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Environmental exposure of N-nitroso compounds (NOCs) from various sources like tobacco smoke, pesticides, smoked meat, and rubber manufacturing industries has been an alarming cause of carcinogenesis. Neonatal exposure to the carcinogenic N-N'ethylnitrosourea (ENU), a NOC has been established to cause leukemogenesis. Our world is constantly battling against cancer with consistent investigations of new anti-cancer therapeutics. Plant derived compounds have grasped worldwide attention of researchers for their promising anti-cancer potentials. Eclipta prostrata is one such ayurvedic herb, renowned for its anti-inflammatory properties. Currently, it has been explored in various cancer cell lines to establish its anti-cancer effect, but rarely in in-vivo cancer models. Wedelolactone (WDL), the major coumestan of E. prostrata is recognized as an inhibitor of IKK, a master regulator of the NF-kB inflammatory pathway. As persistent inflammation and activated inflammasome contribute to leukemogenesis, we tried to observe anti-leukemogenic efficacy of E. prostrata and its active compound WDL on the marrow cells of ENU induced experimental leukemic mice. Treatment groups were administered an oral gavage at a dose of 1200 mg/kg and 50 mg/kg b.w of crude extract and WDL respectively for 4 weeks. Various parameters like hemogram, survivability, cytological and histological investigations, migration assay, cell culture, flowcytometry and confocal microscopy were taken into consideration pre- and post-treatment. Interestingly, the plant concoction portrayed maximum effects in comparison to WDL alone. The study suggests E. prostrata and WDL as vital complementary adjuncts for anti-inflammasome mechanism in ENU-induced leukemia.

Objective: This research focused on the design of fast dissolving herbal film of Eclipta Prostrate leaves extract for mouth ulcers. Methods: The extract of Eclipta Prostrata leaves was formulated as films by solvent casting method using various polymers viz., HPMC E5, HPMC E15, sodium alginate and PVA. The films were designed by using propylene glycol as a plasticizer, SSG as super disintegrate and honey as a sweetener. Furthermore, the films were evaluated for thickness, folding endurance, weight variation, % elongation, surface pH, % moisture uptake, % moisture loss, disintegration and in vitro drug release study. Results: The revealed that all the films were good in appearance and had a smooth texture. Out of all ten formulations, F3 and F5 disintegrated rapidly with a disintegration time of 27 and 32 seconds. The drug release studies revealed that all the formulations had a good release profile, but the F3 formulation showed rapid release i.e. 83.57% in 4 min. The stability studies revealed that the formulations F3 and F5 were found good with non-tackiness, easily separable and disintegrated at 29 and 33 sec respectively with no appearance and drug release. Conclusion: The research revealed that Eclipta prostrate leaves extract can be formulated into oral films for the treatment of mouth ulcers with improved bioavailability and expected patient compliance.

Pathogenesis of Parkinson's disease (PD) specifically involves the degeneration of dopaminergic neurons in the substantia nigra region, which mainly begun with the overwhelmed oxidative stress and neuroinflammation. Considering the antioxidant and other pharmacological properties, Eclipta alba needs to be exploited for its possible neuroprotective efficacy against PD and other neurological disorders. Therefore, the current study was conducted to exemplify the remedial effects of hydro-alcoholic extract of E. alba (EA-MEx) against MPP+-elicited in vitro and in vivo PD models. SH-SY5Y, a neuroblastoma cell culture and male Wistar rats were used to impersonate the hallmarks of PD. Qualitative and quantitative analyses of EA-MEx revealed the presence of quercetin, ellagic acid, catechin, kaempferol, and epicatechin at varying concentrations. EA-MEx was found to deliver considerable protection against MPP+-induced oxidative damages in SH-SY5Y cells. Furthermore, in vivo study also supported the neuroprotective efficacy of EA-MEx, with significant mitigation of behavioral deficits induced by intrastriatal injection of MPP+. Furthermore, the disturbed levels of cellular antioxidant machinery have been significantly improved with the pre-treatment of EA-MEx. Mechanistically, the expression of α-synuclein, tyrosine hydroxylase, and mortalin were also found to be improved with the prior treatment of EA-MEx. Hence, the study suggests Eclipta alba as a suitable candidate for the development of better neuropathological therapeutics.

Purpose. Traditional Chinese medicine (TCM) has been extensively studied for its preventive and treatment properties toward osteoporosis (OP). Pharmacological studies have shown that TCM Eclipta prostrata induce anti-OP effects. Considering the growing evidence demonstrating that gut microbiota (GM) is related to OP, we aimed to study the GM-dependent function and mechanism of E. prostrata for preventing OP in mice. Methodology. Bone micro-structure was obtained using micro-computed tomography (micro-CT) and bone-relating factors were detected by molecular biological test. High-throughput sequencing of the 16S rRNA V4 region was performed for GM diversity analysis. Growth effects of E. prostrata on potential targeted strains Lactobacillus and Lactococcus were investigated by in vitro bacterial assay. By feeding Lactobacillus and Lactococcus in mice, GM and bone condition were analysed. Results. Bone micro-structure was significantly improved by E. prostrata with a potential mechanism of inhibiting osteoclast, increasing the number of osteoblasts and regulating the dynamic balance of bone absorption and formation. Sequencing results indicated that E. prostrata altered the bacterial community. The abundance of bacteria genera Lactobacillus and Lactococcus was markedly decreased in individuals with OP and positively correlated with high dose of E. prostrata. GM of the low-dose E. prostrata-fed group did not significantly differ from that of the chow-fed OP group, which was consistent with bone structure test results. Moreover, E. prostrata could promote Lactobacillus and Lactococcus growth in vitro. GM was altered and bone condition was improved via bacterial feeding in vivo. Conclusion. Our findings suggested that E. prostrata might be a novel therapy for OP prevention by targeting GM.

Eclipta prostrata has long been used as a medicinal herb in China. EAP20-1, a homogeneous polysaccharide with anti-complementary activity had been obtained from E. prostrate by using anion-exchange and size-exclusion chromatography. In this study, we found that EAP20-1 could inhibit in vitro lymphocyte proliferation stimulated by concanavalin–A or anti-CD3/anti-CD28 antibodies. Furthermore, in experimental autoimmune encephalomyelitis (EAE) mice, EAP20-1 treatment relieved the clinical symptoms, accompanied by reduced neuroinflammation and demyelination in spinal cords. Mechanistically, EAP20-1 reduced the mRNA expression of interleukin (IL)-17, IL-22, and RAR-related orphan receptor gamma t (RORγt) in the spleen; inhibited auto-reactive T cell proliferation and decreased the percentage of Th17 cells in response to myelin oligodendrocyte glycoprotein (MOG35-55) ex vivo. Moreover, EAP20-1 directly inhibited naive CD4 + T cells differentiate into Th17 cells in vitro. These results indicating EAP20-1 could benefit EAE through inhibiting Th17 cell differentiation and suggesting a therapeutic potential of EAP20-1 in MS.

