ABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Ecliptea herba, a traditional Chinese herbal medicine for hair loss, was first recorded in the Tang Dynasty's 'Qian Jin Yue Ling', of which the active ingredients and mechanisms of action in the treatment of chemotherapy-induced hair loss remain poorly investigated. AIM OF THE STUDY: To investigate the effects of the petroleum ether extract of Eclipta (PEE) on alopecia and follicle damage and elucidate its potential therapeutic mechanisms using the integration of network pharmacology, bioinformatics, and experimental validation. MATERIALS AND METHODS: UPLC-MS was used to analyse the chemical composition of PEE. A network pharmacology approach was employed to establish the 'components-targets-pathways' network of PEE to explore potential therapeutic pathways and targets. Molecular docking was used for validation, and the mechanism of PEE in treating chemotherapy-induced alopecia (CIA) was elucidated using in vitro and in vivo on CIA models. RESULTS: UPLC-MS analysis of PEE revealed 185 components, while network pharmacology and molecular docking analyses revealed potential active compounds and their target molecules, suggesting the involvement of core genes, such as TP53, ESR1, AKT1, IL6, TNF, and EGFR. The key components included wedelolactone, dimethyl-wedelolactone, luteoloside, linarin, and hispidulin. In vivo, PEE promoted hair growth, restored the number of hair follicles, and reduced follicle apoptosis. Conversely, in vitro, PEE enhanced cell viability, reduced apoptosis, and protected HaCaT cells from damage induced by 4-hydroperoxycyclophosphamide (4-HC). CONCLUSIONS: PEE alleviated hair follicle damage in CIA mice by inhibiting the P53/Fas pathway, which may be associated with inhibiting hair follicle cell apoptosis. This study provides a novel therapeutic strategy for treating cyclophosphamide-induced hair loss.
Subject(s)
Alopecia , Eclipta , Signal Transduction , Animals , Humans , Male , Mice , Alkanes , Alopecia/chemically induced , Alopecia/drug therapy , Antineoplastic Agents/pharmacology , Antineoplastic Agents/toxicity , Apoptosis/drug effects , Cyclophosphamide/toxicity , Eclipta/chemistry , HaCaT Cells , Hair Follicle/drug effects , Hair Follicle/metabolism , Molecular Docking Simulation , Network Pharmacology , Plant Extracts/pharmacology , Plant Extracts/chemistry , Signal Transduction/drug effects , Tumor Suppressor Protein p53/metabolism , Tumor Suppressor Protein p53/geneticsABSTRACT
BACKGROUND: Multiple myeloma (MM) is an incurable hematological malignancy with limited therapeutic efficacy. Eclipta prostrata is a traditional Chinese medicinal plant reported to possess antitumor properties. However, the effects of E. prostrata in MM have not been explored. PURPOSE: The aim of this study was to define the mechanism of the ethanol extract of E. prostrata (EEEP) in treating MM and identify its major components. METHODS: The pro-ferroptotic effects of EEEP on cell death, cell proliferation, iron accumulation, lipid peroxidation, and mitochondrial morphology were determined in RPMI-8226 and U266 cells. The expression levels of nuclear factor erythroid 2-related factor 2 (Nrf2), kelch-like ECH-associated protein 1 (Keap1), heme oxygenase-1 (HO-1), glutathione peroxidase 4 (GPX4), and 4-hydroxynonenal (4HNE) were detected using western blotting during EEEP-mediated ferroptosis regulation. The RPMI-8226 and U266 xenograft mouse models were used to explore the in vivo anticancer effects of EEEP. Finally, high performance liquid chromatography (HPLC) and ultra-high-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry system (UPLC-Q/TOF-MS) were used to identify the major constituents of EEEP. RESULTS: EEEP inhibited MM cell growth and induced cell death in vitro and in vivo. By promoting malondialdehyde and Fe2+ accumulation, lipid peroxidation, and GSH suppression, EEEP triggers ferroptosis in MM. Mechanistically, EEEP regulates the Keap1/Nrf2/HO-1 axis and stimulates ferroptosis. EEEP-induced lipid peroxidation and malondialdehyde accumulation were blocked by the Nrf2 activator NK-252. In addition, HPLC and UPLC-Q/TOF-MS analysis elucidated the main components of EEEP, including demethylwedelolactone, wedelolactone, chlorogenic acid and apigenin, which may play important roles in the anti-tumor function of EEEP. CONCLUSION: In summary, EEEP exerts its anti-MM function by inducing MM cell death and inhibiting tumor growth in mice. We also showed that EEEP can induce lipid peroxidation and accumulation of ferrous irons in MM cells both in vivo and in vitro, leading to ferroptosis. In addition, this anti-tumor function may be achieved by the EEEP activation of Keap1/Nrf2/HO-1 axis. This is the first study to reveal that EEEP exerts anti-MM activity through the Keap1/Nrf2/HO-1-dependent ferroptosis regulatory axis, making it a promising candidate for MM treatment.
