scholarly journals Leismanicidal Activity of Propolis Collected in the Semiarid Region of Brazil

2021 ◽  
Vol 12 ◽  
Author(s):  
Giani Maria Cavalcante ◽  
Celso Amorim Camara ◽  
Eva Monica Sarmento Da Silva ◽  
Mariana Silva Santos ◽  
Anderson Brandão Leite ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Ethanolic Extract ◽  
Ultra Performance Liquid Chromatography ◽  
Semiarid Region ◽  
Array Detector ◽  
Significant Activity ◽  
Exact Mass ◽  
Leishmanicidal Activity ◽  
Etoh Extract

Objective: The aim of the current study is to investigate the chemical composition, cytotoxic effect, and leishmanicidal activity of propolis collected in the semi-arid region of Bahia, Brazil.Methods: EtOH extract, hexane, EtOAc and MeOH fractions from propolis were analyzed by ultra-performance liquid chromatography coupled with diode array detector and quadrupole time-of-flight mass spectrometry. The identification was based on the exact mass, general fragmentation behaviors and UV absorption of the flavonoids. The in vitro cytotoxic effect and leishmanicidal activity of ethanolic extract, hexane, ethyl acetate, and methanolic fractions of propolis were evaluated.Results: Five triterpenes and twenty-four flavonoids were identified. The propolis did not present toxicity to the host cell up to the maximum concentration tested. In addition, all tested samples showed statistically significant activity against promastigotes of Leishmania chagasi and Leishmania amazonensis. Regarding the activity against amastigote forms of L. amazonensis, the hexane fraction, presented statistically significant activity with IC50 of 1.3 ± 0.1 μg/ml.Conclusion: The results support the idea that propolis can be used for future antileishmania studies.

scholarly journals Antiproliferative Activity and Antioxidant Potential of Extracts of Garcinia gardneriana

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3201
Author(s):  
Simone da Cunha Demenciano ◽  
Magalli Costa Barbosa Lima e Silva ◽  
Caroline Almeida Farias Alexandrino ◽  
Wilson Hino Kato Junior ◽  
Patrícia de Oliveira Figueiredo ◽  
...  
Keyword(s):  
Vitamin C ◽  
Antiproliferative Activity ◽  
High Performance ◽  
Ethanolic Extract ◽  
Antioxidant Potential ◽  
Array Detector ◽  
Chloroform Fraction ◽  
Chemical Profile ◽  
Polycarboxylic Acids

The aim of this study was to evaluate the antiproliferative activity, the antioxidant potential, and the chemical profile obtained from the whole fruit and from leaves of Garcinia gardneriana, a fruit tree from Brazilian Cerrado. To determine in vitro antiproliferative activity, the following neoplastic cell lines were considered, along with an immortalized nontumor cell line. The antioxidant potential was determined, and the evaluation of antiradical air activity was performed. The levels of vitamin C and carotenoids were determined. The chemical profile was analyzed by high-performance liquid chromatography coupled to a diode array detector and a mass spectrometer using electrospray ionization interface. The chloroform fraction of the leaf showed antioxidant activity. The vitamin C content had lower values in fruits and higher in leaves. The content of carotenoids for fruits and leaves was expressive. The ethanolic extract and the hexane and chloroform fractions of fruits were active in all neoplastic lines tested. The leaves showed cytotoxic activity in the hexane fraction in the breast carcinoma line. The analysis of data obtained verified the presence of dimers, monomers, and tetramers of hexoses, polycarboxylic acids, xanthones, flavonoids, biflavonoids, and benzophenones.

scholarly journals Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone ofPicramnia gracilisTul. (Picramniaceae) Fruit:In VitroandIn VivoStudies

