Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Council of Scientific and Industrial Research, Jammu, Jammu and Kashmir, India ; Department of Pharmacology, Therapeutics and Toxicology, Faculty of Basic Medical Sciences, College of Medicine, University of Lagos, Lagos, Nigeria.
Cancer Pharmacology Division, Indian Institute of Integrative Medicine, Council of Scientific and Industrial Research, Jammu, Jammu and Kashmir, India.
J Tradit Complement Med. 2014 Dec 18;5(1):35-41. doi: 10.1016/j.jtcme.2014.05.001. eCollection 2015 Jan.
Cancer is a leading cause of death worldwide and sustained focus is on the discovery and development of newer and better tolerated anticancer drugs especially from plants. The sulforhodamine B (SRB) in vitro cytotoxicity assay, sarcoma-180 (S-180) ascites and solid tumor, and L1210 lymphoid leukemia in vivo models were used to investigate the anticancer activity of root extracts of Aristolochia ringens Vahl. (Aristolochiaceae; mǎ dōu líng). AR-A001 (IC50 values of 20 μg/mL, 22 μg/mL, 3 μg/mL, and 24 μg/mL for A549, HCT-116, PC3, and THP-1 cell lines, respectively), and AR-A004 (IC50 values of 26 μg/mL, 19.5 μg/mL, 12 μg/mL, 28 μg/mL, 30 μg/mL, and 22 μg/mL for A549, HCT-116, PC3, A431, HeLa, and THP-1, respectively), were observed to be significantly active in vitro. Potency was highest with AR-A001 and AR-A004 for PC3 with IC50 values of 3 μg/mL and 12 μg/mL, respectively. AR-A001 and AR-A004 produced significant (p < 0.05-0.001) dose-dependent inhibition of tumor growth in the S-180 ascites model with peak effects produced at the highest dose of 120 mg/kg. Inhibition values were 79.51% and 89.98% for AR-A001 and AR-A004, respectively. In the S-180 solid tumor model, the inhibition of tumor growth was 29.45% and 50.50% for AR-A001 (120 mg/kg) and AR-A004 (110 mg/kg), respectively, compared to 50.18% for 5-fluorouracil (5-FU; 20 mg/kg). AR-A001 and AR-A004 were also significantly active in the leukemia model with 211.11% and 155.56% increase in mean survival time (MST) compared to a value of 211.11% for 5-FU. In conclusion, the ethanolic (AR-A001) and dichloromethane:methanol (AR-A004) root extracts of AR possess significant anticancer activities in vitro and in vivo.
癌症是全球主要的死亡原因，人们一直专注于发现和开发新型、耐受性更好的抗癌药物，尤其是来自植物的药物。采用磺酰罗丹明 B（SRB）体外细胞毒性测定、肉瘤 180（S-180）腹水和实体瘤以及 L1210 淋巴白血病体内模型，研究了马兜铃 ringens Vahl 的根提取物（马兜铃科；马兜铃）的抗癌活性。AR-A001（对 A549、HCT-116、PC3 和 THP-1 细胞系的 IC50 值分别为 20μg/mL、22μg/mL、3μg/mL 和 24μg/mL）和 AR-A004（对 A549、HCT-116、PC3、A431、HeLa 和 THP-1 的 IC50 值分别为 26μg/mL、19.5μg/mL、12μg/mL、28μg/mL、30μg/mL 和 22μg/mL）在体外表现出显著的活性。AR-A001 和 AR-A004 对 PC3 的活性最高，IC50 值分别为 3μg/mL 和 12μg/mL。AR-A001 和 AR-A004 在 S-180 腹水模型中产生显著（p<0.05-0.001）的剂量依赖性肿瘤生长抑制作用，最高剂量为 120mg/kg 时达到峰值效应。AR-A001 和 AR-A004 的抑制值分别为 79.51%和 89.98%。在 S-180 实体瘤模型中，AR-A001（120mg/kg）和 AR-A004（110mg/kg）对肿瘤生长的抑制作用分别为 29.45%和 50.50%，而 5-氟尿嘧啶（5-FU；20mg/kg）的抑制作用为 50.18%。AR-A001 和 AR-A004 在白血病模型中也具有显著的活性，与 5-FU 的 211.11%相比，平均生存时间（MST）分别增加了 211.11%和 155.56%。综上所述，AR 的乙醇（AR-A001）和二氯甲烷：甲醇（AR-A004）根提取物在体外和体内均具有显著的抗癌活性。
