Antioxidant and Anti-Inflammatory Activity of the Ethanolic Extract of Euphorbia Hirta Leaf Extract: An In Vitro and In Silico Study.

Objectives: This study presents the antioxidant and anti-inflammatory activity of the ethanolic extract of Euphorbia hirta leaf extract. Materials and Methods: The antioxidant and anti-inflammatory activity of the extract was performed by in vitro assay. Our research employs a comprehensive approach combining experimental assays and computational simulations to assess the extract's potential bioactive components and their interactions with key biomolecules. Results: The study's results demonstrated a progressive rise in the percentage of inhibition, which was dependent on the dosage, in both antioxidant and anti-inflammatory activities. This trend was observed for both the extract and the standard, encompassing concentrations ranging from 100 to 500 µg/ml. Conclusion: The results showed that Euphorbia hirta's possesses antioxidant and anti-inflammatory activity, and this may contribute to a traditional medicinal. The discoveries of this study contribute to a deeper understanding of Euphorbia hirta's medicinal properties and its potential as a source of natural therapeutic agents.

In silico and in vitro studies for the identification of small molecular inhibitors from Euphorbia hirta Linn for rheumatoid arthritis: targeting TNF-α-mediated inflammation.

Rheumatoid arthritis (RA) is a chronic systemic autoimmune disease that is now potentially lethal and has a significant detrimental influence on people's daily lives by affecting bone joints. Inflammation plays a vital role in this type of autoimmune disorder. In rheumatoid arthritis, long-term production of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1) stimulates the immune system against cells in bone joints and helps to develop the pathogenesis of rheumatoid arthritis. So, while treating rheumatoid arthritis, we need to block these kinds of mechanisms. We employed soxhlet extraction, thin-layer chromatography (TLC), and gas chromatography-mass spectroscopy (GC-MS) to analyze the phytocompound information in E. hirta leaves. Furthermore, our research included in vitro investigations using Western blotting and mRNA expression analysis (TNF-α, IL-1ß, IL-6) to affirm the anti-inflammatory effectiveness of our extract. For identifying the lead-like molecules, virtual screening and molecular dynamics simulations were used. TLC results confirmed the presence of phytocompounds in E. hirta crude through spots. The structure elucidation of the phytocompounds was confirmed by the GC-MS chromatogram. The in vitro outcomes collectively underscore the inhibitory influence of E. hirta on cell proliferation and its capacity to attenuate the expression of TNF- α within THP-1 cells. The results of in silico methodologies confirmed six lead-like molecules. We could conclude that phytocompounds from ethanol leaf crude have effective lead-like molecules against the TNF-α.

Gallic acid a flavonoid isolated from Euphorbia hirta antagonizes gamma radiation induced radiotoxicity in lymphocytes in vitro.

OBJECTIVES: The current study was executed to isolate and evaluate gallic acid from Euphorbia hirta for in vitro radioprotective potentials against gamma irradiation caused radiotoxicity in human lymphocytes. METHODS: The defatted E. hirta plant material was treated to methanol extraction using the soxhlet device. Bioflavonoids were isolated from the E. hirta methanol extract using column chromatography. In human cells exhibited to gamma radiation, separated flavonoid gallic acid was examined for in vitro radioprotective potentials using the micronucleus test, DNA fragmentation assay, superoxide free radical scavenging method, and apoptic assay. RESULTS: The frequency of micronuclei was considerably declined when cells were preprocessed with gallic acid (25 g/mL) before being exhibited to 2 Gy gamma radiation, as determined by the cytokinesis blocked micronucleus test. Similarly, pre-gamma radiation treatment of human cells with gallic acid led in markedly less DNA injury, as assessed by comet metrics like olive tail moment and percent tail DNA. Gallic acid (25 g/mL) given to lymphocytes prior to gamma irradiation considerably decreased the percentage of apoptotic bodies. Gallic acid also considerably lowered the reactive oxygen species concentrations elicited by gamma radiation. CONCLUSIONS: Our findings showed that gallic acid protects lymphocytes isolated from human blood from gamma radiation-induced DNA destruction and anti-apoptotic activity, which could be because of inhibition of free radicals formed by gamma radiation as well as the decline of gamma radiation-induced oxidative stress.

