In Vitro and In Vivo Antimalarial Activities and Toxicological Assessment of Pogostemon Cablin (Blanco) Benth

The aim of this study was to investigate the antimalarial activities and toxicity of Pogostemon cablin extracts. In vitro activities against the chloroquine-resistant Plasmodium falciparum K1 strain were assessed by using the Plasmodium lactate dehydrogenase enzyme (pLDH) assay, while in vivo activity against the Plasmodium berghei ANKA strain in mice was investigated using a 4-day suppressive test. The in vitro and in vivo toxicity were determined in Vero cells and mice, respectively. The ethanolic extract possessed antimalarial activity with an IC50 of 24.49 ± 0.01 µg/ml, whereas the aqueous extract showed an IC50 of 549.30 ± 0.07 µg/ml. Cytotoxic analyses of the ethanolic and aqueous extracts revealed a nontoxic effect on Vero cells at a concentration of 80 µg/ml. Based on a preliminary study of in vitro antimalarial activity, the ethanolic extract was chosen as a potential agent for further in vivo antimalarial activity analysis in mice. The ethanolic extract, which showed no toxic effect on mice at a dose of 2000 mg/kg body weight, significantly suppressed parasitemia in mice by 38.41%, 45.12% and 89.00% at doses of 200, 400 and 600 mg/kg body weight, respectively. In conclusion, this study shows that the ethanolic P. cablin extract possesses in vitro and in vivo antimalarial activity without toxic effects.

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In vivo Neurological, Analgesic and In vitro Antioxidant and Cytotoxic Activities of Ethanolic Extract of Leaf and Stem Bark of Wedelia chinensis

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v22i1.40021 ◽

2019 ◽

Vol 22 (1) ◽

pp. 18-26

Author(s):

Sayema Khanum ◽

Md Shahid Sarwar ◽

Mohammad Safiqul Islam

Keyword(s):

Body Weight ◽

Oral Administration ◽

Radical Scavenging ◽

Ethanolic Extract ◽

Ethanol Extract ◽

Pharmaceutical Journal ◽

Stem Bark ◽

Cytotoxic Activities

Wedelia chinensis is a widely used anti-inflammatory and hepatoprotective medicinal plant in Bangladesh. In this study, analgesic, neurological, antioxidant and cytotoxic activities of the ethanolic extract of leaf and stem bark of W. chinensis were investigated. Oral administration of the ethanolic extract of W. chinensis (200- and 300-mg/kg body weight) was investigated on animal model for neurological activity using open field test and hole cross test. Acetic acid induced writhing method was used to assess the analgesic activity. DPPH (1,1-diphenyl, 2-picryl hydrazyl) radical scavenging assay was used for determining the antioxidant activity, while brine shrimp lethality bioassay was used for investigating cytotoxicity. The ethanol extract of the plant produced significant reduction (P<0.05) of locomotion in both doses (200- and 300-mg/kg body weight) indicating pronounced neurological activity. Oral administration of alcoholic leaves and stem extracts significantly (p < 0.05) inhibited writhing response in mice. The percentage of scavenging of DPPH free radical was found to be concentration dependent with IC50 value of 44.10 ± 0.65 and 38.96 ± 0.50 μg/ml for leaves and stem extracts, respectively. Our findings indicate that W. chinensis may be a source of natural antioxidant with potent analgesic, neurological and cytotoxic activities. Bangladesh Pharmaceutical Journal 22(1): 18-26, 2019

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Antiplasmodial and Cytotoxic Cytochalasins from an Endophytic Fungus, Nemania sp. UM10M, Isolated from a Diseased Torreya taxifolia Leaf

Molecules ◽

10.3390/molecules24040777 ◽

2019 ◽

Vol 24 (4) ◽

pp. 777 ◽

Cited By ~ 7

Author(s):

Mallika Kumarihamy ◽

Daneel Ferreira ◽

Edward Croom ◽

Rajnish Sahu ◽

Babu Tekwani ◽

...

