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Triterpenoids from Alisma orientale and their NF-кB Inhibitory Activity 泽泻三萜类化合物及其NF-кB抑制活性研究
Planta Medica International Open Pub Date : 2021-08-25 DOI: 10.1055/a-1543-1261
Qian Yang, Yinqing Li, Xizi Liu, Sh Han, Si-yang Fan
{"title":"Triterpenoids from Alisma orientale and their NF-кB Inhibitory Activity","authors":"Qian Yang, Yinqing Li, Xizi Liu, Sh Han, Si-yang Fan","doi":"10.1055/a-1543-1261","DOIUrl":"https://doi.org/10.1055/a-1543-1261","url":null,"abstract":"Abstract The rhizome of Alisma orientale (sam.) Juz. is used in clinics for eliminating dampness, reducing edema, and promoting diuresis. This study aimed to elucidate the compounds and investigate their nuclear factor-kappa inhibitory activities in human embryonic kidney 293 cells. A new triterpene, alismaketone B (1); a new natural nortriterpene, noralisolic acid A (2); and 13 known protostane-type triterpenes were isolated from the rhizome of A. orientale. The new structures and their absolute configurations were established using HRESIMS, NMR, and electronic circular dichroism experiments. All isolated compounds were evaluated for their inhibitory activity on NF-κB. The compounds 8, 9, 10, and 14 showed moderate NF-κB inhibitory activities with their IC50 values being 64.7, 32.3, 47.3, and 37.3 μM, respectively.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"13 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134508655","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}
引用次数: 1
Neuroprotective Effects of Delta-9-Tetrahydrocannabinol against FeSO4- and H2O2-Induced Cell Damage on Dopaminergic Neurons in Primary Mesencephalic Cell Culture δ -9-四氢大麻酚对FeSO4-和h2o2诱导的中脑细胞多巴胺能神经元损伤的神经保护作用
Planta Medica International Open Pub Date : 2021-08-11 DOI: 10.1055/a-1516-4182
R. Moldzio, A. Unterberger, C. Krewenka, B. Kranner, K. Radad
{"title":"Neuroprotective Effects of Delta-9-Tetrahydrocannabinol against FeSO4- and H2O2-Induced Cell Damage on Dopaminergic Neurons in Primary Mesencephalic Cell Culture","authors":"R. Moldzio, A. Unterberger, C. Krewenka, B. Kranner, K. Radad","doi":"10.1055/a-1516-4182","DOIUrl":"https://doi.org/10.1055/a-1516-4182","url":null,"abstract":"Abstract Delta-9-Tetrahydrocannabinol and other phytocannabinoids have been previously demonstrated to possess neuroprotective effects in murine mesencephalic cell culture models of Parkinson’s disease, in which increased levels of superoxide radicals led to the loss of dopaminergic neurons. In these models, delta-9-tetrahydrocannabinol did not scavenge these radicals but displayed antioxidative capacity by increasing glutathione levels. Based on these findings, in the present study, we investigated whether the neuroprotective effect of delta-9-tetrahydrocannabinol can also be detected in FeSO4- and H2O2-stressed cells. Mesencephalic cultures were concomitantly treated with FeSO4 (350 μM) or H2O2 (150 μM) and delta-9-tetrahydrocannabinol (0.01, 0.1, 1, 10 μM) on the 12th days in vitro for 48 h. On the 14th DIV, dopaminergic neurons were stained immunocytochemically by tyrosine hydroxylase, and fluorescently using crystal violet, Hoechst 33342, and JC-1. FeSO4 and H2O2 significantly reduced the number of dopaminergic neurons by 33 and 36%, respectively, and adversely affected the morphology of surviving neurons. Moreover, FeSO4, but not H2O2, significantly decreased the fluorescence intensity of crystal violet and Hoechst 33342, and reduced the red/green ratio of JC-1. Co-treatment with delta-9-tetrahydrocannabinol at the concentrations 0.01 and 0.1 μM significantly rescued dopaminergic neurons in FeSO4 and H2O2-treated cultures by 16 and 30%, respectively. delta-9-Tetrahydrocannabinol treatment also led to a higher fluorescence intensity of crystal violet and Hoechst 33342, and increased the red/green fluorescence ratio of JC-1 when concomitantly administered with FeSO4 but not H2O2. To conclude, delta-9-tetrahydrocannabinol rescues dopaminergic neurons against FeSO4- and H2O2-induced neurotoxicity. Using fluorescence dyes, this effect seems to be mediated partially by restoring mitochondrial integrity and decreasing cell death, particularly in FeSO4-treated cultures.