scholarly journals BIOLOGICAL ACTIVITIES OF NOVEL IN VITRO RAISED STEVIA PLANT

2017 ◽  
Vol 10 (8) ◽  
pp. 240 ◽  
Author(s):  
Neeta Raj Sharma ◽  
Vineet Meshram ◽  
Mahiti Gupta
Keyword(s):  
Pancreatic Lipase ◽  
Staphylococcus Epidermidis ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Gram Negative Bacteria ◽  
Herbal Formulation ◽  
Further Development

  Objective: This communication explores a lead fraction from methanolic extract of novel Stevia species raised under in vitro conditions for its various biological activities.Methods: The dried Stevia leaves were crushed in methanol to get the polar extract. This methanol extract was tested for pancreatic lipase and alpha-amylase inhibitory activity using quantitative plate assays. Antibacterial property of the extract was also evaluated against Staphylococcus epidermidis, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. Further, the antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl.Results: The methanolic extract inhibited pancreatic lipase with IC50 of 5.74 μg/ml in a similar manner to a well-known anti-obesity drug in the market orlistat. The methanolic extract also showed a better pancreatic α-amylase inhibitory activity (IC50=88 μg/ml) than acarbose. Further, the lead fraction exhibited 88.48% antioxidant activity. It also exhibited broad spectrum antimicrobial activity against the spectrum of Gram-positive and Gram-negative bacteria tested under laboratory conditions with a minimal inhibitory concentration ranging from 1.95 to 31.25 μg/ml.Conclusion: Thus, this study signifies the vast potential of the lead fraction from a novel Stevia species for further development into a herbal formulation for prevention of various infectious and non-infectious diseases.

scholarly journals Synthesis and Biological Evaluation of New Substituted 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one Derivatives asα-Glucosidase Inhibitors

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Yu-ling Wang ◽  
Ting-jian Zhang ◽  
Jing-wei Liang ◽  
Fan-hao Meng ◽  
Shao-jie Wang
Keyword(s):  
Inhibitory Activity ◽  
Methoxy Group ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Further Development ◽  
Synthesis And Biological Evaluation

A series of new substituted 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives bearing groups methoxy,tert-butyl, and atoms of halogens at thepara-position of the A-ring were synthesized andin vitrobiological activities were evaluated as nonsugarα-glucosidase inhibitors. Most of the test compounds demonstrated significantα-glucosidase inhibitory activity relative to that of Acarbose (IC50= 29.26 μM). Thepara-substitution with a methoxy group or halogens could notably increase the potency. Compounds17,18, and23, with IC50values of 0.025 μM, 0.014 μM, and 0.018 μM, respectively, may be of significance for the further development of new nonsugarα-glucosidase inhibitors.

scholarly journals Phytochemical and Biological Profile of Moricandia arvensis (L.) DC.: An Inhibitor of Pancreatic Lipase

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2829 ◽  
Author(s):  
Mariangela Marrelli ◽  
Federica Morrone ◽  
Maria Argentieri ◽  
Lucia Gambacorta ◽  
Filomena Conforti ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Dietary Lipids ◽  
Lipid Absorption ◽  
Flavonoid Glycosides ◽  
Moricandia Arvensis ◽  
Ic50 Values

Pancreatic lipase, a key enzyme for lipid absorption, is one of the most important targets for the treatment of obesity, while natural compounds have recently attracted much interest as potential inhibitors of this enzyme. Here, in an attempt to find new effective agents, the methanolic extract from Moricandia arvensis (L.) DC. and its sub-extracts were investigated for their potential inhibitory activity. The ability to inhibit pancreatic lipase was verified through the in vitro evaluation of the prevention of p-nitrophenyl caprylate hydrolysis. The antioxidant activity was also verified by means of DPPH and β-carotene bleaching tests. Compositional profiling revealed that flavonoid glycosides were the main specialized metabolites present in the methanolic extract from the aerial parts of the plant with kaempferol and quercetin representing the two O-glycosylated aglycones. Kaempferol-3-O-β-(2″-O-glucosyl)-rutinoside and kaempferol-3-O-a-arabinosyl-7-O-rhamnoside were the most abundant flavonols. The crude methanolic extract and the dichloromethane and ethyl acetate sub-extracts showed a strong lipase inhibitory activity, with IC50 values of 2.06 ± 0.02, 1.52 ± 0.02 and 1.31 ± 0.02 mg/mL, respectively. The best capacity to scavenge DPPH radical was detected for the ethyl acetate sub-extract (IC50 = 171.9 ± 1.0 µg/mL), which was also effective in protecting linoleic acid from peroxidation (IC50 = 35.69 ± 2.30 µg/mL). Obtained results support the hypothesis that M. arvensis can be a source of bioactive phytochemicals for the pharmacological inhibition of dietary lipids absorption.

scholarly journals Flavonoid-Coated Gold Nanoparticles as Efficient Antibiotics against Gram-Negative Bacteria—Evidence from In Silico-Supported In Vitro Studies

Antibiotics ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 968
Author(s):  
Hani A. Alhadrami ◽  
Raha Orfali ◽  
Ahmed A. Hamed ◽  
Mohammed M Ghoneim ◽  
Hossam M. Hassan ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
In Silico ◽  
Biological Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Ic50 Values ◽  
Membrane Rigidity ◽  
Further Development

