship between hydrogen bonding strength and controlled release capacity of pressure sensitive adhesive (PSA) was not well understood. The present study shed light on this relationship. Methods: Acrylate PSAs with amide group were synthesized by a free radical-initiated solution polymerization...
May 2020: Acta Pharmaceutica Sinica. B
Kangkang Zhi, Jiacheng Wang, Haitian Zhao, Xin Yang
Natural products, as a gift of nature to humanity, have long been used as drugs or pharmacological actives to help people cure various diseases. Yet we still know comparatively little about their ability to be materials. In recent years, some small molecule natural products isolated from traditional Chinese medicines have been found to have new features, namely, self-assembly to form gels ( i.e ., natural product gels, NPG). However, the application development of these natural products is seriously lacking, which greatly weakens their practical value and delays the maturity of the field...
May 2020: Acta Pharmaceutica Sinica. B
Zi-Dong Qiu, Jin-Long Chen, Wen Zeng, Ying Ma, Tong Chen, Jin-Fu Tang, Chang-Jiang-Sheng Lai, Lu-Qi Huang
Due to numerous obstacles such as complex matrices, real-time monitoring of complex reaction systems ( e.g. , medicinal herb stewing system) has always been a challenge though great values for safe and rational use of drugs. Herein, facilitated by the potential ability on the tolerance of complex matrices of extractive electrospray ionization mass spectrometry, a device was established to realize continuous sampling and real-time quantitative analysis of herb stewing system for the first time. A complete analytical strategy, including data acquisition, data mining, and data evaluation was proposed and implemented with overcoming the usual difficulties in real-time mass spectrometry quantification...
May 2020: Acta Pharmaceutica Sinica. B
Qinglan Guo, Dawei Li, Chengbo Xu, Chenggen Zhu, Ying Guo, Haibo Yu, Xiaoliang Wang, Jiangong Shi
Seven indole alkaloid glycosides containing a 1'-(4″-hydroxy-3″,5″-dimethoxyphenyl)ethyl unit ( 1 - 7 ) were isolated from an aqueous extract of Isatis indigotica leaves (da qing ye). Their structures were determined by spectroscopic data analysis combined with enzymatic hydrolysis as well as comparison of their experimental CD (circular dichroism) and calculated ECD (electrostatic circular dichroism) spectra. Based on analysis of <mml:math xmlns:mml=""> <mml:mrow> <mml:msubsup> <mml:mrow> <mml:mrow> <mml:mo>[</mml:mo> <mml:mrow> <mml:mi>α</mml:mi> </mml:mrow> <mml:mo>]</mml:mo> </mml:mrow> </mml:mrow> <mml:mrow> <mml:mtext>D</mml:mtext> </mml:mrow> <mml:mrow> <mml:mn>20</mml:mn> </mml:mrow> </mml:msubsup> </mml:mrow> </mml:math> and/or Cotton effect (CE) data of 1 - 7 , two simple roles to assign location and/or configuration of β -glycopyranosyloxy and 1'-(phenyl)ethyl units in the indole alkaloid glycosides are proposed...
May 2020: Acta Pharmaceutica Sinica. B
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