Acetic Acid-induced Vascular Permeability Research Articles

Studies on the anti-inflammatory and related pharmacological properties of the aqueous extract of Bridelia ferruginea stem bark

The anti-inflammatory profile of the aqueous extract of Bridelia ferruginea stem bark was investigated using both in vivo and in vitro models. The extract exhibited strong topical anti-inflammatory effect shown as inhibition of croton oil-induced ear oedema in mice, and reduced hind-paw swelling and growth retardation in the adjuvant-induced arthritis model in rats, following oral administration at 10, 20, 40 or 80 mg/kg. The extract (10–80 mg/kg, p.o.) caused an inhibition of increase in vascular permeability in both cyclophosphamide-induced haemorrhagic cystitis and acetic acid-induced vascular permeability in rats and mice, respectively. B. ferruginea produced stabilization of erythrocytes exposed to heat and stress-induced lysis. Antipyretic and analgesic properties of the extract were also observed.

Antiinflammatory effect of Forsythia suspensa V(AHL) and its active principle.

This study was carried out to elucidate the antiinflammatory active principles obtained from 70% methanol extract of the dried fruit of Forsythia suspensa V(AHL) (F. suspensa). The methanol extract was then partitioned between n-hexane and water, and then the n-hexane fraction was evaporated to dryness under vacuum. The n-hexane fraction was chromatographed (Frs. I--V), Fr. IV was rechromatographed (Frs. VI--VIII), and then Fr. VII was rechromatographed (Frs. IX--XI) by silica gel column chromatography. The antiinflammatory activity of these fractions was investigated on acetic acid-induced vascular permeability in rats. The n-hexane fraction showed an antiinflammatory effect and these activities shifted successively to Fr. IV, Fr. VII and Fr. X. The chemical structure of the active principle obtained from Fr. X was identified as 3beta-acetoxy-20,25-epoxydammarane-24-ol. These results suggest that the antiinflammatory and an analgesic effect of 70% methanol extract of F. suspensa may be the result of the compound that it contains.

Antiinflammatory effect of Forsythia suspensa Vahl and its active fraction.

This study was carried out to elucidate the antiinflammatory effect of 70% methanol extract obtained from the dried fruit of Forsythia suspensa Vahl and its active principles. F. suspensa was extracted with 70% methanol and freeze-dried to give a powdered extract. The methanol extract was then dissolved in water and extracted with n-hexane, and the n-hexane fraction was evaporated to dryness under vacuum; the water fraction was freeze-dried to give a powdered extract. The antiinflammatory activity of the extract and fractions was investigated on acetic acid-induced vascular permeability and writhing symptoms in mice, as well as on carrageenin-induced edema and cotton pellet-induced granuloma formation in rats. The methanol extract and the n-hexane fraction (p.o.) showed the antiinflammatory effect and analgesic effect, but the water fraction did not. These results suggested that the antiinflammatory and analgesic activity induced by the methanol extract shifted to the n-hexane fraction and the active principles may be lipophilic compounds.

Antiinflammatory Effect of Trichosanthes kirilowii MAXIM. and Its Effective Parts.

This study was carried out to elucidate the antiinflammatory effect of 50% ethanol extract obtained from the fruit of Trichosanthes kirilowii Maxm, and its effective parts. The cut dried fruit was separated into the whole fruit, seeds and remaining parts, and each part was extracted with 50% ethanol. The antiinflammatory activity of these extracts was investigated on acetic acid-induced vascular permeability in mice, carrageenin-induced edema and cotton pellet-induced granuloma formation in rats, as well as writhing symptoms in mice. The whole fruit and seed extractions showed an antiinflammatory activity and analgesic activity, but the other part did not when given perorally. These results suggest that the antiinflammatory effect and analgesic effect induced by ethanol extract of the fruit of T. kirilowii may be due to the seeds contained in the fruit.

Anti-inflammatory Effect of Zingiber cassumunar ROXB. and Its Active Principles.

The present study was carried out to elucidate the anti-inflammatory effect of the methanol extract obtained from the rhizomes of Zingiber cassumunar Roxb. and its active principles. The methanol extract was partitioned between ether and water, and then the ether-soluble fraction was extracted with n-hexane. The n-hexane-soluble fraction was chromatographed and part of the fraction was rechromatographed by silica gel column. Three compounds were isolated from the n-hexane-soluble fraction and the chemical structures of these compounds were identified as (E)-1-(3,4-dimethoxyphenyl)but-1-ene, (E)-1-(3,4-dimethoxyphenyl)butadiene and zerumbone. The anti-inflammatory activity of these fractions was investigated on carrageenin-induced edema in rats, as well as on acetic acid-induced vascular permeability and writhing symptoms in mice. The methanol extract (p.o.) showed both anti-inflammatory activity and analgesic activity. These activities shifted successively to ether-soluble and n-hexane-soluble fractions and to (E)-1-(3,4-dimethoxyphenyl)but-1-ene. These results suggest that the anti-inflammatory action and analgesic action of Zingiber cassumunar is the result of the (E)-1-(3,4-dimethoxyphenyl)but-1-ene that it contains.