Subject(s)
Eclipta , Ferroptosis , Heme Oxygenase-1 , Kelch-Like ECH-Associated Protein 1 , Multiple Myeloma , NF-E2-Related Factor 2 , Plant Extracts , Ferroptosis/drug effects , Kelch-Like ECH-Associated Protein 1/metabolism , Multiple Myeloma/drug therapy , Animals , NF-E2-Related Factor 2/metabolism , Humans , Plant Extracts/pharmacology , Cell Line, Tumor , Heme Oxygenase-1/metabolism , Mice , Eclipta/chemistry , Lipid Peroxidation/drug effects , Xenograft Model Antitumor Assays , Cell Proliferation/drug effects , Mice, Nude , Mice, Inbred BALB C , Male , Antineoplastic Agents, Phytogenic/pharmacology , EthanolABSTRACT
Eclipta prostrata Linn. is an annual herbaceous plant used in traditional medicine, commonly known as "Trailing Eclipta" or False Daisy in English, ' Keekirindiya ' in Sinhala and ' Kayyantakara' in Tamil. The aim of this study was to conduct a detailed pharmacognostical evaluation of E. prostrata found in Sri Lanka. Anatomical, physicochemical, phytochemical studies, and quantification of phyto - constituents were performed as per WHO guidelines. Whole plant was sequ entially extracted into solvents with different polarities. Phytochemical screening and Thin Layer Chromatography (TLC) fingerprinting were carried out. Anatomical study and powder microscopy revealed useful diagnostic features. Physicochemical parameters such as moisture content, ash values (total, acid insoluble, water soluble) and extractable matter in water and ethanol were evaluated. Phytochemical screening and TLC fingerprinting revealed the presence of different types of phyto - constituents. Alkaloid, tannin, saponin, total flavonoid and total polyphenol contents were quantified. In conclusion, pharmacognostical study aids in establishing the standardization parameters of E. prostrata found in Sri Lanka.
Eclipta prostrata Linn. es una planta herbácea anual utilizada en la medicina tradicional, comúnmente conocida como "Trailing Eclipta" o False Daisy en inglés, 'Keekirindiya' en sinhala y 'Kayyan takara' en tamil. El objetivo de este estudio fue realizar una evaluación farmacognóstica detallada de E. prostrata encontrada en Sri Lanka. Se llevaron a cabo estudios anatómicos, fisicoquímicos, fitoquímicos y cuantificación de fitoconstituyentes según l as directrices de la OMS. Se extrajo secuencialmente la planta entera en solventes con diferentes polaridades. Se realizaron pruebas de tamizaje fitoquímico y huellas dactilares de cromatografía en capa delgada (TLC). El estudio anatómico y la microscopía en polvo revelaron características diagnósticas útiles. Se evaluaron parámetros fisicoquímicos como el contenido de humedad, los valores de ceniza (total, insoluble en ácido, soluble en agua) y la materia extraíble en agua y etanol. Las pruebas de tamizaje fitoquímico y las huellas dactilares de TLC revelaron la presencia de diferentes tipos de fitoconstituyentes. Se cuantificaron los contenidos de alcaloides, taninos, saponinas, flavonoides totales y polifenoles totales. En conclusión, el estudio farmacogn óstico ayuda a establecer los parámetros de estandarización de E. prostrata encontrada en Sri Lanka.
