Nigam V N, Brailovsky C A, Chopra C
Cancer Res. 1978 Oct;38(10):3315-21.
The attempt to synthesize a lipid A-like component (the active portion of lipopolysaccharides, but lacking its endotoxic activity) resulted in the production of fatty acyl sugars of which maltose tetrapalmitate was seen to yield the most promising results. It shows no endotoxic activity and elicits an antitumor response in tumor-transplanted animals as shown by (a) an enhancement of the host's capacity to reject a large number of tumor cells, (b) retardation of growth in tumor size, and (c) induction of hemorrhagic necrosis in certain tumors. Experiments with mammary ascites carcinoma show maltose tetrapalmitate to be as effective as is bacterial glycolipid mR595 in its antitumor activity. The degree of sensitivity to maltose tetrapalmitate varies with the tumor-host system: mammary ascites carcinoma less than NH = Cl2TSV5S = B16 less than L26. The mode of action of maltose tetrapalmitate appears to be via its modulation of the immune system. It is itself noncytotoxic to tumor cells in vitro. It is seen to stimulate the spleen cells of certain animals mitogenically, although it causes tumor rejection in all the types of animals tested. Also, it activates peritoneal exudate macrophages in tumor-bearing animals; whether specifically or nonspecifically has not yet been established.
合成类脂A样成分（脂多糖的活性部分，但缺乏其内毒素活性）的尝试导致了脂肪酰糖的产生，其中麦芽糖四棕榈酸酯显示出最有前景的结果。它没有内毒素活性，并且在肿瘤移植动物中引发抗肿瘤反应，表现为：（a）宿主排斥大量肿瘤细胞的能力增强；（b）肿瘤大小生长减缓；（c）某些肿瘤中出现出血性坏死。对乳腺腹水癌的实验表明，麦芽糖四棕榈酸酯在抗肿瘤活性方面与细菌糖脂mR595一样有效。对麦芽糖四棕榈酸酯的敏感程度因肿瘤-宿主系统而异：乳腺腹水癌＜NH = Cl2TSV5S = B16＜L26。麦芽糖四棕榈酸酯的作用方式似乎是通过调节免疫系统。它本身在体外对肿瘤细胞无细胞毒性。虽然它在所有测试的动物类型中都能引起肿瘤排斥，但它能有丝分裂地刺激某些动物的脾细胞。此外，它能激活荷瘤动物的腹腔渗出巨噬细胞；其激活是特异性的还是非特异性的尚未确定。
