Planta Medica International Open最新文献

{"title":"Studies of the Major Gene Expression and Related Metabolites in\u0000 Cannabinoids Biosynthesis Pathway Influenced by Ascorbic Acid","authors":"K. Soltan, Behnoush Dadkhah","doi":"10.1055/a-1809-7862","DOIUrl":"https://doi.org/10.1055/a-1809-7862","url":null,"abstract":"\u0000 Cannabis sativa L. is an annual dioecious plant that belongs to the\u0000 Cannabaceae family and is essential for different pharmaceutical and nutritional\u0000 properties. The most important and prevalent cannabinoids in cannabis are\u0000 cannabidiol and delta-9-tetrahydrocannabinol. The application of elicitors is an\u0000 effective method to improve secondary metabolite production, leading to a whole\u0000 spectrum of molecular, genetic, and physiological modifications. Therefore, the\u0000 expression changes of four key genes (THCAS, CBDAS, PT, and\u0000 OLS) of the cannabinoids pathway along with the\u0000 delta-9-tetrahydrocannabinol and cannabidiol metabolites fluctuation were\u0000 surveyed following the application of ascorbic acid as an elicitor. Cannabis was\u0000 sprayed immediately before flowering with ascorbic acid. Treated and untreated\u0000 (control) plants were sampled in different time courses for real-time PCR and\u0000 HPLC experiments. Results showed significant increases in THCAS,\u0000 CBDAS, PT, and OLS expression after ascorbic acid\u0000 treatments. The results of metabolite quantification also indicated that\u0000 secondary metabolites, especially delta-9-tetrahydrocannabinol and cannabidiol,\u0000 increased after the ascorbic acid application. This study contributes to the\u0000 growing body of knowledge of the functions of key genes in the cannabinoids\u0000 pathway to the engineering of cannabis for improving the production of\u0000 delta-9-tetrahydrocannabinol and cannabidiol metabolites in this plant.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"46 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"124511179","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":"Coix Seed Extract Prevents Inflammation-mediated Skin Dryness Induced\u0000 by Sodium Dodecyl Sulfate Exposure in HR-1 Hairless Mice","authors":"Feng Li, Yusuke Nakanishi, Kenta Murata, Kanako Shinguchi, Nina Fujita, Shigeki Chiba, Ryuji Takahashi","doi":"10.1055/a-1821-6332","DOIUrl":"https://doi.org/10.1055/a-1821-6332","url":null,"abstract":"Skin inflammation and dryness are the features of surfactant-induced irritant\u0000 contact dermatitis, a common skin disorder. In Japan, Coix seed (CS, Coix\u0000 lacryma-jobi L. var. ma-yuen Stapf) is widely used as a\u0000 traditional medicine and functional supplement to treat skin inflammation and\u0000 dry skin. However, the efficacy of CS against surfactant-induced skin disorders\u0000 has not been reported. Here, we investigated the effect of CS on inflammatory\u0000 dry skin disorders induced by multiple topical applications of sodium dodecyl\u0000 sulfate (SDS), a representative anionic surfactant. Male HR-1 hairless mice\u0000 received a water extract of CS for four weeks. Three weeks after CS\u0000 administration, the dorsal skin of the mice was exposed once daily to\u0000 10% SDS for five days. CS efficacy was then evaluated by measuring\u0000 epidermal water content; erythema index; severity of skin scaling; epidermal\u0000 thickness; inflammatory cell infiltration; production of pro-inflammatory\u0000 mediators, such as interleukin-1α (IL-1α) and prostaglandin E2\u0000 (PGE2); and protein expression of cyclooxygenase 2 (COX-2), in the dorsal skin.\u0000 Administration of CS markedly attenuated the SDS-induced reduction in epidermal\u0000 water content, elevated erythema index, and severity of skin scaling.\u0000 Histological analysis demonstrated that CS suppressed epidermal hyperplasia and\u0000 macrophage infiltration in SDS-exposed skin. Furthermore, CS significantly\u0000 prevented SDS-induced production of IL-1α and PGE2, as well as COX-2\u0000 upregulation. These results indicate that CS prevents SDS-induced\u0000 inflammation-mediated skin dryness by inhibiting the production of\u0000 pro-inflammatory mediators.