Giardisis is a debilitating disease caused by gastrointestinal parasites of the genus Giardia. High-antioxidant T. ferdinandiana fruit extracts were investigated for the ability to block Giardia duodenalis growth. Methanolic and aqueous extracts had the most potent growth inhibitory activity (IC50 values of approximately 700 and 140 μg/ml, respectively). Ethyl acetate and chloroform extracts also inhibited G. duodenalis growth, albeit with lower potency. The hexane extract was completely devoid of G. duodenalis growth inhibitory activity. All extracts were nontoxic in the Artemia fransiscana bioassay. Nontargeted HPLC-quadrupole time-of-flight (QTOF) mass spectroscopy (with screening against three compound databases) putatively identified 17 compounds in all of the inhibitory extracts but not in the inactive hexane extract. The low toxicity of the Terminalia ferdinandiana fruit extracts and their potent G. duodenalis growth inhibitory bioactivity indicate their potential as medicinal agents in the treatment and prevention of this disease.

Giardia duodenalis is a protozoal, intestinal parasite that is a common aetiological agent of infectious diarrhoea in humans worldwide. Chemotherapeutic intervention presently offers a limited range of drugs and these are usually only employed after clinical diagnosis. Moreover, these drugs are ineffective against the infectious cysts, can produce unpleasant side effects, and are expensive with limited availability in developing countries. Frequent reports of drug toxicity, treatment failure and parasite drug resistance have, in some instances, also resulted in the increasing reluctance to over-prescribe synthetic anti-microbials. Alternatively, there is now mounting evidence to suggest that some of the naturally derived, medium-chain, saturated fatty acids (MCSFAs) possess anti-microbial and anti-parasitic properties. We have therefore examined the effects of four different fatty acids on G. duodenalis trophozoites in vitro. Cytotoxicity was determined using fluorescence, scanning and transmission electron microscopic techniques and standard cytotoxicity assays. Our studies have confirmed that the MCSFA, dodecanoic acid (C: 12) (common name: lauric acid), is anti-giardial, with an LD50 concentration comparable to that of metronidazole, the drug of choice in the treatment of giardiasis. Dodecanoic acid appeared to induce trophozoite death by accumulating within the parasite cytoplasm resulting in rupture of the cell membrane. This study has opened fresh avenues for development of natural drug therapy in which food supplementation may augment, or even replace, some of the standard chemotherapeutic agents presently employed in the treatment of giardiasis and possibly other infectious intestinal diseases.

Background: Giardiasis is a debilitating disease caused by gastrointestinal parasites of the genus Giardia. Tasmannia lanceolata (Tasmanian pepper berry) has a high anti-oxidant capacity and has documented therapeutic properties for a variety of pathogenic diseases. Materials and methods: Solvent extracts of T. lanceolata berry and leaf were investigated for the ability to block G. duodenalis growth. The IC 50 values of the extracts which displayed inhibitory activity were determined to quantify and compare their efficacies. Toxicity was determined using the Artemia franciscana nauplii bioassay. Active extracts were analysed by non-targeted HPLC-QTOF mass spectroscopy (with screening against 3 compound databases) for the identification and characterisation of individual components in crude plant extracts. Results: Methanolic, aqueous and ethyl acetate T. lanceolata berry and leaf extracts displayed potent G. duodenalis growth inhibitory activity. The methanolic extracts were the most potent growth inhibitors with IC 50 values of approximately 180 µg/ml and 420 µg/ml for the berry and leaf methanolic extracts respectively. The aqueous, ethyl acetate, chloroform and hexane extracts also inhibited G. duodenalis growth, albeit with lower potency. HPLC-QTOF mass spectroscopy analysis of the extracts

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One of the greatest challenges for healthcare professionals is the prevention and treatment of protozoal and helminthic parasitic infections. From our study we conclude that the prevalence of different pathogenic species of amoeba such as Entamoeba histolytica (4.2 vs. 0%) and G. lamblia (17.9 vs. 14%), (P value was equal to 1) was significantly higher among rural children compared to children from urban areas. In contrast, the prevalence of nematodes such as A. lumbricoides (21% vs. 1.1%), T. trichiura (8% vs. 0%) and A. duodenale (1%) was also significantly higher among rural children.

