In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts
Abstract Background Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpe...
Published in: | Malaria Journal |
---|---|
Main Authors: | , , , |
Format: | Article in Journal/Newspaper |
Language: | English |
Published: |
BMC
2017
|
Subjects: | |
Online Access: | https://doi.org/10.1186/s12936-017-2054-y https://doaj.org/article/f2ecd2257ef345eebd85479e212d973c |
id |
ftdoajarticles:oai:doaj.org/article:f2ecd2257ef345eebd85479e212d973c |
---|---|
record_format |
openpolar |
spelling |
ftdoajarticles:oai:doaj.org/article:f2ecd2257ef345eebd85479e212d973c 2023-05-15T15:13:15+02:00 In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts Claire Beaufay Marie-France Hérent Joëlle Quetin-Leclercq Joanne Bero 2017-10-01T00:00:00Z https://doi.org/10.1186/s12936-017-2054-y https://doaj.org/article/f2ecd2257ef345eebd85479e212d973c EN eng BMC http://link.springer.com/article/10.1186/s12936-017-2054-y https://doaj.org/toc/1475-2875 doi:10.1186/s12936-017-2054-y 1475-2875 https://doaj.org/article/f2ecd2257ef345eebd85479e212d973c Malaria Journal, Vol 16, Iss 1, Pp 1-8 (2017) Keetia leucantha Triterpene esters Anti-malarial Plasmodium Oleanolic Ursolic Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 article 2017 ftdoajarticles https://doi.org/10.1186/s12936-017-2054-y 2022-12-31T15:55:58Z Abstract Background Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts. Results These eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC–UV methods. They account for about 19% of this extract (16.9% for acids and 1.8% for esters). These compounds were also identified in trace in the twigs decoction by HPLC-HRMS. Results also showed that extracts and esters did not produce any haemolysis, and were devoid of any acute toxicity at a total cumulative dose of 800 and 150 mg/kg respectively. Moreover, esters given intraperitoneally at 50 mg/kg/day to Plasmodium berghei-infected mice showed a very significant (p < 0.01) parasitaemia inhibition (27.8 ± 5.4%) on day 4 post-infection compared to vehicle-treated mice. Conclusions These results bring out new information on the safety of K. leucantha use and on the identification of anti-malarial compounds from its dichloromethane extract. Its activity can be explained by the presence of triterpenic acids and esters which in vivo activity and safety were demonstrated for the first time. Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic Malaria Journal 16 1 |
institution |
Open Polar |
collection |
Directory of Open Access Journals: DOAJ Articles |
op_collection_id |
ftdoajarticles |
language |
English |
topic |
Keetia leucantha Triterpene esters Anti-malarial Plasmodium Oleanolic Ursolic Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 |
spellingShingle |
Keetia leucantha Triterpene esters Anti-malarial Plasmodium Oleanolic Ursolic Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 Claire Beaufay Marie-France Hérent Joëlle Quetin-Leclercq Joanne Bero In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
topic_facet |
Keetia leucantha Triterpene esters Anti-malarial Plasmodium Oleanolic Ursolic Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 |
description |
Abstract Background Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts. Results These eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC–UV methods. They account for about 19% of this extract (16.9% for acids and 1.8% for esters). These compounds were also identified in trace in the twigs decoction by HPLC-HRMS. Results also showed that extracts and esters did not produce any haemolysis, and were devoid of any acute toxicity at a total cumulative dose of 800 and 150 mg/kg respectively. Moreover, esters given intraperitoneally at 50 mg/kg/day to Plasmodium berghei-infected mice showed a very significant (p < 0.01) parasitaemia inhibition (27.8 ± 5.4%) on day 4 post-infection compared to vehicle-treated mice. Conclusions These results bring out new information on the safety of K. leucantha use and on the identification of anti-malarial compounds from its dichloromethane extract. Its activity can be explained by the presence of triterpenic acids and esters which in vivo activity and safety were demonstrated for the first time. |
format |
Article in Journal/Newspaper |
author |
Claire Beaufay Marie-France Hérent Joëlle Quetin-Leclercq Joanne Bero |
author_facet |
Claire Beaufay Marie-France Hérent Joëlle Quetin-Leclercq Joanne Bero |
author_sort |
Claire Beaufay |
title |
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
title_short |
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
title_full |
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
title_fullStr |
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
title_full_unstemmed |
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts |
title_sort |
in vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form keetia leucantha and crude extracts |
publisher |
BMC |
publishDate |
2017 |
url |
https://doi.org/10.1186/s12936-017-2054-y https://doaj.org/article/f2ecd2257ef345eebd85479e212d973c |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
Malaria Journal, Vol 16, Iss 1, Pp 1-8 (2017) |
op_relation |
http://link.springer.com/article/10.1186/s12936-017-2054-y https://doaj.org/toc/1475-2875 doi:10.1186/s12936-017-2054-y 1475-2875 https://doaj.org/article/f2ecd2257ef345eebd85479e212d973c |
op_doi |
https://doi.org/10.1186/s12936-017-2054-y |
container_title |
Malaria Journal |
container_volume |
16 |
container_issue |
1 |
_version_ |
1766343834673872896 |