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  • Xue WANG, Ya-hua WANG, Sha LIU, Chong LI
    Acta Pharmaceutica Sinica. 2017, 52(3): 488-493.

    In this study, a novel brain-targeting carrier was made via conformational epitope imprinting. Acrylamide and N, N'-methylene bisacrylamide was used as carrier materials and the N-terminal epitope of nicotinic acetylcholine receptor α7 (nAchR α7) was tested as a template molecule, and the polymer nanoparticles were obtained after polymerization and template removal. The nanoparticles were investigated by particle size analyzer and transmission electron microscopy (TEM). Their targeting capabilities were investigated with a cell uptake assay in vitro and fluorescence imaging in vivo. The results suggest that the nanoparticles had a small particle size (42.1±4.3 nm) with a homogeneous distribution, and good targeting properties in vitro and in vivo. We have made the molecularly imprinted polymer nanoparticles with brain targeting capability, which represents a new tool in the treatment of brain diseases.

  • Xu-zhao LIU, Li-si ZHOU, Jin-xin LIU, Jing JIA, Jing-yuan SONG, Lin-chun SHI
    Acta Pharmaceutica Sinica. 2017, 52(3): 494-499.

    Bubali cornu (water buffalo horn) has been used as the substitute for Cornu rhinoceri asiatici (rhino horn) in clinical applications, and is the essential ingredient of Angong Niuhuang Wan. In recent years, there are a number of adulterants on the commercial herbal medicine markets. An efficient tool is required for species identification. In this study, 155 Bubali cornu samples have been taken from original animals and collected from commercial herbal medicine markets. 153 COI sequences have been successfully obtained from 155 samples through DNA extraction, PCR amplification, bidirectional sequencing and assembly. 93 COI sequences have been added to the DNA barcoding database of traditional Chinese animal medicine after validation using DNA barcoding GAP and tree-based methods. The species identification of the 62 commercial Bubali cornu medicines has been accomplished on the DNA barcoding system for identifying herbal medicine using the updated animal medicine database (www.tcmbarcode.cn). Except two samples failed to obtain COI sequences, 54.8% of the commercial Bubali cornu medicines were water buffalo horns and 29% were yak horns. Our results showed that yak horn was the major adulterant of Bubali cornu and the DNA barcoding method may accurately discriminate Bubali cornu and their adulterants. Therefore, we recommend that supervision on the herbal medicine markets should be strengthened with this new method to warren the effectiveness of herbal medicines.

  • Hui-le GAO, Xin-guo JIANG
    Acta Pharmaceutica Sinica. 2017, 52(2): 181-188.

    The development of pharmaceuticals has been providing many kinds of novel drug delivery systems, which are important for improving therapeutic effect and one of the most important fields in pharmaceutics. According to their application, we can generally divide the novel drug delivery systems into three categories:quickly performed drug delivery system, long-term drug delivery system and high effective drug delivery system. Some diseases, such as asthma, angina pectoris and migraine, require therapeutics urgently, and the drugs have to be absorbed in several minutes. Therefore, quickly performed drug delivery systems are developed, such as oral disintegrating tablets and nasal spray. For normal tablets and capsules, especially the drugs with short blood half life, the drug concentration in blood shows obvious peak-valley phenomenon, which reduces the therapeutic effect and requires multiple administration. To solve this problem, sustained drug release system was developed, which could release the drugs slowly and sustainably even in zero-order kinetics. The pulse drug delivery system was developed that can delayed and pulsed release drug for one or several times. This system is especially useful in the management of asthma and heart disease, which are often found in midnight or early morning when patients are in bed. Transdermal drug delivery system could release drugs sustainably and deliver the drugs through skin to blood circulation, providing long term activity. The water-insoluble drugs are difficult for pharmaceutical development, thus many methods were developed to improve the solubility and bioavailability of drugs. Although biopharmaceuticals are important for disease treatment, the application shadows by the poor stability and low bioavailability. Thus the biopharmaceutical delivery system was developed, which mainly focused on structure modification and encapsulation by carriers. Considering therapeutic effect requires interaction between drugs and their targets, it is important to deliver drugs to their targets. Therefore, targeting delivery systems were developed, which mainly based on the nanoparticles. Furthermore, on-demand release drug delivery systems are also developed with the property of environment-triggered drug release. In conclusion, the novel drug delivery systems were reviewed in this study.

