• Korean Journal of Pharmacognosy
• /
• v.37 no.2 s.145
• /
• pp.74-80
• /
• 2006

We investigated the anti-inflammatory activities of unripe fruit of Citrus grandis Osbeck growing at Jeju Island, through the evaluation of their inhibitory effect on the production of inflammatory markers (IL-6, iNOS, COX, TARC and MDC) in RAW264.7 murine macrophage cells and HaCaT human keratinocyte cells. Among the sequential solvent fractions obtained from crude extract, hexane and chloroform $(CHCI_3)$ fractions showed potential inhibitory activity on the mRNA expressions of IL-6, iNOS and COX-2 at the concentration of $100\;{\mu}g/ml$ in RAW264.7 cells. Also, EtOAc fraction showed inhibitory activity on the thymus and activation-regulated chemokine (TARC)/CCL17 and macrophage-derived chemokine (MDC)/CCL22 at the concentration of $50\;{\mu}g/ml$ in HaCaT cells. These results suggest that the unripe fruit of C. grandis may have anti-inflammatory activity through the suppression of inflammatory markers (IL-6, iNOS, COX, TARC and MDC).

• YAKHAK HOEJI
• /
• v.51 no.5
• /
• pp.313-317
• /
• 2007

A series of luotonin A homologues and their aza-analogues were prepared and evaluated their inhibitory activities on COX-1 and 2 as well as their selectivities on COX-2. The aza-analogue of dimethylene-bridged homologue of luotonin A, 3,3'-dimethylene-2-(1',8'-naphthyrid-2'-yl)-4(3H)-quinazolinone (2b), exhibited strongest inhibitory activity against COX-1 and COX-2 dependent phase of prostaglandin $D_2$ generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with an $IC_{50}$ of 39.3 and $1.89{\mu}M$, respectively. Selectivity of 2b on COX-2 over COX-1 was 21 which implied 2b can be a potential lead for the development of selective COX-2 inhibitor.

• Journal of Life Science
• /
• v.21 no.12
• /
• pp.1689-1697
• /
• 2011

In this study, we investigated the anti-inflammation effect of Persicaria thunbergii (P. thunbergii) on RAW 264.7 murine macrophage cells. The anti-inflammatory activity of P. thunbergii was determined by measuring expression of the LPS-induced inflammatory proteins, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and nuclear factor-${\kappa}B$ (NF-${\kappa}B$), and the production of nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$). Methanol extract of P. thunbergii decreased the expression of iNOS, COX-2 and NF-${\kappa}B$, and increased the expression of HO-1 in LPS-stimulated RAW264.7 cells. Methanol extract was fractioned by n-butanol, hexane and ethyl acetate (EtOAc) and each fraction was tested for inhibitory effects on inflammation. Among the sequential solvent fractions, the EtOAc soluble fraction was investigated by the expression of prostaglandin $E_2$ ($PGE_2$), and showed decreasing form to the dose-dependent manner. EtOAc extract showed the most effective inhibitory activity of the expression of iNOS, COX-2 and NF-${\kappa}B$, and the production of NO. The study showed that P. thunbergii has anti-inflammatory activity through the decrease of NO and inhibition of iNOS, COX-2, $PGE_2$ and NF-${\kappa}B$ expression, and by the increase of HO-1 enzyme. This study needs for more investigation to find out the most effective single compound with anti-inflammatory activity.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2003.11a
• /
• pp.101-101
• /
• 2003

