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Nur Aziz - One of the best experts on this subject based on the ideXlab platform.
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Piper Cubeba l methanol extract has anti inflammatory activity targeting src syk via nf b inhibition
Evidence-based Complementary and Alternative Medicine, 2019Co-Authors: Nurinanda Prisky Qomaladewi, Nur AzizAbstract:Piper Cubeba L. is a plant in the Piperaceae family that is generally found in tropical countries and acts as an antioxidant and anti-inflammatory agent. Unfortunately, the molecular mechanism of the anti-inflammatory activity has not been fully investigated. In this study, we elucidated the anti-inflammatory mechanism by focusing on NF-κB signaling, which is considered a prototypical inflammatory signaling pathway in both innate and adaptive immune functions. Cellular activity and the molecular target of Pc-ME were identified in macrophage RAW264.7 cells and HEK293T cells by assessing NO production, cytokine expression by RT-PCR, luciferase gene reporter assay, and protein regulation in cytoplasm by Western blot upon NF-κB activation. Pc-ME reduced NO production without any cell toxicity; inhibited expression of proinflammatory cytokines such as iNOS and IL-6; downregulated NF-κB activation mediated by both MyD88 and TRIF; and diminished the phosphorylation of IκBα, IKKα/β, Akt, p85, Src, and Syk. Pc-ME inhibited Syk and Src autophosphorylation during overexpression in HEK cells, which confirmed our hypothesis that Syk and Src were signaling targets of Pc-ME. These findings indicate that Piper Cubeba L. has anti-inflammatory activity by targeting Src/Syk in the NF-κB pathway.
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Piper Cubeba L. Methanol Extract Has Anti-Inflammatory Activity Targeting Src/Syk via NF-B Inhibition
Evidence-based Complementary and Alternative Medicine, 2019Co-Authors: Nurinanda Prisky Qomaladewi, Nur AzizAbstract:Piper Cubeba L. is a plant in the Piperaceae family that is generally found in tropical countries and acts as an antioxidant and anti-inflammatory agent. Unfortunately, the molecular mechanism of the anti-inflammatory activity has not been fully investigated. In this study, we elucidated the anti-inflammatory mechanism by focusing on NF-κB signaling, which is considered a prototypical inflammatory signaling pathway in both innate and adaptive immune functions. Cellular activity and the molecular target of Pc-ME were identified in macrophage RAW264.7 cells and HEK293T cells by assessing NO production, cytokine expression by RT-PCR, luciferase gene reporter assay, and protein regulation in cytoplasm by Western blot upon NF-κB activation. Pc-ME reduced NO production without any cell toxicity; inhibited expression of proinflammatory cytokines such as iNOS and IL-6; downregulated NF-κB activation mediated by both MyD88 and TRIF; and diminished the phosphorylation of IκBα, IKKα/β, Akt, p85, Src, and Syk. Pc-ME inhibited Syk and Src autophosphorylation during overexpression in HEK cells, which confirmed our hypothesis that Syk and Src were signaling targets of Pc-ME. These findings indicate that Piper Cubeba L. has anti-inflammatory activity by targeting Src/Syk in the NF-κB pathway.
Juergen Drewe - One of the best experts on this subject based on the ideXlab platform.
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Piper Cubeba demonstrates anti estrogenic and anti inflammatory properties
Planta Medica, 2008Co-Authors: Alexei Schaab, Matthias Kreuter, Juergen DreweAbstract:This present study aims to investigate if P9605, an ethanolic extract of Piper Cubeba L, exhibits anti-estrogenic and anti-inflammatory properties. We found that P9605 significantly inhibited growth induced by beta-estradiol in MCF-7, a human breast cancer cell line. It inhibited aromatase activity, which is responsible for transforming androgens into estrogens. Competitive binding assays also indicated P9605 binding to both human recombinant estrogen a and beta receptors. Furthermore, this extract inhibited the activities of cyclo-oxygenases (COX-1 and COX-2) and 5-lipo-oxygenase (5-LOX), also it attenuated the induction of interleukin 6 (IL-6) in differentiated THP-1 cells stimulated by lipopolysaccharide (LPS). Taken together with our previous results, P9605 possesses anti-androgenic, anti-estrogenic and anti-inflammatory properties. These results support the potential use of P9605 in phytotherapy against benign prostatic hyperplasia (BPH).