Silver nanoparticles synthesized by Euphorbia hirta exhibited antibacterial activity and induced apoptosis through downregulation of PI3Kγ mediated PI3K/Akt/mTOR/p70S6K in human lung adenocarcinoma A549 cells.

Plant extracts were successfully applied to synthesize nanoparticles, and expected such biological processes of effective for chemotherapeutic applications and safe for human use. Our study planned to evaluate the anticancer efficacy of silver nanoparticles (AgNPs) synthesized by Euphorbia hirta on human lung adenocarcinoma A549 cells. The E. hirta synthesized Eh-AgNPs was investigated by UV-spectroscopy, X-ray diffraction, transmission electron microscopy, and Fourier-transform infrared spectroscopy examination. The bactericidal efficacy of Eh-AgNPs was studied by the agar well method, and the cytotoxicity on A549 cells was assessed by MTT assay. Results showed that Eh-AgNPs exhibited effective antibacterial activity against bacterial pathogens, established dose-dependent cytotoxicity on A549 cells, and persuaded apoptosis, as evidenced by increased lipid peroxidation and decreased levels of antioxidants. Eh-AgNPs significantly increased the early apoptosis in A549 cells in a concentration-dependent way. The Eh-AgNPs administration reduced the Bcl-2 expression; however, it increased the expression of p53, Bax, cleaved caspase-3 and -9 apoptotic members. Eh-AgNPs treatment reduced PI3Kγ, phospho-PI3K, phospho-Akt, phospho-mTOR, and p70S6K levels. The obtained results demonstrated that the Eh-AgNPs induce reactive oxygen species-mediated apoptosis by expressing p53, Bax, and inhibiting PI3K/Akt/mTOR/p70S6K signaling pathway.

Anti-Dengue Screening on Several Vietnamese Medicinal Plants: Experimental Evidences and Computational Analyses.

Worldwide, medicinal plants have been known for economic and geographical advantages, thus possibly holding potentiality against dengue hemorrhagic fever. The methanol/water extracts from different parts of fourteen Vietnam-based plant species were subjected for experimental screening on anti-dengue activity using baby hamster kidney cells (BHK21) and plaque reduction neutralisation test (PRNT). Firstly, the methanol/water extracts were tested against serotype dengue virus DENV-1. Seven out from nineteen extracts show the PRNT50 values less than 31.25 µg/mL. Four of the above extracts namely from Euphorbia hirta, Cordyline terminalis, Carica papaya, and Elaeagnus latifolia were chosen for testing against the serotype DENV-2. All of them exhibit good activity with the PRNT50 values less than 31.25 µg/ml, which were further fractionated to obtain hexane, ethyl acetate and butanol fractions. Anti-dengue virus activity of the fractions against four serotypes DENV-1, -2, -3 and -4 was evaluated. As results, the ethyl acetate fraction of Elaeagnus latifolia is highly active against all four serotype viruses. The structural formulae of its nine constituents were input for molecular docking simulation. The docking-based order for static inhibitability is 6-3L6P>7-3L6P>9-3L6P>2-3L6P>3-3L6P≈5-3L6P>9-3L6P>1-3L6P>8-3L6P; QSARIS-based analysis reveals the biocompatibility of the most promising ligands (4-7); ADMET-based analysis expects their pharmacological suitability. Exceptional finding on 2-3LKW hydrophilic interaction at Lys43 (with the associated Gibbs free energy of -10.3 kcal mol-1 ) raises an open explanation for inhibitory effects. The results encourage further investigations for more in-depth mechanisms and drug development, such as in vitro enzyme assays or in vitro clinical trials with natural substances from E. latifolia.

Interactive deciphering electron-shuttling characteristics of agricultural wastes with potential bioenergy-steered anti-COVID-19 activity via microbial fuel cells.

