Shi Li-Shian, Kuo Sheng-Chu, Sun Han-Dong, Morris-Natschke Susan L, Lee Kuo-Hsiung, Wu Tian-Shung
Department of Biotechnology, National Formosa University, Yunlin 632, Taiwan; Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan.
Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung 401, Taiwan.
Bioorg Med Chem. 2014 Mar 15;22(6):1889-98. doi: 10.1016/j.bmc.2014.01.052. Epub 2014 Feb 6.
Eight new cardiac glycosides/aglycones (antiaritoxiosides A-G, 1-7, and antiarotoxinin B, 8), two new coumarins (anticarins A-B, 41-42), and two new flavanones (antiarones L-K, 43-44) were isolated from trunk bark of Antiaris toxicaria together with 53 known compounds. The new structures were established by extensive analysis of spectroscopic data. Compound 1 (10-carboxy and 3α-hydroxy) and compounds 3-6 (10-hydroxy) contain unique substituents that are rarely found in cardiac glycosides. The cytotoxic effects of isolated compounds against ten human cancer cell lines, KB, KB-VIN, A549, MCF-7, U-87-MG, PC-3, 1A9, CAKI-1, HCT-9 and S-KMEL-2, were tested using the sulforhodamine B assay. Five compounds (12, 16, 20, 22, and 31) showed significant cytotoxicity against all ten cancer cell lines, with notable potency at the ng/mL level against some cell lines, which merits further development as clinical trial candidates.
从见血封喉的树干树皮中分离出8种新的强心苷/苷元（抗箭毒苷A - G、1 - 7和抗箭毒宁B、8）、2种新的香豆素（抗香豆素A - B、41 - 42）和2种新的黄烷酮（抗黄酮L - K、43 - 44），以及53种已知化合物。通过对光谱数据的广泛分析确定了新结构。化合物1（10 - 羧基和3α - 羟基）以及化合物3 - 6（10 - 羟基）含有强心苷中罕见的独特取代基。使用磺酰罗丹明B测定法测试了分离出的化合物对10种人类癌细胞系KB、KB - VIN、A549、MCF - 7、U - 87 - MG、PC - 3、1A9、CAKI - 1、HCT - 9和S - KMEL - 2的细胞毒性作用。5种化合物（12、16、20、22和31）对所有10种癌细胞系均显示出显著的细胞毒性，对某些细胞系在纳克/毫升水平具有显著效力，作为临床试验候选药物值得进一步开发。
