scholarly journals In Vitro Testing of Alternative Synthetic and Natural Antiparasitic Compounds against the Monogenean Sparicotyle chrysophrii

Pathogens ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 980
Author(s):  
Ivona Mladineo ◽  
Željka Trumbić ◽  
Adrián Ormad-García ◽  
Oswaldo Palenzuela ◽  
Ariadna Sitjà-Bobadilla ◽  
...  
Keyword(s):  
Seawater Temperature ◽  
Natural Compounds ◽  
Gilthead Seabream ◽  
Fish Parasite ◽  
High Potency ◽  
Synthetic Compound ◽  
Synthetic Drugs ◽  
Induce Resistance ◽  
Temperature Application

Gill monogenean Sparicotyle chrysophrii is considered the most detrimental fish parasite to the Mediterranean aquaculture. Treatment of sparicotylosis relies on frequent gill inspections correlated with the seasonal increase in seawater temperature, application of functional feeds, and treatments with formalin baths where permitted. While the latter is bound to be banned in Europe, other synthetic anthelminthics, such as praziquantel and ivermectin, are prone to induce resistance in the parasites. Therefore, we investigated, in vitro, 14 synthetic and natural compounds against adult S. chrysophrii, developing dose–response modelsm and estimated toxicity levels at 20%, 50%, and 80% parasite mortality. Bactericidal activity of target compounds was also tested in two important aquaculture bacteria; Vibrio harveyi and V. anguillarum, while their potential host toxicity was evaluated in gilthead seabream SAF-1 cell line. Synthetic compound bithionate sodium exerted the most potent toxicity against the monogenean, no host cytotoxicity, and a medium and high potency against two bacterial pathogens. In comparison, target natural compounds were approximately 20 (cedrol) or up to 154 times (camphor) less toxic for the monogenean. Rather than completely dismissing natural compounds, we suggest that their application in combination with synthetic drugs, especially if administered in the feed, might be useful in sparicotylosis treatment.

In Vitro Activity of Phytocannabinoids from High Potency Cannabis sativa

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
A Husni ◽  
S Ross ◽  
O Dale ◽  
C Gemelli ◽  
G Ma ◽  
...  
Keyword(s):  
Cannabis Sativa ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
High Potency

Synthetic and semi-synthetic drugs as promising therapeutic option for the treatment of COVID-19

2020 ◽  
Vol 20 ◽  
Author(s):  
Ekta Shirbhate ◽  
Preeti Patel ◽  
Vijay K Patel ◽  
Ravichandran Veerasamy ◽  
Prabodh C Sharma ◽  
...  
Keyword(s):  
Therapeutic Option ◽  
Antiviral Treatment ◽  
The Novel ◽  
Clinical Experiences ◽  
Synthetic Compounds ◽  
Synthetic Drugs ◽  
Global Pandemic ◽  
The World ◽  
Novel Coronavirus

: The novel coronavirus disease-19 (COVID-19), a global pandemic that emerged from Wuhan, China has today travelled all around the world, so far 216 countries or territories with 21,732,472 people infected and 770,866 deaths globally (as per WHO COVID-19 update dated August 18, 2020). Continuous efforts are being made to repurpose the existing drugs and develop vaccines for combating this infection. Despite, to date, no certified antiviral treatment or vaccine prevails. Although, few candidates have displayed their efficacy in in vitro studies and are being repurposed for COVID-19 treatment. This article summarizes synthetic and semi-synthetic compounds displaying potent activity in their clinical experiences or studies against COVID-19 and also focuses on mode of action of drugs being repositioned against COVID-19.

scholarly journals Natural Compounds Isolated from Stachybotrys chartarum Are Potent Inhibitors of Human Protein Kinase CK2

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4453
Author(s):  
Samer Haidar ◽  
Franziska M. Jürgens ◽  
Dagmar Aichele ◽  
Annika Jagels ◽  
Hans-Ulrich Humpf ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Natural Compounds ◽  
Breast Adenocarcinoma ◽  
Stachybotrys Chartarum ◽  
Mcf7 Cells ◽  
A431 Cells ◽  
Ic50 Values ◽  
Human Lung Carcinoma ◽  
Kinase Ck2

