scholarly journals IN VITRO ANTIPLASMODIAL ACTIVITY OF FLOWER EXTRACTS FROM COMBRETUM LEPROSUM MART (MOFUMBO)

2016 ◽  
Vol 39 (1) ◽  
pp. 84 ◽  
Author(s):  
Guilherme Matos Passarini ◽  
Daniel Sol Medeiros ◽  
Dionatas Ulisses de Oliveira Meneguetti ◽  
Renato Abreu Lima ◽  
Valdir Alves Facundo ◽  
...  
Keyword(s):  
At Risk ◽  
Silica Gel ◽  
Column Chromatography ◽  
Chloroform Extract ◽  
Antiplasmodial Activity ◽  
Pharmacological Studies ◽  
Combretum Leprosum ◽  
Resistant Strains ◽  
Active Substances

Malaria is the cause of hundreds of deaths per year , besides putting billions of people at risk of developing disease. When it comes to its therapy, the drugs used currently are losing its efficacy due to increase inn the frequency of resistant strains of the parasite, highlight the importance for the serach of new classes of molecules prsentign antiplasmodial activity. In the present work, the antiplasmodial activities of five extracts from the flowers of Comretum leprosum are described. The method employed for obtaingine the extracts was silica gel column chromatography, and the techniques used for the analysis of antiplasmodial activity and citotoxicity were ELISA and MTT respectively, were a selectivitu index was calculated after the obtainign of these two values. The extract presenting the highest antiplasmodial activity was the chloroform extract, however, this extrac also presented the higther cytotoxicity and therefore the extract presenting the best overall activity was the hexane extract. The study deminstrated the plant Combretum leprosum has active substances against P. falciparum and therefore is a potential to be expored in funther pharmacological studies.

Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro

2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas da Silva Santos ◽  
Matheus Fillipe Langanke de Carvalho ◽  
Ana Claudia de Souza Pinto ◽  
Amanda Luisa da Fonseca ◽  
Julio César Dias Lopes ◽  
...  
Keyword(s):  
Triazole Ring ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
The World ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Active Substances

Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the urge for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4- dihydroisocoumarin. Method: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively.

In vitro 19-norandrogen synthesis by equine placenta requires the participation of aromatase

1995 ◽  
Vol 144 (3) ◽  
pp. 517-525 ◽  
Author(s):  
S Moslemi ◽  
P Silberzahn ◽  
J-L Gaillard
Keyword(s):  
Silica Gel ◽  
Aromatase Inhibitors ◽  
Column Chromatography ◽  
Microsomal Fraction ◽  
Specific Activity ◽  
Reverse Phase Hplc ◽  
Reverse Phase ◽  
Term Placenta ◽  
Flow Detector

Abstract Explants of equine full-term placenta have been shown to synthesize 19-norandrogens from labelled androgens. Steroid metabolites were purified by silica-gel column chromatography then analysed and quantified by C18-reverse-phase HPLC coupled to a radioactive flow detector. 19-Norandrostenedione was subsequently recrystallized to constant specific activity, providing unequivocal evidence of its synthesis by the equine placenta. 19-Norandrostenedione synthesis appeared to be localized in the microsomal fraction. Regardless of the substrate used, formation of 19-norandrogens was far weaker than that of oestrogens; moreover, the yield of 17-oxosteroids produced was much greater than that of 17β-hydroxysteroids, suggesting the presence of a dehydrogenase with predominant oxidative activity. Sulphoconjugated steroids formed were less than 0·5% of total steroids. Although 19-nortestosterone could not be generated by equine purified aromatase incubated with labelled testosterone, the synthesis of 19-norandrogens and oestrogens by equine placental explants was blocked by two specific aromatase inhibitors, 4-hydroxyandrostenedione and fadrozole. Our results provide evidence for a placental origin of at least a part of the 19-norandrogens previously identified in the blood of the pregnant mare. Furthermore, it is suggested that 19-norandrogen biosynthesis would involve the enzymatic metabolism of 19-oxygenated androgens formed by equine aromatase. Journal of Endocrinology (1995) 144, 517–525

scholarly journals Isolation and Structure Elucidation of Soulatro Coumarin From Stem Bark of Calophyllum soulattri Burm F and In Vivo Antiplasmodial Activity by Using Mice Infected by Plasmodium berghei

