scholarly journals Comparative evaluation of the inhibitory activities of the novel penicillanic acid sulfone Ro 48-1220 against beta-lactamases that belong to groups 1, 2b, and 2be.

1997 ◽  
Vol 41 (2) ◽  
pp. 475-477 ◽  
Author(s):  
L S Tzouvelekis ◽  
M Gazouli ◽  
E E Prinarakis ◽  
E Tzelepi ◽  
N J Legakis
Keyword(s):  
Inhibitory Activity ◽  
Comparative Evaluation ◽  
The Novel ◽  
Beta Lactamases ◽  
Penicillanic Acid ◽  
Inhibitory Activities ◽  
Group 1

The inhibitory activity of the penicillanic acid sulfone Ro 48-1220 against group 1, 2b, and 2be beta-lactamases was evaluated. Ro 48-1220 inhibited TEM and SHV as effectively as clavulanate and tazobactam. It also inhibited group 1 beta-lactamases at lower concentrations than tazobactam. Ro 48-1220, at a concentration of 4 micrograms/ml, protected ceftriaxone and ceftazidime against strains producing group 1 and 2be beta-lactamases.

Novel photochromic inhibitor for mitotic kinesin Eg5 which forms multiple isomerization states

2021 ◽  
Author(s):  
Islam Md Alrazi ◽  
Kei Sadakane ◽  
Shinsaku Maruta
Keyword(s):  
Inhibitory Activity ◽  
Molecular Motor ◽  
The Novel ◽  
Precise Control ◽  
Atpase Assay ◽  
Ic50 Value ◽  
Motor Activities ◽  
Ic50 Values ◽  
Kinesin Eg5 ◽  
Mitotic Kinesin Eg5

Abstract The mitotic kinesin Eg5 is a plus-end directed homotetrameric molecular motor essential for the formation of bipolar spindles during cell division. Kinesin Eg5 is overexpressed in cancer cells and hence considered as a target for cancer therapy; the inhibitors specific for Eg5 have been developed as anticancer drugs. In this study, we synthesized a novel functional photoresponsive inhibitor composed of spiropyran and azobenzene derivatives to control Eg5 function with multistage inhibitory activity accompanied by the formation of different isomerization states. The photochromic inhibitor spiropyran-sulfo-azobenzene (SPSAB) exhibited three isomerization states: spiro (SP)-trans, merocyanine (MC)-cis and MC-trans, upon exposure to visible light, ultraviolet and in the dark, respectively. SPSAB-induced reversible changes in the inhibitory activity of ATPase and motor activities correlating with photoisomerization among the three states. Among the three isomerization states of SPSAB, the SP-trans isomer showed potent inhibitory activity at an IC50 value of 30 µM in the basal ATPase assay. MC-trans and MC-cis exhibited less inhibitory activity at IC50 values of 38 and 86 µM, respectively. The results demonstrated that the novel photochromic inhibitor enabled precise control of Eg5 function at three different levels using light irradiation.

scholarly journals Antioxidant and angiotensin I-converting enzyme inhibitory activities of Xuanwei ham before and after cooking and in vitro simulated gastrointestinal digestion

2018 ◽  
Vol 5 (7) ◽  
pp. 180276 ◽  
Author(s):  
Le Wang ◽  
Xiang Li ◽  
Yingnan Li ◽  
Wenying Liu ◽  
Xiaoyun Jia ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Scavenging Activity ◽  
Angiotensin I ◽  
Gastrointestinal Digestion ◽  
Ace Inhibitory Activity ◽  
Angiotensin I Converting Enzyme ◽  
Before And After ◽  
Inhibitory Activities ◽  
Ace Inhibitory ◽  
Significant Increment

Xuanwei ham is especially rich in a large amount of peptides and free amino acids under the action of protein degradation. Some of these peptides can potentially exert bioactivities of interest for human health. Traditionally, Xuanwei ham should undergo Chinese household cooking treatments before eating. However, it has not been known how its bioactivity changes after cooking and gastrointestinal digestion. Herein, Xuanwei ham is analysed before and after cooking, as well as gastrointestinal digestion being simulated so as to evaluate and compare its effect on antioxidant and angiotensin I-converting enzyme (ACE) inhibitory activities. The antioxidant activity is analysed using five different methods, and results demonstrate that cooking has some negative effects on antioxidative capacity when determined using different antioxidant methods except for a significant increment in 1,1'-diphenyl-2-picrylhydrazyl radical-scavenging activity, while ACE inhibitory activity increases significantly after cooking compared with control samples. After gastrointestinal digestion of samples, there is a significant increment of the antioxidant and ACE inhibitory activities in comparison with control and cooked samples. Particularly, after gastrointestinal digestion, free thiols content and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical-cation-scavenging activity of Xuanwei ham, respectively, increase about twice and fourfold, while ACE inhibitory activity increases about twice compared to cooked samples, reaching the value of 83.73%. Therefore, through cooking the antioxidant activity and ACE inhibitory activity of Xuanwei ham are not completely lost and a part of them is still maintained, while gastrointestinal digestion produces a significant enhancement in both bioactivities, highlighting a greater potential for a beneficial physiological effect on human health after eating it.

