Plant Terpenoids as Lead Compounds Against Malaria and Leishmaniasis

Temperate Zone Plant Natural Products—A Novel Resource for Activity against Tropical Parasitic Diseases

“…Of these 38 compounds, 71% were terpenes with all four parasites showing sensitivity to multiple terpenoids. This is unsurprising, as terpenoids, and sesquiterpenes in particular, have previously been reported to have broad anti-plasmodial and anti-kinetoplastid activity [ 33 , 34 ]. For example, the sesquiterpene 701158, isolated from Arnica montana (commonly known as Mountain Tobacco) was identified as a hit in all parasite screens.…”

“…Similarly, bisobolane sesquiterpene glycosides isolated from Phyllanthus acuminatus, and similar in structure to the phyllanthostatins [ 35 , 36 ], were identified as initial hits against all parasites in this study except L. mexicana . The abietane diterpenoids 700014 and 700063 were identified in the T. brucei and T. evansi screens, respectively, and represent a class of plant-derived natural product known to have a wide range of growth inhibitory activity against L. donovani , L. major , and P. falciparum [ 34 , 37 , 38 ]. Whilst neither 700014 or 700063 showed activity against P. falciparum , they did decrease L. mexicana survival by some 70% and thus fell just below the selection threshold.…”

“…Four of the lanosterone-like sterols (700022, 700107, 700136, 700240) only inhibited growth in L. mexicana . Similar sterols, such as pistagremic acid, have also shown leishmanicidal activity [ 34 , 40 ] and have also been implicated in lipase and anticancer activity [ 41 , 42 ]. Interestingly, 700016, another lanosterone-like sterol, was effective against T. evansi and decreased L. mexicana survival by more than 50% ( Table S1 ).…”

“…As a number of sterols are being explored for their potential as possible leads against Leishmania spp. [ 34 ], this study highlights the importance of including screening novel compounds against drug-resistant lines early in the hit-to-lead process.…”

Anti-Leishmania amazonensis activity of the terpenoid fraction from Eugenia pruniformis leaves

“…Plants are an important source of biologically active compounds such as terpenoids that could be studied in the treatment of the neglected tropical diseases as leishmaniasis (Duarte et al 2019, Ogungbe & Setzer 2013. Terpenoids as β-sitosterol and ursolic acid have shown antileishmanial activity and were found in Eugenia genus (Myrtaceae) (Santos et al 2008, Yamamoto et al 2015, Frighetto et al 2005, which in turn is represented by several species that have been used in folk medicine and are known for their antidiabetic, antirheumatic, antipyretic, antidiarrheal, anti-inflammatory, antifungal, antibacterial, antioxidant andcytotoxic activities (Reynertson et al 2005, de Souza et al 2018).…”