Search

Eclipta prostrata L. (EPL), a medicinal plant, is widely utilized in the central highlands of Vietnam. This study aims to assess the chemical profile and potential medical effects of an EPL extract rich in flavonoids. A total of 36 secondary metabolites were identified from the EPL extract through GC-MS and UHPLC-UV analysis. Among them, 15 volatile compounds and several phenolic and flavonoid chemicals, including salicylic acid, epicatechin gallate, isovitexin, and apigetrin, were reported in EPL extract for the first time. This herbal extract demonstrated moderate inhibition against α-amylase and α-glucosidase, and high anti-oxidant and anti-acetylcholinesterase activities (IC50 = 76.8 ± 0.8 μg/mL). These promising attributes can be likely attributed to the high levels of major compounds, including wedelolactone (1), chlorogenic acid (3), epicatechin gallate (6), salicylic acid (8), isovitexin (9), apigetrin (11), and myricetin (12). These findings align with the traditional use of EPL for enhancing memory and cognitive function, as well as its potential benefits in diabetes management. The results of the molecular docking study reveal that the major identified compounds (1, 6, 9, and 11) showed a more effective acetylcholinesterase inhibitory effect than berberine chloride, with good binding energy (DS values, −12.3 to −14.3 kcal/mol) and acceptable values of RMSD (1.02–1.67 Å). Additionally, almost all the identified major compounds exhibited good ADMET properties within the required limits. [ABSTRACT FROM AUTHOR]

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.

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. The RⅢ radio-protecting effect of Ecliptae Herba was studied in vitro and in vivo. Luteolin plays an important role in it through p53-mediated apoptosis pathway. [Display omitted] [ABSTRACT FROM AUTHOR]

Eclipta prostrata L. (EPL), a medicinal plant, is widely utilized in the central highlands of Vietnam. This study aims to assess the chemical profile and potential medical effects of an EPL extract rich in flavonoids. A total of 36 secondary metabolites were identified from the EPL extract through GC-MS and UHPLC-UV analysis. Among them, 15 volatile compounds and several phenolic and flavonoid chemicals, including salicylic acid, epicatechin gallate, isovitexin, and apigetrin, were reported in EPL extract for the first time. This herbal extract demonstrated moderate inhibition against α-amylase and α-glucosidase, and high anti-oxidant and anti-acetylcholinesterase activities (IC50 = 76.8 ± 0.8 μg/mL). These promising attributes can be likely attributed to the high levels of major compounds, including wedelolactone (1), chlorogenic acid (3), epicatechin gallate (6), salicylic acid (8), isovitexin (9), apigetrin (11), and myricetin (12). These findings align with the traditional use of EPL for enhancing memory and cognitive function, as well as its potential benefits in diabetes management. The results of the molecular docking study reveal that the major identified compounds (1, 6, 9, and 11) showed a more effective acetylcholinesterase inhibitory effect than berberine chloride, with good binding energy (DS values, −12.3 to −14.3 kcal/mol) and acceptable values of RMSD (1.02–1.67 Å). Additionally, almost all the identified major compounds exhibited good ADMET properties within the required limits.

Menopause leads to ovarian hormone loss, which causes symptoms such as weight gain, hot flashes, and depression. Exploring nutraceuticals is important for treating menopausal symptoms that extensively impact women’s quality of life. We hypothesized that a combination of Leonurus japonicus Houtt, Eclipta prostrata L., and Pueraria lobata Ohwi (LEPE) would alleviate menopausal symptoms in an ovariectomized menopausal rat model. Bilateral ovariectomy was performed and animals were assigned to five groups: (1) Sham, (2) Vehicle, (-) Control, (3) LEPE (100 mg/kg bw), (4) LEPE (200 mg/kg bw), and (5) Estradiol (3 μg/kg bw). LEPE was orally administered daily for 12 weeks. LEPE supplementation did not affect growth performance (body weight and feed intake) or body composition (lean mass and fat in tissue). LEPE did not cause deviations in aspartate aminotransferase, alanine aminotransferase, estradiol, and follicle-stimulating hormone levels, indicating no hepatotoxicity or endocrine disturbance. LEPE decreased type I collagen (CTX-1) but did not affect bone mineral density or osteocalcin. LEPE decreased tail temperature and increased rectal temperature, improving menopause-related vasomotor symptoms. Furthermore, LEPE ameliorated depression-related behavior, including in forced swimming and tail suspension tests. Thus, LEPE may improve menopausal symptoms by enhancing vasomotor symptoms and depression in an ovariectomized rat menopause model.

