Xu Feng-Yuan, Shang Wen-Qing, Yu Jia-Jun, Sun Qian, Li Ming-Qing, Sun Jian-Song
National Engineering Research Center of Chemical Synthesis of Monosaccharide, Jiangxi Normal UniversityNanchang, Jiangxi Province 330027, People's Republic of China; Department of Chemistry, High School Affiliated to Shanghai Jiaotong UniversityShanghai 200493, People's Republic of China.
Laboratory for Reproductive Immunology, Hospital of Obstetrics and Gynecology, Fudan University Shanghai Medical College Shanghai 200011, People's Republic of China.
Am J Transl Res. 2016 Apr 15;8(4):1708-18. eCollection 2016.
Ginseng and its components exert various biological effects, including antioxidant, anti-carcinogenic, anti-mutagenic, and antitumor activity. Ginsenosides are the main biological components of ginseng. Protopanaxadiol (PPD) and protopanaxatriol (PPT) are two metabolites of ginsenosides. However, the difference between these compounds in anti-lung cancer is unclear. The present study aimed to evaluate the antitumor activity of PPD, PPT, Ginsenosides-Rg3 (G-Rg3) and Ginsenosides-Rh2 (G-Rh2) in lung cancer cell. After treatment with cisplatin, PPD, PPT, G-Rg3 or G-Rh2, the viability, apoptosis level and invasiveness of lung cell lines (A549 cell, a lung adenocarcinoma cell line and SK-MES-1 cell, a lung squamous cell line) in vitro were analyzed by Cell Counting Kit-8 (CCK8), Annexin V/PI apoptosis and Matrigel invasion assays, respectively. Here we found that all these compounds led to significant decreases of viability and invasiveness and an obvious increase of apoptosis of A549 and SK-MES-1 cells. Among these, the viability of SK-MES-1 cell treated with PPT was decreased to 66.8%, and this effect was closest to Cisplatin. G-Rg3 had the highest stimulatory effect on apoptosis, and PTT had the highest inhibitory effect on cell invasiveness in A549 and SK-MES-1 cells. These results indicate that both ginsenosides and two metabolites have antitumor activity on lung cancer cell in vitro. However, PPT is more powerful for inhibiting the viability and invasiveness of lung cancer cell, especially lung squamous cell. G-Rg3 has the best pro-apoptosis effects. This study provides a scientific basis for potential therapeutic strategies targeted to lung cancer by further structure modification.
人参及其成分具有多种生物学效应，包括抗氧化、抗癌、抗诱变和抗肿瘤活性。人参皂苷是人参的主要生物成分。原人参二醇（PPD）和原人参三醇（PPT）是人参皂苷的两种代谢产物。然而，这些化合物在抗肺癌方面的差异尚不清楚。本研究旨在评估PPD、PPT、人参皂苷-Rg3（G-Rg3）和人参皂苷-Rh2（G-Rh2）对肺癌细胞的抗肿瘤活性。在用顺铂、PPD、PPT、G-Rg3或G-Rh2处理后，分别通过细胞计数试剂盒-8（CCK8）、膜联蛋白V/PI凋亡检测和基质胶侵袭实验分析了肺癌细胞系（A549细胞，一种肺腺癌细胞系；SK-MES-1细胞，一种肺鳞癌细胞系）在体外的活力、凋亡水平和侵袭能力。在此我们发现，所有这些化合物均导致A549和SK-MES-1细胞的活力和侵袭能力显著降低，凋亡明显增加。其中，用PPT处理的SK-MES-1细胞的活力降至66.8%，且这种效果最接近顺铂。G-Rg3对凋亡的刺激作用最强，而PTT对A549和SK-MES-1细胞的侵袭能力抑制作用最强。这些结果表明，人参皂苷及其两种代谢产物在体外对肺癌细胞均具有抗肿瘤活性。然而，PPT在抑制肺癌细胞尤其是肺鳞癌细胞的活力和侵袭能力方面更强。G-Rg3具有最佳的促凋亡作用。本研究为通过进一步的结构修饰针对肺癌的潜在治疗策略提供了科学依据。
