Antiinflammatory, Analgesic and Antipyretic Activities of Mimusops elengi Linn

In the present study, 70% ethanol extract of Mimusops elengi Linn. bark was assessed for antiinflammatory, analgesic and antipyretic activities in animals. The antiinflammatory activity of ethanol extract of Mimusops elengi (200 mg/kg, p.o) was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma models. Analgesic effect was evaluated using acetic acid-induced writhing and Eddy's hot plate models and antipyretic activity was assessed by Brewer's yeast-induced pyrexia in rats. The ethanol extract of Mimusops elengi (200 mg/kg, p.o) significantly inhibited the carrageenan-induced paw oedema at 3rd and 4th h and in cotton pellet model it reduced the transudative weight and little extent of granuloma weight. In analgesic models the ethanol extract of Mimusops elengi decreases the acetic acid-induced writhing and it also reduces the rectal temperature in Brewer's yeast induced pyrexia. However, Mimusops elengi did not increase the latency time in the hot plate test. These results show that ethanol extract of Mimusops elengi has an antiinflammatory, analgesic and antipyretic activity.     

Synthesis of some novel oxadiazole and oxadiazoline analogues for their antiinflammatory activity

The search for newer non-steroidal antiinflammatory drugs (NSAIDs) and the importance of oxadiazoles as antiinflammatory agents prompted us to undertake the synthesis of some novel oxadiazole and related analogues with unreported antiinflammatory activities. The antiinflammatory potential of the compounds was investigated using the carrageenan-induced rat paw edema method and cotton pellet-induced granuloma method. Some compounds demonstrated marked antiinflammatory activities. The antiinflammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 28-55%, 21-36%, and 27-49% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the antiinflammatory properties of oxadiazolines at doses of 100 mg/kg was reflected by their ability to provide 15-47%, 22-39%, and 23-47% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. Structure-activity relationships among synthesized compounds were also studied.     

Antiinflammatory activity of two phenylindandione derivatives.

2-5-Dibromo-2-(beta-naphtyl)indan-1,3-dione (43/63) and 4-bromo-2-phenylindan-1,3-dione (43/13) are two interesting members of a series of "indandione" derivatives which possess an antiinflammatory activity (in the following tests: carrageenin induced rat hind paw edema, cotton pellets granuloma and chronic adjuvant arthritis). The two drugs are devoided of anticoagulant activity and their antiinflammatory effect is not adrenalmediated.     

Evaluation of antiinflammatory and analgesic activities of alcoholic extract of Kaempferia galanga in rats

Alcoholic extract of Kaempferia galanga was tested for analgesic and antiinflammatory activities in animal models. Three doses, 300 mg/kg, 600 mg/kg and 1200 mg/kg of the plant extract prepared as a suspension in 2 ml of 2% gum acacia were used. Acute and sub acute inflammatory activities were studied in rats by carrageenan induced paw edema and cotton pellet induced granuloma models respectively. In both models, the standard drug used was aspirin 100 mg/kg. Two doses 600 mg/kg and 1200 mg/kg of plant extract exhibited significant (P<0.001) antiinflammatory activity in carrageenan model and cotton pellet granuloma model in comparison to control. Analgesic activity was studied in rats using hot plate and tail-flick models. Codeine 5 mg/kg and vehicle served as standard and control respectively. The two doses of plant extract exhibited significant analgesic activity in tail flick model (P<0.001) and hot plate model (P<0.001) in comparison to control. In conclusion K. galanga possesses antiinflammatory and analgesic activities.     

The antiinflammatory effect of budesonide

The systemic and topical antiinflammatory activities of budesonide (B) were studied in rats and mice and compared with those of commercially available steroids. Betamethasone 17-valerate (BV) was used as the main reference compound, and fluosinolone acetonide (FA), hydrocortisone 17-butyrate (HB) and hydrocortisone 21-acetate (HA) were also used. B given systemically had stronger antiinflammatory effect than BV on carrageenin edema, cotton pellet granuloma, adjuvant arthritis, croton oil edema, PCA reaction, Arthus reaction, contact hypersensitivity and histamine or serotonin skin reaction. The potency of antiinflammatory activity of the 5 compounds in carrageenin edema, croton oil edema and contact hypersensitivity tests was in the order of FA, B, BV, HB and HA. B given locally also produced stronger antiinflammatory effects than BV on carrageenin edema, cotton pellet granuloma, croton oil edema and contact hypersensitivity. The order of potency of the 5 compounds in carrageenin edema, croton oil edema and contact hypersensitivity tests was the same as by systemic application. In general, the ratio of the dose required to cause atrophy of the thymus and adrenals to the dose required to produce the antiinflammatory effect was the greatest with B by both systemic and local application. The results suggest that B has a stronger antiinflammatory activity with fewer systemic side effects than conventional steroid compounds.     