2011 ◽  
Vol 2 (2) ◽  
pp. 242
Author(s):  
Jamilah Abbas ◽  
Achmad Darmawan ◽  
Syafruddin Syafruddin
Keyword(s):  
Ethyl Acetate ◽  
Silica Gel ◽  
Column Chromatography ◽  
Plasmodium Berghei ◽  
2D Nmr ◽  
Stem Bark ◽  
Antiplasmodial Activity ◽  
Nmr Techniques ◽  
Coumarin Compound

The soulatro coumarin compound was isolated and elucidated from the stem bark of Calophyllum soulattri Burm F, the samples were collected from Jayapura Papua Irian Island in Indonesia. Isolation process was done by maceration at room temperature in methanol, than partitioned in a mixture of n hexane-water (1:1), followed by dichloromethane-water (1:1)  and ethyl acetate-water (1:1). A portion of ethyl acetate extract was subjected to column chromatography over silica gel packed and eluted with n-hexane a gradient of ethyl acetate to 100% followed by CHCl3  in MeOH (20:1, 10 :1, 5:1, 1:1). Fraction  B (CHCl3 in MeOH 20:1) was subjected to column chromatography  over silica gel 300 mesh  and eluted with EtOAc-MeOH mixtures of increasing polarity. Faction with the same Rf valeus were combined and eluted with EtOAc-MeOH  (19:1) showed one spot on TLC. They were combined and evaporated to yield a solid than was recrystallized in mixture of CH2Cl2-methanol to give soulatro coumarin compound. The structure was determinated by spectroscopic analysis, in particular by 1D and 2D NMR techniques, from these spectra data conclution that compound is soulatro coumarin. Antimalarial assay was tested against Plasmodium berghei parasite as in vivo using 18 mices rodent wich was infected by  Plasmodium berghei parasite. The soulatro coumarin  showed activity against P. berghei with dosage 0.0005867 mM/1 kg body weight ; 0.005867 mM/1 kg bw; 0.05867 mM/1 kg bw; 0.5867 mM/1 kg bw 5.867 mM/1 kg bw and 58.67 mM/1 kg bw could inhibite growth rate of parasite = 57.32%; 63.37%; 43.02%; 53.49%; 47.67% respectively.Keywords : Antiplasmodial activity, coumarin, Calophyllum soulattri Burm. F, in vivo, Chloroquine, Plasmodium berghei.

scholarly journals Antiplasmodial activity against resistant strains, toxicity and effect on mouse liver enzymes of extracts of Terminalia species found in Southwest Cameroon

2020 ◽  
Vol 10 (1) ◽  
pp. 132-138
Author(s):  
Moses Njutain Ngemenya ◽  
Grace Ntube Abwenzoh ◽  
Denis Zofou ◽  
Thierry Roland Kang ◽  
James Ajeck Mbah
Keyword(s):  
High Selectivity ◽  
Liver Enzymes ◽  
Antiplasmodial Activity ◽  
Leaf Extracts ◽  
Growth Inhibition Assay ◽  
Traditional Treatment ◽  
Methanol Extracts ◽  
Resistant Strains ◽  
Further Development

Introduction: Terminalia species have the potential to be exploited in phytomedicine based on their several pharmacological properties including antiplasmodial activity. However, there is need for more data on their antiplasmodial activity and toxicity. This study evaluated the antiplasmodial activities of Terminalia catappa and Terminalia superba found in the coastal area of Cameroon on resistant strains of Plasmodium falciparum not previously tested, and their toxicity. Methods: Three leaf extracts of each plant prepared separately using three organic solvents were screened in vitro on 3 strains of P. falciparum: chloroquine-sensitive 3D7, chloroquine-resistant Dd2 and multi-drug resistant W2mef using the parasite growth inhibition assay. Antiplasmodial activity was assessed using fluorescence microscopy and the parasite lactate dehydrogenase assay. Cytotoxicity of active extracts was assessed on LLC-MK2 monkey kidney epithelial cells and acute toxicity including effect on some liver enzymes in BALB/c mice. Results: The methanol extracts of both plants showed the highest antiplasmodial activity (IC50 between 5.03-9.76 μg/mL) on the three parasite strains. The methanol extracts showed high selectivity for parasites with selectivity index values ranging from 40 to 80 indicating very low risk of toxicity. There was no mortality or adverse effect and no significant effect on the liver enzymes, alanine aminotransferase (P = 0.506) and aspartate aminotransferase (P = 0.243). Conclusion: The antiplasmodial activity, high selectivity and no adverse effects for T. catappa and T. superba demonstrate the potential for use of these plants in traditional treatment of malaria, further development into a phytomedicine against malaria and as source of new antimalarial lead.