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Piper Cubeba targets multiple aspects of the androgen signalling pathway a potential phytotherapy against prostate cancer growth
Planta Medica, 2008Co-Authors: Matthias Kreuter, Juergen DreweAbstract:Despite the high prevalence of prostate cancer (PC) in the Western world, there is a dearth of effective medication. Since the androgen-signalling pathway is very much involved in PC growth and development, we investigated the potential of Piper Cubeba L. extract, P9605, in targeting multiple events simultaneously within this pathway. This may be more effective compared to an antiandrogen monotherapy. Our results indicated that P9605 inhibited proliferation in androgen-dependent LNCaP human prostate cancer cells by reducing DNA synthesis and inducing apoptosis. This antigrowth effect was less pronounced in androgen-independent PC-3 prostate cancer cell lines. P9605 potently inhibited 5 alpha-reductase II activity, which is responsible for converting testosterone to its active form, dihydrotestosterone (DHT), in the prostate. It also acted as an antagonist at recombinant wild-type androgen receptors (AR). P9605 suppressed cell growth and prostate-specific antigen (PSA) secretion stimulated by physiological concentrations of DHT in LNCaP cells. Interestingly, it down-regulated AR levels. In conclusion, our findings suggest that P9605 may potentially retard the growth of androgen-dependent PC via several mechanisms.
Nurinanda Prisky Qomaladewi - One of the best experts on this subject based on the ideXlab platform.
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Piper Cubeba l methanol extract has anti inflammatory activity targeting src syk via nf b inhibition
Evidence-based Complementary and Alternative Medicine, 2019Co-Authors: Nurinanda Prisky Qomaladewi, Nur AzizAbstract:Piper Cubeba L. is a plant in the Piperaceae family that is generally found in tropical countries and acts as an antioxidant and anti-inflammatory agent. Unfortunately, the molecular mechanism of the anti-inflammatory activity has not been fully investigated. In this study, we elucidated the anti-inflammatory mechanism by focusing on NF-κB signaling, which is considered a prototypical inflammatory signaling pathway in both innate and adaptive immune functions. Cellular activity and the molecular target of Pc-ME were identified in macrophage RAW264.7 cells and HEK293T cells by assessing NO production, cytokine expression by RT-PCR, luciferase gene reporter assay, and protein regulation in cytoplasm by Western blot upon NF-κB activation. Pc-ME reduced NO production without any cell toxicity; inhibited expression of proinflammatory cytokines such as iNOS and IL-6; downregulated NF-κB activation mediated by both MyD88 and TRIF; and diminished the phosphorylation of IκBα, IKKα/β, Akt, p85, Src, and Syk. Pc-ME inhibited Syk and Src autophosphorylation during overexpression in HEK cells, which confirmed our hypothesis that Syk and Src were signaling targets of Pc-ME. These findings indicate that Piper Cubeba L. has anti-inflammatory activity by targeting Src/Syk in the NF-κB pathway.
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Piper Cubeba L. Methanol Extract Has Anti-Inflammatory Activity Targeting Src/Syk via NF-B Inhibition
Evidence-based Complementary and Alternative Medicine, 2019Co-Authors: Nurinanda Prisky Qomaladewi, Nur AzizAbstract:Piper Cubeba L. is a plant in the Piperaceae family that is generally found in tropical countries and acts as an antioxidant and anti-inflammatory agent. Unfortunately, the molecular mechanism of the anti-inflammatory activity has not been fully investigated. In this study, we elucidated the anti-inflammatory mechanism by focusing on NF-κB signaling, which is considered a prototypical inflammatory signaling pathway in both innate and adaptive immune functions. Cellular activity and the molecular target of Pc-ME were identified in macrophage RAW264.7 cells and HEK293T cells by assessing NO production, cytokine expression by RT-PCR, luciferase gene reporter assay, and protein regulation in cytoplasm by Western blot upon NF-κB activation. Pc-ME reduced NO production without any cell toxicity; inhibited expression of proinflammatory cytokines such as iNOS and IL-6; downregulated NF-κB activation mediated by both MyD88 and TRIF; and diminished the phosphorylation of IκBα, IKKα/β, Akt, p85, Src, and Syk. Pc-ME inhibited Syk and Src autophosphorylation during overexpression in HEK cells, which confirmed our hypothesis that Syk and Src were signaling targets of Pc-ME. These findings indicate that Piper Cubeba L. has anti-inflammatory activity by targeting Src/Syk in the NF-κB pathway.
