Anti-plasmodial Effects of Zanthoxylum zanthoxyloides

Abstract

Zanthoxylum zanthoxyloides, syn. Fagara zanthoxyloides, is a tree growing in West Africa and is used in traditional medicine against a variety of diseases, including malaria. In the work reported here, root bark and stem bark extracts of this tree, as well as compounds isolated from the extracts, have been investigated for activity in vitro against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. In addition, toxicity against nauplii of the brine shrimp Artemia salina has been studied. Dichloromethane extracts of the root bark and stem bark, and a methanol extract of the stem bark, showed anti-parasitic activity towards chloroquine-sensitive as well as chloroquine-resistant P. falciparum, with IC50 values between 1 and 10 µg/mL. Among the isolated compounds, bis-dihydrochelerythrinyl ether, buesgenine, chelerythrine, γ-fagarine, skimmianine, and pellitorine were the most active, with IC50 values of less than 5 µg/mL. The dichloromethane extracts were toxic to brine shrimp nauplii, with LC50 values of less than 1 µg/mL. Methanol extracts were much less toxic (LC50 between 50 and 100 µg/mL). Among the isolated substances, bis-dihydrochelethrinyl ether was the most toxic (LC50 ca. 2 µg/mL).

Zanthoxylum Species: A Review of Traditional Uses, Phytochemistry and Pharmacology in Relation to Cancer, Infectious Diseases and Sickle Cell Anemia

“…Based on the use of different Z. zanthoxyloides parts for treating malaria ( Adesina 2005 ; Enechi et al, 2019 ), Goodman et al (2019) that four alkaloids, bis-dihydrochelerythrinyl ether, skimmianine, buesgenine and chelerythrine, isolated from roots, root-bark and stem-bark exhibited anti-plasmodial activity against chloroquine-sensitive (3D7) strains of P. falciparum (IC 50 values of 4.3, 0.7, 2.0, and 0.4 μg/ ml, respectively). Previous studies on other alkaloids showed that nitidine from Z. gilletii stem bark exhibited anti-plasmodial activity against P. falciparum strain FcB1 with IC 50 < 5 μg/ml by halting DNA synthesis in the parasite ( Zirihi et al, 2005 ; Zirihi et al, 2009 ).…”

Seasonal Effect on the Chemical Composition, Insecticidal Properties and Other Biological Activities of Zanthoxylum leprieurii Guill. & Perr. Essential Oils

“…Moreover, it is possible that the highlighted activity comes from the presence of minor compounds, as well as from the synergy between different molecules. Nevertheless, studies were carried out on Z. leprieurii and other species of Z. chalybeum and Z. zanthoxyloides plant extracts, showing high anti-plasmodial activities [79][80][81][82], all of which supports the effective use of Zanthoxylum species in traditional medicine for the treatment of malaria.…”

Zanthoxylum Species: A Comprehensive Review of Traditional Uses, Phytochemistry, Pharmacological and Nutraceutical Applications

“…The vast majority of people who use plant extracts as medicine consider them safer compared to synthetic drugs [ 1 ]. In addition, many types of infections, parasitic diseases, and tumors that are resistant to some synthetic drugs have been shown to be treatable using herbal medicines [ 1 , 2 , 3 , 4 , 5 ]. Furthermore, phyto-bioactive compounds have been shown to provide templates that direct the development of some drugs in current use, such as quinine and artemisinins for malaria, and alkaloids and camptothecins for cancer.…”