• Archives of Pharmacal Research
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• v.21 no.5
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• pp.595-598
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• 1998

The rate of the GSH conjugate formation, the inhibition of DNA topoisomerase-I and the cytotoxic activity against L1210 cells of the naphthoquinones showed the same order; 5,8-dimethoxy-1,4-naphthoquinone (DMNQ)>6-(1-hydroxyethyl)-DMNQ>2-(1-hydroxyethyl)-DMNQ; the steric hindrance of the substituents, particularly 2-substutuent, in reacting with cellular nucleophiles must be the main cause for lowering the bioactivities. Acetylation of 2-(1-hydroxyethyl)-DMNQ producing 2-(acetyloxyethyl)-DMNQ potentiated the bioactivities; 2-(-hydroxyethyl)-DMNQ did not react with GSH and the enzyme, and showed $ED_{50}$ of 0.146 mg/ml for the cytotoxcity. Furthermore, the acetylation 2-(1-hydroxyethyl)-DMNQ(T/C, 119%) enhanced the T/C values for the mice bearing S-180 tumor {T/C of 2-(1-acetyloxyethyl)-DMNQ, 276%]. It was assumed that the difference in bioactivities ensued by acetylation was based on the mechanism of the so-called bioreductive alkylation.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.466-470
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• 2003

Nine diarylheptanoids (1-9), one triterpene (10), one sesquiterpenoid (11), one naphthoquinone (12), four tetralones (13-16), one naphthalene carboxylic acid glucoside (17) and six naphthalenyl glycosides (18-23) were isolated from the roots of Juglans mandshurica Maximowicz (Juglandaceae), and their structures determined from the chemical and spectral data. Here, we report the inhibitory effects, on the DNA topoisomerases I and II activities, of all these compounds. Compounds 10 and 23 showed more potent inhibitory effects, on the DNA topoisomerases I and II (94.0 and 86.0% inhibitions at the concentration of 5 $\mu$ g/mL, respectively), than the positive control compounds, camptothecin and etoposide.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.110.3-111
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• 2003

In the previous studies, we have reported that NQ30l, a synthetic l,4-naphthoquinone derivative, displayed a potent antithrombotic activity, and that this might be due to antiplatelet effect, which was mediated by inhibition of cytosolic $Ca^{2+}$ mobilization in activated platelets. In the present study, the effect of NQ301 on arachidonic acid cascade in activated platlets was examined. NQ301 concentration-dependently inhibited washed rabbit platelet aggregation induced by collagen (10 $\mu$g/ml), arachidonic acid (100 $\mu$M) and U46619 (1 $\mu$M), a thromboxane $A_2$receptor agonist, with $IC_50$ values of 0.60$\pm$0.02, 0.79$\pm$0.04 and 0.58$\pm$0.04 $\mu$M, respectively. (omitted)

• Korean Journal of Materials Research
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• v.32 no.5
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• pp.280-286
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• 2022

Corrosion is a natural, inevitable process, and is one of the world's most serious problems. Losses incurred due to corrosion are extremely expensive for society. Several technological strategies have been explored and implemented to address these losses. The use of inhibitors to prevent corrosion is a common and efficient method to reduce corrosion losses. This review covers Al and Al-composite corrosion inhibitors in chloride-containing solutions, because of their popularity in a broad array of industrial applications. A vast number of studies in the literature detail the common tendency of Al and Al-composites with reinforcements to deteriorate. Accordingly, it is worthwhile to employ inhibitors to protect them, as discussed in the present work. The emphasis is on selecting the smartest corrosion inhibitor and evaluating its performance. According to the study, the most commonly used corrosion inhibitors are 1,4-naphthoquinone (NQ), 1,5-naphthalene diol, 3-amino-1,2,4-triazole-5-thiol (ATAT), ammonium tetrathiotungstate, clotrimazole, amoxicillin, antimicrobial and antifungal drugs. Electrochemical impedance spectroscopy (EIS), potentiodynamic (PDP), and weight loss were among the most commonly used modern electrochemical technologies to test inhibitors' efficacy under environmental conditions.

