scholarly journals Antimalarial Activity of Nigella sativa L. Seed Extracts and Selection of Resistance in Plasmodium berghei ANKA in a Mouse Model

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Rahma Udu ◽  
Job Oyweri ◽  
Jeremiah Gathirwa

Background. Chemotherapy plays a crucial role in malaria control. However, the main obstacle to treatment has been the rise of parasite resistance to most antimalarial drugs. Artemisinin-based combination therapies (ACTs) remain the most effective antimalarial medicines available today. However, malaria parasite tolerance to ACTs is now increasingly prevalent especially in Southeast Asia presenting the danger of the spread of ACTs resistance to other parts of the world. Consequently, this creates the need for alternative effective antimalarials. Therefore, this study sought out to determine antimalarial potential, safety, and resistance development of the extracts in a mouse model. Method. Methanolic and ethyl acetate extracts were obtained by solvent extraction. The extracts were assayed for acute toxicity in vivo. Additionally, the two extracts were evaluated for antimalarial activity in vivo against Plasmodium berghei ANKA strain by the 4-day suppressive test at 500, 250, and 125 mg/kg/day. Packed cell volume was evaluated to determine anemia manifestation. Finally, continuous drug pressure experiment at 500 mg/kg and DNA amplification via PCR were conducted. The amplicons underwent through Sanger sequencing. Results. There was no toxicity realized in the animals at 2000 mg/kg. Importantly, high parasitemia suppression of 75.52% and 75.30% using a dose of 500 mg/kg of methanolic and ethyl acetate extracts, respectively, was noted. The extracts were able to reverse packed cell volume reduction. Nigella sativa-resistant phenotype was selected as delayed parasite clearance. However, there was no change in the nucleotide sequences of PbMDR1 and PbCRT genes. Conclusion. The results provide room for future exploitation of the plant as an antimalarial.

2020 ◽  
Author(s):  
Abebe Basazn Mekuria ◽  
Mestayet Geta ◽  
Eshetie Melese Birru ◽  
Desalegn Asmelashe Gelayee

Abstract Background: Due to drug resistance and inefficient eradication techniques, malaria continues to be a major public health issue in countries with low- and middle-income. The seeds of Schinus molle are used in the Ethiopian folklore medicine for the treatment of malaria. However, this claim is not yet supported with scientific researches. Hence, the current study aims to investigate in vivo, antimalarial activity of hydro-alcoholic crude extract and subsequent solvent fraction of Schinus molle seeds on Plasmodium berghe infected mice.Methods: A hydro-alcoholic crude extract and solvent fractions (ethyl acetate, chloroform and aqueous) of Schinus molle seeds were tested at different doses (100, 200 and 400 mg/kg respectively ) to evaluate in vivo antimalarial activity of extracts in a 4-day suppressive, curative, and prophylaxis antimalarial test models. The parasitemia level, packed cell volume, survival of date, body weight, and body temperature were used to evaluate the anti-plasmodia activity of the extracts. One way ANOVA was employed to analyze these data, followed by post hoc Tukey’s HSD multiple comparison test.Results: The chemo-suppressive activities produced by the highest dose (400mg/kg) of crude extract and the aqueous fraction of Schinus molle seeds in the four-day suppressive test were 76.03% and 73.82%(p<0.001), respectively. In the curative test, the highest dose of crude and the aqueous fraction of Schinus molle seeds had 82.12% and 84.30% (p<0.001) suppression activity, respectively. The percentage of suppression in the prophylactic activities test of the aqueous fraction was 79.78% (p<0.001) at 400mg/kg compared to the negative control group. The studied plant extracts were likely anticipated to show rapid rectal temperature reduction and weight loss significantly. Among the extracts, only chloroform fraction has prevented the reduction of packed cell volume, due to the absence of saponin in the fraction. The mice which were treated with crude extract and aqueous fraction survived longer and gained net body weight as compared to vehicle-treated mice (p<0.001).Conclusion: The crude extract and aqueous fraction of Schinus molle seeds possessed significant antimalarial activity. These results collectively indicate that the plant has promising anti-plasmodial activity against Plasmodium berghei. However, further confirmatory studies followed by isolation and characterization of the active antimalarial compound are recommended.


