Agrimonolide

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.

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.

Phytomedicine. 2016 Jul 15;23(8):846-55.

Agrimonolide from Agrimonia pilosa suppresses inflammatory responses through down-regulation of COX-2/iNOS and inactivation of NF-κB in lipopolysaccharide-stimulated macrophages.[Pubmed: 27288920 ]

Agrimonolide from Agrimonia pilosa showed a strong anti-inflammatory activity, and the present study aims to reveal potential mechanisms on molecular level explaining its anti-inflammatory effect.To investigate the mechanism of anti-inflammatory activity of Agrimonolide. Anti-inflammatory activity of Agrimonolide in cells was applied.
METHODS AND RESULTS:
Anti-inflammatory activity of Agrimonolide isolated from Agrimonia pilosa was evaluated using lipopolysaccharide (LPS) stimulated RAW 264.7 cell models. The productions of IL-1β, IL-6, TNF-α and NO were determined by ELISA and nitrite analysis, respectively. The expressions of iNOS and COX-2 were measured by western blotting and RT-PCR analysis. The pre-treatment with Agrimonolide significantly reduced the levels of pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α), as well as attenuated the expression of iNOS and COX-2 in LPS-stimulated macrophages. Furthermore, Agrimonolide inhibited the activation of JNK and p38 MAPKs and decreased the activation of JAK-STAT and NF-κB in LPS-stimulated macrophages.
CONCLUSIONS:
The present study suggested that Agrimonolide exerted anti- inflammatory activity, at least in part, via suppressing LPS-induced activation of JAK-STATs and p38 MAPKs signaling pathway.

J Sep Sci. 2012 Aug;35(15):1977-84.

Preparative purification of five bioactive components from Agrimonia pilosa Ledeb by high-speed counter-current chromatography.[Pubmed: 22865760]

METHODS AND RESULTS:
High-speed counter-current chromatography (HSCCC) coupled with ultraviolet (UV) detection or evaporative light-scattering detection was successfully applied for preparative separation of five bioactive compounds from Agrimonia pilosa Ledeb. In preliminary process, D101 macroporous resin was used to separate the crude extract of the plant and four fractions (20, 40, 50, and 60% aqueous ethanol elutions) were produced. Then, these fractions were directly subjected to HSCCC purification. Five chemicals including taxifolin-3-glucoside (6.4 mg), quercetin-3-rhamnoside (13.0 mg), tiliroside (14.7 mg), Agrimonolide (21.4 mg), and tormentic acid (29.8 mg) with the purities of 94.24, 95.37, 97.42, 95.29, and 96.34% were separated from each 200 mg prepared fraction. The purities were analyzed by high-performance liquid chromatography, and the chemical structures of the products were identified by UV detection, mass spectrometry, nuclear magnetic resonance, and the standards.
CONCLUSIONS:
This paper used a simple method to separate five bioactive compounds from A. pilosa Ledeb, and it could provide a new idea for the purification of bioactive compounds from other medicinal plants.