ETHNOPHARMACOLOGICAL RELEVANCE: Different plants are used for the treatment of various ailments and Acorus calamus L. is one such plant found in Western Himalaya. Rhizome of this plants has ethnomedicinal significance, as its rhizome is used for curing fever, pain and inflammation. An attempt has been made to alter the phytochemicals and increase its antioxidant property in a sustainable way with the help of mycorrhizal inoculation. AIM OF THE STUDY: Study of mycorrhizal (Funneliformis mosseae) impact on the biological activities and phytochemical profile of A. calamus L. rhizome and in silico studies of phytochemicals for their anti-inflammatory property. MATERIALS AND METHODS: F. mosseae was mass multiplied by single spore culture and then A. calamus rhizomes were inoculated with it. Antioxidant potential of rhizome extract was observed by DPPH and FRAP assays and the phytochemical profiling was done with GC-MS analysis. For observing antimicrobial activity disc diffusion method was employed. Dominant phytochemicals α-asarone and monolinolein TMS were chosen for molecular docking studies against four receptors (4COX, 2AZ5, 5I1B, 1ALU). RESULTS: There was increase in antioxidant activity of rhizome extract after mycorrhizal inoculation. However, no change in antimicrobial activity was observed in the plant after mycorrhizal inoculation. The comparison in phytochemicals was observed by GC-MS analysis which showed qualitative and quantitative variation in biochemical content in plants. The phytochemical, α-asarone and monolinolein TMS showed highest docking score and least binding energy against 1ALU and 4COX respectively for anti-inflammatory activity. CONCLUSION: Medicinal plants are potential source of antioxidants which can be increased by mycorrhizal inoculation without addition of chemical fertilizers and also results in altering the phytochemical composition.

• MeSH
• antiflogistika izolace a purifikace   farmakologie   MeSH
• antiinfekční látky izolace a purifikace   farmakologie   MeSH
• antioxidancia izolace a purifikace   farmakologie   MeSH
• diskové difúzní antimikrobiální testy MeSH
• fytonutrienty izolace a purifikace   farmakologie   MeSH
• houby fyziologie   MeSH
• mykorhiza fyziologie   MeSH
• oddenek MeSH
• plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
• počítačová simulace MeSH
• puškvorec chemie   mikrobiologie   MeSH
• rostlinné extrakty farmakologie   MeSH
• simulace molekulového dockingu MeSH
• tradiční lékařství MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Indie MeSH

Six new (1, 2, 6, 8, 13, and 20) and twenty previously isolated (3-5, 7, 9-12, 14-19, and 21-26) steroids featuring thirteen different carbocycle motifs were isolated from the organic extract of the soft coral Sinularia polydactyla collected from the Hurghada reef in the Red Sea. The structures and the relative configurations of the isolated natural products have been determined based on extensive analysis of their NMR and MS data. The cytotoxic, anti-inflammatory, anti-angiogenic, and neuroprotective activity of compounds 3-7, 9-12, 14-20, and 22-26, as well as their effect on androgen receptor-regulated transcription was evaluated in vitro in human tumor and non-cancerous cells. Steroids 22 and 23 showed significant cytotoxicity in the low micromolar range against the HeLa and MCF7 cancer cell lines, while migration of endothelial cells was inhibited by compounds 11, 12, 22, and 23 at 20 µM. The results of the androgen receptor (AR) reporter assay showed that compound 11 exhibited the strongest inhibition of AR at 10 µM, while it is noteworthy that steroids 10, 16, and 20 displayed increased inhibition of AR with decreasing concentrations. Additionally, compounds 11 and 23 showed neuroprotective activity on neuron-like SH-SY5Y cells.

• MeSH
• antiflogistika izolace a purifikace   farmakologie   MeSH
• antitumorózní látky izolace a purifikace   farmakologie   MeSH
• endoteliální buňky pupečníkové žíly (lidské) účinky léků   metabolismus   MeSH
• fyziologická neovaskularizace účinky léků   MeSH
• HeLa buňky MeSH
• inhibitory angiogeneze izolace a purifikace   farmakologie   MeSH
• korálnatci chemie   MeSH
• lidé MeSH
• MFC-7 buňky MeSH
• molekulární struktura MeSH
• nádory farmakoterapie   metabolismus   patologie   MeSH
• neurony účinky léků   metabolismus   patologie   MeSH
• neuroprotektivní látky izolace a purifikace   farmakologie   MeSH
• steroidy izolace a purifikace   farmakologie   MeSH
• viabilita buněk účinky léků   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Geografické názvy
• Indický oceán MeSH

