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D-氨基葡萄糖及其衍生物抗肿瘤活性的初步研究 被引量:13

Preliminary studies on the antitumor activities of D-glucosamine and its derivatives
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摘要 目的 观察氨基葡萄糖盐酸盐(GlcNH2·HCl)、氨基葡萄糖(GlcNH2)和N-乙酰氨基葡萄糖(NAG)体外抑制人肝癌细胞(SMMC-7721)生长的作用,对小鼠S18。肉瘤的肿瘤抑制作用以及对免疫系统的影响并探讨其作用机制。方法 采用MTT法检测不同浓度的单糖对SMMC-7721细胞生长的影响,倒置显微镜观察细胞形态,琼脂糖凝胶电泳进行DNA断裂分析,流式细胞仪检测对细胞周期的影响。采取灌胃给药的方式,观察GlcNH2·HCl对S18。小鼠瘤重、胸腺重和脾重以及荷瘤小鼠淋巴细胞转化率的影响。结果 GlcNH2·HCl和GlcNH2能明显抑制肝癌细胞SMMC-7721的生长,且存在剂量依赖性,在500μg·mL^-1浓度下,Glc-NH2·HCl和GlcNH2的抑制率为50.24%和52.19%,在1000μg·mL^-1浓度下的抑制率分另0为82.21%和83.2%。GlcNH2·HCl对SMMC-7721细胞存在周期特异性,可以使细胞发生S期阻滞。NAG对肝癌细胞的生长没有明显抑制作用。GlcNH2·HCl在125~500mg·kg^-1的剂量范围内,对小鼠S180肉瘤均有一定的抑制作用,平均抑瘤率在27.84%~34.02%之间,其中250mg·kg^-1剂量的抑制作用最强,在该剂量范围下,GlcNH2·HCl对荷瘤小鼠具有明显增加胸腺指数和脾指数的作用,同时促进荷瘤小鼠脾脏T淋巴细胞转化,无明显毒副作用。结论 GlcNH2·HCl体外呈剂量依赖性抑制人肝癌细胞SMMC-7721的生长,体内可能是通过直接杀伤肿瘤细胞的细胞毒作用和提高S180肉瘤小鼠细胞免疫水平来发挥抑瘤作用。 Objective The growth inhibitory effects of GlcNH2 · HCl, GlcNH2 and NAG on human hepatoma SMMC-7721 cells in vitro was investigated. The antitumor activity of GlcNH2 · HCl against Sarcoma180 in KM mice was also investigated. Methods The cell viability in vitro was examined with MTT assay. DNA isolation and cell-cycle analyses were also performed. GlcNH2 · HCl was ig administered to Sarcoma180 KM mice. The inhibition rates, spleen and thymus index were calculated. Results GlcNH2 · HCl and GlcNH2 resulted in a concentration-dependent reduction in hepatoma cell growth. The inhibition rates against SMMC-7721 cell of GlcNH2 · HCl and GlcNH2 at concentration of 500μg·mL^-1 were 50.24% and 52. 19%. As to the concentration of 1000μg·mL^-1, the rates were 82.21% and 83.20% . This effect was accompanied by a marked increase in the proportion of S phase cells. Compared with the control, there was no significant difference among various concentrations of NAG, GlcNH2 · HC1 exhibited inhibitiory effect against Sarcomas80 in mice at the dosage of 125~500 mg ~ kg^-1 , and the inhibition rate was about 27.84%~34. 02%. The optimal inhibitory effect was 250 mg ~ kg^-1. GlcNH2 ~ HCl could enhance the weights of thymus and spleen. In addition, it could promote lymphocyte transformation. Conclusion It is therefore postulated that the antitumor effect of GlcNH2 - HC1 is probably host-mediated and cytocidal.
出处 《中国海洋药物》 CAS CSCD 2006年第2期26-31,共6页 Chinese Journal of Marine Drugs
基金 国家"十五"863课题资助项目(2001AA625050)
关键词 氨基葡萄糖盐酸盐 氨基葡萄糖 N-乙酰氨基葡萄糖 人肝癌细胞 D-glucosamine hydrochloride D-glucosamine N-acetyl glucosamine human hepatoma cell
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  • 1蒋挺大.壳聚糖金属配合物的催化作用研究进展[J].化学通报,1996(1):22-27. 被引量:33
  • 2罗宣干,卓仁禧,李满庆.5-氟脲嘧啶的D-氨基葡萄糖衍生物的合成及其抗肿瘤活性的研究[J].高等学校化学学报,1996,17(9):1416-1420. 被引量:46
  • 3汤世钦 陈仲刚.氨基葡萄糖在保健食品和医药方面的应用[A]..第三届甲壳索化学与应用研讨会论文集[C].,2001.42.
  • 4[3]Brief AA, Maurer SG, Di Cesare PE. Use of gulcosamine and chondroitin sulfate in the management of osteoarthritis [J]. J Am Acad Orthop Surg, 2001;9(2):71-78.
  • 5[5]Pi Perno M, Reboul P, Hellio Le, et al. Glucosamine Sulfate modulates dysregulated activities of human osteoarthritic chondrocytes in vitro [J]. Osteoarthritis Cartilage, 2000; 8(3): 207-212.
  • 6Chun-Cheng Lin, Chun-Hung Lin, Chi-Huey Wong.Siallc acid aldolase-catalyzed condensation of pyruvate and N-substituted mannosamine: a useful method for the synthesis of N-substltuted sialic acids[J]. Tetrahedron Letters ,1997,38(15) :2649.
  • 7Wen-Yang Wu, Betty Jin, David C. et al. A facile synthesis of a useful 5-N-substitiuted- 3,5-dideoxy-D-glycero-D-galacto-2-nonulosonic acid from 2-acetamido-2-deoxy-D-glucose[J]. Carbohydrate Research, 1997,300(5) : 171
  • 8Fabien P. Boulineau, Alexander Wei. Stereoselectire synthesis of [^13C] methyl 2-[^15N] amino-2-deoxy-β-Dglueopyranoside derivatives [J]. Carbohydrate Research,2001 ,SS4(9):271.
  • 9David Crich and Vadim Dudkin. Why are the hydroxy groups of partially protected N-acetyl- glucosamine derivatives such poor glycosyl acceptors, and what can be done about it? A comparative study of the reactivity of N-acetyl-, N-phthalimido-, and 2-azido-2-deoxy-glucosamine derivatives in glycosylation. 2-picolinyl ethers as reactivhy-enhancing replacements for benzyl ethers [J]. J. Am.Chem. Soy. ,2001,123(28):6819.
  • 10Frederic Massiere, Marie-Ange Badet-Denisot,Lo?c Rene, and Bermand Badet. Synthesis, and Evaluation of the First Mechanism-Based Inhibitor of Glucosamine 6-Phosphate Synthase[J]. J. Am. Chem. Soc., 1997, 119(24) :6010.

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