Excessive autophagy plays a crucial role in cigarette smoking extract (CSE)-induced inflammation response and oxidative damage of respiratory epithelial cells. The components from Eclipta prostrata L. (CCE) have been shown to be beneficial for CSE-induced epithelial cells injury. However, whether its protection on CSE-stress injury is related to its regulation on autophagy remains still unclear. In this study, CCE, containing mainly wedelolactone of 45.88% and demethylwedelolactone of 23.74%, could improve significantly 10%CSE-induced cell viability of normal human bronchial epithelial (NHBE) cells using CCK-8 kit. We revealed that CCE could remarkably increase autophagic factors Beclin-1, Atg5, ATF4 proteins expression levels and the transformation of LC3-I to LC3-II. Additionally, CCE up-regulated significantly p-p16 and p-p21 phosphorylation levels whereas down-regulated p-p53 in NHBE cells. The changes of typical autolysosom and representative autophagosome in the presence of CCE or/and autophagy inhibitor chloroquine (CQ) were also observed by transmission electron microscopy. These data demonstrated that CCE reduced CSE-induced autophagy flux activation in NHBE cells. The blockade of CCE on autophagy flux contributes to its protection against CSE-induced NHBE cells damage, and CCE is promising to be combination therapeutic molecules to excessive autophagic damage in respiratory diseases.

Excessive autophagy plays a crucial role in cigarette smoking extract (CSE)-induced inflammation response and oxidative damage of respiratory epithelial cells. The components from Eclipta prostrata L. (CCE) have been shown to be beneficial for CSE-induced epithelial cells injury. However, whether its protection on CSE-stress injury is related to its regulation on autophagy remains still unclear. In this study, CCE, containing mainly wedelolactone of 45.88% and demethylwedelolactone of 23.74%, could improve significantly 10%CSE-induced cell viability of normal human bronchial epithelial (NHBE) cells using CCK-8 kit. We revealed that CCE could remarkably increase autophagic factors Beclin-1, Atg5, ATF4 proteins expression levels and the transformation of LC3-I to LC3-II. Additionally, CCE up-regulated significantly p-p16 and p-p21 phosphorylation levels whereas down-regulated p-p53 in NHBE cells. The changes of typical autolysosom and representative autophagosome in the presence of CCE or/and autophagy inhibitor chloroquine (CQ) were also observed by transmission electron microscopy. These data demonstrated that CCE reduced CSEinduced autophagy flux activation in NHBE cells. The blockade of CCE on autophagy flux contributes to its protection against CSE-induced NHBE cells damage, and CCE is promising to be combination therapeutic molecules to excessive autophagic damage in respiratory diseases. [ABSTRACT FROM AUTHOR]

