Possible Artefacts in the in vitro Determination of Antimalarial Activity of Natural Products that Incorporate into Lipid Bilayer: Apparent Antiplasmodial Activity of Dehydroabietinol, a Constituent of Hyptis suaveolens

In our study, the binding affinities of selected natural products towards PfTrxR, PfGR, human TrxR and human GR were determined using a mass spectrometry based ligand binding assay. The in vitro antimalarial activity and cytotoxicity of these ligands were also determined. Catharanthine, 11-(OH)-coronaridine, hernagine, vobasine and hispolone displayed antiplasmodial activity against PfK1 (IC50 = 0.996–3.63 μg/mL).

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Assessment of Antimalarial Activity againstPlasmodium falciparumand Phytochemical Screening of Some Yemeni Medicinal Plants

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/nem148 ◽

2009 ◽

Vol 6 (4) ◽

pp. 453-456 ◽

Cited By ~ 21

Author(s):

Mohammed A. Alshawsh ◽

Ramzi A. Mothana ◽

Hassan A. Al-shamahy ◽

Salah F. Alsllami ◽

Ulrike Lindequist

Keyword(s):

Medicinal Plants ◽

Antimalarial Activity ◽

Traditional Healers ◽

Antiplasmodial Activity ◽

World Health ◽

Moderate Activity ◽

Phytochemical Screening ◽

Cissus Rotundifolia ◽

Health Organization

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa,Azadirachta indica,Cissus rotundifolia,Echium rauwalfii,Dendrosicyos socotranaandBoswellia elongata) commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates ofPlasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured byin vitromicro test (Mark III) according to World Health Organization (WHO) 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50values less than 4 µg/ml, namely the water extracts ofA. fruticosa,A. indicaandD. socotrana. Six extracts showed moderate activity with IC50values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides.

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In Vitro Antimalarial Activity of Extracts of Some Indigenous Plant Species in Kebbi State

UMYU Journal of Microbiology Research (UJMR) ◽

10.47430/ujmr.2052.001 ◽

2020 ◽

pp. 1-10

Author(s):

Aisha Abdulrazak ◽

Keyword(s):

Medicinal Plants ◽

Aqueous Extract ◽

Antimalarial Activity ◽

Antimicrobial Activities ◽

Antiplasmodial Activity ◽

Phytochemical Screening ◽

Indigenous Plants ◽

Traditional Use ◽

Water As Solvent

The search for antimalarial compounds has been necessitated by the resistance of Plasmodium falciparum to almost all antimalarial drugs. The aim of this research was to determine in-vitro antimalarial activity of extracts of some indigenous plants species in Kebbi State. Plant extraction was carried-out by maceration using ethanol and water as solvent. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates of P. falciparum using WHO method of in-vitro micro test. Phytochemical screening was also carried out on the extract to deduce the active chemicals present in the plant extract. All plant extracts demonstrate dose dependent antimicrobial activities with IC50 Less than 50%. However highest growth inhibition of the P. falciparum was demonstrated by aqueous and ethanol extract of A. indica with IC50 7.4µg/ml and 8.6µg/ml respectively followed by ethanol and aqueous extract of C. occidentalis with IC50 15.3µg/ml and 18.0µg/ml respectively. Least antimalarial activity was demonstrated by aqueous extract of M. oleifera with IC50 33.5µg/ml while ethanolic extract of M. oleifera demonstrated IC50 of 20.50µg/ml. M. indica ethanolic and aqueous extract also demonstrated moderate antimalarial activity with IC50 18.8µg/ml and 24.5µg/ml. The phytochemical screening of medicinal plants showed the presence of tannins, saponins, alkaloids, flavonoid, phenol and cardiac glycosides in the extracts, which may be responsible for the antiplasmodial activity. This result justifies the traditional use of the plant in malaria treatment and further research is suggested to identify and characterize the active principles from the plants. Keywords: Antimalaria, Invitro, Medicinal Plants, Malaria, Kebbi

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In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.01995-20 ◽

2020 ◽

Author(s):

Fidelia Ijeoma Uche ◽

Xiaozhen Guo ◽

Jude Okokon ◽

Imran Ullah ◽

Paul Horrocks ◽

...

Keyword(s):

Metabolic Pathways ◽

High Performance ◽

Antimalarial Activity ◽

Biological Activities ◽

Antiplasmodial Activity ◽

Survival Times ◽

Antiproliferative Effects ◽

Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

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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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The Fungal Metabolites with Potential Antiplasmodial Activity

Current Medicinal Chemistry ◽

10.2174/0929867325666180313105406 ◽

2018 ◽

Vol 25 (31) ◽

pp. 3796-3825 ◽

Cited By ~ 1

Author(s):

Bin Yang ◽

Jingxia Huang ◽

Xuefeng Zhou ◽

Xiuping Lin ◽

Juan Liu ◽

...

