• Proceedings of the PSK Conference
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• 2002.10a
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• pp.347.4-348
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• 2002

Recently it has been demonstrated that selective cyclooxygenase-2 (COX-2) inhibitors retain the antiinflammatory effect but with markedly reduced GI toxicity compared to non selective inhibitors such as traditional NSAIDs. As a consequence, intense efforts have been made to develop selective COX-2 inhibtors during the last decade. Two compounds in this class. celecoxib and rofecoxib. are already in the market and are proved as potent and selective COX-2 inhibitors with much better gastric tolerance. However. there are still strong domands for a COX-2 inhibitor with improved efficacy and safety profiles. Here we report the synthesis and biological profiles of 1.5- and 4.5-disubstituted imidazole analogues as structural equivalents of cefecoxib and refecoxib. The imidazole analogues are overlapped well whth the 3D srructures of celecoxib and rofecoxib.

• Journal of Pharmaceutical Investigation
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• v.26 no.3
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• pp.155-168
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• 1996

The active site of cyclooxygenase was modeled by complementary receptor-cavity mapping procedure using 3D structures of the non-steroidal antiinflammatory drugs (NSAIDs). A total of 50 NSAIDs were chosen as data ligands which compete the same site on the enzyme. Partial atomic charges were estimated, and the energetic differences for various conformations were calculated so as to meet the need for a most efficient overlapping of the probably-equivalent functional groups of the ligand molecules. The structure activity relationships of the NSAIDs, if available, were fully considered throughout the modeling. The overall shape of the model obtained is similar to a boot-without-bottom. Most of inner surface of the cavity appeared as hydrophobic; two polar counterparts except the carboxyl-binding position were found. By this model, some clear explanations could be given on the experimental observations which were not satisfiably understood yet.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.74-74
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• 1997

Chicory is used popularly. We use leaves of the plant as ordinary mea1, and roots as a substitute of tea materials. It also has been asserted that it has clinical effects on weakness, hepatic disease, diabetes, etc. However, experimental evidences are so insufficient that we started these studies. For antiinflammatory activity, MeOH Ex. was orally administered to rats, and decreased amounts of paw edema induced by carrageenan injection were measured. For bile secretion increament, rats were administered total MeOH, EtOAc fraction, and BuOH fraction Ex. respectively. One hour later, bile ducts were cannulated, and we collected bile every 20 minutes for 4 hours. For hepatoprotective activity, CCl$_4$-intoxicated mouse were treated with MeOH Ex., then s-GPT, S-GOT, and liver weight were measured. For antidiabetic activity, rats were induced diabetes by streptozocin 45mg/kg(i.v) injection. One week later, 1000mg/kg of total MeOH Ex. of chicory root was orally administered. We divided rats into three groups. Group 1 rats were administered only once, group 2 ones once a day for one week, and group 3 ones for three weeks. The concentrations of serum glucose were measured before and after administration. For antihypertensive activity, SHR were administrated total MeOH Ex. of chicory once a day for 8 days, and were measured blood pressure on 1st, 3rd, 6th and 8th day. Total MeOH, EtOAc fraction, and BuOH fraction Ex. increased bile secretion in rats, and decreased liver toxicity induced by CCl$_4$ in mouse. Total MeOH, Ex. of chicory roots has antiinflammatory effect, and decreased blood glucose concentration in group 2 and 3 rats. It was revealed not lowering blood pressure significantly in SHR.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.10
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• pp.1289-1294
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• 2009

Inflammation is a pivotal component of a variety of diseases, such as atherosclerosis and tumour progression. Various naturally occurring phytochemicals exhibit antiinflammatory activity and are considered to be potential drug candidates against inflammation-related pathological processes. Red pepper is the most consumed species in Korea. However, the antiinflammatory effects of red pepper have not been characterized. Thus, the present study was designed to evaluate the effects of the aqueous extract from red pepper (RPAE) on lipopolysaccharide (LPS)-induced inflammatory responses in murine macrophages. RPAE demonstrated strong antiinflammatory activity through its ability to reduce nitric oxide and prostaglandin $E_2$ production in the LPS-stimulated mouse macrophage cell, RAW264.7. It also inhibited the production of interleukin-6 (IL-6) on the LPS-stimulated RAW264.7 cells. Further study indicated that LPS-stimulated induction of inducible nitric oxide synthase and cyclooxygenase-2 was significantly inhibited by RPAE exposure (1,000 mg/mL) in RAW264.7 cells. Collectively, these data suggest that the use of RPAE may be a useful therapeutic approach to various inflammatory diseases.

• Biomolecules & Therapeutics
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• v.8 no.3
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• pp.223-227
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• 2000

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used for traditional medicines as early as 300 B .C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. To investigate activities of chrysin, one of propolis effective compounds for blood coagulation system was injected endotoxin (4000 EU/kg, i.v.) in rats at 1 hr after administered chrysin (20 mg/kg, p.o.). This study was resulted that chrysin has antiplatelet aggregation activity in vitro, delay of blood clotting time and prothrombin time, and reduction of fibrinogen and FDP in vivo. Chrysin has increased SOD activity, GSH content and GST activity, and decreased MDA content in liver. The result suggests that the antithrombosis effect of chrysin is suppressive activity for a blood coagulation system and antioxidative activity.

• Advances in Traditional Medicine
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• v.9 no.1
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• pp.83-89
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• 2009

Although many species of Asparagus have been studied scientifically and shoots are used in the diet of Sardinians, there is very little literature available on the medicinal uses of Asparagus acutifolius Linn. The acetone-ethanol (1:1) extract was screened for antioxidant, anti-inflammatory and adaptogenic activities. The extract showed good anti-oxidant activity in DPPH, hydroxyl radical, and nitric oxide radical assays. The extract also exhibited anti-inflammatory activity in the carrageenan-induced rat paw edema and adaptogenic activity in the milk induced leucocytosis assay in rats. The results of the present study suggest need to investigate other pharmacological activities of Asparagus acutifolius.