  • Mao-xu GE, Ju-xian WANG, Rong-guang SHAO, Hong-wei HE
    Acta Pharmaceutica Sinica. 2017, 52(2): 189-197.

    Bile acids play critical roles in the regulation of metabolism and absorption of lipids. The ileal apical sodium-dependent bile acid transporter (ASBT) located at the enterocyte brush border is responsible for the reuptake of bile acids and the maintenance of bile acid homeostasis. Recently, a number of investigations have been made concerning the regulation and control of ASBT and the relationship between ASBT and intestinal inflammation, tumorigenesis, diabetes mellitus and hyperlipemia, which suggests ASBT as a potential therapeutic target of these diseases. In this review, advances in the study of above-mentioned issues were summarized.

  • Yu-xiu YANG, Su-ying LI, Qian ZHANG, Zhi-ning XIA, Feng-qing YANG
    Acta Pharmaceutica Sinica. 2017, 52(2): 198-205.

    It has been an active approach to screen the active ingredients in traditional Chinese medicines (TCMs) according to the affinity property between small molecule compounds and biomaterials such as cells, bacteria and proteins. On the other hand, the biomaterials can be immobilized on a solid support before the screening procedure. The immobilization method not only can maintain the biological activities of biomaterials, but also have other advantages such as high efficiency, simple operation, easy to be continuous and automatic, etc. Carrier materials (solid supports) for the immobilization including silica gel, magnetic materials, hollow fiber, and the surface plasma resonance sensor chips have been used to immobilize biomaterials and successfully applied in the screening of active ingredients from TCMs. In this paper, applications of immobilization techniques in the screening of active components from TCMs were reviewed to provide a scientific reference to the future applications.

  • Guang-zhao LU, Cheng HOU, Yan-qiang ZHONG, Ying LU, Hao ZOU
    Acta Pharmaceutica Sinica. 2017, 52(2): 206-213.

    Excessive reactive oxygen species (ROS) is associated with an array of pathological conditions, including cancer, diabetes, cardiovascular diseases, and neurodegenerative diseases. However, ROS-responsive materials have drawn attention in the development of drug delivery systems. There are many types of ROS-responsive materials explored in drug delivery applications, including sulfur-based responsive polymers, selenium-based responsive polymers, tellurium-based responsive polymers, oxalate ester-containing polymers, phenylboronic ester-containing polymers and unsaturated lipids. When integrated with ROS-responsive drug delivery systems, a photosensitizer is used as a light-sensitive element to generate ROS, mainly singlet oxygen (1O2), which in turn activates the ROS-triggered drug delivery.

  • Jin-long CUI, Shun-xing GUO, Pei-gen XIAO
    Acta Pharmaceutica Sinica. 2017, 52(2): 214-221.

    Research of plant development and metabolism has drawn lots of attention with the fast development of science of mycorrhizal biology, molecular biology and metabonomics technology. It has become one of hot fields in the study of endophytes and plant, which would affect plant's metabolite composition. This would provide opportunity for appraising and modifying traits to medicinal plant, and would also perfect the tranditional standpoint on forming reason of medicinal plant genuineness. Here we provide a review of theory and mechanism, research and application of interaction between plant and endophyte. This review may enhance understanding of medicinal plant, and evaluating the quality of herbs in production.

  • Hong-die CAI, Wei-wei TAO, Shu-lan SU, Sheng GUO, Yue ZHU, Jian-ming GUO, Da-wei QIAN, Xu-dong CONG, Ren-mao TANG, Jin-ao DUAN
    Acta Pharmaceutica Sinica. 2017, 52(2): 222-228.