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"88 5","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114086993","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}
引用次数: 3
Effects of Chronic Administration of P-Cymene in an Animal Model of LPS-Induced Autism 长期给予p -聚伞花素对lps诱导的自闭症动物模型的影响
Planta Medica International Open Pub Date : 2021-08-11 DOI: 10.1055/a-1491-1866
Rick Wilhiam de Camargo, M. G. da Silva, G. C. Daros, Fabiana Durante de Medeiros, Naiana da Rosa, Caroline Liana Menschhein Medeiros, Eduardo de Medeiros Peretti, Juliete Palandi, F. Bobinski, J. Fortunato, Rafael Mariano de Bitencourt
{"title":"Effects of Chronic Administration of P-Cymene in an Animal Model of LPS-Induced Autism","authors":"Rick Wilhiam de Camargo, M. G. da Silva, G. C. Daros, Fabiana Durante de Medeiros, Naiana da Rosa, Caroline Liana Menschhein Medeiros, Eduardo de Medeiros Peretti, Juliete Palandi, F. Bobinski, J. Fortunato, Rafael Mariano de Bitencourt","doi":"10.1055/a-1491-1866","DOIUrl":"https://doi.org/10.1055/a-1491-1866","url":null,"abstract":"Abstract p-Cymene is a monoterpene found in over 100 plant species. It shows a range of biological activity, including anti-inflammatory and antimicrobial effects. It is possibly a new therapeutic alternative for autism spectrum disorder characterized by deficits in interaction and behavioral abnormalities. These symptoms can occur in response to maternal immune activation through prenatal exposure to lipopolysaccharide. Thus, this study aimed to evaluate the behavioral, memory, and biochemical effects of chronic administration of p-cymene in an animal model of autism by prenatal maternal exposure to lipopolysaccharide. Twenty-four pregnant Wistar rats were used, who received 100 μg/kg of lipopolysaccharide or saline intraperitoneally (i.p.) on the 9.5 gestational day. After birth, the male offspring remained with the mothers until weaning and underwent model validation tests on postnatal day 30. From postnatal day 31 on, chronic administration, via i.p., of saline (1 mL/kg), risperidone (0.2 mg/kg), or p-cymene (100 mg/kg) for 22 days was performed. The animals were submitted to behavioral (postnatal day 52) and memory tests (postnatal days 52–53) and subsequently sacrificed (postnatal day 54) when their brain structures were removed for quantification of proinflammatory cytokines (TNF-α, interleukin 1β, and interleukin 6). Prenatal exposure to lipopolysaccharide significantly increased episodes of stereotyped movement (p=0.0001) and decreased parameters of social interaction in offspring, including sniffing, following, mounting, and allowing mounting (p=0.0043, p<0.0001, p=0.0009, and p=0.0200, respectively). Chronic p-cymene treatment was not significant for behavioral, memory, and biochemical tests. However, due to their pharmacokinetic characteristics, p-cymene nanomaterials’ formulation may be an exciting alternative to be tested for further results.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"49 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125227071","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}
引用次数: 0
Screening of 20 Pantanal Wetland Plants for Anti-Candida Activity using HPLC-DAD-MS/MS and Bioautography to Characterize Active Compounds 利用HPLC-DAD-MS/MS和生物图谱技术筛选20种潘塔纳尔湿地植物抗念珠菌活性