Extensive phytochemical analysis of the CHCl3-soluble part of an ethanolic extract of branches and twigs of Broussonetia papyrifera led to the isolation of fourteen compounds, including a novel 5,11-dioxabenzo[b]fluoren-10-one derivative named broussofluorenone C (12). The isolated compounds 1-14 were characterized based on their NMR and HRMS data, and examined for their anti-inflammatory activities in LPS-stimulated THP-1 cells as well as for their cellular antioxidant effects. Compounds 7-10 and 12 showed inhibitory effects on NF-κB/AP-1 activation and compounds 7-9 were subsequently confirmed to suppress the secretion of both IL-1β and TNF-α in LPS-stimulated THP-1 cells more significantly than the prednisone used as a positive control. In the CAA assay, compound 10 exhibited the greatest antioxidant effect, greater than that of the quercetin used as a positive control. The results show possible beneficial effects and utilization of B. papyrifera wood in the treatment of inflammatory diseases as well as oxidative stress.

• MeSH
• antiflogistika chemie   izolace a purifikace   farmakologie   MeSH
• antioxidancia chemie   izolace a purifikace   farmakologie   MeSH
• Broussonetia chemie   MeSH
• interleukin-1beta antagonisté a inhibitory   biosyntéza   MeSH
• kultivované buňky MeSH
• lidé MeSH
• lipopolysacharidy antagonisté a inhibitory   farmakologie   MeSH
• molekulární struktura MeSH
• NF-kappa B analýza   antagonisté a inhibitory   biosyntéza   MeSH
• oxidační stres účinky léků   MeSH
• THP-1 buňky MeSH
• TNF-alfa antagonisté a inhibitory   biosyntéza   MeSH
• transkripční faktor AP-1 analýza   antagonisté a inhibitory   biosyntéza   MeSH
• viabilita buněk účinky léků   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

ETHNOPHARMACOLOGICAL RELEVANCE: Macaranga Thou. (Euphorbiaceae) is a large genus that comprises over 300 species distributed between Western Africa and the islands of the South Pacific. Plants of this genus have a long-standing history of use in traditional medicine for different purposes, including the treatment of inflammation. Fresh and dried leaves of certain Macaranga species (e.g. M. tanarius (L.) Müll.Arg.), have been used to treat cuts, bruises, boils, swellings, sores and covering of wounds in general. Several reports described Macaranga spp. being a rich source of polyphenols, such as prenylated stilbenoids and flavonoids, mostly responsible for its biological activity. Similarly, an abundant content of prenylated stilbenes was also described in M. siamensis S.J.Davies, species recently identified (2001) in Thailand. While the respective biological activity of the prenylated stilbenes from M. siamensis was poorly investigated to date, our recent study pointed out the interest as the natural source of several novel anti-inflammatory stilbenoids isolated from this species. AIM OF THE STUDY: This work investigated the potential anti-inflammatory effects of the stilbenoid macasiamenene F (MF) isolated from M. siamensis S.J.Davies (Euphorbiaceae) on the lipopolysaccharide (LPS)-induced inflammation-like response of monocytes and microglia, major cells involved in the peripheral and central inflammatory response, respectively. MATERIALS AND METHODS: LPS-induced stimulation of TLR4 signaling led to the activation of inflammatory pathways in in vitro models of THP-1 and THP-1-XBlue™-MD2-CD14 human monocytes, BV-2 mouse microglia, and an ex vivo model of brain-sorted mouse microglia. The ability of the stilbenoid MF to intervene in the IкB/NF-кB and MAPKs/AP-1 inflammatory cascade was investigated. The gene and protein expressions of the pro-inflammatory cytokines IL-1β and TNF-α were evaluated at the transcription and translation levels. The protective effect of MF against LPS-triggered microglial loss was assessed by cell counting and the LDH assay. RESULTS: MF demonstrated beneficial effects, reducing both monocyte and microglial inflammation as assessed in vitro. It efficiently inhibited the degradation of IкBα, thereby reducing the NF-кB activity and TNF-α expression in human monocytes. Furthermore, the LPS-induced expression of IL-1β and TNF-α in microglia was dampened by pre-, co-, or post-treatment with MF. In addition to its anti-inflammatory effect, MF demonstrated a cytoprotective effect against the LPS-induced death of BV-2 microglia. CONCLUSION: Our research into anti-inflammatory and protective effects of MF has shown that it is a promising candidate for further in vitro and in vivo investigations of MF interventions with respect to acute and chronic inflammation, including potentially beneficial effects on the inflammatory component of brain diseases such as stroke and Alzheimer's disease.

