Latest ArticlesAllium chinense belongs to the genus Alliums of the lily family. It can be used both as medicine and food. To date, the phylogenetic relationship of Allium species have not be resolved completely. Furthermore, there has been a lack of DNA barcode to distinguish closely related species. In this study, the complete chloroplast genome of A. chinense was obtained using next generation DNA sequencing and bioinformatic analysis, and compared with that from other Allium species. The genome is a circular molecule of 152 525 bp with a typical quadripartite structure. Genome annotation identified a total of 116 genes, including 81 protein-coding genes, 31 tRNA genes, and 4 rRNA genes. Analyses of sequences from six Allium species showed that the most diverse regions are found in the protein coding regions such as ndhA and ycf1 genes, and in the intergenic regions, such as ps16-trnQ, trnT-trnF, ndhF-rpl32, rpl32-trnL and rpl16-rps3. A phylogenetic tree was constructed using 58 protein coding sequences from 53 species. All branches showed strong support with bootstrap scores reaching 66%-100%, except those for the Lilium and Paris. Our results suggest that the completed chloroplast genome could solve the classification problems of these species. Using EcoPrimer software, we identified seven markers from the chloroplast genomes, which can be used to differentiate congeneric species. In summary, we have sequenced the complete chloroplast genome of A. chinense, carried out phylogenetic analysis and identified a series of genus specific DNA barcode sequences. The results have laid the foundation for the systematical determination of the phylogenetic relationship of Allium species and the differentiation of species using the genus specific primers.
The poor solubility of cyclosporine A (CsA) in water limits its oral absorption. We prepared CsA/Soluplus/SDS complex, which can form CsA/Soluplus/SDS supersaturated micelles (CSS-SM) after hydration. Then, We further prepared CSS-SM osmotic pump tablets (CSS-SM-T). CSS-SM had a particle size of 156 nm, where in encapsulation efficiency and drug loading efficiency of CsA were 89.0% and 17.5%, respectively. CSS-SM-T achieved zero-level drug release in vitro. Pharmacokinetic data from Beagle dogs (all animal experiments were conducted under the guidelines approved by the Institutional Animal Care and Use Committee of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences) indicated that CsA in the ordinary osmotic pump tablets was hardly absorbed after orally administered; despite slightly lower bioavailability[relative bioavailability:(85.1 ±47.4)%] than that of Sandimmum Neoral, CSS-SM-T displayed lower fluctuations in CsA plasma concentration and obvious sustained-release characteristics in vivo, implying lower toxicity. Therefore, CSS-SM-T provides a new research idea for the design and development of oral sustained-and controlled-release preparations of poorly water-soluble drugs.
To modernize traditional Chinese medicine, its pharmacodynamic substances should be elucidated firstly. Modern chromatographic technologies play an important role in the clarification of the pharmacodynamic substances of Chinese medicine. In this paper, the advancement and application of current chromatographic techniques in the pharmacodynamic substances of Chinese medicines were reviewed from the aspects of detection, preparation and screening methods.
Using silica gel column chromatography, gel chromatography and HPLC, we isolated secondary metabolites in fermentation broth of a rifamycin resistant mutation strain Streptomyces sp. HS-NF-1046R. Based on spectroscopic data, the chemical structures of three compounds were identified as 3-hydroxyl-2-N-propionyl-anthranilamide (1), 2, 3-dihydro-8-hydroxy-2, 2-dimethyl quinazolin-4-(1H)-one (2) and 2-aminobenzamide (3). Compounds 1 and 2, as new entities, were evaluated for cytotoxicity against A549, HepG2, HCT-116 and K562 cells using the SRB assay. Compounds 1 and 2 exhibited no cytotoxicity with IC50 over 100 μmol·L-1.
Natural products areone source of new drugs, and their target identification is pivotal forelucidating the mechanism of action. Most methods of target discovery and validation utilize labeling natural products with probes. This is time-consuming and laborious, and often results in activity decrease or change of the natural products. Recent methods withoutchemicalmodificationhave become the main force in the target identification of natural products, including direct or indirect methods. Direct methods are mainly based on the principle of affinity and stability of protein, and indirect methods infer the drug target from the change in physiological responses or biochemical signatures. This review summarizes recent methods for target identification and validation of label-freenatural products, providing new ideas and strategies for future research in natural products.