Evaluation of Antiinflammatory Activity of Centratherum anthelminticum (L) Kuntze Seed

In the present study petroleum ether and alcoholic extracts of Centratherum anthelminticum (L) Kuntze seed (100 mg and 200 mg/kg p.o.) were evaluated for antiinflammatory activity in acute and subacute models of inflammation. It was found that both petroleum ether and alcoholic extracts showed significant reduction in paw oedema in carrageenan-induced model. In subchronic inflammatory phase both extracts provoked a significant reduction of transudation phase and too little extent proliferative phase when tested in cotton pellet-induced granuloma model. Both the extracts also reduced alkaline phosphatase activity in serum. The histopathology of granuloma tissue showed significant inhibition of lymphocytes, neutrophils, exudates, necrosis and giant cell when compared with control without ulcerogenic effect. The results suggest that petroleum ether and alcoholic extracts may exert antiinflammatory activity through prostaglandin inhibition, reduced myeloperoxidase and antitransudation.     

Highly selective antiinflammatory and analgesic activity of 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H-naphth[1,2-d]imidazole, a new non-acidic molecule

3-(1-Methylethyl)-2-(4-methoxyphenyl)-3H-naphth[1,2-d] imidazole (MDL-035) has antiinflammatory activity in various antiinflammatory models such as carrageenin and nystatin oedemas, cotton pellet granuloma and adjuvant arthritis. The antiinflammatory potency of MDL-035 is greater than that of acetylsalicylic acid and phenylbutazone, but lower than that of indomethacin. MDL-035 has practically no gastroulcerogenic activity in rats, does not affect water or salt excretion, has no hormonal or antihormonal effects and has no other unwanted pharmacological effects. Its acute toxicity is very low.     

Pharmacological properties of the antiinflammatory agent 10-methylamine-11-H-indeno-[1,2-b]quinolin-11-one (MB432)

10-Methylamine-11-H-indeno [1,2-b] quinolin-11-one (MB432) was found to be a prostaglandin synthetase inhibitor, to display antiinflammatory activity in carrageenin edema and cotton pellet granuloma tests in rats, and to exert analgesic action in paw pressure test in rats and in the writhing test in mice. The therapeutic index (LD50/ED50) for antiinflammatory and analgesic effect of MB432 is higher than that of indomethacin (IND) and phenylbutazone (PHB). The acute toxicity of MB432 is low but the drug showed high ulcerogenic activity. The ratio of medium ulcerogenic to median antiinflammatory and analgesic doses of MB432 is comparable to that of PHB but higher than for IND.     

Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents.

A series of benzobisthiazoles were screened for antiinflammatory activity in the carrageenan paw edema and adjuvant arthritis tests. Compound 26, 2,6-bis(N,N-diethylamino)benzo[1,2-d:5,4-d']bisthiazole, was found to inhibit the swelling of the uninjected paw in the prophylactic adjuvant arthritis model with an ED50 of 2.3 mg/kg orally. As with most compounds of this series, 26 was inactive in acute model of inflammation, such as paw edema; like steroids, it showed activity in the granuloma pouch assay but did not inhibit cyclooxygenase, indicating a mode of action different from the classical nonsteroidal antiinflammatory drugs (NSAID's). At doses higher than those producing antiinflammatory activity, 26 had some immunoregulating properties.     

Antiinflammatory activity of a polyherbal formulation

The antiinflammatory activity of the polyherbal formulation Entox^® was investigated in rats for acute and sub acute models of inflammation using carrageenan-induced rat paw edema and cotton pellet granuloma methods respectively at a dose of 300 mg/kg and 600 mg/kg administered orally. The formulation in doses of 300 mg/kg and 600 mg/kg showed 51.61% and 54.84% inhibition of paw edema, respectively at the end of 3 h. The percent inhibition of granuloma by cotton pellet method was 27.92% and 53.17%, respectively. The formulation showed a significant antiinflammatory activity in both the experimental models and the activity was comparable to that of the standard drug, indomethacin.     

Comparison of the antiinflammatory activities of three medicinal plants known as "meiduoluomi" in Tibetan folk medicine

