scholarly journals IN VITRO ANTIPLASMODIAL AND CYTOTOXIC ACTIVITIES OF A SUNGKAI (PERONEMA CANESCENS) LEAF EXTRACT

2018 ◽  
Vol 10 (10) ◽  
pp. 109
Author(s):  
Jhons Fatriyadi Suwandi ◽  
Mahardika Agus Wijayanti ◽  
Mustofa .
Keyword(s):  
Plasmodium Falciparum ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Selectivity Index ◽  
Antiplasmodial Activity ◽  
Cytotoxic Activities ◽  
Aqueous Extracts ◽  
Diphenyltetrazolium Bromide ◽  
Ic50 Values

Objective: The aim of this study was to assess the antiplasmodial and cytotoxic activities and to evaluate the selectivity indices of acetone, ethanol and aqueous extracts of Peronema canescens leaves.Methods: Antiplasmodial activity was measured in vitro against Plasmodium falciparum strains D10 and FCR3 by 72 h incubation at 37 °C in a candle jar. Parasitaemia was calculated by counting the parasite numbers in thin smears. In vitro cytotoxicity was assayed in Vero cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and reading the absorbency at 595 nm with an ELISA reader. The assessed parameters included: 50% inhibitory concentration (IC50) of antiplasmodial activity, IC50 of cytotoxic activity and the selectivity index of the Peronema canescens leaf extract.Results: The IC50 values for the acetone, ethanol and aqueous extracts were 26.33±1.65, 37.96±8.17 and 12.26±1.05 μg/ml, respectively, against the Plasmodium falciparum D10 strain and 51.14±8.65, 70.22±14.13 and 34.85±6.04 μg/ml, respectively, against the FCR3 strain. For Vero cells, the IC50 values for the acetone, ethanol and aqueous extracts were 23.37±5.63, 629.46±24.85 and 634.00±144.82 μg/ml, respectively. The selectivity indices of these extracts were 0.89, 16.46 and 51.70, respectively, for the D10 strain and 0.46, 8.90 and 18.00, respectively, for the FCR3 strain.Conclusion: The aqueous extract of Peronema canescens leaves had the highest in vitro antiplasmodial activity and the best selectivity index.

scholarly journals In Vitro Antiplasmodial, Heme Polymerization, and Cytotoxicity of Hydroxyxanthone Derivatives

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Mistika Zakiah ◽  
Rul Afiyah Syarif ◽  
Mustofa Mustofa ◽  
Jumina Jumina ◽  
Nela Fatmasari ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
High Selectivity ◽  
In Vitro Cytotoxicity ◽  
Selectivity Index ◽  
Antiplasmodial Activity ◽  
Assay Method ◽  
Hydroxyl Groups ◽  
Inhibition Activity ◽  
Ic50 Values

The previous study showed that xanthone had antiplasmodial activity. Xanthone, with additional hydroxyl groups, was synthesized to increase its antiplasmodial activity. One of the strategies to evaluate a compound that can be developed into an antimalarial drug is by testing its mechanism in inhibiting heme polymerization. In acidic condition, hematin can be polymerized to β-hematin in vitro, which is analog with hemozoin in Plasmodium. This study was conducted to evaluate the antiplasmodial activity of hydroxyxanthone derivative compounds on two strains of Plasmodium falciparum 3D-7 and FCR-3, to assess inhibition of heme polymerization activity and determine the selectivity of hydroxyxanthone derivative compounds. The antiplasmodial activity of each compound was tested on Plasmodium falciparum 3D-7 and FCR-3 with 72 hours incubation period, triplicated in three replications with the microscopic method. The compound that showed the best antiplasmodial activity underwent flow cytometry assay. Heme polymerization inhibition test was performed using the in vitro heme polymerization inhibition activity (HPIA) assay. The antiplasmodial activity and heme polymerization inhibition activity were expressed as the 50% inhibitory concentration (IC50). In vitro cytotoxicity was tested using the MTT assay method on Vero cell lines to determine its selectivity index. The results showed that among 5-hydroxyxanthone derivative compounds, the 1,6,8-trihydroxyxanthone had the best in vitro antiplasmodial activity on both 3D-7 and FCR-3 Plasmodium falciparum strains with IC50 values of 6.10 ± 2.01 and 6.76 ± 2.38 μM, respectively. The 1,6,8-trihydroxyxanthone showed inhibition activity of heme polymerization with IC50 value of 2.854 mM and showed the high selectivity with selectivity index of 502.2–556.54. In conclusion, among 5-hydroxyxanthone derivatives tested, the 1,6,8-trihydroxyxantone showed the best antiplasmodial activity and has heme polymerization inhibition activity and high selectivity.