2020 ◽  
Author(s):  
Melkamu Adigo Shibeshi ◽  
Tezera Jemere Aragaw ◽  
Getnet Mequanint Adinew ◽  
Engdaw Fentahun Enyew

Abstract Background Malaria is an infectious, hematologic disease causing death and illness in children and adults, especially in tropical countries. The aim of this study was to evaluate the antimalarial activity of Combretum molle extract in vivo assays against Plasmodium berghei in Swiss albino mice. Methods Plasmodium berghei a rodent malaria parasite was inoculated to healthy Swiss Albino mice age 6–8 weeks either sex, weight 20–33g. 100, 200 and 400mg/kg/day of Crude methanolic extract of Combretum molle were administered. Parameters such as Percent parasitemia, body weight, Body temperature, packed cell volume and survival time were then determined using standard tests. Data were analyzed using one-way ANOVA followed by the Post hoc Tukey HSD test with SPSS software version 24.0 and P ≤0.05 considered as statistically significant. Results Chemosuppresive effect exerted by the crude extract ranged between 27-68%. The curative effect of the crude extract was in the range of 25-49% and ptophylactic effect of the crude extract was in the range of 51–76.2%%. The maximum effect in all tests on Chemosuppresive, curative, Prophylactic, prevention of weight loss, body temperature and packed cell volume and an increase in mean survival time was observed at higher doses of the crude extract. Conclusion From the present study it can be concluded that the crude extract of Combretum molle leaves has been shown promising antimalarial activity. This finding supports the traditional use of the plant for the treatment of malaria in Ethiopia. Thus, it could be considered as a potential source to develop safe, effective and affordable antimalarial agent.


Author(s):  
Kartika Arum Wardani ◽  
Kholida Nur Aini ◽  
Heny Arwati ◽  
Willy Sandhika

Abstract Sequestration of Plasmodium berghei ANKA-infected erythrocytes occurs in BALB/c mice as characteristic of  Plasmodium falciparum infection in humans. Animals’ bile has been widely used for centuries in Traditional Chinese Medicine. Goat bile has been used in healing infectious and non-infectious diseases; however, no report on the use of goat bile against malaria infection and sequestration. The purpose of this study was to analyze the correlation between parasitemia and sequestration in the liver of P.berghei ANKA-infected BALB/c mice treated with goat bile. This research was an in vivo experimental study using the post-test control group design. The male BALB/c mice aged ± 6 weeks, body weight 20-25 g were used. The mice were divided into five groups where Group 1-3 were mice treated with goat bile 25%, 50%, and 100%, respectively. Group 4-5 were negative (sterile water) and positive controls (DHP). Parasitemia was observed daily from each mouse and the number of sequestered infected erythrocytes on the endothelium of sinusoids. The data were analyzed using t independent test. Antimalarial activity of goat bile was shown by the lower parasitemia in goat bile-treated mice compared with the negative control. The average number of sequestration was goat bile concentration-dependent manner. The higher the concentration, the lower the number of sequestration. Sequestration was correlated with parasitemia (p=0,0001). Sequestration of P.berghei ANKA-infected erythrocytes correlated with parasitemia, and was goat bile concentration-dependent manner. Keywords: Malaria, parasitemia, sequestration, goat bileCorrespondence: [email protected]


2020 ◽  
Vol 2020 ◽  
pp. 1-8 ◽  
Author(s):  
Noumedem Anangmo Christelle Nadia ◽  
Yamssi Cédric ◽  
Simeni Njonnou Sylvain Raoul ◽  
Ngongang Ouankou Christian ◽  
Mounvera Abdel Azizi ◽  
...  

Background. Malaria is one of the most critical diseases causing about 219 million cases worldwide in developing countries. The spread and development of resistance against chemical antimalarial drugs is one of the major problems associated with malaria control. The present study was to investigate the antimalarial efficacy of ethyl acetate extract and one fraction of Bidens pilosa in vivo in order to support the usage of this plant by traditional healers to treat malaria. Methods. The extracts were prepared by maceration of B. pilosa leaf powder in ethyl acetate. The liquid filtrate of the extract and the best in vitro antiplasmodial fraction using HPLC were concentrated and evaporated using a rotavapor under vacuum to dryness. The antimalarial activity of B. pilosa plant products were evaluated in vivo against Plasmodium berghei infected mice according to the Peter and Rane test. The antimalarial efficacy of the a selected crude extract (ethyl acetate extract) was evaluated at 125, 250, and 500 mg/kg, while a selected fraction from ethyl acetate extract (fraction 12) was evaluated at 62.5 and 125 mg/kg. Blood from experimental animals was collected to assess hematological parameters. Results. The crude extract of ethyl acetate and fraction 12 demonstrated 100% in vivo parasite suppressive activity at doses of 500 mg/kg and 125 mg/kg, respectively, for the crude extract and fraction 12. The mice treated with 250 and 500 mg/kg had their parasitemia (intraerythrocytic phase of P. Berghei) drop considerably, disappearing by the 8th day in mice receiving 500 mg/kg. The ethyl acetate extract of B. pilosa, fraction 12 showed an even higher antiplasmodial activity. By the 5th day of the experiment, the treatment led to a modification of hematological parameters in mice. The chloroquine (5 mg/kg), fraction 12 (125 mg/kg), and the crude extract (500 mg/kg) groups all survived the 30 days of the experiment, while the negative control group registered 100% of the deaths. Conclusion. This study scientifically supports the use of Bidens pilosa leaves in the traditional treatment of malaria. However, the mode of action and in vivo toxicity of the plant still need to be assessed.


