• 제목/요약/키워드: Antinociceptive activity

검색결과 69건 처리시간 0.021초

Sulfuretin, an Antinociceptive and Antiinflammatory Flavonoid from Rhus verniciflua

  • Choi, Jong-Won;Yoon, Byung-Jae;Han, Yong-Nam;Lee, Sang-Kook;Lee, Kyung-Tae;Park, Hee-Juhn
    • 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.

Synthesis of Novel 6,7,8,9-Tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted Hydrazino Thiazolo (2,3-b) Quinazoline as Potent Antinociceptive and Anti-inflammatory Agents

  • Selvam, T. Panneer;Kumar, P. Vijayaraj
    • Bulletin of the Korean Chemical Society
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    • 제31권11호
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    • pp.3265-3271
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    • 2010
  • A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index ($0.51{\pm}1.63$, $0.48{\pm}1.28$ and $0.50{\pm}1.53$, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.

Effects of various receptor antagonists on the peripheral antinociceptive activity of aqueous extracts of Dicranopteris linearis, Melastoma malabathricum and Bauhinia purpurea leaves in mice

  • Zakaria, Zainul Amiruddin;Sodri, Nurul Husna;Hassan, Halmy;Anuar, Khairiyah;Abdullah, Fatimah Corazon
    • 셀메드
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    • 제2권4호
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    • pp.38.1-38.6
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    • 2012
  • The present study aimed to determine the possible mechanisms of the peripheral antinociception of the aqueous extracts of Dicranopteris linearis (AEDL), Melastoma malabathricum (AEMM) and Bauhinia purpurea (AEBP) leaves in mice. Briefly, the antinociceptive profile of each extract (300, 500, and 1000 mg/kg; subcutaneous (s.c.)), was established using the abdominal constriction test. A single dose (500 mg/kg) of each extract (s.c.) was pre-challenged for 10 min with various pain receptors' antagonists or pain mediators' blockers and 30 min later subjected to the antinociceptive assay to determine the possible mechanism(s) involved. Based on the results obtained, all extracts exerted significant (p < 0.05) antinociceptive activity with dose-dependent activity observed only with the AEMM. Furthermore, the antinociception of AEDL was attenuated by naloxone, atropine, yohimbine and theophylline; AEMM was reversed by yohimbine, theophylline, thioperamide, pindolol, reserpine, and 4-chloro-DL-phenylalanine methyl ester hydrochloride; and of AEBP was inhibited by naloxone, haloperidol, yohimbine and reserpine. In conclusion, the antinociceptive activity of those extracts possibly involved the activation of several pain receptors (i.e. opioids, muscarinic, ${\alpha}_2$-adrenergic and adenosine receptors, adenosine, H3-histaminergic and $5HT_{1A}$, dopaminergic receptors).

Cytotoxicity and antinociceptive activity of Jasminum sambac leaves

  • Islam, Md Rahatul;Rouf, Razina;Barua, Juwel;Uddin, Shaikh Jamal;Alamgir, Mahiuddin
    • Advances in Traditional Medicine
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    • 제8권2호
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    • pp.204-206
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    • 2008
  • The ethanolic extract of Jasminum sambac leaves were tested for its cytotoxicity and possible antinociceptive activity in experimental animals. The extract showed potent cytotoxic activity in brine shrimp lethality assay and the LC50 was found only 25 mg/ml. The extract significantly and dose dependently inhibited the acetic acid induced writhing in mice (56.83%, P < 0.001 and 43.17%, P < 0.001 for 500 and 250 mg/kg body weight, respectively). The results supported its traditional uses.

Antinociceptive activity of some Bangladeshi medicinal plant extracts

  • Uddin, S.J.;Shilpi, J.A.;Rouf, R.;Ferdous, M.M.;Nahar, L.;Sarker, S.D.
    • Advances in Traditional Medicine
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    • 제6권2호
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    • pp.96-101
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    • 2006
  • The extracts of some Bangladeshi medicinal plants, Possur (Xylocarpus mekongensis), Dhundul (Xylocarpus granatum), Gab (Diospyros peregrina), Kadom (Anthocephalus chinensis) and Sundari (Heritiera fomes), were assessed for their possible antinociceptive activity using acetic acid induced writhing model in mice. Most of these plants have been used in traditional medicine in Bangladesh as well as in other countries for the treatment of various ailments ranging from common cold to cancer. All these extracts significantly inhibited the acetic acid induced writhing in mice at the oral dose of 500 mg/kg body weight. The extract of Anthocephalus chinensis bark showed the most potent writhing inhibition (69.47%, P < 0.001) and that of Diospyros peregrina bark had the least (33.54%, P< 0.02).

음나무 잎 및 수피의 진통소염효과 및 아주반트로 유발된 산화적 스트레스에 대한 효과 (In vivo Antinociceptive Antiinflamatory and Antioxidative Effects of the Leaf and Stem Bark of Kalopanax pictus in Rats)