• MeSH
• antiflogistika izolace a purifikace   farmakologie   terapeutické užití   MeSH
• cytoprotekce účinky léků   fyziologie   MeSH
• Euphorbiaceae * MeSH
• kultivované buňky MeSH
• lidé MeSH
• lipopolysacharidy toxicita   MeSH
• mediátory zánětu antagonisté a inhibitory   metabolismus   MeSH
• mikroglie účinky léků   metabolismus   MeSH
• monocyty účinky léků   metabolismus   MeSH
• myši inbrední C57BL MeSH
• myši MeSH
• nádorové buněčné linie MeSH
• prenylace účinky léků   fyziologie   MeSH
• rostlinné extrakty izolace a purifikace   farmakologie   terapeutické užití   MeSH
• stilbeny izolace a purifikace   farmakologie   terapeutické užití   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• zánět farmakoterapie   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

Here we report the comprehensive characterization of the secondary metabolites from the leaves of Colebrookea oppositifolia Smith, a species used as medicinal plant in the traditional medicine of Nepal. Phytochemical screening of bioactives was performed using an integrated LC-MSn and high resolution MS (Mass Spectrometry) approach. Forty-three compounds were tentatively identified, mainly aglyconic and glycosilated flavonoids and phenolic acids, as well as other bioactives such as coumarins and terpenes were detected. Furthermore, the NF-κB and AP-1 inhibitory activity of C. oppositifolia extract were evaluated, as well as its cytotoxicity against THP-1 cells, in order to assess the potential use of this herb as a source of anti-inflammatory and cytotoxic compounds. The results so far obtained indicate that C. oppositifolia leaves extract could significantly reduce the viability of THP-1 cells (IC50 = 6.2 ± 1.2 µg/mL), as well as the activation of both NF-κB and AP-1 at the concentration of 2 μg/mL. Our results indicate that Nepalese C. oppositifolia is a valuable source of anti-inflammatory and cytotoxic compounds. The phytochemical composition reported here can partially justify the traditional uses of C. oppositifolia in Nepal, especially in the treatment of inflammatory diseases, although further research will be needed to assess the full potential of this species.

• MeSH
• antiflogistika izolace a purifikace   farmakologie   toxicita   MeSH
• chromatografie kapalinová MeSH
• flavonoidy analýza   izolace a purifikace   MeSH
• hluchavkovité metabolismus   MeSH
• hmotnostní spektrometrie MeSH
• hydroxybenzoáty analýza   izolace a purifikace   MeSH
• léčivé rostliny metabolismus   MeSH
• lidé MeSH
• listy rostlin metabolismus   MeSH
• metabolom MeSH
• methanol MeSH
• NF-kappa B antagonisté a inhibitory   MeSH
• rostlinné extrakty chemie   izolace a purifikace   farmakologie   toxicita   MeSH
• THP-1 buňky MeSH
• transkripční faktor AP-1 antagonisté a inhibitory   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Nepál MeSH

This paper describes the synthesis of a new A-homo lactam D-homo lactone androstane derivative from dehydroepiandrosterone. To evaluate the impact of the introduction of nitrogen in the parental scaffold on biological activity, a new androstane enamide-type lactam derivative was prepared and characterized. The new compound as well as starting compounds were screened for cytotoxic, anti-angiogenic and anti-inflammatory activities using several human cancer cell lines (MCF-7, MDA-MB-231, PC3, CEM, G-361, HeLa), endothelial (HUVEC) and non-tumour (MRC-5 and BJ) cell lines. Strong cytotoxic and anti-inflammatory activity with a broad therapeutical window was demonstrated by the A-homo lactam D-homo lactone androstane derivative. The induction of apoptosis in treated PC3 cultures was confirmed using apoptotic morphology screening and a fluorescent double-staining method. New A-homo lactam D-homo lactone androstane derivative induced apoptosis more than the tested reference compounds, Formestane and Doxorubicin. An in silico ADME analysis showed that the compounds possess drug-like properties.