Keyword(s):

Natural Products ◽

Antimicrobial Agents ◽

Antimalarial Activity ◽

Management Strategies ◽

Marine Fungus ◽

Chemical Diversity ◽

Biologically Active ◽

Antiplasmodial Activity ◽

Marine Environments ◽

Tropical Regions

Malaria caused by Plasmodium parasites is amongst many prevalent public health concerns in several tropical regions of the world. Nowadays, the parasite resistance patterns to most currently used drugs in therapy and insecticides have created an urgent need for new chemical entities exhibiting new modes of action and management strategies. Fungus has been proven to be an excellent source of biologically active compounds, which have been screened for antiplasmodial activity as potential sources of new antimalarial drugs. This review summarizes the current 255 natural products from fungus, which may possess antimalarial activity and can be classified as sesquiterpenes, diterpenes, sesterterpenes, alkaloids, peptides depsipeptides, xanthones, anthraquinones, anthrones, bioxanthracenes, bixanthones, preussomerins, depsidones, phenols, trichothecenes, azaphliones, macrolides, and steroids. However, the treatments available for malaria are limited. Thus, the identification of novel antimicrobial agents should be continued, and all possible strategies should be explored. Carrying forward the antimalarial screening in exited terrestrial and marine natural products library, and finding the new natural products in new resources, particularly those living in marine environments, are still important approaches to find new antimalarial agents. Unusual marine environments are associated with chemical diversity, leading to a resource of novel active substances for the development of bioactive products. Finding new antimalarial natural products in marine fungus, particularly those living in deep-sea and special marine environments, is an important approach to identify novel active agents.

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Antiplasmodial activity of faloak bark (Sterculia quadrifida, R.Br.) extract from East Nusa Tenggara, Indonesia

Indonesian Journal of Pharmacology and Therapy ◽

10.22146/ijpther.1975 ◽

2021 ◽

Vol 2 (2) ◽

Author(s):

Priska Ernestina Tenda ◽

Maria Hilaria ◽

Arba Pramundita Ramadani

Keyword(s):

Antimalarial Activity ◽

Ethanolic Extract ◽

Antiplasmodial Activity ◽

Current Development ◽

Antimalarial Drug Resistance ◽

Falciparum Strain ◽

Ic50 Value ◽

Endemic Medicinal Plant ◽

The Relationship

The current development of antimalarial drug resistance encourages researchers to discover and develop novel antimalarials. One of its alternatives for antimalarial discovery is using medicinal plants remembering the success of artemisinin. Sterculia quardrifida R. Br. bark, locally name as faloak, is an endemic medicinal plant from East Nusa Tenggara that has been used traditionally to treat malaria. However, its antimalarial activity has not been investigated, yet. This study was aimed to evaluate the antiplasmodial activity of ethanolic extract of faloak bark against Plasmodium falciparum in vitro. Using FCR-3 P. falciparum strain, the ethanolic extract was evaluated on various concentration (1, 10, 50, and 100 μg/mL, respectively). The IC50 value was determined by the relationship between concentration and percentage of growth inhibition. The result showed that the percentage of inhibition of P. falciparum was concentration dependent, higher concentration resulting on higher percentage of inhibition with the IC50 42.399 ± 9.517 μg/mL. It can be concluded that the ethanolic extract of faloak bark have moderate antiplasmodial activity against P. falciparum in vitro.

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Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate

Journal of Tropical Medicine ◽

10.1155/2011/579518 ◽

2011 ◽

Vol 2011 ◽

pp. 1-6 ◽

Cited By ~ 27

Author(s):

Kirti Mishra ◽

Aditya P. Dash ◽

Nrisingha Dey

Keyword(s):

Plasmodium Falciparum ◽

Life Span ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Andrographis Paniculata ◽

Antiplasmodial Activity ◽

Template Molecule

Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plantAndrographis paniculata. The compound was found to have potent antiplasmodial activity when tested in isolation and in combination with curcumin and artesunate against the erythrocytic stages ofPlasmodium falciparum in vitroandPlasmodium bergheiANKAin vivo. IC50s for artesunate (AS), andrographolide (AND), and curcumin (CUR) were found to be 0.05, 9.1 and 17.4 μM, respectively. The compound (AND) was found synergistic with curcumin (CUR) and addictively interactive with artesunate (AS).In vivo, andrographolide-curcumin exhibited better antimalarial activity, not only by reducing parasitemia (29%), compared to the control (81%), but also by extending the life span by 2-3 folds. Being nontoxic to thein vivosystem this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.

