2019
DOI: 10.1186/s12936-019-2694-1
|View full text |Cite
|
Sign up to set email alerts
|

Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae)

Abstract: Background Optimal adoption of the malaria transmission-blocking strategy is currently limited by lack of safe and efficacious drugs. This has sparked the exploration of different sources of drugs in search of transmission-blocking agents. While plant species have been extensively investigated in search of malaria chemotherapeutic agents, comparatively less effort has been channelled towards exploring them in search of transmission-blocking drugs. Artemisia afra (Asterac… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1
1

Citation Types

0
28
0
1

Year Published

2020
2020
2024
2024

Publication Types

Select...
8
2

Relationship

2
8

Authors

Journals

citations
Cited by 35 publications
(29 citation statements)
references
References 56 publications
0
28
0
1
Order By: Relevance
“…The majority of antimalarial compounds with activity against asexual parasites will retain activity on early-stage gametocytes at a comparable level (or with some loss in activity), but those that then do have activity on late-stage gametocytes are typically characterized by an ∼10-fold loss in activity. , However, evidence is accumulating where compounds are identified with some selectivity toward gametocytes, and with higher potency against these stages than against asexual stage parasites. While this has been shown for diverse chemotypes, ,,, it also holds true for compounds with different chemotypes within the kinase inhibitor space. , Such stage-selective phenotypes have been the topic of much discussion and could be the result of either differences in uptake between asexual stage parasites and gametocytes or differences in target or target availability. Interestingly, a compound like MMV666810 shares some similarity in the core structure with MMV390048, yet it is more potent on late-stage gametocytes compared to early-stage gametocytes.…”
Section: Resultsmentioning
confidence: 99%
“…The majority of antimalarial compounds with activity against asexual parasites will retain activity on early-stage gametocytes at a comparable level (or with some loss in activity), but those that then do have activity on late-stage gametocytes are typically characterized by an ∼10-fold loss in activity. , However, evidence is accumulating where compounds are identified with some selectivity toward gametocytes, and with higher potency against these stages than against asexual stage parasites. While this has been shown for diverse chemotypes, ,,, it also holds true for compounds with different chemotypes within the kinase inhibitor space. , Such stage-selective phenotypes have been the topic of much discussion and could be the result of either differences in uptake between asexual stage parasites and gametocytes or differences in target or target availability. Interestingly, a compound like MMV666810 shares some similarity in the core structure with MMV390048, yet it is more potent on late-stage gametocytes compared to early-stage gametocytes.…”
Section: Resultsmentioning
confidence: 99%
“…The variation in the zones of inhibition between the crude (Table 6), partitioned fraction (Table 8), and fractions obtained from the column (Table 10) may be due to a decrease in the concentration of the phytochemical constituents' present in these fractions as the purification processes progress. It is worthy of note to remember that fractionation does not in all instances increase the level of activity as some of these phytochemicals act in synergy to produce better activity than when acting independently 43,60 .…”
Section: Resultsmentioning
confidence: 99%
“…Another gametocytocidal guaianolide sesquiterpenoid, 1α,4α -dihydroxybishopsolicepolide ( 54 ), was recently isolated from a South African plant of Asteraceae family Artemisia afra (Asteraceae). Compared to its activity against early gametocytes, compound 54 was demonstrated to exert better cidal activity against the late-stage IV/V gametocytes (IC 50 6.3 µM) [ 127 ]. This is however in contrast to derivatives of artemisinin from Artemisia annua (Asteraceae): dihydroartemisinin (DHA), artemether and artesunate with relatively poor activity against late-stage IV/V gametocytes [ 128 ].…”
Section: Transmission-blocking In Pursuit Of Human Disease Eliminatio...mentioning
confidence: 99%