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Chemical Compound Review

Perazolin     [4-[2-[4-(2- methylpropoxycarbonyloxymethyl ...

Synonyms: Sobuzoxano, sobuzoxane, Sobuzoxanum, MST-16, Lopac-S-4692, ...
 
 
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Disease relevance of Perazolin

  • METHODS: As part of a multi-institutional cooperative study, we conducted a study of MST-16 in 27 patients with NHL who were assessable for drug efficacy and toxicity [1].
  • However, when combined with an oral dose of MST-16, DOX-induced body weight loss and diarrhea were significantly ameliorated, and an additive tumor growth delay (8.7 days) was obtained [2].
  • The effects of MST-16, a new antitumor agent derived from bis (2, 6-dioxopiperazine), on cell growth, cell-cycle progression and DNA synthesis, alone and in combination with other antitumor agents, were investigated in murine leukemia L1210 cells in vitro [3].
  • Six patients with ATLL were treated with a new antitumor agent, MST-16, which is a derivative of bis(2,6-dioxopiperazine) [4].
  • Effective treatment of adult T cell leukemia/lymphoma with a novel oral antitumor agent, MST-16 [4].
 

Psychiatry related information on Perazolin

  • The critical period for testicular degeneration was identified to be day 13 and 14 of gestation by single administration experiments and single treatment with 15.6 to 250 mg/kg of sobuzoxane on day 14 of gestation gave a dose-dependent incidence of the tests abnormality [5].
 

High impact information on Perazolin

  • PURPOSE: The present late phase II study was conducted to evaluate the clinical efficacy and toxicity of MST-16 in non-Hodgkin's lymphoma (NHL) [1].
  • The LD50 of DOX administered i.p. to control female BALB/c mice increased more than 1.5-fold when combined with MST-16 [2].
  • RESULTS: Guinea pig corneas protected from desiccation by persistent tarsorrhaphy survived indefinitely in the eyes of C.B-17SCID mice but were rejected acutely (but not hyperacutely) in eyes of normal BALB/c and C57BL/6 mice (median survival times, MST, 16 and 10 days, respectively) [6].
  • The addition of MST-16 followed by VCR was more effective than simultaneous addition of the 2 drugs on inhibition of cell growth [3].
  • Arrest in late G2 or prophase of cell cycle induced by 4,4-(1,2-ethanediyl) bis (1-isobutoxycarbonyloxymethyl 2, 6-piperazinedione) (MST-16) in cultured L1210 cells [3].
 

Chemical compound and disease context of Perazolin

 

Biological context of Perazolin

  • We studied bioavailability, treatment schedule dependence, and therapeutic efficacy of orally administered MST-16, a novel derivative of bis(2,6-dioxopiperazine), against murine tumors and human tumor xenografts [8].
  • Pregnant rats were orally administered sobuzoxane (an antitumor drug) during various days of gestation and the testicular development of their offspring was examined histopathologically on day 21 after birth [5].
  • These results suggest that good antitumor activity of combined treatment with MST-16 and MGBCP resulted from the diminution of DNA condensation and cellular proliferation caused by inhibition of topoisomerase II with MST-16 and by polyamine depletion with MGBCP [9].
  • The combined treatment of human Molt 4B lymphoid cells with MST-16 and MGBCP resulted in greater suppressions of cellular polyamine and protein biosyntheses and decrease of cell number than in the cells treated with either drug alone [9].
  • These results suggest that the testis abnormality in offspring from dams treated with sobuzoxane is due to inhibition of the proliferation of primordial germ cells during testis organogenesis [5].
 

Anatomical context of Perazolin

  • Antiproliferative effects of 1,1'-ethylenedi-4-isobutoxy-carbonyloxymethyl-3,5-d iox opiperazine (MST-16), an inhibitor of topoisomerase II, in combination with methylglyoxal bis (cyclopentylamidinohydrazone) (MGBCP), an inhibitor for polyamine biosynthetic enzymes, were investigated using cultured human lymphoid cells and leukemic mice [9].
  • When 15.6 to 250 mg/kg of sobuzoxane was given every day from day 7 to 17 of gestation, seminiferous tubules devoid of spermatogonia and/or spermatocytes were found in a dose related manner [5].
  • Our results show that Pro was cytotoxic to human tumor cell lines in vitro (IC50 < 50 microM for 48 h), approximately 3 to 20-fold more than MST-16 [10].
 

Associations of Perazolin with other chemical compounds

  • We thus conclude that the administration of ADM, THP and ME combined with MST-16 is synergistic and that the mechanism may not include an increase in the intracellular drug uptake but rather an increase in G2M accumulation [11].
  • Adriamycin (ADM), therarubicin (THP) and ME2303 (ME) showed synergistic cytotoxicity against colon 26 cells, when combined with MST-16 [11].
  • Pro and MST-16 manifested more prolonged cytotoxicity than some other first-line anticancer drugs including 5-fluorouacil, vincristine and doxorubicin, and maintain their cytotoxic effects for 4 days in vitro [10].
  • These findings suggest that Pro is active against more categories of tumors both in vivo and in vitro, which in some circumstances may make it superior to the currently-used anticancer bisdioxopiperazines, including razoxane and MST-16 [10].
 