Erzhi formula (EZF) consists of Ecliptae herba (EH) and Fructus Ligustri Lucidi (FLL) at a ratio 1:1, and constitutes a well-known formula in China that is commonly used for treating menopausal diseases.In this study, we explored the pharmacologic actions and potential molecular mechanisms underlying EZF's action in preventing and treating osteoporosis.The active components and related targets of EZF's anti-osteoporotic effects were predicted by network pharmacology, and functional enrichment analysis was also performed. We then used an osteoporosis model of ovariectomized (OVX) mice to detect the effects of EZF on osteoporosis.The results from network pharmacology identified a total of 10 active ingredients from EH and 13 active ingredients from FLL that might affect 65 potential therapeutic targets. GO enrichment analysis revealed that EZF affected bone tissue primarily via hormone (particularly estradiol)-related pathways and bone resorption by osteoclast differentiation. KEGG analysis demonstrated that bone-related factors such as Runt-related transcription factor 2 (Runx2), Ca2, estrogen receptor1 (ESR1), androgen receptors (AR), and TNFα served as the primary targets during osteoclastic differentiation. In vivo experiments showed that the formula significantly improved the diminution in estrogen and the subsequent uterine atrophy induced by ovariectomy (P 0.01 or 0.05), implying that the EZF exerted its actions via regulation of estradiol and the nourishing effects of the uterus in OVX mice. Dual-energy X-ray absorptiometry and micro-CT showed that EZF significantly inhibited bone loss and improved bone micro-architecture by statistically increasing the number of bone trabeculae and decreasing the separation of bone trabeculae in OVX mice (P 0.01 or 0.05); EZF also inhibited bone loss and enhanced bone-fracture load. Furthermore, we confirmed that EZF reduced the calcium concentrations, augmented protein and mRNA levels for Runx2 in the bone marrow, and reduced PPARγ levels. RANKL-a key downstream regulatory protein of many targets that was referred to in our results of network pharmacology as being involved in the regulation of osteoclastogenesis-was significantly diminished by EZF; it also elevated OPG content. In addition, we used monocytes of bone-marrow origin to detect the effects of the potential components of EZF on osteoclast differentiation and found that wedelolactone, oleanolic acid, echinocystic acid, luteolin, and luteolin-7-o-glucoside significantly inhibited osteoclast differentiation from monocytes induced by 25 ng/mL MCSF and 50 ng/mL RANKL (P 0.01 or 0.05).Our present study indicated that EZF significantly inhibited the bone loss induced by OVX in mice by its regulation of estradiol combined with the nourishing effect of the uterus, and that it also attenuated bone resorption by decreasing the RANKL/OPG ratio so as to inhibit osteoclast maturation.

BackgroundsColon cancer is the third most deadly and one of the most diagnosed diseases in the world. Although routine screening and early detection during last decades has improved the survival, colon cancer still claims hundreds of thousands lives each year worldwide. Surgery and chemotherapy is mainstay of current treatment, nevertheless toxicity associated with this treatment underscores the urgency of demand of a better therapeutics. Close to 50% of current chemotherapeutic drugs are direct or indirect descendants compounds isolated from medicinal plants, which indicate plants are great potential sources of novel therapeutics. In our literature review we foundEclipta albato posses many pharmacological activities, including those with anticancer potentials. However, no study on anticancer activity of this kind has been reported.MethodsPhytochemicals were extracted by maceration method from shade dried whole plant ofEclipta albausing methanol as a solvent. The anticancer effect of extract was investigated on various cancer cell lines like human colorectal carcinoma (HCT-116), human prostate cancer (PC-3), Michigan cancer foundation-breast cancer (MCF-7) and renal cell carcinoma (RCC-45). We have also studied the effects on normal human embryonic lung fibroblast cell (WI-38) using MTT (methyl thiazoldiphenyltetrazolium bromide) assay, clonogenic (colony formation) and migration assay. Finally obtained results were analyzed using ANNOVA and Dunnett’s test.ResultsResults obtained from MTT assay revealed that the methanolic extract ofEclipta albacarried significant (p ConclusionThis is a unique finding of its kind because the specific anticancer effect with minimal toxicity on normal cells has not been reported onEclipta albaextract. Finally this finding opens up a great possibility to develop a novel antitumor drug candidate against deadly colon cancer in the future.

Eclipta alba L., also known as false daisy, is well known and commercially attractive plant with excellent hepatotoxic and antidiabetic activities. Light is considered a key modulator in plant morphogenesis and survival by regulating important physiological cascades. Current study was carried out to investigate growth and developmental aspects of E. alba under differential effect of multispectral lights. In vitro derived callus culture of E. alba was exposed to multispectral monochromatic lights under controlled aseptic conditions. Maximum dry weight was recorded in culture grown under red light (11.2 g/L) whereas negative effect was observed under exposure of yellow light on callus growth (4.87 g/L). Furthermore, red light significantly enhanced phenolics and flavonoids content (TPC: 57.8 mg/g, TFC: 11.1 mg/g) in callus cultures compared to rest of lights. HPLC analysis further confirmed highest accumulation of four major compounds i.e. coumarin (1.26 mg/g), eclalbatin (5.00 mg/g), wedelolactone (32.54 mg/g) and demethylwedelolactone (23.67 mg/g) and two minor compounds (β-amyrin: 0.38 mg/g, luteolin: 0.39 mg/g) in red light treated culture whereas stigmasterol was found optimum (0.22 mg/g) under blue light. In vitro based biological activities including antioxidant, antidiabetic and lipase inhibitory assays showed optimum values in cultures exposed to red light, suggesting crucial role of these phytochemicals in the enhancement of the therapeutic potential of E. alba. These results clearly revealed that the use of multispectral lights in in vitro cultures could be an effective strategy for enhanced production of phytochemicals.

A swift increase has been observed in the number of individuals with metabolic syndrome worldwide. A number of natural compounds have been identified towards combating metabolic syndrome. Adding to this premise, here we report the pleiotropic activities of Ecliptal (EC); a natural compound isolated from the herb Eclipta alba. Administration of EC was shown to have prominent anti-adipogenic effects in 3T3-L1 and hMSC derived adipocytes. It was shown to activate Wnt-pathway and alter AKT signaling. Additionally, it caused cell cycle arrest and inhibited mitotic clonal expansion. EC treatment augmented mitochondrial biogenesis as well as function as estimated by expression of PGC1α, UCP-1, mitochondrial complexes and estimation of oxygen consumption rate. EC also reduced LPS-induced inflammation and tunicamycin induced ER stress. Further, EC enhanced insulin sensitivity by increasing AKT phosphorylation, inhibiting PKCα/βII phosphorylation and reducing leptin/adiponectin ratio. Finally, EC administration in Syrian golden hamsters was shown to have potent anti-dyslipidemic effects. Cumulatively, encompassing pleiotropic activities of EC, it could prove to be a potential drug candidate against obesity, insulin resistance and related metabolic syndrome.

Natural products have always fascinated mankind for their miraculous properties. Eclipta alba (E. alba), a medicinal herb has long been used in traditional medicine for curing several pathologies. It has been shown to have anti-diabetic effect as well as hepato-protective activity. Here, in order to address metabolic derangements, the study was designed to evaluate the efficacy of E. alba and its fractions in adipogenesis inhibition and dyslipidemia. Of the crude extract and fractions screened, ethyl acetate fraction of E. alba inhibited adipocyte differentiation in 3T3-L1 pre-adipocytes and hMSC derived adipocytes. It inhibited mitotic clonal expansion and caused cell cycle arrest in G1 and S phase as suggested by western blot analysis and flow cytometry. It was also shown to have lipolytic effects. Oral administration of ethyl acetate fraction of E. alba to hamsters unveiled its anti-adipogenic as well as anti-dyslipidemic activity in-vivo. Mass spectrometry analysis of ethyl acetate fraction confirmed the presence of several bioactive components, projecting it as an effective phytopharmaceutical agent. In conclusion, ethyl acetate fraction of E. alba possesses potent anti-adipogenic as well as anti-dyslipidemic activity and could be projected as an herbal formulation towards obesity.