A large number of secondary metabolites have been isolated from the filamentous fungus Stachybotrys chartarum and have been described before. Fourteen of these natural compounds were evaluated in vitro in the present study for their inhibitory activity towards the cancer target CK2. Among these compounds, stachybotrychromene C, stachybotrydial acetate and acetoxystachybotrydial acetate turned out to be potent inhibitors with IC50 values of 0.32 µM, 0.69 µM and 1.86 µM, respectively. The effects of these three compounds on cell proliferation, growth and viability of MCF7 cells, representing human breast adenocarcinoma as well as A427 (human lung carcinoma) and A431 (human epidermoid carcinoma) cells, were tested using EdU assay, IncuCyte® live-cell imaging and MTT assay. The most active compound in inhibiting MCF7 cell proliferation was acetoxystachybotrydial acetate with an EC50 value of 0.39 µM. In addition, acetoxystachybotrydial acetate turned out to inhibit the growth of all three cell lines completely at a concentration of 1 µM. In contrast, cell viability was impaired only moderately, to 37%, 14% and 23% in MCF7, A427 and A431 cells, respectively.

scholarly journals Functionalized Nanoplastics (NPs) Increase the Toxicity of Metals in Fish Cell Lines

2021 ◽  
Vol 22 (13) ◽  
pp. 7141
Author(s):  
Carmen González-Fernández ◽  
Francisco Guillermo Díaz Baños ◽  
María Ángeles Esteban ◽  
Alberto Cuesta
Keyword(s):  
Sparus Aurata ◽  
Gilthead Seabream ◽  
Fish Cell ◽  
Test Model ◽  
Fish Cell Lines ◽  
Polystyrene Nanoparticles ◽  
Commercial Fish ◽  
Cellular Protection ◽  
Marine Life

Nanoplastics (NPs) are one of the most abundant environment-threatening nanomaterials on the market. The objective of this study was to determine in vitro if functionalized NPs are cytotoxic by themselves or increase the toxicity of metals. For that, we used 50 nm polystyrene nanoparticles with distinct surface functionalization (pristine, PS-Plain; carboxylic, PS-COOH; and amino PS-NH2) alone or combined with the metals arsenic (As) and methylmercury (MeHg), which possess an environmental risk to marine life. As test model, we chose a brain-derived cell line (SaB-1) from gilthead seabream (Sparus aurata), one of the most commercial fish species in the Mediterranean. First, only the PS-NH2 NPs were toxic to SaB-1 cells. NPs seem to be internalized into the cells but they showed little alteration in the transcription of genes related to oxidative stress (nrf2, cat, gr, gsta), cellular protection against metals (mta) or apoptosis (bcl2, bax). However, NPs, mainly PS-COOH and PS-NH2, significantly increased the toxicity of both metals. Since the coexistence of NPs and other pollutants in the aquatic environment is inevitable, our results reveal that the combined effect of NPs with the rest of pollutants deserves more attention.

scholarly journals The Effects of Bergamot Polyphenolic Fraction, Cynara cardunculus, and Olea europea L. Extract on Doxorubicin-Induced Cardiotoxicity

Nutrients ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 2158
Author(s):  
Jessica Maiuolo ◽  
Irene Bava ◽  
Cristina Carresi ◽  
Micaela Gliozzi ◽  
Vincenzo Musolino ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Apoptotic Cell ◽  
Natural Compounds ◽  
Cynara Cardunculus ◽  
Unfolded Protein ◽  
Wide Range ◽  
Vitro Model ◽  
The Unfolded Protein Response ◽  
Protein Response

