Bioactivity guided isolation of analgesic and anti-inflammatory constituents of Cnestis ferruginea Vahl ex DC (Connaraceae) root

Ethnopharmacological relevance

Cnestis ferruginea (CF) Vahl ex DC (Connaraceae) is a shrub widely used in Traditional African Medicine (TAM) for the treatment of various painful and inflammatory conditions.

Aim of the study

To isolate the active pharmacological constituents responsible for the anti-inflammatory and antinociceptive properties of the methanolic root extract of C. ferruginea.

Materials and methods

The crude methanolic root extract of CF was sequentially fractionated into four sub extracts (chloroform, ethylacetate, n-butanol and the remaining aqueous fraction). The aqueous–butanol fractions, having showed significant inhibition of inflammation and pain, were subjected to fractionation through successive column chromatography on silica gel 60–120 mesh, eluted with a gradient of CHCl₃–MeOH.Sixty five fractions were collected; fractions with similar TLC profiles were grouped into seven major fractions (1–7). Fraction 4 being the most active in bioassay was rechromatographed to obtain CF-2. Analgesic activity was evaluated using the acetic acid-induced writhing and hot plate tests in mice while carrageenan induced paw oedema test was used to investigate the anti-inflammatory actions of the fractions obtained.

Result

Amentoflavone (CF-2) was isolated from the aqueous/n-butanol fraction. CF-2 (12.5, 25 and 100 mg/kg; p.o) produced significant (P<0.05) dose dependent inhibition of pain response elicited by acetic acid and increased nociceptive reaction latency in hot plate test. In addition it produced significant (P<0.05) dose-dependent inhibition of oedema in the carrageenan-induced inflammation.

Conclusion

This study showed that amentoflavone is responsible for the analgesic and anti-inflammatory activity of Cnestis ferruginea.     

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.     

Analgesic and anti-inflammatory activities of Cnestis ferruginea Vahl ex DC (Connaraceae) methanolic root extract

Ethnopharmacological relevance

Cnestis ferruginea Vahl ex DC (Connaraceae) is a shrub widely used in traditional African Medicine (TAM) for the treatment of various painful and inflammatory conditions.

Aim of the study

The objective of this study was to investigate the analgesic and anti-inflammatory properties of the methanolic root extract of Cnestis ferruginea.

Materials and methods

Analgesic activity was evaluated using the acetic acid-induced writhing, formalin, tail clip, and hot plate tests in mice. The carrageenan- and egg albumin-induced rat paw oedema, formaldehyde-induced arthritis inflammation, and xylene-induced ear oedema tests were used to investigate the anti-inflammatory actions of Cnestis ferruginea.

Results

The methanolic root extract of Cnestis ferruginea (100, 200, and 400 mg/kg; p.o.) produced significant (P < 0.05) dose-dependent inhibition of pain response elicited by acetic acid and formalin while also increasing the nociceptive reaction latency in the tail clip and hot plate tests. In respect of anti-inflammatory activity, Cnestis ferruginea caused significant (P < 0.05) dose-dependent inhibition of oedema development in the carrageenan, egg albumin, formaldehyde, and xylene-induced inflammation tests. The effects of the extract in the various models were generally comparable to those of the standard drugs used.

Conclusion

The findings in this study suggest that the methanolic root extract of Cnestis ferruginea possesses analgesic and anti-inflammatory activities possibly mediated through peripheral and central mechanisms involving inhibition of release and/or actions of vasoactive substances (histamine, serotonin and kinins) and prostaglandins. The results justify the use of the extract in TAM for the treatment of painful and inflammatory conditions.     

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.     

Involvement of the L-arginine-nitric oxide pathway in the antinociception caused by fruits of Prosopis strombulifera (Lam.) Benth

Ethnopharmacological relevance

Prosopis strombulifera (Lam.) Benth. is a rhizomatous shrub that grows in the north and central zone of Argentina. In folk medicine, the fruits of this plant have been used as an astringent, anti-inflammatory and odontalgic agent and anti-diarrheic.

Aim of the study

To investigate the antinociceptive effect of ethanol (EE), chloroform (CE) and ethyl acetate (EtOAcE) extracts of Prosopis strombulifera fruits and the involvement of the l-arginine-nitric oxide pathway in this effect.

