Euphorbia Humifusa Willd Research Articles

In vitro Adipocyte Differentiation Inhibition and in vivo Effects on Lipid Metabolism in High-Fat Diet-Induced Obesity of Euphorbia humifusa.

Euphorbia humifusa Willd (Euphorbiaceae) is a functional raw material with various pharmacological activities. This study aimed to validate the inhibitory effect of Euphorbia humifusa extract (EHE) on adipocyte differentiation in vitro and in a high-fat-diet (HFD)-induced mouse model to evaluate the E.a humifusa as a novel anti-obesity and lipid metabolism enhancer agent. EHE effects on obesity and lipid metabolism were assessed in HFD-induced obese mice after 4-week treatments. Results were compared among four treatment groups (n = 7/group): low fat diet (LFD), high fat diet (HFD), and HFD-induced obese mice treated with either 100 or 200 mg/kg/day EHE (EHE100 and EHE200, respectively). EHE (50 to 200 μg/ml) and quercetin (50 μg/ml) significantly reduced 3T3-L1 preadipocyte differentiation (p < 0.001), in a concentration-dependent manner. EHE affected lipid metabolism, as evidenced by changes in serum lipid components. The HFD-EHE100 and HFD-EHE200 groups exhibited significantly (p < 0.05) reduced triglycerides (TG, 97.50 ± 6.56 and 82.50 ± 13.20 mg/dL, respectively) and low-density lipoprotein-cholesterol (LDL-c: 40.25 ± 4.99 and 41.25 ± 6.36 mg/dL, respectively) compared to the HFD group (TG: 129.25 ± 19.81 mg/dL; LDL-c: 51.75 ± 11.59 mg/dL). Haematoxylin and Eosin (H&E) and Oil red O staining showed that EHE markedly reduced lipid accumulation and inhibited lipogenesis in the liver. Interestingly, EHE significantly (p < 0.01) reduced the expression of adipogenic transcription factors in liver tissue. Our results indicated that EHE has the potential to be a therapeutic agent for addressing obesity and lipid metabolism.

Anti-inflammatory activities of triterpenoids from Euphorbia humifusa Willd

Anti-inflammatory activities of triterpenoids from Euphorbia humifusa Willd

Antibacterial and hemostatic polyvinyl alcohol/microcrystalline cellulose reinforced sodium alginate breathable dressing containing Euphorbia humifusa extract based on microfluidic spinning technology

Antibacterial hemostatic medical dressings have become feasible solutions in response to the challenging wound-healing process. In this study, a novel fiber-type medical dressing with excellent breathable, antibacterial, and hemostatic qualities was created using sodium alginate (SA), microcrystalline cellulose (MCC), polyvinyl alcohol (PVA), and Euphorbia humifusa Willd (EHW) based on microfluidic spinning technology, and the properties of the dressing were characterized. The orthogonal test demonstrates that PVA and MCC can enhance the mechanical properties of the fiber, which is a crucial requirement for fiber assembly to form the dressing. Moreover, the presence of EHW enhances the dressing's antibacterial and hemostatic qualities. The dressings have been proven to have potent antibacterial and hemostatic properties as well as the ability to considerably speed up wound healing and skin tissue regeneration in the in-vitro and in-vivo tests. In conclusion, this innovative fiber-type medical dressing containing SA, MCC, PVA, and EHW has enormous potential for managing wounds caused by bacteria.

A new anti-vitiligo unsaturated fatty glycoside from Euphorbia humifusa Willd

A new unsaturated fatty glycoside Humionoactosides A, together with four known compounds were isolated from the whole plant of Euphorbia humifusa Willd. Their structures were identified by MS/MS, NMR and ECD spectroscopic analyses, and comparison with the literature data. All compounds were evaluated for the effect on melanogenesis and tyrosinase activity use B16 cells in vitro, and the results showed that compound 1 could significantly improve the formation of melanin (138.7%, 50 μM) and tyrosinase activity (137.2%, 50 μM) compared with the positive control 8-MOP (125.2%, 138.9%, 50 μM) in a dose-dependent manner. This is the first time that those compounds reported from Euphorbia humifusa Willd. with potential anti-vitiligo activity.