Doxorubicin is an anthracycline that is commonly used as a chemotherapy drug due to its cytotoxic effects. The clinical use of doxorubicin is limited due to its known cardiotoxic effects. Treatment with anthracyclines causes heart failure in 15–17% of patients, resulting in mitochondrial dysfunction, the accumulation of reactive oxygen species, intracellular calcium dysregulation, the deterioration of the cardiomyocyte structure, and apoptotic cell death. Polyphenols have a wide range of beneficial properties, and particular importance is given to Bergamot Polyphenolic Fraction; Oleuropein, one of the main polyphenolic compounds of olive oil; and Cynara cardunculus extract. These natural compounds have particular beneficial characteristics, owing to their high polyphenol contents. Among these, their antioxidant and antoproliferative properties are the most important. The aim of this paper was to investigate the effects of these three plant derivatives using an in vitro model of cardiotoxicity induced by the treatment of rat embryonic cardiomyoblasts (H9c2) with doxorubicin. The biological mechanisms involved and the crosstalk existing between the mitochondria and the endoplasmic reticulum were examined. Bergamot Polyphenolic Fraction, Oleuropein, and Cynara cardunculus extract were able to decrease the damage induced by exposure to doxorubicin. In particular, these natural compounds were found to reduce cell mortality and oxidative damage, increase the lipid content, and decrease the concentration of calcium ions that escaped from the endoplasmic reticulum. In addition, the direct involvement of this cellular organelle was demonstrated by silencing the ATF6 arm of the Unfolded Protein Response, which was activated after treatment with doxorubicin.

Design and Synthesis of Lipophilic Phosphoramidate d4T-MP Prodrugs Expressing High Potency Against HIV in Cell Culture:  Structural Determinants for in Vitro Activity and QSAR

1999 ◽  
Vol 42 (20) ◽  
pp. 4122-4128 ◽  
Author(s):  
Adam Q. Siddiqui ◽  
Christopher McGuigan ◽  
Carlo Ballatore ◽  
Fabio Zuccotto ◽  
Ian H. Gilbert ◽  
...  
Keyword(s):  
Cell Culture ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
High Potency ◽  
Structural Determinants ◽  
Design And Synthesis

scholarly journals UJI AKTIVITAS EKSTRAK BUAS-BUAS (PREMNA SERRATIFOLIA LINN) SEBAGAI ANTI KOLESTEROL SECARA IN VITRO

2017 ◽  
Vol 5 (1) ◽  
Author(s):  
Dini Hadiarti
Keyword(s):  
Solvent Extraction ◽  
Side Effects ◽  
Herbal Medicine ◽  
Cholesterol Concentration ◽  
Standard Curve ◽  
Synthetic Drugs ◽  
Standard Solution ◽  
The Cost

ABSTRACTPremna Serratifolia Linn is believed to reduce cholesterol and as an alternative herbal medicine solution among the cost of medicine and the side effects caused by synthetic drugs. This study was conducted in several phases by using Premna Serratifolia Linn which was drained, mashed, and macerated using ethanol, choloform, and n-heksane. Extract obtained from evaporation, then whighed, and stored in a desiccators. Anti-cholesterol activity was tested test by using in vitro : began with determination of the maximum wavelength of the cholesterol standard solution with a UV-Vis spectrophotometer and continued by manufacturing the standard curve with the cholesterol concentration of 0.5; 0.75; 1; 1.25; and 1.5 mL and 1000 ppm cholesterol solution. Furthermore, maximum absorbance wavelength was measured in order to obtain the maximum wavelength of the cholesterol. The study reveled that the solvent extraction of ethanol produced the largest  rendement. The extract Premna Serratifolia Linn is functioned as an anti-cholesterol. In addition,  the absorbed reduction of 100 ppm cholesterol standard solution found in the addition of 0.5 mL choloform extract.Keywords: Anti-cholesterol, Premna Serratifolia Linn, In Vitro

scholarly journals Computational Analysis for Physicochemical Properties of Compounds in Senna auriculata Leaves Methanolic Extract to have Antidiabetic Potentials and their Molecular Interaction with α-amylase

