Pharmacological evaluation of Alstonia scholaris: Anti-tussive,anti-asthmatic and expectorant activities

Ethnopharmacological relevance

Alstonia scholaris (Apocynaceae) was documented as an effective herb for the treatment of chronic respiratory diseases in “dai” ethnopharmacy historically, and its leaf crude extract, used for releasing tracheitis and cold symptom, was approved to be a commercial formulation by State Food and Drugs Administration of China (SFDA).

Aim of the study

The investigation evaluates the anti-tussive and anti-asthmatic activities of the ethanolic extract, fractions and main alkaloids of Alstonia scholaris leaf to provide experimental evidence for its traditional and modern clinical use. For our most interesting, is to reveal the active components for further new drug development.

Materials and methods

The leaf of Alstonia scholaris was extracted with ethanol and then separated into different fractions. Furthermore, alkaloids were isolated by phytochemical method. The anti-tussive activity was evaluated using three different models including ammonia or sulfur dioxide induced mice coughing, and citric acid induced guinea pigs coughing. The anti-asthmatic activity was investigated on guinea pigs bronchoconstraction induced by histamine. The expectorant activity was evaluated by volume of phenol red in mice's tracheas.

Results

The alkaloids fraction significantly inhibited mice's frequency of cough induced by ammonia, increased mice's latent period of cough induced by sulfur dioxide, and increased guinea pigs’ latent period of cough and inhibited frequency of cough. Besides, the alkaloids fraction increased delitescence of convulsion, and tumble of guinea pigs in anti-asthmatic test, and enhanced tracheal phenol red output in expectorant evaluation. Moreover, the main alkaloid, picrinine exhibited anti-tussive and anti-asthmatic activities in vivo.

Conclusions

The alkaloids fraction was anti-tussive, anti-asthmatic and expectorant activities component of Alstonia scholaris leaf, and it may also be a valuable lead material for respiratory diseases drug development. Picrinine, the main anti-tussive and anti-asthmatic compound, could be applied in quality control of products from Alstonia scholaris leaf.     

The anti-inflammatory effects of Caragana tangutica ethyl acetate extract

Ethnopharmacological relevance

Caragana tangutica KOM has been used to treat arthritis, wounds, fever and other disease conditions in traditional Chinese medicine (TMC). To support the application of the plant in traditional Chinese medicine by investigating the anti-inflammatory effects of the ethyl acetate extract of Caragana tangutica.

Materials and methods

The anti-inflammatory activity was evaluated by animal models including xylene-induced ear edema in mice, carrageenan-induced paw edema in rats, acetic acid induced writhing in mice and LPS-induced acute lung injury (ALI). The anti-inflammatory mechanism was evaluated by detecting prostaglandin E₂ and immunohistochemistry expression of cyclooxygenase-2 (COX-2) using an EIA assay kit and immunohistochemistry, respectively.

Results

The results showed that the xylene-induced ear edema in mice was significantly reduced by the ethyl acetate extract at dosages of 100, 200 and 400 mg/kg, and the carrageenan-induced paw edema in rats was monitored to be reduced by the ethyl acetate extract 3 h after carrageenan injection. The ethyl acetate extract was also found to reduce the inflammation pain of acetic acid-induced writhing model in a dose-dependent manner and cause reduction of the ALI in mice through the inhibition of the release of PGE₂ and the LPS-induced COX-2 expression in the lung.

Conclusion

Our study demonstrates that the ethyl acetate extract of the plant can help to reduce inflammations by inhibiting the expression of COX-2.     

Anti-inflammatory and analgesic effects of ethanol and aqueous extracts of Pterocephalus hookeri (C.B. Clarke) Höeck

Aim of the study

This study evaluates the anti-inflammatory and analgesic activities of the ethanol and aqueous extracts of a Tibetan herb Pterocephalus hookeri (C.B. Clarke) Höeck to provide experimental evidence for its traditional use such as cold, flu and rheumatoid arthritis.

Materials and methods

Investigations on the analgesic effects of P. hookeri (C.B. Clarke) Höeck were carried out, including hot-plate test and acetic acid-induced writhing. The anti-inflammatory activities were observed by utilizing the following models: carrageenin-induced edema of the hind paw of rats, cotton pellet-induced granuloma formation in rats, acetic acid-induced permeability, and xylene-induced ear edema in mice. The effects of the administration of indomethacin were also studied.

