Antiparasitic properties of 4-nerolidylcatechol from Pothomorphe umbellata (L.) Miq. (Piperaceae) in vitro and in mice models with either prepatent or patent Schistosoma mansoni infections.

ETHNOPHARMACOLOGICAL RELEVANCE: Roots of Pothomorphe umbellata (L.) Miq. are used in traditional medicine of Africa and South America for the treatment of malaria and helminthiasis. However, neither P. umbellata nor its isolated compounds have been evaluated against Schistosoma species. AIMS OF THIS STUDY: To investigate the antischistosomal effects of P. umbellata root extracts and the isolated compound 4-nerolidylcatechol (4-NC) against Schistosoma mansoni ex vivo and in murine models of schistosomiasis. MATERIALS AND METHODS: The crude hydroalcoholic (PuE) and hexane (PuH) extracts of P. umbellata roots were prepared and initially submitted to an ex vivo phenotypic screening against adult S. mansoni. PuH was analyzed by HPLC-DAD, characterized by UHPLC-HRMS/MS, and submitted to chromatographic fractionation, leading to the isolation of 4-NC. The anthelmintic properties of 4-NC were assayed ex vivo against adult schistosomes and in murine models of schistosomiasis for both patent and prepatent S. mansoni infections. Praziquantel (PZQ) was used as a reference compound. RESULTS: PuE (EC50: 18.7 µg/mL) and PuH (EC50: 9.2 µg/mL) kill adult schistosomes ex vivo. The UHPLC-HRMS/MS analysis of PuH, the most active extract, revealed the presence of 4-NC, peltatol A, and peltatol B or C. After isolation from PuH, 4-NC presented remarkable in vitro schistosomicidal activity with EC50 of 2.9 µM (0.91 µg/mL) and a selectivity index higher than 68 against Vero mammalian cells, without affecting viability of nematode Caenorhabditis elegans. In patent S. mansoni infection, the oral treatment with 4-NC decreased worm burden and egg production in 52.1% and 52.3%, respectively, also reducing splenomegaly and hepatomegaly. 4-NC, unlike PZQ, showed in vivo efficacy against juvenile S. mansoni, decreasing worm burden in 52.4%. CONCLUSIONS: This study demonstrates that P. umbellata roots possess antischistosomal activity, giving support for the medicinal use of this plant against parasites. 4-NC was identified from P. umbellata roots as one of the effective in vitro and in vivo antischistosomal compound and as a potential lead for the development of novel anthelmintics.

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase.

Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities of cardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three-dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases.

Evaluation of Gibbilimbol B, Isolated from Piper malacophyllum (Piperaceae), as an Antischistosomal Agent.

Infections caused by parasitic worms impose a considerable worldwide health burden. One of the most impactful is schistosomiasis, a disease caused by blood-dwelling of the genus Schistosoma that affects more than 230 million people worldwide. Since praziquantel has also been extensively used to treat schistosomiasis and other parasitic flatworm infections, there is an urgent need to identify novel anthelmintic compounds, mainly from natural sources. In this study, the hexane extract from roots of Piper malacophyllum (Piperaceae) showed to be mainly composed for gibbilimbol B by HPLC/ESI-HRMS. Based on this result, this compound was isolated by chromatographic steps and its structure was confirmed by NMR. In vitro bioassays showed that gibbilimbol B was more active than praziquantel against larval stage of S. mansoni, with effective concentrations of 50 % (EC50 ) and 90 % (EC90 ) values of 2.6 and 3.4 µM, respectively. Importantly, gibbilimbol B showed no cytotoxicity to mammalian cells at a concentration 190 times greater than the antiparasitic effect, giving support for the anthelmintic potential of gibbilimbol B as lead compound for novel antischistosomal agents.

Isolation, synthesis and absolute configuration of 4,5-dihydroxypiperines improving behavioral disorder in AlCl3-induced dementia.