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125019859","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":"Biochemical Characterization of the Pharmacological Effects of Yagari\u0000 in Experimentally Induced Benign Prostatic Hyperplasia","authors":"U. Agatemor, O. Nwodo","doi":"10.1055/a-1729-3499","DOIUrl":"https://doi.org/10.1055/a-1729-3499","url":null,"abstract":"Benign prostatic hyperplasia is a progressive pathologic condition common in ageing men, constituting a health burden. Benign prostatic hyperplasia is characterized by the proliferation of prostatic tissues, prostate enlargement, and lower urinary tract symptoms. The use of herbal medicine in the management and treatment of benign prostatic hyperplasia has shown some promise. The efficacy and potency of some polyherbal extracts have been scientifically proven in the management and treatment of diseases, while many others are yet to be investigated. The aim of this study was to determine the effect of the herbal mixture Yagari on experimentally induced benign prostatic hyperplasia in rats and to identify its pharmacologically active agents. The effect of the herbal mixture on experimentally induced benign prostatic hyperplasia in rats was determined using 36 male Wistar rats grouped randomly into 6 groups of 6 rats each. The test rats were treated subcutaneously using a combination of dihydrotestosterone and estradiol valerate in a 10:1 ratio for 28 days according to the standard method. The test rats were thereafter treated with the herbal mixture for 21 days. Prostate-specific antigen, inflammatory cytokines, assay of prostate function hormonal and prostate function enzyme activities, and kidney function test were evaluated in the blood samples collected by ocular puncture applying standard methods. Prostates were harvested and examined for histopathological changes. Biological activity-guided fractionation of Yagari in a silica gel column was carried out and using phospholipase A2 activity as a biomarker. The identity of the bioactive compounds was determined using mass spectroscopy and nuclear magnetic resonance. The herbal mixture showed a positive effect on prostatic hyperplasia by decreasing urinary obstruction through the inhibition of 5-alpha reductase, anti-inflammatory activity, and decreased level of sex hormones. Characterization by spectral studies revealed apigenin (4´,5,7-trihydroxyflavone, molecular weight).","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129693141","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":"Time-Dependent Anti-inflammatory Effects of a Lipid Extract from\u0000 Macrocystis pyrifera on Toll-Like Receptor 2 Signaling in Human THP-1\u0000 Monocytes","authors":"Jamie Mei-Lin Kok, Georgina C Dowd, J. Cabral, Lyn M. Wise","doi":"10.1055/a-1729-3654","DOIUrl":"https://doi.org/10.1055/a-1729-3654","url":null,"abstract":"Seaweeds reportedly contain anti-inflammatory compounds; however, little is known\u0000 about the therapeutic potential of Macrocystis pyrifera. This study\u0000 investigated the anti-inflammatory properties of a methanol:chloroform extract,\u0000 chromatographic fractions, and fatty acids identified from M. pyrifera\u0000 (Linnaeus) C. Agardh. In human THP-1 monocytes stimulated with the Toll-like\u0000 receptor 2 agonist lipoteichoic acid, the extract decreased mRNA and protein\u0000 levels of interleukin-1β, interleukin-8, and monocyte\u0000 chemoattractant protein-1 to varied degrees at nontoxic concentrations. The\u0000 greatest anti-inflammatory effects were elicited when the extract was applied\u0000 between 6 h prior to, and 6 h after, the stimuli. Reduced levels\u0000 of nuclear factor kappa-light-chain-enhancer of activated B cells signaling\u0000 proteins were observed in extract-treated cells, with a significant decrease in\u0000 the myeloid differentiation factor 88 protein abundance relative to stimulated\u0000 THP-1 cells. Chromatographic fractionation of the extract yielded 40 fractions,\u0000 of which fraction F25 exhibited the greatest inhibition of monocyte\u0000 chemoattractant protein-1 production in activated THP-1 cells. Fatty acids\u0000 abundant within the extract and F25 were identified then tested, individually\u0000 and in combination, for their anti-inflammatory effects. Myristic acid,\u0000 palmitoleic acid, and α-linolenic acid, but not the fatty acid\u0000 combination, inhibited lipoteichoic acid-stimulated monocyte chemoattractant\u0000 protein-1 production without compromising THP-1 cell viability. These findings\u0000 indicate that the fatty acid-rich extract and fraction from M. pyrifera\u0000 provide anti-inflammatory and cytoprotective effects that may be beneficial for\u0000 use as a therapeutic.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129091268","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":"Daikenchuto, a Traditional Kampo Medicine, Facilitates Mucosal\u0000 Hyperemic Responses through Activation of TRPA1- and TRPV1-Expressing Sensory\u0000 Nerves in Rat Stomach","authors":"Masatoshi Yoshikubo, K. Tashima, M. Raimura, Y. Watanabe, Y. Noma, S. Horie","doi":"10.1055/a-1712-8391","DOIUrl":"https://doi.org/10.1055/a-1712-8391","url":null,"abstract":"Daikenchuto is a traditional Kampo medicine used to treat cold sensations and\u0000 dysmotility in the abdomen. This study investigated the roles of transient\u0000 receptor potential ankyrin 1- and transient reporter potential vanilloid\u0000 1-expressing sensory nerves in daikenchuto-induced gastric mucosal blood flow by\u0000 pharmacological and immunohistochemical analyses using male Sprague-Dawley rats.