生物活性

• 描述1-Deoxynojirimycin (DNJ, C₆H13NO₄, 163.17 g/mol), an alkaloid azasugar or iminosugar, is a biologically active natural compound that exists in mulberry leaves and Commelina communis (dayflower) as well as from several bacterial strains such as Bacillus and Streptomyces species. 1-Deoxynojirimycin is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus^[3]. Oral sucrose tolerance test was performed, and the result showed that CSE (culture supernatant extract) was able to significantly suppress the blood glucose elevation and suggested DNJ (1-Deoxynojirimycin) as the main active compound. The recovery rate of 15N from DNJ reached 80% up to 48 hours after oral administration, suggesting its rapid excretion, suggesting the safety of DNJ^[4]. db/db mice were treated with DNJ intravenously (20, 40 and 80 mg·kg(-1)·day(-1)) for four weeks. DNJ significantly reduced body weight, blood glucose and serum insulin levels. DNJ treatment also improved glucose tolerance and insulin tolerance. DNJ significantly improved insulin sensitivity via activating insulin signaling PI3K/AKT pathway in skeletal muscle of db/db mice^[5]. In addition, DNJ delays cellular senescence that is promoted under high glucose condition^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00000692	HIV Infections	Phase 1	Completed	-	United States, California ... more >> Univ of California / San Diego Treatment Ctr San Diego, California, United States, 921036325 Stanford Univ School of Medicine Stanford, California, United States, 94305 United States, Florida Univ of Miami School of Medicine Miami, Florida, United States, 331361013 United States, Illinois Rush Presbyterian - Saint Luke's Med Ctr Chicago, Illinois, United States, 60612 United States, Massachusetts Harvard (Massachusetts Gen Hosp) Boston, Massachusetts, United States, 02114 United States, South Carolina Julio Arroyo West Columbia, South Carolina, United States, 29169 Collapse <<
  NCT00319046	Gaucher Disease Type 1	Phase 3	Completed	-	-
  NCT00041535	Gaucher Disease	Phase 2	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 United Kingdom Institute of Child Health London, United Kingdom Collapse <<

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• 参考文献

• [1] Jiang P, Mu S, et al. Design and application of a novel high-throughput screening technique for 1-deoxynojirimycin. Sci Rep. 2015 Feb 24;5:8563.

  [2] Aguilar AL, Escribano J, et al. Synthetic 1-deoxynojirimycin N-substituted peptides offer prolonged disruption to N-linked glycan processing. ChemMedChem. 2014 Dec;9(12):2809-13.

  [3] Gao K, Zheng C, Wang T, Zhao H, Wang J, Wang Z, Zhai X, Jia Z, Chen J, Zhou Y, Wang W. 1-Deoxynojirimycin: Occurrence, Extraction, Chemistry, Oral Pharmacokinetics, Biological Activities and In Silico Target Fishing. Molecules. 2016 Nov 23;21(11):1600

  [4] Takasu S, Parida IS, Onose S, Ito J, Ikeda R, Yamagishi K, Higuchi O, Tanaka F, Kimura T, Miyazawa T, Nakagawa K. Evaluation of the anti-hyperglycemic effect and safety of microorganism 1-deoxynojirimycin. PLoS One. 2018 Jun 13;13(6):e0199057

  [5] Liu Q, Li X, Li C, Zheng Y, Peng G. 1-Deoxynojirimycin Alleviates Insulin Resistance via Activation of Insulin Signaling PI3K/AKT Pathway in Skeletal Muscle of db/db Mice. Molecules. 2015 Dec 4;20(12):21700-14

  [6] E S, Kijima R, Honma T, Yamamoto K, Hatakeyama Y, Kitano Y, Kimura T, Nakagawa K, Miyazawa T, Tsuduki T. 1-Deoxynojirimycin attenuates high glucose-accelerated senescence in human umbilical vein endothelial cells. Exp Gerontol. 2014 Jul;55:63-9

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