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  • Yan-ying SUN, Xiao-fang ZUO, Peng ZHAN, Xin-yong LIU
    Acta Pharmaceutica Sinica. 2020, 55(4): 720-733.

    Adenovirus is a common cause of infection in children and adults with acute respiratory tract, gastrointestinal tract and urinary tract. It can cause serious and even fatal infections in patients with low immune function. Therefore, it poses a great threat to human health. Currently, there are no specific anti-adenoviral drugs in market. With in-depth investigation of the pathogenic mechanism and biological characteristics of adenovirus, and the rapid development of drug screening technology, new generation of anti-adenovirus drug targets and related inhibitors have been discovered, providing new options for treatment. This review selects the representative case studies in recent years and summarizes the advances in anti-adenoviral medicinal chemistry.

  • Ling-xin HOU, Han JU, Peng ZHAN, Xin-yong LIU
    Acta Pharmaceutica Sinica. 2020, 55(4): 669-678.

    Dengue fever is one of the most important vector-borne human diseases caused by mosquito vector Aedes aegypti and Aedes albopictus. Dengue virus can cause dengue fever, dengue hemorrhagic fever and dengue shock syndrome. There are no approved drugs for the treatment of dengue disease so far. In this paper, combined with the latest progress in the research of anti-dengue virus, the new progress in the research of anti-dengue virus drugs was reviewed from the aspects of protease inhibitors, virus polymerase inhibitors, entry inhibitors, virus replication-related host factor inhibitors, capsid protein inhibitors and nucleic acid inhibitors.

  • Yue MA, Fen-ju WEI, Ji YU, Hai-yong JIA, Xin-yong LIU, Peng ZHAN
    Acta Pharmaceutica Sinica. 2020, 55(4): 554-565.

    Hepatitis B virus (HBV) capsid protein plays an important role in the life cycle, thus becoming an ideal target for drug design. Capsid protein inhibitors can exert a synergistic antiviral effect with nucleoside drugs by inhibiting the replication of HBV. This paper reviews the research progress of capsid protein inhibitors with different structural types from the perspective of medicinal chemistry.

  • Wen-xiu WEI, Lan-lan JING, Xin-yong LIU, Peng ZHAN
    Acta Pharmaceutica Sinica. 2020, 55(4): 575-584.

    At present, the most widely used anti-herpesviruses drugs are acyclovir (ACV) and its derivatives, but the emergence of herpesvirus resistance to these drugs forces people to continue to seek new anti-herpesviruses drugs. More and more new targets and inhibitors against herpesviruses have been discovered, one reason is the in-depth study of the biological characteristics and pathogenic mechanism of herpesviruses, and the other is the rapid development of new drug design and screening technology. Therefore, there are more options for the treatment of herpes infections. This review summarizes the representative achievements in the field of anti-herpesviruses drugs in recent years.

  • Fen-ju WEI, Yue MA, Ji YU, Hai-yong JIA, Xin-yong LIU, Peng ZHAN
    Acta Pharmaceutica Sinica. 2020, 55(4): 566-574.

    Hepatitis B has become one of the major diseases which seriously affect people's health and social development. Hepatitis B, with high incidence and long disease course, cannot be cured by approved drugs such as the nucleoside analogues. Therefore, the discovery of safe and efficient novel HBV inhibitors is of great significance. From the point of view of medicinal chemistry, we summarized and discussed current endeavours towards the discovery and development of anti-HBV agents of RNase H and other novel target inhibitors with various scaffolds or distinct mechanisms of action, besides the existing capsid protein inhibitors.

  • Jing LI, Xiang-yi JIANG, Shu-jing XU, Qing-hua CUI, Rui-kun DU, Dong-wei KANG, Peng ZHAN, Li-jun RONG, Xin-yong LIU
    Acta Pharmaceutica Sinica. 2020, 55(4): 537-553.