Planta Medica International Open Pub Date : 2021-07-14 DOI: 10.1055/a-1494-1117
Daniela Z. de Brito, N. S. Cassemiro, J. M. E. de Souza, G. A. Damasceno-Júnior, R. Oliveira, C. Carollo, M. Chang
{"title":"Screening of 20 Pantanal Wetland Plants for Anti-Candida Activity using HPLC-DAD-MS/MS and Bioautography to Characterize Active Compounds","authors":"Daniela Z. de Brito, N. S. Cassemiro, J. M. E. de Souza, G. A. Damasceno-Júnior, R. Oliveira, C. Carollo, M. Chang","doi":"10.1055/a-1494-1117","DOIUrl":"https://doi.org/10.1055/a-1494-1117","url":null,"abstract":"Abstract The Pantanal wetland harbors a rich flora with uncharted pharmacological potential. This study evaluated 20 Brazilian Pantanal plants against Candida albicans, C. parapsilosis, C. tropicalis, and C. krusei. Fungal susceptibility was determined by agar diffusion and broth microdilution; active compounds were identified by bioautography and HPLC-DAD-MS/MS. Sesbania virgata, Polygala molluginifolia, and Cantinoa mutabilis extracts and their chloroform and ethyl acetate (EtOAc) fractions exhibited the best activity against all Candida species tested. The EtOAc fraction of P. molluginifolia proved to be more efficient in inhibiting C. parapsilosis and C. krusei growth (Minimum inhibitory concentration of 125 and 62.5 μg/mL, respectively). Bioautography of this fraction revealed two active bands, characterized by HPLC-DAD-MS/MS as a mixture of podophyllotoxin derivatives blumenol, besides some flavonoids. This work demonstrated antifungal potential of P. molluginifolia podophyllotoxin derivatives and the versatility of bioautography with HPLC-DAD-MS/MS to identify the bioactive compounds.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"124874534","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}
引用次数: 1
Pachypodostyflavone, a New 3-methoxy Flavone and Other Constituents with Antifilarial Activities from the Stem Bark of Duguetia staudtii 杜鹃茎皮中新型3-甲氧基黄酮及其抗丝活性成分的研究
Planta Medica International Open Pub Date : 2021-06-01 DOI: 10.1055/a-1492-3585
A. Mbobda, A. Ngouonpe, G. Happi, B. Mountessou, Elvis Monya, Jean-Bosco Jouda, B. Toussie, B. Lenta, N. Sewald, S. Kouam, J. Tchouankeu
{"title":"Pachypodostyflavone, a New 3-methoxy Flavone and Other Constituents with Antifilarial Activities from the Stem Bark of Duguetia staudtii","authors":"A. Mbobda, A. Ngouonpe, G. Happi, B. Mountessou, Elvis Monya, Jean-Bosco Jouda, B. Toussie, B. Lenta, N. Sewald, S. Kouam, J. Tchouankeu","doi":"10.1055/a-1492-3585","DOIUrl":"https://doi.org/10.1055/a-1492-3585","url":null,"abstract":"Abstract A new flavone derivative named pachypodostyflavone (1), along with 8 known compounds (2–9) and a mixture of β-sitosterol and stigmasterol were isolated from the stem bark of Duguetia staudtii (Annonaceae), based on a bioassay-guided fractionation. Their structures were determined using high-resolution mass spectrometry and NMR spectroscopic data, as well as by comparison with the literature values of their analogs. Selected isolated compounds were evaluated for their in vitro antifilaricidal activities on Onchocerca ochengi microfilariae and adult worms. Inhibition of motility was evaluated spectroscopically on microfilaria and adult male worms. Viability was determined on adult female worms by the MTT/ Formazan assay. Auranofin at 10 µM and 2% DMSO were used as positive and negative controls, respectively. Compounds 1 and 7 showed potent anti-onchocerca activities with 100% activity at 250 µg/mL on both O. ochengi adult male and female worms, while compound 5 displayed 100% activity at 30 µg/mL.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114642935","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}
