• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.291-297
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• 2002

For preventing and curing the stretching mark, TECA Niosome/W/O system creams were formulated using Titrated Extract of Centella Asiatica (TECA) which is well known for its excellent wound healing effect. The lipid-water partition coefficients and the stabilities of TECA were evaluated and TECA Niosome/W/O system (TECA N/W/O) creams were prepared with different concentrations of cetyl alcohol and ceramide. TECA N/W/O cream was evaluated with respect to their rheological properties, permeation through excised skin of hairless mouse and in vitro and in vivo accumulation in the skin of hairless mouse. In addition, dermal thicknesses of hairless mouse skins were determined following the in vivo application of TECA N/W/O cream and control cream. TECA N/W/O creams showed pseudoplastic flow and hysteresis loop. The permeation of TECA from formulations through excised skin of hairless mouse did not observed. Amount of accumulated drug in the excised skin of hairless mouse was deσeased with an increase in the concentration of cetyl alcohol and showed no relationship with concentration of ceramide. Amount of accumulated drug in formulation A-3 was higher than in niosome suspension and other formulations. In in vivo experiment, amount of accumulated drug in formulation A-2 and A-3 was much higher than that of niosome suspension. Being treated with the N/W/O cream for 8 weeks, the dermal thickness of hairless mouse skin was increased 3.2 times than that of 16 weeks-control group.

• Korean Journal of Veterinary Research
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• v.44 no.2
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• pp.251-257
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• 2004

This study was designed to determine optimal condition for expression of cloned Shigatoxin2e(Stx2e) gene from transformed E. coli PED18, to compare the cytotoxicity titer between cloned Stx2e and Stx2e from original strain, and to confirm of receptor binding affinity of Stx2e for use of development of receptor binding ELISA to detect of Stx2e. The optimum composition of medium for expression of Stx2e gene in E.coli host-vector system was definded as the medium containing 0.5% glucose and 0.5 mM IPTG. The cytotoxicity titer of expressed Stx2e for Vero cell was 1000 fold higher than that of Stx2e from original strain AY93258. The binding affinity of Stx2e to receptor globotetraosyl ceramide($Gb_4$) was confirmed by immunobloting.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.24 no.3
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• pp.6-16
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• 1998

Ceramides are currently emerging as the major skin care ingredients due to !heir barrier properties in the stratum corneum of the human skin. Thus, major cosmetic companies have developed synthetic ceramide analogs for their own use. In this study, several ceramide mimic compounds , new skin barrier lipids, were designed and synthesized, and their physical and biological properties were investigated to evaluate their skin care capability. Several structures were designed from the variation of hydrophobic alkyl chain and hydrophilic moiety by the use of molecular modeling software. The selected targets were synthesized, and their properties and activities were studied as the pure form, in the emulsion, or in the lamellar mixture containing cholesterol and fatty acid. Some compounds, such as 1,3-bis(N-(2-hydroxyethyl)-palmitoylamino)-2-hydroxypropane, enhanced the restoration of skin barrier damaged by SDS(sodium dodecyl sulfate), and by acetone treatment. The rate of restoration was comparable to that of natural ceramides. The synthesized compounds alleviated SDS induced skin irritation and facilitated lamellar phase liquid crystal formation. The treatment of 1,3-Dis(N-(2-hydroxyethyl)-palmitoylam ino)-2-hyd roxypropane on the acetone damaged skin revealed that the compound promoted the recovery of intercellular lipid lamellar structure of stratum corneum layer. The replacement of palmitoyl groups of the compound with shorter alkyl chain gave lower emulsion viscosity and liquid crystal density, suggesting easier formulation and poorer barrier activity. Most of the synthesized compounds were non-irritable in various toxicological tests proving that they can be safely introduced to the skin care formulations.

• YAKHAK HOEJI
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• v.41 no.6
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• pp.789-796
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• 1997

