• Korean Journal of Pharmacognosy
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• v.35 no.2 s.137
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• pp.147-151
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• 2004

Water extracts from Thesium chinense Tunczaninov (TCTW) and Prunella vulgaris L. (PVW) were tested for aromatase and cyclooxygenase activities. TCTW and PVW were capable of suppressing aromatase in a human placenta microsomal assay. PVW was shown to be more effective than TCTW in the suppression of aromatase activity. TCTW significantly inhibited cyclooxygenase-2 (COX-2) activity at the concentration of 0.25 (p<0.05), 0.5 (p<0.01) and 2.5 mg/ml (p<0.005). PVW also inhibited COX-2 activity in a dose-dependent manner in a concentration range of $0.05{\sim}2.5\;mg/ml$. The expression of COX-2 was inhibitied by TCTW and PVW in western blot analysis. These results suggest that TCTW and PVW may have breast cancer chemopreventive potentials by inhibiting aromatase and cyclooxygenase activities.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.137-138
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• 2001

There has been accumulating evidence for the association of inflammatory tissue damage with the process of cancer development. Cyclooxygenase (COX), an important enzyme involved in mediating the inflammation, catalyzes the formation of prostaglandins (PGs) from arachidonic acid. There are two isoforms of COX, designated as COX-l and COX-2. COX-l is a housekeeping enzyme which is constitutively expressed and is thought to be involved in maintaining physiological functions.(omitted)

• Journal of Applied Biological Chemistry
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• v.66
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• pp.114-121
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• 2023

Selective cyclooxygenase (COX)-2 inhibition is a novel strategy to reduce the risk of gastrointestinal side effects caused by conventional nonsteroidal anti-inflammatory drugs. However, some selective COX-2 inhibitors have become apparent to increase the risk of severe cardiovascular disease. The aim of this study was to examine the anti-inflammatory effect of rosemary extract (RE) and confirm the safety of cardiovascular side effects. Inhibition of COX enzyme activity was assessed, and the levels of COX-2 and prostaglandin E₂ (PGE₂) and COX-1 and thromboxane B₂ (TXB₂) were evaluated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. The 40% RE group showed increased COX-2 inhibition activity in a dose-dependent manner, whereas the 50% RE group only exhibited at 100 ㎍/mL. In a cell-based study, COX-2 mRNA expression was similar in both RE groups and PGE₂ levels tended to decrease in the 40% RE group compared to the LPS group in the LPS pretreatment condition. In the LPS posttreatment condition, the COX-2 mRNA expression decreased in the 40% RE group, and PGE₂ levels were increased in the 40 and 50% RE groups. In both conditions, there was no significant difference in COX-1 and TXB₂ levels. In conclusion, 40 and 50% RE showed significant COX-2 inhibition, similar to the positive control group. It was confirmed that the inhibition of the COX-2 expression, but the effect did not affect the balance between prostacyclin and TXB₂. These results indicate that rosemary showed COX-2 inhibition activity with a low risk of cardiovascular diseases.

• Korean Journal of Medicinal Crop Science
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• v.22 no.4
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• pp.262-269
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• 2014

Complex of mulberry extract (CME) is composed of extracts of mulberry (Morus alba L.) fruit, mulberry leaves and black beans (Glycine max (L.) Merr.). In this study, we investigated prevention effects of CME on degenerative arthritis. The $SC_{50}$ value of DPPH radical scavenging by CME was $158.49{\pm}11.35{\mu}/mL$. We found that CME significantly reduced the production of nitric oxide (NO) and protein expression of cyclooxygenase-2 (COX-2) in RAW 264.7 cells which were activated by LPS. Experiments using animal model of degenerative arthritis showed that CME (400 mg/kg body weight) inhibited the production of TNF-${\alpha}$ (77.5%) and IL-$1{\beta}$ (95.0%). Furthermore, it was observed that CME reduced to 85.9% of paw edema induced by carrageenan. These results suggest that CME could improve degenerative arthritis.

• Biomolecules & Therapeutics
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• v.8 no.1
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• pp.73-77
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• 2000

Rheum undulatum L. has been used as Rhei Radix in Korean Pharmacopea although their pharmacological effects were not studied much. In this studym, we tested anti-inflammatory effect as a representative activity of Rheum undulatum L. extracts using cyclooxygenase (COX)-2 inhibition. Murine macrophage, Raw 264.7 cells were incubated with lipopolysaccharide (1 $\mu\textrm{g}$/ml) to induce COX-2. The prostagladin $E_2$ ($PGE_2$) levels as an indicator of COX-2 activity were determined in the culture medium using ELISA. Inhibition of acetylsalicylic acid (ASA) as a standard, aloe-emodin, chrysophanol, rhein, 80% ethanol extract of Rheum undulatum L. (Ex) and ether fraction (Fr) after acid hydrolysis of Rheum undulatum L. were tested in induced COX-2 described above. $IC_{50}$ values were 0.082 $\mu\textrm{g}$/ml for ASA. 181 $\mu\textrm{g}$/ml for aloe-emodin, 3.65 $\mu\textrm{g}$/ml for emodin, 144 $\mu\textrm{g}$/ml for chrysophanol, 39.8 $\mu\textrm{g}$/ml for rhein, 141 $\mu\textrm{g}$ of herb/ml for Ex, and 95.7 $\mu\textrm{g}$ of herb/ml for Fr. We found that Ex and Fr of Rheum undulatum L. were more effective than other anthraquinones, since their $IC_{50}$ are lower than others.

