Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Department of Pharmacognosy, Faculty of Pharmacy, Horus University in Egypt, New Damietta, Egypt.
Pharm Biol. 2022 Dec;60(1):1374-1383. doi: 10.1080/13880209.2022.2098346.
Traditionally, Oleaceae plants are used to treat many diseases, such as rheumatism, hypercholesterolaemia, or ulcers.
To investigate the cytotoxic potential of L., L., and L. (Oleaceae) extracts against selected human cancer cells lines, followed by a phytochemical investigation of the most potent one.
The 95% ethanol extracts of aerial parts of three oleaceous plants were examined for their cytotoxicity against HepG-2, MCF-7, and THP-1 cell lines using MTT assay and doxorubicin (positive control). was bio-selected and submitted to bio-guided fractionation. Chromatographic workup of ethyl acetate and -butanol fractions afforded two new compounds; 1-methoxyjasmigenin () and 1-methyl-9-aldojasmigenin (), along with five known ones (). Structures were unambiguously elucidated using 1D/2D NMR and ESI-HRMS. Isolated compounds were assessed for their anti-proliferative potential, and both selectivity index and statistical significance were determined. Molecular docking was conducted against the Mcl-1 receptor using (AZD5991) as a standard.
Jasmoside () was the most potent anticancer compound showing IC values of 66.47, 41.32, and 27.59 µg/mL against HepG-2, MCF-7, and THP-1 cell lines, respectively. Moreover, isojasminin () exhibited IC values of 33.49, 43.12, and 51.07 µg/mL against the same cell lines, respectively. Interestingly, exhibited the highest selectivity index towards MCF-7 and THP-1, even greater than doxorubicin. Molecular docking results were in full agreement with the MTT assay and the proposed SAR.
In this study, two new compounds were purified. The biological activity highlighted jasmoside () as a lead anticancer drug for further future investigation.
传统上，木犀科植物被用于治疗多种疾病，如风湿、高胆固醇血症或溃疡。
研究木犀科植物的 L.、L.和 L.（木犀科）提取物对选定的人类癌细胞系的细胞毒性作用，然后对最有效的一种进行植物化学研究。
用 MTT 法和阿霉素（阳性对照）检测三种木犀科植物地上部分的 95%乙醇提取物对 HepG-2、MCF-7 和 THP-1 细胞系的细胞毒性。对具有生物活性的进行生物导向分离。乙酸乙酯和 -丁醇部分的色谱分离得到两个新化合物；1-甲氧基齐墩果苷（）和 1-甲基-9-醛齐墩果苷（），以及五个已知化合物（）。使用 1D/2D NMR 和 ESI-HRMS 明确阐明了结构。评估了分离化合物的抗增殖潜力，并确定了选择性指数和统计学意义。使用（AZD5991）作为标准，对 Mcl-1 受体进行分子对接。
齐墩果酸苷（）是最有效的抗癌化合物，对 HepG-2、MCF-7 和 THP-1 细胞系的 IC 值分别为 66.47、41.32 和 27.59μg/ml。此外，异齐墩果苷（）对相同细胞系的 IC 值分别为 33.49、43.12 和 51.07μg/ml。有趣的是，对 MCF-7 和 THP-1 的选择性指数最高，甚至高于阿霉素。分子对接结果与 MTT 测定和提出的 SAR 完全一致。
在这项研究中，纯化了两种新化合物。生物活性突出了齐墩果酸苷（）作为进一步未来研究的潜在抗癌药物。