This work first showed that the skin anti-inflammatory activities of Eclipta prostrata L. (E. prostrata L.)n be increased through an ultrasonic extraction process at a frequency of 120 kHz with 70% ethanol at 40 °C for 6 h. The extract from the ultrasound extraction (UE) contained 378.6 mg/100 g of wedelolactone (a major bioactive substance in E. prostrata L.), compared with the 172.9 mg/100 g from a conventional extraction process with 70% ethanol at 80 °C for 12 h (EE). The UE showed less than 10% of low cytotoxicity against normal fibroblast cells, and also exhibited much higher antioxidant activities than that from the EE when treating with 0.3 mg/mL of the extracts. It was proved that the high antioxidant activities of the UE were closely correlated with the enhancement of skin anti-inflammatory activities by effectively suppressing the production of tumor necrosis factor-alpha and interleukin-6 from macrophages. The production of prostaglandin E2 from human skin cells was also greatly reduced, compared with the EE for all ranges of the treatments. These results strongly indicate that the various biological activities of E. prostrata L. can be improved by a simple ultrasound extraction process because of the high elution of bioactive substances even at a low temperature. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Eclipta prostrata L. (Asteraceae) has been prescribed for whole body nourishment and nervine tonic in Asia. However, the effects of E. prostrata in learning and memory have not been fully explored. Aim of the study To scientifically elucidate the effects of E. prostrata on cognitive functions, we examined whether E. prostrata could ameliorate a cholinergic blockade-induced memory impairment, and we also investigated the effects of E. prostrata on the synaptic plasticity in the hippocampus. Materials and methods Memory impairment was induced by scopolamine, a cholinergic muscarinic receptor antagonist. The anti-amnesic effects of the ethanolic extract of Eclipta prostrata L. (EEEP) were measured in mice by the passive avoidance, Y-maze and Morris water maze tasks. To test the effects of EEEP on synaptic plasticity, we measured long-term potentiation (LTP) in the hippocampus. We also studied several signaling molecules related to learning and memory, such as phosphorylated protein kinase B (Akt) or phosphorylated glycogen synthase kinase-3β (GSK-3β). Results In the passive avoidance task, EEEP (50 or 100 mg/kg, p.o.) significantly ameliorated the shortened step-through latency induced by scopolamine. EEEP (100 mg/kg, p.o.) also showed significant increase in alternation behavior during the Y-maze task. In the Morris water maze task, scopolamine-induced a decrease in both the swimming time within the target zone and the number of crossings where the platform had been placed were significantly reversed by EEEP (50 or 100 mg/kg, p.o.). Moreover, EEEP (100 μg/ml) significantly enhanced hippocampal LTP without affecting basal synaptic transmission. The administration of EEEP (100 mg/kg) increased the phosphorylation levels of Akt and GSK-3β in the hippocampal region. Conclusion These results suggest that EEEP has memory-ameliorating activity against scopolamine-induced cognitive impairment and facilitates LTP in the hippocampus. This could be, at least in part, mediated by the activation of the Akt-GSK-3β signaling pathway. [ABSTRACT FROM AUTHOR]

A simple and rapid method was developed using microwave-assisted extraction (MAE) combined with HPLC–DAD–ESI–MS/MS for the simultaneous extraction, identification, and quantification of phenolic compounds in Eclipta prostrata , a common herb and vegetable in China. The optimized parameters of MAE were: employing 50% ethanol as solvent, microwave power 400 W, temperature 70 °C, ratio of liquid/solid 30 mL/g and extraction time 2 min. Compared to conventional extraction methods, the optimized MAE can avoid the degradation of the phenolic compounds and simultaneously obtained the highest yields of all components faster with less consumption of solvent and energy. Six phenolic acids, six flavonoid glycosides and one coumarin were firstly identified. The phenolic compounds were quantified by HPLC–DAD with good linearity, precision, and accuracy. The extract obtained by MAE showed significant antioxidant activity. The proposed method provides a valuable and green analytical methodology for the investigation of phenolic components in natural plants. [ABSTRACT FROM AUTHOR]

