Analgesic and anti-inflammatory properties of Thespesia populnea leaf extracts

Analgesic and anti-inflammatory activities of the aqueous and ethanol extracts of Thespesia populnea Soland. ex. Correa (Malvaceae) leaves were evaluated in animal models. Orally-administered aqueous and ethanol extracts (100, 200 and 400?mg?kg?1 bw) showed significant analgesic activity in chemical-, mechanical- and thermally-induced pain test models in mice. The extracts also reduced paw oedema induced by carrageenan in rats. The results obtained in this study suggest that Thespesia populnea extracts have analgesic and anti-inflammatory properties.     

Anti-Inflammatory and Analgesic Activity of Total Flavone of <em>Cunninghamia lanceolata</em>

The present study was undertaken to investigate the anti-inflammatory and analgesic activity of total flavone of branches and leaves of Cunninghamia lanceolata (TFC) to provide a scientific basis for its clinical use and resource development. TFC was evaluated for anti-inflammatory and analgesic activity in mice or rats using chemical and thermal models of nociception, including acetic acid-induced writhing test, hot plate latency test, formalin test and carrageenan induced paw oedema test. Results showed that TFC given orally can significantly attenuate acetic acid-induced writhing in mice in a dose-dependent manner. In the hot plate latency test, TFC showed common activity in prolonging duration time only at the highest dose (400 mg/kg). Each dose of TFC could not significantly inhibit the first phase but was active in the later phase of formalin-induced pain, whereas morphine showed notable activity in the two phases. In the carrageenan-induced paw oedema model, TFC could significantly and dose-dependently reduce the carrageenan-induced paw edema at the third and fifth hour, and decrease the content of PEG₂ in paw edema tissue and that of COX-2 in blood serum. It may be concluded that TFC showed both anti-inflammatory and analgesic effects, showing that it can be of importance in drug development, especially in the field of pain and inflammation.     

A novel antinociceptive sulphated polysaccharide of the brown marine alga Spatoglossum schroederi

Sulfated polysaccharides (SP) of brown algae (Phaeophyta) are composed mainly of alpha- L-fucose, being classified as fucans, with recognized role in inflammation but not in nociception, which was already described for SP obtained from red algae. Here the SP of the brown marine alga S. schroederi (named Ss-SP) was isolated and assayed for the antinociceptive effect. Ss-SP was isolated by DEAE-cellulose, analyzed by agarose gel electrophoresis and evaluated in nociception models (Formalin, Hot plate, Von Frey) using Swiss mice (20-25g). Anion exchange chromatography provided four major fractions being F1 (Ss-SP) that of highest metachromatic activity and sugar content. Ss-SP inhibited both phases of the formalin test. In the first phase the paw licking (55.2 +/- 8.07s) was reduced by 45% (30.5 +/- 6.51s) and 40% (32.85 +/- 8.66s) at 0.1 and 1 mg/kg, respectively. In the second phase, Ss-SP was also inhibitory about 39%, but only at 1 mg/kg (83.0 +/- 15.70s) compared to formalin (136.8 +/- 10.27s). This inhibitory effect suggests a mixed mechanism similar to morphine, which was not confirmed in the hot plate test, a model of pain associated with central neurotransmission. However, Ss-SP reduced the animal reaction in response to stimulation withVon Frey filament at the 2nd and 3rd h (20.8 +/- 6.86% versus carrageenan: 47.9 +/- 5.83%; 33.3 +/- 7.71% versus carrageenan: 62.5 +/- 9.83%). Accordingly, the paw edema induced by carrageenan (0.08 +/- 0.01g) was potently reduced in 45.35% by Ss-SP pre-treatment (0.02 +/- 0.003g), corroborating the anti-inflammatory activity demonstrated for brown seaweed polysaccharides. In conclusion our data revealed for the first time the antinociceptive effect of Ss-SP which could be used as a new source of analgesic substances.     

