scholarly journals In vivo antiplasmodial activity and toxicological assessment of hydroethanolic crude extract of Ajuga remota

2017 ◽  
Vol 16 (1) ◽  
Author(s):  
Aschalew Nardos ◽  
Eyasu Makonnen
Keyword(s):  
Crude Extract ◽  
Antiplasmodial Activity ◽  
Toxicological Assessment ◽  
Ajuga Remota

scholarly journals Crude Ethanolic Stem Bark Extract of Zanthoxylum zanthoxyloides and Its Fractions: In-Vitro and In-Vivo Antiplasmodial Activity

2021 ◽  
pp. 4153-4163
Author(s):  
Sulaiman S. Rukayyah ◽  
Jigam, Audu Ali ◽  
Abubakar Abdulkadir ◽  
Salau, Rasaq Bolakale
Keyword(s):  
Crude Extract ◽  
Stem Bark ◽  
Multidrug Resistant ◽  
Positive Control ◽  
Antiplasmodial Activity ◽  
Bark Extract ◽  
Zanthoxylum Zanthoxyloides ◽  
Stem Bark Extract

Malaria is a global problem, as treatment failure has hampered the efficacy of most anti-malarial medications. The goal of this study was to see if stem bark extract from Zanthoxylum zanthoxyloides had antiplasmodial properties that could be used to treat both susceptible and resistant parasites. The stem bark of Z. zanthoxyloides (500g) was crushed and extracted with ethanol. The extract was tested for antiplasmodial activity in vitro against the chloroquine-sensitive (CQS) strain NF54 and chloroquine-resistant strains (CQR) K1 of P. falciparum, as well as in vivo against the CQS(NK65) strain of P. berghei at 100, 200, and 400 mg/kg bw. Bioassay-guided fractionation of the extract was performed. The crude extract had an in vitro activity of 1076.4 56.4 and 1315.1 121.6 ng/ml against chloroquine sensitive and resistant parasites, respectively while standard drugs (chloroquine and artesunate) were 10.94 nM (3478.92 ng/ml) and 9.24 nM (3215.52ng/ml) for CQS and 310.68 nM (98796 ng/ml) and 10.94 nM (3650.52 ng/ml) for CQR respectively. At Day 7, mice treated with 100, 200, and 400 mg/kg bw crude extract had parasite densities of 1159, 928, and 869 parasites/ µl, respectively (compared to positive control that had 123 parasites /µl). In vitro antiplasmodial activity was best in the K2, K4, and K6 fractions (IC50 were 6670, 6890, and 6480 ng/ml), but in vivo antiplasmodial activity was best in the K4 fraction (1183 parasites/ µl).The stem bark extract of Z. zanthoxyloides have remarkable antiplasmodial activity against both chloroquine sensitive and drug resistant P. falciparum supporting it ethnomedicinal use in malaria treatment.The extract of Z. zanthoxyloides has promising antiplasmodial activity and could be used to generate therapeutic leads against the multidrug-resistant K1 strain of P. falciparum, in addition to providing an alternative allopathic antiplasmodial medication.

scholarly journals In vivo Antiplasmodial and Toxicological Effects of Goniothalamus lanceolatus Crude Extracts

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Rozaini Mohd Zohdi ◽  
Shahida Muhamad Mukhtar ◽  
Nur Vicky Bihud ◽  
Nurulfazlina Edayah Rasol ◽  
Fasihuddin Badruddin Ahmad ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Crude Extract ◽  
Stem Bark ◽  
Antiplasmodial Activity ◽  
Bark Extract ◽  
Phytochemical Analysis ◽  
Root Extract ◽  
Crude Extracts ◽  
Leaves And Roots

This study is aimed at investigating the antiplasmodial activity and acute toxicity of the methanol (MeOH) extracts of the leaves and roots, and the dichloromethane (DCM) extracts of the stem bark, leaves, and roots of Goniothalamus lanceolatus. Phytochemical analysis was then carried out on the most active extract. In vivo antiplasmodial activity was assessed using the 4-day suppressive test against Plasmodium berghei ANKA (PbANKA) in mice. The plant extracts were administered intraperitoneally (i.p.) as a single dose (30 mg/kg) starting 4 h after infection. At a dose level of 30 mg/kg (i.p.), the DCM extracts of the stem bark and leaves, and the MeOH root extracts, prolonged the survival period of infected mice compared to that of the negative control. In addition, all crude extracts, except for the DCM root extract, exhibited parasitemia suppressive activity. The highest level of parasitemia suppression was recorded in mice treated with the DCM stem bark extract at 66.3%. No mortality was observed in mice treated with the DCM extracts of the stem bark and leaves, and the MeOH extract of the leaves, indicating that the LD50 is greater than 300 mg/kg. On the other hand, both the MeOH and DCM extracts of the roots showed toxic effects at a dose of 300 mg/kg (i.p) with an 83.3% mortality rate. The results obtained indicate that the stem bark of G. lanceolatus (DCM crude extract) possesses good antiplasmodial activity against PbANKA infected mice without causing acute toxicity. Five known styrylpyrone derivatives namely goniodiol 1, 8-epi-9-deoxygoniopypyrone 2, 9-deoxygoniopypyrone 3, digoniodiol 4 and goniothalamin 5 have been isolated from the bark of Goniothalamus lanceolatus (DCM crude extract). The structures and stereochemistry of all compounds were elucidated by interpretation of spectroscopic data. This study provides a scientific basis to support the traditional use of the plant as a remedy for malaria.