    Abelmoschus manihot (L.) Medic., a folk herbal medicine in China, is a flowering plant belonging to Abelmoschus L. genus and Malvaceae family, which has been reported with an antidepressant activity. The study was designed to isolate flavonoids from Abelmoschus manihot corolla and explore the action mechanism of antidepressant activities. The flavonoids were isolated and purified by D101 macroporous resin column, polyamide column and Sephadex LH-20 sequentially and identified as myricetin-3-O-β-D-glucoside (1), gossypetin-8-O-β-D-glucuronide (2, G-8-G), gossypetin-3'-O-β-D-glucoside (3), quercetin-3'-glucoside (4, Q-3-G), isoquercitrin (5, IQT), hyperoside (6, HY), myricetin (7), quercetin (8, QT). Compounds 2, 4, 5, 6 and 8 (15, 30 and 60 mg·kg-1) were orally administered to mice and the reaction was observed in tail suspension test (TST) and forced swimming test (FST). Western blot analysis was used in determination of the protein expressions of brain-derived neurotrophic factor (BDNF), tyrosine receptor kinase B (TrkB) and phosphorylation eukaryotic elongation factor 2 (p-eEF2). The results revealed that only Q-3-G and G-8-G (15, 30, 60 mg·kg-1) significantly reduced the immobility time in FST and TST. Furthermore, Q-3-G and G-8-G remarkably increased the expression of BDNF and TrkB, and decreased the expression of p-eEF2. These results suggest that Q-3-G and G-8-G had an obvious antidepressant activity via up-regulation of BDNF expression. The new observation will provide a new direction in the development of antidepressant in the treatment of major depressive disorder (MDD).

  • Yu SONG, Hui ZHANG, Rui-li LIU, Guang-fan HAI, Tong WANG, Jia-xin YUE, Wei-li ZHANG, Yu-ke REN
    Acta Pharmaceutica Sinica. 2017, 52(2): 229-235.

    Postoperative intra-abdominal adhesion is one of the most common complications in the postoperative period. Current remedies are very ineffective to prevent the pathological outcomes except steroid hormones. Rhynchophylline is deemed as a pharmacologically active component from traditional Oriental medicine Uncaria rhynchophylla (Miq.) Jacks. (Rubiaceae). This study was designed to investigate the preventative effect of rhynchophylline on the abdominal adhesions in rats. Rhynchophylline relieved the experimental abdominal adhesion and decreased the levels of interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in the blood serum in a dose-dependent manner. The levels of transforming growth factor-β1 (TGF-β1) and connective tissue growth factor (CTGF) were reduced significantly in the peritoneal fluid. The potential mechanism of the activity is related to inhibition of the TGF-β1/Smad signaling pathway.

  • Jin TAO, Min JIANG, Lu-ying CHEN, Yuan-yuan HOU, De-qin ZHANG, Feng QIU, Gang BAI
    Acta Pharmaceutica Sinica. 2017, 52(2): 236-244.

    Property and flavor theory of traditional Chinese medicine (TCM) is the core base for clinical treatment of diseases. However, few research about its chemical and biological characterization was performed. In this paper, network pharmacology was adopted to review patterns around the theory of TCM. "Xiaoke" prescription database, which combinations of herb medicines for diabetes therapy, was firstly built to explore prescription regularity and screen core paired-components. The prescription regularity and molecular mechanism of flavor composition were explored through the relationship of "drug-compound-target-pathway-function" by ChEMBL, CTD and KEGG datebase. As a result, the tastes of "Gan" (sweetish taste) and "Ku" (bitter taste) were the popular therapeutic flavor to regulate the disorder of glucose and lipid metabolisms. The mechanism of Xiaoke was summarized from representative traditional Chinese medicine partner "Zhimu-Huangbai" and "Huangqi-Gegen". The key components of "Gan", including saponins stimulated insulin secretion, improve insulin resistance and promote glucose utilization. The components of "Ku", including flavonoids and alkaloids regulate inflammatory cytokines, promoted the utilization of glucose, improve endocrine and metabolism through MAPK, PI3K-Akt, PPAR signal pathway. The TCM therapeutic mechanism about "Xiaoke" was preliminarily summarized to clear "heat" by anti-inflammation and immunoregulation, to regulate glucolipid metabolism for removing the satiation of digestion, and to improve the utilization of insulin and diabetes complications for endocrine adjusting. The results demonstrate that therapeutic principle of TCM for "Xiaoke" is comprehensive via multi pathway. This study provides a new research method and strategy for exploring the mechanism of TCM for diabetes therapy.