scholarly journals Phytochemical Analysis and Trypanocidal Activity of Marrubium incanum Desr.

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3140
Author(s):  
Claudio Frezza ◽  
Alessandro Venditti ◽  
Armandodoriano Bianco ◽  
Mauro Serafini ◽  
Massimo Pitorri ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Central Italy ◽  
Target Cells ◽  
Phytochemical Analysis ◽  
Isolation And Identification ◽  
Etoh Extract ◽  
Lead Compounds ◽  
Aerial Parts ◽  
Traditional Remedy ◽  
Ch2cl2 Extract

The rationale inspiring the discovery of lead compounds for the treatment of human parasitic protozoan diseases from natural sources is the well-established use of medicinal plants in various systems of traditional medicine. On this basis, we decided to select an overlooked medicinal plant growing in central Italy, Marrubium incanum Desr. (Lamiaceae), which has been used as a traditional remedy against protozoan diseases, and to investigate its potential against Human African trypanosomiasis (HAT). For this purpose, we assayed three extracts of different polarities obtained from the aerial parts of M. incanum—namely, water (MarrInc-H2O), ethanol (MarrInc-EtOH) and dichloromethane (MarrInc-CH2Cl2)—against Trypanosoma brucei (TC221), with the aim to discover lead compounds for the development of antitrypanosomal drugs. Their selectivity index (SI) was determined on mammalian cells (BALB/3T3 mouse fibroblasts) as a counter-screen for toxicity. The preliminary screening selected the MarrInc-CH2Cl2 extract as the most promising candidate against HAT, showing an IC50 value of 28 μg/mL. On this basis, column chromatography coupled with the NMR spectroscopy of a MarrInc-CH2Cl2 extract led to the isolation and identification of five compounds i.e. 1-α-linolenoyl-2-palmitoyl-3-stearoyl-sn- glycerol (1), 1-linoleoyl-2-palmitoyl-3-stearoyl-sn-glycerol (2), stigmasterol (3), palmitic acid (4), and salvigenin (5). Notably, compounds 3 and 5 were tested on T. brucei, with the latter being five-fold more active than the MarrInc-CH2Cl2 extract (IC50 = 5.41 ± 0.85 and 28 ± 1.4 μg/mL, respectively). Furthermore, the SI for salvigenin was >18.5, showing a preferential effect on target cells compared with the dichloromethane extract (>3.6). Conversely, stigmasterol was found to be inactive. To complete the work, also the more polar MarrInc-EtOH extract was analyzed, giving evidence for the presence of 2″-O-allopyranosyl-cosmosiin (6), verbascoside (7), and samioside (8). Our findings shed light on the phytochemistry of this overlooked species and its antiprotozoal potential, providing evidence for the promising role of flavonoids such as salvigenin for the treatment of protozoal diseases.

scholarly journals Evaluation of cytotoxicity, anti-herpes simplex virus type 1 (HSV-1) and antibacterial activities of Ficus vasta and phytoconstituents

2013 ◽  
Vol 3 (1) ◽  
pp. 211-218 ◽  
Author(s):  
Khaled Rashed ◽  
Lucy Ono
Keyword(s):  
Methanol Extract ◽  
Biological Activities ◽  
Vero Cells ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Phytochemical Analysis ◽  
Potential Candidate ◽  
Isolation And Identification ◽  
Aerial Parts ◽  
Hsv 1

