背景:熊果酸(1)和齐墩果酸(2)的混合物(1:1和1:2),齐墩果酸(2),角鲨烯(3),叶绿素a(4),wrightiadione(5),和α-amyrin乙酸酯(6)从阴毛的叶子和树枝的二氯甲烷(CH2Cl2)提取物中分离出来(R。Br.).
目的:测试1-6的细胞毒性电位。
方法:1-6对三种人类癌细胞系的抗增殖活性,乳腺(MCF-7)和结肠(HT-29和HCT-116),和一个正常的细胞系,人真皮成纤维细胞新生儿(HDFn),使用PrestoBlue®细胞活力测定进行评估。
结果:化合物4、1和2(1:2),2,1和2(1:1),和5对HT-29表现出最大的细胞毒性作用,半数最大抑制浓度(IC50)值为0.68、0.74、0.89、1.70和4.07μg/mL,分别。将2与1的1:1混合物与1(HT-29和HCT-116的IC50分别为1.70和7.18μg/mL)和1:2的混合物与1(HT-29和HCT-116的混合物分别为0.74和3.46μg/mL)进行比较,2还显示出对HT-29和HCT-116的强细胞毒性潜力(0.89和2.33μg/mL,分别)。与对MCF-7具有低影响的混合物不同(对于1:1和1:2,IC50分别为20.75和30.06μg/mL),图2显示了对MCF-7(10.99μg/mL)的中等活性。化合物6对HCT-116显示最高的细胞毒性(IC50=4.07μg/mL)。
结论:1和2的混合物(1:1和1:2),2、3、4、5和6来自毛竹叶和树枝的CH2Cl2提取物(R。Br.)表现出不同的细胞毒性活性。除6以外的所有化合物对HT-29表现出最强的细胞毒性作用。另一方面,6对HCT-116的细胞毒性最大。总的来说,1-6对HT-29的毒性最高,其次是HCT-116和MCF-7。所有化合物均显示不同的抗HDFn活性(IC50<30μg/mL)。
结论:熊果酸(1)和齐墩果酸(2)的混合物(1:1和1:2),齐墩果酸(2),角鲨烯(3),叶绿素a(4),wrightiadione(5),和α-戊酸乙酸盐(6),从毛竹叶和树枝的二氯甲烷提取物中分离出来(R.Br.),对三种人类癌细胞系表现出不同的细胞毒性活性,乳腺(MCF-7)和结肠(HT-29和HCT-116),和一个正常的细胞系,人真皮成纤维细胞新生儿(HDFn),如使用PrestoBlue®细胞活力测定所评估的。所用缩写:IC50:半数最大抑制浓度。
BACKGROUND: Mixtures of ursolic acid (1) and oleanolic acid (2) (1:1 and 1:2), oleanolic acid (2), squalene (3), chlorophyll a (4), wrightiadione (5), and α-amyrin acetate (6) were isolated from the dichloromethane (CH2 Cl2) extracts of the leaves and twigs of Wrightia pubescens (R.Br.).
OBJECTIVE: To test for the cytotoxicity potentials of 1-6.
METHODS: The antiproliferative activities of 1-6 against three human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast neonatal (HDFn), were evaluated using the PrestoBlue® cell viability assay.
RESULTS: Compounds 4, 1 and 2 (1:2), 2, 1 and 2 (1:1), and 5 exhibited the most cytotoxic effects against HT-29 with half maximal inhibitory concentration (IC50) values of 0.68, 0.74, 0.89, 1.70, and 4.07 μg/mL, respectively. Comparing 2 with its 1:1 mixture with 1 (IC50 = 1.70 and 7.18 μg/mL for HT-29 and HCT-116, respectively) and 1:2 mixture with 1 (0.74 and 3.46 μg/mL for HT-29 and HCT-116, respectively), 2 also showed strong cytotoxic potential against HT-29 and HCT-116 (0.89 and 2.33 μg/mL, respectively). Unlike the mixtures which exhibited low effects on MCF-7 (IC50 = 20.75 and 30.06 μg/mL for 1:1 and 1:2, respectively), 2 showed moderate activity against MCF-7 (10.99 μg/mL). Compound 6 showed the highest cytotoxicity against HCT-116 (IC50 = 4.07 μg/mL).
CONCLUSIONS: Mixtures of 1 and 2 (1:1 and 1:2), 2, 3, 4, 5, and 6 from the CH2 Cl2 extracts of the leaves and twigs of W. pubescens (R.Br.) exhibited varying cytotoxic activities. All the compounds except 6 exhibited the strongest cytotoxic effects against HT-29. On the other hand, 6 was most cytotoxic against HCT-116. Overall, the toxicities of 1-6 were highest against HT-29, followed by HCT-116 and MCF-7. All the compounds showed varying activities against HDFn (IC50 < 30 μg/mL).
CONCLUSIONS: Mixtures of ursolic acid (1) and oleanolic acid (2) (1:1 and 1:2), oleanolic acid (2), squalene (3), chlorophyll a (4), wrightiadione (5), and α-amyrin acetate (6), isolated from the dichloromethane extracts of the leaves and twigs of Wrightia pubescens (R.Br.), showed varying cytotoxic activities against three human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast-neonatal (HDFn), as evaluated using the PrestoBlue® cell viability assay.Abbreviation Used: IC50: Half maximal inhibitory concentration.