A pair of stereoisomers of new 4,5-dihydroxypiperine was isolated from P. retrofractum and showed profound activity on AlCl3-induced dementia. In order to determine their absolute configurations and biological activities, all four possible stereoisomers of 4,5-dihydroxypiperine were synthesized from piperidine by Sharpless asymmetric dihydroxylation and Mitsunobu reaction. Their absolute configurations were established as (4R,5R) (1), (4S,5S) (2), (4S,5R) (3) and (4R,5S) (4) by NMR, optical rotation and CD spectra. It is note that only compound 4 improved behavioral disorder in AlCl3-induced dementia. Accordingly, the pair of stereoisomers isolated from P. retrofractum was determined to be (4S,5S) and (4R,5S)-isomers (2 and 4). The ratio of the epimers was present as 1:0.7 (4:2).

Phytochemistry and anti-inflammatory activities of Piper kadsura (Choisy) Ohwi ­ a review / Actividades fitoquímicas y antiinflamatorias de Piper kadsura (Choisy) Ohwi - una revisión

Piper kadsura (Choisy) Ohwi which belongs to the family Piperaceae, is a well-known medicinal plant possessing high medicinal and various therapeutic properties. It is widely used in traditional Chinese medicine for the treatment of asthma and rheumatic arthritis. Numerous studies on this species have also corroborated the significant anti-inflammatory potential of its extracts and secondary metabolites. The main chemical constituents which have been isolated and identified from P. kadsura are lignans and neolignans, which possess anti-inflammatory activities. The present article aims to provide a review of the studies done on the phytochemistry and antiinflammatory activities of P. kadsura. The scientific journals for this brief literature review were from electronic sources, such as Science Direct, PubMed, Google Scholar, Scopus, and Web of Science. This review is expected to draw the attention of the medical professionals and the general public towards P. kadsura and to open the door for detailed research in the future.

Piper kadsura (Choisy) Ohwi, perteneciente a la familia Piperaceae, es una planta medicinal conocida que posee importantes propiedades medicinales y diversas propiedades terapéuticas. Es ampliamente utilizada en la medicina tradicional china para el tratamiento del asma y la artritis reumática. Numerosos estudios sobre esta especie también han corroborado el destacado potencial antiinflamatorio de sus extractos y metabolitos secundarios. Los principales componentes químicos que se han aislado e identificado de P. kadsura son los lignanos y los neolignanos, que poseen actividades antiinflamatorias. El presente artículo tiene como objetivo proporcionar una revisión de los estudios realizados sobre las actividades fitoquímicas y antiinflamatorias de P. kadsura. Las revistas científicas para esta breve revisión de literatura fueron de fuentes electrónicas, como Science Direct, PubMed, Google Scholar, Scopus y Web of Science. Se espera que esta revisión atraiga la atención de los profesionales médicos y el público en general respecto de P. kadsura y abra la puerta a una investigación detallada en el futuro.

Antitrypanosomal activity and effect in plasma membrane permeability of (-)-bornyl p-coumarate isolated from Piper cernuum (Piperaceae).

This work describes the isolation of six metabolites from leaves and branches of Piper cernuum (Piperaceae): (-)-cubebin (1), (-)-hinokinin (2), (-)-kusunokinin (3), trans-dehydroagarofuran (4), 11-hydroxi-4,5-secoeudesmane-4,5-dione (5), and (-)-bornyl p-coumarate (6). Antitrypanosomal activity and toxicity of purified compounds were performed in vitro against trypomastigote forms of Trypanosoma cruzi and NCTC cells, respectively. Compounds 2, 3 and 5 showed moderate activities with IC50 values of 33.1, 31.8 and 45.9 µM, respectively, while compounds 1 and 4 were inactive (IC50 > 100 µM). On the other hand, compound 6 displayed an IC50 value of 2.1 µM, a selectivity index (SI) of 18 and induced a considerable interference in the plasma membrane permeability (87%) in trypomastigotes of T. cruzi. Additionally, the lethal effect of compound 6 in T. cruzi could be associated to the plasma membrane permeability. Finally, experiments using scanning electron microscopy (SEM) confirmed the obtained results in which was possible to observe total alteration parasites topography after treatment with compound 6 in comparison to untreated parasites. These data indicated that the lethal action of compound 6 is directly related to structural disruption of the membrane.