This study deals with the evaluation of in vitro cytotoxicity of the methanol 80% extract of Ficus vasta aerial parts in Vero cells, anti-HSV-1 and antibacterial activities and the determination of the phytochemical content of the F. vasta methanol extract. The extract was tested for its cytotoxicity in Vero cells and for anti-HSV-1 and against bacterial strains as S. aureus, S. epidermidis, E. coli and P. aeruginosa and also phytochemical constituents were detected. The results showed that this extract presented a CC50 value of 389 µg/mL, an intermediate value taking into account other researchers reported for some Moraceae species. Regarding the other biological activities, antiviral effect was not demonstrated by a HSV-1 challenge dilution of 100x tissue culture infective dose 50% (TCID50) and also by the disk-diffusion method at the higher non-toxic concentration of the extract (119 µg/mL). Phytochemical analysis of the methanol extract proved the presence of carbohydrates, tannins, flavonoids, coumarins, alkaloids and triterpenes. Chromatographic separation of the methanol extract resulted in the isolation and identification of ?-sitosterol, stigmasterol, lupeol, ursolic acid, naringenin, luteolin, quercetin, vitexin, quercetin 3-O-?-glucoside and rutin. The results indicated that F. vasta aerial parts methanol extract is potential candidate for experiments of biological activity screening that are not anti-HSV-1 or antibacterial against the strains evaluated in this study, to be carried on in the future.DOI: http://dx.doi.org/10.3329/icpj.v3i1.17295 International Current Pharmaceutical Journal, December 2013, 3(1): 211-218

scholarly journals Phytochemical Analysis and Biological Activities of the Ethanolic Extract of Daphne sericea Vahl Flowering Aerial Parts Collected in Central Italy

Biomolecules ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 379
Author(s):  
Claudio Frezza ◽  
Alessandro Venditti ◽  
Daniela De Vita ◽  
Fabio Sciubba ◽  
Pierpaolo Tomai ◽  
...  
Keyword(s):  
Biological Activities ◽  
Central Italy ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Phytochemical Analysis ◽  
Pheophorbide A ◽  
Antioxidant Power ◽  
Aerial Parts ◽  
Anisic Acid ◽  
First Time

In this paper, the first phytochemical analysis of the ethanolic extract of Daphne sericea Vahl flowering aerial parts collected in Italy and its biological activities were reported. Eleven compounds were identified i.e., α-linolenic acid (1), tri-linoleoyl-sn-glycerol (2), pheophorbide a ethyl ester (3), pilloin (4), sinensetin (5), yuanhuanin (6), rutamontine (7), syringin (8), p-coumaric acid (9), p-anisic acid (10) and caffeic acid (11). To the best of our knowledge, compounds (1-4, 7-8 and 10) were isolated from D. sericea for the first time during this work, whereas sinensetin (5) represents a newly identified component of the entire Thymelaeaceae family. The extract was found to possess radical scavenging against both DPPH• and 2,2′-azino-bis(3-thylbenzothiazoline-6-sulfonic acid (ABTS•+) radicals, with at least a 40-fold higher potency against the latter. Moreover, chelating abilities against both ferrous and ferric ions have been highlighted, thus suggesting a possible indirect antioxidant power of the extract. Although the precise bioactive compounds remain to be discovered, the polyphenolic constituents, including phenolic acids, tannins and flavonoids, seem to contribute to the antioxidant power of the phytocomplex. In addition, the extract produced cytotoxic effects in MDA-MB-231 and U87-MG cancer cell lines, especially at the concentration of 625 μg/mL and after 48–72 h. Further studies are required to clarify the contribution of the identified compounds in the bioactivities of the extract and to support possible future applications.

Cell-Specific Chemical Delivery Using a Selective Nitroreductase–Nitroaryl Pair

2018 ◽  
Author(s):  
Todd D. Gruber ◽  
Chithra Krishnamurthy ◽  
Jonathan B. Grimm ◽  
Michael R. Tadross ◽  
Laura M. Wysocki ◽  
...  
Keyword(s):  
Small Molecules ◽  
Mammalian Cells ◽  
Target Cells ◽  
Specific Chemical ◽  
E Coli ◽  
Enzyme Substrate ◽  
Cell Specificity ◽  
General Chemical ◽  
Increased Activity ◽  
Enzyme Variant