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Sara M. Robledo ◽  
Wilson Cardona ◽  
Karen Ligardo ◽  
Jéssica Henao ◽  
Natalia Arbeláez ◽  
...  
Keyword(s):  
Native Species ◽  
Folk Medicine ◽  
Ethanolic Extract ◽  
Phytochemical Analysis ◽  
Medicinal Uses ◽  
Leishmanicidal Activity ◽  
Antileishmanial Drug ◽  
Low Toxicity

Species ofPicramniagenus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition.P. gracilisTul. is a native species from Central and South America and although its fruits are edible, phytochemical analysis or medicinal uses of this species are not known. In the search of candidates to antileishmanial drugs, this work aimed to evaluate the antileishmanial activity ofP. gracilisTul. inin vitroandin vivostudies. Only ethanolic extract of fruits showed leishmanicidal activity. The majoritarian metabolite was5,3′-hydroxy-7,4′-dimethoxyflavanoneether that exhibited high activity againstL. (V.) panamensis(EC5017.0 + 2.8 mg/mL, 53.7 μM) and low toxicity on mammalian U-937 cells, with an index of selectivity >11.8.In vivostudies showed that the flavanone administered in solution (2 mg/kg/day) or cream (2%) induces clinical improvement and no toxicity in hamsters with CL. In conclusion, this is the first report about isolation of5,3′-hydroxy-7,4′-dimethoxyflavanoneofP. gracilisTul. The leishmanicidal activity attributed to this flavanone is also reported for the first time. Finally, thein vitroandin vivoleishmanicidal activity reported here for5,3′-hydroxy-7,4′-dimethoxyflavanoneoffers a greater prospect towards antileishmanial drug discovery and development.

scholarly journals In vitro effect of Acanthospermum australe (Asteraceae) extracts on Acanthamoeba polyphaga trophozoites

2013 ◽  
Vol 15 (4) ◽  
pp. 589-594
Author(s):  
LC Castro ◽  
IP Sauter ◽  
EM Ethur ◽  
C Kauffmann ◽  
R Dall'agnol ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Cytotoxic Effect ◽  
Folk Medicine ◽  
Ethanolic Extract ◽  
Acanthamoeba Keratitis ◽  
New Drugs ◽  
Acanthamoeba Polyphaga ◽  
Aerial Parts ◽  
Vitro Effect

Acanthamoeba is a free-living protozoan widely distributed in the environment, occurring in vegetative trophozoite and resistance cyst stages during its life cycle. It constitutes an etiological agent of Acanthamoeba keratitis, a disease that may cause severe ocular inflammation and blindness. New drugs can be developed from molecules found in plants and thus help in its difficult treatment. Acanthospermum australe (Asteraceae), a plant used in folk medicine, had its effect tested on Acanthamoeba polyphaga. Aqueous and ethanolic extracts of A. austral were obtained from aerial parts for infusion and static maceration, respectively. Concentrations of 10, 5, 2.5, 1.25 and 0.625 mg/ml of the extract were tested against Acanthamoeba polyphaga trophozoites. The cytotoxic effect of the extracts was tested in mammalian cells using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. RESULTS: The 10 mg/ml concentration of ethanolic extract was lethal to 100% of the A. polyphaga trophozoites in 24 h and both extracts presented cytotoxic effect against mammalian cells. These findings suggest that the A. austral ethanolic extract may have compounds with relevance to the development of new amoebicidal drugs.

Improved In Vitro Anti-Tumoral Activity, Intracellular Uptake and Apoptotic Induction of Gemcitabine-Loaded Pegylated Unilamellar Liposomes

2008 ◽  
Vol 8 (4) ◽  
pp. 2102-2113 ◽  
Author(s):  
Christian Celia ◽  
Maria Grazia Calvagno ◽  
Donatella Paolino ◽  
Stefania Bulotta ◽  
Cinzia Anna Ventura ◽  
...  
Keyword(s):  
Thyroid Carcinoma ◽  
Cytotoxic Effect ◽  
Anaplastic Thyroid Carcinoma ◽  
Chemotherapeutic Agents ◽  
Free Drug ◽  
Parp Cleavage ◽  
Significant Activity ◽  
Intracellular Uptake ◽  
Cell Mortality

