scholarly journals In Vivo Antimalarial Activity of the Beta-Carboline Alkaloid Manzamine A

2000 ◽  
Vol 44 (6) ◽  
pp. 1645-1649 ◽  
Author(s):  
Kenny K. H. Ang ◽  
Michael J. Holmes ◽  
Tatsuo Higa ◽  
Mark T. Hamann ◽  
Ursula A. K. Kara
Keyword(s):  
Plasmodium Berghei ◽  
Malaria Parasite ◽  
Antimalarial Activity ◽  
Single Injection ◽  
Morphological Changes ◽  
Rodent Malaria Parasite ◽  
Manzamine A ◽  
Antimalarial Agents ◽  
Single Intraperitoneal Injection

ABSTRACT Manzamine A, a β-carboline alkaloid present in several marine sponge species, inhibits the growth of the rodent malaria parasitePlasmodium berghei in vivo. More than 90% of the asexual erythrocytic stages of P. berghei were inhibited after a single intraperitoneal injection of manzamine A into infected mice. A remarkable aspect of manzamine A treatment is its ability to prolong the survival of highly parasitemic mice, with 40% recovery 60 days after a single injection. Oral administration of an oil suspension of manzamine A also produced significant reductions in parasitemia. The plasma manzamine A concentration peaked 4 h after injection and remained high even at 48 h. Morphological changes of P. berghei were observed 1 h after treatment of infected mice. (−)-8-Hydroxymanzamine A also displayed antimalarial activity, whereas manzamine F, a ketone analog of manzamine A, did not. Our results suggest that manzamine A and (−)-8-hydroxymanzamine A are promising new antimalarial agents.

scholarly journals Antimalarial Activity of Hydroalcoholic Root Extract of Acanthus polystachyus Delile (Acanthaceae) Against Plasmodium berghei–Infected Mice

2019 ◽  
Vol 24 ◽  
pp. 2515690X1988532 ◽  
Author(s):  
Dagninet Derebe ◽  
Muluken Wubetu
Keyword(s):  
Crude Extract ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Negative Control ◽  
New Drugs ◽  
Root Extract ◽  
Root Extracts ◽  
Antimalarial Agents ◽  
Mean Survival Time

Failure of the efficacy of antimalarial drugs is recognized in different classes of medicines for treating malaria, which urges the need for new drugs. This study tried to check the in vivo antimalarial activity of the root extracts of Acanthus polystachyus Delile against Plasmodium berghei–infected mice. The study revealed that the methanolic crude extract of the root of Acanthus polystachyus Delile showed significant ( P < .01) parasitemia suppressive activities in both models compared with the negative control. Parasitemia suppressive activities were 25.26%, 33.46%, and 51.48% in a 4-day suppressive test and 23.31%, 31.20%, and 43.54% in prophylaxis test at 100, 200, and 400 mg/kg of the extract, respectively, as compared to the negative control. Besides, the extract increases mean survival time significantly in all tested doses in a 4-day suppressive test, but in the prophylaxis model, only mice treated with 200 and 400 mg/kg significantly lived longer. Based on this finding, the root of Acanthus polystachyus Delile has strong antimalarial activity, which may be a good candidate for new antimalarial agents.

Bioactive compounds from coral reef invertebrates

2001 ◽  
Vol 73 (3) ◽  
pp. 589-593 ◽  
Author(s):  
Tatsuo Higa ◽  
Junichi Tanaka ◽  
Ikuko I. Ohtani ◽  
Musri Musman ◽  
Michael C. Roy ◽  
...  
Keyword(s):  
Coral Reef ◽  
Bioactive Compounds ◽  
Plasmodium Berghei ◽  
Malaria Parasite ◽  
Spectroscopic Analysis ◽  
Antimalarial Activity ◽  
Manzamine A ◽  
Theonella Swinhoei ◽  
Parasite Plasmodium ◽  
High Level

Manzamine A (1) known as a cytotoxin exhibited potent antimalarial activity with 40% recovery 60 days after single intraperitoneal (i.p.) injection against mice infected with the malaria parasite Plasmodium berghei. Pachastrisamine (6), a simple derivative of a sphingosine, isolated from a sponge, Pachastrissa sp. showed a high level of cytotoxicity. New sesquiterpene carbonimidic dichlorides and related aldehydes (8­12) have been isolated as cytotoxic constituents of the sponge Stylotella aurantium and shown to have moderate cytotoxicity. Cyclic undecapeptides, barangamides A­D (13­16), have been isolated from the sponge Theonella swinhoei. Their structures were established by spectroscopic analysis and chemical reaction.

scholarly journals A Multifactorial Mechanism in the Superior Antimalarial Activity ofα-C-GalCer

2010 ◽  
Vol 2010 ◽  
pp. 1-11 ◽  
Author(s):  
John Schmieg ◽  
Guangli Yang ◽  
Richard W. Franck ◽  
Moriya Tsuji
Keyword(s):  
Proliferative Response ◽  
Malaria Parasite ◽  
Antimalarial Activity ◽  
Plasmodium Yoelii ◽  
Th2 Cytokines ◽  
Therapeutic Activity ◽  
Rodent Malaria Parasite ◽  
Rodent Malaria ◽  
In Vivo Administration

