Effects of qinghaosu (artemisinin) and its derivatives on experimental cutaneous leishmaniasis

Yang, Dong; Liew, F Y

doi:10.1017/s0031182000074758

Cited by 97 publications

(56 citation statements)

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“…Artemisinins inhibited 90% of parasite growth at 46.5 M to 50.8 M for T. cruzi and 44.8 M to 49.6 M for T. brucei rhodesiense. The IC 50 values for the trypanosomes are comparable to those obtained with L. donovani promastigotes, which have previously been shown to be susceptible to artemisinin compounds in vitro and in vivo (1,15,23). Similar results were also obtained in drug IC 50 determinations for Leishmania and Trypanosoma spp.…”

supporting

confidence: 83%

Artemisinins Inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense In Vitro Growth

Mishina

Krishna

Haynes

et al. 2007

Antimicrob Agents Chemother

129

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Artemisinin compounds inhibit in vitro growth of cultured Trypanosoma cruzi and Trypanosoma brucei rhodesiense at concentrations in the low micromolar range. Artemisinin also inhibits calcium-dependent ATPase activity in T. cruzi membranes, suggesting a mode of action via membrane pumps. Artemisinins merit further investigation as chemotherapeutic options for these pathogens.Diseases caused by insect-borne trypanosomatid parasites are a significant and neglected public health problem worldwide. Chagas' disease, caused by infection with Trypanosoma cruzi, is a major agent of disease in Latin America, with 16 to 18 million infected individuals and an annual death toll of 50,000. It is also an emerging problem in the United States, where an estimated 100,000 infected individuals reside (16). Trypanosoma brucei subspp., the causative agents of human African trypanosomiasis or "sleeping sickness," infect 50,000 annually. Approximately 300,000 to 500,000 people have trypanosomiasis and will die if not treated (18). Current therapeutic options for Trypanosoma infections, benznidazole and nifurtimox for Chagas' disease treatment and suramin, pentamidine, melarsoprol, and eflornithine for treatment of sleeping sickness, are far from ideal (8,17). These drugs all suffer from one or more disadvantages-high cost, parenteral administration, long treatment courses (months), high clinical failure rates, or parasite drug resistance-and they elicit multiple, serious, and potentially fatal toxic side effects. New therapeutic alternatives are obviously desirable for treatment of these lifethreatening infections.Artemisinin is a sesquiterpene lactone isolated from Artemisia annua, an annual herb that has been used in traditional Chinese medicine for over 2,000 years (21). Artemisinin is hydrophobic, passes biological membranes easily, and is a potent antimalarial with effective 50% inhibitory concentrations (IC 50 values) ranging from 4.2 to 16.2 nM for different derivatives. Oral, parenteral, or rectal dosages achieve micromolar plasma concentrations (22). Artemisinin derivatives have been used to treat malaria cases around the world, and their extensive usage has not been associated with any significant toxicity (19). Artemisinin generates bioreactive radicals capable of intracellular damage, depolarizes mitochondrial membrane potential in yeast, and inhibits the Plasmodium falciparum endoplasmic reticulum calcium pump (SERCA), and artemisininresistant P. falciparum contains SERCA mutations (9,13,14,(20)(21)(22).Artemisinin compounds also show efficacy against Leishmania spp. of trypanosomatid parasites, achieving 50% killing at 750 nM for Leishmania major promastigotes, at 3 to 30 M for intracellular amastigote stages in macrophages, and at 1.4 to 382.9 M against Leishmania infantum promastigotes (1, 23). Artemether treatment (50 mg/kg of body weight/day) of footpad lesions in mice, by oral, intralesional, intramuscular, or intravenous administration, significantly reduces lesion size and L. major parasite numbers (23). Oral dih...

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confidence: 83%

Artemisinins Inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense In Vitro Growth

Mishina

Krishna

Haynes

et al. 2007

Antimicrob Agents Chemother

129

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“…Dentre eles, podem ser citados os terpenóides (Yang;Liew, 1992;Camacho et al, 2000), aminoglicosteróides e aminosteróides (Kam et al, 1997), naftoquinonas (Fournet et al, 1992a;Kayser et al, 2000), chalconas (Chen et al, 1993), glicosídios iridóides (Mittal et al, 1998); fl avonóides (Araújo et al, 1998), neolignanas (Barata et al, 2000) e os alcalóides (Mahiou et al, 1994;Fournet et al, 1994;Queiroz et al, 1996;Akendengue et al, 1999).…”

Section: Discussionunclassified

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Moreira¹,

Costa²,

Lopes³

et al. 2007

Rev. bras. farmacogn.