Guilherme V Simaro - One of the best experts on this subject based on the ideXlab platform.
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evaluation of lignans from Piper Cubeba against schistosoma mansoni adult worms a combined experimental and theoretical study
Chemistry & Biodiversity, 2018Co-Authors: Renato L T Parreira, Wilson Roberto Cunha, Eveline S Costa, Vladimir Constantino Gomes Heleno, Lizandra Guidi Magalhaes, Julia Medeiros Souza, Patricia Mendonca Pauletti, Ana Helena Januario, Guilherme V Simaro, Jairo Kenupp BastosAbstract:: Six dibenzylbutyrolactonic lignans ((-)-hinokinin (1), (-)-cubebin (2), (-)-yatein (3), (-)-5-methoxyyatein (4), dihydrocubebin (5) and dihydroclusin (6)) were isolated from Piper Cubeba seed extract and evaluated against Schistosoma mansoni. All lignans, except 5, were able to separate the adult worm pairs and reduce the egg numbers during 24 h of incubation. Lignans 1, 3 and 4 (containing a lactone ring) were the most efficient concerning antiparasitary activity. Comparing structures 3 and 4, the presence of the methoxy group at position 5 appears to be important for this activity. Considering 1 and 3, it is possible to see that the substitution pattern change (methylenedioxy or methoxy groups) in positions 3' and 4' alter the biological response, with 1 being the second most active compound. Computational calculations suggest that the activity of compound 4 can be correlated with the largest lipophilicity value.
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Antibacterial activity of (-)-cubebin isolated from Piper Cubeba and its semisynthetic derivatives against microorganisms that cause endodontic infections
Revista Brasileira de Farmacognosia, 2016Co-Authors: Karen C S Rezende, Guilherme V Simaro, Rodrigo Lucarini, Patricia M. Pauletti, Ana H. Januário, Viviane R. Esperandim, Carlos H. G. Martins, Mislaine A. Silva, Wilson R. Cunha, Jairo K. BastosAbstract:Recent publications have highlighted the numerous biological activities attributed to the lignan (-)-cubebin ( 1 ), Piper Cubeba L. f., Piperaceae, and ongoing studies have focused on its structural optimization, in order to obtain derivatives with greater pharmacological potential. The aim of this study was the obtain-ment of ( 1 ), its semisynthetic derivatives and evaluation of antibacterial activity. The extract of the seeds of P. Cubeba was chromatographed, subjected to recrystallization and was analyzed by HPLC and spectro-metric techniques. It was used for the synthesis of: (-)- O -methylcubebin ( 2 ), (-)- O -benzylcubebin ( 3 ), (-)- O -acetylcubebin ( 4 ), (-)- O -( N,N -dimethylamino-ethyl)-cubebin ( 5 ), (-)-hinokinin ( 6 ) and (-)-6.6’-dinitrohinokinin ( 7 ). The evaluation of the antibacterial activity has been done by broth microdilution technique for determination of the minimum inhibitory concentration and the minimum bactericidal concentration against Porphyromonas gingivalis, Prevotella nigrescens, Actinomyces naeslundii, Bacteroides fragilis and Fusobacterium nucleatum. It was possible to make an analysis regarding the relationship between structure and antimicrobial activity of derivatives against microorganisms that cause endodontic infections. The most promising were minimum inhibitory concentration =50 μg/ml against P. gingivalis by ( 2 ) and ( 3 ), and minimum inhibitory concentration =100 μg/ml against B. fragilis by ( 6 ). Cytotoxicity assays demonstrated that ( 1 ) and its derivatives do not display toxicity.