Antiinflammatory effect of Curcuma xanthorrhiza Roxb. and its active principles.

The rhizomes of Curcuma xanthorrhiza Roxb, are used in Indonesian folk medicine as cholagogues, aromatic stomachics, analgesics, a rheumatic remedy, etc. The present study was carried out to elucidate the antiinflammatory effect of the methanol extract obtained from these rhizomes and its active principles. The methanol extract was partitioned between ether and water, and then the ether-soluble fraction was extracted with n-hexane. The n-hexane-soluble fraction was chromatographed (fr. I-IV), fr. II was rechromatographed (fr. V-VII), and then fr. V was rechromatographed (fr. VIII-X) by silica gel column chromatography. The antiinflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability as well as the writhing symptom in mice. The methanol extract (p.o.) showed both an antiinflammatory activity and an analgesic activity and these activities shifted successively to the ether-soluble fraction, the n-hexane-soluble fraction, fr. II, V and IX. The chemical structure of fr. IX was identified as germacrone. These results suggest that the antiinflammatory action of Curcuma xanthorrhiza is the result of the germacrone that it contains.

Antiinflammatory effect of Graptophyllum pictum (L.) Griff.

The red leaves of Graptophyllum pictum (L.) Griff. (G. pictum) are used in Indonesian folk medicine. The present study was carried out to elucidate the antiinflammatory effect of the ethanol extract obtained from this crude drug. The extract was partitioned between ether and water, and then the water-soluble fraction was extracted with 1-butanol. The 1-butanol-soluble fraction was extracted with chloroform-acetone, hot methanol and water, successively, and the hot methanol-soluble fraction (fr.) was chromatographed (frs. I-III). The antiinflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability as well as the writhing symptom in mice. The ethanol extract (p.o.) showed an antiinflammatory activity as well as an analgesic activity and these activities shifted to the water-soluble fraction, 1-butanol-soluble fraction, methanol-soluble fraction and fr. II, successively. It was found that fr. II contained flavonoids. These results suggest that these flavonoids are at least partly responsible for the antiinflammatory effect of the ethanol extract of G. pictum.

Antiinflammatory effect of mace, aril of Myristica fragrans Houtt., and its active principles.

Mace which is the aril of the fruit of Myristica fragrans HOUTT, has been used in Indonesian folk medicine as aromatic stomachics, analgesics, a medicine for rheumatism, etc. The present study was carried out to elucidate the antiinflammatory effect of methanol extract obtained from Mace and its active principles. The methanol extract was extracted with ether, and then the ether soluble fraction was extracted with n-hexane. The n-hexane soluble fraction was fractionated by silica gel column chromatography (Fr-l-Fr-V), and the active principle was isolated from Fr-II by thin layer chromatography (Fr-VI-Fr-VII). The antiinflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability in mice. All fractions and indomethacin were suspended in 2% C.M.C. solution and administered p.o. The methanol extract (1.5 g/kg), ether fraction (0.9 g/kg), n-hexane fraction (0.5 g/kg), Fr-II (0.19 g/kg) and Fr-VI (0.17 g/kg) showed a lasting antiinflammatory activity, and the potencies of these fractions were approximately the same as that of indomethacin (10 mg/kg). Fr-VI was determined to be myristicin. These results suggest that the antiinflammatory action of Mace is due to the myristicin that it contains.

Antiinflammatory Effect of Mace, Aril of Myristica fragrans HOUTT., and Its Active Principles

Mace which is the aril of the fruit of Myristica fragrans HOUTT. has been used in Indonesian folk medicine as aromatic stomachics, analgesics, a medicine for rheumatism, etc. The present study was carried out to elucidate the anti-inflammatory effect of methanol extract obtained from Mace and its active principles. The methanol extract was extracted with ether, and then the ether soluble fraction was extracted with n-hexane. The n-hexane soluble fraction was fractionated by silica gel column chromatography (Fr-I-Fr-V), and the active principle was isolated from Fr-II by thin layer chromatography (Fr-VI-Fr-VII). The anti-inflammatory activity of these fractions was investigated on carrageenin-induced edema in rats and acetic acid-induced vascular permeability in mice. All fractions and indomethacin were suspended in 2% C.M.C. solution and administered p.o. The methanol extract (1.5 g/kg), ether fraction (0.9 g/kg), n-hexane fraction (0.5 g/kg), Fr-II (0.19 g/kg) and Fr-VI (0.17 g/kg) showed a lasting antiinflammatory activity, and the potencies of these fractions were approximately the same as that of indomethacin (10 mg/kg). Fr-VI was determined to be myristicin. These results suggest that the antiinflammatory action of Mace is due to the myristicin that it contains.

