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Suppression of the NF-<i>k</i>B signalling pathway by ergolide, sesquiterpene lactone, in HeLa cells
Chun, Jae Kwang,Seo, Dong-Wan,Ahn, Seong Hoon,Park, Jae Hyun,You, Jueng-Soo,Lee, Chang-Hee,Lee, Jae Cheol,Kim, Yong Kee,Han, Jeung-Whan Pharmaceutical Society of Great Britain 2007 Journal of pharmacy and pharmacology Vol.59 No.4
Silymarin inhibits melanin synthesis in melanocyte cells.
Choo, Soo-Jin,Ryoo, In-Ja,Kim, Young-Hee,Xu, Guang-Hwa,Kim, Won-Gon,Kim, Ki-Ho,Moon, Seong-Joon,Son, Eui-Dong,Bae, KiHwan,Yoo, Ick-Dong Pharmaceutical Society of Great Britain 2009 Journal of pharmacy and pharmacology Vol.61 No.5
<P>OBJECTIVES: The aim was to search for inhibitors of melanogenesis from natural resources. METHODS: The inhibitory effect of silymarin on melanogenesis in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab, was studied. KEY FINDINGS: Silymarin significantly prevented melanin production in a dose-dependent manner with an IC50 value (concentration producing 50% maximal inhibition) of 28.2 microg/ml, without effects on cell viability. Also, silymarin inhibited L-DOPA oxidation activity of tyrosinase, the rate-limiting melanogenic enzyme, in cell based-systems but it did not directly affect cell-free tyrosinase activity. Furthermore, Western blot analysis indicated that silymarin decreased the expression of tyrosinase protein. CONCLUSIONS: This study suggests that the depigmenting effect of silymarin might be attributable to inhibition of tyrosinase expression and that silymarin may be useful as a natural skin-lightening agent.</P>
Choi, Young H,Lee, Young S,Kim, Tae K,Lee, Bong-Y,Lee, Myung G Pharmaceutical Society of Great Britain 2009 Journal of pharmacy and pharmacology Vol.61 No.10
<P>OBJECTIVES: It has been reported that mirodenafil is primarily metabolized via hepatic cytochrome P450 (CYP) 1A1/2, 2B1/2, 2D1 and 3A1/2 in rats. It has also been reported that the protein expression of hepatic CYP3A1 and intestinal CYP1A1 and 3A1/2 increases and that of hepatic CYP2D1 decreases in rats with acute renal failure induced by uranyl nitrate (U-ARF rats). Thus, the pharmacokinetics of mirodenafil were studied in control and U-ARF rats. METHODS: The pharmacokinetic parameters of mirodenafil and SK3541 (a metabolite of mirodenafil) were compared after the intravenous and oral administration of mirodenafil at a dose of 20 mg/kg to U-ARF and control rats. KEY FINDINGS: After interavenous administration of mirodenafil to U-ARF rats, the total area under the concentration-time curve (AUC) of mirodenafil was significantly smaller (36.5% decrease) than controls, possibly due to the significantly faster non-renal clearance (66.1% increase; because of increase in the protein expression of hepatic CYP3A1) than controls. After the oral administration of mirodenafil to U-ARF rats, the AUC of mirodenafil was also significantly smaller (47.8% decrease) due to the increase in the protein expression of hepatic CYP3A1 and intestinal CYP1A1 and 3A1/2 compared with controls. CONCLUSIONS: After both intravenous and oral administration of mirodenafil to U-ARF rats, the AUC(SK3541)/AUC(mirodenafil) ratios were comparable with that in controls and this could be due to further metabolism of SK3541 in rats.</P>
Effect of wild ginseng on scopolamine-induced acetylcholine depletion in the rat hippocampus.
