• Archives of Pharmacal Research
• /
• 제20권4호
• /
• pp.372-374
• /
• 1997

In order to develop new anti-inflammatory agents having different action mechanisms compared with nonsteroidal and steroidal anti-inflammatory drugs, the culture broths of various actinomycetes isolated from soil were screened using an in vivo mouse ear edma assay and one strain (Streptomyces sp. MT 2705-4: KCTC 8651 P) was selected. Activity-guided purification led to the isolation of a polyether compound, dianemycin. Topically, dianemycin showed a potent anti-inflammatory activity in mouse ear edema induced by croton-oil or arachidonic acid.$ED_{50}$value of dianemycin was found to be 0.8 mg,/ear compared to 0.4 mg/ear of prednisolone in croton-oil ear edema. However, dianemycin did not show the inhibitory activity in UV-erythema and delayed hypersensitivity reaction. These results indicate that dianemycin is a potential topical anti-inflammatory agent.

• 동아시아식생활학회지
• /
• 제22권6호
• /
• pp.772-781
• /
• 2012

This study was conducted to examine the development of a new anti-inflammatory substance with potent anti-inflammatory activities that was derived from the Platycodi Radix butanol fraction. To accomplish this, the chemical structures and anti-inflammatory activities of the components were elucidated. Upon column chromatography of the tertiary subfraction, fractions 8-4-1 and 8-4-2 were identified as platycodin D and D3, respectively, following recrystallization, based on melting point (MP), infrared (IR), and positive fast atom bombardment (FAB)-mass and nuclear magnetic resonance (NMR) spectral data. Platycodin D and D3 exhibited strong anti-inflammatory activities in rats when administerd at oral doses of 12 mg/kg and 36 mg/kg, p.o., respectively. Platycodin D and D3 induced inhibitory effects on capillary vascular permeability in rats at oral doses of 16 mg/kg and 24 mg/kg, p.o., respectively, and potent inhibition of leukocyte emigration in a carboxymethyl cellulose (CMC)-pouch when administered at doses of 3 mg/rat and 7 mg/rat, s.c., respectively. These results verified the high antiinflammatory potency of the platycodin D and D3 components in Platycodi Radix.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.213.1-213.1
• /
• 2003

Alpha-viniferin was isolated from Carex humilis (Cyperaceae), and showed anti-inflammatory effects on carrageenin or histamine-induced paw edema in mice. To understand mode of the anti-inflammatory action. effects of alpha-viniferin on cyclooxygenase (COX)-2, iNOS, oxygen radicals and proinflammatory cytokines have been analyzed. Alpha-viniferin showed selective inhibitory effect with an IC50 value of 5 $\mu\textrm{m}$ on COX-2 activity but showed weak inhibitory effect on the synthesis of COX-2 transcript which was identified by RT-PCR. (omitted)

• Journal of Pharmaceutical Investigation
• /
• 제36권4호
• /
• pp.253-262
• /
• 2006

This study was performed to investigate the effects of treatment for dermatitis using the herbal gel preparations. Scutellariae Radix(SR) and Zingiberis Rhizoma(ZR) were used for the purpose of herbal preparations. Baicalin, baicalein are the ingredients of SR, having biological effects like anti-inflammatory, anti-oxidative, anti-bacterial and antiallergic action. 6-Gingerol is one of the ingredients of ZR having biologicai effects like anti-inflammatory and analgesic action. The three types of hydrogels(SRE, SRH, SZH) were formulated with Carbopol 940, Labrasol, Triethanolamine etc. Baicalin was hydrolysed to baicalein by $\beta$-glucuronidase for the purpose to increase rate of skin permeation. Content of ingredients by HPLC determination, rate of skin permeation using Franz type diffusion cell, anti-oxidative activity for the free radical, hydroxyl radical, superoxide, anti-inflammatory by using carrageenan injection, efficacy on the dermatitis induced by 2,4-dinitro-chlorobenzene(DNCB) were experimented. Baicalein showed higher permeability than baicalin, so it is considered that baicalein was more suitable form than baicalin for transdermal absorption by its lipophilic property. In the anti-oxidative experiments, SZH gel was the most effective scavenging activity than the other gels in all experiments. In anti-inflammatory test, SRM and SZH gel more decreased edma rapidly than SRE gel. In case of using SZH gel, treatment period for the dermatitis was more declined than that of other gel groups. These results suggests that the SZH hydrogel could be suitable preparations for the treatment of dermatitis.

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2001년도 International Symposium on Signal transduction in Toxicology
• /
• pp.14-21
• /
• 2001

Many epidemiological studies have revealed that the use of aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs) can reduce the risk of colon cancer. Since the well-documented pharmacological action of aspirin and other NSAIDs is the inhibition of cyclooxygenase [COX, the rate-limiting enzyme in prostaglandin (PG) biosynthesis], it has been inferred that the beneficial effect of NSAIDs may be mediated through the inhibition of PG biosynthesis.(omitted)

• Molecules and Cells
• /
• 제26권1호
• /
• pp.48-52
• /
• 2008

We here demonstrate an anti-inflammatory action of raloxifene, a selective estrogen receptor modulator, in lipopolysaccharide (LPS)-induced murine macrophage RAW264.7 cells. Treatment with raloxifene at micromolar concentrations suppressed the production of nitric oxide (NO) by down-regulating expression of the inducible nitric oxide synthase (iNOS) gene in LPS-activated cells. The decreased expression of iNOS and subsequent reduction of NO were due to inhibition of nuclear translocation of transcription factor NF-${\kappa}B$. These effects were significantly inhibited by exposure to the phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor, LY294002, or by expression of a dominant negative mutant of PI 3-kinase. In addition, pretreatment with raloxifene reduced LPS-induced Akt phosphorylation as well as NF-${\kappa}B$ DNA binding activity and NF-${\kappa}B$-dependent reporter gene activity. Thus our findings indicate that raloxifene exerts its anti-inflammatory action in LPS-stimulated macrophages by blocking the PI 3-kinase-Akt-NF-${\kappa}B$ signaling cascade, and eventually reduces expression of pro-inflammatory genes such as iNOS.

