Peganine hydrochloride dihydrate an orally active antileishmanial agent

Khaliq, Tanvir; Misra, Pragya; Gupta, Swati; Reddy, K. Papi; Kant, Ravi; Maulik, Prakas R.; Dube, Anuradha; Narender, Tadigoppula

doi:10.1016/j.bmcl.2009.03.039

Cited by 37 publications

(16 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It has great importance in Ayurveda due to its bronchodilatory effect. It also has anti-inflammatory, anti-bacterial activity 14 , anticestodal activity 15 , antileishmanial activity 16 and anti-helminthic activity 17 .…”

Section: Resultmentioning

confidence: 99%

Untitled

2012

IJPSR

View full text Add to dashboard Cite

In this study, α-naphthyl acetic acid and mannitol were used as elicitors to improve the productivity of useful metabolite, vasicine for archiving high concentration in Justicia adhatoda L. cell suspension cultures. When the cells were treated with 3mg 100 ml -1 suspension of α-naphthyl acetic acid, the vasicine concentration was increased by 1.65 mg ml -1 in 15 days culture compared to untreated cells. 0.32M 100ml -1 mannitol could also promote the synthesis of vasicine in the cell cultures. After 15 days of the cell culture, it was found that the vasicine concentration was 1.48 mg ml -1 more than the control cell cultures.

show abstract

Section: Resultmentioning

confidence: 99%

Untitled

2012

IJPSR

View full text Add to dashboard Cite

show abstract

“…; however, the in vitro evidences of inter-species differences in the susceptibility of parasites to antileishmanial drugs have also been reported (Escobar et al, 2002;Obonaga et al, 2014). In recent years, considerable attention has been given to new compounds in an attempt to search for new antileishmanial drugs (Croft & Coombs, 2003;Khaliq et al, 2009;Seifert et al, 2010;Vendrametto et al, 2010). Despite the efficacy in our in vitro studies, it is important to consider that the use of other Leishmania spp.…”

Section: Discussionmentioning

confidence: 99%

“…It has been shown that the number of natural product-derived drugs present in the total amount of drug launchings in the market from 1981 to 2002 represented a significant source of new compounds (Newman et al, 2003). In recent years, considerable attention has been given to secondary plant-purified products, in an attempt to search for new antileishmanial drugs (Tiuman et al, 2005;Khaliq et al, 2009;Vendrametto et al, 2010). The Strychnos genus includes approximately 200 plant species, many of which are known for their potential medicinal secondary metabolites (Thongphasuk et al, 2003;Philippe et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Antileishmanial activity and evaluation of the mechanism of action of strychnobiflavone flavonoid isolated from Strychnos pseudoquina against Leishmania infantum

et al. 2015

View full text Add to dashboard Cite

The present study aimed to investigate the in vitro antileishmanial activity of strychnobiflavone flavonoid against Leishmania infantum, as well as its mechanism of action, and evaluate the ex vivo biodistribution profile of the flavonoid in naive BALB/c mice. The antileishmanial activity (IC 50 value) of strychnobiflavone against stationary promastigote and amastigote-like stages of the parasites was of 5.4 and 18.9 μM, respectively; with a 50% cytotoxic concentration (CC 50 ) value of 125.0 μM on murine macrophages, resulting in selectivity index (SI) of 23.2 and 6.6, respectively. Amphotericin B, used as a positive control, presented SI values of 7.6 and 3.3 for promastigote and amastigote-like stages of L. infantum, respectively. The strychnobiflavone was also effective in reducing in significant levels the percentage of infected macrophages, as well as the number of amastigotes per macrophage, after the treatment of infected macrophages using the flavonoid. By using different fluorescent probes, we investigated the bioenergetics metabolism of L. infantum promastigotes and demonstrated that the flavonoid caused the depolarization of the mitochondrial membrane potential, without affecting the production of reactive oxygen species. In addition, using SYTOX ® green as a fluorescent probe, the strychnobiflavone demonstrated no interference in plasma membrane permeability. For the ex vivo biodistribution assays, the flavonoid was labeled with technetium99m and studied in a mouse model by intraperitoneal route. After a single dose administration, the scintigraphic images demonstrated a highest uptake by the liver and spleen of the animals within 60 min, resulting in low concentrations after 24 h. The present study therefore demonstrated, for the first time, the antileishmanial activity of the strychnobiflavone against L. infantum, and suggests that the mitochondria of the parasites may be the possible target organelle. The preferential distribution of this compound into the liver and spleen of the animals could warrant its employ in the treatment of visceral leishmaniasis.

show abstract

“…Harmine (1) and harmaline (2) showed moderate in vitro antiplasmodial activity against Plasmodium falciparum. Vascinine (peganine) has been found to be safe and effective against Leishmania donovani, a protozoan parasite that can cause potentially fatal visceral leishmaniasis (Lala et al, 2004;Khaliq et al, 2009). Powdered seeds of Pgh have also been used as an anthelmintic agent (Panda, 2000).…”

Section: Anti-infectivementioning

confidence: 99%

“…Pgh has antibacterial activity against drug-resistant bacteria and protozoa (Arshad et al, 2008). The potential role of the alkaloids in crude extracts of Pgh was also investigated regarding their antimicrobial activity (Astulla et al, 2008;Khaliq et al, 2009). Harmine (1) and harmaline (2) showed moderate in vitro antiplasmodial activity against Plasmodium falciparum.…”

Section: Anti-infectivementioning

confidence: 99%