Lee, Bombi,Park, Jongbong,Kwon, Sunoh,Park, Moo-Won,Oh, Sang-Muk,Yeom, Mi-Jung,Shim, Insop,Lee, Hye-Jung,Hahm, Dae-Hyun Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.2
<P>Objectives The ameliorating effects of wild ginseng on learning and memory deficits were investigated in rats. Methods Rats were treated daily with wild ginseng or cultivated ginseng for 7 days at 30 min before scopolamine injection (2 mg/kg, i.p.). After inducing cognitive impairment by the administration of scopolamine, behavioural assessment using the Morris water maze was performed. Changes in cholinergic system reactivity were also examined by measuring the immunoreactive neurons of choline acetyltransferase and the reactivity of acetylcholinesterase in the hippocampus. Key findings Scopolamine injection induced impaired performance in the water maze test and severe cell losses in hippocampal cholinergic neurons, as indicated by decreased choline acetyltransferase immunoreactivity and increased acetylcholinesterase reactivity. Daily administration of wild ginseng produced a significant improvement in the escape latency for finding the platform in the Morris water maze and reduced the loss of cholinergic immunoreactivity in the hippocampus. The reduced expression of brain-derived neurotrophic factor mRNA due to the scopolamine injection was recovered to normal levels by the administration of wild ginseng. Conclusions Wild ginseng demonstrates a significant neuroprotective effect against scopolamine-induced neuronal and cognitive impairment.</P>
Kim, Dong-Seok,Park, Seo-Hyoung,Kwon, Sun-Bang,Kwon, Nyoun Soo,Park, Kyoung-Chan Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.2
<P>Objectives Sphingolipids act as structural components in cell membranes, and form lipid intermediates that have functional roles as signalling molecules in various cellular processes. Our previous findings have suggested that sphingolipid metabolites are deeply involved in the regulation of melanogenic processes. In this study we aimed to examine sphingosylphosphorylcholine-mediated signalling pathways related to melanogenesis. Methods We determined the hypopigmenting effects and the related signalling pathways of sphingosylphosphorylcholine in Mel-Ab cells. In particular, we analysed the involvement of the G-protein-coupled receptor in sphingosylphosphorylcholine-induced MITF degradation. Key findings Western blotting revealed that sphingosylphosphorylcholine induced the activation of extracellular signal-regulated kinase (ERK), as well as Akt. Moreover, the specific Akt pathway inhibitor LY294002 blocked the hypopigmenting effect of sphingosylphosphorylcholine and abrogated the sphingosylphosphorylcholine-mediated down-regulation of microphthalmia-associated transcription factor (MITF), showing that the Akt pathway is involved in sphingosylphosphorylcholine-mediated melanin inhibition. Treatment with the proteasome inhibitor MG132 blocked the decrease in MITF by sphingosylphosphorylcholine, but sphingosylphosphorylcholine did not decrease the level of MITF mRNA, indicating that the reduction in the level of MITF results from MITF degradation. Furthermore, pre-incubation of Mel-Ab cells with pertussis toxin completely abolished the hypopigmenting effects and the activation of ERK and Akt by sphingosylphosphorylcholine, suggesting that the effects of sphingosylphosphorylcholine are mainly dependent on the G-protein-coupled receptor). Conclusions Together, these results suggest that sphingosylphosphorylcholine reduces melanin synthesis via pertussis toxin-sensitive ERK and Akt activation, and subsequent MITF degradation.</P>
Li, Dong Xun,Park, Young-Joon,Oh, Dong Hoon,Joe, Kwan Hyung,Lee, Jung Hoon,Yeo, Woo Hyun,Yong, Chul Soon,Choi, Han-Gon Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.4
<P>OBJECTIVES: The aim of this study was to develop a novel itraconazole-loaded gelatin microcapsule without ethanol with enhanced oral bioavailability. METHODS: Various gelatin microcapsules were prepared using a spray-drying technique. Their physicochemical properties, dissolution, characteristics and pharmacokinetics in rats were evaluated and compared with those of a commercial product. KEY FINDINGS: The gelatin microcapsule at a weight ratio for itraconazole/gelatin/citric acid of 1 : 3 : 0.3 was spherical in shape with a smooth surface and inner hole, and gave a maximum drug solubility of about 700 microg/ml. The gelatin microcapsule dramatically increased the initial dissolution rate of itraconazole compared with a commercial product in simulated gastric fluids (pH 1.2). Moreover, at the same dose as the commercial product, it gave significantly higher initial plasma concentrations, C(max) and AUC of itraconazole in rats than did the commercial product, indicating that providing the drug in the gelatin microcapsule caused enhanced absorption in rats. At half dose, it gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. CONCLUSIONS: The itraconazole-loaded gelatin microcapsule without ethanol developed using a spray-drying technique at half the dose of the commercial product can deliver itraconazole in a pattern that allows fast absorption in the initial phase, making it bioequivalent to the commercial product.</P>
Bioavailability of indomethacin-saccharin cocrystals.