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Antibacterial activity of (−)-cubebin isolated from Piper Cubeba and its semisynthetic derivatives against microorganisms that cause endodontic infections
Revista Brasileira De Farmacognosia-brazilian Journal of Pharmacognosy, 2016Co-Authors: Karen C S Rezende, Wilson Roberto Cunha, Carlos Henrique Gomes Martins, Patricia Mendonca Pauletti, Ana Helena Januario, Guilherme V Simaro, Viviane Rodrigues Esperandim, Rodrigo Lucarini, Mislaine A. Silva, Jairo Kenupp BastosAbstract:Recent publications have highlighted the numerous biological activities attributed to the lignan (-)-cubebin (1), Piper Cubeba L. f., Piperaceae, and ongoing studies have focused on its structural optimization, in order to obtain derivatives with greater pharmacological potential. The aim of this study was the obtainment of (1), its semisynthetic derivatives and evaluation of antibacterial activity. The extract of the seeds of P. Cubeba was chromatographed, subjected to recrystallization and was analyzed by HPLC and spectrometric techniques. It was used for the synthesis of: (-)-O-methylcubebin (2), (-)-O-benzylcubebin (3), (-)-O-acetylcubebin (4), (-)-O-(N, N-dimethylamino-ethyl)-cubebin (5), (-)-hinokinin (6) and (-)-6.6'-dinitrohinokinin (7). The evaluation of the antibacterial activity has been done by broth microdilution technique for determination of the minimum inhibitory concentration and the minimum bactericidal concentration against Porphyromonas gingivalis, Prevotella nigrescens, Actinomyces naeslundii, Bacteroides fragilis and Fusobacterium nucleatum. It was possible to make an analysis regarding the relationship between structure and antimicrobial activity of derivatives against microorganisms that cause endodontic infections. The most promising were minimum inhibitory concentration =50 µg/ml against P. gingivalis by (2) and (3), and minimum inhibitory concentration =100 µg/ml against B. fragilis by (6). Cytotoxicity assays demonstrated that (1) and its derivatives do not display toxicity.
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in vitro antiparasitic activity and chemical composition of the essential oil obtained from the fruits of Piper Cubeba
Planta Medica, 2013Co-Authors: Viviane Rodrigues Esperandim, Lizandra Guidi Magalhaes, Julia Medeiros Souza, Patricia Mendonca Pauletti, Ana Helena Januario, Jairo Kenupp Bastos, Daniele Da Silva Ferreira, Karen C S Rezende, Rosangela S Laurentz, Guilherme V SimaroAbstract:Protozoans of the trypanosomatid family cause the neglected tropical diseases leishmaniasis and trypanosomiasis, for which few drugs are available. In this context our group has recently reported that the essential oil obtained by steam distillation of the fruits of Piper Cubeba is active against Schistosoma mansoni . Therefore, we have investigated the in vitro effects of the essential oil against the trypomastigote and amastigote forms of Trypanosoma cruzi isolated from an LLCMK 2 cell line culture and the promastigote forms of Leishmania amazonensis . The in vitro activity of the essential oil against trypomastigotes of T. cruzi increased upon rising concentrations, giving IC 50 values of 45.5 and 87.9 µg · mL −1 against trypomastigotes and amastigotes, respectively. The essential oil was not active against L. amazonensis , since it displayed lyses of only 24 % at 400 µg · mL −1 , and an IC 50 of 326.5 µg · mL −1 . Therefore, the essential oil should be further investigated to determine the compounds responsible for the observed activities, as well as its mechanism of action.