引用次数: 4
Cytokinin Mediated Increased In Vitro Production of Secondary Metabolites with Special Reference to Solasodine in Solanum erianthum 细胞分裂素介导的菊苣次生代谢物体外产量增加,特别以索拉索定为参考
Planta Medica International Open Pub Date : 2021-06-01 DOI: 10.1055/a-1484-9750
Jeeta Sarkar, N. Banerjee
{"title":"Cytokinin Mediated Increased In Vitro Production of Secondary Metabolites with Special Reference to Solasodine in Solanum erianthum","authors":"Jeeta Sarkar, N. Banerjee","doi":"10.1055/a-1484-9750","DOIUrl":"https://doi.org/10.1055/a-1484-9750","url":null,"abstract":"Abstract Steroid alkaloid solasodine is a nitrogen analogue of diosgenin and has great importance in the production of steroidal medicines. Solanum erianthum D. Don (Solanaceae) is a good source of solasodine. The aim of this study was to evaluate the effect of different cytokinins on the production of secondary metabolites, especially solasodine in the in vitro culture of S. erianthum. For solasodine estimation, field-grown plant parts and in vitro tissues were extracted thrice and subjected to high-performance liquid Chromatography. Quantitative analysis of different secondary metabolites showed that the amount was higher in the in vitro regenerated plantlets compared to callus and field-grown plants. The present study critically evaluates the effect of the type of cytokinin used in the culture medium on solasodine accumulation in regenerated plants. The highest solasodine content (46.78±3.23 mg g-1) was recorded in leaf extracts of the in vitro grown plantlets in the presence of 6-γ,γ-dimethylallylamino purine in the culture medium and the content was 3.8-fold higher compared to the mother plant.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"179 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122333057","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}
引用次数: 0
Wound Healing Effects from 3 Hypericum spp. Essential Oils 3种金丝桃精油的伤口愈合效果
Planta Medica International Open Pub Date : 2021-06-01 DOI: 10.1055/a-1492-3634
M. Grafakou, A. Diamanti, Eleytheria Simirioti, A. Terezaki, C. Barda, I. Sfiniadakis, M. Rallis, H. Skaltsa
{"title":"Wound Healing Effects from 3 Hypericum spp. Essential Oils","authors":"M. Grafakou, A. Diamanti, Eleytheria Simirioti, A. Terezaki, C. Barda, I. Sfiniadakis, M. Rallis, H. Skaltsa","doi":"10.1055/a-1492-3634","DOIUrl":"https://doi.org/10.1055/a-1492-3634","url":null,"abstract":"Abstract Hypericum species have a long-term use as wound healing agents, with the most common preparation being the infused oil from the aerial parts. It contains naphthodianthrones, phloroglucinols, and essential oil. An extensive literature survey shows that, unlike napthodianthrones and phloroglucinols, essential oils from Hypericum spp. have not yet been evaluated for their wound healing efficacy. The present study aims to assess the wound healing efficacy of essential oils from H. perforatum, a plant recognized in European Pharmacopoeia for having wound healing properties, as well from 2 other Hypericum species commonly used in Greece as wound healing agents since classical antiquity, namely, H. empetrifolium and H. triquetrifolium. So far, only the wound healing effects of Hypericum oil are known, which is a different herbal preparation containing nonvolatile compounds, while the essential oils under investigation contain only volatile constituents. The essential oils were subjected to GC-MS analyses. Wounds were created on the upper back of hairless SKH-hr1 mice. Healing was evaluated by clinical, histopathological, and biophysical assessment. The essential oils showed a significantly faster wound healing rate in comparison to the controls and the vehicle-treated groups. H. empetrifolium possessed the most significant healing properties while for H. perforatum and H. triquetrifolium skin inflammation persisted. The essential oils from Hypericum spp. showed promising results as wound healing agents and are likely to contribute to the wound healing efficacy of the Hypericum preparations. H. empetrifolium, being the most potent anti-inflammatory and wound healing agent, confirms the traditional use of this plant in Greece for wounds and skin inflammations.