scholarly journals Extraction and Fractionation Effects on Antiplasmodial Activity and Phytochemical Composition of Palicourea hoffmannseggiana

2021 ◽  
Vol 8 (01) ◽  
pp. e34-e42
Author(s):  
Leticia Hiromi Ohashi ◽  
Douglas Costa Gontijo ◽  
Maria Fernanda Alves do Nascimento ◽  
Luciano Ferreira Margalho ◽  
Geraldo Célio Brandão ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Scale Up ◽  
Indole Alkaloid ◽  
Ethanol Extract ◽  
Parasite Growth ◽  
In Vitro Activity ◽  
Acid Base ◽  
Leaf Extracts ◽  
Leaf Powder

AbstractThe present study on Palicourea hoffmannseggiana, which was collected at Marapanim, state of Pará, Brazil, comprises the preparation of different stem and leaf extracts and fractions. Ethanol, hydroethanol, and water extracts were prepared by several methods and evaluated for in vitro activity against resistant Plasmodium falciparum (W2 strain), disclosing a low parasite growth inhibition effect (< 50%). Dereplication by UPLC-DAD-ESI−MS of the leaf ethanol extract showed the presence of two known alkaloids, lyalosidic and strictosidinic acids, along with a sinapoyl ester of lyalosidic acid, with m/z 719.33 [M+H]+, which is possibly a new monoterpene indole alkaloid representative. Sequential liquid-liquid acid-base alkaloid separations from the leaf ethanol extract as well as directly from leaf powder afforded fractions of increased parasite growth inhibition, reaching up to 92.5±0.7%. The most bioactive fractions were shown to contain the β-carboline alkaloids harmane and 4-methyl-β-carboline, along with N-methyl-tryptamine and N-acetyl-tryptamine, while monoterpene indole alkaloids were detected in inactive fractions of these processes. The present results demonstrate that these preliminary fractionation methods can lead to significantly active fractions supporting an adequate scale-up to carrying out the isolation of anti-plasmodial compounds.

scholarly journals Burdock (Arctium lappa) Leaf Extracts Increase the In Vitro Antimicrobial Efficacy of Common Antibiotics on Gram-positive and Gram-negative Bacteria

2017 ◽  
Vol 15 (1) ◽  
pp. 92-102 ◽  
Author(s):  
Lucia Pirvu ◽  
Isabela Nicorescu ◽  
Cristina Hlevca ◽  
Bujor Albu ◽  
Valentin Nicorescu
Keyword(s):  
Staphylococcus Aureus ◽  
Ethanol Extract ◽  
Leaf Extracts ◽  
Gram Positive ◽  
Polyphenol Compounds ◽  
Arctium Lappa ◽  
Gram Negative ◽  
E Coli ◽  
Polar Extracts

AbstractThis work aimed to study the potential effects of four Arctii folium extracts, 5 mg gallic [GAE] acid equivalents per 1 mL sample, on six antibiotics (Ampicillin/AM, Tetracycline/TE, Ciprofloxacin/CIP, Sulfamethoxazole-Trimethoprim/SXT, Chloramphenicol/C and Gentamicin/CN) tested on four Gram-positive (Staphylococcus aureus ATCC 6538, Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, and Staphylococcus epidermidis ATCC 12228) and five Gram-negative (Proteus mirabilis ATCC 29245, Escherichia coli ATCC 35218, E. coli ATCC 11229, E. coli ATCC 8739, and Bacillus cereus ATCC 11778) bacteria. Arctii folium extracts were the whole ethanol extract/W and subsequent ethyl acetate/EA, aqueous/AQ, and chloroform/CHL fractions. Chemical qualitative analysis (HPTLC method) emphasized five main polyphenol compounds in Arctii folium polar extracts: chlorogenic acid (Rf≈0.52/0.55) and its isomer, 1,5-di-O-caffeoylquinic acid (Rf≈0.90/0.92), plus cynarin (Rf≈0.77), hyperoside (Rf≈0.68/0.64) and isoquercitrin (Rf≈0.69/0.71). Microbiological screening indicated Arctii folium polar extracts (AQ and W) efficacy on S. epidermidis ATCC 12228; the MIC values were in the range of common antibiotics, being 32 and 128 μg GAE per mL sample respectively. The unpredictable effects (stimulatory or inhibitory) of Arctii folium extracts in combination with typical antibiotics as well as a potential use of the whole ethanol extract/W for restoring the antimicrobial potency of susceptible antibiotics have also been evidenced.

