Trypanocidal Sesquiterpenes from Lychnophora Species

The bioguided fractionation of the crude extracts of Lychnophora passerina (Mart. ex DC) Gardn., L. pinaster Mart. and L. trichocarpha Spreng. led to the isolation of four compounds active against the trypomastigote forms of Trypanosoma cruzi : the sesquiterpene lactones goyazensolide (1), eremantholide C (2), and lychnopholide (3) and a new caryophyllene derivative, which was named lychnophoic acid (4).     

Sedative activity of hexane extract of Keampferia galanga L. and its active compounds

Ethnopharmacological relevance

It is well known that fragrance impacts behaviors and autonomic functions, and is increasingly used as relaxant, carminative, as well as sedative in aromatherapy. Kaempferia galanga L. is one of the popular traditional aromatic medicinal plants used in tropics and subtropics of Asia including China, Japan and Indochina.

Aim of the study

The aim of present study was to investigate sedative effects of hexane extract of Kaempferia galanga L.and 2 active aromatic compounds (compound 1: ethyl trans-p-methoxycinnamate and compound 2: ethyl cinnamate ) included in the extyract by means of inhalation in mice.

Materials and methods

Sedative activity was assessed by inhalation of the hexane extract and two major aromatic compounds.

Results

Inhalation of hexane extract at the doses of 1.5 and 10 mg showed significant reduction of locomotor activity, indicating considerable sedative and relaxant effects. Compound 1 and 2 were proved to possess sedative effects at 0.0014 mg and 0.0012 mg respectively.

Conclusions

These results suggest the promising application of Kaempferia galanga L. and its constituents in aromatherapy.     

Genotoxic and mutagenic properties of Bauhinia platypetala extract,a traditional Brazilian medicinal plant

Ethnopharmacological relevance

Bauhinia platypetala Burch. is a traditionally used Brazilian medicinal plant, although no evidence in the literature substantiates the safety of its use.

Aim of the study

The aim of this study was to investigate the safety of the ethanolic extract and the ethereal fraction of B. platypetala leaves.

Materials and methods

The identification of chemical compounds from the B. platypetala ethanolic extract and its ethereal fraction was performed by GC/MS and ESI-MS/MS. The plant’s toxicological, cytotoxic, mutagenic and genotoxic properties were determined in Saccharomyces cerevisiae strains and V79 cell culture by survival assays and comet assay.

Results

The major compound identified in the B. platypetala ethanolic extract is palmitic acid, kaempferitirin and quercitrin, while the B. platypetala ethereal fraction was found to be rich in phytol, gamma-sitosterol and vitamin E. Moreover, the results indicated that the B. platypetala ethanolic extract has an anti-oxidative effect against H₂O₂ in yeast. In addition, the B. platypetala ethanolic extract did not induce mutagenic effects on the S. cerevisiae N123 strain, but the ethereal fraction of B. platypetala at higher concentrations (250–500 μg/mL) induced cytotoxicity and mutagenicity. A slight cytotoxic effect was observed in mammalian V79 cells; however, both the B. platypetala ethanolic extract and its ethereal fraction were able to induce DNA strand breaks in V79 cells, as detected by the alkaline comet assay.

Conclusion

The B. platypetala ethanolic extract has antioxidant action and showed absence of mutagenic effects in yeast S. cerevisiae. On the other hand B. platypetala ethereal fraction is mutagenic and does not show antioxidant activity in yeast. In mammalian cells B. platypetala ethanolic extract and it's ethereal fraction induce cyotoxic and genotoxic action.     

Erythropoietic activity of Asteracantha longifolia (Nees.) in rats

Ethnopharmacological relevance

Asteracantha longifolia Nees. (Family-Acanthaceae) is a wild herb commonly used in traditional ayurvedic medicine as Kokilaaksha and the Unani drug as Talimakhana in India and Srilanka for various medicinal uses as aphrodisiac, tonic, sedative and blood diseases etc.