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"336 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123215848","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}
引用次数: 2
Anti-inflammatory and Anti-arthritic Activities of Aqueous Extract and Flavonoids from Tripodanthus acutifolius Leaves in Mice Paw Oedema 三脚戟叶水提物及黄酮类化合物对小鼠足跖水肿的抗炎和抗关节炎作用
Planta Medica International Open Pub Date : 2021-05-27 DOI: 10.1055/a-1471-8947
Luis Apaza Ticona, A. Serban, Daly Apaza Ticona, K. Slowing
{"title":"Anti-inflammatory and Anti-arthritic Activities of Aqueous Extract and Flavonoids from Tripodanthus acutifolius Leaves in Mice Paw Oedema","authors":"Luis Apaza Ticona, A. Serban, Daly Apaza Ticona, K. Slowing","doi":"10.1055/a-1471-8947","DOIUrl":"https://doi.org/10.1055/a-1471-8947","url":null,"abstract":"Abstract Tripodanthus acutifolius, commonly known as Jamillo, is an herbal remedy used in traditional Andean medicine to treat joint problems, such as sprains, dislocations, and rheumatic pain. This study aimed to evaluate the in vitro and in vivo anti-inflammatory and anti-arthritic activity of the aqueous extract and isolated compounds of T. acutifolius. A bioguided phytochemical analysis based on NMR/MS was performed to identify the compounds of the aqueous extract from T. acutifolius. The anti-inflammatory and anti-arthritic activity were evaluated by measuring inflammatory parameters (TNF-α, C-reactive protein, and fibrinogen) in murine models. The chemical structure determination led to the identification of four flavonoids: (E)-2’,4’-dihydroxy-6’-methoxy-chalcone (1), 6,2’,4’-trimethoxyflavone (2), 5,3’,4’-trihydroxy-6,7,8-trimethoxyflavone (3), and 5,4’-dihydroxy-6,7,8-trimethoxyflavone (4). All compounds inhibited the production of TNF-α in the RAW 264.7 cell line, with IC50 values of 0.78, 1.43, 5.73, and 9.71 μM, respectively. In addition, all flavonoids decreased the levels of TNF-α, C-reactive protein, and fibrinogen at a concentration of 5 mg/kg in murine models. Our research shows that these compounds isolated from T. acutifolius have anti-inflammatory and anti-arthritic properties, providing scientific evidence for the traditional use of this plant species.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"36 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114790494","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}
引用次数: 3
Antimalarial Activity of Bidens pilosa Root Extract Co-spray Dried in the Presence of β-Cyclodextrin or Aerosil:Microcrystalline Cellulose Blend β-环糊精或Aerosil -微晶纤维素共喷雾干燥Bidens pilosa根提取物的抗疟活性
Planta Medica International Open Pub Date : 2021-03-01 DOI: 10.1055/a-1348-5707
D. Cortés-Rojas, Thales Lira de Medeiros, C. B. S. Oliveira, Ywlliane da Silva Rodrigues Meurer, V. Andrade-Neto, W. P. Oliveira