Subject(s)
Eclipta/chemistry , Saponins/analysis , Sri Lanka , Flavonoids/analysis , Chromatography, Thin Layer , Eclipta/anatomy & histology , Polyphenols/analysisABSTRACT
Constructed wetlands (CWs) provide a low-cost, effective solution for domestic wastewater treatment in developing nations compared to costly traditional wastewater systems. Biochar which is an organic material created by pyrolysis offers straightforward, affordable methods for treating wastewater and lowering carbon footprint by acting as a substrate in CWs. Batch mode biochar-amended subsurface flow (SSF) CWs planted with Eclipta alba (L) with a hydraulic retention time (HRT) of 3 days were used for the treatment of rural domestic wastewater in the present investigation. Two control CWs, without plants (C1) and with plants (C2), and five different amendments of biochar 5% (B5), 10% (B10), 15% (B15), 20% (B20) and 25% (B25) in ratio with soil were set up to check the treatment efficiency of CWs. Removal efficiency (RE%) of the CWs for parameters namely chemical oxygen demand (COD), biochemical oxygen demand (BOD), phosphate (PO42-), sulphate (SO42-), nitrate (NO3-) and total Kjeldhal nitrogen (TKN) was determined using standard methods. Removal efficiency of 93%, 91%, 74% and 77% was observed for BOD, COD, nitrate and sulphate, respectively, in the B25 amendment at HRT 72 h. The highest removal of TKN (67%) was also observed in the B25 amendment at HRT of 72 h. No stable trend for the removal of phosphates was found during the study, and maximum removal was observed at HRT 48 h; afterward, phosphate was slightly inclined with the increasing HRT. The findings of one-way ANOVA using Tukey's test show significant variations (p < 0.05) in the removal efficiencies of pollutants after 72 h between two controls (C1 and C2) and various biochar amendments in CWs, indicating a significant role of the wetland plants and concentration of the biochar as substrate. Biochar shows a positive impact on the removal of organic pollutants and nitrates. Hence, biochar-amended CWs can be a sustainable way of treating rural domestic wastewater.
Subject(s)
Charcoal , Eclipta , Environmental Pollutants , Water Purification , Wastewater , Waste Disposal, Fluid/methods , Wetlands , Nitrates , Plants , Water Purification/methods , Nitrogen/analysis , Phosphates , SulfatesABSTRACT
Safety regarding herbal products is very necessary; therefore, routine identification of raw materials should be performed to ensure that the raw materials used in pharmaceutical products are suitable for their intended use. In order for the identification-related data obtained to be accurate, the identification of various kinds of markers is also very necessary. The purpose of this study was to describe the characteristics of Eclipta alba (L.) Hassk. based on qualitative morpho-anatomical markers and quantitative DNA coding. The morphology of this plant has herbaceous habit with a taproot and a stem with branches that appear from the middle. Leaves are single type imperfectly arranged oppositely, lanceolatus, finely serrated on the edges, tapered at the base, pointed at the end, and have a pinnate and hairy leaf surface. The flowers consist of ray flowers and tube flowers with a cup shape. Meanwhile, in terms of anatomy, E. alba has aerenchyma, which are scattered in the cortex of the root and stem. In addition, there are anisocytic stomata, glandular trichomes, and non-glandural trichomes with an elongated shape accompanied by ornamentation found on the leaf epidermis. The results of sequence alignment and phylogenetic tree reconstruction show that the sample plants are closely related to species in the genus Eclipta.
Subject(s)
Eclipta , DNA Barcoding, Taxonomic , Phylogeny , Plant Leaves/anatomy & histology , FlowersABSTRACT
The primary objective of this study was to elucidate the chemical composition, antioxidant properties, and antiproliferative activities of Eclipta prostrata extracts. Two flavonoids, 3'-O-methylorobol and apigenin 7-sulfate, were isolated from the ethyl acetate (EtOAc) extract of E. prostrata. The total phenolic and flavonoid contents of the E. prostrata extracts, as well as their overall antioxidant activities as measured using the 2,2-diphenyl-1-picrylhydrazyl and reducing power assays, were investigated. The E. prostrata EtOAc extract exhibited significantly greater antioxidant activities in both assays and higher phenol and flavonoid contents than the other extracts. The potential antiproliferative properties of the E. prostrata extracts and isolated compounds were investigated in vitro against the AGS, A549, and HT-29 cancer cell lines and the normal human HEK-293 cell line using the MTT assay. Annexin V-FITC/PI staining analysis and quantitative real-time PCR were used to assess AGS cell apoptosis. At a concentration of 100 µg/mL, the EtOAc extract of E. prostrata reduced AGS cell viability and proliferation by inducing apoptosis through the alteration of gene expression in the apoptotic cascade. These results highlight E. prostrata as a promising source of anticancer compounds.