scholarly journals Occurrence of Sesquiterpene Derivatives in Scleria Striatonux De Wild (Cyperaceae)

2009 ◽  
Vol 4 (1) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Kennedy Nyongbela ◽  
Karine Ioset Ndjoko ◽  
Reto Brun ◽  
Sergio Wittlin ◽  
James Mbah ◽  
...  
Keyword(s):  
Silica Gel ◽  
Column Chromatography ◽  
Structure Elucidation ◽  
Methylene Chloride ◽  
Methanol Extract ◽  
Antiplasmodial Activity ◽  
Spectral Studies ◽  
Preparative Hplc ◽  
Combination Of Methods

Scleria striatonux (Cyperaceae), a spice traditionally used in Cameroon, displayed an antiplasmodial activity. Two new sesquiterpenes, 1 (sclerienone A) and 2 (sclerienone B), have subsequently been isolated from the methylene chloride/methanol extract of the rhizome. Their separation involved a combination of methods including repeated silica gel open column chromatography, Sephadex LH-20 and semi-preparative HPLC. Structure elucidation was achieved by means of chemical tests and extensive spectral studies.

scholarly journals Multistage antiplasmodial activity of hydroxyethylamine compounds, in vitro and in vivo evaluations

RSC Advances ◽  
2020 ◽  
Vol 10 (58) ◽  
pp. 35516-35530
Author(s):  
Neha Sharma ◽  
Yash Gupta ◽  
Meenakshi Bansal ◽  
Snigdha Singh ◽  
Prateek Pathak ◽  
...  
Keyword(s):  
Human Population ◽  
Antiplasmodial Activity ◽  
Drug Resistant ◽  
Fast Growing ◽  
Resistant Strains ◽  
Global Threat ◽  
Drug Resistant Strains

Malaria, a global threat to the human population, remains a challenge partly due to the fast-growing drug-resistant strains of Plasmodium species.

Antiplasmodial activity of sulfonylhydrazones: in vitro and in silico approaches

2020 ◽  
Author(s):  
Fernando de Moura Gatti ◽  
Renan Augusto Gomes ◽  
Amanda Luisa da Fonseca ◽  
Elys Juliane Cardoso Lima ◽  
Drielli Gomes Vital-Fujii ◽  
...  
Keyword(s):  
Antiplasmodial Activity ◽  
Public Health Issue ◽  
Hydrogen Bond Acceptor ◽  
Continuous Generation ◽  
Relationship Model ◽  
Life Threatening ◽  
Molecular Modeling Studies ◽  
Resistant Strains ◽  
Imine Bond

Malaria is still a life-threatening public health issue, and the upsurge of resistant strains requires continuous generation of active molecules. In this work, 35 sulfonylhydrazone derivatives were synthesized and evaluated against Plasmodium falciparum chloroquine-sensitive (3D7) and resistant (W2) strains. The most promising compound, 5b, had an IC50 of 0.22 μM against W2 and was less cytotoxic and 26-fold more selective than chloroquine. The structure–activity relationship model, statistical analysis and molecular modeling studies suggested that antiplasmodial activity was related to hydrogen bond acceptor count, molecular weight and partition coefficient of octanol/water and displacement of frontier orbitals to the heteroaromatic ring beside the imine bond. This study demonstrates that the synthesized molecules with a simple scaffold allow the hit-to-lead process for new antimalarials to commence.