Background: This first-attempt study explored indigenous herbs from agricultural waste with bioenergy and biorefinery-stimulating potentials for possible anti-COVID-19 drug development. As prior novel study revealed, medicinal herbs abundant in ortho-dihydroxyl substituents and flavonoid-bearing chemicals were likely not only electron shuttle (ES)-steered, but also virus transmission-resisted. Methods: Herbal extract preparation from agricultural wastes were implemented via traditional Chinese medicine (TCM) decoction pot. After filtration and evaporation, a crude extract obtained was used for evaluation of bioenergy-stimulating and electron-mediating characteristics via microbial fuel cells (MFCs). Combined with cyclic voltammetric analysis, MFCs provided a novel platform to distinguish electron shuttles from antioxidants with electron-transfer steered antiviral potentials of herbal extracts. Significant findings: After 50 serial cyclic voltammogram traces, considerable ES activities of herbal extracts still stably remained, indicating that possible medication-associated capabilities could be persistent. This work also extended to explore bioenergy-stimulating herbs from agricultural waste recycling for bioenergy and biorefinery applications. Water extract of Coffea arabica was more biotoxic than ethanolic extract, resulting in its lower power-generating capability. The findings revealed that water extract of Trichodesma khasianum and Euphorbia hirta could exhibit considerable bioenergy-enhancing effects. For cradle-to-cradle circular economy, agricultural waste could be specifically screened for possible regeneration of value-added anti-COVID-19 drugs via bioenergy selection.

Formulation, characteristics and anti-bacterial effects of Euphorbia hirta L. mouthwash.

Objective: Mouthwash is a liquid solution used to improve oral health and breath freshness as well as reduce oral bacteria. This study aims to formulate a Euphorbia hirta L. ethanol extract for mouthwash, evaluate the physical properties, and determine its anti-bacterial effects against Streptococcus mutans. Methods: Each mouthwash formula was created by utilising a solubilisation technique. Three mouthwash formulas were created from different concentrations of Euphorbia hirta L. ethanol extract (0.5%, 1%, and 2%), and referred to as F1, F2, and F3. The organoleptic properties, pH levels, specific gravity, viscosity, flow properties, stability, irritation level, contact time, and anti-bacterial effects were evaluated for each concentration. Result: The resulting formulas featured a distinctive smell of oleum menthae piperitae and had a sweet and spicy taste. These characteristics remained unaffected during storage. The acidity levels ranged from 4.59 to 6.0, the weight masses ranged from 0.9693 to 1.0710 g/ml, and the viscosity ranged from 1.50 to 3.00 cP. F3 concentration was non-irritating with mucus production at 11.325%, had lower contact time with a neutralisation of 57.14% of Streptococcus mutans colonies in 30 seconds, and showed stable anti-bacterial control against Streptococcus mutans (p = 0.000) within the first week of use. Conclusion: The study results offer the first proof of Euphorbia hirta L. used for improving human health. The formulation features the ideal physical and stability characteristics of mouthwash, and possesses anti-bacterial properties that can potentially combat Streptococcus mutans. Clinical use of the formulated mouthwash must be explored in future research.

Euphorbia hirta Leaf Ethanol Extract Suppresses TNF-α/IFN-γ-Induced Inflammatory Response via Down-Regulating JNK or STAT1/3 Pathways in Human Keratinocytes.

Skin inflammation may cause allergic diseases such as allergic rhinitis, asthma, and atopic dermatitis. Euphorbia hirta (E. hirta) is a member of the Euphorbiaceae family and is well-known for its anti-asthma effects. E. hirta has traditionally been used to treat respiratory ailments, dysentery, jaundice, and digestive problems. However, its effects on skin inflammation remain unclear. Here, we determined the effects of 70% ethanol extract of E. hirta leaves (ELE) in vitro using human keratinocyte HaCaT cells, which constitute most epidermal skin cells. We determined the inhibitory effects of ELE on the inflammation caused by tumor necrosis factor (TNF)-α/interferon (IFN)-γ in keratinocytes using ELISA, immunoblotting, and qRT-PCR assay. ELE was found to reduce the production and mRNA expression of pro-inflammatory cytokines such as TNF-α or interleukin-6 and the expression of various proteins, including signal transducers, activators of transcription 1/3, and mitogen-activated protein kinase. Expression levels of these proteins were found to be upregulated in the TNF-α/IFN-γ-stimulated condition and downregulated by ELE treatment. These results indicate that ELE protects HaCaT cells against TNF-α/IFN-γ-induced skin inflammation.

