Acid-induced Increase In Capillary Permeability Research Articles

From nutrition to medicine: Assessing hemorrhoid healing activity of Solanum melongena L. via in vivo experimental models and its major chemicals

Ethnopharmacological relevanceSolanum melongena L. (eggplant) is used for treatment of rheumatism, beriberi, itching, toothache, bleeding, asthma, bronchitis, cholera, neuralgia and hemorrhoids in traditional medicine (Turkish, Chinese, and Indian). Hemorrhoids from these diseases, are common illness in all over the world, which are treated with various approaches including ethnobotanicals.Aim of the study: This study aimed to evaluate the anti-hemorrhoidal activity of eggplant, an edible plant, which is commonly utilized around the world. Materials & methodsIn vivo anti-hemorrhoidal activity of the methanolic extract prepared from eggplant was evaluated by experimental hemorrhoid model, subsequently histological and biochemical analysis. Hemorrhoid, which was induced by applying croton oil to the anal area of the rats. Furthermore, the extract was screened for anti-inflammatory activity which is based on the inhibition of acetic acid-induced increase in capillary permeability. The healing potential was comparatively assessed with a reference Pilex® tablet and cream. Phytochemical analysis performed by HPLC. The amount of the major phenolic compound (chlorogenic acid) in extract was found by using HPLC method. ResultsHistological and biochemical analysis demonstrated that eggplant extract is highly effective against hemorrhoid in comparison to the controls and the commercial preparation. In addition, the methanolic extract demonstrated significant inhibitory effect on acetic acid-induced increase in capillary permeability.The phytochemical studies identified major compound as chlorogenic acid (2.86%) by liquid chromatography. ConclusionThe eggplant calyxes, not edible, are easy to reach, by products/vast from the food sources. This is the first scientific evidence revealing that the eggplant extract has significant anti-hemorrhoidal and anti-inflammatory activity.

In vivo activity assessment of some Tanacetum species used as traditional wound healer along with identification of the phytochemical profile by a new validated HPLC method.

Objective(s):Tanacetum species are traditionally used as insecticide, and externally wound healer as well as for anti-inflammatory and antihistaminic properties. The in vivo wound-healing and anti-inflammatory potential of four Tanacetum species, Tanacetum argenteum (Lam.) Willd. subsp. argenteum (TA), Tanacetum heterotomum (Bornm.) Grierson (TH), Tanacetum densum (Lab.) Schultz Bip. subsp. sivasicum (TD), and Tanacetum vulgare L. (TV) was investigated.Materials and Methods:The chloroform (CHCl3) and methanol:water (80:20) extracts were prepared from the aerial parts of each plant. For assessment of the wound-healing activity, linear incision on rats and circular excision on mice wound models were used and histopathological analyses were conducted on the tissues treated with the test materials. For the evaluation of the anti-inflammatory activity, Whittle Method based on the inhibition of the acetic acid-induced increase in capillary permeability was used. In order to elucidate the phytochemical contents of the extracts, HPLC profiles of active fractions were screened and quantitative analysis was conducted within the scope of HPLC analysis.Results:The CHCl3 extracts of TD, TA and TV were found to have significant wound healing activity (37.1%, 30.8% and 26.1% tensile strength; 88.05%, 72.93% and 44.88% contraction values, respectively) and anti-inflammatory activities (31.5% and 26.6% inhibition values for TD and TA). Parthenolide content of the CHCl3 extracts of TA, TH and TV were found 242.66±1.53, 190.16±5.62 and 177.51±3.73 µg/100 mg plant material, respectively.Conclusion:According to the results, the other secondary metabolites present in the aerial parts of the Tanacetum species possibly exerted synergistic effects on the observed healing of the wounds.

