Studies on hindered phenols and analogs. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity

1990 ◽  
Vol 33 (5) ◽  
pp. 1491-1496 ◽  
Author(s):  
Yuichi Aizawa ◽  
Tsutomu Kanai ◽  
Kazuo Hasegawa ◽  
Takeshi Yamaguchi ◽  
Yoshio Iizuka ◽  
...  
Keyword(s):  
Inhibiting Activity ◽  
Hindered Phenols

HERG channel inhibiting activity of Rauvolfia nukuhivensis alkaloid content

Planta Medica ◽  
2014 ◽  
Vol 80 (16) ◽  
Author(s):  
NJ Martin ◽  
EA López ◽  
G Lecellier ◽  
M Nicolas ◽  
C Paetz ◽  
...  
Keyword(s):  
Alkaloid Content ◽  
Herg Channel ◽  
Inhibiting Activity

Substituted Amides of Quinoline Derivatives: Preparation and Their Photosynthesis-inhibiting Activity

2006 ◽  
Author(s):  
Robert Musiol ◽  
Josef Jampilek ◽  
Katarina Kralova ◽  
Dominik Tabak ◽  
Barbara Podeszwa ◽  
...  
Keyword(s):  
Inhibiting Activity ◽  
Quinoline Derivatives

Isolation and Identification of a Potent PTP1B Inhibitor, Ursolic Acid, from Carolina Jasmine (Gelsemium sempervirens (L.) J.St.-Hil.)

2020 ◽  
Vol 17 (12) ◽  
pp. 939-943
Author(s):  
Toshiro Noshita ◽  
Yusuke Kakizoe ◽  
Satoshi Tanabe ◽  
Hidekazu Ouchi ◽  
Akihiro Tai
Keyword(s):  
Ursolic Acid ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Active Agent ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibiting Activity ◽  
Inhibition Activity ◽  
Isolation And Identification ◽  
Gelsemium Sempervirens

Extracts of Carolina jasmine (Gelsemium sempervirens (L.) J.St.-Hil.) petals were evaluated in vitro for inhibition activity against protein tyrosine phosphatase 1B (PTP1B). The principle active agent was also isolated from the extract and identified as ursolic acid (1). This is the first report of ursolic acid from G. sempervirens and of PTP1B-inhibiting activity in the genus Gelsemium.

The Anticholinesterase Activity of Three Local Food Spices and Their Anti-Alzheimer Application

2020 ◽  
Vol 01 ◽  
Author(s):  
Ruqia Bibi ◽  
Saima Gul ◽  
Abdul Wahab ◽  
Mohammad Iqbal Khan ◽  
Murad Ali Khan
Keyword(s):  
Neurodegenerative Disorder ◽  
Curcuma Longa ◽  
Chloroform Extract ◽  
Food Plants ◽  
In Vivo Studies ◽  
Assay Method ◽  
Inhibiting Activity ◽  
Asian Countries ◽  
Phytochemical Study ◽  
The World

Background: The incidence of dementia is increasing as the aging population of the world is increasing. Alzheimer’s disease (AD) is the neurodegenerative disorder of the central nervous system. There are presently 7.3 million patents of AD and the number may rise to 34 million at this pace in the coming thirty years. In the disease, the level of Acetylcholine is reduced and as a result, causes the loss of cholinergic neurons in the brain. The disease is less common in Asian countries as compared to the western nations of the world. This work aimed to establish the role of the common medicinal and food plants against Alzheimer. Methods: The enzyme acetylcholinesterase (AChE) is the enzyme responsible for hydrolysis and reduction of Acetylcholine. The anti-acetylcholinesterase activity of different extracts of three local plants used as spices in the daily food, Curcuma longa, Cinnnamomum tamala, and Zingiber officinale, were determined using the Microplate Assay method. Results: The phytochemical study of the selected plants revealed the presence of alkaloids, terpenes, flavones, saponins, and tannins in these plants. The chloroform extract of all the three plants presented promising AChE inhibiting activity having IC50 >200μg/ml. A probable reason will be the alkaloids and terpenes present in the chloroform extract. Conclusion: The chloroform extract of all three plants presented promising AChE inhibiting activity and can become a reasonable therapy for the cure/ prevention of Alzheimer disease. The frequent use of these spices may be a possible reason for the fever incidence of Alzheimer in Asian countries. Further in vivo studies are required to find its action and studies to find the exact compound responsible for the action.

Some 6-substituted derivatives of D-8-cyanomethylergoline-I and D-8-methylergoline-I

1979 ◽  
Vol 44 (3) ◽  
pp. 946-951 ◽  
Author(s):  
Antonín Černý ◽  
Jiří Křepelka ◽  
Miroslav Semonský
Keyword(s):  
Inhibiting Activity ◽  
Chloro Derivatives ◽  
Derivatives Of

Compounds III-XX exhibiting antilactation and antinidation effects in tests on rats were prepared on N(6)-alkylation of D-8-cyanomethylergoline-I (I) or D-8-methylergoline-I (II) with corresponding bromo (chloro) derivatives in dimethylformamide. The most distinct prolactin-inhibiting activity was found in compound III.

GENETIC HETEROGENEITY OF RABBIT ALPHA-1-ANTITRYPSIN

Genetics ◽  
1984 ◽  
Vol 106 (4) ◽  
pp. 695-703
Author(s):  
F Kueppers ◽  
C C Lee ◽  
R R Fox ◽  
J K Mills
Keyword(s):  
Sexual Dimorphism ◽  
Genetic Heterogeneity ◽  
Inbred Strains ◽  
Quantitative Variation ◽  
Moderate Degree ◽  
Inhibiting Activity ◽  
Interindividual Differences ◽  
Alpha 1 Antitrypsin ◽  
Serum Trypsin

ABSTRACT Sixteen inbred or partially inbred strains of rabbits were investigated for electrophoretic and quantitative variations of alpha-1-antitrypsin (A-1-AT). We found interindividual differences in the electrophoretic A-1-AT patterns as well as quantitative differences in the concentrations of A-1-AT and the serum trypsin-inhibiting activity. Three electrophoretic phenotypes were distinguished: M, P and MP. M was characterized by a predominant anodal A-1-AT band, and P had a major cathodal component. The MP pattern can be explained by the occurrence of the M and P components in the same serum due to heterozygosity. The P pattern was associated with an A-1-AT concentration of approximately 56% of that in sera with the M phenotype. The levels of A-1-AT in sera with the MP phenotype were intermediate between those in M and P types. In addition to the type-specific quantitative variation, we found a quantitative sexual dimorphism of a moderate degree: Female rabbits had A-1-AT concentrations 16% less than males.

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