Results

It has been shown that the ethanol and aqueous extracts significantly increased the hot-plate pain threshold and reduced acetic acid-induced writhing response in mice. The ethanol and aqueous extracts remarkably inhibited the increase in vascular permeability induced by acetic acid and ear edema induced by xylene. The ethanol extract also significantly decreased the carrageenin-induced rat paw edema perimeter and inhibited the increase of granuloma weight.

Conclusion

The results show that the ethanol and aqueous extracts have both central and peripheral analgesic activities and as anti-inflammatory effects, supporting the traditional application of this herb in treating various diseases associated with inflammation and pain.     

Alstonia scholaris (L.) R. Br. and Alstonia macrophylla Wall. ex G. Don: A comparative review on traditional uses,phytochemistry and pharmacology

Ethnopharmacological relevance

Alstonia scholaris (L.) R. Br. and Alstonia macrophylla Wall. ex G. Don are two vital medicinal plant species (family: Apocynaceae). In India, the therapeutic use of Alstonia scholaris has been described in both codified and non-codified drug systems for the treatment of malaria, jaundice, gastrointestinal troubles, cancer and in many other ailments. Other species, Alstonia macrophylla has been used in conventional medicines in Thailand, Malaysia and Philippines as a general tonic, aphrodisiac, anticholeric, antidysentery, antipyretic, emmenagogue, and vulnerary agents. In India, Alstonia macrophylla is used as a substitute for Alstonia scholaris in various herbal pharmaceutical preparations. However, one certainly cannot evaluate the truthfulness of a practice (i.e. in scientific terms). In this article we discuss and summarize comparative data about traditional uses, phytochemistry, pharmacology and toxicity of Alstonia scholaris and Alstonia macrophylla. Moreover, in order to unfold future research opportunities, lacunae in the present knowledge are also highlighted.

Materials and methods

Literature about Alstonia scholaris and Alstonia macrophylla was collected by using electronic and library search. Additionally, referred books on traditional medicine and ethnopharmacology were also utilized for receiving traditional records about both the plant species.

Results

Both Alstonia scholaris and Alstonia macrophylla are rich in different types of bioactive alkaloids. So far, broad spectrum of in vitro and in vivo biological and pharmacological activities have been reported to both the species. Amongst them, antimicrobial and anticancer activities were promising.

Conclusions

The use of Alstonia macrophylla as a substitute for Alstonia scholaris is not at all justifiable as both the species are distinct from each other in their phytochemistry and pharmacology. Further detail chemical fingerprinting and metabolic studies of these two species are warranted to prevent their mutual adulteration most importantly in the context of commercial preparations.     

Analgesic and anti-inflammatory effects of Ligularia fischeri leaves in experimental animals

Aim of the study

The ethanol extract (LF) of Ligularia fischeri var. spiciformis (leaf) has been evaluated for antinociceptive and anti-inflammatory activities in mice.

Materials and Methods

Analgesic and anti-inflammatory activities were studied by measuring nociception induced by formalin, acetic acid and hot-plate, and inflammation induced by carrageenan, formalin, and arachidonic acid.

Results

The acute treatment of mice with LF at doses of 100 and 200 mg/kg, by oral administration, produced a significant antinociceptive effect in the acetic acid-induced writhing, formalin-induced pain licking and hot-plate-induced pain. Also, the LF significantly inhibited both carrageenan- and formalin-induced inflammation as well as arachidonic acid-induced ear edema in mice.

Conclusions

These inhibitions were statistically significant (P < 0.05). Thus, our investigation suggests a potential benefit of Ligularia fischeri in treating conditions associated with inflammatory pain.     

Antiinflammatory, analgesic and antioxidant activities of Cyathula prostrata (Linn.) Blume (Amaranthaceae)

Ethnopharmacological relevance

Cyathula prostrata (Linn) Blume (Amaranthaceae) is an annual herb widely used traditionally in the treatment of various inflammatory and pain related health disorders in Nigeria. The aim of this study is to evaluate the anti-inflammatory, analgesic and antioxidant activities of the methanolic extract of Cyathula prostrata (Linn) Blume.

