Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt.
Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, Japan.
Nat Prod Res. 2022 Feb;36(4):1118-1122. doi: 10.1080/14786419.2020.1855162. Epub 2020 Dec 4.
In our promising project toward discovery of secondary metabolites with potential anticancer activity against human cervical cancer, seven marine organisms were screened for their cytotoxic activity against HeLa cancer cell line using MTT colorimetric assay. The crude extract of the outer shell of showed promising activity with 88.02% inhibition at a concentration 250 µg/ml. Chromatographic investigation of the Ethyl acetate fraction, which is the main contributor to the activity (IC= 43.1 ± 5.94 µg/ml), led to isolation of five compounds. Structures of the isolates were elucidated by 1 D and 2 D NMR spectroscopy and HR-ESI-MS analysis. 5,8-epidioxycholest-6-en-3 ol () and 5,8-epidioxycholest-6,9(11)-en-3 ol () showed the highest cytotoxic activity with IC values 12.1 ± 2.74 µg/ml and 21.8 ± 6.32 µg/ml, respectively. Epidioxy steroids with cholestane nucleus could be a prospective candidate for the development of drugs for treatment of human cervical cancer.
在我们探索具有潜在抗癌活性的次生代谢产物的项目中，我们筛选了 7 种海洋生物，以 MTT 比色法测定它们对 HeLa 癌细胞系的细胞毒性。研究结果显示，壳外层的粗提物在 250µg/ml 的浓度下表现出有希望的活性，抑制率为 88.02%。对活性主要贡献的乙酸乙酯部分进行色谱分析（IC=43.1±5.94µg/ml），导致分离出 5 种化合物。通过 1D 和 2D NMR 光谱和 HR-ESI-MS 分析，阐明了这些化合物的结构。化合物 5,8-epidioxycholest-6-en-3ol () 和 5,8-epidioxycholest-6,9(11)-en-3ol () 的细胞毒性最强，IC 值分别为 12.1±2.74µg/ml 和 21.8±6.32µg/ml。具有胆甾烷核的环氧甾体可能是开发治疗人类宫颈癌药物的有前途的候选物。
