scholarly journals Total Phenolics, Flavonoids, Condensed Tannins Content of Eight Centaurea Species and Their Broad Inhibitory Activities against Cholinesterase, Tyrosinase, α-Amylase and α-Glucosidase

2016 ◽  
Vol 44 (1) ◽  
pp. 195-200 ◽  
Author(s):  
Gokhan ZENGIN ◽  
Marcello LOCATELLI ◽  
Simone CARRADORI ◽  
Andrei M. MOCAN ◽  
Abdurrahman AKTUMSEK
Keyword(s):  
Ethyl Acetate ◽  
Condensed Tannins ◽  
Total Phenolics ◽  
Condensed Tannin ◽  
Folk Medicine ◽  
Chloroform Extract ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Synthetic Drugs ◽  
Starting Point

Several bioactive compounds originate from natural sources and their uses are generally related with traditional or folk medicine. Synthetic drugs can have adverse side effects and, for this reason, the investigation of novel, safe, and natural-occurring products can account for the development of new drugs. The genus Centaurea L. is one of the most important genera of the Asteraceae family, containing more than 200 species in the Turkish flora, about 140 of which are endemic. The aim of the present work was to determine enzyme inhibitory potentials of two extracts (chloroform and ethyl acetate) from eight Centaurea species against cholinesterase, tyrosinase, amylase, and glucosidase. The total phenolics, flavonoids and condensed tannin contents were also reported for each extract. These components in the extracts varied according to species and extraction solvents as well as enzyme inhibitory effects. The highest level of phenolics was found to be in the chloroform extract of C. pulchella (119.23 mg GAEs/g extract). Generally, chloroform extracts exhibited stronger enzyme inhibitory effects as compared to ethyl acetate. Additionally, possible correlations with total phenolics, flavonoids, and condensed tannins content were also highlighted. This paper is the first report of the inhibitory capacities of the eight Centaurea species on the selected enzymes. The present results may be a valuable starting point in the development of new bioactive formulations.

Phytochemical Screening and Total Phenolics and Flavonoids Contents of Hibiscus Rosa Sinensis. L Cultivated in Viet Nam

MedPharmRes ◽  
2017 ◽  
Vol 1 (1) ◽  
pp. 52-57 ◽  
Author(s):  
Han Truong ◽  
Ly Le ◽  
Minh Tran ◽  
◽  
◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Crude Extract ◽  
Methanol Extract ◽  
Total Phenolics ◽  
Ethyl Acetate Extract ◽  
Hexane Extract ◽  
New Drugs ◽  
Total Phenolic ◽  
Total Flavonoids ◽  
Hibiscus Rosa Sinensis

Background: Phenolics and flavonoids are regarded as the highest potential of chemotherapeutic activities. This investigation was carried out to evaluate phytochemical and total phenolics content (TPC) and total flavonoids content (TFC) and Fourier-transform infrared spectroscopy (FTIR) spectral analysis of Hibiscus Rosa Sinensis L. extracts (crude extract, n-hexane extract, ethyl acetate extract, and methanol extract) for further applications in pharmaceutical development. Method: Total phenolics were estimated by Folin-Ciocalteu method; while, Aluminum chloride was employed to quantify total flavonoids in the sample extracts. And, functional groups of Hibiscus Rosa Sinensis compound was determined using a FTIR-spectrophotometer. Result: Results showed the leaves extracts to encompass the high amount of total phenolic and total flavonoid content. TPC values for crude extract, methanol extract, ethyl acetate extract and n-hexane extract were 57.09 ± 0.35 mg/g, 70.98 ± 0.03 mg/g, 21.31 ± 0.01 mg/g, and 18.45 ± 0.003 mg/g as gallic acid equivalent, respectively. Crude extract, methanol extract, ethyl acetate extract and n-hexane extract showed total flavonoids 26.87 ± 0.01 mg/g, 21.08 ± 0.03 mg/g, 21.70 ± 0.001 mg/g, 14.95 ± 0.02 mg/g as rutin equivalent. FTIR spectra of four extracts were comparable and showed the presence of nitro compounds and ring aromatic compounds. Conclusion: Our results indicate the potential of exploiting Hibiscus Rosa Sinensis leaves as a source of chemotherapeutic compounds, and it is worthy doing further researches on isolated bioactive compounds for developing novel functional foods or new drugs.