Subject(s)
Antioxidants , Eclipta , Humans , Antioxidants/pharmacology , Plant Extracts/pharmacology , Plant Extracts/chemistry , Eclipta/chemistry , HEK293 Cells , Flavonoids/pharmacologyABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: Chinese Ecliptae herba (Eclipta prostrata (L.) L.) is an ethnomedicinal herb, which is used mainly to nourish kidney and thus strengthen bones according to traditional Chinese medicine theory. Pharmacological studies have supported the ethnomedicine use, showing that Ecliptae herba extract has an anti-osteoporotic effect in vivo and promoted osteoblast proliferation and activity in vitro. However, the molecular mechanism of Ecliptae herba on osteoblast differentiation from bone marrow mesenchymal stem cells (BMSC), the progenitors of osteoblasts, is still unclear. AIM OF THE STUDY: N6-methyladenosine (m6A) mRNA epigenetic modification may play a key role in promoting osteoblastic differentiation, and thus treating osteoporosis. This study sought to assess the mechanism through which Eclipate herba and its component wedelolactone influence m6A modification during the process of osteoblastogenesis from BMSC. MATERIAL AND METHODS: The alkaline phosphatase (ALP) and Alizarin red S (ARS) staining were applied to determine osteoblastogenesis from BMSC. Western blot and quantitative real-time PCR were performed. RNA sequencing analysis was used to determine the characteristics of m6A methylation. Stable knocking down of METTL3 using lentiviral-based shRNA was performed. RESULTS: Upon 9 d treatment of BMSC with ethyl acetate extract of Ecliptae herba (MHL), ALP activity and ossification level increased in comparison with osteogenic medium (OS)-treated control. The expression of methyltransferase METTL3 and METTL14 was significantly increased, but WTAP expression had no change in response to MHL treatment. Knocking down of METTL3 resulted in a decrease in MHL-induced ALP activity, ossification level as well as mRNA expression of Osterix and Osteocalcin, two bone formation-related markers. The level of m6A increased when BMSC was treated with MHL for 9 d. RNA sequencing analysis indicated that MHL treatment altered mRNA m6A modification of genes associated with osteoblastogenesis. By kyoto encyclopedia of genes and genomes (KEGG) pathway analysis, HIF-1α, PI3K/Akt, and Hippo signaling pathways were enriched and associated with m6A modification. The expression of m6A-modified genes including HIF-1α, VEGF-A, and RASSF1, was upregulated by MHL, but the upregulation was reversed after METTL3 knockdown. Additionally, the enhanced expression of METTL3 was also observed after treatment with wedelolactone, a component from MHL. CONCLUSIONS: These results suggested a previously uncharacterized mechanism of MHL and wedelolactone on osteoblastogenesis, by which METTL3-mediated m6A methylation is involved and thus contributes to the enhancement of osteoblastogenesis.
Subject(s)
Eclipta , Mesenchymal Stem Cells , Methylation , Phosphatidylinositol 3-Kinases/metabolism , Methyltransferases/genetics , Methyltransferases/metabolism , Methyltransferases/pharmacology , RNA, Small Interfering , RNA, Messenger/metabolismABSTRACT
The Eclipta alba plant is considered hepatoprotective, owing to its phytoconstituents wedelolactone. In the current study, effect of elevated ultraviolet-B (eUV-B) radiation was investigated on biochemical, phytochemical, and antioxidative enzymatic activities of E. alba (Bhringraj) plant. The UV-B exposure resulted in an increase in oxidative stress, which has caused an imbalance in phytochemical, biochemical constituents, and induced antioxidative enzymatic activities. It was observed that the UV-B exposure promoted wedelolactone yield by 23.64%. Further, the leaf extract of UV-B-exposed plants was used for the synthesis of carbon quantum dots (CQDs) using low cost, one-step hydrothermal technique and its biocompatibility was studied using in vitro MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay on HepG2 liver cell line. It revealed no toxicity in any treatment groups in comparison to the control. Both CQDs and leaf extract were orally administered to the golden hamster suffering from alcohol-induced liver cirrhosis. In the morphometric study, it was clearly observed that a combination of UV-B-exposed leaf extract and synthesized CQDs delivered the best result with maximum recovery of liver tissues. The present study reveals the positive impact of UV-B exposure on the medicinally important plant, increased yield of wedelolactone, and its enhanced hepatoprotective efficacy for the treatment of damaged liver tissues.