scholarly journals New Antiproliferative Triflavanone from Thymelaea hirsuta—Isolation, Structure Elucidation and Molecular Docking Studies

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 739
Author(s):  
Sameh S. Elhady ◽  
Reda F. A. Abdelhameed ◽  
Mayada M. El-Ayouty ◽  
Amany K. Ibrahim ◽  
Eman S. Habib ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Liver Tumors ◽  
Fold Increase ◽  
In Vitro Cytotoxicity ◽  
Mitogen Activated Protein Kinase ◽  
Wild Plant ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
Thymelaea Hirsuta

In this study isolates from Thymelaea hirsuta, a wild plant from the Sinai Peninsula of Egypt, were identified and their selective cytotoxicity levels were evaluated. Phytochemical examination of the ethyl acetate (EtOAc) fraction of the methanolic (MeOH) extract of the plant led to the isolation of a new triflavanone compound (1), in addition to the isolation of nine previously reported compounds. These included five dicoumarinyl ethers found in Thymelaea: daphnoretin methyl ether (2), rutamontine (3), neodaphnoretin (4), acetyldaphnoretin (5), and edgeworthin (6); two flavonoids: genkwanin (7) and trans-tiliroside (8); p-hydroxy benzoic acid (9) and β sitosterol glucoside (10). Eight of the isolated compounds were tested for in vitro cytotoxicity against Vero and HepG2 cell lines using a sulforhodamine-B (SRB) assay. Compounds 1, 2 and 5 exhibited remarkable cytotoxic activities against HepG2 cells, with IC50 values of 8.6, 12.3 and 9.4 μM, respectively, yet these compounds exhibited non-toxic activities against the Vero cells. Additionally, compound 1 further exhibited promising cytotoxic activity against both MCF-7 and HCT-116 cells, with IC50 values of 4.26 and 9.6 μM, respectively. Compound 1 significantly stimulated apoptotic breast cancer cell death, resulting in a 14.97-fold increase and arresting 40.57% of the cell population at the Pre-G1 stage of the cell cycle. Finally, its apoptosis-inducing activity was further validated through activation of BAX and caspase-9, and inhibition of BCL2 levels. In silico molecular docking experiments revealed a good binding mode profile of the isolates towards Ras activation/pathway mitogen-activated protein kinase (Ras/MAPK); a common molecular pathway in the development and progression of liver tumors.

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽  
2018 ◽  
Vol 84 (17) ◽  
pp. 1292-1299 ◽  
Author(s):  
Guo-Chun Yang ◽  
Jia-Hui Hu ◽  
Bing-Long Li ◽  
Huan Liu ◽  
Jia-Yue Wang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

scholarly journals Antiplasmodial and Cytotoxic Activities of Extracts of Selected Medicinal Plants Used to Treat Malaria in Embu County, Kenya

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Bibianne Waiganjo ◽  
Gervason Moriasi ◽  
Jared Onyancha ◽  
Nelson Elias ◽  
Francis Muregi
Keyword(s):  
Side Effects ◽  
Medicinal Plants ◽  
Stem Bark ◽  
Antiplasmodial Activity ◽  
Chloroquine Resistance ◽  
Cytotoxic Activities ◽  
Aqueous Extracts ◽  
Methanolic Extracts