Topical Wound-Healing Effects and Phytochemical Composition of Heartwood Essential Oils ofJuniperus virginianaL.,Juniperus occidentalisHook., andJuniperus asheiJ. Buchholz

Ethnobotanical surveys indicated that in the traditional medicines worldwide, several Juniperus species are utilized as antihelmintic, diuretic, stimulant, antiseptic, carminative, stomachic, antirheumatic, antifungal, and for wound healing. In the present study, essential oils obtained from heartwood samples of Juniperus virginiana L., Juniperus occidentalis Hook. and Juniperus ashei J. Buchholz were evaluated for wound healing and anti-inflammatory activities by using in vivo experimental methods. The essential oils were obtained by the supercritical carbon dioxide extraction method. Linear incision and circular excision wound models were performed for the wound-healing activity assessment. The tissues were also evaluated for the hydroxyproline content as well as histopathologically. To evaluate the anti-inflammatory activity of the essential oils, the test used was an acetic acid-induced increase in capillary permeability. The essential oil of J. occidentalis showed the highest activity on the in vivo biological activity models. Additionaly, the oil of J. virginiana was found highly effective in the anti-inflammatory activity method. The experimental data demonstrated that essential oil of J. occidentalis displayed significant wound-healing and anti-inflammatory activities.

Comparative evaluation of traditional prescriptions from Cichorium intybus L. for wound healing: Stepwise isolation of an active component by in vivo bioassay and its mode of activity

Ethnopharmacological relevanceEthnobotanical field surveys revealed that various parts of Cichorium intybus L. has been used for wound healing in Turkish folk medicine. Aim of the studyThe present study aimed at verifying the efficiency of various traditional prescriptions prepared from the aerial parts and roots of C. intybus experimentally and to define the components responsible from the activity by bioassay-guided procedures. Material and methodsInitially, wound healing activity of the aerial parts, leaves, and roots as well as ashes of either leaves or roots were investigated. Subsequently, roots of the plant were submitted to further detailed investigations. The wound healing activity of the methanolic extract, its subextracts, and fractions were evaluated by using in vivo linear incision and circular excision wound models in rats. The hydroxyproline content of the tissues treated with test ointments were also assessed for the activity evaluation. Moreover, in order to find out a possible involvement of antioxidant activity in wound healing, the test samples were also investigated by DPPH radical scavenging activity and total phenolic concentration were also determined. Additionally anti-inflammatory activity was assessed by using the method of Whittle, which is based on the inhibition of acetic acid-induced increase in capillary permeability. Through the bioassay guided fractionation one compound was isolated and its structure was elucidated by spectroscopic methods. For the determination of the activity mechanisms, the fractions were screened for hyaluronidase, collagenase and elastase enzyme inhibitory activities. ResultsMethanolic extract of C. intybus roots was found to possess potent wound healing activity. Then this extract was subjected to successive solvent extraction with n-hexane, dichloromethane (DCM), ethyl acetate and n-butanol. Each solvent extracts were also applied on the same wound models. DCM subextract was found to be the most active one and through chromatographic techniques DCM subextract was fractionated into several fractions and compound 1 was isolated as the compound being responsible from the wound healing activity. ConclusionThe experimental study revealed that C. intybus methanolic extract displays wound healing effect and β-sitosterol was determined as the active compound responsible from the activity.

Appraisal on the wound healing and anti-inflammatory activities of the essential oils obtained from the cones and needles of Pinus species by in vivo and in vitro experimental models

Ethnopharmacological relevanceAccording to ethnobotanical data, Pinus species have been used against rheumatic pain and for wound healing in Turkish folk medicine.Essential oils from the cones and needles of five different Pinus species (Pinus brutia Ten., Pinus halepensis Mill., Pinus nigra Arn., Pinus pinea L. and Pinus sylvestris L.) were evaluated for their in vivo wound healing and anti-inflammatory activities. Materials and methodsIn vivo wound healing activity of the ointments prepared from essential oils was evaluated by linear incision and circular excision experimental wound models subsequently histopathological analysis and hydroxyproline content. Furthermore, the essential oils were screened for anti-hyaluronidase activity. Additionally anti-inflammatory activity was assessed by using the method of Whittle, which is based on the inhibition of acetic acid-induced increase in capillary permeability. ResultsThe essential oils obtained from the cones of Pinus pinea and Pinus halepensis demonstrated the highest effects on the wound healing activity models. On the other hand, the rest of the essential oils did not show any significant wound healing and anti-inflammatory activities. ConclusionThe experimental study revealed that essential oils obtained from the cones of Pinus pinea and Pinus halepensis display remarkable wound healing activity.