Keyword(s):

Mouse Model ◽

Solid Tumor ◽

Endophytic Fungus ◽

Antimalarial Activity ◽

Vero Cells ◽

Antiplasmodial Activity ◽

Etoac Extract ◽

Bioassay Guided Fractionation

Bioassay-guided fractionation of an EtOAc extract of the broth of the endophytic fungus Nemania sp. UM10M (Xylariaceae) isolated from a diseased Torreya taxifolia leaf afforded three known cytochalasins, 19,20-epoxycytochalasins C (1) and D (2), and 18-deoxy-19,20-epoxy-cytochalasin C (3). All three compounds showed potent in vitro antiplasmodial activity and phytotoxicity with no cytotoxicity to Vero cells. These compounds exhibited moderate to weak cytotoxicity to some of the cell lines of a panel of solid tumor (SK-MEL, KB, BT-549, and SK-OV-3) and kidney epithelial cells (LLC-PK11). Evaluation of in vivo antimalarial activity of 19,20-epoxycytochalasin C (1) in a mouse model at 100 mg/kg dose showed that this compound had weak suppressive antiplasmodial activity and was toxic to animals.

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In VitroandIn VivoAntimalarial Activities of T-2307, a Novel Arylamidine

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.05856-11 ◽

2012 ◽

Vol 56 (4) ◽

pp. 2191-2193 ◽

Cited By ~ 7

Author(s):

Akiko Kimura ◽

Hiroshi Nishikawa ◽

Nobuhiko Nomura ◽

Junichi Mitsuyama ◽

Shinya Fukumoto ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Body Weight ◽

Broad Spectrum ◽

Antimalarial Activity ◽

Liver Stage ◽

Rodent Malaria ◽

Content Type ◽

Clinically Significant

ABSTRACTT-2307, a novel arylamidine, has been shown to exhibit broad-spectrum antifungal activities against clinically significant pathogens. Here, we evaluated thein vitroandin vivoantimalarial activity of T-2307. The 50% inhibitory concentrations (IC50s) of T-2307 againstPlasmodium falciparumFCR-3 and K-1 strains were 0.47 and 0.17 μM, respectively. T-2307 at 2.5 to 10 mg/kg of body weight/day exhibited activity against blood stage and liver stage parasites in rodent malaria models. In conclusion, T-2307 exhibitedin vitroandin vivoantimalarial activity.

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Preventive effects of the antioxidant and antigenotoxic Achyrocline satureioides extract against zearalenone-induced mammal cytogenotoxicity and histological damage

World Mycotoxin Journal ◽

10.3920/wmj2020.2571 ◽

2021 ◽

pp. 1-10

Author(s):

M.C. Sabini ◽

L.N. Cariddi ◽

F.M. Escobar ◽

F. Mañas ◽

D. Roma ◽

...

Keyword(s):

Lipid Peroxidation ◽

Body Weight ◽

Aqueous Extract ◽

Vero Cells ◽

Neutral Red ◽

In Vivo Studies ◽

Low Cytotoxicity ◽

Achyrocline Satureioides

Zearalenone (ZEN), a Fusarium’s mycotoxin, is immunotoxic, genotoxic, hepatonephrotoxic and, affects the reproductive system. ZEN induces toxic and genotoxic effects on humans and other animals. Achyrocline satureioides has several medicinal properties. Moreover, the aqueous extract of A. satureioides is a safe agent that exerts low cytotoxicity and no genotoxicity. This extract is a promissory candidate to counteract ZEN effects. The present study aimed to investigate the capacity of cold aqueous extract from A. satureioides to protect against ZEN multi-target toxicity in different experimental mammal models. Anticytotoxicity was evaluated by neutral red uptake and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium reduction assays. Comet assay and micronuclei test, oxidative stress (TBARs), and histopathological damage were evaluated in Balb/C mice. Anticytotoxic studies indicated that cold aqueous extract (100 and 300 μg/ml) protected from damage induced by ZEN (50 μg/ml) on Vero cells. In vivo studies indicated that ZEN (40 mg/kg body weight) induced an increase of genotoxicity: micronuclei (34 MNPCE/1000 PCE) and increase of damage (tail moment) in blood cells. Also, it increased lipid peroxidation in liver and kidneys and generated several histopathological alterations in both organs. Cold aqueous extract (100 mg/kg body weight) protected from genotoxicity induced by ZEN in both tests. Cold aqueous extract, also, reduced the lipid peroxidation and histopathological damage in liver and kidneys. In conclusion, the cold aqueous extract of A. satureioides that contains bioactive flavonoids prevents the multi-target toxicity induced by ZEN improving all the parameters evaluated in vitro and in vivo, which is a valuable and original finding in order to develop future treatments for human and veterinary medicine.