Subject(s)
Eclipta , Quantum Dots , Animals , Cricetinae , Plant Extracts/pharmacology , Mesocricetus , Antioxidants/pharmacology , Liver Cirrhosis , Carbon/pharmacologyABSTRACT
BACKGROUND: The search for bioactive molecules from medicinal plants of the family Asteraceae has been one of the targets in various phytochemical and pharmacological investigations for many years. According to these studies, wedelolactone, a coumestan of the secondary metabolite type, is a key compound found in several Eclipta and Wedelia herbal plants. To date, numerous experimental studies with intention of highlighting its role in drug development programs were carried out, but an extensive review is not sufficient. OBJECTIVE: The current review aims to fill the gaps in extensive knowledge about phytochemistry, synthesis, pharmacology, and pharmacokinetics of coumestan wedelolactone. MATERIALS AND METHODS: The databases Google Scholar, Scopus, PubMed, Web of Science, Science Direct, Medline, and CNKI were used to compile the list of references. In order to find references, "wedelolactone" was considered separately or in combination with "phytochemistry", "synthesis", "pharmacology", and "pharmacokinetics." Since the 1950s, >100 publications have been collected and reviewed. RESULTS: Wedelolactone is likely to be a characteristic metabolite of two genera Eclipta and Wedelia, the family Asteraceae, while it could be synthetically derived from mono-phenol derivatives, through Sonogashira and cross-coupling reactions. Numerous biomedical investigations on wedelolactone revealed that its pharmacological values included anticancer, antiinflammatory, antidiabetic, antiobesity, antimyotoxicity, antibacterial, antioxidant, antivirus, anti-aging, cardiovascular, serine protease inhibition, especially its protective health benefits to living organs such as liver, kidney, lung, neuron, eye, bone, and tooth. The combination of wedelolactone and potential agents is a preferential approach to improve its biomedical values. Pharmacokinetic study exhibited that wedelolactone was metabolized in rat plasma due to hydrolysis, open-ring lactone, methylation, demethylation, and glucuronidation. CONCLUSIONS: Wedelolactone is a promising agent with the great pharmacological values. Molecular mechanisms of the actions of this compound at both in vitro and in vivo levels are now available. However, reports highlighting biosynthesis and structure-activity relationship are still not adequate. Moreover, chemo-preventive records utilizing nano-technological approaches to improve its bioavailability are needed since the solubility in the living body environment is still limited.
Subject(s)
Asteraceae , Eclipta , Plants, Medicinal , Rats , Animals , Molecular Structure , Plant Extracts/chemistry , Asteraceae/chemistry , Eclipta/chemistry , Phytochemicals/pharmacology , EthnopharmacologyABSTRACT
Hepatitis C virus has a major role in spreading chronic liver disease and hepatocellular carcinoma. Factors such as high costs, pharmacological side effects, and the development of drug resistance strains require the development of new and potentially effective antiviral to treat the various stages of Hepatitis C. Bioactive chemicals have been extracted from medicinal plants and are utilized by humans for the goal of maintaining a healthy lifestyle. The goal of this work is to recognize phytochemicals from Eclipta alba and assess their potentiality activity against the hepatitis C virus envelope glycoprotein using in silico approaches. Phytochemicals from Eclipta alba were virtually screened by Auto dock raccoon and 12 compounds were selected for molecular docking to probe the active binding site. The top two compounds based on the binding score like ecliptalbine and oleanolic acid with HCV E2 glycoprotein exhibit binding energy -8.88 and -8.02 kcal/mol, respectively. The chemicals' usefulness was reinforced by positive pharmacokinetic data. The phytocompounds were identified as potent HCV inhibitors based on the drug likeness and ADMET properties. Both ecliptalbine and oleanolic acid underwent molecular dynamics simulations to determine features such as RMSD, RMSF, SASA, hydrogen-bond number, and MM-PBSA-based binding free energy. From the molecular docking and molecular dynamics simulation study revealed that oleanolic acid obtained from Eclipta alba can be used as inhibitors against Hepatitis C. The identified inhibitor from our study will be study in vitro and in vivo studies to check their efficacy against Hepatitis C.Communicated by Ramaswamy H. Sarma.