scholarly journals Inhibitory activity of the novel CB2 receptor agonist, GW833972A, on guinea-pig and human sensory nerve function in the airways

2008 ◽  
Vol 155 (4) ◽  
pp. 547-557 ◽  
Author(s):  
M G Belvisi ◽  
H J Patel ◽  
V Freund-Michel ◽  
D J Hele ◽  
N Crispino ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Inhibitory Activity ◽  
Receptor Agonist ◽  
Sensory Nerve ◽  
The Novel ◽  
Nerve Function ◽  
Cb2 Receptor

scholarly journals COMPARATIVE EVALUATION OF SAFETY AND IMMUNOGENICITY INACTIVATED VACCINE FOR POLYOMIELITIS PREVENTION (NETHERLANDS) AND VACCINE «IMOVAX POLIO» (FRANCE) IN CHILDREN USING TRIPLE IMMUNIZATION

2019 ◽  
Vol 1 (3) ◽  
pp. 53-60
Author(s):  
I. V. Feldblyum ◽  
V. V. Romanenko ◽  
M. G. Menshikova ◽  
I. A. Okuneva ◽  
A. E. Makarov ◽  
...  
Keyword(s):  
Russian Federation ◽  
Multicenter Study ◽  
Safety Profile ◽  
Comparative Evaluation ◽  
Vaccination Schedule ◽  
Inactivated Vaccine ◽  
Poliomyelitis Vaccine ◽  
The Russian Federation ◽  
Group 2 ◽  
Group 1

Aim is comparative evaluation of the safety and immunogenicity of inactivated poliomyelitis vaccine (IPV) «Bilthoven Biologicals B.V.» (Netherlands) and «Imovax Polio» (France) with subcutaneous and intramuscular modes of administration. Materials and methods. In a doubleblind, comparative clinical randomized multicenter study, 120 children at the age of 3 months participated as volunteers. They were divided into 4 groups: 1 and 2 groups were given IPV intramuscular (group 1) and subcutaneous (group 2) mode of administration, children of groups 3 and 4 were given the vaccine «Imovax Polio». Results. IPV is characterized by a high safety profile and immunogenicity both in subcutaneous and intramuscular modes of administration and it is comparable in its characteristics with the vaccine «Imovax Polio». Conclusion. Vaccine IPV (Netherlands) is recommended for registration in the territory of the Russian Federation and its further using in the National Vaccination Schedule.

scholarly journals Artemisinin-independent inhibitory activity of Artemisia sp. infusions against different Plasmodium stages including relapse-causing hypnozoites

2021 ◽  
Vol 5 (3) ◽  
pp. e202101237
Author(s):  
Kutub Ashraf ◽  
Shahin Tajeri ◽  
Christophe-Sébastien Arnold ◽  
Nadia Amanzougaghene ◽  
Jean-François Franetich ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Plasmodium Falciparum ◽  
Inhibitory Activity ◽  
Parasite Species ◽  
Artemisia Annua ◽  
Combination Therapies ◽  
Lead Compounds ◽  
Low Concentrations ◽  
Inhibitory Activities

Artemisinin-based combination therapies (ACT) are the frontline treatments against malaria worldwide. Recently the use of traditional infusions from Artemisia annua (from which artemisinin is obtained) or Artemisia afra (lacking artemisinin) has been controversially advocated. Such unregulated plant-based remedies are strongly discouraged as they might constitute sub-optimal therapies and promote drug resistance. Here, we conducted the first comparative study of the anti-malarial effects of both plant infusions in vitro against the asexual erythrocytic stages of Plasmodium falciparum and the pre-erythrocytic (i.e., liver) stages of various Plasmodium species. Low concentrations of either infusion accounted for significant inhibitory activities across every parasite species and stage studied. We show that these antiplasmodial effects were essentially artemisinin-independent and were additionally monitored by observations of the parasite apicoplast and mitochondrion. In particular, the infusions significantly incapacitated sporozoites, and for Plasmodium vivax and P. cynomolgi, disrupted the hypnozoites. This provides the first indication that compounds other than 8-aminoquinolines could be effective antimalarials against relapsing parasites. These observations advocate for further screening to uncover urgently needed novel antimalarial lead compounds.

scholarly journals The novel trisubstituted pyran derivative D-142 has triple monoamine reuptake inhibitory activity and exerts potent antidepressant-like activity in rodents

2011 ◽  
Vol 671 (1-3) ◽  
pp. 39-44 ◽  
Author(s):  
Aloke K. Dutta ◽  
Bhaskar Gopishetty ◽  
Sanjib Gogoi ◽  
Solav Ali ◽  
Juan Zhen ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
The Novel ◽  
Pyran Derivative

Transferable cefoxitin resistance in enterobacteria from Greek hospitals and characterization of a plasmid-mediated group 1 beta-lactamase (LAT-2).