<p>The utility of<b> </b>small molecules to probe or perturb biological systems is limited by the lack of cell-specificity. ‘Masking’ the activity of small molecules using a general chemical modification and ‘unmasking’ it only within target cells could overcome this limitation. To this end, we have developed a selective enzyme–substrate pair consisting of engineered variants of <i>E. coli</i> nitroreductase (NTR) and a 2‑nitro-<i>N</i>-methylimidazolyl (NM) masking group. To discover and optimize this NTR–NM system, we synthesized a series of fluorogenic substrates containing different nitroaromatic masking groups, confirmed their stability in cells, and identified the best substrate for NTR. We then engineered the enzyme for improved activity in mammalian cells, ultimately yielding an enzyme variant (enhanced NTR, or eNTR) that possesses up to 100-fold increased activity over wild-type NTR. These improved NTR enzymes combined with the optimal NM masking group enable rapid, selective unmasking of dyes, indicators, and drugs to genetically defined populations of cells.</p>

scholarly journals The Prospective Use of Brazilian Marine Macroalgae in Schistosomiasis Control

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 234
Author(s):  
Erika M. Stein ◽  
Sara G. Tajú ◽  
Patrícia A. Miyasato ◽  
Rafaela P. de Freitas ◽  
Lenita de F. Tallarico ◽  
...  
Keyword(s):  
Multivariate Analysis ◽  
Marine Algae ◽  
Pearson Correlation ◽  
Marine Macroalgae ◽  
Parasitic Disease ◽  
Isolation And Identification ◽  
Promising Alternative ◽  
Schistosomiasis Control ◽  
Lead Compounds ◽  
Correlation Tests

Schistosomiasis is a parasitic disease that affects more than 250 million people. The treatment is limited to praziquantel and the control of the intermediate host with the highly toxic molluscicidal niclosamide. Marine algae are a poorly explored and promising alternative that can provide lead compounds, and the use of multivariate analysis could contribute to quicker discovery. As part of our search for new natural compounds with which to control schistosomiasis, we screened 45 crude extracts obtained from 37 Brazilian seaweed species for their molluscicidal activity against Biomphalaria glabrata embryos and schistosomicidal activities against Schistosoma mansoni. Two sets of extracts were taxonomically grouped for metabolomic analysis. The extracts were analyzed by GC–MS, and the data were subjected to Pattern Hunter and Pearson correlation tests. Overall, 22 species (60%) showed activity in at least one of the two models. Multivariate analysis pointed towards 3 hits against B. glabrata veliger embryos in the Laurencia/Laurenciella set, 5 hits against B. glabrata blastula embryos, and 31 against S. mansoni in the Ochrophyta set. Preliminary annotations suggested some compounds such as triquinane alcohols, prenylated guaianes, dichotomanes, and xenianes. Despite the putative identification, this work presents potential candidates and can guide future isolation and identification.

scholarly journals Antihepatotoxic Activity of Phyllanthus atropurpureus Cultivated in Egypt

2011 ◽  
Vol 66 (9-10) ◽  
pp. 447-452 ◽  
Author(s):  
Taha Sarg ◽  
Afaf Abdel Ghani ◽  
Rawia Zayed ◽  
May El-Sayed
Keyword(s):  
Liver Injury ◽  
Active Ingredient ◽  
Ornamental Plants ◽  
Hepatoprotective Activity ◽  
Maximum Activity ◽  
Phytochemical Analysis ◽  
Root Extract ◽  
Aerial Parts ◽  
Serum Aspartate Aminotransferase ◽  
Antihepatotoxic Activity

The genus Phyllanthus (family Euphorbiaceae) is considered one of the important medicinal and ornamental plants. A phytochemical analysis of the extracts was performed to search for the active ingredient. Results of the investigation of the hepatoprotective activity of Phyllanthus atropurpureus Boj. Hort. Maurit. revealed that the activities of alcoholic extracts of its aerial parts and roots were quite similar to those of silymarin. Both of them improve the parameters of CCl4-induced liver injury including serum aspartate aminotransferase and alanine aminotransferase. Among the extracts tested, the root extract showed maximum activity compared to the aerial parts extract and to silymarin.

scholarly journals Mammalian cell invasion and intracellular trafficking by Trypanosoma cruzi infective forms

