• The Korean Journal of Physiology and Pharmacology
• /
• 제19권5호
• /
• pp.473-478
• /
• 2015

To see the inhibitory mechanism of gentamicin in response to electrical field stimulation (EFS) using the rat bladder smooth muscle, atropine or guanethidine was treated but had no effect. Methylsergide, a non-selective 5-$HT_1$, 5-$HT_2$ receptor antagonist was also treated but had on effect. Kinase inhibitors, such as chelerythrine (PKC inhibitor), ML-9 (MLCK inhibitor), or Y27632 (rho kinase inhibitor) were pretreated before gentamicin treatment, but did not have effect. For U73122, a phospholipase C (PLC) inhibitor however, the inhibitory effect to gentamicin was significantly attenuated in all frequencies given by the EFS. Therefore gentamicin induced inhibitory effect on EFS response in rat bladder smooth muscle was not mediated by the activation of adrenergic, cholinergic, or serotonergic receptor. The inhibition of gentamicin might be mediated through the PLC dependent pathway, but not through the PKC, MLCK or rho kinase dependent pathway.

• 대한한방부인과학회지
• /
• 제22권2호
• /
• pp.43-59
• /
• 2009

Purpose: This study was performed to determine the inhibitory effect of Persimmon Leaves extract (PL) on melanin synthesis in B16F10 melanoma cells B16F10. Methods: The inhibitory effects of PL on melanin synthesis were determined by in vitro assay. To elucidate inhibitory effects of PL on melanin synthesis, we determined the melanin release and melanin production in B16F10. And to investigate the action mechanism, we assessed the gene expression of tyrosinase, TRP-1, TRP-2, PKA, PKC${\beta}$, ERK-1, ERK-2, AKT-1, MITF in B16F10. Results: 1. PL inhibited melanin release, melanin production in B16F10. 2. PL inhibited tyrosinase activity in vitro and in B16F10. 3. PL suppressed the expression of tyrosinase, TRP-1, TRP-2 in B16F10. 4. PL suppressed the expression of PKA, PKC${\beta}$ in B16F10. 5. PL increased the expression of ERK-1, ERK-2, AKT-1 in B16F10. 6. PL suppressed the expression of MITF in B16F10. Conclusion: From these results, it may be concluded that PL is possesed of the antimelanogenetic effects.

• 한국자기공명학회:학술대회논문집
• /
• 한국자기공명학회 2002년도 International Symposium on Magnetic Resonance
• /
• pp.31-31
• /
• 2002

• 한국생물물리학회:학술대회논문집
• /
• 한국생물물리학회 2003년도 정기총회 및 학술발표회
• /
• pp.62-62
• /
• 2003

The native form of serpin (serine protease inhibitor) is kinetically trapped in metastable state. Metastability in these proteins is critical to their biological function. Serpins inhibit target proteases by forming a stable covalent complex in which the cleaved reactive site loop of the serpin is inserted into $\beta$-sheet A of the serpin with concomitant translocation of the protease to the opposite of the initial binding site. Despite recent determination of the crystal structures of a Michaelis protease-serpin complex as well as a stable covalent complex, details on the kinetic mechanism remain unsolved. In this study we constructed several $\alpha$$_1$-antitrypsin variants and examined their kinetic mechanism of loop translocation and formation of protease-serpin complex by stopped-flow experiments of fluorescence resonance energy transfer as well as quenched-flow experiment. We report here the relationship of serpin's conformational switch mechanism with Inhibitory activity. There is little direct correlation between loop insertion rate and inhibitory activity. Rather, disrupting a salt bridge between R196 and E354 accelerates loop translocation even though it impairs the inhibitory activity. Moreover, the serpin's reactive site loop is translocated, at least partially, prior to loop cleavage.

• Environmental Analysis Health and Toxicology
• /
• 제8권3_4호
• /
• pp.33-41
• /
• 1993

This study was designed to determine the hemolytic mechanism of antitumor agent tetraphosphine platinum (II) complex (RC-1), which was synthesized recently. Erythrocytes treated with RC-1 showed concentration and time dependent lipid peroxydation, methemoglobin synthesis and hemolysis. And also treatment of radical scavengers showed the inhibitory effect of hemolysis and the decrease of malondialdehyde levels in RC-1 treated erythrocytes. So, the mechanism of hemolysis was considered to be the generation of free radicals, methemoglobin synthesis and the lipid peroxidation of phospholipid which composed of erythrocyte membrane.

