Tahsin Tasmia, Wansi Jean Duplex, Al-Groshi Afaf, Evans Andrew, Nahar Lutfun, Martin Claire, Sarker Satyajit Dey
Medicinal Chemistry and Natural Products Research Group, School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, James Parsons Building, Byrom Street, Liverpool, L3 3AF, UK.
Department of Chemistry, University of Douala, Faculty of Sciences, 24157, Douala, Cameroon.
Phytother Res. 2017 Aug;31(8):1215-1219. doi: 10.1002/ptr.5842. Epub 2017 Jun 1.
The bioassay-guided fractionation of the n-hexane extract of Citrus reticulata Blanco (Rutaceae) stem bark yielded scoparone (1), xanthyletin (2), lupeol (3), β-amyrin (4), stigmasterol (5), β-sitosterol (6) and palmitic acid. The structures of these compounds were determined by comprehensive spectroscopic analyses, i.e., 1D and 2D NMR and EI-MS, and by comparison with the reported data. Extracts, fractions and isolated compounds 1-6 were assessed for cytotoxicity by the 3-(4,5-dimethylthiazol-2-yl)-2,5-dphenyltetrazolium bromide (MTT) assay against three human cancer cell lines, i.e., human lung adenocarcinoma cell line A549, human breast adenocarcinoma cell line MCF7 and human Caucasian prostate adenocarcinoma cell line PC3. Significant activity of the n-hexane and the dichloromethane extracts was observed against the breast cancer cell line MCF7 with IC s of 45.6 and 54.7 μg/mL, respectively. Moreover, the 70% ethyl acetate in n-hexane chromatographic fraction showed significant activity displaying IC values of 53.0, 52.4 and 49.1 μg/mL against the cancer cell lines A549, MCF7 and PC3, respectively. Encouragingly, an IC of 510.0 μg/mL against the human normal prostate cell line PNT2 indicated very low toxicity and hence favourable selectivity indices for the 70% ethyl acetate in n-hexane fraction in the range of 9.6-10.4 towards cell lines A549, MCF7 and PC3. Because compounds isolated from the above fraction only delivered IC values in the range of 18.2-96.3, 9.2-34.1 and 7.5-97.2 μg/mL against A549, MCF7 and PC3 cell lines, respectively, synergistic action between compounds is suggested. Bioassay results valorize the anticancer effectivity of the stem bark of this plant in Cameroonian pharmacopoeia. Copyright © 2017 John Wiley & Sons, Ltd.
对芸香科植物橘（Citrus reticulata Blanco）茎皮的正己烷提取物进行生物测定导向的分离，得到了滨蒿内酯（1）、黄辛亭（2）、羽扇豆醇（3）、β-香树脂醇（4）、豆甾醇（5）、β-谷甾醇（6）和棕榈酸。这些化合物的结构通过综合光谱分析确定，即一维和二维核磁共振以及电子轰击质谱，并与已报道的数据进行比较。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四氮唑（MTT）法，针对三种人类癌细胞系，即人肺腺癌细胞系A549、人乳腺腺癌细胞系MCF7和人高加索前列腺腺癌细胞系PC3，对提取物、馏分和分离出的化合物1 - 6进行细胞毒性评估。观察到正己烷提取物和二氯甲烷提取物对乳腺癌细胞系MCF7具有显著活性，其IC50分别为45.6和54.7μg/mL。此外，正己烷色谱馏分中70%的乙酸乙酯馏分显示出显著活性，对癌细胞系A549、MCF7和PC3的IC50值分别为53.0、52.4和49.1μg/mL。令人鼓舞的是，对人正常前列腺细胞系PNT2的IC50为510.0μg/mL，表明其毒性非常低，因此正己烷馏分中70%的乙酸乙酯馏分对细胞系A549、MCF7和PC3的选择性指数在9.6 - 10.4范围内较好。由于从上述馏分中分离出的化合物对A549、MCF7和PC3细胞系的IC50值分别仅在18.2 - 96.3、9.2 - 34.1和7.5 - 97.2μg/mL范围内，提示化合物之间存在协同作用。生物测定结果证实了该植物茎皮在喀麦隆药典中的抗癌有效性。版权所有© 2017约翰威立父子有限公司。