Determination of three active components in Euphorbia humifusa willd. Using high-performance liquid chromatography with diode-array detection and autophagy and apoptosis analysis of normal rat kidney and hela cells

Background: Euphorbia humifusa Willd. (EH) is a kind of Chinese medicinal plant belonging to the family Euphorbiaceae, which is traditionally used for influenza, jaundice, hepatitis B virus, hypotension, inflammation, etc. In a modern study, active ingredients of EH reported to exhibit antioxidant, anticancer, and other properties. However, there are few reports showing that EH and its active compounds have inhibitory effects on cervical cancer through autophagy and apoptosis. Objective: To evaluate the anticervical cancer activity of EH and its main active ingredient Gallic acid (GA) by studying on autophagy and apoptosis of normal rat kidney (NRK) and HeLa cell lines, respectively. Materials and Methods: GA, kaempferol (KA), and quercetin (QU) are the main active compounds of EH. Identification and quantification of three substances from four batch samples obtained from four areas in Xinjiang were analyzed by high-performance liquid chromatography with diode-array detection. The potent effects of EH on anticervical cancer were investigated through autophagy and apoptosis in HeLa and NRK cells with varying concentrations of extracts and active compound GA treatment. The antiproliferation activity against HeLa cells was evaluated by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay. Autophagy and apoptosis in NRK and HeLa cells were observed by laser scanning confocal microscope. Quantitative data of apoptosis were estimated by Hoechst staining and Annexin-V binding assay using flow cytometry. The expression levels of autophagy-related protein (LC3 and P62) were subjected to western blot. Moreover, the autophagic vacuoles and other ultrastructures of cells were observed under transmission electron microscopy. Results: The contents of GA, KA, and QU were measured as 2.3342–3.4688, 0.4636–1.5922, and 0.9349–3.1500 mg/g, respectively. We used different concentrations of GA and the extracts of EH to treat with the line of cells, respectively. The best concentration of GA, water, and ethanol extracts inducing autophagy was 25 μg/ml, 10 mg/ml, and 10 mg/ml, respectively. The autophagy mediated with EH induced the accumulation of autophagosome, and even resulted in apoptosis. Conclusion: From our study, these results indicated that EH and GA may induce both autophagy and apoptosis in NRK and HeLa cells. The activity we studied on autophagy and apoptosis of HeLa cells may provide a new foundation for cervical cancer therapy or other related applications. Abbreviations used: EH: Euphorbia humifusa Willd.; HPLC-DAD: High-performance liquid chromatography with diode-array detection; NRK: Normal rat kidney; GA: Gallic acid; FC: Flow cytometry; LSCM: Laser scanning confocal microscope; MTT: 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide; TEM: Transmission electron microscopy; KA: Kaempferol; QU: Quercetin; LC3: The light chain 3; DMEM: Dulbecco's Modified Eagle's medium; FBS: Fetal bovine serum; DMSO: Dimethyl sulfoxide; PBS: Phosphate-buffered saline; PI: Propidium iodide; IC50: Half-maximal inhibitory concentration; BFA: Bafilomycin A1.

Jiangtang decoction ameliorate diabetic nephropathy through the regulation of PI3K/Akt-mediated NF-\u03baB pathways in KK-Ay mice

BackgroundJiangtang decoction (JTD) is a China patented drug which contains Euphorbia humifusa Willd, Salvia miltiorrhiza Bunge, Astragalus mongholicus Bunge, Anemarrhena asphodeloides Bunge, and Coptis chinensis Franch. For decades, it has also been used clinically to treat diabetic nephropathy (DN) effectively; however, the associated mechanisms remain unknown. Thus, the present study aimed to examine the protective efficacy of JTD in DN and elucidate the underlying molecular mechanisms.MethodsA diabetic model using KK-Ay mice received a daily administration of JTD for 12 weeks. Body weight, blood glucose, triglycerides (TGs), total cholesterol (TC), urea nitrogen (UN), creatinine (Cr), and microalbumin/urine creatinine (MA/UCREA) was measured every 4 weeks. Furthermore, on the day of the sacrifice, blood, urine, and kidneys were collected to assess renal function according to general parameters. Pathological staining was performed to evaluate the protective renal effect of JTD. In addition, the levels of inflammatory cytokines (tumor necrosis factor-α [TNF-α], interleukin [IL]-6 and intercellular adhesion molecule [ICAM]-1), insulin receptor substrate [IRS]-1, advanced glycation end products [AGEs], and receptor of glycation end products [RAGE] were assessed. Finally, the phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) signaling pathway and involvement of nuclear factor-κB (NF-κB) was further analyzed.ResultsAfter 12 weeks of metformin and JTD administration, the mice exhibited a significant amelioration in glucose and lipid metabolism dysfunction, reduced morphological changes in the renal tissue, decreased urinary albumin excretion, and normalized creatinine clearance. JTD treatment also reduced the accumulation of AGEs and RAGE, up-regulated IRS-1, and increased the phosphorylation of both PI3K (p85) and Akt, indicating that the activation of the PI3K/Akt signaling pathway was involved. Additionally, JTD administration reduced the elevated levels of renal inflammatory mediators and decreased the phosphorylation of NF-κB p65.ConclusionsThese results demonstrate that JTD might reduce inflammation in DN through the PI3K/Akt and NF-κB signaling pathways.