Prostaglandins (PGs) and nitric oxide (NO) produced by inducible cyclooygenase (COX-2) and nitric oxide synthase (iNOS), respectively, have been implicated as important mediators in the process of inflammation and carcinogenesis. On this line, the potential COX-2 or iNOS inhibitors have been considered as anti-inflammatory and cancer chemopreventive agents. In our continuing efforts of searching for novel cancer chemopreventive agents from natural products, we isolated natural sesquiterpenoids as potential COX-2 and iNOS inhibitors in cultured lipopolysaccharide (LPS)-activated mouse macrophage RAW 264.7 cells. Alantolactone, a natural eudesmane-type sesquiterpenoid, exhibited a potent inhibition of COX-2 (IC50 = 0.4 $\mu\textrm{g}$/$m\ell$) and iNOS activity (IC50 = 0.08 $\mu\textrm{g}$/$m\ell$) in the assay system determined by PGE2 and NO accumulation, respectively. The inhibitory potential of alantolactone on the PGE2 and NO production was well coincided with the suppression of COX-2 and iNOS protein and mRNA expression in LPS-induced macrophages. Furthermore, alantolactone inhibited NF-kB but not AP-l binding activity on nuclear extracts evoked by LPS-stimulated macrophage cells, suggesting the possible involvement of NF-kB in the regulation of COX-2 and iNOS expression. In further study with COX-2-expressing human colon HT-29 cells, alantolactone inhibited the cell proliferation, down-regulated COX-2, and inhibited the ERK phosphorylation in the early time. These results suggest that a natural sesquiterpenoid alantolactone might be a potential lead candidate for further developing COX-2 or iNOS inhibitor possessing cancer chemopreventive or anti-inflammatory activity

• Asian Pacific Journal of Cancer Prevention
• /
• v.13 no.9
• /
• pp.4453-4458
• /
• 2012

Angiogenesis plays a significant role in colorectal cancer (CRC) and cyclooxygenase-2 (COX-2) appears to be involved with multiple aspects of CRC angiogenesis. Our aim was to investigate the inhibitory effects of Tan II-A (Tanshinone II-A, Tan II-A) on tumor growth in mice, as well as alteration of expression of COX-2 and VEGF in CRC. We established the mice xenograft model of C26 CRC cell line, and injected 0.5, 1, 2mg/kg of Tan II-A and 1mg/kg of 5-FU in respectively in vivo. Then, we assayed tumor weight and volume, and evaluated microvascular density and expression of VEGF. COX-2 promoter and COX-2 plasmids were transfected into HCT-116 cells, followed by detection of COX-2 promoter activity by chemiluminescence, and detection of COX-2 mRNA expression by fluorescence quantitative PCR. Taken together, the results showed Tan II-A could inhibit tumor growth and suppress the VEGF level in vivo. HCT-116 cell experiments showed marked inhibitory effects of Tan II-A on COX-2 and VEGF in a dose-dependent manner. The results indicate that Tan II-A can effectively inhibit tumor growth and angiogenesis of human colorectal cancer via inhibiting the expression level of COX-2 and VEGF.

• Microbiology and Biotechnology Letters
• /
• v.50 no.4
• /
• pp.512-521
• /
• 2022

Since the main symptoms of COVID-19 involve the respiratory system, the infection rate of this disease is predicted to be higher in patients with other respiratory conditions such as allergic rhinitis. In such a situation, it will be meaningful to conduct research on an allergy treatment that has fewer side effects and can effectively reduce allergy symptoms. Here, we prepared experimental samples under various fermentation conditions with mixed extracts of six medicinal plants. To examine the anti-allergic efficacy of these samples, an egg albumin-induced allergic rhinitis animal model experiment, a serum histamine and IgE experiment, and a COX and LO inhibitory activity experiment were conducted. As a result of animal experiments, OVA+SP-4 showed superior efficacy compared to OVA+SP-1 in nasal rubbing and sneezing experiments and had anti-allergic efficacy similar to that of OVA-cetirizine. The serum histamine concentration of OVA+SP-4 was also 1.3 times higher than that of the OVA+cetirizine group, showing a high histamine reduction ability, and IgE showed the same trend. An analysis of COX inhibitory efficacy also confirmed that COX-1 and COX-2 inhibitory efficacy is high, and the longer the fermentation time, the higher the antiallergic efficacy. The composition proposed by this study is expected to have a significant effect on sustainable allergy prevention and treatment in the future by applying it to human patients.