Antiulcerogenic Activity of Crude Extract, Fractions and Populnoic Acid Isolated from Austroplenckia populnea (Celastraceae)

2006 ◽  
Vol 61 (5-6) ◽  
pp. 329-333 ◽  
Author(s):  
Sérgio F. Andrade ◽  
Daiane Antoniolli ◽  
Eros Comunello ◽  
Luis G. V. Cardoso ◽  
José C. T. Carvalho ◽  
...  
Keyword(s):  
Oral Administration ◽  
Folk Medicine ◽  
Chloroform Extract ◽  
Negative Control ◽  
New Drugs ◽  
Gastric Ulcers ◽  
Reduced Pressure ◽  
Crude Extracts ◽  
Antiulcerogenic Activity ◽  
Lesion Index

Many plant crude extracts and their isolated compounds are the most attractive sources of new drugs and show promising results for the treatment of gastric ulcers. Austroplenckia populnea is commonly known as “marmelinho-do campo, mangabeira-brava, mangabarana and vime” and it has been used in folk medicine as anti-dysenteric and anti-rheumatic. Powdered bark wood (3.25 kg) was macerated with aqueous ethanol (96%) and the extract was concentrated under reduced pressure to yield 406 g of crude hydralcoholic extract. The hydralcoholic extract was suspended in aqueous methanol and partitioned with hexane, chloroform and ethyl acetate (EtOAc) in sequence, yielding 8.0 g, 9.5 g and 98.17 g of crude extracts, respectively. Chromatography of the hexane extract over a silica gel column led to the isolation of the triterpene populnoic acid. The oral administration of hydralcoholic, hexane, chloroform and EtOAc extracts (200 mg/kg) decreased the ulcer lesion index (ULI) by 83.15%, 46.87%, 32.2%, 68.12%, respectively. Oral administration of populnoic acid (100 mg/ kg) diminished the ULI by 55.29%. All the obtained results were significant in comparison with the negative control, with exception of the chloroform extract.

scholarly journals Effects of Osthol Isolated from Cnidium monnieri Fruit on Urate Transporter 1

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2837 ◽  
Author(s):  
Yuusuke Tashiro ◽  
Ryo Sakai ◽  
Tomoko Hirose-Sugiura ◽  
Yukio Kato ◽  
Hirotaka Matsuo ◽  
...  
Keyword(s):  
Uric Acid ◽  
Active Ingredient ◽  
Folk Medicine ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Mature Fruit ◽  
Urate Transporter ◽  
New Chemical Entities ◽  
Crude Drugs ◽  
Inhibitory Potential

(1) Background: Crude drugs used in traditional Japanese Kampo medicine or folk medicine are major sources of new chemical entities for drug discovery. We screened the inhibitory potential of these crude drugs against urate transporter 1 (URAT1) to discover new drugs for hyperuricemia. (2) Methods: We prepared the MeOH extracts of 107 different crude drugs, and screened their inhibitory effects on URAT1 by measuring the uptake of uric acid by HEK293/PDZK1 cells transiently transfected with URAT1. (3) Results: We found that the extract of the dried mature fruit of Cnidium monnieri inhibited urate uptake via URAT1. We isolated and identified osthol as the active ingredient from this extract. Osthol noncompetitively inhibited URAT1 with an IC50 of 78.8 µM. We evaluated the effects of other coumarins and found that the prenyl group, which binds at the 8-position of coumarins, plays an important role in the inhibition of URAT1. (4) Conclusions: Cnidium monnieri fruit may be useful for the treatment of hyperuricemia or gout in traditional medicine, and its active ingredient, osthol, is expected to be a leading compound for the development of new drugs for hyperuricemia.

scholarly journals Biological activities of the liverwort Marchantia polymorpha L. collected at Da Lat, Lam Dong province

2019 ◽  
Vol 2 (5) ◽  
pp. 26-34
Author(s):  
Tan Quoc Tran ◽  
Tam Thien Luong ◽  
Hoang Ngo Phan ◽  
Phuong Ngo Diem Quach
Keyword(s):  
Ethyl Acetate ◽  
Biological Activities ◽  
Folk Medicine ◽  
Secondary Compounds ◽  
Chloroform Extract ◽  
Marchantia Polymorpha ◽  
Traditional Treatment ◽  
Potential Applications ◽  
Contemporary Medicine ◽  
Mcf 7

Marchantia polymorpha L. is used as a folk medicine in India, China and some European countries for the treatment of inflammation, cure cuts, wounds, diuretics, etc. Natural compounds and biological activities of this liverwort have been studied in the world for few years. At present time, the studies on bryophytes (non-vascular plants) are quite limited, especially in Vietnam. Therefore, this research focused on investigating some biological activities and analyzing of major secondary metabolites of M. polymorpha L. collected at Da Lat, Lam Dong. Among four extracted fractions (nhexane, chloroform, ethyl acetate and ethanol), the chloroform extract exhibited the best antioxidant, antibacterial, anti-proliferation of MCF-7 cell line activities. The ethyl acetate extract exhibited better activity of tyrosinase and α-glucosidase inhibition than others. Main secondary compounds in this species were phenolics, steroids and glycosidederivatives. These results were scientific evidences that might help us to understand rigorously about the ultilization of Marchantia liverwort in the traditional treatment and new potential applications in the contemporary medicine.