High-performance thin-layer chromatographic quantification of three active compounds in Euphorbia humifusa Willd. and TLC—DPPH test for screening antioxidant components

The aim of this study was to identify and quantitatively determine kaempferol, quercetin, and gallic acid in the methanol–water extract of the herb Euphorbia humifusa Willd. using high-performance thin-layer chromatography (HPTLC). The antioxidant compounds in E. humifusa Willd. were screened by thin-layer chromatography—1,1-diphenyl-2-trinitrobenzene hydrazine (TLC—DPPH). Kaempferol, quercetin, and gallic acid were used as the reference substances to optimize a highly suitable deployment system. Analysis was performed on silica gel G F254 plates with chloroform—ethyl acetate—formic acid with 5.2:4.4:1 proportion as the mobile phase. Antioxidant activity was screened preliminarily by spraying 10% DPPH ethanol solution on the developed silica gel plate. The quantification of E. humifusa Willd. was done at 300 nm for gallic acid and at 400 nm for quercetin and kaempferol. The linearity ranges of gallic acid, quercetin, and kaempferol were 0.168–0.448, 0.179–0.47, and 0.183–0.488 μg spot−1, respectively, wit...

Euphorbia humifusa Willd exerts inhibition of breast cancer cell invasion and metastasis through inhibition of TNFα-induced MMP-9 expression.

BackgroundBreast cancer is the most common type of malignancy in women worldwide. Euphorbia humifusa Willd (EuH) is a plant that is widely used as a traditional medicine. However, no systemic studies on the anti-cancer effects of EuH have been reported. The aim of this study is to evaluate the anti-metastatic effect of the EuH.MethodsEthyl acetate fraction was prepared from EuH methanol extracts (EA/EuH). Inhibitory effect of EA/EuH on cell migration was determined using an in vitro scratch-wound healing assay. The anti-invasive activity was determined by in vitro three-dimensional spheroid culture system and in vivo syngenic experimental lung metastasis experiment. Gene expression profiles were analyzed by using RT-PCR, real-time PCR, and luciferase reporter assay systems.ResultsEthyl acetate fraction from the EuH extract (EA/EuH) inhibited the migration and invasive capabilities of highly metastatic MDA-MB-231 breast cancer cells and attenuated syngeneic lung metastasis of mouse 4 T1 breast cancer cells in vivo. Mechanistically, EA/EuH decreased tumor necrosis factor alpha (TNFα)-induced matrix metalloproteinase (MMP)-9 mRNA expression through the inhibition of NF-κB activity in MDA-MB-231 cells.ConclusionEuH may be beneficial in the prevention of invasion and metastasis of early stage breast cancer and can be served as an anti-metastatic agent or adjuvant therapy against metastatic breast cancer.

Effect of Euphorbia humifusa Willd extract on the amelioration of innate immune responses

Euphorbia humifusa Willd is an annual plant widely used as a vegetable and traditional medicinal herb. E. humifusa Willd displays a variety of pharmacological actions; however, the effect of E. humifusa Willd on the innate immune response has not been well characterized. The aim of this study is to investigate the effect of an E. humifusa Willd methanolic extract (EuH) on the activation of innate immune cells. Here, we found that the EuH increased the expression of the innate cytokines, TNFα and IL-1β, in THP-1 monocytes and THP-1-derived macrophages. In addition, the EuH enhanced the phagocytosis of THP-1-derived macrophages. These findings suggest that E. humifusa Willd may be helpful for preventing bacterial infection and could be developed as a dietary supplement for ameliorating innate immune response.

