Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid Palythoa aff. clavata

Abstract

Leishmaniasis and Chagas disease are neglected tropical diseases that cause problems in developing countries. The causative agents, Leishmania spp. and Trypanosoma cruzi, produce a clinical picture that can be fatal for the patient, such as Chagas heart disease, visceral leishmaniasis and megacolon, among others. Current treatments for these diseases are not very effective and highly toxic, since they require very prolonged treatments. The development of innovative, effective and safe drugs to fight infections caused by these parasites remains a challenge. For this reason, in recent years, there has been an increase in the search for new therapies. In this study, the antikinetoplastid activity of 13 sesquiterpene lactones obtained from Palythoa aff. clavata was screened against L. amazonensis, L. donovani and T. cruzi. The results revealed that the sesquiterpene lactones anhydroartemorin (2), cis,trans-costunolide-14-acetate (3) and 4-hydroxyarbusculin A (11) were the most selective against the kinetoplastid species studied. These molecules seem to induce the mechanisms involved in an apoptotic-like death or programmed cell death (PCD) in the kinetoplastids, and since they do not cause necrosis, the inflammatory events associated with this type of cell death will not be triggered.

Marine natural products

“…and Trypanosoma cruzi . 546 As with each year, the dominant number of metabolites reported from cnidarians are diterpenoids. Bebrycin A 1225 , sourced from Bebryce grandis , was identified as a weakly active (IC 50 1.1 μM) growth inhibitor of P. falciparum Dd2 strain, blocking parasite maturation at the schizont life stage.…”

Global Health Priority Box: Discovering Flucofuron as a Promising Antikinetoplastid Compound

“…After 15 min of incubation with the kit, fluorescence (GFP light cube, excitation 504 nm/emission 523 nm) pictures were taken with the EVOS ® FL Cell Imaging System (ThermoFisher Scientific, Waltham, MA, USA). Standard treatments were added, including benznidazole for T. cruzi and miltefosine for L. amazonensis and a positive control, triton 0.1% [39].…”

The First Phytochemical Investigation of Artemisia divaricate: Sesquiterpenes and Their Anti-Inflammatory Activity

“…Apart from compounds 1-9, 30 other known components were isolated and identified as austroyunnane H (10) [17], baynol C (11) [18], jatrophaeudesmene C (12) [19], dihydro-β-cyclopyrethrosin (13) [20], β-Cyclopyrethrosin (14) [21], yomogin (15) [22], (11S)-1β-Hydroxyeudes-m-4(14)-eno-13,6α-lactone (16) [23], reynosin (17) [24], 1β,8β-Dihydroxy-reynosin (18) [25], artemorin (19) [26], 1-epi-Dihydrochrysanolide (20) [27], dihydrochrysanolide (21) [27], 5β,6α-Hydroxygermacra-1(10)E,4(15),11(13)-trien-12,8α-olide (22) [28], tulirinol (23) [29], chamissarin (24) [19], 6β-Acetoxy-14-hydroxygermacra-4E,1(10)E,11(13)trien-12,8α-olide (25) [30], 6β-Acetoxy-3-formyl-3Z,9E,11(13)-trien-12,8α-olide (26) [31], chrysanolide (27) [22], haagenolide (28) [32], 14-hydroxygermacra-4E,1(10)E, 11(13)-trien-12,7α-olide (29) [30], Chihuahuin (30) [29], austroliolide (31) [29], pyrethrosin (32) [29], 9α,10β-epoxi-8α-Hydrox-germacra-3Z,11(13)-dien-6α,12-olide (33) [33], sinugibberodiol (34) [34], (3R,7S,9S)-3,9-Dihydroxygermacra-4(15),10(14),11(12)-triene (35) …”