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Published on: March 20, 2018
Anticancer activity of Aristolochia ringens Vahl. (Aristolochiaceae)
Abidemi James Akindele1, Zahoor Wani2, Girish Mahajan2
1Cancer 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.
Abstract:
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.
Insights
Plant-derived Aristolochia ringens root extracts show significant anticancer potential. AR-A001 and AR-A004 demonstrated potent activity against various cancer cell lines and tumor models, offering new avenues for cancer drug development.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Oncology
Background:
- Cancer remains a major global health challenge, driving the search for novel, well-tolerated anticancer agents.
- Plant-derived compounds are a promising source for discovering new anticancer drugs.
- Aristolochia ringens Vahl. (Aristolochiaceae) is a plant traditionally used, prompting investigation into its medicinal properties.
Purpose of the Study:
- To evaluate the anticancer activity of Aristolochia ringens root extracts.
- To assess the efficacy of specific extracts (AR-A001 and AR-A004) in vitro and in vivo cancer models.
Main Methods:
- In vitro cytotoxicity was assessed using the sulforhodamine B (SRB) assay against multiple human cancer cell lines (A549, HCT-116, PC3, THP-1, A431, HeLa).
- In vivo anticancer activity was investigated using sarcoma-180 (S-180) ascites and solid tumor models, and the L1210 lymphoid leukemia model.
- Standard chemotherapy drug 5-fluorouracil (5-FU) was used as a positive control for in vivo studies.
Main Results:
- AR-A001 and AR-A004 exhibited significant in vitro anticancer activity, with notable potency against PC3 cells (IC50 values of 3 µg/mL and 12 µg/mL, respectively).
- Both extracts demonstrated significant dose-dependent inhibition of tumor growth in the S-180 ascites model (79.51% for AR-A001, 89.98% for AR-A004 at 120 mg/kg).
- In vivo studies showed substantial tumor growth inhibition in the S-180 solid tumor model and significant increases in mean survival time (MST) in the leukemia model, comparable to 5-FU.
Conclusions:
- The ethanolic (AR-A001) and dichloromethane:methanol (AR-A004) root extracts of Aristolochia ringens possess significant anticancer properties.
- These findings support the potential of Aristolochia ringens root extracts as a source for developing novel anticancer therapeutics.
- Further research into the active compounds and mechanisms of action is warranted.
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