Malaria is a deadly disease caused by a protozoan parasite whose mode of transmission is through a female Anopheles mosquito. It affects persons of all ages; however, pregnant mothers, young children, and the elderly suffer the most due to their dwindled immune state. The currently prescribed antimalarial drugs have been associated with adverse side effects ranging from intolerance to toxicity. Furthermore, the costs associated with conventional approach of managing malaria are arguably high especially for persons living in low-income countries, hence the need for alternative and complementary approaches. Medicinal plants offer a viable alternative because of their few associated side effects, are arguably cheaper, and are easily accessible. Based on the fact that studies involving antimalarial medicinal plants as potential sources of efficacious and cost-effective pharmacotherapies are far between, this research was designed to investigate antiplasmodial and cytotoxic activities of organic and aqueous extracts of selected plants used by Embu traditional medicine practitioners to treat malaria. The studied plants included Erythrina abyssinica (stem bark), Schkuhria pinnata (whole plant), Sterculia africana (stem bark), Terminalia brownii (leaves), Zanthoxylum chalybeum (leaves), Leonotis mollissima (leaves), Carissa edulis (leaves), Tithonia diversifolia (leaves and flowers), and Senna didymobotrya (leaves and pods). In vitro antiplasmodial activity studies of organic and water extracts were carried out against chloroquine-sensitive (D6) and chloroquine-resistance (W2) strains of Plasmodium falciparum. In vivo antiplasmodial studies were done by Peter’s four-day suppression test to test for their in vivo antimalarial activity against P. berghei. Finally, cytotoxic effects and safety of the studied plant extracts were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) rapid calorimetric assay technique. The water and methanolic extracts of T. brownii and S. africana and dichloromethane extracts of E. abyssinica, S. pinnata, and T. diversifolia leaves revealed high in vitro antiplasmodial activities (IC50≤10 μg/ml). Further, moderate in vivo antimalarial activities were observed for water and methanolic extracts of L. mollissima and S. africana and for dichloromethane extracts of E. abyssinica and T. diversifolia leaves. In this study, aqueous extracts of T. brownii and S. africana demonstrated high antiplasmodial activity and high selectivity indices values (SI≥10) and were found to be safe. It was concluded that T. brownii and S. africana aqueous extracts were potent antiplasmodial agents. Further focused studies geared towards isolation of active constituents and determination of in vivo toxicities to ascertain their safety are warranted.

In vitro antiplasmodial activity of aqueous extracts of Ochna schweinfurthiana leaf on Plasmodium falciparum

2018 ◽  
Vol 14 (2) ◽  
pp. 269
Author(s):  
Babasoji P. Omoniwa ◽  
Titilayo O. Johnson ◽  
Omolola Soji-Omoniwa ◽  
Istifanus Gurumtet ◽  
Ruth A. Manzah
Keyword(s):  
Plasmodium Falciparum ◽  
Antiplasmodial Activity ◽  
Aqueous Extracts

scholarly journals Plasmodium falciparum: In Vitro Cytotoxicity Testing Using MTT

1998 ◽  
Vol 3 (1) ◽  
pp. 49-53 ◽  
Author(s):  
J. Enrico Lazaro ◽  
Frederick Gay
Keyword(s):  
Plasmodium Falciparum ◽  
Culture System ◽  
Inhibitory Concentration ◽  
In Vitro Cytotoxicity ◽  
Mtt Method ◽  
Diphenyltetrazolium Bromide ◽  
Wide Range ◽  
In Vitro Culture System ◽  
Comparative Results

The microculture tetrazolium assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) was used to estimate the 50% inhibitory concentration of chloroquine, quinine, artemisinin, and atovaquone using a Plasmodium falciparum in vitro culture system. The MTT assay was compared to the standard tritiated hypoxan-thine assay and to a previously described method, the 2,2′-di-p-nitrophenyl-5,5′-diphenyl-3,3′-[3,3′-dimethoxy-4,4′-diphenylenel-ditetrazolium chloride (NBT) assay. In general, the results show that the three assays generate comparative results. The results of this study suggest that the MTT method is able to give a profile of cytotoxic dose response effects over a wide range of concentrations of a drug. The method may be used in work that does not require extreme pre-cision and sensitivity, for instance, as a portable rapid screen to assay natural products for in vitro cytotoxic ac-tivity against Plasmodium falciparum.