scholarly journals An In vivo Antiplasmodial Activity of Aqueous and Ethanol Crude Plant Extracts of Phyllanthus fraternus Using Plasmodium berghei Infected balb/c Mice

2019 ◽  
pp. 1-8
Author(s):  
Daniel Amiteye ◽  
Abraham Quarcoo ◽  
Bright K. Azumah ◽  
George M. Aryitey ◽  
Lateef A. Oseni ◽  
...  
Keyword(s):  
Plant Extracts ◽  
Crude Extract ◽  
Plasmodium Berghei ◽  
Antiplasmodial Activity ◽  
Dependent Manner ◽  
Cotton Wool ◽  
Standard Drug ◽  
Ethanol Extracts ◽  
Phyllanthus Fraternus

Background: Phyllanthus fraternus is a tropical plant that has numerous pharmacological activities such as blennorrhagia, colic, diabetes, dysentery, fever, flu, tumours, jaundice, vaginitis, dyspepsia, anti-inflammatory, antioxidant, anticoagulant, anti-diabetic, antiviral and analgesic. The study evaluated in vivo anti-plasmodial activity of aqueous and ethanol crude plant extracts of Phyllanthus fraternus using Plasmodium berghei infected Balb/c mice. Methodology: The preparation of the aqueous crude extract was done by boiling 195 g of the dried plant material in 4 L of water for 30 minutes and cooled. The resultant extract was filtered through a cotton wool and put in an oven at 50°C to concentrate it before it was pre- freeze and lyophilized into powder using a freeze dryer (Heto powder dry LL 300, Sapa). Similarly the preparation of the ethanol crude extract was obtained by simple maceration of 195 g of dried sample of the plant in 2 L aqueous ethanol (1.4 L of ethanol plus 0.6 L of distilled water) for 72 h. It was then filtered through cotton wool and subjected to rotary evaporator (ILA CCA-1111 Japanese branch) to evaporate the ethanol and then pre-freeze and freeze- dried. The crude extracts were screened for their phytochemical constituents which showed the presence of secondary metabolites. The LD50 of both extracts were investigated using Sprague-Dawley rats and found to be greater than 5000 mg/kg. The in vivo antiplasmodial activity (percentage parasitaemia (%P) and the percentage chemo-suppression (%C)) of the extracts were evaluated using Balb/c mice. Results: The aqueous and ethanol extracts established modest antiplasmodial activity in a dose dependent manner. The standard drug (coartem 2 mg/kg) with percentage parasitaemia (%P) of 28.57±4.70 and 2.48±0.48 caused percentage chemosupression (%C) of 44.38±7.63 and 81.27±2.07 in day four and six respectively. The test groups (aqueous and ethanol extracts) for two different doses (100 mg/kg and 200 mg/kg) each administered with percentage parasitaemia (%P) 39.67±1.35, 39.58±1.64, 37.32±2.37, 36.23±1.99 and 10.24±1.32, 9.33±0.66, 8.61±0.96, 7.27±1.26 caused percentage chemosuppressions (%C) of 22.78±2.20, 22.96±2.66, 27.35±3.84, 29.48±3.23 and 22.54±9.93, 29.43±4.99, 34.87±6.66, 44.99 ±5.98 in day four and six respectively. The aqueous extract demonstrated better inhibition of plasmodium in doses 100 mg/kg and 200 mg/kg with chemosuppressions (27.35 ± 3.84 and 29.48 ± 3.23) respectively compared with the ethanol extract of the same doses 100 mg/kg and 200 mg/kg with chemosuppressions (22.78 ± 2.20 and 22.96 ± 2.66) respectively. The activity of the standard drug, coartem at 2.0 mg/kg was significantly higher (p< 0.05) with chemosupression (44.38±7.63) than those of the extracts. The extracts were also screened for phytochemicals for which some were found in the extracts which have previously been implicated as antiplasmodial agents. The LD50 of both extracts were investigated and found to be greater than 5000 mg/kg. Conclusion: The aqueous and ethanol crude plant extracts of P. fraternus possess antiplasmodial activity and would be useful in the search for novel antimalarial agents.

