scholarly journals Pentacyclic triterpene acids: use, mode of action, Biological activity and synthesis

2020 ◽  
Vol 10 (3) ◽  
Keyword(s):  
Biological Activity ◽  
Mode Of Action ◽  
Pentacyclic Triterpene ◽  
Triterpene Acids

scholarly journals Tetra- and Pentacyclic Triterpene Acids from the Ancient Anti-inflammatory Remedy Frankincense as Inhibitors of Microsomal Prostaglandin E2Synthase-1

2014 ◽  
Vol 77 (6) ◽  
pp. 1445-1451 ◽  
Author(s):  
Moritz Verhoff ◽  
Stefanie Seitz ◽  
Michael Paul ◽  
Stefan M. Noha ◽  
Johann Jauch ◽  
...  
Keyword(s):  
Pentacyclic Triterpene ◽  
Triterpene Acids ◽  
Anti Inflammatory

Design, synthesis and biological activity evaluation of novel conjugated sialic acid and pentacyclic triterpene derivatives as anti-influenza entry inhibitors

MedChemComm ◽  
2016 ◽  
Vol 7 (10) ◽  
pp. 1932-1945 ◽  
Author(s):  
Xu Han ◽  
Yongying Shi ◽  
Longlong Si ◽  
Zibo Fan ◽  
Han Wang ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Biological Activity ◽  
Sialic Acid ◽  
Virus Entry ◽  
Pentacyclic Triterpene ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Activity Evaluation ◽  
Virus Entry Inhibitors

A total of 24 novel sialic acid–pentacyclic triterpene conjugates were synthesized and evaluated as anti-influenza virus entry inhibitors.

scholarly journals Thiol-Modification as Important Mode of Action for Allicin from Garlic (Allium sativum)

Proceedings ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 27 ◽  
Author(s):  
Martin C. H. Gruhlke
Keyword(s):  
Molecular Weight ◽  
Biological Activity ◽  
Active Compound ◽  
Mode Of Action ◽  
Allium Sativum ◽  
Cysteine Residues ◽  
Low Molecular Weight ◽  
Thiol Groups ◽  
Ancient Times ◽  
In Cells

Garlic is a common ingredient in food, normally used as spice but is also used since ancient times for its health beneficial activity. The thiosulfinate allicin is the first active compound in freshly damaged garlic tissue and reacts with thiol-groups. Hence, allicin is able to modify thiol groups, both of protein cysteine-residues and low-molecular weight thiols like glutathione. This thiol-modification is supposed to be an important mechanism for allicin’s biological activity. Here, the mechanisms and possible targets for allicin in cells are discussed.

scholarly journals AFN-1252 is a potent inhibitor of enoyl-ACP reductase from B urkholderia pseudomallei -Crystal structure, mode of action, and biological activity

2015 ◽  
Vol 24 (5) ◽  
pp. 832-840 ◽  
Author(s):  
Krishnamurthy Narasimha Rao ◽  
Anirudha Lakshminarasimhan ◽  
Sarah Joseph ◽  
Swathi U. Lekshmi ◽  
Ming-Seong Lau ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
Mode Of Action ◽  
Potent Inhibitor ◽  
Enoyl Acp Reductase

scholarly journals The effect of chemical modifications induced in insulin on the reactivity of the interchain disulphide bonds towards sodium sulphite

1968 ◽  
Vol 108 (2) ◽  
pp. 247-255 ◽  
Author(s):  
A. Massaglia ◽  
F. Pennisi ◽  
U. Rosa ◽  
S. Ronca-Testoni ◽  
C. A. Rossi
Keyword(s):  
Biological Activity ◽  
Mode Of Action ◽  
High Reactivity ◽  
Sodium Sulphite ◽  
Thiol Groups ◽  
Chemical Modifications ◽  
Amperometric Titration ◽  
Disulphide Bonds ◽  
Native Insulin

The reactivity of the three disulphide bridges of insulin towards sodium sulphite was studied by amperometric titration of the liberated thiol groups. In the native, acetylated or succinylated molecule two bridges react at pH7, but in the methylated or phenylcarbamoylated molecule only one bridge reacts. All three bridges react in all derivatives in 8m-urea or at pH9. Loss in biological activity parallels the loss in reactivity of one of the bridges during methylation. It is suggested that change in reactivity of the S·S bonds reflects the occurrence of a conformational modification of the protein. The possibility is discussed that the unusually high reactivity of the S·S bonds in native insulin depends strictly on the integrity of the native molecule, suggesting that S·S bonds are in some way involved in the hormone's mode of action.