scholarly journals Metallocene Antimalarials: The Continuing Quest

2008 ◽  
Vol 2008 ◽  
pp. 1-10 ◽  
Author(s):  
Margaret A. L. Blackie ◽  
Kelly Chibale
Keyword(s):  
Plasmodium Falciparum ◽  
Antiplasmodial Activity ◽  
Side Chain ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Resistant Strains ◽  
Antimalarial Compounds

Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine in order to develop a series of ferroquine derivatives. The replacement of the ferrocenyl moiety with ruthenocene has given rise to ruthenoquine and a modest series of analogues. The reaction of ferroquine and selected analogues with Au(PPh3)NO3, Au(C6F5)(tht), and [Rh(COD)Cl2] has resulted in a series of heterobimetallic derivatives. In all cases, compounds have been evaluated for in vitro antiplasmodial activity in both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Preliminary structure-activity relationships have been delineated.

scholarly journals Antiplasmodial Activity of the Ethnobotanical Plant Cassia fistula

2012 ◽  
Vol 7 (10) ◽  
pp. 1934578X1200701 ◽  
Author(s):  
Mary H. Grace ◽  
Carmen Lategan ◽  
Rocky Graziose ◽  
Peter J. Smith ◽  
Ilya Raskin ◽  
...  
Keyword(s):  
Chinese Hamster ◽  
Chloroform Extract ◽  
Antiplasmodial Activity ◽  
Cassia Fistula ◽  
Leaf Extracts ◽  
Native Populations ◽  
Flash Column Chromatography ◽  
New Compounds ◽  
Line Compound

In our ongoing investigation of new compounds with activity against malaria parasites, we tested the in vitro antiplasmodial activity of fractions and purified compounds from Cassia fistula L., a plant traditionally used by native populations of Tanzania, Zimbabwe, Mozambique and Brazil to treat malaria or symptoms associated with this disease. Crude extracts from leaves, bark and fruits were tested for their antiplasmodial activity against the chloroquine-sensitive strain of Plasmodium falciparum(D10), where leaf extracts showed the highest activity. The chloroform extract of the leaves was further bioassay-guided fractionated using a combination of centrifugal partition chromatography and flash column chromatography. Three main antiplasmodial principles, phytol (1) (IC50 18.9 ± 0.60 μM), lutein (2) (IC50 12.5 ± 0.35 μM), and di-lineolylgalactopyranosyl-glycerol (DLGG) (IC50 5.8 ± 0.27 μM) (3), were isolated and identified using spectroscopic methods. When the three active principles were tested for their cytotoxicity using a Chinese Hamster Ovarian (CHO) cell line, compound 3 showed very weak toxicity (IC50 75.9 ± 0.28 μM), while the other two compounds were nontoxic, even at the highest concentration tested. The study provides evidence to support the use of Cassia fistula as an antimalarial remedy and describes the antiplasmodial constituents from the leaves.

scholarly journals Anti-oxidant and hepatoprotective activities of total flavonoids of Indocalamus latifolius

2015 ◽  
Vol 10 (4) ◽  
pp. 779 ◽  
Author(s):  
Juan Tan ◽  
Li Shenghua ◽  
Junying Zeng ◽  
Xianjin Wu
Keyword(s):  
Silica Gel ◽  
Rat Liver ◽  
Column Chromatography ◽  
Total Flavonoids ◽  
Flavonoid Compounds ◽  
Anti Oxidant ◽  
Histopathological Studies ◽  
Hepatoprotective Drug

<p class="Abstract">The total flavonoids of <em>Indocalamus latifolius</em> were evaluated in term of their anti-oxidant and hepatoprotective activities. The results showed that<em> in vitro</em> hepatoprotective and anti-oxidant activities of total flavonoids at doses of 200 and 400 mg/kg and 100 mg/kg, respectively, were comparable to those of the known hepatoprotective drug silymarin at 100 mg/kg. These data were supplemented with histopathological studies of rat liver sections. Seven of the main flavonoid compounds purified by column chromatography using silica gel, sephadex LH-20 and develosil ODS, and determined to be vitexin, orientin, isovitexin, homoorientin, tricin, tricin-7-O-β-D-glucopyranoside and quercetin-3-O-glucopyranoside.</p><p> </p>

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