scholarly journals Effect of Zinc(II)-2,4,5-triphenyl-1H-imidazole Complex Against Replication DENV-2 in Vero Cell

2020 ◽  
Vol 8 (3) ◽  
pp. 183
Author(s):  
Teguh Hari Sucipto ◽  
Aswandi Wibrianto ◽  
Fahimah Martak ◽  
Siti Churrotin ◽  
Ilham Harlan Amarullah ◽  
...  
Keyword(s):  
Dengue Virus ◽  
Vero Cell ◽  
Complex Compound ◽  
Inhibitory Activity ◽  
Vero Cells ◽  
Inhibitory Effect ◽  
Complex Compounds ◽  
Antiviral Compound ◽  
First Time

Dengue virus (DENV) is a significant pathogen emerging worldwide as a cause of infectious disease. DENVs are transmitted to humans through female mosquitoes from Aedes aegypti and Aedes albopictus species. Indonesia is one of the largest countries in the world in dengue endemic regions worldwide. Dengue fever was occurred for the first time as an outbreak in Surabaya and Jakarta in 1968. Many efforts have been made to prevent and treat DENV infections, and clinical trials of a number of vaccines are currently underway. Antiviral testing of DENV is an important alternative for drug characterization and development. Complex compounds are formed as a result of metal and organic complex reactions. Complex compounds can be used as an anti-inflammatory, antimicrobial antifungal, antibacterial, antivirus. The Zn2+ ion can be used as an antiviral candidate. The purpose of this project was investigated Zinc(II)-2,4,5-triphenyl-1H-imidazole antiviral compound to be further tested for inhibitory effect on the replication of DENV-2 in cell culture. DENV replication was measured by antiviral activity assay and cytotoxicity assay. The inhibitory activity of Zinc(II)-2,4,5-triphenyl-1H-imidazole complex compound was determined by Viral ToxGloTM Assay. The cytotoxicity of Zinc(II)-2,4,5-triphenyl-1H-imidazole complex compound was determined by CellTiter96® AQuoeus assay. The inhibitory concentration (IC50) of Zinc(II)-2,4,5-triphenyl- 1H-imidazole against dengue virus type-2 was 34.42 μg/ml. The cytotoxic concentration (CC50) of compound against Vero cell was <100 μg/ml. The results of this study demonstrate the antidengue serotype 2 inhibitory activity of investigated Zinc(II)-2,4,5-triphenyl-1H-imidazole complex and its high toxicity in Vero cells. Further studies are not required before investigated Zinc(II)-2,4,5-triphenylimidazole can be applied in the treatment of DENV-2 infections

scholarly journals ANTI-DENGUE TYPE 2 VIRUS ACTIVITIES OF ZINC (II) COMPLEX COMPOUNDS WITH 2-(2,4 -DIHYDROXYPHENYL)-3,5,7-TRIHYDROXYCROMEN-4-ONE LIGANDS IN VERO CELLS

2019 ◽  
Vol 7 (5) ◽  
pp. 105 ◽  
Author(s):  
Teguh Hari Sucipto ◽  
Harsasi Setyawati ◽  
Siti Churrotin ◽  
Ilham Harlan Amarullah ◽  
Sri Sumarsih ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Virus Type ◽  
Complex Compound ◽  
Vero Cells ◽  
Complex Compounds ◽  
Dengue Type 2 Virus ◽  
Dengue Virus Type 2 ◽  
Metal Ligand

