Uptake of a cholesterol-rich emulsion by breast cancer
Uptake of a cholesterol-rich emulsion by breast cancer
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DOI：
10.1006/gyno.2002.6654
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发表时间：
2002-06-01
影响因子：
4.7
通讯作者：
Maranhao, RC
中科院分区：
文献类型：
--
作者：
Graziani, SR;Igreja, FAF;Maranhao, RC
客观的。低密度脂蛋白（LDL）受体的过表达发生在几种癌细胞系中，并通过使用LDL作为载体提供了独特的药物靶向策略。但是，本地脂蛋白很难获得和处理。以前，我们表明，类似于天然LDL的脂质结构的脂质乳液（LDE）可能与LDL受体结合，并被急性脊髓细胞性白血病细胞吸收。我们还表明，LDE也可以集中在卵巢癌组织中。在这项研究中，我们测试了LDE是否被乳腺癌吸收。将标记为TC-99M标记的LDE注入了18名乳腺癌患者，并获得了肿瘤和转移性部位的核医学图像。随后，在全乳房切除术手术前24-30小时，将LDE标记为WIT [H-3]胆汁胆汁脂蛋白。用氯仿/甲醇提取脂质在手术过程中切除的正常和乳腺癌组织的碎片，并在闪烁溶液中测量其放射性。在所有18名乳腺癌患者中，获得了原发性肿瘤和转移部位的TC-99M-LDE图像。正如在肿瘤和正常乳腺组织中直接测量的那样，肿瘤中乳液放射性标记的量比正常组织（范围1.2-至8.8倍）大4.5倍。结论。与正常组织相比，LDE在恶性乳腺肿瘤组织中的浓度要多得多。因此，它具有携带针对乳腺癌细胞的药物或放射性核素，以诊断或治疗目的。 （C）2002 Elsevier Science（美国）。
Objective. Overexpression of low-density lipoprotein (LDL) receptors occurs in several cancer cell lines and offers a unique strategy for drug targeting by using LDL as vehicle. However, the native lipoprotein is difficult to obtain and handle. Previously, we showed that a lipidic emulsion (LDE) similar to the lipid structure of native LDL may bind to LDL receptors and be taken up by acute myelocytic leukemia cells. We also showed that LDE can also concentrate in ovarian cancer tissue. In this study, we tested whether LDE is taken up by breast carcinoma.Methods. LDE labeled with Tc-99m was injected into 18 breast cancer patients, and nuclear medicine images of the tumor and metastatic sites were acquired. Subsequently, LDE labeled wit [H-3]cholesteryl oleate was intravenously injected into 14 breast cancer patients 24-30 h before total mastectomy procedure. Fragments of normal and of breast cancer tissue excised during surgery were lipid extracted with chloroform/methanol and their radioactivity was measured in a scintillation solution.Results. Tc-99m-LDE images of the primary tumor and of metastasis sites were obtained in all 18 breast cancer patients. As directly measured in the tumor and in the normal mammary tissue, the amount of the emulsion radioactive label in the tumor was 4.5 times greater than in the normal tissue (range 1.2- to 8.8-fold).Conclusion. LDE concentrates much more in malignant breast tumor tissue than in the normal tissue. Thus it has potential to carry drugs or radionuclides directed against mammary carcinoma cells for diagnostic or therapeutic purposes. (C) 2002 Elsevier Science (USA).