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In Vivo Antiplasmodial Activity of Terminalia mantaly Stem Bark Aqueous Extract in Mice Infected by Plasmodium berghei

Journal of Parasitology Research ◽

10.1155/2020/4580526 ◽

2020 ◽

Vol 2020 ◽

pp. 1-9

Author(s):

Mariscal Brice Tchatat Tali ◽

Cedric Derick Jiatsa Mbouna ◽

Lauve Rachel Yamthe Tchokouaha ◽

Patrick Valere Tsouh Fokou ◽

Jaures Marius Tsakem Nangap ◽

...

Keyword(s):

Acute Toxicity ◽

Aqueous Extract ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Lethal Dose ◽

Stem Bark ◽

Antiplasmodial Activity ◽

Bark Extract

Background. Terminalia mantaly is used in Cameroon traditional medicine to treat malaria and related symptoms. However, its antiplasmodial efficacy is still to be established. Objectives. The present study is aimed at evaluating the in vitro and in vivo antiplasmodial activity and the oral acute toxicity of the Terminalia mantaly extracts. Materials and Methods. Extracts were prepared from leaves and stem bark of T. mantaly, by maceration in distilled water, methanol, ethanol, dichloromethane (DCM), and hexane. All extracts were initially screened in vitro against the chloroquine-resistant strain W2 of P. falciparum to confirm its in vitro activity, and the most potent one was assessed in malaria mouse model at three concentrations (100, 200, and 400 mg/kg/bw). Biochemical, hematological, and histological parameters were also determined. Results. Overall, 7 extracts showed in vitro antiplasmodial activity with IC50 ranging from 0.809 μg/mL to 5.886 μg/mL. The aqueous extract from the stem bark of T. mantaly (Tmsbw) was the most potent (IC50=0.809 μg/mL) and was further assessed for acute toxicity and efficacy in Plasmodium berghei-infected mice. Tmsbw was safe in mice with a median lethal dose (LD50) higher than 2000 mg/kg of body weight. It also exerted a good antimalarial efficacy in vivo with ED50 of 69.50 mg/kg and had no significant effect on biochemical, hematological, and histological parameters. Conclusion. The results suggest that the stem bark extract of T. mantaly possesses antimalarial activity.

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Aktivitas Antimalaria Ekstrak Kasar Etanol dan Fraksi n-Heksana Rumput Bambu (Lophatherum gracile B.) secara in Vitro

ALCHEMY ◽

10.18860/al.v6i1.6766 ◽

2018 ◽

Vol 6 (1) ◽

pp. 18

Author(s):

Ella Wulandari ◽

Dewi Yuliani ◽

Elok Kamilah Hayati ◽

Roihatul Muti'ah

Keyword(s):

Mass Spectrometry ◽

Plasmodium Falciparum ◽

Liquid Chromatography ◽

Antimalarial Activity ◽

Ethanol Extract ◽

Hexane Fraction ◽

Liquid Chromatography Mass Spectrometry ◽

Mosquito Bite

Malaria is a disease caused by infectious parasite Plasmodium falciparum and can be transmitted through mosquito bite. The aim of this research was to study antimalarial activity in vitro on crude ethanol extract and n-hexane fraction of bamboo grass (Lophatherum gracile B.). Extraction was carried out by ethanol 80% solvent and fractionation was conducted by n-hexane. Determination of antimalarial activity was subjected to P. falciparum strain 3D7. According to phytochemical test, crude ethanol extract contained tannin and terpenoid, whilst n-hexane fraction contained tannin and steroid. The capability of crude ethanol extract and n-hexane fraction to inhibit P. falciparum was represented by IC50 value. The value of both samples respectively was 12.49 and 61.49 µg/mL. Identification based on LC-MS (liquid chromatography-mass spectrometry), n-hexane fraction shown the presence of tannin and steroid compounds. Malaria merupakan penyakit yang disebabkan oleh infeksi parasit Plasmodium falciparum yang dapat ditularkan melalui gigitan nyamuk. Penelitian ini bertujuan untuk mengetahui aktivitas antimalaria secara in vitro pada ekstrak kasar etanol dan fraksi n-heksana rumput bambu (Lophatherum gracile B.). Proses ekstraksi dilakukan dengan pelarut etanol 80% dan fraksinasi dengan n-heksana. Uji aktivitas antimalaria dilakukan pada parasit P. falciparum strain 3D7. Hasil uji fitokimia menunjukkan ekstrak etanol mengandung tanin dan terpenoid, sedangkan fraksi n-heksana mengandung tanin dan steroid. Kemampuan ekstrak etanol dan fraksi n-heksana dalam menghambat parasit P. falciparum menghasilkan nilai IC50 masing-masing sebesar 12,49 dan 61,49 µg/mL. Identifikasi senyawa dengan KC-SM (kromatografi cair-spektrometri massa) pada fraksi n-heksana menunjukkan adanya senyawa tanin dan steroid.

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