We have previously shown that the C-glycoside analog ofα-galactosylceramide (α-GalCer),α-C-GalCer, displays a superior inhibitory activity against the liver stages of the rodent malaria parasitePlasmodium yoeliithan its parental glycolipid,α-GalCer. In this study, we demonstrate that NK cells, as well as IL-12, are a key contributor for the superior activity displayed byα-C-GalCer. Surprisingly, the diminished production of Th2 cytokines, including IL-4, byα-C-GalCer has no affect on its superior therapeutic activity relative toα-GalCer. Finally, we show that the in vivo administration ofα-C-GalCer induces prolonged maturation of dendritic cells (DCs), as well as an enhanced proliferative response of mouse invariant Vα14 (Vα14i) NKT cells, both of which may also contribute to some degree to the superior activity ofα-C-GalCer in vivo.

scholarly journals Antimalarial Activity of Hydromethanolic Crude Extract and Chloroform Fraction of Brucea antidysenterica Leaves in Plasmodium berghei-Infected Mice

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Tezera Jemere Aragaw ◽  
Kefyalew Ayalew Getahun
Keyword(s):  
Crude Extract ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Negative Control ◽  
Chloroform Fraction ◽  
Curative Effect ◽  
Antimalarial Agents ◽  
Different Doses

Background. Different parts of Brucea antidysenterica are used in traditional and alternative medicine in Ethiopia for the treatment of different health problems including malaria and have good in vitro antimalarial activity. However, no in vivo study was conducted to substantiate the claim. Our study planned to determine the antimalarial effect of B. antidysenterica extract. Methods. Swiss albino mice (6–8 weeks old, 20–28 g) were inoculated with Plasmodium berghei. Different doses of both hydromethanolic extract and chloroform fraction were orally given at 100, 200, and 400 mg/kg/day. Results. The parasitemia suppression percent of hydromethanolic crude extract and chloroform fraction in chemosuppressive tests ranged between 33.48 and 75.93% and 38.32 and 76.64%, respectively. The hydromethanolic crude extract and chloroform fraction exhibited the curative effect of 46.75–70.91% and 50.30–80.06% parasitemia suppression, respectively ( p  < 0.001), compared with negative control. Conclusion. From our study, it is concluded that the hydromethanolic crude extract and chloroform fraction of B. antidysenterica leaves showed promising antiplasmodial effects against Plasmodium berghei. This upholds the folkloric use of B. antidysenterica leaves and the thought of as a possible source to develop new antimalarial agents.

Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Haicheng Liu ◽  
Yushi Futamura ◽  
Honghai Wu ◽  
Aki Ishiyama ◽  
Taotao Zhang ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antimalarial Activity ◽  
In Vitro Assays ◽  
Compound Library ◽  
Antimalarial Agents ◽  
Phenotypic Screen ◽  
Ic50 Values ◽  
Substituted Benzamides

Background: Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear. Objective: This study focuses on the discovery, design, synthesis, and antimalarial evaluation of 3-cinnamamido-N-substituted benzamides. Method: In this study, a screening of our compound library was carried out against the multidrug-sensitive Plasmodium falciparum 3D7 strain. Derivatives of the hit were designed, synthesized and tested against P. falciparum 3D7 and the in vivo antimalarial activity of the most active compounds was evaluated using the method of Peters’ 4-day suppressive test. Results: The retrieved hit compound 1 containing a 3-cinnamamido-N-substituted benzamide skeleton showed moderate antimalarial activity (IC50 = 1.20 µM) for the first time. A series of derivatives were then synthesized through a simple four-step workflow, and half of them exhibited slightly better antimalarial effect than the precursor 1 during the subsequent in vitro assays. Additionally, compounds 11, 23, 30 and 31 displayed potent activity with IC50 values of approximately 0.1 µM, and weak cytotoxicity against mammalian cells. However, in vivo antimalarial activity is not effective which might be ascribed to the poor solubility of these compounds. Conclusion: In this study, phenotypic screen of our compound library resulted in the first report of 3-cinnamamide framework with antimalarial activity and 40 derivatives were then designed and synthesized. Subsequent structure-activity studies showed that compounds 11, 23, 30 and 31 exhibited the most potent and selective activity against P. falciparum 3D7 strain with IC50 values around 0.1 µM. Our work herein sets another example of phenotypic screen-based drug discovery, leading to potentially promising candidates of novel antimalarial agents once given further optimization.

scholarly journals Antimalarial Effect of the Total Glycosides of the Medicinal Plant, Ranunculus japonicus

Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 532
Author(s):  
Hae-Soo Yun ◽  
Sylvatrie-Danne Dinzouna-Boutamba ◽  
Sanghyun Lee ◽  
Zin Moon ◽  
Dongmi Kwak ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Hematological Parameters ◽  
Significant Inhibition ◽  
Ic50 Values ◽  
The Republic

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.

