Planta Medica International Open最新文献

{"title":"An Ethanolic Extract of Boehmeria caudata Aerial Parts Displays Anti-inflammatory and Anti-tumor Activities","authors":"P. P. de Paiva, F. R. Nonato, A. Ruiz, I. Sousa, R. R. T. Zafred, D. D. de Oliveira, R. Catharino, M. Foglio, J. D. de Carvalho","doi":"10.1055/a-1111-9907","DOIUrl":"https://doi.org/10.1055/a-1111-9907","url":null,"abstract":"Abstract The tumor microenvironment presents several therapeutic targets, with inflammation being one of them. In search of new drugs, plants have shown to be an effective source of potent anti-inflammatory and anticancer agents. This study aimed to evaluate the antitumoral and inflammatory activities of Boehmeria caudata aerial parts extract. Bioguided in vitro antiproliferative screening showed that phenanthroquinolizidine obtained from the aerial B. caudata ethanolic extract had a straight relationship with activity. Moreover, the orally administered ethanolic extract reduced Ehrlich solid tumor growth and displayed an anti-inflammatory effect in both evaluated experimental models (carrageenan-induced paw edema and croton oil-induced ear edema). These results suggest that the antitumor activity of the ethanolic extract could be explained by antiproliferative effects associated with anti-inflammatory action.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"30 1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123581682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chemical Constituents of the Terrestrial Stems of Ephedra sinica and their PPAR-γ Ligand-Binding Activity","authors":"Y. Matsuo, M. Sasaki, H. Fukaya, Katsunori Miyake, Riko Takeuchi, H. Kumata, Y. Mimaki","doi":"10.1055/a-1094-9229","DOIUrl":"https://doi.org/10.1055/a-1094-9229","url":null,"abstract":"Abstract Bioassay-guided fractionation of the MeOH extract of Ephedra sinica terrestrial stems, using a PPAR-γ ligand binding assay, resulted in the isolation of 10 compounds, including one new bisabolane-type sesquiterpenoid (10). The structure of the new compound was determined by extensive spectroscopic analysis, including two-dimensional (2D) NMR. Among the isolated compounds, the sitosterol derivatives (1 and 2), flavonoid glucoside (7), and the new sesquiterpenoid (10), showed significant PPAR-γ ligand-binding activity.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"66 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114757117","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Inhibition of HIF-1α through Suppression of NF-κB Activation by Compounds Isolated from Senecio graveolens","authors":"Luis Apaza Ticona, Nuria Cano-Adamuz, A. Serban, Ángel Rumbero Sánchez","doi":"10.1055/a-1063-6722","DOIUrl":"https://doi.org/10.1055/a-1063-6722","url":null,"abstract":"Abstract One of the characteristics of cancer is that the lack of oxygen in the cancer cells triggers changes in their gene expression. This hypoxia activates hypoxia-inducible factor 1-alpha and this in turn sets in motion the whole family of important angiogenic genes for the tumour. Hypoxia-inducible factor 1-alpha therefore increases the density and vascular permeability within the tumours, facilitating their rapid growth and, later, the metastasis. Senecio graveolens is a South American medicinal plant commonly used for mountain sickness (lack of adaptation of the organism to hypoxia). Additionally, pharmacological studies showed that its alcoholic extracts have cytotoxic properties. This research aimed to perform a guided phytochemical study of S. graveolens to identify compounds capable of inhibiting hypoxia-inducible factor 1-alpha through suppression of nuclear factor kappa-light-chain-enhancer of activated B cell activation. The isolation led to the characterisation of phanurane (1), damsine (2), and scoparone (3), first reported in the S. graveolens species. Phanurane (1 ) showed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=20.66±0.04 μM), A549 (IC50=25.80±0.04 μM), Hep G2 (IC50=29.21±0.03 μM), and Caco-2 (IC50=38.58±0.02 μM). Damsine (2) hypoxia-inducible factor 1-alpha displayed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=2.29±0.07 μM), A549 (IC50=4.13±0.04 μM), Hep G2 (IC50=6.40±0.03 μM), and Caco-2 (IC50=9.80±0.04 