Luo Yanping, Yu Hongjuan, Yang Yunshang, Tian Weihua, Dong Kaizhong, Shan Jinyu, Ma Xingming
a Department of Immunology , School of Basic Medical Sciences, Lanzhou University , Lanzhou , China .
b Institute of Organic and Medicinal Chemistry, School of Petrochemical Engineering, Lanzhou University of Technology , Lanzhou , China .
Pharm Biol. 2016 Jul;54(7):1133-9. doi: 10.3109/13880209.2015.1055634. Epub 2015 Oct 1.
Gastric cancer remains highly prevalent, but treatment options are limited. Natural products have proved to be a rich source of anticancer drugs. Chrysosplenium nudicaule Ledeb. (Saxifragaceae) is a perennial herb that grows in the highlands of China. It has been used as a traditional Chinese medicine to treat digestive diseases for hundreds of years. Recent studies revealed that this herb had anticancer activity, and the flavonoids were speculated to be the effective components. 6,7,3'-Trimethoxy-3,5,4'-trihydroxy flavone (TTF) and 5,4'-dihydroxy-3,6,3'trimethoxy-flavone-7-O-β-d-glucoside (DTFG) are flavonoid compounds isolated from Chrysosplenium nudicaule.
This study examined the effect of TTF and DTFG on SGC-7901 human stomach cancer cell in vitro to determine the anticancer and induction of apoptosis properties of TTF.
The proliferation of cells treated with 32, 16, 8, 4, and 2 μg/mL of TTF or DTFG for 24, 48, and 72 h was assessed by the MTT assay. After being treated with TTF, the apoptosis of SGC-7901 cells was assessed by acridine orange staining, ultrastructure, electrophoresis of DNA fragmentation, and flow cytometry.
Results indicated that TTF inhibited the growth of cancer cells with an IC50 value of 8.33 μg/mL after 72 h incubation. However, DTFG showed no inhibitory effect on the growth of the cancer cell. Further studies on TTF also confirmed that it was able to induce apoptosis of SGC-7901 cells at a concentration as low as 4 μg/mL.
The apoptotic effect of TTF makes it a promising candidate for future chemotherapeutic application in treating stomach cancer.
胃癌仍然非常普遍,但治疗选择有限。天然产物已被证明是抗癌药物的丰富来源。裸茎金腰子(虎耳草科)是一种生长在中国高地的多年生草本植物。数百年来,它一直被用作治疗消化系统疾病的传统中药。最近的研究表明,这种草药具有抗癌活性,推测黄酮类化合物是其有效成分。6,7,3'-三甲氧基-3,5,4'-三羟基黄酮(TTF)和5,4'-二羟基-3,6,3'-三甲氧基黄酮-7-O-β-D-葡萄糖苷(DTFG)是从裸茎金腰子中分离出的黄酮类化合物。
本研究检测TTF和DTFG对SGC-7901人胃癌细胞的体外作用,以确定TTF的抗癌和诱导凋亡特性。
用32、16、8、4和2μg/mL的TTF或DTFG处理细胞24、48和72小时后,通过MTT法评估细胞增殖。用TTF处理后,通过吖啶橙染色、超微结构、DNA片段电泳和流式细胞术评估SGC-7901细胞的凋亡情况。
结果表明,孵育72小时后,TTF抑制癌细胞生长,IC50值为8.33μg/mL。然而,DTFG对癌细胞生长没有抑制作用。对TTF的进一步研究还证实,它能够在低至4μg/mL的浓度下诱导SGC-7901细胞凋亡。
TTF的凋亡作用使其成为未来胃癌化疗应用的有希望的候选药物。