Selected α-pyrones from the plants Cryptocarya novoguineensis (Lauraceae) and Piper methysticum (Piperaceae) with activity against Haemonchus contortus in vitro.

Due to the widespread occurrence and spread of anthelmintic resistance, there is a need to develop new drugs against resistant parasitic nematodes of livestock animals. The Nobel Prize-winning discovery and development of the anti-parasitic drugs avermectin and artemisinin has renewed the interest in exploring natural products as anthelmintics. In the present study, we screened 7500 plant extracts for in vitro-activity against the barber's pole worm, Haemonchus contortus, a highly significant pathogen of ruminants. The anthelmintic extracts from two plants, Cryptocarya novoguineensis and Piper methysticum, were fractionated by high-performance liquid chromatography (HPLC). Subsequently, compounds were purified from fractions with significant biological activity. Four α-pyrones, namely goniothalamin (GNT), dihydrokavain (DHK), desmethoxyyangonin (DMY) and yangonin (YGN), were purified from fractions from the two plants, GNT from C. novoguineensis, and DHK, DMY and YGN (= kavalactones) from P. methysticum. The three kavalactones induced a lethal, eviscerated (Evi) phenotype in treated exsheathed third-stage larvae (xL3s), and DMY and YGN had moderate potencies (IC50 values of 31.7 ±â€¯0.23 µM and 23.7 ±â€¯2.05 µM, respectively) at inhibiting the development of xL3s to fourth-stage larvae (L4s). Although GNT had limited potency (IC50 of 200-300 µM) at inhibiting L4 development, it was the only compound that reduced L4 motility (IC50 of 6.25-12.50 µM). The compounds purified from each plant affected H. contortus in an irreversible manner. These findings suggest that structure-activity relationship studies of α-pyrones should be pursued to assess their potential as anthelmintics.

Leishmanicidal Effects of Piperlongumine (Piplartine) and Its Putative Metabolites.

Piperlongumine is an amide alkaloid found in Piperaceae species that shows a broad spectrum of biological properties, including antitumor and antiparasitic activities. Herein, the leishmanicidal effect of piperlongumine and its derivatives produced by a biomimetic model using metalloporphyrins was investigated. The results showed that IC50 values of piperlongumine in promastigote forms of Leishmania infantum and Leishmania amazonensis were 7.9 and 3.3 µM, respectively. The IC50 value of piperlongumine in the intracellular amastigote form of L. amazonensis was 0.4 µM, with a selectivity index of 25. The piperlongumine biomimetic derivatives, Ma and Mb, also showed leishmanicidal effects. We also carried out an in vitro metabolic degradation study showing that Ma is the most stable piperlongumine derivative in rat liver microsome incubations. The results presented here indicate that piperlongumine is a potential leishmanicidal candidate and support the biomimetic approach for development of new antileishmanial derivatives.

Structure-Activity Relationships and Docking Studies of Hydroxychavicol and Its Analogs as Xanthine Oxidase Inhibitors.

Hydroxychavicol (HC), which is obtained from the leaves of Piper betle LINN. (Piperaceae), inhibits xanthine oxidase (XO) with an IC50 value of 16.7 µM, making it more potent than the clinically used allopurinol (IC50=30.7 µM). Herein, a structure-activity relationship analysis of the polar part analogs of HC was conducted and an inhibitor was discovered with a potency 13 times that of HC. Kinetic studies have revealed that HC and its active analog inhibit XO in an uncompetitive manner. The binding structure prediction of these inhibitor molecules to the XO complex with xanthine suggested that both compounds (HC and its analog) could simultaneously form hydrogen bonds with xanthine and XO.

