| Description: |
Agrimonolide is a potential α1 adrenergic receptor antagonist, it exerts anti-inflammatory activity, at least in part, via suppressing LPS-induced activation of JAK-STATs and p38 MAPKs signaling pathway. Agrimonolide and desmethylagrimonolide can effectively increase insulin-mediated glycogen level in heptocytes, they may play an important role in regulating glucose metabolism in insulin-resistance HepG2 cells and could be developed as a promising natural material for diabetes prevention and treatment. |
| Targets: |
TNF-α | NO | NOS | COX | JNK | p38MAPK | JAK | STAT | NF-kB | IL Receptor | Adrenergic Receptor |
| In vitro: |
| Food Funct. 2016 Oct 12;7(10):4400-4409. | | The potential beneficial effects of phenolic compounds isolated from A. pilosa Ledeb on insulin-resistant hepatic HepG2 cells.[Pubmed: 27704066 ] | The present study aims at investigating the effect of bioactive compounds isolated from AP on the improvement of insulin resistance, figuring out the mechanism in insulin-responsive cell lines.
METHODS AND RESULTS:
Five compounds were isolated from AP using column chromatography, including Agrimonolide (K1), desmethylAgrimonolide (K2), tormentic acid (K3), ursolic acid (K4), and quercetin (K5). Glucose metabolism was evaluated in insulin-resistant HepG2 cells. Ursolic acid had the strongest activity among all isolated compounds with the lowering value of 71.5% (1.24 mM glucose in DMEM) and 71.7% (1.23 mM) when compared to the control. K1 consisting of K2 effectively increased the insulin-mediated glycogen level in hepatocytes. At a concentration level of 20 μM, K2 significantly elevated the hepatic glucokinase (GK) activity (3.2 U min-1 mg-1 protein), followed by K1 (3.0 U min-1 mg-1 protein). Both of them significantly increased (p < 0.05) the GK activity as compared to the control. On the same lines, K2 and K1 caused a significant reduction of the glucose-6-phosphatase (G6Pase) activity and a significant change in the phosphoenolpyruvate carboxykinase (PEPCK) activity.
CONCLUSIONS:
In summary, bioactive compounds in AP may play an important role in regulating the glucose metabolism in insulin-resistant HepG2 cells and could be developed as a promising natural material for diabetes prevention and treatment. |
|
| In vivo: |
| Anal. Methods., 2012, 4(10):3351-7. | | Screening active components acting on α1A adrenergic receptors from agrimony using a Sprague-Dawley rat prostate cell membrane chromatography online coupled HPLC/MS method[Reference: WebLink] |
Agrimony is a traditional Chinese medicine and a herb of Agrimonia pilosa Ledeb belonging to the Rosaceae family. Many pharmacological effects of agrimony have been demonstrated in previous studies. Few studies have screened the active compounds in this complex product for chronic prostatitis.
METHODS AND RESULTS:
In this study, a two dimensional online method was established. A Sprague-Dawley (SD) rat prostate CMC-online-HPLC/MS method was used to screen, analyze, and identify active compounds acting on α1 adrenergic receptor from agrimony. Via this online method Agrimonolide was screened, analyzed, and identified as the active compound acting on α1 adrenergic receptor.
CONCLUSIONS:
Thus, Agrimonolide is a potential α1 adrenergic receptor antagonist and requires further study. |
|
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