Ovarian cancer is the most lethal gynecological malignancy worldwide. Thiophenes such as terthiophene have been shown to have anti-tumor effects on several cancer cell lines, including ovarian cancer cells. However, the underlying mechanisms behind the anti-proliferative effect of thiophenes are poorly understood. In this study, we investigated the molecular mechanisms underlying the anti-proliferative effect of α-terthienylmethanol, a terthiophene isolated from Eclipta prostrata (False Daisy), on human ovarian cancer cells. We found that α-terthienylmethanol is a more potent inhibitor of cell growth than is cisplatin in human ovarian cancer cells. α-Terthienylmethanol induces cell cycle arrest in ovarian cancer cells, as shown by the accumulation of cells in S phase. In addition, α-terthienylmethanol induced a change in S phase-related proteins cyclin A, cyclin-dependent kinase 2, and cyclin D2. Knockdown of cyclin A using specific siRNAs significantly compromised α-terthienylmethanol-induced S phase arrest. We further demonstrated that α-terthienylmethanol induced an increase in intracellular ROS, and the antioxidant N-acetyl-l-cysteine significantly reversed the S phase arrest induced by α-terthienylmethanol. Moreover, α-terthienylmethanol significantly increased the levels of p-H2AX, a DNA damage marker. These results suggest that α-terthienylmethanol inhibits the growth of human ovarian cancer cells by S phase cell cycle arrest via induction of ROS stress and DNA damage.

Ethnopharmacological relevance Polygoni multiflori radix praeparata (PMRP), Ecliptae herba (EH) and Rehmanniae radix praeparata (RRP) a re the most frequently-used herbs by Traditional Chinese Medicine practitioners for the treatment of vitiligo. Their abilities to stimulate melanogenesis, melanocyte migration and MITF (microphthalmia associated transcription factor) protein expression were evaluated in this study. Materials and methods The effects of aqueous extracts of PMRP, EH and RRP on human melanocytes in vitro were examined by MTT assay, tyrosinase activity, melanin synthesis, migration assay and Western blot. Results Treatment with EH (at 100 μg/ml and 400 μg/ml) significantly increased intracellular tyrosinase activity in accordance with the elevation of melanin content at the same concentrations. Treatment with RRP (at 100 μg/ml and 400 μg/ml) promoted melanin production but had no stimulatory effect on tyrosinase activity. Treatment with PMRP and EH (at 100 μg/ml) promoted the migration of human melanocytes in a type IV collagen-coated transwell migration assay. Western blot analysis showed MITF protein expression was elevated by PMRP, EH and RRP (at 100 μg/ml). Conclusion An aqueous extract of EH has a synergistic effect on melanocytes by up-regulating tyrosinase activity, enhancing melanin synthesis and promoting melanocyte migration as well as elevating MITF protein expression. RRP exhibits a significant stimulating effect on melanogenesis and MITF protein expression. These results suggest that EH and RRP contain substances with direct enhancing effects on melanogenesis and migration, possibly via their effects on MITF protein expression.

Eclipta, a traditional Chinese medicine, has been used to treat liver disease for centuries. However, the chemical basis and biological mechanisms of Eclipta remain elusive. The current study aims to investigate the hepatoprotective effect of wedelolactone (WEL), a major coumarin in Eclipta, using C57BL/6 mice with carbon tetrachloride CCl4-induced acute liver injury (ALI). Our data showed that WEL markedly decreased the CCl4-induced elevation of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, and improved hepatic histopathology changes. WEL also significantly decreased the content of MDA in liver tissues, meanwhile increased the activities of antioxidant enzymes SOD and GSH-Px. In addition, WEL reduced the protein expression of TNF-α, IL-1β and IL-6, as well as mRNA expression. Western blot results revealed that WEL repressed phosphorylation of extracellular signal-regulated kinase (ERK) and translocation of NF-κB p65 from cytoplasm to nucleus and enhanced the phosphorylation of c-Jun. N-terminal kinase (JNK). Moreover, results showed that WEL significantly inhibited CCl4-induced hepatocytes apoptosis, markedly suppressed the down-regulation of Bax and active Caspase-3 expression and accelerated the expression of Bcl-2. Overall, the findings indicate that WEL exhibits a protective effect against CCl4-induced ALI in mice by enhancing the antioxidative defense system, suppressing the inflammatory response and cell apoptosis of liver.

Background: The Plumbago zeylanica (family: Plumbaginaceae) is a widely accepted ethnomedicine around the world including India, Pakistan, Bangladesh, Sri Lanka, and Australia. Early in vitro researches of Plumbago zeylanica were focused on antioxidant activity in root only a few were concerned with stem. Similarly in Eclipta alba antioxidant activity of whole plant is explored. Objective: The present study highlights the comparative antioxidant potential and enzymatic contents of both plants along with recent updates on phytochemical contents. Materials and Methods: The antioxidant potential of the plants was established by DPPH free radical scavenging assay, Nitric oxide (NO) free radical scavenging activity, Hydrogen peroxide (H2O2) scavenging activity, Catalase activity along with determination of Total Phenolic Contents in the plant extracts. Results: The results revealed that Eclipta alba has notable activity than Plumbago zeylanica in quenching of DPPH while Plumbago zeylanica shows comparatively better activity in nitric oxide scavenging, super oxide scavenging and Catalase activity. The Eclipta at 10 μg/ml showed maximum scavenging of DPPH (16.60 %), nitric oxide (66.21%), super oxide (4.76%) and Catalase activity 31.9 at 1 mg/g fresh weight against the Plumbago zeylanica which showed maximum scavenging of DPPH 13.24%, Polyherbal extract 11.78%, nitricoxide (69.45%), super oxide (5.12%) and catalase activity 23.7 at 1 mg/g fresh weight respectively at the same concentration. The phytochemical screening of the extract revealed the presence of considerable amount of alkaloids, saponins, tannins, phenolic compounds and glycosides which might be responsible for the antioxidative potential of the selected plants. Conclusion: The results of this study strongly indicate that the Plumbago zeylanica has comparatively more potent antioxidant potential than Eclipta alba. Moreover, the study reveals that polyherbal extract for the very first time for this combination have shown a strong antioxidant activity which is directly correlated with suppression of free radical induced diseases i.e. cancer. These findings encourage studying these plants and their polyherb al extracts further as a potential agents against cancer.

A novel analytical method for neutral monosaccharide composition analysis of plant-derived oligo- and polysaccharides was developed using hydrophilic interaction liquid chromatography coupled to a charged aerosol detector. The effects of column type, additives, pH and column temperature on retention and separation were evaluated. Additionally, the method could distinguish potential impurities in samples, including chloride, sulfate and sodium, from sugars. The results of validation demonstrated that this method had good linearity (R(2) ≥ 0.9981), high precision (relative standard deviation ≤ 4.43%), and adequate accuracy (94.02-103.37% recovery) and sensitivity (detection limit: 15-40 ng). Finally, the monosaccharide compositions of the polysaccharide from Eclipta prostrasta L. and stachyose were successfully profiled through this method. This report represents the first time that all of these common monosaccharides could be well-separated and determined simultaneously by high performance liquid chromatography without additional derivatization. This newly developed method is convenient, efficient and reliable for monosaccharide analysis.