μM). Finally, scoparone (3) displayed inhibitory activity of hypoxia-inducible factor 1-alpha on the cancer cell lines U-373 MG (IC50=15.22±0.01 μM), A549 (IC50=17.47±0.02 μM), Hep G2 (IC50=18.26±0.06 μM), and Caco-2 (IC50=19.75±0.04 μM). In addition, phanurane (1 ) displayed inhibitory activity over nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=7.13±0.03 μM), A549 (IC50=8.64±0.03 μM), Hep G2 (IC50=8.87±0.04 μM), and Caco-2 (IC50=15.11±0.01 μM). Likewise, damsine (2) showed inhibitory activity over nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=2.28±0.01 μM), A549 (IC50=3.79±0.02 μM), Hep G2 (IC50=3.98±0.05 μM), and Caco-2 (IC50=6.41±0.02 μM). Lastly, scoparone (3) displayed inhibitory activity of nuclear factor kappa-light-chain-enhancer of activated B cells on cancer cell lines U-373 MG (IC50=3.62±0.06 μM), A549 (IC50=4.48±0.03 μM), Hep G2 (IC50=5.25±0.01 μM), and Caco-2 (IC50=11.90±0.02 μM). This study corroborates the cytotoxic activity of the isolated compounds through the inhibition of hypoxia-inducible factor 1-alpha as well as its modulator nuclear factor kappa-light-chain-enhancer of activated B cells.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130449861","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Laccaridione C, a Bioactive Polyketide from the Fungus Montagnula sp.","authors":"C. Almeida, Thomas A. Mackenzie, V. González-Menéndez, N. de Pedro, I. Pérez‐Victoria, G. Crespo, Jesús Martín, O. Genilloud, F. Vicente, B. Cautain, F. Reyes","doi":"10.1055/a-1032-3346","DOIUrl":"https://doi.org/10.1055/a-1032-3346","url":null,"abstract":"Abstract The new polyketide laccaridione C (1) was obtained by bioassay-guided isolation of organic extracts of the fungal strain CF-223743, isolated from dung collected in a forest of Grand Comoros Island. Its structure was established using spectroscopic methods, namely HRMS and 1D and 2D NMR. The new compound was tested against seven cancer cell lines, evidencing effective activity against melanoma (A2058) with an IC50 of 13.2 µM, and an increased activity against breast cancer (MCF-7) with an IC50 of 3.7 µM. The strain CF-223743 was taxonomically identified as Montagnula sp. based on ITS/28S analysis","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"42 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130382692","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Supercritical Extracts from Arctium lappa as a Potential Inhibitor for the Activation of Complement System ","authors":"P. Fontana, L. Bavia, F. Bovo, A. R. C. Souza, M. Corazza, I. Messias-Reason","doi":"10.1055/a-1025-0085","DOIUrl":"https://doi.org/10.1055/a-1025-0085","url":null,"abstract":"Abstract Arctium lappa is a perennial species of the Asteraceae family originally from Europe and Asia. Considered a weed species in the southern region of Brazil, it is popularly used as a natural anti-inflammatory. The complement system is an important component of the innate immune response. However, its exacerbated activation can lead to harmful conditions like autoimmune and inflammatory disorders. Plants that inhibit the activation of complement can be a promising tool in the treatment of inflammatory diseases. Here, we evaluated the effect of A. lappa leaves extracts on the activation of the classical and alternative pathways of complement system. Two extracts were obtained under supercritical conditions using scCO2 with ethanol as cosolvent, at 313.15K, 15 MPa (E1) and 25 MPa (E2). Classical and alternative activation were evaluated using complement fixation test. Different concentrations of A. lappa extracts E1 and E2 showed an inhibitory effect on both complement pathways, and heparin was used as control. The IC50 of E1, E2, and heparin were 28.26, 20.12 and 92.54 µg/mL for classical and 26.12, 27.70, 27.78 µg/mL for the alternative pathway. Results demonstrate that A. lappa is a promising complementary treatment for diseases associated with complement activation.