Studies on biliary excretion in the rabbit - II. The relationship between the chemical structure of certain natural or synthetic pentacyclic triterpenes and their icterogenic activity - Part 2: The substituents on carbon atoms 17, 19, 20 and 22

1964 ◽  
Vol 160 (979) ◽  
pp. 246-257 ◽  
Keyword(s):  
Chemical Structure ◽  
Hydroxyl Group ◽  
Side Chain ◽  
Fatty Acid Residue ◽  
Structural Variations ◽  
Modified Technique ◽  
Considerable Decrease ◽  
Pentacyclic Triterpene ◽  
Triterpene Acids ◽  
The Relationship

Previously reported work in this series (Brown, Rimington & Sawyer 1963) produced evidence that icterogenic activity (i.a.) of the pentacyclic triterpene acids is based upon the presence of a β-equatorially orientated hydroxyl group at C (3), or a hydroxyl at C (24), and a 22β-angeloyloxy side chain in the molecule of the particular active compound. The second part of this work, dealing with certain structural variations in triterpenes of the oleanane, 24-noroleanane (hedragane) and ursane series, is reported in this paper. These variations involve i.a. esterification of the C (28) carboxyl, saturation of the 22β-angeloyl side chain or replacement of this by simple saturated aliphatic acids. Assays are recorded of a further thirteen of these compounds for icterogenic activity using the modified technique described in the second paper of this series (Brown et al . 1963). It has been concluded from this work that the icterogenicity of 3β- or 24β-hydroxy triterpene acids is undoubtedly associated with the 22β-angeloyloxy side chain. Removal of the esterifying group at C (22) or its replacement by a simple saturated fatty acid residue is followed by complete loss of activity. Esterification of the C (28) carboxyl produces a considerable decrease in icterogenic potency due, probably, to a decrease in solubility of the compound.

Studies on the Mode of Action of Insulin: Properties and Biological Activity of an Insulin-Dextran Complex

Endocrinology ◽  
1972 ◽  
Vol 90 (5) ◽  
pp. 1220-1230 ◽  
Author(s):  
FUJIO SUZUKI ◽  
YASUSHI DAIKUHARA ◽  
MASAYOSHI ONO ◽  
YOSHIRO TAKEDA
Keyword(s):  
Biological Activity ◽  
Mode Of Action

THE UPTAKE OF LOCALLY APPLIED [6:7-3H]OESTRADIOL-17β BY THE VAGINA OF THE OVARIECTOMIZED MOUSE

1964 ◽  
Vol 30 (3) ◽  
pp. 337-346 ◽  
Author(s):  
L. MARTIN
Keyword(s):  
Biological Activity ◽  
Mode Of Action ◽  
Common Site ◽  
Tissue Levels ◽  
Ovariectomized Mouse ◽  
Receptor Sites ◽  
Site Of Action

SUMMARY Locally applied [6:7-3H]oestradiol was taken up rapidly by the vagina, at a rate similar to that of oestrone. Levels of radioactivity in the tissue reached their highest value 1–3 min. after application, and thereafter dropped slowly to reach 20% of the injected dose at 12 hr. This is in contrast to the behaviour of oestrone, the tissue levels of which fell rapidly over the first ½ hr. It is suggested that this difference accounts for the relative biological activity of the two hormones in the vagina, and results from varying affinities for receptor sites associated with the initiation of vaginal growth. Evidence is presented that oestrone, oestradiol and oestriol have a common site of action. Dimethylstilboestrol (DMS) converted the retention pattern of oestradiol to one resembling that of oestrone, and it is suggested that this involves blocking of receptor sites. The results are discussed in relation to the mode of action of oestrogens.

Biological Activity and Mode of Action of a Specific Antiphage Substance, AFS

1975 ◽  
Vol 39 (5) ◽  
pp. 1137-1142
Author(s):  
Takeshi Uchida ◽  
Teruhiko Beppu ◽  
Kei Arima
Keyword(s):  
Biological Activity ◽  
Mode Of Action
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