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  4. Trypaflavin

Trypaflavin is an acridine compound and antimalarial agent. Trypaflavin invades germ cells. Trypaflavin induces aberrations in unfertilized oocytes. Trypaflavin increases the frequency of chromosomal aberrations. Trypaflavin shows weak mutagenicity. Trypaflavin is highly toxic to Leishmania, causing immediate lysis of the leptomonads.

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Trypaflavin

Trypaflavin Chemical Structure

CAS No. : 86-40-8

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Description

Trypaflavin is an acridine compound and antimalarial agent. Trypaflavin invades germ cells. Trypaflavin induces aberrations in unfertilized oocytes. Trypaflavin increases the frequency of chromosomal aberrations. Trypaflavin shows weak mutagenicity. Trypaflavin is highly toxic to Leishmania, causing immediate lysis of the leptomonads[1][2].

IC50 & Target[2]

Leishmania

 

In Vivo

Trypaflavin (50 mg/kg; p.o.; single acute dose; day 7 post conception) induces dominant lethal mutations in F1 female offspring of pregnant C3H mice, with an induced mutation frequency of 13.25[1].
Trypaflavin (2 mg/kg/day; p.o.; 50 days) slightly elevates preimplantation egg loss and dead implants without inducing significant dominant lethal mutations in female C3H mice, and weakly increases total chromosome aberration frequencies to 21.1% in metaphase-II oocytes of female NMRI mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C3H (female; parental generation; pregnant; prenatal in utero treatment to target oogonia/early meiotic oocyte stages); C3H F1 (female; 10 weeks old at mating)
Dosage: 50 mg/kg
Administration: p.o.; single acute dose; day 7, 11, 14, or 15 post conception
Result: Induced significant mutagenic effects only with day 7 post conception treatment:
Increased preimplantation egg loss to 24.9%.
Increased dead implants per female to 1.4.
Decreased living embryos per female to 7.2.
Induced dominant lethal mutations of 13.25.
Showed no significant effects with treatment on days 11, 14, or 15 post conception.
Animal Model: C3H (female; 3 weeks old at study start)
Dosage: 2 mg/kg/day
Administration: p.o.; daily; 50 days
Result: Increased preimplantation egg loss to 13.3%.
Increased dead implants per female to 2.2.
Induced dominant lethal mutations of -1.27.
Animal Model: NMRI (female; 3 weeks old at study start)
Dosage: 2 mg/kg/day
Administration: p.o.; daily; at least 50 days
Result: Increased the frequency of aberrant metaphase-II oocytes to 21.1%, aneuploidies to 13.5%, structural aberrations including gaps to 9.3%, and structural aberrations excluding gaps to 8.1%.
Increased yield of all aberration types (aneuploidies, gaps, breaks and fragments, satellite associations, deletions, interchanges).
Molecular Weight

259.73

Formula

C14H14ClN3
CAS No.
SMILES

C[N+]1=C2C=C(N)C=CC2=CC3=C1C=C(N)C=C3.[Cl-]
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References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trypaflavin86-40-8ParasiteLeishmaniaunfertilized oocytesmutagenicityInhibitorinhibitorinhibit

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