2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Gebru Hagos Atsbha ◽  
Rajkapoor Balasubramanian ◽  
Abadi Kahsu Gebre

Background. Malaria remains a major public health problem globally. Poor access to antimalarial drugs compounded with rapidly evolving drug resistance encourages researchers to continuously look for new drugs. Of importance, traditionally used medicines of plant origin are the highest priority as the ethnobotanical claim can be used as an important clue for its safety and efficacy profiles. Silene macrosolen A. Rich (Caryophyllaceae) has been traditionally used for malaria treatment in Ethiopia. Therefore, this study was aimed to evaluate the in vivo antimalarial activity of the plant against Plasmodium-berghei-infected (ANKA strain) Swiss albino mice. Methods. The dried powdered root of Silene macrosolen was extracted using 80% methanol. The crude extract was fractionated using chloroform, ethyl acetate, and distilled water that have different affinities to plant phytoconstituents. The in vivo antimalarial activities of the crude extract were evaluated using 4-day suppressive, prophylactic, and curative tests. The antimalarial activity of the solvent fractions was evaluated in a 4-day suppressive test. The oral acute toxicity of the crude extract was also determined according to the OECD guidelines. Results. The percentage of parasite suppression on the crude extract was 31.02%, 35.82%, and 39.23% in prophylactic, curative, and 4-day suppressive tests, respectively, at the tested dose level of 400 mg/kg. The percentages of chemosuppression of the solvent fractions (400 mg/kg) were 43.07%, 42.61%, and 38.38% in aqueous, ethyl acetate, and chloroform fractions, respectively. Both the crude extract and solvent fractions also significantly prolonged survival time except in the prophylactic test. In addition, prevention of weight loss and reduction in temperature and packed cell volume (PCV) were observed in crude extract as well as solvent fractions. The acute toxicity test of the plant extract also exhibited no sign of toxicity. Conclusion. The result indicated that Silene macrosolen has a significant antimalarial activity, justifying the traditional use of the plant material for treatment of malaria.


2019 ◽  
Vol 2019 ◽  
pp. 1-6 ◽  
Author(s):  
Sakaewan Ounjaijean ◽  
Manas Kotepui ◽  
Voravuth Somsak

Plant species of the genus Tinospora (Menispermaceae) possess several pharmacological properties, and T. crispa has been reported to have antimalarial activity. T. baenzigeri (Chingcha Chalee) is a rich source of terpenes and quinoline alkaloids; however, it still has not yet been investigated the antimalarial activity of this plant extract. Hence, this study was aimed to evaluate the antimalarial activity of T. baenzigeri stem extract against Plasmodium berghei-infected mice. The aqueous crude extract of T. baenzigeri stem was prepared using a microwave-assisted method and tested for acute toxicity in mice. For evaluating the antimalarial activity in vivo, the standard 4-day test was carried out using groups of ICR mice infected with P. berghei ANKA administered orally by gavage with the extract (100, 250, and 500 mg/kg) for 4 consecutive days. Parasitemia, body weight, packed cell volume, and mean survival time were then measured. It was found that the aqueous crude extract of T. baenzigeri stem did not exhibit any sign of toxicity up to the dose of 2,000 mg/kg. The extract significantly (P<0.01) inhibited parasitemia in a dose-dependent manner, with 22.02%, 50.81%, and 74.95% inhibition. Moreover, the marked prevention of body weight loss and packed cell volume reduction was observed at doses of 100, 250, and 500 mg/kg of extract-treated mice. Additionally, the extract prolonged the mean survival time of P. berghei-infected mice, compared to the untreated group. In conclusion, the aqueous crude extract of T. baenzigeri stem has demonstrated potent antimalarial activity against P. berghei-infected mice with prolonged mean survival time and prevention of body weight loss and packed cell volume reduction.