  • 박희준;남정환;정현주;김원배;박광균;정원윤;최종원
    • 생약학회지
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    • 제36권4호통권143호
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    • pp.318-323
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    • 2005
  • The leaves (KPL) of Kalopanax pictus (KP) are used as a vegetable or a functional food in Korean society. The stem bark (Kalopanacis Cortex, KPS) has been traditionally used to treat neurotic pain, rheumatoid arthritis and diabetic disease. This research was undertaken to demonstrate that the leaf extract of KP (KPL) has also the antinociceptive and antiinflammatory effects like the extract (KPS) of Kalopanacis Cortex and to compare the activity levels of several extracts obtained from KP. Antinociceptive and antiinflammatory effects were measured against the extracts described as followings; KPL-1 (the MeOH extract obtained from the leaf shoot of KP collected on May), KPL-2 (the MeOH extract from KP collected on June), KPL-3 (the MeOH ectract from KP with no thorns), KPS-1 (MeOH extract from KPS of a Korean habitat), KPS-2 (MeOH extract from KPS of a Chinese habitat). The antimociceptive test undertaken by acetic acid-induced writhing, hot plate-, and tail-flick methods using mice. The anti-inflammatory test was also undertaken by measuring the edema in the carrageenan-induced test. The order of activity potency in the antinociceptive and antiinflammatory assays was commonly shown as followings: KPL-3>KPS>1>KPS-2>KPL-1>KPL-2. This order was also observed in acetic acid-induced vascular permeability test. The antiinflammatory activity in carrageenan-induced assay was also observed as the following order: KPL-3>KPS- 1>PS-2>KPL-1>KPL-2. In addition, adjuvant-induced rats were used for a model to assess the oxidative stress. Treatment of the rat with the extracts reduced serum thiobarbituric acid-reactive substances (TBARS), hydroxy radical(OH) and superoxide dismutase(SOD) activity caused by FCA together together with the inhibition of hepatic TBARS level and lipofuscin content. The above finding suggests that the leaf extract has the antinociceptive and antinflammatory activity. It is also suggested that KPL-3 with more potent activity than other tested extracts could be developed for a new available biomaterial.

Analgesic and antipyretic actions of Muntingia calabura leaves chloroform extract in animal models

  • Zakaria, ZA;Kumar, G Hanan;Zaid, Siti NH Mohd;Ghani, Marwiza A;Hassan, MH;Hazalin, Nurul AMN;Khamis, Mahirah M;Devi, G Rathna;Sulaiman, MR
    • Advances in Traditional Medicine
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    • 제7권1호
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    • pp.34-40
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    • 2007
  • The present study was carried out to elucidate the potential of Muntingia (M.) calabura leaves chloroform extract (MCCE) as antinociceptive, anti-inflammatory and antipyretic agents using various animal models. The dried powdered leaves of M. calabura (20 g) were soaked in chloroform for 72 h and the supernatant obtained was then evaporated to dryness. The crude dried extract (0.912 g), dissolved in dimethyl sulfoxide (1:20; w/v) and considered as a stock solution (100% concentration/strength), was then diluted to the concentrations of 10 and 50% and used together in all experimental models. The MCCE was found to show significant (P < 0.05) antinociceptive and antipyretic activities, but less remarkable anti-inflammatory activity. Only the antinociceptive activity of MCCE measured using the abdominal constriction test and in the first phase of the formalin test occurred in a concentration-dependent manner. The anti-inflammatory activity of 50 and 100% concentrations MCCE was observed only at the range of time interval of 60 - 120 and 60 min, respectively. Based on the results, we conclude that the M. calabura leaves chloroform extract possessed remarkable antinociceptive and antipyretic, but less effective anti-inflammatory, activities and thus justifies the Peruvian folklore claims of its medicinal values.

Antinociceptive, antidiarrhoeal and cytotoxic activity of Aegiceras corniculatum

  • Ahmed, F;Mamun, AH AI;Shahid, IZ;Rahman, AA;Sadhu, SK
    • Advances in Traditional Medicine
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    • 제7권2호
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    • pp.191-196
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    • 2007
  • The ethanol extract of leaves of the mangrove Aegiceras corniculatum Blanco (Myrsinaceae) was screened for its antinociceptive, antidiarrhoeal and cytotoxic activities. The extract produced significant writhing inhibition in acetic acid-induced writhing in mice at the oral dose of 250 and 500 mg/kg body weight (P < 0.001), which was comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. When tested for its antidiarrhoeal effects on castor oil induced diarrhoea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the oral dose of 500 mg/kg body weight (P<0.05; P<0.01) comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. Moreover, when tested for toxicity using brine shrimp, the extract showed potent activity against the brine shrimp Artemia salina ($LC_{50}$ 10 mg/ml). The overall results tend to suggest the antinociceptive, antidiarrhoeal and cytotoxic activities of the extract.

Anti-inflammatory, antinociceptive and diuretic activities of Amoora cucullata Roxb.

  • Das, AK;Shahid, IZ;Choudhuri, MSK;Shilpi, JA;Ahmed, Firoj
    • Advances in Traditional Medicine
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    • 제5권1호
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    • pp.37-42
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    • 2005
  • The crude methanolic extract of the leaves of Amoora cucullata Roxb. was investigated for its possible anti-inflammatory activity using carrageenin induced rat paw edema model and cotton pellet implantation method in rat. The extract was also studied for its antinociceptive activity using acetic acid induced writhing model in mice. At the doses of 200 and 400 mg/kg body weight, the extract showed significant anti-inflammatory activity in both models. At the same doses, the extract also significantly reduced the number of acetic acid-induced abdominal constriction (writhing) in mice. The crude extract also showed significant diuretic activity in albino mice.

Antinociceptive and Sedative Hypnotic effect of Artemisia pallens Wall

  • Karunanidhi, Natesan;Saravanan, Sampath;Vinothkumar, Vinothkumar;Selvamani, Selvamani;Ghosh, Shruti;Gupta, Jayanta Kumar
    • Natural Product Sciences
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    • 제9권2호
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    • pp.91-92
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    • 2003
  • The present investigation was carried out to evaluate the antinociceptive and sedative - hypnotic effect of a vacuum dried methanol extract of aerial parts of Artemisia pallens. In the tail-flick method with Swiss albino mice the methanol extract at the doses of (1500 mg/kg, 2000 mg/kg, and 2500 mg/kg) showed significant antinociceptive activity. Significant potentiation of Pentobarbitone sodium - induced sleeping time was observed in mice on co-administration of the various doses of the methanol extract of Artemisia pallens.