Dengue virus (DENV) is a disease that is transmitted through Aedes aegypti and Aedes albopictus mosquitoes, and is spread in tropical and sub-tropical regions. Now, dengue or antiviral vaccines for humans do not yet exist, but there are great efforts to achieve this goal. Complex compounds are reported to fungicidal, bactericidal and antiviral activity. Antiviral activity against DENV is an important alternative to the characterization and development of drugs candidate. The purpose of this study was to study zinc(II) compounds with 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxycromen-4-one ligand on DENV-2 replication in Vero cells. Vero cell lines (African green monkey kidney) was used in this study, maintained and propagated in Minimum Essential Eagle Medium containing 10% fetal bovine serum at 37°C in 5% CO2. The activity of dengue virus was carried out by enzyme-immunosorbent assay (ELISA) method and CellTiter96® Non-Radioactive Proliferation. The value of activity inhibition (IC50) of complex compounds with variations of mol metal: ligand 1:2, 1:3, and 1:4 against dengue virus type 2 (DENV2) was 2.44 μg/ml, 2.75 μg/ml, respectively and 2.00 μg/ml, also the toxicity value (CC50) of complex compounds with variation mol metal: ligand 1:4 for Vero cells is 3.59 μg/ml. The results of this study were indicate that these properties have been shown to inhibit anti-dengue type 2 virus (DENV-2), but are also toxic in Vero cells. Including previous study about complex compound interaction with dengue virus type 2 activity, Zn(II) more reactive compound then Cu(II), and Co(II). The comparison with Cu(II) complex compound, it has been revealed that Co(II) and Zn(II) is more toxic, was found to be nontoxic to human erythrocyte cells even at a concentration of 500 μg/ml.

scholarly journals Inhibition of dengue virus serotype 2 in Vero cells with [Cu(2,4,5-triphenyl-1H-imidazole)2(H2O)2].Cl2

2020 ◽  
Author(s):  
Teguh H. Sucipto ◽  
Fahimah Martak
Keyword(s):  
Dengue Virus ◽  
Inhibitory Concentration ◽  
Platinum Complexes ◽  
Hemorrhagic Fever ◽  
Fold Increase ◽  
Vero Cells ◽  
Inhibitory Effect ◽  
Selectivity Index ◽  
Antiviral Compound ◽  
Virus Serotype

Dengue fever and dengue hemorrhagic fever are transmitted to humans by the Aedes aegypti and Aedes albopictus mosquitoes, with an observed 30-fold increase in global incidence the last 50 years. Despite the tremendous efforts invested anti-dengue virus research, no clinically approved vaccine or antiviral chemotherapeutics are available for humans, and disease treatment is limited to supportive care. Over the years there has been a continuous interest in the chemistry of metal complexes with biological activity, including platinum complexes with antitumor activity and silver complexes with antimicrobial action. Aim of the project was to investigate [Cu(2,4,5-triphenyl-1H- imidazole)2 (H2O)2].Cl2 as antiviral compound that was further tested for inhibitory effect on the replication of dengue virus type 2 (DENV-2) in Vero cell. DENV-2 were infected in Vero cells and replication of virus was measured by Viral ToxGlo with selectivity index value (SI) and determined as the ratio of cytotoxic concentration 50 (CC50) to inhibitory concentration 50 (IC50) for com- pound. The standard curve between concentration of compound (μg/mL) and %viability of cells was analyzed by logarithmic cor- relation regression with regression equation. For infection rates, t-test was used to exam- ine the statistical significances among the concentrations of compound. P<0.05 was considered to be significant. The maximum inhibitory concentration (IC50) of [Cu(2,4,5- triphenyl-1H-imidazole)2 (H2O)2].Cl2 against DENV-2 was 98.62 μg/mL. The cytotoxic concentration (CC50) of compound against Vero cells was 300.36μg/mL. The SI values for [Cu(2,4,5-triphenyl-1H-imidazole)2 (H2O)2].Cl2 1.86. Based on selectivity index values, [Cu(2,4,5-triphenyl-1H-imidazole)2 (H2O)2].Cl2 can inhibit the growth of DENV- 2 and has low toxicity values for Vero cells.

scholarly journals INHIBITORY ACTIVITY OF COBALT(II)–MORIN COMPLEX AGAINST THE REPLICATION OF DENGUE VIRUS TYPE 2

2017 ◽  
Vol 6 (6) ◽  
pp. 141
Author(s):  
Teguh Hari Sucipto ◽  
Siti Churrotin ◽  
Harsasi Setyawati Setyawati ◽  
Kris Cahyo Mulyatno ◽  
Ilham Harlan Amarullah ◽  
...  
Keyword(s):  
Dengue Virus ◽  
Inhibitory Activity ◽  
Vero Cells ◽  
Inhibitory Effect ◽  
Enzyme Linked Immunosorbent Assay ◽  
High Concentration ◽  
Cell Monolayers ◽  
Metal Organic ◽  
Tropical Areas ◽  
Antiviral Activities