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In vitro efficacy of the essential oil of Piper Cubeba L. (Piperaceae) against Schistosoma mansoni
Parasitology Research, 2012Co-Authors: Lizandra G. Magalhães, Guilherme V Simaro, Karen C S Rezende, Jairo K. Bastos, Julia M. Souza, Kamila A. L. Wakabayashi, Rosangela Laurentiz, Adriana H. C. Vinhólis, Vanderlei Rodrigues, Viviane R. EsperandimAbstract:In this paper, cercariae, schistosomula, and adult Schistosoma mansoni worms were incubated in vitro with the essential oil of Piper Cubeba (PC-EO) at concentrations from 12.5 to 200 μg/mL, and the viability was evaluated using an inverted microscopy. The effects of PC-EO at 100 and 200 μg/mL on the stages of S. mansoni were similar to those of the positive control (PZQ at 12.5 μg/mL), with total absence of mobility after 120 h. However, at concentrations from 12.5 to 50 μg/mL, PC-EO caused a reduction in the viability of cercariae and schistosomula when compared with the negative control groups (RPMI 1640 or dechlorinated water) or (RPMI 1640 + 0.1% DMSO or dechlorinated water + 0.1% DMSO). On the other hand, adult S. mansoni worms remained normally active when incubated with PC-EO at concentrations of 12.5 and 25 μg/mL, and their viabilities were similar to those of the negative control groups. In addition, at concentrations ranging from 50 to 200 μg/mL, separation of all the coupled adult worms was observed after 24 h of incubation, which is related to the fact of the reduction in egg production at this concentration. The main chemical constituents of PC-EO were identified by gas chromatography-mass spectrometry as being sabinene (19.99%), eucalyptol (11.87%), 4-terpineol (6.36%), β-pinene (5.81%), camphor (5.61%), and δ-3-carene (5.34%). The cytotoxicity of the PC-EO was determined, and a significant cytotoxicity was only obtained in the concentration of 200 μg/mL after 24 h treatment. The results suggest that PC-EO possesses an effect against cercariae, schistosomula, and adult worms of the S. mansoni .
Rosangela Da Silva De Laurentiz - One of the best experts on this subject based on the ideXlab platform.
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in vitro anthelmintic activity of the crude hydroalcoholic extract of Piper Cubeba fruits and isolated natural products against gastrointestinal nematodes in sheep
Veterinary Parasitology, 2019Co-Authors: Matheus Souza De Paula Carlis, Antonio Carlos De Laurentiz, Rosemeire Da Silva Filardi, Marcio Luis Andrade E Silva, Lizandra Guidi Magalhaes, Aline Feboli, Anna Helena Prizantelli De Oliveira, L A Anjos, Rosangela Da Silva De LaurentizAbstract:Abstract This study describes the in vitro anthelmintic activity of a hydroalcoholic extract from the fruit of Piper Cubeba and its major isolated components against the eggs and larvae of gastrointestinal nematodes obtained from naturally-infected ovines. In vitro anthelmintic activity was evaluated using the egg hatch test (EHT), larval development test (LDT) and L3 migration inhibition test (LMT). The extract showed ovicidal and larvicidal activity, with an EC50 of 200 μg/mL and 83.00 μg/mL in the EHT and LDT, respectively. The extract inhibited 100% of larval migration at the lowest tested concentration (95 μg/mL). The crude extract was purified using successive silica gel chromatographic columns, which revealed the lignans hinokinin, cubebin and dihydrocubebin as the major compounds that were present, which were then used in in vitro tests. Cubebin, dihydrocubebin and hinokinin showed higher activity than the crude extract, with an EC50 for ovicidal activity of 150.00 μg/mL, 186.70 μg/mL and 68.38 μg/mL, respectively. In the LDT, cubebin presented an EC50 of 14.89 μg/mL and dihydrocubebin of 30.75 μg/mL. Hinokinin inhibited 100% the larval development at all concentrations evaluated. In the LMT, dihydrocubebin inhibited 100% the larval migration in all concentrations evaluated while cubebin and hinokinin showed EC50 values of 0.89 μg/mL and 0.34 μg/mL, respectively. P. Cubeba extract is rich in several classes of active compounds, but here we demonstrate that the described anthelmintic activity may be related to the presence of these lignans, which are present in larger concentrations than other components of the extract. Our results demonstrate for first time the anthelmintic activity against gastrointestinal nematodes in sheep for this class of special metabolites that are present in P. Cubeba fruit. However, future detailed studies are needed to evaluate the effectiveness of P. Cubeba fruits extract and active lignans in in vivo tests.