Giardiasis, one of the most common causes of diarrhoeal disease, is caused by gastrointestinal protozoal parasites of the genus Giardia. Metronidazole is the most commonly used drug to treat giardiasis. However, metronidazole resistance is increasingly common, making the development of new anti-giardial drugs a high priority. A panel of 11 compounds previously identified in T. ferdinandiana fruit extracts with potent G. duodenalis growth inhibitory activity were investigated for the ability to inhibit G. duodenalis proliferation. Eight of the 11 compounds inhibited the growth of all three G. duodenalis strains. 2,3-Dihydroxyphenyl B-Dglucopyranosiduronic acid (DPGA)DPGA was the most potent anti-giardial compound, with IC50 values as low as 126μM (38µg/mL). Notably, DPGA inhibited a metronidazole resistant G. duodenalis strain with similar potency as determined for the metronidazole sensitive strains. Furthermore, the potency of DPGA was greatly potentiated when it was tested in combination with ascorbic acid, to approximately 17μM (5µg/mL) for the metronidazole sensitive G. duodenalis strains and 40μM (12mg/mL) for the resistant strain. The T. ferdinandiana tannins (gallic acid and chebulic acid) were also moderate inhibitors of G. duodenalis growth when tested in combination with ascorbic acid, although they had only low levels of activity when tested alone. All of the tested compounds (and their combinations with ascorbic acid) displayed low toxic and all compounds conformed to Lipinski's rules of 5 with few violations, indicating their potential as drug leads and chemotherapies for the treatment and prevention of giardiasis.

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Background:High antioxidant capacities have been linked to the treatment and prevention of several cancers. Recent reports have identified several native Australian fruits with high antioxidant capacities. Despite this, several of these species are yet to be tested for anticancer activity.Materials and Methods:Solvent extracts prepared from high antioxidant native Australian fruits were analyzed for antioxidant capacity by the di (phenyl)-(2,4,6-trinitrophenyl) iminoazanium free radical scavenging assay. Antiproliferative activities against CaCo2 and HeLa cancer cells were determined by a multicellular tumor spheroid-based cell proliferation assay. Toxicity was determined by Artemia franciscana bioassay.Results:Methanolic extracts of all plant species displayed high antioxidant contents (equivalent to approximately 7–16 mg of vitamin C per gram of fruit extracted). Most aqueous extracts also contained relatively high antioxidant capacities. In contrast, the ethyl acetate, chloroform, and hexane extracts of most species (except lemon aspen and bush tomato) had lower antioxidant contents (below 1.5 mg of vitamin C equivalents per gram of plant material extracted). The antioxidant contents correlated with the ability of the extracts to inhibit proliferation of CaCo2 and HeLa cancer cell lines. The high antioxidant methanolic extracts of all species were potent inhibitors of cell proliferation. The methanolic lemon aspen extract was particularly effective, with IC50 values of 480 and 769 μg/mL against HeLa and CaCo2 cells, respectively. In contrast, the lower antioxidant ethyl acetate and hexane extracts (except the lemon aspen ethyl acetate extract) generally did not inhibit cancer cell proliferation or inhibited to only a minor degree. Indeed, most of the ethyl acetate and hexane extracts induced potent cell proliferation. The native tamarind ethyl acetate extract displayed low-moderate toxicity in the A. franciscana bioassay (LC50 values below 1000 μg/mL). All other extracts were nontoxic. A total of 145 unique mass signals were detected in the lemon aspen methanolic and aqueous extracts by nonbiased high-performance liquid chromatography-mass spectrometry analysis. Of these, 20 compounds were identified as being of particular interest due to their reported antioxidant and/or anticancer activities.Conclusions:The lack of toxicity and antiproliferative activity of the high antioxidant plant extracts against HeLa and CaCo2 cancer cell lines indicates their potential in the treatment and prevention of some cancers.SUMMARY Australian fruit extracts with high antioxidant contents were potent inhibitors of CaCo2 and HeLa carcinoma cell proliferationMethanolic lemon aspen extract was particularly potent, with IC50 values of 480 μg/mL (HeLa) and 769 μg/mL (CaCo2)High-performance liquid chromatography-mass spectrometry-quadrupole time-of-flight analysis highlighted and putatively identified 20 compounds in the antiproliferative lemon aspen extractsIn contrast, lower antioxidant content extracts stimulated carcinoma cell pr...