scholarly journals Compounds from the Medicines for Malaria Venture Box Inhibit In Vitro Growth of Babesia divergens, a Blood-Borne Parasite of Veterinary and Zoonotic Importance

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7118
Author(s):  
Mohamed Abdo Rizk ◽  
Shimaa Abd El-Salam El-Sayed ◽  
Mahmoud S. Alkhoudary ◽  
Khalaf F. Alsharif ◽  
Mohamed M. Abdel-Daim ◽  
...  
Keyword(s):  
Structural Similarity ◽  
Inhibitory Effect ◽  
In Vitro Growth ◽  
High Concentration ◽  
Diminazene Aceturate ◽  
Babesia Divergens ◽  
Ic50 Value ◽  
Imidocarb Dipropionate ◽  
Drug Pipeline

Babesiosis is an infectious disease with an empty drug pipeline. A search inside chemical libraries for novel potent antibabesial candidates may help fill such an empty drug pipeline. A total of 400 compounds (200 drug-like and 200 probe-like) from the Malaria Box were evaluated in the current study against the in vitro growth of Babesia divergens (B. divergens), a parasite of veterinary and zoonotic importance. Novel and more effective anti-B. divergens drugs than the traditionally used ones were identified. Seven compounds (four drug-like and three probe-like) revealed a highly inhibitory effect against the in vitro growth of B. divergens, with IC50s ≤ 10 nanomolar. Among these hits, MMV006913 exhibited an IC50 value of 1 nM IC50 and the highest selectivity index of 32,000. The atom pair fingerprint (APfp) analysis revealed that MMV006913 and MMV019124 showed maximum structural similarity (MSS) with atovaquone and diminazene aceturate (DA), and with DA and imidocarb dipropionate (ID), respectively. MMV665807 and MMV665850 showed MMS with each other and with ID. Of note, a high concentration (0.75 IC50) of MMV006913 caused additive inhibition of B. divergens growth when combined with DA at 0.75 or 0.50 IC50. The Medicines for Malaria Venture box is a treasure trove of anti-B. divergens candidates according to the obtained results.

scholarly journals Potential Effect of Pomegranate Peels Extract (Punica Granatum.) against Covid-19 Virus .

2021 ◽  
Author(s):  
Ashraf fawzy mosa ◽  
Mostafa abo Elhoda Mohamed
Keyword(s):  
Tissue Culture ◽  
Water Extract ◽  
Punica Granatum ◽  
Inhibitory Effect ◽  
Potential Effect ◽  
Laboratory Methods ◽  
Global Epidemic ◽  
Ic50 Value ◽  
The World

Abstract Background: Covid-19 Virus infection poses significant global health challenges and considered a global epidemic sweeping all countries of the world Which prompted scientists around the world to search for a quick or safe treatment to preserve people's lives .So far, options for controlling and treating the disease have not been revealed. The current study was conducted to evaluate the effectiveness of pomegranate peels extract against the Covid-19 virus in the laboratory. Methods: In this research, tow methods of extraction are carried out ethyl alcohol and distal water extract of pomegranate peels . activity of the extract assessed using 50% Tissue Culture Infectious Doses (TCID50) method in Vero E6 cells. Results: Pomegranate peels extract had the highest inhibitory effect against Covid -19 virus with IC50 value of 0.125, 0.0625 and 0.031256 μl in Vero E6 cells. Conclusion: Based on our results, the aqueous extract of pomegranate peels can inhibit Covid-19 virus replication in vitro.

Inhibitory Effect Of High Concentration Of Oxygen On LPS-Induced Inflammation In Vivo And In Vitro

2011 ◽  
Author(s):  
MUNEHIRO YAMAGUCHI ◽  
AKIHIKO TANAKA ◽  
SHIN OHTA ◽  
TAKUYA YOKOE ◽  
YOSHITAKA YAMAMOTO ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
High Concentration

scholarly journals Screening and Application of Chitin Synthase Inhibitors

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1029
Author(s):  
Xiaozai Shi ◽  
Shuo Qiu ◽  
Yingling Bao ◽  
Hanchi Chen ◽  
Yuele Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Chitin Synthase ◽  
Fungal Cell ◽  
Ic50 Value ◽  
Further Development ◽  
Fungicide Target ◽  
Better Than

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

INHIBITORY EFFECT OF LACTOFERRIN ON IN VITRO GROWTH OF BABESIA CABALLI

2005 ◽  
Vol 73 (4) ◽  
pp. 710-712 ◽  
Author(s):  
HIROMI IKADAI ◽  
TETSUYA TANAKA ◽  
IKUO IGARASHI ◽  
TAKASHI OYAMADA ◽  
AYA MATSUU ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
In Vitro Growth ◽  
Babesia Caballi

scholarly journals The Inhibitory Effect ofPrunella vulgarisL. on Aldose Reductase and Protein Glycation

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Hong Mei Li ◽  
Jin Kyu Kim ◽  
Jai Man Jang ◽  
Sang Oh Kwon ◽  
Cheng Bi Cui ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Inhibitory Effect ◽  
Protein Glycation ◽  
Prunella Vulgaris ◽  
Inhibitory Effects ◽  
Advanced Glycation ◽  
High Concentration ◽  
Potent Inhibition ◽  
Glycation End Products