Subject(s)
Eclipta , Hepatitis C , Oleanolic Acid , Humans , Molecular Dynamics Simulation , Hepacivirus , Molecular Docking Simulation , Oleanolic Acid/pharmacology , Phytochemicals/pharmacology , GlycoproteinsABSTRACT
BACKGROUND: Benign prostatic hyperplasia (BPH) is a urinary system disease with high prevalence among the middle and elder men. In BPH, proliferation of prostate cells and the imbanlance between androgen and estrogen are both important inducers. Previous studies have demonstrated that compounds from Ligustri Lucidi Fructus (LLF) and Ecliptae Herba (EH) are of phytoestrogenic or phytoandrogenic activities. The combination of LLF with EH at the ratio of 1:1 on crude drugs quantity is called Erzhi formula (EZF), which is used for in vivo research of our study. PURPOSE: This study aimed to investigate potential mechanisms of EZF and its active pharmaceutical ingredients on BPH in vitro and in vivo. METHODS: Therapeutic effects of EZF was evaluated in E2/testosterone (1:100) induced BPH rats model. The pathological changes of prostate, concentrations of testosterone, DHT, E2, PSA in rats' plasma and prostate were detected. The expressions of PCNA, AR, ERα, ERß, SRD5A1, SRD5A2 were measured in BPH rat prostates and E2-stimulated human benign prostatic epithelial cells (BPH-1). RESULTS: EZF treatment significantly attenuated rat prostate enlargement, alleviated BPH pathological features, and decreased the expression of PCNA. The up-regulation of AR, ERα, SRD5A1/2 expressions, and down-regulation of ERß expression at prostate of rat BPH model were significantly blocked by EZF administration. The expression levels of testosterone, DHT, E2, PSA were strongly inhibited by EZF treatment. At the cellular level, ligustrosidic acid and echinocystic acid inhibited E2-induced BPH-1 cell proliferation and PCNA expressions, which were consistent with the results in vivo. And these two ingredients also down-regulated the expressions of AR, ERα, SRD5A1/2 and up-regulated the expression of ERß in BPH-1 cells. CONCLUSION: EZF, ligustrosidic acid from LLF and echinocystic acid from EH showed inhibitive effects on BPH via down-regulating prostatic AR, ERα, SRD5A1/2 expressions and up-regulating ERß expression.
Subject(s)
3-Oxo-5-alpha-Steroid 4-Dehydrogenase , Androgens , Drugs, Chinese Herbal , Eclipta , Ligustrum , Phytoestrogens , Prostatic Hyperplasia , 3-Oxo-5-alpha-Steroid 4-Dehydrogenase/metabolism , Aged , Androgens/pharmacology , Animals , Drugs, Chinese Herbal/pharmacology , Eclipta/chemistry , Estradiol/metabolism , Humans , Ligustrum/chemistry , Male , Membrane Proteins/metabolism , Phytoestrogens/pharmacology , Prostatic Hyperplasia/chemically induced , Prostatic Hyperplasia/drug therapy , Prostatic Hyperplasia/metabolism , Rats , Testosterone/metabolismABSTRACT
Eclipta alba (L.) is a valuable medicinal plant. However, its medicinal efficacy can be affected by geminivirus infection. Therefore, identification of healthy specimen is essential before to use as medicine. The present study provided the taxonomic characterization of geminivirus infected and healthy E. alba plant by studying apparent morphology and microscopic features through light and scanning electron microscopy. Before taxonomic characterization infected and healthy specimens were separated through molecular detection of geminivirus. Results of morphological studies reported that geminivirus infected E. alba plant showed systematic symptoms of infection like stunted growth, distortion and chlorosis of leaves, decrease in size of root, shoot and fruit, and so forth in comparison to healthy specimen. Anatomical findings reported that in both plants anomocytic and anisocytic types of stomata with multicellular warty trichomes were present. However, variations were observed in quantitative measures such as size of trichomes, epidermal, subsidiary and guard cells. Palynological observations identifies that both plants possessed tricolporate type of pollen but variation was mainly observed in size and shape of pollen, thickness of exine and intine, P/E ratio, pore size, interspecific difference, size of colpi, and pollen ornamentation. Overall this study concluded that both healthy and infected E. alba do not reported much variations in qualitative taxonomic features, but can be differentiated in terms of quantitative taxonomic evidences. Future studies are recommended for pharmacological analysis of both healthy and virus infected plants. RESEARCH HIGHLIGHTS: Eclipta alba has incredible therapeutic worth, but due to geminivirus infection the plant is affecting badly. Hence, the present studies give a comprehensive taxonomic report on the geminivirus infected and healthy plant species.
Subject(s)
Eclipta , Geminiviridae , Electrons , Microscopy, Electron, Scanning , Trichomes/ultrastructureABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: 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. AIM OF THE STUDY: We aimed to assess the effect of E. prostrata L. EtOH extract (EP) and elucidate the associated molecular mechanisms. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.
