Pothomorphe umbellata : Antifungal activity against strains of Trichophyton rubrum

Rodrigues, E. R.; Nogueira, N.G.P.; Zocolo, Guilherme Julião; Leite, Fernanda Sangalli; Januário, AH; Fusco-Almeida, A. M.; Fachin, Ana Lúcia; Marchi, Mary Rosa Rodrigues de; Santos, André Gonzaga dos; Pietro, Rosemeire Cristina Linhari Rodrigues

doi:10.1016/j.mycmed.2012.05.005

Cited by 13 publications

(8 citation statements)

References 27 publications

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“…This species was included in the Brazilian Pharmacopoeia first edition (1926) and 94 traditional medicinal uses for P. umbellatum are registered [ 3 ]. Indeed, there are several pharmacological activities described, such as antioxidant [ 4 ], anti-inflammatory and analgesic [ 5 ], antibacterial [ 6 ], antifungal [ 7 ], antitumor [ 8 ] activities and protection against photoaging [ 9 ] and anticonvulsants [ 10 ]. Moreover, phytochemical studies of P. umbellatum leaves extracts have demonstrated the presence of terpenes, alkaloids, flavonoids, and sterols, the catechol 4-nerolidylcatechol (4-NC) being the majority compound [ 3 , 6 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract fromPiper umbellatumL. Leaves

Iwamoto

Vendramini–Costa

Monteiro

et al. 2015

Evidence-Based Complementary and Alternative Medicine

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Despite the advances in anticancer drug discovery field, the worldwide cancer incidence is remarkable, highlighting the need for new therapies focusing on both cancer cell and its microenvironment. The tumor microenvironment offers multiple targets for cancer therapy, including inflammation. Nowadays, almost 75% of the anticancer agents used in chemotherapy are derived from natural products, and plants are an important source of new promising therapies. Continuing our research on Piper umbellatum species, here we describe the anticancer (in vitro antiproliferative activity and in vivo Ehrlich solid tumor model) and anti-inflammatory (carrageenan-induced paw edema and peritonitis models) activities of a standardized dichloromethane extract (SDE) from P. umbellatum leaves, containing 23.9% of 4-nerolidylcatechol. SDE showed in vitro and in vivo antiproliferative activity, reducing Ehrlich solid tumor growth by 38.7 and 52.2% when doses of 200 and 400 mg/kg, respectively, were administered daily by oral route. Daily treatments did not produce signals of toxicity. SDE also reduced paw edema and leukocyte migration on carrageenan-induced inflammation models, suggesting that the anticancer activity of SDE from Piper umbellatum leaves could involve antiproliferative and anti-inflammatory effects. These findings highlight P. umbellatum as a source of compounds against cancer and inflammation.

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Section: Introductionmentioning

confidence: 99%

Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract fromPiper umbellatumL. Leaves

Iwamoto

Vendramini–Costa

Monteiro

et al. 2015

Evidence-Based Complementary and Alternative Medicine

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“…The plates were incubated at 28 o C for 7 days and then observed for T.rubrum growth. MFC was defined as the lowest concentration of the subculture showing no development of T.rubrum on Sabouraud dextrose agar (Rodrigues et al, 2012). Both MIC and MFC determinations were performed in independent triplicate.…”

Section: Mic and Mfc Determinationmentioning

confidence: 99%

Cloning and characterization of a putative gene encoding serine protease inhibitor (251Hbpi) with antifungal activity against Trichophyton rubrum from Hevea brasiliensis leaves

Chinnapun

Palipoch²,

Hongphruk³

2016

Plant Omics

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A novel serine protease inhibitor gene was isolated from Hevea brasiliensis leaves, a RRIT251 cultivar and designated RRIT251 H. brasiliensis protease inhibitor (251Hbpi). Reverse transcription polymerase chain reaction (RT-PCR) and rapid amplification of cDNA ends (RACE) were used to isolate 251Hbpi. A full-length cDNA of 251Hbpi encoded a 70 amino acid protein. 251HbPI is a member of the potato inhibitor I (PI-I) family of serine protease inhibitors. The amino acid residues at the active site of 251HbPI were predicted as Met 46-Glu 47. Multiple alignments of the homologous PI-I family revealed one motif WPELVG of 251HbPI conserved across the family. 251Hbpi was cloned into expression vector pFLAG-ATS and expressed in Escherichia coli strain BL21. Molecular weight of the recombinant 251HbPI (r251HbPI) was approximately 11 kDa. Protease inhibition analysis revealed that r251HbPI inhibited the activity of chymotrypsin and subtilisin A but did not trypsin protease. Moreover, purified r251HbPI protein inhibited Trichophyton rubrum with a minimum inhibitory concentration of 0.7 mg/ml and a minimum fungicidal concentration of 1.4 mg/ml. The specific T. rubrum protease targets of r251HbPI were analyzed by co-immunoprecipitation. r251HbPI interacted with approximate 27 and 61 kDa T. rubrum proteins, suggesting a role in the inhibition of T. rubrum growth. These results suggest that 251HbPI could be a candidate for the development of a novel drug to treat T. rubrum infection.

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“…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

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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.

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Pothomorphe umbellata : Antifungal activity against strains of Trichophyton rubrum

Cited by 13 publications

References 27 publications

Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract fromPiper umbellatumL. Leaves

Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract fromPiper umbellatumL. Leaves

Cloning and characterization of a putative gene encoding serine protease inhibitor (251Hbpi) with antifungal activity against Trichophyton rubrum from Hevea brasiliensis leaves

4-Nerolidylcatechol analogues as promising anticancer agents

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