来自卡朱卡拉巴豆的两种19-降-克罗烷二萜类化合物反式脱氢巴豆素和顺式巴豆素的抗肿瘤活性。

Anti-tumour activity of two 19-nor-clerodane diterpenes, trans-dehydrocrotonin and trans-crotonin, from Croton cajucara.

作者信息

Grynberg N F, Echevarria A, Lima J E, Pamplona S S, Pinto A C, Maciel M A

机构信息

Departamento de Química, Universidade Federal Rural do Rio de Janeiro, Brazil.

出版信息

Planta Med. 1999 Dec;65(8):687-9. doi: 10.1055/s-1999-14042.

DOI:10.1055/s-1999-14042

PMID:10630105

Abstract

The effects of two nor-diterpenes, trans-dehydrocrotonin (DCTN) and trans-crotonin (CTN) from Croton cajucara (Euphorbiaceae), on the survival of mice bearing Sarcoma 180 and Ehrlich carcinoma ascitic tumours, on the proliferation of cultured Ehrlich cells and TNF alpha activity were determined. When the mice were treated with 80 and 120 mg/kg of DCTN or 38 mg/kg of 5-FU a significant anti-tumour activity was obtained (%T/C of 128-140). The cytotoxicity against Ehrlich carcinoma was 16 microM for DCTN and CTN whereas the flavonoid quercetin was cytotoxic at 44 microM in 48 h cell culture. No apoptosis was seen on in vitro electrophoresis of DNA extracted from the tumour cells treated with DCTN and CTN. A significant TNF alpha activity was detected in Ehrlich tumour-bearing mice treated with DCTN suggesting an enhanced immune function.

摘要

测定了来自大戟科卡朱卡拉巴豆（Croton cajucara）的两种去甲二萜类化合物反式脱氢巴豆毒素（DCTN）和顺式巴豆毒素（CTN）对荷肉瘤180和艾氏腹水癌小鼠存活、培养的艾氏细胞增殖以及肿瘤坏死因子α（TNFα）活性的影响。当用80和120mg/kg的DCTN或38mg/kg的5-氟尿嘧啶（5-FU）处理小鼠时，获得了显著的抗肿瘤活性（%T/C为128 - 140）。DCTN和CTN对艾氏癌的细胞毒性为16μM，而在48小时细胞培养中，类黄酮槲皮素在44μM时具有细胞毒性。在用DCTN和CTN处理的肿瘤细胞提取的DNA的体外电泳中未观察到凋亡。在用DCTN处理的荷艾氏瘤小鼠中检测到显著的TNFα活性，表明免疫功能增强。