Aim of the study

The aim of the current study was to validate and explore the folk use of Asteracantha longifolia Nees. (AL) (Leaf part) on pharmacological grounds using haloperidol induced iron deficiency anemia for the assessment of erythropoietic activity.

Materials and methods

Determination of iron in plant extracts was carried out using spectrophotometric method. Plant extract was obtained from crude drugs using extraction with ethanol. In vivo study, haloperidol induced iron deficiency anemia model was used in experimental studies.

Results

An administration of ethanolic extract of AL at the doses of 100 mg/kg and 200 mg/kg body weight, i.p., demonstrated a significant (P < 0.05) increase in erythrocyte count, haemoglobin count, serum iron and serum protein etc. This effect may be due to the presence of iron (622 μg/50 mg) in extract estimated by spectrophotometric method.

Conclusion

An ethanolic extract of AL effectively restored the hematological parameters, serum iron and serum protein and normalized the microcytic (smaller in size), anisocytosis (disturbed shape) and hypochromic RBCs. These observations could justify the inclusion of this plant in the management of iron deficiency anemia due the presence of iron and other constituents as flavonoids, terpenoids, steroids, lupeol and betulin.     

In vivo antimalarial activities of Enantia polycarpa stem bark against Plasmodium berghei berghei in mice

Ethnopharmacological relevance

Enantia polycarpa (PC) Engl. Et Diels (Annonaceae) is used in traditional medicine as an antimalarial remedy in Southern Nigeria.

Aim of the study

The antimalarial activities of ethanolic stem bark extracts of Enantia polycarpa was studied in vivo, in mice infected with Plasmodium berghei berghei.

Materials and methods

The ethanolic stem bark extract of Enantia polycarpa was administered at doses ranging from 200 to 600 mg/kg/day to Plasmodium berghei infected mice in both early and established models of antiplasmodial studies.

Results

The extract of Enantia polycarpa exhibited promising antimalarial activity against both early and established infections. At a dose of 600 mg/kg the extract achieved a 75.8% and 72% chemosuppression of parasitaemia in the study of acute and established infections, respectively. The extract also prolonged mean survival time of Plasmodium berghei infected mice during the study of established infection. The mean survival time of mice administered Enantia polycarpa extract at 600 mg/kg/day (27 days) was significantly longer than infected/untreated control (12 days). For the acute toxicity study the extract had an intraperitoneal LD₅₀ of 186 mg/kg but caused no mortality when administered orally at doses as high as 2,000 and 4,000 mg/kg.

Conclusions

Collectively, the results indicate that Enantia polycarpa is safe when administered orally and possesses promising antimalarial activity, thus supporting its use in traditional medicine for the treatment of malaria.     

Anti-inflammatory and antinociceptive activities of the ethanolic extract of Bougainvillea xbuttiana

Ethnopharmacological relevance

Bougainvillea xbuttiana is widely distributed in Mexico and it is used as an analgesic in folk medicine.

Aim of the study

In the present study the in vivo antinociceptive and anti-inflammatory effects of the Bougainvillea xbuttiana ethanolic extract have been studied in mice.

Materials and methods

The phytochemical analysis was performed. Antinociceptive activity was evaluated through writhing and formalin test in mice. The anti-inflammatory activity was determined with the carrageenan-induced mice paw oedema model. IL-6, IL-10 and IFN-γ levels were determined by enzyme-like immunosorbent assay, whereas TNF and nitrite levels were detected by standard assay with L929 cells and colorimetric Griess reactive, respectively.

Results

The results showed that the ethanolic extract of the Bougainvillea xbuttiana has significant anti-inflammatory and antinociceptive activities, by inhibition of nociception induced by acetic acid and paw oedema. This extract also induced a decrease in TNF levels and an increase of IL-6, IFN-γ and NO levels that we observed up to 2 h. The highest levels of IL-10 were observed up to 4 h. The ratios of pro-/anti-inflammatory cytokines in sera from mice injected with the ethanolic extract, may be manifesting an anti-inflammatory status.