scholarly journals Assessment of Antiplasmodial Activity and Toxicity of Crude Extracts and Isolated Compounds from Oncoba spinosa (Flacourtiaceae)

2019 ◽  
pp. 1-14
Author(s):  
Kodi Philip ◽  
Peter Kiplagat Cheplogoi ◽  
Mwangi Muthoni Elizabeth ◽  
M. Akala Hoseah ◽  
Moses K. Langat
Keyword(s):  
Acute Toxicity ◽  
Ethyl Acetate ◽  
Crude Extract ◽  
Antimalarial Activity ◽  
Local Communities ◽  
Antiplasmodial Activity ◽  
Isolation And Purification ◽  
Crude Extracts

Aims: The medicinal plant Oncoba spinosa is used by the local communities in Butebo County in Eastern Uganda for treatment of malaria and other diseases. In vitro antiplasmodial activities of the crude extracts and isolated compounds were screened against chloroquine sensitive 3D7 and resistant Dd2 strains. In vivo acute toxicity of the extracts and structure elucidation were also determined in the study. Experimental: Crude extracts of: n-hexane, dichloromethane, ethyl acetate and methanol were prepared. Isolation and purification of these extracts were done using chromatographic techniques which consisted of column and thin layer chromatography. The structures were elucidated on the basis of spectroscopic evidence. In vitro antiplasmodial activity was performed on chloroquine sensitive 3D7 and resistant Dd2 strains of Plasmodium falciparum using SYBR Green 1 assay technique. Lorke’s method of acute toxicity was used to determine the in vivo acute toxicity of the crude extracts in mice. Results: The root ethyl acetate crude extract had highest antiplasmodial activity of IC50:4.69 ± 0.01 µg/mL and 3.52 ± 0.02 µg/mL against 3D7 and Dd2 strains respectively while the remaining three were inactive against both strains of Plasmodium. Isolation resulted in the identification of three known compounds which included: β-sitosterol, benzoic acid and chaulmoogric acid. Among the tested compounds β-sitosterol showed the highest activity of IC50 3D7: 5.51 µM. Dichloromethane and hexane extracts were non-toxic with LD50 > 5000 mg/kg while the EtOAc and MeOH extracts were slightly toxic with LD50 of 547.72 mg/kg. Statistically significance existed between the antiplasmodial activity of the crude extracts and compounds when compared with the controls at (p < 0.05). Extracts and compounds exerted a significant (P < 0.05) decrease in antiplasmodial activity compared to the positive controls. Conclusion: The findings confirm the ethnobotanical use of O. spinosa by the local communities in Butebo County for the treatment of malaria. The results also suggest that the crude extract of this plant is safe and possesses antimalarial activity which can be used as a basis for in vivo and clinical studies to be done. Therefore the plant can offer a potential drug lead for developing a safe, effective and affordable antimalarial.

In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization

2021 ◽  
Vol 215 ◽  
pp. 113271
Author(s):  
Juliane Aparecida Marinho ◽  
Daniel Silqueira Martins Guimarães ◽  
Nícolas Glanzmann ◽  
Giovana de Almeida Pimentel ◽  
Izabelle Karine da Costa Nunes ◽  
...  
Keyword(s):  
Quinoline Derivative ◽  
Antiplasmodial Activity ◽  
Molecular Hybridization

In vitro and in vivo Antiplasmodial Activity of Momordica balsamina Alone or in a Traditional Mixture

Chemotherapy ◽  
2006 ◽  
Vol 52 (6) ◽  
pp. 288-292 ◽  
Author(s):  
F. Benoit-Vical ◽  
P. Grellier ◽  
A. Abdoulaye ◽  
I. Moussa ◽  
A. Ousmane ◽  
...  
Keyword(s):  
Antiplasmodial Activity

scholarly journals Exploring heteroaromatic rings as a replacement for the labile amide of antiplasmodial pantothenamides

2020 ◽  
Author(s):  
Jinming Guan ◽  
Christina Spry ◽  
Erick T. Tjhin ◽  
Penghui Yang ◽  
Tanakorn Kittikool ◽  
...  
Keyword(s):  
Contact Time ◽  
High Selectivity ◽  
Amide Group ◽  
Antiplasmodial Activity ◽  
Time Data ◽  
Facile Synthesis ◽  
Isoxazole Derivative ◽  
Nanomolar Range