The purpose of this study was to determine the effect of sulfinpyrazone on fumonisin $B_1$-induced elevation of free sphingoid bases in LLC-$PK_1$ cells. Fumonis ins are a family of mycotoxins produced by the fungi Fusarium moniliforme which is common contaminant in corn. Fumonisins are also potent inhibiors of sphingosine and sphinganine N-acyltransferases (ceramide synthases), key enzymes in sphingolipid metabolism resulting in the elevation of free sphinganine. The cytosolic concentration of fumonisin B1 was known to be closely proportional to the elevation of free sphinganine in LLC-PK1 cells [Yoo, H.-S., Norred, W.P., Wang, E., Merrill, A.H., Jr., and Riley, R.T. (1992) Toxicol. Appl.Pharmacol. 114. 9-15]. Sulfinpyrazone, an anion transport inhibitor, reduced the elevated level of free sphinganine resulting from fumonisin B1 inhibition of de novo sphingolipid biosynthesis. Fumonisin B1 at a concentration of 20${\mu}$M showed approximately 120pmol/$10^6$ cells relative to 3-10pmol/$10^6$ cells in control cultures, and sulfinpyrazone at a concentration of 200${\mu}$M partially reversed the increased level of free sphinganine induced by fumonisin $B_1$ down to normal level after exposure to fumonisin $B_1$ for 8 to 24hr. However, the reduced effect of sulfinpyrazone on the fumonisin $B_1$-induced elevation of intracellular sphinganine was not shown after 24hr. Fumonisin $B_1$ exposure to LLC-PK1 cells for 36 and 48hr showed approximately 74 and 80pmol per $10^6$ cells relative to 82 and 76pmol,respectively, in fumonisin $B_1$ plus sulfinpyrazone-treated cultures. Sulfinpyrazone-induced less elevation of free sphinganine in confluent cells after exposure to fumonisin $B_1$ suggested that either sulfinpyrazone may block the availability of fumonisin $B_1$ to cells or act on the fumonisin $B_1$ interaction with ceramide synthase.

• Bulletin of the Korean Chemical Society
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• v.28 no.6
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• pp.1021-1030
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• 2007

The effects of the creamide III (CER3) and cholesterol (CHOL) on the structure of a non-hydrous distearoyl phosphatidylcholine (DSPC)-based lamellar liquid crystal (LC) hydrated by only propylene glycol (PG) without water were investigated by differential scanning calorimetry (DSC), X-ray diffractions (XRDs), and polarized microscope (PM). As soon as CER3 was incorporated into the lamellar phase, the characteristic LPP was appeared as well as the characteristic SPP, and the formation of separated CER3 crystalline phase was observed depending upon the increase of CER3 content by XRDs. Also, by DSC, it was shown that the increase of CER3 made the monotectic thermal transition be changed to the eutectic thermal transition which indicates the formation of separated CER3 crystalline phases and the main transition temperatures (Tc1) to be gradually decreased and the enthalpy change (ΔH) to be linearly increased. Incorporating CHOL, the formation of LPP and SPP showed almost similar behaviors to CER3, but incorporating small amounts of CHOL showed the characteristic peaks of CHOL which meant the existence of crystalline CHOL phase due to the immiscibility of CHOL with DSPC swollen by PG differently from CER3, and increasing CHOL made the intensity of the 1st order diffraction for LPP weakened as well as the intensities of the characteristic diffractions for DSPC. Also, in the results of DSC, it showed more complex thermal behaviors having several Tc than CER3 due to its bulky chemical structure. In the present study, the inducement of CER3 and CHOL as other lipids present in human stratum corneum (SC) into a non-hydrous lamellar phase is discussed in terms of the influence on their structural and thermal transition.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.20 no.1 s.32
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• pp.99-114
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• 2007

Objectives : Atopic dermatitis has a close relationship with damage of skin barrier function. To investigate the effects of Bangpungtongsungsan(BT) extract to the skin damage on mice model after atopic dermatitis elicitation, this study was done through forcing injury to mice's skin. Methods : The BALB/c mice were distributed into three groups: control(CON) group, atopic dermatitis(AD)-elicited group, Bangpungtongsungsan(BT)-treated group. AD-elicited and BT-treated group were caused AD according to the method of Christophers E., Mrowietz and Minehiro. The BT extract was administered for 48 hours to BT-treated group. We observed changes of external dermal formation, eosinophils in vasculature, lipid formation in stratum corneum, distribution of ceramide, distribution of capillary, $I{\kappa}B$ kinase(IKK) and induce nitric oxide synthase(iNOS) mRNA expression. We used the statistical methods of student t-test(p<0.05). Results : After dispensing BT extract into the AD-elicited group, the number of eosinophil as an atopic index in mice noticeably decreased and dermal injury decreased. Also the decrease of hyperplasia, degranulated mast cells, angiogenesis and substance P were shown. The lipid lamellae, lipid protect formation, were repaired and the distribution of ceramide which inhibit protein kinase C(PKC) activation increased, and the PKC caused inhibition of nuclear $factor(NF)-{\kappa}B$ activation. As a result of inhibition of $NF-{\kappa}B$ activation, iNOS production were inhibited and apoptotic cell were increased. Moreover the decrease of IKK and iNOS mRNA expression in BT-treated RAW 264.7 cell were noted. Conclusion : BT mitigated skin damage on mice model after atopic dermatitis elicitation through recovering skin barrier function and inhibiting nuclear $factor(NF)-{\kappa}B$ activation.

