Ecliptasaponin A
(Synonyms: 早莲苷 A) 目录号 : GC35960Ecliptasaponin A, a natural triterpenoid glucoside, has protective effects against the pulmonary fibrosis induced by bleomycin via reducing the oxidative stress, lung tissue inflammation, and the subsequent epithelial-mesenchymal transition.
Cas No.:78285-90-2
Sample solution is provided at 25 µL, 10mM.
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Ecliptasaponin A, a natural triterpenoid glucoside, has protective effects against the pulmonary fibrosis induced by bleomycin via reducing the oxidative stress, lung tissue inflammation, and the subsequent epithelial-mesenchymal transition.
Cas No. | 78285-90-2 | SDF | |
别名 | 早莲苷 A | ||
Canonical SMILES | CC1(C)[C@@H](O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O)CC[C@]3(C)[C@@]4([H])CC=C5[C@]6([H])CC(C)(C)CC[C@@](C(O)=O)6[C@H](O)C[C@](C)5[C@@](C)4CC[C@@]13[H] | ||
分子式 | C36H58O9 | 分子量 | 634.84 |
溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.5752 mL | 7.876 mL | 15.752 mL |
5 mM | 0.315 mL | 1.5752 mL | 3.1504 mL |
10 mM | 0.1575 mL | 0.7876 mL | 1.5752 mL |
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Ecliptasaponin A induces apoptosis through the activation of ASK1/JNK pathway and autophagy in human lung cancer cells
Ann Transl Med 2019 Oct;7(20):539.PMID:31807521DOI:10.21037/atm.2019.10.07.
Background: Non-small cell lung cancer (NSCLC) is one of the causes of carcinomas mortality worldwide. Ecliptasaponin A (ES), a natural product extracted from the plant known as Eclipta prostrata, has been reported as an anti-cancer drug against various cancer cell lines. However, the exact mechanisms of ES have not yet been fully characterized. Methods: Numerous studies have been done to support that ES has a powerful inhibiting effect on the growth of cancers via the activation of apoptosis and autophagy. To explore the underlying mechanisms of anti-cancer and investigate the relationships of the apoptosis and autophagy, we used apoptosis signal-regulating kinase 1 (ASK1) inhibitor (GS-4997), c-Jun N-terminal kinase (JNK) inhibitor (SP600125), and autophagy inhibitor [chloroquine (CQ) and 3-methyladenine (3-MA)]. Results: ES could potently suppress cell viability and induces apoptotic cell death of human lung cancer cells H460 and H1975. ES activated apoptosis via ASK1/JNK pathway, GS-4997 and SP600125 can attenuated these effects. Furthermore, ES could triggered autophagy in lung cancer cell lines, and the autophagy inhibitor 3-MA and CQ reversed ES-induced apoptosis in H460 and H1975 cells. Furthermore, SP600125 can inhibit autophagy. Conclusions: This study showed that ES induces apoptosis in human lung cancer cells by triggering enhanced autophagy and ASK1/JNK pathway, which may thus be a promising agent against lung cancer.
Determination of Ecliptasaponin A in rat plasma and tissues by liquid chromatography-tandem mass spectrometry
Biomed Chromatogr 2016 Jun;30(6):846-51.PMID:26378987DOI:10.1002/bmc.3617.
A sensitive, rapid and specific high-performance liquid chromatography tandem mass spectrometry method (HPLC-MS/MS) was developed to determine Ecliptasaponin A in rat plasma and tissues after oral administration. Ginsenoside Rg1 was used as the internal standard (IS). The plasma and tissues samples were prepared by liquid-liquid extraction with ethyl acetate and separated on an Eclipse Plus C18 column (2.1 mm × 150 mm, 5 µm) at a flow rate of 0.4 mL/min using acetonitrile and water (containing 0.05% acetic acid) as the mobile phase. The tandem mass detection was carried out with eletrospray ionization in negative mode. Quantification was performed by using multiple reaction monitoring (MRM), which monitored the fragmentation of m/z 633.4→587.2 for Ecliptasaponin A and m/z 859.4→637.4 for the IS. The calibration curves obtained were linear in different matrices, and the lower limit of quantification (LLOQ) achieved was 0.5 ng/mL both for rat plasma and tissues. The intra- and inter-day precisions were below 15%. This method was successfully applied to pharmacokinetic study of Ecliptasaponin A in rat plasma and tissues after oral administration. Copyright © 2015 John Wiley & Sons, Ltd.
Inhibition of Osteoarthritis-Related Molecules by Isomucronulatol 7- O-β-d-glucoside and Ecliptasaponin A in IL-1β-Stimulated Chondrosarcoma Cell Model
Molecules 2018 Oct 29;23(11):2807.PMID:30380653DOI:10.3390/molecules23112807.