Ethnopharmacological relevance Lei-gong-gen formula granule (LFG) is a folk prescription derived from Zhuang nationality, the largest ethnic minority among the 56 nationalities in China. It is composed of three herbs, namely Centella asiatica (L.) Urb., Eclipta prostrata (L.) L., Smilax glabra Roxb. It has been widely used as health protection tea for many years to prevent cardiovascular and cerebrovascular diseases such as hyperlipidemia and hypertension. Aim of the study This study validated the lipid-lowering effect of LFG in a hyperlipidemia rat model. Then we employed network pharmacology and molecular biological approach to identify the active ingredients of LFG, corresponding targets, and its anti-hyperlipidemia mechanisms. Materials and methods Hyperlipidemia rat model was established by feeding male Sprague-Dawley rats with high-fat diet for two weeks. LFG (two doses of 10 and 20 g/kg) was administered orally to hyperlipidemia rat model for 4 weeks, twice per day. Serum levels of total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C) were monitored in rats pre and post-treatment. Hematoxylin-eosin staining was applied to observe the pathology and lipid accumulation of liver. We then performed network pharmacology analysis to predict the ingredients, their associated targets, and hyperlipidemia associated targets. Pathway analysis with significant genes was carried out using KEGG pathway. These genes and proteins intersectioned between compound targets and hyperlipidemia targets were further verified with samples from hyperlipidemia rats treated with LFG using Real-time RT-PCR and Western Blot. Results LFG attenuated hyperlipidemia in rat model, and this was characterized with decreased serum levels of TC, LDL-C, liver wet weight, and liver index. LFG alleviated the hepatic steatosis in hyperlipidemia rats. Network pharmacology analysis identified 53 bioactive ingredients from LFG formula (three herbs), which link to 765 potential targets. 53 hyperlipidemia associated genes were retrieved from public databases. There were 10 common genes between ingredients-targets and hyperlipidemia associated genes, which linked to 20 bioactive ingredients. Among these 10 genes, 3 of them were validated to be involved in LFG's anti-hyperlipidemia effect using Real-time RT-PCR, namely ADRB2 encoding beta-2 adrenergic receptor, NOS3 encoding nitric oxide synthase 3, LDLR encoding low-density lipoprotein receptor. The cGMP-PKG signaling pathway was enriched for hyperlipidemia after pharmacology network analysis with ADRB2, NOS3, and LDLR. Interestingly, expression of cGMP-dependent protein kinase (PKG) was downregulated in hyperlipidemia rat after LFG treatment. Molecular docking study further supported that ferulic acid, histidine, p-hydroxybenzoic acid, and linalool were potential active ingredients for LFG's anti-hyperlipidemia effect. LC-MS/MS analysis confirmed that ferulic acid and p-hydroxybenzoic acid were active ingredients of LFG. Conclusion LFG exhibited the lipid-lowering effect, which might be attributed to downregulating ADRB2 and NOS3, and upregulating LDLR through the cGMP-PKG signaling pathway in hyperlipidemia rat. Ferulic acid and p-hydroxybenzoic acid might be the underlying active ingredients which affect the potential targets for their anti-hyperlipidemia effect.

Ethnopharmacological relevance Eclipta prostrata, a traditional herbal medicine, has long been used in Asia and South America for the therapy of hemorrhagic diseases (e.g. hemoptysis, hematemesis, hematuria, epistaxis and uterine bleeding), skin diseases, respiratory disorders, coronary heart disease, hair loss, vitiligo, snake bite and those caused by the deficiency of liver and kidney. Aim of the review In this review, we highlight relatively comprehensive and up-to-date information of E. prostrata on traditional uses, phytochemistry, pharmacology and toxicity, along with featuring the gaps in current knowledge, aiming to provide references for future research and possible opportunities for well applications of this medicinal plant. Materials and methods Information on E. prostrata was gathered from scientific databases (Google Scholar, Web of Science, Scifinder, Baidu Scholar, PubMed and CNKI). Information was also obtained from local books, Ph.D. theses and M.Sc. dissertations and Chinese Pharmacopoeia. The plant taxonomy was validated by the database “The Plant List”. Results Various phytochemical classes has been identified and isolated from the plant covering triterpenes, flavonoids, thiopenes, coumestans, steroids and others. Among these, coumestans are reported as the most common ingredients. The isolated crude extracts and individual compounds have been reported to exhibit promising pharmacological properties, such as hepatoprotective, osteoprotective, cytotoxic, hypoglycaemic, anti-inflammatory, anti-microbial, hypolipidemic, promoting hair growth, rejuvenative and neuroprotective effects. Conclusions Until now, significant progress has been witnessed in phytochemistry and pharmacology of E. prostrata. Thus, some traditional uses has been well supported and clarified by modern pharmacological studies. Moreover, E. prostrata also showed therapeutic potential in some refractory diseases such as cancer, dementia and diabetes. But, present findings are still insufficient that cannot satisfactorily explain some mechanisms of action. More well-designed studies in vitro especially in vivo are required to establish links between the traditional uses and bioactivities, discover new skeletons and activity molecules, as well as ensure safety before clinical use.

Non-alcoholic fatty liver disease is a leading cause of chronic liver disease in western countries. The current study aimed to detect and evaluate lipidomic biomarkers for early detection of NAFLD as well as the potential efficiency of methanolic extract of Eclipta prostrata (E. prostrata) on disease management. In this study, Phytochemical screening of E. prostrata methanolic extract was performed using HPLC. NAFLD was induced in albino rats using a high-fat diet together with cholesterol and cholic acid. Comprehensive lipidomic analyses on sera from rats bearing NAFLD as well as normal healthy animals were carried out based on GC MS and multivariate data analysis. The results showed that high doses (300&200 mg/kg.BW) of E. prostrata extract exhibited significant improvement in liver enzymes (ALT & AST) and lipid profile [total cholesterol (TC), triacylglycerides (TAGs), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein-cholesterol (LDL-C)] in rats bearing NAFLD. Glycerol, linoleic acid, arachidonic acid and cholest-5-en-3-ol (3β) acetate were detected as lipidomic biomarkers for early detection of NAFLD in rats’ sera. Furthermore, E. prostrata extract showed a significant amelioration in the levels of these metabolic biomarkers in both protective and treated groups. These finding devoutly recommend using of lipidomic biomarkers for early detection of NAFLD and E. prostrata could be used as a protective agent as well as ameliorate this disease through its probable action on the fore-mentioned metabolites.

Eclipta prostrata L. is a traditional Chinese herbal medicine that has been used in the treatment of liver diseases. However, its biological mechanisms remain elusive. The current study aimed to investigate the hepatoprotective effect of wedelolactone, a major coumarin ingredient of Eclipta prostrata L., on immune-mediated liver injury. Using the well-established animal model of Concanavalin A (ConA)-induced hepatitis (CIH), we found that pretreatment of mice with wedelolactone markedly reduced both the serum levels of transaminases and the severity of liver damage. We further investigated the mechanisms of the protective effect of wedelolactone. In mice treated with wedelolactone prior to the induction of CIH, increases of serum concentrations of tumor necrosis factor (TNF)-[Formula: see text], interferon (IFN)-[Formula: see text], and interleukin (IL)-6 were dramatically attenuated. Additionally, expressions of the interferon-inducible chemokine (C-X-C motif) ligand 10 gene CXCL10 and intercellular adhesion molecule 1 gene ICAM1 were lower in livers of the treated mice. Moreover, wedelolactone-treated CIH mice exhibited reduced leukocyte infiltration and T-cell activation in liver. Furthermore, wedelolactone suppressed the activity of nuclear factor-kappa B (NF-[Formula: see text]B), a critical transcriptional factor of the above-mentioned inflammatory cytokines by limiting the phosphorylation of I kappa B alpha (I[Formula: see text]B[Formula: see text] and p65. In conclusion, these findings demonstrate the inhibitory potential of wedelolactone in immune-mediated liver injury in vivo, and show that this protection is associated with modulation of the NF-[Formula: see text]B signaling pathway.

Eclipta prostrata, a traditional Chinese medication, has been used for the treatment of several diseases. However, the molecular mechanism underlying the effects of Eclipta prostrata extracts (EPE) on human oral cancer cell metastasis remains unclear. We thus examined the effects of EPE on metastasis promoting proteins in oral cancer. Our results revealed that the EPE attenuated SCC-9, HSC-3, and TW2.6 cell migration and invasiveness by reducing matrix metalloproteinase (MMP)-2 enzyme activities. In addition, Western blot analysis revealed that EPE significantly reduced the levels of phosphorylated extracellular signal-regulated kinase 1/2 (ERK 1/2) but not those of c-Jun N-terminal kinase (JNK) 1/2 and p38. In conclusion, we found that EPE could inhibit oral cancer metastasis through the inhibition of MMP-2 expression. Therefore, EPE may be used to prevent the metastasis of oral cancer, and has the potential to be applied to cancer treatment.

