| Description: |
Corosolic acid has antitumor, anti-inflammatory and hypoglycemic activities, it can ameliorate hypertension, abnormal lipid metabolism, and oxidative stress as well as the inflammatory state in SHR-cp rats; it can improve glucose metabolism by reducing insulin resistance, it inhibits the enzymatic activities of several diabetes-related non-receptor protein tyrosine phosphatases (PTPs) in vitro, such as PTP1B, T-cell-PTP, src homology phosphatase-1 and src homology phosphatase-2. Corosolic acid can suppress the M2 polarization of macrophages and tumor cell proliferation by inhibiting both STAT3 and NF-κB activation, it also can enhance the antitumor effects of adriamycin and cisplatin in in vitro. |
| Targets: |
FAK | ERK | Caspase | PARP | VEGFR | Src | Bcl-2/Bax | NF-κB | STAT | PTPs |
| In vitro: |
| Nat Prod Res. 2014;28(21):1879-86. | | Microbial transformation of the anti-diabetic agent corosolic acid.[Pubmed: 25190540] |
METHODS AND RESULTS:
Biotransformation of corosolic acid (1) by Cochliobolus lunatus and Streptomyces asparaginoviolaceus afforded four metabolites, which were identified by using (1)H NMR, (13)C NMR, DEPT, HSQC, HMBC and NOESY spectral data. Biotransformation of corosolic acid by C. lunatus R.R. Nelson & Haasis CGMCC 3.4381 produced three metabolites: 2α,3β,21β-trihydroxyurs-12-en-28-oic acid (2), 2α,3β,7β,21β-tetrahydroxy-urs-12-en-28-oic acid (3) and 2α,3β-dihydroxy-21-oxours-12-en-28-oic acid (4). Incubation of corosolic acid with growing cultures of S. asparaginoviolaceus CGMCC 4.0175 afforded metabolite 2α,3β,30-trihydroxyurs-12-en-28-oic acid (5). All the metabolites were reported for the first time.
CONCLUSIONS:
The substrate and four metabolites, along with four products obtained previously, were evaluated for their inhibitory effects on α-glucosidase; all the triterpenes tested showed potent inhibitory effects. |
|
| In vivo: |
| Phytother Res. 2015 May;29(5):714-23. | | Corosolic Acid Exhibits Anti-angiogenic and Anti-lymphangiogenic Effects on In Vitro Endothelial Cells and on an In Vivo CT-26 Colon Carcinoma Animal Model.[Pubmed: 25644809] | We describe the anti-angiogenic and anti-lymphangiogenic effects of corosolic acid, a pentacyclic triterpenoid isolated from Cornus kousa Burg.
METHODS AND RESULTS:
A mouse colon carcinoma CT-26 animal model was employed to determine the in vivo anti-angiogenic and anti-lymphangiogenic effects of corosolic acid. Corosolic acid induced apoptosis in CT-26 cells, mediated by the activation of caspase-3. In addition, it reduced the final tumor volume and the blood and lymphatic vessel densities of tumors, indicating that it suppresses in vivo angiogenesis and lymphangiogenesis. Corosolic acid inhibited the proliferation and tube formation of human umbilical vein endothelial cells and human dermal lymphatic microvascular endothelial cells. In addition, corosolic acid decreased the proliferation and migration of human umbilical vein endothelial cells stimulated by angiopoietin-1.
CONCLUSIONS:
Pretreatment with corosolic acid decreased the phosphorylation of focal adhesion kinase (FAK) and ERK1/2, suggesting that corosolic acid contains anti-angiogenic activity that can suppress FAK signaling induced by angiopoietin-1. |
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