First phytochemical description of essential oils from Piper cachimboense (Piperales, Piperaceae) / Primeira descrição fitoquímica de óleos essenciais de Piper cachimboense (Piperales, Piperaceae)

Piper cachimboense is recorded only for the Amazon region of Brazil and Colombia, and the objective of this study was to report the first phytochemical assessment of the composition of the essential oils (EOs) from this species collected in the Amazon rainforest, in Novo Progresso, Pará State, Brazil. Samples of leaves were subjected to hydrodistillation in a Clevenger-type apparatus. The chemical identification was carried out by gas chromatography. The yield of oils was of 11.03 ± 5.94% for fresh leaves, and 1.07 ± 0.27% for dry leaves. The analysis showed 36 volatile compounds from fresh leaves and 49 from dried leaves. Main constituents in EOs of both fresh and dried leaves from P. cachimboense were (E)-caryophyllene, germacrene-D, -amorfene, -cadinene and apiole.

Piper cachimboense é registrada apenas para a região amazônica do Brasil e Colômbia, e o objetivo deste estudo foi relatar, pela primeira vez, a composição fitoquímica dos óleos essenciais (OEs) desta espécie coletada na floresta amazônica, em Novo Progresso/PA, Brasil. Amostras de folhas foram submetidas a hidrodestilação em aparelho tipo Clevenger. A identificação química foi realizada por cromatografia gasosa e o rendimento dos óleos foi de 11,03 ± 5,94% para as folhas frescas e de 1,07 ± 0,27% para as folhas secas. A análise mostrou 36 compostos voláteis para folhas frescas e 49 para folhas secas. Os constituintes principais dos OEs de folhas frescas e secas de P. cachimboense foram (E)-cariofileno, germacreno-D, -amorfeno, -cadineno e apiol.

Effect of piplartine and cinnamides on Leishmania amazonensis, Plasmodium falciparum and on peritoneal cells of Swiss mice.

CONTEXT: Plants of the Piperaceae family produce piplartine that was used to synthesize the cinnamides. OBJECTIVE: To assess the effects of piplartine (1) and cinnamides (2-5) against the protozoa responsible for malaria and leishmaniasis, and peritoneal cells of Swiss mice. MATERIALS AND METHODS: Cultures of Leishmania amazonensis, Plasmodium falciparum-infected erythrocytes, and peritoneal cells were incubated, in triplicate, with different concentrations of the compounds (0 to 256 µg/mL). The inhibitory concentration (IC50) in L. amazonensis and cytotoxic concentration (CC50) in peritoneal cell were assessed by the MTT method after 6 h of incubation, while the IC50 for P. falciparum-infected erythrocytes was determined by optical microscopy after 48 or 72 h of incubation; the Selectivity Index (SI) was calculated by CC50/IC50. RESULTS: All compounds inhibited the growth of microorganisms, being more effective against P. falciparum after 72 h of incubation, especially for the compounds 1 (IC50 = 3.2 µg/mL) and 5 (IC50 = 6.6 µg/mL), than to L. amazonensis (compound 1 = 179.0 µg/mL; compound 5 = 106.0 µg/mL). Despite all compounds reducing the viability of peritoneal cells, the SI were <10 to L. amazonensis, whereas in the cultures of P. falciparum the SI >10 for the piplartine (>37.4) and cinnamides 4 (>10.7) and 5 (= 38.4). DISCUSSION AND CONCLUSION: The potential of piplartine and cinnamides 4 and 5 in the treatment of malaria suggest further pre-clinical studies to evaluate their effects in murine malaria and to determine their mechanisms in cells of the immune system.

Local Anesthetic Activity from Extracts, Fractions and Pure Compounds from the Roots of Ottonia anisum Spreng. (Piperaceae).

Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage) is demonstrated for the first time in vivo guinea pig model. Phytochemical investigation led to the isolation of three amides (pipercallosidine, piperine and valeramide) and in an enriched mixture of seven amides (valeramide, 4,5-dihydropiperlonguminine, N-isobutil-6-piperonil-2-hexenamide, piperovatine, dihydropipercallosidine, pipercallosidine and pipercallpsine). Our findings demonstrated the anesthetic potential for the methanolic extract from roots, its n-hexane partition and amides from O. anisum and it is in agreement with ethnobotanical survey.

Effects of Extracts from Thai Piperaceae Plants against Infection with Toxoplasma gondii.