Erigeron breviscapus (Vant.) Hand-mazz (EB), Erigeron multiradiatus (Lindl.) Benth (EM), and Aster brachytrichus Franch (AB), confused under the vernacular name "meiduoluomi" by native people and traditional healers, have been used for the treatment of meningitis, polyneuritis, hepatitis, adenolymphitis, and enteronitis in traditional Tibetan medicine. In this study, the antiinflammatory activity of methanol extracts of all three plants was investigated in the xylene-induced ear edema model, carrageenan-induced paw edema model, and cotton pellet-induced granuloma model. It was found that the methanolic extracts of both EB and EM had strong inhibitory effects on the acute phase of inflammation in carrageenan-induced paw edema in rats. On the other hand, the methanolic extract of EM showed stronger effects than those of EB in xylene-induced ear edema. In the chronic test, the methanolic extracts of EB and EM resulted in a significant reduction in granuloma weight in rats. In addition, myeloperoxidase (MPO) activity was strongly reduced in the EB-treated and EM-treated groups, which indicated that EB and EM can inhibit certain inflammatory modulator factors that cause neutrophil aggregation in inflamed tissue, e.g., nuclear factor-kappaB. However, the methanolic extracts of AB had no antiinflammatory effects in the tested models and MPO assay. The similar effects of EM and EB in tested models provided some scientific basis for the traditional usage of meiduoluomi in inflammatory disease. However, the results also suggest that further study is needed to investigate the antiinflammatory profile of AB and provide a scientific basis for the use of AB in inflammatory diseases.     

A novel class of local antiinflammatory steroids. 1st communication: analogues of methyl 11 beta,17 alpha,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16 alpha-carboxylate

A novel class of steroidal 16-esters and amides, 1-8 has been synthesized and evaluated as safer local antiinflammatory agents. These compounds retain the intact ketol side-chain of prednisolone and have an alkanoate ester or carboxamide function at the C-16 of the steroid nucleus. In the cotton pellet granuloma assay a correlation was observed between the size of the C-16 substituent group and the local antiinflammatory activity. The incorporation of a methyl carboxylate group at the C-16 position of prednisolone as in methyl 11 beta,17 alpha,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16 alpha-carboxylate, 5, resulted in an increase in antiinflammatory activity. The 17-deoxy analogue of 5, 1, retained one-half the activity of prednisolone. These two compounds were further evaluated for their effects on plasma corticosterone, adrenal and thymic weights at their ID50 doses for granuloma formation. Neither 5 nor 1 depressed plasma corticosterone levels or significantly altered adrenal weights. Compound 1 was also devoid of thymolytic activity, whereas 5 produced a 33% thymic involution at its ID50 compared to 47% for prednisolone at its equiactive dose.     

Antiinflammatory Activity of Aqueous Extract of Stereospermum kunthianum (Cham, Sandrine Petit) Stem Bark in Rats

Stereospermum kunthianum, Cham, Sandrine Petit (family: Bignoniaceae) is used in traditional medicine to treat bronchitis, pneumonia and coughs, gastritis, wounds, rheumatic arthritis, ulcers, dysentery, leprosy and venereal diseases in humans. The antiinflammatory activity of the aqueous extract of the stem bark was investigated with experimental animal models using the carrageenan-induced paw oedema, leucocytes migration and granuloma air pouch tests in rats. The extract (100, 200 or 400 mg/kg) at 3 h post-treatment caused a significant (p<0.05) reduction in the paw oedema in rats. The effect of the extract was most pronounced at the dose of 400 mg/kg and was higher than that of indomethacin (10 mg/kg). The extract (400 mg/kg) caused a significant (p<0.05) reduction in the number of recruited leucocytes and it''s inhibition of peritoneal exudate formation was comparable to that of indomethacin at a dose of 10 mg/kg. The exudate formation inhibited by 400 mg/kg of the extract in the granuloma air pouch test was comparatively less to that of indomethacin at a dose of 10 mg/kg. The findings of the study indicate that the aqueous extract of Stereospermum kunthianum stem bark possesses antiinflammatory activity which is probably related to the inhibition of prostaglandin synthesis. This is a possible rationale for its folkloric use as an antiinflammatory agent.     

二苯噁丙酸的抗炎作用及其机理

以多种炎症模型观察了二苯丙酸的抗炎作用。给动物灌服二苯丙酸,能抑制角叉莱胶致足跖肿胀和棉球致内芽组织增生,对大鼠佐剂性关节炎也有明显的抑制作用。该药的抗炎作用强度与阿司匹林相似,但作用时间明显延长。探讨其作用机理表明,二苯丙酸能降低毛细血管通透性,抑制白细胞游走反应,但对血浆皮质醇的含量无明显影响。     

Evaluation of anti-inflammatory activity of latex of Calotropis procera in different models of inflammation

AThe anti-inflammatory activity of dry latex (DL) of Calotropis procera was evaluated in various acute and chronic models of inflammation, namely, carrageenan-induced oedema, Freund's adjuvant-induced oedema, cotton pellet granuloma, carrageenan air pouch inflammation, vascular permeability and UV-induced erythema. Oral administration of DL significantly inhibited oedema formation induced by carrageenan and Freund's Adjuvant. It also inhibited granuloma formation induced by cotton pellet and carrageenan. DL significantly inhibited fluid exudation, possibly due to its effect on vascular permeability. Besides, it also delayed the onset and intensity of UV induced erythema. In all these models, the anti-inflammatory activity of DL was comparable to standard antiinflammatory drugs.     