Materials and methods

The anti-inflammatory (phorbol 12-myristate 13-acetate (PMA)-induced reactive oxygen species (ROS), lipopolysaccharide (LPS) induced nitric oxide production in U937 macrophages, LPS-induced COX-2 expression, carrageenan-induced rat paw oedema, arachidonic acid-induced ear oedema and xylene-induced ear oedema), analgesic (acetic acid-induced writhing and hot plate tests) and antioxidant activities (DPPH [1,1-diphenyl-2-picrylhydrazyl] and lipid peroxidation assays) activities of the plant extract were investigated.

Results

The methanolic extract of Cyathula prostrata did not show inhibitory activity in the in vitro PMA-induced reactive oxygen species, LPS-induced nitric oxide production and LPS-induced COX-2 expression assays. In the in vivo anti-inflammatory assays, the extract (50, 100 and 200 mg/kg) showed a significant (P < 0.05) dose-dependent inhibition in the carrageenan, arachidonic acid and xylene-induced tests. Cyathula prostrata produced a significant (P < 0.05, 0.001) dose-dependent inhibition in the acetic acid and hot plate analgesic tests respectively. The plant extract did not exhibit any antioxidant activity in the DPPH and lipid peroxidation assays.

Conclusion

The results suggest that the methanolic extract of Cyathula prostrata possesses anti-inflammatory and analgesic activities and this authenticates the use of the plant in the traditional treatment of ailments associated with inflammation and pain.     

Anti-inflammatory,anti-angiogenic and anti-nociceptive activities of an ethanol extract of Salvia plebeia R. Brown

Ethnopharmacological relevance

Salvia plebeia R. Brown has been used for the treatment of a variety of inflammatory diseases, cold and tumors in many countries, including Korea and China.

Aim of the study

This study aimed to assess anti-inflammatory and related activities of an ethanol extract (SPEE) prepared from the dried whole parts of Salvia plebeia.

Materials and methods

Anti-angiogenic and anti-nociceptive activities of SPEE were analyzed using the chick chorioallantoic membrane (CAM) assay and acetic acid-induced writhing response, respectively. Anti-inflammatory activity of SPEE was evaluated using acetic acid-induced vascular permeability, carrageenan-induced inflammation in the air pouch and analyses of nitrite content and induced nitric oxide synthase (iNOS) level in the macrophage cells.

Results

SPEE gave rise to a significant inhibition in chick chorioallantoic membrane angiogenesis. SPEE exhibited anti-inflammatory activities in vascular permeability and air-pouch models. In the air-pouch model, SPEE was able to diminish exudate volume, number of polymorphonulcear leukocytes and nitrite content. SPEE also displayed anti-nociceptive activity in the writhing response model in mice. SPEE significantly decreased nitrite content and induced nitric oxide synthase (iNOS) in the lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells, while it could not modulate cyclooxygenase-2 (COX-2) and matrix metalloproteinase-9 levels in the stimulated phages. SPEE decreased reactive oxygen species (ROS) level in the stimulated macrophages.

Conclusion

The ethanol extract (SPEE) of Salvia plebeia possesses anti-inflammatory and related anti-angiogenic, anti-nociceptive and antioxidant activities, which offers partial support to its folkloric use.     

Anti-inflammatory and anti-arthritic activity of total flavonoids of the roots of Sophora flavescens

Ethnopharmacological relevance

The roots of Sophora flavescens have long been used in Chinese medicine for the treatment of fever, inflammatory disorders, ulcers and skin burns. Sophora flavescens contains flavonoids and alkaloids.

Aim of the study

This study was conducted to develop a plant-based anti-inflammatory agent focused on chronic inflammatory disorders. To accomplish this, the alkaloid-free prenylated flavonoid-enriched fraction (PFS) of rhizomes of Sophora flavescens was prepared and its in vitro and in vivo anti-inflammatory activities were then evaluated for the first time.

Materials and methods

The inhibitory activity of PFS on PGE₂, NO, IL-6 and TNF-α production of lipopolysaccharide (LPS)-treated RAW 264.7 cells was measured. Additionally, adjuvant-induced arthritis in rats was used as an animal model of chronic inflammation to establish the in vivo anti-inflammatory effects of PFS.