• Biomolecules & Therapeutics
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• v.32 no.5
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• pp.531-539
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• 2024

Sleep is one of the most essential physiological phenomena for maintaining health. Sleep disturbances, such as insomnia, are often accompanied by psychiatric or physical conditions such as impaired attention, anxiety, and stress. Medication used to treat insomnia have concerns about potential side effects with long-term use, so interest in the use of alternative medicine is increasing. In this study, we investigated the hypnotic effects of β-lapachone (β-Lap), a natural naphthoquinone compound, using pentobarbital-induced sleep test, immunohistochemistry, real-time PCR, and western blot in mice. Our results indicated that β-Lap exerts a significant hypnotic effect by showing a decrease in sleep onset latency and an increase in total sleep time in pentobarbital-induced sleep model. The results of c-Fos immunostaining showed that β-Lap decreased neuronal activity in the basal forebrain and lateral hypothalamus, which are wakefulness-promoting brain regions, while increasing in the ventrolateral preoptic nucleus, a sleep-promoting region; all these effects were significantly abolished by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), an adenosine A₁ receptor (A₁R) antagonist. Western blot analysis showed that β-Lap increased extracellular signal-regulated kinase phosphorylation and nuclear factor-kappa B translocation from the cytoplasm to the nucleus; these effects were inhibited by DPCPX. Additionally, β-Lap increased the mRNA levels of A₁R. Taken together, these results suggest that β-Lap exerts hypnotic effects, potentially through A₁R.

• The Journal of Dong Guk Oriental Medicine
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• v.6 no.1
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• pp.107-115
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• 1997

Hapatic tissues of ICR mouse intraperitoneally injected with Triton WR-1339 were observed to investigate the morphologic change of liver by destruction of lipid metabolism as hyperlipidemia. The hepatic tissues were obtained at hour-24, 48, and 72 after triton injection that were fixed in fromol-calcium solution and were cryocut. These tissues were stained by H&E for general morphology, sudan black B for lipid, and perchloric acid-naphthoquinone method for cholesterol. The increase of hepatocyte having meshlike cytoplasm were shown in all hepatic lobules after triton injection and the hepatic plates were disappeared in the region aggregated meshlike hepatocyte. The number of blue black colored lipid drop and dark green colored asterisk shaped cholesterol particle in hepatic cytoplasm were increased than the saline injected mouse and the size of lipid drop was enlarged. As results indicated that the lipid metabolism were destructed by triton injection, subsequently hepatocyes accumulated with lipid including cholesterol.

• Journal of Korean Society on Water Environment
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• v.26 no.4
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• pp.681-686
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• 2010

Two different MFC designs were evaluated in batch mode: single compartment combined membrane-electrodes (SCME) design and twin-compartment brush-type anode electrodes (TBE) design (single chamber with two air cathodes and brush anodes at each side of the reactor). In SCME MFC, carbon anode and cathode electrodes were assembled with a proton exchange membrane (PEM). TBE MFC was consisted of brush-type anode and carbon cloth cathode electrodes without the PEM. A brush-type anode was fabricated with carbon fibers and was placed close to the cathode electrode to reduce the internal resistance. Substrates used in this study were glucose, leachate from cattle manure, or sucrose at different concentrations with phosphate buffer solution (PBS) of 200 mM to increase the conductivity thereby reduce the internal resistance. Hydrogen generating bacteria (HGB) were only inoculated in TBE MFC. The peak power densities ($P_{peak}$) produced from the SCME systems fed with glucose and leachate were 18.8 and $28.7mW/m^2$ at external loads of 1000 ohms, respectively. And the $P_{peak}$ produced from TBE MFC were 40.1 and $18.3mW/m^2$ at sucrose concentration of 5 g/L and external loads of 470 ohms, with a mediator (2-hydroxy-1, 4-naphthoquinone) and without the mediator, respectively. The maximum power density ($P_{max}$) produced from mediator present TBE MFC was $115.3mW/m^2$ at 47 ohms of an external resistor.

