• Archives of Pharmacal Research
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• v.28 no.1
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• pp.111-114
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• 2005

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

• The Journal of Korean Medicine
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• v.21 no.4
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• pp.193-203
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• 2000

Objectives : Hindered barrier function of vascular endothelium has been implicated in the initiation and progression of degenerative vascular diseases such as atherosclerosis. In this study, the effect of Sunghyangchungisan(SHCS) as a protectant against oxidant-induced destruction of endothelial barrier function was assessed. Methods : Toward this end, endothelial cells derived from the human umbilical vein were cultured as monolayers on permeable membrane filters. Endothelial permeability was monitored by measuring transendothelial electrical resistance and movement of low density lipoprotein (LDL) across the endothelial monolayer. Results : Along with increased movement of LDL, $H_2O_2$-induced increase in endothelial permeability was paralleled by a decrease in transendotheliaI electrical resistance. The effect of $H_2O_2$ was mimicked by phorbol 12-myristate 13-acetate (PMA), a potent activator of proteinkinase C. Calphostin-C, a protein kinase C inhibitor, effectively blocked the increase in endothelial permeability induced by $H_2O_2$ or PMA, indicating that activation of protein kinase C is associated with the $H_2O_2-induced$ permeability change. SHCS effectively protected the endothelial monolayer against $H_2O_2-induced$ increase in permeability, whereas, it did not affect PMA-induced change. Forskolin, a potent activator of adenylyl cyclase, antagonized $H_2O_2$ to increase endothelial permeability. In addition, in ${H_2O_2}-treated$ cens, intracenular cAMP concentration was significantly decreased, indicating that impaired cAMP production as well as activation of proteinkinase C is a mechanism underlying ${H_2O_2}>-induced$$H_2O_2$ with regard to its effect on intracellular cAMP content. However, SHCS itself did not affect resting cAMP concentration in endothelial cells. Conclusions : These results suggest that SHCS might operate as an effective protectant against oxidant-induced destruction of endothelial barrier function. The mechanism does not appear to involve direct interaction with protein kinase C- or cAMP-associated signaling mechanism.

• YAKHAK HOEJI
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• v.36 no.2
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• pp.140-149
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• 1992

Anti-allergic action of each water extracts of some crude drugs was investigated in mice and rats. The activity of hyaluronidase which was used in the screening test of anti-allergic action was inhibited significantly by Amomi Semen, Asiasari Radix, Cimicifugae Rhizoma, Cinnamomi Ramulus, Glycyrrhizae Radix and Scutellariae Radix. The 48-hour homologous passive cutaneous anaphylaxis(48-hr PCA) in mouse ear was inhibited significantly by intraperitoneal(i.p.) injection of Amomi Semen, Cimicifugae Rhizoma, and ketotifen, a comparative drug of an anti-allergic action. The increase of vascular permeability induced by histamine or serotonin was inhibited significantly by i.p. injection of Amomi Semen, Cimicifugae Rhizoma, Cinnamomi Ramulus and ketotifen. In rat dorsal skin, the increase of vascular permeability which was induced by histamine, serotonin or compound 48/80 was inhibited significantly by i.p. injection of Amomi Semen, Asiasari Radix, Cimicifugae Rhizoma, Scutellariae Radix and ketotifen. Armeniacae Semen and Liriopis Tuber which had not inhibited hyaluronidase activity did not inhibit 48-hr PCA and the increase of histamine, serotonin or compound 48/80-induced vascular permeability in mice and rats. These results suggest that each water extract of Amomi Semen and Cimicifugae Rhizoma has anti-allergic action.