Result

PFS inhibited cyclooxygenase-2 (COX-2)-catalyzed PGE₂ and inducible nitric oxide synthase (iNOS)-catalyzed NO production by lipopolysaccharide (LPS)-treated RAW 264.7 cells at 10–50 μg/ml, and these effects primarily occurred via COX-2 inhibition and iNOS down-regulation, respectively. PFS also inhibited IL-6 and TNF-α production. When tested against adjuvant-induced arthritis in rats (chronic inflammation), PFS strongly inhibited arthritic inflammation when administered orally at doses of 10–100 mg/kg/day. In addition, PFS administered orally potently inhibited acetic acid-induced writhing in mice.

Conclusions

Our results suggest that PFS inhibits chronic inflammatory response and the inhibition of proinflammatory molecules such as COX-2, iNOS and IL-6 may contribute, at least in part, to the anti-inflammatory activity in vivo. Overall, these results indicate that PFS from Sophora flavescens may have the potential for treatment of chronic inflammatory disorders such as rheumatoid arthritis.     

Evaluation of Cissus quadrangularis extracts as an inhibitor of COX, 5-LOX, and proinflammatory mediators

Ethnopharmacological relevance

Cissus quadrangularis is an ancient medicinal plant. It is an active ingredient of one Ayurvedic formula called “Laksha Gogglu”. Its stem is used in food preparation in India. Traditionally it is used to treat various diseases like asthma, indigestion, ear diseases, irregular menstruation, skin diseases, piles, fractured bones, etc.

Aim of the study

This study aimed to evaluate the ability of the plant extracts to inhibit cycloxygenase (COX-1), cycloxygenase (COX-2), and 5-lipoxygenase (5-LOX) enzyme activity. Western blot analysis was also carried out in the quest to determine the effect of active acetone fraction of Cissus quadrangularis (AFCQ) on proinflammatory mediators as acetone extract is found to be the most effective in this study.

Materials and methods

The differential extract of the stem were tested for enzyme inhibition of COX and 5-LOX using spectroscopic and polarigraphic method. Effective acetone extract was partially purified by silica column, one of the active fraction showed dual inhibition against COX and 5-LOX. Western blotting shows downregulation of proinflammatory mediators as well as upregulation of phase-II enzymes.

Results

AFCQ extract showed COX and 5-LOX inhibition with IC₅₀ values of 7 μg/ml, 0.4 μg/ml, and 20 μg/ml for COX-1, COX-2 and 5-LOX respectively. It also showed anti-inflammatory activity on RAW 264.7 cell line with IC₅₀ value 65 μg/ml. In addition to this it is showing inhibition of proinflammatory mediators like iNOS and TNFα, along with translocation of Nrf-2 and upregulation of HO-1.

Conclusion

AFCQ is a COX and 5-LOX inhibitor isolated from the stems of Cissus quadrangularis. It is also effectively downregulate the iNOS, TNFα, and upregulation of HO-1.     

Antinociceptive and anti-inflammatory activities of extract and two isolated flavonoids of Carthamus tinctorius L

Ethnopharmacological relevance

Safflower (Carthamus tinctorius L.) has been long used both in the traditional system and folk medicine as an analgesic anti-inflammatory agent in China. The aim of the study was to evaluate the antinociceptive and anti-inflammatory activities of hydroalcoholic extract (HE) and two isolated kaempferol glycosides of Carthamus tinctorius L. to provide experimental evidence for its traditional use.

Materials and methods

Antinociceptive effects of HE, kaempferol 3-O-rutinoside (K-3-R) and kaempferol 3-O-glucoside (K-3-G) were assessed in mice using the acetic acid-induced writhing test, formalin test and cinnamaldehyde test. The anti-inflammatory effects of HE, K-3-R and K-3-G were determined in two animal models: carrageenan-induced paw edema and xylene-induced ear edema.

Results

The HPLC analysis showed the presence of K-3-R and K-3-G in Carthamus tinctorius L. HE (500 and 1000 mg/kg) as well as K-3-R and K-3-G (150, 300 and 600 mg/kg) produced significant inhibition on nociception induced by acetic acid and formalin. Oral treatment of HE, K-3-R and K-3-G at all doses significantly reduced both the nociceptive response and cinnamaldehyde-induced paw edema, effect that was superior to aspirin. In anti-inflammatory tests, HE and K-3-G significantly inhibited the paw edema during the both phases of carrageenan-induced inflammation while K-3-G suppressed the late phase inflammation only. HE (400 and 800 mg/kg) and K-3-G (200, 400, 800 mg/kg) produced significant dose-dependent inhibition of xylene-induced ear edema development. K-3-R only suppressed ear edema formation at a high dose (800 mg/kg).