2021 ◽  
Vol 4 (1) ◽  
pp. 5
Author(s):  
Putri Rahayu ◽  
Yetti Hernaningsih ◽  
Heny Arwati

Introduction: Malaria is one of the infectious diseases found in tropical countries and sub-tropical countries. In 2016 there were an estimated 445,000 people died to malaria. Alternative medicine is needed, such as natural based ingredient. Morinda citrifolia or noni plant is a medicinal plant found in all parts of Indonesia which has many benefits, such as antibacterial, analgesic, anticancer, antioxidant, and anti-inflammatory. The aims of this study were to determine the antimalarial activity of ethanol extract of noni leaves and its effect on splenomegaly and hepatomegaly.Methods: Extract of noni leaves was prepared by maceration using ethanol solvent. In vivo experiments were conducted using Plasmodium berghei infected BALB/c mice treated with the doses of 100, 10, 1 mg/kg body weight(BW) orally of ethanolic extract of noni leaves. Then, the percentage of parasitemia was calculated from day 1 to day 4 after treatment and at the end of the test, mice were sacrificed then spleen and liver were collected. Results: The highest parasite growth was found in the group treated with noni leaves ethanol extract at a dose of 1 mg/kg WB and vice versa. Probit analysis resulted in ED50 was 0.882 mg/kg WB. Spearmen test showed there was no correlation between doses and the size of splenomegaly with p=0,2 and between doses and the size of hepatomegaly with p=0,6.Conclusion: Ethanol extract of noni leaves possessed antimalaria activity and there was no correlation between doses of extract and t he splenomegaly and hepatomegaly.


2021 ◽  
pp. 114448
Author(s):  
Liliane Laure Toukam ◽  
Bertrand Tatsinkou Fossi ◽  
Germain Sotoing Taiwe ◽  
Raymond Bess Bila ◽  
David Denis Feugaing Sofeu ◽  
...  

2019 ◽  
Vol 44 (3-4) ◽  
pp. 161-166 ◽  
Author(s):  
Custodiana Colmenarez ◽  
María Acosta ◽  
Miguel Rodríguez ◽  
Jaime Charris

The synthesis of five new ( S)-methyl-(7-chloroquinolin-4-ylthio)acetamidoalquilate derivatives is carried out under a modified version of the Steglich esterification reaction between different l-amino acid methyl esters and 2-(7-chloroquinolin-4-ylthio)acetic acid. Two of the compounds showed significant inhibition (>50%) of β-hematin formation. The two active structures were tested in vivo as potential antimalarials in mice infected with Plasmodium berghei ANKA, a chloroquine susceptible strain. Compounds 6b and 6e exhibited antimalarial activity comparable to that of chloroquine.


2021 ◽  
Vol 36 (2) ◽  
pp. 109-120
Author(s):  
Mekuanent Zemene ◽  
Mestayet Geta ◽  
Solomon Assefa Huluka ◽  
Eshetie Melese Birru

Malaria continues to be a global public health threat. In Africa, malaria accounts for a substantial morbidity and mortality. The emergence of drug resistant malaria parasites and subsequent decrement in effectiveness of current antimalarial medications have complicated  malaria control. This urged developing an effective alternative antimalarial agent. Leaves and root of Stephania abyssinica (Dill. & A. Rich.) Walp. is traditionally used for the treatment of malaria in east African countries such as Ethiopia and proved for its in vitro antimalarial efficacy. Hence, this study aimed at evaluating the antimalarial activity of S. abyssinica. Cold maceration technique was employed to prepare the 80% methanol crude extract followed by fractionation using n-hexane, chloroform and ethyl acetate. The in vivo antimalarial property of different dose levels (100, 200 and 400 mg/kg/day) of the hydroalcoholic extract and solvent fractions were investigated using prophylactic and 4-day suppressive mice models, against Plasmodium berghei (ANKA strain). Highest (400 mg/kg) doses of the  hydroalcoholic extract and solvent fractions (hexane, chloroform and ethyl acetate) exhibited a statistically significant (p < 0.001) chemosuppressive activities. The chloroform fraction revealed the highest  chemosuppresion (55.80%) and chemoprophylactic (57.59%) potency in 4-day suppressive and prophylactic tests, respectively, at 400 mg/kg dose level. Furthermore, 400 mg dose of the chloroform fraction significantly prevented malaria associated haemolysis as compared to vehicle treated group in both prophylactic (p < 0.05) and suppressive (p < 0.01) models. In conclusion, the current study gave evidence that the plant has a potential antimalarial activity against P. berghei, which upholds traditional claims and justifies a need to undertake  advanced pharmacological and toxicological investigations.


Sign in / Sign up

Export Citation Format

Share Document