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"7 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"132883074","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Melanin Production Inhibitors from the West African Cassipourea congoensis","authors":"Dieudonné M. Takou, A. Waffo, M. Langat, J. Wansi, Lauren E. Mulcahy-Ryan, S. Schwikkard, E. Opara, E. Mas-Claret, D. Mulholland","doi":"10.1055/a-1006-2880","DOIUrl":"https://doi.org/10.1055/a-1006-2880","url":null,"abstract":"Abstract Cassipourea congoensis (syn. Cassipourea malosana) is used in African countries as a skin-lightening agent. Two previously unreported cycloartane triterpenoids, 26-hydroxy-3-keto-24-methylenecycloartan-30-oic acid 1 and 24-methylenecycloartan-3β,26,30-triol 2 along with the known mahuannin B 3, 7-methoxymahuannin B 4, 7-methoxygeranin A 5, methyl-3-(4-hydroxy-3-methoxyphenyl)-2E-propenoate, glycerol-1-alkanoate, (E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enal 6 , (-)-syringaresinol 7, and stigmast-5-en-3-O-β-D-glucoside, were isolated from the roots of C. congoensis. The crude extract and compounds 1 and 5 were found to inhibit the production of melanin at 10 µM with low cytotoxicity validating the ethnomedicinal use of this plant.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"399 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123542095","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetic-Pharmacodynamic (PK-PD) Modeling of Effect of Naringenin and Its Surface Modified Nanocarriers on Associated and Core Behaviors of Autism Spectrum Disorders (ASD)","authors":"R. Bhandari, J. Paliwal, A. Kuhad","doi":"10.1055/a-1001-2378","DOIUrl":"https://doi.org/10.1055/a-1001-2378","url":null,"abstract":"Abstract The pharmacokinetic and pharmacodynamic (PK-PD) model was developed to describe the relationship between plasma/brain concentration of naringenin and its nanocarriers with behavioral and biochemical alterations in a rat model of autism spectrum disorders (ASD). Behavioral parameters like sensorimotor dysfunction, hyperlocomotion, anxiety-like behavior, social interaction, and repetitive behavior were investigated by rotarod, actophotometer, open-field, reciprocal social interaction, and repetitive self-grooming test respectively. Naringenin was administered in doses (25, 50, and 100 mg/kg) and in the form of its uncoated and glutathione as well as tween 80–coated PLGA nanocarriers (25 mg/kg) thrice daily (8 hourly). Sigmoid Emax model was applied to study the relationship between the concentration of naringenin in plasma/brain and behavioral effects (in terms of sensorimotor dysfunction, locomotor activity, anxiety-like behavior, social interaction ability, repetitive behavior) as well as biochemical changes (plasma levels of TNF-α, MMP-9, and HSP-70, and Pgp at BBB). Model parameters such as Eo, Emax, and EC50 indicate that maximum effect occurred after administration of GSH-coated naringenin nanoparticles and the minimum effect occurred with the 25 mg/kg dose of unencapsulated naringenin. The R2 value of 0.99 and small Akaike information criterion indicate the goodness of fit of the model. The PK-PD modeling done by sigmoid Emax model showed a positive correlation between plasma/brain drug concentration and neuroinflammatory markers as well as behaviors consistent with the ASD phenotype.  ","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"97 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126833338","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cytotoxicity and Antibacterial Potential of Halogenated Chamigrenes from Malaysian Red Alga, Laurencia majuscula","authors":"T. Kamada, Chin-Soon Phan, T. Okino, C. Vairappan","doi":"10.1055/a-0977-4418","DOIUrl":"https://doi.org/10.1055/a-0977-4418","url":null,"abstract":"Abstract Red algae of the genus Laurencia have been known to produce a wide array of bioactive secondary metabolites. Here, we report the isolation of two new halogenated chamigrenes, lauremantanones A (1) and B (2), along with seven known compounds, dendroidiol (3), (+)-elatol (4), cartilagineol (5), obtusol (6), (+)-laurencenone B (7), 2-chloro-3-hydroxy-α-chamigren-9-one (8), and puertitol A (9), from a population of Laurencia majuscula (Harvey) Lucas from Mantanani Island (North Borneo). The structures of the two new metabolites were determined based on spectroscopic data (IR, 1D and 2D NMR, and MS). Compounds isolated from this alga exhibited potent cytotoxic (HeLa, MCF-7, P-388) and antibacterial (against antibiotic-resistant clinical bacteria) activities. The major metabolite of this population has significant importance in the geographical distribution of this species globally.