Conclusions

The present study provides convincing evidences that Bougainvillea xbuttiana extract possesses significant anti-nociceptive and anti-inflammatory effects.     

Novel bisabolane derivative from “arnica-da-serra” (Vernonieae: Asteraceae) reduces pro-nociceptive cytokines levels in LPS-stimulated rat macrophages

Ethnopharmacology relevance

Hydro alcoholic leaves extracts (HALE) of Lychnophora ericoides Mart. (“false arnica” or “arnica-da-serra”) had been popularly used against pain and inflammatory process.

Aim

The present work aimed to look for possible active volatile compounds that could be found in HALE of Lychnophora ericoides among the non volatile anti-inflammatory and analgesic compounds previously reported.

Methods

Harvests were performed during the end of the wet summer season (April) when scented branches were instantly collected and frozen. HALE's were simulated at the lab by following the procedures lectured by the locals. Mass Spectrometry experiments suggested structural information when using both EI–MS and ESI–MS/MS. After isolation through classical thin layer chromatography (TLC) procedures, the NMR experiments and signals assignments were carried out. The effects on the cytokines or nitric oxide (NO) production were assessed at in vitro assays that had monitored the levels of these substances on the supernatant of LPS-stimulated macrophage primary cell culture.

Results

The major metabolite from HALE was isolated from the essential oil and the major compound had its molecular formulae established by Mass Spectrometry (High Resolution) and its structure by NMR. Literature-based investigation enables us to define the structure of the new metabolite as 6-methyl-2-(4-methylcyclohex-4-enyl-2-acetyloxy) hept-5-en-2-ol and its name as orto-acetoxy-bisabolol. In vitro assay of interleukins release inhibition was carried out using rat peritoneal macrophages cultures. IL-1β and TNF-α levels were significantly reduced when cells were previously treated with low doses of orto-acetoxy-bisabolol, but neither IL-6 nor NO levels have their levels reduced. Results suggest that ethnical knowledge of anti-inflammatory and analgesic effects of the “arnica-da-serra” HALE may be associated to the orto-acetoxy-bisabolol ability on synthesis inhibition of the key inflammatory/hypernociceptive mediators.

Conclusions

Phytochemical investigation of the volatile active compounds in Lychnophora ericoides HALE allows us to isolate a new bisabolane derivative (orto-acetoxy-bisabolol) and to infer that this compound inhibits the synthesis of TNF-α and IL-1β, two important inflammatory mediators in the hypernociception. Our present data, in addition to literature's data, furnish scientific support to folk's use of Lychnophora ericoides as an endemic wound healer.     

Combretum leprosum Mart. (Combretaceae): Potential as an antiproliferative and anti-inflammatory agent

Ethnopharmacological relevance

Combretum leprosum is a species that is popularly used in Brazil as a healing agent to treat skin problems and lesions. In this study we investigated the possible potential of this extract to treat inflammatory and hyperproliferative skin conditions.

Materials and methods

Classical models of skin inflammation such as TPA- and croton oil-induced mouse ear oedema were applied in order to verify the potential topical anti-inflammatory activity of the ethanolic extract from flowers of Combretum leprosum.

Results

Topical application of ethanolic extract promoted a dose-dependent inhibition of phorbol ester-induced ear oedema, reduced myeloperoxidase activity and IL-6 tissue levels with inhibition comparable to dexamethasone (positive control). Histological and immunohistochemical analysis revealed that ethanolic extract also suppressed cell infiltration. Ethanolic extract altered inflammatory parameters on a chronic skin inflammation model induced by repeated applications of croton oil, decreasing ear oedema, epidermal hyperproliferation and cell infiltration. In addition, immunohistochemical analysis showed that the extract decreased PCNA expression on the epidermis.