Two isoprenylated flavonoids from Dorstenia psilurus activate AMPK, stimulate glucose uptake, inhibit glucose production and lower glycemia

2019 ◽  
Vol 476 (24) ◽  
pp. 3687-3704 ◽  
Author(s):  
Aphrodite T. Choumessi ◽  
Manuel Johanns ◽  
Claire Beaufay ◽  
Marie-France Herent ◽  
Vincent Stroobant ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Human Cancer ◽  
Glucose Production ◽  
Liver Mitochondria ◽  
New Drugs ◽  
Structural Isomer ◽  
Rat Liver Mitochondria ◽  
Ionization Mass ◽  
Ampk Activation ◽  
Starting Point

Root extracts of a Cameroon medicinal plant, Dorstenia psilurus, were purified by screening for AMP-activated protein kinase (AMPK) activation in incubated mouse embryo fibroblasts (MEFs). Two isoprenylated flavones that activated AMPK were isolated. Compound 1 was identified as artelasticin by high-resolution electrospray ionization mass spectrometry and 2D-NMR while its structural isomer, compound 2, was isolated for the first time and differed only by the position of one double bond on one isoprenyl substituent. Treatment of MEFs with purified compound 1 or compound 2 led to rapid and robust AMPK activation at low micromolar concentrations and increased the intracellular AMP:ATP ratio. In oxygen consumption experiments on isolated rat liver mitochondria, compound 1 and compound 2 inhibited complex II of the electron transport chain and in freeze–thawed mitochondria succinate dehydrogenase was inhibited. In incubated rat skeletal muscles, both compounds activated AMPK and stimulated glucose uptake. Moreover, these effects were lost in muscles pre-incubated with AMPK inhibitor SBI-0206965, suggesting AMPK dependency. Incubation of mouse hepatocytes with compound 1 or compound 2 led to AMPK activation, but glucose production was decreased in hepatocytes from both wild-type and AMPKβ1−/− mice, suggesting that this effect was not AMPK-dependent. However, when administered intraperitoneally to high-fat diet-induced insulin-resistant mice, compound 1 and compound 2 had blood glucose-lowering effects. In addition, compound 1 and compound 2 reduced the viability of several human cancer cells in culture. The flavonoids we have identified could be a starting point for the development of new drugs to treat type 2 diabetes.

Chemometric Analysis for the Classification of some Groups of Drugs with Divergent Pharmacological Activity on the Basis of some Chromatographic and Molecular Modeling Parameters

2018 ◽  
Vol 21 (2) ◽  
pp. 125-137
Author(s):  
Jolanta Stasiak ◽  
Marcin Koba ◽  
Marcin Gackowski ◽  
Tomasz Baczek
Keyword(s):  
Correlation Analysis ◽  
Pharmacological Activity ◽  
Correlation Coefficients ◽  
Principal Component ◽  
Cardiovascular Drugs ◽  
New Drugs ◽  
Analgesic Drugs ◽  
Starting Point ◽  
Chromatographic Parameters

Aim and Objective: In this study, chemometric methods as correlation analysis, cluster analysis (CA), principal component analysis (PCA), and factor analysis (FA) have been used to reduce the number of chromatographic parameters (logk/logkw) and various (e.g., 0D, 1D, 2D, 3D) structural descriptors for three different groups of drugs, such as 12 analgesic drugs, 11 cardiovascular drugs and 36 “other” compounds and especially to choose the most important data of them. Material and Methods: All chemometric analyses have been carried out, graphically presented and also discussed for each group of drugs. At first, compounds’ structural and chromatographic parameters were correlated. The best results of correlation analysis were as follows: correlation coefficients like R = 0.93, R = 0.88, R = 0.91 for cardiac medications, analgesic drugs, and 36 “other” compounds, respectively. Next, part of molecular and HPLC experimental data from each group of drugs were submitted to FA/PCA and CA techniques. Results: Almost all results obtained by FA or PCA, and total data variance, from all analyzed parameters (experimental and calculated) were explained by first two/three factors: 84.28%, 76.38 %, 69.71% for cardiovascular drugs, for analgesic drugs and for 36 “other” compounds, respectively. Compounds clustering by CA method had similar characteristic as those obtained by FA/PCA. In our paper, statistical classification of mentioned drugs performed has been widely characterized and discussed in case of their molecular structure and pharmacological activity. Conclusion: Proposed QSAR strategy of reduced number of parameters could be useful starting point for further statistical analysis as well as support for designing new drugs and predicting their possible activity.