Assessing a Medicinally Important Common Indian Weed Growing in the Arsenic-Affected Areas of West Bengal, India, Considering Its Impact on Human Health.

Euphorbia hirta is used traditionally for medicinal purposes. A vast stretch of land in West Bengal is arsenic affected, where agricultural activities present the hazard of arsenic entering the food chain putting the entire community at health risk. The present work tried to study if these areas could be safely utilized to grow this medicinal plant. In this study, the medicinal plant Euphorbia hirta and a known hyperaccumulator Brassica juncea were exposed to a high level of arsenic, and after a certain span of time, arsenic translocation in both the plants was checked. The data revealed that Euphorbia hirta is not a hyperaccumulator and does not translocate high levels of arsenic to the aerial parts of the plant as compared to Brassica juncea. It was also found that the biochemical and genetic effects of arsenic stress were enhanced significantly more in Brassica juncea than in Euphorbia hirta. Thus, the present study points to the growth potential of the common medicinal weed Euphorbia hirta in the arsenic-affected areas without being a cause of human health concern.

Lignans from Euphorbia hirta L.

Five new lignans, euphorhirtins A-D (1-4), 5-methoxyvirgatusin (5), three artefacts, 7S-ethoxyisolintetralin (6), 7R-ethoxyisolintetralin (7), and 7R-ethoxy-3-methoxyisolintetralin (8), together with 13 known ones (9-21) were isolated from the medicinal plant Euphorbia hirta L. The structures of the compounds were elucidated by means of extensive spectroscopic analysis, including 1D and 2D NMR and HR-ESI-MS experiments. The absolute configurations of compound 1 was determined by ECD calculation. The isolates were evaluated for their inhibitory effects against the proliferation of the cancer cell lines (Hep G2, A549, and DU145) and compounds 14 and 18 showed inhibitory activity against the Hep G2 cells with IC50 values 7.2 ± 0.17 and 8.5 ± 0.36 µM.

Pharmacological evaluation of Euphorbia hirta, Fagonia indica and Capparis decidua in hypertension through in-vivo and in vitro-assays.

OBJECTIVE: This study determines the efficacy and probable underlying mode of action to the folk usage of Euphorbia hirta, Fagonia indica and Capparis decidua in hypertension. METHODS: The aqueous-methanol extracts of E. hirta (EH.Cr), F. indica (FI.Cr) and C. decidua (CD.Cr) were tested for antihypertensive effects in rats using non-invasive and in-vasive blood pressure measuring apparatus. In-vitro assays were carried out using isolated rat aortae using PowerLab station. RESULTS: EH.Cr, FI.Cr and CD.Cr at 500 mg/kg (orally) caused a fall in the mean systolic blood pressure in arsenic-induced hypertensive and normotensive rats, similar to nifedipine. In rat aortae, EH.Cr, CD.Cr and FI.Cr reversed low (20 mM), high (80 mM) K+ and phenylephrine (P.E)-driven contractions, while F. indica partially inhibited high K+ contractions. In the presence of TEA, F. indica remained unable to relax low K+ contractions. EH.Cr and CD.Cr moved Ca++ concentrations response curves to the right, like nifedipine. All fractions of EH.Cr and CD.Cr except aqueous, pet-ether and chloroform fractions of FI.Cr displayed Ca++ antagonistic activity. FI.Cr, its ethyl acetate and aqueous fraction exhibited TEA-sensitive potassium channel activation. On baseline tension, test materials also produced phentolamine-sensitive vasospasm. CONCLUSION: E. hirta, F. indica and C. decidua possess antihypertensive activity in arsenic-induced hypertensive rats possibly mediated via endothelium-dependent vasorelaxation. In normotensive rats, E. hirta and C. decidua showed antihypertensive activities through endothelium-dependent and Ca++ antagonistic pathways, while F. indica exhibited potassium channel activation and Ca++ antagonistic like effects in its vasorelaxation. Additional weaker vasospastic effects were derived through α-adrenergic like pathways.