Osteoarthritis (OA) is the common form of arthritis and is characterized by disability and cartilage degradation. Although natural product extracts have been reported to have anti-osteoarthritic effects, the potential bioactivity of Ryupunghwan (RPH), a traditional Korean medicinal botanical formula that contains Astragalus membranaceus, Turnera diffusa, Achyranthes bidentata, Angelica gigas, Eclipta prostrata, Eucommia ulmoides, and Ilex paraguariensis, is not known well. Therefore, the inhibitory effects of single compounds isolated from RPH on the OA-related molecules were investigated using IL-1β-stimulated chondrosarcoma SW1353 (SW1353) cell model. Two bioactive compounds, isomucronulatol 7-O-β-d-glucoside (IMG) and Ecliptasaponin A (ES) were isolated and purified from RPH using column chromatography, and then the structures were analyzed using ESI-MS, ¹H-NMR, and 13C-NMR spectrum. The expression or amount of matrix metalloproteinase 13 (MMP13), COX1/2, TNF-α, IL-1β or p65 was determined by RT-PCR, Western blot, and enzyme-linked immunosorbent assay (ELISA). RPH pretreatment reduced the expression and amounts of MMP13, and the expression of collagen II, COX1/2, TNF-α, IL-1β or p65, which were increased in IL-1β-stimulated SW1353 cells. IMG reduced the expression of all OA-related molecules, but the observed inhibitory effect was less than that of RPH extract. The other single compound ES showed the reduced expression of all OA-related molecules, and the effect was stronger than that in IMG (approximately 100 fold). Combination pretreatment of both single components remarkably reduced the expression of MMP13, compared to each single component. These synergic effects may provide potential molecular modes of action for the anti-osteoarthritic effects of RPH observed in clinical and animal studies.
Preventive effects of Ecliptae Herba extract and its component, Ecliptasaponin A, on bleomycin-induced pulmonary fibrosis in mice
J Ethnopharmacol 2015 Dec 4;175:172-80.PMID:26385580DOI:10.1016/j.jep.2015.08.034.
Ethnopharmacological relevance: Ecliptae Herba, a nourishing traditional Chinese medicine, is also a folk medicine for the treatment of lung diseases. Aim of the study: To investigate the anti-fibrosis effects and the underlying mechanism of the extract of Ecliptae Herba and its potential active components. Materials and methods: The resulting extract (EXT) was prepared from the 80% ethanol extract of Ecliptae Herba. After intratracheally administrated with bleomycin (BLM, 5mg/kg), mice were orally treated with EXT at 2.5, 1.25, 0.625 g/kg and eclipta saponin A (ESA) at 80 mg/kg once daily for 28 day. The bodyweight, survival rate, pathological changes of lung and levels of hydroxyproline (HYP) were used to evaluate the anti-fibrotic effects. The malonaldehyde (MDA), superoxidae dismutase (SOD) activity, and the protein expressions of matrix metalloproteinase (MMP)-2, 9, tissue inhibitor of metalloproteinase-1 (TIMP-1), cyclooxygenase-2 (COX-2), α-smooth muscle actin (α-SMA) and transforming growth factor-β1 (TGF-β1) in lung tissue were analyzed by kits or western blot. Results: Compared with BLM group, EXT administration could significantly ameliorated the pathological changes of lung, decreased the HYP content, enhanced the SOD activity, and reduced the MDA content of lung tissues. In mechanism, EXT significantly alleviated the levels of COX-2, TGF-β1, MMP-2 and α-SMA, as well as elevated the ratio value of MMP-9/TIMP-1. Additionally, the anti-fibrosis effects of ESA, a large amount of saponins isolated from Eclipta prostrata , was also evaluated by the BLM-induced model. The results showed that ESA could block BLM-induced histological changes of lung tissue and decrease the high levels of TGF-β1 and α-SMA. Conclusions: Ecliptae Herba has protective effects against the pulmonary fibrosis induced by BLM via reducing the oxidative stress, lung tissue inflammation, and the subsequent epithelial-mesenchymal transition. The active chemical constituents may be involved with triterpenoid saponins, such as ESA.
A Comprehensive Study on the Chemical Constituents and Pharmacokinetics of Erzhi Formula and Jiawei Erzhi Formula Based on Targeted and Untargeted LC-MS Analysis
Curr Drug Metab 2023;23(14):1130-1142.PMID:36718973DOI:10.2174/1389200224666230130093412.
Background: Erzhi formula (EZF) is a traditional Chinese medicine prescription, which has been widely used in the treatment of osteoporosis and premature ovarian failure. Objective: To enhance curative effects, the other two herbal medicines, including Spatholobi Caulis (SC) and Achyranthes bidentata Blume (ABB), were added into the original EZF formula to obtain two new Jiawei-EZF (JW-EZF) preparations. To clarify the effect of the compatibility of herbs for original formulas, the chemical constituents and bioactive compounds in vivo were detected. Methods: An efficient and sensitive targeted and untargeted UHPLC/ESI-Q-Orbitrap MS method, together with mass defect filter and precursor ion list, was established firstly for the profiling of different EZF formulas. Furthermore, eleven absorbed compounds (apigenin, luteoloside, luteolin, oleuropein, wedelolactone, acteoside, specnuezhenide, 11-methyloleoside, Ecliptasaponin A, formononetin, and β-ecdysone) were simultaneously quantified in rat plasma. Results: A total of 124, 162, and 177 compounds were identified or tentatively identified in EZF, JW-3-EZF (EZF+SC) and JW-4-EZF (EZF+SC+ABB), respectively. 110 compounds were found to be common constituents in the three formulas. Moreover, 66 prototypes were unambiguously identified in the rats' plasma after oral administration of the three formulas using the same strategy. 11 out of the 66 absorbed components were simultaneously quantitated in the pharmacokinetic (PK) study. Compared to the original EZF, the plasma AUC(0-24h) and AUC(0-∞) of apigenin, 11-methyloleoside, luteolin, luteoloside, wedelolactone, and acteoside were found to be significantly increased after oral administration of JW-3-EZF, and plasma AUC(0-24h) and AUC(0-∞) of apigenin, wedelolactone, and acteoside, were also found to be significantly increased after JW-4-EZF administration. Conclusion: The combined qualitative and quantitative methods were used to provide a potential approach to the characterization and quality control of the Traditional Chinese Medicine (TCM) and its preparations.