Subject(s)
Dermatitis, Atopic , Eclipta , Animals , Anti-Inflammatory Agents/adverse effects , Cytokines/metabolism , Dermatitis, Atopic/chemically induced , Dermatitis, Atopic/drug therapy , Dermatophagoides pteronyssinus/metabolism , Dinitrochlorobenzene , Humans , Inflammation/drug therapy , Mice , Mice, Inbred BALB C , Pyroglyphidae , SkinABSTRACT
BACKGROUND: Ecliptae prostrata (L.) L. has been widely used in East Asia with reported biological activities, including anti-cancer properties. OBJECTIVES: We aimed to investigate the effect of ethyl acetate extract of Ecliptae prostrata (L.) L. (EAE) and its component wedelolactone on the proliferation and migration of head and neck squamous cancer cells. METHODS: The proliferation of human SCC-4 and mouse CU110-1 tongue squamous carcinoma cells was assessed using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) method. Scratch wound assays were performed to assess cell migration rates. The levels of Ecadherin and vimentin were used as markers of the epithelial-to-mesenchymal transition (EMT). AhR, CYP1A1, and CYP1B1 levels were examined to uncover the mechanism of inhibition of cell migration by wedelolactone. RESULTS: We found that EAE and wedelolactone decreased the proliferation of human SCC-4 cells and mouse CU110-1 cells at doses of EAE at > 25 µg/ml and wedelolactone at > 6.25 µg/ml. Similarly, both EAE and wedelolactone produced inhibitory effects against migration, but the effective doses that significantly inhibited migration were lower than those affecting proliferation. Wedelolactone below 12.5 µg/ml inhibited the epithelial-to-mesenchymal transition (EMT) with increased expression of E-cadherin and decreased expression of vimentin in SCC-4 and CU110-1 cells. Further analysis showed wedelolactone inhibited the expression of AhR and its downstream target molecules CYP1A1 and CYP1B1 in both squamous carcinoma cells at the same doses inhibiting cell migration. The addition of benzo (a)pyrene [B(a)P], an agonist of AhR, stimulated migration, especially in the CU110-1 cells with reported cancer stem cell-like characteristics. Instructively, B(a)P reversed the inhibitory effects of wedelolactone on AhR expression and cell migration, suggesting that wedelolactone antagonizes cell migration through the AhR pathway. Moreover, the higher activity of EAE and wedelolactone against the migration of cancer stem-like CU110-1 cells relative to SCC-4 cells suggests selective activity against cancer stem cells. CONCLUSION: Our study identifies wedelolactone as a major active component of Ecliptae prostrata (L.) L. with promising anti-cancer properties against head and neck squamous cancer cells.
Subject(s)
Carcinoma, Squamous Cell , Eclipta , Humans , Mice , Animals , Vimentin/pharmacology , Cytochrome P-450 CYP1A1/pharmacology , Bromides/pharmacology , Cadherins , Carcinoma, Squamous Cell/drug therapy , Carcinoma, Squamous Cell/pathology , Epithelial-Mesenchymal Transition , Cell Movement , Cell Proliferation , Pyrenes/pharmacology , Cell Line, TumorABSTRACT
Exposure to N-nitroso compounds (NOCs) in our environment via pesticides, tobacco, and smoked meat can be potentially carcinogenic. The induction of N-N' ethylnitrosourea (ENU), a genotoxic NOC, leads to leukemogenesis. The study aimed to explore the ameliorating effect of the Ayurvedic herb Eclipta alba on the bone marrow cells of ENU-induced leukemic mice. Eclipta alba is investigated for its anti-cancer effect on various cell lines, but never on haematological malignant models. Theefficacy of the extract was explored on leukemia by changes in body weight, survivability, peripheral blood hemogram, bone marrow cytological, histological, and cell culture studies pre-and post-treatment. The treated group revealed significant immunomodulation of the expressional profile of NF-kB family and IL-1ß in marrow cells, by flow-cytometry, and immunofluorescence study. Through our experimental endeavour we depicted the cellular mechanism, signaling modality and tried to establish the anti-cancer potency of Eclipta alba on ENU-induced leukemia.
Subject(s)
Eclipta , Environmental Pollutants , Leukemia , Neoplasms , Pesticides , Animals , Disease Models, Animal , Environmental Pollutants/toxicity , Ethylnitrosourea/toxicity , Leukemia/chemically induced , Leukemia/metabolism , Leukemia/pathology , Mice , NF-kappa B , Pesticides/toxicity , Plant Extracts/pharmacology , Plant Extracts/therapeutic useABSTRACT
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.