\u0000 Gastric mucosal blood flow was measured in ex vivo stomachs using a laser\u0000 Doppler flowmeter. Transient receptor potential ankyrin 1 activator allyl\u0000 isothiocyanate or transient reporter potential vanilloid 1 activator capsaicin\u0000 were applied for 10 min, and daikenchuto was applied for 10 or\u0000 30 min to the rat stomach. Transient reporter potential vanilloid 1\u0000 blocker N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl)\u0000 tetrahydropyrazine-1(2H)-carboxamide and transient receptor potential\u0000 ankyrin 1 blocker A-967079 were also administered intragastrically. Capsaicin\u0000 and allyl isothiocyanate increased gastric mucosal blood flow immediately after\u0000 the intragastric application, which was almost completely inhibited by\u0000 N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl)\u0000 tetrahydropyrazine-1(2H)-carboxamide and A-967079, respectively.\u0000 Daikenchuto increased gastric mucosal blood flow in a concentration-dependent\u0000 manner. A-967079 significantly inhibited the increase in gastric mucosal blood\u0000 flow induced by daikenchuto. In contrast,\u0000 N-(4-t-butylphenyl)-4-(3-chlopyridin-2-yl)\u0000 tetrahydropyrazine-1(2H)-carboxamide inhibited the responses to\u0000 daikenchuto only in the late phase but not in the initial phase. Interestingly,\u0000 in the deafferentation of capsaicin-sensitive sensory fiber in rats, the\u0000 increased gastric mucosal blood flow induced by daikenchuto was only decreased\u0000 in the late phase. Although transient receptor potential ankyrin 1- and\u0000 transient reporter potential vanilloid 1-immunoreactive fibers were observed\u0000 around the submucosal blood vessels of normal subjects, they were completely\u0000 absent in the deafferentation of capsaicin-sensitive sensory fibers. Thus,\u0000 daikenchuto increases gastric mucosal blood flow via transient receptor\u0000 potential ankyrin 1- and transient reporter potential vanilloid 1-co-expressing\u0000 sensory nerves in rat stomachs.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"25 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125343014","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":"Antidiabetic Activity of Caulerpa racemosa: Role of\u0000 Proinflammatory Mediators, Oxidative Stress, and Other\u0000 Biomarkers","authors":"R. Mandlik, S. Naik, S. Zine, H. Ved, G. Doshi","doi":"10.1055/a-1712-8178","DOIUrl":"https://doi.org/10.1055/a-1712-8178","url":null,"abstract":"A marine alga, Caulerpa racemose (seaweed), exhibits few biological\u0000 activities, such as antinociceptive/anti-inflammatory, antitumor, and\u0000 growth regulator. This study aimed to determine the antidiabetic activity of\u0000 this seaweed. High-performance thin-layer chromatography of C. racemosa\u0000 ethanolic extract was performed to identify its active constituents.\u0000 Antidiabetic activity of C. racemosa ethanolic extract (100 and\u0000 200 mg/kg) was evaluated using various biochemical paradigms\u0000 against glipizide (5 mg/kg) in a streptozotocin-induced diabetes\u0000 rat model. High-performance thin-layer chromatography revealed\u0000 β-sitosterol as an active constituent and also indicated the\u0000 presence of saponins and alkaloids. Treatment with C. racemosa ethanolic\u0000 extract significantly reduced blood glucose levels in diabetic rats, and the\u0000 degree of glucose reduction was comparable to that attained by glipizide\u0000 treatment. The C. racemosa ethanolic extract treatment restored the\u0000 impaired glycosylated hemoglobin level, liver glycogen level, glucose uptake by\u0000 hemidiaphragm, and glucose transport by hepatic cells. Pretreatment with C.\u0000 racemosa ethanolic extract also restored lipid abnormalities, elevated\u0000 liver enzymes, elevated inflammatory markers, and depleted endogenous\u0000 antioxidants. A superior effect was shown by C. racemosa ethanolic\u0000 extract (200 mg/kg) over glipizide (5 mg/kg).\u0000 Moreover, the restoration of the histoarchitecture of the pancreas by C.\u0000 racemosa ethanolic extract (200 mg/kg) was comparable to\u0000 that of the glipizide (5 mg/kg) treatment group. The present\u0000 experimental findings demonstrate significant antidiabetic activity of C.