• YAKHAK HOEJI
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• v.45 no.6
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• pp.565-569
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• 2001

Five novel cinmetacin amide derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity was compared with cinmetacin. Cinmetacin and hydroxysuccinimide were reacted with dicyclohexyl carbodiimide to give cinmetacin active ester (4), which was treated with amines to yield cinmetacin amides (5-9). Compounds (5) and (9) gave stronger analgesic activity than cinmetacin and compounds (5), (6), (9) showed comparable antiinflammatory activity to cinmetacin.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.1-6
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• 2001

Nine cinmetacin derivatives as potential nonsteroidal analgesic and antiinflammatory compounds were prepared and their analgesic-antiinflammatory activity was compared with cinmetacin. Salicylic acid and phenols were reacted with dicyclohexyl carbodiimide (DCC) to give phenol salicylates (1-4). Cinmetacin was treated with DCC and phenol derivatives to yield cinmetacin esters (5-13). Compounds (5, 7, 8, 10, 12, and 13) showed stronger analgesic activity than cinmetacin, but only compound (5) showed comparable antiinflammatory activity to cinmetacin.

• Archives of Pharmacal Research
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• v.17 no.1
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• pp.31-35
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• 1994

For comparing with flavones/flavonols, isoflavonoids isolated from Pueraria radix and chemically synthesized from biochanin A were evaluated for the antiinflammatory activity using mouse ear edema test, Isoflavonoids such as daildzein and puerarin hsowed the significant antiinflammatory activity at a dose of 2 mg/mouse, although their activity was generally less than that of flavones/flavonols. 7-O-Substitution of biochanin A was not facorable for the antiinflammatory activity.

• Natural Product Sciences
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• v.2 no.1
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• pp.1-8
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• 1996

Flavonoids are widely distributed polyphenol compounds in plant kingdom and known to possess varieties of biological/pharmacological activities in vitro and in vivo. A search for antiinflammatory/immunoregulatory flavonoids as potential therapeutic agents has been continued, since serious side effects of currently used nonsteroidal and steroidal antiinflammatory drugs limit their long term uses for the inflammatory disorders. In this reserch, various flavonids were isolated and tested for their in vivo antiinflammatory activity and in vitro inhibitory activity of lymphocyte proliferation. Using a mouse ear edema assay, it was found that certain flavones/flavonols possess mild antiinflammatory activity and a C-2,3-double bond might be essential. Isoflavones were less active. These flavonoids inhibited in vitro lymphocyte proliferation, relatively specific for T-cell proliferation $(IC_{50}=1-10\;{\mu}M)$ and the inhibition was reversible. We have also tested several biflavonoid derivatives, since we recently found that biflavones were phospholipase $A_2$ inhibitors. It was demonstrated that biflavones such as ochnaflavone and ginkgetin inhibited lymphocyte proliferation induced by both concanavaline A and lipopolysaccharide. The inhibition was irreversible in contrast to that of flavones/flavonols. And antiinflammatory activity of biflavonoids are discussed.

• YAKHAK HOEJI
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• v.36 no.1
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• pp.7-11
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• 1992

2-Substituted benzimdazoles were prepared by reacting o-phenylenediamine with acid chlorides, which has advantages over the known synthetic procedures. The compounds prepared showed no significant antiinflammatory activity, thus are of no interest as antiinflammatory agents.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.149-154
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• 2002

Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity were compared with antiprine. Succinyl chloride and Ac $_2$O were reacted with glycine, respectively, to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6, 11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac $_2$O, respectively, to give succinyl bis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.

• Advances in Traditional Medicine
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• v.5 no.2
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• pp.124-136
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• 2005

Two popular ethnomedicines of the Onge, a Negrito tribe of Andaman Islands, were evaluated for analgesic and antiinflammatory activity. The methanol extract as well as the different fractions of methanol extract of both Alstonia macrophylla and Mallotus peltatus leaves were studied using Swiss albino mice and Wistar albino rats. Acetic acid induced writhing, Tail flick and Tail immersion; Carrageenin- and Dextran-induced paw oedema tests were used. Dose-dependent analgesic and antiinflammatory activity were demonstrated for both methanol leaf extracts as well as fractions. Results were highly comparable with that of the standard drug pethidine.

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.25-28
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• 1993

Our previous report demonstrated that certain flavonoid aglycones such as apigenin (flavone), quercetin, morin (flavonols), and biochanin A (isoflavone) showed in vivo antiinflammatory activity via topical and oral routes of adminstation. As a continual study, the various flavonoid glycosides have been evaluated in mouse ear edema assay using archidonic acid or croton-oil as a inflammagen. Flavonoids were orally administered (2 mg/mouse) and ear edema inhibition was measured. Significant antiinflammatory activities were found esepcially in flavone and flavonol glycosides (15-29% inhibition) although the flavonoid derivatives tested showed less antiinflammatory activity than hydrocortisone or indomethacin. Chalcone and flavanone derivatives were not significantly active. And in general, flavonol glycosides of kaempferol-type were found to have a higher oral antiinflammatory activity than that of flavonol glycosides of quercetin-type in mice.

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.1-8
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• 2003

In this study, a series of new $N^2$ substituted 1,2-dihydro-3H-indazol-3-ones (3a-d) as well as their condensed pyrazolo, pyridazino derivatives such as pyridazino[1,2-a]indazole-6,9,11-triones (4a-h) and 3,9-dioxo-3H,9H-pyrazolo[1,2-a]indazole (7) were synthesized. The antiinflammatory activity of some synthesized compounds was determined by carrageenan-induced rat paw edema technique using diclofenac as reference drug. The pharmacological data showed that most of the tested compounds exhibited a significant long lasting antiinflammatory activity, which in the case of compound 3b was superior to that of diclofenac.

• Journal of Periodontal and Implant Science
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• v.26 no.2
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• pp.557-566
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• 1996

It is known that some natural extracts from plants have a various range of antimicrobial and antiinflammatory activity. There are lots of clinical trials to develop toothpastes containing natural extracts for prevention of dental caries and gingival inflammation. The purpose of this study was to evaluate antimicrobial and antiinflammatory activity of magnolol containing toothpastes and other commercial toothpastes. Eleven kinds oftoothpastes were used. They include magnolol, sanguinarine, Myrrha, Mori radicis cortex,Cimicifugae rhizoma, sodium fluoride, aminocaprolactic acid etc. Six strains of bacteria were used for this test, ego Porphylomonas gingivalis, Prevotellain-termedia, Actinobacillus actinomy cetemcomitans, Streptococcus mutans, Stretococcus sanguis, and Actinomyces species. Antimicrobial activity was determined by an agar dillution method and a broth microdillution method. Antiinflammatory activity was assessed by the inhibition of $PGE_2$ production from gingival fibroblast with the addition of rHIL-1 and centrifuged solution of toothpastes. Control group was only rHIL-1 additive sample. $PGE_2$ enzyme immunoassay systemfAmersham, In. Buckinghamshire, U.K). $PGE_2$ level was measured by ELISA reader with 450 nm, The results from the study revealed that toothpastes containing natural extracts generally had high antimicrobial and antiinflammatory activity. Especially magnolol containing toothpaste showed higher antimicrobial activity than other toothpastes, and sanguinarine containing toothpaste showed particularly high antimicrobial activity in A. actinomicetemcomitans and A. viscosus. In some degree all toothpastes inhibited $PGE_2$ production, but magnolol containing toothpaste was potent inhibitor of $PGE_2$. Sodium chloride containing toothpaste had also effective result. The results suggested that toothpastes containing natural extracts were promising in plaque control and prevention of dental caries and gingivitis.