Crude Extract Of Aerial Parts Research Articles

Phytochemical isolation and biological screening of Cotoneaster microphyllus

ABSTRACT The root and aerial parts of Cotoneaster microphyllus were subjected to extraction and isolation of phytochemicals. The extracts were evaluated for their antioxidant anthelmintic, antimicrobial, and anticholinesterase potentials using standard protocols. Crude extract of aerial parts and roots, more potently scavenged DPPH free radicals with IC50 values of 83 and 66 μg/mL while ABTS with 92 and 90 μg/mL respectively. Chloroform fraction exhibited highest anthelmintic activity followed by ethyl acetate fraction. Ethyl acetate fraction produced high zone of inhibition against selected bacterial and fungal strains. Maximum phenolic contents and vitamin C were found in the ethyl-acetate and chloroform fractions and were therefore, biologically the most potent fractions. Ethyl acetate fraction exhibited highest anticholinesterase potential and was therefore subjected to silica gel column chromatography which resulted in the isolation of one new (1) and four known (2–5) compounds. The isolated compounds were also screened for anticholinesterase potentials. Compound 3, most potently inhibited acetyl cholinesterase and butyryl cholinesterase with IC50 value of 66 and 114 μg/mL, respectively. The extracts exhibited antioxidant, anticholinesterase, anthelmintic and antimicrobial potentials that should be further subjected for the isolation of other responsible compounds in pure state. As anticholinesterase compound 3 is a good candidate to be tested in animal models.

New bicyclic [3.2.1] octane neolignans derivatives from Aniba firmula with potent in vivo anti-inflammatory activity on account of dual inhibition of PGE2 production and cell recruitment

Two new bicyclic octane neolignans, 1, 2, and the known bicyclic octane neolignan 3 were obtained by HPLC fractionation of the crude extract of aerial parts and the stem of Aniba firmula (Lauraceae’s family). The identification of its structures was made by spectroscopic analysis. The Lauraceae is well-known for its anti-inflammatory potential and is a rich source of bioactive compounds. The eff ;ects of 1 and 2 on inflammation were evaluated in an in vivo assay in mice. It was found that 1 and 2 significantly inhibited croton oil-induced ear edema when compared with their respective reference drugs. Moreover, 1 also inhibited neutrophil recruitment in an MPO assay. The level of PGE2 was further evaluated and supported the hypothesis that edema was inhibited through the COX pathway. As long as the level of LTB4 of 1 was similar to that of the negative control, we assert that the LOX pathway was not inhibited for this compound. Thus, these findings demonstrate that 1 has anti-inflammatory activity by a mechanism of action different from the common anti-inflammatory drugs available. This may mean that different neolignan classes could be sources of lead compounds prior to the development of new anti-inflammatory drugs, aiding in the search for higher efficacy and leading to fewer potential side effects.

Silver nanoparticles mediated by Callistemon citrinus extracts and their antimalaria, antitrypanosoma and antibacterial efficacy

In this report, three biosynthesized silver nanoparticles (AgNPs) obtained from the reduction of silver nitrate (AgNO3) by the aqueous crude extracts of aerial parts of Callistemon citrinus plant were characterized by means of ultraviolet–visible spectroscopy (UV–vis), X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-ray (EDX), transmission electron microscopy (TEM) and Fourier transformed infrared (FTIR).The XRD revealed that the AgNPs were crystalline in nature while the TEM showed that the shapes were spherical with an average size of 29 nm. The SEM and EDX demonstrated triangular shaped materials and that the AgNPs were made up of silver and oxygen only, absorption spectra confirm by UV–vis signifies the dispersed nature of the synthesized nanoparticles with absorption band observed at 280 nm for the leaf. FTIR had absorption bands at about 1700 cm−1 in all spectra's establishing the CO stretching owing to amide bond, another remarkable peak at 3400 cm−1 was seen in the crude extract which was ascribed to the OH stretching from water as a result of the aqueous nature of the plant extracts used. It is interesting to know that this peak was not seen in the AgNPs demonstrating the development of calcined AgNPs, in addition to this, peak at 420 cm−1 was observed for all the three nanoparticles synthesized and this shows the successfully synthesis of the AgNPs. The antimicrobial activities of the of the AgNPs was also confirm via both gram positive and gram negative bacteria strains with a very significant inhibitory action, MIC values of 7.8125 mg/mL were documented for all the silver nanoparticles. Potent antiplasmodial activities with IC50 ranging from 2.99–5.34 μg/mL were also recorded and a poor IC50 of 107.30 μg/mL for antitrypanosoma activity of the leaf AgNPs was also documented.

