Antimalarial Activity of Aspilia pruliseta, a Medicinal Plant from Uganda

Department of Pharmaceutical Sciences, College of Pharmacy, University of Hawaii at Hilo, Hilo, Hawaii 96720, USA.
Planta Medica (Impact Factor: 2.15). 11/2010; 76(16):1870-3. DOI: 10.1055/s-0030-1250028
Source: PubMed


Aspilia pruliseta Schweinf. (Asteraceae) is a medicinal plant indigenous to Uganda and the neighboring countries of East Africa. It has been used extensively by the rural population for the treatment of fevers and malaria. During the antimalarial evaluation of this plant, four nontoxic diterpenes were isolated that possessed moderate activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) clones of Plasmodium falciparum, with IC(50) values ranging from 14 to 23 µM. These moderately active compounds included the previously undescribed diterpene, ENT-15 β-senecioyloxy-16,17-epoxy-kauran-18-oic acid that demonstrated an IC(50) value of 23.4 µM against clone D6, but was devoid of activity against clone W2. Four additional diterpenes were obtained from the aerial parts of A. pruliseta, but these known compounds were essentially inactive. The moderate activities of select diterpenes of A. pruliseta could account collectively for the historical and enduring use of this plant in traditional African medicine.

Download full-text


Available from: Ghee T. Tan, Oct 07, 2015
83 Reads
  • Source
    • "Chloroform extracts of whole plants of Artemisia maciverae has shown effectiveness in vivo using chloroquine-resistant and chloroquine-sensitive Plasmodium berghei NK65-infected Swiss albino mice (Ene et al., 2009). Four non-toxic diterpenes have been isolated from an indigenous Ugandan plant, Aspilia pruliseta, showing moderate activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) clones of Plasmodium falciparum, with IC(50) values ranging from 14 to 23 micromolar (Sebisubi et al., 2010). The dichloromethane extract of aerial parts of Ageratum conyzoides reportedly gave an IC(50) value against Plasmodium falciparum of 8 microg/ml (Nour et al., 2010). "
    [Show abstract] [Hide abstract]
    ABSTRACT: Acanthaceae and Asteraceae family plants used by folk medicinal practitioners for treatment of malaria in Chittagong and Sylhet Divisions of Bangladesh ABSTRACT Malaria is a debilitating disease causing high mortality rates among men and women if not treated properly. The disease is prevalent in many countries of the world with the most prevalence noted among the sub-Saharan countries, where it is in an epidemic form. The disease is classified as hypo-endemic in Bangladesh with the southeast and the northeastern regions of the country having the most malaria-affected people. The rural people suffer most from malaria, and they rely on folk medicinal practitioners for treatment, who administer various plant species for treatment of the disease as well as associated symptoms like pain and fever. Plant species have always formed the richest sources of anti-malarial drugs, the most notable being quinine and artemisinin. However, quinine has developed drug-resistant vectors and artemisinin is considered by some to developing initial resistance, particularly in China, where it has been used for thousands of years to combat malaria. Thus new sources of anti-malarial drugs need to be found before artemisinin develops drug-resistance, and plant species can form the easiest sources for exploring and discovering new anti-malarial drugs. Since Acanthaceae and Asteraceae family plants have been reported to be excellent families of plants with a number of species demonstrating anti-malarial properties, the objective of the present study was to conduct an ethnomedicinal survey among the folk medicinal practitioners of Chittagong and Sylhet Divisions Bangladesh for these two family species, which are used by the practitioners for treatment of malaria. Three plant species belonging to the Acanthaceae family and five plant species belonging to the Asteraceae family were observed by the folk medicinal practitioners of Bangladesh for malaria treatment. The Acanthaceae family plants were Andrographis paniculata, Justicia adhatoda, and Justicia aurea. The Asteraceae family plants were Blumea lacera, Eclipta alba, Helianthus annuus, Parthenium hysterophorus, and Siegesbeckia orientalis. A perusal of the scientific literature demonstrated that a number of plants in use in Bangladesh as anti-malarials have been reported to contain relevant bio-activities which can justify the use of these species for malaria treatment. Taken together, the plants used in Bangladesh as anti-malarials deserve further scientific study towards discovery of novel anti-malarial drugs.