Thiophenes are a class of heterocyclic aromatic compounds based on a five-membered ring made up of one sulfur and four carbon atoms. The thiophene nucleus is well established as an interesting moiety, with numerous applications in a variety of different research areas. Naturally occurring thiophenes are characteristic secondary metabolites derived from plants belonging to the family Asteraceae, such as Tagetes, Echinops, Artemisia, Balsamorhiza, Blumea, Pluchea, Porophyllum and Eclipta. Furthermore, naturally occurring thiophenes are generally composed of one to five thiophene rings that are coupled together through their α-carbons, and carry alkyl chains on their free ortho-positions. Thiophene-containing compounds possess a wide range of biological properties, such as antimicrobial, antiviral, HIV-1 protease inhibitor, antileishmanial, nematicidal, insecticidal, phototoxic and anticancer activities. This review focuses on naturally occurring thiophene derivatives; their sources, physical and spectral data, and biological activities.

Eclipta prostrata (Linn.) Linn. is a traditional Chinese medicine and has previously been reported to have hypolipidemic effects. However, its mechanism of action is not well understood. This study was conducted to identify the active fraction of Eclipta, its toxicity, its effect on hyperlipidemia, and its mechanism of action. The ethanol extract (EP) of Eclipta and fractions EPF1-EPF4, obtained by eluting with different concentrations of ethanol from a HPD-450 macroporous resin column chromatography of the EP, were screened in hyperlipidemic mice for lipid-lowering activity, and EPF3 was the most active fraction. The LD50 of EPF3 was undetectable because no mice died with administration of EPF3 at 10.4 g/kg. Then, 48 male hamsters were used and randomly assigned to normal chow diet, high-fat diet, high-fat diet with Xuezhikang (positive control) or EPF3 (75, 150 and 250 mg/kg) groups. We evaluated the effects of EPF3 on body weight gain, liver weight gain, serum lipid concentration, antioxidant enzyme activity, and the expression of genes involved in lipid metabolism in hyperlipidemic hamsters. The results showed that EPF3 significantly decreased body-weight gain and liver-weight gain and reduced the serum lipid levels in hyperlipidemic hamsters. EPF3 also increased the activities of antioxidant enzymes; up-regulated the mRNA expression of peroxisome proliferator-activated receptor α (PPARα), low density lipoprotein receptor (LDLR), lecithin-cholesterol transferase (LCAT) and scavenger receptor class B type Ι receptor (SR-BI); and down-regulated the mRNA expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGR) in the liver. These results indicate that EPF3 ameliorates hyperlipidemia, in part, by reducing oxidative stress and modulating the transcription of genes involved in lipid metabolism.

Complement-mediated inflammation and tissue damage is an important drive to pathology in autoimmune diseases, targeting inhibit the complement activation is promising treatment strategy for these diseases. We performed anticomplement activity-guided fractionation of the water extract of Eclipta prostrata by ion-exchange and size-exclusion chromatography, yielding two bioactive polysaccharides EAP20-1 and EAP20-2. The molecular weights of EAP20-1 and EAP20-2 were respectively calculated to be 5.2 kDa and 6.3 kDa by HPGPC, both polysaccharides was composed by d -Gal, l -Glc, and Ara at different ratios of 7.3:2.7:1 and 7.6:3.1:1. In addition, the main linkage types of EAP20-1 and EAP20-2 were β-1,4-Gal, β-1,6-Gal and α-1,4,6-Glc according to methylation analyses. EAP20-1 and EAP20-2 exhibited significant inhibitory effect on the complement activation through both classical and alternative pathways and with no influence on the coagulation system. Preliminary mechanism study indicated that both EAP20-1 and EAP20-2 inhibited the activation of the complement system by interacting with C1q, C1r, C1s, C2, C4, C5, C7, and C9 components.

Eclipta prostrata (EP) and its compounds are known to have several pharmacological effects including anti-inflammatory effects. In the present study, we demonstrated that EP improves the dextran sulfate sodium (DSS)-induced colitis symptoms such as body weight loss, colon length shortening and disease activity index. In DSS-induced colitis tissue, EP controls the protein expressions of cyclooxygenase-2 (COX-2) and hypoxia inducible factor-1[Formula: see text] (HIF-1[Formula: see text]). In addition, the release of prostaglandin E2and vascular endothelial growth factor-A were significantly reduced by EP administration. EP also inhibited COX-2 and HIF-1[Formula: see text] expressions in the tumor necrosis factor-[Formula: see text] stimulated HT-29 cells. These inhibitory effects of EP occurred by reducing the phosphorylation of I[Formula: see text]B and the translocation of the nuclear factor-[Formula: see text]B (NF-[Formula: see text]B). Additionally, we found through HPLC analysis that wedelolactone, which is an inhibitor of NF-[Formula: see text]B transcription, was contained in water extract of EP. These results indicate that EP can improve colitis symptoms through the modulation of immune function in intestinal epithelial cells and suggests that EP has the potential therapeutic effect to intestinal inflammation.

Eclipta prostrata belongs to a family of medicinal plants (Asteraceae) and plays a role in the treatment of several diseases, including infectious hepatitis, snake venom poisoning, gastritis, and respiratory diseases such as a cough and asthma. A number of compounds, including thiophene derivatives, steroids, triterpenes, flavonoids, polyacetylenes, polypeptides, and coumestans, have been isolated from E. prostrata. The plant functional compounds can act as reducing agent in the field of nanoparticle synthesis. The extracts of E. prostrata are widely used for green biosynthesis of various metal and metal oxide nanoparticles, nanoparticles, which showed a potential for pharmaceutical, biotechnological, and biomedical applications. Establishment of a efficient in vitro regeneration and genetic transformation method of E. prostrata is a vital prerequisite for application of biotechnology in order to improve secondary metabolite yields. The present mini-review discusses its pharmacological profile, chemical constituents, biotechnological, and ethnomedical uses, mainly focusing on antimyotoxic, antihemorrhagic, antiproliferative, antioxidant, antitumor, antihyperglycemic, antidementia, antimicrobial, antihyperlipidemic, antivenom, anti-HIV, and larvicidal activities, so that the pharmaceutical potential of the plant can be better evaluated. The mini review, providing up-to-date phytochemical and other information on E. prostrata, will serve a reference for further studies.

As per WHO estimates, 80% of people around the world use medicinal plants for the cure and prevention of various diseases including cancer owing to their easy availability and cost effectiveness.Eclipta albahas long been used in Ayurveda to treat liver diseases, eye ailments, and hair related disorders. The promising medicinal value ofE. albaprompted us to study the antioxidant, nontoxic, and anticancer potential of its alcoholic extract. In the current study, we evaluated thein vitrocytotoxic and antioxidant effect of the alcoholic extract ofEclipta alba(AEEA) in multiple cancer cell lines along with control. We have also evaluated its effect on differentin vivotoxicity parameters. Here, we found that AEEA was found to be most active in most of the cancer cell lines but it significantly induced apoptosis in human breast cancer cell lines by disrupting mitochondrial membrane potential and DNA damage. Moreover, AEEA treatment inhibited migration in both MCF 7 and MDA-MB-231 cells in a dose dependent manner. Further, AEEA possesses robustin vitroantioxidant activity along with high total phenolic and flavonoid contents. In summary, our results indicate thatEclipta albahas enormous potential in complementary and alternative medicine for the treatment of cancer.