Anaplastic thyroid carcinoma is one of the most aggressive and lethal solid carcinomas affecting humans. A major limit of the chemotherapeutic agents is represented by their low therapeutic index. In this work, we investigated the possibility of improving the anti-tumoral activity of gemcitabine by using pegylated unilamellar liposomes. Liposomes were made up of 1,2-dipalmitoyl-sn-glycero-3-phospocholine monohydrate/cholesterol/N-(carbonyl-methoxypolyethylene glycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (6:3:1 molar ratio) and they were prepared with a pH gradient to improve the gemcitabine loading capacity. The anti-tumoral efficacy of the liposomal formulation was tested in vitro on human anaplastic thyroid carcinoma cells (ARO) in culture, comparing the effects with those of the free drug. Gemcitabine-loaded unilamellar liposomes had a mean size ∼200 nm with a zeta potential ∼–2mV. The liposomal carrier noticeably improved the anti-tumoral activity of gemcitabine against ARO cells in terms of both dose-dependent cytotoxic effect and of drug exposition effect. Namely, gemcitabine-loaded liposomes showed a cytotoxic effect (58.2% increase of cell mortality at 1 μM with respect to free drug) after 12 h incubation, while the free drug showed a significant activity only after 72 h incubation. Moreover, a significant effect on the cell mortality appeared at 0.1 μM and 100% mortality was detected at a concentration of 1 μM of gemcitabine-loaded liposomes, while the free drug elicited the same effect at a concentration of 100 μM. The improved anti-tumoral activity of gemcitabine determined by the liposomal carrier was due to a greater intracellular uptake. The intracellular gemcitabine levels as a function of time showed a sinusoidal profile with peaks after 2 h, 6 h and 11 h, related to the cellular cycle of ARO. PARP cleavage and DNA fragmentation analysis provided clear evidence of the apoptosis induction in ARO cells by treatment with liposomally entrapped gemcitabine after 72 h incubation. Thus, gemcitabine-loaded liposomes may have a potential therapeutic relevance for the treatment of anaplastic thyroid carcinoma.

scholarly journals Report on a New Opioid NPS: Chemical and In Vitro Functional Characterization of a Structural Isomer of the MT-45 Derivative Diphenpipenol

2020 ◽  
Author(s):  
Annelies Cannaert ◽  
Fabian Hulpia ◽  
Martijn Risseeuw ◽  
Katleen Van Uytfanghe ◽  
Eric Deconinck ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Liquid Chromatography ◽  
Functional Characterization ◽  
Gas Chromatography Mass Spectrometry ◽  
Structural Isomer ◽  
New Psychoactive Substances ◽  
Array Detector ◽  
Exact Mass

Abstract In this paper, the identification and full characterization of a novel non-fentanyl opioid sourced online, which is a member of the 1-substituted-4-(1,2-diphenylethyl)piperazine derivatives related to MT-45, is reported. The sample was sold under the name “diphenpipenol,” (3-[2-[4-(2-methoxyphenyl)piperazin-1-yl]-2-phenylethyl]phenol), although extensive NMR analysis showed that the product obtained was actually a diphenpipenol structural isomer, (2-[4-(2-methoxyphenyl)piperazin-1-yl]-1,2-diphenylethanol). Liquid chromatography time-of-flight mass spectrometry identified an exact mass for the protonated molecule of m/z 389.2264, with two prominent fragment ions (m/z 91.0567 and 150.0937), which were not reported in earlier literature describing MT-45 derivatives. The chemical characterization was finalized by gas chromatography–mass spectrometry, high-performance liquid chromatography diode array detector and Fourier-transform infrared spectroscopy analyses. This product is a clear example of the trend that new non-fentanyl opioids are reappearing on the recreational drug market to escape the recent changes in (inter)national legislation concerning fentanyl analogues. Although in this particular case, the product’s potency and efficacy were relatively low, other new non-fentanyl opioids might possess stronger potencies and therefore pose greater health risks for ignorant users. The fact that the product was sold under the wrong name further demonstrates the well-known problematic issue of a mismatch between the adverted and true identity, confirming the irregularities of the online new psychoactive substances market.