雷醇内酯的抗炎作用

雷醇内酯（Ｔ９）能抑制角叉菜胶、巴豆油和Ｆｒｅｕｎｄ完全佐剂引起的炎性水肿。减少急性胸膜炎渗液量．抑制白细胞游走和棉球肉芽增生。可降低血浆中ＰＧＥ２含量．对肾上腺重量及肾上腺ＶｉｔＣ含量无影响。其抗炎作用的治疗指数为９．８６。结果与雷公藤其它抗炎免疫活性成分的结果相似，证明其为有效成分之一。Ｐ＜０．０１２．３对佐剂致大鼠原发性关节肿胀的影响［６］大鼠随机分为４组，每组８只。分别ｉｐＴ９１．０、０．５ｍｇ·ｋｇ－１，强的松龙１０ｍｇ·ｋｇ－１及等量生理盐水。给药后０．５ｈ，大鼠有足跖ｓｃＦｒｅｕｎｄ完全佐剂０．１ｍｌ致炎，测量致炎前及致炎后１８ｈ的关节周长（ｃｍ），以周长差作为肿胀度指标。结果显示，Ｔ９１．０、０．５ｍｇ·ｋｇ－１均能明显抑制大鼠佐剂性关节肿胀，有量效关系（表３）。表１Ｔ９对角叉菜致大鼠关节肿胀的影响与对照组比较．＊Ｐ＜０．０５．Ｐ＜０．０１表３Ｔ９对大鼠１８ｈ佐剂关节肿胀的影响与对照组比较．＊Ｐ＜０．０５，Ｐ＜０．０１２．４对大鼠急性胸膜炎的影响［７］大鼠随机分为４组，分别ｉｐＴ９０．８、０．４ｍｇ·ｋｇ－１等量生理盐水及ｐｏ阿斯匹林３００ｍｇ·ｋｇ－１。ｉｐ后０．５ｈ或ｐｏ后１ｈ，在乙醚麻?     

Pharmacological Studies On Sterculia Foetida Leaves

An alcoholic extract of Sterculia foetida L. leaves was subjected to pharmacological screening using various animal models. The extract caused reduced exploratory activity in mice. Further it potentiated pentobarbitone sleeping time in normal and chronic pentobarbitone-treated mice. It also potentiated barbital sodium-induced hypnosis, indicating central nervous system depressant activity. The extract also exhibited significant antiinflammatory activity in the acute carrageenan-induced rat paw edema and the chronic granuloma pouch models. However, it was devoid of analgesic activity in the tail flick model.     

美洛昔康抗炎作用的实验研究

目的观察美洛昔康的抗炎作用。方法采用大鼠急性、亚急性及免疫性炎症模型,观察美洛昔康对角叉菜胶致大鼠足跖肿胀和大鼠棉球肉芽肿的影响以及美洛昔康对大鼠佐剂性关节炎的预防和治疗作用。结果美洛昔康对多种致炎剂引起的炎性水肿均具有明显的抑制作用,1.0和3.0mg     

Pharmacological studies on sterculia foetida leaves

An alcoholic extract of Sterculia foetida L. leaves was subjected to pharmacological screening using various animal models. The extract caused reduced exploratory activity in mice. Further it potentiated pentobarbitone sleeping time in normal and chronic pentobarbitone-treated mice. It also potentiated barbital sodium-induced hypnosis, indicating central nervous system depressant activity. The extract also exhibited significant antiinflammatory activity in the acute carrageenan-induced rat paw edema and the chronic granuloma pouch models. However, it was devoid of analgesic activity in the tail flick model.     

The antiinflammatory effect of EB-382

This study was conducted to clarify the antiinflammatory profile of EB-382, comparing it with those of ibuprofen and other antiinflammatory agents. EB-382 had a more potent inhibition on the acetic acid-induced intensive mouse intraperitoneal vascular permeability and carrageenin-induced rat hind paw edema, but a less potent inhibition on the ultraviolet-induced guinea-pig erythema and the prostaglandin biosynthesis in vitro than ibuprofen. The inhibition by EB-382 was equipotent to that of indomethacin on carrageenin-induced rat pleurisy and the zymosan air pouch, and it demonstrated a strong inhibition on the kallikrein and zymosan-induced intensive guinea-pig skin vascular permeability. EB-382 had a more effective activity on paper disk-induced granuloma and adjuvant arthritis, and it had a less potent action on the gastric mucosal membrane than ibuprofen. EB-382 had a weak action on histamine-induced rat back skin vascular permeability and heat-induced protein denaturation and hemolysis in vitro, as also shown by other test agents. The above results indicate that EB-382 will be useful as an antiinflammatory agent with a new pharmacological effectiveness besides possessing properties common to other acidic non-steroidal antiinflammatory agents in clinical studies.