Chaetochromin, also known as 4548-G05, is an
orally active,
small-molecule
Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs ar ...
,
selective agonist of the
insulin receptor
The insulin receptor (IR) is a transmembrane receptor that is activated by insulin, IGF-I, IGF-II and belongs to the large class of receptor tyrosine kinase. Metabolically, the insulin receptor plays a key role in the regulation of glucose ho ...
.
It has
potent and long-lasting
antidiabetic activity ''
in vivo
Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, and ...
'' in mice.
The drug may represent a novel potential therapeutic agent for the treatment of
diabetes
Diabetes, also known as diabetes mellitus, is a group of metabolic disorders characterized by a high blood sugar level ( hyperglycemia) over a prolonged period of time. Symptoms often include frequent urination, increased thirst and increased ...
which is more convenient and
tolerable to
administer than
injected insulin.
It was discovered in 1981 in ''
Chaetomium
''Chaetomium'' is a genus of fungi in the Chaetomiaceae family. It is a dematiaceous (dark-walled) mold normally found in soil, air, cellulose and plant debris. According to the ''Dictionary of the Fungi'' (10th edition, 2008), there are about 9 ...
gracile'' fungi, and its interaction with the insulin receptor was identified in 2014.
Stereochemistry
Chaetochromin A and B are
stereoisomer
In stereochemistry, stereoisomerism, or spatial isomerism, is a form of isomerism in which molecules have the same molecular formula and sequence of bonded atoms (constitution), but differ in the three-dimensional orientations of their atoms in ...
s of this structure, while chaetochromin C and D are related but different compounds.
[''Pubchem'']
Chaetochromin
It is not known whether the insulin mimetic effect was found in chaetochromin A or B, or in a mixture.
See also
*
Anti-diabetic medication
Drugs used in diabetes treat diabetes mellitus by altering the glucose level in the blood. With the exceptions of insulin, most GLP receptor agonists ( liraglutide, exenatide, and others), and pramlintide, all are administered orally and are th ...
References
{{Reflist
Polyphenols
Anti-diabetic drugs
Benzochromenes
Diketones
Heterocyclic compounds with 3 rings
Insulin receptor agonists
3-Hydroxypropenals
Resorcinols
Biphenyls