Structural,functional, molecular,and biological evaluation of novel triterpenoids isolated from Helichrysum stoechas (L.) Moench. Collected from Mediterranean Sea bank: Misurata- Libya

Helichrysum stoechas (L.) Moench (Family Compositae) is a medicinal herb endowed with several pharmacological activities. Ethanolic extract of the aerial parts of the plant was used for the isolation of lignoceric acid (HS-02), lanost-5- en-3β-ol- 26-oic acid (HS-03), and lanost-5-en-26-oic acid-3β-olyl palmitate (HS-04). All molecules were screened for anti-inflammatory and analgesic activities at 5 and 10 mg/kg body weight doses, and the TEST program assessed their toxicity. The molecular interaction profile with numerous anti-inflammatory drug targets was investigated by molecular docking. Compounds HS-03 and HS-04 showed a significant reduction in paw volume compared to the control group challenged with carrageenan in the rats, and prolongation of the paw licking/jumping and reduction in the number of writhes was noted after the injection of acetic acid in mice. In a hot plate test, all compounds showed significant pain inhibition. These findings might aid in the development of anti-inflammatory and anti-analgesic therapies.     

Antinociceptive and anti-inflammatory activities of the essential oil of Nepeta crispa Willd. in experimental rat models

This study was conducted to evaluate the antinociceptive and anti-inflammatory activities of the essential oil of Nepeta crispa. The study was done using the tail-flick and formalin test pain models and the paw oedema model of inflammation. Male Wistar rats were used as the animal model. The essential oil dose-dependently produced analgesia in the acute pain models, including the tail-flick (p?相似文献   

Antinociceptive profile of 2,3,6-trisubstituted piperidine alkaloids: 3-O-acetyl-spectaline and semi-synthetic derivatives of (-)-spectaline

In early studies, we have reported the antinociceptive profile of (-)-spectaline, a piperidine alkaloid from Cassia spectabilis. The present study describes the synthesis, the antinociceptive and anti-inflammatory activities of a series of 2,3,6-trialkyl-piperidine alkaloids: the natural (-)-3-O-acetyl-spectaline (LASSBio-755) and ten semi-synthetic spectaline derivatives. Structure-activity relationship (SARs) studies were performed. The structures of all synthesized derivatives were confirmed by means of nuclear magnetic resonance. Compounds were evaluated for their analgesic (acetic acid-induced mouse abdominal constrictions, hot-plate test, formalin-induced pain test) and some of them for the anti-inflammatory activities (carrageenan-induced rat paw edema test). The pharmacological results showed that several of the new compounds given orally at a dose of 100 micromol/kg significantly inhibited the acetic acid-induced abdominal constrictions, but they were less active than (-)-spectaline. LASSBio-755 and LASSBio-776 were the most actives with 37% and 31.7% of inhibition. In the formalin-induced pain only LASSBio-776 was able to inhibit by 34.4% the paw licking response of the inflammatory phase, (-)-spectaline and LASSBio-755 did show any activity. In the carrageenan-induced rat paw edema, only (-)-spectaline exhibited an anti-inflammatory profile, showing an ED(50) value of 56.6 micromol/kg. Our results suggest different mechanisms of action for the analgesic activity observed for LASSBio-776 (3-O-Boc-spectaline), LASSBio-755 (3-O-acetyl-spectaline) and (-)-spectaline (LASSBio-754). The antinociceptive profile of some of the semi-synthetic spectaline derivatives extends our research concerning the chemical and pharmacological optimization of isolated natural products in the search of new drug candidates from Brazilian biodiversity.     

Analysis of alkannin derivatives from Alkanna species by high-performance liquid chromatography/photodiode array/mass spectrometry

Alkannin, shikonin (A/S) and their derivatives are enantiomeric hydroxynaphthoquinone red pigments found in the roots of almost 150 species of the Boraginaceae family. A/S have been shown to exhibit strong wound healing, antimicrobial, anti-inflammatory and antioxidant activities and recent extensive research has well established their antitumor properties. A/S and their derivatives comprise the active ingredients of several pharmaceutical and cosmetic preparations. Although A/S have been efficiently synthesized and have been produced by cell tissue cultures in high yield, most of the pharmaceutical preparations worldwide contain A/S extracted from the roots of Boraginaceous species, found in nature. In the present study, a high-performance liquid chromatography/photodiode array/mass spectrometry (HPLC/PDA/MS) method was established to identify monomeric hydroxynaphthoquinones of the alkannin series and other metabolites from Boraginaceous root extracts. This method can be applied for the identification of alkannin derivatives and other metabolites from Boraginaceous cell cultures, and also to determine active ingredients in pharmaceutical preparations containing A/S derivatives. A phytochemical investigation of the Alkanna genus grown in Greece was also performed. Fifty-three root samples belonging to 10 species of the genus Alkanna (A. calliensis, A. corcyrensis, A. graeca, A. methanaea, A. orientalis, A. pindicola, A. primuliflora, A. sieberi, A. stribrnyi and A. tinctoria) were collected from several regions of the Greek flora and analyzed for their constituent hydroxynaphthoquinones and other metabolites. In most of the above Alkanna samples tested, the main hydroxynaphthoquinones were determined to be beta,beta-dimethylacrylalkannin, isovalerylalkannin + alpha-methyl-n-butylalkannin and acetylalkannin. The hydroxynaphthoquinone constituents and their proportions were found to vary among Alkanna species. Unknown metabolites (not monomeric hydroxynaphthoquinones) were detected by HPLC-PDA-MS, while in several Alkanna species hydroxynaphthoquinones were detected for the first time.     