scholarly journals In Vitro Antiplasmodium Effects of Dermaseptin S4 Derivatives

2002 ◽  
Vol 46 (4) ◽  
pp. 1059-1066 ◽  
Author(s):  
Arie Dagan ◽  
Leah Efron ◽  
Leonid Gaidukov ◽  
Amram Mor ◽  
Hagai Ginsburg
Keyword(s):  
Growth Inhibition ◽  
Variable Structure ◽  
Dose Dependence ◽  
Parasite Growth ◽  
Host Cells ◽  
Antimalarial Agents ◽  
Infected Cells ◽  
Parasite Viability ◽  
Acyl Derivatives

ABSTRACT The 13-residue dermaseptin S4 derivative K4S4(1-13)a (P) was previously shown to kill intraerythrocytic malaria parasites through the lysis of the host cells. In this study, we have sought peptides that will kill the parasite without lysing the erythrocyte. To produce such peptides, 26 compounds of variable structure and size were attached to the N terminus of P and screened for antiplasmodium and hemolytic activities in cultures of Plasmodium falciparum. Results from this screen indicated that increased hydrophobicity results in amplified antiplasmodium effect, irrespective of the linearity or bulkiness of the additive. However, increased hydrophobicity also was generally associated with increased hemolysis, with the exception of two derivatives: propionyl-P (C3-P) and isobutyryl-P (iC4-P). Both acyl-peptides were more effective than P, with 50% growth inhibition at 3.8, 4.3, and 7.7 μM, respectively. The antiparasitic effect was time dependent and totally irreversible, implying a cytotoxic effect. The peptides were also investigated in parallel for their ability to inhibit parasite growth and to induce hemolysis in infected and uninfected erythrocytes. Whereas the dose dependence of growth inhibition and hemolysis of infected cells overlapped when cells were treated with P, the acyl-peptides exerted 50% growth inhibition at concentrations that did not cause hemolysis. Noticeably, the acyl derivatives, but not P, were able to dissipate the parasite plasma membrane potential and cause depletion of intraparasite potassium under nonhemolytic conditions. These results clearly demonstrate that the acyl-peptides can affect parasite viability in a manner that is dissociated from lysis of the host cell. Overall, the data indicate the potential usefulness of this strategy for development of selective peptides as investigative tools and eventually as antimalarial agents.

scholarly journals Phytochemical, physicochemical, TLC, minerals analysis and in-vitro antioxidant activity of ethanolic extract of leaves of Heldigardia populifolia

2018 ◽  
Vol 1 (1) ◽  
pp. 22-26
Author(s):  
T Bhanumathi ◽  
P Keerthana ◽  
A Cheenakesavulu ◽  
M Neeharika ◽  
E Sandhya ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Phytochemical Screening ◽  
Permissible Limits ◽  
Leaf Powder ◽  
Composition Of Minerals ◽  
Tlc Analysis ◽  
In Vitro Antioxidant Activity

The aim of present study was to investigate the preliminary phytochemical, physicochemical, TLC, minerals analysis and In-vitro antioxidant activity of leaves of ethanolic extract of Heldigardia populifolia. The preliminary phytochemical screening of ethanolic extract showed the presence of triterpenoids, flavonoids, glycosides, sterols, steroids, phenols, carbohydrates and saponins. The composition of minerals found in the leaf powder was within the permissible limits. TLC analysis of ethanol extract showed the five spots which indicate the presence of five phytoconstituents. The extractive value of ethanol was high than acetone. Ash values were within the limits. The in-vitro antioxidant activity of ethanolic extract increased with increasing the concentration. The ethanolic extract in all the concentration showed the significant antioxidant activity.

scholarly journals The Glutamate-Rich Protein (GLURP) of Plasmodium falciparum Is a Target for Antibody-Dependent Monocyte-Mediated Inhibition of Parasite Growth In Vitro

1998 ◽  
Vol 66 (1) ◽  
pp. 11-17 ◽  
Author(s):  
Michael Theisen ◽  
Soe Soe ◽  
Claude Oeuvray ◽  
Alan W. Thomas ◽  
Jens Vuust ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Growth Inhibition ◽  
Cross Reactivity ◽  
Parasite Growth ◽  
Biologically Active ◽  
Dependent Manner ◽  
Igg Antibodies ◽  
Inhibitory Effects ◽  
Direct Invasion

