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Journal ArticleDOI

Antileishmanial amides and lignans from Piper cubeba and Piper retrofractum

22 May 2007-Journal of Natural Medicines (Springer-Verlag)-Vol. 61, Iss: 4, pp 418-421
TL;DR: The n-hexane, ethyl acetate, methanol, and acetone extracts of Piper cubeba Linn and P. retrofractum were evaluated in vitro against promastigotes of Leishmania donovani, and all exhibited significant in vitro activity at 100 μg/ml.
Abstract: The n-hexane, ethyl acetate, methanol, and acetone extracts of Piper cubeba Linn. and P. retrofractum Vahl. (Piperaceae) were evaluated in vitro against promastigotes of Leishmania donovani, and all exhibited significant in vitro activity at 100 μg/ml. Two lignans, cubebin and hinokinin, were isolated from the hexane extract of P. cubeba; and one bis-epoxy lignan, (−)-sesamin, and two amides, pellitorine and piplartine, were isolated from the hexane and methanol extracts of P. retrofractum. Cubebin and piplartine showed significant antileishmanial activity in vitro at 100 μM and were further tested in vivo in a hamster model of visceral leishmaniasis. Piplartine showed activity at 30 mg/kg dose. This is the first report of antileishmanial activity of these two plants and their isolated constituents.
Citations
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Journal ArticleDOI
TL;DR: It is concluded that piplartine is effective for use in cancer therapy and its safety using chronic toxicological studies should be addressed to support the viability of clinical trials.

244 citations


Cites background from "Antileishmanial amides and lignans ..."

  • ...…al., 1990a, 1990b; Bezerra et al., 2005, 2007, 2008a; Tsai et al., 2005; Kong et al., 2008; Lin et al., 2007; Jyothi et al., 2009; Raj et al., 2011; Bokesch et al., 2011; Golovine et al., 2013; Adams et al., 2012), genotoxic (Bezerra et al., 2008b, 2009), antitumor (Bezerra et al., 2006, 2008a;…...

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  • ...…over cancer cells and presents only a weak activity in normal cells (Duh et al., 1990a, 1990b; Bezerra et al., 2005, 2007, 2008a; Kong et al., 2008; Lin et al., 2007; Jyothi et al., 2009; Lee and Mandinova, 2009; Raj et al., 2011; Bokesch et al., 2011; Golovine et al., 2013; Adams et al., 2012)....

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  • ...Additionally, Bokesch et al. (2011) tested the ability of this compound to modulate hypoxia inducible factor-2 (HIF-2) transcription activities in the renal carcinoma cell line, 786-0....

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Journal ArticleDOI
TL;DR: An overview of current status of research on sesame lignans with respect to the analytical methods employed, the biological activities and biosynthesis of sesamol is presented.

140 citations

Journal ArticleDOI
TL;DR: The in vitro effect of piplartine, an amide isolated from Piper tuberculatum (Piperaceae), on Schistosoma mansoni adult worms is reported, the first time that the schistosomicidal activity has been reported for piplarine.

135 citations

Journal ArticleDOI
TL;DR: An overview of the current status of plant derived pharmaceuticals and their chemical modifications to target parasite-specific peculiarities in order to interfere with their proliferation in the human host is provided.
Abstract: Infectious diseases caused by parasites are a major threat for the entire mankind, especially in the tropics More than 1 billion people world-wide are directly exposed to tropical parasites such as the causative agents of trypanosomiasis, leishmaniasis, schistosomiasis, lymphatic filariasis and onchocerciasis, which represent a major health problem, particularly in impecunious areas Unlike most antibiotics, there is no “general” antiparasitic drug available Here, the selection of antiparasitic drugs varies between different organisms Some of the currently available drugs are chemically de novo synthesized, however, the majority of drugs are derived from natural sources such as plants which have subsequently been chemically modified to warrant higher potency against these human pathogens In this review article we will provide an overview of the current status of plant derived pharmaceuticals and their chemical modifications to target parasite-specific peculiarities in order to interfere with their proliferation in the human host

125 citations

Journal ArticleDOI
TL;DR: New discoveries related to the phytochemistry and biological activities of bioactive compounds from Piper species are reviewed for further clinical applications, which could pave the way for the proper therapeutic use ofBioactive compounds and extracts from this plant species.

118 citations

References
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Journal ArticleDOI
TL;DR: It is demonstrated that miltefosine induces apoptosis-like death in L. donovani based on observed phenomena such as nuclear DNA condensation, DNA fragmentation with accompanying ladder formation, and in situ labeling of DNA fragments by the terminal deoxyribonucleotidyltransferase-mediated dUTP-biotin nick end labeling method.
Abstract: Miltefosine causes leishmanial death, but the possible mechanism(s) of action is not known. The mode of action of miltefosine was investigated in vitro in Leishmania donovani promastigotes as well as in extra- and intracellular amastigotes. Here, we demonstrate that miltefosine induces apoptosis-like death in L. donovani based on observed phenomena such as nuclear DNA condensation, DNA fragmentation with accompanying ladder formation, and in situ labeling of DNA fragments by the terminal deoxyribonucleotidyltransferase-mediated dUTP-biotin nick end labeling method. Understanding of miltefosine-mediated death will facilitate the design of new therapeutic strategies against Leishmania parasites.

230 citations


"Antileishmanial amides and lignans ..." refers background or methods in this paper

  • ...The standards miltefosine and pentamidine were used at reported IC50 values [6, 7]....

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  • ...The mean percentage of posttreatment viable cells was calculated relative to control, and results were expressed as the concentration inhibiting the parasite growth [6]....

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Journal ArticleDOI
TL;DR: Berberine, an alkaloid from Berberis aristata Linnaeus, may be a useful drug for the treatment of visceral leishmaniasis and was found to interact in vitro with nuclear DNA from L. donovani promastigotes.

159 citations


"Antileishmanial amides and lignans ..." refers methods in this paper

  • ...Spleen parasitic burden was assessed from Giemsa-stained impression smears [8]....

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Journal ArticleDOI
TL;DR: This work highlights some of these agents, while trying to emphasize the importance of plants as a source of new and powerful drugs against this widespread disease of Leishmaniasis.

116 citations


"Antileishmanial amides and lignans ..." refers background in this paper

  • ...Leishmaniasis patients are highly susceptible to HIV infection, and leishmaniasis accelerates the onset of AIDS by cumulative immunosuppression and by stimulation of the replication of the virus in HIV-infected patients [2]....

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  • ...If untreated, it often leads to death [2]....

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Journal ArticleDOI
TL;DR: From the aerial parts of Artemisia dracunculus, one known alkamide, pellitorine, two new alkamides neopellitorine A and neopelitorine B, and one known coumarin herniarine were isolated and showed insecticidal activity against Sitophilus oryzae and Rhyzopertha dominica.

72 citations


"Antileishmanial amides and lignans ..." refers background in this paper

  • ...Compound 4 was identified as pellitorine by comparison of spectral data with literature values [14, 15]....

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