Bioactive compounds,anti-inflammatory,anti-nociceptive and antioxidant potentials of ethanolic leaf fraction of Sida linifolia L. (Malvaceae)

This study investigated the bioactive compounds, anti-inflammatory, anti-nociceptive, and antioxidant properties of the ethanolic leaf fraction of Sida linifolia (ELFSL). The in vitro anti-inflammatory study employed membrane stabilization, phospholipase A2, platelet aggregation, albumin denaturation, and protease inhibition assays. Intraperitoneal injection of freshly prepared carrageenan solution (0.1 mL of 0.01 g/mL), undiluted egg albumin (0.1 mL), acetic acid (0.6 % (v/v) (10 mL/kg bw), and formalin solution (0.02 mL of 1 % v/v) into mice hind paw, were used to evaluate the anti-inflammatory and anti-nociceptive mechanisms, respectively. In vitro antioxidant potentials were determined using 1,1-Diphenyl-2-picryl-hydrazyl (DPPH), nitric oxide (NO), ferric reducing power (FRAP), and total antioxidant capacity (TAC) assays. Varying quantities of flavonoids, phenols, tannins, saponins, terpenoids, steroids, and alkaloids, were detected in the fraction. GC-FID phytochemical profiling of ELFSL revealed a high level of epicatechin, moderate levels of catechin, kaempferol, flavone, naringenin, rutin flavanones, tannins, sapogenins, proanthocyanidin, and steroids, and small amounts of sparteine, resveratrol, and lunamarine. The ELFSL exerted excellent dose-dependent in vitro anti-inflammatory activities comparable with standard drugs (aspirin/prednisolone). The LD₅₀ test showed safety up to 5000 mg/kg body weight (per oral) ELFSL. Interestingly, mice pre-administered various doses (200, 400, 600 mg/kg bw, po) of ELFSL showed significant (P < 0.05) reduction in edema, writhing, and time spent licking paw in all phases compared with control and were at par with 100 mg/kg bw (po) aspirin. The result also registered good concentration-dependent antioxidant potentials for ELFSL and was comparable to standards (gallic acid, butylated hydroxytoluene, and ascorbic acid). These imply that ELFSL possesses excellent antioxidant, anti-inflammatory, and anti-nociceptive potentials mediated by peripheral and central mechanisms.     

Anti-inflammatory activity of an alkaloid from Solanum trilobatum on acute and chronic inflammation models

The solasodine isolated from Solanum trilobatum has been examined for possible anti-inflammatory activity in acute and chronic inflammatory animal models. Solasodine (5, 30 and 75?mg?kg?1) exerted statistically significant and dose-dependent anti-inflammatory activity in carrageenan-induced rat paw oedema, which was similar to that of indomethacin (10 mg?kg?1), a known anti-inflammatory agent. At the dose of 75?mg?kg?1, solasodine inhibited the arachidonic acid-elicited rat paw oedema 1 h after arachidonic acid challenge. Topical application of solasodine significantly inhibited the ear inflammation induced by multiple applications of tetradecanoyl-phorbol 13-acetate. It also suppressed the volume of exudates, total leucocytes and amount of neutrophil migration into the rat pleural cavity. Administration of solasodine at a dose of 75 mg?kg?1 significantly inhibited the adjuvant-induced rat paw oedema. These results suggest that solasodine exerts anti-inflammatory activity, at least partly through the inhibition of cyclooxygenase and 5-lipoxygenase pathways.     