• MeSH
• androstany chemie   izolace a purifikace   farmakologie   MeSH
• antiflogistika chemie   izolace a purifikace   farmakologie   MeSH
• antitumorózní látky fytogenní chemie   izolace a purifikace   farmakologie   MeSH
• apoptóza účinky léků   MeSH
• E-selektin antagonisté a inhibitory   biosyntéza   MeSH
• kultivované buňky MeSH
• laktony chemie   izolace a purifikace   farmakologie   MeSH
• léky antitumorózní - screeningové testy MeSH
• lidé MeSH
• molekulární konformace MeSH
• optické zobrazování MeSH
• proliferace buněk účinky léků   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

The antimicrobial, cytotoxic, anti-inflammatory, and antioxidant properties of aqueous extracts of raw and culinary processed shiitake mushrooms were evaluated and compared with those of lenthionine (1,2,3,5,6-penta-thiepane), the principal aroma-bearing substance of the shiitake medicinal mushroom (Lentinus edodes). Antimicrobial activity was tested using a panel of 4 strains of bacteria, 2 yeasts, and 2 fungi. Cytotoxic properties were evaluated against 3 cell lines (HepG2, HeLa, PaTu), whereas the anti-inflammatory activity of tested samples was assayed based on their ability to attenuate the secretion of the cytokine tumor necrosis factor-α. Antioxidant activity was measured using in vitro DPPH and ABTS assays. It was found that lenthionine possesses significant antimicrobial properties; it is remarkably effective in inhibiting the growth of yeasts and fungi (minimum inhibitory concentration, 2-8 μg/mL) and thus is comparable to standard antifungal agents. Lenthionine is also able to decrease significantly the production of tumor necrosis factor-a and thus could be at least partly responsible for the observed anti-inflammatory effect of shiitake. On the other hand, lenthionine does not seem to contribute significantly to the well-known anticancer and antioxidant effects of the mushroom.

• MeSH
• antibakteriální látky izolace a purifikace   farmakologie   MeSH
• antiflogistika izolace a purifikace   farmakologie   MeSH
• antifungální látky izolace a purifikace   farmakologie   MeSH
• antioxidancia izolace a purifikace   farmakologie   MeSH
• Bacteria účinky léků   MeSH
• buňky Hep G2 MeSH
• cytokiny účinky léků   MeSH
• cytotoxiny izolace a purifikace   farmakologie   MeSH
• HeLa buňky MeSH
• houby šii-take chemie   MeSH
• houby účinky léků   MeSH
• kvasinky účinky léků   MeSH
• lidé MeSH
• mikrobiální testy citlivosti MeSH
• nádorové buněčné linie MeSH
• thiepiny chemie   farmakologie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

ETHNOPHARMACOLOGICAL RELEVANCE: Leucosidea sericea is a southern African tree used for treating different diseases including microbial infections and inflammatory-related conditions. AIM OF THE STUDY: To isolate and identify the chemicals in Leucosidea sericea which possibly account for the diverse therapeutic effects of the species. MATERIALS AND METHODS: Leaf material was extracted using 20% methanol and subsequently partitioned with different solvents (hexane, dichloromethane, ethyl acetate and butanol). Resultant fractions were subjected to bioactive (antimicrobial)-guided isolation and the structural elucidation was conducted using NMR (1D and 2D) spectroscopic methods. Given the broad uses of Leucosidea sericea in traditional medicine, the extract, fractions and isolated compounds were evaluated in five (5) biological assays in vitro (antimicrobial, antioxidant, acetylcholinesterase (AChE) and anti-inflammatory inhibition as well as cytotoxicity effect). RESULTS: As the most active fractions, from ethyl acetate yielded 5,7-dihydroxychromone (1); 1-hydroxy-2-oxopomolic acid (2); 3,5,7,3´,4´-pentahydroxyflavone (3) and Tiliroside (4). For the first time, these four (4) compounds were isolated from leaves of Leucosidea sericea. These aforementioned compounds demonstrated broad-spectrum antibacterial activity (1.95-125 µg/mL) and noteworthy antifungal (3.9-250 µg/mL) potential. In addition to its noteworthy antimicrobial activity, compound 3 also demonstrated significant antioxidant (EC50 = 14 µg/mL in DPPH assay) and anti-inflammatory (inhibited the level of ELAM by approximately 36% and decreased also the viability of endothelial cells) activities in vitro. Overall, AChE inhibition activity and cytotoxic response was generally weak for the extracts, fractions and isolated compounds. CONCLUSION: The pool of chemicals in Leucosidea sericea were enriched with the isolation and identification of four (4) compounds obtained from the leaf extract. Among these compounds, the significant antimicrobial activity of compound 3 provides strong evidence that support the use of Leucosidea sericea for microbial-related infections in folk medicine.

