• Archives of Pharmacal Research
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• 제26권1호
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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.

• 약학회지
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• 제38권5호
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• pp.525-529
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• 1994

Antiinflammatory activity of an 1% flurbiprofen transdermal gel was evaluated using the carrageenan-Induced rat paw edema method. The application of 50 mg of the gel on the rat hind paw, at various time intervals from 0 to 24 hrs before the carrageenan injection, significantly inhibited edema formation in all groups of dosed rats, indicating that the antiinflammatory activitv was maintained up to 24 hrs after the transdermal application of the 1% flurbiprofen gel. The topical $ED_{50}$ of flurbiprofen in the gel was 1.0 mg/kg, whereas the oral $ED_{50}$ of the drug in a suspension was 1.7 mg/kg.

• 약학회지
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• 제43권3호
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• pp.320-327
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• 1999

Six novel aryl alkanoic acid derivatives as potential nonsteroidal antiinflammatory and analgesic compounds, were prepared through consecutive reactions of Ullman ether synthesis, $NaBH_4$ reduction ; bromination ; $SN_2$ reaction with nitrile and alkaline hydrolysis of the nitrile.

• Biomolecules & Therapeutics
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• 제6권1호
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• pp.45-49
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• 1998

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, $C_{max}$ were 316 $\pm$22.3 ng/ml and 163 $\pm$ 12.2 ng/ml, respectively, at the same Tma of 2 hours postdose, while $C_{max}$ and $T_{max}$ after oral administration of the drug were 1,030$\pm$89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and I-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageeneninduced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while I-lotion showed 34.\\\\`r%. The calculated ED5o after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.n.n.n.

• 한국염색가공학회지
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• 제31권4호
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• pp.323-331
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• 2019

Sorghum is a rich source in phytochemicals, such as tannins, phenolic acids, anthocyanins, phytosterols and policosanols. Sorghum has been known to have antimicrobial, antiinflammatory, antioxidant properties. In this study, poly(vinyl alcohol)(PVA)-sorghum extract(SE) composite nanoweb was produced by electrospinning and its characteristics including bioactivities were investigated. The SE had antimicrobial and antiinflammatory activities as well as a reduced cytotoxicity. The PVA-SE nanoweb had a highly enhanced antimicrobial activity compared to PVA nanoweb. The amount of proinflammatory cytokine released from macrophages treated with the PVA-SE nanoweb was reduced. The PVA-SE nanoweb can be a potential candidate for medical and cosmeceutical materials providing antimicrobial and antiinflammatory activities with a low degree of cytotoxicity.

• Natural Product Sciences
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• 제9권2호
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• pp.97-101
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• 2003

This study was undertaken to evaluate the antinociceptive and antiinflammatory effects of the heartwood extract of Rhus verniciflua (Anacardiaceae) and the two major components, sulfuretin and fustin. The MeOH extract, its EtOAc-soluble portion and sulfuretin showed significant antinociceptive activity in writhing and hot plate test assays and antiinflammaory effects in carrageenan-induced hind paw edema in rats. In particular, treatment of sulfuretin with 10 mg/kg dose (i.p.) reduced writhing frequency by 48.0% (p<0.01) compared to that of a control group. Further, the treatment of sulfuretin (5, 10 mg/kg, i.p.) for 7 days prevented the carrageenan-induced hind paw edema significantly (p<0.01). The antiinflammatory effect of sulfuretin was also confirmed by microscopic observation of mast cell numbers in muscle. In addition, sulfuretin suppressed the cyclooxygenase- 2 (COX-2) activity $(IC_{50}\;=\;28.7\;{\mu}M)$ in lipopolysaccharide-activated macrophage cells. This result indicates that the inhibitory effect of sulfuretin on COX-2 may be one of the antinociceptive/antiinflammatory mechanism.

• Journal of Pharmaceutical Investigation
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• 제16권1호
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• pp.24-30
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• 1986

Ssangwhatang which has been known to have antipyretic, analgesic and antifatigue effects are composed of Paeoniae Radix, Angelicae gigantis Radix, Astragali Radix, Rehmaniae Radix, Cnidii Rhizoma, Cassiae Cortex, Glycyrrhizae Radix and Puerariae Radix. Effects of some formulations of Ssangwhatang were studied with respect to the analgesic, antipyretic, hypothermic, anticonvulsive and antiinflammatory actions in experimental animals. The results obtained were as follows: 1) Prescription A, B, C and D of Ssangwhatang were showed significant analgesic effect by the acetic acid stimulating method in mice. 2) All Ssangwhatang-prescriptions used in this studies had hypothermic effect in normal mice. 3) Significant antipyretic effect in febrile rabbits were recognized in prescription A and C of Ssangwhatang, while not in prescription B and D of Ssangwhatang. 4) Prescription A, B, C and D of Ssangwhatang showed marked antiinflammatory effect against the edema induced by carrageenin in rats. 5) Prescriptions of Ssangwhatang did not show significant anticonvulsive effect against the convulsion induced by picrotoxin and strychnine in mice. From the above results, analgesic, hypothermic, antipyretic and antiinflammatory effects were recognized in Ssangwhatang. Ssangwhatang A- and C- prescriptions added with Pueraiae Radix showed better effects than prescription B and C of Ssangwhatang.

• Journal of Periodontal and Implant Science
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• 제26권2호
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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.

• Journal of Ginseng Research
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• 제44권1호
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• pp.145-153
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• 2020

Background: Panax ginseng Meyer (Araliaceae) is a highly valued medicinal plant in Asian regions, especially in Korea, China, and Japan. Chemical and biological studies on P. ginseng have focused primarily on its roots, whereas the seeds remain poorly understood. This study explores the phytochemical and biological properties of compounds from P. ginseng seeds. Methods: P. ginseng seeds were extracted with methanol, and 16 compounds were isolated using various chromatographic methods. The chemical structures of the isolates were determined by spectroscopic data. Antiinflammatory activities were evaluated for triterpene and steroidal saponins using lipopolysaccharide-stimulated RAW264.7 macrophages and THP-1 monocyte leukemia cells. Results: Phytochemical investigation of P. ginseng seeds led to the isolation of a novel triterpene saponin, pseudoginsenoside RT₈, along with 15 known compounds. Pseudoginsenoside RT₈ exhibited more potent antiinflammatory activity than the other saponins, attenuating lipopolysaccharide-mediated induction of proinflammatory genes such as interleukin-1β, interleukin-6, inducible nitric oxide synthase, cyclooxygenase-2, and matrix metalloproteinase-9, and suppressed reactive oxygen species and nitric oxide generation in a dose-dependent manner. Conclusion: These findings indicate that pseudoginsenoside RT₈ has a pharmaceutical potential as an antiinflammatory agent and that P. ginseng seeds are a good natural source for discovering novel bioactive molecules.

• 약학회지
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• 제39권4호
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• pp.385-394
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• 1995

Antiinflammatory activities of the solvent fractionates of several herbal medicines were investigated and SKI306X was prepared from the active principles of three herbal medicines, Prunella vulgaris, Trichosantlies kirilowii and Clematis mandshurica. SK1306X was shown to have strong inhibitory effects on acetic acid-induced pain, carrageenan-induced paw edema and adjuvant induced arthritis. LD50 of SKI306X was more than 5 g/kg in rat, so generally nontoxic. Chemical analysis revealed that oleanolic acid and rutin, which are known to have various antiinflammatory activities, were contained in it. These results suggest SK1306-X may become a useful drug for the treatment of inflammatory diseases such as rheumatoid arthritis.