Conclusion

Taken together, these results suggest that the extract from flowers of Combretum leprosum could be considered as a new potential tool for the treatment of several skin inflammatory diseases since it reversed the skin inflammatory and hyperproliferative process in a very significant manner. Further investigations are needed in order to verify the cellular mechanism and safety of Combretum leprosum extract.     

Identification of rosmarinic acid as the major active constituent in Cordia americana

Ethnopharmacological relevance

Preparation from leaves of Cordia americana have been widely used in traditional medicine in South Brazil to treat wounds and various inflammations.

Aim of the study

The objective of this work was to identify the effective compounds in the ethanolic extract prepared from the leaves of Cordia americana, which is used in traditional South Brazilian medicine as anti-inflammatory and wound healing remedy.

Materials and methods

Isolation and structure elucidation techniques were performed in order to identify the compounds of Cordia americana and HPLC analysis was used for the quantification. The major constituent and the ethanolic extract were investigated for inhibition of 5-lipoxygenase, p38α MAPK, TNFα release and NF-κB as well as in the fibroblast scratch assay.

Results

Rosmarinic acid (1) was identified as the major compound with an amount of 8.44% in the ethanolic extract of the leaves of Cordia americana. The ethanolic extract as well as (1) exhibited the highest inhibitory effects on 5-lipoxygenase (IC₅₀ = 0.69 and 0.97 μg/mL, resp., IC₅₀ of BWA4C as reference: 0.3 μM) and p38α (IC₅₀ = 3.25 and 1.16 μg/mL, resp., IC₅₀ of SB203580 as reference: 0.046 μM) and moderate inhibitory effects on TNFα release. Slight effects were observed in the fibroblast scratch assay.

Conclusions

This study increases our knowledge on the effective compound in Cordia americana and supports its use in traditional medicine. We demonstrated for the first time pharmacological effects of Cordia americana and we provide evidences for a crucial role of rosmarinic acid as the major key player.     

Genotoxic and antigenotoxic effects of Hemidesmus indicus R. Br. root extract in cultured lymphocytes

Aim of the study

The genotoxic and antigenotoxic potential of the ethanolic extract of Hemidesmus indicus roots were evaluated in cultured human lymphocytes using cisplatin as the positive mutagen.

Materials and methods

Cytogenetic damage and cytotoxicity were determined in cells exposed to different doses of the extract, ranging from 2 to 32 μg/ml of culture medium, either alone or together with cisplatin.

Results

There was a significant reduction in cisplatin-induced frequencies of sister chromatid exchanges, chromosome aberrations and micronucleated binucleate cells at the lower concentrations of 4 and 8 μg/ml (P < 0.05). However, the extract by itself reduced the proliferative rate index, mitotic index and cytokinesis-block proliferative index (P < 0.05). Further, a significant increase in the percentage of chromosome aberrations was noticed at the higher concentrations.

Conclusion

Hemidesmus indicus root extract possesses significant genoprotective effect at the lower concentrations although it is cytotoxic and probably genotoxic at higher doses.     

Evaluation of anxiolytic and sedative effects of 80% ethanolic Carica papaya L. (Caricaceae) pulp extract in mice

Ethnopharmacological relevance

Carica papaya has been used in the Ethiopian traditional medicine to relieve stress and other disease conditions.

Aim of the study

The present study was undertaken to evaluate the anxiolytic and sedative effects of 80% ethanolic Carica papaya (Caricaceae) pulp extract in mice.

Materials and methods

Carica papaya pulp extract was screened for anxiolytic effect by using elevated plus maze, staircase and open field tests, and ketamine-induced sleeping time test for sedation at doses of 50, 100, 200, 400 mg/kg. Distilled water and Diazepam were employed as negative and positive control groups, respectively.