Herbal medicines and natural herb extracts are widely used as alternative treatments for various parasitic diseases, and such extracts may also have potential to decrease the side effects of the standard regimen drugs used to treat toxoplasmosis (sulfadiazine-pyrimethamine combination). We evaluated how effective the Thai piperaceae plants Piper betle, P. nigrum and P. sarmentosum are against Toxoplasma gondii infection in vitro and in vivo. Individually, we extracted the piperaceae plants with ethanol, passed them through a rotary evaporator and then lyophilized them to obtain crude extracts for each one. The in vitro study indicated that the P. betle extract was the most effective extract at inhibiting parasite growth in HFF cells (IC50 on RH-GFP: 23.2 µg/mL, IC50 on PLK-GFP: 21.4 µg/mL). Furthermore, treatment of experimental mice with the P. betle extract for 7 days after infection with 1,000 tachyzoites of the T. gondii PLK strain increased their survival (survival rates: 100% in 400 mg/kg-treated, 83.3% in 100 mg/kg-treated, 33.3% in 25 mg/kg-treated, 33.3% in untreated mice). Furthermore, treatment with 400 mg/kg of the P. betle extract resulted in 100% mouse survival following infection with 100,000 tachyzoites. The present study shows that P. betle extract has the potential to act as a medical plant for the treatment of toxoplasmosis.

Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.

The essential oils from leaves of Piper malacophyllum (Piperaceae) showed to be mainly composed by two alkenylphenol derivatives: gibbilimbols A and B. After isolation and structural characterization by NMR and MS data analysis, both compounds were evaluated against promastigote/amastigote forms of Leishmania (L.) infantum as well as trypomastigote/amastigote forms of Trypanosoma cruzi. The obtained results indicated that gibbilimbol B displayed potential against the tested parasites and low toxicity to mammalian cells, stimulating the preparation of several quite simple synthetic analogues in order to improve its activity and to explore the preliminary structure-activity relationships (SAR) data. Among the prepared derivatives, compound LINS03003 (n-octyl-4-hydroxybenzylamine) displayed the most potent IC50 values of 5.5 and 1.8 µM against amastigotes of T. cruzi and L. (L.) infantum, respectively, indicating higher activity than the natural prototype. In addition, this compound showed remarkable selectivity index (SI) towards the intracellular forms of Leishmania (SI=13.1) and T. cruzi (SI=4.3). Therefore, this work indicated that preparation of synthetic compounds structurally based in the bioactive natural products could be an interesting source of novel and selective compounds against these protozoan parasites.

Investigation of local anesthetic and antimycobacterial activity of Ottonia martiana Miq. (Piperaceae).

Ottonia martiana is a plant popularly known in Brazil by the use for toothache. Ethanolic extract (EE), hexane fraction (HF), dichloromethane fraction (DF) and piperovatine obtained from O. martiana were assayed in vitro and in vivo. The acute toxicity of EE was determined, and LD50 values of 164.5 and 65.0 mg/kg by the oral and intraperitoneal routes, respectively, indicated a high toxicity for EE in vivo, explaining its popular use by topical administration only. A local anesthetic-like effect of EE and its fractions was observed in experimental models using pain induction, and such effect involved an analgesic action. The antimycobacterial activity of EE, HF, DF and piperovatine was evaluated against Mycobacterium tuberculosis H37Rv ATCC 27924. EE, HF, DF, and piperovatine showed a potential antimycobacterial effect with MICs of 16.0, 62.0, 62.0 and 8.0 µg/mL, respectively. Piperovatine was more effective than the EE or the other fractions. The selectivity index (SI=IC50/MIC) values calculated for EE, HF, DF and piperovatine based on the MICs and the cytotoxicity against J774 macrophages (IC50 by MTT assay) revealed values of 6.43, 2.34, 1.5 and 9.66, respectively.

Cytotoxic Amides from Fruits of Kawakawa, Macropiper excelsum.