Evaluation of anti-HSV-1 activity and toxicity of hydroethanolic extract of Tanacetum parthenium (L.) Sch.Bip. (Asteraceae)

BackgroundHerpes simplex type 1 (HSV-1) is widely distributed throughout the world's population. The virus spreads through direct contact with an infected individual. After primary infection, the virus remains in a latent state, and the recurrence of herpetic lesions is common. Standard treatment is performed with nucleoside analogues, but the selection of resistant strains have occurred, thus requiring the continual search for new antiviral agents. Plant extracts, fractions, and isolated compounds are a good source for studying possible antiviral compounds. HypothesisAmong plants with antiviral activity, the crude extract of aerial parts of Tanacetum parthenium (L.) Sch.Bip. (Asteraceae) have previously shown to inhibit HSV-1 infection in vitro. MethodsThe present study investigated the chemical composition of a crude hydroethanolic extract (CHE) of T. parthenium, and in vivo safety and therapeutic efficacy against HSV-1 infection. ResultsLiquid chromatography-mass spectrometry showed that the CHE was composed of phenolic acids (chlorogenic acids) and sesquiterpene lactones (parthenolide). Acute and subchronic toxicity and genotoxicity tests in vivo showed that oral CHE administration did not result in signs of toxicity, with no genotoxic potential. The CHE was also safe for topical administration, in which no irritation of the epidermis was observed in treated animals. Tests of topical and oral therapeutic efficacy showed that the CHE was effective against HSV-1 infection. Topical administration was the most effective, the results for which were comparable to acyclovir. ConclusionThese findings indicate that the CHE from aerial parts of Tanacetum parthenium has in vivo anti-HSV-1 activity and is safe for oral and topical application.

Industrial case study on alkaloids purification by pH-zone refining centrifugal partition chromatography

The industrial potential of pH-zone refining centrifugal partition chromatography has been evaluated by studying the purification of pharmaceutical ingredients at the pilot scale. For the first time, a scale up methodology based on both column capacity and mass transfer efficiency as invariants was developed. The purification of catharanthine and vindoline from an industrial crude extract of aerial parts of Catharanthus roseus, was used as a case of study. Toluene/CH3CN/water (4/1/5, v/v/v) was selected as biphasic solvent system, triethylamine as retainer in the organic stationary phase and sulphuric acid as displacer in the aqueous mobile phase. The separation intensification was performed on a 36mL CPC column equipped with 832 partition twin-cells. The combined effects of four parameters (displacer and retainer concentrations for intensive parameters, flow rate and rotational speed for extensive parameters) were studied by design of experiment in order to maximize both recoveries and productivities. Then, scale change was done on two larger columns (305mL and 1950mL of capacity) equipped with only 231 and 238 partition cells. For this step, it has been shown that the global mass transfer coefficient k0a (the efficiency of a column design) and the stationary phase retention (the capacity of the column) were relevant and useful scale up invariants.A CPC model based on acid-base equilibriums and interfacial mass transfer in continuously stirred tank reactors in series was used to predict fully separations on larger CPC column at the optimized operating conditions and to guide the CPC user in its scale-up strategy. The experimental validation on pilot CPC column, by injecting up to 150g of Catharanthus roseus crude extract on the 1950mL column highlighted the preservation of the separation quality, the non-linear character of the scale up in centrifugal partition chromatography and that a productivity of about 4kg of processed crude extract per day can be reached by implementing developed methodology.

Phenolic Metabolites of Dalea ornata Affect Both Survival and Motility of the Human Pathogenic Hookworm Ancylostoma ceylanicum.

