Ruphin Fatiany Pierre, Baholy Robijaona, Emmanue Andrianarivo, Amelie Raharisololalao, Martin Marie-Therese, Koto-te-Nyiwa Ngbolua
Department of Organic Chemistry, Faculty of Sciences, P.O. Box 187, University of Toliara, 601 Toliara Madagascar; Malagasy Institute of Applied Research, Avarabohitra Itaosy lot AVB 77, P. O. BOX 3833, 102 Antananarivo Madagascar.
Asian Pac J Trop Biomed. 2013 Oct;3(10):780-4. doi: 10.1016/S2221-1691(13)60155-0. Epub 2013 Sep 4.
To validate scientifically the traditional use of Salacia leptoclada Tul. (Celastraceae) (S. leptoclada) and to isolate and elucidate the structure of the biologically active compound.
Bioassay-guided fractionation of the acetonic extract of the stem barks of S. leptoclada was carried out by a combination of chromatography technique and biological experiments in viro using Plasmodium falciparum and P388 leukemia cell lines as models. The structure of the biologically active pure compound was elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.
Biological screening of S. leptoclada extracts resulted in the isolation of a pentacyclic triterpenic quinone methide. The pure compound exhibited both in vitro a cytotoxic effect on murine P388 leukemia cells with IC50 value of (0.041±0.020) μg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC50 value of (0.052±0.030) μg/mL. Despite this interesting anti-malarial property of the lead compound, the therapeutic index was weak (0.788). In the best of our knowledge, the quinone methide pentacyclic triterpenoid derivative compound is reported for the first time in S. leptoclada.
The results suggest that furthers studies involving antineoplastic activity is needed for the development of this lead compound as anticancer drug.
科学验证薄叶五层龙（Salacia leptoclada Tul.，卫矛科）的传统药用价值，并分离鉴定其生物活性化合物的结构。
采用色谱技术与体外生物学实验相结合的方法，以恶性疟原虫和P388白血病细胞系为模型，对薄叶五层龙茎皮的丙酮提取物进行生物活性导向分离。通过一维和二维核磁共振光谱及质谱对生物活性纯化合物的结构进行鉴定。
对薄叶五层龙提取物进行生物活性筛选，分离得到一种五环三萜醌甲基化物。该纯化合物在体外对小鼠P388白血病细胞具有细胞毒性作用，IC50值为(0.041±0.020) μg/mL，对恶性疟原虫氯喹耐药株FC29具有抗疟活性，IC50值为(0.052±0.030) μg/mL。尽管该先导化合物具有有趣的抗疟特性，但其治疗指数较低（0.788）。据我们所知，五环三萜醌甲基化物衍生物化合物首次在薄叶五层龙中被报道。
结果表明，为了将该先导化合物开发为抗癌药物，需要进一步开展有关抗肿瘤活性的研究。
