Discovery of the radio-protecting effect of Ecliptae Herba, its constituents and targeting p53-mediated apoptosis in vitro and in vivo

Radiation protection drugs are often accompanied by toxicity, even amifostine, which has been the dominant radio-protecting drug for nearly 30 years. Furthermore, there is no therapeutic drug for radiation-induced intestinal injury (RIII). This paper intends to find a safe and effective radio-protecting ingredient from natural sources. The radio-protecting effect of Ecliptae Herba (EHE) was discovered preliminarily by antioxidant experiments and the mouse survival rate after 137Cs irradiation. EHE components and blood substances in vivo were identified through UPLC‒Q-TOF. The correlation network of "natural components in EHE-constituents migrating to blood-targets-pathways" was established to predict the active components and pathways. The binding force between potential active components and targets was studied by molecular docking, and the mechanism was further analyzed by Western blotting, cellular thermal shift assay (CETSA), and ChIP. Additionally, the expression levels of Lgr5, Axin2, Ki67, lysozyme, caspase-3, caspase-8,8-OHdG, and p53 in the small intestine of mice were detected. It was found for the first time that EHE is active in radiation protection and that luteolin is the material basis of this protection. Luteolin is a promising candidate for RⅢ. Luteolin can inhibit the p53 signaling pathway and regulate the BAX/BCL2 ratio in the process of apoptosis. Luteolin could also regulate the expression of multitarget proteins related to the same cell cycle.

A new stigmasterol glucoside from aerial parts of Ecliptae Herba / 中草药

Objective: To investigate the bioactive chemical constituents of the aerial parts of Eclipta prostrata. Methods: The compounds were isolated and purified by macroporous absorption resin, silica gel, Sephadex LH-20 and semi-preparative HPLC chromatography. Their structures were determined by MS and NMR data. The α-glucosidase inhibitory activities of compounds 1 and 2 were tested by in vitro screening assay. Results: A total of eight compounds were isolated from the ethyl acetate partition of the ethanol extract of E. prostrata. They were identified as 7β-hydroxystigmasterol 3-O-β-D-glucopyranoside (1), 7α-hydroxystigmasterol 3-O-β-D-glucopyranoside (2), 7α-hydroxysitosterol 3-O-β-D-glucopyranoside (3), 3β,23-dihydroxy-30-norolean-12,20 (29)-dien-28- oic acid (4), camellenodiol (5), echinocystic acid-3-O-(6-O-acetyl)-β-D-glucopyranoside (6), eclalbasaponin I (7) and eclalbasaponin IV (8). Compound 2 exhibited strong inhibition against α-glucosidase with an IC50 value of (11.7 ± 4.2) μmol/L. Conclusion: Compound 1 is a new compound named eclalbasaponin XIV and compounds 3-5 are reported from this herb for the first time. Steroidal glycosides could be the anti-hyperglycaemic components in E. prostrata by inhibiting α-glucosidase.

Chemical constituents of Eclipta prostrata / 中草药

Objective To study their chemical components of Eclipta prostrata and identify their chemical structures. Methods The compounds were isolated by chromatography, purified by Sephadex LH-20 gel, identified by spectral analyses, and compared with the published data. Results Ten compounds were isolated and identified as 2, 2', 5″, 2″-terthiophene-5-carboxylic acid (Ⅰ), ?-sitosterol (Ⅱ), apigenin (Ⅲ), quercetin (Ⅳ), luteolin (Ⅴ), wedelolactone (Ⅵ), demethyl wedelolactone (Ⅶ), ecliptasaponin C (Ⅷ), luteoloside (Ⅸ), and linarin (Ⅹ). Conclusion Compound Ⅰ is a new compound from nature and compound Ⅹ is obtained from E. prostrata for the first time.

Genetic transformation of Eclipta prostrata by Ri T-DNA / 中草药

Object To establish the culture system of hairy root of Eclipta prostrata (L.) L.. Methods Hairy root of E. prostrata was obtained from infected cotyledon explants after infection with Agrobacterium rhizogenes strains A4, R1601 and ATCC15834, elite strains were screened and growth curves determined. The transformation of Ri T DNA was examined through high voltage paper electrophoresis. Results The hairy root was originally obtained from E.prostrata. The result of high voltage paper elctrophoresis confirmed the transformation of T DNA from Ri plasmid to the hairy root. Conclusion The acquisition of hairy root of E. prostrata provided further a foundation for the industrial production of active drug component.