• 동의생리병리학회지
• /
• 제23권2호
• /
• pp.452-456
• /
• 2009

The purpose of this study was to investigate the anti-inflammatory effects and cellular mechanism of piperine on murine peritoneal macrophages. To evaluate the effects of piperine, we examined the production of nitric oxide (NO), interleukin (IL)-10 and IL-12. To investigate inhibitory mechanism of piperine, we examined the MAPKs and Ik-Ba in murine peritoneal macrophages, Piperine itself does not have any cytotoxic effect and reduced lipopolysaccharid (LPS), Poly(I:C), CpG-ODN -induced production of NO, IL-10 and IL-12 in peritoneal macrophages. Piperine inhibited the activation of extracelluar signal-regulated kinase (ERK 1/2) and c-Jun NH2-terminal kinase (JNK 1/2) not the activation of p38 and the degradation of inhibitory kappa B a (Ik-Ba) in the LPS-stimulated murine peritoneal macrophages.ln conclusion, Piperine down-regulated LPS-induced production of NO, IL-10 and IL-12, which could provide a clinical basis for anti-inflammatory properties of piperine.

• Journal of Microbiology and Biotechnology
• /
• 제16권4호
• /
• pp.531-537
• /
• 2006

Lactic acid-producing bacteria (LABs) are known to have various beneficial properties for health. However, they are generally considered to have an adverse effect on teeth, since they produce acid. Nonetheless, milk and cheese containing specific LAB strains were recently found to have an inhibitory effect on dental caries in children, with an inhibitory activity towards the growth of Streptococcus mutans suggested as the responsible mechanism. Accordingly, the current study selected a probiotic candidate for oral health and studied its inhibitory mechanism against dental caries. Twenty-two LAB species belonging to eleven genuses were screened for promoting bone nodule formation using direct microscopic examination. Only one isolate, Weissella kimchii strain PL9001, increased the bone nodule formation significantly. The addition of W. kimchii strain PL9001 to bone cells prepared from mouse calvaria increased the bone nodule formation, calcium accumulation, and activity of alkaline phosphatase (the osteoblastic marker). Moreover, W. kimchii strain PL9001 inhibited the invasion of Streptococcus mutans into bone cells, and an organic extract of the culture supernatant of W. kimchii strain PL9001 inhibited the growth of Strep. mutans. Therefore, the results suggest that W. kimchii strain PL9001 can be used as a preventive measure against dental caries. This is the first time that a LAB has been shown to promote bone nodule formation and prevent the invasion of Strep. mutans into bone cells.

• Natural Product Sciences
• /
• 제6권1호
• /
• pp.36-39
• /
• 2000

Acorenone, a diterpene isolated from Acorus gramineus, showed strong resistance inhibitory activity against multi-drug resistant microorganisms such as Staphylococcus aureus SA2, which has resistance to 10 usual antibiotics including chloramphenicol (Cm). At the level of $5\;{\mu}g/ml$ when combined with $50\;{\mu}g/ml$ of Cm. Bacterial resistance to Cm is due to the presence in resistant bacteria of an enzyme, chloramphenicol acetyltransferase (CAT), which catalyses the acetyl-CoA dependent acetylation of the antibiotic at C-3 hydroxyl group. To elucidate the mechanism of resistant inhibitory effect, the acorenone which had the strongest resistant inhibitory activity, was investigated on the CAT assay. As the result, the combination of Cm and acorenone showed the strongest inhibitory activity on CAT as noncompetitive and dose dependent manner.

• 약학회지
• /
• 제34권6호
• /
• pp.407-414
• /
• 1990

The relationships of inhibitory activities of inflammation and wound healing of flavonoids were studied in vitro and in vivo. Generally flavonoids have not only significantly anti-inflammatory activity in carrageenin-induced paw edema and Freund's complete adjuvant-induced arthritis, but also inhibitory activity of wound healing. The more inhibitory activities of wound healing flavonoids have, the more they have the anti-inflammatory activities; apigenin > guercetin > flovone > rutin > hesperidin > naringin. Their inhibitory mechanism seems to be inhibition of the inflammatory cell infiltration and fibroblast proliferation, and so they decreased the granulomatous activity and tensile strength.

• 생약학회지
• /
• 제31권2호
• /
• pp.196-202
• /
• 2000

This study was conducted to search for the ${\alpha}-glucosidase$ inhibitor from the natural products. In the previous study, the water extract of Gyrophora esculenta exhibited a potent inhibitory effect on ${\alpha}-glucosidase$ activities. Then, by bioassay-guided fractionation followed by chromatographic separation of the water extract of Gyrophora esculenta, ${\alpha}-glucosidase$ inhibitor was isolated as GE974. GE974 showed significant inhibitory activities on some kinds of ${\alpha}-glucosidase$ in vitro. Its inhibitory mechanism seemed to be competitive for disaccharides. Also, it markedly inhibited ${\alpha}-glucosidases$ of intestine separated from both nondiabetics and diabetics.