• MeSH
• acetylcholinesterasa účinky léků   metabolismus   MeSH
• antiflogistika izolace a purifikace   farmakologie   MeSH
• antiinfekční látky izolace a purifikace   farmakologie   MeSH
• antioxidancia izolace a purifikace   farmakologie   MeSH
• lidé MeSH
• listy rostlin MeSH
• magnetická rezonanční spektroskopie MeSH
• mikrobiální testy citlivosti MeSH
• Rosaceae chemie   MeSH
• rostlinné extrakty farmakologie   MeSH
• tradiční africká medicína MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

BACKGROUND: The aim of this work was to compare water and organic extracts, infusions and tinctures from flowers and leaves of Calendula officinalis in terms of their biological activity and composition. The purpose of work was investigation whether the leaves and stems are really the waste or they contain interesting substances which could be utilized. Antimicrobial, antifungal, antioxidant and anti-inflammatory activities were studied. Then, the ability to inhibit collagenase was studied as well. Cytotoxicity was tested for all the samples on mammalian cell lines. METHODS: To determine the composition of extracts, infusions and tinctures phytochemical analysis (the set of colour reactions for the detection of groups of biologically active compounds) was carried out and showed that samples from flowers and leaves contain the same groups of biologically active substances (proteins and amino acids, reducing sugars, flavonoids, saponins, phenolics, terpenoids, steroids, glycosides). The antimicrobial activity of tested samples was proved, where the most sensitive bacterium was Micrococcus luteus and the most sensitive yeast was Geotrichum candidum. RESULTS: The study of anti-collagenase activity has shown that the enzymatic reaction of collagenase was affected by all tested samples and their effect was concentration dependent. Cytotoxicity of water and methanol extracts at cell lines HEK 293T and HepG2 was observed. CONCLUSION: Cells HepG2 were more sensitive than cells HEK 293T. Using cell line RAW 264.7, antiinflammatory activity of all samples was observed. Tincture of leaves was the most effective.

• MeSH
• antiflogistika izolace a purifikace   toxicita   MeSH
• antiinfekční látky izolace a purifikace   toxicita   MeSH
• antioxidancia izolace a purifikace   toxicita   MeSH
• buněčné linie MeSH
• buňky Hep G2 MeSH
• HEK293 buňky MeSH
• květy chemie   MeSH
• lidé MeSH
• listy rostlin chemie   MeSH
• měsíček chemie   MeSH
• rostlinné extrakty izolace a purifikace   toxicita   MeSH
• viabilita buněk účinky léků   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

Geranyl flavones have been studied as compounds that potentially can be developed as anti-inflammatory agents. A series of natural geranylated flavanones was isolated from Paulownia tomentosa fruits, and these compounds were studied for their anti-inflammatory activity and possible mechanism of action. Two new compounds were characterized [paulownione C (17) and tomentodiplacone O (20)], and all of the isolated derivatives were assayed for their ability to inhibit cyclooxygenases (COX-1 and COX-2) and 5-lipoxygenase (5-LOX). The compounds tested showed variable degrees of activity, with several of them showing activity comparable to or greater than the standards used in COX-1, COX-2, and 5-LOX assays. However, only the compound tomentodiplacone O (20) showed more selectivity against COX-2 versus COX-1 when compared with ibuprofen. The ability of the test compounds to interact with the above-mentioned enzymes was supported by docking studies, which revealed the possible incorporation of selected test substances into the active sites of these enzymes. Furthermore, one of the COX/LOX dual inhibitors, diplacone (14) (a major geranylated flavanone of P. tomentosa), was studied in vitro to obtain a proteomic overview of its effect on inflammation in LPS-treated THP-1 macrophages, supporting its previously observed anti-inflammatory activity and revealing the mechanism of its anti-inflammatory effect.

• MeSH
• antiflogistika chemie   izolace a purifikace   farmakologie   MeSH
• arachidonát-5-lipoxygenasa metabolismus   MeSH
• cyklooxygenasa 1 metabolismus   MeSH
• cyklooxygenasa 2 metabolismus   MeSH
• flavonoidy chemie   izolace a purifikace   farmakologie   MeSH
• inhibitory cyklooxygenasy 2 chemie   izolace a purifikace   farmakologie   MeSH
• inhibitory lipoxygenas chemie   izolace a purifikace   farmakologie   MeSH
• Magnoliopsida chemie   MeSH
• molekulární struktura MeSH
• ovoce chemie   MeSH
• proteomika * MeSH
• Publikační typ
• časopisecké články MeSH