A call for using natural compounds in the development of new antimalarial treatments – an introduction

Ginsburg, Hagai; Deharo, Eric

doi:10.1186/1475-2875-10-S1-S1

Malaria Journal

Table 1 Anti-malarial compounds from plants- recent reviews

From: A call for using natural compounds in the development of new antimalarial treatments – an introduction

Source	Number of plant species or compounds	Nature of compound	Availability of chemical structure	Quantitative toxicity tests
Tgaboto and Townson 2001¹[36]	270 species	extracts or purified components	No	No
Schwikkard and and van Heerden 2002²[37]	170 compounds	purified	Yes	No
Saxena et al 2003³[38]	250 compounds	purified	Yes	Few
Frederich et al, 2008⁴[39]	31 compounds	purified	Yes	vitro, vivo, good selectivity
Pillay et al, 2008⁵[40]	216 species and 24 compounds	extracts or purified components	For purified compounds	No
Batista et al, 2009⁶[41]	60 species	extracts or purified components	for some	vitro, vivo, many with good selectivity
Kaur et al, 2009⁷[42]	266 compounds	purified	Yes	vitro, vivo, many with good selectivity
Mariath et al, 2009⁸[43]	198 species	extracts	No	vitro, vivo
Bero et al, 2009⁹[44]	301 compounds	purified	Yes	vitro, vivo

1. Compiled a list of 270 plant species whose extracts or purified components have anti-malarial activity but no chemical structures or details about their potency were provided.
2. A total of 170 structures have been reviewed from 186 references found in the literature up to December 2000
3. Provides a critical account of crude extracts, essential oils and anti-plasmodial secondary metabolites with diverse chemical structures from higher plants, covering the period 1993-2003. A total of 127 alkaloids, 18 quassinoids, 23 sesquiterpenes, 27 triterpenoids, 21 flavonoids/xanthones, nine quinones and 25 miscellaneous compounds were highlighted in their work, although very few quantitative details are provided.
4. Three ethnobotanical screening programmes have been conducted on South African plants while there have been a few studies adopting a more direct approach, where plants within a particular genus were screened for anti-plasmodial activity. The paper also summarizes the bioactive molecules identified from selected plants having anti-plasmodial activity.
5. Covers 31 indole alkaloids isolated from natural sources with high anti-plasmodial activity (in vitro and in vivo), most of them displaying IC₅₀ values under the micromolar range and with a good selectivity index.
6. Review anti-plasmodial non-alkaloids natural products from reports published in the period Jan/2008-May/2009. Compounds include the classes of terpenes, limonoids, flavonoids, chromones, xanthones, anthraquinones, and other miscellaneous and related compounds .The review covers 60 plant species belonging to 34 families, some of them extracted by 3 different solvents. Twenty four extracts were found with significant activity, e.g., IC₅₀<3 μg/ml. Some were also tested in vivo. Most extracts show only weak activity in culture or in mouse models. Many recent reports on anti-plasmodial activity of plants used in local ethnic medicine are, however, not reviewed.
7. Review focusing on anti-plasmodial compounds discovered during 1998-2008 from all natural sources, including crude extracts from plant and marine organisms. A total of 266 anti-plasmodial natural products, for most the available chemical and pharmacological details are shown. The compounds listed in this compilation belong to the classes of alkaloids, terpenes, quassinoids, flavonoids, limonoids, chalcones, peptides, xanthones, quinones, coumarins and miscellaneous compounds, as well as 37 promising semisynthetic anti-malarials. The review also presents progress in recent semi-synthetic approaches to develop drugs from natural sources which display some anti-malarial activity. The semi-synthetic compounds belong to different classes: alkaloids – naphthylisoquinoline, bisbenzylisoquinoline, protoberberine, aporphine, indole alkaloids, manzamine alkaloids and others. Terpenes – sesquiterpenes, triterpenes, diterpenes and others. Other semi-synthetic compounds belong to quassinoids, flavonoids, limonoids, chalcones, peptides, xanthones, quinones and coumarins. For many of them, data on anti-plasmodial activity in culture and anti-malarial activity in mouse models and toxicity facts are provided. Most importantly, several compounds containing unique structural composition have been isolated and characterized.
8. Review plants of the American continent with anti-malarial activity, describing 198 plants whose extracts were active in vitro and in vivo. In vivo tests were done on P. berghei, P. gallinaceum, P. vinckei, P. lophurae, P. cathemerium and P. yoelii strains.
9. Review only compounds purified from plants used in traditional medicine, covering publications between 2005 and 2008. The list of compounds contains flavonoid derivatives, xanthones, coumarins, lignans, tannins, diterpenes and triterpenes, steroids, and derivatives of ornithine, lysine, phenylalanine, tyrosine and tryptophane derivatives, as well as steroidal alkaloids. Alkaloids and diterpenes are the most numerous among the highly active compounds (IC₅₀ ≤2 μM), while coumarins, steroids, stilbenes and tannins provide only moderate activity (2 < IC₅₀ ≤ 11 μM). The Caesalpiniaceae family provides the highest number of highly active compounds. But the Asteraceae, Leguminosae and Moraceae are significant contributors.

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ISSN: 1475-2875

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