• Animal Bioscience
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• v.35 no.9
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• pp.1444-1453
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• 2022

Objective: Acetate plays an important role in host lipid metabolism. However, the network of acetate-regulated lipid metabolism remains unclear. Previous studies show that mitogen-activated protein kinases (MAPKs) and mechanistic target of rapamycin (mTOR) play a crucial role in lipid metabolism. We hypothesize that acetate could affect MAPKs and/or mTOR signaling and then regulate lipid metabolism. The present study investigated whether any cross talk occurs among MAPKs, mTOR and acetate in regulating lipid metabolism. Methods: The ceramide C6 (an extracellular signaling-regulated kinases 1 and 2 [ERK1/2] activator) and MHY1485 (a mTOR activator) were used to treat rabbit adipose-derived stem cells (ADSCs) with or without acetate, respectively. Results: It indicated that acetate (9 mM) treatment for 48 h decreased the lipid deposition in rabbit ADSCs. Acetate treatment decreased significantly phosphorylated protein levels of ERK1/2 and mTOR but significantly increased mRNA level of hormone-sensitive lipase (HSL). Acetate treatment did not significantly alter the phosphorylated protein level of p38 MAPK and c-Jun aminoterminal kinase (JNK). Activation of ERK1/2 and mTOR by respective addition in media with ceramide C6 and MHY1485 significantly attenuated decreased lipid deposition and increased HSL expression caused by acetate. Conclusion: Our results suggest that ERK1/2 and mTOR signaling pathways are associated with acetate regulated HSL gene expression and lipid deposition.

• The Korea Journal of Herbology
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• v.38 no.3
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• pp.19-26
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• 2023

Objectives : Agrimoniae Herba is a herbal medicine widely distributed in Asia and contains flavonoids including catechin, quercitrin, rutin, hyperoside, and quercetin. This study aimed to investigate the anti-oxidant activity and skin barrier function of different solvent fractions (Hexane; methylene chloride, MC; ethyl acetate, EA; n-butanol, Bu; Water) obtained from Agrimoniae Herba. Methods : Anti-oxidant activity of different solvent fractions obtained from Agrimoniae Herba was investigated through total polyphenol contents, total flavonoid contents, 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity measurements. Then, filament aggregating protein (Filaggrin), Type I collagen, ceramide synthase (CERS) 3, and CERS4 were analyzed to evaluate the skin barrier strengthening effect of different solvent fractions obtained from Agrimoniae Herba on UVB-stimulated HaCaT cells. Results : As a result of measuring total polyphenol contents, total flavonoid contents, DPPH free radical scavenging activity, and ABTS radical scavenging activity, antioxidant activity was found to be excellent in the order of EA > Bu > MC > Hexane > Water. As a result of measuring mRNA gene expression of Type I collagen, Filaggrin, CERS3, and CERS4 after UVB-stimulated was applied to HaCaT cells treated with different solvent fractions obtained from Agrimoniae Herba, it was found to increase significantly in the Bu-treated group. Conclusion : Our findings show that the Bu sample obtained from Agrimoniae Herba has excellent anti-oxidant ability, which increases Type I collagen, Filaggrin, and ceramide synthetase in UVB-stimulated HaCaT cells to control the skin barrier improvement effect.

• Biomolecules & Therapeutics
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• v.22 no.2
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• pp.83-92
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• 2014

Fatty acids (FAs) are highly diverse in terms of carbon (C) chain-length and number of double bonds. FAs with C>20 are called very long-chain fatty acids (VLCFAs). VLCFAs are found not only as constituents of cellular lipids such as sphingolipids and glycerophospholipids but also as precursors of lipid mediators. Our understanding on the function of VLCFAs is growing in parallel with the identification of enzymes involved in VLCFA synthesis or degradation. A variety of inherited diseases, such as ichthyosis, macular degeneration, myopathy, mental retardation, and demyelination, are caused by mutations in the genes encoding VLCFA metabolizing enzymes. In this review, we describe mammalian VLCFAs by highlighting their tissue distribution and metabolic pathways, and we discuss responsible genes and enzymes with reference to their roles in pathophysiology.

• The Journal of Pediatrics of Korean Medicine
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• v.22 no.3
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• pp.63-73
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• 2008

Objectives : The purpose of this study is to analyze the baby moisturizers and give information about basis of herbal moisturizer. Methods : We selected 243 goods by searching with keywords as "baby moisturizer" at 6 major web search engines, 12 web shopping malls in Korea. 10 items were evaluated under three evaluation criteria such as type of product, ingredient and function of goods. Results : Study resulted that the most type of moisturizers were lotion type. 80% of the products contained medical agents. Ingredients of medical agents were herbal medicine, aroma oil, vitamin and extract. The moisturizer for atopic dermatitis contained ceramide about half. The ingredient of herbal medicine existed usually as excipients, not as active ingredient. Conclusion : It is necessary to study and develop new products contained herbal medicine as active ingredient based on the oriental medical theory.