Analgesic properties of extracts and fractions from Erythrina crista-galli (Fabaceae) leaves

The present study describes the analgesic activity of extracts and some fractions obtained from Erythrina crista-galli leaves in different in vivo analgesic models, using mice as experimental animals. The results showed that extract E(2) was the most active, inhibiting 48% of the abdominal constrictions when evaluated against the writhing test at 10 mg kg(-1), intraperitoneal. It also caused dose-dependent inhibition in the same model, with a calculated ID(50) value and respective confidence interval of 10 (9-14) mg kg(-1), and was more potent than reference drugs. Administered orally, E(2) caused potent antinociceptive action, with a calculated ID(50) value of 35 (26-47) mg kg(-1). The fractions F(1) and F(2) obtained from E(2) were evaluated against the writhing test at 10 mg kg(-1), causing inhibitions of 41 and 88%, respectively. The most active fraction, F(2), presented ID(50) calculated value of 3 (2-4) mg kg(-1), being about 7-fold more active than the reference drugs (acetyl salicylic acid and acetaminophen). In the formalin test, F(2) inhibited both phases of pain (44%, first phase; 58%, second phase). However, in contrast to the results observed for E(2), it was not active against the hot-plate test. The phytochemical results showed that at least four main components are present in F(2), which show a positive reaction of terpenes with TLC spray reagents.     

Evaluation of the Antinociceptive,Antiallodynic, Antihyperalgesic and Anti-Inflammatory Effect of Polyalthic Acid

Nonsteroidal anti-inflammatory drugs (NSAIDs) are very commonly used, but their adverse effects warrant investigating new therapeutic alternatives. Polyalthic acid, a labdane-type diterpenoid, is known to produce gastroprotection, tracheal smooth muscle relaxation, and antitumoral, antiparasitic and antibacterial activity. This study aimed to evaluate the antinociceptive, antiallodynic, antihyperalgesic and anti-inflammatory effect of polyalthic acid on rats. Moreover, the effectiveness of treating hyperalgesia with a combination of polyalthic acid and naproxen was analyzed, as well as the type of drug–drug interaction involved. Nociception was examined by injecting 1% formalin into the right hind paw and thermal hyperalgesia and inflammation by injecting a 1% carrageenan solution into the left hind paw of rats. Allodynia was assessed on an L5/L6 spinal nerve ligation model. Polyalthic acid generated significant antinociceptive (56–320 mg/kg), antiallodynic (100–562 mg/kg), and antihyperalgesic and anti-inflammatory (10–178 mg/kg) effects. Antinociception mechanisms were explored by pretreating the rats with naltrexone, ODQ and methiothepin, finding the effect blocked by the former two compounds, which indicates the participation of opioid receptors and guanylate cyclase. An isobolographic analysis suggests synergism between polyalthic acid and naproxen in the combined treatment of hyperalgesia.     

Analgesic and anti-inflammatory activities of the sesquiterpene fraction from Annona reticulata L. bark

The sesquiterpene fraction of Annona reticulata bark was studied by GC/MS. Three major components were identified: copaene (35.40%), patchoulane (13.49%) and 1H-cycloprop(e)azulene (22.77%). The fraction was also screened for its analgesic and anti-inflammatory activities. The sesquiterpene fraction at doses 12.5 and 25?mg?kg?1 and the unsaponified petroleum ether extract at a dose of 50?mg?kg?1 exhibited significant central as well as peripheral analgesic and anti-inflammatory activities. These activities were comparable with the standard drugs used in the respective experiments.     

Antinociceptive activity of discretamine isolated from Duguetia moricandiana

The phytochemical study of Duguetia moricandiana Mart. (Annonaceae) yielded the isolation of the alkaloid which was identified by spectral analysis as discretamine. The evaluation of antinociceptive activity carried out by the acetic acid-induced writhing, formalin and hot plate tests in mice, suggests a potent antinociceptive effect. Discretamine (5, 10 and 20?mg?kg?1, i.p.) significantly reduced the number of writhes similarly at all doses tested and the number of paw licks during the first phase of formalin test when compared to control. The effect of discretamine on hot plate response provides a confirmation of its central effect. These results indicate antinociceptive properties of this alkaloid.     

