Dutra Lívia M, Bomfim Larissa M, Rocha Suellen L A, Nepel Angelita, Soares Milena B P, Barison Andersson, Costa Emmanoel V, Bezerra Daniel P
Department of Chemistry, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
Gonçalo Moniz Research Center, Oswaldo Cruz Foundation (Fiocruz), Rua Waldemar Falcão, 121, Candeal, 40296-710 Salvador, Bahia, Brazil.
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3315-20. doi: 10.1016/j.bmcl.2014.06.005. Epub 2014 Jun 11.
This work describes a novel ent-kaurane diterpene, ent-3β-hydroxy-kaur-16-en-19-al along with five known ent-kaurane diterpenes, ent-3β,19-dihydroxy-kaur-16-eno, ent-3β-hydroxy-kaur-16-eno, ent-3β-acetoxy-kaur-16-eno, ent-3β-hydroxy-kaurenoic acid and kaurenoic acid, as well as caryophyllene oxide, humulene epoxide II, β-sitosterol, stigmasterol and campesterol from the stem bark of Annona vepretorum Mart. (Annonaceae). Cytotoxic activities towards tumor B16-F10, HepG2, K562 and HL60 and non-tumor PBMC cell lines were evaluated for ent-kaurane diterpenes. Among them, ent-3β-hydroxy-kaur-16-en-19-al was the most active compound with higher cytotoxic effect over K562 cell line (IC50 of 2.49 μg/mL) and lower over B16-F10 cell line (IC50 of 21.02 μg/mL).
这项研究描述了一种新型对映-贝壳杉烷二萜，对映-3β-羟基-贝壳杉-16-烯-19-醛，以及五种已知的对映-贝壳杉烷二萜，对映-3β,19-二羟基-贝壳杉-16-烯、对映-3β-羟基-贝壳杉-16-烯、对映-3β-乙酰氧基-贝壳杉-16-烯、对映-3β-羟基-贝壳杉烯酸和贝壳杉烯酸，还有氧化石竹烯、环氧葎草烯II、β-谷甾醇、豆甾醇和菜油甾醇，它们都来自马氏番荔枝（番荔枝科）的茎皮。评估了对映-贝壳杉烷二萜对肿瘤B16-F10、HepG2、K562和HL60以及非肿瘤PBMC细胞系的细胞毒性活性。其中，对映-3β-羟基-贝壳杉-16-烯-19-醛是活性最高的化合物，对K562细胞系具有较高的细胞毒性作用（IC50为2.49μg/mL），对B16-F10细胞系的毒性较低（IC50为21.02μg/mL）。