A correlation between the species differences in anti-inflammatory activity of AD-1590, a non-steroidal anti-inflammatory drug, and its plasma level

Authors have reported that the oral potency ratio of AD-1590 to indomethacin varies with the animal models employed; the ratio is 4, 2.3 and 31 in the tests of acetic acid-induced vascular permeability (male mice), carrageenan hind paw edema (male rats) and UV-erythema (female guinea pigs), respectively. Thus, the relationship between the difference in the anti-inflammatory activity of AD-1590 among animal models and the species difference of the plasma AD-1590 level was investigated in experimental animals in order to ascertain the cause of the difference in the potency ratio. Inhibitory potency of AD-1590 on UV-erythema and increased vascular permeability induced by acetic acid in male rats was about 2.1 and 2.3 times, respectively, that of indomethacin. On the other hand, after a single oral administration of 5 mg/kg, the highest plasma AD-1590 level was seen in female guinea pigs (AUC9-8 hr = 63.1 micrograms.hr/ml); and followed by that in mice (male, 32.1; female, 36.1) greater than male dogs (11.5) greater than or equal to rats (male, 9.02; female, 12.5), male rabbits (9.17) greater than male monkeys (9.34 at 6 mg/kg). Hucker et al. have reported that the plasma level of indomethacin in rats is several times higher than that in guinea pigs, rabbits and monkeys. These results suggest that most of the species difference in the relative potency of AD-1590 to indomethacin in the anti-inflammatory activity results from the species difference in the plasma level of both drugs.

Anti-inflammatory, analgesic and anti-pyretic activities of a new anti-inflammatory compound, 2-[4-(3-methyl-2-butenyl)phenyl] propionic acid (TA), in experimental animals

Anti-inflammatory, analgesic and anti-pyretic activities of orally administered TA were investigated in experimental animals. Against acetic acid-induced vascular permeability in mice, carrageenin-induced hind paw edema in rats and ultra-violet ray-induced erythema in guinea pigs, TA produced a dose related inhibition at doses of 40-160 mg/kg, 10-40 mg/kg and 10-40 mg/kg, respectively. TA produced no inhibition against histamine-induced vascular permeability even at a dose of 200 mg/kg in rats. Cotton pellet-induced granuloma and adjuvant-induced arthritis in rats were significantly inhibited by repeated administration of TA at a dose of 50 mg/kg/day for 6 days and 25 mg/kg/day for 6 days, respectively. TA showed a dose related analgesic effect at a dose of 50-200 mg/kg in acetic acid writhing, Randall-Selitto and adjuvant arthritic pain methods. A high dose of TA was needed to produce an analgesic effect in the pressure method using mice. TA produced an anti-pyretic effect against the pyrexia induced by yeast in rats. On the other hand, TA showed no effect against normal body temperature in rats. These results suggest that anti-inflammatory, analgesic and anti-pyretic activities of TA are generally a little weaker than those of ibuprofen, and the mode of action of TA is similar to that of a typical acidic non-steroidal anti-inflammatory drug such as ibuprofen, indomethacin or phenylbutazone. The ulcerogenic activity of TA was about 2 and 4 times weaker than that of ibuprofen in rats and mice, respectively. TA showed a protective effect against gastric necrosis induced by HCl.(ABSTRACT TRUNCATED AT 250 WORDS)

A correlation between the species differences in antiinflammatory activity of AD-1590, a new non-steroidal anti-inflammatory drug, and its plasma level

A relationship between the difference in the anti-inflammatory activity of AD-1590 among animal models and the species difference of the plasma AD-1590 level was investigated in experimental animals. The oral potency ratio of AD-1590 to indomethacin varied with the animal models; the ratio was 4, 2.3 and 31 in the tests of acetic acid-induced vascular permeability (male mice), carrageenin hind paw edema (male rats) and UV-erythema (female guinea pigs), respectively. However,the anti-inflammatory activity of AD-1590 was 2.1 and 2.3 times that of indomethacin in the UV-erythema and acetic acid-induced vascular permeability tests, respectively, in rats. On the other hand, the decreasing order of the plasma AD-1590 level after a single oral administration of 5 mg/kg was as follows: female guinea pig(the relative level=7.5) >male mouse(3.6) > male dog(1.3)≧ male rat (1.0), male rabbit(1.0) and male monkey(0.9). Hucker et al. (1966) have reported that the plasma level of indomethacin in rats is several times higher than that in guinea pigs and rabbits. Thus, these results demonstrate that most of the species difference in the potency ratio of AD-1590 to indomethacin on the anti-inflammatory activity results from the species difference in the plasma levels of AD-1590 and indomethacin.