The present study investigates the anticancer and multidrug resistance (MDR) reversal potential of hydro-alcoholic Eclipta alba extract (EAE) through in vivo experiments. Diethylnitrosamine (DEN) and 2-acetylaminofluorene (AAF) were used for liver cancer induction in animal model, whereas for MDR induction, AAF was used. The level of antioxidant enzymes was studied in serum along with biochemical parameters. Cancer and MDR-induced liver cells have higher levels of reactive oxygen species (ROS) and, in turn, are responsible for the maintenance of the cancer phenotype. Treatment with EAE declines the ROS level and revealed the ROS scavenging properties. Alfa feto protein levels were found to increase significantly in cancer-induced animals confirming induction and progression of liver cancer, EAE treatment was found to bring back the altered levels within normal range indicating the therapeutic effect of plant extract over liver cancer. Zymogram showed the inhibition of MMPs and RT-PCR analysis revealed that the mRNA expression of nuclear factor-kB was markedly decreased upon EAE treatment. Further, our results showed that EAE could significantly inhibit mdr1 gene encode P-glycoprotein expression. Our data suggest that EAE is a novel anticancer and potent MDR reversal agent and may be a potential adjunctive agent for tumor chemotherapy.

Context: Eclipta alba (Linn) Hassk. (Asteraceae) has been reported to be a nerve tonic and has been used to treat epilepsy in folk medicine. Objective: The present study isolates and characterizes luteolin from E. alba and evaluates its antiepileptic potential in chemically induced acute and chronic models in mice. Materials and methods: The methanol extract (16.85% w/w) of E. alba leaves was subjected to fractionation for isolation of luteolin. In acute pentylenetetrazole (PTZ) model, luteolin (5, 10, 20 mg/kg, i.p.) was administered 30 min prior to PTZ injection (100 mg/kg) in Swiss albino mice. Kindling was induced by chronic administration of PTZ (35 mg/kg) on every alternate day (48 days). Luteolin was investigated on the course of kindling development and oxidative stress markers [reduced glutathione (GSH) and malondialdehyde (MDA)] in kindled mice. Results: Single-dose pretreatment with luteolin (10 and 20 mg/kg, i.p.) was found to be effective in an acute PTZ model (100% protection from mortality) and it did not exhibit any effect on motor coordination at the same doses. PTZ-induced kindling was significantly (p

Cancer is the final outcome of a plethora of events. Targeting the proliferation or inducing programmed cell death in a proliferating population is a major standpoint in the cancer therapy. However, proliferation is regulated by several cellular and immunologic processes. This study reports the inhibition of proliferation by augmenting immune surveillance, silencing acute inflammation, and inducing p53-mediated apoptosis of skin cancer by 3 promising medicinal extracts. We used the well-characterized model for experimental skin carcinogenesis in mice for 32 weeks to study the chemopreventive effect of the methanolic extracts of Trigonella foenumgraecum, Eclipta alba, and Calendula officinalis. All 3 extracts reduced the number, incidence, and multiplicity of tumors, which was confirmed by the pathologic studies that showed regressed tumors. There was a significant reduction in the PCNA+ nuclei in all treatment groups 32 weeks after the initiation. Mechanistic studies revealed that proliferative population in tumors is diminished by the restoration of the endogenous antioxidant defense, inhibition of the stress-related signal-transducing element NFκB, reduction of inflammation, enhancement of immunosurveillance of the genetically mutated cells, along with silencing of the cell cycle progression signals. Finally, all 3 medicinal extracts induced stable expression of p53 within the tumors, confirmed by the CFDA-Cy3 apoptosis assay. Results of our study confirm that these extracts not only limit the rate of proliferation by inhibition of the processes integral to cancer development but also induce stable cytoplasmic expression of p53-mediated apoptosis, leading to fewer and regressed tumors in mice.

The development of multidrug resistance (MDR) causes problems in the chemotherapy of human cancer. The present study was designed to evaluate and establish the role of Eclipta alba as MDR reversal agent using multidrug resistant hepatocellular carcinoma cell line (DR-HepG2). To develop DR-HepG2, hepatocellular carcinoma cell line (HepG2) was transfected with 2-Acetylaminofluorene (AAF) and Aflatoxin B1 (AFB). Cytotoxic effects of the Eclipta alba hydroalcoholic extract (EAE) and standard anti-ancer drug Doxorubicin (DOX) were determined in DR-HepG2 and the parental cells HepG2 using MTT assay. The expression level of MDR1 gene and P-glycoprotein (P-gp) level was analyzed by RT-PCR and western blotting. From the present investigation, it was found that EAE (10 and 20 μg/ml) could significantly inhibit cell proliferation in DR-HepG2 whereas DOX (0.5 μg/ml) could not because of enhancement effect of MDR1/P-gp. This study demonstrated for the first time the antiproliferative activities of EAE in multidrug resistant DR-HepG2 cells. The findings revealed that Eclipta alba components are effective inhibitors of MDR1/P-gp.

Objective Ecliptae herba (EH) has long been used in China to strengthen bones. Accumulating evidence indicates that EH may have antiosteoporotic effects. The aim of this study was to evaluate the effects of aqueous EH extract (EHE) on rats that had osteoporosis-like features induced by ovariectomy, using aqueous Fructus Ligustri Lucidi extract as positive control agent. Methods Three-month-old female rats that underwent ovariectomy were treated with EHE (1.4 g/kg per day). After 12 weeks, bone mineral density and bone histomorphometric indices of tibiae were measured. Protein and messenger RNA expressions of osteoprotegerin and receptor activator of nuclear factor κ-B ligand (RANKL) in tibiae were evaluated by immunohistochemistry and in situ hybridization. In addition, serum concentrations of osteocalcin, interleukin-1β, interleukin-6 (IL-6), calcitonin (CT), and parathyroid hormone were determined by enzyme-linked immunosorbent assay. Results EHE treatment prevented body weight gain and loss of uterine wet weight in ovariectomized rats. It remarkably increased bone mass in ovariectomized rats compared with ovariectomized controls. EHE treatment significantly down-regulated RANKL expression in tibiae from ovariectomized rats compared with controls; however, it had no significant effect on osteoprotegerin expression. In addition, EHE treatment significantly reduced serum IL-6 levels and remarkably increased CT levels but had no effect on parathyroid hormone. Conclusions EHE increases bone mass in ovariectomized rats by inhibiting bone loss: down-regulated RANKL expression in tibiae and IL-6 level in serum, and up-regulated CT level in serum. This suggests that EHE may be developed as an alternative therapeutic agent for osteoporosis induced by postmenopause.

The antidiabetic effect of the ethanolic extract of Eclipta alba (EEA) on hyperglycaemia and diabetic nephropathy was investigated in streptozotocin-induced diabetic rats. Single-dose treatment of EEA to streptozotocin-induced diabetic rats lowered the blood glucose level by 17.6% (p < 0.05) at 250 mg kg(-1) dose after 5 h post oral administration. Treatment of animals after 10 weeks of STZ-treatment with EEA (250 mg kg(-1)) for 21 days significantly reduced the elevated levels of blood glucose, %HbA1C, urea, uric acid and creatinine, and significantly increased the depressed serum insulin level. The extract exerted a significant inhibitory effect on alpha-glucosidase in a noncompetitive manner with an IC(50) value of around 54 µg mL(-1) and was found inhibitory to eye lens aldose reductase with an IC(50) value of around 4.5 µg mL(-1). The results suggest that EEA possesses antidiabetic effect associated with alpha-glucosidase and aldose reductase inhibition.

Ethnopharmacological relevance Eclipta prostrata (L.) L. (Asteraceae) has been used in Brazilian traditional medicine to treat asthma and other respiratory illnesses. Aims of the study To investigate the effects of different doses of a standardized extract of E. prostrata using a murine model of allergen induced asthma. Materials and methods Balb/c mice were sensitized twice with ovalbumin (OVA) administered intraperitoneally and challenged over four alternate days with nasal instillations of OVA solution. The standardized methanol extract of E. prostrata was administered in doses of 100, 250 and 500 mg kg − 1 concomitantly with nasal instillation over seven consecutive days. Control animals were treated with dexamethasone or saline solution. Bronchial hyperresponsiveness, production of Th1 and Th2 cytokines, allergen sensitization, airway and lung inflammation, mucous secretion and airway remodeling were assessed. Results The concentrations of chemical markers in the standardized methanol extract were 0.02% oroboside, 1.69% demethylwedelolactone and 1.71% wedelolactone. Treatment with 250 mg kg −1 of extract, which provided 0.745, 4.22 and 4.30 mg kg − 1 day −1 of oroboside, demethylwedelolactone and wedelolactone, respectively, significantly reduced ( P P E. prostrata. Conclusion The results presented herein demonstrate for the first time the anti-inflammatory activity of E. prostrata in a murine model of asthma, thereby supporting the ethnopharmacological uses of the plant.