In vitro antiviral activity of peptide-rich extracts from seven Nigerian plants against three non-polio enterovirus species C serotypes.

BACKGROUND: As frequent viral outbreaks continue to pose threat to public health, the unavailability of antiviral drugs and challenges associated with vaccine development underscore the need for antiviral drugs discovery in emergent moments (endemic or pandemic). Plants in response to microbial and pest attacks are able to produce defence molecules such as antimicrobial peptides as components of their innate immunity, which can be explored for viral therapeutics. METHODS: In this study, partially purified peptide-rich fraction (P-PPf) were obtained from aqueous extracts of seven plants by reverse-phase solid-phase extraction and cysteine-rich peptides detected by a modified TLC method. The peptide-enriched fractions and the aqueous (crude polar) were screened for antiviral effect against three non-polio enterovirus species C members using cytopathic effect reduction assay. RESULTS: In this study, peptide fraction obtained from Euphorbia hirta leaf showed most potent antiviral effect against Coxsackievirus A13, Coxsackievirus A20, and Enterovirus C99 (EV-C99) with IC50 < 2.0 µg/mL and selective index ≥ 81. EV-C99 was susceptible to all partially purified peptide fractions except Allamanda blanchetii leaf. CONCLUSION: These findings establish the antiviral potentials of plants antimicrobial peptides and provides evidence for the anti-infective use of E. hirta in ethnomedicine. This study provides basis for further scientific investigation geared towards the isolation, characterization and mechanistic pharmacological study of the detected cysteine-rich peptides.

The complete chloroplast genome of Euphorbia hirta (Euphorbiaceae), a commonly used medicinal plant in China.

Plants in the genus Euphorbia have been widely used as herbal medicine, and for ornamental horticulture and biofuel production. In this study, we report the complete chloroplast genome of Euphorbia hirta which is known as the 'asthma-plant' due to its medicinal use. The chloroplast genome of this species is 164,340 bp in length, including a pair of inverted repeat regions (IRs) (27,354 bp) that are divided by a large single-copy region (LSC) (91,373 bp) and a small single-copy region (SSC) (18,259 bp). The chloroplast genome of E. hirta contains 111 unique genes (77 protein-coding, 30 tRNA, and four rRNA), 19 of which are duplicated in the IR regions. The overall GC content is 35.4%. Phylogenetic analysis fully resolved E. hirta groups with other species of Euphorbia. The complete chloroplast genome of E. hirta provides useful information that can be used to distinguish related species and reconstruct evolutionary relationships.

Phytochemicals of Euphorbia hirta L. and Their Inhibitory Potential Against SARS-CoV-2 Main Protease.

Euphorbia hirta L. is a medicinal plant widely used in the Philippines and across tropical Asia against various diseases, including respiratory disorders. In this study, the phytochemical components of E. hirta were investigated in silico for their potential to inhibit the severe acute respiratory syndrome-coronavirus-2 main protease (SARS-CoV-2 Mpro), a coronavirus disease 2019 (COVID-19) drug target that plays a critical role in the infection process of SARS-CoV-2. Phytochemical mining in tandem with virtual screening (PM-VS) was the strategy implemented in this study, which allows efficient preliminary in silico assessment of the COVID-19 therapeutic potential of the reported phytochemicals from the plant. The main rationale for considering E. hirta in the investigation was its reported efficacy against respiratory disorders. It is very promising to investigate the phytochemicals of E. hirta for their potential efficacy against diseases, such as COVID-19, that also target the respiratory system. A total of 298 E. hirta phytochemicals were comprehensively collected from the scientific literature. One hundred seventy of these phytochemicals were computed through molecular docking and were shown to have comparable or better binding properties (promising inhibitors) toward SARS-CoV-2 Mpro than known in vitro inhibitors. In connection to our previous work considering different medicinal plants, antiviral compounds were also rediscovered from the phytochemical composition of E. hirta. This finding provides additional basis for the potential of the plant (or its phytochemicals) as a COVID-19 therapeutic directly targeting drug targets such as SARS-CoV-2 Mpro and/or addressing respiratory-system-related symptoms. The study also highlights the utility of PM-VS, which can be efficiently implemented in the preliminary steps of drug discovery and development.

