Magalhães Hemerson Iury Ferreira, Veras Maria Leopoldina, Torres Márcia Rocha, Alves Ana Paula Negreiros Nunes, Pessoa Otília Deusdênia Loiola, Silveira Edilberto Rocha, Costa-Lotufo Letícia Veras, de Moraes Manoel Odorico, Pessoa Cláudia
Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, CP 3157, Ceará 60430-270, Brazil.
J Pharm Pharmacol. 2006 Feb;58(2):235-41. doi: 10.1211/jpp.58.2.0011.
We have evaluated the in-vitro and in-vivo antitumour activity of physalin B and physalin D isolated from the aerial parts of Physalis angulata. In-vitro, both compounds displayed considerable cytotoxicity against several cancer cell lines, showing IC50 values in the range of 0.58 to 15.18 microg mL(-1) for physalin B, and 0.28 to 2.43 microg mL(-1) for physalin D. The antitumour activity of both compounds was confirmed in-vivo using mice bearing sarcoma 180 tumour cells. The in-vivo antitumour activity was related to the inhibition of tumour proliferation, as observed by the reduction of Ki67 staining in tumours of treated animals. Histopathological examination of the kidney and liver showed that both organs were affected by physalin treatment, but in a reversible manner. These compounds were probably responsible for the previously described antitumour activity of ethanol extracts of P. angulata, and their identification and characterization presented here could explain the ethnopharmacological use of this species in the treatment of cancer.
我们评估了从酸浆地上部分分离得到的酸浆苦素B和酸浆苦素D的体外和体内抗肿瘤活性。在体外,这两种化合物对多种癌细胞系均显示出相当大的细胞毒性,酸浆苦素B的IC50值在0.58至15.18微克/毫升范围内,酸浆苦素D的IC50值在0.28至2.43微克/毫升范围内。使用携带肉瘤180肿瘤细胞的小鼠在体内证实了这两种化合物的抗肿瘤活性。如在接受治疗动物的肿瘤中观察到Ki67染色减少所示,体内抗肿瘤活性与肿瘤增殖的抑制有关。肾脏和肝脏的组织病理学检查表明,这两个器官均受到酸浆苦素处理的影响,但方式是可逆的。这些化合物可能是酸浆乙醇提取物先前所述抗肿瘤活性的原因,此处对它们的鉴定和表征可以解释该物种在癌症治疗中的民族药理学用途。