Synergistic antinociceptive activity of combined aqueous extracts of Artemisia campestris and Artemisia herba-alba in several acute pain models

In this study, total phenolic and flavonoid contents, acute toxicity and the antinociceptive activity of Artemisia campestris and Artemisia herba-alba, individually and in combination, were investigated using multiple forms of pain in animals. Our results have been shown that plants are relatively safe without clinical signs of toxicity in animals. Thus, extracts were presented high levels in phenolic and flavonoid contents. Artemisia decoctions with 100, 200, 400 mg/kg b-w studied dose, clearly attenuate chemical and thermal noxious stimuli in writhing, formalin and hot-plate tests, and significantly reduced paw oedema in formalin test. Additionally, binary combination forms exhibited a great improvement in intensity and amplitude of antinociceptive activity in comparison with both plants used individually by a relative interference with opioid system. Our findings suggested the central and peripheral analgesic properties and confirmed the folkloric medicinal use of these plants in pain symptom treatment.     

Synthesis and characterization of cobalt and manganese complexes of indomethacin and comparative study of local analgesic,anti-inflammatory,and anti-ulcerogenic properties

The aim of the study was to synthesize cobalt and manganese complexes of indomethacin and their biological activity screening to uncover. The structures of metal complexes were elucidated by FT-IR, UV-Vis and atomic absorption spectroscopy, X-ray diffraction and calorimetric DSC. Heat radiant tail-flick test for local analgesic activity of cobalt complex of indomethacin in the doses of 50 and 100 μg/mL demonstrated potent local analgesic response. Manganese complex of indomethacin exhibited similar potent of activity at the dose of 100 μg/mL. Anti-inflammatory study of the indomethacin-manganese and indomethacin-cobalt complexes demonstrated their activity (paw edema inhibition of 71.67% at 20 mg/kg dose in the 1 h and 83.33% at 10 mg/kg dose in the 4 h) comparable with the standard diclofenac sodium. Gastrointestinal efficacy of cobalt and manganese complexes was close to that of indomethacin.     

Anti-inflammatory,analgesic and molecular docking studies of Lanostanoic acid 3-O-α-D-glycopyranoside isolated from Helichrysum stoechas

Helichrysum stoechas has been conventionally used as herbal tea due to its anti-inflammatory, antioxidant, antimicrobial and diuretic activities. Ethanolic extract of the aerial parts of the plant (HSE) afforded a lanostane triterpenoid glycoside. The isolated compound was characterized as Lanostan-3β-olyl-26-oic acid 3-O-α-D-glycopyranoside (HS-01) with the help of UV, IR, ¹H, ¹³C NMR and MS spectroscopic techniques. HSE (at 100 and 200 mg/kg doses) and the isolated compound, HS-01 (at 10 mg/kg dose) has been investigated for anti-inflammatory and analgesic activities against chemically challenged experimental animal. Both the HSE as well as HS-01 showed a substantial decline in paw volume when compared with the relevant control groups (p < 0.01 & p < 0.001). The HSE and HS-01 also confirms a significant prolongation of the paw licking or jumping towards the Eddy’s hot plate and reduction in quantity of writhes after the introduction of acetic acid in mice (p < 0.01 & p < 0.001). In order to have a better understanding of the binding interactions of HS-01 at molecular level, docking studies were performed with various macromolecular drug targets using AutoDock 4.2 and AutoDock Vina 1.1. Both programs predicted Galectin-3 as most favorable target for HS-01 followed by iNOS, whereas TNFα and COX-2 were among less favorable. Therefore, HS-01 could be developed as suitable therapy against inflammation and associated disorders.     

Anti-inflammatory and analgesic effects of human placenta extract

In this study, we investigated the effects of human placenta extract (HPE, Laennec inj.) on pro-inflammatory cytokines and mediators secreted from lipopolysaccharide-stimulated RAW264.7 macrophages. We found that HPE significantly inhibited the production of nitric oxide, tumour necrosis factor-α and cyclooxygenase-2. We studied the anti-inflammatory and analgesic potential of HPE in murine models of inflammation/inflammatory pain. Rats were assigned to six groups and were administered either saline or HPE (0.33, 1, 3 and 6 mL kg?1) intraperitoneally. Diclofenac was used as a positive control. HPE attenuated the swelling of the rat's hind paw. The vascular permeability induced by acetic acid was significantly reduced by HPE. HPE reduced the formation of granuloma in carrageenan air pouch and hind paw oedema in complete Freund's adjuvant-induced chronic arthritis in rats. HPE attenuated writhing episodes. An increase in hot-plate latency was observed in mice receiving HPE. HPE also increased the pain threshold in the Randall-Selitto test. In the tail-flick assay, HPE prolonged the reaction time of rats to radiant heat stimulation. These results suggest that HPE has potent anti-inflammatory and anti-nociceptive activities.     