Jung, Min-Sook,Kim, Jeong-Soo,Kim, Min-Soo,Alhalaweh, Amjad,Cho, Wonkyung,Hwang, Sung-Joo,Velaga, Sitaram P Pharmaceutical Society of Great Britain 2010 Journal of pharmacy and pharmacology Vol.62 No.11
<P>Objectives??Pharmaceutical cocrystals are new solid forms with physicochemical properties that appear promising for drug product development. However, the in-vivo bioavailability of cocrystals has rarely been addressed. The cocrystal of indomethacin (IND), a Biopharmaceutical Classification System class II drug, with saccharin (SAC) has been shown to have higher solubility than IND at all pH. In this study, we aimed to evaluate the in-vitro dissolution and in-vivo bioavailability of IND-SAC cocrystals in comparison with IND in a physical mixture and the marketed product Indomee®. Methods??Scale-up of the cocrystals was undertaken using cooling batch crystallisation without seeding. The chemical and physical purity of the up-scaled material was verified using high-performance liquid chromatography, differential scanning calorimetry and powder X-ray diffraction. The IND-SAC cocrystals and IND plus SAC were mixed with lactose and the formulations were placed into gelatin capsules. In-vitro dissolution studies were then performed using the rotating basket dissolution method. The intrinsic dissolution rate of IND and IND-SAC cocrystals was also determined. Finally, a bioavailability study for the formulations was conducted in beagle dogs. The plasma samples were analysed using high-performance liquid chromatography and the pharmacokinetic data were analysed using standard methodologies. Key findings??The bulk cocrystals (i.e. scaled-up material) were chemically and physically pure. The in-vitro dissolution rate of the cocrystals was higher than that of IND and similar to that of Indomee® at pH 7.4 and pH 1.2. The in-vivo bioavailability of the IND-SAC cocrystals in dogs was significantly higher (ANOVA, P??lt;??.05) than that of IND but not significantly different from Indomee® (ANOVA, P??gt;??.05). Conclusions??The study indicates that the improved aqueous solubility of the cocrystals leads to improved bioavailability of IND. Thus, the cocrystals are a viable alternative solid form that can improve the dissolution rate and bioavailability of poorly soluble drugs.</P>
Coptidis Rhizoma attenuates repeated nicotine-induced behavioural sensitization in the rat.
Lee, Bombi,Yang, Chae Ha,Hahm, Dae-Hyun,Lee, Hye-Jung,Choe, Eun Sang,Pyun, Kwang-Ho,Shim, Insop Pharmaceutical Society of Great Britain 2007 Journal of pharmacy and pharmacology Vol.59 No.12
<P>Repeated injections of nicotine can produce an increase in locomotor activity and the expression of immediate-early gene, c-fos, in the central dopaminergic areas. Many studies have shown that Coptidis Rhizoma (CR) and its main alkaloid compound, berberine (BER), have a suppressive effect on the central nervous system. We examined the influence of CR or BER on repeated nicotine-induced locomotor activity in rats and the change of c-Fos expression in the brain by using immunohistochemistry. Male Sprague-Dawley rats were given CR and BER before repeated injections of nicotine hydrochloride (0.4 mg kg(-1), s.c.) twice daily for 7 days. After 3 days withdrawal, rats received a challenge injection of nicotine. Pretreatment with CR (100 mg kg(-1), i.p.) and BER (100 mg kg(-1), i.p.) significantly inhibited the nicotine-induced locomotor activity and expression of c-Fos in the striatum and the nucleus accumbens. These results suggest that CR and BER may produce inhibitory effects of nicotine on behavioural sensitization by possibly reducing postsynaptic neuronal activation in the central dopaminergic systems.</P>