scholarly journals Reveal Cytotoxicity and Antigenotoxicity of Piper nigrum L. Ethanolic Extract and its Combination with Doxorubicin on CHO-K1 Cells

2018 ◽  
Vol 8 (3) ◽  
pp. 110
Author(s):  
Nur Fitra Sari ◽  
Beni Lestari ◽  
Dian Saputri ◽  
Anisa Fauzia Ahsani ◽  
Ragil Anang Santoso ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Topoisomerase Ii ◽  
Micronucleus Test ◽  
Morphological Changes ◽  
Ethanolic Extract ◽  
Black Pepper ◽  
Piper Nigrum ◽  
Therapeutic Effects ◽  
Dna Topoisomerase

Black pepper (Piper nigrum L.), one of the most popular Indonesian spices has been reported to possess various therapeutic effects. The aim of this study is to evaluate the cytotoxicity and antigenotoxicity of black pepper ethanolic extract (BPE) and its combination with doxorubicin (Dox) on CHO-K1 cells. Based on thin layer chromatographyanalysis, BPE contained piperine.Under MTT assay, BPE showed cytotoxic effect with the IC50 value of 68 μg/mL and performed synergism in combination with Dox. In vitro micronucleus test using Giemsa staining revealed that BPE did not cause morphological changes qualitatively on CHO-K1 cells at concentration of 8.5 μg/mL, whereas using flow cytometry analysis showed that BPE could decrease the number of micronucleus (MN) formation induced by doxorubicin. In addition, BPE reduced the ROS level on the CHO-K1 cells which observed by reactive oxygen species (ROS) intracellular assay. The decrease in ROS level indicated that the antioxidant activity of BPE contribute to the antigenotoxicity. Furthermore, molecular docking performed that piperine interacted with DNA Topoisomerase II with docking score of -80.68. Overall,BPE performed cytotoxic effect in single treatment, increased the cytotoxicity and reduced the genotoxicity of doxorubicin. Thus, BPE has potential to be developed further as co-chemotherapeutic and antigenotoxic agent.Keywords: Cytotoxic, genotoxic, Piper nigrum L., CHO-K1, micronucleus

scholarly journals In-vitro screening of antihelmintic and antibacterial activity of malvastrum coromandelianum leaves

2021 ◽  
pp. 4-7
Author(s):  
Tirupathi Rao Annavarapu ◽  
Pragna Malavika B ◽  
Aravinda Swami P
Keyword(s):  
Antibacterial Activity ◽  
Anthelmintic Activity ◽  
Ethanolic Extract ◽  
The Other ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Zone Of Inhibition ◽  
Gram Negative ◽  
Malvastrum Coromandelianum

The main objective of the work is to investigate the antithelmintic and antibacterial activity of the Malvastrumcoromandelianum leaves. The extract was tested for antithelmintic activity against adult Indian earthworm and also tested for antibacterial activity against the gram positive bacteriaS.aureus,B.subtilis and gram negative bacteria against E.Coli, P.aerugenosa, P.putida.The anthelmintic activity was observed at 100mg/ml with reference to standardAlbendazole(10mg/ml).The maximum antibacterial activity was observed in S.aureus at 500mg/ml with of zone of inhibition17 mm and next is S.aureus, the best antibacterial activity was observed against P.aerugenosa and P.putidawith 15 mm of zone of inhibition. The zone of inhibition of extract was compared with standard Gentamycin 25 µg/ml. The extract shows significant activity against the other bacterial pathogens. From the results, it was concluded that the ethanolic extract of Malvastrumcoromandelianum leaves have anthelmintic and antibacterial activity.

