黑树莓提取物及其组分含有血管生成抑制剂。

Black raspberry extract and fractions contain angiogenesis inhibitors.

作者信息

Liu Zhijun, Schwimer Joshua, Liu Dong, Greenway Frank L, Anthony Catherine T, Woltering Eugene A

机构信息

Louisiana State University Agricultural Center, 227 Renewable Natural Resources Building, Baton Rouge, Louisiana 70803, USA.

出版信息

J Agric Food Chem. 2005 May 18;53(10):3909-15. doi: 10.1021/jf048585u.

DOI:10.1021/jf048585u

PMID:15884816

Abstract

Targeted therapies, such as agents that inhibit angiogenesis, offer hope as complementary agents in cancer therapy. Angiogenesis-inhibiting agents have the potential for inhibiting tumor growth and limiting the dissemination of metastasis, thus keeping cancers in a static growth state for prolonged periods. Black raspberry (Rubus occidentalis) extract was discovered to be antiangiogenic (0.1% w/v) in a novel human tissue-based in vitro fibrin clot angiogenesis assay. Assay-guided fractionation of a crude black raspberry extract resulted in a highly potent antiangiogenic fraction that accounted for only 1% of the fresh weight of whole black raspberries. At 0.075% (w/v), the active fraction completely inhibited angiogenic initiation and angiogenic vessel growth. Further subfractionation of this active fraction revealed the coexistence of multiple antiangiogenic compounds, one of which has been identified as gallic acid. However, the individual subfractions did not outperform the active whole fraction. These findings suggest that an active black raspberry fraction may be a promising complementary cancer therapy. It is natural and potent enough for manageable dosing regimens. These extracts contain multiple active ingredients that may be additive or synergistic in their antiangiogenic effects. These observations warrant further investigations in animals and human trials.

摘要

靶向治疗，如抑制血管生成的药物，有望成为癌症治疗中的辅助药物。血管生成抑制药物具有抑制肿瘤生长和限制转移扩散的潜力，从而使癌症长期处于静止生长状态。在一种基于人体组织的新型体外纤维蛋白凝块血管生成试验中，发现黑树莓（Rubus occidentalis）提取物具有抗血管生成作用（0.1% w/v）。对黑树莓粗提物进行分析引导的分级分离，得到了一种高效的抗血管生成级分，其重量仅占整个黑树莓鲜重的1%。在0.075%（w/v）时，该活性级分完全抑制血管生成起始和血管生成血管生长。对该活性级分进一步细分发现多种抗血管生成化合物共存，其中一种已被鉴定为没食子酸。然而，各个细分级分的效果并不优于活性全级分。这些发现表明，活性黑树莓级分可能是一种有前景的辅助癌症治疗方法。它天然且效力足够，适用于可控的给药方案。这些提取物含有多种活性成分，它们的抗血管生成作用可能是相加或协同的。这些观察结果值得在动物和人体试验中进一步研究。