Wound healing and anti-inflammatory activities of the Michauxia L’Hérit (Campanulaceae) species native to Turkey

Ethnopharmacological relevanceThe leaves of Michauxia species are used for the treatment of wounds in Turkish traditional medicine. In the present study, wound healing, anti-inflammatory and antioxidant activities of the extracts obtained from the root and herb of 5 species of Michauxia collected in different parts of Turkey were evaluated. Material and methodsIn vivo incision and excision wound models were used in order to assess the wound healing effects of the methanolic extracts of the plants. Skin samples were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. TBA (thiobarbituric acid) test, qualitative and quantitative DPPH (2,2-diphenyl-1-picrylhydrazyl) tests were used to evaluate the antioxidant activity. ResultsNoteworthy wound healing activity was observed for the ointment formulation prepared with 1% Michauxia nuda (root) and Michauxia tchihatchewii (herb) extracts. The results of histopathological evaluation supported the outcome of incision and excision wound models. Moreover, the Michauxia nuda (root) exerted remarkable anti-inflammatory effect. The highest antioxidant activity was observed with the ethyl acetate extract of Michauxia tchihatchewii herb. ConclusionThe experimental study revealed that Michauxia displays remarkable wound healing and anti-inflammatory and antioxidant activities.

Wound healing and anti-inflammatory activities of the Michauxia L'Hérit (Campanulaceae) species native to Turkey

Michauxia L'Hérit (Campanulaceae) species are used as vegetable and medicinal plants in Turkey, and five species of this genus grow naturally in Turkey. The leaf of M. campanuloides L'Hérit ex Aiton is used in traditional medicine the treatment of wounds in Kahramanmaraş (Turkey). The present study was designed to investigate the wound healing and anti-inflammatory activities of the water and methanol (MeOH) extracts obtained from the root and herb of five Michauxia species. The incision by using tensiometer and excision models were used in order to assess the effect of the plant extracts on wound healing in mice and rats. Results were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. The wound healing effect was comparatively evaluated with a reference ointment Madecassol®. Noteworthy wound healing activity was observed for the ointment formulation prepared with 1% M. nuda A.DC. (root MeOH) and M. tchihatchewii Fisch. et Mey. (herba MeOH) extracts. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Moreover, the root extract of the M. nuda exerted remarkable anti-inflammatory activity also demonstrated. The experimental study revealed that Mictauxia displays remarkable wound healing and anti-inflammatory activities.

Wound healing acceleration effect of endemic Ononis species growing in Turkey

Ononis L. species have been used for healing of wounds, eczema and rheumatic complaints, against skin cancer and lesions and topically used as antiseptic and antimicrobial agent in folk medicine. In the present study, the aqueous and methanolic extracts of three endemic Ononis species growing in Turkey, including Ononis sessilifolia Bornm., Ononis basiadnata Hub.-Mor. and Ononis macrosperma Hub.-Mor. were assessed for their in vivo wound healing and anti-inflammatory activities. In vivo wound healing activities of the plants were evaluated by using linear incision and circular excision experimental models subsequently histopathological analysis. The healing potential was comparatively assessed with a reference ointment Madecassol(®), which contains 1% extract of Centella asiatica. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. The aqueous and ethanolic extracts of the aerial parts of O. macrosperma demonstrated the highest activity in both wound models and significant anti-inflammatory activity in acetic acid-induced increase in capillary permeability test. Furthermore, ethanolic extract of the aerial parts of O. sessilifolia showed anti-inflammatory effect but was devoid of wound healing activity. The rest of the species did not show remarkable wound healing effect. Ethyl acetate fraction of O. macrosperma ethanolic extract demonstrated significant but reduced wound healing activity, which revealed a possible combined effect. The results of histopathological examination supported the outcome of linear incision and circular excision wound models. The experimental study revealed that the aerial parts of O. macrosperma display remarkable wound healing and anti-inflammatory activities.

