scholarly journals In vitro and in vivo antiplasmodial activity and cytotoxicity of extracts from Vernonia amygdalina Del. Leaves

2010 ◽  
Vol 9 (S2) ◽  
Author(s):  
Ehimwenma S Omoregie ◽  
Anirban Pal ◽  
Mahendra P Darokar ◽  
Debabrata Chanda ◽  
Brijesh Sisodia
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 ◽  
...  

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

2020 ◽  
Author(s):  
Jinming Guan ◽  
Christina Spry ◽  
Erick T. Tjhin ◽  
Penghui Yang ◽  
Tanakorn Kittikool ◽  
...  

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.


2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Bibianne Waiganjo ◽  
Gervason Moriasi ◽  
Jared Onyancha ◽  
Nelson Elias ◽  
Francis Muregi

Malaria is a deadly disease caused by a protozoan parasite whose mode of transmission is through a female Anopheles mosquito. It affects persons of all ages; however, pregnant mothers, young children, and the elderly suffer the most due to their dwindled immune state. The currently prescribed antimalarial drugs have been associated with adverse side effects ranging from intolerance to toxicity. Furthermore, the costs associated with conventional approach of managing malaria are arguably high especially for persons living in low-income countries, hence the need for alternative and complementary approaches. Medicinal plants offer a viable alternative because of their few associated side effects, are arguably cheaper, and are easily accessible. Based on the fact that studies involving antimalarial medicinal plants as potential sources of efficacious and cost-effective pharmacotherapies are far between, this research was designed to investigate antiplasmodial and cytotoxic activities of organic and aqueous extracts of selected plants used by Embu traditional medicine practitioners to treat malaria. The studied plants included Erythrina abyssinica (stem bark), Schkuhria pinnata (whole plant), Sterculia africana (stem bark), Terminalia brownii (leaves), Zanthoxylum chalybeum (leaves), Leonotis mollissima (leaves), Carissa edulis (leaves), Tithonia diversifolia (leaves and flowers), and Senna didymobotrya (leaves and pods). In vitro antiplasmodial activity studies of organic and water extracts were carried out against chloroquine-sensitive (D6) and chloroquine-resistance (W2) strains of Plasmodium falciparum. In vivo antiplasmodial studies were done by Peter’s four-day suppression test to test for their in vivo antimalarial activity against P. berghei. Finally, cytotoxic effects and safety of the studied plant extracts were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) rapid calorimetric assay technique. The water and methanolic extracts of T. brownii and S. africana and dichloromethane extracts of E. abyssinica, S. pinnata, and T. diversifolia leaves revealed high in vitro antiplasmodial activities (IC50≤10 μg/ml). Further, moderate in vivo antimalarial activities were observed for water and methanolic extracts of L. mollissima and S. africana and for dichloromethane extracts of E. abyssinica and T. diversifolia leaves. In this study, aqueous extracts of T. brownii and S. africana demonstrated high antiplasmodial activity and high selectivity indices values (SI≥10) and were found to be safe. It was concluded that T. brownii and S. africana aqueous extracts were potent antiplasmodial agents. Further focused studies geared towards isolation of active constituents and determination of in vivo toxicities to ascertain their safety are warranted.


Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  

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.


Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 777 ◽  
Author(s):  
Mallika Kumarihamy ◽  
Daneel Ferreira ◽  
Edward Croom ◽  
Rajnish Sahu ◽  
Babu Tekwani ◽  
...  

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.


Planta Medica ◽  
2014 ◽  
Vol 80 (06) ◽  
pp. 482-489 ◽  
Author(s):  
Raymond Muganga ◽  
Luc Angenot ◽  
Monique Tits ◽  
Michel Frédérich

2012 ◽  
Vol 112 (2) ◽  
pp. 637-642 ◽  
Author(s):  
Anil Prakash ◽  
S. K. Sharma ◽  
P. K. Mohapatra ◽  
K. Bhattacharjee ◽  
K. Gogoi ◽  
...  

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