ABSTRACTThe Plasmodium parasites that cause malaria are adept at developing resistance to antimalarial drugs, necessitating the search for new antiplasmodials. Although several amide analogs of pantothenate (pantothenamides) show potent antiplasmodial activity, hydrolysis by pantetheinases (or vanins) present in blood rapidly inactivates them. We report herein the facile synthesis and biological activity of a small library of pantothenamide analogs in which the labile amide group is replaced with a variety of heteroaromatic rings. Several of the new analogs display antiplasmodial activity in the nanomolar range against P. falciparum and/or P. knowlesi in the presence of pantetheinase. A previously reported triazole and an isoxazole derivative presented here were further characterized and found to possess high selectivity indices, medium or high Caco-2 permeability, and medium or low microsomal clearance in vitro. Although we show here that the two compounds fail to suppress proliferation of P. berghei in vivo, pharmacokinetic and contact time data presented provide a benchmark for the compound profile required to achieve antiplasmodial activity in mice and should facilitate lead optimization.

scholarly journals Toxicity and teratogenicity evaluation of hydroethanolic extract of momordica charantia fruit using zebrafish (DANIO RERIO) embryos model

2019 ◽  
Vol 10 (SPL1) ◽  
Author(s):  
Noor Izati Abd Aziz ◽  
Vikneswari Perumal ◽  
Suganya Murugesu ◽  
Qamar Uddin Ahmed ◽  
Bisha Fathamah Uzir ◽  
...  
Keyword(s):  
Danio Rerio ◽  
Crude Extract ◽  
Momordica Charantia ◽  
Spinal Curvature ◽  
Zebrafish Embryos ◽  
Chemical Toxicity ◽  
Active Constituent ◽  
Hydroethanolic Extract ◽  
Danio Rerio Embryos

 The use of zebrafish vertebrate model in vivo analysis of the drug toxicity and efficacy, chemical toxicity, and safety is increasing in recent researches. Momordica charantia Linn (Cucurbitaceae) has been traditionally claimed for its many protective roles. However, the development of toxicity effect may cause morphological abnormalities by using an embryo of zebrafish (Danio Rerio) is unknown. Hence, this study was designed to determine the toxicity and teratogenic effect of hydroethanolic extract of M. charantia fruit using Zebrafish (Danio Rerio) embryos. The crude extract was prepared from the fruit of M. charantia using 80% hydroethanolic solvent. The zebrafish embryos were exposed to serial dilution of crude extract. The active constituent was analyzed using gas chromatography coupled with mass spectrophotometry (GC-MS) Momordica charantia Linn (Cucurbitaceae) has been widely commercialized based on traditional usage as an antidiabetic product. The current study has shown the toxic effects of the M.  charantia fruit extract on the developing zebrafish embryos, and the median lethal concentration (LC50) was calculated to be 725.90 mg/L at 48 hpt. The observed effects are dependent on the time of exposure and concentrations of the extract. At higher concentration, the extract causes some morphological defects such as less pigmentation, dented tail, spinal curvature, oedema, reduced hatchability, and growth retardation, that indicates the presence of toxicant(s). Based on the GC-MS profiling, some of the compounds identified in the hydroethanolic extract, such as propanedioic acid and glutamine, may have caused the teratogenic effects to the embryos. Further research on the M. charantia fruit's metabolites should be carried out prior to any nutraceutical or pharmaceutical application.

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 A Pilot Study on Antimalarial Effects of Moringa oleifera Leaf Extract in Plasmodium berghei Infection in Mice

2017 ◽  
Vol 15 (2) ◽  
pp. 151-156
Author(s):  
Somrudee NAKINCHAT ◽  
Voravuth SOMSAK
Keyword(s):  
Plasma Glucose ◽  
Crude Extract ◽  
Plasmodium Berghei ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Dependent Manner ◽  
Glucose Levels ◽  
New Compounds ◽  
Dose Dependent

The emergence and spread of antimalarial drug resistance of Plasmodium parasites, as well as hypoglycemia, during malaria infection, and subsequent death, are critical problems in malaria-endemic areas. Hence, finding new compounds, especially plant extracts having antimalarial and anti-hypoglycemic activities, are urgently needed. The present study aimed to investigate the antimalarial and anti-hypoglycemic effects of Moringa oleifera leaf extract in Plasmodium berghei infection in mice. Aqueous crude extract of M. oleifera leaves was freshly prepared and used for an efficacy test in vivo. Groups of ICR mice (5 mice in each) were infected with 1´107 infected red blood cells of P. berghei ANKA by intraperitoneal injection and given the extract orally with doses of 100, 500, and 1000 mg/kg for 4 consecutive days. Parasitemia and plasma glucose levels were subsequently measured. The results showed that M. oleifera leaf extract presented significant (p < 0.001) inhibition of parasitemia in a dose-dependent manner. Moreover, this extract exerted anti-hypoglycemia effects in infected mice in a dose-dependent manner. The highest degrees of activity were found at a dose of 1000 mg/kg of the extract. Additionally, no effect on plasma glucose was found in normal mice treated with this extract. It can be concluded that aqueous crude extract of M. oleifera leaves exerted antimalarial and anti-hypoglycemic effects in P. berghei infection in mice.

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