Hookworms are ubiquitous human parasites, infecting nearly one billion people worldwide, and are the leading cause of anemia and malnutrition in resource-limited countries. Current drug treatments rely on the benzimidazole derivatives albendazole and mebendazole, but there is emerging resistance to these drugs. As part of a larger screening effort, using a hamster-based ex vivo assay, anthelmintic activity toward Ancylostoma ceylanicum was observed in the crude extract of aerial parts of Dalea ornata. These studies have led to the isolation and characterization of phenolic metabolites 1-10. The structures were determined by 1D and 2D NMR spectroscopy, and the absolute configuration of 1 was assigned using electronic circular dichroism data. The new compound, (2S)-8-(3-methylbut-2-en-1-yl)-6,7,4'-trihydroxyflavanone (1), was weakly active at 7.3 μM, with 17% reduction in survival of the hookworms after 5 days. The rotenoids deguelin (9) and tephrosin (10), predictably perhaps, were the most active, with complete worm mortality observed by day 4 (or earlier) at 6.3 and 6.0 μM, respectively. The effects of 1-10 on hookworm motility and on toxicity to hamster splenocytes were also explored as important measures of treatment potential.

Evaluation of in vivo antitrypanosomal activity of crude extracts of Artemisia abyssinica against aTrypanosoma congolense isolate

BackgroundAfrican trypanosomiasis is a major disease of economic and public health importance affecting agricultural and human development. The search for alternative compounds against African trypanosomiasis is justified by various limitations of existing chemotherapeutic agents. This study was aimed at screening the hydromethanolic and dichloromethane (DCM) crude extracts of aerial parts of Artemisia abyssinica for in vivo antitrypanosomal activity against Trypanosoma congolense isolate in mice.MethodsThe aerial parts of the plant were extracted by maceration technique using dichloromethane and 80% methanol to obtain the corresponding crude extracts. The plant extracts at doses of 100, 200 and 400 mg/kg body weight were administered intraperitoneally daily for 7 days to mice infected with Trypanosoma congolense. Diminazene aceturate and distilled water were used as positive and as negative controls respectively. The level of parasitaemia, body weight, packed cell volume, differential leukocyte counts and mean survival period were monitored.ResultsThe study showed that the DCM extract at 200 and 400 mg/kg, and the hydromethanolic extract at 400 mg/kg reduced parasitaemia (p < 0.05), ameliorated anaemia (p < 0.05), prevented body weight loss (p < 0.05) and resulted in significant increase in neutrophil levels (p < 0.05) and marked decrease in lymphocyte levels (p < 0.05) compared to the negative control.ConclusionsThis study established that aerial parts of A. abyssinica have antitrypanosomal potential and can be considered a potential source of new drugs for the treatment of tropical diseases caused by trypanosomes.

Screening of biological activities of Polygonum maritimum L. from Algerian coast

ObjectiveTo investigate the antioxidant and the antibacterial activities of crude extract from aerial part of Polygonum maritimum L. (Polygonaceae) (P. maritimum) and to find new actives biomolecules. MethodsThe whole plant was collected from the Rechgoune coast (West of Algeria), and methanolic crude extract of aerial parts of P. maritimum (PMCE) was prepared. The extract was tested against different bacterial strain and tested for his ability to neutralize free radical (DPPH) and to scavenge the H2O2. ResultsPMCE had a very high content of total phenol, which was (352.49±18.03) mg/g dry weight, expressed as gallic acid equivalent. PMCE exhibited excellent antioxidant activity, as measured using DPPH and H2O2scavenging assays. It also showed a high antibacterial activity against gram–positive bacterial strains: Bacillus cereus, Bacillus subtilis and Staphylococcus aureus with an highest MIC of 120 μg/mL. ConclusionsThe antioxidant and antibacterial activity of the PMCE is probably due to phenolic compounds present in the extract. The contemporary presence of antioxidant and antibacterial activities in the PMCE suggests that this plant may be a source of bioactive substances with multifaceted activity.

