148707-39-5Relevant articles and documents
(-)-Epigallocatechin gallate derivatives reduce the expression of both urokinase plasminogen activator and plasminogen activator inhibitor-1 to inhibit migration, adhesion, and invasion of MDA-MB-231 cells
Shin, Sunhye,Kim, Mi Kyoung,Jung, Woong,Chong, Youhoon
, (2018)
Urokinase plasminogen activator (uPA) and its inhibitor plasminogen activator inhibitor-1 (PAI-1) are established independent biomarkers for high metastasis risk in breast cancer. In this study, we investigated the regulatory activity of (-)-epigallocatechin-3-gallate (EGCG) and its derivatives on uPA and PAI-1 expression and thereby their anti-metastatic potential. EGCG showed only marginal effects on the uPA system and on the metastatic behavior of breast cancer cells (MDA-MB-231). However, the EGCG derivative 3e with a methyl-substituted carbonate substituent at the 4″-position showed potent inhibition of PAI-1 (62%) and uPA (50%) expression. The Ras-extracellular-signal-regulated kinase (ERK), p38 mitogen-activated protein kinase (MAPK), and phosphatidylinositol-3-kinase (PI3K)/Akt/NF-κB pathways, which regulate uPA and PAI-1 expression, were also affected by 3e (25%, 45%, and 25% reduction, respectively). In line with these findings, substantial reduction in metastatic behavior of MDA-MB-231 cells, such as adhesion (40%), invasion (56%), and migration (40%), was observed in the presence of 3e. It is also noteworthy that, in MDA-MB-231 cells, 3e did not exert any beneficial effect on the expression of matric metalloprotein (MMP) 2 and 9, which indicates that the anti-metastatic activity of 3e in MDA-MB-231 cells is not related to its regulation of the expression of MMPs. Taken together, we have shown that the EGCG derivative 3e could suppress the metastatic behavior of MDA-MB-231 cells through regulation of uPA and PAI-1.
FLAVAN-3-OLS AND PROANTHOCYANIDINS FROM CISTUS INCANUS
Petereit, Frank,Kolodziej, Herbert,Nahrstedt, Adolf
, p. 981 - 985 (1991)
Four monomeric and seven oligomeric flavanoids have been identified from a Cistus incanus subspecies traditionally used for treatment of skin diseases in northern parts of Greece and identified as subsp. tauricus.Flavan-3-ols are (+)-catechin, (+)-gallocatechin, the novel (+)-gallocatechin 3-gallate and the rarely occurring (+)-catechin 3-O-α-L-rhamnoside; proanthocyanidins are procyanidins B1 and B3, gallocatechin-(4α->8)-gallocatechin, its novel (4α->6)-regioisomer, gallocatechin-(4α->8)-catechin, the tentatively identified novel catechin-(4α->8)-gallocatechin and the trimer gallocatechin-(4α->8)-gallocatechin-(4α->8)-catechin.The uncommon flavanone 2R,3R-dihydromyricetin was also obtained.
(-)-epigallocatechin gallate prodrugs , preparation method thereof and composition for mitochondrial biosis
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Paragraph 0169; 0172; 0173, (2019/12/31)
The present invention relates to an epigallocatechin gallate prodrug, a method for manufacturing the same, and a composition for promoting mitochondrial biosynthesis comprising the same. A compound represented by chemical formula (1) according to the present invention increases the activity of PGC-1andalpha;, AMPK, and SIRT1, known as mitochondrial biosynthesis regulators, increases the amount of mitochondrial DNA, and increases a NAD+/NADH ratio, a level of cytochrome c, the synthesis of ATP, and oxygen consumption, thereby confirming an effect of increasing the mitochondrial activity and biosynthesis. In addition, it is confirmed that the compound has an effect of having a high absorption rate and slow metabolism in vivo compared to an existing epigallocatechin gallate, thereby being useful for a purpose of preventing or treating diseases related to mitochondrial dysfunction.COPYRIGHT KIPO 2020
ACTIVE AGENTS AND METHODS OF THEIR USE FOR THE TREATMENT OF METABOLIC DISORDERS AND NONALCOHOLIC FATTY LIVER DISEASE
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Page/Page column 67; 69, (2019/12/28)
Disclosed herein are active agents, compositions containing them, unit dosage forms containing them, and methods of their use, e.g., for treating a metabolic disorder or nonalcoholic fatty liver disease or for modulating a metabolic marker or nonalcoholic fatty liver disease marker.