English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

Background  Plants represent an intricate and innovative source for the discovery of novel therapeutic remedies for the management of infectious diseases. The current study aimed at discovering new inhibitors of  Leishmania  spp., using anti-leishmanial activity-guided investigation approach of extracts from  Diospyros gracilescens  Gürke (1911) (Ebenaceae), targeting the extracellular (promastigotes) and intracellular (amastigotes) forms of  Leishmania donovani .    Methods  The plant extracts were prepared by maceration using H 2 0: EtOH (30:70, v/v) and further fractionated using a bio-guided approach. Different concentrations of  D. gracilescens  extracts, fractions and isolated compounds were tested in triplicate against  L. donovani  promastigotes and amastigotes in vitro. The antileishmanial potency and cytotoxicity on RAW 264.7 cells were determined using the resazurin colorimetric assay. The time kill kinetic profile of the most active sample was also investigated. The structures of all compounds were elucidated on the basis of extensive spectroscopic analyses, including 1D and 2D NMR, and HR-ESI-MS and by comparison of their data with those reported in the literature.    Results  The hydroethanolic crude extract of  D. gracilescens  trunk showed the most potent antileishmanial activity (IC 50  = 5.84 μg/mL). Further fractionation of this extract led to four (4) fractions of which, the hexane fraction showed the most potent activity (IC 50  = 0.79 μg/mL), and seven (07) compounds that exhibited moderate potency (IC 50  = 13.69–241.71 μM) against  L. donovani . Compound 1-deoxyinositol (7) inhibited the promastigote and amastigote forms of  L. donovani  with IC 50  values of 241.71 μM and 120 μM respectively and also showed the highest selectivity against  L. donovani  promastigotes (SI > 5.04). To the best of our knowledge, the antileishmanial activity of this compound is being reported here for the first time. The promising hexane fraction showed significant inhibition of parasites growth at different concentrations, but with no evidence of cidal effect over an exposure period of 120 h.    Conclusions  The results obtained indicated that the hydroethanolic extract from the  D. gracilescens  trunk and the derived hexane fraction have very potent inhibitory effect on cultivated promastigotes and amastigotes of  L. donovani  parasite. The isolated compounds showed a lesser extent of potency and selectivity. However, further structure-activity-relationship studies of 1-deoxyinositol could lead to more potent and selective hit derivatives of interest for detailed drug discovery program against visceral leishmaniasis.    Supplementary Information  The online version contains supplementary material available at 10.1186/s12906-021-03279-1.

Bio-guided isolation of anti-leishmanial natural products from Diospyros gracilescens L. (Ebenaceae)