Related Experiment Video
Updated: Dec 22, 2025
Evaluation of the In vivo Antitumor Activity of Polyanhydride IL-1α Nanoparticles
Published on: June 28, 2021
Experimental Evaluation of Anticancer Efficiency and Acute Toxicity of Anthrafuran for Oral Administration
Andrey E Shchekotikhin1, Helen M Treshalina2, Michael I Treshchalin1
1Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Russia.
Abstract:
The new antitumor agent anthrafuran has demonstrated a consistent effect in murine tumor models when administered parenterally due to the simultaneous inhibition of multiple cellular targets such as topoisomerases I/II and protein kinases. In this study, we assessed the anticancer efficiency and acute toxicity of anthrafuran administered orally. The action of anthrafuran was studied on transplanted tumor models which included P388 leukemia, Ca755 mammary adenocarcinoma, LLC lung carcinoma, and T47D human breast cancer xenografts on Balb/c nude mice. A significant antitumor efficacy of oral anthrafuran was revealed for all tested tumor models as follows: T/Cmax = 219% for P388, TGImax = 91% for Ca755, TGImax = 84% with CRmax = 54% for LLC, and T/C = 38% for T47D. The optimal treatment schedule of orally administered anthrafuran was 70-100 mg/kg given daily for five days. The LD50 value of orally administered anthrafuran (306.7 mg/kg) in mice was six times higher than that for i.p. administration (52.5 mg/kg). The rates of antitumor efficacy and acute toxicity indicate the high potential for further research on anthrafuran as a new original oral anticancer multitarget agent with an expected satisfactory tolerability and bioavailability.
Insights
Anthrafuran shows significant antitumor effects against various cancers when taken orally. This new oral anticancer drug has a high safety profile, making it a promising candidate for further research.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Anthrafuran is a novel antitumor agent effective in murine models via parenteral administration.
- Its mechanism involves simultaneous inhibition of topoisomerases I/II and protein kinases.
Purpose of the Study:
- To evaluate the anticancer efficacy and acute toxicity of orally administered anthrafuran.
- To assess anthrafuran's potential as an oral anticancer agent.
Main Methods:
- Tested anthrafuran on transplanted tumor models: P388 leukemia, Ca755 mammary adenocarcinoma, LLC lung carcinoma, and T47D human breast cancer xenografts.
- Determined optimal oral dosage and treatment schedule.
- Assessed acute toxicity via LD50 determination for oral and intraperitoneal administration.
Main Results:
- Significant antitumor efficacy observed across all tested models (P388, Ca755, LLC, T47D).
- Optimal oral dosage: 70-100 mg/kg daily for five days.
- Oral LD50 (306.7 mg/kg) was six times higher than intraperitoneal LD50 (52.5 mg/kg), indicating improved safety.
Conclusions:
- Oral anthrafuran demonstrates potent antitumor activity and favorable acute toxicity.
- Anthrafuran is a promising multitarget oral anticancer agent with potential for satisfactory tolerability and bioavailability.