Conclusions

These results demonstrate that Carthamus tinctorius L. extract possess remarkable antinociceptive and anti-inflammatory activities which may be due to K-3-R and K-3-G at least in part, supporting the folkloric usage of the plant to treat various inflammatory and pain diseases.     

Anti-inflammatory activity of Markhamia tomentosa (Benth.) K. Schum. Ex Engl. ethanolic leaf extract

Ethnopharmacological relevance

The leaves of Markhamia tomentosa (Benth.) K. Schum (Bignoniaceae) are used traditionally for the treatment of oedema and rheumatoid arthritis in Nigeria.

Aim of the study

The aim of the work was to investigate the anti-inflammatory activity of the ethanolic leaf extract of Markhamia tomentosa.

Materials and methods

The extract was screened using the carrageenan-induced paw oedema in rats, xylene-induced oedema in mice and the formalin-induced oedema in mice at 50, 100, 200 mg/kg doses p.o respectively. The mechanism by which the extract mediated the anti-inflammatory activity was assessed using the histamine-induced rat paw oedema and serotonin-induced rat paw oedema at the highest dose (200 mg/kg).

Results

The results showed that the extract produced a significant dose-dependent inhibition in carrageenan-induced, xylene-induced and the formalin tests. The extract exerted a significant inhibition of 54.55% (P<0.0001) and 42.11% (P<0.01) at 90 min in the histamine-induced and serotonin-induced rat paw oedema models respectively.

Conclusions

These findings suggest that the ethanolic leaf extract of Markhamia tomentosa possesses anti-inflammatory activity possibly mediated by histamine. The results justify the use of the plant in the preparation of ethno medicines used in the treatment of ailments associated with inflammation.     

Comparison of active constituents,acute toxicity,anti-nociceptive and anti-inflammatory activities of Porana sinensis Hemsl., Erycibe obtusifolia Benth. and Erycibe schmidtii Craib

Ethnopharmacological relevance

Erycibe obtusifolia and Erycibe schmidtii, which belong to the same genus as Erycibe, are widely used in traditional medicine for the treatment of joint pain and rheumatoid arthritis (RA). Porana sinensis has become a widely used substitute for Erycibe obtusifolia and Erycibe schmidtii as they have declined in the wild. In the present work, the content of the main active components, the acute toxicity, the anti-nociceptive and anti-inflammatory activities of Porana sinensis, Erycibe obtusifolia and Erycibe schmidtii were compared, and the mechanisms of anti-nociceptive and anti-inflammatory activities were discussed.

Materials and methods

A quantitative HPLC (high performance liquid chromatography) method was first developed to compare the content of the main active components (scopoletin, scopolin and chlorogenic acid). The anti-inflammatory and anti-nociceptive activities of 40% ethanolic extracts of the three plants were compared using the models of xylene-induced ear edema, formalin-induced inflammation, carrageenan-induced air pouch inflammation, acetic acid-induced writhing and formalin-induced nociception. The acute toxicity of the 40% ethanolic extracts of the three plants was studied.

Results

The assay suggested a large content of scopoletin, scopolin and chlorogenic acid in the three plants. The 40% ethanolic extracts of the three plants were almost non-toxic at the dose of 5 g/kg and all of them showed significant anti-inflammatory effects in the tests of xylene-induced ear edema and formalin-induced inflammation. In the carrageenan-induced air pouch inflammation test, the synthesis of PGE2 was significantly inhibited by all the extracts. They significantly inhibited the number of contortions induced by acetic acid and the second phase of the formalin-induced licking response. Naloxone was not able to reverse the analgesic effect of these extracts.

Conclusion

The study identifies the similarity of the three plants in their main active components as well as acute toxicity, anti-nociceptive and anti-inflammatory activities. It supports the use of Porana sinensis as a suitable substitute, but further studies are needed to confirm this.     

Anti-inflammatory and analgesic activities of methanolic extract of Kigelia pinnata DC flower

Ethnopharmacological relevance

Kigelia pinnata DC is extensively used in Indian traditional medicine for several diseases including inflammatory and painful disorders.