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: The emergence and spread of Plasmodium falciparum with resistance to chloroquine (CQ), the safest and cheapest anti-malarial drug, coupled with the increasing cost of alternative drugs especially in developing countries have necessitated the urgent need to tap the potential of plants for novel anti-malarials. The present study investigates the anti-malarial activity of the methanolic extracts of 13 medicinal plants from the Malaiyur and Javadhu hills of South India against blood stage CQ-sensitive (3D7) and CQ-resistant (INDO) strains of P. falciparum in culture using the fluorescence-based SYBR Green I assay. Sorbitol-synchronized parasites were incubated under normal culture conditions at 2% hematocrit and 1% parasitemia in the absence or presence of increasing concentrations of plant extracts. CQ and artemisinin were used as positive controls, while 0.4% DMSO was used as the negative control. The cytotoxic effects of extracts on host cells were assessed by functional assay using HeLa cells cultured in RPMI containing 10% fetal bovine serum, 0.21% sodium bicarbonate and 50 μg/mL gentamycin (complete medium). Plant extracts (bark methanol extracts of Annona squamosa (IC(50), 30 μg/mL), leaf extracts of Ocimum gratissimum (IC(50), 32 μg/mL), Ocimum tenuiflorum (IC(50), 31 μg/mL), Solanum torvum (IC(50), 31 μg/mL) and Justicia procumbens (IC(50), 63 μg/mL), showed moderate activity. The leaf extracts of Aristolochia indica (IC(50), 10 μg/mL), Cassia auriculata (IC(50), 14 μg/mL), Chrysanthemum indicum (IC(50), 20 μg/mL) and Dolichos biflorus (IC(50), 20 μg/mL) showed promising activity and low activity was observed in the flower methanol extracts of A. indica , leaf methanol extract of Catharanthus roseus, and Gymnema sylvestre (IC(50), >100 μg/mL). These four extracts exhibited promising IC(50) (μg/mL) of 17, 24, 19 and 24 respectively also against the CQ resistant INDO strain of P. falciparum. The high TC(50) in mammalian cell cytotoxicity assay and the low IC(50) in anti-malarial P. falciparum assay indicates selectivity and good resistance indices in the range of 0.9-1.7 for leaf extracts of A. indica, C. auriculata, C. indicum and D. biflorus suggests that these may serve as anti-malarial agents even in their crude form. These results indicate a possible explanation of the traditional use of some of these medicinal plants against malaria or malaria-like conditions.
    Parasitology Research 06/2011; 111(2):703-15. DOI:10.1007/s00436-011-2457-6 · 2.10 Impact Factor
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: Infections with protozoan parasites are a major cause of disease and mortality in many tropical countries of the world. Diseases caused by species of the genera Trypanosoma (Human African Trypanosomiasis and Chagas Disease) and Leishmania (various forms of Leishmaniasis) are among the seventeen "Neglected Tropical Diseases" (NTDs) defined by the WHO. Furthermore, malaria (caused by various Plasmodium species) can be considered a neglected disease in certain countries and with regard to availability and affordability of the antimalarials. Living organisms, especially plants, provide an innumerable number of molecules with potential for the treatment of many serious diseases. The current review attempts to give an overview on the potential of such plant-derived natural products as antiprotozoal leads and/or drugs in the fight against NTDs. In part I, a general description of the diseases, the current state of therapy and need for new therapeuticals, assay methods and strategies applied in the search for new plant derived natural products against these diseases and an overview on natural products of terpenoid origin with antiprotozoal potential were given. The present part II compiles the current knowledge on natural products with antiprotozoal activity that are derived from the shikimate pathway (lignans, coumarins, caffeic acid derivatives), quinones of various structural classes, compounds formed via the polyketide pathways (flavonoids and related compounds, chromenes and related benzopyrans and benzofurans, xanthones, acetogenins from Annonaceae and polyacetylenes) as well as the diverse classes of alkaloids. In total, both parts compile the literature on almost 900 different plant-derived natural products and their activity data, taken from over 800 references. These data, as the result of enormous efforts of numerous research groups world-wide, illustrate that plant secondary metabolites represent an immensely rich source of chemical diversity with an extremely high potential to yield a wealth of lead structures towards new therapies for NTDs. Only a small percentage, however, of the roughly 200,000 plant species on earth have been studied chemically and only a small percentage of these plants or their constituents has been investigated for antiprotozoal activity. The repository of plant-derived natural products hence deserves to be investigated even more intensely than it has been up to present.
    Current Medicinal Chemistry 03/2012; 19(14):2176-228. · 3.85 Impact Factor
Show more