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medicinal attributes of lignans extracted from Piper Cubeba current developments
ChemistryOpen, 2018Co-Authors: Regiane Godoy De Lima, Maria Teresa Barros, Rosangela Da Silva De LaurentizAbstract:: Lignans are a large class of natural products that have been isolated from many plants. They reveal diverse biological activities, especially antiviral and antitumor properties. From Piper Cubeba, lignans of several classes can be isolated from the roots, rhizomes, stems, leaves, seeds, and fruits. Among its various chemical constituents, (-)-cubebin and (-)-hinokinin are found in significant quantities. Although they have been known for some time, during the last few decades their biological properties have been studied by several research groups. The cubebins have been identified as a lactol monomer and dimers as a mixture of diastereoisomers. Recently, their structural characterization and the synthesis of the possible structures have led to the correction of some earlier structural proposals. This review describes the more recent developments in the study of the medicinal attributes of cubebin and hinokinin extracted from Piper Cubeba and the synthesis and biological testing of some analogues.
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parâmetros sanguineos de frangos de corte alimentados com dietas suplementadas com sementes secas de Piper Cubeba como aditivo fitogenico
Pesquisa Veterinaria Brasileira, 2016Co-Authors: Rodolfo M Domingues, Antonio Carlos De Laurentiz, Alan Peres Ferraz De Melo, E S Mello, Rosemeire Da Silva Filardi, Sergio Sobrane T Filho, Marcio Luis Andrade E Silva, Rosangela Da Silva De LaurentizAbstract:Two experiments were conducted to evaluate the use of dried seeds of Piper Cubeba in the diets of 1 to 21-day-old broilers and its effect on biochemical blood profile and biometry of the organs. In each experiment, 240 one-day-old male broiler chicks Cobb were distributed in a completely randomized design with five treatments and four replicates of 12 birds per experimental plot. The first experiment evaluated the use of Piper Cubeba in considered highly digestible diets based on corn and soybean meal, and the second evaluated the use of pepper in low digestibility diets, which were obtained with the inclusion of meat and bone meal. Regarding the blood chemistry profile data of the experiment I, with the exception of gamma glutamyl transferase, all other serum levels were within recommended limits for poultry, and only triglyceride levels differed between treatments (P 0.05) for the biometry of organs. The conditions under which the experiments were performed at inclusion of Piper Cubeba seeds in feed for broilers has not provided any toxicity to poultry.
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avaliacao da atividade antimicobacteriana da lignana diidrocubebina extraida da Piper Cubeba e de seus derivados semissinteticos
Revista Brasileira de Plantas Medicinais, 2015Co-Authors: Rosangela Da Silva De Laurentiz, Antonio Carlos De Laurentiz, Marcio Luis Andrade E Silva, Alexandre Luiz Souto Borges, Carlos Henrique Gomes MartinsAbstract:The antimycobacterial activity of the dihydrocubebin (1), a dibenzylbutanedioiclignan obtained from ethanolic extract of Piper Cubeba seeds, and its derivatives were examined in vitro against three different strains of Mycobacterium using amicrodilution method. Among the lignans evaluated, the 3 and 4 samples were the most active ones, displaying MIC values of 62.5 μg/mL against M. avium and M. tuberculosis, respectively. The derivatives 2-6, obtained for partial synthesis, had different substituents in the carbons 9 and 9’, fact thatalters the polarity, solubility and restricts the free rotations between the bonds C8-C8’ in relation to the starting material (1). The structural differences among these compounds provide important information about the antimycobacterial structure-activity relationship of the dibenzylbutanodioic skeleton, obtained from natural source, such as a possible target for the development of more powerful drugs against tuberculosis.