Dengue virus (DENV) is a significant pathogen emerging worldwide as a cause of infectious disease. Antidengue treatments are urgently required to control the emergence of dengue. DENV is a mosquito-borne disease responsible for acute systemic diseases and serious health conditions. DENVs were distributed in the tropical and sub-tropical areas and transmitted to humans by Aedes agypty and Aedes albopictus. Dengue vaccine or antiviral has not yet been clinically approved for humans, even though there have been great efforts toward this end. Antiviral activity against DENV is an important alternative for the characterization and development of drugs. Metal–organic compounds were reported to exhibit fungicidal, bactericidal, and antiviral activities its inhibitory activity was not significant, at high concentration it was more toxic to replicating cells than to stationary cell monolayers of Vero cells. The aim of this study is to investigate the antiviral effects of Cobalt(II)–Morin complex. This compound was further investigated for its inhibitory effect on the replication of DENV-2 in Vero cells. The replication of DENV was measured by enzyme-linked immunosorbent assay and the value of selectivity index (SI). SI was determined as the ratio of the 50% cytotoxic concentration (CC50) to the 50% inhibitory concentration (IC50). The IC50 value of the Cobalt(II)–Morin complex for DENV-2 was 3.08 µg/ml, and the CC50 value of the complex for Vero cells was 3.36 µg/ml; thus, the SI value was 1.09. The results of this study demonstrate the antidengue serotype 2 inhibitory activity of Cobalt(II)–Morin complex and its high toxicity in Vero cells. Further studies are not required before Co(II)–Morin can be applied in the treatment of DENV-2 infections.

scholarly journals ANTIVIRAL ACTIVITY OF COPPER(II)CHLORIDE DIHYDRATE AGAINST DENGUE VIRUS TYPE-2 IN VERO CELL

2017 ◽  
Vol 6 (4) ◽  
pp. 84 ◽  
Author(s):  
Teguh Hari Sucipto ◽  
Siti Churrotin ◽  
Harsasi Setyawati ◽  
Tomohiro Kotaki ◽  
Fahimah Martak ◽  
...  
Keyword(s):  
Cell Culture ◽  
Dengue Virus ◽  
Vero Cell ◽  
Virus Type ◽  
Inhibitory Concentration ◽  
Enzyme Linked Immunosorbent Assay ◽  
Antiviral Compound ◽  
Chloride Dihydrate ◽  
Dengue Virus Type 2

Infection of dengue virus (DENV) was number of globally significant emerging pathogen. Antiviral dengue therapies ar importantly needed to control emerging dengue. Dengue virus (DENV) is mosquito-borne arboviruses responsible for causing acute systemic diseases and grievous health conditions in humans. To date, there is no clinically approved dengue vaccine or antiviral for humans, even though there have been great efforts towards this end. Copper and copper compounds have more effective in inactivation viruses, likes an influenza virus and human immunodeficiency virus (HIV). Purpose in this project was investigated of Copper(II)chloride Dihydrate antiviral compound were further tested for inhibitory effect on the replication of DENV-2 in cell culture. DENV replication was measures by Enzyme linked Immunosorbent Assay (ELISA) with selectivity index value (SI) was determined as the ratio of cytotoxic concentration 50 (CC50) to inhibitory concentration 50 (IC50) for compound. The maximal inhibitory concentration (IC50) of Copper(II)chloride Dihydrate against dengue virus type-2 was 0.13 μg/ml. The cytotoxic concentration (CC50) of compound against Vero cell was 5.03 μg/ml. The SI values for Copper(II)chloride Dihydrate 38.69. Result of this study suggest that Copper(II)chloride Dihydrate demonstated significant anti-DENV-2 inhibitory activities and not toxic in the Vero cells. Copper mechanisms play an important role in the prevention of copper toxicity, exposure to excessive levels of copper can result in a number of adverse health effects, as a result increased reactive oxygen species and oxidative damage to lipid, DNA, and proteins have been observed in human cell culture models or clinical syndromes of severe copper deficiency and inhibition was attributed to released cupric ions which react with cysteine residues on the surface of the protease.

scholarly journals Inhibitory Effects of Secondary Metabolites from the Lichen Stereocaulon evolutum on Protein Tyrosine Phosphatase 1B

