Antiplasmodial activity

Very recently elisapterosin A (30) [18, 19] was found to exhibit strong antiplasmodial activity (IC5010 pg/ml) against Plasmodium falciparum, the parasite responsible for the most severe forms of malaria. 

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Barbaras D, Kaiser M, Brun R, Gademann K. (2008) Potent and selective antiplasmodial activity of the cyanobacterial alkaloid nostocarbohne and its dimers. Bioorg Med Chem Lett 18 4413 4415. 

Troupin has also been reported . These alkaloids were found to exhibit antimicrobial and antiplasmodial activities. Epinetrum villosum is a twining liana, growing in secondary forests in the coastal areas in Congo and Angola and is used in traditional medical for the treatment of fever, malaria and dysentery . The genus Cissampelos contains cissampareine, which has potential medicinal uses, but it is also psychoactive. It is a principal alkaloid of dawidjiewortel (Cissampelos capensis), which grows in South Africa. 

Sairafianpour, M. et al., Leishmanicidal and antiplasmodial activity of constituents of Smirnowia iranica. Journal of Natural Products, 65, 1754, 2002. 

From dried leaves of a Brazilian plant, a triterpene ozonide 165 was isolated. It was also obtained at — 78 °C in hexane by ozonolysis of its precursor 164 isolated from the same plant. In contrast to natural endoperoxides, such as artemisinin, this 1,2,4-trioxolane does not show antiplasmodial activity (Equation 13) <2003AP205>. 

Wu X, Tiekink ERT, Kostetski I, Kocherginsky N, Tan ALC, Khoo SB, Wilairat P, Go M-L (2006) Antiplasmodial activity of ferrocenyl chalcones investigations into the role of ferrocene. Eur J Pharm Sci 27 175-187... 

The results showed that the location of ferrocene influenced the ease of oxidation of iron II and the polarity of the carbonyl linkage. These parameters were found to influence antiplasmodial activity. Better antimalarial activities were obtained when the ferrocene moiety is adjacent to the carbonyl group [101]. 

For the determination of the antiplasmodial activity of the compounds, the multi-resistant Dd2 strain of Plasmodium falciparum was used and [8-3H]-hypoxanthine incorporated into the parasitic nucleic acids measured. The plasmodia were incubated with 0.3% parasitemia and an erythrocyte hematocrit of 2.5% in the presence of different concentrations of selected experimental agents in a final volume of 200 xl. The medium employed was RPMI 1640 containing 10% of heat-treated human serum and 3 mg/1 of gentamycin. In the incubations, the concentrations of the compounds varied from 0.3 to 100 xM. After 48 hours, each batch was treated with 50 xl [8-3H]hypoxanthine and incubated additional 18 hours. Testing results are provided in Table 1. 

II. Antiplasmodial Activity Against the 3D7 Chloroquine-sensitive Strain Antiplasmodial activity against the 3D7 chloroquine-sensitive strain of P. falciparum was determined using the method of Wright (1). Testing results are provided in Table 1. 

Loyola, L. A., Bdrquez, J., Morales, G., San-Martin, A., Darias, J., Flores, N., Gimenez, A. 2004. Mulinane-type diterpenoids from Azorella compacta display antiplasmodial activity. Phytochemistry 65 1931-1935. 

Vernonia oligocephala (DC.) Sch. Bip. Ex Walp. lihlunguhlungu, wiletee] (Asteraceae) root bark decoction is used for diarrhoea. The root bark contains flavonoids, glycosides, polyphenols, saponins and steroids 15). The plant is also used for diabetes and stomachache 28). The plant has weak antiplasmodial activity 39). 

Antiplasmodial Activity of Twenty Essential Oils from Malagasy Aromatic Plants. 

Table I. The Main Chemical Constituents and Antiplasmodial Activity of Twenty Essential oils Against Plasmodium falciparum FCM29 strain...

The antiplasmodial activity of five akaloids (y - fagarine, N-benzoyltryamine, skimmianine, dictamnine and 4-methoxy-l methyl-2(lH)-quinoline), extracted by decoction from Zanthoxylum tsihanimposa stem bark were tested upon P. falciparum. The quinoline alkaloid y-fagarine was the most potent of five alkaloids, being found to be 3. 4 times more active than dictamnine and 1.4 times more active than skimmianine. The presence of the methoxy group in positions C4 and C8 appears to be important for bioactivity (20). 

Argemone subfusiformis dried leaves, flowers and seeds were extracted with ethanol-water (70-30%) for 48 h, the aqueous-solution obtained was evaporated under vacuum and the resdue was directly assayed. The antiplasmodial activity was good (24), and extracts were rich in isoquinolleinic Akaloids. In above ground parts, protopine, berberine and allocryptopine were identified (27). According to Sriwilaijaron et al. (28) berberine prevents the development of Plasmodium falciparum by inhibition of its telomerase activity. 

Garcinia kola Heckel (stem bark) GBi (176). GBi (176) exhibited a-glucosidase and aromatase inhibitory activities, as well as antiplasmodial activity, but was not toxic against cell lines tested. GB] (176) may be a potential dietary supplement or phytomedicine for the prevention of breast cancer and type 2 diabetes mellitus. Antia et ah, 2010[194]. 

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