Phenyl propanoid rich extract of edible plant Halosarcia indica exert diuretic,analgesic, and anti-inflammatory activity on Wistar albino rats

Abstract

Halosarcia indica (Amaranthaceae), an Edible food used in Indian traditional folk medicine. The present study aims to evaluate the diuretic, analgesic, and anti-inflammatory properties of Halosarcia indica aqueous extract (HAE) on Wistar albino rats. HAE was found to contain chlorogenic acid, sinapic acid, caffeic acid, ferulic acid, scopoletin, quercetin 3-O-β-D-glucoside and β-sitosterol-D-glucopyranoside. HAE increased the urine excreted (Diuretic Index: 1.62–1.96 over 2–10?h) and curbed writhing responses significantly (40%) compared to aspirin (54.56%). It showed significant reduction in carrageenan plantar edema (42%) similar to indomethacin (48%). Anti-inflammatory activity by Cotton Granuloma method proved that HAE significantly reduced weights of pellets (dry weight 44.93?mg, wet weight 127.45?mg) similar to diclofenac sodium (dry weight 33.2?mg, wet weight 123.58?mg). Acute toxicity studies showed HAE to be safe until 2000?mg/kg. The above findings evidently propose that HAE has diuretic, analgesic and anti-inflammatory activity as observed with rodent models.     

Topical anti-inflammatory constituents of lipophilic leaf fractions of Alchornea floribunda and Alchornea cordifolia

The leaves of Alchornea floribunda and Alchornea cordifolia are used traditionally as topical anti-inflammatory agents. In this study, two highly lipophilic fractions AFLF and ACLF isolated from A. floribunda and A. cordifolia leaves respectively were investigated for topical anti-inflammatory effects using xylene-induced mice ear oedema as a model of inflammation. AFLF and ACLF at 5?mg per ear showed significant (p?相似文献   

Anti-Inflammatory,Antipyretic, and Analgesic Properties of Potamogeton perfoliatus Extract: In Vitro and In Vivo Study

Natural antioxidants, especially those of plant origins, have shown a plethora of biological activities with substantial economic value, as they can be extracted from agro-wastes and/or under exploited plant species. The perennial hydrophyte, Potamogeton perfoliatus, has been used traditionally to treat several health disorders; however, little is known about its biological and its medicinal effects. Here, we used an integrated in vitro and in vivo framework to examine the potential effect of P. perfoliatus on oxidative stress, nociception, inflammatory models, and brewer’s yeast-induced pyrexia in mice. Our results suggested a consistent in vitro inhibition of three enzymes, namely 5-lipoxygenase, cyclooxygenases 1 and 2 (COX-1 and COX-2), as well as a potent antioxidant effect. These results were confirmed in vivo where the studied extract attenuated carrageenan-induced paw edema, carrageenan-induced leukocyte migration into the peritoneal cavity by 25, 44 and 64% at 200, 400 and 600 mg/kg, p.o., respectively. Moreover, the extract decreased acetic acid-induced vascular permeability by 45% at 600 mg/kg, p.o., and chemical hyperalgesia in mice by 86% by 400 mg/kg, p.o., in acetic acid-induced writhing assay. The extract (400 mg/kg) showed a longer response latency at the 3 h time point (2.5 fold of the control) similar to the nalbuphine, the standard opioid analgesic. Additionally, pronounced antipyretic effects were observed at 600 mg/kg, comparable to paracetamol. Using LC-MS/MS, we identified 15 secondary metabolites that most likely contributed to the obtained biological activities. Altogether, our findings indicate that P. perfoliatus has anti-inflammatory, antioxidant, analgesic and antipyretic effects, thus supporting its traditional use and promoting its valorization as a potential candidate in treating oxidative stress-associated diseases.