1.Recent advance in carbohydrate-based cancer vaccines.
Acta Pharmaceutica Sinica 2012;47(3):261-70
The abnormal glycans expressing on the surface of tumor cells are good targets to develop carbohydrate-based anti-cancer vaccines. However, one of the major problems is that carbohydrate antigens possess weak immunogenicity. This review summarizes the recent efforts to overcome this problem: glycoconjugates produced by coupling the carbohydrate antigens and proper carrier proteins improve their immunogenicity, many glycoconjugates have entered clinical trials; the vaccines become chemically well-defined when coupling the carbohydrate antigens with a T-cell peptide epitope and an immunostimulant to form fully synthetic multi-component glycoconjugate vaccines; the modification of carbohydrate antigens in combination with the technology of metabolic oligosaccharide engineering of tumor cells induces a strong immune response; and the fact that the antibodies elicited against the unnatural carbohydrate antigens can recognize the native carbohydrate antigens on tumor cells provides a new promising strategy for the development of anti-cancer vaccines.
2.Design, synthesis, and bioassay of 5-epi-aminoglycosides.
Ribai YAN ; Youhong NIU ; Yuheng LIU ; Junfeng DENG ; Xinshan YE
Chinese Journal of Natural Medicines (English Ed.) 2022;20(11):854-862
For the purpose of seeking new antibiotics, researchers usually modify the already-existing ones. However, this strategy has been extensively used and is close to its limits, especially in the case of aminoglycosides, and it is difficult to find a proper aminoglycoside antibiotic for novel modification. In this paper, we reported the design, synthesis, and evaluation of a series of 5-epi-neamine derivatives based on the structural information of bacterial 16S RNA A-site binding with aminoglycosides. Bioassay results showed that our design strategy was feasible. Our study offers a new way to search for structurally novel aminoglycosides. Meanwhile, our study provides valuable structure-activity relationship information, which will lead to better understanding and exploitation of the drug target, and improved development of new aminoglycoside antibiotics.
Aminoglycosides/chemistry*
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Anti-Bacterial Agents/chemistry*
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RNA, Ribosomal, 16S/metabolism*
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Structure-Activity Relationship
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Biological Assay
3.Novel carbohydrate-triazole derivatives as potential α-glucosidase inhibitors.
Zi-Pei ZHANG ; Wan-Ying XUE ; Jian-Xing HU ; De-Cai XIONG ; Yan-Fen WU ; Xin-Shan YE
Chinese Journal of Natural Medicines (English Ed.) 2020;18(10):729-737
A series of novel pyrano[2, 3-d]trizaole compounds were synthesized and their α-glucosidase inhibitory activities were evaluated by in vitro enzyme assay. The experimental data demonstrated that compound 10f showed up to 10-fold higher inhibition (IC74.0 ± 1.3 μmol·L) than acarbose. The molecular docking revealed that compound 10f could bind to α-glucosidase via the hydrophobic, π-π stacking, and hydrogen bonding interactions. The results may benefit further structural modifications to find new and potent α-glucosidase inhibitors.