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Antimalarial Activity ofCocos nuciferaHusk Fibre: Further Studies

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/742476 ◽

2013 ◽

Vol 2013 ◽

pp. 1-9 ◽

Cited By ~ 8

Author(s):

J. O. Adebayo ◽

E. A. Balogun ◽

S. O. Malomo ◽

A. O. Soladoye ◽

L. A. Olatunji ◽

...

Keyword(s):

Body Weight ◽

Ethyl Acetate ◽

Ethyl Acetate Extract ◽

Antimalarial Activity ◽

Cocos Nucifera ◽

Normal Liver ◽

Creatinine Concentration ◽

Extract Fraction

In this study, the antimalarial and toxicity potentials of husk fibre extracts of five Nigerian varieties ofCocos nuciferawere evaluatedin vitro. The only active extract fraction, West African Tall (WAT) ethyl acetate extract fraction, was then evaluated for its phytochemical constituents, antimalarial and toxicity potentials at varying doses (31.25–500 mg/kg body weight) using various organ function indices. The results revealed that WAT ethyl acetate extract fraction (WATEAEF) contained alkaloids, tannins, and flavonoids and was active againstPlasmodium falciparumW2 strain maintained in continuous culture, with a selectivity index of 30.3. The same extract fraction was activein vivoagainstPlasmodium bergheiNK65, causing more than 50% reduction in parasitaemia on days 4 and 6 after inoculation at various doses administered. WATEAEF did not significantly alter (P>0.05) function indices of the liver and cardiovascular system at all doses administered but significantly increased (P<0.05) plasma creatinine concentration at 250 and 500 mg/Kg body weight compared to controls. The results of this study suggest that WATEAEF possesses antimalarial activity and may not adversely affect normal liver function nor predispose subjects to cardiovascular diseases but may impair normal kidney function at higher doses. Further studies are underway to isolate the active principles.

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Antioxidant and antimalarial properties of Sophora exigua Craib. root extract in Plasmodium berghei-infected mice

Tropical Medicine and Health ◽

10.1186/s41182-021-00314-2 ◽

2021 ◽

Vol 49 (1) ◽

Author(s):

Kantarakorn Kaewdana ◽

Prapaporn Chaniad ◽

Pitchanee Jariyapong ◽

Arisara Phuwajaroanpong ◽

Chuchard Punsawad

Keyword(s):

Body Weight ◽

Aqueous Extract ◽

Plasmodium Berghei ◽

Antioxidant Activities ◽

Antimalarial Activity ◽

Ethanolic Extract ◽

Histopathological Analysis ◽

Root Extract ◽

Breast Milk Production

Abstract Background Sophora exigua Craib. is commonly used in Thailand to reduce fever and increase postpartum breast milk production in women who have hypogalactia. However, there has been no report on the antioxidant and antimalarial properties of this plant. This study aimed to investigate the antioxidant and antimalarial activities of S. exigua root extract and to evaluate its acute toxicity in mice to confirm its safety. Methods The in vitro antioxidant activities were determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide radical, and hydroxyl radical scavenging assays. The in vivo antioxidant activities were determined by detecting the malondialdehyde (MDA) content and superoxide dismutase (SOD) activity in the livers of malaria-infected mice. The in vivo antimalarial activity was determined by Peters’ 4-day suppressive test in mice infected with Plasmodium berghei ANKA and orally administered S. exigua root aqueous and ethanolic extracts at different doses (200, 400, and 600 mg/kg body weight). In addition, the acute oral toxicity of the plant extracts was assessed in mice at a dose of 2000 mg/kg body weight. Results The ethanolic extract of S. exigua root exhibited inhibition of DPPH radicals, superoxide anions, and hydroxyl radicals, with half maximal inhibitory concentration (IC50) values of 24.63 ± 1.78, 129.78 ± 0.65, and 30.58 ± 1.19 μg/ml, respectively. Similarly, research on the in vivo antioxidant activity indicated that the ethanolic extract of S. exigua root exerted a stronger effect than the aqueous extract. The aqueous extract at doses of 200, 400, and 600 mg/kg had stronger antimalarial activity than the ethanolic extract. The aqueous extract at 600 mg/kg exhibited 60.46% suppression of parasitemia. Increased levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP) and blood urea nitrogen (BUN) were detected in the mice treated with 2000 mg/kg ethanolic extract, which was related to the results of histopathological analysis of liver tissue, showing ballooning degeneration of hepatocytes, diffuse hepatic hemorrhage, and infiltration of inflammatory cells. Conclusions This study demonstrated that the ethanolic S. exigua root extract possessed antioxidant properties, and the aqueous extract also had antimalarial activity. Therefore, this plant is an alternative source of new antioxidant and antimalarial agents.