Results

Carica papaya pulp extract 100 mg/kg significantly increased the percentage of open arm time and entry, and reduced the percentage of entry and time spent in closed arm in elevated plus maze test; reduced the number of rearing in the staircase test; and increased the time spent and entries in the central squares while the total number of entries into the open field were not significantly affected, suggesting anxiolytic activity without altering locomotor and sedative effects. A synergistic reduction in the number of rearing and an inverted U-shaped dose response curves were obtained with important parameters of anxiety

Conclusions

The results of this study established a support for the traditional usage of Carica papaya as anxiolytic medicinal plant.     

Anti-inflammatory effects of ethanolic extract and alkamides-derived from Heliopsis longipes roots

Ethnopharmacological relevance

Heliopsis longipes (A. Gray) Blake (Asteraceae) is a broadly used species in the Mexican, Central and South American Traditional Medicine for its anaesthetic, analgesic, anti-inflammatory and anti-ulcerative properties. The ethanolic extract contains alkamides, mainly affinin (spilanthol). This family of compounds exerts an in vitro inhibitory action on the cyclooxygenase and lipoxygenase enzymes.

Aim of the study

The present study approaches the anti-inflammatory effect of the extract and its main bioactive component affinin and derived isobutyl-decanamide.

Materials and methods

The anti-inflammatory effect was evaluated through the mouse ear oedema test by means of two irritating agents, arachidonic acid (AA) and phorbol myristate acetate (PMA).

Results

Heliopsis longipes, affinin and isobutyl-decanamide displayed a marked anti-inflammatory effect on the AA model with ED₅₀ = 0.8, 1.2 and 0.9 mg/ear, respectively. Nimesulide (1 mg/ear) was used as a reference drug. In PMA model, the extract and two alkamides also showed a dose-dependent anti-inflammatory effect with ED₅₀ = 2.0, 1.3 and 1.1 mg/ear, respectively. Indomethacin (3 mg/ear) was used as reference drug.

Conclusions

These results could represent an important contribution to explain the anti-inflammatory ethnobotanical effects reported for Heliopsis longipes and other species containing affinin (spilanthol). For the first time the topical anti-inflammatory effects of Heliopsis longipes, affinin and isobutyl-decanamide were studied.     

In vitro and in vivo antioxidant activity of the ethanolic extract from Meconopsis quintuplinervia

Aims of the study

Meconopsis quintuplinervia, a medicinal herb endemic to the Tibetan region, is used to treat hepatitis. The aim of this study is to evaluate the antioxidant potential of the ethanolic extract of this herb using different assays.

Materials and methods

The antioxidant capacity of Meconopsis quintuplinervia was investigated using various established in vitro systems. An in vivo study of carbon tetrachloride (CCl₄)-induced antioxidant activity in mice was also conducted by examining the levels of malondialdehyde (MDA) and the activities of antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH).

Results

The extract showed strong in vitro antioxidant ability. In the in vivo study, CCl₄-induced oxidative stress caused significant decreases in the SOD, CAT, and GSH levels and a significant increase in the MDA level, most of which were significantly reversed (except for SOD in the liver.) by treatment with the extract and standard Vitamin E.

Conclusion

This study clearly indicates that the ethanolic extract of Meconopsis quintuplinervia is a valuable source of natural antioxidants. These findings provide scientific support for the traditional use of this herb as a Tibetan medicine for liver diseases.     

Anti-tumor and pro-apoptotic activity of ethanolic extract and its various fractions from Polytrichum commune L.ex Hedw in L1210 cells

Ethnopharmacological relevance

Polytrichum commune L.ex Hedw is a traditional Chinese herb for treatment of fever, hemostatic, uterine prolapse and especially for lymphocytic leukemia, but the antitumor effect and its potential mechanism remains unclear.

Aims of the study

The present study was to investigate the possible anti-proliferative activity of ethanolic extract and the organic fractions from P. commune on murine leukemia L1210 cells.