1996 ◽  
Vol 40 (7) ◽  
pp. 1736-1740 ◽  
Author(s):  
M Gazouli ◽  
L S Tzouvelekis ◽  
E Prinarakis ◽  
V Miriagou ◽  
E Tzelepi
Keyword(s):  
Escherichia Coli ◽  
Amino Acids ◽  
Klebsiella Pneumoniae ◽  
Enterobacter Aerogenes ◽  
Citrobacter Freundii ◽  
Beta Lactamase ◽  
Beta Lactamases ◽  
Greek Hospitals ◽  
Group 1

Cefoxitin resistance in Klebsiella pneumoniae from Escherichia coli strains isolated in Greek hospitals was found to be due to the acquisition of similar plasmids coding for group 1 beta-lactamases. The plasmids were not self-transferable but were mobilized by conjugative plasmids. These elements have also been spread to Enterobacter aerogenes. The most common enzyme was a Citrobacter freundii-derived cephalosporinase (LAT-2) which differed from LAT-1 by three amino acids.

GC-MS Investigation and Acetylcholinesterase Inhibitory Activity of Galanthus rizehensis

2013 ◽  
Vol 68 (3-4) ◽  
pp. 118-124 ◽  
Author(s):  
Buket Bozkurt Sarikaya ◽  
Nehir Unver Somer ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
Jaume Bastida ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Inhibitory Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Chromatography Mass Spectrometry ◽  
Inhibitory Activities ◽  
Alkaloid Extracts ◽  
Potent Inhibitory Activity

GC-MS (gas chromatography-mass spectrometry) analyses of alkaloids in the aerial parts and bulbs of Galanthus rizehensis Stern (Amaryllidaceae), collected during two different vegetation periods, was performed. Twenty three alkaloids were identified in four different alkaloid extracts. Acetylcholinesterase (AChE) inhibitory activities of the alkaloid extracts were tested. Both the highest alkaloid diversity and the most potent inhibitory activity (IC50 12.94 μg/ml) were obtained in extracts from the bulbs of G. rizehensis collected during the fruiting period.

scholarly journals Antimicrobial and Alpha-Amylase Inhibitory Activities of Organic Extracts of Selected Sri Lankan Bryophytes

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Annalingam Kirisanth ◽  
M. N. M. Nafas ◽  
Ranga K. Dissanayake ◽  
Jayantha Wijayabandara
Keyword(s):  
Inhibitory Activity ◽  
Pathogenic Fungus ◽  
Fungal Species ◽  
Biologically Active ◽  
Alpha Amylase ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Plant Materials ◽  
Natural Product Research ◽  
Inhibitory Activities

Medicinal plants have been the main focus of natural product research. However, recent research has revealed that lower plants including bryophytes are also a major resource of biologically active compounds with novel structures. Sri Lanka is considered as a biodiversity hotspot with a higher degree of endemism flora including bryophytes. In this study, different species of bryophytes were investigated for their antimicrobial and alpha-amylase inhibitory activities. The air-dried plant materials of 6 different bryophyte species, Marchantia sp., Fissidens sp., Plagiochila sp., Sematophyllum demissum, Hypnum cupressiforme, and Calymperes motley, were subjected to sequential cold extraction with 3 different organic solvents. All three types of organic crude extracts were subjected to screening of antimicrobial bioassays using the disc-diffusion method against 3 bacterial strains and 1 fungal strain. According to the results obtained, 6 extracts out of 18 showed antibacterial activity for tested Gram-positive bacteria and 1 active against Gram-negative bacteria. Two extracts showed activity against the pathogenic fungus strain. Extracts from some plants were active against tested bacterial as well as fungal species. TLC-based bioautographic study was carried out to identify the corresponding active bands which is useful for active compound isolation. Furthermore, the ethyl acetate extracts were subjected to evaluate alpha-amylase inhibitory activity where three extracts out of six extracts showed moderate inhibitory activity for alpha-amylase with IC50 ranging 8–30%.

scholarly journals New Alkaloids and Anti-inflammatory Constituents from the Leaves of Antidesma ghaesembilla

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200
Author(s):  
Phan Van Kiem ◽  
Le Canh Viet Cuong ◽  
Do Thi Trang ◽  
Nguyen Xuan Nhiem ◽  
Hoang Le Tuan Anh ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inhibitory Activity ◽  
No Production ◽  
Raw 264.7 ◽  
Chemical Methods ◽  
Raw 264.7 Macrophages ◽  
Chemical Structures ◽  
Bv2 Cells ◽  
Inhibitory Activities ◽  
Physical And Chemical

Using various chromatographic methods, two new alkaloids, antidesoic acids A (1) and B (2) along with fourteen known compounds (3-16) were isolated from the leaves of Antidesma ghaesembilla Gaertn. Their chemical structures were elucidated by physical and chemical methods. All the isolated compounds were evaluated for their inhibitory activity on LPS-stimulated nitric oxide (NO) production in BV2 cells and RAW 264.7 macrophages. Bisflavone 8 significantly inhibited LPS-stimulated NO production in BV2 cells and RAW 264.7 macrophages with IC50 values of 5.4 and 8.0 μM, respectively. Compounds 1–3, 7, 10, 12, 14, and 16 showed moderate inhibitory activities with IC50 values ranging from 11.7 to 77.4 μM.

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