Phytochemical composition analysis and evaluation of in vitro medicinal properties and cytotoxicity of five wild weeds: A comparative study.

Background: Medicinal plants are a source of phytochemicals and they are used for the treatment of several oxidative stress-related or other diseases for their effectiveness, low toxicity and easy availability. Five traditionally used and less characterized herbaceous weeds of West Bengal, India, namely, Heliotropium indicum, Tridax procumbens, Cleome rutidosperma, Commelina benghalensis and Euphorbia hirta, were investigated for the current research study. Methods: Aqueous and 70% ethanolic extracts of the leaves were analyzed for estimation of essential phytochemicals and to evaluate their in vitro antioxidant status, medicinal properties and cytotoxic effects. To the best of our knowledge, several assays and comparative evaluations using these herbs are reported for the first time. For quantitative study, UV-vis spectrophotometry and high-performance liquid chromatography with diode array detector HPLC-DAD techniques were used. Antibacterial properties were investigated using the Kirby-Bauer disc diffusion method. For in vitro anti-lithiatic study, a titration method was used. The cell viability assay was done using peripheral blood mononuclear cells. Results: The aqueous extract exhibits higher content of polyphenols, flavonoids, tannins and inhibition percentage values for free radical scavenging assays, whereas the 70% ethanolic extract exhibits higher content of alkaloids and cardiac glycosides. HPLC-DAD analysis of 70% ethanolic extracts led us to identify 10 predominant phenolic constituents. Euphorbia hirta extracts showed minimum cytotoxicity (cell death ~2.5% and 4% in water and 70% ethanolic extract, respectively ), whereas Cleome rutidosperma and Tridax procumbens' 70% ethanolic extracts showed higher cell death (~13% and 28%, respectively), compared with the control (cell death ~10-12%). Conclusions: The study concluded that of all the medicinal weeds selected for the current study, Euphorbia hirta possesses the highest amount of bioactive compounds and hence exhibits the highest in vitro antioxidant activity and promising in vitro medicinal properties.

Spray-Drying Microencapsulation of High Concentration of Bioactive Compounds Fragments from Euphorbia hirta L. Extract and Their Effect on Diabetes Mellitus.

The present study was performed to spray-dry the high concentration of bioactive compounds from Euphorbia hirta L. extracts that have antidiabetic activity. The total phenolic content (TPC) and total flavonoid content (TFC) of four different extracts (crude extract, petroleum ether extract, chloroform extract and ethyl acetate extract) from the dried powder of Euphorbia hirta L. were determined using a spectrophotometer. After that, the fragment containing a high number of bioactive compounds underwent spray-dried microencapsulation to produce powder which had antidiabetic potential. The total phenolic content values of the crude extract, petroleum ether extract, chloroform extract and ethyl acetate extract were 194.55 ± 0.82, 51.85 ± 3.12, 81.56 ± 1.72 and 214.21 ± 2.53 mg/g extract, expressed as gallic acid equivalents. Crude extract, petroleum ether extract, chloroform extract and ethyl acetate extracts showed total flavonoids 40.56 ± 7.27, 29.49 ± 1.66, 64.99 ± 2.60 and 91.69 ± 1.67 mg/g extract, as rutin equivalents. Ethyl acetate extract was mixed with 20% maltodextrin in a ratio of 1:10 to spray-dry microencapsulation. The results revealed that the moisture content, bulk density, color characteristic, solubility and hygroscopicity of the samples were 4.9567 ± 0.00577%, 0.3715 ± 0.01286 g/mL, 3.7367 ± 0.1424 Hue, 95.83 ± 1.44% and 9.9890 ± 1.4538 g H2O/100 g, respectively. The spray powder was inhibited 51.19% α-amylase at 10 mg/mL and reduced 51% in fast blood glucose (FBG) after 4 h treatment. Furthermore, the administration of spray powder for 15 days significantly lowered the fast blood glucose level in streptozotocin-diabetic mice by 23.32%, whereas, acarbose-a standard antidiabetic drug-and distilled water reduced the fast blood glucose level by 30.87% and 16.89%. Our results show that obtained Euphorbia hirta L. powder has potential antidiabetic activity.