ABSTRACT Monocyte-dependent as well as direct inhibitory effects of antimalarial antibodies point toward antigens accessible at the time of merozoite release as targets for biologically active antibodies capable of mediating protection against Plasmodium falciparum. The glutamate-rich protein (GLURP), being an antigen associated with mature schizont-infected erythrocytes, was therefore the object of the present investigation, in which we analyzed whether anti-GLURP antibodies can either interfere directly with merozoite invasion or act indirectly by promoting a monocyte-dependent growth inhibition, antibody-dependent cellular inhibition. GLURP-specific human immunoglobulin G (IgG) antibodies, from pooled IgG of healthy Liberian adults who were clinically immune to malaria, were purified by affinity chromatography on columns containing R0 (N-terminal nonrepetitive region of GLURP) or R2 (C-terminal repetitive region of GLURP) recombinant protein or synthetic peptides as ligands. Analysis of the pattern of reactivity of highly purified anti-GLURP antibodies led to the definition of at least four B-cell epitopes. One epitope was specific for R0, two were specific for R2, and the fourth displayed cross-reactivity between R0 and R2. None of the purified IgG antibodies had direct invasion-inhibitory effects, even at high concentrations. In contrast, when allowed to cooperate with monocytes, all anti-GLURP IgG preparations mediated a strong monocyte-dependent parasite growth inhibition in a dose-dependent manner.

scholarly journals Two novel human anti-CD25 antibodies with antitumor activity inversely related to their affinity and in vitro activity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Deyong Song ◽  
Xiu Liu ◽  
Chuangchuang Dong ◽  
Qiaoping Wang ◽  
Chunjie Sha ◽  
...  
Keyword(s):  
T Cells ◽  
Tumor Growth ◽  
Growth Inhibition ◽  
Treg Cells ◽  
Tumor Growth Inhibition ◽  
In Vitro Activity ◽  
Limited Efficacy ◽  
Cancer Models ◽  
Excellent Candidate

AbstractHigh tumor regulatory T (Treg) cell infiltration is associated with poor prognosis of many cancers. CD25 is highly expressed on tumor Treg cells and is a potential target for Treg deletion. Previously characterized anti-CD25 antibodies appear to have limited efficacy in tumor inhibition. Here we identified two human anti-CD25 antibodies, BA9 and BT942, which did not prevent the activation of IL-2R signaling pathway by IL-2. BT942 had weaker binding and cytotoxic activity to human CD25-expressing cell lines than BA9. But both demonstrated significant tumor growth inhibition in early and late-stage animal cancer models. BT942 resulted in a higher expansion of CD8+ T cells and CD4+ T cells in tumor microenvironment in mouse MC38 model compared to BA9. BT942 also demonstrated significant higher tumor growth inhibition and higher expansion of CD8+ T cells and CD4+ T cells in combination with an anti-PD1 antibody. Pharmacokinetic study of BT942 in cynomolgus monkeys demonstrated a half-life of 206.97 ± 19.03 h. Structural analysis by cryo-EM revealed that BT942 recognizes an epitope on opposite side of the CD25-IL-2 binding site, consistent with no IL-2 signaling blockade in vitro. BT942 appears to be an excellent candidate for cancer immunotherapy.

scholarly journals In Vitro and In Silico Screening and Characterization of Antimicrobial Napin Bioactive Protein in Brassica juncea and Moringa oleifera

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2080
Author(s):  
Sangeeta Chandrashekar ◽  
Raman Vijayakumar ◽  
Ramachandran Chelliah ◽  
Eric Banan-Mwine Daliri ◽  
Inamul Hasan Madar ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Brassica Juncea ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Cell Aggregation ◽  
Bacterial Strains ◽  
Leaf Extracts ◽  
Inhibition Concentration ◽  
Potent Inhibition

The study aimed to investigate the antibacterial activity of Mustard (Brassica juncea) and Moringa (Moringa oleifera) leaf extracts and coagulant protein for their potential application in water treatment. Bacterial cell aggregation and growth kinetics studies were employed for thirteen bacterial strains with different concentrations of leaf extracts and coagulant protein. Moringa oleifera leaf extract (MOS) and coagulant protein showed cell aggregation against ten bacterial strains, whereas leaf extract alone showed growth inhibition of five bacterial strains for up to 6 h and five bacterial strains for up to 3 h. Brassica juncea leaf extract (BJS) showed growth inhibition for up to 6 h, and three bacterial strains showed inhibition for up to 3 h. The highest inhibition concentration with 2.5 mg/mL was 19 mm, and furthermore, the minimum inhibitory concentration (MIC) (0.5 mg/mL) and MBC (1.5 mg/mL) were determined to have a higher antibacterial effect for <3 KDa peptides. Based on LCMS analysis, napin was identified in both MOS and BJS; furthermore, the mode of action of napin peptide was determined on lipoprotein X complex (LpxC) and four-chained structured binding protein of bacterial type II topoisomerase (4PLB). The docking analysis has exhibited moderate to potent inhibition with a range of dock score −912.9 Kcal/mol. Thus, it possesses antibacterial-coagulant potential bioactive peptides present in the Moringa oleifera purified protein (MOP) and Brassica juncea purified protein (BJP) that could act as an effective antimicrobial agent to replace currently available antibiotics. The result implies that MOP and Brassica juncea purified coagulant (BJP) proteins may perform a wide degree of antibacterial functions against different pathogens.

