Avaliação por análise fatorial das condições da extração do 4-nerolidilcatecol de Pothomorphe umbellata (L). Miq.

Noriega, Peky; Röpke, Cristina Dislich; Camilo, César M.; Freitas, Paulo Chanel Deodato de; Barros, Sílvia Berlanga de Moraes

doi:10.1590/s1516-93322005000200015

Cited by 8 publications

(4 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Thus, screenings of water, water‐alcohol, hexane and ethanol extracts for in vitro antiplasmodial activity in blood stages of P. falciparum revealed extracts exhibiting IC 50 as low as 3.7 μg/mL (Atindehou et al , ). There is ample evidence in the literature on P. peltatum and P. umbellatum (Ropke et al , , ; Noriega et al , ) which is reinforced by our own experience in the laboratory (with P. peltatum ) that extracts prepared with solvents of differing polarity contain significant and variable amounts of the secondary metabolite 4‐NC (Pinto et al , ) which previous studies have shown to be an in vitro inhibitor of chloroquine‐resistant K1 P. falciparum (Andrade‐Neto et al , ).…”

Section: Discussionmentioning

confidence: 93%

In Vivo and In Vitro Antimalarial Activity of 4‐Nerolidylcatechol

Silva

Pinto

Pohlit

et al. 2011

Phytotherapy Research

View full text Add to dashboard Cite

4-Nerolidylcatechol (4-NC) isolated from Piper peltatum L. (Piperaceae) was evaluated for in vitro antiplasmodial activity against Plasmodium falciparum (cultures of both standard CQR (K1) and CQS (3D7) strains and two Amazonian field isolates) and for in vivo antimalarial activity using the Plasmodium berghei-murine model. 4-NC exhibits significant in vitro and moderate in vivo antiplasmodial activity. 4-NC administered orally and subcutaneously at doses of 200, 400 and 600 mg/kg/day suppressed the growth of P. berghei by up to 63% after four daily treatments (days 1-4). Also, 4-NC exhibited important in vitro antiplasmodial activity against both standard and field P. falciparum strains in which 50% inhibition of parasite growth (IC(50) ) was produced at concentrations of 0.05-2.11 μg/mL and depended upon the parasite strain. Interestingly, healthy (non-infected) mice that received 4-NC orally presented (denatured) blood plasma which exhibited significant in vitro activity against P. falciparum. This is evidence that mouse metabolism allows 4-NC or active metabolites to enter the blood. Further chemical and pharmacological studies are necessary to confirm the potential of 4-NC as a new antimalarial prototype.

show abstract

Section: Discussionmentioning

confidence: 93%

In Vivo and In Vitro Antimalarial Activity of 4‐Nerolidylcatechol

Silva

Pinto

Pohlit

et al. 2011

Phytotherapy Research

View full text Add to dashboard Cite

show abstract

“…4-Nerolidylcatechol (1) is a major component of infusions and other extracts prepared from the roots and leaves (22)(23)(24)(25)55) of the traditionally used caapeba plant (Piper peltatum and P. umbellata) (56). Caapeba extracts are active in vitro against P. falciparum and inactive or variably active against P. berghei in mice (57)(58)(59)(60)(61)(62).…”

Section: Discussionmentioning

confidence: 99%

In Vivo Antimalarial Activity and Mechanisms of Action of 4-Nerolidylcatechol Derivatives

Silva

Nogueira

Pinto

et al. 2015

Antimicrob Agents Chemother

View full text Add to dashboard Cite

“…Brazilian plants such as Pothomorphe umbellata L. (Piperaceae) (Noriega et al 2005;Viana et al 2004). Several biological properties has been attributed to this compound, including antioxidant , chemopreventive (Valadares et al 2007), antitumor (Sacoman et al 2008), cytotoxic Mongelli et al 1999), antimalarial ) and antifungal (Rodrigues et al 2012) …”

Section: -Nerolidylcatechol (4-nrc) (1) Is a Phenolic Compound Isolamentioning

confidence: 99%

4-Nerolidylcatechol analogues as promising anticancer agents

Cortez

Ávila

Cunha

et al. 2015

European Journal of Pharmacology

View full text Add to dashboard Cite

4-Nerolidylcatechol (1) is an isolated compound from Pothomorphe umbellata L. (Piperaceae) with promising antitumor cells properties. However it presents lability under light and room temperatures. Many efforts have been directed towards discovering anticancer agents endowed with cytotoxic activities. Here, we evaluated cytotoxic effects of 4-NRC analogues (LQFMs 2-6) and the cell death pathways induced by these compounds in multidrug-resistant K562 cells. Compounds (2-6) exhibited cytotoxic activities in a concentration-dependent manner against leukaemic cells, specially the compounds (3) and (5). Additionally, compounds (1), (3) and (5) promoted marked alterations on the cell morphology, including nuclear changes as demonstrated by Hoescht 33342 staining. Moreover, these compounds promoted apoptosis induction in K562 cells by phosphatidylserine exposure, increase of sub-G1 cells and modulation of the caspases-3/7, -8 and -9 activation. In addition, the pancaspase inhibitor z-VAD-fmk partially reduced the apoptosis induced by the compounds (1) and (5)-induced, suggesting caspase-dependent and caspase-independent cell death pathways. Compounds (1) and (5) also modified the cell cycle progression by G0/G1 and S arrest, respectively. Furthermore, compounds (1), (3) and (5) promoted mitochondrial dysfunction associated to accumulation of cytosolic cytochrome c and modulated the NF-ĸB activation. In addition, unlike their analogues, 4-NRC (1) also promoted a significant cyclin D1 inhibition. Together, these data suggest that the mechanism of cell death of 4-NRC and its analogues (3) and (5) occurs by apoptosis through mitochondrial mechanisms. Considering that LQFMs are biocompatible synthetic analogues produced by molecular simplification of (1) without the chiral centre, which is associated with the instability found in compound (1), we suggest that these compounds are promising candidates for further pre-clinical studies.

show abstract

Avaliação por análise fatorial das condições da extração do 4-nerolidilcatecol de Pothomorphe umbellata (L). Miq.

Cited by 8 publications

References 8 publications

In Vivo and In Vitro Antimalarial Activity of 4‐Nerolidylcatechol

In Vivo and In Vitro Antimalarial Activity of 4‐Nerolidylcatechol

In Vivo Antimalarial Activity and Mechanisms of Action of 4-Nerolidylcatechol Derivatives

4-Nerolidylcatechol analogues as promising anticancer agents

Contact Info

Product

Resources

About