\u0000 racemosa ethanolic extract in diabetic rats using various biochemical\u0000 paradigms. Further, C. racemosa ethanolic extract seems to be safe and\u0000 does not affect vital organs adversely.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"120 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"116617086","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":"Effect of Environmental Factors on Plectranthus Neochilus Volatile Composition: A GC-MS-Based Metabolomics Approach","authors":"Maria Isabel Galbiatti, G. Pinheiro, E. M. Antunes, V. V. Hernandes, A. Sawaya","doi":"10.1055/a-1648-8111","DOIUrl":"https://doi.org/10.1055/a-1648-8111","url":null,"abstract":"Abstract Plectranthus neochilus Schltr. is an aromatic species, commonly used for digestive, antispasmodic, and analgesic purposes. Although many studies have reported the chemical composition of its essential oil, variations in the volatile profile were observed, which may be due to multiple factors linked to growth and field conditions. In order to detect metabolic variations in this species, we employed a GC-MS-based untargeted metabolomics approach analyzing samples of four P. neochilus individuals collected over a year. From all analyses, 24 mass features were detected and 21 were identified according to their respective chromatographic peaks. All features varied among samples, particularly (2E)-hexenal, 3-octanone and δ-3-carene, which showed the highest coefficient of variation percentage in our study. Although the four individuals presented the same peaks in the chromatograms, significant differences in the intensity of specific mass features were detected between individuals throughout the year. Time of sampling did not affect P. neochilus volatile composition; the chemical profile remained constant throughout the day. Seasonal trends were observed for the species. Winter months coincided with a drop in the intensity of most components. Air temperature showed a positive correlation with some feature intensities, while myrcene and α-thujene resulted in a positive and a negative correlation with rainfall, respectively. This study was the first attempt to correlate metabolic variation and environmental factors in P. neochilus. Our approach was successful in identifying the composition and variation of the headspace volatiles of P. neochilus leaves.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121572594","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":"In vitro Inhibitory Action of the Essential Oils of Origanum Vulgare and Rosmarinus Officinalis against Aspergillus Fumigatus","authors":"Antonia Carolina Melo Monteiro, Aminata Doucoure Drame, F. Nascimento, A. Miranda-Vilela, A. V. Lima, M. A. N. da Silva, I. F. Ribeiro","doi":"10.1055/a-1588-2875","DOIUrl":"https://doi.org/10.1055/a-1588-2875","url":null,"abstract":"Abstract Aspergillus fumigatus is the main etiological agent of aspergillosis. Considering azole antifungal drug resistance in A. fumigatus, which compromises treatment, new alternatives are needed. Among them, essential oils (EOs) can be an alternative treatment, having shown positive results in inhibiting phytopathogenic fungi in vitro. We aimed to determine the in vitro antifungal activity of Origanum vulgare L. subsp. hirtum (Link) (oregano) and Rosmarinus officinalis L. (rosemary) EOs alone and in association (O. vulgare+R. officinalis) against A. fumigatus. EOs were analyzed by gas chromatography (GC-FID and GC/MS systems), and analyses showed that the major components of O. vulgare EO were carvacrol (67.8%), p-cymene (14.8%), and thymol (3.9%); for R. officinalis, they were the monoterpenes 1,8-cineole (49.1%), camphor (18.1%) and α-pinene (8.1). For biological assays, five EO concentrations, 0.2; 0.4; 0.6; 0.8 and 1.0%, were used in disk diffusion and agar dilution tests for 21 days. In disk diffusion, O. vulgare EO alone and in association (O. vulgare+R. officinalis) showed fungicidal activity at all concentrations. In agar dilution, inhibitory action was demonstrated from 0.6% for O. vulgare EO and in association (O. vulgare+R. officinalis). R. officinalis EO at 1.0% showed no fungal growth, determining the minimum inhibitory concentration (MIC). The present study demonstrated inhibitory actions of O. vulgare and R. officinalis EOs in A. fumigatus. GC analyses corroborated the literature regarding their antibacterial and antifungal effects. However, further in vitro and in vivo studies are needed to evaluate EOs as alternative antifungals for treating aspergillosis.