荆草苷:一种新型抗癌化合物

A. Oriola, A. J. Aladesanmi, T. Idowu, G. Arthur
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引用次数: 2

摘要

癌症目前是世界范围内的主要死亡原因。在尼日利亚,每100人中就有1人患有癌症。在各种癌症类型中,前列腺癌是报告的头号癌症病例,也是全球男性癌症死亡的第二大原因。非洲和中国的民族药中使用的少女乳房植物,Massularia acuminata作为鱼毒和治疗癌症。用80%乙醇浸渍法分别提取荆芥的根、茎、叶。采用甲基乙硫磺酸法(MTS, Promega®)检测三种提取物在浓度分别为25、50、75、100、150、200和250 μg/mL的5个重复下对前列腺癌细胞DU 145的抑制作用。将各萃取物及分离物与标准药物(氯苄星,150 μg/mL)进行比较。其中叶提取物(M L)的抗癌活性最高。mcl对前列腺癌细胞的抑制作用显著(P <0.05), cc50 = 225.05±2.25 μg/mL。但与氯霉素相比,其活性显著(P < 0.05)降低(CC 50≥135.05 μg/mL)。用TLC生物自显像技术对叶提取物进行活性引导柱层析,得到一种棕色半固体化合物,表征为4-(3”,3”-二羟基-1-巯基丙基)苯基葡萄糖吡喃苷。该化合物经鉴定为一种新的酚类糖苷,命名为“紫荆苷”。在250 μg/mL浓度下,荆草苷对活的前列腺癌细胞的抑制作用显著(P < 0.05)(75.28±4.76%)。这是首次证实尖锐支原体是一种抗前列腺癌的抗癌药物。关键词:荆草苷,抗癌化合物,少女乳腺植物,MTS法,DU-145
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Acuminatoside: a new anticancer compound from the maiden breast plant
Cancer is currently a leading cause of death worldwide. In Nigeria, one out of every one hundred people lives with cancer. Among various cancer types is prostate cancer, the number one reported cancer cases and the second leading cause of cancer mortality in men worldwide. The maiden breast plant, Massularia acuminata used in the African and Chinese ethno-medicines as fish poison and for the management of cancer. The root, stem, and leaf of M. acuminata were extracted separately with 80% ethanol by maceration. The three extracts were tested against Prostate cancer cell line DU 145 at concentrations 25, 50, 75, 100, 150, 200, and 250 μg/mL in five replicates, using methanethiosulphonate assay (MTS, Promega®). All extracts and isolated compound were compared with standard drug (chlorambucil, 150 μg/mL). The leaf extract (M L ) was the most anticancer active. M L demonstrated significant ( P <0.05) percentage reduction in viable prostate cancer cell with a CC 50 = 225.05±2.25 μg/mL. However, it was significantly ( P < 0.05) lower in activity when compared to chlorambucil (CC 50 ≥ 135.05 μg/mL). An activity-guided column chromatographic fractionation of the leaf extract (ML) monitored with TLC bioautography afforded a brown semi-solid compound characterized as 4-(3'', 3''-dihydroxy-1-mercaptopropyl) phenyl glucosylpyranoside. This compound was identified as a new phenolic glycoside, and named “acuminatoside”. At 250 μg/mL, acuminatoside demonstrated significant ( P < 0.05) reduction (75.28±4.76 %) in viable prostate cancer cells. This is the first validation of M. acuminata as an anticancer agent against Prostate cancer. Keywords: Acuminatoside, anticancer compound, maiden breast plant, MTS assay, DU-145
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