Famojuro Tayo I, Elufioye Taiwo O, Olajide Olumayokun A, Dybek Michael, Adejare Adeboye
Department of Pharmacognosy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
Department of Pharmacy, School of Applied Sciences, University of Huddersfield, West Yorkshire, England.
Avicenna J Phytomed. 2021 Jan-Feb;11(1):54-67.
The incidence of multi-drug resistant cancer and the adverse effects associated with available chemotherapy have necessitated the search for new drug candidates. This study investigates the cytotoxic activity of .
Column chromatography (CC) and preparative thin layer chromatography (PTLC) were used to isolate compounds. Structural elucidation was done by spectroscopic analysis. MTT assay was used to evaluate cytotoxicity of the compounds against three human adenocarcinoma cells, using methotrexate and dimethyl sulfoxide (DMSO) as positive and negative controls, respectively. CyQuant direct cell proliferation and caspase-3/7 green detection assays were used to investigate the dichloromethane fraction. IC values of isolated compounds were determined from sigmoidal dose-response curve.
Four new cytotoxic compounds, benthamianoate (2), benthamiacone (3), benthamianin (5) and benthamianol (6), and two known compounds, methyl gallate (1) and 2-methoxyacrylic acid (4) were identified. All the compounds were active with the new monoterpenoid characterized as benthamiacone exhibiting the highest activity (IC 13.23-21.97 μg/ml) across cancer cell lines investigated. CyQuant direct cell proliferation assay showed significant reduction in the number of live carcinoma cells, while caspase-3/7 green detection assay showed significant increase in the number of dead carcinoma cells.
This study revealed potential cytotoxic compounds which are here reported for the first time from .
多重耐药癌症的发病率以及现有化疗相关的不良反应促使人们寻找新的候选药物。本研究调查了……的细胞毒性活性。
采用柱色谱法(CC)和制备型薄层色谱法(PTLC)分离化合物。通过光谱分析进行结构解析。使用MTT法评估化合物对三种人腺癌细胞的细胞毒性,分别以甲氨蝶呤和二甲基亚砜(DMSO)作为阳性和阴性对照。使用CyQuant直接细胞增殖和caspase-3/7绿色检测法研究二氯甲烷馏分。从S形剂量反应曲线确定分离化合物的IC值。
鉴定出四种新的细胞毒性化合物,即本氏酸酯(2)、本氏锥酮(3)、本氏宁(5)和本氏醇(6),以及两种已知化合物,即没食子酸甲酯(1)和2-甲氧基丙烯酸(4)。所有化合物均具有活性,其中新的单萜类化合物本氏锥酮在所研究的癌细胞系中表现出最高活性(IC为13.23 - 21.97μg/ml)。CyQuant直接细胞增殖试验显示活癌细胞数量显著减少,而caspase-3/7绿色检测试验显示死癌细胞数量显著增加。
本研究揭示了潜在的细胞毒性化合物,本文首次报道来自……