Four structurally unique guanidine alkaloids ecliptamines A–D ( 1 – 4 ) and one known analog ( 5 ) were isolated from the aerial parts of Eclipta prostrata (Asteraceae). Their structures were elucidated on the basis of spectroscopic analyses and chemical methods. The inhibitory activities of 1 , 2 and 5 were assayed with respect to cyclooxygenase-1 (COX-1) and -2 (COX-2). Compound 5 showed moderate inhibitory activities against COX-1 and -2 with IC 50 values of 3.0 × 10 −3 M and 8.3 × 10 −4 M, respectively, whereas aspirin as a positive control displayed the IC 50 values of 4.2 × 10 −4 M (against COX-1) and 7.1 × 10 −4 M (against COX-2). [ABSTRACT FROM AUTHOR]

Atopic dermatitis (AD) is a kind of inflammation on the skin following with swollen, itchy, dryness and cracked skin. Though the exact cause of AD is unknown, there are evidence that people with AD have a compromised skin barrier along with inflammation. Eclipta prostrata Linné is a traditional herbal medicinal plant, has been used for the diabetes, obesity, jaundice, and inflammation. We supposed E. prostrata L. has an anti-inflammatory effect on the skin. We aimed to assess the effect of E. prostrata L. EtOH extract (EP) and elucidate the associated molecular mechanisms. The effect of EP and the molecular mechanisms were eluciated in house dust mite (HDM)-induced AD mice model and TNF-α/IFN-γ-stimulated HaCaT keratinocytes by histological analysis, enzyme-linked immunosorbent assay, quantitative real time polymerase chain reaction, and Western blot. The results revealed that EP improved the progression of AD symptoms, decreasing epidermis/dermis thickness, infiltrated immune cells, and restored the skin barrier dysfunction and imbalanced immune response. EP suppressed the expressions of T helper (Th)1, Th2, Th17 cytokines, phosphorylation of extracellular signal-regulated kinase/signal transducer and activator of transcription 1 in skin of HDM-induced AD mice as well as inhibition the translocation of nuclear factor-κB in HaCaT keratinocytes. Collectively, EP improved the allergic inflammation of the skin through recovery the skin barrier, and regulation the immune balance. These results suggest EP may have therapeutic potential as an anti-atopic agent. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: Eclipta prostrata L., (Asteraceae), is used in China for both food and medicine purposes. This research is concerned with the isolation and purification of phytochemical constituents from the aerial parts of E. prostrata, using gradient solvent fractionation, macroporous resin, silica gel, Sephadex LH-20 and ODS columns, and TLC analyses. Four fractions (water, 30% ethanol, 60% ethanol and 90% ethanol) were obtained. Four compounds, wedelolactone (I), eclalbasaponin I (II), luteolin (III) and luteolin-7-O-glucoside (IV) were purified and their structures were identified by the interpretation of spectroscopic analyses including MS, 1H and 13C NMR. Antitumor activities of extracts (total fraction), four fractions and the isolated compounds were assessed using hepatoma cell smmc-7721 as an in vitro assay system. The 30% ethanol fraction and eclalbasaponin I dose-dependently inhibited the proliferation of hepatoma cell smmc-7721 with IC50 values of 74.2399 and 111.1703μg/ml, respectively, more strongly compared with 5-fluorouracil positive control group with the IC50 value of 195.3131μg/ml. Antitumor activities of other fractions and compounds were lower than positive control. These results suggested that some specific compounds or extracts from E. prostrata are potential sources of natural anti-tumor materials and worthy of further study. [Copyright &y& Elsevier]

Field experiments were conducted at two Texas peanut growing locations to study weed control and peanut response to sulfentrazone. Sulfentrazone applied preemergence caused up to 96% peanut stunting when rated 4 weeks after planting. The severity of stunting increased as sulfentrazone rate increased. Eclipta control varied between 89 and 100% while Texas panicum control was never less than 73% regardless of rate. Yellow nutsedge control with sulfentrazone increased as the rate of sulfentrazone increased with control no higher than 81%. Purple nutsedge control varied from 83 to 100% and was not rate dependent. Peanut yields reflect the effect of sulfentrazone injury on plant growth and development as peanut yields decreased as sulfentrazone rate increased. [ABSTRACT FROM AUTHOR]