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RESUMO:ABSTRACT: "In vitro leishmanicidal effect of Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)". Leishmanicidal activity of the hydroalcoholic extract of Stachytarpheta cayennensis, species that is usually employed in ulcers caused by Leishmania, was evaluated in vitro using Leishmania braziliensis and L. amazonensis promastigotes forms. The hydroalcoholic extract was prepared from dried leaves and used in L. amazonensis and L. braziliensis promastigotes cultures at concentrations of 500 to 32.5 g/mL. After 24 hours the promastigotes forms were quantifi ed and the IC 50 was calculated. The cytotoxicity of the extract was evaluated using peritoneal macrophages. The extract presented a dose and specie-dependent leishmanicidal effect to Leishmania promastigotes, mainly to the L. braziliensis ones. The cytotoxic effect was not observed in macrophage cultures. In conclusion, the hydroalcoholic extract of S. cayennensis inhibits the growing of Leishmania promastigotes forms in vitro accounting for the folk use of this vegetal in skin ulcers caused by Leishmania.

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“…Recent studies have demonstrated that artemisinin derivatives are equally potent and efficacious against several other common infectious parasites of man including Toxoplasma gondii (Jones-Brando et al, 2006) which causes toxoplasmosis that is responsible for behavioral abnormalities in patients, Trypanosoma and Schistosoma species (Mishina et al, 2007;Utzinger et al, 2001) that are responsible for human trypanosomiasis or 'sleeping sickness' and schistosomiasis, respectively. Artemisinin derivatives are also effective against some other pathogens including those responsible for cryptosporidiosis, amoebiasis, giardiasis, clonorchiasis and leishmaniasis (Ma et al, 2004;Yang and Liew, 1993). Moreover, artemisinin has been recently indicated as a potential and effective compound against a number of viruses including hepatitis B, C and others (Efferth et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Controlling bruchid pests of stored cowpea seeds with dried leaves of Artemisia annua and two other common botanicals

Ebiamadon¹,

Brisibe²,

Sophia³

et al. 2011

Afr. J. Biotechnol.

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Insecticidal activities of dried Artemisia annua L. leaves were evaluated against bruchid (Callosobruchus maculatus F.) pests in comparison with those of Azadirachta indica, Ocimum gratissimum and a conventional grain storage insecticide, Actellic® 2% dust. Each treatment was added to a mixture of 250 g cowpea seeds and 25 adult bruchids and laid out in a completely randomized design with four replicates. Irrespective of the concentration tested, all three plant materials significantly (P < 0.05) increased mortality rate of adult insects earlier than the control. Higher concentrations of the botanical pesticides equally resulted in an increased reduction in the number of surviving bruchids and reduction to seed damage through a lower number of eggs laid and weevil perforation index (WPI) after 90 days. Comparatively, A. annua was more effective than the other plant materials at all levels evaluated though it was not as effective as Actellic 2% dust. Moreover, differences amongst the efficiency rates and interactions between A. annua and A. indica in three treatment combinations produced a significant (P < 0.05) effect on two of the parameters evaluated. Taken together, all plant materials evaluated here were seen to have significant insecticidal properties and could therefore, be used as environmentally friendly products for controlling bruchid pests during storage of cowpeas with no adverse effects on eventual mammalian consumers as observed during an animal feeding trial in this study.

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Effects of qinghaosu (artemisinin) and its derivatives on experimental cutaneous leishmaniasis

Cited by 97 publications

References 2 publications

Artemisinins Inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense In Vitro Growth

Artemisinins Inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense In Vitro Growth

Efeito leishmanicida in vitro de Stachytarpheta cayennensis (Rich.) Vahl (Verbenaceae)

Controlling bruchid pests of stored cowpea seeds with dried leaves of Artemisia annua and two other common botanicals

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