Materials and methods

The antinociceptive effects of the EE, CE and EtOAcE of Prosopis strombulifera fruits were evaluated in vivo using the formalin-induced pain test in mice with aspirin and morphine as reference antinociceptive compounds. The participation of the l-arginine-nitric oxide pathway in the antinociceptive effect was investigated in the same animal model using l-arginine as a nitric oxide (NO) precursor. The in vitro inhibitory effect of the extracts on LPS-induced nitric oxide production and iNOS expression was investigated in a J774A.1 macrophage-derived cell line.

Results

CE (300 mg/kg), in contrast to EE and EtOAcE, caused significant inhibition (p < 0.05) of the in vivo nociceptive response. Moreover, CE (100–1000 mg/kg, p.o.) produced a dose-dependent inhibition of the neurogenic and the inflammatory phases of the formalin test with inhibition values (at 600 mg/kg) of 42 ± 7% and 62 ± 7%, respectively. CE inhibition was more potent in the inflammatory phase, with an ID₅₀ of 400.1 (252.2–634.8) mg/kg. The antinociception caused by CE (600 mg/kg, p.o.) was significantly attenuated (p < 0.05) by i.p. treatment of mice with l-arginine (600 mg/kg). In addition, CE (100 μg/mL) produced significant in vitro inhibition (p < 0.001) of LPS-induced NO production, which was not observed with EE and EtOAcE at the same concentration. The inhibition of NO production by CE (10–100 μg/mL) was dose-dependent, with an IC₅₀ of 39.8 (34.4–46.1) μg/mL, and CE significantly inhibited LPS-induced iNOS expression in J774A.1 cells.

Conclusions

This study supports, in part, the ethnomedical use of Prosopis strombulifera fruits by showing that its CE produces moderate antinociception in vivo. The findings also provide scientific information for understanding the molecular mechanism involved in the analgesic effect of this plant.     

Aegiceras corniculatum extract suppresses initial and late phases of inflammation in rat paw and attenuates the production of eicosanoids in rat neutrophils and human platelets

Aim of the study

The present study is designed to explore the anti-inflammatory potential of Aegiceras corniculatum Linn. Blanco stems extracts and their mechanism of action against various pro-inflammatory mediators and to validate its traditional use against inflammatory diseases.

Materials and methods

Rat paw edema and peritonitis models were employed for in vivo studies. For in vitro studies human platelets and rat neutrophils were stimulated with Ca²⁺-ionophore A23187 leading to the production of various pro-inflammatory metabolites, i.e., 12-HTT, 12-HETE and LTB₄ and 5-HETE which were quantified by HPLC.

Results

The highly polar methanol extract (100 mg/kg) caused ∼90% reduction in the carrageenan- and prostaglandin E2-induced paw edema in rats. It also caused the inhibition of cycloxygenase-1 metabolite, 12-HHT (IC₅₀ 41.1 ± 1.5 μg/ml) with a concomitant rise in 12-lipoxygenase metabolite, 12-HETE in A23187 stimulated human platelets. Conversely, the non-polar hexane extract attenuated (IC₅₀ 0.36 ± 0.12 μg/ml) 12-HETE formation with a parallel rise in 12-HHT, thereby displaying a selectivity towards 12-lipoxygenase. Non-polar hexane extract also antagonized the production of 5-lipoxygenase metabolites, i.e., leukotriene B₄ and 5-HETE in the rat neutrophils. Furthermore, ethyl acetate extract inhibited both COX and 5-LOX with a marked decline in the production of 12-HHT (IC₅₀ 0.08 ± 0.002 μg/ml) and LTB₄ (IC₅₀ 0.86 ± 0.03 μg/ml), respectively. The anti-inflammatory effect of hexane and ethyl acetate extracts was also reflected by the diminution of carrageenan-induced cell infiltration in rat peritoneum. Additionally, plant extracts caused ∼60% suppression in dextran-induced paw edema implying that they also ameliorate histamine and serotonin release.

Conclusion

Hexane, ethyl acetate and methanol extracts derived from Aegiceras corniculatum possess significant anti-inflammatory activity via multiple mechanisms and validate their traditional use against inflammation-related diseases.     

Anti-nociceptive and anti-inflammatory activity of sophocarpine

Aim of the study

This study aimed to assess the anti-nociceptive and anti-inflammatory activity of sophocarpine in rodents.

Materials and methods

The anti-nociceptive effect was evaluated in two experimental animal models and anti-inflammatory effect in three animal models, and sophocarpine was given by tail vein injection for the above study.