Aim of the study

The aim of the present study is to investigate the possible anti-inflammatory and analgesic activities of methanolic extract of Kigelia pinnata flower (MKFL) to support the medicinal uses claimed by folklore practitioners.

Materials and methods

MKFL is evaluated for its anti-inflammatory activity in carrageenan-induced paw edema model in rats and analgesic activity in acetic acid-induced writhing, hot plate and formalin-induced paw licking models in mice.

Results

MKFL exhibited a significant (P < 0.01) anti-inflammatory and analgesic activities with the doses of 100, 200 and 400 mg/kg b.w. in rats and mice respectively.

Conclusions

The results of the experimental study thus strongly support the traditional use of this plant for inflammatory and pain disorders.     

Anti-inflammatory and analgesic activity of aqueous extract of Flos populi

Ethnopharmacological relevance

Flos populi is an important traditional Chinese medicine prepared from the male inflorescence of Populus tomentosa Carr. or Populus canadensis Moench (Salicaceae family). Flos populi is mainly used for the treatment of various inflammatory diseases and anti diarrhea in East Asian countries. The objective of this study was to investigate the anti-inflammatory and analgesic properties of the aqueous extract of Flos populi (FPAE).

Materials and methods

Cotton pellets-induced granuloma, carrageenan-induced paw oedema, arachidonic acid-induced right ear oedema and xylene-induced ear oedema were used to assess anti-inflammatory activity of FPAE and analgesic activity was evaluated by hot plate test, acetic acid-induced abdominal writhing test and formalin test.

Results

FPAE produced significant dose–response anti-inflammatory activity against cotton pellets-induced granuloma. FPAE at dosages of 50, 100 and 200 mg/kg b w. significantly reduced carrageenan-induced paw edema by 48.84% (P<0.05), 54.95% (P<0.05), and 62.05% (P<0.05) at 5 h after carrageenan injection, respectively. FPAE significantly (P<0.05) reduced the ear oedema induced by arachidonic acid and peaked at the dose of 200 mg/kg b w. (40.78%). A significant (P<0.05) dose dependent inhibition of xylene-induced oedema was produced by FPAE and peaked at the highest dose of 200 mg/kg b w. (23.95%). FPAE (50, 100 and 200 mg/kg b w.) produced significant dose–response analgesic activity in the hot-plate test. However, the low percentage inhibition (<50%) suggests that it is not a centrally acting analgesic. Extract at dosages of 50, 100 and 200 mg/kg b w., p.o. significantly reduced acetic acid-induced writhing by 39.6% (P<0.05), 45.4% (P<0.05), and 51.8% (P<0.05), respectively. The extract also caused marked dose-dependent inhibition of formalin-induced pain in the second phase (P<0.05).

Conclusion

The findings in this study suggest that the aqueous extract of Flos populi possesses anti-inflammatory and analgesic activities. These results may support the fact that this plant is used traditionally to cure inflammatory diseases.     

Anti-nociceptive and anti-inflammatory effects of Croton crassifolius ethanol extract

Ethnopharmacological relevance

Croton crassifolius has been used to treat snake bites, stomach ache, sternalgia, joint pain, as well as pharyngitis, jaundice, and rheumatoid arthritis in traditional Chinese medicine. However, there is no scientific evidence which supports the use in the literature.

Aim of the study

To investigate the anti-nociceptive and anti-inflammatory effects of ethanol extract of C. crassifolius.

Materials and methods

Anti-nociceptive actions of C. crassifolius were assessed in mice using the hot-plate test, acetic acid-induced writhing test, and formalin test. Anti-inflammatory effects of C. crassifolius were determined in three animal models: acetic acid-induced capillary permeability accentuation in mice, carrageenan-induced edema of the hind paw in rats, and cotton pellet-induced granuloma formation in rats.

Results

Ethanol extract of C. crassifolius showed no significant anti-nociceptive activity in the hot-plate test. However, extract at dosages of 45, 90 and 180 mg/kg significantly reduced acetic acid-induced writhing by 28.89% (P<0.05), 38.37% (P<0.05), and 56.53% (P<0.001), respectively. The extract also caused marked dose-related inhibition of formalin-induced pain in the second phase (P<0.05 for 45 mg/kg, P<0.001 for 90 and 180 mg/kg extract). C. crassifolius extract at dosages of 45, 90 and 180 mg/kg significantly reduced acetic acid-induced capillary permeability accentuation in mice by 26.18% (P<0.05), 65.70% (P<0.001), and 79.19% (P<0.001), and suppressed carrageenan-induced paw edema by 21.28% (P<0.05), 30.69% (P<0.01), and 49.17% (P<0.001) at 6 h after carrageenan injection, respectively. 180 mg/kg of the extract also showed significant activity against carrageenan-induced paw edema at 4 h. At 90 and 180 mg/kg, the extract inhibited cotton pellet-induced granuloma formation in rats.