Design of Inhibitors for Glyceraldehyde-3-phosphate Dehydrogenase (GAPDH) Enzyme of Leishmania mexicana

2020 ◽  
Vol 16 (6) ◽  
pp. 784-795
Author(s):  
Krisnna M.A. Alves ◽  
Fábio José Bonfim Cardoso ◽  
Kathia M. Honorio ◽  
Fábio A. de Molfetta
Keyword(s):  
Molecular Dynamics ◽  
Molecular Dynamics Simulations ◽  
Binding Site ◽  
Point Of View ◽  
New Drugs ◽  
Leishmania Mexicana ◽  
Receptor Complexes ◽  
Starting Point ◽  
Dynamics Simulations ◽  
Selection Of

Background:: Leishmaniosis is a neglected tropical disease and glyceraldehyde 3- phosphate dehydrogenase (GAPDH) is a key enzyme in the design of new drugs to fight this disease. Objective:: The present study aimed to evaluate potential inhibitors of GAPDH enzyme found in Leishmania mexicana (L. mexicana). Methods: A search for novel antileishmanial molecules was carried out based on similarities from the pharmacophoric point of view related to the binding site of the crystallographic enzyme using the ZINCPharmer server. The molecules selected in this screening were subjected to molecular docking and molecular dynamics simulations. Results:: Consensual analysis of the docking energy values was performed, resulting in the selection of ten compounds. These ligand-receptor complexes were visually inspected in order to analyze the main interactions and subjected to toxicophoric evaluation, culminating in the selection of three compounds, which were subsequently submitted to molecular dynamics simulations. The docking results showed that the selected compounds interacted with GAPDH from L. mexicana, especially by hydrogen bonds with Cys166, Arg249, His194, Thr167, and Thr226. From the results obtained from molecular dynamics, it was observed that one of the loop regions, corresponding to the residues 195-222, can be related to the fitting of the substrate at the binding site, assisting in the positioning and the molecular recognition via residues responsible for the catalytic activity. Conclusion:: he use of molecular modeling techniques enabled the identification of promising compounds as inhibitors of the GAPDH enzyme from L. mexicana, and the results obtained here can serve as a starting point to design new and more effective compounds than those currently available.

scholarly journals Characterisation of nitrogen-containing organic compounds by UHPLC-Qtof-MS and anti-amylase activity from the chloroform extract of the bark of Rhizophora mucronata

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
P. Resmi ◽  
G. Jitha ◽  
Vishnu Murali ◽  
Anu Gopinath
Keyword(s):  
Diabetes Mellitus ◽  
Amylase Activity ◽  
Chloroform Extract ◽  
Significant Activity ◽  
Rhizophora Mucronata ◽  
Inhibition Assay ◽  
Mangrove Plant ◽  
Starting Point ◽  
Treatment Of Diabetes ◽  
Nitrogen Containing Compounds

Abstract Background Medicinal importance of mangrove plant Rhizophora mucronata, a red mangrove species found in the Asian countries, has long been recognised in traditional systems of medicine. The identification of its phytoconstituents can be a starting point for the drug development. The aim of the work was to extend the current knowledge of phytoconstituents from R. mucronata and to explore its pharmacological importance in the treatment of diabetes mellitus. In the present study, we analysed the chloroform extract from the bark of the mangrove plant R. mucronata for nitrogen-containing constituents using UHPLC QTOF MS profiling, and α-amylase inhibition assay was carried out. Results Four nitrogen-containing compounds were identified from the chloroform extract of the bark of R. mucronata using UHPLC QTOF MS profiling. The compounds identified were N,N′-dicyclohexyl urea, a cryptolepine derivative (C17H15N3O), an aliphatic cyclic compound with hydroxyl and amino groups (C22H43NO), and C16H19NO2 (m/z 258.1495). The anti-amylase activity, an in vitro antidiabetic bioassay, of chloroform extract showed an IC50 value of 220.09 μg/ml. Conclusions This is the first report on the identification of nitrogen-containing compounds from the chloroform extract of the bark of the R. Mucronata. One of the compounds identified was a novel cryptolepine derivative (C16H13N3O), and it falls under the rare category indoloquinoline alkaloid. The chloroform extract also showed significant activity towards α-amylase inhibition assay. Thus, the study has gone some way towards our understanding of the efficacy of bark of the R. mucronata for the treatment of diabetes mellitus and is open for further research.