Results

Pretreatment with a single dose of sophocarpine (20 and 40 mg/kg) produced dose-dependent anti-nociceptive effects in thermally and chemically induced mouse pain models. Pretreatment with a single dose of sophocarpine also produced significant dose-dependent anti-inflammatory effects on carrageenan-induced rat hind paw edema (15 and 30 mg/kg), xylene-induced mouse ear edema (20 and 40 mg/kg) and acetic acid-induced mouse vascular permeation (20 and 40 mg/kg).

Conclusions

Sophocarpine possesses peripheral and central analgesic properties as well as anti-inflammatory activity on acute inflammatory processes.     

Analgesic and anti-inflammatory activities of ethanol root extract of Mahonia oiwakensis in mice

Aims of the study

This study investigated the anti-inflammatory and analgesic activities, and protoberberine alkaloid contents of ethanol extract of MO roots (MOR_EtOH).

Materials and methods

The analgesic activity of MOR_EtOH was determined using acetic acid-induced writhing response and formalin test. The anti-inflammatory activity of MOR_EtOH was determined using the λ-carrageenan-induced paw oedema model. The protoberberine alkaloid contents of MOR_EtOH were identified by high-performance liquid chromatography (HPLC).

Results

MOR_EtOH (100 and 500 mg/kg) decreased the acetic acid-induced writhing responses and licking times of the second phase in the formalin test. Moreover, carrageenan-induced paw oedema was significantly reduced in a dose-dependent manner by administering MOR_EtOH (100 and 500 mg/kg) at 3, 4, and 5 h after the carrageenan injection. The serum levels of tumor necrosis factor-α (TNF-α) and nitric oxide (NO) of MOR_EtOH-treated mice were significantly reduced compared with those in the serum of animals administered carrageenan. Notably, MOR_EtOH attenuated the expression of cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS) and neutrophil infiltration in paw tissues injected with carrageenan. The anti-inflammatory mechanisms of MOR_EtOH appear to be related to the inhibition of neutrophil infiltration, iNOS and COX-2 protein expression, NO release, and the decreasing TNF-α level in serum. The analytical results showed that the contents of berberine, palmatine and jatrorrhizine were 191.45 mg/g extract, 100.15 mg/g extract and 66.45 mg/g extract, respectively.

Conclusion

These experimental results suggest that MOR_EtOH produced both analgesic and anti-inflammatory effects in mice and may be a candidate for the development of pharmacological agents used in the treatment of inflammatory disorders.     

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.     

Anticonvulsant activity of the essential oil and methanolic extract of Bunium persicum (Boiss). B. Fedtsch

Ethnopharmacological relevance

Bunium persicum is an endemic plant to Iran which its seeds have a long history of medicinal uses.

Aim of the study

This work aimed to study the anticonvulsant effect of the essential oil and methanolic extract of the plant.

Materials and methods

The essential oil and methanolic extract of the plant were studied against pentylenetetrazole (PTZ) and maximal electroshock (MES) induced convulsions in mice in different doses. The neurotoxicity of the essential oil and methanolic extract was investigated using rotarod method.

Results

The essential oil and methanolic extract prolonged the onset of clonic and tonic seizures in PTZ. The tonic seizures were prevented by essential oil in both methods at dose of 1 mL/kg and higher doses. The methanolic extract inhibited PTZ-convulsions at dose 3 g/kg and was ineffective against MES induced convulsion.

Conclusions

The essential oil of the plant might be useful to control absence and grand mal seizures at dose 1 mL/kg. This activity might be due to its content of monoterpenes.     

A report on anti-oedemogenic activity of Byttneria herbacea roots--possible involvement of histamine receptor (type I)

Ethnopharmacological relevance

The traditional healers of the Kol tribes of West Bengal, Bihar and Jharkhand (India), widely use the woody rootstock of Byttneria herbacea to reduce the swelling of limbs, due to filariasis. Besides filariasis different part of this plant is used for the treatment of cholera, diarrhoea and asthma.

Aim of this study

This study is a preliminary attempt to evaluate the anti-oedemogenic activity of the roots of Byttneria herbacea.

Materials and methods

The anti-oedemogenic activity of the hydroalcoholic extract of the roots of Byttneria herbacea (HBH) was evaluated against carrageenan and histamine induced rat paw oedema, acetic acid induced writhing and histamine induced vascular permeability in mice. Further, the effect of HBH on the expression of human histamine receptor type I (H1R) was studied in HeLa cells.