Materials and methods

The content of ethanolic extract and its fractions was performed on HPLC analysis with gradient elution. L1210 cells were treated with different concentrations of ethanolic extract and its fractions at different time intervals. Cell viability was evaluated using MTT assay. Apoptotic cell death was monitored by nuclear condensation and confirmed by exposure of phosphatidylserine to outer leaflet of plasma membrane. Loss of mitochondrial membrane potential was analyzed by flow cytometry using rhodamine 123 staining.

Results

The obtained results showed that the cell viability of L1210 cells was reduced by ethanolic extract of P. commune in a concentration-dependent manner, and the IC₅₀ value was about 77.22 μg/ml at 24 h post treatment. The ethylacetate fraction displayed higher anti-tumor effect than that of chloroform and butanol fractions with 32.29 μg/ml (IC₅₀ value, 48 h). Microscopy studies revealed that ethanolic extract and ethylacetate fraction treated cells showed morphological characteristics of apoptosis such as chromatin condensation and DNA aggregation. Further, Annexin V-PE/ 7-AAD double staining showing the out leaflet of phosphatidylserine and the decline of mitochondrial membrane potential by flow cytometry confirmed that the extracts do, in fact, induce apoptosis in L1210 cells.

Conclusion

This is the first report on anti-tumor and pro-apoptotic effect of P. commune in cultured leukemia cells, which provides scientific basis for its usefulness as traditional medicine. Further studies are needed to confirm the precise mechanism not only the crude extract but as well the monomeric chemical substances of Polytrichum commune L.ex Hedw.     

Antiplasmodial activity of root extract and fractions of Croton zambesicus

Aim of the study

Antiplasmodial activity of root extract and fractions of Croton zambesicus were evaluated to ascertain the folkloric claim of its antimalarial activity and elucidate its antiplasmodial mechanism of action.

Material and method

The crude ethanolic root extract (27–81 mg/kg) and gradient fractions ( n- hexane, chloroform, ethyl acetate and methanol; 54 mg/kg) of Croton zambesicus were investigated for antiplasmodial activity against chloroquine - sensitive Plasmodium berghei infections in mice. The antiplasmodial activity during early and established infections as well as the prophylactic activity were investigated. Chloroquine (5 mg/kg) and pyrimethamine (1.2 mg/kg) were used as positive controls. Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice. Oxidant generation potentials of the crude extract and fractions was also evaluated to elucidate their mechanism of action.

Results

The crude root extract (27 – 81 mg/kg) demonstrated significant (P < 0.01–0.001) schizonticidal activity during early and established infections and also had prophylactic activity. The activity was comparable to that of the standard drug used (chloroquine 5 mg/kg, pyrimethamine 1.2 mg/kg). Methanol, ethyl acetate and chloroform fractions had comparative in vivo antiplasmodial activity and oxidant generation potentials.

Conclusion

The antiplasmodial activity of this root extract and fractions which is likely to be through peroxidation confirms the folkloric use of this plant.     

Anti‐Inflammatory Sesquiterpene Lactones from Lychnophora trichocarpha Spreng. (Brazilian Arnica)

The aerial parts of Lychnophora trichocarpha Spreng. (Asteraceae) are used macerated in water or ethanol to treat inflammation, pain, rheumatism, contusions, bruises and insect bites in Brazilian traditional medicine. In this study, anti‐inflammatory activity of ethanol extract from aerial parts of L. trichocarpha and its ethyl acetate fraction was investigated. Sesquiterpene lactones, lychnopholide (Lyc) and eremantholide C (EreC), isolated of ethyl acetate fraction, were also assayed for in vitro and in vivo anti‐inflammatory activity. Topical treatment with ointments containing ethanol extract, its ethyl acetate fraction and sesquiterpene lactones significantly reduced carrageenan‐induced mice paw oedema. In vitro assays demonstrated that Lyc inhibited interferon ‐γ/lipopolysaccharide ‐stimulated nitric oxide (NO) production in J774A.1 macrophages and increased production of IL‐10 anti‐inflammatory cytokine. The reduction of tumor necrosis factor‐α (TNF‐α) production by EreC was accompanied by an increased production of IL‐10 in a concentration‐dependent manner in J774A.1 macrophages. The anti‐inflammatory effect of Lyc seems to involve the inhibition of production of NO and increased production of IL‐10. The mechanism of the effect of EreC on the reduction of carrageenan‐induced paw oedema may be attributed to inhibition of production of TNF‐α and stimulation of IL‐10 production. The results corroborate the use of ethanol extract from Lychnophora trichocarpha in folk medicine for anti‐inflammatory action and indicate that the topical route is suitable for use. Copyright © 2012 John Wiley & Sons, Ltd.     