Cytotoxic amides have been isolated from the fruits of the endemic New Zealand medicinal plant kawakawa, Macropiper excelsum (Piperaceae). The main amide was piperchabamide A and this is the first report of this rare compound outside the genus Piper. Eleven other amides were purified including two new compounds with the unusual 3,4-dihydro-1(2H)-pyridinyl group. The new compounds were fully characterized by 2D NMR spectroscopy, which showed a slow exchange between two rotamers about the amide bond, and they were chemically synthesized. In view of the antitumor activity of the related piperlongumine, all of these amides plus four synthetic analogs were tested for cytotoxicity. The most active was the piperine homolog piperdardine, with an IC50 of 14 µM against HT 29 colon cancer cells.

Psychoneuropharmacological activities and chemical composition of essential oil of fresh fruits of Piper guineense (Piperaceae) in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Piper guineense Schum & Thonn (Piperaceae) is a medicinal plant used in the Southern States of Nigeria to treat fever, mental disorders and febrile convulsions. AIMS OF THE STUDY: This study aims at determining the chemical composition and the central nervous system (CNS) activities of the essential oil obtained from the plant׳s fresh fruits in order to rationalize its folkloric use. MATERIALS AND METHODS: Essential oil of P. guineense (EOPG) obtained by hydrodistillation was analysed by GC/MS. EOPG (50-200mg/kg, i.p.) was evaluated for behavioural, hypothermic, sedative, muscle relaxant, anti-psychotic and anticonvulsant activities using standard procedures. RESULTS AND DISCUSSION: Analysis of the oil reveals 44 compounds of which 30 compounds constituting 84.7% were identified. The oil was characterized by sesquiterpenoids (64.4%) while only four monoterpeneoids (21.3%) were found present in the oil. Major compounds identified were ß-sesquiphellandrene (20.9%), linalool (6.1%), limonene (5.8%), Z-ß-bisabolene (5.4%) and α-pinene (5.3%). The EOPG (50-200mg/kg, i.p.) caused significant (p<0.01) inhibition on rearing {F(4,20)=43}, locomotor {F(4,20)=22} activity and decreased head dips in hole board {F(4,20)=7} indicating CNS depressant effect; decreased rectal temperature {F(4,20)=7-16}, signifying hypothermic activity; decreased ketamine-induced sleep latency {F(4,20)=7.8} and prolonged total sleeping time {F(4,20)=8.8}, indicating sedative effect; reduced muscular tone on the hind-limb grip test {F(4,20)=22}, inclined board {F(4,20)=4-49} and rota rod {F(4,20)=13-106}, implying muscle relaxant activity; induced catalepsy {F(4,20)=47-136}, inhibited apomorphine-induced climbing behaviour {F(4,20)=9} and inhibited apomorphine-induced locomotor {F(4,20)=16}, suggesting anti-psychotic effect; and protected mice against pentylenetetrazole-induced convulsions, indicating anticonvulsant potential. CONCLUSION: The most abundant component of the fresh fruits essential oil of P. guineense was ß-sesquiphellandrene (20.9%); and the oil possesses CNS depressant, hypothermic, sedative, muscle relaxant, antipsychotic and anticonvulsant activities, thus providing scientific basis for its ethnomedicinal applications.

Effect of ripening and heat processing on the physicochemical and rheological properties of pepper pectins.

Water-, chelator-, and alkali-soluble pectins were isolated from raw and heat-processed Jalapeño peppers (green and red) and their physiochemical and rheological properties were determined. The yield, tristimulus color, degree of methyl esterification, monosaccharide composition, molecular weights distribution, and protein content depended on ripening and heat processing. The viscosity properties of pectins were independent of ripening. The water-soluble pectin was the most abundant pectin. Pectins from grilled peppers showed the lowest L* values. The alkali-soluble pectin showed the highest protein content. The content of xylose, rhamnose, and mannose in pectins was highly altered by tested factors. The degree of methyl esterification of pectins ranged from 26.8 to 91.6%. The peak Mw of the main fraction of tested pectins was sequentially reduced by ripening and heat processing. Pectins from raw peppers showed the best viscosity properties.