In vitro and in vivo anti-inflammatory effects of pegmatite

Pegmatite is a coarse-grained intrusive igneous rock rich in rare elements such as uranium, tungsten, and tantalum with Ca, K, Mg, Fe, Se, Ge, and Ho. We tested in vitro and in vivo assays for the anti-inflammatory activity of pegmatites. We firstly evaluated the suppressive effects of pegmatite on macrophage cell line RAW 264.7 cells stimulated with proinflammatory stimuli lipopolysaccharide (LPS) to determine nitric oxide (NO) production and TNF-α and IL-6 release. The IC50 values of pegmatite exceeded 5,000 μg/mL. Treatment of RAW 264.7 cells with pegmatite significantly inhibited LPS-stimulated NO production and proinflammatory cytokines such as TNF-α and IL-6 secretion in a dose-dependent manner (P<0.05). In vivo studies were tested with two animal models of arachidonic acid-induced mouse ear edema and an acetic acid-induced increase in capillary permeability. The pegmatite significantly attenuated ear edema induced by arachidonic acid and reduced the acetic acid-induced increase in capillary permeability in mice (P<0.05) when the pegmatite was administered topically (10 mg per ear) for 24 h. Therefore, pegmatite potentially shows an anti-inflammatory activity in the in vitro and in vivo mice and in the development of newer anti-inflammatory agents as mineral materials.

Investigations on the in vivo wound healing potential of Hypericum perforatum L.

Ethnopharmacological relevance Olive oil extract of the flowering aerial parts of Hypericum perforatum L. (Hypericaceae) is a popular folk remedy for the treatment of wounds in Turkey. Aim of the study In order to prove the claimed utilization of the plant, the effects of the extracts and the fractions were investigated by using bioassay-guided procedures. For the wound healing activity assessment, in vivo excision and incision wound models were applied. For the anti-inflammatory activity, an in vivo model, based on the inhibition of acetic acid-induced increase in capillary permeability was used as well. Moreover, a parallel study was run on Hypericum scabrum L., which is a widespread species of the gender but not known as a folk remedy for wound healing, to provide a preliminary data to compare and emphasize the selection of correct plant species. Results Initial investigations proved that the olive oil extract of Hypericum perforatum has a significant wound healing effect on excision (5.1–82.6% inhibition) and circular incision (20.2–100.0% inhibition) wound models. In order to determine the active wound healing ingredient(s), aerial parts of the plant was extracted with ethanol, noteworthy wound healing activity profile was observed with the wound models; between 18.3% and 95.6% in excision model and from 13.9% to 100.0% inhibitions in incision model were determined. The ethanolic extract was then submitted to successive solvent extractions with n-hexane, chloroform and ethyl acetate (EtOAc). Each solvent extract was also applied on the same wound models, consequently, EtOAc subextract was found to be the most active one by inhibiting wounds between 17.9% and 100.0% in excision model, subsequently between 9.4% and 100.0% in incision model. However, all subfractions obtained from the EtOAc subextract using Sephadex LH-20 column chromatography showed wound healing activity not more than the whole EtOAc subextract, which revealed that a possible synergistic activity that might be questioned. Among the active Sephadex fractions, Fr. A further yielded hyperoside, isoquercitrin, rutin and (−)-epicatechin and Fr. B yielded hypericin as the major components. Moreover, a dose-dependent anti-inflammatory activity was found for the ethanol extract, EtOAc subextract and Sephadex fractions of Hypericum perforatum. These results suggest that anti-inflammatory activity of the active fractions might have a contributory role in the wound healing effect of the plant. Conclusion Results of the present study have proved that aerial parts of Hypericum perforatum possess remarkable wound healing and anti-inflammatory activities supporting the folkloric assertion of the plant in Turkish folk medicine. Flavonoids [hyperoside, isoquercitrin, rutin and (−)-epicatechin] and naphthoquinones (hypericins) were found as the active components of Hypericum perforatum. On the other hand, ethanol extract of Hypericum scabrum showed neither remarkable wound healing nor anti-inflammatory activity demonstrating the importance of correct plant species selection in therapeutic applications.