• Korean Journal of Pharmacognosy
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• v.38 no.1
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• pp.22-26
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• 2007

Leaves and stem of Viburnum sargentii for. sterile(Caprifoliaceae) has been used as therapeutic agents as a pain of the joints, skin disease as styptics, analgesics for traditional folk medicines. The present study describes the preliminary evaluation of biological activities-analgesic, anti-inflammatory, hepatoprotective activities, of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in inflammation and writhing test.

• Korean Journal of Pharmacognosy
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• v.24 no.3
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• pp.197-202
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• 1993

Three components, fraxetin-8-glucoside, esculetin-6-glucoside and mannitol, were isolated from the stem bark of Fraxinus chiisanensis var. stenophylla, F. japonica var. intermedia and F. densata. The MeOH extract of the cortex of F. densata had the antiinflammatory activity on the carrageenin-induced paw edema in rat. The MeOH extracts of the cortex of all three Fraxinus spp. have the potent analgesic activity on the HOAc-induced writhing syndrome in mouse and the hepatoprotective activity on the $CCl_4-induced$ fatty liver in rat: protection of ballooning formation and inhibition of sGPT and sGOT increased by $CCl_4$.

• Journal of Korean Medicine Rehabilitation
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• v.28 no.1
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• pp.19-31
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• 2018

Objectives The object of this study was to investigate the antioxidative and antiinflammatory effects of Jinmu-tang extract (JMT) on the Monosodium iodoacetate (MIA)-induced rat osteoarthritis. Methods To investigate the antioxidant capacities of JMT, we measured the total polyphenol and flavonoid, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis(3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity. To evaluate the antioxidative and antiinflammatory effects of JMT, the rats were divided into 5 groups (n=8). Normal group was not induced by MIA and treated at all (N), control group was induced by MIA and not treated at all (Con), positive control group was induced by MIA and orally administered indomethacin 5 mg/kg (Indo) and experimental groups were induced by MIA and orally administered JMT 100 mg/kg (JMT100) and JMT 200 mg/kg (JMT200) for 4 weeks. The changes of anti-type II collagen antibody in serum, heme oxygenase-1 (HO-1), phosphorylated inhibitor of ${\kappa}B{\alpha}$ ($p-I{\kappa}B{\alpha}$), cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) and tumor necrosis factor alpha ($TNF-{\alpha}$) in knee joint tissue and histopathological observation (Hematoxylin & Eosin and Safranin-O stain) were measured. Results Total polyphenol and flavonoid levels of JMT were $26.90{\pm}0.33mg/g$ and $6.02{\pm}0.34mg/g$. $IC_{50}$ of L-ascorbic acid and JMT of DPPH radical scavenging activity were $1.35{\pm}0.07{\mu}g/ml$ and $52.95{\pm}0.97{\mu}g/ml$. $IC_{50}$ of L-ascorbic acid and JMT of ABTS radical scavenging activity were $3.18{\pm}0.02{\mu}g/ml$ and $91.49{\pm}1.74{\mu}g/ml$. In serum, the anti-type II collagen antibody levels of JMT100 and JMT200 groups were decreased significantly. In knee joint tissue, the HO-1 level of JMT200 was increased significantly. The $p-I{\kappa}B{\alpha}$ and $TNF-{\alpha}$ levels of JMT200 were decreased significantly. The COX-2 and iNOS levels of JMT groups were decreased significantly. In histopathological observation, in comparison with Con, synovial tissue, cartilage and proteoglycan of JMT100 and JMT200 were well preserved. Conclusions According to the results, It is considered that JMT has antioxidant and antiinflammatory effects for MIA-induced rat osteoarthritis, so it could be applied to osteoarthritis treatment.

• Korean Journal of Pharmacognosy
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• v.41 no.2
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• pp.73-88
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• 2010

Traditionally, the root of Lithospermum erythrorhizon Sieb. et Zucc(L.E) has been used as efficacious therapy for inflammation, burns, frostbite and skin ailments (e.g eczema and psoriasis). It contains isohexenylnaphthoquinone derivatives (shikonin and its esters) and furylhydroquinones (shikonofurans) in lipophilic fractions and caffeic acid oligomers (rosmarinic acid, lithospermic acid B) in polar fractions. Recently, new preparative isolation and analysis procedures of shikonin along with its oligomers from the extract of L. erythrorhizon by the combination of high-speed counter-current chromatography with high-performance liquid chromatography-diode array detection have also been introduced. Although there have been many reports on the wound healing, antiinflammatory, and anticancer effects, the research on the effects of anti-atopic dermatitis of the root of L. erythrorhizon were relatively scarce. However, in recent years, new information gathered from research efforts, on the anti-atopic dermatitis properties of the extract or constituents of L. erythrorhizon has been accumulated. In this paper, the findings and advance on the in vitro and in vivo activities of L. erythrorhizon and its constituents especially focused on antiinflammatory and anti-atopic dermatitis effects are summarized. The phytochemical constituents of L. erythrorhizon or its tissue cultures are also presented. Although there are few to verify or refute its activity in human, one result of clinical study of the extract of L. erythrorhizon on the atopic dermatitis patients was introduced to assess the possibility of its clinical use. The reported mechanisms of action and in vivo pharmacological studies in different animal models for the various types of extracts or constituents of L. erythrorhizon are supportive of its therapeutic potential or dietary supplement, however, more evidence from clinically relevant models, as well as systemic studies on the active constituents or the various types of standardized extracts at the cellular and molecular level, are required.