The infection of Eclipta yellow vein virus [EcYVV-IN, Accession No. KC476655], recently reported for the first time, on Andrographis paniculata was studied for redox-mediated alteration mechanism in infected plants. A. paniculata, an important medicinal plant, is used in traditional Indian, Chinese and modern system of medicine. Andrographolide, one of the foremost components of this plant, is known for its varied pharmacological properties. Our investigation provides insight into the effect of virus-induced changes in the singlet oxygen quenching due to the alteration in pigment content (chlorophyll and carotenoids) as well as activation of plant secondary metabolism along with defense activation leading to changes in enzymatic and non-enzymatic redox status. Due to infection, a reduction in carotenoid content was observed which leads to reduced quenching of singlet oxygen. An increased level of enzymatic (SOD and APX) and non-enzymatic antioxidant (DPPH, FRAP, RP, NO, TAC and TP) activities were also observed in virus-infected plants with a positive correlation (0.9). However, CAT activity was diminished which could be either due to its proteolytic degradation or inactivation by superoxide anions (O(2-.)), NO or peroxynitrite radicals. A significant (p 0.05) increase in total phenolic content was observed in the infected plants while no considerable difference was seen in the total flavonoid content. Our results highlighted the alteration in redox status caused by virus-induced biotic stress on the plants and could be useful for understanding the after effects of viral infection This study could also be helpful in developing biomimetic methods for improving the production of secondary metabolites of pharmaceutical importance.

Major challenges for current therapeutic strategies against breast cancer are associated with drug-induced toxicities. Considering the immense potential of bioactive phytochemicals to deliver non-toxic, efficient anti-cancer therapeutics, we performed bio-guided fractionation of Eclipta alba extract and discovered that particularly the chloroform fraction of Eclipta alba (CFEA) is selectively inducing cytotoxicity to breast cancer cells over non-tumorigenic breast epithelial cells. Our unbiased mechanistic hunt revealed that CFEA specifically activates the intrinsic apoptotic pathway by disrupting the mitochondrial membrane potential, upregulating Hsp60 and downregulating the expression of anti-apoptotic protein XIAP. By utilizing Hsp60 specific siRNA, we identified a novel pro-apoptotic role of Hsp60 and uncovered that following CFEA treatment, upregulated Hsp60 is localized in the endoplasmic reticulum (ER). To our knowledge, this is the first evidence of ER specific localization of Hsp60 during cancer cell apoptosis. Further, our LC-MS approach identified that luteolin is mainly attributed for its anti-cancer activities. Moreover, oral administration of CFEA not only offers potential anti-breast cancer effects in-vivo but also mitigates tumor induced hepato-renal toxicity. Together, our studies offer novel mechanistic insight into the CFEA mediated inhibition of breast cancer and may potentially open up new avenues for further translational research.

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.

This article was published in Journal of Pharmacology and Toxicology [© 2011 Academic Journals Inc.] and the definite version is available at: http://docsdrive.com/pdfs/academicjournals/jpt/0000/28817-28817.pdf

Ethnopharmacological relevance Eclipta alba is traditionally used as hepatoprotective agent. The study was designed to explore its antiproliferative activity on liver and other related cancer. Aim of the study The present study was designed to assess and establish the role of Eclipta alba as anti-cancer agent using HepG2, C6 glioma and A498 cell lines as model system. Materials and methods Antiproliferative and cytotoxic effects of the Eclipta alba hydroalcoholic extract (EAE) was determined using MTT assay. The expression level of NF-kB was analysed by western blotting and RT PCR. Gelatin zymography was done for gelatinase matrix metalloproteinases (MMP-2 and 9) analysis. Results EAE inhibited the cell proliferation in dose dependent manner in HepG2, A498 and C6 glioma cell lines with an IC50 of 22 ± 2.9, 25 ± 3.6 and 50 ± 8.7 μg/ml, respectively. The expression of MMP (2 and 9) was down-regulated with EAE treatment. DNA damage was observed following 72 h of extract treatment, leading to apoptosis. Additionally, the expression level of NF-kB was evaluated with western blotting and RT-PCR and was found to be down-regulated/inactivated. Conclusions The data establish the existence of anti-proliferative, DNA damaging and anti-metastasis properties in EAE which is yet unexplored and hold high therapeutic impact.

Mosquitoes transmit serious human diseases, causing millions of deaths every year. Use of synthetic insecticides to control vector mosquitoes has caused physiological resistance and adverse environmental effects in addition to high operational cost. Insecticides of synthesized natural products for vector control have been a priority in this area. In this study, larvicidal activity of synthesized silver nanoparticles (AgNPs) utilizing aqueous extract from Eclipta prostrata, a member of the Asteraceae was investigated against fourth instar larvae of filariasis vector, Culex quinquefasciatus say and malaria vector, Anopheles subpictus Grassi (Diptera: Culicidae). The synthesized AgNPs characterized by UV-vis spectrum, scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) and X-ray diffraction (XRD). SEM analyses of the synthesized AgNPs were clearly distinguishable measured 35-60 nm in size. Larvae were exposed to varying concentrations of aqueous extract of synthesized AgNPs for 24h. The maximum efficacy was observed in crude aqueous, and synthesized AgNPs against C. quinquefasciatus (LC(50)=27.49 and 4.56 mg/L; LC(90)=70.38 and 13.14 mg/L), and against A. subpictus (LC(50)=27.85 and 5.14 mg/L; LC(90)=71.45 and 25.68 mg/L) respectively. The chi-square value were significant at p

Eclipta prostrata has been used as a traditional medicinal plant to prevent dementia and to enhance memory in Asia. Its potential as a nootropic and as an antioxidant have been reported in mice. We hypothesized that Eclipta may affect the formation of neurotransmitters and the inhibition of oxidative stress. Charles River cesarean-derived rats (male, 180 ± 10 g) were fed experimental diets supplemented with 0 mg (control), 25 mg (E25), 50 mg (E50), or 100 mg (E100) of a freeze-dried butanol fraction of E prostrata per kilogram of diet for 6 weeks. The acetylcholine level was significantly increased by 9.6% and 12.1% in the brains of E50 and E100 groups, respectively, as compared with the control group that was fed standard diet alone. The acetylcholine esterase activity was significantly increased by 13.1% and 19.7% in the brains of E50 and E100 groups, respectively, compared with the control group. Monoamine oxidase-B activity was significantly decreased by 10.5% in the brains of the E100 group, and the superoxide radical level was significantly reduced by 9.4% in the serum of the E100 group compared with the control group. Superoxide dismutase activity was significantly increased by 9.6% and 11.6% in the serum of E50 and E100 groups, respectively, compared with the control group. These results clearly demonstrate the effects of E prostrata on the formation of acetylcholine in the brain and the inhibition of oxidative stress in the brain and serum of rats. These findings may have implications for preventing dementia and enhancing memory function in humans.