Antinociceptive activity of aqueous extract and isolated compounds of Lithrea molleoides

Ethnopharmacological relevance

Lithrea molleoides (Vell.) Engl. (Anacardiaceae) is a medicinal plant commonly used in traditional medicine in South America.

Aim of the study

In the present study, the in vivo antinociceptive effect of L. molleoides' aqueous extract and its isolated compounds has been investigated.

Materials and Methods

Antinociceptive activity was evaluated through writhing, formalin and hot plate tests in mice. The phytochemical analysis was performed.

Results

The extract produced significant inhibition on nociception induced by acetic acid (ED50: 8.7 mg/kg, i.p.) and formalin (ED50: 7.7 mg/kg, i.p.) administered intraperitoneally and also orally. Yohimbine diminished the activity of the extract in the acetic acid test meanwhile haloperidol enhanced its effect. Two majority compounds, shikimic and vanillic acid were active in chemical nociceptive models used in this work, producing the highest inhibition of the writhing response at a dose of 30 mg/kg i.p. (55.4% and 57.1%, respectively) meanwhile at 100 mg/kg p.o. produced a slight response (23.3% and 23.9%, respectively).

Conclusions

These results suggest that L. molleoides' aqueous extract produced antinociception possibly related to the presence of shikimic and vanillic acid. The adrenergic and dopaminergic systems seem to be involved in the mechanism of antinociception of the extract.     

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.     

Protective effects of Puerariae radix extract and its single compounds on methylglyoxal-induced apoptosis in human retinal pigment epithelial cells

Ethnopharmacological relevance

In Korea, Puerariae radix is a medicinal plant traditionally used to treat various diseases including diabetes mellitus. To provide pharmacological basis for Puerariae radix in the treatment of diabetes, we investigated the protective effects of the ethanolic extract and its single compounds on apoptosis associated with glycation in human retinal pigment epithelial (RPE) cells.

Materials and methods

In the present work, a quantified ethanolic extract or single compounds of Puerariae radix were selected to determine its anti-apoptotic effect in human RPE cells cultured with methylglyoxal (MG), which is a stimulator of glycation. To assess the protective effect of the extract or single compounds, the cytotoxicity assessment was performed using an MTT assay in the human RPE cells. Selected active compounds or extracts were tested by FACS analysis with annexin V staining for apoptosis.

Results

Daidzein (1), daidzin (2), puerarin (3), 3'-hydroxy-daidzein 8-C-apiosyl (1→6) glucoside (4), and daidzein 8-C-apiosyl (1→6) glucoside (5), and pueroside B (6) were isolated from an ethanolic extract of Puerariae radix. MG-induced apoptosis was completely inhibited by Puerariae radix, ethanolic extract, and single compounds. Of the six major compounds, daidzin (2) and 3'-hydroxy-daidzein 8-C-apiosyl (1→6) glucoside (4) significantly inhibited MG-induced apoptosis.

Conclusion

Our results provide the first evidence that, due to its anti-glycation effect, Puerariae radix extract could inhibit MG-induced apoptosis in the cultured human RPE cells. These data suggest that Puerariae radix extract, especially its single compounds daidzin and 3'-hydroxy-daidzein 8-C-apiosyl (1→6) glucoside, has potential utility as a preventive agent for glycation-related diabetic retinopathy.     

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.