Abstract

Three novel 14-membered cyclopeptide alkaloids, justicianenes B-D (1-3), were isolated from the EtOH extract of the whole plant of Justicia procumbens L., and their structures were determined on the basis of detailed NMR spectroscopic data and the absolute stereochemistry of the ring-bonded α-amino acids in the cyclopeptide alkaloids were determined by ECD spectra. The isolated compounds were evaluated for their in vitro cytotoxicity against human cancer cell lines, including brest cancer MCF-7, cervix carcinoma HeLa, lung cancer A549 and H460, and diphyllin (14) showed moderate cytotoxicity against the HeLa, A549 and H460 cells with IC₅₀ of 9.13, 23.12, 42.34 µM, respectively, justicianene D showed weak cytotoxicity against the MCF-7 cell with inhibition rate of 50% at the concentration of 90 µM.

摘要

从Justicia procumbens L.全草的EtOH提取物中分离出三种新型14元环肽生物碱justicianenes BD ( 1 - 3 )，并根据详细的NMR光谱数据和绝对立体化学确定了它们的结构。通过ECD光谱测定环肽生物碱中的环状α-氨基酸。评估了分离的化合物对人类癌细胞系（包括乳腺癌 MCF-7、宫颈癌 HeLa、肺癌 A549 和 H460）的体外细胞毒性，并且 diphyllin ( 14 ) 对 HeLa、A549 和 H460 细胞具有中等的细胞毒性集成电路₅₀分别为 9.13、23.12、42.34 µM，justicianene D 对 MCF-7 细胞表现出较弱的细胞毒性，在 90 µM 浓度下抑制率为 50%。

抽象的

从Justicia procumbens L.全草的EtOH提取物中分离出三种新型14元环肽生物碱justicianenes BD ( 1 - 3 )，并根据详细的NMR光谱数据和绝对立体化学确定了它们的结构。通过ECD光谱测定环肽生物碱中的环状α-氨基酸。评估了分离的化合物对人类癌细胞系（包括乳腺癌 MCF-7、宫颈癌 HeLa、肺癌 A549 和 H460）的体外细胞毒性，并且 diphyllin ( 14 ) 对 HeLa、A549 和 H460 细胞具有中等的细胞毒性集成电路₅₀分别为 9.13、23.12、42.34 µM，justicianene D 对 MCF-7 细胞表现出较弱的细胞毒性，在 90 µM 浓度下抑制率为 50%。