Subject(s)
Coumarins/pharmacology , Eclipta , Environmental Pollutants , Ethylnitrosourea/toxicity , Plant Extracts/pharmacology , Animals , Eclipta/chemistry , Environmental Pollutants/toxicity , Inflammasomes , Mice , NLR Family, Pyrin Domain-Containing 3 ProteinABSTRACT
The overuse of cisplatin (>50 mg/m2) is limited to nephrotoxicity, ototoxicity, gastrotoxicity, myelosuppression, and allergic reactions. The objective of this study was to investigate the nephroprotective effects of Daucus carota and Eclipta prostrata extracts on cisplatin-induced nephrotoxicity in Wistar albino rats. The study involved male Wistar albino rats of 8 weeks weighing 220-270 g. A single injection of 5 mg/kg was injected into the rats for nephrotoxicity. Rats were divided into four groups based on dose conentrations. Blood and urine samples of rats were collected on the 0, 7th, 14th, and 21st days for nephrological analysis. The results showed that Cis + DC/Cis + EP (600 mg/kg) significantly (p < 0.001) increased the body weight and reduced the kidney weight of cisplatin-induced nephrotoxicity in rats (p < 0.001) as compared to Cis group. The results showed that 600 mg/kg administration of Cis + DC/Cis +EP successfully (p < 0.005) improved the urine and plasmin creatinine, Na, and K level compared to the Cis group. Histopathological results confirmed that Cis + EP/Cis + DC effectively improved the renal abnormalities. It is concluded that the co-administration of Cis + EP extract showed exceptional nephroprotective effects at a dose rate of 600 mg/kg.
Subject(s)
Cisplatin/adverse effects , Daucus carota/chemistry , Eclipta/chemistry , Kidney Diseases/chemically induced , Kidney Diseases/drug therapy , Protective Agents/therapeutic use , Animals , Body Weight/drug effects , Creatinine/blood , Kidney/drug effects , Kidney/pathology , Kidney Diseases/blood , Kidney Diseases/urine , Male , Organ Size/drug effects , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Potassium/urine , Protective Agents/pharmacology , Rats, Wistar , Sodium/urine , Urination/drug effectsABSTRACT
Eclipta prostrata (L.) L. (Syn.: Eclipta alba (L.) Hassak, Family: Asteraceae) is an important medicinal plant in the tropical and subtropical regions. It is widely used in treating various diseases of skin, liver and stomach in India, Nepal, Bangladesh, and other countries. The main aim of this review was to collect and analyze the available information on traditional uses, phytoconstituents, and biological activities of E. prostrata. The scientific information was collected from the online bibliographic databases such as Scopus, MEDLINE/PubMed, Google Scholar, SciFinder, etc. and books and proceedings. The active phytochemicals were coumestan derivatives, phenolic acid derivatives, flavonoids, triterpenoid and steroid saponins, substituted thiophenes, etc. Various extracts and isolated compounds of E. prostrata showed a wide range of biological activities such as antimicrobial, anticancer, hepatoprotective, neuroprotective and hair growth promoting activities. Relatively a few studies have been performed to reveal the exact phytoconstituents responsible for their corresponding pharmacological activities. Future studies should focus on detailed mechanism based studies using animal models and clinical studies.
Subject(s)
Eclipta , Asteraceae , Medicine, TraditionalABSTRACT
The UV-B-induced signals play a crucial role in improving the analeptic values of medicinally important plants. Eclipta alba L. (Hassak), commonly known as False Daisy, holds supreme stature with its pharmaceutical association in treating various ailments, particularly in Ayurvedic medicine. The present study aimed to evaluate the response of E. alba plants exposed to ambient (AT) and two different supplemental UV-B doses (eUV-B, ambient ±7.2 kJ m-2 day-1), i.e., intermittent (IT) and continuous (CT) UV-B treatment for 130 and 240 h respectively. Antioxidative activities and medicinally important compounds (wedelolactone) were measured in different plants' parts at three growth stages. Under both the eUV-B treatments, the photosynthetic pigments were adversely affected (along with reductions in protein content) with a concomitant increase in secondary metabolites. Substantial variations in enzymatic antioxidants and non-enzymatic compounds showed the adaptive resilience strategies of plants against eUV-B. The wedelolactone content increased in leaves but compromised in stem and roots under IT. The results concluded that IT UV-B exposure led to the improvement of plant growth and the yield of wedelolactone compared to CT, suggesting its ameliorative role in improving the test plant's medicinal value.
Subject(s)
Eclipta , Antioxidants , Coumarins , Plant Extracts/pharmacology , Ultraviolet RaysABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: 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. AIM OF THE STUDY: In this study, we explored the pharmacologic actions and potential molecular mechanisms underlying EZF's action in preventing and treating osteoporosis. MATERIALS AND METHODS: 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. RESULTS: 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). CONCLUSIONS: 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.