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"9 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121189547","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evidence for Involvement of TRPV1 Receptors and Potassium Channels in the Seizures Induced by α-Sanshool","authors":"B. Reyes-Trejo, Mario Noel Morales-Hernández, Gloria Melisa González-Anduaga, J. Balderas-López, J. Tavares-Carvalho, A. Navarrete","doi":"10.1055/a-0871-2496","DOIUrl":"https://doi.org/10.1055/a-0871-2496","url":null,"abstract":"Abstract α-Sanshool is an alkamide isolated from the stem bark of Zanthoxylum liebmannianum, a Mexican medicinal plant known as Colopahtle. Our research group has reported that the intraperitoneal administration of α-sanshool induces tonic-clonic seizures in mice. In the present study, we investigated the convulsive effect of this alkamide and elucidated its mechanism of action by comparing with well-known convulsive and anticonvulsive drugs in an in vivo approach. α-Sanshool showed a potent (ED50 [CL 95%]=3.06 [2.92–3.22] mg/kg) and immediate (2±2 s) seizure effect after the intraperitoneal administration in mice. The convulsive effect of this alkamide was only observed for intraperitoneal administration; the oral route did not show any effect. α-Sanshool was less potent than strychnine (ED50 [CL 95%]=1.53 [1.44–1.62] mg/kg), but more effective than bicuculline, 4-aminopyridine, affinin, and pentylenetetrazol, in that order. The seizures induced by α-sanshool were reduced by capsazepine and diazoxide, suggesting the involvement of TRPV1 and potassium channels in the mechanism of action of this compound.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"26 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123535332","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Acute and Subacute Toxicological Studies of Annona Vepretorum in Experimental Animals","authors":"J. Silva, T. Diniz, É. Lavor, M. Silva, S. Lima-Saraiva, R. Oliveira-Júnior, V. N. Souza, Lívia B.A. Sousa, R. Mendes, L. Quintans-Júnior, M. Nascimento, R. Pereira-Filho, R. Albuquerque-Júnior, J. Almeida","doi":"10.1055/a-0833-8785","DOIUrl":"https://doi.org/10.1055/a-0833-8785","url":null,"abstract":"Abstract Annona vepretorum is endemic from the Brazilian Caatinga biome and is used in human nutrition. The present study aimed to investigate the toxic effects of the ethanolic extract from the leaves of this species. The leaves of A. vepretorum were collected, dried, pulverized, and macerated with ethanol to yield the crude ethanol extract of A. vepretorum. HPLC-diode array detection was used to determine the fingerprint chromatogram of the extract. In toxicity studies, the acute toxicity experimental group was administered a single dose of the ethanol extract of A. vepretorum (1 g/kg), while in the subacute toxicity experimental group, the ethanol extract of A. vepretorum was administered orally, daily for 30 days, at doses of 100 and 400 mg/kg. Death and signs of toxicity were observed and at the end, the animals were anesthetized, and blood and organs were then collected. The presence of the flavonoid rutin in the extract was confirmed using HPLC-diode array detection. In the evaluation of acute and subacute toxicity, there were no behavioral and physiological changes or signs of toxicity, and no occurrences of mice deaths were registered. The organs had normal color and preserved architecture, and no statistical variations in weight were observed. The results of the hematological and biochemical parameters after the administration of the ethanol extract of A. vepretorum showed no significant change, except in the count of the number of leukocytes and triglycerides. The histopathologic analysis of the liver, kidneys, and stomach indicated architecture with normal aspects. Thus, the toxicity study indicates low toxicity of the ethanol extract of A. vepretorum. Such information will be helpful in future clinical studies.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133223659","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}