2005 ◽  
Vol 77 (1) ◽  
pp. 77-94 ◽  
Author(s):  
Renato A. Mortara ◽  
Walter K. Andreoli ◽  
Noemi N. Taniwaki ◽  
Adriana B. Fernandes ◽  
Claudio V. da Silva ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Host Cell ◽  
Mammalian Cells ◽  
Parasitophorous Vacuole ◽  
Host Cells ◽  
Mammalian Host ◽  
Target Cells ◽  
Sylvatic Cycle ◽  
Final Destination ◽  
Different Strains

Trypanosoma cruzi, the etiological agent of Chagas’ disease, occurs as different strains or isolates that may be grouped in two major phylogenetic lineages: T. cruzi I, associated with the sylvatic cycle and T. cruzi II, linked to the human disease. In the mammalian host the parasite has to invade cells and many studies implicated the flagellated trypomastigotes in this process. Several parasite surface components and some of host cell receptors with which they interact have been identified. Our work focused on how amastigotes, usually found growing in the cytoplasm, can invade mammalian cells with infectivities comparable to that of trypomastigotes. We found differences in cellular responses induced by amastigotes and trypomastigotes regarding cytoskeletal components and actin-rich projections. Extracellularly generated amastigotes of T. cruzi I strains may display greater infectivity than metacyclic trypomastigotes towards cultured cell lines as well as target cells that have modified expression of different classes of cellular components. Cultured host cells harboring the bacterium Coxiella burnetii allowed us to gain new insights into the trafficking properties of the different infective forms of T. cruzi, disclosing unexpected requirements for the parasite to transit between the parasitophorous vacuole to its final destination in the host cell cytoplasm.

scholarly journals NEW FLAVONOIDS FROM THE AERIAL PARTS OF POLYGONUM EQUISETIFORME SM (POLYGONACEAE)

2017 ◽  
Vol 9 (2) ◽  
pp. 166 ◽  
Author(s):  
Sayed A. El-toumy ◽  
Joslin Y. Salib ◽  
Nabila H. Shafik ◽  
Asmaa S. Abd Elkarim ◽  
Gihan A. Mick
Keyword(s):  
Antioxidant Activity ◽  
Methyl Ester ◽  
Secondary Metabolites ◽  
Gallic Acid ◽  
Total Phenolic ◽  
Flavonoid Content ◽  
Isolation And Identification ◽  
Aerial Parts ◽  
Dpph Method ◽  
Phenolic And Flavonoid

<p><strong>Objective: </strong>The current study was to deal the isolation and identification of secondary metabolites from <em>Polygonum equisetiforme</em> and evaluation of antioxidant activity of its extract.</p><p><strong>Methods: </strong>The methanol-water extract (7:3) of the air-dried aerial parts of <em>Polygonum equisetiforme</em> was fractionated and separated to obtain the isolated compounds by different chromatographic techniques. Structures of these compounds were elucidated by UV and 1D⁄2D H⁄ C NMR spectroscopy and compared with the literature data. The crude extract was evaluated for <em>in vitro</em> antioxidant activity using the 2,2 diphenyl dipicryl hydrazine (DPPH) method.</p><p><strong>Results: </strong>Ten secondary metabolites were isolated from <em>Polygonum equisetiforme</em> in this study. Of which three new flavonoids named as 3,5,7,2’,5’ pentahydroxyflavone 3-<em>O</em>-b-D-glucopyranoside (1), 3,5,7,2’,5’ pentahydroxyflavone 3-<em>O</em>-b-D-glucopyranoside 8 C-sulphated (2) and quercetin 3-<em>O-β</em>-D-glucucorinde 6''-methyl ester 8-sulphated (3) as well as quercetin 3-<em>O-β</em>-D-glucucorinde methyl ester (4), quercetin 3-<em>O-</em>β-D-glucopyranoside (5), quercetin 7-<em>O-β-</em>D-glucopyranoside (6),<em> </em>quercetin(7)<sub>, </sub>myricetin (8), <em>P</em><sub>-</sub>methoxy gallic acid methyl ester (9) and gallic acid (10). The antioxidant potential of <em>P. equisetiforme</em> extract was evaluated by investigating it's total phenolic and flavonoid content and DPPH radical scavenging activity whereby the extract showed significant antioxidant activity (IC<sub>50 </sub>= 37.45 μg/ml). The total phenolic and flavonoid content was found to be 130.79±5.502 and 45.8±1.63 μg/ml, respectively.</p><p><strong>Conclusion: </strong><em>Polygonum equisetiforme</em> is a promising medicinal plant, and our study tends to support the therapeutic value of this plant as an antioxidant drug.</p>