Planta Medica ◽  
2021 ◽  
Author(s):  
Birgit Waltenberger ◽  
Françoise Lohézic-Le Dévéhat ◽  
Thi Huyen Vu ◽  
Olivier Delalande ◽  
Claudia Lalli ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Tyrosine Phosphatase ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Values ◽  
A Cell

AbstractProtein tyrosine phosphatase 1B plays a significant role in type 2 diabetes mellitus and other diseases and is therefore considered a new drug target. Within this study, an acetone extract from the lichen Stereocaulon evolutum was identified to possess strong protein tyrosine phosphatase 1B inhibition in a cell-free assay (IC50 of 11.8 µg/mL). Fractionation of this bioactive extract led to the isolation of seven known molecules belonging to the depsidones and the related diphenylethers and one new natural product, i.e., 3-butyl-3,7-dihydroxy-5-methoxy-1(3H)-isobenzofurane. The isolated compounds were evaluated for their inhibition of protein tyrosine phosphatase 1B. Two depsidones, lobaric acid and norlobaric acid, and the diphenylether anhydrosakisacaulon A potently inhibited protein tyrosine phosphatase 1B with IC50 values of 12.9, 15.1, and 16.1 µM, respectively, which is in the range of the protein tyrosine phosphatase 1B inhibitory activity of the positive control ursolic acid (IC50 of 14.4 µM). Molecular simulations performed on the eight compounds showed that i) a contact between the molecule and the four main regions of the protein is required for inhibitory activity, ii) the relative rigidity of the depsidones lobaric acid and norlobaric acid and the reactivity related to hydrogen bond donors or acceptors, which interact with protein tyrosine phosphatase 1B key amino acids, are involved in the bioactivity on protein tyrosine phosphatase 1B, iii) the cycle opening observed for diphenylethers decreased the inhibition, except for anhydrosakisacaulon A where its double bond on C-8 offsets this loss of activity, iv) the function present at C-8 is a determinant for the inhibitory effect on protein tyrosine phosphatase 1B, and v) the more hydrogen bonds with Arg221 there are, the more anchorage is favored.

In Vitro Antiviral Activity of Pinus merkusii (Pinaceae) Stem Bark and Cone against Dengue Virus Type-2 (DENV-2)

2021 ◽  
pp. 3705-3708
Author(s):  
Arif Nur Muhammad Ansori ◽  
Amaq Fadholly ◽  
Annise Proboningrat ◽  
Suhailah Hayaza ◽  
Raden Joko Kuncoroningrat Susilo ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Virus Type ◽  
Stem Bark ◽  
Endemic Region ◽  
In Vivo Evaluation ◽  
African Green Monkey Kidney ◽  
Antiviral Compound ◽  
Dengue Virus Type 2

Dengue is a major mosquito-borne disease that currently has no effective antiviral or vaccine available. Recently, Indonesia is one of the largest countries in the dengue-endemic region, with a total population of more than 250 million. In the present study, the antiviral activity of P. merkusii stem bark and cone were evaluated against dengue virus type-2 (DENV-2; NCBI accession number: KT012509) isolated from Surabaya, Indonesia. We revealed that P. merkusii stem bark and cone inhibited DENV-2 in Vero cells (originally from African green monkey kidney) with IC50= 140.63 μg/mL and 73.78 μg/mL, CC50= 89.65 μg/mL and 249.5 μg/mL, SI= 0.64 and 3.38, respectively. The findings presented here suggest that P. merkusii stem bark and cone exerts potent antiviral activity against DENV-2. Hence, P. merkusii stem bark and cone are potent to inhibit DENV-2 and should be considered for in vivo evaluation in the development of an effective antiviral compound against DENV-2.

scholarly journals Natural vertical transmission by Stegomyia albopicta as dengue vector in Brazil

2009 ◽  
Vol 69 (1) ◽  
pp. 123-127 ◽  
Author(s):  
AB. Cecílio ◽  
ES. Campanelli ◽  
KPR. Souza ◽  
LB. Figueiredo ◽  
MC. Resende
Keyword(s):  
Dengue Virus ◽  
Vertical Transmission ◽  
Dengue Vector ◽  
Infection Rates ◽  
Dengue Viruses ◽  
Stegomyia Albopicta ◽  
First Time ◽  
Minimum Infection Rate ◽  
Dengue Virus Type 2