scholarly journals Antiplasmodial activity of Anthocleista djalonensis leaves extracts against clinical isolates of Plasmodium falciparum and multidrug resistant K1 strains

2020 ◽  
Vol 8 (3) ◽  
pp. 130-138
Author(s):  
Brice Kouakou Bla ◽  
Oléfongo Dagnogo ◽  
Rolland Gueyraud Kipré ◽  
Opportune Gogo Ballé ◽  
Jonhson David Trébissou ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Multidrug Resistant ◽  
Traditional Healers ◽  
Antiplasmodial Activity ◽  
Clinical Isolates ◽  
Aqueous Extracts ◽  
Phytochemical Screening ◽  
Primary Health ◽  
Ethanolic Extracts

Information collected from nine (09) traditional healers in the Moronou village in the Department of Toumodi revealed that Anthocleista djanlonensis is regularly used by the population for primary health care in the processing of malaria. Evaluation of the In vitro antiplasmodial activity showed that the aqueous extracts inhibit growth of clinical isolates and chloroquinoresistant strains (K1) with IC50 of 8.29 µg/mL and 10.23 µg/mL while the ethanolic extracts had IC50 of 37.65 µg/mL and 46.07 µg/mL on the same strains respectively. Results of the In vitro antimalarial bioassay showed that aqueous extracts have promising antiplasmodial effects on clinical isolates and on Plasmodium falciparum multidrug resistant K1 strain (3 µg/mL <IC50 <15 µg/mL). Phytochemical screening revealed that the extracts contain mainly alkaloids, polyphenols, polyterpenes and flavonoids

scholarly journals In Vitro Cytotoxicity of Aspilia Pluriseta Schweinf. Extract Fractions

2020 ◽  
Author(s):  
Sospeter Ngoci Njeru ◽  
Jackson Mbithi Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extracts ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives: We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on A. pluriseta cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemicals characterization of A. pluriseta root extracts, here we report the missing data on cytotoxicity of tested extracts. We evaluated the potential cytotoxicity of the root extracts on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results: We show that all solvent extracts (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) of greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivity are within the acceptable cytotoxicity and selective index limits. This scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

scholarly journals In Vitro Activity of Pentamidine Isethionate against Trophozoite and Cyst of Acanthamoeba

2021 ◽  
Author(s):  
Massoud Behnia ◽  
Alireza Latifi ◽  
Mostafa Rezaian ◽  
Sharmin Kharazi ◽  
Mehdi Mohebali ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Vero Cells ◽  
Acanthamoeba Keratitis ◽  
Inhibitory Effect ◽  
Blue Staining ◽  
Medical Sciences ◽  
Diphenyltetrazolium Bromide ◽  
Pentamidine Isethionate ◽  
Ic50 Values

Background: Acanthamoebae are a causative agent of Acanthamoeba keratitis (AK) in immunocompetent individuals. Since access to propamidine isethionate (Brolene®) as a first-line treatment has been limited in recent years, in the current study, we examined the effects of pentamidine isethionate against trophozoite and cyst forms of Acanthamoeba. Methods: This experimental study was conducted in the Department of Medical Parasitology and Mycology, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran, during 2019-2020. Pentamidine isethionate at concentrations of 50, 100, 200, 400, 600, 800, and 1000 µM were tested against trophozoites and cyst stages of T4 genotype, at 24- and 48-hour incubation period, and the viability was determined by trypan blue staining. In addition, the cytotoxic effect of the drug was examined in Vero cells using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Results: The 50% inhibitory concentration (IC50) of pentamidine isethionate on trophozoite after 24 and 48h were 97.4 µM and 60.99 µM. These results on cyst after 24 and 48h were 470 µM and 175.5 µM, respectively. In MTT assay, the drug showed an inhibitory effect on Vero cell growth with IC50 values of 115.4 µM and 87.42 µM after 24h and 48h, respectively. Conclusion: Pentamidine isethionate exhibited an inhibitory effect on trophozoite and cyst. Given that the trophozoicidal activity of the drug is in the safe dose, it could be suggested as an alternative in patients with AK; however, further investigation is needed in an animal model to confirm the data.

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