    The epidemic caused by coronavirus poses a serious threat to human health, but there is no specific drug or vaccine for the treatment of this kind of virus infection. Herein, this article selects typical case studies in recent years and reviews the medicinal chemistry strategies of anti-SARS-CoV, MERS-CoV and other coronavirus drugs from the perspective of medicinal chemistry, and tries to provide some clues to current drug research againstSARS-CoV-2.

  • Yu-cen TAO, Xia HAO, Xin-yong LIU, Peng ZHAN
    Acta Pharmaceutica Sinica. 2020, 55(4): 744-753.

    In recent years, enterovirus infection has become a frequent epidemic and developed into an important public health problem. For example, hand-foot-mouth disease has become a common infection among children in China. Hand-foot-mouth disease (HFMD) has been spreading globally since 1997, especially in the Asia-Pacific region. Enterovirus 71 (EV71) is one of the main pathogens causing HFMD. And now there is no drug available to treat EV71 infection. This review summarizes the research progress of anti-enterovirus-71 drugs from the perspective of medicinal chemistry.

  • Tian-guang HUANG, Lin SUN, Peng ZHAN, Xin-yong LIU
    Acta Pharmaceutica Sinica. 2020, 55(4): 679-693.

    Viral infections have always threatened human health. Broad-spectrum antiviral agents (BSAs) can either target host proteins that are essential for viral replication, or act on multiple viruses or multiple genotypes of the same virus. More importantly, BSAs could reduce the possibility of drug resistance. From the perspective of medicinal chemistry, this review summarizes recent advances in the research of broad-spectrum antiviral drugs with privileged structures or targeting specific targets in the viral life cycle.

  • Yu-hong WANG, Cong LI, Shuang JIANG, Jian-dong JIANG
    Acta Pharmaceutica Sinica. 2020, 55(3): 392-397.

    Higenamine (HG) is an active cardiotonic component isolated from Aconite. Chinese and foreign scholars have done a lot of research on the metabolism and pharmacological effects of HG, which confirmed that it has cardiovascular pharmacological effects of cardiactonic action and vasodilation for the treatment of heart failure and bradycardia, anti-oxidative and anti-apoptotic effects which can be used to protect the heart and reduce heart ischemia and reperfusion injury. In addition, HG inhibits the expression of iNOS mRNA by inhibiting the activity of the transcription factor NF-κB, inhibits the lipopolysaccharide (LPS)-induced NO product, and inhibits platelet aggregation and thrombus formation, thereby improving the experimental septic shock in animals. This article reviews the recent progress in cardiovasular pharmacology of HG, which will contribute to the further development and clinical application of it in the future.

  • Hui-jia WANG, Yuan-jian WANG, Chen LIANG, Qian CAI, Hong-sheng XU, Qing LI
    Acta Pharmaceutica Sinica. 2020, 55(3): 501-505.

    HPLC-RID and HPIC-CD methods were established for the determination of sucrose octasulfate content in irinotecan hydrochloride liposomes for injection. HPLC-RID:This method was performed on a Kromasil 100-5-NH2 column (250 mm×4.6 mm, 5 μm) with a mobile phase of 0.8 mol·L-1 ammonium sulfate buffer (pH 3.5)-acetonitrile (83:17). The flow rate, column temperature and detector temperature were maintained at 1 mL·min-1, 30℃ and 30℃ respectively. HPIC-CD:This method was performed on an anion exchange column Dionex InPacTM AS11-HC (250 mm×4 mm, 9 μm) with an eluent of 30 mmol·L-1 sodium hydroxide solution. The flow rate was 1.5 mL·min-1, the column temperature was 30℃ and the detector temperature was 35℃. The HPLC-RID method and HPIC-CD method were validated with respects to specificity, limit of detection, limit of quantitation, linearity, precision, accuracy, stability and robustness and met the validation requirements. There were no significant differences between the HPIC-CD and HPLC-RID methods according to T-test analysis, both of which were applicable for the measurement of sucrose octasulfate concentration in irinotecan hydrochloride liposomes for injection. However, the HPLC-CD was better at the following aspects:higher detection sensitivity, simpler sample pretreatment, lower time and money spent, better environmental protection.