Gene context of Perazolin

 

Analytical, diagnostic and therapeutic context of Perazolin

  • These results indicate that MST-16 may be effective chemotherapy for cancer patients when combined with DOX [2].
  • To elucidate the mechanism of synergy between these anthracyclines and MST-16, the concentration of anthracyclines in the treated cells was measured by flow cytometry [11].
  • Therapeutic efficacy of MST-16 was heavily dependent on the treatment schedule: 9 daily oral administrations and treatment every 4 h on day 1 only were much more effective against s.c.-implanted L1210 leukemia than a single dose or five daily administrations giving the same total dose [8].
  • After approximately 1 year of intermittent multiagent salvage therapy for pericardial recurrences, a treatment that resulted in a partial response, 3 cycles of monotherapy with sobuzoxane were administered [13].

References

  1. Phase II study: treatment of non-Hodgkin's lymphoma with an oral antitumor derivative of bis(2,6-dioxopiperazine). Ohno, R., Yamada, K., Hirano, M., Shirakawa, S., Tanaka, M., Oguri, T., Kodera, Y., Mitomo, Y., Ikeda, Y., Yokomaku, S. J. Natl. Cancer Inst. (1992) [Pubmed]
  2. MST-16, a novel bis-dioxopiperazine anticancer agent, ameliorates doxorubicin-induced acute toxicity while maintaining antitumor efficacy. Yoshida, M., Maehara, Y., Sugimachi, K. Clin. Cancer Res. (1999) [Pubmed]
  3. Arrest in late G2 or prophase of cell cycle induced by 4,4-(1,2-ethanediyl) bis (1-isobutoxycarbonyloxymethyl 2, 6-piperazinedione) (MST-16) in cultured L1210 cells. Liu, Y.P., Araya, S., Nakamura, T. Int. J. Cancer (1992) [Pubmed]
  4. Effective treatment of adult T cell leukemia/lymphoma with a novel oral antitumor agent, MST-16. Ichihashi, T., Kiyoi, H., Fukutani, H., Kubo, K., Yamauchi, T., Naoe, T., Yamada, K., Ohno, R. Oncology (1992) [Pubmed]
  5. Testicular degeneration induced in rat offspring by maternal treatment with sobuzoxane. Kato, I., Nobuhara, A., Wakasugi, N. Reprod. Toxicol. (1996) [Pubmed]
  6. Xenoreactive CD4+ T cells and acute rejection of orthotopic guinea pig corneas in mice. Tanaka, K., Yamada, J., Streilein, J.W. Invest. Ophthalmol. Vis. Sci. (2000) [Pubmed]
  7. Anti-proliferative effects, cell cycle G2/M phase arrest and blocking of chromosome segregation by probimane and MST-16 in human tumor cell lines. Lu, d.a. .Y., Huang, M., Xu, C.H., Yang, W.Y., Hu, C.X., Lin, L.P., Tong, L.J., Li, M.H., Lu, W., Zhang, X.W., Ding, J. BMC Pharmacol. (2005) [Pubmed]
  8. Antitumor activities and schedule dependence of orally administered MST-16, a novel derivative of bis(2,6-dioxopiperazine). Narita, T., Koide, Y., Yaguchi, S., Kimura, S., Izumisawa, Y., Takase, M., Inaba, M., Tsukagoshi, S. Cancer Chemother. Pharmacol. (1991) [Pubmed]
  9. Dioxopiperazine derivative potentiates antitumor effect of methylglyoxal bis(cyclopentylamidinohydrazone) on human and mouse leukemia cells. Hibasami, H., Tsukada, T., Shirakawa, S., Narita, T., Inagaki, M., Nakashima, K. Anticancer Res. (1994) [Pubmed]
  10. Medicinal chemistry of probimane and MST-16: comparison of anticancer effects between bisdioxopiperazines. Lu, D.Y., Huang, M., Xu, C.H., Zhu, H., Xu, B., Ding, J. Medicinal chemistry (Sh⁻ariqah, United Arab Emirates) (2006) [Pubmed]
  11. MST-16, a novel derivative of bis(2,6-dioxopiperazine), synergistically enhances the antitumor effects of anthracyclines. Inutsuka, S., Baba, H., Maehara, Y., Sugimachi, K. Cancer Chemother. Pharmacol. (1998) [Pubmed]
  12. Secondary acute promyelocytic leukemia in a patient with non-Hodgkin's lymphoma treated with VP-16 and MST-16. Okamoto, T., Okada, M., Wakae, T., Mori, A., Takatsuka, H., Kakishita, E. Int. J. Hematol. (2002) [Pubmed]
  13. Durable remission by sobuzoxane in an HIV-seronegative patient with human herpesvirus 8-negative primary effusion lymphoma. Inoue, Y., Tsukasaki, K., Nagai, K., Soda, H., Tomonaga, M. Int. J. Hematol. (2004) [Pubmed]
 
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