• Journal of Pharmaceutical Investigation
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• v.35 no.4
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• pp.255-263
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• 2005

Research was undertaken to compare the pharmacological activity of Lithospermi radix (LR) reported as an oriental medicine for classical uses. LR contains naphthoquinone pigments : shikonin, acetylshikonin, isobutylshikonin, etc. LR is used for the treatment of excision wound, burn, eczema, blister, scarlatina and septicemia as antifebrile, antidotic and antiphlogistic. Gardeniae fructus (GF) has been used for the treatment to jaundice, hepatic disease, anti-inflammatory and analgesic effects, and it contains crocin, geniposide and its derivatives. The therapeutic effects of burn and excision wound healing from LR & GF hydrogel with $Nano-ATP^{\circledR}$ (GLN) were investigated. To evaluate the therapeutic value of various hydrogels, thermal burn model and excision wound mouse model were used. The burn and wound reduction rate and therapeutic period were measured to calculate the healing extent after 5 experiments. The 2nd degree burn was prepared on hairless mouse back skin and dressing with collagen. The burn and wound reduction rate of GLN hydrogel treated group decreased more rapidly than that of other gel group in animal model. Furthermore therapeutic periods of GLN hydrogel treated group was shorter than that of other gel group. In anti-inflammatory test, GLN hydrogel treated group decreased edema rapidly than that of other gel group. These results suggest that the GLN hydrogel treatment has an therapeutic effect on burn and excision wound healing.

• Journal of Applied Biological Chemistry
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• v.52 no.4
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• pp.221-225
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• 2009

Lithospermum erythrorhizon has been known well as one of traditional medicine for fever reduction, detoxication, and blood circulation improvement. This study was carried out to isolate biological active compounds from roots of Lithospermum erythrorhizon and to investigate their low density lipoprotein (LDL) antioxidant and anticancer activities. The hexane extract of Lithospermi Radix has been separated on silica gel chromatography and a naphthoquinone pigment compound 1 has been isolated. The structure of the compound 1 has been identified by spectroscopic technique, including MS and NMR, as acetylshikonin (1). Acetylshikonin showed significantly inhibitory activity on $Cu^{2+}$-induced human LDL oxidation with $IC_{50}$ value of $8.8\;{\mu}M$ and obvious anticancer effect by inhibiting farnesyl:protein transferase (FPTase) activity with $IC_{50}$ value of $23\;{\mu}M$, which suggested that acetylshikonin might be useful for the treatment of atherosclerosis and cancer.

• Journal of Photoscience
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• v.7 no.1
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• pp.1-4
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• 2000

The photosensory ciliates Blepharisma japonicum and Stentor coeruleus use the hypericin-derived pigments blepharismin and stentorin, respectively, as photoreceptor chromophores. Fluorescence quenching studies have shown that the first excited singlet state of hypericin and the purified chromophores blepharismin and stentorin can be deactivated by electron transfer to an acceptor molecule with a suitable reducing potential [1,2]. This paper reports the result of a series of photobehavioral experiments performed with the aim to ascertain if the same electron accepters which quench the photoreceptor pigment fluorescence in vitro may also compete with the native acceptor molecule in its natural physiological environment. Individual cell trajectories were examined before and after light stimulation, in the presence and in the absence of potential "in vivo" electron accepters, with a microvideo-recording apparatus. Our data, on Blepharisma cells, showed that as the negative reduction potential of the electron acceptor increases, a pronounced decrease in cell photoresponsiveness was detected. A dramatic effect on cell photoresponsiveness was noticed in the presence of 1,4-benzoquinone that has the lowest negative reduction potential. Such an effect on the percentage of photoreacting cells was moderate in the case of 1,4-naphthoquinone, with a relatively higher negative reduction potential. In the presence of benzophenone, which has the highest negative reduction potential, no significant effect on photoreacting cells was noticed. Our results can support the hypothesis that in the pigment granules such a light-induced charge transfer from excited blepharismin to a suitable electron acceptor triggers sensory transduction processes in B. japonicum.