Journal ArticleDOI
Antimalarial Activity of Tropical Meliaceae Extracts and Gedunin Derivatives
S. MacKinnon,T. Durst,J. T. Arnason,Cindy K. Angerhofer,John M. Pezzuto,Pablo Sanchez-Vindas,Luis Poveda,M Gbeassor +7 more
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TLDR
Extracts of 22 species of Meliaceae were examined for antimalarial activity using in vitro tests with two clones of Plasmodium falciparum, one sensitive tochloroquine (W2) and one chloroquine-resistant (D6), suggesting there is no cross-resistance to chloroquines.Abstract:
Extracts of 22 species of Meliaceae were examined for antimalarial activity using in vitro tests with two clones of Plasmodium falciparum, one sensitive to chloroquine (W2) and one chloroquine-resistant (D6). Twelve extracts were found to have activity, including extracts of Cedrela odorata wood and Azadirachta indica leaves, which contained the limonoid gedunin. These extracts were more effective against the W2 clone than the D6 clone, suggesting there is no cross-resistance to chloroquine. Gedunin was extracted in quantity, and nine derivatives prepared for a structure-activity study, which revealed essential functionalities for activity. The study also included four other limonoids derived from related Meliaceae. Only gedunin had better activity than chloroquine against the W2 clone. This active principle could be used to standardize a popular crude drug based on traditional use of A. indica in West Africa.read more
Citations
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Journal ArticleDOI
Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators
Haley Hieronymus,Justin Lamb,Kenneth N. Ross,Xiao P. Peng,Xiao P. Peng,Cristina C. Clement,Anna Rodina,Maria Nieto,Jinyan Du,Kimberly Stegmaier,Srilakshmi M. Raj,Srilakshmi M. Raj,Katherine N. Maloney,Jon Clardy,William C. Hahn,William C. Hahn,Gabriela Chiosis,Todd R. Golub,Todd R. Golub,Todd R. Golub +19 more
TL;DR: This work identifies new modes of HSP90 modulation through a gene expression-based strategy that is similar to celastrol and gedunin and blocks the ability of androgen receptor (AR) signaling states to be modulated.
Journal ArticleDOI
In vitro antiplasmodial activity of medicinal plants native to or naturalised in South Africa.
Cailean Clarkson,Vinesh Maharaj,Neil R. Crouch,Olwen M. Grace,Pamisha Pillay,Motlalepula G. Matsabisa,Niresh Bhagwandin,Pete Smith,Peter I. Folb +8 more
TL;DR: The results of the present study support a rational rather than random approach to the selection of antiplasmodial screening candidates, and identify a number of promising taxa for further investigation as plant-based antimalarial agents.
Journal ArticleDOI
Antimalarials from nature
TL;DR: Recent advances in antimalarial drug discovery from natural sources are presented, including plant extracts, and compounds isolated from plants, bacteria, fungi and marine organisms, which offer new and novel scaffolds for development as antimalarials.
Journal ArticleDOI
Meliaceous limonoids: chemistry and biological activities.
Qin-Gang Tan,Xiao-Dong Luo +1 more
TL;DR: This paper aims to demonstrate the efforts towards in-situ applicability of EMMARM, as to provide real-time information about concrete mechanical properties such as E-modulus and compressive strength.
Journal ArticleDOI
Natural products as antiparasitic drugs.
TL;DR: This review shows that many novel lead structures in natural products, including plant-derived alkaloids, terpenes and phenolics, have severe chemico-physical drawbacks such as poor solubility and here, innovative drug formulations and carrier systems might help.
References
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Journal ArticleDOI
Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique.
TL;DR: A rapid, semiautomated microdilution method was developed for measuring the activity of potential antimalarial drugs against cultured intraerythrocytic asexual forms of the human malaria parasite Plasmodium falciparum, and results demonstrated that the method is sensitive and precise.
Book
Handbook of African Medicinal Plants
TL;DR: This book discusses healing and the African Culture, medicinal plants, and traditional healing methods, as well as some of the aspects of traditional healing that have changed over time.
Journal ArticleDOI
Potential antimalarial candidates from African plants: An in vitro approach using Plasmodium falciparum☆
TL;DR: In this protocol, the flavonoid quercetin purified from Diosma pilosa was found to have the same activity as a commercially obtained preparation, and simple radiometric assays for antimalarial activity can be used to rapidly screen purified plant material or secondary plant metabolites.
Book ChapterDOI
Tropical Plants as Sources of Antiprotozoal Agents
TL;DR: Protozoa are the cause of a number of major diseases which spread massive misery and death, mainly throughout the tropical world, but other protozoal diseases such as leishmaniasis, trypanosomiasis, amoebiasis and giardiasis cause havoc for many millions of people.
Journal ArticleDOI
Die Chukrasine A, B, C, D und E, fünf neue Tetranortriterpene aus Chukrasia tabularisA. JUSS
Thomas Ragettli,Christoph Tamm +1 more
TL;DR: In this article, five tetranortriterpenes, chukrasins A, B, C, D and E, have been isolated from the wood of Chukrasia tabularis.
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