The mechanism of T cell mediated cytotoxicity IV. Studies on communicating junctions between cells in contact

1977 ◽  
Vol 196 (1122) ◽  
pp. 73-84 ◽  
Keyword(s):  
T Cell ◽  
Mammalian Cells ◽  
Cytotoxic T Cells ◽  
Diploid Cell ◽  
Target Cells ◽  
Cytotoxic Lymphocytes ◽  
Communicating Junctions ◽  
Unique System ◽  
Pass Through ◽  
Autoradiographic Technique

A modified autoradiographic technique has been developed which makes it possible to demonstrate the intercellular transfer of diffusible molecules through communicating junctions. This technique has been used to decide whether or not there is a cytoplasmic union between cytotoxic lymphocytes and the target cells they destroy. The transfer of 51 Cr, [ 3 H]uridine and [ 3 H]choline has been demonstrated between human diploid cell line cells (MRC 5) in contact. This has provided a system in which the techniques could be assessed. The demonstration that 51 Cr can pass through communicating junctions provides a unique system for the investigations of these structures. Despite the fact that all three labels could transfer between MRC 5 cells in contact, no transfer between cytotoxic T cells and P815 target cells could be demonstrated during a cytotoxic reaction. The reported transfer of fluorescein can probably be attributed to the transfer of fluorescein ester via the extracellular space. It is concluded, therefore, that communicating junctions of the type that can form between certain mammalian cells in contact do not contribute to the mechanism of T cell cytotoxicity.

scholarly journals Phytochemical Screening and TLC Profiling of Various Extracts of Reinwardtia indica

2017 ◽  
Vol 9 (4) ◽  
Author(s):  
Mehta Sonam ◽  
Rana Pawan Singh ◽  
Pooja Saklani
Keyword(s):  
Aqueous Extract ◽  
Methanol Extract ◽  
Scientific Basis ◽  
Phytochemical Screening ◽  
Isolation And Identification ◽  
Aerial Parts ◽  
Biochemical Compound ◽  
Ethanol Extracts ◽  
Layer Chromatography ◽  
The Himalaya

Reinwardtia indica, belongs to family Linaceae known as yellow flax or pyoli commonly found in the Himalaya. The plant has varied ethno medicinal importance such as aerial parts are used to prevent bleeding of cuts and as mouthwash; leaves are used in the treatment of paralysis and as natural antibiotic. Qualitative phytochemical screening of chloroform, acetone, ethanol, methanol and aqueous extracts was performed to explore scientific basis of ethno medicinal potential. It confirmed the presence of many phytochemicals like alkaloids, flavanoids, phenols, tannins, saponins, terpenoids, phlobatanins etc. in various extracts. Most of the phytochemicals were found in methanol and ethanol extracts. Thin Layer chromatography (TLC) of the acetone, methanol, chloroform and aqueous extract was performed for four important phytochemicals alkaloids, flavanoids, tannins and phenol. Flavanoids showed their presence in all extracts with one spot in each (Rf 0.8 for acetone, 0.918 for methanol, 0.816 for chloroform and 0.737 for aqueous extract). Alkaloids and tannins were found in acetone and methanol extract while phenol was present only in methanol extract (Rf 0.8). These findings provided the evidence that Reinwardtia indica is a potent source for some medicinally important phytochemicals and it justifies its use as a medicinal plant. This can be further investigated for the isolation and identification of active biochemical compound of medicinal utilities

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