Results

HBH exhibited significant dose-dependent inhibition (*p < 0.05) against carrageenan and histamine induced rat paw oedema. Similar significant dose-dependent inhibition was observed against acetic acid induced writhing and histamine-induced vascular permeability in mice. Moreover, H1R specific mRNA expression was also significantly (*p < 0.05) suppressed by HBH.

Conclusion

HBH was observed to possess anti-oedemogenic activity which is probably mediated through suppression of H1R.     

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-inflammatory and anti-nociceptive activities of ethanolic extract and its various fractions from Adiantum capillus veneris Linn

Aim of the study

To investigate the anti-inflammatory and anti-nociceptive activities of the crude ethanolic extract of Adiantum capillus veneris Linn. (Adiantaceae) and its various fractions.

Materials and methods

The ethanolic extract and its fractions were given at a dose of 200 mg/kg po and 300 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 300 mg/kg po. Gastric ulceration studies have been further carried out to study the antiulcer effect of the ethanolic extract and its various fractions at dose of 900 mg/kg body weight.

Results

Amongst the tested fractions, the ethyl acetate fraction exhibited better inhibition (67.27%) at 300 mg/kg po dosage when compared to the standard drug Indomethacin (63.63%) after 3 h in the carrageenan induced hind paw edema. The anti-inflammatory activity of the ethanolic extract and its various fractions appear to be related to the inhibition of NO release, and the decreasing TNF-α level. The ethanolic extract and all its fractions especially the ethyl acetate (p < 0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug, i.e. ibuprofen. The histopathological study of ethanolic extract and its fractions reveals that none of them cause ulcer.

Conclusion

The present study indicates that Adiantum capillus veneris Linn. has significant anti-inflammatory and analgesic effect.     

Studies on the analgesic,anti-inflammatory and antipyretic effects of Parquetina nigrescens leaf extract

Ethnopharmacological relevance

Parquetina nigrescens is a shrub that is commonly used in different parts of West Africa for the treatment of several ailments which includes pain, fever and inflammatory conditions.

Aim of the study

The present study was designed to investigate the analgesic, anti-inflammatory and antipyretic effects of the aqueous extract of Parquetina nigrescens leaves in rats.

Materials and methods

Five groups were used for each study, groups 1 and 5 served as control (saline) and reference (indomethacine) respectively, while groups 2–4 received the extract (50–200 mg/kg) orally. Formalin paw licking and hot plate latency tests were used for analgesic studies. Carrageenan oedema, cotton pellet granuloma and formaldehyde arthritis models were used to quantify the anti-inflammatory activities while the brewer’s yeast was used for inducing pyrexia.

Results

The results of the analgesic study show that the extract produced significant (p < 0.05) analgesia in the hot plate and in the formalin tests. In the anti-inflammatory study, Parquetina nigrescens produced significant (p < 0.05) inhibition of the various types of inflammation. The extract also inhibited the pyrexia induced by brewer’s yeast.

Conclusion

The result justifies the traditional uses of Parquetina nigrescens for the treatment of fever, inflammatory and painful conditions.     

Suppressive effects of wild bitter gourd (Momordica charantia Linn. var. abbreviata ser.) fruit extracts on inflammatory responses in RAW 264.7 macrophages

Aim of the study

Bitter gourd (Momordica charantia) is used to treat various diseases including inflammation. A wild species of bitter gourd, Momordica charantia Linn. var. abbreviata ser. (WBG), is considered to be more potent in disease prevention than is bitter gourd; however, little is known about the biological and physiological characteristics of WBG.

Materials and methods

The present study investigated the anti-inflammatory effect of WBG on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages.

Results

Among the hot water, 95% ethanol, and ethyl acetate extracts of WBG, the ethanol extract showed the greatest reduction of LPS-induced nitric oxide (NO) and prostaglandin E₂ (PGE₂) production and inducible nitric oxide synthase (iNOS) and pro-interleukin-1β expression. LPS-induced cyclooxygenase-2 expression was not affected by WBG extracts. Compared with WBG, extracts from bitter gourd showed a lesser inhibition of LPS-induced events. Electrophoretic mobility shift assay further showed that both the hot water and the ethanol extracts of WBG inhibited NF-κB activation. Although information is lacking on the bioactive components of WBG, the phenolic compound contents of each extract significantly paralleled its anti-inflammatory ability (r = 0.74, 0.88 and 0.65 for NO, PGE₂ and iNOS expression, respectively, P < 0.05).