A non-reduced SDS-PAGE purity method for quantitation of conbercept fragments was established based on gel screening, comparison of gel imaging system, linearity range of main band, screening of destaining conditions. The results indicated that the bands could be separated effectively with good clearness and flatness on 4%-15% gradient concentration gel, the peaks of all bands could be separated from baseline using high-distinguishability gel imaging system, the signal intensity of a main band had shown a good linearity with ≤ 3 μg of loading amount, and that the destaining was set as a total of ≤ 3 h with exchanging 100 mL destaining buffer every 60 min. The established non-reduced SDS-PAGE method could demonstrate the purity of conbercept more objectively. After validation, the established non-reduced SDS-PAGE method was submitted to FDA in the form of supplementary materials, which laid a quality basis for the direct entry of conbercept to the clinical Ⅲ study in the United States.
Currently, single-target drugs are often difficult to achieve the desired results in the treatment of multifactorial diseases such as tumors, cardiovascular and endocrine diseases, and may also cause toxicity. Multi-target drugs can improve the efficacy, reduce side effect and drug resistance by regulating multiple links of the disease, showing good prospects for the application. The main aim of this article is to review the strategies of designing multi-target directed ligands (MTDLs) (including conjugated-pharmacophore, fused-pharmacophore and merged-pharmacophore) and the research progress in recent years. The existing problems and challenges of multi-target drugs are also discussed, to provide new ideas for the study of multi-target drugs.
Present study investigated the role of mesenchyme homeobox 2 (MEOX2) gene in neurovascular dysfunction in Alzheimer's disease (AD) model rats by bilateral intracerebroventricular injection of Aβ1-42. One week after surgery, Morris water maze, immunohistochemistry, biochemical detection, Western blot and real-time PCR were used to detect the indexes. The animal studies were conducted in accordance with the Regulations of Experimental Animal Administration issued by the State Committee of Science and Technology of the People's Republic of China. Compared to the Sham-operated rats, Aβ1-42-operated rats showed obviously cognitive dysfunction, accompanied by increased Aβ, glial fibrillary acidic protein (GFAP), allograft inflammatory factor 1 (AIF1), endothelial nitric oxide synthase (eNOS) and decreased neuron specific enolase (NSE), synaptophysin (SYN), CD34, vascular endothelial growth factor (VEGF) expressions of brain. Aβ1-42-operated rats also increased the endothelin (ET) level and decreased nitric oxide (NO) level in brain tissue. Moreover, MEOX2 expression was decreased correlated with low density lipoprotein receptor-related protein 1 (LRP-1) decreasing and receptor for advanced glycation end products (RAGE) increasing in brain tissues of AD model rats. We found the correlation between MEOX2 gene expression and neurovascular dysfunction, in addition, the decreased MEOX2 may involve in increasing the accumulation of Aβ in brain by relating to the decreased LRP-1 and increased RAGE which is located in blood-brain barrier (BBB) in senescence-accelerated mice.
The Nrf2-Keap1-ARE pathway is an important signaling axis that functions to protect cells against oxidative stress and harmful chemicals through the induction of cytoprotective genes. The maintenance and protective role of Nrf2 pathway has been recognized as a means for chemoprevention. On the other hand, constitutive activation of Nrf2, due to somatic mutations of genes that control Nrf2 degradation, promotes carcinogenesis and imparts chemoresistance to cancer cells. Autophagy is another tightly regulated complex cellular process that functions as a cellular quality control system to remove damaged proteins or organelles. Recently, these two cellular pathways were shown to intersect through the direct interaction between p62 (an autophagy adaptor protein) and Keap1. Dysregulation of autophagy was shown to result in prolonged activation of Nrf2 in a p62-dependent manner, which is associated with the pathogenesis and therapies of several human diseases including cancer. In this review, we discuss the molecular mechanisms of p62-mediated Nrf2 signaling pathway, with a special emphasis on their impact on nervous system disease, cardiovascular disease and cancer.
Naphthoquinones are a kind of important active ingredients in the traditional Chinese medicinal herb "Zicao". In recent years, researches on pharmacology and clinical application of naphthoquinones in Zicao have been gradually deepened and made extensive progress around the world. On the other hand, the plant origins of the herbal materials of Zicao in market are complex and their qualities are quite different, thus more and more studies have been focused on the quantitative determination and quality assessment of the medicinal herb as well as its products by using various naphthoquinones as quality chemical markers. In this paper, we review recent advances in the research on pharmacological actions and multi-components content determination of shikonin/alkannin and its derivatives in Zicao so as to provide a scientific guidance for further research and development of medicinal resource of Zicao, and to establish more comprehensive and systematic method for their quality control and evaluation.
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