Antileishmanial Activity of an Indole Alkaloid from<i>Peschiera australis</i>

Delorenzi, Jan Carlo; Attias, Márcia; Gattass, Cerli Rocha; Andrade, Mônica Calixto de; Rezende, Cláudia M.; Pinto, Ângelo da Cunha; Henriques, A. T.; Bou-Habib, Dumith Chequer; Saraiva, Elvira M.

doi:10.1128/aac.45.5.1349-1354.2001

Cited by 178 publications

(133 citation statements)

References 26 publications

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“…In general, indole alkaloids are a class of compound having a range of biological activities, including antibacterial, trypanocidal, leishmanicidal and anticancer (Sakamoto-Hojo et al 1988, Delorenzi et al 2001, Ferreira et al 2006, Tanaka et al 2006). The antiplasmodial activity of monoterpene indole alkaloids has been investigated (Wright et al 1994, Iwu et al 1994).…”

Section: Discussionmentioning

confidence: 99%

In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

Andrade‐Neto

Pohlit

Pinto

et al. 2007

Mem. Inst. Oswaldo Cruz

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In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhibition (more active than quinine and chloroquine) of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.Key words: neosergeolide -ellipticine -aspidocarpine -4-nerolidylcatechol -Pothomorphe peltata -Picrolemma spruceiAspidosperma spp.Malaria is the main cause of economic loss and high morbidity in the world today and continues to be endemic to tropical regions such as the Amazon. In the Brazilian Amazon, 1.6 million positive plates (thick smears) in a total of 8 million diagnostic tests for malaria were registered from January 2004 to February 2007 (Ministério da Saúde, Sivep-Malaria 2007). The lack of an effective vaccine and the increasing expansion of strains of Plasmodium falciparum presenting resistance towards commonly used, low-cost antimalarials make control of this disease difficult (Olliaro & Bloland 2001, Wellens & Plowe 2001, Vieira et al. 2001, Gonzales et al. 2003, Alecrim et al. 2006. As a result, the World Health Organization (WHO 1978(WHO , 1995 has been promoting research on natural product based drugs for treatment of disease and many plant species have been evaluated for antimalarial activity (Weniger et al. 2004). In these studies, emphasis has been on the discovery of lead compounds for drug development (Gundidza & Chinyanganya 1999). The rational search for active substances in medicinal plants is a very promising and cost-effective strategy for antimalarial drug discovery. This approach benefits from the accumulated knowledge of the curing capacity of plants possessed by inhabitants of malaria endemic regions and permits the extensive evaluation of natural products derived from these sources (Campbell et al. 1997, 1998, Brandão et al. 1992, 1997, Krettli et al. 2001, Andrade-Neto et al. 2004a.This triage of useful and effective plants is at the heart of traditional medicinal knowledge and is an extremely important source of therapeutic compounds in use today. Important semi-synthetic, low-cost, highly effective antimalarial drugs such as the quinolines (chloroquine, mefloquine, primaquine, etc.) and artemisinin derivatives (sodium artesunate, arteether, artemether, etc.) owe their initial discovery to the isolation and structural identi...

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Section: Discussionmentioning

confidence: 99%

In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

Andrade‐Neto

Pohlit

Pinto

et al. 2007

Mem. Inst. Oswaldo Cruz

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“…Results were expressed as percent of reduction of the infection rate (% IR) in comparison with those obtained with positive controls. The infection rates were obtained by multiplying the percentage of infected macrophages by the number of amastigotes per infected macrophages (Delorenzi et al, 2001). The IC 50 value was calculated by linear regression analysis.…”

Section: Antiamastigote Activitymentioning

confidence: 99%

Antileishmanial activity of leaf extract from Calophyllum rivulare against Leishmania amazonensis

Oubada

García

Bello

et al. 2014

Emir. J. Food Agric

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Calophyllum rivulare is an endemic tree from Cuba that belongs to Clusiaceae family. This plant had revealed it to be a rich source of pyranochromanone acids including compounds with a variety of biological potentialities such as antioxidant, antiulcer, anticancer and anti-Helicobacter pylori activities. Herein, antileishmanial and cytotoxic activities of extracts obtained from C. rivulare leaves (rich in pyranochromanone acids) and amentoflavone were compared. Extracts were prepared by maceration employing ethyl acetate (CR-1) and methanol (CR-2) as solvents and amentoflavone was isolated from both extracts. The CR-2 extract showed the better activity against the parasite, with an IC 50 value of 95.1 ± 5.4 µg/mL and 20.6 ± 1.4 µg/mL against promastigote and amastigote forms, respectively. This extract showed lower cytotoxicity (IC 50 =182.4 ± 2.3 µg/mL) against peritoneal macrophage from BALB/c mice and a selectivity index of 9. Amentoflavone showed an IC50 of 5.9 ± 0.3 µg/mL against amastigote form and a selectivity index of 9. Results suggest that CR-2 extract and amentoflavone could be explored as new antileishmanial alternatives.

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“…Even though experimental cutaneous leishmaniasis caused by L. amazonensis has been used in several studies evaluating new natural 4,9,13,28 and synthetic antileishmanial products 4,26 , treatment of animals infected with L. amazonensis with the extract of E. echinophorus reduced the size of the lesions and the parasite load in the infected footpads without causing death, loss of weight or any observable signs of toxicity. However, the cure was not complete; possibly because L. amazonensis-infected BALB/c mice are not adequate for testing the effectiveness of products against leishmaniasis, because a high multiplication rate of parasites at the site of the lesion occurs 14 .…”

Section: Discussionmentioning

confidence: 99%

“…The number of intracellular amastigotes was determined by counting the amastigotes residents on 100 macrophage per each sample, and the results were expressed as percent of reduction of the infection rate (% IR) in comparison to that of the controls [(IRTC = infection rate of the treated culture; IRUC = infection rate of the untreated culture)]. The infection rates were obtained by multiplying the percentage of infected macrophages by the number of amastigotes per infected macrophages 9 . The IC 50 value was calculated by linear regression analysis.…”

Section: Antiamastigote Activitymentioning

confidence: 99%

Leishmanicidal activity of Echinaster (Othilia) echinophorus crude extract

Parra

Fidalgo

Martínez

et al. 2010

Rev. Inst. Med. trop. S. Paulo

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SUMMARYIn this study, a methanolic extract from Echinaster (Othilia) echinophorus was evaluated for activity against Leishmania amazonensis. The extract showed activity against the promastigote and amastigote forms with IC 50 values of 62.9 and 37.5 μg.mL -1 respectively. This extract showed a moderate toxicity on macrophages from BALB/c mice. A dose of 100 mg/kg/day was effective when administered during 15 days by intraperitoneal route to BALB/c mice infected experimentally.

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Antileishmanial Activity of an Indole Alkaloid fromPeschiera australis

Cited by 178 publications

References 26 publications

In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants

Antileishmanial activity of leaf extract from Calophyllum rivulare against Leishmania amazonensis

Leishmanicidal activity of Echinaster (Othilia) echinophorus crude extract

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