Conclusions

These results suggest that WBG is beneficial for reducing LPS-induced inflammatory responses by modulating NF-κB activation.     

Potentiality of standardized extract and isolated flavonoids from Zuccagnia punctata for the treatment of respiratory infections by Streptococcus pneumoniae: in vitro and in vivo studies

Ethnopharmacological relevance

Zuccagnia punctata Cav. (Fabaceae) is a monotypic species distributed in western Argentina and is traditionally used for the treatment of bacterial and fungal infections. The aim of this study was to demonstrated the antibacterial activity of the Zuccagnia punctata standardized extract and the structurally related non-methoxylated flavonoids with similar pattern of substitution and differences in ring C present in this plant species: 7-hydroxyflavanone (HF), 2′,4′-dihydroxychalcone (DHC) and 3,7-dihydroxyflavone (DHF), against Streptococcus pneumoniae clinical isolates using in vitro and in vivo models.

Materials and Methods

MIC values of natural products were determined by agar macrodilution method. In vivo activities were investigated in a Streptococcus pneumoniae infection model in mice. Lung and blood samples were obtained for bacterial cell counts. The serum was used by biochemical analysis (alanine transaminase, aspartate transaminase, urea and creatinine) in order to evaluate the toxicity of natural products.

Results

All samples showed antimicrobial activity in vitro with MIC values between 50 and 500 μg/ml. Zuccagnia punctata extract (1 mg/mice) and HF (1 mg/mice) significantly reduced the number of viable Streptococcus pneumoniae in lung (p < 0.01) while lower quantities has not effect. Therefore, the present study has shown that intake once or twice a day of 1 mg of Zuccagnia punctata extract or HF for seven days did not result in toxicity.

Conclusions

Our results showed that Zuccagnia punctata extract as well as one of its isolated flavonoids, 7-hydroxyflavanone, could be useful for the development of a novel respiratory infections treatment.     

Anti-inflammatory and anti-nociceptive activities of Platanus orientalis Linn. and its ulcerogenic risk evaluation

Ethnopharmacological relevance

Leaves of Platanus orientalis Linn. are used in folk medicine as a wound-healer and ophthalmologic agent. Phytol derivatives from the leaves of plane-tree show anti-ulcer activity. Its analgesic and anti-inflammatory effects for knee pain were known to Persian scientists and hakims.

Materials and methods

The ethanolic extract of Platanus orientalis Linn. and its various fractions were given at a dose of 100 mg/kg po and 200 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 200 mg/kg po. Gastric ulceration studies have been further carried out to study the ulcerogenic risk evaluation of the ethanolic extract and its various fractions at a dose of 600 mg/kg body weight.

Results

Among the tested fractions, chloroform fraction exhibited better inhibition (68.33%) at 200 mg/kg po dosage when compared to the standard drug Ibuprofen (66.66%) after 3 h in the carrageenan induced hind paw edema. The ethanolic extract and all its fractions especially the chloroform (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug i.e. Ibuprofen. The histopathological study of ethanolic extract and its fractions revealed that none of them cause ulcer.

Conclusion

The present study indicates that Platanus orientalis Linn. has significant anti-inflammatory and analgesic effect.     

Anti-aromatase activity of the constituents from damiana (Turnera diffusa)

Ethnopharmacological relevance

Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac.

Aim of the study

The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from Turnera diffusa.

Materials and methods

The methanolic extract and 24 compounds isolated from the leaves of Turnera diffusa were evaluated for aromatase activity by using a tritiated-water release assay and for estrogenic activity by using yeast estrogen screen (YES) assay.

Results

The methanolic extract demonstrated a dose-dependent inhibitory activity of the aromatase enzyme with the IC₅₀ value of 63.1 μg/ml. Among the 24 tested compounds, pinocembrin and acacetin showed the most potent inhibition with IC₅₀ values of 10.8 and 18.7 μM, respectively. Estrogenic activity was also observed in the extract and three compounds including apigenin 7-glucoside, Z-echinacin and pinocembrin with EC₅₀ values of 10, 20 and 67 μM, respectively.

Conclusions

The extract of Turnera diffusa and two isolated compounds pinocembrin and acacetin could significantly suppress aromatase activity. Moreover, apigenin 7-glucoside, Z-echinacin and pinocembrin showed estrogenic activity.