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Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA ◽

10.20473/jfiki.v3i1.4088 ◽

2017 ◽

Vol 3 (1) ◽

pp. 17 ◽

Cited By ~ 1

Author(s):

Wiwied Ekasari ◽

Nindya Tresiana ◽

Suciati Iryani ◽

Tutik Sri Wahyuni ◽

Heny Arwaty

Keyword(s):

Plasmodium Falciparum ◽

Methanol Extract ◽

Antimalarial Activity ◽

Ethanolic Extract ◽

Ethanol Extract ◽

In Vivo Test ◽

Ic50 Value ◽

Cassia Spectabilis

Background: Antimalarial screening against nine species of the genus Cassia showed that the methanol extract of leaves Cassia spectabilis have the highest activity. Since it will be used as a traditional medicine, hence it is needed further studies of antimalarial activity of these plants by choosing a safer solvent, namely ethanol. Objective: In vitro anti-malarial activity against Plasmodium falciparum was conducted using the method of Trager and Jensen. Methods: The serial solution tested were: 100, 10, 1, 0.1 and 0.01 µg/ mL, while the in vivo test was performed based on Peter’s test (The days suppressive test) that using P. berghei (strain ANKA) infected mice. Results: The results showed that ethanolic extract of C. spectabilis leaves has inhibitory activity against P. falciparum with IC50 value of 12.52 µg/ mL and against P. berghei with ED50 value of 131.5 mg/kg body weight. Conclusions: A further study to see the potential of ethanol extract from C. Spectabilis leaves as anti-malaria is warranted.

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Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA ◽

10.20473/jfiki.v3i12016.17-21 ◽

2017 ◽

Vol 3 (1) ◽

pp. 17

Author(s):

Wiwied Ekasari ◽

Nindya Tresiana ◽

Suciati Iryani ◽

Tutik Sri Wahyuni ◽

Heny Arwaty

Keyword(s):

Plasmodium Falciparum ◽

Methanol Extract ◽

Antimalarial Activity ◽

Ethanolic Extract ◽

Ethanol Extract ◽

In Vivo Test ◽

Ic50 Value ◽

Cassia Spectabilis

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

Medicinal Chemistry ◽

10.2174/1573406416666200817160708 ◽

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.

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Stage-dependent effect of deferoxamine on growth of Plasmodium falciparum in vitro

Blood ◽

10.1182/blood.v76.6.1250.1250 ◽

1990 ◽

Vol 76 (6) ◽

pp. 1250-1255 ◽

Cited By ~ 36

Author(s):

S Whitehead ◽

TE Peto

Keyword(s):

Plasmodium Falciparum ◽

Growth Inhibition ◽

Antimalarial Activity ◽

Clinical Malaria ◽

Inhibitory Effect ◽

Parasite Development ◽

And Control ◽

Speed Of Onset

Abstract Deferoxamine (DF) has antimalarial activity that can be demonstrated in vitro and in vivo. This study is designed to examine the speed of onset and stage dependency of growth inhibition by DF and to determine whether its antimalarial activity is cytostatic or cytocidal. Growth inhibition was assessed by suppression of hypoxanthine incorporation and differences in morphologic appearance between treated and control parasites. Using synchronized in vitro cultures of Plasmodium falciparum, growth inhibition by DF was detected within a single parasite cycle. Ring and nonpigmented trophozoite stages were sensitive to the inhibitory effect of DF but cytostatic antimalarial activity was suggested by evidence of parasite recovery in later cycles. However, profound growth inhibition, with no evidence of subsequent recovery, occurred when pigmented trophozoites and early schizonts were exposed to DF. At this stage in parasite development, the activity of DF was cytocidal and furthermore, the critical period of exposure may be as short as 6 hours. These observations suggest that iron chelators may have a role in the treatment of clinical malaria.

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