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131521370","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":"Anticipate, Target and Characterize: MS²-anticipated C-glycosylflavones from Erythrococca anomala","authors":"Tapé Kouamé, T. Okpekon, N. Bony, S. Ferron, D. Bonnaffé, J. Vanheuverzwijn, Zhiyu Zhou, V. Fontaine, Amon Diane N'Tamon, J. Gallard, K. Leblanc, Jean-Christophe Jullian, C. Miel, P. Champy, M. Beniddir, P. Le Pogam","doi":"10.1055/a-1576-4351","DOIUrl":"https://doi.org/10.1055/a-1576-4351","url":null,"abstract":"Abstract We herein report on the first chemical assessment of Erythrococca anomala (Juss. ex Poir.) Prain (Euphorbiaceae), a genus that was – to the best of our knowledge – not studied yet from a phytochemical perspective. A molecular networking strategy was implemented to rapidly identify the known specialized metabolites from untargeted MS/MS analyses of E. anomala leaves ethanolic extract. This strategy allowed for the identification of diverse C-glycosyl flavones and a cursory examination of MS/MS spectra could extend the GNPS-provided annotation to pinpoint the structural novelty of further derivatives. The isolation of the sought-after structures could be streamlined based on MS-guidance and their structures, determined through extensive NMR analyses, displayed structural features in line with MS²-based predictions. Anticipating sharp structural features at an early stage of the dereplication process through a critical assessment of the tandem mass spectrometric landmarks was essential to embark on the isolation of the newly reported structures owing to the elevated number of flavonoid glycosides isomers thereof formerly known, which would have deterred us from isolating them without the support of additional tandem mass spectrometric information. The isolation of the main components of the ethanolic extract completed the currently provided chemical report on E. anomala, also resulting in the description of a new phenylethanoid derivative (3) and of a new orcinol-based dimer (4). Anomaloflavone (1) exhibit significant activities with minimal inhibitory concentration values of 25 µg/mL against Staphylococcus aureus and Mycobacterium smegmatis while failing to exert an antibacterial activity against Pseudomonas aeruginosa, while being devoid of cytotoxicity against SiHa cells.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"96 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133805126","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":"Thymol and Piperine-Loaded Poly(D,L-lactic-co-glycolic acid) Nanoparticles Modulate Inflammatory Mediators and Apoptosis in Murine Macrophages","authors":"J. Dzoyem, N. Boulens, E. Allémann, F. Delie","doi":"10.1055/a-1543-1190","DOIUrl":"https://doi.org/10.1055/a-1543-1190","url":null,"abstract":"Abstract This study aimed at preparing and characterizing thymol, eugenol, and piperine-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles and evaluating the effect on inflammatory mediators secretion and apoptosis in Raw 264.7 macrophage cells. Nanoparticles were produced by the solvent evaporation technique. Dynamic light scattering and scanning electron microscopy were used to study the physicochemical characteristics. Raw 264.7 macrophage cells were used as a model for in vitro assays. The 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium assay was used to determine the cytotoxicity of the formulated nanoparticles. An annexin V apoptosis detection kit was used to assess apoptosis. Nitric oxide production was determined using the Griess reagent, and the inflammatory mediators level was evaluated with Th1/Th2 cytokine and fluorometric cyclooxygenase kits. The loaded nanoparticles showed a particle size around 190 nm with a low polydispersity between 0.069 and 0.104 and a zeta potential between–1.2 and–9.5 mV. Reduced cytotoxicity of nanoparticles compared to free molecules against Raw 264.7 macrophage cells was observed and seemed to occur through a mechanism associated with apoptosis. A decrease in cyclooxygenase enzyme activity with an increasing concentration was observed. Both free molecules and nanoparticles showed their capacity to modulate the inflammatory process mostly by inhibiting the investigated inflammatory cytokines. The data presented in this study indicate that thymol and piperine-loaded poly(D,L-lactic-co-glycolic acid nanoparticles could serve as a novel anti-inflammatory colloidal drug delivery system with reduced toxicity. However, further study should be considered to optimize the formulation’s loading capacity and thereby probably enhance their bioactivity in treating inflammatory diseases.","PeriodicalId":199864,"journal":{"name":"Planta Medica International Open","volume":"6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121748102","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}