To evaluate the aldose reductase (AR) enzyme inhibitory ability ofPrunella vulgarisL. extract, six compounds were isolated and tested for their effects. The components were subjected toin vitrobioassays to investigate their inhibitory assays using rat lens aldose reductase (rAR) and human recombinant AR (rhAR). Among them, caffeic acid ethylene ester showed the potent inhibition, with the IC50values of rAR and rhAR at3.2±0.55 μM and12.58±0.32 μM, respectively. In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, this compound showed noncompetitive inhibition against rhAR. Furthermore, it inhibited galactitol formation in a rat lens incubated with a high concentration of galactose. Also it has antioxidative as well as advanced glycation end products (AGEs) inhibitory effects. As a result, this compound could be offered as a leading compound for further study as a new natural products drug for diabetic complications.

Babesia divergens (Phylum Apicomplexa) in vitro growth in the presence of calf serum

2004 ◽  
Vol 122 (2) ◽  
pp. 127-130 ◽  
Author(s):  
A Zintl ◽  
H.E Skerrett ◽  
J.S Gray ◽  
P.O Brophy ◽  
G Mulcahy
Keyword(s):  
Calf Serum ◽  
In Vitro Growth ◽  
Babesia Divergens

scholarly journals Tyrosinase Inhibitory Effect, Antioxidant and Anticancer Activities of Bioactive Compounds in Ripe Hog Plum (Spondias Pinnata) Fruit Extracts

2019 ◽  
Vol 35 (3) ◽  
pp. 916-926
Author(s):  
Supawadee Patathananone ◽  
Jureerut Daduang ◽  
Amonrat Koraneekij ◽  
Chia-Ying Li
Keyword(s):  
High Performance ◽  
Antioxidant Property ◽  
Inhibitory Effect ◽  
Tyrosinase Activity ◽  
Normal Fibroblast ◽  
Anticancer Activities ◽  
Ic50 Value ◽  
Bioactive Agents ◽  
Hog Plum

The usage of ripe hog plum fruit (Spondias pinnata) extracts in cosmetics and food products, including cancer therapeutic agents, have a few studies. Herein, the strong anti-tyrosinase activity found in the extracted part of isopropanol is reported. This extract was separated by liquid/liquid extraction using hexane: methanol+H2O. The hydrophilic layer (6A*) exhibited the anti-tyrosinase, antioxidant, and anticancer activities in vitro. The IC50 value of each bioactivity was presented as approximately 0.18, 0.04, and 1.40 mg/ml, respectively. In addition, 6A* fraction showed a very low cytotoxic effect in normal fibroblast cells (NHDF cells). The bioactive agents in 6A* were purified by C18 reverse-phase High-Performance Liquid Column Chromatography (HPLC). The 12 purified peaks were shown in the chromatogram profile. All peaks (excepted 6A-06 and 6A-09) displayed anti-tyrosinase activity, whereas the antioxidant property was not found in 6A-01, 6A-06, and 6A-08 but was represented in other peaks. Most purified peaks were indicated to be the aromatic alcohol or derivative phenol compounds.

scholarly journals Effects of Methanolic Extract from Turmeric (Curcuma longa) against the In Vitro Multiplication of Several Babesia Species and Theileria equi

Parasitologia ◽  
2021 ◽  
Vol 1 (4) ◽  
pp. 188-196
Author(s):  
Mohamed Abdo Rizk ◽  
Shimaa Abd El-Salam El-Sayed ◽  
Ikuo Igarashi
Keyword(s):  
Methanolic Extract ◽  
Curcuma Longa ◽  
In Vitro Growth ◽  
Theileria Equi ◽  
Diminazene Aceturate ◽  
Novel Drugs ◽  
Ic50 Values ◽  
Fluorescence Test ◽  
Novel Strategy

Anti-piroplasm drugs currently on the market have proven toxicity to the host and parasite resistance. Plants are possible sources of novel drugs. Subsequently, a novel strategy should be used to find new anti-piroplasm agents that are both effective and safe. In the present study, we have evaluated the effect of turmeric (Curcuma longa) methanolic extract on the in vitro growth of Babesia (B.) bovis, B. divergens, B. caballi, and Theileria (T.) equi. The in vitro inhibitory effectiveness of turmeric was assessed using a fluorescence test. The enhancement in the in vitro inhibitory efficacy of turmeric when administrated in combination with diminazene aceturate (DA) was investigated using in vitro cultures of different piroplasm parasites. Turmeric reduced the in vitro growth of B. bovis, B. divergens, T. equi, and B. caballi with IC50 values of 0.830 0.078, 0.375 0.055, 1.405 0.575, and 0.720 0.090 mg/mL, respectively. An amount of 1 mg/mL turmeric for B. bovis, 0.5 mg/mL turmeric for B. divergens, 1 mg/mL turmeric for T. equi, and 0.5 mg/mL turmeric for B. caballi exhibited 73.43%, 80.065%, 73.47%, and 47.375% inhibitions in the growth of the parasites, respectively. When turmeric was combined with DA, its in vitro inhibitory impact on bovine Babesia and equine Babesia/Theileria parasites was amplified. These findings show that a methanolic extract of turmeric could be a promising medicinal plant for the treatment of babesiosis, especially when administered in conjunction with DA.

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