ANTITUMOR AGENTS .129. TANNINS AND RELATED-COMPOUNDS AS SELECTIVE CYTOTOXIC AGENTS
ANTITUMOR AGENTS .129. TANNINS AND RELATED-COMPOUNDS AS SELECTIVE CYTOTOXIC AGENTS
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DOI：
10.1021/np50086a002
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发表时间：
1992-08-01
影响因子：
5.1
通讯作者：
LEE, KH
中科院分区：
文献类型：
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作者：
KASHIWADA, Y;NONAKA, G;LEE, KH
57单宁和相关化合物，包括没食子单宁，鞣花单宁，缩合和复杂的单宁，进行了评估，对人类肿瘤细胞系，包括恶性黑色素瘤，肺癌，回盲腺癌，表皮样癌，恶性黑色素瘤，髓母细胞瘤细胞系的细胞毒性。其中，诃子酸[1]、老鹳草素[2]、sanguiin H-11 [3]、4，5-二-O-没食子酰奎尼酸[12]、1，3，4，5-四-O-没食子酰奎尼酸[15]、1（β）-O-没食子酰pedunculagin [24]、fusrosin [29]、castalagin [38]、sanguiin H-2 [34]、vescalagin [39]、grandinin [40]、phylryraeoidin A [42]、（-）表儿茶素3-O-没食子酸酯[50]、肉桂单宁B2 [55]和acutissimin A [56]对PRMI-7951黑素瘤细胞表现出中等选择性细胞毒性，ED 50值在0.1-0.8 μ g/ml范围内。还观察到了strictinin [22]、pedunculagin [23]、eugeniin [25]、elaeocarpusin [28]、punicacortein C [37]、pedunculagin [41]、sanguiin H-6 [43]、矢车菊苷配质B-2 3，3 '-二-O-没食子酸酯[51]、矢车菊苷配质C-1 3，3'，3”-三-O-没食子酸酯[52]和肉桂单宁B对黑素瘤细胞的选择性细胞毒性。[54] ED 5值为1-4 μ g/ml。发现所有单宁对肺癌（A-549）、回盲部腺癌（HCT-8）、鼻咽癌表皮样癌（KB）和髓母细胞瘤（TE-67 - 1）肿瘤细胞无活性（> 10 μ g/ml）。
Fifty-seven tannins and related compounds, including gallotannins, ellagitannins, and condensed and complex tannins, were evaluated for their cytotoxicities against human tumor cell lines, including malignant melanoma, lung carcinoma, ileocecal adenocarcinoma, epidermoid carcinoma, malignant melanoma, and medulloblastoma cell lines. Among them, chebulagic acid [1], geraniin [2], sanguiin H-11 [3], 4,5-di-O-galloylquinic acid [12], 1,3,4,5-tetra-O-galloylquinic acid [15], 1(beta)-O-galloylpedunculagin [24], furosin [29], castalagin [38], sanguiin H-2 [34], vescalagin [39], grandinin [40], phyllyraeoidin A [42], (-)epicatechin 3-O-gallate [50], cinnamtannin B2 [55], and acutissimin A [56] exhibited moderate selective cytotoxicity against PRMI-795 1 melanoma cells with ED50 values in the range of 0.1-0.8-mu-g/ml. Selective cytotoxicities against the melanoma cells were also observed for strictinin [22], pedunculagin [23], eugeniin [25], elaeocarpusin [28], punicacortein C [37], casuarinin [41], sanguiin H-6 [43], procyanidin B-2 3,3'-di-O-gallate [51], procyanidin C-1 3,3',3"-tri-O-gallate [52], and cinnamtannin B, [54] with ED5, values of 1-4-mu-g/ml. All of the tannins were found to be inactive (> 10-mu-g/ml) against lung carcinoma (A-549), ileocecal adenocarcinoma (HCT-8), epidermoid carcinoma of nasopharnyx (KB), and medulloblastoma (TE-67 1) tumor cells.