Evaluación de la actividad repelente de aceites esenciales de plantas Piperáceas del departamento de Chocó, Colombia / Evaluation of repellent activity of essential oils from plants Piperaceae Department of Chocó, Colombia

El objetivo de este trabajo fue determinar la composición química volátil del aceite esencial de varias especies de Piperáceas (Piper dilatatum, Piper aduncum, Piper divaricatum, Piper sp, Piper sanctifelicis) y la actividad repelente de ellos contra el gorgojo de granos almacenados Tribolium castaneum Herbst. Los aceites esenciales se obtuvieron por hidrodestilación, la separación e identificación de los componentes volátiles se realizó por cromatografía de gases acoplada a espectrometría de masas y para la evaluación de la actividad repelente se empleó el método de área de preferencia. Los compuestos mayoritarios encontrados en Piper dilatatum fueron el apiol 89,0% y trans-cariofileno (3,5%); en Piper divaricatum, eugenol (37,5%) y metil eugenol (36,3%); Piper sp, alpha-gurjuneno (o guaieno) (24,9%) y elemol (14,2%); Piper sanctifelicis, Delta-3-careno (35,3%) y limoneno (27,1%); Piper aduncum, dilapiol (48,2%) y 1,8 cineol (11,4%). Los porcentajes de repelencia de los aceites esenciales a una concentración de 1 µL/cm2, a un tiempo de exposición de 2 horas frente al T. castaneum fueron: Piper aduncum (99%), Piper sp (96%), Piper dilatatum (82%), Piper divaricatum (76%), Piper santifelicis (33%) (AU)

The objective of this study was to determine the volatile chemical composition of the essential oil of various species of Piperaceae (Piper dilatatum, Piper aduncum, Piper divaricatum, Piper sp, Piper sanctifelicis) and repellent activity of them against weevil stored grain Tribolium castaneum Herbst . Essential oils were obtained by hydrodistillation, the separation and identification of volatile components was performed by gas chromatography-mass spectrometry and to evaluate the repellent activity the area method was used preferably. The major compounds found in Piper dilatatum were 89.0% and apiol trans-caryophyllene (3.5%); Piper divaricatum, eugenol (37.5%) and methyl eugenol (36.3%); -gurjunene (or guaiene) (24.9%) and elemol (14.2%);Piper sp, Piper sanctifelicis, -(35.3%) and limonene (27.1%);3-carene Piper aduncum, dilapiol (48.2%) and 1,8 cineole (11.4%). Percent repellency of essential oils at a concentration of 1 uL / cm2, to an exposure time of 2 hours against T. castaneum were: Piper aduncum (99%), Piper sp (96%), Piper dilatatum (82 %), Piper divaricatum (76%), Piper santifelicis (33%)

Anti-inflammatory, antinociceptive activity of an essential oil recipe consisting of the supercritical fluid CO2 extract of white pepper, long pepper, cinnamon, saffron and myrrh in vivo.

This study was designed to investigate the anti-inflammatory and antinociceptive activities of essential oil recipe (OR) in rodents. The anti-inflammatory activity was evaluated by inflammatory models of dimethylbenzene (DMB)-induced ear vasodilatation and acetic acid-induced capillary permeability enhancement in mice whereas the antinociceptive activity was evaluated using acetic acid-induced writhes and hot plate test methods in mice. Additionally, the chemical composition of OR has been also analyzed by gas chromatography and mass spectrometry (GC/MS). 37 compounds, representing 74.42% of the total oil content, were identified. ß-Selinene (7.38%), aromadendrene (5.30%), ß-elemene (5.22%), cis-piperitol (5.21%), cis-ß-guaiene (4.67%), ylangene (3.70%), 3-heptadecene (3.55%), δ-cadinene (3%) and ß-cadinene (2.87%) were found to be the major constituents of the oil. Oral pretreatment with OR (62.5-1000 mg/kg) not only decreased the DMB-induced ear vasodilatation but also attenuated capillary permeability under acetic acid challenge in mice. OR significantly reduced the writhing number evoked by acetic acid injection. All test samples showed no significant analgesic activity on the hot plate pain threshold in mice. These data demonstrated that the OR inhibits inflammatory and peripheral inflammatory pain. These results may support the fact that the essential oil of traditional Hui prescription played a role in the inflammation of stroke.