Anti-spasmodic action of crude methanolic extract and a new compound isolated from the aerial parts of Myrsine africana

BackgroundMyrsine africana is an herbaceous plant that is traditionally used as appetizer and carminative. Locally, it is used for the treatment of pulmonary tuberculosis, rheumatism and diarrhea by healers. The aims of the current study were to screen the crude methanol extract obtained from the aerial parts (leaves and stem) of M. africana, for antispasmodic actions on isolated tissues and further to subject the ethyl acetate (EtOAc) fraction of plant to column chromatography for isolation of pure compounds.MethodsThe antispasmodic action of the crude methanol extract was measured on the spontaneous rabbit's jejunum preparations at concentration 0.01, 0.03, 0.1, 0.3, 1.0, 5.0 and 10.0 mg/ml. The crude extract was also applied, in similar concentrations, on KCl (80 mM) induced contractions to explain its possible mode of action.ResultsA new compound Myrsigenin was isolated from the EtOAc fraction of M. africana. The structure of the compound was identified with the help of 13C-NMR, 1H-NMR, HMBC, HMQC, NOESY and COSY. The plant crude methanol extract showed a significant antispasmodic action on rabbit jejunum and abolished the tissue contraction completely at concentration of 5.0 mg/ml.ConclusionThe study concludes that the methanol crude extract of aerial parts of M. africana has antispasmodic action possibly through the calcium channel blocking mechanisms. A new compound Myrsigenin was isolated from the EtOAc fraction of the plant.

Monoamine oxidase inhibitory activity of some Hypericum species native to South Brazil.

The total methanol crude extracts and petroleum ether, chloroform, and methanol fractions obtained from Hypericum species, H. caprifoliatum, H. carinatum, H. connatum, H. cordatum, H. myrianthum, H. piriai, H. polyanthemum and H. brasiliense, all native to South Brazil, were assayed for monoamine oxidase A (MAO A) and MAO B inhibitory activity in rat brain mitochondrial preparations at concentrations ranging from 1 to 20microg mL(-1). Three benzopyrans, HP1 (6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran), HP2 (7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran) and HP3 (5-hydroxy-6-isobutyryl-7-methoxy-2,2dimethylbenzopyran) isolated from H. polyanthemum were also tested at maximal concentrations of 150, 150 and 75/microM, respectively. The lipophilic extracts of H. polyanthemum, H. caprifoliatum and H. piriai displayed MAO A inhibitory activity greater than 50%. Among the benzopyrans, only HP3 showed significant activity, with an IC50 value of 22 microM. The total methanol crude extracts of aerial parts from H. carinatum, H. connatum, H. cordatum, H. polyanthemum and H. piriai were evaluated for antidepressant activity in the Porsolt's forced swimming test in Wistar rats (270 mg kg(-1) day(-1); i.p); however, none of them showed activity.

Antispasmodic and bronchodilator activities of St John's wort are putatively mediated through dual inhibition of calcium influx and phosphodiesterase

The crude extract of aerial parts of St John's wort (Hypericum perforatum) (Hp.Cr) and its fractions were studied in vitro for its possible spasmolytic and bronchodilator activities to rationalize some of its medicinal uses. In rabbit jejunum preparations, Hp.Cr caused a concentration-dependent relaxation of both spontaneous and K+ (80 mm)-induced contractions at a similar concentration range (0.1-1.0 mg/mL), similar to that produced by papaverine, whereas verapamil was relatively potent against K+-induced contractions. Hp.Cr shifted the Ca2+ concentration-response curves (CRCs) to the right, similar to that caused by papaverine or verapamil and also caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In guinea-pig tracheal preparations, Hp.Cr caused relaxation of carbachol and K+-induced contractions at similar concentrations (0.01-0.3 mg/mL) and also shifted the isoprenaline-induced inhibitory CRCs to the left, similar to that caused by papaverine. In rabbit aorta preparations at rest, Hp.Cr produced a moderate vasoconstriction, while exhibited vasodilator effect against phenylephrine and K+-induced contractions. Papaverine and verapamil also produced similar non-specific vasodilation, but were devoid of any vasoconstrictor effect. Hp.Cr caused suppression of atrial force of contractions at concentrations about 20 times higher than those that produced inhibitory effect in smooth muscle preparations, similar to papaverine. These results suggest that the spasmolytic effects of Hp.Cr are mediated through dual inhibition of calcium influx and phosphodiesterase (PDE)-like mechanisms, which might explain the medicinal use of St John's wort in the disorders of gastrointestinal and respiratory tracts. Furthermore, the presence of Ca2+ antagonist and PDE inhibitory-like constituents might also be contributing to some extent in the well established use of plant in depression.