131436-22-1 Usage
Description
Cercosporamide is a potent broad-spectrum antifungal agent belonging to the class of dibenzofurans. It is a natural product isolated from the fungus Cercosporidium henningsii, which infects the leaves of cassava plants. Cercosporamide exhibits antiproliferative and proapoptotic activities in cancer cells in vitro and is known for its potent and selective inhibition of Pkc1 kinase, which plays a central role in cell wall biosynthesis.
Uses
Used in Pharmaceutical Industry:
Cercosporamide is used as an antifungal agent for its potent and selective inhibition of fungal PKC-like 1 kinases (Pkc1), which are essential for maintaining cell wall integrity. It has demonstrated an IC50 of 25 nM for Candida Pkc1, making it a promising candidate for treating fungal infections.
Used in Cancer Research:
Cercosporamide is used as an inhibitor of MAP-kinase interacting kinase-2 (Mnk2) and JAK3, effectively inhibiting eIF4E phosphorylation and Pkc1. This leads to antiproliferative and proapoptotic effects in cancer cells, making it a potential therapeutic agent for cancer treatment.
Used in Agriculture:
Originally identified as a host-selective phytotoxin, Cercosporamide has broad-spectrum antifungal properties. It can be used in the agricultural industry to protect crops from fungal infections, thereby increasing crop yield and quality.
Used in Hyperglycemia Treatment:
Cercosporamide has been shown to lower plasma glucose levels in hyperglycemic mice, making it a potential candidate for the development of treatments for hyperglycemia and related conditions.
Used in Drug Delivery Systems:
Cercosporamide's oral bioavailability and potent inhibition of MAPK-interacting kinases Mnk1 and Mnk2 suggest its potential use in drug delivery systems. These systems could be developed to enhance the delivery, bioavailability, and therapeutic outcomes of Cercosporamide in various applications, including cancer treatment and antifungal therapies.
Biochem/physiol Actions
Cercosporamide was initially identified as a phytotoxin with broad-spectrum anti-fungal activity. Studies have shown that cercosporamide is a specific, highly potent fungal inhibitor of the cell wall integrity-signaling pathway mediator, protein kinase (Pkc1) inhibitor. Semisynthetic cercosporamide analogues demonstrated hypoglycemic activity and therefore, serve as candidates for potential new anti diabetic drugs. Cercosporamide was found to block eIF4E (Eukaryotic Initiation Factor) phosphorylation in cultured cancer cells, inducing apoptosis, suppressing proliferation, and reducing soft agar colonization. Its eIF4E phosphorylation inhibitory effect was also shown when administrated orally on xenograft human tissue and mouse liver tissue. Cercosporamide is a potent and selective Mnk inhibitor. It reduces tumor growth in xenografted HCT116 tumor and suppresses the outgrowth of B16 melanoma lung metastases. Hence, blocking Mnk function and eIF4E phosphorylation may be an attractive anticancer strategy.
Check Digit Verification of cas no
The CAS Registry Mumber 131436-22-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,1,4,3 and 6 respectively; the second part has 2 digits, 2 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 131436-22:
(8*1)+(7*3)+(6*1)+(5*4)+(4*3)+(3*6)+(2*2)+(1*2)=91
91 % 10 = 1
So 131436-22-1 is a valid CAS Registry Number.
InChI:InChI=1/C16H13NO7/c1-5(18)10-7(20)4-9-16(2,14(10)22)12-8(21)3-6(19)11(15(17)23)13(12)24-9/h3-4,19-21H,1-2H3,(H2,17,23)/t16-/m1/s1
