Asterriquinol (ARQ) is an antitumor metabolite of Aspergillus terreus IFO 6123. ARQ is a quinone admixture and the apparatus of its antitumor action was compared with that of its analog ARQDMe which was dimethylated at the dihydroxy benzoquinone moiety, and adriamycin (ADR). The cytotoxicity of ARQ adjoin P388 beef was beneath than that of ADR, and ARQDMe showed hardly any cytotoxicity. ARQ and ADR formed DNA-interstrand cantankerous links (ISC) in P388 beef in a absorption while the ISC basis by ARQDMe was actual low even at 10 microM. P388 beef advised with ARQ and ADR for 18 hours showed, dose-dependently, nucleosomal ladder accumulation as able-bodied as the actualization of base DNA. Difference amid the action of ARQ and ADR were empiric by breeze cytometric corpuscle aeon analysis. ARQ acquired the beef to accrue at the G1 appearance of the corpuscle cycle, while use of ADR led to arrest in the G2/M phase. ARQDMe never acquired apoptotic changes or corpuscle aeon alterations. These after-effects announce that ARQ intercalates in the genomic DNA, causes G1 arrest, and leads to apoptotic corpuscle death, this suggests that the dihydroxybenzoquinone atom of the admixture is capital to arm-twist these actions.
Asterriquinol D was calmly actinic in three accomplish from 2,5-dichloro-1,4-benzoquinone. The acknowledgment of benzoquinone with indole in the attendance of Pd(OAc)2, followed by blaze with cerium (IV) ammonium nitrate (CAN) produced 3,6-dichloro-2,5-bis (3-indolyl)-1,4-benzoquinone. The methoxylation of the dichloride with NaOH in CH3OH afforded asterriquinone D.
The alternation of asterriquinone (ARQ), a atypical antitumor abettor abandoned from Aspergillus fungi, with deoxyribonucleic acerbic (DNA), has been studied. The bounden of ARQ in vitro with DNA (calf thymus) was absolute by its behavior in gel filtration application a Sephadex G-25 cavalcade at pH 5.4. Some ARQ analogs accepting no, or less, antitumor action did not display any affirmation of alternation with DNA beneath the aforementioned condition. From the after-effects acquired in this work, the pKa amount of ARQs seemed to be analytical amid 6 and 7 for their bounden to DNA and for exhibition of antitumor activity. Also, ARQ showed austere film deformations and an inhibitory aftereffect on the bleary adenosine triphosphatase of Ehrlich blight cells.
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