Flavonoids are a class of bioactive plant-derived natural products that exhibit a broad range of biological activities, including antibacterial ones. Their inhibitory activity toward Gram-positive bacterial was found to be superior to that against Gram-negative ones. In the present study, a number of flavonoid-coated gold nanoparticles (GNPs) were designed to enhance the antibacterial effects of chrysin, kaempferol, and quercetin against a number of Gram-negative bacteria. The prepared GNPs were able to conjugate to these three flavonoids with conjugation efficiency ranging from 41% to 80%. Additionally, they were able to exert an enhanced antibacterial activity in comparison with the free flavonoids and the unconjugated GNPs. Quercetin-coated GNPs were the most active nano-conjugates and were able to penetrate the cell wall of E. coli. A number of in silico experiments were carried out to explain the conjugation efficiency and the antibacterial mechanisms of these flavonoids as follows: (i) these flavonoids can efficiently bind to the glutathione linker on the surface of GNPs via H-bonding; (ii) these flavonoids, particularly quercetin, were able to increase the bacterial membrane rigidity, and hence decrease its functionality; (iii) these flavonoids can inhibit E. coli’s DNA gyrase (Gyr-B) with IC50 values ranging from 0.9 to 3.9 µM. In conclusion, these bioactive flavonoid-based GNPs are considered to be very promising antibiotic candidates for further development and evaluation.

scholarly journals Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Significant Inhibition ◽  
Isolation And Identification ◽  
Vasorelaxant Effect ◽  
Methanolic Extracts ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

Antimicrobial activity of Pycnarrhena cauliflora (Miers.) Diels. methanol extract

2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Methanolic Extract ◽  
Biological Activities ◽  
Positive Control ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Methanolic Extracts

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.

Synthesis,Characterization and Evaluation of Biological Activity of Sulfonylhydrazide-Schiff Base" (E)- N’-(2,5-dimethoxybenzalidene) naphthalene-2-sulfonohydrazide"

2020 ◽  
Vol 8 (1) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Inhibitory Concentration ◽  
Condensation Reaction ◽  
Gram Negative Bacteria ◽  
Biological Applications ◽  
Bacteriostatic Effect ◽  
1H And 13C Nmr ◽  
13C Nmr Analysis ◽  
Ft Ir

Condensation reaction of naphthalene -2-Sulfonylhydrazide, as starting material with 2,5-dimethoxy benzaldehyde was used to produce (E)-N’-(2,5-dimethoxybenzalidene)naphthalene-2-sulfonohydrazide. The Schiff base product was isolated, purified and then spectrally characterized via UV-Vis, GC/MS, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Antimicrobial activity of Schiff base product was evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. The tests showed a promising bacteriostatic effect of this compound against gram negative bacteria such as P. aeruginosa and K. pneumoniae, such character is valuable for biological applications.

IN VITRO STUDIES OF SOME EDIBLE SPICES ON PANCREATIC LIPASE INHIBITORY ACTIVITY

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 62-68
Author(s):  
S Mhatre ◽  
◽  
A. Bhagit ◽  
R. P Yadav
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Syzygium Aromaticum ◽  
High Potency ◽  
Good Source ◽  
Zanthoxylum Armatum ◽  
Methanolic Extracts ◽  
Cinnamomum Tamala

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.

scholarly journals Secondary Metabolites from Gorgonian Corals of the Genus Eunicella: Structural Characterizations, Biological Activities, and Synthetic Approaches

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 129
Author(s):  
Dario Matulja ◽  
Maria Kolympadi Markovic ◽  
Gabriela Ambrožić ◽  
Sylvain Laclef ◽  
Sandra Kraljević Pavelić ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Antimicrobial Activities ◽  
Chemical Structures ◽  
Gorgonian Corals ◽  
Synthetic Approaches ◽  
Further Development

Gorgonian corals, which belong to the genus Eunicella, are known as natural sources of diverse compounds with unique structural characteristics and interesting bioactivities both in vitro and in vivo. This review is focused primarily on the secondary metabolites isolated from various Eunicella species. The chemical structures of 64 compounds were divided into three main groups and comprehensively presented: a) terpenoids, b) sterols, and c) alkaloids and nucleosides. The observed biological activities of depicted metabolites with an impact on cytotoxic, anti-inflammatory, and antimicrobial activities were reviewed. The most promising biological activities of certain metabolites point to potential candidates for further development in pharmaceutical, cosmetic, and other industries, and are highlighted. Total synthesis or the synthetic approaches towards the desired skeletons or natural products are also summarized.

scholarly journals In vitro activities of oxazolidinone compounds U100592 and U100766 against Staphylococcus aureus and Staphylococcus epidermidis.

1996 ◽  
Vol 40 (3) ◽  
pp. 799-801 ◽  
Author(s):  
G W Kaatz ◽  
S M Seo
Keyword(s):  
Staphylococcus Aureus ◽  
Staphylococcus Epidermidis ◽  
Inhibitory Activity ◽  
Antimicrobial Agents ◽  
Methicillin Resistant ◽  
Clinical Strains ◽  
Time Kill

The new oxazolidinone antimicrobial agents U100592 and U100766 demonstrated good in vitro inhibitory activity against clinical strains of Staphylococcus aureus and Staphylococcus epidermidis regardless of methicillin susceptibility. Both agents appeared bacteriostatic by time-kill analysis. Stable resistance to low multiples of the MIC of either drug could be produced only in methicillin-resistant S. aureus.

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