羽扇豆烷三萜及其新衍生物作为抗前列腺癌细胞的增殖剂
Lupane Triterpenoids and New Derivatives as Antiproliferative Agents Against Prostate Cancer Cells.
作者信息
Castro María Julia, Careaga Valeria Pilar, Sacca Paula Alejandra, Faraoni María Belén, Murray Ana Paula, Calvo Juan Carlos
机构信息
Institute of Chemistry of the South (INQUISUR), CONICET, Department of Chemistry, National University of the South, Bahía Blanca, Argentina
Microanalysis Unit and Physical Methods in Organic Chemistry (UMYMFOR), UBA-CONICET, Department of Organic Chemistry, School of Exact and Natural Sciences, University of Buenos Aires, Buenos Aires, Argentina.
出版信息
Anticancer Res. 2019 Jul;39(7):3835-3845. doi: 10.21873/anticanres.13533.
BACKGROUND/AIM: This study examined the potential role of natural triterpenoids lupeol, calenduladiol and heliantriol B2, and a set of 19 derivatives, as antiproliferative and antimetastatic agents against prostate cancer cells.
MATERIALS AND METHODS
Natural triterpenoids were isolated from Chuqiraga erinaceae. Analogs were obtained by transformations of lupeol and calenduladiol. The effects of compounds on PC-3 and LNCaP cells were determined using the MTT assay. Compounds with half-maximal inhibitory concentration <70 μM were evaluated as antimetastatic agents by a wound-healing assay.
RESULTS
Lupeol-3β-sulfate, a new semisynthetic lupane, was the most active compound. In general, sulfated derivatives displayed higher activity than the lead against both cell lines. A new analog, calenduladiol-3β-monosulfate, inhibited the migration of PC-3 cells; heliantriol B2 and 3β-aminolupane inhibited the migration of LNCaP cells in a concentration-dependent manner.
CONCLUSION
Our study provides novel agents with cytotoxic effects on prostate cancer cells, which may represent a potential new therapeutic approach for prostate cancer.
背景/目的：本研究考察了天然三萜类化合物羽扇豆醇、金盏二醇和半日花三醇B2以及一组19种衍生物作为抗前列腺癌细胞增殖和转移剂的潜在作用。
材料与方法
从刺叶楚葵中分离出天然三萜类化合物。通过羽扇豆醇和金盏二醇的转化获得类似物。使用MTT法测定化合物对PC-3和LNCaP细胞的作用。通过伤口愈合试验评估半数抑制浓度<70 μM的化合物作为抗转移剂的效果。
结果
新型半合成羽扇烷类化合物羽扇豆醇-3β-硫酸盐是活性最高的化合物。总体而言，硫酸化衍生物对两种细胞系的活性均高于先导化合物。一种新的类似物金盏二醇-3β-单硫酸盐可抑制PC-3细胞的迁移；半日花三醇B2和3β-氨基羽扇烷以浓度依赖性方式抑制LNCaP细胞的迁移。
结论
我们的研究提供了对前列腺癌细胞具有细胞毒性作用的新型药物，这可能代表一种潜在的前列腺癌新治疗方法。
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