In vivo anti-inflammatory and wound healing activities of Centaurea iberica Trev. ex Spreng

Aim of the study Several Centaurea species (Asteraceae) are used in Turkish folk medicine to alleviate pain and inflammatory symptoms in rheumatoid arthritis, high fever, head ache and for wound healing. Particularly, the aerial part of Centaurea iberica Trev. ex Spreng. has been practiced on wounds for healing. In order to evaluate the anti-inflammatory and wound healing activities of the plant, extracts were prepared with variety of solvents: hexane, chloroform, ethyl acetate and aqueous methanol (85%) from the aerial parts of Centaurea iberica. Materials and methods The incision by using tensiometer and excision models were used in order to assess the effect of the plant extracts on wound healing in mice and rats. Results were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. Results The wound healing effect was comparatively evaluated with a reference ointment Madecassol ®. Noteworthy wound healing activity was observed for the ointment formulation prepared with 1% methanol extract. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Moreover, the methanol extract exerted remarkable wound healing activity and also demonstrated a significant and dose-dependent anti-inflammatory activity. Conclusion The experimental study revealed that Centaurea iberica displays remarkable wound healing and anti-inflammatory activity.

A new therapeutic approach in Alzheimer disease: Some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics

The increasing life expectancy in our population makes Alzheimer’s disease (AD) a growing public health problem. There is a great need to find a way to prevent and delay the disease. It was shown that monoamine oxidase-B (MAO-B) inhibitors and antiinflammatory agents might be effective in treating AD. Therefore, a novel series of 1-thiocarbamoyl-3-substituted phenyl-5-(2-pyrrolyl)-4,5-dihydro-(1 H)-pyrazole derivatives as promising MAO-B inhibitors was synthesized and investigated for the ability to inhibit selectively the activity of the A and B isoforms of monoamine oxidase (MAO). Most of the synthesized compounds showed high activity against both the MAO-A (compounds 3e– 3h) and the MAO-B (compounds 3i– 3l) isoforms. All the synthesized compounds were also tested for their in vivo antiinflammatory activity by two different bioassays namely, carrageenan-induced oedema and acetic acid-induced increase in capillary permeability in mice. In addition, analgesic and ulcerogenic activities were determined. The combined antiinflammatory data from in vivo animal models showed that compound 3k exhibited anti-inflammatory activity comparable to that of indomethacin with no ulcerogenic effects. Since compound 3k exhibits both antiinflammatory-analgesic activity and MAO-B inhibition, it needs further detailed studies.

Vasogenic brain edema induced by arachidonic acid: role of extracellular arachidonic acid in blood-brain barrier dysfunction.

The effects of free arachidonic acid on the capillary permeability of normal rat brains were studied by measuring the regional uptake of [14C]aminoisobutyric acid by a quantitative autoradiographic technique. Intracerebral infusion of sodium arachidonate increased capillary permeability in a dose-dependent manner up to a concentration of 2 mmol/L. A high dose of arachidonic acid (more than 5 mmol/L) produced marked tissue destruction around the injection site (needle track) and increased capillary permeability less than 2 mmol/L arachidonic acid did. A time-course study demonstrated that about 80% of the maximum increase in capillary permeability produced by arachidonic acid was observed within 2 hours after the infusion was initiated. In addition, capillary permeability gradually increased with time up to 24 hours, after which it declined to about half of the maximum increase 48 hours after infusion. These effects of arachidonic acid on capillary permeability were localized within about 1.6 mm around the injection site. Pretreatment with dexamethasone did not completely, but did significantly, inhibit the arachidonic acid-induced increase in capillary permeability. The inhibitory effect of dexamethasone was completely suppressed by the administration of actinomycin D, which inhibits de novo protein synthesis, 1 hour before the treatment with dexamethasone. These results suggest that arachidonic acid, which is released and accumulated in the extracellular space, increases the capillary permeability of the brain in at least two different ways. One is the direct action of the arachidonic acid itself, which can stimulate perturbation of the membrane of the capillary endothelial cells, thus promoting an increase in capillary permeability.(ABSTRACT TRUNCATED AT 250 WORDS)