scholarly journals Assessment of cytotoxicity and antiplasmodial activities of Prosopis africana leaf extracts

2020 ◽  
Vol 12 (1) ◽  
pp. 380-385
Author(s):  
M.M. Idris ◽  
U. Idris
Keyword(s):  
Ethanol Extract ◽  
Negative Control ◽  
Sub Saharan Africa ◽  
Antiplasmodial Activity ◽  
Health Concern ◽  
Leaf Extracts ◽  
Methanol Fraction ◽  
Prosopis Africana ◽  
Ethnomedicinal Plant

Malaria is a major health concern in Sub Saharan Africa and there are few effective treatment options. Nigeria has diverse flora with potent antimalarial phytochemicals and high ethnomedicinal plants uses. This study investigated the phytochemicals, Cytotoxicity and in-vitro antiplasmodial activity of ethnomedicinal plant which is Prosopis africana. Crude ethanol extract and macerated fractions from the ethnomedicinal plant were screened for major classes of antiplasmodial phytochemical compounds i.e., terpenoids, alkaloids, flavonoids, anthraquinones and Steroids. The antiplasmodial assay was conducted at 5% parasitaemia for 24 and 48 hours, against P. falciparum. Artemether-Lumefantrine was used as a positive control while 0.5% DMSO in RPMI 1640 medium was used as negative control. Moreover, all plant extract and fractions of P. africana were found to be effective in vitro for antiplasmodial activity, they demonstrated remarkable bioactivities at all concentrations; Methanol fraction (Pa-05) shows the highest activity with percentage elimination of 83.9% at 625µg/ml, 87.5% at 1250µg/ml, 92.9% at 2500µg/ml and 96.4% at 5000µg/ml. However, all the extract fractions have shown a good activity against the Brine Shrimp nauplii larvae. Crude Ethanol extract (PA-01) and n-Hexane fraction displayed the highest activity (LC50 58.482µg/ml and 75.462 µg/ml) respectively. However, the results suggested that extracts of P. africana showed the most curative anti-plasmodia effect in infected blood which may be attributed to the presence of phytochemical constituents such as a alkaloids, flavonoids, and terpenoids. Keywords: Ethanol extract, Fractions, Phytochemicals, Cytotoxicity and Antiplasmodial

scholarly journals In Vitro Test of Antibacterial Ethanol Extract, n-Hexane Fraction and Ethyl acetate Fraction of Sungkai Leaf (Peronema cenescens) Against Salmonella typhi

1970 ◽  
Vol 8 (3) ◽  
pp. 59-61
Author(s):  
Sitepu Nadroh Br.
Keyword(s):  
Ethyl Acetate ◽  
Antibacterial Properties ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
Salmonella Typhi ◽  
Hexane Fraction ◽  
In Vitro Test ◽  
Leaf Powder ◽  
Vitro Test

Object: This study aims to look at the class of compounds and the comparison of the antibacterial activity of ethanol extract, n-hexane fraction and ethyl acetate of Sungkai leaves against Salmonella typhi. Methods: Study included phytochemical screening and in vitro antibacterial testing of ethanol extract, n-hexane fraction and ethyl acetate of Sungkai leaves against Salmonella typhi. Results: obtained groups of chemical compounds alkaloids, flavonoids, glycosides, anthraquinones, tannins and triterpenoids/steroids on Sungkai leaf powder. Ethanol extract of Sungkai leaves obtained resistance at a concentration of 20% by 12.7 mm, and inhibition of the ethyl acetate fraction at a concentration of 20% of 14.8 mm. Conclusion: Ethyl acetate fraction of Sungkai leaves have antibacterial properties against S. typhi which is greater than ethanol extract and hexane fraction of leaf heal.  

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