Anti-nociceptive Effect of Euphorbia hirta Leaf Extract: Involvement of Adenosine, Cholinergic, and Opioid Receptors.

OBJECTIVE: The study was designed to investigate the anti-nociceptive activity of Euphorbia hirta leaf and its possible mechanism of action. METHODS: The extract of Euphorbia hirta obtained from the leaf was prepared as per standard procedures and evaluated at the three doses (300, 600, and 1200 mg/kg, i.p). The extract was screened for anti-nociceptive activity using heat-induced (tail-flick) and chemical-induced (acetic acid-induced writhing and formalin-induced paw lick) nociception models in mice. The possible mechanism of action of the extract was evaluated using antagonists of notable nociceptive pathways. RESULTS: Intraperitoneal administration of Euphorbia hirta extract at the doses of 600 and 1200 mg/kg significantly (p<0.05) reduced the formalin-induced paw licking in both neurogenic and inflammatory phases of the test. While administration of the extract at the dose of 300 mg/kg significantly inhibited the pain due to formalin in the inflammatory phase but not in the neurogenic phase. The anti-nociceptive effect of Euphorbia hirta extract increased the reaction time to thermal stimulus, also inhibited the acetic acid-induced writhing dose-dependently. The antinociceptive effect exhibited by Euphorbia hirta extract in the formalin test was reversed by the administration of naloxone, theophylline, and atropine. Glibenclamide, nifedipine, and yohimbine, however, did not significantly block the anti-nociceptive effect of the extract. Meanwhile, methylene blue administration enhanced the anti-nociceptive effect of the extract. CONCLUSION: The results indicated that Euphorbia hirta extract produces a dose-related antinociceptive effect in several models of chemical and thermal pain, through mechanisms that might involve interaction with adenosine, cholinergic, and opioid receptors.

Antityrosinase Activity of Combretum micranthum, Euphorbia hirta and Anacardium occidentale Plants: Ultrasound Assisted Extraction Optimization and Profiling of Associated Predominant Metabolites.

Tyrosinase is an important component of the enzyme polyphenol oxidase, which upon contact with the phenolic substrates forms the pigment melanin and induces undesirable food browning. The phenolic and triterpenoid compounds that naturally occur in plants are well known as tyrosinase inhibitors. Combretum micranthum (CM) leaves, Euphorbia hirta (EH) plant, and Anacardium occidentale (AO) fruits are traditionally known to have potential anti-tyrosinase activities. The aim of this study was to optimize the ultrasound-assisted extraction of secondary metabolites from these matrices, and to evaluate in tubo the antityrosinase activity of these extracts. Efforts were also taken to profile the secondary metabolites, mainly the phenolic and triterpenoid compounds, in order to understand their probable association with tyrosinase inhibition. The optimal ultrasound-assisted extraction conditions for simultaneous extraction of phenolic, and triterpenoid compounds were determined. The aqueous fraction of these extracts showed significant antityrosinase activity, with the CM leaves exhibiting the strongest inhibitory effect (IC50 of 0.58 g·L-1). The predominant metabolic compounds from these natural extracts were putatively identified by using a high-resolution quadrupole-time of flight (QToF) LC-MS instrument. The high-resolution accurate mass-based screening resulted in identification of 88 predominant metabolites, which included dihydrodaidzein-7-O-glucuronide, micromeric acid, syringic acid, morin, quercetin-3-O-(6″-malonyl-glucoside), 4-hydroxycoumarin, dihydrocaffeic acid-3-O-glucuronide, to name some, with less than 5 ppm of mass error.

Phytochemical analysis and in vitro cytostatic potential of ethnopharmacological important medicinal plants.

