Antiplasmodial

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. 

Chalcones are one of the classes of flavonoids well known for their antiplasmodial properties. Licochalcone A (65), isolated from Chinese licorice roots, was shown to display strong in vitro activity against both chloroquine-susceptible (3D7) and chloroquine-resistant (Dd2) P. falciparum strains it also displayed a strong in vivo acitivity in mice infected with P. yoelii, when administered intraperitoneally or orally for 3 to 6 days. The compound appeared to inhibit the growth of the parasites at all stages (rings, trophozoites, and schizonts). Although licochalcone and some derivatives interred the clinical trials as anti-malarials, none of them have ever made it to the market due to severe toxicity observed in phase II clinical trials. 

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. 

Kirsch G Koeng GM, Wright AD, Kamisnky RA. (2000) New bioactive sesterterpene and antiplasmodial alkaloids from marine sponge Hyrtios. JNat Prod 63 825-829. 

Efferth T. (2007) Willmar Schwabe Award 2006 Antiplasmodial and antitumor activity of artemisinin — from bench to bedside. Planta Med 73 299-309. 

QUINIDINE GLUCONATE - P. falciparum malaria The following 2 regimens are effective empirically. As soon as practical, institute standard oral antiplasmodial therapy. 

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. 

Staerk, D., Lemmich, E., Christensen, J., Kharazmi, A., Olsen, C. E. and Jaroszewski, J. W. 2000. Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras. Planta Medica, 66 531-536. 

Frederich, M., Tits, M. and Angenot, L. 2003. Indole alkaloids from Strychnos species and their antiplasmodial and cytotoxic activities. Chemistry of Natural Compounds, 39(6) 513-519. 

Kohler, I. et al.. In vitro antiplasmodial investigation of medicinal plants from El Salvador, Z. Naturforsch., 58c, 277, 2002. 

Kraft, C. et al., Andinermals A-C, antiplasmodial constituents from Andira inermis. Phytochemistry, 58, 769, 2001. 

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

Macleaya cordata (Willd.) R. Br. Bo Lou Hui (whole plant including root, fruit) Sanguinarine, oxysanguinarine, ethoxysanguinarine, protopine, alpha-allocryptopine, bocconine, chelerythrine, coptisine, herberinecorysamine, bocconoline, ethoxychelerythrine, chelilutine, chelirubine.33 This herb is toxic. Antiplasmodial, treat vaginal trichomonas, antibacterial. 

Senecio argunensis Turcz. S. nemorensis L. S. scandens Buch-Ham ex D. Don Qian Li Guang (Ragwort) (aerial part) Lavoxanthin, macrophylline, cynarin, chlorogenic acid, chrysanthemaxanthin, sarracine.33,48 Antibacterial, antiplasmodial, treat acute bacterial dysentery and bronchitis. 

Verbena officinalis L. V. oxysepalum Turcz. Ma Bian Cao (Vervain) (aerial part) Verbenalin, verbenalol, adenosine, tannins, essential oils.33 Antiplasmodial, antibacterial, antitoxin, anti-inflammatory. 

Wei X, Rodriguez AD, Baran P, Raptis RG, Sanchez JA, Ortega-Barria E, Gonzalez J (2004) Antiplasmodial Cembradiene Diterpenoids from a Southwestern Caribbean Gorgonian Octocoral of the Genus Eunicea. Tetrahedron 60 11813... 

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]. 

The antimalarial activity of FQ was initially compared with that of the purely organic CQ in an effort to understand how the presence of the ferrocene contributes to the antiplasmodial property. Over the years, the mechanism of CQ has been (and is still) the subject of many discussions and arguments. Nevertheless, there is strong evidence that the action of CQ is linked to its localization in the DV of the parasite and to the inhibition of the formation of hemozoin ([37], see [155-157]). 

DNA (intercalation) (mAChR, nAChR, RNA synthesis) [anti-amoebic, anticancer, antiplasmodial, apoptotic, poison, apoptotic, toxic]... 

A special problem arose with respect to the antiplasmodial drugs chloroquine (Resochin) and quinacrine (Atebrin). Plasmodia can not be propagated in cell-free lifeless media and the limited availability of erythrocytic plasmodial cultures severely limits biochemical or molecular pharmacological studies on the action of antimalarials. The actions of chloroquine and quinacrine were, therefore, studied in Bacillus megaterium or E. coli, respectively 22 ... 

---