• Biomolecules & Therapeutics
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• v.4 no.1
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• pp.36-45
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• 1996

The antihistaminic action of eighteen herbal medicines was investigated by the radioligand binding and functional assays. The hexane fractions of Trichosanthis radix, Mori cortex radicis and Evodiae fructus dosedependently inhibited [$^3$H] mepyramine binding to H$_1$, receptor in guinea-pig brain homogenates and histamine-induced contraction of isolated guinea-pig ileum. Antihistaminic action of the hexane and ethyl acetate fractions of Mori cortex radicis and the hexane fraction of Evodiae fructus was more potent than their antimuscarinic action evaluated from the inhibition of [$^3$H]QNB binding and carbachol response. The ethyl acetate and chloroform fractions from Scutellariae radix also inhibited histamine-induced contraction, but antihistaminic potencies of these fractions were almost identical with their antimuscarinic potencies. The hexane fractions of Mori cortex radicis and Evodiae fructus inhibited selectively the increase of histamine-induced cutaneous vascular Permeability in the rat dorsal skins. However, the ethyl acetate fraction from Scutellariae radix inhibited eqipotently the effects of histamine and serotonin on the vascular permeability. These results demonstrate that the hexane and ethyl acetate fractions of Mori cortex radicis and the hexane fraction of Evodiae fructus have the selective histamine H$_1$receptor blocking activity.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.124-128
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• 1993

The anti-inflammatory activity of the aqueous extract from Gleditsiae spina was investigated utilizing carrageenin-induced edema, granuloma pouch and adjuvant arthritis in rats. The effects of this agent on vascular permeability and acetic acid-induced writhing in mice were also examined. Its anti-inflammatory activity on carrageenin edema was observed with oral administration. The aqueous extract from Gleditsiae spina(400 mg/kg, 7 days) showed significant inhibitory effects on granuloma and exudate formation in rats. In the method of adjuvant arthritis, the aqueous extract(400 mg/kg), orally administered for 21 days, inhibited the development of hind paw edema in rats. The aqueous extract was also inhibited the increase in vascular permeability and the number of writhings induced by acetic acid in mice. In the present study, the aqueous extract of Gleditsiae spina was indicated to have the anti-inflammatory action.

• Archives of Pharmacal Research
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• v.29 no.4
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• pp.302-309
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• 2006

Lupus-like syndrome is characterized by multiple organ injuries including lungs and kidneys. Endotoxin induces a transiently intent systemic inflammatory response and indirectly transient acute lung injury in normal condition. However, whether endotoxin may trigger the persistent development of lung injury in chronic, inflammatory lupus-like syndrome compared with normal condition remains unclear. We examined the pulmonary vascular permeability and production of proinflammatory cytokines, such as TNF-${\alpha}$, IL-6, IL-10 and IFN-${\gamma}$, which play prominent roles in the pathogenesis of lupus-like tissue injury, 6 hand 72 h after i.p. lipopolysaccharide (LPS; endotoxin) injection in pristane-primed chronic inflammation ICR mice characterized by a lupus-like syndrome. These results demonstrated that levels of serum IL-6, IL-10 and IFN-${\gamma}$ and bronchoalveolar lavage (BAL) IL-6 and IFN-${\gamma}$ were remarkably increased 6 h in LPS-exposed pristane-primed mice compared with pristane-primed controls, while pulmonary vascular permeability and levels of serum and BAL TNF-${\alpha}$ were not. And levels of BAL TNF-${\alpha}$, IL-6 and IL-10 were significantly enhanced 72 h in LPS-exposed pristane-primed mice compared with pristane-primed controls. Also, LPS significantly induced the increased in vitro production of TNF-${\alpha}$, IL-6 and IL-10 by lung cells obtained from LPS-exposed pristane-primed mice compared with LPS-exposed normal mice. Our findings indicate that LPS may trigger persistent progression of lung injury through late overproduction of BAL TNF-${\alpha}$, IL-6, and IL-10 in lupuslike chronic inflammation syndrome compared with normal condition.