• The Korean Journal of Pain
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• v.35 no.3
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• pp.261-270
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• 2022

Background: The rostral ventromedial medulla (RVM) is a critical region for the management of nociception. The RVM is also involved in learning and memory processes due to its relationship with the hippocampus. The purpose of the present study was to investigate the molecular mechanisms behind orexin-A signaling in the RVM and hippocampus's effects on capsaicin-induced pulpal nociception and cognitive impairments in rats. Methods: Capsaicin (100 g) was applied intradentally to male Wistar rats to induce inflammatory pulpal nociception. Orexin-A and an orexin-1 receptor antagonist (SB-334867) were then microinjected into the RVM. Immunoblotting and immunofluorescence staining were used to check the levels of cyclooxygenase-2 (COX-2) and brain-derived neurotrophic factor (BDNF) in the RVM and hippocampus. Results: Interdental capsaicin treatment resulted in nociceptive responses as well as a reduction in spatial learning and memory. Additionally, it resulted in decreased BDNF and increased COX-2 expression levels. Orexin-A administration (50 pmol/1 µL/rat) could reverse such molecular changes. SB-334867 microinjection (80 nM/1 µL/rat) suppressed orexin's effects. Conclusions: Orexin-A signaling in the RVM and hippocampus modulates capsaicin-induced pulpal nociception in male rats by increasing BDNF expression and decreasing COX-2 expression.

• Archives of Pharmacal Research
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• v.29 no.3
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• pp.209-212
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• 2006

We investigated the effect of protein extract of Asterina pectinifera on the activity of 4 enzymes that may playa role in adenocarcinoma of the colon: quinone reductase (QR), glutathione Stransferase (GST), ornithine decarboxylase (ODC), and cyclooxygenase (COX)-2. QR and GST activity increased in HT-29 human colon adenocarcinoma cells increased that had been exposed to 4 concentrations of the protein extract (80, 160, 200, and $240{\mu}g/mL$). Additionally, 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ODC activity decreased significantly in cells exposed to the extract in concentrations of $160{\mu}g/mL$ (p<0.05), $200{\mu}g/mL$ (p<0.005), and $240{\mu}g/mL$ (p<0.005). TPA-induced COX-2 activity also decreased in cells exposed to extract concentrations of 10, 20, 40, and $60{\mu}g/mL$. COX-2 expression was also inhibited in cells exposed to this extract. These results suggest that this protein extract of A pectinifera has chemopreventive activity in HT-29 human colon adenocarcinoma cells, and therefore, may have the potential to function as a chemopreventive agent in human colorectal cancer.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.322.3-323
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• 2002

Curcumin derived from turmeric (Curcuma longa L.. Zingiberaceae) has been shown to possess marked chemopreventive activities, but the underlying molecular mechanisms remain unclear. In the present work. curcumin was found to inhibit 12-Ο-tetradecanoylphorbol-13-acetate(TPA)-induced expression of cyclooxygenase-2 (COX-2) in female ICr mouse skin as determined by Western and Northern blot analysis as well as immunohistochemical staining. Curcumin treatment atlenuated TPA-stimulated epidermal NF-${\kappa}$B activation. which was associated with its blockade of degradation and phosphorylation of the inhibitory protein l${\kappa}$ Bu and also of subequent translocation of the p65 subunut to nucleus. (omitted)

• Advances in Traditional Medicine
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• v.9 no.1
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• pp.74-82
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• 2009

Pharmacological investigations were carried out with aqueous methanolic extract (AME) of Swietenia mahagoni (L.) Jacq. (Meliaceae) leaves. Acute toxicity studies revealed that the $LD_{50}$ dose of AME was 600 mg/kg, i.p. AME was found to possess significant anti-inflammatory activity in acute, sub-chronic and chronic models of inflammation. AME selectively inhibited cyclooxygenase (COX)-2 activity, which is involved in arachidonic acid metabolism and biosynthesis of prostaglandins under inflammatory conditions. Treatment with AME significantly enhanced total peritoneal cell count and the number of macrophages in normal mice, which revealed that AME may also alter the immune response along with its anti-inflammatory effect. The saponins or the alkaloids present in AME may be responsible for the anti-inflammatory activity.

• The Korean Journal of Physiology and Pharmacology
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• v.10 no.3
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• pp.161-165
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• 2006

NO and cyclooxygenase-2 (COX-2) are contributes to vascular inflammation induced by various stimulation. The mechanism, which explains a linkage between NO and COX-2, could be of importance in promoting pathophysiological conditions of vessel. We investigated the effects of NO donors on the COX-l and COX-2 mRNA/protein expression, as well as the nitrite production in culture medium of vascular smooth muscle cell (VSMC). VSMC was primarily cultured from thoracic aorta of rat. In this experiments, COX-l and COX-2 mRNA/protein expressions were analysed and nitrite productions were investigated using Griess reagent. VSMC did not express COX-2 protein in basal condition (Nonlipopolysaccharide (LPS) stimulated). In LPS-stimulated experiments, after 3 hours of NO donor pretreatment, LPS $10{\mu}g/ml$ was treated for 24 hours. COX-l protein expressions were unchanged by SNP and NOR-3. NOR-3 significantly increased COX-2 mRNA/protein expression under LPS stimulation. In contrast, SNP did not increase COX-2 mRNA/protein expression under LPS stimulation. Nitrite production was higher in NOR-3 treatment than SNP treatment under LPS stimulation. These results suggest that the expression of COX-2 in VSMC is regulated by NOR-3, COX-2 expressions were depending on the types of NO donor and LPS stimulation in VSMC.