• Environmental Analysis Health and Toxicology
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• 제15권4호
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• pp.157-163
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• 2000

2- [(4- Cyanophenyl)amino] -3-chloro-1, 4- naphthalenedione (NQ-Y15) was asssayed for its genotoxic potential by using Salmonella typhimurium reversion assay and in vitro chromosome aberration test on Chinese hamster lung cells. In the Ames test, NQ-Y15 induced his + revertants of Salmonella typhimurium TA 98 and TA1537, reaching levels twice the negative control values. But, NQ-Y15 induced only his+ revertants of Salmonella typhimurium TA1537 more than twice the control values under the condition with metabolic activation system. In the cytogenetic test on chinese hamster lung cells. NQ -Y15 showed significant chromosomal aberrations, but the incidence was significantly reduced in the presence of metabolic activation.

• Archives of Pharmacal Research
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• 제16권4호
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• pp.327-330
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• 1993

A series of 2-chloro and 2-bromo-3-(substituted)-1, 4-naphthalenedione derivatives (1-25) were tested for antifungal and antibacterial activities in vitro against Candida albicans 10231 aand Local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Fusarium oxysporium KTCC 6501, Bacillus subtilis ATCC 6633, Pseudomonas arruginosa NCTC 10490, Staphylococcus aureus ATCC 6358p, Escherichia coli NIHJ and Acinetobacter baumanii Local. The MiC values were determined by twofold afar diution/streak method. Among thee derivatives, 1, 9, 20, 21, 23 and 25 showed more potent antifungal activities than fluconazole. 20 and 23 completely inhibited the gorwth of fungi, such as Candida albicans, Aspegillus niger, Ticophyton mentagrophytes and fusarium oxysporium, at $3.2\;\mu{g/ml}$. Also some derivatives had the antibacterial activities against Gram-positive bacteria.

• 약학회지
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• 제43권6호
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• pp.809-817
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• 1999

The effect of 2-(4-cyanophenyl)amino-1,4-naphthalenedione-3-pyridinium perchlorate (PQ5) on pla-telet aggregation and its action mechanisms were investigated with rat platelet. PQ5 inhibited the platelet aggregation induced by collagen ($6{\;}{\mu\textrm{g}}/ml$), thrombin (0.4 U/ml) and A23187 ($3{\mu}M$) in concentration-dependent manner with $IC_{50}$ values of 5.50, 25.89 and $37.12{\;}{\mu}M$, respectively. PQ5 also significantly reduced the thromboxane $A_2$ (TXA2) formation in a concentration dependent manner. The collagen-induced arachidonic acid (AA) release in [-3H]-AA incorporated platelet, an indication of the phospholipase $A_2$ activity, was decreased by PQ5 pretreatment PQ5 significantly inhibited the activity of thormboxane synthase only at high concentration ($100{\mu}M$), but did not affect the cyclooxygenase activity at all. Collagen-induced ATP release was significantly reduced by PQ5. Calcium-induced platelet aggregation experiment suggests that the elevation of intracellular free $Ca^{2+}$ concentration ($[Ca^{2+}]_i$) by collagen stimulation is decreased by the pretreatment of PQ5, which is due to the inhibition of calcium release from intracellular store and influx from outside of the cell. PQ5 did not showed the effect of anticoagulation as prothrombin time (PT) or activated partial thromboplastin time (APTT). Form these results, it is suggested that PQ5 exerts its antiplatelet activity through the inhibition of the intracellular $Ca^{2+}$ mobilization and the decrease of the $TXA_2$ synthesis.

• Biomolecules & Therapeutics
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• 제7권3호
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• pp.227-233
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• 1999

The effects of 2-bromo-3-(3,5-tert-butyl-4-hydroxylphenyl)-1,4-naphthalenedione(TPN2), a synthetic vitamin K derivative, on platelet aggregation and its action mechanisms were investigated in rat platelet. TPN2 inhibited the platelet aggregation induced by collagen($10\mu\textrm{g}$/ml), thrombin(0.1 U/ml), A23187($10\mu\textrm{M}$) and arachidonic acid($100\mu\textrm{M}$) in concentration-dependent manner with $IC_{50}$ values of 6.5$\pm$1.3, 59.3$\pm$4.5, 13.0$\pm$2.37 and 2.9$\pm$$1.0\mu\textrm{M}$, respectively. Collagen-induced serotonin release was significantly reduced by TPN2. The elevation of intracellular free $Ca^{2+}$ concentration ([$Ca^{2+}$]i) by collagen stimulation was greatly decreased by the pretreatment of TPN2, which was due to the inhibition of calcium release from intracellular store and influx from outside of the cell. TPN2 also significantly reduced the thromboxane $A_2$($TXA_2$) formation in a concentration-dependent manner. The collagen-induced arachidonic acid (AA) release in [$^3H$]-AA incorporated platelet, an indicative of the phospholipase $A_2$ activity, was decreased by TPN2 pretreatment. TPN2 significantly inhibited the activity of thromboxane synthase, but did not affect the cyclooxygenase activity. From these results. it is suggested that TPN2 exert its antiplatelet activity through the inhibition of the intra-cellular $Ca^{2+}$ mobilization and the decrease of the $TXA_2$ synthesis.

• Archives of Pharmacal Research
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• 제16권2호
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• pp.161-163
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• 1993

In order to evaluate the antimicrobial effect of 2,3-disubstituted-1,4-naphthalenedione derivatives, we synthesized several 2-chloro, 2-bromo and 2-hydroxy-3(substituted)-1, 4-naphthalene-diones (1-25). These derivatives were tested for antifugal and antibacterial activities, in vitro, against Candida albicans 10231 and local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Baciilus subtilis ACTT 6633, Pseudomonas aeruginsa NCTC 10490, Staphylococcus aureus ATCC 6538P, Escherichia coli NIHJ. The MIC values were determined by the two-fold agar dilution/strea method. Among these derivatives, 4, 5 and 6 showed the potent antifungal activities. Also 5 and 6 had the antibacterial activities. 5 with (1,2,4-triazolyl)-amino moirty was the most effective in preventing the growth of fungi, such as Candida albicans, Aspergillus niger and Tricophyton mentagrophytes.