2021 ◽  
pp. 30-42
Author(s):  
Abdulaziz Bin Dukhyil
Keyword(s):  
Molecular Docking ◽  
Physicochemical Properties ◽  
Methanolic Extract ◽  
Natural Compounds ◽  
Physicochemical Analysis ◽  
Dynamics Simulation ◽  
Carbohydrate Hydrolysis ◽  
Catalytic Active Site ◽  
Inhibitory Potential

Aims: Diabetes mellitus (DM) is chronic disorder well known for increased glucose level in blood. This disease can be controlled by inhibiting the enzyme (e.g., α-amylase) involve in carbohydrate hydrolysis. Senna auriculata leaves methanolic extract (SALME) have potential antidiabetic properties and it was also found to be safe in preclinical studies. In this study the aim was to explore the molecular interactions of α-amylase and bioactive compounds in SALME and their physicochemical properties. Methodology: Computational approach such as molecular docking and physicochemical analysis prediction was applied to understand the antidiabetic potential of natural compounds present in SALME. Results: The results showed from physicochemical analysis that out of 11 only 7 compounds are having drug like properties which are orally and intestinally better bioavailable. Furthermore, molecular docking analysis explained that three compounds (C3, C4, and C7) have lower binding energy, ΔG (-8, -9.1, -9.5 kcal/mol) and better binding affinity, Ki (7.31 x 105, 4.68 x 106, and 9.2 x 106 M-1, respectively) than the acarbose ΔG (-7.8 kcal/mol) and Ki (6.18 x 105 M-1), a well-known FDA approved medication for DM. The study also explained the binding pattern that the catalytic residue such as Asp197, Glu233 and Asp300 are involved in stabilizing the natural compounds with in the catalytic active site of target enzyme. Conclusions: From the results it has been concluded that these three compounds found in SALME have better inhibitory potential for α-amylase in comparison with acarbose. Further validation of the findings is required through molecular dynamics simulation, ADME-T study, and in-vitro enzyme inhibition by the purified compounds.

scholarly journals In Vitro Anti-Diabetic Activities and UHPLC-ESI-MS/MS Profile of Muntingia calabura Leaves Extract

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 287
Author(s):  
Nur Khaleeda Zulaikha Zolkeflee ◽  
Nurul Shazini Ramli ◽  
Azrina Azlan ◽  
Faridah Abas
Keyword(s):  
Published Data ◽  
Drying Methods ◽  
Esi Ms ◽  
Synthetic Drugs ◽  
Ic50 Values ◽  
Phytochemical Profile ◽  
Ultrahigh Performance Liquid Chromatography ◽  
Diabetic Treatment ◽  
Muntingia Calabura

Anti-diabetic compounds from natural sources are now being preferred to prevent or treat diabetes due to adverse effects of synthetic drugs. The decoction of Muntingia calabura leaves was traditionally consumed for diabetes treatment. However, there has not been any published data currently available on the processing effects on this plant’s biological activity and phytochemical profile. Therefore, this study aims to evaluate the effect of three drying methods (freeze-drying (FD), air-drying (AD), and oven-drying (OD)) and ethanol:water ratios (0, 50, and 100%) on in vitro anti-diabetic activities of M. calabura leaves. In addition, an ultrahigh-performance-liquid chromatography–electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) method was used to characterize the metabolites in the active extract. The FD M. calabura leaves, extracted with 50% ethanol, is the most active extract that exhibits a high α-glucosidase and α-amylase inhibitory activities with IC50 values of 0.46 ± 0.05 and 26.39 ± 3.93 µg/mL, respectively. Sixty-one compounds were tentatively identified by using UHPLC-ESI-MS/MS from the most active extract. Quantitative analysis, by using UHPLC, revealed that geniposide, daidzein, quercitrin, 6-hydroxyflavanone, kaempferol, and formononetin were predominant compounds identified from the active extract. The results have laid down preliminary steps toward developing M. calabura leaves extract as a potential source of bioactive compounds for diabetic treatment.

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