A natural component from Euphorbia humifusa Willd displays novel, broad-spectrum anti-influenza activity by blocking nuclear export of viral ribonucleoprotein

The need to develop anti-influenza drugs with novel antiviral mechanisms is urgent because of the rapid rate of antigenic mutation and the emergence of drug-resistant viruses. We identified a novel anti-influenza molecule by screening 861 plant-derived natural components using a high-throughput image-based assay that measures inhibition of the influenza virus infection. 1,3,4,6-tetra-O-galloyl-β-D-glucopyranoside (TGBG) from Euphorbia humifusa Willd showed broad-spectrum anti-influenza activity against two seasonal influenza A strains, A/California/07/2009 (H1N1) and A/Perth/16/2009 (H3N2), and seasonal influenza B strain B/Florida/04/2006. We investigated the mode of action of TGBG using neuraminidase activity inhibition and time-of-addition assays, which evaluate the viral release and entry steps, respectively. We found that TGBG exhibits a novel antiviral mechanism that differs from the FDA-approved anti-influenza drugs oseltamivir which inhibits viral release, and amantadine which inhibits viral entry. Immunofluorescence assay demonstrated that TGBG significantly inhibits nuclear export of influenza nucleoproteins (NP) during the early stages of infection causing NP to accumulate in the nucleus. In addition, influenza-induced activation of the Akt signaling pathway was suppressed by TGBG in a dose-dependent manner. These data suggest that a putative mode of action of TGBG involves inhibition of viral ribonucleoprotein (vRNP) export from the nucleus to the cytoplasm consequently disrupting the assembly of progeny virions. In summary, TGBG has potential as novel anti-influenza therapeutic with a novel mechanism of action.

Antifungal Activity of Ellagic Acid In Vitro and In Vivo.

Ellagic acid (EA) has been shown to have antioxidant, antibacterial, and anti-inflammatory activities. In Uighur traditional medicine, Euphorbia humifusa Willd is used to treat fungal diseases, and recent studies suggest that it is the EA content which is responsible for its therapeutic effect. However, the effects of EA on antifungal activity have not yet been reported. This study aimed to investigate the inhibitory effect of EA on fungal strains both in vitro and in vivo. The minimal inhibitory concentration (MIC) was determined by the National Committee for Clinical Laboratory Standards (M38-A and M27-A2) standard method in vitro. EA had a broad spectrum of antifungal activity, with MICs for all the tested dermatophyte strains between 18.75 and 58.33 µg/ml. EA was also active against two Candida strains, with MICs between 25.0 and 75.0 µg/ml. It was inactive against Candida glabrata. The susceptibility of six species of dermatophytes to EA was comparable with that of the commercial antifungal, fluconazole. The most sensitive filamentous species was Trichophyton rubrum (MIC = 18.75 µg/ml). Studies on the mechanism of action using an HPLC-based assay and an enzyme linked immunosorbent assay showed that EA inhibited ergosterol biosynthesis and reduced the activity of sterol 14α-demethylase P450 (CYP51) in the Trichophyton rubrum membrane, respectively. An in vivo test demonstrated that topical administration of EA (4.0 and 8.0 mg/cm(2) ) significantly enhanced the cure rate in a guinea-pig infection model of Trichophyton rubrum. The results suggest that EA has the potential to be developed as a natural antifungal agent.

Anti-inflammatory components of Euphorbia humifusa Willd.

Two new compounds, euphorbinoside (1) and dehydropicrorhiza acid methyl diester (2), along with 24 known compounds (3–26) were isolated from Euphorbia humifusa Willd. The effects of these compounds on soluble epoxide hydrolase (sEH) inhibitory activity were evaluated. Flavonoid compounds (10–21) exhibited high sEH inhibitory activity. Among them, compounds 12, 13, and 19 greatly inhibited sEH enzymatic activity, with IC50 values as low as 18.05±1.17, 18.64±1.83, and 17.23±0.84μM, respectively. In addition, the effects of these compounds on lipopolysaccharide (LPS)-induced nitric oxide (NO) and tumor necrosis factor alpha (TNF-α) production by RAW 264.7 cells were investigated. Compounds 3–6, 8, 18, 20–23, and 25–26 inhibited the production of both NO and TNF-α, with IC50 values ranging from 11.1±0.9 to 45.3±1.6μM and 14.4±0.5 to 44.5±1.2μM, respectively.