scholarly journals Phytochemical Composition and Biological Activities of Scorzonera Species

2021 ◽  
Vol 22 (10) ◽  
pp. 5128
Author(s):  
Karolina Lendzion ◽  
Agnieszka Gornowicz ◽  
Krzysztof Bielawski ◽  
Anna Bielawska
Keyword(s):  
Biological Activities ◽  
Folk Medicine ◽  
Quinic Acid ◽  
Hepatoprotective Activity ◽  
Phytochemical Composition ◽  
Starting Point ◽  
Microbial Infections ◽  
Bacteria And Fungi ◽  
Bioactive Potential

The genus Scorzonera comprises nearly 200 species, naturally occurring in Europe, Asia, and northern parts of Africa. Plants belonging to the Scorzonera genus have been a significant part of folk medicine in Asia, especially China, Mongolia, and Turkey for centuries. Therefore, they have become the subject of research regarding their phytochemical composition and biological activity. The aim of this review is to present and assess the phytochemical composition, and bioactive potential of species within the genus Scorzonera. Studies have shown the presence of many bioactive compounds like triterpenoids, sesquiterpenoids, flavonoids, or caffeic acid and quinic acid derivatives in extracts obtained from aerial and subaerial parts of the plants. The antioxidant and cytotoxic properties have been evaluated, together with the mechanism of anti-inflammatory, analgesic, and hepatoprotective activity. Scorzonera species have also been investigated for their activity against several bacteria and fungi strains. Despite mild cytotoxicity against cancer cell lines in vitro, the bioactive properties in wound healing therapy and the treatment of microbial infections might, in perspective, be the starting point for the research on Scorzonera species as active agents in medical products designed for miscellaneous skin conditions.

scholarly journals Effects of Elevated CO2 and Nitrogen Loading on the Defensive Traits of Three Successional Deciduous Broad-Leaved Tree Seedlings

Forests ◽  
2021 ◽  
Vol 12 (7) ◽  
pp. 939
Author(s):  
Yoko Watanabe ◽  
Kiyomi Hinata ◽  
Laiye Qu ◽  
Satoshi Kitaoka ◽  
Makoto Watanabe ◽  
...  
Keyword(s):  
Elevated Co2 ◽  
Environmental Changes ◽  
Total Phenolics ◽  
Condensed Tannin ◽  
N Uptake ◽  
Nitrogen Loading ◽  
Total Phenolic ◽  
Tree Seedlings ◽  
N Supply ◽  
Successional Species

To elucidate changes in the defensive traits of tree seedlings under global environmental changes, we evaluated foliar defensive traits of the seedlings of successional trees, such as beech, oak, and magnolia grown in a natural-light phytotron. Potted seedlings were grown under the combination of two CO2 concentrations (360 vs. 720 ppm) and two nitrogen (N) treatments (4 vs. 15 kg N ha−1 yr−1) for two growing seasons using quantitative chemical analyses and anatomical method. We hypothesized that the effects of CO2 and N depend on the successional type, with late successional species providing greater defense of their leaves against herbivores, as this species exhibits determinate growth. Beech, a late successional species, responded the most to both elevated CO2 concentration (eCO2) and high N treatment. eCO2 and low N supply enhanced the defensive traits, such as the high leaf mass per area (LMA), high carbon to N ratio (C/N ratio), and increase in the concentrations of total phenolic and condensed tannin in agreement with the carbon–nutrient balance (CNB) hypothesis. High N supply decreased the C/N ratio due to the high N uptake in beech leaves. Oak, a mid–late successional species, exhibited different responses from beech: eCO2 enhanced the LMA, C/N ratio, and concentration of total phenolics of oak leaves, but only condensed tannin increased under high N supply. Magnolia did not respond to all treatments. No interactive effects were observed between CO2 and N supply in all species, except for the concentration of total phenolics in oak. Although the amounts of phenolic compounds in beech and oak varied under eCO2 and high N treatments, the distribution of these compounds did not change. Our results indicate that the changes in the defensive traits of forest tree species under eCO2 with N loading are related to the successional type.

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