• 대한한방소아과학회지
• /
• 제30권2호
• /
• pp.96-106
• /
• 2016

Objectives The purpose of this study is to investigate the effects of Gleditsiae Fructus 70% EtOH extract (JS_E) on anti-inflammatory action in HaCaT cells (A spontaneously immortalized human keratinocyte cell line) and inhibiting triglyceride genesis in SEB-1 cells (Immortalized human sebocyte). Methods The anti-inflammatory effect of JS_E was analyzed by enzyme-linked immunosorbent assays (ELISA) which measured levels of IP-10, RANTES and MDC in HaCaT cells. Also the effect on secretion of sebum of JS_E was analyzed by TG-S kit which measured the quantity of triglyceride in SEB-1 cells. Results JS_E inhibited IP-10, RANTES and MDC expression in a dose dependent manner. IP-10 expression was inhibited significantly in comparison to TNF-${\alpha}$ and IFN-${\gamma}$ recombination (TI) control group at concentration of JS_E $200{\mu}g/ml$ and RANTES and MDC expressions were inhibited significantly at concentration of JS_E 100, $200{\mu}g/ml$. JS_E also inhibited triglyceride secretion of SEB-1 cells significantly in comparison to the control group in a dose dependent manner. Conclusions This study shows that JS_E has the effects of anti-inflammatory action and inhibiting sebum secretion. According to these results, JS_E can be used for treating skin diseases such as acne and dermatitis caused by inflammation and excessive secretion of sebum by controlling the activity of the HaCaT and SEB-1 cells.

• 한국자원식물학회지
• /
• 제19권6호
• /
• pp.660-664
• /
• 2006

The aerial part of Siegesbeckia pubescens (Compositae) has been used to treat rheumatoid arthritis and hypertension in the Oriental medicine. This crude drug has been used without process (SP-0) or with three times-process of steaming and drying (SP-3) or the nine times of that process (SP-9). To search for the antinociceptive anti-inflammatory components from this crude drug, activity-directed fractionation was performed on this crude drug. Since the $CHCl_3$ extract was shown to have a more potent effect than other extracts, it was subjected to silica gel & ODS column chromatography to yield two diterpene compounds (1). Compound 1 was structurally identified as ent-16 (H, 17-hydroxykauran-19-oic acid, which were tentatively named siegeskaurolic acid A. A main diterpene, siegeskaurolic acid A was tested for the antiiflammatory antinociceptive effects using both hot plate- and writhing anti-nociceptive assays and carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with siegeskaurolic acid A (20 and 30mg/kg) significantly reduced the stretching episodes, action time of mice and carrageenan-induced edema. These results support that siegeskaurolic acid is a main diterpene responsible for antinociceptive and antiiflammatory action of S. pubescens. In addition, the assays on SP-0, SP-3 and SP-9 produced the experimental results that SP-9 had more significant effects than other two crude drugs. These results suggest that the processing on the original plant may lead to the higher pharmacological effect.

• 생약학회지
• /
• 제45권1호
• /
• pp.23-27
• /
• 2014

Atopic dermatitis (AD) were caused by localized hypersensitivity reaction to an allergen. Therefore, to reduce inflammatory response of AD had been developed that natural extracts and oils with anti-inflammatory activities. This study were investigated that anti-inflammatory effects of Malva verticillata L. oil induced by LPS with RAW 264.7 cells. We measured to production of NO and expression of COX-2, iNOS, TNF-${\alpha}$ by RT-PCR. The Malva verticillata L. oil had decreased the production of NO (p<0.05) and the mRNA level of iNOS in concentration dose dependent manner. In conclusion, this study have shown here may be of help to understand the action mechanism of the anti-inflammatory and we hope that Malva verticillata L. oil used in skin diseases such as AD.

• Biomolecules & Therapeutics
• /
• 제23권5호
• /
• pp.414-420
• /
• 2015

Flavonoids, such as fisetin (3,7,3',4'-tetrahydroxyflavone), are plant secondary metabolites. It has been reported that fisetin is able to perform numerous pharmacological roles including anti-inflammatory, anti-microbial, and anti-cancer activities; however, the exact anti-inflammatory mechanism of fisetin is not understood. In this study, the pharmacological action modes of fisetin in lipopolysaccharide (LPS)-stimulated macrophage-like cells were elucidated by using immunoblotting analysis, kinase assays, and an overexpression strategy. Fisetin diminished the release of nitric oxide (NO) and reduced the mRNA levels of inducible NO synthase (iNOS), tumor necrosis factor (TNF)-${\alpha}$, and cyclooxygenase (COX)-2 in LPS-stimulated RAW264.7 cells without displaying cytotoxicity. This compound also blocked the nuclear translocation of p65/nuclear factor (NF)-${\kappa}B$. In agreement, the upstream phosphorylation events for NF-${\kappa}B$ activation, composed of Src, Syk, and I${\kappa}B{\alpha}$, were also reduced by fisetin. The phospho-Src level, triggered by overexpression of wild-type Src, was also inhibited by fisetin. Therefore, these results strongly suggest that fisetin can be considered a bioactive immunomodulatory compound with anti-inflammatory properties through suppression of Src and Syk activities.