• The Journal of Korean Medicine
• /
• v.29 no.5
• /
• pp.111-117
• /
• 2008

Objectives and methods : Previous mechanistic studies suggest the cyclooxygenase-2 (COX-2) inhibitors represent the good candidates against tumor progression. MeOH extract of the stem barks of Euonymus alatus induced the strong inhibition of COX-2. A phenolic compound responsible for the anti- COX-2 known to involve in tumor adhesion and invasion has been studied through the methanol extracts. The compound, rosmarinic acid (ROS-A) was an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid. ROS-A showed a strong inhibitory effect of COX-2 activity in a concentration-dependent manner. Then we have measured the IL-1${\beta}$, IL-6 and TNF-${\alpha}$ production related the immune regulation, induction of inflammatory related genes. Results and Conclusions :Hep3B cells produce proinflammatory cytokines of IL-1${\beta}$, IL-6 and TNF-${\alpha}$ while ROS A inhibited the cytokines production. Since IL-1${\beta}$, IL-6 and TNF-${\alpha}$ need the transcription factors such as nuclear factor- ${\kappa}$B (NF-${\kappa}$B) and activated protein-1 (AP-1), we measured the transcription factors. ROS-A inhibited the activation of p65, p50, c-Rel subunits of NF-${\kappa}$B and AP-1 transcription factors. These findings indicate that ROS A from the stem bark of E. alatus inhibits proliferation in metastatic cancer cells. It was suggested that stem barks of E. alatus could be suitable for anti-cancer drugs.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.20 no.2
• /
• pp.455-459
• /
• 2006

The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

• Korean Journal of Pharmacognosy
• /
• v.37 no.4 s.147
• /
• pp.235-240
• /
• 2006

We investigated the antioxidant activities such as DPPH radical scavenging capacity, xanthine oxidase inhibitory activity, and superoxide radical scavenging capacity of the aqueous EtOH extract and its solvent fractions of Artemisia scoparia. The ethyl acetate fraction showed high antioxidant activity, compared to positive controls such as ascorbic acid, butylated hydroxy anisole (BHA), trolox, and allopurinol in these assay systems. Moreover, we examined the inhibitory effect of solvent fractions of A. scoparia on the production of pro-inflammatory factors that the nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and prostaglandin E2 $(PGE_2)$ production activated with LPS $(1{\mu}g/ml)$ in murine macrophage cell line RAW264.7. The amounts of protein levels were determined by immunoblottting. Tn the sequential fractions of hexane and dichloromethane inhibited the NO and $PGE_2$ production and the protein level of iNOS and COX-2. These results suggest that A. scoparia may have anti-inflammatory activity through the antioxidant activity and inhibition of pro-inflammatory factors.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.37 no.1
• /
• pp.29-41
• /
• 2024

Objectives : The purpose of this study is to confirm the anti-inflammatory, antioxidant and anti-aging efficacy of Pyeonggangaeuljihyeol-tang(PGJT) extract. Methods : In order to confirm the anti-inflammatory activity of PGJT extract, the inhibitory effect on NO PGE₂ production were evaluated and the expression level of iNOS, COX-2 and IL-6 mRNA were measured through qRT-PCR, Antioxidant activity was evaluated for radical scavenging activity using DPPH and ABTS, anti-aging activity was evaulated for collagenase, elastase, tyrosinase and L-DOPA oxidation inhibitory activity. Results : PGJT extract shows anti-inflammatory effect by inhibiting the production of NO and PGE₂ by reducing the expression level of iNOS, COX-2 and IL-6 mRNA, antioxidant effect by increasing DPPH and ABTS scavenging abillity in a concentration dependent manner. In addition, the anti-aging effect was confirmed by inhibiting collagenase, elastase, tyrosinase production and L-DOPA oxidation. Conclusion : This suggests that PGJT showed an overall excellent anti-inflammatory effect and an inhibitory effect on the activity of antioxidant and anti-aging related enzymes.