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葡聚糖衍生物在针对可移植小鼠腹水瘤和实体瘤的单一及联合化疗中的应用。

Dextran derivatives in single and combination chemotherapy against transplantable mouse ascites and solid tumors.

作者信息

Suzuki M, Mikami T, Kadowaki M, Matsumoto T, Suzuki S

出版信息

Cancer Res. 1977 Sep;37(9):3448-54.

PMID:69495
Abstract

Dextran, a typical homopolysaccharide without antitumor activity, was modified by palmitoylation and/or phosphorylation to yield three derivatives: palmitoyldextran phosphate, dextran phosphate, and palmitoyldextran. Of these compounds, only palmitoyldextran phosphate showed growth-inhibitory activity against Ehrlich solid tumor in mice. In combination therapy with mitomycin C, bleomycin, cyclophosphamide, and 5-fluorouracil, palmitoyldextran phosphate manifested strong synergistic effects against both Sarcoma 180 ascites and L1210 leukemic tumors. The compound is not directly cytocidal against Sarcoma 180 ascites tumor, but it appears to act via activation of peritoneal macrophage. The antitumor activity of palmitoyldextran phosphate apparently is mainly due to immunological host-mediated mechanisms.

摘要

葡聚糖是一种典型的无抗肿瘤活性的同多糖,通过棕榈酰化和/或磷酸化进行修饰,得到三种衍生物:棕榈酰磷酸葡聚糖、磷酸葡聚糖和棕榈酰葡聚糖。在这些化合物中,只有棕榈酰磷酸葡聚糖对小鼠艾氏实体瘤具有生长抑制活性。在与丝裂霉素C、博来霉素、环磷酰胺和5-氟尿嘧啶的联合治疗中,棕榈酰磷酸葡聚糖对肉瘤180腹水瘤和L1210白血病肿瘤均表现出强烈的协同作用。该化合物对肉瘤180腹水瘤没有直接的杀细胞作用,但它似乎是通过激活腹腔巨噬细胞起作用。棕榈酰磷酸葡聚糖的抗肿瘤活性显然主要归因于宿主介导的免疫机制。

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