scholarly journals Inhibition of In Vivo Growth of Plasmodium berghei by Launaea taraxacifolia and Amaranthus viridis in Mice

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Adewale Adetutu ◽  
Olubukola S. Olorunnisola ◽  
Abiodun O. Owoade ◽  
Peter Adegbola
Keyword(s):  
Survival Time ◽  
Plasmodium Berghei ◽  
Packed Cell Volume ◽  
Haematological Parameters ◽  
Antimalarial Agents ◽  
Western Africa ◽  
Methanolic Extracts ◽  
Crude Extracts ◽  
In Vivo Growth

Launaea taraxacifolia and Amaranthus viridis used by people of Western Africa in the treatment of malaria and related symptoms were assessed for their antiplasmodial value against the chloroquine sensitive strain of Plasmodium berghei. Crude extracts (200 mg/kg) and chloroquine (5 mg/kg) were administered to different groups of Swiss mice. The percentage of parasitemia, survival time, and haematological parameters were determined. Both extracts significantly (p<0.05) inhibited parasitemia and improved survival time in infected mice. The crude extracts prevented loss of some haematological parameters. A. viridis had a distinct effect on the packed cell volume. The extract was able to protect the liver from some of the damage. This study however showed that the methanolic extracts of A. viridis and L. taraxacifolia possess antiplasmodial activity. The results of this study can be used as a basis for further phytochemical investigations in the search for new and locally affordable antimalarial agents.

scholarly journals Sequestration of erythrocytes infected with Plasmodium berghei ANKA in BALB/c mice treated with goat bile

2020 ◽  
Vol 4 (2) ◽  
pp. 179
Author(s):  
Kartika Arum Wardani ◽  
Kholida Nur Aini ◽  
Heny Arwati ◽  
Willy Sandhika
Keyword(s):  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Negative Control ◽  
Control Group ◽  
Dependent Manner ◽  
Plasmodium Berghei Anka ◽  
Concentration Dependent Manner ◽  
Control Group Design ◽  
Bile Concentration

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]

scholarly journals In-vivo antimalarial activity of aqueous leaf and bark extracts of Trema orientalis against Plasmodium berghei in mice

2016 ◽  
Vol 41 (2) ◽  
pp. 398-404 ◽  
Author(s):  
Oluwatoyosi Eniola Oyebola ◽  
Olajumoke Abimbola Morenikeji ◽  
Isaiah Oluwafemi Ademola
Keyword(s):  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Trema Orientalis

scholarly journals Antimalarial activity of hydromethanolic extract and its solvent fractions of Vernonia amygdalina leaves in mice infected with Plasmodium berghei

2019 ◽  
Vol 7 ◽  
pp. 205031211984976 ◽  
Author(s):  
Temesgen Bihonegn ◽  
Mirutse Giday ◽  
Getnet Yimer ◽  
Abebe Animut ◽  
Mekonnen Sisay
Keyword(s):  
Weight Loss ◽  
Survival Time ◽  
Rectal Temperature ◽  
Crude Extract ◽  
Plasmodium Berghei ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Vernonia Amygdalina ◽  
Oral Toxicity

Background: Vernonia amygdalina Del. (Asteraceae) is reported to be traditionally used for the treatment of malaria. Based on folkloric repute of this plant in Ethiopian traditional medicine and crude extract-based ethnopharmacological studies conducted in few countries, this study was undertaken to evaluate the in vivo antimalarial activity of 80% methanol extract and its solvent fractions of the leaves of V. amygdalina in mice infected with Plasmodium berghei. Methods: A 4-day suppressive test was conducted on mice infected with P. berghei to find out antimalarial effect of chloroform, butanol and aqueous fractions obtained from the 80% methanol crude extract. In all the activity tests, mice were randomly assigned in five groups (three tests and two controls) of six animals in each and received respective treatments. Data were analyzed using one way analysis of variance followed by Tukey’s post hoc test for multiple comparisons. Results: Acute oral toxicity test showed that all solvent fractions of the leaves of V. amygdalina revealed neither mortality nor overt signs of toxicity up to 2000 mg/kg. This study indicated that the percentage parasitemia suppression of 80% methanol extract was 32.47% (±2.65), 35.40% (±3.14) and 37.67% (±2.50) at 200, 400 and 600 mg/kg, respectively. All doses of the 80% methanol extract of V. amygdalina prolonged survival time and prevented weight loss and packed cell volume reduction in infected mice. All doses of chloroform and butanol fractions significantly suppressed parasitemia (p < 0.05), increased survival time (p < 0.05) compared to negative control and exhibited a significant reduction in rectal temperature (p < 0.05). All solvent fractions significantly prevented weight loss (p < 0.05) at all tested doses. The 80% methanol extract and chloroform and butanol fractions significantly (p < 0.05) prevented further reduction in rectal temperature of P. berghei-infected mice at all doses. Conclusion: The results of this study indicated that 80% methanol extract and solvent fractions of the leaves of V. amygdalina demonstrated promising antimalarial activity. The study corroborated the folklore use of this plant for the treatment of malaria in ethnomedicine in Ethiopia.

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