Research Unit of Environmental and Applied Chemistry, Department of Chemistry, Faculty of Science, University of Dschang, P O Box 183, Dschang, Cameroon.
International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Afr Health Sci. 2020 Mar;20(1):469-475. doi: 10.4314/ahs.v20i1.53.
Biological significance of is well advocated from the literature. In Cameroon, plants from this family are routinely used for the cure of liver, cancer and cardiovascular diseases. To date, no scientific investigation corresponding to the anti-cancer activity of extracts and isolated compounds of is available.
Current study is focused to elaborate the anti-proliferative effects of natural isolates (compounds 1-6, 9) and hemi-synthetic analogs (compounds 7-8) extracted from
Column chromatography of the ethyl acetate extract followed by purification of different fractions led to the isolation of seven compounds (1 - 6, 9). Esterification reaction of compound 6 was carried out using butyroyl chlorides and triethylamin to produce two derivatives (7 - 8). The cytotoxic activity was performed after staining of treated cells with florescent dye propidium iodide. Dead cells were detected using cytometer FL2 or FL3 channels/filters.
Trans-derivative of narciclasine (a natural isolate from ), was found to be most potent among all tested compounds. Its effects were more significant on low malignant follicular lymphoma (DoHH2 cells) as compared to highly malignant (EBV infected) Burkitts lymphoma (Raji cells).
From our results, narciclasine appears to hold the potential of a lead molecule that can be used to bridge the therapeutic gaps in cancer research.
文献中充分论证了 的生物学意义。在喀麦隆，该科植物常用于治疗肝脏、癌症和心血管疾病。迄今为止，尚无针对 提取物和分离化合物的抗癌活性的科学研究。
目前的研究集中于阐述从 中提取的天然分离物（化合物 1-6、9）和半合成类似物（化合物 7-8）的抗增殖作用。
用乙酸乙酯提取物进行柱层析，然后对不同馏分进行纯化，得到 7 种化合物（1-6、9）。用丁酸酰氯和三乙胺对化合物 6 进行酯化反应，生成两种衍生物（7-8）。用荧光染料碘化丙啶对处理过的细胞进行染色，然后进行细胞毒性活性测定。用细胞仪 FL2 或 FL3 通道/滤波器检测死亡细胞。
纳曲色林（一种来源于 的天然分离物）的反式衍生物在所有测试化合物中最为有效。与高度恶性（EBV 感染）伯基特淋巴瘤（Raji 细胞）相比，其对低恶性滤泡性淋巴瘤（DoHH2 细胞）的作用更为显著。
根据我们的结果，纳曲色林似乎具有成为一种潜在的先导分子的潜力，可用于弥合癌症研究中的治疗空白。