{"title":"Antimalarial Activity of Bidens pilosa Root Extract Co-spray Dried in the Presence of β-Cyclodextrin or Aerosil:Microcrystalline Cellulose Blend","authors":"D. Cortés-Rojas, Thales Lira de Medeiros, C. B. S. Oliveira, Ywlliane da Silva Rodrigues Meurer, V. Andrade-Neto, W. P. Oliveira","doi":"10.1055/a-1348-5707","DOIUrl":"https://doi.org/10.1055/a-1348-5707","url":null,"abstract":"Abstract The purpose of this work was to evaluate if the antimalarial activity of Bidens pilosa L. root extract could be enhanced by co-spray drying with the pharmaceutical excipients blend of colloidal silicon dioxide:microcrystalline cellulose and β-cyclodextrin. The in vivo antimalarial activity of the products was evaluated in mice infected with Plasmodium berghei. Acute in vivo and in vitro toxicity in S5 HeLa cells were also carried out. B. pilosa L. root extract was lyophilized and used as a control. The spray-dried preparations enhanced the survival of the infected mice compared to the lyophilized crude root extract. The Bidens extract formulations were able to inhibit up to 71% of the growth of the parasite in the lowest tested dose, being about five times more active than the crude extract, thus showing significant partial antiplasmodial activity. The dried preparations did not show signals of toxicity in both the in vitro and in vivo assays. The results showed strong evidence that the co-spray drying of B. pilosa root extract with the selected pharmaceutical excipients might stabilize the bioactive compounds and enhance its antimalarial activity compared with the lyophilized crude extract.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"8 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131140517","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}
引用次数: 0
Carbamazepine Shows Plasma and Tissue Pharmacokinetic Interactions with Ajuga bracteosa Extract in Rats 卡马西平与小苞草提取物在大鼠体内的血浆和组织药动学相互作用
Planta Medica International Open Pub Date : 2021-03-01 DOI: 10.1055/a-1375-6570
E. Ahmad, M. Jahangir, Saiqa Ishtiaq, Hafiz Muhammad Faizan Haider, P. Shah, N. Bukhari
{"title":"Carbamazepine Shows Plasma and Tissue Pharmacokinetic Interactions with Ajuga bracteosa Extract in Rats","authors":"E. Ahmad, M. Jahangir, Saiqa Ishtiaq, Hafiz Muhammad Faizan Haider, P. Shah, N. Bukhari","doi":"10.1055/a-1375-6570","DOIUrl":"https://doi.org/10.1055/a-1375-6570","url":null,"abstract":"Abstract Carbamazepine (CBZ) is the first-line anticonvulsant drug with a narrow therapeutic index (NTI) and is a substrate for CYP3A4 and MRP-2. Ajuga bracteosa (AB), family Lamiaceae is widely used to treat epilepsy, gastric diseases, and protects against liver damage in folk. It contains bioactive metabolites, which are powerful inhibitors of CYP3A4, CYP3A5, CYP19, CYP2C19 enzymes and P-gp transporter. Concomitant use of NTI drugs with herbs, like AB increase the chances of herb-drug interactions (HDIs). This study was aimed to analyze the Ajuga bracteosa crude extract (ABCE) and to investigate its effect on the pharmacokinetics of CBZ in rats. In the pre-treatment study, rats received ABCE (1000 mg/kg) orally for 14 days, followed by a single dose of CBZ (80 mg/kg) on the 15th day. In the co-administration study, single doses of ABCE and CBZ were administered concomitantly in one session. All the doses were administered in 0.5% carboxymethylcellulose (CMC) as a vehicle. HPLC analysis showed that extract contained 1.3 mg/g ursolic acid, 2.1 mg/g sitosterol and 2.9 mg/g stigmasterol. Non-compartmental pharmacokinetic analysis showed an increase in Cmax, AUC0-∞, MRT, and t1/2 with a decrease in tmax, Vd and Cl of CBZ in both, pre-treated and co-administered groups vs controls. An increase in CBZ concentration in liver tissue of both pre-treated as well as co-administered animals was observed as compared to control. The above results suggested possible HDIs between AB and CBZ thus, may warrant CBZ dose adjustment in epileptic patients with simultaneous administration of AB or its products.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"550 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123133221","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}
引用次数: 0
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