Annonareticulate (Mart.), Lablab purpureus (L.) Sweet, Murrayakoenigii (L.) Spreng, Moringaoleifera (Lam.), Hibiscussabdariffa (L.) and Euphorbiahirta (L.) are most commonly used medicinal plants by the traditional healers of Karbi Anglong district of Assam, India against different human ailments including cancer suspected cases. The proposed study includes field survey related to ethnomedicinal aspects of medicinal plants, phytochemical analysis, and evaluation of their cytostatic potential with the possible mode of action against Dalton's lymphoma (DL) cell line. The phytochemical analysis of all the plant's extract was studied using standard protocol. The cytotoxicity of the methanol extracts was determined by MTT reduction assay. The effect of the same extract was also tested for development of apoptosis features in DL cells using a fluorescence microscope and flowcytometry. The underlying mechanism closely associated with apoptotic cell death was also studied by measuring reactive oxygen species (ROS), mitochondrial membrane potential, and expression level of apoptosis inducing proteins. Murraya koenigii induced more apoptotic features in DL cells, followed by Annona reticulate. The decrease in mitochondrial membrane potential, release of cytochrome- c, increase in ROS level and higher expression of caspases (3 and 9) after plant extracts treatment may cause involvement of mitochondria in the process of apoptosis. From this study, it can be concluded that the plant species mainly Murraya koenigi and Annona reticulate significantly induced cytotoxicity in DL cells through apoptosis by utilizing mitochondrial pathway.

The use of Euphorbia hirta L. (Euphorbiaceae) in diarrhea and constipation involves calcium antagonism and cholinergic mechanisms.

BACKGROUND: Euphorbia hirta (Linn) family Euphorbiaceae has been used in indigenous system of medicine for the treatment of gastrointestinal disorders. This study was designed to determine the pharmacological basis for the medicinal use of E. hirta in diarrhea and constipation. METHODS: The aqueous-methanol extract of whole herb of E. hirta (EH.Cr) and its petroleum ether (Pet.EH), chloroform (CHCl3.EH), ethyl acetate (Et.Ac.EH) and aqueous (Aq.EH) fractions were tested in the in-vivo experiments using Balb/c mice, while the in-vitro studies were performed on isolated jejunum and ileum preparations of locally bred rabbit and Sprague Dawley rats, respectively, using PowerLab data system. RESULTS: Qualitative phytochemical analysis showed the presence of alkaloids, saponins, flavonoids, tannins, phenols, cardiac glycosides, while HPLC of EH.Cr showed quercetin in high proportion. In mice, EH.Cr at the dose of 500 and 1000 mg/kg showed 41 and 70% protection from castor oil-induced diarrhea, respectively, similar to the effect of quercetin and loperamide, while at lower doses (50 and 100 mg/kg), it caused an increase in the fecal output. In loperamide-induced constipated mice, EH.Cr also displayed laxative effect with respective values of 28.6 and 35.3% at 50 and 100 mg/kg. In rabbit jejunum, EH.Cr showed atropine-sensitive inhibitory effect in a concentration-dependent manner, while quercetin and nifedipine exhibited atropine-insensitive effects. Fractions of E. hirta also produced atropine-sensitive inhibitory effects except Pet.EH and CHCl3.EH. On high (80 mM) and low (20 mM) K+ - induced contractions, the crude extract and fractions exhibited a concentration-dependent non-specific inhibition of both spasmogens and displaced concentration-response curves of Ca++ to the right with suppression of the maximum effect similar to the effect quercetin and nifedipine. Fractions showed wide distribution of spasmolytic and Ca++ antagonist like effects. In rat ileum, EH.Cr and its fractions exhibited atropine-sensitive gut stimulant effects except Pet.EH. CONCLUSION: The crude extract of E. hirta possesses antidiarrheal effect possibly mediated through Ca++ antagonist like gut inhibitory constituents, while its laxative effect was mediated primarily through muscarinic receptor agonist like gut stimulant constituents. Thus, these findings provide an evidence to the folkloric use of E. hirta in diarrhea and constipation.