The mosquito Stegomyia albopicta is among the most important arbovirus vectors in the world, particularly for Dengue viruses. Their natural history suggests that biologically these viruses are highly adapted to their mosquito hosts and they were most likely mosquito viruses prior to becoming adapted to lower primates and humans. As well as being maintained by transmission among susceptible humans, Dengue viruses may also be maintained by vertical transmission in mosquitoes during inter-epidemic periods. The larvae and mosquitoes of Stegomyia albopicta were used to identify the vertical transmission of the dengue virus in nature and to confirm the vectorial capacity concerning the Dengue virus type 2 infection. The minimum infection rate concerning S. albopicta infection with the Dengue virus was 1:36.45. In Brazil this was the first time that high minimum infection rates of vertical transmission of S. albopicta were detected in this species.

scholarly journals Flavonoids from Milletia leucantha and Their Cytotoxicity

2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300
Author(s):  
Uraiwan Sriphana ◽  
Chavi Yenjai ◽  
Siriporn Tungnoi ◽  
Jongjai Srirapa ◽  
Auemporn Junsongduang
Keyword(s):  
Cytotoxic Activity ◽  
Vero Cell ◽  
Cell Line ◽  
Vero Cells ◽  
2D Nmr ◽  
Nmr Techniques ◽  
Vero Cell Lines ◽  
First Time ◽  
Flavonol Derivatives ◽  
Mcf 7

Two known chalcones (1–2), five known flavonol derivatives (3 and 5–8) and one flavone (4) were isolated for the first time from fruits of Millettia leucantha Kurz. In addition, 5 was found for the first time from this genus. Their structures were elucidated on the basis of IR, MS, 1D and 2D NMR techniques. Chalcone 1 exhibited moderate cytotoxicity against the MCF-7 cell line with an IC50 value of 50.93 μM, whereas this compound showed inactive cytotoxicity against Vero cells. Compound 2 exhibited cytotoxicity against the KB, NCI-H187 and Vero cell lines with IC50 values of 63.64, 114.44 and 28.44 μM, respectively. Compound 8 only showed cytotoxic activity against the KB cell line with an IC50 value of 110.23 μM.

scholarly journals Zinc accelerates dengue virus type 2-induced apoptosis in Vero cells

FEBS Letters ◽  
2002 ◽  
Vol 524 (1-3) ◽  
pp. 20-24 ◽  
Author(s):  
Norazizah Shafee ◽  
Sazaly AbuBakar
Keyword(s):  
Dengue Virus ◽  
Virus Type ◽  
Vero Cells ◽  
Induced Apoptosis ◽  
Dengue Virus Type 2

scholarly journals Chemical Composition andα-Glucosidase Inhibitory Activity of VietnameseCitrusPeels Essential Oils

2016 ◽  
Vol 2016 ◽  
pp. 1-5 ◽  
Author(s):  
Nguyen Hai Dang ◽  
Pham Huong Nhung ◽  
Bui Thi Mai Anh ◽  
Dinh Thi Thu Thuy ◽  
Chau Van Minh ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Potential Use

Background. Inhibition ofα-glucosidase is an important factor to control postprandial hyperglycemia in type 2 diabetes mellitus.Citrusessential oils (CEO) are among the most widely used essential oils, and some of them exhibited promising antidiabetic effect. However, theα-glucosidase inhibition of CEO has not been investigated so far. The present work aims to evaluate theα-glucosidase inhibition of essential oils from six VietnameseCitruspeels.Methods. The chemical composition of essential oils obtained by hydrodistillation from sixCitruspeels was analyzed by GC-MS. All essential oils were tested for their inhibitory activity onα-glucosidase usingp-nitrophenyl-α-D-glucopyranoside as substrate.Results. In Buddha’s hand and lime peels, the major components were limonene (59.0–61.31%) andγ-terpinene (13.98–23.84%) while limonene (90.95–95.74%) was most abundant in pomelo, orange, tangerine, and calamondin peels. Among the essential oils, the Buddha’s hand oil showed the most significantα-glucosidase inhibitory effect with the IC50value of 412.2 μg/mL. The combination of the Buddha’s hand essential oil and the antidiabetic drug acarbose increased the inhibitory effect.Conclusions. The results suggested the potential use of Buddha’s hand essential oil as an alternative in treatment of type 2 diabetes mellitus.

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