Conclusions

These results collectively demonstrate that the ethanol extract of C. crassifolius possesses peripheral anti-nociceptive and anti-inflammatory effects, providing evidence to rationalize the traditional use of C. crassifolius for the treatment of pain and inflammation.     

Analgesic and anti-inflammatory activities of a water extract of Trachelospermum jasminoides (Apocynaceae)

Aims of the study

This study investigated the analgesic and anti-inflammatory effects of a water extract of Trachelospermum jasminoides (WET) in ICR mice.

Materials and methods

In HPLC analysis, the fingerprint chromatogram of WET was established. Acetic acid-induced writhing response and formalin-induced pain were examined the analgesics effects of WET. WET on λ-Carrageenan(carr)-induced paw edema was performed. We investigate the anti-inflammatory mechanism of WET via studies of the activities of glutathione peroxidase (GPx), glutathione reductase (GRx) in the liver and the levels of malondialdehyde (MDA) and nitrite oxide (NO) in the edema paw. Serum NO and TNF-α were also measured.

Results

The fingerprint chromatogram of WET was established through HPLC analysis, and implies that WET contains the active ingredient gallic acid, chlorgenic acid, caffeic acid, taxifolin, isoquercitrin and quercetin. WET significantly inhibited the numbers of acetic acid-induced writhing responses and the formalin-induced pain in the late phase. In the anti-inflammatory test, WET inhibited the development of paw edema induced by carr. WET decreased the paw edema at the third, fourth and fifth hour after carr administration, and increased the activities of SOD, GPx and GRx in the liver tissue and decreased the MDA level in the edema paw at the third hour after carr injection. WET decreased the level of NO in edematous paw tissue and in serum level, and diminished the level of serum TNF-α at the fifth hour after carr injection.

Conclusions

These results demonstrated that WET is an effective anti-inflammatory agent in carr-induced inflammation. WET probably exerts anti-inflammatory effects by suppressing TNF-α and NO. The anti-inflammatory mechanism of WET might be related to the decrease in the level of MDA in the edema paw via increasing the activities of SOD, GPx and GRx in the liver.     

Analgesic and anti-inflammatory effects of the dry matter of culture broth of Termitomyces albuminosus and its extracts

Aim of the study

The objectives of this study were to investigate the analgesic and anti-inflammatory effects of the dry matter of culture broth (DMCB) of Termitomyces albuminosus in submerged culture and its crude saponin extract (CSE) and crude polysaccharide extract (CPE).

Materials and methods

The analgesic effects of DMCB, CSE and CPE were evaluated with models of acetic acid-induced writhing response and formalin test in mouse. The anti-inflammatory effects of DMCB, CSE and CPE were evaluated by using models of xylene-induced mouse ear swelling and carrageen-induced mouse paw edema.

Results

The DMCB, CSE and CPE significantly decreased the acetic acid-induced writhing response and the licking time on the late phase in the formalin test. Treatment of DMCB (1000 mg/kg), CSE (200 mg/kg) or CPE (200 mg/kg) inhibited the mouse ear swelling by 61.8%, 79.0% and 81.6%, respectively. In the carrageen-induced mouse paw edema test, the group treated with indomethacin showed the strongest inhibition of edema formation by 77.8% in the third hour after carrageenan administration, while DMCB (1000 mg/kg), CSE (200 mg/kg) and CPE (200 mg/kg) showed 48.4%, 55.6% and 40.5%, respectively.

Conclusions

The results suggested that DMCB of Termitomyces albuminosus possessed the analgesic and anti-inflammatory activities. Saponins and polysaccharides were proposed to be the major active constituents of Termitomyces albuminosus in submerged culture.     