scholarly journals Antiviral, Antioxidant, and Antihemolytic Effect of Annona muricata L. Leaves Extracts

Plants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1650
Author(s):  
Ana Paola Balderrama-Carmona ◽  
Norma Patricia Silva-Beltrán ◽  
Juan-Carlos Gálvez-Ruiz ◽  
Saúl Ruíz-Cruz ◽  
Cristóbal Chaidez-Quiroz ◽  
...  
Keyword(s):  
Viral Infections ◽  
Ethanolic Extract ◽  
Ultra Performance Liquid Chromatography ◽  
Human Erythrocytes ◽  
Tropical Tree ◽  
Protective Effects ◽  
Annona Muricata ◽  
Leaf Extracts ◽  
Trolox Equivalent

Annona muricata L. is a tropical tree that is used in traditional medicine around the world. The high content of flavonoid, alkaloid, acetogenin, phenolic and lipophilic compounds of this tropical tree forms the basis of its traditional medical uses. Our objective was to study soursop leaf extracts to support their use as antiviral therapies and investigate their protective effects against oxidative damage. The aqueous extract (AE) and acidified ethanolic extract (AEE) of soursop leaves were characterized by ultra performance liquid chromatography (UPLC), and their effects on human erythrocytes and in vitro antioxidant capacity, as evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays, were investigated. The antiviral effects were evaluated using a bacteriophage surrogate. AEE showed the highest phenolic content, with rutin as the predominant compound. This extract showed higher values in the DPPH and ABTS assays, with 23.61 ± 0.42 and 24.91 ± 0.16 mmol of Trolox equivalent per gram, respectively. Inhibition of hemolysis was 34% and 51% for AE and AEE, respectively. AEE was selected for the antiviral study because of its higher antioxidant activity. The viral reduction ranged from 5–6 log10 plaque-forming units/volume (PFU) at contact times of 15–360 min. Soursop leaves have a positive effect on reducing oxidative stress in human erythrocytes and viral infections.

scholarly journals Leishmanicidal activity of Artemisinin against cutaneous Leishmaniasis, in Vitro

2019 ◽  
Vol 13 (1) ◽  
pp. 16-22
Author(s):  
Guffran M. Hassan ◽  
Hayder Z. Ali
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Cytotoxic Effect ◽  
Leishmania Tropica ◽  
Herbal Drug ◽  
Undesirable Side Effect ◽  
Leishmanicidal Activity ◽  
Herbal Compound

Background: Cutaneous leishmaniasis (CL) is a neglected disease in tropical countries, including Iraq. Several studies have sought to examine chemotherapies for leishmaniasis treatment but most of them are of toxic and/or undesirable side effect, therefore, the need for investigating new fewer toxic therapies is essential. Aim of study: In this study, the cytotoxic effect of Artemisinin (ART), a novel herbal compound, was screened against the two forms, promastigotes and amastigotes, of the Iraqi isolate of Leishmania tropica, the causative agent of Baghdad boil. Material and methods:  Different concentrations (1000, 500, 250, 125, 62.5, 31.25, 15.6 and 7.8) µM of Artemisinin were screened to investigate the leishmanicidal activity of the herbal compound against the two forms of the parasite along three times of follow up (24, 48, 72) hour using MTT cytotoxicity assay. Results: The results showed that growth rate and cell viability were significantly decreased at all studied concentrations. The IC50 was measured after 72 hours of follow up and was 2.625 µM and 2.636 µM for promastigotes and amastigotes, respectively. Conclusion: These findings approved the leishmanicidal efficacy of Artemisinin against the of L. tropica and can be further studied to screen its effectiveness in vivo for exploring a safer herbal drug for treatment of cutaneous leishmaniasis.  

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