Field studies were conducted during the 1997 and 1998 growing seasons to evaluate diclosulam alone and in combination with ethalfluralin for Eclipta prostrata, Ipomoea lacunosa, Panicum texanum, and Cyperus esculentus control. Diclosulam alone or in combination with ethalfluralin-applied preplant incorporated (PPI), preemergence (PRE), or postemergence (POST) at 0.009 to 0.024 kg ai/ha provided at least 93% season-long Eclipta control. Ethalfluralin, in combination with diclosulam-applied PPI at 0.016 or 0.024 kg ai/ha controlled C. esculentus at least 82% season-long. Ethalfluralin followed by diclosulam-applied POST at 0.016 or 0.024 kg/ha controlled at least 90% Ipomoea season long, while ethalfluralin followed by diclosulam-applied PPI or PRE at 0.024 kg/ha controlled 81%. Ethalfluralin in combination with diclosulam at 0.016 kg/ha or ethalfluralin followed by diclosulam at 0.016 or 0.024 kg/ha applied POST controlled greater than 80% P. texanum throughout the growing season. Diclosulam offers more effective Eclipta control than the commerical standards now being used. [Copyright &y& Elsevier]

Menopause leads to ovarian hormone loss, which causes symptoms such as weight gain, hot flashes, and depression. Exploring nutraceuticals is important for treating menopausal symptoms that extensively impact women's quality of life. We hypothesized that a combination of Leonurus japonicus Houtt, Eclipta prostrata L., and Pueraria lobata Ohwi (LEPE) would alleviate menopausal symptoms in an ovariectomized menopausal rat model. Bilateral ovariectomy was performed and animals were assigned to five groups: (1) Sham, (2) Vehicle, (-) Control, (3) LEPE (100 mg/kg bw), (4) LEPE (200 mg/kg bw), and (5) Estradiol (3 μg/kg bw). LEPE was orally administered daily for 12 weeks. LEPE supplementation did not affect growth performance (body weight and feed intake) or body composition (lean mass and fat in tissue). LEPE did not cause deviations in aspartate aminotransferase, alanine aminotransferase, estradiol, and follicle-stimulating hormone levels, indicating no hepatotoxicity or endocrine disturbance. LEPE decreased type I collagen (CTX-1) but did not affect bone mineral density or osteocalcin. LEPE decreased tail temperature and increased rectal temperature, improving menopause-related vasomotor symptoms. Furthermore, LEPE ameliorated depression-related behavior, including in forced swimming and tail suspension tests. Thus, LEPE may improve menopausal symptoms by enhancing vasomotor symptoms and depression in an ovariectomized rat menopause model. [ABSTRACT FROM AUTHOR]

The white-flowered leaves of Eclipta prostrata L. together with leaves of Scoparia dulcis and Cynodon dactylon are mixedly boiled in water and given to diabetic patients resulting in the significant improvement in the management of diabetes. However, the active constituents from this plant for antidiabetic and anti-obesity properties are remaining unclear. Thus, this study was to discover anti-diabetes and anti-obesity activities through protein tyrosine phosphatases (PTP)1B inhibitory effects. We found that the fatty acids (23, 24) showed potent PTP1B inhibition with IC 50 values of 2.14 and 3.21 µM, respectively. Triterpenoid-glycosides (12-15) also exhibited strong to moderate PTP1B inhibitory effects, with IC 50 values ranging from 10.88 to 53.35 µM. Additionally, active compounds were investigated for their PTP1B inhibitory mechanism and docking analysis. On the other hand, the anti-inflammatory activity from our study revealed that compounds (1-4, 7, 8, 10) displayed the significant inhibition nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Especially, compound 9 showed the potent inhibitory effects in LPS-induced NO production on RAW264.7 cell. Therefore, further Western blot analysis was performed to identify the inhibitory expression including heme oxygenase-1 (HO-1) and inhibitor of kappaB (IκB) phosphorylation.