Antimicrobial and Antitumor Activities of Crude Extracts and Isolated Compounds from Euphorbia humifusa

Euphorbia humifusa Willd. has been used in traditional Chinese medicine. Herein we report the isolation of its constituents and the testing results of their antimicrobial and antitumor activities. The results show that the crude petroleum ether, chloroform, ethyl acetate, butanol and residual methanol fractions exert such activities. Particularly, the crude petroleum ether and ethyl acetate fractions exhibit antigrowth activity against Staphyloccocus aureus with MIC 0.5 mg/mL. Petroleum ether and chloroform fractions significantly exhibit potent antigrowth activity against Caco-2 cells, with IC50 value of 0.059 and 0.025 mg/mL, respectively. The promising bioactivities of the crude petroleum ether fractions guided the first isolation of compounds: 24-methylene cycloartanone (2), dibutyl phthalate (3), hexacosanol (4) and bis-(2-ethylhexyl) phthalate (5) from this species. The antimicrobial activities of compounds 1-2 were evaluated. The tested compounds exhibit potent antigrowth activity against Staphyloccocus aureus, Escherichia coli and Canidia albicans.

The Application of Antibacterial Components of Euphorbia Humifusa Willd on Silk Fabrics

The minimal inhibitory concentration of the natural antibacterial components extracted from euphorbia humifusa willd (EHW) was investigated. The optimized fixation process and the antimicrobial activity of the treated silk fabrics were also studied. The results of the experiments indicated that the optimized fixation process parameters were extract concentration 60%, pH 4, 90°C and 60 minutes and the silk fabric had excellent antibacterial property. After 30 washing cycles the inhibitory rate of the silk fabric decreased from 100% to 61.8% and from, 89.31% to 67.86% against St.aureus and E. coli, respectively. A further treatment with rare earth improved the antibacterial durability of the silk fabric.

New α-pyrrolidinonoids and glycosides from Euphorbia humifusa

A phytochemical investigation on the constituents from Euphorbia humifusa Willd. has resulted in the isolation of three new α-pyrrolidinonoidal compounds, 5β-methoxy-4β-hydroxy-3-methylene-α-pyrrolidinone (1), 5β-methoxy-4α-hydroxy-3-methylene-α-pyrrolidinone (2), and 5β-butoxy-4α-hydroxy-3-methylene-α-pyrrolidinone (3), and three new glycosides including an indole glycoside, 3-(2-hydroxyethyl)-5-(1-O-β-glucopyranosyloxy)-indole (4), an ionone glycoside, 3-oxo-7,8-dihydro-α-ionone-11-O-β-glucoside (5), and a hemiterpene glycoside, 1-(4-hydroxy-2-methyl-2-buten-1-yl)-6- (3,4,5-trihydroxybenzoyl)-β-d-glucose (6), along with 10 known compounds. Their structures were elucidated by analysis of 1D and 2D NMR spectral data. The structure of 1 was further confirmed by a single-crystal X-ray diffraction analysis.

Triterpenoids and other Constituents from Euphorbia Humifusa

AbstractA novel lupane‐type triterpenoid, 3,4‐seco‐lupa‐4(23), 20(29)‐dien‐24‐hydroxy‐3‐oic acid (1) and a new cycloartane‐type triterpenoid, 23(E)‐cycloart‐23‐en‐25‐ethoxy‐3β‐ol (7), as well as eighteen known compounds, were isolated from the hot ethanol extract of the whole plant of Euphorbia humifusa Willd. The new structures were characterized by means of spectroscopic methods including 1D, 2D NMR and HRESIMS, and the known ones were established on the basis of comparing their NMR data with those of the corresponding compounds in the literature. In addition, cytotoxicity against selected cancer cell human gastric carcinoma (SGC‐7901) of compounds 1,3,4,6 were measured in vitro.