Appraisal of antinociceptive and anti-inflammatory potential of extract and fractions from the leaves of Torreya grandis Fort Ex. Lindl

Torreya grandis (Taxaceae) was studied for antinociceptive and anti-inflammatory effects. Leaves were extracted with 80% ethanol at 80 °C for 3 h and fractionated with petroleum ether, chloroform, ethylacetate and n-butanol. The aqueous ethanolic extract (aq.EE), ethylacetate fraction (EaF) and butanol fraction (BtF) at the doses of (100 and 200 mg/kg, i.g.) body weight were used for study. Evaluation of antinociceptive activity was carried out by acetic acid-induced writhing response and formalin-induced paw licking time in the first and second phases of mice. The paw edema induced by formalin- and xylene-induced ear edema were used to assess anti-inflammatory activity. It was found that Torreya grandis extract and fractions at the doses of (100 and 200 mg/kg, i.g.) were significantly attenuated the writhing responses induced by acetic acid and second phase of pain response induced by subplantar injection of formalin in mice. In addition, these extract and fractions inhibiting the formaldehyde-induced arthritis as well as xylene-induces edema prolifically. From acute oral toxicity studies no mortality was pragmatic even at highest dose (2500 mg/kg, i.g.). Furthermore, our phytochemical studies indicated that the aq. ethanolic extract of leaves contains alkaloids, flavonoids, tannins, terpenoids and saponins. The results provide justification for the folkloric uses of Torreya grandis in the treatment of analgesic and inflammatory-based diseases across the China.     

Antipyretic,analgesic, anti-inflammatory and antioxidant activities of two major chromenes from Melicope lunu-ankenda

Aim of the study

Melicope lunu-ankenda (Gaertn.) T.G. Hartley is used in Indian traditional medicine for fever, improving complexion and as a tonic. Previous studies have isolated fungicidal, antifeedant, anti-inflammatory and immunomodulatory compounds from Melicope lunu-ankenda. This study is aimed at the isolation and biological activity screening of potential molecules from the volatile oils and extracts of Melicope lunu-ankenda in the light of traditional applications.

Materials and methods

Volatile oil of Melicope lunu-ankenda leaves was isolated by hydrodistillation, characterized by GC–FID, GC–MS, LRI determination, Co-GC and database searches. Major chromene-type compounds in Melicope lunu-ankenda leaf oil, evodione and leptonol, were isolated by preparative TLC and characterized by UV–Vis, IR, 1H-, 13C-, 13C-DEPT NMR and EIMS. They were also isolated from the petroleum ether and acetone extracts of the leaves of Melicope lunu-ankenda by column chromatography in petroleum ether–ethyl acetate. Their contents in leaf oil, leaf and inflorescence extracts were estimated by HPTLC. Antipyretic (Baker's yeast-induced fever test), analgesic (acetic acid-induced writhing, tail immersion assays), anti-inflammatory (carrageenan-induced paw edema) and in vitro antioxidant (DPPH radical, superoxide radical scavenging) activities of evodione and leptonol were tested.

Results and conclusions

Gas chromatographic analyses found 50.7% monoterpene hydrocarbons, 0.4% oxygenated monoterpenes, 3.2% sesquiterpene hydrocarbons, 0.7% oxygenated sesquiterpenes and 43.7% chromene-type compounds in Melicope lunu-ankenda leaf oil, with evodione (20.2%) and leptonol (22.5%) as its two major constituents. HPTLC estimations in the petroleum ether, acetone extracts (leaf, inflorescence) and leaf oil found evodione 1.0% (dr. wt., leaf), 1.1% (inflorescence), 0.04% (fr. wt. leaves, leaf oil), and leptonol 0.3% (leaf), 0.3% (inflorescence) and 0.04% (leaf oil). Leptonol (200 mg/kg) showed good antipyretic activity. DPPH radical scavenging assay found moderate activity for leptonol (68.7%, 500 μM), whereas evodione showed near-zero activity. A very similar trend was found in superoxide radical scavenging activity of leptonol (64.5%) and evodione (10.3%), both at 100 μg/ml. Evodione and leptonol showed moderate analgesic activities in acetic acid-induced writhing and tail immersion assays. Moderate anti-inflammatory activity was found for both evodione (59.4%) and leptonol (49.0%) at 100 mg/kg.

Ethnopharmacological relevance

Biological activities of evodione and leptonol isolated from Melicope lunu-ankenda justify its traditional uses as a remedy for fever, inflammation and as a tonic.