Reyes-Chilpa Ricardo, Estrada-Muñiz Elizabet, Apan Teresa Ramírez, Amekraz Badia, Aumelas Andre, Jankowski Christopher K, Vázquez-Torres Mario
Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Delagación Coyoacan México D.F. 04510, Mexico.
Life Sci. 2004 Aug 13;75(13):1635-47. doi: 10.1016/j.lfs.2004.03.017.
Calophyllum brasiliense (Clusiaceae) is a big tree from the Tropical Rain Forests of the American continent. The organic extracts from the leaves yielded coumarins of the mammea type: mammea A/BA, A/BB, B/BA, B/BB, C/OA, C/OB, B/BA cyclo F, B/BB cyclo F, and isomammeigin. The triterpenoids friedelin and canophyllol, as well as the biflavonoid amentoflavone, protocatechuic and shikimic acids, were also obtained. Most of the isolated compounds were tested in vitro against K562, U251, and PC3 human tumor cell lines. The coumarins were cytotoxic against the three cell lines, the highest activity was shown by mammea A/BA (IC50 = 0.04 to 0.59 microM). The mixtures of mammea A/BA + A/BB, mammea B/BA + B/BB and mammea C/OA + C/OB were also highly active (IC50 < 4.05 microM). Friedelin was cytotoxic only against PC3, and U251 lines. Inhibition of HIV-1 reverse transcriptase was also assayed in vitro; however, none of the tested compounds (250 microM) prevented the activity of this enzyme. Most of the isolated compounds were also inactive against fourteen bacterial strains; however mammea A/BA + A/BB, and mammea C/OA + C/OB inhibited the growth of Staphylococcus aureus, S. epidermidis and Bacillus subtilis.
巴西红厚壳(藤黄科)是一种源自美洲大陆热带雨林的大树。从其叶子中提取的有机提取物含有山竹子型香豆素:山竹子素A/BA、A/BB、B/BA、B/BB、C/OA、C/OB、B/BA环F、B/BB环F和异山竹子素。还获得了三萜类化合物木栓酮和红厚壳醇,以及双黄酮穗花杉双黄酮、原儿茶酸和莽草酸。对分离得到的大多数化合物进行了体外抗K562、U251和PC3人肿瘤细胞系的测试。香豆素对这三种细胞系均具有细胞毒性,其中山竹子素A/BA的活性最高(IC50 = 0.04至0.59微摩尔)。山竹子素A/BA + A/BB、山竹子素B/BA + B/BB和山竹子素C/OA + C/OB的混合物也具有高活性(IC50 < 4.05微摩尔)。木栓酮仅对PC3和U251细胞系具有细胞毒性。还进行了体外对HIV-1逆转录酶抑制作用的测定;然而,所测试的化合物(250微摩尔)均未抑制该酶的活性。大多数分离得到的化合物对十四种细菌菌株也无活性;然而,山竹子素A/BA + A/BB和山竹子素C/OA + C/OB抑制了金黄色葡萄球菌、表皮葡萄球菌和枯草芽孢杆菌的生长。