Objective : The present study focuses on the antioxidant mediated protective effect of a popular medicinal herb Ecliptaalba against CCl 4 induced oxidative stress in the liver of rats. Methods: Rats divided into four groups were administered with CCl 4 andCCl 4 along with methanol extract of leaves of Eclipta herb (200 and 400 mg/kg b. wt) for three weeks. At the end of treatment, rats were anaesthetized and blood samples were collected for serum separation. Biochemical analysis such as alanineaminotransferase (ALT), aspartateaminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) and total bilirubin (TB) were done in serum. Liver tissue was used for glutathione (GSH), lipid peroxidation (LPO), gluatathione peroxidase (GPx), glutathione Stransferase (GST), superoxide dismutase (SOD)and catalase (CAT) analysis. CCl 4 administration caused significant elevation of the serum enzymes and total bilirubin content. Results : Antioxidant enzymes were drastically inhibited with significant reduction of glutathione and increased lipid peroxidation in CCl4 treated rats. Ecliptaalba extracts administrated rats, however did not show much changes in marker enzyme level. Antioxidant enzyme status was also not affected and found nearer to the control levels. Increased gluatathione level and reduced lipid peroxidation was also evident in Eclipta alba treated rats. Conclusion : The findings show that Eclipta alba extract offers better protection against the free radical toxicity of CCl 4 .

A green, low-cost and reproducible Eclipta leaves negotiated synthesis of silver nanoparticles is reported. The synthesis is performed at room temperature. X-ray and transmission electron microscopy analyses are performed to ascertain the formation of Ag nanoparticles. Nanoparticles almost spherical in shape having a size of 2-6 nm are found. UV-visible study revealed the surface plasmon resonance at 419 nm. The lattice strain is estimated to be 0.0045 using Williamson-Hall approach. The use of Eclipta for the synthesis of silver nanoparticles offers the benefit of ecofriendliness and amenability for large scale production through scaling up.

The case of a 64 year old female patient is presented who has treated herself for 9 months with various Indian Ayurvedic herbal products for her vitiligo and experienced a causally related severe hepatotoxicity (ALT, 601 U/L; AST, 663 U/L; Bilirubin, 5.0 mg/dL). After discontinuation, a rapid improvement was observed. Causality assessment with the updated CIOMS (Council for International Organizations of Medical Sciences) scale showed a probable causality (+8 points) for Bakuchi tablets containing extracts from Psoralea corylifolia leaves with psoralens as ingredients, as the primary candidate causing the hepatotoxic reaction. The degree of probability was lower with +6 points for other used herbs: Khadin tablets containing extracts from Acacia catechu leaves; Brahmi tablets containing Eclipta alba or Bacopa monnieri; and Usheer tea prepared from Vetivexia zizaniodis. The case is the first report of Indian Ayurvedic herbal products being potentially hepatotoxic in analogy to some other herbs.

Eclipta prostrata grows abundantly in the tropical and the sub-tropical parts of the world includingmost part of the Korean Peninsula. The plant has been traditionally used for the treatment of a number ofinflammatory diseases including hepatitis and enteritis but the nature of its immuno-modulating activity needsmore studies. In this study, water-soluble sugar-containing fractions were purified from the herb and their effectson the culture of mouse splenocytes were examined. One of the fractions significantly suppressed apoptosis ofthe splenocytes in culture, which involves the gene expression regulation of a number of cytokines and cytok-ine receptors including MIP1-β. This study could explain an immunological activity of Eclipta prostrata andwould lead to identify an immuno-active compound from the plant. Keywords: Apoptosis, Eclipta , Splenocytes, Carbohydrates, MIP1- β INTRODUCTION Eclipta prostrata is an annual tropical and subtropicalplant and also grows abundantly throughout the KoreanPeninsula. It is regarded as an edible plant in Korea andalso a traditional medicinal herb used for the treatment ofa number of inflammatory diseases including hepatitisand enteritis (Han

Experiments were conducted to determine the influence of various environmental factors on seed germination and seedling emergence of eclipta. Seed germination was completely inhibited in the dark, whereas in the light/dark it was 76, 93, and 87% at 25/15, 30/20, and 35/25 C alternating day/night temperatures, respectively. Germination was greater than 80% up to a temperature of 140 C, when seed were placed in an oven for 5 min followed by incubation at 30/20 C for 14 d, but declined progressively with a further increase in exposure temperature with no germination at 200 C. Seed germination was tolerant of salt stress but highly sensitive to water stress. Seed germinated (87 to 93%) over a pH range of 4 to 10. Seedling emergence was greatest (83%) for the seed placed on the soil surface but declined thereafter, and no seedlings emerged from a depth of 0.5 cm. Seedling emergence was slower and lower with the addition of 4 to 6 t ha−1of plant residue. The information gained from this study identifies some of the factors facilitating eclipta becoming a widespread weed in the humid tropics and might contribute to its control.

Alopecia is a dermatological disorder with psychosocial implications on patients with hair loss. Eclipta alba Hassk. is a well-known Ayurvedic herb with purported claims of hair growth promotion. In the reported work attempts were undertaken to evaluate petroleum ether and ethanol extract of E. alba Hassk. for their effect on promoting hair growth in albino rats. The extracts were incorporated into oleaginous cream (water in oil cream base) and applied topically on shaved denuded skin of albino rats. The time (in days) required for hair growth initiation as well as completion of hair growth cycle was recorded. Minoxidil 2% solution was applied topically and served as positive control for comparison. Hair growth initiation time was significantly reduced to half on treatment with the extracts, as compared to control animals. The time required for complete hair growth was also significantly reduced. Quantitative analysis of hair growth after treatment with petroleum ether extract (5%) exhibited greater number of hair follicles in anagenic phase (69 +/- 4) which were higher as compared to control (47 +/- 13). The result of treatment with 2 and 5% petroleum ether extracts were better than the positive control minoxidil 2% treatment.

Summary Background Cuscuta reflexa (Roxb.), Citrullus colocynthis (Schrad.), and Eclipta alba (Hassk.) are traditionally acclaimed herbs for their hair growth–promoting potential. Aim In the present study, it was envisaged to prepare herbal formulations containing petroleum ether extracts of the three herbs in varying ratio and evaluating the formulations for the hair growth–promoting activity. Methods The formulations as well as minoxidil (2%) solution (positive control) were applied topically on shaved skin of rats, and the time required for initiation and completion of hair growth cycle was recorded. Results and conclusions Hair growth initiation time was markedly reduced to one third on treatment with the prepared formulation compared with control animals. The time required for complete hair growth was also reduced by 32%. Quantitative analysis of hair growth cycle after treatment with formulations and minoxidil (2%) exhibited greater number of hair follicles in anagenic phase compared with control. The results thus corroborate with the traditionally acclaimed hair growth–promoting capabilities of the plants. The prepared formulation also holds potential for treatment of alopecia.

Echinocystic acid (EA) is a natural triterpone enriched in various herbs and has been used for medicinal purposes in China. In the present study, we systematically examined the effects of EA on ovariectomy-induced osteoporosis in rats for the first time. Three-month-old female ovariectomy (OVX) Sprague–Dawley rats were used to evaluate the osteoprotective effect of EA. Results showed that administration of EA (5 or 15 mg/kg/day) for 12 weeks prevented lower levels of maximum stress and Young’s modulus of femur induced by OVX. EA also recovered bone metabolic biomarkers levels in OVX rats, including osteocalcin, alkaline phosphatese, deoxypyridinoline, and urinary calcium and phosphorus. EA (5 and 15 mg/kg/day) could prevent the alteration of total bone mineral density in the femur caused by OVX. However, only high dose (15 mg/kg/day) of EA significantly improved trabecular architecture, as evidenced by higher levels of bone volume/tissue volume, trabecula number, and trabecula thickness, and lower levels of trabecula separation and structure model index compared with OVX rats. In addition, EA treatment decresed the serum levels of IL-1β and TNF-α in OVX rats. In conclusion, EA could prevent reduction of bone mass and strength and improve the cancellous bone structure and biochemical properties in OVX rats. Hence, EA may serve as a new candidate or a leading compound for anti-osteoporosis.

Ethanopharmacological 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, 5 mg/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.