• Archives of Plastic Surgery
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• v.37 no.1
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• pp.12-21
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• 2010

Purpose: This work aimed to elucidate the anti-inflammatory effect of pegmatite in vitro and in vivo. Methods: Author evaluated the suppressive effects of pegmatite on lipopolysaccharide (LPS)-stimulated nitric oxide (NO) production, TNF-${\alpha}$ and IL-6 release in the RAW 264.7 murinemacrophages. Results: Treatment of RAW 264.7 cells with pegmatite significantly reduced LPS-stimulated NO production and inflammatory cytokine such as TNF-${\alpha}$ and IL-6 secretion in a concentration-dependent manner. Also pegmatite showed topical anti-inflammatory activity in the arachidonic acid (AA)-induced ear edema and acetic acid-induced increase in capillary permeability assessment in mice. It was also found that pegmatite (10 mg per ear in DW) inhibited arachidonic acid induced edema at 24 h more profoundly than 1 h by topical application. Furthermore, the vascular permeability increase induced by acetic acid was significantly reduced in mice that received pegmatite in 50 mg per mouse. Conclusion: Therefore the results of the present study suggest that pegmatite is a potent inhibitor of the LPS-induced NO and inflammatory cytokine in RAW 264.7 macrophages and showed anti-inflammatory activities in vivo animal model.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.202-202
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• 1996

The antihistaminic action of eighteen herbal medicines was investigated by the radioligand binding and functional assays. The hexane fractions of Trichosanthis radix, Mori cortex radicis and Evodiae fructus dose-dependently inhibited [$^3$H]mepyramine binding to H$_1$ receptor and histamine-induced contraction in guinea-pig brain homogenates and isolated guinea-pig ilea, respectively. Antihistaminic action of the hexane and ethylacetate fractions of Mori cortex radicis and the hexane fraction of Evodiae fructus was more potent than their antimuscarinic action evaluated from the inhibition of [$^3$H]QNB binding and carbachol response. The ethylacetate and chloroform fractions and six known flavonoids from Scutellariae radix also inhibited histamine-induced contraction, but antihistaminic potencies of these fractions and compounds were almost identical with their antimuscarinic potencies. The hexane fractions of Mori cortex radicis and Evodiae fructus, as shown in ketotifen, inhibited selectively the increase of cutaneous vascular permeability induced by histamine. However, wogonin (SC-1) from Scutellariae radix was a nonselective inhibitor for the effect of histamine and serotonin on the vascular permeability. These results demonstrate that the hexane and ethylacetate fractions of Mori cortex radicis and the hexane fraction of Evodiae fructus have the selective histamine H$_1$ receptor blocking activities.

• Applied Microscopy
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• v.23 no.1
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• pp.77-90
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• 1993

The mechanism by which blastocysts implant to uterine endometrium has not been clearly understood. In the present study, the following question was investigated: how are hormonal levels changed and how is uterine endometrium morphologically changed? Results obtained are as follows: Concentrations of serum estradiol and progesterone were significantly increased on day 4 and 5 of pregnancy. Uterine concentrations of PGE and $PGE_{2a}$ were sharply increased on day 1 and maintained similar concentrations thereafter, reaching the maximum on day 5. Both prostaglandins (PGs) concentrations were gradually decreased thereafter. Furthermore, concentrations of PGs in implant sites were greater than those in non-implant sites. PBR (pontamine blue reaction) in uterine endometrium was positive on day 6 of pregnancy, indicating that vascular permeability was increased. Edema and changes in structure of cell components were pronounced in stroma where PBR was developed. Moreover, these were more prominent in implant sites than non-implant sites. These results suggest that uterine PGs as well as steroid hormones increase during implantation in rats and these hormones might be involved in the process of implantation by modulating vascular permeability and the fine structures of uterine endometrial cells.

• Tribology and Lubricants
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• v.15 no.3
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• pp.272-277
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• 1999

The objective of this investigation is to examine the influence of the micro catheters, which mimic the intravascular micro active endoscopes, on local pressure changes and flow rate in an arterial branch model similar to the femoral artery of human. The effects of branch to main lumen flow rate ratios and the locations of a catheter tip were found to be significant on the local pressure changes. Relatively large pressure drops and an increase in shear stress due to the obstruction effects may induce an endothelial cell damage and a change in arterial wall permeability, which have been reported to be the primary cause of the initiation of the atherosclerosis and other major vascular diseases.