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Open AccessArticle

Experimental Evaluation of Anticancer Efficiency and Acute Toxicity of Anthrafuran for Oral Administration

1
Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Russia
2
Federal State Budgetary Institution «National Medical Research Center of Oncology of N.N.Blokhin», Ministry of Health of Russia, 24 Kashirskoye sh., Moscow 115548, Russia
*
Author to whom correspondence should be addressed.
We dedicate this work to the memory of corresponding Member of RAS professor Alexander A. Firsov, the eminent scholar in pharmacology and pharmacokinetic, scientific director of Gause Institute of New Antibiotics.
Pharmaceuticals 2020, 13(5), 81; https://doi.org/10.3390/ph13050081
Received: 19 February 2020 / Revised: 21 April 2020 / Accepted: 26 April 2020 / Published: 28 April 2020
(This article belongs to the Section Pharmacology)
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. View Full-Text
Keywords: anthrafuran; antitumor activity; oral administration; acute toxicity; LD50 anthrafuran; antitumor activity; oral administration; acute toxicity; LD50
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MDPI and ACS Style

Shchekotikhin, A.E.; Treshalina, H.M.; Treshchalin, M.I.; Pereverzeva, E.R.; Isakova, H.B.; Tikhomirov, A.S. Experimental Evaluation of Anticancer Efficiency and Acute Toxicity of Anthrafuran for Oral Administration. Pharmaceuticals 2020, 13, 81.

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